Icatibant (icatibant acetate)
Bradykinin B2 Receptor Antagonists (Acute) Subcutaneous Syringe (Ml)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Icatibant acetate, a synthetic decapeptide similar in structure to bradykinin, is a selective bradykinin type 2 (B2) receptor antagonist.
Icatibant, a synthetic decapeptide similar in structure to bradykinin, is a selective, competitive bradykinin type 2 (B2) receptor antagonist. Hereditary angioedema (HAE) is characterized by low plasma concentrations of functionally active complement 1 (C1)-esterase inhibitor; the deficiency in C1-esterase inhibitor results in unrestrained activity of plasma kallikrein and an elevation in bradykinin levels, which leads to increased vascular permeability and angioedema. Binding of bradykinin to the bradykinin B2 receptor on endothelial cells causes vasodilation and acute pain.
Icatibant is a potent bradykinin B2 receptor antagonist with similar affinity for the B2 receptor as bradykinin. Competitive inhibition of the bradykinin B2 receptor by icatibant reduces the vasodilatory effects of excess bradykinin.
Icatibant is principally metabolized by proteolytic enzymes to inactive metabolites that are mainly excreted in urine. Following subcutaneous injection, absorption is rapid with peak plasma concentrations achieved in 30 minutes. The duration of action of subcutaneous icatibant is not dose dependent; effects of the drug against a bradykinin challenge are expected to be present for at least 6 hours after a dose based on exposure-response analysis.
More severe injection site reactions were observed with higher dosages of icatibant in a phase 2 study. Dose- and time-dependent inhibition of development of bradykinin-induced effects (e.g., hypotension, vasodilation, reflex tachycardia) have been observed in healthy individuals receiving IV+ icatibant.
The absolute bioavailability of icatibant following a 30-mg subcutaneous dose is approximately 97%. In a phase 1 trial, the bioavailability of subcutaneous and IV+ icatibant in healthy individuals was similar. Reduced clearance of and increased systemic exposure to icatibant have been observed in patients with low body weight and in geriatric patients; however, the manufacturer does not recommend dosage adjustments in these individuals.
The mean terminal elimination half-life of icatibant is approximately 1.4 hours.
In controlled trials in which patients received repeated treatments with icatibant, 4 patients tested positive for anti-icatibant antibodies; however, results of subsequent tests in 3 of these patients were negative. No hypersensitivity or anaphylactic reactions to icatibant have been reported to date. An association between the presence of anti-icatibant antibodies and efficacy has not been observed.
USES: Icatibant is used to treat sudden attacks of a certain immune system condition passed down through families called hereditary angioedema (HAE). Although this medication is not a cure for HAE, icatibant may lessen the symptoms of an attack such as rapid swelling and pain of the hands, arms, feet, legs, face, tongue, and upper airway. When attacks involve the stomach/intestines, symptoms may include abdominal pain/cramps, diarrhea, constipation, or vomiting.
Attacks may happen at any time. However, stress, injury, or illness may trigger attacks in some people. Icatibant works by blocking the action of a natural substance in the body called bradykinin.
Bradykinin is thought to cause the symptoms of an HAE attack.
Generic name: icatibant acetate
Pronunciation: (eye-KAT-i-bant)
Drug class: Bradykinin B2 Receptor Antagonists (Acute)
Therapeutic class: Cardiovascular Therapy Agents
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Icatibant
Indications
The following indications are listed for Icatibant:
- Hereditary Angioedema
Also known as: Hereditary Angioneurotic Edema.
Dosing
No dosing information is available for this tab.
Icatibant is administered by subcutaneous injection.
