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Clonidine


Pronunciation

 (KLON i deen)


U.S. Brand Names

 Catapres®; Catapres-TTS®; Duraclon™


Synonyms

 Clonidine Hydrochloride


Generic Available

 Yes: Tablet


Canadian Brand Names

 Apo-Clonidine®; Carapres®; Dixarit®; Novo-Clonidine; Nu-Clonidine


Use

 Management of mild to moderate hypertension; either used alone or in combination with other antihypertensives

Orphan drug: Duraclon™: For continuous epidural administration as adjunctive therapy with intraspinal opiates for treatment of cancer pain in patients tolerant to or unresponsive to intraspinal opiates


Use - Unlabeled/Investigational

 Heroin or nicotine withdrawal; severe pain; dysmenorrhea; vasomotor symptoms associated with menopause; ethanol dependence; prophylaxis of migraines; glaucoma; diabetes-associated diarrhea; impulse control disorder, attention-deficit/hyperactivity disorder (ADHD), clozapine-induced sialorrhea


Pregnancy Risk Factor

 C


Pregnancy Implications

 Clonidine crosses the placenta. Caution should be used with this drug due to the potential of rebound hypertension with abrupt discontinuation.


Lactation

 Enters breast milk/not recommended


Contraindications

 Hypersensitivity to clonidine hydrochloride or any component of the formulation


Warnings/Precautions

 Gradual withdrawal is needed (over 1 week for oral, 2-4 days with epidural) if drug needs to be stopped. Patients should be instructed about abrupt discontinuation (causes rapid increase in BP and symptoms of sympathetic overactivity). In patients on both a beta-blocker and clonidine where withdrawal of clonidine is necessary, withdraw the beta-blocker first and several days before clonidine. Then slowly decrease clonidine.

Use with caution in patients with severe coronary insufficiency; conduction disturbances; recent MI, CVA, or chronic renal insufficiency. Caution in sinus node dysfunction. Discontinue within 4 hours of surgery then restart as soon as possible after. Clonidine injection should be administered via a continuous epidural infusion device. Epidural clonidine is not recommended for perioperative, obstetrical, or postpartum pain. It is not recommended for use in patients with severe cardiovascular disease or hemodynamic instability. In all cases, the epidural may lead to cardiovascular instability (hypotension, bradycardia). Transdermal patch may contain conducting metal (eg, aluminum); remove patch prior to MRI. Clonidine cause significant CNS depression and xerostomia. Caution in patients with pre-existing CNS disease or depression. Elderly may be at greater risk for CNS depressive effects, favoring other agents in this population.


Adverse Reactions

 Incidence of adverse events is not always reported.

>10%:

Central nervous system: Drowsiness (35% oral, 12% transdermal), dizziness (16% oral, 2% transdermal)

Dermatologic: Transient localized skin reactions characterized by pruritus, and erythema (15% to 50% transdermal)

Gastrointestinal: Dry mouth (40% oral, 25% transdermal)

1% to 10%:

Cardiovascular: Orthostatic hypotension (3% oral)

Central nervous system: Headache (1% oral, 5% transdermal), sedation (3% transdermal), fatigue (6% transdermal), lethargy (3% transdermal), insomnia (2% transdermal), nervousness (3% oral, 1% transdermal), mental depression (1% oral)

Dermatologic: Rash (1% oral), allergic contact sensitivity (5% transdermal), localized vesiculation (7%), hyperpigmentation (5% at application site), edema (3%), excoriation (3%), burning (3%), throbbing, blanching (1%), papules (1%), and generalized macular rash (1%) has occurred in patients receiving transdermal clonidine.

