Dosing & Uses
Dosage Forms & Strengths
injectable solution
- 100mcg/mL
- 500mcg/mL
patch, extended-release
- 0.1mg/day
- 0.2mg/day
- 0.3mg/day
tablet, immediate-release
- 0.1mg
- 0.2mg
- 0.3mg
tablet, extended-release
- 0.1mg
Hypertension
Immediate-release tablets
- 0.1 mg PO q12hr
- Range: 0.1-0.2 mg/day q12hr; not to exceed 2.4 mg/day
Transdermal
- Apply 1 patch q7Days; start with 0.1 mg; increase by 0.1 mg after q1-2Week interval; usual dose range is 0.1-0.3 mg qWeek
Cancer Pain
Epidural infusion
- Severe pain in patients with cancer not adequately relieved by opioid analgesics alone
- Initial: 30 mcg/hr
- Titrate as required for pain relief or presence of side effects
- Limited data on doses exceeding 40 mcg/hr
-
Dosing considerations
- Epidural administration (Duraclon) is indicated in combination with opiates for the treatment of severe pain in patients with cancer not adequately relieved by opioid analgesics alone
- More likely to be effective in patients with neuropathic pain than in those with somatic or visceral pain
- Safety and effectiveness of epidural administration in this limited indication and clinical population have been established in patients old enough to tolerate placement and management of an epidural catheter; these conclusions are based on evidence from adequate and well-controlled studies in adults and through experience with the use of clonidine in the pediatric age group for other indications
Acute Hypertension (Off-label)
0.1-0.2 mg PO; may follow with additional doses of 0.1 mg qhr PRN to maximum 0.6 mg total dose
EtOH Withdrawal (Off-label)
0.3-0.6 mg PO q6hr
Smoking Cessation (Off-label)
PO administration: 0.1 mg qDay; increase by 0.1 mg/day to 0.15-0.75 mg/day if required
TD administration: 100-200 mcg/day patch q7Days
Restless Legs Syndrome (Off-label)
100-300 mcg PO 2 hours befor bedtime, up to 900 mcg/day
Tourette's Syndrome (Off-label)
0.0025-0.015 mg/kg/day PO for 6 weeks to 3 months
Cyclosporine Nephrotoxicity (Off-label)
100-200 mcg/day transdermal patch; change q7Days
Menopausal Flushing (Off-label)
Apply 100 mcg/day patch; change q7Days, OR
50 mcg PO q12hr initially; may increase up to 400 mcg q12hr
Dysmenorrhea (Off-label)
PO administration: 0.025 mg q12hr for 2 weeks prior to menstruation
Opioid Withdrawal (Off-label)
PO administration: 0.1-0.3 mg q4-6hr; increase by 0.1 mg/day to 0.15-0.75 mg/day if required; do not exceed 2.4 mg/day
TD administration: 100-200 mcg/day patch q7Days; initiate 0.1-0.3 mg PO q4-6hr for first 2 days to allow for adequate drug levels
Postherpetic Neuralgia (Off-label)
PO administration: 0.1 mg q12hr
Psychosis (Off-label)
PO administration: 0.4-1.4 mg/day in divided doses
Pheochromocytoma Diagnosis (Off-label)
Clonidine suppression testing: 0.3 mg PO for 60-80 kg patient; obtain blood sample 3 hours after administration to supine patient
Dosing Considerations
Extended-release is not to be used interchangeably with immediate-release tablets
Dosing Modifications
Renal Impairment
- Impact of renal impairment not assessed
- Initial dose adjustment should be based on amount of renal impairment
- Monitor carefully for hypotension and bradycardia
- Removed minimally during hemodialysis; no need to redose following dialysis
Dosage Forms & Strengths
injectable solution
- 100mcg/mL
- 500mcg/mL
patch
- 0.1mg/day
- 0.2mg/day
- 0.3mg/day
tablet, immediate-release
- 0.1mg
- 0.2mg
- 0.3mg
tablet, extended-release
- 0.1mg
Hypertension
>12 years old
- Immediate-release tablets: 0.2 mg/day PO divided q12hr; increase qWeek; maintenance dose range, 0.2-0.6 mg/day q12hr; not to exceed 2.4 mg/day
- Transdermal patch: 0.1 mg patch q7Day initially; may increase by weekly 0.1-mg increments after 1-2 weeks if desired blood pressure reduction not achieved; not to exceed 0.6 mg/week (ie, 2 clonidine 0.3 mg patches)
<12 years old
- Immediate-release tablets and transdermal patch: Safety and efficacy not established
ADHD
<6 years old: Not established
≥6 years old (extended-release tablets, Kapvay): 0.1 mg PO qHS initially; may adjust dose by increments of 0.1 mg/day at weekly intervals until desired response; not to exceed 0.4 mg/day
When discontinuing, taper gradually by decrements not to exceed 0.1 mg q3-7Days
Dosing considerations
- May be given as monotherapy or as adjunctive therapy with stimulants
- Extended-release not interchangeable with immediate-release product
Cancer Pain
Severe pain in patients with cancer not adequately relieved by opioid analgesics alone
Epidural infusion: 0.5 mcg/kg/hr initially; adjust according to clinical response
Dosing considerations
- Epidural administration (Duraclon) is indicated in combination with opiates for the treatment of severe pain in patients with cancer not adequately relieved by opioid analgesics alone
- Restrict use to pediatric patients with severe, intractable pain from malignancy that is unresponsive to epidural or spinal opiates or to other, more conventional analgesic techniques
- More likely to be effective in patients with neuropathic pain than in those with somatic or visceral pain
- Safety and effectiveness of epidural administration in this limited indication and clinical population have been established in patients old enough to tolerate placement and management of an epidural catheter; these conclusions are based on evidence from adequate and well-controlled studies in adults and through experience with the use of clonidine in the pediatric age group for other indications
Dosing Modifications
Renal Impairment
- Impact of renal impairment not assessed
- Initial dose adjustment should be based on amount of impairment
- Monitor carefully for hypotension and bradycardia
- Removed minimally during hemodialysis, so no need to redose following dialysis
Hypertension
Immediate-release tablets: 0.1 mg PO qHS
Dosing considerations
Not recommended as routine treatment for hypertension (Beers criteria)
Potential for orthostatic hypotension and adverse CNS effects
May cause bradycardia
Immediate release: Lower initial doses than for nongeriatric adult dosing, as well as gradual adjustments, are recommended
Extended release: May require lower initial dose than for nongeriatric adult dosing
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (72)
- adagrasib
adagrasib will increase the level or effect of clonidine by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Avoid coadministration of adagrasib, a P-gp inhibitor, with sensitive P-gp substrates unless otherwise recommended in the prescribing information for these substrates.
- alfentanil
clonidine, alfentanil. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- amitriptyline
amitriptyline decreases effects of clonidine by Other (see comment). Avoid or Use Alternate Drug. Comment: Inhibition of uptake by adrenergic neurons.
- amoxapine
amoxapine decreases effects of clonidine by Other (see comment). Avoid or Use Alternate Drug. Comment: Inhibition of uptake by adrenergic neurons.
- atenolol
clonidine, atenolol. Either increases toxicity of the other by unspecified interaction mechanism. Avoid or Use Alternate Drug. Can increase risk of bradycardia.
- azelastine
clonidine, azelastine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Enhanced CNS depressant effects.
- betaxolol
clonidine, betaxolol. Either increases toxicity of the other by unspecified interaction mechanism. Avoid or Use Alternate Drug. Can increase risk of bradycardia.
- bisoprolol
clonidine, bisoprolol. Either increases toxicity of the other by unspecified interaction mechanism. Avoid or Use Alternate Drug. Can increase risk of bradycardia.
