Astemizole

Drug #61

Astemizole is an antihistamine. Astemizole is an oral H-1 receptor antagonist that is similar in structure to terfenadine, another H-1 receptor antagonist. It provides relief from symptoms of allergies such as rash, hives, watery eyes, runny nose, itching of eyes and sneezing.

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Primary Characteristics

It is of Synthetic origin and belongs to Benzimidazole.

It belongs to H1-antagonist pharmacological group on the basis of mechanism of action.

Molecular Weight: 459 · pK_a: 8.35 · Solubility in Alcohol: 1 in 30 · Non-proprietary name: Astemizole.

Pharmacokinetics

Absorption: Astemizole has an oral bioavailability is 90%, pre-systemic (first-pass) metabolism accounts for 94.5% (±4.5%).

Distribution: Astemizole has a volume of distribution is 48 l/kg. plasma protein binding is 97%.

Elimination: it is metabolised via via liver, plasma half-life is 20hr (oral), 30hr (IV), renal excretion is 5-6%.

Indications

Astemizole is primarily indicated in conditions like Allergic conjunctivitis, Allergic rhinitis, Asthma, Dermatitis, Urticaria.

Contraindications

Astemizole is contraindicated in conditions like Cardiac insufficiency, Hepatic dysfunction.

Dosage

Astemizole's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
0.285 mg/kg	0.285 mg/kg	Every 24h	PO	-
Paediatric Dosage (20kg)
0 – 0	—	—	—	Not Recommended in this Age Group
Neonatal Dosage (3kg)
0 – 0	—	—		Not recommended in this age group

Drug Interactions

Unknown21 interactions

5 interactions

Major9 interactions

Moderate3 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Astemizole produces potentially life-threatening effects which include Ventricular fibrillation, Stevens Johnson syndrome. Careful monitoring is needed with proper medical management.

The signs and symptoms that are produced after acute overdosage of Astemizole are Cardiac dysrhythmias.

Astemizole is known to cause more or less tolerable side effects which are usually transient. These include Anxiety, Dizziness, Drowsiness, Dry mouth, Headache, Nausea, Pain , Xerostomia .

Warnings / Precautions

Astemizole should be used with caution in patients with pre-existing heart, kidney or liver disease, asthma or breathing problems, allergy or a history of drug dependance. It is classified as pregnancy category C. This drug should be used only if clearly needed during pregnancy or lactation.

Available Brands

None recorded.

Storage Conditions

Astemizole should be stored Tab.

Drug Classification

1.3 — Anti-allergics (Antihistamines) and drugs used in anaphylaxis