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Indications and Dosage
Oral
Allergic conditions Adult: 10 mg once daily.
Child: 6-12 yr: 5 mg once daily. |
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Administration
Should be taken on an empty stomach.
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Contraindications
Porphyria.
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Special Precautions
Prostatic hypertrophy, urinary retention, glaucoma, pyloroduodenal obstruction, epilepsy; children and elderly. Avoid in patients with cardiac disease, significant hepatic disease, known or suspected prolongation of the QT interval, hypokalaemia and other electrolyte imbalances. Not to exceed recommended doses due to risk of arrhythmias.
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Adverse Reactions
Increased appetite, wt gain. Rashes, hypersensitivity reactions. CNS depression eg, drowsiness, headache, psychomotor impairments; urinary retention, dry mouth, blurred vision, GI disturbances.
Potentially Fatal: Ventricular arrhythmias, including torsades de pointes. |
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Drug Interactions
Imidazole, triazole antifungals, and the macrolide antibacterials inhibit the hepatic metabolism of astemizole. Avoid concomitant admin of other potentially arrhythmogenic drugs. Co-admin with diuretics may cause electrolyte imbalance. Concurrent use with terfenadine is not recommended.
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Food Interaction
Grapefruit juice may inhibit the metabolism of astemizole.
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Action
Description:
Mechanism of Action: Astemizole is a piperidine derivative, non-sedating antihistamine. Pharmacokinetics: Absorption: Rapid absorption from GI tract. Distribution: Unchanged astemizole: Highly bound to plasma proteins Metabolism: Extensive 1st pass metabolism. Excretion: Metabolites are slowly excreted in the urine and faeces, and undergo enterohepatic recycling. |
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MIMS Class
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