Catapres Prescribing Information

Drug Detail:Catapres (Clonidine (oral) [ kloe-ni-deen ])

Drug Class: Antiadrenergic agents, centrally acting

Oral Antihypertensive
Tablets of 0.1, 0.2 and 0.3 mg

Catapres Description

Catapres® (clonidine hydrochloride, USP) is a centrally acting alpha-agonist hypotensive agent available as tablets for oral administration in three dosage strengths: 0.1 mg, 0.2 mg and 0.3 mg. The 0.1 mg tablet is equivalent to 0.087 mg of the free base.

The inactive ingredients are colloidal silicon dioxide, corn starch, dibasic calcium phosphate, FD&C Yellow No. 6, gelatin, glycerin, lactose, and magnesium stearate. The Catapres 0.1 mg tablet also contains FD&C Blue No.1 and FD&C Red No.3.

Clonidine hydrochloride is an imidazoline derivative and exists as a mesomeric compound. The chemical name is 2-(2,6-dichlorophenylamino)-2-imidazoline hydrochloride. The following is the structural formula:

Clonidine hydrochloride is an odorless, bitter, white, crystalline substance soluble in water and alcohol.

Catapres - Clinical Pharmacology

Clonidine stimulates alpha-adrenoreceptors in the brain stem. This action results in reduced sympathetic outflow from the central nervous system and in decreases in peripheral resistance, renal vascular resistance, heart rate, and blood pressure. CATAPRES tablets act relatively rapidly. The patient’s blood pressure declines within 30 to 60 minutes after an oral dose, the maximum decrease occurring within 2 to 4 hours. Renal blood flow and glomerular filtration rate remain essentially unchanged. Normal postural reflexes are intact; therefore, orthostatic symptoms are mild and infrequent.

Acute studies with clonidine hydrochloride in humans have demonstrated a moderate reduction (15% to 20%) of cardiac output in the supine position with no change in the peripheral resistance: at a 45° tilt there is a smaller reduction in cardiac output and a decrease of peripheral resistance. During long term therapy, cardiac output tends to return to control values, while peripheral resistance remains decreased. Slowing of the pulse rate has been observed in most patients given clonidine, but the drug does not alter normal hemodynamic response to exercise.

Tolerance to the antihypertensive effect may develop in some patients, necessitating a reevaluation of therapy.

Other studies in patients have provided evidence of a reduction in plasma renin activity and in the excretion of aldosterone and catecholamines. The exact relationship of these pharmacologic actions to the antihypertensive effect of clonidine has not been fully elucidated.

Clonidine acutely stimulates growth hormone release in both children and adults, but does not produce a chronic elevation of growth hormone with long-term use.

Pharmacokinetics

The pharmacokinetics of clonidine is dose-proportional in the range of 100 to 600 µg. The absolute bioavailability of clonidine on oral administration is 70% to 80%. Peak plasma clonidine levels are attained in approximately 1 to 3 hours.

Following intravenous administration, clonidine displays biphasic disposition with a distribution half-life of about 20 minutes and an elimination half-life ranging from 12 to 16 hours. The half-life increases up to 41 hours in patients with severe impairment of renal function. Clonidine crosses the placental barrier. It has been shown to cross the blood-brain barrier in rats.

Following oral administration about 40% to 60% of the absorbed dose is recovered in the urine as unchanged drug in 24 hours. About 50% of the absorbed dose is metabolized in the liver. Neither food nor the race of the patient influences the pharmacokinetics of clonidine.

The antihypertensive effect is reached at plasma concentrations between about 0.2 and 2.0 ng/mL in patients with normal excretory function. A further rise in the plasma levels will not enhance the antihypertensive effect.

Indications and Usage for Catapres

CATAPRES tablets are indicated in the treatment of hypertension. CATAPRES tablets may be employed alone or concomitantly with other antihypertensive agents.

Contraindications

Catapres® (clonidine hydrochloride, USP) tablets should not be used in patients with known hypersensitivity to clonidine (see PRECAUTIONS).

