Icatibant Universal Farma

What Is Icatibant Universal Farma and What Is It Used For?

Icatibant Universal Farma contains the active substance icatibant, a bradykinin B2 receptor antagonist indicated for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in adults, adolescents, and children aged 2 years and older with C1-esterase inhibitor deficiency.

Hereditary angioedema (HAE) is a rare genetic disorder affecting approximately 1 in 50,000 people worldwide. It is caused by a deficiency or dysfunction of C1-esterase inhibitor (C1-INH), a protein that normally regulates several inflammatory pathways in the body. When C1-INH is deficient, the body produces excessive amounts of bradykinin, a powerful vasodilator peptide that increases blood vessel permeability and causes tissue swelling.

HAE attacks are characterized by recurring episodes of severe swelling (angioedema) that can affect the face, extremities, genitals, gastrointestinal tract, and upper airway. Abdominal attacks can cause intense pain, nausea, vomiting, and diarrhea, often mimicking a surgical emergency. Laryngeal attacks represent the most dangerous manifestation, as swelling of the throat can obstruct the airway and become life-threatening if not treated promptly.

Icatibant works by selectively and competitively blocking the bradykinin B2 receptor. As a synthetic decapeptide structurally similar to bradykinin itself, icatibant binds to the B2 receptor with high affinity but does not activate it, thereby preventing bradykinin from exerting its swelling-inducing effects. This targeted mechanism of action directly addresses the root cause of HAE symptoms rather than simply suppressing general inflammation.

The medication was originally developed and marketed under the brand name Firazyr. Icatibant Universal Farma is a generic version that contains the same active substance in the same concentration (30 mg per 3 mL pre-filled syringe) and has been demonstrated to be bioequivalent to the originator product through rigorous regulatory assessment by the European Medicines Agency (EMA).

What Should You Know Before Taking Icatibant Universal Farma?

Before using Icatibant Universal Farma, inform your doctor about all medical conditions, other medications you are taking, and whether you are pregnant or breastfeeding. This medication requires proper training in self-injection technique before use at home.

Contraindications

Icatibant Universal Farma should not be used if you are allergic (hypersensitive) to icatibant or any of the other ingredients in the medicine. The pre-filled syringe solution contains sodium chloride, glacial acetic acid, sodium hydroxide (for pH adjustment), and water for injections. If you have previously experienced a severe allergic reaction to any of these components, this medication is not suitable for you.

Icatibant has not been studied in patients with ischaemic heart disease or acute stroke within the weeks before treatment. Since bradykinin may have cardioprotective effects, theoretical concerns exist about blocking the B2 receptor in patients with active cardiovascular events. Your physician will carefully assess the benefit-risk ratio if you have a recent history of these conditions.

Warnings and Precautions

If you experience a laryngeal attack (swelling of the throat or voice box), you should inject icatibant immediately and then seek emergency medical care right away. Laryngeal attacks can be life-threatening due to the risk of airway obstruction. Even after treatment with icatibant, medical observation is recommended until symptoms have fully resolved.

If your symptoms are not adequately relieved or recur after the first injection, additional injections may be administered at intervals of at least 6 hours. No more than 3 injections should be administered in any 24-hour period. If your symptoms persist despite 3 injections, or if you experience unusual or worsening symptoms, seek immediate medical attention.

The first self-administered injection should ideally be performed under the supervision of a healthcare professional to ensure proper technique. Patients should be trained in subcutaneous injection technique, including recognition of the signs and symptoms of HAE attacks that warrant treatment.

Patients with coronary artery disease or unstable angina should be closely monitored during icatibant treatment, as bradykinin has been shown to have vasodilatory and potentially cardioprotective properties in some experimental models. Blocking the bradykinin B2 receptor could theoretically reduce these protective effects, although no clinically significant adverse cardiovascular events have been attributed to icatibant in clinical trials.

Pregnancy and Breastfeeding

Icatibant is not recommended during pregnancy unless clearly necessary. There are limited data from the use of icatibant in pregnant women. Animal reproductive studies have not shown direct harmful effects on embryo-fetal development, but adequate and well-controlled studies in humans are not available. If you are pregnant or planning to become pregnant, discuss treatment options with your HAE specialist. Women of childbearing potential should use effective contraception during treatment.

It is not known whether icatibant is excreted in human breast milk. Animal studies have shown that icatibant passes into breast milk. A risk to the nursing infant cannot be excluded. A decision must be made whether to discontinue breastfeeding or to abstain from icatibant therapy, taking into account the benefit of breastfeeding for the child and the benefit of treatment for the mother.

