Nikethamide

Nikethamide
Systematic (IUPAC) name
N,N-Diethyl-3-pyridinecarboxamide
Clinical data
AHFS/Drugs.com International Drug Names
Pregnancy cat.  ?
Legal status  ?
Pharmacokinetic data
Half-life 0.5 h
Identifiers
CAS number 59-26-7
ATC code R07AB02
PubChem CID 5497
ChemSpider 5296 Y
UNII 368IVD6M32 Y
KEGG D07408 Y
Chemical data
Formula C10H14N2O 
Mol. mass 178.231
SMILES eMolecules & PubChem
 Y(what is this?)  (verify)

Nikethamide is a stimulant which mainly affects the respiratory cycle. Widely known by its former trade name of Coramine, it was used in the mid-1900s as a medical countermeasure against tranquilizer overdoses, before the advent of endotracheal intubation and positive-pressure lung expansion. It is now considered to be of no value for such purposes, and may in fact be dangerous.[1]

In alternate terminology, it is known as nicotinic acid diethylamide, which meaningfully emphasizes its laboratory origins, as well as the phonemes of its common name.

Contents

Former and current medical use

Coramine was used by suspected serial killer Dr John Bodkin Adams when treating patient Gertrude Hullett, who he was suspected of murdering[2]. However, the toxicity of nikethamide is quite low (LD50 rabbits 650 mg/Kg oral, LD50 rats 240 mg/Kg s.c.).

Theodor Morell, Adolf Hitler's personal physician, would inject the German ruler with Coramine when Hitler was unduly sedated with barbiturates. In addition, Morell would use Coramine as part of an all-purpose "tonic" for Hitler.[3]

It is available as a short-acting over-the-counter drug in several South American and European countries, combined with glucose in form of lozenges. It is especially useful for mountain climbers to increase endurance at high altitudes. Contraindications include hypertension, cardiovascular pathologies and epilepsy.[4]

Use in sports

In sports, nikethamide is listed by the World Anti-Doping Agency as a banned substance.

Cyclists Jaime Huelamo and Aad van den Hoek were both caught using the drug at the 1972 Summer Olympics; at the time it was a permitted substance according to the International Cyclists Union but not the International Olympic Committee.

When it was discovered that American sprinter and world champion Torri Edwards had used nikethamide, she was banned for two years.

In 2005, however, WADA downgraded nikethamide so that one would only receive a maximum one-year ban.

Official sources have stated that former Russian ice hockey player Alexei Cherepanov had been taking nikethamide and that it had been taken 3 hours prior to the game in which he died.

13-year old Polish kart driver Igor Walilko was given a two year ban from competition in 2010 due to testing positive for nikethamide after a win in Germany in July, 2010. He's currently appealing the verdict.[5]

References

  1. ^ Martindale, The Extra Pharmacopoeia, 30th ed, p1229
  2. ^ Cullen, Pamela V., "A Stranger in Blood: The Case Files on Dr John Bodkin Adams", London, Elliott & Thompson, 2006, ISBN 1-904027-19-9
  3. ^ Doyle D (February 2005). "Adolf Hitler's medical care" (PDF). J. R. Coll. Physicians Edinb. 35 (1): 75–82. ISSN 1478-2715. OCLC 49953788. PMID 15825245. http://www.rcpe.ac.uk/journal/issue/journal_35_1/Hitler's_medical_care.pdf. Retrieved 2009-03-15. 
  4. ^ [Nikethamid, III-3.3, Toxcenter http://www.toxcenter.de/stoff-infos/n/nikethamid.pdf]
  5. ^ FIA Igor Walilko ruling

External links