Friday, February 16, 2018

Icatibant- Selective bradykinin antagonist drug and its therapeutic uses

DESCRIPTION
Icatibant is a bradykinin B2 receptor blocker. It works by blocking bradykinin, a substance which is thought to be responsible for the HAE symptoms of swelling, inflammation, and pain.


PHARMACOKINETICS
1. The absolute bioavailability of icatibant following a 30 mg subcutaneous dose is approximately          97%.
2. Volume of distribution is subcutaneous injection = 29.0 ± 8.7 L.
3. Icatibant is metabolized by proteolytic enzymes into inactive metabolites. The cytochrome P450          enzyme system is not involved with the metabolism of icatibant.
4. Route of elimination is Urine (<10% unchanged).
5. After subcutaneous administration, mean elimination half-life was 1.4 ± 0.4 hours.


THERAPEUTIC USES
Treating sudden attacks of hereditary angioedema (HAE).


SIDE EFFECTS
1. Fever or dizziness may occur.
2. Injection site reactions (such as redness, burning, swelling, bruising, irritation, pain) may also              occur.


DRUG-DRUG INTERACTIONS
1. Icatibant + Trandolapril = Icatibant may decrease the antihypertensive activities.
2. Icatibant + Ramipril = Icatibant may decrease the antihypertensive activities.
3. Icatibant + Quinapril = Icatibant may decrease the antihypertensive activities.
4. Icatibant + Perindopril = Icatibant may decrease the antihypertensive activities.




REFERENCE- Tripathi K.D. "Essentials of Medical Pharmacology", 7th Edition, page no- 511

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