Astemizole

Astemizole was a second-generation antihistamine drug that has a long duration of action.

Astemizole

Astemizole; Hismanal; Histaminos; Paralergin

Acemiz, Astelong, Hismanal, Stemiz

1-[(4-fluorophenyl) methyl]-N-{1-[2-(4-methoxyphenyl) ethyl] piperidin-4-yl}-1H-1,3-benzodiazol-2-amine

• Absorption: Rapidly absorbed from the gastrointestinal tract.
• Distribution: 96.7% protein binding
• Metabolism: Liver
• Excretion: Feces

Astemizole is a second generation H₁-receptor antagonist. It does not cross the BBB significantly due to this reason do not cause CNS depression or drowsiness at normal doses. 

10 mg once daily, should be taken on an empty stomach

Relieving allergy symptoms, particularly rhinitis and conjunctivitis.

Ventricular arrhythmias, drowsiness, urinary retention, headache, psychomotor impairments; dry mouth, blurred vision, GI disturbances. Increased appetite, hypersensitivity reactions, weight gain, and rashes.

• Grapefruit juice may inhibit the metabolism of astemizole
• Avoid concomitant administration of other potentially arrhythmogenic drugs.
• Concurrent use with terfenadine is not recommended.
• Imidazole, triazole antifungals, and the macrolide antibacterials inhibit the hepatic metabolism of astemizole.
• Co-administration with diuretics may cause electrolyte imbalance. 

Contraindicated in patients with bruising/Porphyria

Store it at room temperature

Molecular weight

458.5703

Molecular formula

C28H31FN4O

CAS number

68844-77-9

Precautions

•  Avoid in patients with significant hepatic disease, cardiac disease, suspected or known prolongation of the QT interval, hypokalaemia and other electrolyte imbalances. 
• Prostatic hypertrophy, glaucoma, pyloroduodenal obstruction, urinary retention, children, epilepsy and elderly.
• Not to exceed recommended doses due to risk of arrhythmias.