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Pyridostigmine

 
Drug Info: Pyridostigmine
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Brand names: Mestinon®, Regonol®

Chemical formula:



Pyridostigmine tablets or extended-release tablets

What are pyridostigmine tablets or extended-release tablets?

PYRIDOSTIGMINE (Mestinon®, Mestinon Timespan®) can improve muscle strength. It can help to treat myasthenia gravis, a disease that affects your muscles. Pyridostigmine tablets may also be used by the military before an anticipated threat of exposure to certain nerve gas agents. Generic pyridostigmine regular-release tablets are available. Extended-release tablets are not yet available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• asthma
• difficulty passing urine
• heart disease or irregular heartbeat
• kidney disease
• over active thyroid
• seizures (convulsions)
• stomach obstruction or ulcers
• an unusual or allergic reaction to pyridostigmine, bromides, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I take this medicine?

Take pyridostigmine tablets by mouth. Follow the directions on the prescription label. Swallow the tablets with a drink of water. If pyridostigmine upsets your stomach, take it with food or milk. If you are taking the extended-release tablets, swallow them whole; do not crush or chew. Take your doses regularly. The interval between doses is very important. You must take your tablets day and night. Do not take your medicine more often than directed.

If you are in the military and instructed to use pyridostigmine in case of threatened exposure to Soman nerve gas, be sure to get instructions on the use of the antidote atropine and pralidoxime. In this case, you will need to get an adequate supply of these drugs. Pyridostigmine tablets are only to be used prior to exposure to Soman. Pyridostigmine should not be used during or after exposure to Soman.

What if I miss a dose?

Try not to miss a dose and try to keep to your prescribed medication schedule for the best effect. If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.

What drug(s) may interact with pyridostigmine?

• atropine
• certain antibiotics given by injection
• disopyramide
• mecamylamine
• medicines that cause muscle relaxation
• other medicines that improve muscle strength or tone for conditions like myasthenia gravis
• quinine
• trimethaphan

Tell your prescriber or health care professional about all other medicines you are taking, including nonprescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking pyridostigmine?

Each patient can take pyridostigmine tablets on a schedule that best suits their individual needs. These needs can increase at certain times of the day. Your prescriber or health care professional may want you to keep a record of when you take your tablets, how you feel after taking them, and if you get any side effects. This information will help your prescriber or health care professional to plan a schedule and dose best suited to your condition.

Always carry an identification card describing your disease and the details of your medication regimen.

If you are in the military and are asked to use or carry pyridostigmine in the event of threatened exposure to Soman nerve gas, be sure to get adequate instructions on the use and administration of this drug.

What side effects may I notice from taking pyridostigmine?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• changes in vision
• diarrhea
• difficulty breathing
• dizziness
• difficulty moving
• headache
• increase in the need to pass urine
• increased saliva
• increased sweating
• muscle cramps or spasms
• nausea, vomiting
• skin rash
• slow or irregular heartbeat
• stomach pain
• unusual weakness or tiredness

Where can I keep my medicine?

Keep out of the reach of children in a container that small children cannot open.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Keep container tightly closed. Throw away any unused medicine after the expiration date.


Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

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Veterinary Dictionary: pyridostigmine
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Home > Library > Animal Life > Veterinary Dictionary

A cholinesterase inhibitor; used as the bromide in the treatment of myasthenia gravis and as an antidote to nondepolarizing muscle relaxants, e.g. tubocurarine.

Wikipedia: Pyridostigmine
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Home > Library > Miscellaneous > Wikipedia
Pyridostigmine
Systematic (IUPAC) name
3-[(dimethylcarbamoyl)oxy]-1-methylpyridinium
Identifiers
CAS number 155-97-5
ATC code N07AA02
PubChem 4991
DrugBank APRD00380
Chemical data
Formula C9H13N2O2 
Mol. mass 181.212 g/mol
Pharmacokinetic data
Bioavailability 7.6 +/- 2.4%
Metabolism  ?
Half life 1.78 +/- 0.24hrs
Excretion Renal
Therapeutic considerations
Pregnancy cat.

