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Indications/Uses
Treatment of hypertension; may be used alone or concomitantly with other antihypertensives.
Dosage/Direction for Use
Individualize and adjust dose according to patient's blood pressure response and tolerance: Mild to moderate hypertension: Initial Dose Orally, 75 to 150 mcg twice daily, in the morning and at bedtime.
Dose may be increased in increments of 100 mcg/day until optimum response is achieved.
Maintenance Dose: Most common range is 200 to 600 mcg/day given in two divided doses.
Maximum Dose: 2400 mcg/day in two or three divided doses.
Sedative effects may be minimized by giving bulk of the daily dose at bedtime.
Severe hypertension: Increase initial dose to 300 mcg three times daily (900 mcg/day total loading dose).
Or, as prescribed by a physician.
Dose may be increased in increments of 100 mcg/day until optimum response is achieved.
Maintenance Dose: Most common range is 200 to 600 mcg/day given in two divided doses.
Maximum Dose: 2400 mcg/day in two or three divided doses.
Sedative effects may be minimized by giving bulk of the daily dose at bedtime.
Severe hypertension: Increase initial dose to 300 mcg three times daily (900 mcg/day total loading dose).
Or, as prescribed by a physician.
Overdosage
Symptoms: In a patient who ingested 100 mg clonidine, plasma levels were 60 ng/mL (1 hour), 100 ng/mL (1.5. hours), 370 ng/mL (2 hours) and 120 ng/mL (5.5 and 6.5 hours). The patient developed hypertension followed by hypotension, bradycardia, apnea, hallucinations, semicoma, and premature ventricular contractions. The patient fully recovered after intensive treatment.
Other symptoms of clonidine overdosage are bradycardia, hypotension, CNS depression, respiratory depression, apnea, hypothermia, miosis, coma, seizures, lethargy, agitation, irritability, vomiting, hypoventilation, reversible cardiac conduction defects, arrhythmias, transient hypotension, profound hypotension, weakness, somnolence, and diminished or absent reflexes.
Treatment: Naloxone may be a useful adjunct for the management of clonidine-induced respiratory depression.
Induction of emesis is usually not recommended because of rapid onset of CNS depression. Establish respiration if necessary, perform gastric lavage and administer activated charcoal. A saline cathartic limited because a maximum of 5% of circulating clonidine is removed.
Supportive care may include atropine sulfate for the treatment of persistent bradycardia, and dopamine infusion and IV for hypotension.
Hypertension can be treated with IV furosemide or diazoxide or α-blocking agents such as phentolamine. Tolazoline, an α-blocker, in IV doses of 10 mg at 30 minute intervals may reverse clonidine's effects if other efforts fail. Naloxone may be a useful adjunct for the management of clonidine-induced respiratory depression, hypotension or coma.
Other symptoms of clonidine overdosage are bradycardia, hypotension, CNS depression, respiratory depression, apnea, hypothermia, miosis, coma, seizures, lethargy, agitation, irritability, vomiting, hypoventilation, reversible cardiac conduction defects, arrhythmias, transient hypotension, profound hypotension, weakness, somnolence, and diminished or absent reflexes.
Treatment: Naloxone may be a useful adjunct for the management of clonidine-induced respiratory depression.
Induction of emesis is usually not recommended because of rapid onset of CNS depression. Establish respiration if necessary, perform gastric lavage and administer activated charcoal. A saline cathartic limited because a maximum of 5% of circulating clonidine is removed.
Supportive care may include atropine sulfate for the treatment of persistent bradycardia, and dopamine infusion and IV for hypotension.
Hypertension can be treated with IV furosemide or diazoxide or α-blocking agents such as phentolamine. Tolazoline, an α-blocker, in IV doses of 10 mg at 30 minute intervals may reverse clonidine's effects if other efforts fail. Naloxone may be a useful adjunct for the management of clonidine-induced respiratory depression, hypotension or coma.
Administration
May be taken with or without food.
Contraindications
Hypersensitivity to clonidine or any component of the product.
Special Precautions
Caution in patients with cerebrovascular disease, ischemic heart disease including myocardial infarction, renal impairment, occlusive peripheral vascular disorders such as Raynaud's disease, or those with a history of depression.
