Pill Identifier App

Efalizumab

Pronunciation: EF-a-LIZ-oo-mab
Class: Immunosuppressive

Trade Names:
Raptiva
- Injection, lyophilized powder for solution 150 mg (designed to deliver 125 mg per 1.25 mL)

Pharmacology

Inhibits binding of leukocyte function antigen-1 to intercellular adhesion molecule-1, thereby interfering with the adhesion of leukocytes to other cell types.

Pharmacokinetics

Absorption

Bioavailability following subcutaneous administration is 50%. Steady-state trough concentrations are about 9 mcg/mL.

Elimination

Mean steady-state Cl is 24 mL/kg/day; mean time to elimination following the last steady-state dose is 25 days.

Indications and Usage

Treatment of chronic moderate to severe plaque psoriasis in adult patients who are candidates for systemic therapy or phototherapy.

Contraindications

Standard considerations.

Dosage and Administration

Adults

Subcutaneous Single 0.7 mg/kg conditioning dose followed by weekly doses of 1 mg/kg (max single dose, 200 mg).

General Advice

  • For subcutaneous administration only. Not for intradermal, IM, or IV administration.
  • Reconstitute powder for injection following manufacturer's guidelines using the prefilled diluent syringe provided with medication.
  • Do not shake the vial during reconstitution. Do not reconstitute with diluents other than those supplied or add other medications to vial.
  • Do not administer if particulate matter, cloudiness, or discoloration is noted.
  • Rotate injection sites (thigh, buttocks, abdomen, upper arm). Give new injections at least 1 inch from previous site and never into areas where the skin is tender, bruised, red, or hard.

Storage/Stability

Reconstituted solution should be administered immediately after reconstitution but can be stored, if necessary, for up to 8 h at room temperature. Discard any unused solution or reconstituted solution that is not used within 8 h of dilution. Do not save for future administration. Store vials in refrigerator (36° to 46°F). Store in original carton until time of use. Protect from light.

Drug Interactions

Immunosuppressive agents

Do not use efalizumab with other immunosuppressive agents.

Live vaccines (eg, acellular, live, live-attenuated)

Do not use during efalizumab therapy.

Laboratory Test Interactions

Increased lymphocyte counts related to pharmacologic action are frequently observed.

Adverse Reactions

CNS

Headache (32%); chronic inflammatory demyelinating polyneuropathy, facial palsy, Guillain-Barré syndrome, transverse myelitis, (postmarketing).

Dermatologic

Acne (4%); psoriasis (1% or 2% more than placebo); urticaria (1%); photosensitivity, toxic epidermal necrolysis (postmarketing).

Hematologic-Lymphatic

Lymphoma (postmarketing).

Hypersensitivity

Hypersensitivity (8%).

GI

Nausea (11%).

Lab Tests

lymphocytosis (40%); leukocytosis (26%); elevated alkaline phosphatase (4%); elevated LFTs.

Musculoskeletal

Myalgia (8%); arthralgia (1% or 2% more than placebo); myositis (postmarketing).

Respiratory

Eosinophilic pneumonitis (postmarketing).

Miscellaneous

Infection (29%); chills (13%); pain (10%); fever, flu-like syndrome (7%); antibodies to efalizumab (6%); back pain (4%); malignancies (2%); asthenia, peripheral edema (1% or 2% more than placebo); serious bacterial, viral, fungal, and opportunistic infections; worsening of infections (postmarketing).

Precautions

Warnings

Infections

Infections, including serious infections leading to hospitalization or death, may occur. Use with caution in patients with a chronic infection or history of recurrent infections.

Leukoencephalopathy

Progressive multifocal leukoencephalopathy (PML) resulting from virus infection may occur. Consider PML in any patient with new-onset neurologic manifestations.


Monitor

Monitor platelet counts prior to and periodically during treatment.

Allergic reaction

Monitor patient for signs and symptoms of anaphylactic or serious allergic reactions. Be prepared to treat appropriately if noted.


Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Use with caution because of increased incidence of infections in elderly patients.

Arthritis events

Infrequent new-onset or recurrent severe arthritis events, including psoriatic arthritis, have been reported in clinical trials and postmarketing experience. These events may occur during or following treatment.

First-dose reaction

The conditioning dose is recommended to reduce the incidence and severity of reactions associated with initiation of therapy (eg, headache, fever, nausea, vomiting).

Hemolytic anemia

Hemolytic anemia, some serious, has been reported 4 to 6 mo after starting treatment.

Immunizations

Psoriatic patients should receive all age-appropriate immunizations prior to the start of treatment.

Infections

The risk of infection and reactivation of latent, chronic infections may be increased. Ensure that patient does not have an active infection prior to starting therapy. Monitor patient for signs and symptoms of infection. Be prepared to discontinue efalizumab if infection is determined to be serious.

Malignancies

Because many immunosuppressants have the potential to increase the risk of malignancies, use with caution in patients at high risk for malignancy or history of malignancy.

Neurologic events

Guillain-Barré syndrome, chronic inflammatory demyelinating polyneuropathy, facial palsy, and transverse myelitis have been reported during postmarketing experience.

Thrombocytopenia

Thrombocytopenia may occur. Ensure that platelet counts are determined before starting therapy and periodically during treatment. Be prepared to discontinue efalizumab if thrombocytopenia develops or signs or symptoms of thrombocytopenia (eg, petechiae, easy bruising or bleeding) are noted.

Worsening of psoriasis

May occur during or after discontinuation of efalizumab.

Overdosage

Symptoms

Vomiting.

Patient Information

  • Advise patient to read the patient package insert before starting therapy and with each refill.
  • Ensure that the patient or caregiver understands how to store, prepare, and administer the dose, and dispose of used equipment and supplies if administering at home. The first injection should be performed under the supervision of a qualified health care provider.
  • Advise patient that if a dose is missed, to contact health care provider to find out when the next dose should be taken and the schedule to follow after that.
  • Advise patient to notify health care provider if psoriasis is not improving or appears to be worsening.
  • Instruct patient to continue taking other psoriasis medications as prescribed by health care provider.
  • Advise patient to report any of the following to health care provider: easy bleeding from gums, fever or other signs of infection, hives, intolerable injection-site reactions, itching, new neurological signs or symptoms, rash, small purple spots under the skin, sore throat, unexplained bruising, unexplained shortness of breath or difficulty breathing.
  • Advise women to notify health care provider if they become pregnant while on treatment or within 6 wk after stopping therapy.

Copyright © 2009 Wolters Kluwer Health.

Hide
(web2)