Drug information of pilocarpine oral

pilocarpine oral

Drug group:

A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine affects the nervous system and increases saliva secretion in the mouth.

Mechanism of effect

Cholinergic parasympathomimetic with predominant muscarinic action; increases secretion of exocrine glands (sweat, lacrimal, salivary, intestinal, pancreatic glands, and mucous cells of the respiratory tract( may be stimulated

Tone and mobility of gallbladder, biliary duct, and urinary tract may be increased

Pharmacodynamic

Pilocarpine is a cholinergic parasympathomimetic agent exerting a broad spectrum of pharmacologic effects with predominant muscarinic action. Pilocarpine , in appropriate dosage, can increase secretion by the exocrine glands. The sweat, salivary, lacrimal, gastric, pancreatic, and intestinal glands and the mucous cells of the respiratory tract may be stimulated. Dose-related smooth muscle stimulation of the intestinal tract may cause increased tone, increased motility, spasm, and tenesmus.

 Bronchial smooth muscle tone may increase. The tone and motility of urinary tract, gallbladder, and biliary duct smooth muscle may be enhanced. Pilocarpine may have paradoxical effects on the cardiovascular system. The expected effect of a muscarinic agonist is vasodepression, but administration of Pilocarpine may produce hypertension after a brief episode of hypotension. Bradycardia and tachycardia have both been reported with use of Pilocarpine.

Pharmacokinetics

  • Half-Life: 0.76-1.35 hr
  • Onset: 20 min (initial response for xerostomia)
  • Duration: 3-5 hr (single dose), >10 hr (multiple dose)
  • Peak plasma time: 85-1.25 hr
  • Bioavailability: High fat meal decreases rate & extent of absorption
  • Protein bound: None

Drug indications

dry mouth

Dosage

Adult

Radiation-induced Xerostomia

5 mg PO q8hr; may titrate up to 10 mg PO q8hr; not to exceed 30 mg/day

Xerostomia Associated with SjÖgren's Syndrome

5 mg PO q6hr

Pediatric

Safety & efficacy not established

Drug contraindications

Asthma , Hypersensitivity

Alerts

Use caution in cardiovascular disease, cholelithiasis, biliary tract disease, COPD, chronic bronchitis, history of nephrolithiasis, concomitant use of beta adrenergic agonist, renal insufficiency, PUD, Parkinson's, hyperthyroidism, urinary tract obstruction

May require up to 12 wk to determine if head/neck cancer patients will respond

Points of recommendation

Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.

You may take pilocarpine with or without food.

Drink plenty of liquids while you are taking pilocarpine. This medicine can cause increased sweating and you may get dehydrated easily.

Use pilocarpine regularly to get the most benefit. Get your prescription refilled before you run out of medicine completely.

Store at room temperature away from moisture and heat.

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Pregnancy level

C

Related drugs

Cevimeline , Echothiophate


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