Dosing and uses of Kineret (anakinra)
Adult dosage forms and strengths
prefilled syringes
- 100mg/0.67mL
Rheumatoid Arthritis
Indicated to reduce signs and symptoms, and slow structural damage progression in moderate-to-severe active rheumatoid arthritis in patients 18 years or older who have failed 1 or more disease modifying antirheumatic drugs (DMARDs)
May use alone or in combo with DMARDs (not TNF-blocking agents)
100 mg SC qDay
Cryopyrin-Associated Periodic Syndromes (CAPS)
Indicated for treatment of Neonatal-Onset Multisystem Inflammatory Disease (NOMID), also known as chronic infantile neurologic cutaneous articular syndrome (CINCA)
1-2 mg/kg SC qDay (initially); may increase by 0.5-1 mg/kg increments to control active inflammation, not to exceed 8 mg/kg
Once daily administration recommended; may be split into twice daily
Renal Impairment
CrCl <30 mL/min or ESRD: Consider every other day administration of prescribed dose
Dosing Considerations
Measure WBCs before initiating, then qMonth x3 months, then quarterly up to 1 year
Still Disease (Orphan)
Orphan designation for Still disease including systmic juvenile isiopathic arithritis and adult-onset Still disease
Sponsor
- Swedish Orphan Biovitrum AB, SE-112; 75 Stockholm
Pediatric dosage forms and strengths
prefilled syringes
- 100mg/0.67mL
Rheumatoid Arthritis
Safety and efficacy not established
Cryopyrin-Associated Periodic Syndromes (CAPS)
Indicated for treatment of Neonatal-Onset Multisystem Inflammatory Disease (NOMID), also known as chronic infantile neurologic cutaneous articular syndrome (CINCA)
1-2 mg/kg SC qDay (initially); may increase by 0.5-1 mg/kg increments to control active inflammation, not to exceed 8 mg/kg
Once daily administration recommended; may be split into twice daily
Renal Impairment
CrCl <30 mL/min or ESRD: Consider every other day administration of prescribed dose
Dosing Considerations
Measure WBCs before initiating, then qMonth x3 months, then quarterly up to 1 year
Still Disease (Orphan)
Orphan designation for Still disease including systmic juvenile isiopathic arithritis and adult-onset Still disease
Sponsor
- Swedish Orphan Biovitrum AB, SE-112; 75 Stockholm
Kineret (anakinra) adverse (side) effects
>10%
Rheumatoid arthritis
- Injection-site reaction (71%)
- Headache (12%)
Neonatal-onset multisystem inflammatory disease
- Most common during first 6 months of treatment
- Injection site reaction (16.3%)
- Headache (14%)
- Vomiting (14%)
- Arthralgia (11.6%)
- Pyrexia (11.6%)
- Nasopharyngitis (11.6%)
1-10%
Nausea (7%)
Diarrhea (7%)
<1%
Neutropenia (0.3%) especially with TNF antagonists
Postmarketing Reports
Hepatobiliary disorders: Elevated transaminases, noninfectious hepatitis
Cholesterol elevation
Thrombocytopenia
Warnings
Contraindications
Hypersensitivity to anakinra, E. coli-derived proteins
Cautions
Renal impairment, chronic infections, immunosuppression, neutropenia
In rheumatoid arthritis, discontinue if severe infection develops and do not initiate with active infection
Use in combination with TNF blocker not recommended
Use caution in geriatric patients because of higher incidence of infection
Not for concomitant administration with live vaccines
Neutrophil counts should be assessed prior to initiating therapy, and while receiving treatment, monthly for 3 months, and thereafter quarterly for a period of up to 1 year
Hypersensitivity reactions, including angioedema and anaphylactic reactions reported
Pregnancy and lactation
Pregnancy category: B
Lactation: not known if excreted in breast milk, use caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Kineret (anakinra)
Mechanism of action
Interleukin-1 receptor antagonist (recombinant E. coli-derived product)
Blocks activity of IL-1 alpha and beta by competitively inhibiting IL-1 binding to the IL-1 type I receptor
IL-1 production is induced in response to inflammatory stimuli and mediates various physiologic responses including inflammatory and immunological responses
Proteolytic maturation and secretion of IL-1 beta has an important role in the systemic inflammation and manifestations of NOMId
Absorption
Bioavailability: 95%
Peak Plasma Time: 3-7 hr (RA)
Peak Plasma Concentration: 3,628 ng/mL (NOMID)
Elimination
Half-Life: 4-6 hr (RA); 5.7 hr (NOMID)
Hemodialysis or CAPD: <2.5%
Excretion: urine
Administration
SC Injection
Rotate injection site (thigh, abdomen, upper arm, upper buttocks)
CAPs
- Each syringe intended for single use (ie, new syringe must be used for each dose); discard unused portion after each dose
- Graduated syringe allows for doses between 20 and 100 mg