C(AU) C(US)
Legal status

POM(UK) ℞-only(US)
Routes Oral, intravenous
 Yes check.svgY(what is this?)  (verify)

Pyridostigmine is a parasympathomimetic and a reversible cholinesterase inhibitor. Since it is a quaternary amine, it is poorly absorbed in the gut and doesn't cross the blood-brain barrier, except possibly in stressful conditions.[1]

Contents

Mode of action

Here is a brief description of how a synapse works. Action potentials are conducted along motor nerves to their terminals where they initiate a Ca2+ influx and the release of acetylcholine (ACh). The ACh diffuses across the synaptic cleft and binds to receptors on the post synaptic membrane, causing an influx of Na+ and K+ ions, resulting in depolarisation. If large enough, this depolarisation results in an action potential. To prevent constant stimulation once the ACh is released, an enzyme called acetylcholinesterase is present in the endplate membrane close to the receptors on the post synaptic membrane, and quickly hydrolizes ACh.

Pyridostigmine inhibits acetylcholinesterase in the synaptic cleft, thus slowing down the hydrolysis of acetylcholine.

Clinical uses

Pyridostigmine is used to treat muscle weakness in people with myasthenia gravis and to combat the effects of curariform drug toxicity. Pyridostigmine bromide has been FDA approved for military use during combat situations as an agent to be given prior to exposure to the nerve agent Soman in order to increase survival. Used in particular during the first Gulf War, pyridostigmine bromide has been implicated as a causal factor in Gulf War syndrome[2].

Pyridostigmine is now also used to treat orthostatic hypotension.[3]

Pyridostigmine bromide is available under the trade names Mestinon (Valeant Pharmaceuticals) and Regonol.

Contraindications

Pyrostigmine bromide is contraindicated in cases of mechanical intestinal or urinary obstruction and should be used with caution in patients with bronchial asthma [4][5].

Side effects

Common side effects include[4]:

  • Nausea
  • Vomiting
  • Diarrhea
  • Abdominal cramps
  • Increased salivation
  • Tearing
  • Increased bronchial secretions
  • Constricted pupils

References

  1. ^ Gulf War Syndrome: More Complex Than Middle East Politics. JWatch Psychiatry 1997;1997:15-15.
  2. ^ Golomb, B. (2008) "Acetylcholinesterase inhibitors and Gulf War illnesses" Proc Natl Acad Sci; Reuters; MedPageToday.com
  3. ^ Gales BJ, Gales MA. (2007). "Pyridostigmine in the treatment of orthostatic intolerance". Ann Pharmacother. 41 (2): 314–8. doi:10.1345/aph.1H458. PMID 17284509. 
  4. ^ a b Mestinon | Home
  5. ^ Mestinon Official FDA information, side effects and uses

Related publications

  1. Brenner, G. M. (2000). Pharmacology. Philadelphia, PA: W.B. Saunders Company. ISBN 0-7216-7757-6
  2. Canadian Pharmacists Association (2000). Compendium of Pharmaceuticals and Specialties (25th ed.). Toronto, ON: Webcom. ISBN 0-919115-76-4
  3. Neal, M.J. (2002). Medical Pharmacology at a Glance (5th ed.). London, England: Blackwell Publishing. ISBN 1405133600
v • d • e
Parasympathomimetics / cholinergic agonists / acetylcholinesterase inhibitors (N06DA, N07AA)
Direct
(at receptor)
Indirect/AIs
(in synapse)
very short acting: Edrophonium

carbamates/stigmine: Ambenonium · Rivastigmine · Distigmine · tertiary/CNS (Physostigmine) · quaternary/peripheral (Neostigmine, Pyridostigmine)

anti-dementia (Galantamine, Donepezil, Tacrine)

This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)

 
 

 

Copyrights:

Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Veterinary Dictionary. Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.  Read more
Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Pyridostigmine".  Read more