(eye KAT i bant)
- HOE 140
- Icatibant Acetate
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Subcutaneous [preservative free]:
Firazyr: 30 mg/3 mL (3 mL)
Brand Names: U.S.
- Selective Bradykinin B2 Receptor Antagonist
Icatibant is a selective competitive antagonist for the bradykinin B2 receptor. Patients with HAE have an absence or dysfunction of C1-esterase-inhibitor which leads to the production of bradykinin. The presence of bradykinin may cause symptoms of localized swelling, inflammation, and pain. Icatibant inhibits bradykinin from binding at the B2 receptor, thereby treating the symptoms associated with acute attack.
Vdss: 20.3 to 37.7 L
Metabolized by proteolytic enzymes to metabolites (inactive)
Urine (<10% unchanged)
Onset of Action
Median time to 50% decrease of symptoms: ~2 hours
Time to Peak
Duration of Action
Inhibits symptoms caused by bradykinin for ~6 hours
1 to 1.8 hours
Special Populations: Elderly
Elderly subjects had a 2-fold higher AUC compared with younger subjects. Only minor differences (12% to 14%) in Cmax were observed. No dosage adjustment is needed.
Special Populations: Gender
Women have a 2-fold higher AUC and Cmax compared with men because of differences in body weight. Dosage adjustment is not needed.
Use: Labeled Indications
Hereditary angioedema: Treatment of acute attacks of hereditary angioedema (HAE)
Off Label Uses
Angiotensin-converting enzyme (ACE) inhibitor-induced angioedema
Data regarding the efficacy of icatibant for the treatment of ACE inhibitor–induced angioedema involving the upper aerodigestive tract (ie, face, lips, cheeks, tongue, soft palate or uvula, pharynx, larynx) are conflicting. In 2 placebo-controlled, double-blind studies, no difference in response was found between icatibant and placebo. However, data from an earlier multicenter, randomized, double-blind, double-dummy trial support the use of icatibant for the treatment of ACE inhibitor–induced angioedema. In the setting of life-threatening airway compromise, rescue procedures (including intubation or tracheotomy with mechanical ventilation) may still be required. Additional trials may be necessary to further define the role of icatibant in this condition.
There are no contraindications listed in the U.S. manufacturer’s labeling.
Canadian labeling: Hypersensitivity to icatibant acetate or any component of the formulation.
Hereditary angioedema (HAE): SubQ: 30 mg; may repeat every 6 hours if response is inadequate or symptoms recur (maximum daily dose: 90 mg).
ACE inhibitor-induced angioedema (off-label use): SubQ: 30 mg; if symptoms of angioedema continue to worsen after 6 hours, a second injection may be administered. The authors administered intravenous prednisolone (not available in the US) with the second dose of icatibant (Bas, 2015).
Refer to adult dosing. Systemic exposure may be increased; however, no dosage adjustments are recommended.
Dosing: Renal Impairment
No dosage adjustments are recommended (has not been studied); however, icatibant is cleared by nonrenal mechanisms and is not expected to accumulate in patients with renal impairment.
Dosing: Hepatic Impairment
No dosage adjustments necessary.
For SubQ injection only. Inject into the abdomen over ≥30 seconds, using the 25 gauge needle provided. Inject 2 to 4 inches below belly button and away from any scars; do not inject into an area that is bruised, swollen, or painful.
Store between 2°C to 25°C (36°F to 77°F); do not freeze. Store in original container until time of administration.
ACE Inhibitors: Icatibant may diminish the antihypertensive effect of ACE Inhibitors. Monitor therapy
>10%: Local: Injection site reaction (97%)
1% to 10%:
Central nervous system: Dizziness (3%)
Hepatic: Increased serum transaminase (4%)
Miscellaneous: Fever (4%)
<1% (Limited to important or life-threatening): Antibody development (anti-icatibant, no association with efficacy observed), chest pain, headache, myocardial infarction, nausea, skin rash
Concerns related to adverse effects:
• Airway obstruction: Airway obstruction may occur during acute laryngeal attacks of HAE. Patients with laryngeal attacks should be instructed to seek medical attention immediately in addition to treatment with icatibant.
• CNS effects: Dizziness has been observed following use; advise patients to use caution when driving or operating machinery.
Symptom relief; laryngeal symptoms or airway obstruction (immediate medical attention required in addition to icatibant therapy)
Pregnancy Risk Factor
Adverse events were observed in animal reproduction studies with doses close to or less than the recommended human dose. Has not been adequately studied in pregnant women.
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience dizziness, nausea, or headache. Have patient report immediately to prescriber severe injection site irritation (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.
More about icatibant
- Side Effects
- During Pregnancy
- Dosage Information
- Drug Interactions
- Support Group
- En Español
- 4 Reviews – Add your own review/rating
- Drug class: miscellaneous cardiovascular agents
Other brands: Firazyr