- bremelanotide
bremelanotide will decrease the level or effect of clonidine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- brigatinib
brigatinib will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Brigatinib induces CYP3A4 in vitro. Coadministration with CYP3A4 substrates, particularly those with a narrow therapeutic index, can result in decreased concentrations and loss of efficacy. If unable to avoid coadministration, monitor CYP3A4 substrate levels and adjust dose as needed.
- buprenorphine
clonidine, buprenorphine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- buprenorphine buccal
clonidine, buprenorphine buccal. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- buprenorphine subdermal implant
clonidine, buprenorphine subdermal implant. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- buprenorphine transdermal
clonidine, buprenorphine transdermal. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- buprenorphine, long-acting injection
clonidine, buprenorphine, long-acting injection. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- butorphanol
clonidine, butorphanol. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- calcium/magnesium/potassium/sodium oxybates
clonidine, calcium/magnesium/potassium/sodium oxybates. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Profound sedation, respiratory depression, coma, and death may result if coadministered. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation.
- clomipramine
clomipramine decreases effects of clonidine by Other (see comment). Avoid or Use Alternate Drug. Comment: Inhibition of uptake by adrenergic neurons.
- codeine
clonidine, codeine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- desipramine
desipramine decreases effects of clonidine by Other (see comment). Avoid or Use Alternate Drug. Comment: Inhibition of uptake by adrenergic neurons.
- diltiazem
clonidine, diltiazem. unknown mechanism. Avoid or Use Alternate Drug. Reports of sinus bradycardia resulting in hospitalization and pacemaker insertion reported with concomitant use. Possible life-threatening effect, monitor closely.
- doxepin
doxepin decreases effects of clonidine by Other (see comment). Avoid or Use Alternate Drug. Comment: Inhibition of uptake by adrenergic neurons.
- esmolol
clonidine, esmolol. Either increases toxicity of the other by unspecified interaction mechanism. Avoid or Use Alternate Drug. Can increase risk of bradycardia.
- ethanol
clonidine, ethanol. Either increases toxicity of the other by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- hydrocodone
clonidine, hydrocodone. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- hydromorphone
clonidine, hydromorphone. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- imipramine
imipramine decreases effects of clonidine by Other (see comment). Avoid or Use Alternate Drug. Comment: Inhibition of uptake by adrenergic neurons.
- iobenguane I 131
clonidine will decrease the level or effect of iobenguane I 131 by Other (see comment). Avoid or Use Alternate Drug. Based on the mechanism of action of iobenguane, drugs that reduce catecholamine uptake or that deplete catecholamine stores may interfere with iobenguane uptake into cells, and thus, reduce iobenguane efficacy. Discontinue interfering drugs for at least 5 half-lives before administration of either the dosimetry or an iobenguane dose. Do not administer these drugs until at least 7 days after each iobenguane dose.
- levobunolol
clonidine, levobunolol. Either increases toxicity of the other by unspecified interaction mechanism. Avoid or Use Alternate Drug. Can increase risk of bradycardia.
- lofepramine
lofepramine decreases effects of clonidine by Other (see comment). Avoid or Use Alternate Drug. Comment: Inhibition of uptake by adrenergic neurons.
- lofexidine
lofexidine, clonidine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Lumacaftor is a strong inducer of CYP3A. Avoid coadministration with sensitive CYP3A substrates or CYP3A substrates with a narrow therapeutic index.
- macimorelin
clonidine, macimorelin. unspecified interaction mechanism. Avoid or Use Alternate Drug. Drugs that may transiently elevate growth hormone (GH) concentrations may impact the accuracy of the macimorelin diagnostic test. Allow sufficient washout time of drugs affecting GH release before administering macimorelin.
- maprotiline
maprotiline decreases effects of clonidine by Other (see comment). Avoid or Use Alternate Drug. Comment: Inhibition of uptake by adrenergic neurons.
- meperidine
clonidine, meperidine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- methadone
clonidine, methadone. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- metoclopramide intranasal
clonidine, metoclopramide intranasal. Either increases effects of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Avoid use of metoclopramide intranasal or interacting drug, depending on importance of drug to patient.
- metoprolol
clonidine, metoprolol. Either increases toxicity of the other by unspecified interaction mechanism. Avoid or Use Alternate Drug. Can increase risk of bradycardia.
- mirtazapine
mirtazapine decreases effects of clonidine by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Risk of hypertensive urgency.
- mobocertinib
mobocertinib will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information.
- morphine
clonidine, morphine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- nadolol
clonidine, nadolol. Either increases toxicity of the other by unspecified interaction mechanism. Avoid or Use Alternate Drug. Can increase risk of bradycardia.
- nalbuphine
clonidine, nalbuphine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- nebivolol
clonidine, nebivolol. Either increases toxicity of the other by unspecified interaction mechanism. Avoid or Use Alternate Drug. Can increase risk of bradycardia.
- nortriptyline
nortriptyline decreases effects of clonidine by Other (see comment). Avoid or Use Alternate Drug. Comment: Inhibition of uptake by adrenergic neurons.
- olopatadine intranasal
clonidine and olopatadine intranasal both increase sedation. Avoid or Use Alternate Drug. Coadministration increases risk of CNS depression, which can lead to additive impairment of psychomotor performance and cause daytime impairment.
- olutasidenib
olutasidenib will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of olutasidenib (a CYP3A4 inducer) with sensitive CYP3A substrates unless otherwise instructed in substrates prescribing information. If unavoidable, monitor for loss of therapeutic effect of sensitive CYP3A4 substrates.
- opium tincture
clonidine, opium tincture. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- orphenadrine
clonidine, orphenadrine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Enhanced CNS depressant effects.
- oxycodone
clonidine, oxycodone. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- oxymorphone
clonidine, oxymorphone. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- pacritinib
pacritinib will increase the level or effect of clonidine by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.
- pentazocine
clonidine, pentazocine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- perampanel
clonidine, perampanel. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- ponesimod
ponesimod, clonidine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Consult cardiologist if considering treatment. Coadministration of ponesimod with drugs that decrease HR may have additive effects on decreasing HR and should generally not be initiated in these patients.
- propranolol
clonidine, propranolol. Either increases toxicity of the other by unspecified interaction mechanism. Avoid or Use Alternate Drug. Can increase risk of bradycardia.
- protriptyline
protriptyline decreases effects of clonidine by Other (see comment). Avoid or Use Alternate Drug. Comment: Inhibition of uptake by adrenergic neurons.
- remifentanil
clonidine, remifentanil. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- repotrectinib
repotrectinib will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Repotrectinib is a CYP3A4 inducer. Avoid coadministration with CYP3A substrates where minimal concentration changes can cause reduced efficacy, unless otherwise recommended their prescribing information.
- sodium oxybate
clonidine, sodium oxybate. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- sotalol
clonidine, sotalol. Either increases toxicity of the other by unspecified interaction mechanism. Avoid or Use Alternate Drug. Can increase risk of bradycardia.
- sotorasib
sotorasib will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use is unavoidable, refer to the prescribing information of the CYP3A4 substrate for dosage modifications
- sufentanil
clonidine, sufentanil. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- sufentanil SL
clonidine, sufentanil SL. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- tapentadol
clonidine, tapentadol. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- thalidomide
clonidine, thalidomide. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Enhanced CNS depressant effects.
- timolol
clonidine, timolol. Either increases toxicity of the other by unspecified interaction mechanism. Avoid or Use Alternate Drug. Can increase risk of bradycardia.
- tramadol
clonidine, tramadol. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
- trazodone
trazodone decreases effects of clonidine by Other (see comment). Avoid or Use Alternate Drug. Comment: Inhibition of uptake by adrenergic neurons.