HAE attacks can increase in frequency and severity during pregnancy due to hormonal changes, particularly elevated estrogen levels. A comprehensive management plan should be developed with your specialist before or early in pregnancy, including access to appropriate acute treatments and monitoring protocols.

Use in Children and Adolescents

Icatibant is approved for use in children and adolescents aged 2 years and older who weigh at least 12 kg. The dose is adjusted based on body weight for pediatric patients. Children weighing 12 kg to less than 25 kg receive 10 mg (1 mL), those weighing 25 kg to less than 40 kg receive 15 mg (1.5 mL), those weighing 40 kg to less than 50 kg receive 20 mg (2 mL), and those weighing 50 kg to less than 65 kg receive 25 mg (2.5 mL). Children and adolescents weighing 65 kg or more receive the full adult dose of 30 mg (3 mL).

The safety and efficacy of icatibant in children younger than 2 years of age have not been established. No data are available for this age group.

How Does Icatibant Universal Farma Interact with Other Drugs?

Icatibant has a relatively limited drug interaction profile. The most clinically significant interaction is with ACE inhibitors, where icatibant may reduce their blood pressure-lowering effect. Always inform your healthcare provider about all medications you are taking.

Formal drug interaction studies with icatibant have been limited. However, based on its mechanism of action as a bradykinin B2 receptor antagonist, several pharmacological interactions are theoretically possible and clinically relevant. The most important interaction involves angiotensin-converting enzyme (ACE) inhibitors, which work in part by preventing the breakdown of bradykinin, thereby increasing its levels and contributing to blood pressure reduction.

When icatibant blocks the bradykinin B2 receptor, it may counteract the bradykinin-mediated portion of the antihypertensive effect of ACE inhibitors. This does not mean ACE inhibitors become ineffective, as they also lower blood pressure through inhibition of angiotensin II formation, but the overall blood pressure-lowering effect may be temporarily attenuated during and shortly after icatibant treatment.

It is also important to note that ACE inhibitors themselves can provoke angioedema through bradykinin accumulation. ACE inhibitor-induced angioedema is a separate condition from HAE, although patients with HAE who are also taking ACE inhibitors may be at increased risk for more frequent or severe attacks.

Icatibant is metabolized primarily by proteolytic enzymes and is not a substrate, inhibitor, or inducer of cytochrome P450 enzymes. This means it is unlikely to significantly alter the metabolism of other drugs processed through the CYP450 system, and other drugs are unlikely to significantly alter icatibant metabolism. No formal pharmacokinetic drug interaction studies have been conducted, but the metabolic profile suggests a low potential for clinically meaningful pharmacokinetic interactions.

What Is the Correct Dosage of Icatibant Universal Farma?

The standard adult dose is one subcutaneous injection of 30 mg (3 mL) at the onset of an HAE attack. If symptoms persist, additional injections may be given at 6-hour intervals, up to a maximum of 3 injections in 24 hours. Pediatric dosing is weight-based.

Icatibant Universal Farma is supplied as a clear, colorless solution in a pre-filled syringe ready for subcutaneous injection. The injection should be administered into the abdominal skin fold. Patients or caregivers should be trained in the correct injection technique by a healthcare professional before self-administering the medication at home.

Adults (18 years and older)

Children and Adolescents (2 to 17 years)

Elderly Patients

No dose adjustment is necessary for elderly patients (65 years and older). The same adult dosing recommendations apply. However, limited clinical data are available in elderly patients with HAE, as the condition typically presents earlier in life. Elderly patients may have comorbidities and concurrent medications that warrant careful clinical assessment before and during treatment, particularly regarding cardiovascular conditions and ACE inhibitor use.

Renal and Hepatic Impairment

No dose adjustment is required in patients with renal impairment or hepatic impairment. Icatibant is metabolized primarily by proteolytic enzymes rather than hepatic cytochrome P450 enzymes, and its renal excretion involves mostly inactive metabolites. However, no specific studies have been conducted in patients with severe renal or hepatic impairment.

Missed Dose

Icatibant is used on an as-needed basis for acute HAE attacks, so the concept of a "missed dose" does not apply in the traditional sense. The medication should be administered as soon as possible after the onset of an HAE attack. Delay in administration may result in progression of symptoms and longer time to resolution. Patients should always keep at least one pre-filled syringe available and accessible for immediate use when an attack occurs.

Overdose

In clinical studies, healthy volunteers received doses up to 3.2 mg/kg (approximately 8 times the standard therapeutic dose) without serious adverse effects. The most likely manifestation of overdose would be intensified injection site reactions, including redness, warmth, swelling, and itching. There is no specific antidote for icatibant. In the event of overdose, the patient should be treated symptomatically and monitored closely. If clinically indicated, standard supportive measures should be employed.