Warnings

Withdrawal

Patients should be instructed not to discontinue therapy without consulting their physician. Sudden cessation of clonidine treatment has, in some cases, resulted in symptoms such as nervousness, agitation, headache, and tremor accompanied or followed by a rapid rise in blood pressure and elevated catecholamine concentrations in the plasma. The likelihood of such reactions to discontinuation of clonidine therapy appears to be greater after administration of higher doses or continuation of concomitant beta-blocker treatment and special caution is therefore advised in these situations. Rare instances of hypertensive encephalopathy, cerebrovascular accidents and death have been reported after clonidine withdrawal. When discontinuing therapy with CATAPRES tablets, the physician should reduce the dose gradually over 2 to 4 days to avoid withdrawal symptomatology.

An excessive rise in blood pressure following discontinuation of CATAPRES tablets therapy can be reversed by administration of oral clonidine hydrochloride or by intravenous phentolamine. If therapy is to be discontinued in patients receiving a beta-blocker and clonidine concurrently, the beta-blocker should be withdrawn several days before the gradual discontinuation of CATAPRES tablets.

Because children commonly have gastrointestinal illnesses that lead to vomiting, they may be particularly susceptible to hypertensive episodes resulting from abrupt inability to take medication.

Precautions

Pregnancy

Teratogenic Effects

Reproduction studies performed in rabbits at doses up to approximately 3 times the oral maximum recommended daily human dose (MRDHD) of Catapres® (clonidine hydrochloride, USP) tablets produced no evidence of a teratogenic or embryotoxic potential in rabbits. In rats, however, doses as low as 1/3 the oral MRDHD (1/15 the MRDHD on a mg/m2 basis) of clonidine were associated with increased resorptions in a study in which dams were treated continuously from 2 months prior to mating. Increased resorptions were not associated with treatment at the same time or at higher dose levels (up to 3 times the oral MRDHD) when the dams were treated on gestation days 6 to 15. Increases in resorption were observed at much higher dose levels (40 times the oral MRDHD on a mg/kg basis; 4 to 8 times the MRDHD on a mg/m2 basis) in mice and rats treated on gestation days 1 to 14 (lowest dose employed in the study was 500 µg/kg).

No adequate, well-controlled studies have been conducted in pregnant women. Clonidine crosses the placental barrier (see CLINICAL PHARMACOLOGY, Pharmacokinetics). Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Nursing Mothers

As clonidine hydrochloride is excreted in human milk, caution should be exercised when CATAPRES tablets are administered to a nursing woman.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established in adequate and well-controlled trials (see WARNINGS, Withdrawal).

Adverse Reactions/Side Effects

Most adverse effects are mild and tend to diminish with continued therapy. The most frequent (which appear to be dose-related) are dry mouth, occurring in about 40 of 100 patients; drowsiness, about 33 in 100; dizziness, about 16 in 100; constipation and sedation, each about 10 in 100.

The following less frequent adverse experiences have also been reported in patients receiving CATAPRES tablets, but in many cases patients were receiving concomitant medication and a causal relationship has not been established.

Body as a Whole: Fatigue, fever, headache, pallor, weakness, and withdrawal syndrome. Also reported were a weakly positive Coombs’ test and increased sensitivity to alcohol.

Cardiovascular: Bradycardia, congestive heart failure, electrocardiographic abnormalities (i.e., sinus node arrest, junctional bradycardia, high degree AV block and arrhythmias), orthostatic symptoms, palpitations, Raynaud’s phenomenon, syncope, and tachycardia. Cases of sinus bradycardia and atrioventricular block have been reported, both with and without the use of concomitant digitalis.

Central Nervous System: Agitation, anxiety, delirium, delusional perception, hallucinations (including visual and auditory), insomnia, mental depression, nervousness, other behavioral changes, paresthesia, restlessness, sleep disorder, and vivid dreams or nightmares.

Dermatological: Alopecia, angioneurotic edema, hives, pruritus, rash, and urticaria.

Gastrointestinal: Abdominal pain, anorexia, constipation, hepatitis, malaise, mild transient abnormalities in liver function tests, nausea, parotitis, pseudo-obstruction (including colonic pseudo-obstruction), salivary gland pain, and vomiting.

Genitourinary: Decreased sexual activity, difficulty in micturition, erectile dysfunction, loss of libido, nocturia, and urinary retention.

Hematologic: Thrombocytopenia.

Metabolic: Gynecomastia, transient elevation of blood glucose or serum creatine phosphokinase, and weight gain.