- trimipramine
trimipramine decreases effects of clonidine by Other (see comment). Avoid or Use Alternate Drug. Comment: Inhibition of uptake by adrenergic neurons.
- yohimbe
yohimbe decreases effects of clonidine by pharmacodynamic antagonism. Contraindicated.
- zolpidem
clonidine, zolpidem. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration enhances CNS depressant effects.
Monitor Closely (166)
- abrocitinib
abrocitinib will increase the level or effect of clonidine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor and titrate dose of P-gp substrate appropriately.
- acebutolol
acebutolol, clonidine. Mechanism: pharmacodynamic synergism. Modify Therapy/Monitor Closely. Selective beta blocker administration during withdrawal from centrally acting alpha agonists may result in rebound hypertension.
- acrivastine
acrivastine and clonidine both increase sedation. Use Caution/Monitor.
- aldesleukin
aldesleukin increases effects of clonidine by pharmacodynamic synergism. Use Caution/Monitor. Risk of hypotension.
- alprazolam
clonidine, alprazolam. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- amifostine
amifostine, clonidine. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration with blood pressure lowering agents may increase the risk and severity of hypotension associated with amifostine. When amifostine is used at chemotherapeutic doses, withhold blood pressure lowering medications for 24 hr prior to amifostine; if blood pressure lowering medication cannot be withheld, do not administer amifostine.
- amiodarone
clonidine, amiodarone. Either decreases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration increases risk of bradycardia, sinus arrest, and AV block; monitor heart rate in patients on concomitant drugs that slow heart rate.
- amisulpride
amisulpride and clonidine both increase sedation. Use Caution/Monitor.
- aripiprazole
clonidine, aripiprazole. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- asenapine
asenapine and clonidine both increase sedation. Use Caution/Monitor.
- asenapine transdermal
asenapine transdermal and clonidine both increase sedation. Use Caution/Monitor.
- atenolol
atenolol, clonidine. Mechanism: pharmacodynamic synergism. Modify Therapy/Monitor Closely. Selective beta blocker administration during withdrawal from centrally acting alpha agonists may result in rebound hypertension.
clonidine, atenolol. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Sympatholytic action may worsen sinus node dysfunction and atrioventricular (AV) block. - avanafil
avanafil increases effects of clonidine by pharmacodynamic synergism. Use Caution/Monitor. Risk of hypotension.
- avapritinib
avapritinib and clonidine both increase sedation. Use Caution/Monitor.
- benperidol
clonidine, benperidol. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- benzhydrocodone/acetaminophen
benzhydrocodone/acetaminophen and clonidine both increase sedation. Use Caution/Monitor.
- betaxolol
betaxolol, clonidine. Mechanism: pharmacodynamic synergism. Modify Therapy/Monitor Closely. Selective beta blocker administration during withdrawal from centrally acting alpha agonists may result in rebound hypertension.
clonidine, betaxolol. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive sympatholytic action may worsen sinus node dysfunction and atrioventricular (AV) block. - bisoprolol
bisoprolol, clonidine. Mechanism: pharmacodynamic synergism. Modify Therapy/Monitor Closely. Selective beta blocker administration during withdrawal from centrally acting alpha agonists may result in rebound hypertension.
- blinatumomab
blinatumomab increases levels of clonidine by decreasing metabolism. Modify Therapy/Monitor Closely. Treatment initiation causes transient release of cytokines that may suppress CYP450 enzymes; highest drug-drug interaction risk is during the first 9 days of the first cycle and the first 2 days of the 2nd cycle in patients who are receiving concomitant CYP450 substrates, particularly those with a narrow therapeutic index.
- bretylium
clonidine, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.
- brexanolone
brexanolone, clonidine. Either increases toxicity of the other by sedation. Use Caution/Monitor.
- brexpiprazole
brexpiprazole and clonidine both increase sedation. Use Caution/Monitor.
- brimonidine
brimonidine and clonidine both increase sedation. Use Caution/Monitor.
- brivaracetam
brivaracetam and clonidine both increase sedation. Use Caution/Monitor.
- brodalumab
brodalumab, clonidine. Other (see comment). Use Caution/Monitor. Comment: Formation of CYP450 enzymes can be altered by increased levels of certain cytokines during chronic inflammation; thus, brodalumab could normalize the formation of CYP450 enzymes. Upon initiation or discontinuation of brodalumab in patients who are receiving concomitant CYP450 substrates, particularly those with a narrow therapeutic index, consider monitoring for therapeutic effect.
- buprenorphine subdermal implant
buprenorphine subdermal implant and clonidine both increase sedation. Use Caution/Monitor.
- buprenorphine transdermal
buprenorphine transdermal and clonidine both increase sedation. Use Caution/Monitor.
- buprenorphine, long-acting injection
buprenorphine, long-acting injection and clonidine both increase sedation. Use Caution/Monitor.
- carbidopa
carbidopa increases effects of clonidine by pharmacodynamic synergism. Use Caution/Monitor. Therapy with carbidopa, given with or without levodopa or carbidopa-levodopa combination products, is started, dosage adjustment of the antihypertensive drug may be required.
- cariprazine
cariprazine and clonidine both increase sedation. Use Caution/Monitor.
- celiprolol
celiprolol, clonidine. Mechanism: pharmacodynamic synergism. Modify Therapy/Monitor Closely. Selective beta blocker administration during withdrawal from centrally acting alpha agonists may result in rebound hypertension.
- cenobamate
cenobamate, clonidine. Either increases effects of the other by sedation. Use Caution/Monitor.
- chlordiazepoxide
clonidine, chlordiazepoxide. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- chlorpromazine
clonidine, chlorpromazine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- citalopram
clonidine, citalopram. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- clobazam
clonidine, clobazam. Other (see comment). Use Caution/Monitor. Comment: Concomitant administration can increase the potential for CNS effects (e.g., increased sedation or respiratory depression).
- clonazepam
clonidine, clonazepam. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Enhanced CNS depressant effects.
- clorazepate
clonidine, clorazepate. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- clozapine
clonidine, clozapine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- daridorexant
clonidine and daridorexant both increase sedation. Modify Therapy/Monitor Closely. Coadministration increases risk of CNS depression, which can lead to additive impairment of psychomotor performance and cause daytime impairment.
- dexmethylphenidate
dexmethylphenidate increases toxicity of clonidine by unknown mechanism. Use Caution/Monitor.
- diazepam
clonidine, diazepam. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- difelikefalin
difelikefalin and clonidine both increase sedation. Use Caution/Monitor.
- doxazosin
clonidine, doxazosin. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive sympatholytic action may worsen sinus node dysfunction and atrioventricular (AV) block.
- doxylamine
clonidine, doxylamine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- dronabinol
clonidine, dronabinol. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- droperidol
clonidine, droperidol. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- dulaglutide
dulaglutide, clonidine. Other (see comment). Use Caution/Monitor. Comment: Dulaglutide slows gastric emptying and may impact absorption of concomitantly administered oral medications; be particularly cautious when coadministered with drugs that have a narrow therapeutic index.
- dupilumab
dupilumab, clonidine. Other (see comment). Use Caution/Monitor. Comment: Formation of CYP450 enzymes can be altered by increased levels of certain cytokines during chronic inflammation; thus, dupilumab could normalize the formation of CYP450 enzymes. Upon initiation or discontinuation of dupilumab in patients who are receiving concomitant CYP450 substrates, particularly those with a narrow therapeutic index, consider monitoring for therapeutic effect.
