Ablukast

A leukotriene receptor antagonist used in the treatment of asthma and allergic rhinitis

Ablukast
INN
Drug class
Routes of administration	Oral
Pregnancy category
Bioavailability	64%
Metabolism	Hepatic
Elimination half-life	2.7–5.5 hours
Excretion	Fecal (86%), renal (10%)
Legal status	Rx-only
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

Ablukast is a leukotriene receptor antagonist (LTRA) used primarily in the management of asthma and allergic rhinitis. It functions by blocking the action of leukotrienes, which are chemicals in the body that react to allergens and cause inflammation, bronchoconstriction, and mucus production.

Mechanism of Action

Ablukast works by selectively inhibiting the cysteinyl leukotriene receptor type 1 (CysLT1) in the lungs and bronchial tubes. This inhibition prevents leukotrienes from binding to their receptors, thereby reducing inflammation, bronchoconstriction, and mucus secretion associated with asthma and allergic rhinitis.

Pharmacokinetics

Ablukast is administered orally and has a bioavailability of approximately 64%. It is highly protein-bound (99%) and undergoes extensive hepatic metabolism. The elimination half-life of Ablukast ranges from 2.7 to 5.5 hours, and it is primarily excreted in the feces (86%) with a small amount excreted renally (10%).

Clinical Use

Ablukast is indicated for the prophylaxis and chronic treatment of asthma in adults and children. It is also used to relieve symptoms of allergic rhinitis, such as sneezing, runny nose, and nasal congestion. Ablukast is not indicated for the relief of acute asthma attacks.

Side Effects

Common side effects of Ablukast include headache, dizziness, abdominal pain, and fatigue. Rare but serious side effects may include liver dysfunction and neuropsychiatric events such as agitation, aggression, and hallucinations.

Contraindications

Ablukast is contraindicated in patients with known hypersensitivity to the drug or any of its components. Caution is advised in patients with hepatic impairment.

Related Pages

• Asthma
• Allergic rhinitis
• Leukotriene receptor antagonist
• Bronchoconstriction

Gallery

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  Chemical structure of Ablukast