Musculoskeletal: Leg cramps and muscle or joint pain.

Oro-otolaryngeal: Dryness of the nasal mucosa.

Ophthalmological: Accommodation disorder, blurred vision, burning of the eyes, decreased lacrimation, and dryness of eyes.

Overdosage

Hypertension may develop early and may be followed by hypotension, bradycardia, respiratory depression, hypothermia, drowsiness, decreased or absent reflexes, weakness, irritability and miosis. The frequency of CNS depression may be higher in children than adults. Large overdoses may result in reversible cardiac conduction defects or dysrhythmias, apnea, coma and seizures. Signs and symptoms of overdose generally occur within 30 minutes to two hours after exposure. As little as 0.1 mg of clonidine has produced signs of toxicity in children.

There is no specific antidote for clonidine overdosage. Clonidine overdosage may result in the rapid development of CNS depression; therefore, induction of vomiting with ipecac syrup is not recommended. Gastric lavage may be indicated following recent and/or large ingestions. Administration of activated charcoal and/or a cathartic may be beneficial. Supportive care may include atropine sulfate for bradycardia, intravenous fluids and/or vasopressor agents for hypotension and vasodilators for hypertension. Naloxone may be a useful adjunct for the management of clonidine-induced respiratory depression, hypotension and/or coma; blood pressure should be monitored since the administration of naloxone has occasionally resulted in paradoxical hypertension. Dialysis is not likely to significantly enhance the elimination of clonidine.

The largest overdose reported to date involved a 28-year old male who ingested 100 mg of clonidine hydrochloride powder. This patient developed hypertension followed by hypotension, bradycardia, apnea, hallucinations, semicoma, and premature ventricular contractions. The patient fully recovered after intensive treatment. Plasma clonidine levels were 60 ng/ml after 1 hour, 190 ng/ml after 1.5 hours, 370 ng/ml after 2 hours, and 120 ng/ml after 5.5 and 6.5 hours. In mice and rats, the oral LD50 of clonidine is 206 and 465 mg/kg, respectively.

Catapres Dosage and Administration

Adults

The dose of Catapres® (clonidine hydrochloride, USP) tablets must be adjusted according to the patient's individual blood pressure response. The following is a general guide to its administration.

Initial Dose

0.1 mg tablet twice daily (morning and bedtime). Elderly patients may benefit from a lower initial dose.

Maintenance Dose

Further increments of 0.1 mg per day may be made at weekly intervals if necessary until the desired response is achieved. Taking the larger portion of the oral daily dose at bedtime may minimize transient adjustment effects of dry mouth and drowsiness. The therapeutic doses most commonly employed have ranged from 0.2 mg to 0.6 mg per day given in divided doses. Studies have indicated that 2.4 mg is the maximum effective daily dose, but doses as high as this have rarely been employed.

Renal Impairment

Patients with renal impairment may benefit from a lower initial dose. Patients should be carefully monitored. Since only a minimal amount of clonidine is removed during routine hemodialysis, there is no need to give supplemental clonidine following dialysis.

How is Catapres supplied

Catapres® (clonidine hydrochloride, USP) tablets are supplied as follows:

Dose (mg)	Color	Marking	Bottle of 100
0.1	Tan	BI 6	NDC 0597-0006-01
0.2	Orange	BI 7	NDC 0597-0007-01
0.3	Peach	BI 11	NDC 0597-0011-01

Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F) [see USP Controlled Room Temperature].

Dispense in tight, light-resistant container.

Catapres 0.1 mg
100 tablets
NDC-0597-0006-01

Catapres 0.2 mg
100 tablets
NDC-0597-0007-01

Catapres 0.3 mg
100 tablets
NDC-0597-0011-01

CATAPRES
clonidine hydrochloride tablet

Product Information
Product Type	HUMAN PRESCRIPTION DRUG	Item Code (Source)	NDC:0597-0006
Route of Administration	ORAL

Ingredient Name	Basis of Strength	Strength
Active Ingredient/Active Moiety
clonidine hydrochloride (UNII: W76I6XXF06) (clonidine - UNII:MN3L5RMN02)	clonidine hydrochloride	0.100 mg