Clonidine discontinuation: Instruct patients not to discontinue clonidine therapy without consulting a physician. Abrupt withdrawal of clonidine treatment may result in symptoms such as nervousness, agitation, headache, and tremor followed by a rapid rise in blood pressure and increase in plasma catecholamine concentration. Such occurrences have usually been associated with previous administration of high oral doses (exceeding 1200 mcg/day) or with continuation of concomitant α-blocker therapy. Rare cases of hypertensive encephalopathy, cerebrovascular accidents and death have been reported after clonidine withdrawal. When discontinuing therapy, clonidine dose should be reduced gradually over 2 to 4 days to avoid withdrawal symptoms.
Use with caution in patients with severe coronary conduction disturbances, recent myocardial infarction or cerebrovascular disease, and chronic renal failure.
Use in Children: Safety and effectiveness in pediatric patients below the age of twelve years have not been established.
Clonidine discontinuation: Instruct patients not to discontinue clonidine therapy without consulting a physician. Abrupt withdrawal of clonidine treatment may result in symptoms such as nervousness, agitation, headache, and tremor followed by a rapid rise in blood pressure and increase in plasma catecholamine concentration. Such occurrences have usually been associated with previous administration of high oral doses (exceeding 1200 mcg/day) or with continuation of concomitant α-blocker therapy. Rare cases of hypertensive encephalopathy, cerebrovascular accidents and death have been reported after clonidine withdrawal. When discontinuing therapy, clonidine dose should be reduced gradually over 2 to 4 days to avoid withdrawal symptoms.
Use with caution in patients with severe coronary conduction disturbances, recent myocardial infarction or cerebrovascular disease, and chronic renal failure.
Use in Children: Safety and effectiveness in pediatric patients below the age of twelve years have not been established.
Use In Pregnancy & Lactation
Pregnancy Category C: There are no adequate and well controlled studies in pregnant women. Use in pregnancy only when clearly needed. Exercise caution when clonidine is administered to a breastfeeding woman as it can be excreted in human milk.
Adverse Reactions
Most common: Dry mouth, drowsiness, dizziness, sedation, constipation.
Cardiovascular: Syncope, congestive heart failure, orthostatic symptoms, palpitations, tachycardia, bradycardia, Raynaud's phenomenon, ECG abnormalities (e.g., sinus node arrest) manifested as Wenckebach period or ventricular trigeminy, conduction disturbances, arrhythmias, sinus bradycardia and atrioventricular block (rare).
CNS: Dreams or nightmares, insomnia, hallucinations, delirium, nervousness, agitation, restlessness, anxiety, depression, headache.
Dermatologic: Rash, angioneurotic edema, hives, urticaria, alopecia, pruritus.
Gastrointestinal: Abdominal pain, anorexia, malaise, nausea, vomiting, mild transient abnormalities in liver function tests, hepatitis, parotitis (rare).
Genitourinary: Impotence, decreased sexual activity, loss of libido, nocturia, in micturition, and urinary retention.
Hematologic: Thrombocytopenia (rare).
Metabolic: Weight gain, transient elevation of blood glucose or serum creatinine phosphokinase (rare), gynecomastia.
Musculoskeletal: Weakness, fatigue, muscle or joint pain, cramps of the lower limbs.
Miscellaneous: Increased sensitivity to alcohol, dryness and itching or burning of the eyes, dryness of the nasal mucosa, pallor, fear, weakly positive Coombs' test, blurred vision.
Cardiovascular: Syncope, congestive heart failure, orthostatic symptoms, palpitations, tachycardia, bradycardia, Raynaud's phenomenon, ECG abnormalities (e.g., sinus node arrest) manifested as Wenckebach period or ventricular trigeminy, conduction disturbances, arrhythmias, sinus bradycardia and atrioventricular block (rare).
CNS: Dreams or nightmares, insomnia, hallucinations, delirium, nervousness, agitation, restlessness, anxiety, depression, headache.
Dermatologic: Rash, angioneurotic edema, hives, urticaria, alopecia, pruritus.
Gastrointestinal: Abdominal pain, anorexia, malaise, nausea, vomiting, mild transient abnormalities in liver function tests, hepatitis, parotitis (rare).
Genitourinary: Impotence, decreased sexual activity, loss of libido, nocturia, in micturition, and urinary retention.
Hematologic: Thrombocytopenia (rare).
Metabolic: Weight gain, transient elevation of blood glucose or serum creatinine phosphokinase (rare), gynecomastia.