What Are the Side Effects of Icatibant Universal Farma?

The most common side effects of icatibant are injection site reactions, which occur in nearly all patients. These include redness, swelling, warmth, pain, itching, and bruising at the injection site. Most reactions are mild to moderate and resolve within a few hours.

Like all medicines, Icatibant Universal Farma can cause side effects, although not everybody gets them. Injection site reactions are by far the most frequently reported adverse effect and are considered an expected consequence of subcutaneous administration rather than a true adverse drug reaction. In clinical trials, injection site reactions were reported in approximately 97% of patients but were overwhelmingly mild or moderate in severity.

The side effects listed below are based on data from controlled clinical trials and post-marketing surveillance. If you experience any side effects not listed in this guide, or if any side effects become severe, contact your doctor or pharmacist immediately.

Injection site reactions typically develop within minutes of the injection and resolve within 1 to 4 hours. They tend to become less pronounced with repeated use. Applying a cold compress to the injection site after administration may help alleviate discomfort. Rotating the injection site within the abdominal area between doses can also help minimize local irritation.

In the pivotal clinical trials (FAST-1, FAST-2, and FAST-3), icatibant demonstrated a favorable safety profile compared to placebo and tranexamic acid. The overall incidence of serious adverse events was low and comparable between treatment groups. No significant hepatotoxicity, nephrotoxicity, or cardiovascular adverse effects were observed.

Post-marketing surveillance has not identified any new significant safety signals beyond those observed in clinical trials. However, as with any medication, rare and unexpected adverse effects may occur. Patients should report any unusual symptoms to their healthcare provider and to their national pharmacovigilance authority.

How Should You Store Icatibant Universal Farma?

Store Icatibant Universal Farma below 25°C in the original packaging to protect from light. Do not freeze. Keep out of the sight and reach of children. Do not use after the expiry date printed on the carton and syringe label.

Proper storage of icatibant is essential to maintain its efficacy and safety. The pre-filled syringes should be stored at or below 25°C (77°F). Do not refrigerate or freeze the solution, as freezing may damage the protein structure of the active substance and compromise its therapeutic effect. Store the syringes in the original carton to protect them from light.

The solution should be a clear, colorless liquid. Before each use, visually inspect the syringe. Do not use it if the solution appears cloudy, discolored, or contains visible particles. Do not use the syringe if the packaging seal has been broken or the syringe appears damaged.

Patients who travel should ensure they carry their icatibant supply in appropriate conditions. During air travel, icatibant should be kept in hand luggage and stored at ambient temperature. Avoid exposing the syringes to extreme temperatures, such as leaving them in a hot car or near heating sources. If you are travelling to regions with temperatures consistently above 25°C, consult your pharmacist about temporary storage options.

Keep this medicine out of the sight and reach of children. Do not use this medicine after the expiry date stated on the carton and pre-filled syringe label after "EXP." The expiry date refers to the last day of that month. Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. These measures will help protect the environment.

What Does Icatibant Universal Farma Contain?

Each pre-filled syringe contains 30 mg of icatibant (as icatibant acetate) in 3 mL of solution. The other ingredients are sodium chloride, glacial acetic acid, sodium hydroxide (for pH adjustment), and water for injections.

The active substance in Icatibant Universal Farma is icatibant, present as icatibant acetate. Icatibant is a synthetic decapeptide (a protein fragment composed of 10 amino acids) with the chemical sequence H-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg-OH. It has a molecular weight of approximately 1304 daltons. The acetate salt form ensures stability and solubility of the active substance in the aqueous solution.

The excipients (inactive ingredients) serve specific pharmaceutical functions. Sodium chloride provides isotonicity, making the injection solution compatible with body fluids and reducing pain upon injection. Glacial acetic acid and sodium hydroxide act as buffering agents, maintaining the pH of the solution at approximately 5.5 to ensure stability of the icatibant peptide and tolerability of the injection. Water for injections serves as the solvent.

The pre-filled syringe is made of Type I borosilicate glass fitted with a bromobutyl rubber plunger stopper and a needle cap containing dry natural rubber (a latex derivative). Patients with known latex allergy should be informed that the needle cap may cause allergic reactions, although the risk is considered low with dry natural rubber components.

Icatibant Universal Farma does not contain preservatives, which means each pre-filled syringe is for single use only. Any unused portion of the solution remaining in the syringe after injection should be discarded according to local pharmaceutical waste disposal regulations. The product does not contain gluten, lactose, or any animal-derived components other than the synthetic peptide itself.

Frequently Asked Questions About Icatibant Universal Farma