Instruction for use: Zenapax

Dosage form: Concentrate for solution for infusion

Active substance: Daclizumabum

ATX

L04AC01 Daclizumab

Pharmacological group:

Immunodepressants

Composition and release form

1 bottle with 5 ml concentrate for infusion contains daclizumab 25 mg; In the box 1 or 3 bottles.

Description of dosage form

Round biconvex tablets covered with a white film shell, with an engraving "HCQ" on one side and "200" on the other.

Pharmachologic effect

Mode of action - Immunosuppressive.

It is a recombinant antibody IgG1 (anti-Tas), blocks receptors sensitive to interleukin-2 (IL-2): specifically binds to the alpha-subunit (Tas) of the high-affinity IL-2 receptor complex, which is expressed on activated T cells, depresses Mediated IL-2 activation of lymphocytes and inhibits the immune response of graft rejection.

Pharmacokinetics

Cmax in patients who underwent allogeneic kidney transplantation after single administration at a dose of 1 mg / kg - 21 ± 14 μg / ml, after 5 infusions every 14 days - 32 ± 22 μg / ml. Complete saturation of the receptors for IL-2 occurs at serum concentrations of 0.5-0.9 μg / ml, inhibition of IL-2 mediated biological activity is 5-10 μg / ml. The recommended dosing regimen allows maintaining sufficient serum concentrations over 90 days after transplantation. T1 / 2 in patients with renal allograft - 270-919 hours (average 480 hours), which is equivalent to human T1 / 2 IgG. The system Cl is affected by body weight, age, sex, race, the presence of proteinuria.

Clinical Pharmacology

Reliably reduces during 6 months after transplantation the probability of rejection of the renal allograft and extends the time to the first episode of rejection. There is no increase in the frequency of the "graft versus host" reaction. Antibodies to daclizumab are found in 9% of patients, but they do not change the serum concentrations of the drug, its effectiveness and safety. The risk of rejection after drug withdrawal is not increased.

Indication of the drug Zenapax

Prevention of acute rejection of the kidney allograft.

Contraindications

Hypersensitivity, pregnancy, breast-feeding (excluded).

Side effects

On the part of the digestive tract: constipation, nausea, vomiting, dyspepsia, abdominal pain, flatulence, diarrhea.

From the side of metabolism: exacerbation of diabetes, edema or dehydration.

From the side of the central nervous system: headache, dizziness, insomnia, tremor, tingling and cramps in the legs, depression, anxiety.

From the urinary system: dysuria, oliguria, necrosis of the renal tubules, hydronephrosis, renal failure, hematuria, urinary retention.

From the cardiovascular system: arterial hypertension or hypotension, tachycardia, bleeding or thrombosis.

On the part of the respiratory system: coughing, wheezing, shortness of breath, atelectasis, congestion and pulmonary edema, pleural effusions, wheezing, pharyngitis, rhinitis, hypoxia.

On the part of the skin: a decrease in skin regeneration, acne, pruritus, hirsutism, rash, sweating, local reactions in the field of administration.

From the musculoskeletal system: pain in the joints, bones and muscles, pain in the lower back.

Other: chest pain, chills, fever, weakness, lymphocele, impaired vision, anaphylactoid reactions.

Dosing and Administration

IV slowly (over 15 min), previously adjusted to the recommended daily dose of 0.9% sodium chloride to 50 ml, the recommended dose - 1 mg / kg body weight. The first administration should be performed 24 hours prior to transplantation, the second and subsequent doses are administered at intervals of 14 days, in total - 5 doses. The time of administration of subsequent doses should not differ from the planned one for more than one day in both directions. Treatment should be combined with the administration of cyclosporine and corticosteroids.

Special instructions

The prepared solution under storage conditions at room temperature is suitable for no more than 4 hours, in the refrigerator (2-8 ° C) for 24 hours.

Storage conditions of the drug Zenapax

In the dark place at a temperature of 2-8 ° C (do not freeze).

Keep out of the reach of children.

Shelf life of the drug Zenapax

2 years.

Do not use after the expiry date printed on the package.