- elacestrant
elacestrant will increase the level or effect of clonidine by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Reduce dose of P-gp substrates per their Prescribing Information when minimal concentration changes may lead to serious or life-threatening adverse reactions.
- elranatamab
elranatamab will increase the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Elranatamab causes cytokine release syndrome (CRS) that may suppress activity of CYP enzymes, resulting in increased exposure of CYP substrates. This is more likely to occur from initiation of elranatamab step-up dosing up to 14 days after the first treatment dose and during and after CRS.
- eluxadoline
eluxadoline increases levels of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution when CYP3A substrates that have a narrow therapeutic index are coadministered with eluxadoline.
- epcoritamab
epcoritamab, clonidine. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Epcoritamab causes release of cytokines that may suppress activity of CYP enzymes, resulting in increased exposure of CYP substrates. For certain CYP substrates, minimal changes in their concentration may lead to serious adverse reactions. If needed, modify therapy as recommended in the substrate's prescribing information. .
- epinephrine inhaled
clonidine, epinephrine inhaled. Either increases effects of the other by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor.
- escitalopram
clonidine, escitalopram. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- esketamine intranasal
esketamine intranasal, clonidine. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely.
esketamine intranasal, clonidine. Either increases toxicity of the other by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor. Closely monitor blood pressure with concomitant use of esketamine nasal with stimulants. . - esmolol
esmolol, clonidine. Mechanism: pharmacodynamic synergism. Modify Therapy/Monitor Closely. Selective beta blocker administration during withdrawal from centrally acting alpha agonists may result in rebound hypertension.
clonidine, esmolol. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive sympatholytic action may worsen sinus node dysfunction and atrioventricular (AV) block. - estazolam
clonidine, estazolam. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- fentanyl
fentanyl and clonidine both increase sedation. Use Caution/Monitor.
- fentanyl intranasal
fentanyl intranasal and clonidine both increase sedation. Use Caution/Monitor.
- fentanyl iontophoretic transdermal system
fentanyl iontophoretic transdermal system and clonidine both increase sedation. Use Caution/Monitor.
- fentanyl transdermal
fentanyl transdermal and clonidine both increase sedation. Use Caution/Monitor.
- fentanyl transmucosal
fentanyl transmucosal and clonidine both increase sedation. Use Caution/Monitor.
- ferric maltol
ferric maltol, clonidine. Either increases levels of the other by unspecified interaction mechanism. Modify Therapy/Monitor Closely. Coadministration of ferric maltol with certain oral medications may decrease the bioavailability of either ferric maltol and some oral drugs. For oral drugs where reductions in bioavailability may cause clinically significant effects on its safety or efficacy, separate administration of ferric maltol from these drugs. Duration of separation may depend on the absorption of the medication concomitantly administered (eg, time to peak concentration, whether the drug is an immediate or extended release product).
- flibanserin
flibanserin increases levels of clonidine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Increase monitoring of concentrations of drugs transported by P-gp that have a narrow therapeutic index if coadministered with flibanserin.
- fluoxetine
clonidine, fluoxetine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- fluphenazine
clonidine, fluphenazine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- flurazepam
clonidine, flurazepam. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- fluvoxamine
fluvoxamine, clonidine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. CNS derpressant effects enhanced.
- ganaxolone
clonidine and ganaxolone both increase sedation. Use Caution/Monitor.
- givinostat
givinostat will increase the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Givinostat is a weak CYP3A4 inhibitor. Closely monitor if coadministered with orally administered CYP3A4 sensitive substrates for which a small change in substrate plasma concentration may lead to serious toxicities.
- glofitamab
glofitamab, clonidine. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Glofitamab causes release of cytokines that may suppress activity of CYP enzymes, resulting in increased exposure of CYP substrates. For certain CYP substrates, minimal changes in their concentration may lead to serious adverse reactions. If needed, modify therapy as recommended in the substrate's prescribing information. .
- glycerol phenylbutyrate
glycerol phenylbutyrate will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Glycerol phenylbutyrate is a weak inducer of CYP3A4. Monitor for decreased efficacy of CYP3A4 substrates that have a narrow therapeutic index.
- guanfacine
clonidine, guanfacine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Sympatholytic action may worsen sinus node dysfunction and atrioventricular (AV) block.
- haloperidol
clonidine, haloperidol. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
clonidine increases toxicity of haloperidol by Other (see comment). Use Caution/Monitor. Comment: High doses of clonidine IV may increase arrhythmogenic potential (QT-prolongation, ventricular fibrillation) of high dose haloperidol IV in patients experiencing alcoholic delirium. - hydroxyzine
clonidine, hydroxyzine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- iloperidone
clonidine, iloperidone. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- insulin degludec
clonidine, insulin degludec. Other (see comment). Modify Therapy/Monitor Closely. Comment: Clonidine may either increase or decrease the blood glucose lowering effect of antidiabetic agents; clonidine may also mask hypoglycemic symptoms.
- insulin degludec/insulin aspart
clonidine, insulin degludec/insulin aspart. Other (see comment). Modify Therapy/Monitor Closely. Comment: Clonidine may either increase or decrease the blood glucose lowering effect of antidiabetic agents; clonidine may also mask hypoglycemic symptoms.
- insulin inhaled
clonidine, insulin inhaled. Other (see comment). Modify Therapy/Monitor Closely. Comment: Clonidine may either increase or decrease the blood glucose lowering effect of antidiabetic agents; clonidine may also mask hypoglycemic symptoms.
- isavuconazonium sulfate
isavuconazonium sulfate will increase the level or effect of clonidine by Other (see comment). Use Caution/Monitor. Isavuconazonium sulfate, an inhibitor of P-gp and CYP3A4, may increase the effects or levels of sensitive P-gp or CYP3A4 substrates, which may require dose adjustment.
- ivabradine
ivabradine, clonidine. Either decreases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Most patients receiving ivabradine will also be treated with a beta-blocker. The risk of bradycardia increases with coadministration of drugs that slow heart rate (eg, digoxin, amiodarone, beta-blockers). Monitor heart rate in patients taking ivabradine with other negative chronotropes.
- ixekizumab
ixekizumab, clonidine. Other (see comment). Use Caution/Monitor. Comment: Formation of CYP450 enzymes can be altered by increased levels of certain cytokines during chronic inflammation; thus, ixekizumab could normalize the formation of CYP450 enzymes. Upon initiation or discontinuation of ixekizumab in patients who are receiving concomitant CYP450 substrates, particularly those with a narrow therapeutic index, consider monitoring for therapeutic effect.
- lasmiditan
lasmiditan, clonidine. Either increases effects of the other by sedation. Use Caution/Monitor. Coadministration of lasmiditan and other CNS depressant drugs, including alcohol have not been evaluated in clinical studies. Lasmiditan may cause sedation, as well as other cognitive and/or neuropsychiatric adverse reactions.
- lemborexant
lemborexant, clonidine. Either increases effects of the other by sedation. Modify Therapy/Monitor Closely. Dosage adjustment may be necessary if lemborexant is coadministered with other CNS depressants because of potentially additive effects.
- levetiracetam
levetiracetam and clonidine both increase sedation. Use Caution/Monitor.
- levodopa
levodopa increases effects of clonidine by pharmacodynamic synergism. Use Caution/Monitor. Consider decreasing dosage of antihypertensive agent.
- levomilnacipran
levomilnacipran decreases effects of clonidine by pharmacodynamic antagonism. Use Caution/Monitor. Because levomilnacipran decreases reuptake of NE, it may antagonize clonidine antihypertensive effect.
