Ecallantide

Pronunciation: ee-KAL-lan-tide
Class: Kallikrein inhibitor

Trade Names

Kalbitor
- Injection, solution 10 mg/mL

Pharmacology

Directly inhibits plasma kallikrein and blocks the conversion of high molecular weight kininogen to bradykinin, which is thought to relieve symptoms of localized swelling, inflammation, and pain in hereditary angioedema.

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Pharmacokinetics

Absorption

C _max is 586 ng /mL. T _max is 2 to 3 h. Mean AUC is 3,017 ng•h/mL.

Distribution

Vd is 26.4 L.

Elimination

Plasma Cl is 153 mL/min. Elimination half-life is 2 h. Renal elimination in the urine has been demonstrated.

Special Populations

Renal Function Impairment

Pharmacokinetic data are not available.

Hepatic Function Impairment

Pharmacokinetic data are not available.

Elderly

Age was not found to significantly affect exposure.

Gender

Gender was not found to significantly affect exposure.

Indications and Usage

Treatment of acute attacks of hereditary angioedema.

Contraindications

Standard considerations.

Dosage and Administration

Adults and children 16 yr of age and older

Subcutaneous 30 mg in three 10 mg injections. An additional 30 mg may be administered within a 24-h period if the attack persists.

General Advice

• Inject subcutaneously into the skin of the abdomen, thigh, or upper arm.
• The injection site for each of the 3 injections may be in the same or different anatomic locations. There is no need for site rotation.
• Separate injection sites by at least 2 inches and away from anatomical site of attack.

Storage/Stability

Store at 36° to 46°F. Store vials removed from refrigeration below 86°F and use within 14 days or return to refrigeration until use. Protect from light.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache (16%); fatigue (12%).

Dermatologic

Pruritus (5%).

EENT

Nasopharyngitis (6%).

GI

Nausea (13%); diarrhea (11%); vomiting (6%); upper abdominal pain (5%).

Hypersensitivity

Anaphylaxis (4%).

Local

Injection-site reactions, including erythema, irritation, local bruising, pain, pruritus, and urticaria (7%).

Respiratory

Upper respiratory tract infections (8%).

Miscellaneous

Pyrexia (5%).

Precautions

Warnings Anaphylaxis has been reported after administration. Ensure that ecallantide is only administered by a health care provider with appropriate medical support to manage anaphylaxis and hereditary angioedema. Be aware of the similarities between hypersensitivity reactions and hereditary angioedema and monitor patients closely. Do not administer to patients with known hypersensitivity to ecallantide.

Monitor Observe patients for an appropriate period of time after administration, taking into account the time to onset of anaphylaxis seen in clinical trials.

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 16 yr of age.

Elderly

In general, exercise caution in dose selection, usually starting at the low end of the dosing range, reflecting greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Hypersensitivity

Severe hypersensitivity reactions, including anaphylaxis, have occurred. These reactions occurred within the first hour after dosing.

Immunogenicity

Patients have developed antibodies to ecallantide; long-term effects are unknown.

Overdosage

Symptoms

Overdosage has not been reported.

Patient Information

• Advise patients that ecallantide may cause anaphylaxis and other hypersensitivity reactions. Ensure that ecallantide is administered by a health care provider with appropriate medical support to manage anaphylaxis and hereditary angioedema.
• Instruct patients with known clinical hypersensitivity to ecallantide not to receive additional doses.
• Advise patients to consult the Medication Guide for additional information regarding the risk of anaphylaxis and other hypersensitivity reactions.

Copyright © 2009 Wolters Kluwer Health.