Monograph: |
Acenocoumarol
An almost white to buff-coloured odourless or almost odour-
less powder. Practically insoluble in water and in ether;
slightly soluble in alcohol and in chloroform; dissolves in
aqueous solutions of alkali hydroxides.
Adverse Effects, Treatment, and Precautions
As for Warfarin Sodium
see warfarin sod
Interactions
The interactions associated with oral anticoagulants are dis-
cussed in detail under warfarin .Specific references to
interactions involving nicoumalone can be found there under
the headings for the following drug groups: analgesics; an-
tiarrhythmics: antibacierials: antifungals; antigout drugs: an-
tihistamines; antineoplaslics: antiplatelets: diuretics; gastro-
intestinal drugs: lipid regulating drugs: prostaglandins: sex
hormones: and vaccines.
Pharmacokinetics
Nicoumalone is readily absorbed from the gastro-intestinal
tract and is excreted chiefly in the unne mainly as metabo-
lites. Nicoumalone is extensively bound to plasma proteins.
Figures reported for elimination half-life vary; 8 to I I hours
appears a reasonable range. Nicoumalone crosses the placen-
ta: only small quantities have been detected in breast milk,
Nicoumalone is administered as a racemic mixture: the R-iso-
mer is reported to be more potent. The stereo-isomers have
different pharmacokinetics.
Uses and Administration
Nicoumalone is an orally administered coumarin anticoagu-
lant with actions similar to those of warfarin sodium.
It is used in the management of thrombo-embolic disorders
(p.801). The usual dose on the first day is 8 to 12 mg. on the
second day 4 to 8 mg: subsequent maintenance doses range
from I to 8 mg depending on the response. Nicoumalone is
given in a single dose at the same time every day.
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