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Anakinra


General


Pronunciation

(an a KIN ra)


Brand Names: U.S.

  • Kineret

Indications


Use: Labeled Indications

Neonatal-onset multisystem inflammatory disease: Treatment of neonatal-onset multisystem inflammatory disease (NOMID).

Rheumatoid arthritis: Reduction in signs and symptoms and slowing the progression of structural damage of moderately to severely active rheumatoid arthritis (RA) in patients 18 years and older who have failed 1 or more disease-modifying antirheumatic drugs (DMARDs).


Contraindications


Hypersensitivity to E. coli-derived proteins, anakinra, or any component of the formulation


Dosing and Administration


Dosing: Adult

Neonatal-onset multisystem inflammatory disease (NOMID): SubQ: Initial: 1 to 2 mg/kg daily in 1 to 2 divided doses; adjust dose in 0.5 to 1 mg/kg increments as needed; usual maintenance dose: 3 to 4 mg/kg daily (maximum: 8 mg/kg daily). Note: Once-daily administration is preferred; however, the dose may also be divided and administered twice daily.

Rheumatoid arthritis (RA): SubQ: 100 mg once daily (administer at approximately the same time each day)


Dosing: Geriatric

Refer to adult dosing.


Dosing: Pediatric

Neonatal-onset multisystem inflammatory disease (NOMID): Infants, Children, and Adolescents: SubQ: Refer to adult dosing.

Juvenile idiopathic arthritis, systemic (off-label use): Children and Adolescents: SubQ: Initial: 1 to 2 mg/kg once daily; maximum initial dose: 100 mg; if no response after 1 to 2 weeks, may titrate up to 4 mg/kg once daily (maximum: 200 mg/day) (Dewitt 2012; Hedrich 2012; Lequerre 2008; Nigrovi 2011; Quartier 2011; Ringold 2013).


Dosing: Renal Impairment

CrCl ≥30 mL/minute: No dosage adjustment necessary.

CrCl <30 mL/minute or end-stage renal disease (ESRD): Consider administering the prescribed dose every other day.


Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer 's labeling (has not been studied).


Administration

SubQ: Allow solution to warm to room temperature prior to use (30 minutes). Inject into outer area of upper arms, abdomen (do not use within 2 inches of belly button), front of middle thighs, or upper outer buttocks. Rotate injection sites; do not administer into tender, swollen, bruised, red, or hard skin or skin with scars or stretch marks.


Storage

Store in refrigerator at 2 ‚ °C to 8 ‚ °C (36 ‚ °F to 46 ‚ °F); do not freeze. Do not shake. Protect from light. Discard any unused portion.


Dosage Forms/Strengths


Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Prefilled Syringe, Subcutaneous [preservative free]:

Kineret: 100 mg/0.67 mL (0.67 mL) [contains disodium edta, polysorbate 80]


Drug Interactions

Abatacept: Anakinra may enhance the adverse/toxic effect of Abatacept. Avoid combination

Anti-TNF Agents: May enhance the adverse/toxic effect of Anakinra. An increased risk of serious infection during concomitant use has been reported. Avoid combination

BCG (Intravesical): Immunosuppressants may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

Canakinumab: Interleukin-1 Receptor Antagonist may enhance the adverse/toxic effect of Canakinumab. Whether such a combination will also alter the therapeutic response to one or both agents is unclear. Avoid combination

Coccidioides immitis Skin Test: Immunosuppressants may diminish the diagnostic effect of Coccidioides immitis Skin Test. Monitor therapy

Denosumab: May enhance the adverse/toxic effect of Immunosuppressants. Specifically, the risk for serious infections may be increased. Monitor therapy

Echinacea: May diminish the therapeutic effect of Immunosuppressants. Consider therapy modification

Fingolimod: Immunosuppressants may enhance the immunosuppressive effect of Fingolimod. Management: Avoid the concomitant use of fingolimod and other immunosuppressants when possible. If combined, monitor patients closely for additive immunosuppressant effects (eg, infections). Consider therapy modification

Leflunomide: Immunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Management: Consider not using a leflunomide loading dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and another immunosuppressant should be monitored for bone marrow suppression at least monthly. Consider therapy modification

Natalizumab: Immunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased. Avoid combination

Nivolumab: Immunosuppressants may diminish the therapeutic effect of Nivolumab. Consider therapy modification

Pimecrolimus: May enhance the adverse/toxic effect of Immunosuppressants. Avoid combination

Roflumilast: May enhance the immunosuppressive effect of Immunosuppressants. Consider therapy modification

Sipuleucel-T: Immunosuppressants may diminish the therapeutic effect of Sipuleucel-T. Monitor therapy

Tacrolimus (Topical): May enhance the adverse/toxic effect of Immunosuppressants. Avoid combination

Tofacitinib: Anakinra may enhance the adverse/toxic effect of Tofacitinib. Avoid combination

Trastuzumab: May enhance the neutropenic effect of Immunosuppressants. Monitor therapy

Vaccines (Inactivated): Immunosuppressants may diminish the therapeutic effect of Vaccines (Inactivated). Management: Vaccine efficacy may be reduced. Complete all age-appropriate vaccinations at least 2 weeks prior to starting an immunosuppressant. If vaccinated during immunosuppressant therapy, revaccinate at least 3 months after immunosuppressant discontinuation. Consider therapy modification

Vaccines (Live): Immunosuppressants may enhance the adverse/toxic effect of Vaccines (Live). Immunosuppressants may diminish the therapeutic effect of Vaccines (Live). Management: Avoid use of live organism vaccines with immunosuppressants; live-attenuated vaccines should not be given for at least 3 months after immunosuppressants. Avoid combination