- lonapegsomatropin
lonapegsomatropin will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Limited published data indicate that growth hormone treatment increases cytochrome P450 (CYP450)-mediated antipyrine clearance. Caution with sensitive CYP substrates
- lorazepam
clonidine, lorazepam. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- loxapine
clonidine, loxapine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- loxapine inhaled
clonidine, loxapine inhaled. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- lurasidone
lurasidone increases effects of clonidine by Other (see comment). Use Caution/Monitor. Comment: Potential for increased risk of hypotension with concurrent use. Monitor blood pressure and adjust dose of antihypertensive agent as needed.
- methohexital
methohexital and clonidine both increase sedation. Use Caution/Monitor.
- methyldopa
clonidine, methyldopa. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Sympatholytic action may worsen sinus node dysfunction and atrioventricular (AV) block.
- metoprolol
metoprolol, clonidine. Mechanism: pharmacodynamic synergism. Modify Therapy/Monitor Closely. Selective beta blocker administration during withdrawal from centrally acting alpha agonists may result in rebound hypertension.
clonidine, metoprolol. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive sympatholytic action may worsen sinus node dysfunction and atrioventricular (AV) block. - metyrosine
clonidine, metyrosine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- midazolam intranasal
midazolam intranasal, clonidine. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Concomitant use of barbiturates, alcohol, or other CNS depressants may increase the risk of hypoventilation, airway obstruction, desaturation, or apnea and may contribute to profound and/or prolonged drug effect.
- milnacipran
milnacipran decreases effects of clonidine by pharmacodynamic antagonism. Use Caution/Monitor.
- nabilone
clonidine, nabilone. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- nadolol
nadolol, clonidine. Mechanism: pharmacodynamic synergism. Modify Therapy/Monitor Closely. Non selective beta blocker administration during withdrawal from centrally acting alpha agonists may result in rebound hypertension.
- nebivolol
nebivolol, clonidine. Mechanism: pharmacodynamic synergism. Modify Therapy/Monitor Closely. Selective beta blocker administration during withdrawal from centrally acting alpha agonists may result in rebound hypertension.
clonidine, nebivolol. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive sympatholytic action may worsen sinus node dysfunction and atrioventricular (AV) block. - neratinib
neratinib increases levels of clonidine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Neratinib inhibits P-gp transport. Caution if coadministered with a P-gp substrate with a narrow therapeutic index.
- nitroglycerin rectal
nitroglycerin rectal, clonidine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .
- nitroprusside sodium
nitroprusside sodium, clonidine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects.
- olanzapine
clonidine, olanzapine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- olanzapine/samidorphan
olanzapine/samidorphan increases effects of clonidine by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Monitor blood pressure and reduce antihypertensive drug dosage in accordance with its product labeling.
- omaveloxolone
omaveloxolone will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Omaveloxolone may reduce systemic exposure of sensitive CYP3A4 substrates. Check prescribing information of substrate if dosage modification is needed.
- oritavancin
oritavancin will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Oritavancin is a weak CYP3A4 inducer; caution if coadministered with CYP3A4 substrates that have a narrow therapeutic index
- oxazepam
clonidine, oxazepam. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- palbociclib
palbociclib will increase the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. The dose of sensitive CYP3A substrates with a narrow therapeutic index may need to be reduced if coadministered with palbociclib
- paliperidone
clonidine, paliperidone. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- paroxetine
clonidine, paroxetine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- penbutolol
penbutolol, clonidine. Mechanism: pharmacodynamic synergism. Modify Therapy/Monitor Closely. Selective beta blocker administration during withdrawal from centrally acting alpha agonists may result in rebound hypertension.
- perphenazine
clonidine, perphenazine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- pimozide
clonidine, pimozide. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- pindolol
pindolol, clonidine. Mechanism: pharmacodynamic synergism. Modify Therapy/Monitor Closely. Non selective beta blocker administration during withdrawal from centrally acting alpha agonists may result in rebound hypertension.
- pirtobrutinib
pirtobrutinib will increase the level or effect of clonidine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Pirtobrutinib (a P-gp inhibitor) may increase plasma concentrations of sensitive P-gp substrates, which may increase the risk of adverse reactions related to these substrates.
- pitolisant
pitolisant will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Pitolisant is a borderline/weak inducer of CYP3A4. Monitor sensitive CYP3A4 substrates for reduced effectiveness if coadministered.
- pramipexole
clonidine, pramipexole. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- prazosin
clonidine, prazosin. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Sympatholytic action may worsen sinus node dysfunction and atrioventricular (AV) block.
- prochlorperazine
clonidine, prochlorperazine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- promethazine
clonidine, promethazine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- propranolol
propranolol, clonidine. Mechanism: pharmacodynamic synergism. Modify Therapy/Monitor Closely. Non selective beta blocker administration during withdrawal from centrally acting alpha agonists may result in rebound hypertension.
- quazepam
clonidine, quazepam. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- quetiapine
clonidine, quetiapine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- ribociclib
ribociclib will increase the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- risperidone
clonidine, risperidone. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- ritlecitinib
ritlecitinib will increase the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.
- rolapitant
rolapitant will increase the level or effect of clonidine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Oral rolapitant (P-gp inhibitor) may increase plasma concentrations of P-gp substrates and may result in potential adverse reactions. Monitor possible adverse reactions if concomitant use of P-gp substrates and rolapitant can not be avoided.
- ropeginterferon alfa 2b
ropeginterferon alfa 2b will increase the level or effect of clonidine by Other (see comment). Use Caution/Monitor. Certain proinflammatory cytokines, including interferons, can suppress CYP450 enzymes resulting in increased exposures of some CYP substrates. Therefore, monitor patients who are receiving concomitant drugs that are CYP450 substrates with a narrow therapeutic index from toxicities to such drugs.
- ropinirole
clonidine, ropinirole. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- rotigotine
clonidine, rotigotine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- rufinamide
clonidine, rufinamide. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- sarilumab
sarilumab, clonidine. Other (see comment). Use Caution/Monitor. Comment: Formation of CYP450 enzymes can be altered by increased levels of cytokines such as IL-6. Elevated IL-6 concentration may down-regulate CYP activity, such as in patients with RA, and, hence, increase drug levels compared with subjects without RA. Blockade of IL-6 signaling by IL-6 antagonists (eg, sarilumab) might reverse the inhibitory effect of IL-6 and restore CYP activity, leading to decreased drug concentrations. Caution when initiating or discontinuing sarilumab if coadministered with CYP450 substrates, especially those with a narrow therapeutic index.
- schisandra
schisandra will increase the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- secukinumab
secukinumab, clonidine. Other (see comment). Use Caution/Monitor. Comment: Formation of CYP450 enzymes can be altered by increased levels of certain cytokines during chronic inflammation; thus, secukinumab could normalize the formation of CYP450 enzymes. Upon initiation or discontinuation of secukinumab in patients who are receiving concomitant CYP450 substrates, particularly those with a narrow therapeutic index, consider monitoring for therapeutic effect.
- serdexmethylphenidate/dexmethylphenidate
serdexmethylphenidate/dexmethylphenidate increases toxicity of clonidine by unknown mechanism. Use Caution/Monitor.
- sertraline
clonidine, sertraline. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- sofosbuvir/velpatasvir
sofosbuvir/velpatasvir increases levels of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Velpatasvir inhibits CYP3A4. Caution if coadministered with drugs with narrow therapeutics indexes.
