Dosing and uses of Firazyr (icatibant)
Adult dosage forms and strengths
SC injection, prefilled syringe
- 30mg (10 mg/mL)
Hereditary Angioedema
Bradykinin B2 receptor antagonist indicated for treatment of acute attacks of hereditary angioedema (HAE)
3 mL (30 mg) SC in abdominal area
If response inadequate or symptoms recur, additional injection of 30 mg may be administered at intervals of at least 6 hr
Do not exceed a total of 3 injections/24 hr
Dosage modifications
Hepatic or renal impairment: No dosage adjustment required
Pediatric dosage forms and strengths
<18 years: Safety and efficacy not established
Geriatric dosage forms and strengths
Limited information is available for patients >65 years old
Increased Cmax and AUC in elderly patients (particularly women) have been observed
Differences in efficacy and safety between elderly and younger patients have not been identified, no dose adjustment recommended
Hereditary Angioedema
Bradykinin B2 receptor antagonist indicated for treatment of acute attacks of hereditary angioedema (HAE)
3 mL (30 mg) SC in abdominal area
If response inadequate or symptoms recur, additional injection of 30 mg may be administered at intervals of at least 6 hr
Do not exceed a total of 3 injections/24 hr
Firazyr (icatibant) adverse (side) effects
>10%
Injection site reactions (97%)
1-10%
Pyrexia (4%)
Transaminase increased (4%)
Dizziness (3%)
Warnings
Contraindications
Hypersensitivity
Cautions
Given the potential for airway obstruction during acute laryngeal HAE attacks, patients should be advised to seek medical attention in an appropriate healthcare facility immediately in addition to treatment
Patients should be advised not to drive or use machinery if they feel tired or dizzy
Report suspected adverse reactions to Shire Human Genetic Therapies at OnePath phone # 1-866-888-0660 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch
Pregnancy and lactation
Pregnancy category: C
Lactation: Unknown whether distributed in breast milk; caution advised
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Firazyr (icatibant)
Mechanism of action
Competitive antagonist selective for bradykinin B2 receptor
Bradykinin formation results in vascular leakage and edema, the most recognizable symptoms of hereditary angioedema
Absorption
Bioavailability: 97%
Peak Plasma Time: 45 minutes
Duration: Inhibits symptoms caused by bradykinin for 6 hr on average
Peak Plasma Concentration: 974 ng/mL
AUC: 2165 ng•hr/mL
Distribution
Vd: 20-37 L
Metabolism
Extensively metabolized by proteolytic enzymes to inactive metabolites primarily excreted in urine
No evidence of clinically relevant inhibition or induction of CYP450 enzymes
Elimination
Half-life elimination: 1.4 hr
Plasma clearance: 245 mL/min
Excretion: Urine
Administration
SC Administration
Dose may be self-administered by patient after training under the guidance of a healthcare professional or dose can be administered by a healthcare professionaL
Inspect visually for particulate matter and discoloration prior to administration; do not administer if product contains particulates or is discolored
Attach provided 25 gauge needle to syringe hub and screw on securely; do not use a different needle
Disinfect injection site
Administer by subcutaneous (SC) injection over at least 30 sec
Storage
Refrigerate between 2-25°C (36-77°F)
Store in carton until time of administration
Do not freeze