Endocrine & metabolic: Sodium and water retention, sexual dysfunction (3% oral, 2% transdermal), impotence (3% oral, 2% transdermal)

Gastrointestinal: Nausea (5% oral, 1% transdermal), vomiting (5% oral), anorexia and malaise (1% oral), constipation (10% oral, 1% transdermal), dry throat (2% transdermal), taste disturbance (1% transdermal), weight gain (1% oral)

Genitourinary: Nocturia (1% oral)

Hepatic: Liver function test (mild abnormalities, 1% oral)

Neuromuscular & skeletal: Weakness (10% transdermal)

Miscellaneous: Withdrawal syndrome (1% oral)

<1% (Limited to important or life-threatening): Hepatitis (oral), difficulty in micturition (oral, transdermal), urinary retention (oral), hives (oral, transdermal), angioedema (oral, transdermal), urticaria (oral, transdermal), alopecia (oral, transdermal), parotid pain (oral), gynecomastia (oral, transdermal), transient elevation of blood glucose (oral), elevation of creatinine phosphokinase (oral), palpitation (oral, transdermal), tachycardia (oral, transdermal), bradycardia (oral), sinus bradycardia (oral, transdermal), atrioventricular block (oral, transdermal), CHF (oral, transdermal), ECG abnormalities (oral, transdermal), flushing, pallor, Raynaud's phenomenon (oral, transdermal), chest pain (transdermal), increase in blood pressure (transdermal), weakness, muscle or joint pain (0.6% oral), leg cramps (0.3% oral), fever (oral, transdermal), malaise (transdermal), withdrawal syndrome (transdermal), vivid dreams (oral, transdermal), nightmares (oral, transdermal), insomnia (oral), behavioral changes (transdermal), restlessness (oral, transdermal), anxiety (oral, transdermal), mental depression (transdermal), visual and auditory hallucinations (oral, transdermal), delirium (transdermal), CVA (transdermal), irritability (transdermal), weight gain (transdermal), rash (transdermal), orthostatic symptoms (transdermal), syncope (oral, transdermal), agitation (transdermal), contact dermatitis (transdermal), localized hypo- or hyperpigmentation (transdermal), anorexia (transdermal), vomiting (transdermal), loss of libido (transdermal), decreased sexual activity (transdermal), blurred vision (transdermal), burning of the eyes (transdermal), dryness of the eyes (transdermal), weakly positive Coombs' test (oral), increased sensitivity to ethanol (oral), thrombocytopenia (oral), abdominal pain (oral), pseudo-obstruction (oral)


Overdosage/Toxicology

 Symptoms of overdose include bradycardia, CNS depression, hypothermia, diarrhea, respiratory depression, and apnea. Treatment is supportive and symptomatic. Naloxone may be utilized in treating CNS depression and/or apnea and should be given I.V., 0.4-2 mg, with repeated doses as needed up to a total of 10 mg, or as an infusion.


Drug Interactions

Antipsychotics: Concurrent use with antipsychotics (especially low potency) or nitroprusside may produce additive hypotensive effects

Beta-blockers: May potentiate bradycardia in patients receiving clonidine and may increase the rebound hypertension of withdrawal; discontinue beta-blocker several days before clonidine is tapered

CNS depressants: Sedative effects may be additive; monitor for increased effect; includes barbiturates, benzodiazepines, narcotic analgesics, ethanol, and other sedative agents

Cyclosporine: Clonidine may increase cyclosporine (and perhaps tacrolimus) serum concentrations; cyclosporine dosage adjustment may be needed

Hypoglycemic agents: Clonidine may decrease the symptoms of hypoglycemia; monitor patients receiving antidiabetic agents

Levodopa: Effects may be reduced by clonidine in some patients with Parkinson's disease (limited documentation); monitor

Local anesthetics: Epidural clonidine may prolong the sensory and motor blockade of local anesthetics

Mirtazapine: Antihypertensive effects of clonidine may be antagonized by mirtazapine (hypertensive urgency has been reported following addition of mirtazapine to clonidine); in addition, mirtazapine may potentially enhance the hypertensive response associated with abrupt clonidine withdrawal. Avoid this combination; consider an alternative agent.

