Active Ingredient: hydroxychloroquine
Release form, composition and packaging
Amount of packaging and dosage (pcs, mg ml) 200 mg N60
Release form (tablets, capsules, suspensions, solution, ampoules, suppositories, units) and composition of the medical preparation (medicine) Active ingredient: hydroxychloroquine; 1 tablet contains 200 mg hydroxychloroquine sulfate excipients: lactose, povidone, corn starch, magnesium stearate shell: Opadry OY-L-28900 (hypromellose, titanium dioxide (E 171), polyethylene glycol, lactose). Dosage form. Film-coated tablets.
The main indications for use The treatment of rheumatoid arthritis, juvenile rheumatoid arthritis, discoid and systemic lupus erythematosus, as well as dermatological diseases caused by the occurrence or worsening of the course of which the action of sunlight.
After oral administration, hydroxychloroquine is rapidly and almost completely absorbed from the digestive tract. Tmax is 2-4.5 hours, Cmax after oral administration at a dose of 155 mg – 948 ng / ml, after oral administration at a dose of 310 mg – 1895 ng / ml.
Plasma protein binding – 45%. Vd is 5-10 l / kg. It is well distributed in the body, accumulating in the blood cells, in the liver, lungs, kidneys, and in the retina. It accumulates in tissues with a high level of metabolism – in the liver, kidneys, lungs, spleen, in these organs the concentration exceeds the plasma by 200-700 times; in the central nervous system, red blood cells, white blood cells and in tissues rich in melanin. Penetrates through the placental barrier. In small quantities is determined in breast milk.
Metabolism and excretion
In the liver, hydroxychloroquine is partially converted into active ethylated metabolites and excreted mainly by the kidneys, as well as with bile. Excretion of the drug is slow. T1 / 2 is about 50 days (whole blood) and 32 days (plasma).
juvenile chronic arthritis;
lupus erythematosus (systemic and discoid);
Malaria (except for chloroquine-resistant cases):
for the treatment of acute attacks and for the suppression of malaria caused by Plasmodium vivax, P.ovale and P. malariae, as well as sensitive strains of P. falciparum;
for the radical treatment of malaria caused by susceptible strains of P. falciparum.
Plaquenil is for oral use only. The drug is taken with meals or with a glass of milk. All doses of the drug are based on hydroxychloroquine sulfate and are not equivalent to the doses of the base. With rheumatic diseases, therapeutic activity is noted with the cumulation of the drug.
To develop a therapeutic effect, the drug should be taken for several weeks, while side effects can occur relatively early. An adequate therapeutic effect develops after a few months of taking the drug. If objective improvement in the patient’s condition is not observed within 6 months of treatment, then the drug should be discontinued.
Rheumatoid arthritis: for adults, the initial dose is 400-600 mg / day, the maintenance dose is 200-400 mg / day. Juvenile chronic arthritis: the dose should not exceed 6.5 mg / kg body weight or 400 mg / day (the lowest effective dose should be chosen). Systemic and discoid lupus erythematosus: for adults, the initial dose is 400-800 mg / day, the maintenance dose is 200-400 mg / day. Photodermatitis: treatment should be limited to periods of maximum exposure to light. For adults, 400 mg / day may be sufficient.