Anakinra is a biopharmaceutical drug used to treat rheumatoid arthritis It is a recombinant and slightly modified version of the human interleukin 1 receptor antagonist protein. It is a recombinant, nonglycosylated human interleukin-1 receptor antagonist (IL-1Ra). The difference between anakinra and the native human IL-1Ra is that anakinra has an extra methionine residue at the amino terminus. It is manufactured by using the E. coli expression system.

Mechanism of action of Anakinra

Anakinra binds competitively to the Interleukin-1 type I receptor (IL-1RI), thereby inhibiting the action of elevated levels IL-1 which normally can lead to cartilage degradation and bone resorption. Used to treat rheumatoid arthritis, Anakinra blocks the biologic activity of IL-1 by competitively inhibiting IL-1 binding to the interleukin-1 type I receptor (IL-1RI), which is expressed in a wide variety of tissues and organs. IL-1 production is induced in response to inflammatory stimuli and mediates various physiologic responses including inflammatory and immunological responses. Patients with rheumatoid arthritis have elevated levels of IL-1. The levels of the naturally occurring IL-1Ra in synovium and synovial fluid from rheumatoid arthritis (RA) patients are not sufficient to compete with the elevated amount of locally produced IL-1. Increasing the levels of IL-1Ra by artificial means reduces the negative effects (cartilage degradation, bone resorption) of IL-1.

Indications of Anakinra

• Juvenile idiopathic arthritis
• Neonatal-onset multisystemic inflammatory disease
• Moderate rheumatoid arthritis
• Recurrent pericarditis
• Severe rheumatoid arthritis
• Cryopyrin-associated periodic syndromes
• Rheumatoid arthritis
• Schnitzler syndrome

Contra-Indications of Anakinra

• Tuberculosis
• Infection caused by Blastomyces dermatitidis Fungus
• Opportunistic fungal infection
• Pneumonia 
• Severe infection
• Infection that lasts a long time
• Malignant melanoma
• Leukemia
• Diabetes that is not under control
• Reduction in the body’s resistance to infection
• The acquired decrease of all cells in the blood
• Low blood counts due to bone marrow failure
• Decreased neutrophils a type of white blood cell
• Multiple sclerosis
• Demyelinating Disease
• Sudden blindness and pain Upon moving the eye
• Heart failure
• Decreased Blood Platelets
• Decreased white blood cells
• Low Level of Granulocytes in the Blood
• Chronic heart failure
• Pneumonia caused by legionella pneumophila bacteria
• Hardening of the liver caused by alcohol
• Liver inflammation caused by the body’s own immune response
• Seizures
• Reactivated tuberculosis
• Sepsis syndrome
• Malignant lymphoma
• Relapse of hepatitis B infection symptoms
• Hepatitis B
• Hepatosplenic T-cell lymphoma

Dosage of Anakinra

Strengths: 100 mg/0.67 mL

Rheumatoid Arthritis

• 100 mg subcutaneously once daily

Cryopyrin-Associated Periodic Syndrome

• Initial dose: 1 to 2 mg/kg subcutaneously daily
• Maximum dose: 8 mg/kg subcutaneously daily

Side Effects of Anakinra

The most common

• Nausea and vomiting
• Severe stomach ache
• multiple sclerosis,
• Severe diarrhea
• Vaginal thrush
• Skin rash redness or itching, pain, or swelling at the injection site
• Headache
• chest pain
• constipation
• cough
• diarrhea or loose stools
• difficulty with breathing
• dizziness
• heartburn
• muscle pain

More common

• Abdominal or stomach pain, discomfort, or tenderness
• chills or fever
• difficulty with moving
• headache, severe and throbbing
• joint or back pain
• Loss of energy or weakness
• pain or burning in the throat
• runny or stuffy nose
• muscle aching or cramping
• muscle pains or stiffness
• chest pressure or squeezing pain in chest
• discomfort in arms, shoulders, neck or upper back
• excessive sweating
• feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
• sudden tingling or coldness in an arm or leg
• sudden slow or difficult speech
• sudden drowsiness or need to sleep
• fast breathing
• sharp pain when taking a deep breath
• fast or slow heartbeat
• coughing up blood
• rust colored urine
• decreased amount of urine

Rare

• Anxiety
• change in vision
• seizures
• abnormal or fast heart rate
• tremors
• weight loss
• chest pain or tightness
• confusion
• cough
• Agitation
• arm, back, or jaw pain
• blurred vision
• chest pain or discomfort
• convulsions
• extra heartbeats
• fainting
• hallucinations
• headache
• irritability
• lightheadedness
• mood or mental changes
• muscle pain or cramps
• muscle spasm or jerking of all extremities

Drug Interactions of Anakinra

Anakinra may interact with the following drugs, supplements, & may change the efficacy of drugs

• abatacept
• bacillus Calmette-Guérin (BCG)
• belimumab
• canakinumab
• certolizumab pegol
• cyclophosphamide
• denosumab
• fingolimod
• immunosuppressants (e.g., cyclosporine, mycophenolate, tacrolimus)
• medications that weaken the immune system (e.g., medications for cancer or organ transplants)
• other biologics (e.g., abatacept, adalimumab, infliximab, anakinra)
• leflunomide
• nivolumab
• natalizumab
• pimecrolimus
• roflumilast
• sulfasalazine
• tacrolimus
• tocilizumab
• tofacitinib
• trastuzumab
• vaccines (e.g., yellow fever, BCG, cholera, typhoid, varicella, meningococcal, diphtheria)
• vedolizumab

Pregnancy Catagory of Anakinra

FDA Pregnancy Category B

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

It is not known if anakinra passes into breast milk. If you are a breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding. The safety and effectiveness of this medication have not been established for children less than 18 years of age.

References

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