Narcotic analgesics: May potentiate hypotensive effects of clonidine

Tricyclic antidepressants: Antihypertensive effects of clonidine may be antagonized by tricyclic antidepressants; in addition, tricyclic antidepressants may enhance the hypertensive response associated with abrupt clonidine withdrawal; avoid this combination; consider an alternative agent

Verapamil: Concurrent administration may be associated with hypotension and AV block in some patients (limited documentation); monitor


Ethanol/Nutrition/Herb Interactions

Ethanol: Avoid ethanol (may increase CNS depression).

Herb/Nutraceutical: Avoid dong quai if using for hypertension (has estrogenic activity). Avoid ephedra, yohimbe, ginseng (may worsen hypertension). Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression).


Compatibility

Y-site administration: Compatible: Lorazepam

Compatibility in syringe: Compatible: Bupivacaine with morphine, fentanyl with lidocaine, ketamine with tetracaine


Mechanism of Action

 Stimulates alpha2-adrenoceptors in the brain stem, thus activating an inhibitory neuron, resulting in reduced sympathetic outflow from the CNS, producing a decrease in peripheral resistance, renal vascular resistance, heart rate, and blood pressure; epidural clonidine may produce pain relief at spinal presynaptic and postjunctional alpha2-adrenoceptors by preventing pain signal transmission; pain relief occurs only for the body regions innervated by the spinal segments where analgesic concentrations of clonidine exist


Pharmacodynamics/Kinetics

Onset of action: Oral: 0.5-1 hour

Duration: 6-10 hours

Distribution: Vd: Adults: 2.1 L/kg; highly lipid soluble; distributes readily into extravascular sites

Protein binding: 20% to 40%

Metabolism: Extensively hepatic to inactive metabolites; undergoes enterohepatic recirculation

Bioavailability: 75% to 95%

Half-life elimination: Adults: Normal renal function: 6-20 hours; Renal impairment: 18-41 hours

Time to peak: 2-4 hours

Excretion: Urine (65%, 32% as unchanged drug); feces (22%)


Dosage

Children:

Oral:

Hypertension: Initial: 5-10 mcg/kg/day in divided doses every 8-12 hours; increase gradually at 5- to 7-day intervals to 25 mcg/kg/day in divided doses every 6 hours; maximum: 0.9 mg/day

Clonidine tolerance test (test of growth hormone release from pituitary): 0.15 mg/m 2 or 4 mcg/kg as single dose

ADHD (unlabeled use): Initial: 0.05 mg/day; increase every 3-7 days by 0.05 mg/day to 3-5 mcg/kg/day given in divided doses 3-4 times/day (maximum dose: 0.3-0.4 mg/day)

Epidural infusion: Pain management: Reserved for patients with severe intractable pain, unresponsive to other analgesics or epidural or spinal opiates: Initial: 0.5 mcg/kg/hour; adjust with caution, based on clinical effect

Adults:

Oral:

Acute hypertension (urgency): Initial 0.1-0.2 mg; may be followed by additional doses of 0.1 mg every hour, if necessary, to a maximum total dose of 0.6 mg.

Unlabeled route of administration: Sublingual clonidine 0.1-0.2 mg twice daily may be effective in patients unable to take oral medication

Hypertension: Initial dose: 0.1 mg twice daily (maximum recommended dose: 2.4 mg/day); usual dose range (JNC 7): 0.1-0.8 mg/day in 2 divided doses

Nicotine withdrawal symptoms: 0.1 mg twice daily to maximum of 0.4 mg/day for 3-4 weeks

Transdermal: Hypertension: Apply once every 7 days; for initial therapy start with 0.1 mg and increase by 0.1 mg at 1- to 2-week intervals (dosages >0.6 mg do not improve efficacy); usual dose range (JNC 7): 0.1-0.3 mg once weekly

Epidural infusion: Pain management: Starting dose: 30 mcg/hour; titrate as required for relief of pain or presence of side effects; minimal experience with doses >40 mcg/hour; should be considered an adjunct to intraspinal opiate therapy

Elderly: Initial: 0.1 mg once daily at bedtime, increase gradually as needed

Dosing adjustment in renal impairment: Clcr<10 mL/minute: Administer 50% to 75% of normal dose initially

Dialysis: Not dialyzable (0% to 5%) via hemo- or peritoneal dialysis; supplemental dose not necessary


Administration

Oral: Do not discontinue clonidine abruptly. if needed, gradually reduce dose over 2-4 days to avoid rebound hypertension

Transdermal patch: Patches should be applied weekly at bedtime to a clean, hairless area of the upper outer arm or chest. Rotate patch sites weekly. Redness under patch may be reduced if a topical corticosteroid spray is applied to the area before placement of the patch.


