Action and Spectrum

Actions and Spectrum: 

sarilumab works by attaching to the IL-6 receptor and blocking the IL-6 cytokine’s ability to function. As a result, the inflammation and discomfort brought on by autoimmune illnesses are reduced. 

Adult patients with mild to severe rheumatoid arthritis who have not reacted well to other disorder modifying antirheumatic medications can be treated with sarilumab, according to its range of activities (DMARDs). Those who are sensitive to methotrexate may also receive sarilumab alone or in conjunction with the drug. Also, it has been authorised for use in patients two years of age and older suffering from juvenile idiopathic arthritis. 

Drug Interaction

Adverse Reaction

Frequency Defined  

<1% 

AST>5x ULN (0.2-0.7%) 

ANC <500 /mm³ (0.7%) 

1-10% 

Injection site pruritics (4-5%) 

ALT>5x ULN (0.7-1%) 

Upper respiratory tract infection (3-4%) 

ALT >3x to 5x ULN (3-4%) 

Neutropenia (7-10%) 

ANC <1000/mm³ (4-6%) 

Injection site erythema (4-5%) 

AST >3x to 5x ULN (1%) 

Urinary tract infection (3%) 

Leukopenia (0.9-2%) 

Decreased platelet counts (0.7-1%) 

Hypertriglyceridemia (1-3%) 

>10% 

AST >ULN to ≤3 x ULN (27-30%) 

ALT >ULN to ≤3 x ULN (38-43%) 

Black Box Warning

Black Box Warning:

The risk of serious infections, including as bacterial sepsis tuberculosis, and invasive fungal infections, has been observed to rise with the use of sarilumab and other IL-6 receptor antagonists, which is the subject of the warning. 

As sarilumab may trigger latent tuberculosis infections, the warning suggests that patients should be tested for the disease before beginning therapy. Before the infection has been sufficiently treated, patients with active infections shouldn’t receive sarilumab. 

sarilumab may raise the risk of malignancy, including lymphoma, according to the black box warning.   

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

Those who have a known hypersensitivity to sarilumab or any of its components should not receive sarilumab.  

Caution: 

Serious infections, such as tuberculosis, bacterial sepsis, and invasive fungal infections, are made more likely by sarilumab. Consequently, before beginning sarilumab treatment, patients should be tested for tuberculosis. Before the infection has been sufficiently treated, patients with active infections should also not receive sarilumab. Throughout sarilumab therapy, medical professionals should closely watch patients for indications of infection.  

• Immunizations: Patients receiving sarilumab shouldn’t receive live immunisations because doing so could reduce the vaccine’s efficacy. 
• Hepatic impairment: Sarilumab users who have significant hepatic impairment may be at higher risk for side effects. As a result, these patients should utilise sarilumab with caution. 
• Breastfeeding: It is unknown whether sarilumab is safe for use in pregnant or nursing women. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:  

A monoclonal antibody called sarilumab, functions as an interleukin-6 receptor antagonist. 

sarilumab inhibits the downstream signalling pathways that cause inflammation and joint degeneration by binding to the IL-6 receptor. As a result, autoimmune illnesses, including rheumatoid arthritis, are less inflammatory and painful. 

Pharmacodynamics:  

In clinical trials, sarilumab’s pharmacodynamic effects on rheumatoid arthritis patients were established. Several studies have demonstrated that sarilumab therapy improves physical performance and quality of life while also reducing disease activity, as well as the amount of swollen and painful joints. 

A pro-inflammatory cytokine called IL-6, or interleukin-6, has a role in the pathophysiology of several autoimmune illnesses, most notably rheumatoid arthritis. 

Pharmacokinetics:  

Absorption   

sarilumab is absorbed quickly into the bloodstream after being injected subcutaneously. After subcutaneous injection, sarilumab has a bioavailability of about 63%. 

Distribution 

The volume of the distribution has the biggest impact on how sarilumab is distributed throughout the body. sarilumab’s distribution volume in steady state is roughly 7.2 L. 

Metabolism   

sarilumab undergoes the same type of proteolytic metabolism as endogenous immunoglobulin G antibodies. The liver is where sarilumab is primarily metabolised. 

Elimination and excretion 

Both renal and non-renal pathways are used to remove sarilumab from the body. sarilumab is primarily removed through non-renal pathways, with the kidneys accounting for about 35% of a dose. 

Adminstartion

Administration:  

Subcutaneous administration refers to the injection of sarilumab directly beneath the skin. Typically, the patient administers it themselves after receiving the necessary instruction from a healthcare professional. 

Every two weeks, 200 mg of sarilumab should be delivered as a subcutaneous injection. The upper arm, abdomen or thigh should be alternated as the injection location. To ensure that the patient can properly self-administer the medication, the very first dose of sarilumab should be given under the direction of a medical expert. 

In order to avoid any visible veins or arteries, the injection should be administered subcutaneously into the fatty tissue. Before administering, the injection site needs to be cleansed with an alcohol swab. To help the medicine distribute, the area should be gently rubbed after the injection.

Patient Information Leaflet

Patient information leaflet 

Generic Name: sarilumab 

Why do we use sarilumab? 

Rheumatoid arthritis and juvenile idiopathic arthritis are two autoimmune illnesses that are treated with the prescription drug sarilumab. 

sarilumab is used to treat pain and joint deterioration in rheumatoid arthritis and juvenile idiopathic arthritis, as well as to improve athletic performance.