ASTEMIZOLE

 ASTEMIZOLE

BRAND NAME:- Hismanal  ,Acipax, Alestol , Astem 

ASTEMIZOLE are the earliest second generation H1 antihistamine drug. It treats allergy symptoms such as itching, swelling, and rashes by blocking the effects of a chemical messenger (histamine) in the body. 

It has anticholinergic and antipruritic effects.

PHARMACODYNAMIC:-

Astemizole is a second generation H1-receptor antagonist. It has anticholinergic and antipruritic effects.It does not significantly cross the blood brain barrier and therefore does not cause drowsiness or CNS depression at normal doses. Several studies  have shown high permeability and high binding to protein folds associated with Alzheimer's.

MECHANISM OF ACTION:- 

Astemizole competes with histamine for binding at H1-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. This reversible binding of astemizole to H1-receptors suppresses the formation of edema, flare, and pruritus resulting from histaminic activity. As the drug does not readily cross the blood-brain barrier and preferentially binds at H1 receptors in the peripehery rather than within the brain, CNS depression is minimal. Astemizole may also act on H3-receptors, producing adverse effects .

Astemizole does also act as FIASMA (functional inhibitor of acid sphingomyelinase. 

USED:-treatment of allergic conditions, inching, swelling 

SIDE EFFECTS:- common side are Sleepiness.

DOSE:- DIRECTION BY PHYSICIAN