Pharmacology and mechanism of action
Bephenium is a quaternary ammonium compound first introduced into clinical medicine in 1958. It has a wide anthelminthic activity, in particular against Ancylostoma duodenale and Ascaris lumbricoides.
The mechanism of action of bephenium is similar to that of pyrantel and levamisole (see the monograph on levamisole, p. 74).
Indications
Infections with Ancylostoma duodenale, Ascaris lumbricoides and Necator americanus. Superior alternative drugs are available today.
Side effects
The drug has a bitter taste which might cause some patients especially children to refuse intake or vomit. This may be minimized by giving the drug with a sweet drink. Some individuals experience transient nausea, vomiting and headache after drug intake. Vertigo is occasionally reported.
Contraindications
There are no known contraindications to the drug.
Interactions
Bephenium has antagonistic effects to piperazine. However, no interactions were reported when the two drugs were combined together during helminthic therapy
[1].
Preparations
5 g bephenium hydroxynaphthoate contains 2.9 g bephenium.
• Alcopar® (Wellcome). Sachet containing 5 g of bephenium hydroxynaphthoate.
References
1. Goodwin LG, Jayewardene LG, Standen OD (1958). Clinical trials with bephenium hydroxynaphthoate against hookworm in Ceylon. BMJ, 2, 1572–1576.
Uses
antibacterial, antilepretic, antituberculosis
Uses
Bephenium Hydroxynapthoate is an anthelmintic agent used to treat hookworm infections and ascariasis.
Indications
This drug exhibits antihelmintic action by acting as a cholinergic agonist, causing paralysis
of the parasite musculature. This facilitates its removal from the intestines. It is used for
treating ascariasis, ankylostomiasis, enterobiasis, trichostrongyliasis, and tricocefalosis. A
single dose of bephenium heals from 80 to 100% of patients infected with A. duodenale. It
is less effective with respect to N. americanus. Synonyms of this drug are aclopar and
others.
Clinical Use
Bephenium can be used against Ascaris,
Ancylostoma, and Trichostrongylus infections;
it is less effective against Necator. Occasional
adverse reactions occur: nausea, diarrhea, vomiting,
headache, vertigo.
Synthesis
Bephenium, 3-hydroxy-2-naphthoat benzyldimethyl(2-phenoxyethyl)
ammonia (38.1.37), is made by reacting the sodium salt of 3-hydroxy-2-naphthoic acid
with benzyldimethyl(2-phenoxyethyl)ammonia chloride (38.1.36). This is in turn made
from benzyl chloride and N-(2-phenoxyethyl)dimethylamine (38.1.35), which is synthesized by reacting sodium phenolate with 2-dimethylaminoethylchloride.
