A-Z Drug Facts > Pyridostigmine Bromide

Pyridostigmine Bromide

Pronouncation: (pihr-id-oh-STIG-meen BROE-mide)
Class: Anticholinesterase muscle stimulant

Trade Names:
Mestinon
- Tablets 60 mg
- Tablets, extended-release 180 mg
- Syrup 60 mg/5 mL
- Injection 5 mg/mL

Pharmacology

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Facilitates myoneural junction impulse transmission by inhibiting acetylcholine destruction by cholinesterase.

Pharmacokinetics

Elimination

Primarily excreted unchanged by the kidney.

Indications and Usage

Treatment of myasthenia gravis; reversal agent or antagonist to nondepolarizing muscle relaxants such as curariform drugs and gallamine triethiodide (IV only).

Contraindications

Mechanical intestinal or urinary obstruction; hypersensitivity to anticholinesterase agents.

Dosage and Administration

Adults

PO Individualize dosage to meet the needs of the patients.

Syrup/Conventional tablet

Average dose is ten 5 mL tsp (60 mg/5 mL) daily or ten 60 mg tablets spaced to provide max relief when max strength is needed (range is usually 1 to 25 tablets or tsp/day).

Extended-release tablets

One to three 180 mg tablets, once or twice daily with at least 6 h between doses.

IV To supplement oral dosage preoperatively and postoperatively during labor and postpartum, during myasthenic crisis, or when oral therapy is impractical, give approximately 1/30 the oral dose, either IM or very slow IV.

Neonates

IV Neonates of myasthenic mothers may have transient difficulty in swallowing, sucking, and breathing. Injectable pyridostigmine may be indicated (by symptoms and use of the edrophonium test) until syrup can be taken. Dosage requirements range from 0.05 to 0.15 mg/kg IM.

Reversal of Nondepolarizing Muscle Relaxants
Injection

Give atropine sulfate (0.6 to 1.2 mg) IV immediately prior to pyridostigmine to minimize adverse reactions. Pyridostigmine 10 or 20 mg IV is usually sufficient. Full recovery usually occurs in no more than 15 min but at least 30 min may be required.

General Advice

• Administer without regard to meals. Administer with food if GI upset occurs.
• Do not chew or crush extended-release tablet. Instruct patient to swallow tablet(s) whole.
• Store at controlled room temperature (59° to 86°F).

Drug Interactions

Atropine

May mask signs of overdosage, leading to inadvertent induction of cholinergic crisis.

Corticosteroids

The therapeutic effects of pyridostigmine may be antagonized.

Succinylcholine

Neuromuscular blockade produced by succinylcholine may be prolonged or antagonized.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Dermatologic

Skin rash.

EENT

Miosis.

GI

Nausea; vomiting; diarrhea; abdominal cramps; increased peristalsis; increased salivation.

Musculoskeletal

Muscle cramps and fasciculation; weakness.

Respiratory

Increased bronchial secretions.

Miscellaneous

Increased sweating.

Precautions

Pregnancy

Category C .

Lactation

Excreted in breast milk.

Renal Function

Lower doses may be required in patients with renal disease.

Bronchial asthma

Use with caution.

Cardiac dysrhythmias (IV only)

Use with caution. Transient bradycardia may occur and be relieved by atropine sulfate.

Cholinergic crisis

Observe patients closely for cholinergic reactions, particularly if the IV route is used. May be difficult to distinguish from myasthenic crisis. Differentiation is important because increasing the dose of pyridostigmine or other drugs of this class may have grave consequences in patients in cholinergic crisis.

Overdosage

Symptoms

Cholinergic crisis, characterized by increasing muscle weakness (including respiratory paralysis and death).

Patient Information

• Advise patient that dose and frequency of administration may be adjusted to achieve max benefit.
• Advise patient to take exactly as prescribed and not to change the dose or stop taking unless advised by health care provider.
• Advise patient to take prescribed dose without regard to meals but to take with food if upset stomach occurs.
• Instruct patient to contact health care provider immediately if any of the following occur: worsening muscle weakness, difficulty breathing, slow heart rate, dizziness, fainting.

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