Musculoskeletal: Weakness, fatigue, muscle or joint pain, cramps of the lower limbs.
Miscellaneous: Increased sensitivity to alcohol, dryness and itching or burning of the eyes, dryness of the nasal mucosa, pallor, fear, weakly positive Coombs' test, blurred vision.
Drug Interactions
Concomitant administration of substances with a negative chronotropic or dromotropic effect such as non-steroidal agents can reduce the therapeutic effect of clonidine.
Central Nervous System (CNS) Depressants: Clonidine may be additive with, or may potentiate the action of other CNS depressants such as opiates or other analgesics, barbiturates or other sedatives, anesthetics, or alcohol. Concomitant administration of opiate analgesics with clonidine may also potentiate the hypotensive effects of clonidine.
Psychotherapeutic Agents: Tricyclic antidepressants (e.g., imipramine, desipramine) may block the antihypertensive effects of clonidine and possibly life-threatening elevations in blood pressure may occur.
Beta-adrenergic Blocking Agents: Concomitant administration with clonidine may result in attenuation or reversal of antihypertensive effect and potentially life-threatening increases in blood pressure.
Central Nervous System (CNS) Depressants: Clonidine may be additive with, or may potentiate the action of other CNS depressants such as opiates or other analgesics, barbiturates or other sedatives, anesthetics, or alcohol. Concomitant administration of opiate analgesics with clonidine may also potentiate the hypotensive effects of clonidine.
Psychotherapeutic Agents: Tricyclic antidepressants (e.g., imipramine, desipramine) may block the antihypertensive effects of clonidine and possibly life-threatening elevations in blood pressure may occur.
Beta-adrenergic Blocking Agents: Concomitant administration with clonidine may result in attenuation or reversal of antihypertensive effect and potentially life-threatening increases in blood pressure.
Storage
Store at temperature not exceeding 30°C.
Action
Pharmacology: Pharmacodynamics: Clonidine, an imidazoline derivative, is a central α-adrenergic stimulant that inhibits sympathetic cardio-accelerator and vasoconstrictor centers. Clonidine stimulates peripheral α-adrenergic receptors producing transient vasoconstriction. Stimulation of α-adrenergic receptors in the brain stem results in reduced sympathetic from the central nervous system (CNS) and a decrease in peripheral resistance, renal vascular resistance, heart rate and blood pressure. Renal blood and glomerular rate remain essentially unchanged.
Orthostatic effects are mild and infrequent. The drug does not alter normal hemodynamic responses to exercise. Acute studies have demonstrated a moderate reduction (15% to 20%) of cardiac output and a decrease or peripheral resistance. During long-term therapy, cardiac output tends to return to control values while peripheral resistance remains decreased. The coadministration of a diuretic enhances antihypertensive of clonidine.
Blood pressure declines within 30 to 60 minutes after an oral clonidine dose.
Pharmacokinetics: The peak plasma clonidine level occurs approximately 3 to 5 hours after oral dosing, the plasma half-life is 12 to 16 hours and the elimination half-life is 6 to 24 hours. About 50% of the absorbed dose is metabolized in the liver. The half-life increases up to 41 hours in patients with impaired renal function. About 40% to 60% of the absorbed dose is recovered in the urine as unchanged drug in 24 hours.
Orthostatic effects are mild and infrequent. The drug does not alter normal hemodynamic responses to exercise. Acute studies have demonstrated a moderate reduction (15% to 20%) of cardiac output and a decrease or peripheral resistance. During long-term therapy, cardiac output tends to return to control values while peripheral resistance remains decreased. The coadministration of a diuretic enhances antihypertensive of clonidine.
Blood pressure declines within 30 to 60 minutes after an oral clonidine dose.
Pharmacokinetics: The peak plasma clonidine level occurs approximately 3 to 5 hours after oral dosing, the plasma half-life is 12 to 16 hours and the elimination half-life is 6 to 24 hours. About 50% of the absorbed dose is metabolized in the liver. The half-life increases up to 41 hours in patients with impaired renal function. About 40% to 60% of the absorbed dose is recovered in the urine as unchanged drug in 24 hours.
MedsGo Class
Other Antihypertensives
Features
Dosage
75mcg
Ingredients
- Clonidine
Packaging
Tablet 100's
Generic Name
Clonidine Hydrochloride
Registration Number
DRP-1868-01
Classification
Prescription Drug (RX)
Product Questions
Questions