Product Characteristics
Color	BROWN (TAN)	Score	2 pieces
Shape	OVAL (OVAL)	Size	8mm
Flavor		Imprint Code	BI;6
Contains

#	Item Code	Package Description	Marketing Start Date	Marketing End Date
Packaging
1	NDC:0597-0006-01	100 in 1 BOTTLE, PLASTIC; Type 0: Not a Combination Product	05/01/1999

Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
Marketing Information
NDA	NDA017407	05/01/1999

CATAPRES
clonidine hydrochloride tablet

Product Information
Product Type	HUMAN PRESCRIPTION DRUG	Item Code (Source)	NDC:0597-0007
Route of Administration	ORAL

Ingredient Name	Basis of Strength	Strength
Active Ingredient/Active Moiety
clonidine hydrochloride (UNII: W76I6XXF06) (clonidine - UNII:MN3L5RMN02)	clonidine hydrochloride	0.200 mg

Product Characteristics
Color	ORANGE (ORANGE)	Score	2 pieces
Shape	OVAL (OVAL)	Size	8mm
Flavor		Imprint Code	BI;7
Contains

#	Item Code	Package Description	Marketing Start Date	Marketing End Date
Packaging
1	NDC:0597-0007-01	100 in 1 BOTTLE, PLASTIC; Type 0: Not a Combination Product	05/01/1999

Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
Marketing Information
NDA	NDA017407	05/01/1999

CATAPRES
clonidine hydrochloride tablet

Product Information
Product Type	HUMAN PRESCRIPTION DRUG	Item Code (Source)	NDC:0597-0011
Route of Administration	ORAL

Ingredient Name	Basis of Strength	Strength
Active Ingredient/Active Moiety
clonidine hydrochloride (UNII: W76I6XXF06) (clonidine - UNII:MN3L5RMN02)	clonidine hydrochloride	0.300 mg

Product Characteristics
Color	ORANGE (PEACH)	Score	2 pieces
Shape	OVAL (OVAL)	Size	9mm
Flavor		Imprint Code	BI;11
Contains

#	Item Code	Package Description	Marketing Start Date	Marketing End Date
Packaging
1	NDC:0597-0011-01	100 in 1 BOTTLE, PLASTIC; Type 0: Not a Combination Product	05/01/1999

Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
Marketing Information
NDA	NDA017407	05/01/1999

Labeler - Boehringer Ingelheim Pharmaceuticals Inc. (603175944)

Registrant - Boehringer Ingelheim Pharmaceuticals Inc. (603175944)

Name	Address	ID/FEI	Business Operations
Establishment
Boehringer Ingelheim Promeco, S.A. de C.V.		812579472	LABEL(0597-0007, 0597-0006, 0597-0011) , PACK(0597-0011, 0597-0007, 0597-0006) , MANUFACTURE(0597-0007, 0597-0006, 0597-0011) , ANALYSIS(0597-0006, 0597-0011, 0597-0007)

Name	Address	ID/FEI	Business Operations
Establishment
Boehringer Ingelheim Pharma GmbH and Co. KG		551147440	API MANUFACTURE(0597-0007) , ANALYSIS(0597-0007)

Name	Address	ID/FEI	Business Operations
Establishment
West-Ward Columbus Inc.		058839929	LABEL(0597-0011)

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Catapres Prescribing Information

Pharmacokinetics

Withdrawal

General

Perioperative Use

Information for Patients

Drug Interactions

Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

Pregnancy

Teratogenic Effects

Nursing Mothers

Pediatric Use

Adults

Initial Dose

Maintenance Dose

Renal Impairment

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Catapres Description

Catapres - Clinical Pharmacology

Pharmacokinetics

Related/similar drugs

Indications and Usage for Catapres

Contraindications

Warnings

Withdrawal

Precautions

General

Perioperative Use

Information for Patients

Drug Interactions

Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

Pregnancy

Teratogenic Effects

Nursing Mothers

Pediatric Use

Adverse Reactions/Side Effects

Overdosage

Catapres Dosage and Administration

Adults

Initial Dose

Maintenance Dose

Renal Impairment

How is Catapres supplied

Latest News

Depression and anxiety: Exercise may counter effects of Western diet

Related Drugs

Categories

About US

Quick Link

Drugs

News

Find US