- somapacitan
somapacitan will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Limited published data indicate that growth hormone treatment increases cytochrome P450 (CYP450)-mediated antipyrine clearance. Caution with sensitive CYP substrates
- somatrogon
somatrogon will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Limited published data indicate that growth hormone treatment increases cytochrome P450 (CYP450)-mediated antipyrine clearance. Caution with sensitive CYP substrates
- somatropin
somatropin will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Limited published data indicate that growth hormone treatment increases cytochrome P450 (CYP450)-mediated antipyrine clearance. Caution with sensitive CYP substrates
- sotalol
sotalol, clonidine. Mechanism: pharmacodynamic synergism. Modify Therapy/Monitor Closely. Selective beta blocker administration during withdrawal from centrally acting alpha agonists may result in rebound hypertension.
- stiripentol
stiripentol, clonidine. Either increases effects of the other by sedation. Use Caution/Monitor. Concomitant use stiripentol with other CNS depressants, including alcohol, may increase the risk of sedation and somnolence.
- tadalafil
tadalafil increases effects of clonidine by pharmacodynamic synergism. Use Caution/Monitor. Risk of hypotension.
- talquetamab
talquetamab will increase the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Talquetamab causes cytokine release syndrome (CRS) that may suppress activity of CYP enzymes, resulting in increased exposure of CYP substrates. This is more likely to occur from initiation of talquetamab step-up dosing up to 14 days after the first treatment dose and during and after CRS.
- teclistamab
teclistamab will increase the level or effect of clonidine by altering metabolism. Use Caution/Monitor. Teclistamab causes release of cytokines that may suppress activity of CYP450 enzymes, resulting in increased exposure of CYP substrates. Monitor for increased concentrations or toxicities of sensitive CYP substrates. Adjust dose of CYP substrate drug as needed.
- teduglutide
teduglutide increases levels of clonidine by Other (see comment). Use Caution/Monitor. Comment: Teduglutide may increase absorption of concomitant PO medications; caution with with drugs requiring titration or those with a narrow therapeutic index; dose adjustment may be necessary.
- telotristat ethyl
telotristat ethyl will decrease the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Telotristat ethyl induces CYP3A4 and may reduce systemic exposure of sensitive CYP3A4 substrates. Monitor for suboptimal efficacy and consider increasing the dose of the CYP3A4 substrate.
- temazepam
clonidine, temazepam. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- thioridazine
clonidine, thioridazine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- thiothixene
clonidine, thiothixene. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- timolol
timolol, clonidine. Mechanism: pharmacodynamic synergism. Modify Therapy/Monitor Closely. Non selective beta blocker administration during withdrawal from centrally acting alpha agonists may result in rebound hypertension.
- triazolam
clonidine, triazolam. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- trifluoperazine
clonidine, trifluoperazine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- trofinetide
trofinetide will increase the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Monitor CYP3A4 substrates for which a small increase in plasma concentration may lead to serious toxicities if coadministered with trofinetide (a weak CYP3A4 inhibitor).
- ustekinumab
ustekinumab, clonidine. Other (see comment). Use Caution/Monitor. Comment: Formation of CYP450 enzymes can be altered by increased levels of certain cytokines during chronic inflammation; thus, normalizing the formation of CYP450 enzymes. Upon initiation or discontinuation of ustekinumab in patients who are receiving concomitant CYP450 substrates, particularly those with a narrow therapeutic index, consider monitoring for therapeutic effect.
- verapamil
clonidine, verapamil. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Sinus bradycardia resulting in hospitalization and pacemaker insertion has been reported in association with the use of clonidine concurrently with verapamil. Monitor heart rate in patients receiving concomitant verapamil and clonidine.
verapamil, clonidine. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Sinus bradycardia resulting in hospitalization and pacemaker insertion has been reported in association with the use of clonidine concurrently with verapamil. Monitor heart rate in patients receiving concomitant verapamil and clonidine. - vilazodone
clonidine, vilazodone. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- voclosporin
voclosporin will increase the level or effect of clonidine by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Coadministration of voclosporin (a P-gp inhibitor) increases exposure and risk of adverse reactions of P-gp substrates. For certain P-gp substrates with a narrow therapeutic window, refer to prescribing information of these substrates for dosage modifications, if needed.
- vonoprazan
vonoprazan will increase the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Vonoprazan is weak CYP3A inhibitor. Caution with sensitive CYP3A substrates.
- vortioxetine
clonidine, vortioxetine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration enhances CNS depressant effects.
- xipamide
xipamide increases effects of clonidine by pharmacodynamic synergism. Use Caution/Monitor.
- ziprasidone
clonidine, ziprasidone. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
- zotepine
clonidine, zotepine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Additive hypotensive effects; potential delirium.
Minor (35)
- acarbose
clonidine decreases effects of acarbose by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, acarbose. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - agrimony
agrimony increases effects of clonidine by pharmacodynamic synergism. Minor/Significance Unknown.
- brimonidine
brimonidine increases effects of clonidine by pharmacodynamic synergism. Minor/Significance Unknown.
- chlorpropamide
clonidine decreases effects of chlorpropamide by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, chlorpropamide. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - cornsilk
cornsilk increases effects of clonidine by pharmacodynamic synergism. Minor/Significance Unknown.
- cyclosporine
clonidine increases levels of cyclosporine by unknown mechanism. Minor/Significance Unknown.
- forskolin
forskolin increases effects of clonidine by pharmacodynamic synergism. Minor/Significance Unknown.
- glimepiride
clonidine decreases effects of glimepiride by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, glimepiride. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - glipizide
clonidine decreases effects of glipizide by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, glipizide. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - glyburide
clonidine decreases effects of glyburide by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, glyburide. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - insulin aspart
clonidine decreases effects of insulin aspart by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, insulin aspart. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - insulin detemir
clonidine, insulin detemir. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production.
clonidine decreases effects of insulin detemir by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia. - insulin glargine
clonidine, insulin glargine. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production.
clonidine decreases effects of insulin glargine by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia. - insulin glulisine
clonidine, insulin glulisine. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production.
clonidine decreases effects of insulin glulisine by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia. - insulin lispro
clonidine decreases effects of insulin lispro by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, insulin lispro. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - insulin NPH
clonidine, insulin NPH. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production.
clonidine decreases effects of insulin NPH by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia. - insulin regular human
clonidine decreases effects of insulin regular human by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, insulin regular human. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - maitake
maitake increases effects of clonidine by pharmacodynamic synergism. Minor/Significance Unknown.
- metformin
clonidine decreases effects of metformin by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, metformin. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - miglitol
clonidine decreases effects of miglitol by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, miglitol. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - nateglinide
clonidine decreases effects of nateglinide by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, nateglinide. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - octacosanol
octacosanol increases effects of clonidine by pharmacodynamic synergism. Minor/Significance Unknown.
- pioglitazone
clonidine decreases effects of pioglitazone by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, pioglitazone. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - reishi
reishi increases effects of clonidine by pharmacodynamic synergism. Minor/Significance Unknown.
- repaglinide
clonidine decreases effects of repaglinide by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, repaglinide. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - rosiglitazone
clonidine decreases effects of rosiglitazone by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, rosiglitazone. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - saxagliptin
clonidine decreases effects of saxagliptin by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, saxagliptin. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - shepherd's purse
shepherd's purse, clonidine. Other (see comment). Minor/Significance Unknown. Comment: Theoretically, shepherd's purse may interfere with BP control.
- sitagliptin
clonidine decreases effects of sitagliptin by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, sitagliptin. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - tacrolimus
clonidine increases levels of tacrolimus by unknown mechanism. Minor/Significance Unknown.
- tizanidine
tizanidine increases effects of clonidine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of hypotension.
- tolazamide
clonidine decreases effects of tolazamide by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, tolazamide. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - tolbutamide
clonidine decreases effects of tolbutamide by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, tolbutamide. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production. - treprostinil
treprostinil increases effects of clonidine by pharmacodynamic synergism. Minor/Significance Unknown.
