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neostigmine

 
Dictionary: ne·o·stig·mine   (nē'ō-stĭg'mēn, -mĭn) pronunciation
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n.
Either of two related white crystalline compounds, C12H19BrN2O2 or C13H22N2O6S, that opposes the action of acetylcholinesterase and is used in the treatment of glaucoma, myasthenia gravis, and various postoperative conditions.

[NEO- + (PHYSO)STIGMINE.]


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Drug Info: Neostigmine
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Brand names: Prostigmin®



Neostigmine tablets

What are neostigmine tablets?

NEOSTIGMINE (Prostigmin®) can improve muscle strength. It can help to treat myasthenia gravis, a disease that affects your muscles. You can take tablets providing there is no difficulty in swallowing. Generic neostigmine tablets are 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
• low blood pressure
• over-active thyroid
• peritonitis
• seizures (convulsions)
• stomach obstruction or ulcers
• an unusual or allergic reaction to neostigmine, bromides, other medicines, foods, dyes, or preservatives

How should I take this medicine?

Take neostigmine tablets by mouth. Follow the directions on the prescription label. Swallow the tablets with a drink of water. If neostigmine upsets your stomach, take the tablets with food or milk. 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.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What if I miss a dose?

If you miss a dose, you may precipitate a crisis. Use a non-electric alarm clock to remind you of exact dose time. Do not take double or extra doses.

What drug(s) may interact with neostigmine?

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

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 neostigmine?

Each patient can take neostigmine 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 details of your medicine and dosage times.

What side effects may I notice from taking neostigmine?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• difficulty breathing
• dizziness
• difficulty moving
• muscle cramps or spasms
• slow or irregular heartbeat
• vomiting

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• changes in vision
• diarrhea
• increase in the need to pass urine
• increased saliva
• increased sweating
• nausea
• 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). 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.

 
Columbia Encyclopedia: neostigmine
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neostigmine (nē'ōstĭg'mēn, -mĭn), drug used to mimic the effects of stimulation of the parasympathetic nervous system. Along with several other drugs that have a similar mode of action, it inhibits the action of the enzyme cholinesterase, which destroys the substance acetylcholine at nerve endings. Because neostigmine increases the effective concentration of acetylcholine, it causes such body changes as contraction of the pupils, increased activity of intestinal muscles, and increased secretion by the salivary and sweat glands. It will cause menstrual bleeding in a nonpregnant woman whose menstrual period is delayed, and it is therefore used as a pregnancy test. Neostigmine and related drugs are also used to diagnose and control the neuromuscular disease myasthenia gravis. Because neostigmine causes decreased fluid pressure in the eye it is used to treat certain types of glaucoma. The drug atropine is sometimes given along with neostigmine to prevent the latter's side effects. Ephedrine often enhances the action of neostigmine.

Veterinary Dictionary: neostigmine
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An anticholinesterase used in the treatment of myasthenia gravis and glaucoma and as an antidote for nondepolarizing muscle relaxants, such as tubocurarine.

  • n. test — muscle weakness caused by myastenia gravis is temporarily reversed following the administration of neostigmine; used as a diagnostic test.
Wikipedia: Neostigmine
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Neostigmine
Systematic (IUPAC) name
3-{[(dimethylamino)carbonyl]oxy}-N,N,N-trimethylbenzenaminium
Identifiers
CAS number 59-99-4
ATC code N07AA01 S01EB06 QA03AB93
PubChem 5824
Chemical data
Formula C12H19N2O2 
Mol. mass 223.294 g/mol
Pharmacokinetic data
Bioavailability Unclear, probably less than 5%
Metabolism Slow hydrolysis by acetylcholinesterase and also by plasma esterases
Half life 50–90 minutes
Excretion Unchanged drug (up to 70%) and alcoholic metabolite (30%) are excreted in the urine
Therapeutic considerations
Pregnancy cat.

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Legal status
Routes  ?
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Neostigmine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor.

Neostigmine is available under several trade names such as Prostigmin and Vagostigmin.


Contents

Synthesis

Neostigmine was first synthesized by Aeschlimann and Reinert in 1931.

