Skip to Content

Icatibant

Medically reviewed on March 25, 2018

Pronunciation

(eye KAT i bant)

Index Terms

  • HOE 140
  • Icatibant Acetate

Dosage Forms

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.

  • Firazyr

Pharmacologic Category

  • Selective Bradykinin B2 Receptor Antagonist

Pharmacology

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.

Distribution

Vdss: 20.3 to 37.7 L

Metabolism

Metabolized by proteolytic enzymes to metabolites (inactive)

Excretion

Urine (<10% unchanged)

Onset of Action

Median time to 50% decrease of symptoms: ~2 hours

Time to Peak

0.75 hours

Duration of Action

Inhibits symptoms caused by bradykinin for ~6 hours

Half-Life Elimination

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.

Special Populations: Gender

Women have a 2-fold higher AUC and Cmax compared with men because of differences in body weight.

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.

Contraindications

There are no contraindications listed in the manufacturer’s labeling.

Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to icatibant acetate or any component of the formulation.

Dosing: Adult

Hereditary angioedema (HAE): SubQ: 30 mg; may repeat every 6 hours if response is inadequate or symptoms recur (maximum dose: 90 mg/day).

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).

Dosing: Geriatric

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.

Administration

SubQ: For SubQ injection only. Patients may self-administer upon recognition of an HAE attack. 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.

Storage

Store between 2°C to 25°C (36°F to 77°F); do not freeze. Store in original container until time of administration.

Drug Interactions

Angiotensin-Converting Enzyme Inhibitors: Icatibant may diminish the antihypertensive effect of Angiotensin-Converting Enzyme Inhibitors. Monitor therapy

Adverse Reactions

>10%: Local: Injection site reaction (97%)

1% to 10%:

Central nervous system: Dizziness (3%)

Hepatic: Increased serum transaminase (4%)

Miscellaneous: Fever (4%)

<1%: Antibody development (anti-icatibant, no association with efficacy observed), chest pain, headache, myocardial infarction, nausea, skin rash

Warnings/Precautions

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: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving).

Monitoring Parameters

Symptom relief; laryngeal symptoms or airway obstruction (immediate medical attention required in addition to icatibant therapy)

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events were observed in some animal reproduction studies.

Information related to the use of icatibant in pregnancy is limited (Boufleur 2014; Farkas 2016; Kaminsky 2017; Tran 2013; Zanichelli 2015). When treatment for hereditary angioedema (HAE) in pregnancy is needed, other agents are recommended (WAO/EEACI [Maurer 2018]).

Patient Education

• 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.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Hide