Questions and Answers
What is the trade name of pyridostigmine?
What is the pregnancy category of pyridostigmine?
Category C
What therapeutic class does pyridostigmine belong to?
Antimyasthenics
What pharmacological class is pyridostigmine part of?
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List one indication for the use of pyridostigmine.
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What is the action of pyridostigmine on acetylcholine?
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What is one therapeutic effect of pyridostigmine?
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How is pyridostigmine absorbed after oral administration?
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Pyridostigmine is safe to use during pregnancy.
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Does pyridostigmine cross the placenta?
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What is the half-life of pyridostigmine for oral administration?
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The contraindication for pyridostigmine includes hypersensitivity to _____.
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List two adverse reactions of pyridostigmine.
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What are the common routes for administering pyridostigmine?
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What conditions does pyridostigmine treat?
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What is the typical dosage of pyridostigmine for adults?
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What is the recommended dosage of pyridostigmine for children?
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What is the antidote use of pyridostigmine?
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Study Notes
Pyridostigmine Overview
- Trade Names: Mestinon, Mestinon SR (Canada), Mestinon Timespan, Regonol
- Pregnancy Category: C (risk cannot be ruled out)
Classification
- Therapeutic Class: Antimyasthenics
- Pharmacologic Class: Cholinergics
Indications
- Increases muscle strength in myasthenia gravis.
- Reverses effects of nondepolarizing neuromuscular blocking agents.
- Provides prophylaxis against nerve agent soman toxicity.
Mechanism of Action
- Inhibits breakdown of acetylcholine (anticholinesterase effect).
- Causes miosis, increased intestinal/skeletal muscle tone, bronchial/ureteral constriction, bradycardia, increased salivation, lacrimation, and sweating.
Therapeutic Effects
- Improves muscular function in myasthenia gravis patients.
- Reverses paralysis due to nondepolarizing neuromuscular blockers.
- Prevents toxicity from soman nerve gas.
Pharmacokinetics
- Absorption: Poor after oral administration, requires larger oral doses.
- Distribution: Crosses the placenta.
- Metabolism: Processed by plasma cholinesterases and the liver.
Half-Life
- Oral administration: Approximately 3.7 hours.
- Intravenous administration: Approximately 1.9 hours.
Time/Action Profile
- Oral: Onset 30-35 min, Duration 3-6 hr.
- Oral-SR: Onset 30-60 min, Duration 6-12 hr.
- Intramuscular: Onset 15 min, Duration 2-4 hr.
- Intravenous: Onset 2-5 min, Duration 2-3 hr.
Contraindications
- Hypersensitivity to pyridostigmine or bromides.
- Mechanical GI or GU tract obstruction.
- Known alcohol intolerance (for syrup formulation).
Precautions
- History of asthma, ulcer disease, cardiovascular disease, epilepsy, hyperthyroidism.
- Caution in pregnant women; risk of uterine irritability and transient muscle weakness in newborns during lactation.
Adverse Reactions/Side Effects
- CNS effects: Seizures, dizziness, weakness.
- EENT effects: Lacrimation, miosis.
- Respiratory: Bronchospasm, excessive secretions.
- Cardiovascular: Bradycardia, hypotension.
- Gastrointestinal: Abdominal cramps, diarrhea, excessive salivation, nausea, vomiting.
- Dermatologic: Sweating, rashes.
- Life-threatening symptoms are emphasized in capital letters.
Drug Interactions
- Potential antagonism with anticholinergic drugs (e.g., antihistamines, antidepressants).
- Prolongation of effects with muscle-relaxing agents and cholinesterase inhibitors.
- Increased toxicity when used with other cholinesterase inhibitors (e.g., echothiophate).
Administration Routes
- Available routes: Oral (PO), Intravenous (IV), Intramuscular (IM).
Dosing Guidelines
- Adults: PO 30-60 mg every 3-4 hours, usual maintenance 600 mg/day; IM/IV 2 mg (1/30 of oral dose), repeat every 2-3 hours if needed.
- Children: 7 mg/kg/day in 5-6 divided doses.
- Neonates: 50-150 mcg/kg every 4-6 hours.
- Antidote dosing: IV 10-20 mg with pre-treatment of atropine.
Soman Exposure Prevention
- Adults: PO 30 mg every 8 hours before exposure, discontinue upon contact with the agent.
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Test your knowledge on pyridostigmine with these flashcards. Covering trade names, pregnancy category, therapeutic classification, pharmacological class, and indications, this quiz is an essential tool for students and professionals alike.
