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FDA Approved Cardiovascular & Renal

Icatibant

also known as: Firazyr, HOE 140

The bradykinin blocker for angioedema — a synthetic decapeptide B2 receptor antagonist that stops acute swelling attacks within 30 minutes.

A synthetic 10-amino-acid peptidomimetic that selectively antagonizes bradykinin B2 receptors, FDA-approved for the treatment of acute attacks of hereditary angioedema (HAE) in adults.

Mechanism of action

Selective competitive antagonist at bradykinin B2 receptor. In HAE, C1-esterase inhibitor deficiency leads to excess bradykinin causing vascular leak and edema. Icatibant blocks B2R activation, reversing swelling within 30-60 minutes.

Primary uses

  • Acute hereditary angioedema attacks (FDA-approved)
  • ACE inhibitor-induced angioedema (off-label)

Typical dosing

30 mg single SC injection per attack; may repeat q6h (max 3/24h) (subcutaneous)

Self-administered using prefilled syringe. Onset typically within 30-60 minutes.

Regulatory status

FDA-approved August 2011 as Firazyr for acute HAE attacks in adults. Self-administered via subcutaneous injection.

References

  1. [pubmed] Cicardi M, et al. "Icatibant, a new bradykinin-receptor antagonist, in hereditary angioedema." N Engl J Med. 2010;363(6):532-541.

Related peptides

Bradykinin

The vasoactive peptide behind ACE inhibitor cough — an endogenous inflammatory mediator that connects cardiovascular pharmacology to angioedema, pain, and allergic responses.

Angiotensin II

Giapreza — the first new vasopressor class approved in decades. FDA-approved December 2017 (La Jolla Pharmaceutical) for catecholamine-resistant septic / distributive shock based on the ATHOS-3 trial (NEJM 2017, n=321). Engages a third vasoconstrictor pathway (RAAS / AT1) independent of catecholamines and vasopressin — useful when both of those axes are desensitised.

Vasopressin

Vasostrict — the endogenous antidiuretic hormone as an ICU vasopressor. FDA-approved April 2014 for adults with vasodilatory shock (post-cardiotomy, sepsis) who remain hypotensive despite fluids and catecholamines. Works through V1a receptors on vascular smooth muscle — a receptor axis pharmacologically distinct from catecholamine receptors, preserving its vasopressor effect when adrenergic receptors are desensitised.

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Disclaimer

This entry is for educational purposes only and does not constitute medical advice. Dosing information reflects published regulatory or research data and is not a recommendation. Many compounds described here are not approved for human use in the United States. Consult a licensed medical professional before considering any peptide therapy.