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Astemizole
Astemizole (Hismanil)
Astemizole
(ah-
STEM-ih-zohl)
Pregnancy Category: C
Hismanil
(Rx)
Classification: Antihistamine,
miscellaneous
See Also: See also
Antihistamines
[. ]
Action/Kinetics: Low to no
sedative, antiemetic, or anticholinergic effects. Absorption decreased up to 60% when
taken with food. Metabolized in the liver to both active and inactive metabolites and
excreted through the feces.
t
1/2: About 1.6 days.
Onset: 2-3 days.
Duration:
Up to several weeks. Over 95% is bound to plasma protein. Mainly excreted through the
feces.
Uses: Allergic rhinitis,
urticaria.
Contraindications: Impaired
hepatic function. Concomitant use with erythromycin, clarithromycin, itraconazole,
ketoconazole, mibefradil, quinine, and troleandomycin.
Special Concerns: Dose should
not exceed 10 mg/day.
Additional Side Effects
Serious
CV side effects, including death, cardiac arrest, QT interval prolongation, torsades de
pointes and other ventricular arrhythmias have been observed in clients
exceeding the recommended dose of astemizole. Severe hepatic impairment. Syncope may
precede severe arrhythmias. Overdose may be observed with doses as low as 20-30 mg/day.
Drug Interactions:
Clarithromycin
/ Possible serious CV effects, including death, cardiac arrest, torsades de pointes,
and other ventricular arrhythmias (including QT interval prolongation).
-
Erythromycin
/ Possible serious CV effects, including death, cardiac arrest, torsades de pointes, and
other ventricular arrhythmias (including QT interval prolongation).
-
Itraconazole /
Possible serious CV effects, including death, cardiac arrest, torsades de pointes, and
other ventricular arrhythmias (including QT interval prolongation).
-
Ketoconazole /
Possible serious CV effects, including death, cardiac arrest, torsades de pointes, and
other ventricular arrhythmias (including QT interval prolongation).
-
Miconazole /
Possible serious CV effects, including death, cardiac arrest, torsades de pointes, and
other ventricular arrhythmias (including QT interval prolongation).
-
Mibefradil /
Possible serious CV effects, including death, cardiac arrest, torsades de pointes, and
other ventricular arrhythmias (including QT interval prolongation).
-
Protease inhibitors
(indinavir, nelfinavir, ritonavir, saquinavir) / Inhibition of metabolism of
astemizole
-
Quinine / Possible serious CV effects, including death, cardiac arrest,
torsades de pointes, and other ventricular arrhythmias (including QT interval
prolongation).
-
Serotonin reuptake inhibitors (fluoxetine, fluvoxamine, nefazodone,
paroxetin, sertraline) / Inhibition of metabolism of astemizole
-
Troleandomycin /
Possible serious CV effects, including death, cardiac arrest, torsades de pointes, and
other ventricular arrhythmias (including QT interval prolongation).
-
Zileuton /
Inhibition of metabolism of astemizole
How Supplied:
Tablet: 10
mg
Dosage
•Tablets
Adults and children over 12 years: 10 mg once daily.
Children, 6-12 years: 5
mg daily;
children, less than 6 years: 0.2 mg/kg/day. |
