Icatibant


Generic Medicine Info
Indications and Dosage
Subcutaneous
Hereditary angioedema
Adult: For the treatment of acute attacks in patients with C1-esterase inhibitor deficiency: 30 mg as a single dose via SC inj over ≥30 seconds. Additional doses may be given at intervals of ≥6 hours if relief is insufficient or symptoms recur. Max: 3 doses (90 mg) daily.
Child: Dosage recommendations may vary among countries and individual products. Refer to specific product guidelines.
Special Precautions
Patient with acute ischaemic heart disease or unstable angina pectoris, recent stroke. Advise patients with laryngeal hereditary angioedema (HAE) attacks to seek immediate medical attention in an appropriate healthcare facility in addition to treatment with icatibant. Children. Pregnancy and lactation.
Adverse Reactions
Significant: CNS depression.
Gastrointestinal disorders: Nausea.
General disorders and administration site conditions: Pyrexia, inj site reactions (e.g. bruising, burning, haematoma, erythema, hypoaesthesia, irritation, numbness, oedema, pain, pressure sensation, swelling, urticaria, warmth).
Investigations: Increased transaminases and creatine phosphokinase, prolonged prothrombin time.
Nervous system disorders: Dizziness, headache.
Skin and subcutaneous tissue disorders: Erythema, pruritus, rash.
Patient Counseling Information
This drug may cause lethargy, tiredness, fatigue, somnolence, or dizziness; if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor symptom relief; laryngeal symptoms or airway obstruction.
Drug Interactions
May decrease the antihypertensive effect of ACE inhibitors.
Action
Description:
Mechanism of Action: Icatibant, a synthetic decapeptide, is a selective competitive inhibitor at the bradykinin type 2 (B2) receptor. Bradykinin is a vasodilator thought to be responsible for the characteristic HAE symptoms of localised swelling, inflammation, and pain. Competitive inhibition of the bradykinin B2 receptor reduces the vasodilatory effects of excess bradykinin, thereby treating the symptoms associated with the acute attacks of HAE.
Onset: 50% decrease in symptoms: Approx 2 hours.
Duration: Approx 6 hours.
Pharmacokinetics:
Absorption: Bioavailability: Approx 97%. Time to peak plasma concentration: 0.75 hours.
Distribution: Plasma protein binding: 44%.
Metabolism: Extensively metabolised by proteolytic enzymes to inactive metabolites.
Excretion: Mainly via urine (<10% as unchanged drug). Elimination half-life: Approx 1-2 hours.
Chemical Structure

Chemical Structure Image
Icatibant

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 6918173, Icatibant. https://pubchem.ncbi.nlm.nih.gov/compound/Icatibant. Accessed Apr. 27, 2022.

Storage
Store between 2-25°C. Do not freeze. Protect from light. Follow applicable procedures for receiving, handling, administration, and disposal.
MIMS Class
Antihistamines & Antiallergics / Other Cardiovascular Drugs
ATC Classification
B06AC02 - icatibant ; Belong to the class of drugs used in the treatment of hereditary angioedema.
References
Anon. Icatibant Acetate. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 16/12/2021.

Anon. Icatibant. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 16/12/2021.

Buckingham R (ed). Icatibant Acetate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 16/12/2021.

Firazyr Solution for Injection in Pre-filled Syringe 30 mg/3 mL (Takeda Pharmaceuticals [Hong Kong] Ltd). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 16/12/2021.

Icatibant 30 mg Solution for Injection in Pre-filled Syringe (Kensington Pharma Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 16/12/2021.

Icatibant Acetate Injection, Solution (Apotex Corp.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 16/12/2021.

Sajazir Injection (Cycle Pharmaceuticals Ltd-UK). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 16/12/2021.

Takeda New Zealand Limited. Firazyr 30 mg/3 mL Solution for Injection data sheet 28 September 2020. Medsafe. http://www.medsafe.govt.nz. Accessed 16/12/2021.

Disclaimer: This information is independently developed by MIMS based on Icatibant from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2024 MIMS. All rights reserved. Powered by MIMS.com
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