Monitoring Parameters

 Blood pressure, standing and sitting/supine, mental status, heart rate


Reference Range

 Therapeutic: 1-2 ng/mL (SI: 4.4-8.7 nmol/L)


Dietary Considerations

 Hypertensive patients may need to decrease sodium and calories in diet.


Patient Education

 Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take anything new (especially cough or cold remedies and sleep or stay-awake medications that might affect blood pressure) during treatment unless approved by prescriber. Take as directed, at bedtime. If using patch, check daily for correct placement. Avoid alcohol. Do not skip doses or discontinue without consulting prescriber (this drug must be discontinued on specific schedule to prevent serious adverse effects). This medication may cause drowsiness, dizziness, or impaired judgment (use caution when driving or engaging in tasks that require alertness until response is known); decreased libido or sexual function (will resolve when drug is discontinued); postural hypotension (use caution when rising from sitting or lying position or when climbing stairs); constipation (increase roughage, bulk in diet); or dry mouth or nausea (frequent mouth care or sucking lozenges may help). Report difficulty, pain, or burning on urination; increased nervousness or depression; sudden weight gain (weigh yourself in the same clothes at the same time of day once a week); unusual or persistent swelling of ankles, feet, or extremities; wet cough or respiratory difficulty; chest pain or palpitations; muscle weakness, fatigue, or pain; or other persistent side effects. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Breast-feeding is not recommended.


Additional Information

 Transdermal clonidine should only be used in patients unable to take oral medication. The transdermal product is much more expensive than oral clonidine and produces no better therapeutic effects.


Anesthesia and Critical Care Concerns/Other Considerations

 Abrupt withdrawal from clonidine therapy should be avoided. Clonidine patch has provided an important alternative to frequent daily dosing; may be used in patients unable to take oral medication.


Cardiovascular Considerations

 Tolerance to the blood pressure lowering effects of clonidine may develop with long-term therapy. Abrupt withdrawal from clonidine therapy should be very specifically avoided. The advent of the clonidine patch has provided an important alternative to frequent daily dosing. However, it is important that overlap of therapy be maintained when switching from oral medications to the patch. Important side effects of clonidine include drowsiness. It has also been suggested that clonidine may be useful in promoting smoking cessation.

Note that the use of moxonidine to lower sympathetic activation in patients with heart failure was associated with increased mortality.


Dental Health: Effects on Dental Treatment

 Key adverse event(s) related to dental treatment: Significant xerostomia (normal salivary flow resumes upon discontinuation), orthostatic hypotension, and abnormal taste.


Dental Health: Vasoconstrictor/Local Anesthetic Precautions

 No information available to require special precautions


Mental Health: Effects on Mental Status

 Drowsiness is common


Mental Health: Effects on Psychiatric Treatment

 Dry mouth, orthostatic hypotension, and sedation may be increased with concurrent psychotropic use; used to treat clozapine-induced sialorrhea (unlabeled use); TCAs may antagonize clonidine's hypotensive effect


Dosage Forms

Injection, epidural solution, as hydrochloride [preservative free] (Duraclon™): 100 mcg/mL (10 mL); 500 mcg/mL (10 mL)

Patch, transdermal [once-weekly patch]:

Catapres-TTS®-1: 0.1 mg/24 hours (4s)

Catapres-TTS®-2: 0.2 mg/24 hours (4s)

Catapres-TTS®-3: 0.3 mg/24 hours (4s)

Tablet, as hydrochloride (Catapres®): 0.1 mg, 0.2 mg, 0.3 mg


References

"American Academy of Pediatrics Subcommittee on Attention-Deficit/Hyperactivity Disorder and Committee on Quality Improvement. Clinical Practice Guidelines: Treatment of the School-Aged Child With Attention-Deficit/Hyperactivity Disorder," Pediatrics , 2001, 108(4):1033-44.

