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Indications

REMS


Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

Interactions

Drug-drug:

Availability

(Generic available)

Route/Dosage

Myasthenia Gravis

Antidote for Nondepolarizing Neuromuscular Blocking Agents

US Brand Names

Mestinon, Regonol

Action

  • Inhibits the breakdown of acetylcholine and prolongs its effects (anticholinesterase).
  • Effects include:
    • Miosis,
    • Increased intestinal and skeletal muscle tone,
    • Bronchial and ureteral constriction,
    • Bradycardia,
    • Increased salivation,
    • Lacrimation,
    • Sweating.
Therapeutic effects:
  • Improved muscular function in patients with myasthenia gravis.
  • Reversal of paralysis from nondepolarizing neuromuscular blocking agents.

Classifications

Therapeutic Classification: antimyasthenics

Pharmacologic Classification: cholinergics

Pharmacokinetics

Absorption: Poorly absorbed after oral administration, necessitating large oral doses compared with parenteral doses. IV administration results in complete bioavailability.

Distribution: Appears to cross the placenta.

Metabolism/Excretion: Metabolized by plasma cholinesterases and the liver.

Half-Life: PO: 3.7 hr; IV: 1.9 hr.

Canadian Brand Names

Mestinon SR

Time/Action Profile

(cholinergic effects)

ROUTEONSETPEAKDURATION
PO30–35 minunknown3–6 hr
PO-SR30–60 minunknown6–12 hr
IM15 minunknown2–4 hr
IV2–5 minunknown2–3 hr

Patient/Family Teaching

Pronunciation

peer-id-oh-STIG-meen

Code

NDC Code