- vildagliptin
clonidine decreases effects of vildagliptin by pharmacodynamic antagonism. Minor/Significance Unknown. Diminished symptoms of hypoglycemia.
clonidine, vildagliptin. Other (see comment). Minor/Significance Unknown. Comment: Decreased symptoms of hypoglycemia. Mechanism: decreased hypoglycemia induced catecholamine production.
Adverse Effects
>10%
Skin reactions; patch (15-50%)
Dry mouth (40%)
Somnolence (19-38%)
Headache (19-29%)
Fatigue (13-24%)
Drowsiness (33%)
Dizziness (13-16%)
Hypotension, epidural (45%)
Postural hypotension, epidural (32%)
Anxiety (11%)
1-10%
Constipation (10%)
Sedation (10%)
Nausea/vomiting, PO (5%)
Malaise (3%)
Orthostatic hypotension (3%)
Anorexia, PO (1%)
Abnormal LFTs (1%)
Rash (1%)
Weight gain, PO (1%)
Frequency Not Defined
Children with ADHD
- Upper respiratory tract infection
- Irritability
- Throat pain
- Nightmares
- Insomnia
- Emotional disorder
- Constipation
- Nasal congestion
Postmarketing Reports
Hallucinations
AV block
Warnings
Black Box Warnings
Epidural clonidine is not recommended for obstetric postpartum or perioperative pain management because the risk of hemodynamic instability (eg, hypotension, bradycardia) may be unacceptable in this population
Dilute product with strength of 500 mcg/mL prior to use
Contraindications
Hypersensitivity
Epidural
- Concurrent anticoagulants, bleeding diathesis
- Presence of injection site infections
- Administration above C4 dermatome, due to lack of adequate safety data
- Obstetric/perioperative pain
Cautions
Epidural: Hemodynamically unstable patients (risk of severe hypotension)
Do not discontinue suddenly (risk of rebound hypertension)
Patch: May need to remove if severe erythema and/or localized vesicle formation develop at application site or generalized rash; consult physician
Severe coronary insufficiency
May cause xerostomia
Recent MI
Cerebrovascular disease
Chronic renal failure
Raynaud's disease
Thromboangiitis obliterans
History of depression (may exacerbate depression in cancer patients)
May impair ability to perform hazardous tasks
Remove patch before MRI (may cause burns)
Hypotension may occur; usually responsive to IV fluids and, if necessary, appropriate parenterally administered pressor agents
Cardiac conduction abnormalities: Sympatholytic action may worsen sinus node dysfunction and atrioventricular (AV) block, especially if coadministered with other sympatholytic drugs
Titrate slowly and monitor vital signs frequently in patients at risk for hypotension, heart block, bradycardia, syncope, cardiovascular disease, vascular disease, cerebrovascular disease or chronic renal failure; measure heart rate and blood pressure prior to initiation of therapy, following dose increases, and periodically while on therapy; avoid concomitant use of drugs with additive effects unless clinically indicated; advise patients to avoid becoming dehydrated or overheated
Epidural administration may result in mild respiratory depression (usually with higher than recommended dose)
Use with caution in cerebrovascular disease
Avoid as first line antihypertensive in the elderly due to high risk for adverse side effects
Children may be particularly susceptible to hypertensive episodes when experiencing GI illnesses that lead to vomiting
Discontinue oral immediate release formulations within 4 hr of surgery; restart as soon as possible following surgery
Due to different pharmacokinetic profiles, oral formulations are not interchangeable with extended release on a mg-mg basis due to different pharmacokinetic profiles
Pregnancy & Lactation
Pregnancy
There is pregnancy exposure registry that monitors pregnancy outcomes in women exposed to ADHD medications, during pregnancy; healthcare providers are encouraged to register patients by calling the National Pregnancy Registry for ADHD Medications at 1-866- 961-2388 or visiting https://womensmentalhealth.org/adhd-medications
Prolonged experience with clonidine in pregnant women over several decades, based on published literature, including controlled trials, a retrospective cohort study and case reports, have not identified a drug associated risk of major birth defects, miscarriage, and adverse maternal or fetal outcomes
Based on findings in animal studies revealed that drug may impair fertility in females and males of reproductive potential
Animal data
- In animal embryofetal studies, increased resorptions were seen in rats and mice administered oral clonidine hydrochloride from implantation through organogenesis at 10 and 5 times, respectively, the maximum recommended human dose (MRHD) given to adolescents on a mg/m2 basis; no developmental effects were seen in rabbits administered drug during organogenesis at doses up to 3 times the MRHD
Lactation
Based on published lactation studies, clonidine hydrochloride is present in human milk at relative infant doses ranging from 4.1 to 8.4% of maternal weight-adjusted dosage; although in most cases, there were no reported adverse effects in breastfed infants exposed to clonidine, there is one case report of sedation, hypotonia, and apnea in an infant exposed to clonidine through breast milk; if an infant is exposed to clonidine hydrochloride through breastmilk, monitor for symptoms of hypotension and bradycardia, such as sedation, lethargy, tachypnea and poor feeding
Consider developmental and health benefits of breastfeeding along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from drug or from underlying maternal condition; exercise caution when drug is administered to a nursing woman
Monitor breastfeeding infants exposed to drug through breast milk for symptoms of hypotension and/or bradycardia such as sedation, lethargy, tachypnea, and poor feeding
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Central sympatholytic via stimulation of central alpha receptors; results in reduced sympathetic outflow, causing decreased PVR, HR, BP, and renal vascular resistance; produces presynaptic and postjunctional alpha-2 adrenoreceptor analgesia by preventing pain signal transmission to brain
Postsynaptic alpha2-agonist stimulation may regulate subcortical activity in the prefrontal cortex, which may regulate the area of the brain responsible for attention, emotions, and behaviors, and thereby reduces hyperactivity, distractibility, and impulsiveness
Absorption
Bioavailability: Immediate release (75-85%); extended release (89%)
Onset: <1 hr (2-4 hr peak effect in blood pressure)
Duration: 6-10 hr
Peak plasma time: 1-3 hr (immediate release); 7-8 hr (extended release)
Distribution
Protein bound: 20-40%
Vd: 2.9 L/kg
Metabolism
Liver
Elimination
Half-life: 12-16 hr
Excretion: Urine (40-60%)
Administration
Hypertension
Immediate release
- May administer with or without food
- The dose must be adjusted according to the patient’s individual blood pressure response
- Increments of 0.1 mg per day may be made at weekly intervals if necessary until desired response achieved; taking the larger portion of the oral daily dose at bedtime may minimize transient adjustment effects of dry mouth and drowsiness; therapeutic doses most commonly used have ranged from 0.2 mg to 0.6 mg per day given in divided doses; studies have indicated that 2.4 mg is maximum effective daily dose, but rarely used
Transdermal patch
- Apply the transdermal therapeutic system once every 7 days to a hairless area of intact skin on upper outer arm or chest; each new application of transdermal therapeutic system should be on a different skin site from previous location
- If the system loosens during 7-day wearing, the adhesive cover should be applied directly over system to ensure good adhesion; there have been rare reports of need for patch changes prior to 7 days to maintain blood pressure control
- To initiate therapy, titrate the transdermal therapeutic system dosage according to individual therapeutic requirements, starting with CATAPRES-TTS-1; if after one or two weeks the desired reduction in blood pressure not achieved, increase dosage by adding another CATAPRES-TTS-1 or changing to a larger system; an increase in dosage above two CATAPRES-TTS-3 is usually not associated with additional efficacy
- When substituting CATAPRES-TTS transdermal therapeutic system for oral clonidine or for other antihypertensive drugs, physicians should be aware that the antihypertensive effect of CATAPRES-TTS transdermal therapeutic system may not commence until 2-3 days after initial application; gradual reduction of prior drug dosage is advised; some or all previous antihypertensive treatment may have to be continued, particularly in patients with more severe forms of hypertension
Conversion of dosage forms
-
Oral to transdermal
- Day 1: Place Catapress-TTS-1; administer 100% of oral dose
- Day 2: Administer 50% of oral dose
- Day 3: Administer 25% of oral dose