Capogna G, Celleno D, Zangrillo A, et al, "Addition of Clonidine to Epidural Morphine Enhances Postoperative Analgesia After Cesarean Delivery," Reg Anesth , 1995, 20(1):57-61.

Chobanian AV, Bakris GL, Black HR, et al, "The Seventh Report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure: The JNC 7 Report," JAMA , 2003, 289(19):2560-71.

Corazza M, Mantovani L, Virgil A, et al, "Allergic Contact Dermatitis From a Clonidine Transdermal Delivery System," Contact Dermatitis , 1995, 32(4):246.

Fizer DH, Moss MN, and Walker W, "Critical Care for Clonidine Poisoning in Toddlers," Crit Care Med , 1990, 18(10):1124-8.

Fowler MA, Wheeler CA, and Wasserman GS, "Case 01-1995: A Two Year Old Female With Alteration of Consciousness," Pediatr Emerg Care , 1995, 11(1):62.

Hart-Santora D and Hart LL, "Clonidine in Attention Deficit Hyperactivity Disorder," Ann Pharmacother , 1992, 26(1):37-9.

Henretig F, Wiley J, and Brown L, "Clonidine Patch Toxicity: The Proof's in the Poop!" Clin Toxicol , 1995, 33(5):520-1.

Hunt RD, Minderaa RB, and Cohen DJ, "The Therapeutic Effect of Clonidine in Attention Deficit Disorder With Hyperactivity: A Comparison With Placebo and Methylphenidate," Psychopharmacol Bull , 1986, 22(1):229-35.

Klein MD, "An Unusual Cause of Clonidine Toxicity," Am J Emerg Med , 1991, 9(4):409-10.

Kulig K, Duffy JP, Rumack BH, et al, "Naloxone for the Treatment of Clonidine Overdose," JAMA , 1982, 247(12):1697.

Rocchini AP, "Childhood Hypertension: Etiology, Diagnosis, and Treatment," Pediatr Clin North Am , 1984, 31(6):1259-73.

Sinaiko AR, "Pharmacologic Management of Childhood Hypertension," Pediatr Clin North Am , 1993, 40(1):195-212.

"Smoking Cessation Clinical Practice Guidelines. The Agency for Health Care Policy and Research," JAMA , 1996, 275:1270-80.


International Brand Names

 Adesipress-TTS® (IT); Apo-Clonidine® (CA); Aruclonin® (CZ, DE, HU); Atensina® (BR); Carapres® (CA); Catapresan® (AR, AT, CH, CL, CO, CZ, DE, DK, ES, FI, IT, NL, NO, PL, PT, SE); Catapresan TTS® (IT); Catapres® (AU, CY, EG, GB, HK, ID, IE, IN, JO, JP, KW, LB, MT, NZ, TH, TR); Catapressan® (BE, FR, LU); Catapres-TTS® (NZ); Clonidina Clorhidrat® (RO); Clonidina Drawer® (AR); Clonidina Larjan® (AR); Clonidina® (RO); Clonidine® (GB); Clonidin-ratiopharm® (DE); Clonidin Riker® (DE); Clonid-Ophtal® (DE); Clonidural® (AR); Clonistada® (DE, PL); Clonnirit® (IL); Dispaclonidin® (DE); Dixarit® (BE, CA, CY, EG, GB, HK, IE, JO, KW, LB, LU, MT, NL, NZ, SG, TR, ZA); Glausine® (AT); Haemiton® (DE, RO, RU); Iporel® (PL); Isoglaucon® (AT, DE, ES, IT); Menograine® (ZA); Mirfat® (DE); Normopresan® (IL); Novo-Clonidine (CA); Nu-Clonidine (CA); Paracefan® (DE); Paracefan® [inj.] (DE)


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