Firatibant (Solution) Instructions for Use

Marketing Authorization Holder

Jodas Expoim, LLC (Russia)

Manufactured By

Jodas Expoim, Pvt. Ltd. (India)

ATC Code

B06AC02 (Icatibant)

Active Substance

Icatibant

Dosage Form

Firatibant

Solution for subcutaneous administration 10 mg/ml

Dosage Form, Packaging, and Composition

Solution for subcutaneous administration

3 ml – syringes – cardboard packs – Prescription only
3 ml – syringes – cardboard packs /in a set with a needle-1 pc./ – Prescription only

Clinical-Pharmacological Group

Bradykinin B₂-receptor blocker. Antiallergic drug

Pharmacotherapeutic Group

Other hematological agents; agents used in hereditary angioedema

Pharmacological Action

Icatibant is a selective competitive antagonist of bradykinin B₂ receptors, a synthetic decapeptide structurally similar to bradykinin but containing 5 non-proteinogenic amino acids.

Bradykinin is formed from high molecular weight kininogen with the participation of kallikrein. Approximately 40% of plasma kallikrein is inactivated by the action of C1-esterase inhibitor. Deficiency or dysfunction of C1-esterase inhibitor leads to an increase in plasma kallikrein levels.

This contributes to an increase in bradykinin levels, which is the main biologically active substance responsible for the development of clinical symptoms of angioedema, directly causing increased vascular permeability, vasodilation, and contractions of visceral smooth muscles.

Therefore, exposure to an etiological factor against a background of C1-esterase inhibitor deficiency leads to excessive production of bradykinin with a subsequent marked increase in vascular permeability.

Icatibant acts as a bradykinin inhibitor by blocking the binding of endogenous bradykinin to bradykinin B₂ receptors, thereby preventing the pharmacological action of bradykinin.

Pharmacokinetics

After subcutaneous administration, absorption is rapid, with a T_max of approximately 30 minutes. Plasma protein binding is 44±3%. The V_ss is approximately 20-25 L.

Icatibant is metabolized to form metabolites M1 and M2. Metabolism appears to be mediated by NADP-independent proteolytic enzymes and occurs without the involvement of CYP450 isoenzymes.

The clearance of icatibant is approximately 15-20 L/h. The terminal T_1/2 is approximately 1-2 hours. It is excreted primarily as metabolites in the urine (80-90%) and feces. A small portion (<10%) is excreted unchanged in the urine.

Indications

Symptomatic treatment of acute attacks of hereditary angioedema in adults with C1-esterase inhibitor deficiency.

ICD codes

Dosage Regimen

Administer Firatibant as a subcutaneous injection into the abdominal wall.

Use the single-dose pre-filled syringe containing 30 mg of icatibant in 3 ml of solution.

The recommended dose for an acute hereditary angioedema attack is 30 mg.

Inject the entire contents of the syringe subcutaneously.

Do not administer intravenously or intramuscularly.

If an attack persists, a second dose may be administered after at least 6 hours.

Do not exceed three injections within a 24-hour period.

Self-administration by the patient is permissible only after proper training by a healthcare professional.

Seek immediate medical attention for laryngeal attacks, even after administration.

The duration of therapy is determined by the physician based on clinical response.

Adverse Reactions

Very common reactions at the subcutaneous injection site.

Common nausea, abdominal pain, asthenia, increased CPK, ALT, AST activity, headache, dizziness, nasal congestion.

Sometimes vomiting, weakness, increased body temperature, pharyngitis, weight gain, increased prothrombin time, hyperuricemia, proteinuria, cough, asthma, skin itching, erythema, feeling of heat.

Contraindications

Hypersensitivity to icatibant.

Use in Pregnancy and Lactation

The safety of icatibant use during pregnancy and lactation has not been studied.

Pediatric Use

Clinical data on the use of icatibant in children are not available.

Geriatric Use

Clinical data on the use of icatibant in patients over 65 years of age are not available.

Special Precautions

Treatment with icatibant should be carried out by physicians experienced in its use.

Treatment of patients with laryngeal edema should be carried out only in a hospital setting.

Use with caution in patients with exacerbation of coronary artery disease, unstable angina, and within one week after a stroke.

Clinical data on the use of icatibant in children and patients over 65 are not available.

Drug Interactions

ACE inhibitors are contraindicated in patients with hereditary angioedema (due to a possible increase in bradykinin levels in the body), therefore the drug interaction of icatibant with drugs of this group has not been studied.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.