Oral pyridostigmine bromide (Mestinon): Side effects, Dosage

What is oral pyridostigmine? What are the uses for oral pyridostigmine?

Pyridostigmine (Mestinon) is an oral cholinesterase inhibitor. Acetylcholine is one of many neurotransmitters in our bodies. Neurotransmitters are chemicals that help our cells communicate with each other. Depending on the organ that it acts upon, acetylcholine produces different effects. One important function of acetylcholine is to produce muscle contractions and movement. In people with myasthenia gravis or people treated with neuromuscular blocking medicines there is a decrease in the levels of acetylcholine. In such cases pyridostigmine may be used to increase acetylcholine levels and improve muscle contraction or movement. Pyridostigmine increases the concentration of acetylcholine at nerve junctions by inhibiting cholinesterase, the enzyme that destroys acetylcholine.

In comparison to neostigmine (Bloxiverz, Prostigmin), another cholinesterase inhibitor, pyridostigmine has a longer duration of action. Pyridostigmine was approved by the FDA for the treatment of myasthenia gravis in 1955.

What brand names are available for oral pyridostigmine?

Mestinon

Is oral pyridostigmine available as a generic drug?

GENERIC AVAILABLE: Yes

Do I need a prescription for oral pyridostigmine?

Yes

What are the side effects of oral pyridostigmine?

Possible side effects of pyridostigmine therapy include:

• nausea,
• vomiting,
• diarrhea,
• stomach cramps,
• the digestion process (creased peristalsis)
• increased salivation,
• increased bronchial secretions,
• pupil constriction (miosis),
• sweating,
• muscle cramps,
• muscle twitching, and
• weakness.

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What is the dosage for oral pyridostigmine?

• For the treatment of myasthenia gravis in adults: The dose and frequency of administration must be adjusted to the needs of the individual patient.
• The average dose is ten 60 mg regular release tablets or ten 5-ml teaspoonful (600 mg).
• In individuals with severe disease, as many as 25 doses (1 dose = 60 mg regular release tablet or 5 ml syrup) may be required.
• For in mild disease, 1 to 6 doses may be sufficient.
• If using timespan tablets, one to three 180 mg tablets (180 to 540 mg) once or twice daily usually would be sufficient for providing adequate symptom control. Administration of timespan tablets should be separated by at least 6 hours. To provide coverage for break-thru symptoms, use of more rapidly acting regular tablets or syrup with timespan tablets may be necessary.
• The safety and effectiveness of pyridostigmine use in pediatrics has not been established.
• As pyridostigmine is primarily removed from the body by the kidneys, lower doses may be required in patients with kidney disease.

Which drugs or supplements interact with oral pyridostigmine?

Pyridostigmine should not be used with other cholinesterase inhibitors such as neostigmine (Bloxiverz, Prostigmin) or edrophonium (Tensilon, Enlon, Reversol) because of the risk of additive toxicity.

Use of quinine (Qualaquin) with pyridostigmine should be avoided as the actions of quinine on skeletal muscle are opposite to those of pyridostigmine.

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Is oral pyridostigmine safe to take while pregnant or breastfeeding?

The safety of pyridostigmine during pregnancy has not been evaluated. Therefore, pyridostigmine should only be used during pregnancy if the benefits of treatment outweigh the potential risk to the mother and the unborn baby. Pyridostigmine is classified as FDA pregnancy risk category C.

Pyridostigmine can be excreted into human milk. The American Academy of Pediatrics considers pyridostigmine to be generally compatible with nursing. Pyridostigmine should be used cautiously in nursing mothers.

What else should I know about oral pyridostigmine?

What preparations of oral pyridostigmine are available?

Oral: 60 mg tablets, 60 mg/5 ml syrup, 180 mg timespan (slow release) tablets.

How should I store oral pyridostigmine?

Pyridostigmine tablets and syrup should be stored at room temperature between 59 F to 86 F (15 C to 30 C). Pyridostigmine should be protected from light.