Monitoring Parameters

CBC with differential (baseline, then monthly for 3 months, then every 3 months for a period up to 1 year); TB test (baseline); serum creatinine; signs/symptoms of infection


Adverse Reactions


>10%:

Central nervous system: Headache (12% to 14%)

Infection: Infection (39%; serious infection 2% to 3%)

Local: Injection site reaction (RA: ≤71%; mild: 73%; moderate: 24%; severe: 3%; NOMID: 16%)

Neuromuscular & skeletal: Arthralgia (6% to 12%)

Respiratory: Nasopharyngitis (12%)

Miscellaneous: Fever (12%)

1% to 10%:

Gastrointestinal: Nausea (8%), diarrhea (7%)

Hematologic & oncologic: Neutropenia (5% to 8%)

<1% (Limited to important or life-threatening): Bacterial pneumonia, cellulitis, hepatitis (noninfectious), hypersensitivity reaction (including anaphylaxis, angioedema, pruritus, skin rash, urticaria), increased serum transaminases, leukopenia, metastases (malignant lymphoma, malignant melanoma), opportunistic infection, pulmonary fibrosis, thrombocytopenia


Warnings/Precautions


Special Populations: Renal Function Impairment

Mean plasma clearance in patients with mild (CrCl 50 to 80 mL/minute), moderate (CrCl 30 to 49 mL/minute), severe (CrCl <30 mL/minute), and end-stage renal disease (ESRD) was decreased by 16%, 50%, 70%, and 75%, respectively. Less than 2.5% of the dose is removed by hemodialysis or CAPD.


Warnings/Precautions

Concerns related to adverse effects:

- Anaphylaxis/hypersensitivity reactions: Hypersensitivity reactions, including anaphylactic reactions and angioedema, have been reported; discontinue use if severe hypersensitivity occurs; medications for the treatment of hypersensitivity reactions should be available for immediate use.

- Infections: Associated with an increased risk of serious infections in rheumatoid arthritis studies. Anakinra should not be initiated in patients with an active infection. If a patient receiving anakinra for rheumatoid arthritis develops a serious infection, therapy should be discontinued; if a patient receiving anakinra for neonatal-onset multisystem inflammatory disease (NOMID) develops a serious infection, the risk of a NOMID flare should be weighed against the risks associated with continued treatment. Safety and efficacy have not been evaluated in immunosuppressed patients or patients with chronic infections; the impact on active or chronic infections has not been determined. Immunosuppressive therapy (including anakinra) may lead to reactivation of latent tuberculosis or other atypical or opportunistic infections; test patients for latent TB prior to initiation, and treat latent TB infection prior to use.

- Injection site reactions: Injection site reactions commonly occur (within first 4 weeks of therapy) and are generally mild with a duration of 14 to 28 days.

- Malignancy: May affect defenses against malignancies; impact on the development and course of malignancies is not fully defined. As compared to the general population, an increased risk of lymphoma has been noted in clinical trials; however, rheumatoid arthritis has been previously associated with an increased rate of lymphoma.

- Neutropenia: A decrease in neutrophil count may occur during treatment. Assess neutrophil count at baseline, monthly for 3 months, then every 3 months for up to 1 year. In a limited number of patients with NOMID, neutropenia resolved over time with continued anakinra administration.

Disease-related concerns:

- Asthma: Use with caution in patients with asthma; may have increased risk of serious infection.

- Renal impairment: Use caution in patients with renal impairment; extended dosing intervals (every other day) are recommended for severe renal insufficiency (CrCl <30 mL/minute) and ESRD.

Concurrent drug therapy issues:

- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

- Elderly: Use caution due to the potential higher risk for infections.

Dosage form specific issues:

- Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade 1986; CDC 1984). See manufacturer 's labeling.

Other warnings/precautions:

- Immunizations: Patients should be brought up to date with all immunizations before initiating therapy; live vaccines should not be given concurrently. There is no data available concerning the effects of therapy on vaccination or secondary transmission of live vaccines in patients receiving therapy.


Pregnancy Risk Factor

B


Pregnancy Considerations

Adverse events have not been observed in animal reproduction studies.

Information related to the use of anakinra during pregnancy is limited (Makol 2011; Ostensen 2011). Specific guidelines for use in pregnancy are not available (Saag [ACR] 2008); use should not be continued during pregnancy until more data is available (Makol 2011; Ostensen 2011).

Women exposed to anakinra during pregnancy may contact the Organization of Teratology Information Services (OTIS), Rheumatoid Arthritis and Pregnancy Study at 1-877-311-8972.


Actions


Pharmacology

Antagonist of the interleukin-1 (IL-1) receptor. Endogenous IL-1 is induced by inflammatory stimuli and mediates a variety of immunological responses, including degradation of cartilage (loss of proteoglycans) and stimulation of bone resorption.


Time to Peak

SubQ: 3 to 7 hours


Half-Life Elimination

Terminal: 4 to 6 hours; Severe renal impairment (CrCl <30 mL/minute): ~7 hours; ESRD: 9.7 hours (Yang 2003)


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Patient may experience headache, nausea, vomiting, diarrhea, joint pain, pharyngitis, rhinorrhea, rhinitis, or abdominal pain. Have patient report immediately to prescriber signs of infection, bruising, bleeding, severe injection site irritation, severe dizziness, passing out, tachycardia, arrhythmia, or sweating a lot (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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