DrugindexOnline^{2nd edition}

Pronouncation: (an-a-KIN-ra)
Class: Immunomodulator

Trade Names:
Kineret
- Solution 100 mg per 0.67 mL

Mechanism of Action

Pharmacology

Blocks the biologic activity of interleukin-1 (IL-1) by competitively inhibiting IL-1 binding to IL-1 type I receptor, which is expressed in a wide variety of organs and tissues.

Pharmacokinetics

Absorption

Bioavailability is 95%; T _max is 3 to 7 h.

Elimination

The t _½ is 4 to 6 h.

Special Populations

Renal Function Impairment

Mean plasma Cl decreased 70% to 75% in those with Ccr less than 30 mL/min.

Indications and Usage

Reduction in signs and symptoms, and slowing the progression of structural damage in moderately to severely active rheumatoid arthritis in patients who have failed at least 1 disease-modifying antirheumatic drug.

Contraindications

Hypersensitivity to Escherichia coli -derived proteins, anakinra, or any component of product.

Dosage and Administration

Adults

Subcutaneous 100 mg/day.

Renal Function Impairment

Subcutaneous 100 mg every other day for severe renal function impairment (Ccr less than 30 mL/min).

General Advice

• Rotate injection sites (eg, thigh, abdomen, upper arm). Give new injection at least 1 inch from old site and never into areas where the skin is tender, bruised, red, or hard.
• Do not use prefilled syringe if particulate matter, cloudiness, or discoloration are noted.
• Disease-modifying antirheumatic drugs (except etanercept), glucocorticoids, salicylates, NSAIDs, and analgesics may be continued during treatment with anakinra.
• Discard any unused portion. Do not save unused solution for later administration.

Storage/Stability

Store prefilled syringes in refrigerator (36° to 46°F). Do not freeze or shake. Protect from light.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache (12%).

EENT

Sinusitis (7%).

GI

Nausea (8%); diarrhea (7%); abdominal pain (5%).

Hematologic

Neutropenia.

Local

Injection-site reaction (71%).

Respiratory

Upper respiratory tract infection (14%).

Miscellaneous

Worsening of rheumatoid arthritis (19%); arthralgia, flu-like symptoms (6%); hypersensitivity, serious infections (eg, cellulitis, pneumonia, bone and joint [3%]).

Precautions

Monitor Disease state activity Document baseline disease state activity (eg, number of tender or swollen joints, pain, disability). Reassess periodically to document response to therapy. Neutrophil count Ensure that neutrophil count is assessed prior to starting therapy, then monthly for 3 mo, and thereafter quarterly for a period of up to 1 yr.

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Use with caution because of higher rate of infection in this population.

Renal Function

Because anakinra is substantially excreted by the kidneys, risk of toxicity is increased in patients with renal function impairment.

Hematologic

Decreased neutrophil count may occur.

Infection

Serious infections may occur. Monitor patient for signs and symptoms of infection (eg, persistent fever, sore throat, cellulitis). Immediately report to health care provider if noted. Be prepared to discontinue therapy if a serious infection develops or is suspected.

Vaccinations

Do not give live vaccines concomitantly.

Patient Information

• If patient or caregiver is administering at home, provide the Information for Patients and Caregivers insert. Ensure that the patient or caregiver understands how to store, prepare, and administer the dose, and how to dispose of used equipment and supplies. Perform the first injection under the supervision of a qualified health professional.
• Advise patient to administer daily at about the same time.
• Caution patient to discard any unused portions and not to save unused drug for later administration.
• Advise patient to continue other arthritis medications as recommended by health care provider.
• Advise patient or caregiver that beneficial effects develop slowly and may take up to 12 wk to occur.
• Advise patient to immediately report any of the following to health care provider: fever or other signs of infection, sore throat, unusual bruising or bleeding, rash, hives, sudden shortness of breath.
• Advise patient to report intolerable injection site reactions or unusual symptoms to health care provider.