Neostigmine is made by first reacting 3-dimethylaminophenol with N-dimethylcarbamoyl chloride, which forms a dimethylcarbamate. Next, that product is alkylated using dimethylsulfate, which forms neostigmine.[1]

Pharmacology

By interfering with the breakdown of acetylcholine, neostigmine indirectly stimulates both nicotinic and muscarinic receptors. Unlike physostigmine, neostigmine has a quarternary nitrogen; hence, it is more polar and does not enter the CNS. its effect on skeletal muscle is greater than that of physostigmine, and it can stimulate contractility before it paralyzes. Neostigmine has short duration of action, usually thirty minutes to two hours.[2] Neostigmine binds to the anionic site of cholinesterase. The drug blocks the active site of acetylcholinesterase so the enzyme can no longer break down the acetylcholine molecules before they reach the postsynaptic membrane receptors. This allows for the threshold to be reached so a new impulse can be triggered in the next neuron. In myasthenia gravis there are too few acetylcholine receptors so with the acetylcholinesterase blocked, acetylcholine can bind to the few receptors and trigger a muscular contraction.

Clinical uses

It is used to improve muscle tone in people with myasthenia gravis and routinely, in anesthesia at the end of an operation, to reverse the effects of non-depolarizing muscle relaxants such as rocuronium and vecuronium.

It can also be used for urinary retention resulting from general anaesthesia and to treat curariform drug toxicity.

Another indication for use is the Ogilvie syndrome which is a pseudoobstruction of the colon in critically ill patients.

Historically, it has been used as a test for early pregnancy. In a non-pregnant female whose menstrual period is delayed, administration of neostigmine can provoke menstrual bleeding. Modern tests which rely on detecting hCG in urine have rendered this application obsolete.

Though one of only two treatments available for myasthenia gravis this drug is no longer available to anyone using the Medicare Part D program.

Side Effects

Neostigmine can induce generic occular side effects including: headache, brow pain, blurred vision, phacodinesis,pericorneal injection, congestive iritis, various allergic reactions, and rarely, retinal detachment.[3]

Neostigmine will cause slowing of the heart rate (bradycardia), for this reason it is usually given along with a parasympatholytic drug such as atropine or glycopyrrolate.

Gastrointestial symptoms occur earliest after ingestion and include anorexia, nausea and vomiting, abdominal cramps and diarrhea.[4]

Spectral Data

Neostigmine shows notable UV/VIS absorption at 261nm, 267nm, and 225nm.[5]

Neostigmine's 1H NMR Spectroscopy reveals shifts at: 7.8, 7.7, 7.4, 7.4, 3.8, and 3.1 parts per million. The higher shifts are due to the aromatic hydrogens. The lower shifts at 3.8ppm and 3.1ppm are due to the electronic withdrawing nature of the tertiary and quaterary nitrogen, respectively.[6]

See also

Notes

  1. ^ Gilman, A.G..; Goodman L.S.; Gilman A. Goodman and Guildman's The Pharmacological Basis of Therapeutics; 6th ed. Macmillan Publishing Co., Inc., 1980; pp 103
  2. ^ Howland, R. D., Mycek, M. J., Harvey, R. A., Champe, P. C., & Mycek, M. J. Pharmacology 3rd edition, Lippincott's Illustrated Reviews, 2008, pg. 51.
  3. ^ [Gilman, A. G., L. S. Goodman, and A. Gilman. (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 6th ed. New York: Macmillan Publishing Co., Inc. 1980.,p.114]
  4. ^ [Gilman, A. G., L. S. Goodman, and A. Gilman. (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 6th ed. New York: Macmillan Publishing Co., Inc. 1980., p.109]
  5. ^ Porst, Hella; Kny, L. Pharmazie, 1985 , vol. 40, # 5 p. 325 - 328
  6. ^ Ferdous, Abu J.; Waigh, Roger D. Journal of Pharmacy and Pharmacology, 1993 , vol. 45, # 6 p. 559 - 562

References

  • Brenner, G. M. (2000). Pharmacology. Philadelphia, Penn.: W.B. Saunders Company. ISBN 0-7216-7757-6.
  • Canadian Pharmacists Association (2000). Compendium of Pharmaceuticals and Specialties (25th ed.). Toronto, ON: Webcom. ISBN 0-919115-76-4.


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)
v • d • e
Ophthalmologicals: antiglaucoma preparations and miotics (S01E)
Sympathomimetics
Parasympathomimetics
muscarinic/nicotinic
Carbonic anhydrase inhibitors/
(sulfonamides)
Beta blocking agents
Prostaglandin analogues (F2α)
Other agents

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

 
 

 

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Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved.  Read more
Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Columbia Encyclopedia. The Columbia Electronic Encyclopedia, Sixth Edition Copyright © 2003, Columbia University Press. Licensed from Columbia University Press. All rights reserved. www.cc.columbia.edu/cu/cup/.  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 "Neostigmine".  Read more