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Icatibant

Medically reviewed by Drugs.com. Last updated on Jul 14, 2020.

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)

Generic: 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:

Children ≥2 years: 0.39 ± 0.11 L/kg (Farkas 2017)

Adolescents: 0.44 ± 0.18 L/kg (Farkas 2017)

Adults: 29 ± 8.7 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

Children ≥2 years: 0.42 ± 0.13 hours (Farkas 2017)

Adolescents: 0.55 ± 0.19 hours (Farkas 2017)

Adults: ~0.75 hours

Duration of Action

Inhibits symptoms caused by bradykinin for ~6 hours

Half-Life Elimination

Children ≥2 years: 0.8 ± 0.04 hours (Farkas 2017)

Adolescents: 1.34 ± 0.96 hours (Farkas 2017)

Adults: 1.4 ± 0.4 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 inhibitor–induced angioedema, severe or life-threatening

Data regarding the efficacy of icatibant for the treatment of angiotensin-converting enzyme (ACE) inhibitor-induced angioedema involving the upper aerodigestive tract (ie, face, lips, cheeks, tongue, soft palate or uvula, pharynx, larynx) are conflicting. In 2 randomized, double-blind, placebo-controlled studies, no difference in time to meet discharge criteria or resolution of symptoms was found between icatibant and placebo [Sinert 2017], [Straka 2017]. However, data from an earlier multicenter, randomized, double-blind, double-dummy trial suggest that the use of icatibant for the treatment of ACE inhibitor–induced angioedema may be beneficial to improve time to resolution of edema and symptom relief.[Baş 2015] In the setting of life-threatening airway compromise, rescue procedures (including intubation or tracheotomy with mechanical ventilation) may still be required [Baram 2013].

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

Angiotensin-converting enzyme inhibitor-induced angioedema, severe or life-threatening (off-label use): SubQ: 30 mg; a second 30 mg injection may be administered if symptoms of angioedema continue to worsen after 6 hours (Baş 2015; Hirschy 2018). Note: Most likely to be effective if administered within the first few hours of angioedema attack (ie, ≤6 hours) when swelling is increasing and has not yet peaked and/or stabilized (Baş 2015; Guyer 2019). IV prednisolone (not available in the US) was administered with the second dose of icatibant (Baş 2015).

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Hereditary angioedema (HAE): Limited data available: Children ≥2 years and Adolescents: SubQ: 0.4 mg/kg once; maximum dose: 30 mg/dose. Dosing based on an open-label study of 32 patients (mean age: 12.3 ± 3.5 years) with HAE (Farkas 2017).

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

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

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

1% to 10%:

Hepatic: Increased serum transaminase (4%)

Immunologic: Antibody development (4%; anti-icatibant, no association with efficacy observed)

Nervous system: Dizziness (3%)

Miscellaneous: Fever (4%)

Frequency not defined:

Dermatologic: Skin rash

Gastrointestinal: Nausea

Nervous system: Headache

Postmarketing: Dermatologic: Urticaria

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 Considerations

Information related to the use of icatibant in pregnancy is limited (Boufleur 2014; Farkas 2016; Hakl 2018; Kaminsky 2017; Tran 2013; Zanichelli 2015).

When treatment for hereditary angioedema in pregnancy is needed, other agents are recommended (Betschel 2019; WAO/EEACI [Maurer 2018]).

Patient Education

What is this drug used for?

• It is used to treat swelling attacks in people with hereditary angioedema (HAE).

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Dizziness

• Nausea

• Headache

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Severe injection site irritation

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

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

Frequently Asked Questions