Golimumab - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Immunosuppressive drugs

Included in the formulation

Simponi®

solution PC

MSD FARMASYUTIKALS, LLC Russia

Simponi®

solution PC

MSD FARMASYUTIKALS, LLC Russia

Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

VED

ONLS

АТХ:

L.04.A.B.06 Golimumab

Pharmacodynamics:Golimumab, the inhibitor of TNF-α, the preparation of human monoclonal antibodies of class IgG1κ, obtained from the mouse hybridoma cell line recombinantly, binds and neutralizes by the antigen-antibody reaction and soluble and membrane-bound forms of TNF, a pro-inflammatory cytokine, which plays a dominant role in the development of various inflammatory disorders, with chronic pathologies, such as rheumatoid arthritis, spondyloarthropathies: psoriatic arthritis and ankylosing spondylitis. The affinity of the drug for soluble TNF exceeds that of infliximab and adalimumab by 2.4 and 7.1 times, respectively.

Inhibits the expression of adhesion molecules, including E-selectin, vascular cell adhesion molecules (VCAM-1) and intercellular adhesion molecules (ICAM-1), on the surface of endothelial cells, inhibits TNFα-induced secretion of interleukin-6, interleukin-8 and granulocyte- macrophage colony-stimulating factor by human endothelial cells.

Pharmacokinetics:Pharmacokinetics with subcutaneous administration is practically proportional to the dose, the average absolute bioavailability is 51%, there is no difference in absorption when administered under the skin of the abdomen, thigh or shoulder. The maximum serum concentration is achieved within 2-6 days. Half-life 12 days.

Indications:Treatment of rheumatoid and psoriatic arthritis, severe ankylosing spondylitis and moderate to severe ulcerative colitis with an inadequate response to standard therapy.

ICD-10

XI.K50-K52.K51 Ulcerative colitis

XIII.M05-M14.M05 Seropositive rheumatoid arthritis

XIII.M05-M14.M07 * Psoriatic and enteropathic arthropathies

XIII.M45-M49.M45 Ankylosing spondylitis

Contraindications:Severe infectious processes, such as active tuberculosis, sepsis and opportunistic infections; moderate or severe heart failure (NYHA class III-IV); pregnancy and breastfeeding; age to 18 years; hypersensitivity.

Carefully:Patients with mild heart failure (NYHA class I-II) should be monitored and therapy should be discontinued in the event of new or worsening signs of heart failure. The drug should not be administered to patients with a clinically active infection.With caution in diseases of the liver and kidneys.

Pregnancy and lactation:The drug is contraindicated in pregnancy and lactation. Women need to be protected for at least 6 months after the last injection.

Dosing and Administration:The drug is administered only subcutaneously!

With rheumatoid or psoriatic arthritis, ankylosing spondylitis, 50 mg of the drug is administered subcutaneously every month on the same day of the month. The clinical response develops between 12-14 weeks of therapy (3-4 injections). In patients with a body weight of more than 100 kg in the absence of an adequate response to 3-4 injections, the dose may be increased to 100 mg monthly, taking into account the risk of serious adverse reactions.

With ulcerative colitis, the initial dose of the drug is 200 mg subcutaneously, then 100 mg after 2 weeks, and then 100 mg every 4 weeks. Correction of dose in elderly patients (≥ 65 years) is not required.

If the injection was not performed on the scheduled date, the next injection should be as soon as possible. If less than 2 weeks have elapsed since the planned injection date, the next injection is given at the same dose as usual,Further therapy is continued in accordance with the previous regime, if more than 2 weeks - the next injection should be performed at the same dose as usual, the therapy is continued in a new mode (the next injection is a month after this administration).

Side effects:Infectious and parasitic diseases: infection of the upper respiratory tract (rhinitis, nasopharyngitis, pharyngitis, laryngitis), bacterial infections (phlegmon), viral infections (influenza and herpes), bronchitis, sinusitis, superficial fungal infections, septic shock, sepsis, tuberculosis, lower respiratory tract infections (pneumonia) , opportunistic infections (invasive fungal infections (histoplasmosis, coccidioidomycosis, pneumocystosis), bacterial, atypical mycobacterial and protozoal), abscess, bacterial arthritis, hepatitis B reactivation, pyelonephritis, infectious bursitis.

Benign, malignant tumors and unspecified neoplasms: cancer of the skin, squamous cell carcinoma and myelocytic nevus, lymphoma, leukemia.

On the part of the hematopoiesis system: anemia, leukopenia, thrombocytopenia, pancytopenia, aplastic anemia.

From the immune system: allergic reactions (bronchospasm, hypersensitivity, urticaria), a positive reaction to autoantibodies, anaphylactic reactions, systemic vasculitis, sarcoidosis.

From the endocrine system: thyroid disorders (hypothyroidism, hyperthyroidism and goiter).

From the side of metabolism: increased blood glucose and increased lipids.

From the nervous system: dizziness, paresthesia, headache, depression, insomnia, demyelinating diseases (central and peripheral forms), imbalances, personality disorders.

On the part of the organs of vision: visual impairment (opacification), conjunctivitis, allergic reactions (redness, irritation).

From the cardiovascular system: arterial hypertension, congestive heart failure (first detected or worsening of the present), arrhythmia, angina pectoris, thrombosis (including deep vein thrombosis and arteries), Raynaud's disease, hyperemia.

From the respiratory system: bronchial asthma and accompanying symptoms (dyspnea, bronchial hyperactivity), interstitial lung disease.

From the digestive system: constipation, dyspepsia, pain in the gastrointestinal tract, nausea, inflammatory diseases of the digestive tract (gastritis, colitis), reflux, stomatitis, increased activity of hepatic transaminases, cholelithiasis, impaired liver function.

From the skin and subcutaneous tissues: itching, rash, psoriasis (first detected or worsening of the existing disease, palmar-plantar, pustular), urticaria, systemic vasculitis, alopecia, dermatitis.

From the osteomuscular system and connective tissue: lupus-like syndrome, fractures of bones.

From the urinary system: diseases of the bladder, kidneys.

From the genitals and mammary glands: diseases of the mammary glands, menstruation disorders.

Common violations: hyperthermia, asthenia, discomfort in the chest.

Local reactions: erythema, urticaria, denseness, pain, bruising, itching, irritation, paresthesia at the injection site, slow healing at the injection site.

Overdose:With intravenous administration of a dose of 10 mg / kg, no toxicity was detected. In case of an overdose, the patient should monitor the symptoms of side effects and immediately prescribe symptomatic treatment.

Interaction:It is not recommended joint use with anakinra or abatacept, live vaccines.

Special instructions:Patients receiving therapy with the drug are at greater risk of developing the infectious process, it is impossible to exclude the risk of developing lymphomas, leukemias and other malignant tumors. Patients can be vaccinated, but not live vaccines!

Instructions

Golimumab (Golimumabum)