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Icatibant (Monograph)

Brand name: Firazyr
Drug class: Bradykinin Receptor Antagonists

Medically reviewed by Drugs.com on Nov 16, 2023. Written by ASHP.

Introduction

Synthetic decapeptide similar in structure to bradykinin; a selective bradykinin type 2 (B2) receptor antagonist.

Uses for Icatibant

Hereditary Angioedema

Treatment of acute attacks of hereditary angioedema (HAE); designated an orphan drug by FDA for this use.

Currently not FDA-labeled or recommended for prophylaxis of HAE attacks.

Icatibant Dosage and Administration

General

Administration

Sub-Q Administration

Inject sub-Q into abdomen over at least 30 seconds until entire contents of syringe have been expelled; administer about 5–10 cm (2–4 inches) below the umbilicus and ≥5 cm (≥2 inches) from scars.

Use 25-gauge needle supplied by manufacturer; do not use any other needle.

Dosage

Available as icatibant acetate; dosage expressed in terms of icatibant.

Adults

Hereditary Angioedema
Sub-Q

Inject 30 mg at onset of acute attack. May repeat dose every 6 hours as needed for recurring symptoms or inadequate response, up to maximum of 3 doses (90 mg total) within a 24-hour period.

Prescribing Limits

Adults

Hereditary Angioedema
Sub-Q

Maximum 90 mg in 24-hour period.

Special Populations

Hepatic Impairment

No dosage adjustment required.

Renal Impairment

No dosage adjustment required.

Geriatric Patients

No dosage adjustment required.

Cautions for Icatibant

Contraindications

Warnings/Precautions

Warnings

Laryngeal Attacks

Risk of airway obstruction during acute laryngeal HAE attack; immediately seek medical attention in appropriate healthcare facility in addition to treatment with icatibant.

Specific Populations

Pregnancy

Available data have not established an association between the drug and major birth defects, miscarriage, or adverse maternal or fetal outcomes.

Lactation

No data on presence in human milk, effects on the breastfed infant or effects on milk production. Distributed into milk in rats; likely to also distribute into human milk. However, sytemic absorption in infants not expected after oralexposure through breastmilk. Consider benefits of breastfeeding along with mother's clinical need for icatibant and any potential adverse effects on the breastfed child from the drug or underlying maternal condition.

Pediatric Use

Safety and efficacy in patients <18 years of age not established. In juvenile animal studies, sub-Q administration of icatibant associated with delayed sexual maturation, impaired fertility, and impared reproductive performance in male rats.

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger patients.

Common Adverse Effects

Injection site reactions (e.g., bruising, hematoma, burning, erythema, hypoesthesia, irritation, numbness, edema, pain, pressure sensation, pruritus, swelling, urticaria, warmth), pyrexia, elevated serum aminotransferase concentrations, dizziness, rash.

Drug Interactions

No formal drug interaction studies to date. However, icatibant is not metabolized by CYP isoenzymes.

Specific Drugs

Drug

Interaction

ACE inhibitors (e.g., captopril)

Potential for decreased hypotensive effect of ACE inhibitor

Icatibant Pharmacokinetics

Absorption

Bioavailability

Mean absolute bioavailability of approximately 97% when given sub-Q dose.

Peak plasma concentrations achieved after approximately 0.75 hours after sub-Q dose.

Special Populations

Hepatorenal syndrome (Clcr 30–60 mL/minute): Plasma concentrations similar to those in patients with normal renal function.

Geriatric patients (male and female): AUC increased approximately twofold compared with young men and women.

Patients with low body weight: Increased systemic exposure.

Female patients (with typically lower body weight than males): AUC and peak plasma concentration increased approximately twofold compared with males.

Distribution

Extent

Distributed into milk in rats; not known whether distributed into human milk.

Elimination

Metabolism

Metabolized extensively by proteolytic enzymes.

Elimination Route

Excreted principally in urine as inactive metabolites.

Half-life

Approximately 1.4 hours.

Special Populations

Mild to moderate hepatic impairment (Child-Pugh score 5–8): Following continuous IV infusion [off-label], pharmacokinetic parameters similar to those in healthy individuals.

Hepatic impairment (Child-Pugh score 7–15): Clearance similar to that in healthy individuals.

Geriatric patients: Reduced clearance, resulting in increased systemic exposure.

Patients with low body weight: Reduced clearance, resulting in increased systemic exposure.

Stability

Storage

Parenteral

Injection

2–25°C. Do not freeze. Protect from light.

Actions

Advice to Patients

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Icatibant Acetate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

Injection, for subcutaneous use

10 mg (of icatibant) per mL (30 mg)

Firazyr (available as disposable prefilled syringes)

Takeda

AHFS DI Essentials™. © Copyright 2024, Selected Revisions November 16, 2023. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Off-label: Use is not currently included in the labeling approved by the US Food and Drug Administration.

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Frequently asked questions