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Sunday, February 15, 2009

Disulfiram reaction & Other drugs causing it.

490024328_323fa90acaAlcohol intake is strictly prohibited when we take these drugs!Let us know what these drugs are.

 

First lets know something about Disulfiram.

antabusebig

Disulfiram (Antabuse), is an aversive agent that inhibits the metabolism of alcohol. The usual dose of disulfiram is 250 mg once daily.

 

Disulfiram is an irreversible and nonspecific enzyme-inhibitory agent which inhibits the enzyme acetaldehyde-dehydrogenase (ALDH),leading to an accumulation of acetaldehyde in the body ,leading to the ethanol-disulfiram reaction.

Formula_acetaldehyde Disulfiram irreversibly inhibits the oxidation of acetaldehyde by competing with the cofactor nicotinamide adenine dinucleotide (NAD) for binding sites on ALDH . Ultimately, disulfiram reduces the rate of oxidation of acetaldehyde, causing a 5- to 10-fold increase in the concentration of acetaldehyde. An increased serum acetaldehyde concentration is thought to be responsible for the unpleasant side effects associated with the disulfiram-ethanol reaction.source:medscape

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The disulfiram-ethanol reaction (DER) is the classic manifestation of patients with disulfiram toxicity. This reaction occurs after the ingestion of even small amounts of ethanol with the concomitant use of disulfiram or disulfiram-like agents.

Disulfiram-ethanol reaction:

  • Head, neck, and chest flushing - Histamine-induced vasodilation
  • Throbbing headaches
  • Nausea, vomiting (may be refractory), diarrhea, and abdominal pain
  • Weakness, dizziness, confusion, and anxiety
  • Vertigo and ataxia
  • Orthostatic hypotension - Hypotensive flushing reaction with warm extremities
  • Diaphoresis
  • Palpitations and dysrhythmias
  • Pruritus
  • Refractory cyanosis (eg, methemoglobinemia)

 

Drugs that may produce disulfiramlike reactions with ethanol include the following:

  • Mushrooms (eg, Coprinus atramentarius [inky cap], Clitocybe claviceps)
  • Antibiotics
  1. metronidazole,Tinidazole is chemically similar to metronidazole and so may cause the same reaction
  2. sulfonamides(trimethoprim-sulfamethoxazole)
  3. some cephalosporins( eg: cephamandole, cefoperazone, cefmenoxime, cefotetan, Moxalactam)- due to METHYLTETRAZOLETHIOL side chain.
  4. nitrofurantoin,
  5. chloramphenicol
  6. furazolidine
  7. Antimalarial Quinacrine
  • Oral hypoglycemics (eg: chlorpropamide, tolbutamide)- these sulphonylureas compete with acetaldehyde for binding sites on ALDH.
  • Pesticides (eg: carbamates, monosulfiram [Tetmosol])
  • Chloral hydrate
  • Antifungals (griseofulvin)

4 comments:

Anonymous said...

i am wondering if anyone out there is taking Disulfirum, so that I can get some education (lamen terms) on the do's and don'ts before i begin my prescription?

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