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mecamylamine

 

Classes: Antihypertensives, Other

Dosing and uses of Mecamylamine

 

Adult dosage forms and strengths

tablet

  • 2.5mg

 

Hypertension

Indicated for moderately severe-to-severe essential hypertension and uncomplicated malignant hypertension

2.5 mg PO BID intially; may increase by 2.5 mg increments at interval not less than 2 days

Average total daily dose is 25 mg (in 3 divided doses); however, as little as 2.5 mg/day may be sufficient

 

Administration

Take after meals; may cause more gradual absorption and smoother control of excessively high blood pressure

 

Pediatric dosage forms and strengths

Safety and efficacy not established

 

Mecamylamine adverse (side) effects

Frequency not defined

Common

  • Orthostatic hypotension
  • Dizziness, lightheadedness
  • Fatigue
  • Sedation
  • Constipation
  • Dry mouth
  • Nausea/Vomiting
  • Xerostomia

Serious

  • Syncope
  • Seizure
  • Tremor
  • Paralytic ileus
  • Chorea
  • Dysuria

 

Warnings

Contraindications

Hypersensitivity to mecamylamine

Coronary insufficiency, glaucoma, recent MI, pyloric stenosis, renal insufficiency, uremia

Do not use w/antibiotics, sulfonamides

 

Cautions

Arteriosclerosis, bladder neck obstruction, urethral stricture, cerebral insufficiency, gastrointestinal obstruction, prostatic hypertrophy

Potentiation of hypotensive effects due to excessive heat, fever, infection, hemorrhage, pregnancy, anesthesia, alcohol consumption, salt depletion, or diarrhea

Avoid abrupt withdrawaL

Rarely used

 

Pregnancy and lactation

Pregnancy category: C

Lactation: may cross into the breast milk, use caution

 

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 Mecamylamine

Mechanism of action

Ganglionic blocker, inhibits acetylcholine at autonomic ganglia resulting in decreased blood pressure

 

Pharmacokinetics

Half-Life: 24 hr

Onset: 0.5-2 hr

Duration: 6-12 hr

Excretion: urine 100%