- Day 4: Patch remains, no further oral supplement needed
-
Transdermal to oral
- Clonidine levels persist for 8 hr after removing transdermal patch and decrease slowly over several days; effects may persist for 24-48 hr after removal
- Consider a persistent effect on blood pressure when initiating immediate release clonidine; consider initiating immediate release oral clonidine no sooner than 8 hr after patch removal
Attention Deficit Disorder
Extended-release tablets
- Substitution of extended-release for other clonidine products on an mg-per-mg basis not recommended
- Doses 0.2 mg/day or greater should be divided BID, with either an equal or higher split dosage being given at bedtime
- Tablet must be swallowed whole, never crushed, cut, or chewed, and may be taken with or without food; when initiating treatment, provide dosage escalation instructions
Cancer pain
- Dilute 500 mcg/mL to 100 mcg/mL with 0.9% NaCl before administration
- Epidural infusion considered as adjunct to intraspinal opiate therapy; epidural administration (Duraclon) is indicated in combination with opiates for the treatment of severe pain in patients with cancer not adequately relieved by opioid analgesics alone
- More likely to be effective in patients with neuropathic pain than in those with somatic or visceral pain
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Catapres-TTS-2 transdermal - | 0.2 mg/24 hr transdermal system |  | |
| Catapres-TTS-1 transdermal - | 0.1 mg/24 hr transdermal system |  | |
| Catapres-TTS-3 transdermal - | 0.3 mg/24 hr transdermal system |  | |
| clonidine transdermal - | 0.3 mg/24 hr transdermal system |  | |
| clonidine transdermal - | 0.1 mg/24 hr transdermal system |  | |
| clonidine transdermal - | 0.3 mg/24 hr transdermal system |  | |
| clonidine transdermal - | 0.2 mg/24 hr transdermal system |  | |
| clonidine transdermal - | 0.1 mg/24 hr transdermal system |  | |
| clonidine transdermal - | 0.3 mg/24 hr transdermal system |  | |
| clonidine transdermal - | 0.2 mg/24 hr transdermal system |  | |
| clonidine transdermal - | 0.1 mg/24 hr transdermal system |  | |
| clonidine transdermal - | 0.3 mg/24 hr transdermal system |  | |
| clonidine transdermal - | 0.2 mg/24 hr transdermal system |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
clonidine transdermal
CLONIDINE - TRANSDERMAL
(KLON-i-deen)
COMMON BRAND NAME(S): Catapres-TTS
USES: This medication is used alone or with other medications to treat high blood pressure (hypertension). Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Clonidine belongs to a class of drugs (central alpha agonists) that act in the brain to lower blood pressure. It works by relaxing blood vessels so blood can flow more easily.
HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start taking clonidine and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Peel off the backing from the patch and apply the patch to a clean, dry, and hairless area of the skin on the upper outer arm or upper chest. Press the patch firmly in place for about 10 seconds to make sure it stays on. Do not apply the patch on oily, broken, or irritated skin. Avoid applying the patch to areas of the skin where it might be easily rubbed off (such as on skin folds). Use this medication as directed by your doctor. The patch is usually worn for 1 week and then replaced. Follow the dosing schedule carefully. Wash your hands after handling the patch.The dosage is based on your medical condition and response to treatment.When replacing your patch, make sure to apply the new patch to a different area. Fold the old patch in half with the sticky side together and throw away in the trash away from children and pets. Do not flush the patch down the toilet.If the patch starts to loosen from the skin, you may apply the "adhesive cover" over the patch so that it does not fall off during the 1-week period. The "adhesive cover" does not contain any medication. If the patch falls off or if you have mild redness/itching/irritation around the application site, discard the patch as directed and apply a new patch to a different area.Use this medication regularly to get the most benefit from it. To help you remember, change the patch on the same day each week. It may help to mark your calendar with a reminder. Keep using this medication even if you feel well. Most people with high blood pressure do not feel sick.Do not stop using this medication without consulting your doctor. You may experience symptoms such as nervousness, agitation, shaking, and headache. A rapid rise in blood pressure may also occur if the drug is suddenly stopped. The risk is greater if you have used this drug for a long time or in high doses, or if you are also taking a beta blocker (such as atenolol). There have also been rare reports of severe, possibly fatal reactions (such as stroke) from stopping this drug too quickly. It is important that you do not run out of clonidine patches or miss any doses. To prevent any reactions while you are stopping treatment with this drug, your doctor may reduce your dose gradually. Consult your doctor or pharmacist for more details. Report any new or worsening symptoms right away.When used for a long time, this medication may not work as well and may require different dosing or an additional medication. Talk with your doctor if this medication stops working well (such as your blood pressure readings remain high or increase).
SIDE EFFECTS: Dizziness, lightheadedness, drowsiness, dry mouth, unusual tiredness, headache, or mild redness/itching/irritation at the application site may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.To reduce the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.To relieve dry mouth, suck on (sugarless) hard candy or ice chips, chew (sugarless) gum, drink water, or use a saliva substitute.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: fainting, slow/irregular heartbeat, mental/mood changes (such as irritability, depression).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before using clonidine, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney disease, heart rhythm problems (such as slow/irregular heartbeat, second- or third-degree atrioventricular block).This drug may make you dizzy or drowsy. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).If you are going to have an MRI test or cardioversion, tell health care personnel that you are using this patch. Some patches may contain metals that can cause serious burns during an MRI or cardioversion. Ask your doctor whether you will need to remove your patch before the procedure and apply a new patch afterward, and how to do so properly.Contact lens wearers may need to use wetting eye drops since this medication can cause dry eyes.Older adults may be more sensitive to the side effects of this product, especially dizziness, or drowsiness. These side effects may increase the risk of falling.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.This drug passes into breast milk and may have undesirable effects on a nursing infant. Consult your doctor before breastfeeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Tell your doctor or pharmacist if you are taking other products that cause drowsiness including alcohol, marijuana (cannabis), antihistamines (such as cetirizine, diphenhydramine), drugs for sleep or anxiety (such as alprazolam, diazepam, zolpidem), muscle relaxants, and opioid pain relievers (such as codeine).Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.Some products have ingredients that could raise your blood pressure. Tell your pharmacist what products you are using, and ask how to use them safely (especially cough-and-cold products, diet aids, or NSAIDs such as ibuprofen/naproxen).
OVERDOSE: This medication patch may be harmful if chewed or swallowed. If someone has overdosed, remove the patch if possible. For serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe dizziness/drowsiness, fainting, slow/irregular heartbeat, slow/shallow breathing, seizures.
NOTES: Do not share this medication with others.Lifestyle changes such as stress reduction programs, exercise, and dietary changes may increase the effectiveness of this medicine. Talk to your doctor or pharmacist about lifestyle changes that might benefit you.Check your blood pressure and pulse (heart rate) regularly while using this medication. Learn how to monitor your own blood pressure and pulse at home, and share the results with your doctor.
MISSED DOSE: If you forget to replace a patch at the scheduled time, replace it as soon as you remember. Call your doctor right away if you are late replacing a patch by 3 or more days.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed (see also How to Use section).
Information last revised March 2024. Copyright(c) 2024 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
