Class: Complement Inhibitors
Chemical Name: d-Arginyl-l-arginyl-l-prolyl-trans-4-hydroxy-l-prolylglycyl-3-(2-thienyl)-l-alanyl-l-seryl-d-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-l-(2α,3aβ,7aβ)-octahydro-1H-indole-2-carbonyl-l-arginine acetate (salt)
Molecular Formula: C59H89N19O13S.xC2H4O2
CAS Number: 138614-30-9
Synthetic decapeptide similar in structure to bradykinin; a selective bradykinin type 2 (B2) receptor antagonist.
Uses for Icatibant
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
Patients may self-administer drug after receiving training from healthcare provider.
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.
Available as icatibant acetate; dosage expressed in terms of icatibant.
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.
Maximum 90 mg in 24-hour period.
No dosage adjustment required.
No dosage adjustment required.
No dosage adjustment required.
Cautions for Icatibant
No known contraindications.
Risk of airway obstruction during acute laryngeal HAE attack; immediately seek medical attention in appropriate healthcare facility in addition to treatment with icatibant.
Distributed into milk in rats; not known whether distributed into human milk. Use caution.
Safety and efficacy in patients <18 years of age not established.
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.
Interactions for Icatibant
No formal drug interaction studies to date. However, icatibant is not metabolized by CYP isoenzymes.
ACE inhibitors (e.g., captopril)
Potential for decreased hypotensive effect of ACE inhibitor
Mean absolute bioavailability of approximately 97% when given sub-Q dose.
Peak plasma concentrations achieved after approximately 0.75 hours after sub-Q dose.
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.
Distributed into milk in rats; not known whether distributed into human milk.
Metabolized extensively by proteolytic enzymes.
Excreted principally in urine as inactive metabolites.
Approximately 1.4 hours.
Mild to moderate hepatic impairment (Child-Pugh score 5–8): Following continuous IV infusion†, 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.
2–25°C. Do not freeze. Protect from light.
A synthetic decapeptide similar in structure to bradykinin; a selective bradykinin type 2 (B2) receptor antagonist.
HAE is a rare autosomal-dominant genetic disorder characterized by a mutation in the complement 1 (C1)-inhibitor gene; deficiency in C1-esterase inhibitor results in unrestrained activity of plasma kallikrein and elevated bradykinin levels, which leads to increased vascular permeability and angioedema.
Competitive inhibition of the bradykinin B2 receptor reduces the vasodilatory effects of excess bradykinin.
Advice to Patients
Advise patients of maximum dosage; do not administer >3 doses of 30 mg each (total of 90 mg) within a 24-hour period.
Advise patients to immediately seek medical attention after treating a laryngeal HAE attack with icatibant.
Risk of injection site reactions. Importance of patients informing clinicians if any erythema, bruising, swelling, warmth, burning sensation, pruritus, irritation, urticaria, numbness, pressure, or pain occurs at injection site.
Risk of pyrexia, elevated serum aminotransferases (ALT, AST), and rash.
Risk of fatigue, drowsiness, and dizziness; do not perform hazardous activities requiring mental alertness or physical coordination (e.g., operating machinery, driving a motor vehicle) if such symptoms occur.
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.
Importance of informing patients of other important precautionary information. (See Cautions.)
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.
Injection, for subcutaneous use
10 mg (of icatibant) per mL (30 mg)
Firazyr (available as disposable prefilled syringes)
AHFS DI Essentials™. © Copyright 2022, Selected Revisions February 15, 2013. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
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