Anakinra: Indication, Dosage, Side Effect, Precaution

This information is not country-specific. Please refer to the Indonesia prescribing information.

Generic Medicine Info

Indications and Dosage

Subcutaneous
Rheumatoid arthritis

Adult: 100 mg daily, administered at approx the same time each day. May be used w/ methotrexate.

Subcutaneous
Cryopyrin associated periodic syndromes

Adult: Initially, 1-2 mg/kg daily. Severe: Adjust dose in increments of 0.5-1 mg/kg after 1-2 mth if necessary. Maintenance: 3-4 mg/kg daily. Max: 8 mg/kg daily.
Child: ≥8 mth ≥10 kg: Same as adult dose.

Renal Impairment

CrCl (mL/min)	Dosage
<30	Contraindicated.

Contraindications

Hypersensitivity to E. coli-derived proteins or anakinra. Neutropenia (absolute neutrophil count <1.5 x 10⁹/L). Severe renal impairment (CrCl <30 mL/min).

Special Precautions

Patient w/ active infections, including chronic or localised infections, history of recurrent infections or w/ underlying conditions that may predispose to infections, asthma. Moderate renal (CrCl 30-50 mL/min) and severe hepatic impairment. Pregnancy and lactation.

Adverse Reactions

Infection (e.g. upper resp tract infection, sinus infection), mild to moderate inj site reactions w/ symptoms of erythema, bruising, swelling and pain, headache, nausea, diarrhoea, abdominal pain, elevated transaminases, non-infectious hepatitis. Rarely, allergic reactions e.g. rashes.

Monitoring Parameters

Monitor neutrophil counts before initiating treatment, mthly during the 1st 6 mth, and quarterly thereafter.

Drug Interactions

Enhanced adverse effects of live vaccines. Co-admin w/ etanercept or other tumour necrosis factor (TNF) inhibitors may induce serious infection and neutropenia.

Action

Description:
Mechanism of Action: Anakinra is a recombinant receptor antagonist of interleukin-1 (IL-1). It competitively inhibits IL-1 binding to interleukin-1 type I receptor (IL-1RI) and hence blocks the activity of endogenous IL-1α and IL-1β. IL-1 is involved in inflammatory and immunological responses, cartilage degradation (loss of proteoglycans), stimulates bone resorption and its production is induced by inflammatory stimuli.
Pharmacokinetics:
Absorption: Absolute bioavailability: 95%. Time to peak plasma concentration: 3-7 hr.
Excretion: Excreted mainly in the urine. Terminal half-life: Approx 4-6 hr.

Chemical Structure

Storage

Store between 2-8°C. Do not freeze. Protect from light.

MIMS Class

Disease-Modifying Anti-Rheumatic Drugs (DMARDs)

ATC Classification

L04AC03 - anakinra ; Belongs to the class of interleukin inhibitors. Used as immunosuppressants.

References

Anon. Anakinra. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/12/2015.

Buckingham R (ed). Anakinra. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/12/2015.

Kineret Injection Solution (Swedish Orphan Biovitrum AB). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 01/12/2015.

McEvoy GK, Snow EK, Miller J et al (eds). Anakinra. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 01/12/2015.

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