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Icatibant Acetate

Pronunciation: eye-KAT-i-bant AS-e-tate
Class: Bradykinin inhibitor

Trade Names

Firazyr
- Injection, solution 10 mg/mL

Pharmacology

Inhibits bradykinin from binding to the B2 receptor. Bradykinin is a vasodilator and is thought to be responsible for the hereditary angioedema symptoms of localized swelling, inflammation, and pain.

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Pharmacokinetics

Absorption

Bioavailability after subcutaneous administration is 97%. C max is 974 ng/mL. T max is 0.75 h.

Distribution

Vd is 29 L.

Metabolism

Extensively metabolized by proteolytic enzymes to inactive metabolites.

Elimination

Plasma Cl is 245 mL/min. Elimination half-life is 1.4 h. Inactive metabolites are primarily excreted in the urine; less than 10% of the dose is eliminated as unchanged drug.

Special Populations

Renal Function Impairment

Cl is not dependent on renal function and, therefore, no differences were seen in plasma levels in patients with renal impairment compared with subjects with healthy renal function.

Hepatic Function Impairment

Pharmacokinetic parameters are comparable in hepatically impaired patients and healthy subjects.

Elderly

Elderly subjects had a 2-fold higher AUC compared with younger subjects. Only minor differences (12% to 14%) in C max were observed. No dosage adjustment is needed.

Gender

Women have a 2-fold higher AUC and C max compared with men because of differences in body weight. Dosage adjustment is not needed.

Indications and Usage

Treatment of acute attacks of hereditary angioedema.

Contraindications

None well documented.

Dosage and Administration

Adults

Subcutaneous 30 mg. Additional doses may be administered at intervals of at least 6 h if response is inadequate or if symptoms recur (max, 3 doses per 24 h).

General Advice

  • For subcutaneous use in the abdominal area. Administer over at least 30 seconds.
  • Patients may self-administer upon recognition of symptoms of a hereditary angioedema attack after training under the guidance of a health care provider.

Storage/Stability

Store between 36° and 77°F. Do not freeze. Store in carton until time of administration.

Drug Interactions

ACE inhibitors (eg, captopril)

Icatibant is a bradykinin B2 receptor antagonist and has the potential to attenuate the antihypertensive effect of ACE inhibitors. Use with caution and monitor BP.

Adverse Reactions

CNS

Dizziness (3%); headache.

Dermatologic

Rash.

GI

Nausea.

Hepatic

Transaminase increased (4%).

Local

Injection-site reactions, including bruising, hematoma, burning, erythema, hypoesthesia, irritation, numbness, edema, pain, pressure sensation, pruritus, swelling, urticaria, and warmth (97%).

Miscellaneous

Pyrexia (4%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Cardiovascular effects

The B2 receptor has been implicated in the cardioprotective effects of bradykinin; antagonism of this receptor may have negative cardiovascular effects during reperfusion after acute ischemia. Use icatibant during acute coronary ischemia, unstable angina pectoris, or in the weeks following a stroke only if the benefit exceeds the theoretical risk to the patient.

Immunogenicity

Patients have developed antibodies to icatibant. No hypersensitivity or anaphylactic reactions were reported with icatibant, and no association between anti-icatibant antibodies and efficacy was observed.

Laryngeal attacks

Because of the potential for airway obstruction during acute laryngeal hereditary angioedema attacks, patients should seek medical attention in addition to treatment with icatibant.

Overdosage

Symptoms

Erythema, itching, hypotension.

Patient Information

  • Instruct patients on self-administration of icatibant.
  • Advise patients with laryngeal symptoms to seek medical attention in an appropriate health care facility after administration of icatibant.
  • Inform patients that injection-site reactions are reported in most patients after administration of icatibant and that other adverse reactions reported after administration include pyrexia, increase in transaminases, dizziness, and rash.
  • Inform patients that tiredness, drowsiness, and dizziness have been reported following the use of icatibant. Advise patients not to drive or use machinery if they feel tired or dizzy.

Copyright © 2009 Wolters Kluwer Health.

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