The 25-gauge needle supplied by the manufacturer should be attached to the syringe hub and tightened securely; no other needle should be used. Icatibant should be injected subcutaneously over at least 30 seconds into the abdominal area, about 5-10 cm (2-4 inches) below the umbilicus and at least 5 cm (2 inches) from scars.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Icatibant 30 Mg/3 Ml Syringe | Maintenance | Inject 3 milliliters (30 mg) by subcutaneous route once, may repeat every 6 hours as needed; do not exceed 3 doses (90 mg) in 24 hours. |
| Drug label | Dosing type | Instructions |
|---|---|---|
| Icatibant 30 Mg/3 Ml Syringe | Maintenance | Inject 3 milliliters (30 mg) by subcutaneous route once, may repeat every 6 hours as needed; do not exceed 3 doses (90 mg) in 24 hours. |
Drug interactions
Icatibant is not metabolized by cytochrome P-450 (CYP) isoenzymes. No formal drug interaction studies have been performed to date; however, in vitro studies indicate that the drug does not inhibit or induce CYP isoenzymes.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
The manufacturer states that there are no known contraindications to the use of icatibant.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
- No disease contraindications
Adverse reactions
Adverse effects occurring in more than 1% of patients receiving icatibant and more frequently than in those receiving placebo include injection site reactions, pyrexia, elevated serum aminotransferase concentrations, rash, and dizziness.
Injection site reactions were reported in 97% of patients in clinical trials following subcutaneous injection of icatibant. Injection site reactions include bruising, hematoma, burning, erythema, hypoesthesia, irritation, numbness, edema, pain, pressure sensation, pruritus, swelling, urticaria, and warmth.
Less Frequent
- Abnormal hepatic function tests
- Hypersensitivity drug reaction
Rare or Very Rare
- Cardiac arrhythmia
- Increased alanine transaminase
- Increased aspartate transaminase
- Laryngeal edema
More Frequent
- Injection site erythema
- Injection site sequelae
Less Frequent
- Abdominal distension
- Diarrhea
- Dizziness
- Fatigue
- Fever
- Headache disorder
- Nasal congestion
- Nausea
- Pharyngitis
- Pruritus of skin
- Sinusitis
- Skin rash
- Urinary tract infection
- Xerostomia
Rare or Very Rare
- Non-cardiac chest pain
- Urticaria
Precautions
No enhanced messaging available.
Safety and efficacy of icatibant in patients younger than 18 years of age have not been established. Subcutaneous administration of icatibant to young rats during the juvenile period of development delayed sexual maturation and also impaired fertility and reproductive performance in male rats; no effects were observed in female rats.
Available data on icatibant use during pregnancy have not established an association between the drug and major birth defects, miscarriage, or adverse maternal or fetal outcomes.
In animal reproduction studies, subcutaneous administration of icatibant during the period of organogenesis did not cause structural abnormalities in rats or rabbits. Premature birth and abortion were observed in rabbits at doses approximately 0.025 times the maximum recommended human dose (MRHD) and higher, and decreased embryofetal survival was observed in rabbits at a subcutaneous dose that was 13 times the MRHD. In a pre andpost-natal development study in rats, delayed parturition was observed at subcutaneous doses 0.5 times the MRHD and higher, whichresulted in deaths of dams at doses 2 times the MRHD and higher. Fetal death and early pup deaths were observed with doses 2 times theMRHD.
There are no data on the presence of icatibant in human milk, the effects on the breastfed infant, or the effects on milk production. Icatibant and its M2 metabolite are distributed into milk in rats; when a drug is present in animal milk, it is likely to also be present in human milk. However, systemic absorption of icatibant in infants is not expected after oralexposure through breast milk. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for icatibant and any potential adverse effects on the breastfed child from the drug or from the underlying maternal condition.
Clinical studies of icatibant did not include sufficient numbers of patients 65 years of age and older to determine whether geriatric patients respond differently than younger patients. Other clinical experience has not revealed age-related differences in response and safety. Systemic exposure (area under the concentration-time curve (AUC)) and peak plasma concentration following a single 30-mg dose of icatibant were increased by approximately 100 and 12-14%, respectively, in geriatric patients compared with younger patients.
ICD codes
| Code | Type | Description |
|---|---|---|
| Hereditary angioedema | ||
| D84.1 | ICD10CM | Defects in the complement system |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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