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reserpine (Serpasil)

 

Classes: Antihypertensives, Other

Dosing and uses of Serpasil (reserpine)

 

Adult dosage forms and strengths

tablet

  • 0.1mg
  • 0.25mg

 

Hypertension

InitiaL

  • 0.5 mg daily for 1 or 2 weeks

Maintenance

  • 0.1-0.25 mg PO qDay
  • Use higher dosages cautiously occurrence of mental depression or other adverse reactions may increase

 

Psychiatric Disorders

0.5 mg daily, but may range from 0.1 to 1 mg

 

Pediatric dosage forms and strengths

tablet

  • 0.1mg
  • 0.25mg

 

Hypertension

0.02 mg/kg/d POqD or div BID, no more than 0.25 mg/d

 

Geriatric dosage forms and strengths

Adverse CNS effects; may cause bradycardia and orthostatic hypotension; not recommended as routine treatment for hypertension (Beers criteria)

0.05 mg PO qDay; may increase by 0.05 mg after 1 week as needed; not to exceed 0.1 mg/day

 

Serpasil (reserpine) adverse (side) effects

Frequency not defined

Angina

Bradycardia

Syncope

Dizziness

Depression

Lethargy

Nightmare

Tardive dyskinesia

GI hypersecretion

Impotence

Nasal congestion

 

Warnings

Contraindications

Hypersensitivity, active peptic ulcer, ulcerative colitis, history of depression, history of gallstones; electroconvulsive treatment within 1 week

MAOIs: discontinue several days before starting reserpine therapy

Avoid during breast-feeding

 

Cautions

Asthma

History of gall stones, PUD, ulcerative colitis

Breastfeeding

 

Pregnancy and lactation

Pregnancy category: C

Lactation: unsafe; excreted into breast milk

 

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 of Serpasil (reserpine)

Mechanism of action

Peripheral adrenergic neuron antagonist via depletion of tissue store of catecholamines resulting in bradycardia

 

Absorption

Bioavailability: 30-40%

Duration: 1-6 wk

 

Distribution

Protein binding: 96%

 

Metabolism

Extensively metabolized in the liver

Metabolites: trimethylbenzoic acid, methyl reserpate (inactive)

 

Elimination

Half-Life: 50-100 hr

Excretion: Feces 60%; urine 12%