Firazir
Firazir Uses, Dosage, Side Effects, Food Interaction and all others data.
Firazir (Firazyr) is a synthetic peptidomimetic drug consisting of ten amino acids, and acts as an effective and specific antagonist of bradykinin B2 receptors. It has been approved in the EU for use in hereditary angioedema, and is under investigation for a number of other conditions in which bradykinin is thought to play a significant role. Firazir currently has orphan drug status in the United States and FDA approved on August 25, 2011.
Firazir is a potent, specific, competitive, and selective peptidomimetic bradykinin beta2-receptor antagonist (pA2 = 9.04). It has a modified peptide structure, and is the first bradykinin receptor antagonist to act on the guinea-pig trachea without demonstrating agonist effects. It also inhibits aminopeptidase N (Ki = 9.1 μM). If an IV dose of 0.4 and 0.8 mg/kg was infused over 4 hours, one may observe an inhibited response to bradykinin challenge for 6 - 8 hours following completion of infusion.
| Trade Name | Firazir |
| Availability | Prescription only |
| Generic | Icatibant |
| Icatibant Other Names | Icatibant |
| Related Drugs | Orladeyo, Firazyr, Haegarda, Ruconest, Berinert, Cinryze, Kalbitor |
| Type | |
| Formula | C59H89N19O13S |
| Weight | Average: 1304.54 Monoisotopic: 1303.660795176 |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Russia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Firazir is a bradykinin B2 receptor antagonist used to treat acute episodes of swelling and inflammation associated with hereditary angioedema (HAE).
Approved for use in acute attacks of hereditary angioedema (HAE). Investigated for use/treatment in angioedema, liver disease, and burns and burn infections.
Firazir is also used to associated treatment for these conditions: ACE Inhibitor-associated Angioedema, Hereditary angioedema breakthrough attack
How Firazir works
Bradykinin is a peptide-based hormone that is formed locally in tissues in response to a trauma and acts to increases vessel permeability, dilates blood vessels and causes smooth muscle cells to contract. Bradykinin plays an important role in the mediation of pain as surplus bradykinin is partly responsible for producing signs of inflammation by activating bradykinin B2 receptors. In patients with HAE, they have an absent or dysfunctional C1-esterase inhibitor. This inhibitor is responsible for the production of bradykinin in which displacement of bradykinin from B2 receptors by icatibant has an inhibitory effect on the receptor for a relatively long time.
Food Interaction
No interactions found.Volume of Distribution
Vdss, subcutaneous injection = 29.0 ± 8.7 L.
Elimination Route
The absolute bioavailability of icatibant following a 30 mg subcutaneous dose is approximately 97%. Maximum plasma concentrations (Cmax) of 974 ± 280 ng/mL was reached when a single subcutaneous dose of 30 mg was administered. The AUC was 2165 ± 568 ng∙hr/mL. Firazir did not accumulate following multiple doses.
Half Life
After subcutaneous administration, mean elimination half-life was 1.4 ± 0.4 hours.
Clearance
Plasma clearance following subcutaneous administration was 245 ± 58 mL/min.
Elimination Route
Urine (<10% unchanged)
Innovators Monograph
You find simplified version here Firazir
