Composition, form of production and packaging
The tablets covered with a film shell of white or almost white color, round, biconcave, with engraving "HCQS" on one side.
hydroxychloroquine sulphate 200 mg
Excipients: corn starch, calcium hydrophosphate, talc, silicon dioxide colloid, polysorbate 80, magnesium stearate.
Composition of the coating: titanium dioxide, macrogol, hypromellose, talc.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
10 pieces. - blisters (6) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2010.
Antimalarial drug, actively suppresses erythrocyte forms (hematoschotropic drug). It compacts lysosomal membranes and prevents the release of lysosomal enzymes, disrupts DNA reduplication, RNA synthesis and hemoglobin utilization by erythrocyte forms of plasmodia.
It also has an immunosuppressive and anti-inflammatory effect, suppresses the processes in which free radicals are formed, weakens the activity of proteolytic enzymes (protease and collagenase), leukocytes, chemotaxis of lymphocytes.
Absorption of the drug is variable. The half-absorption period is 3.6 h (1.9-5.5 h). Bioavailability - 74%.
T max in the blood plasma - 3.2 h (2-4.5 h). After taking the drug inside the dose of 155 mg C max in blood plasma is 948 ng / ml, in a dose of 310 mg - 1895 ng / ml.
Binding to plasma proteins - 45%. Accumulates in tissues with a high level of metabolism (in the liver, kidneys, lungs, spleen - in these organs the concentration exceeds the plasma concentration by 200-700 times, in the central nervous system, erythrocytes, leukocytes) and in tissues rich in melanin. In very low concentrations found in the walls of the gastrointestinal tract. Penetrates through the placental barrier, in small amounts is determined in breast milk. V d in the blood - 5 522 liters, in the plasma - 44 257 liters.
It is partially metabolized in the liver with the formation of active de-ethylated metabolites.
T 1/2 - 50 days, from the plasma - 32 days. It is excreted by the kidneys (23-25% unchanged) and with bile (less than 10%). It is withdrawn very slowly and can be permanently detected in the urine after discontinuation of treatment.
- Malaria: treatment of acute attacks and suppressive therapy for malaria caused by Plasmodium vivax, Plasmodium ovale and Plasmodium malariae (excluding hydroxychloroquine-resistant cases) and sensitive strains of Plasmodium falciparum; radical treatment of malaria caused by sensitive strains of Plasmodium falciparum;
- rheumatoid arthritis;
- systemic lupus erythematosus, discoid lupus erythematosus;
- bronchial asthma;
- Sjogren's syndrome.
Is taken orally during a meal or with a glass of milk.
200 mg of hydroxychloroquine sulfate is equivalent to 155 mg of hydroxychloroquine base.
With malaria as an overwhelming therapy, adults are prescribed 400 mg / day every 7 days; Children 6.5 mg / kg weekly, but regardless of body weight, the dose for children should not exceed the adult dose (400 mg). If conditions allow, overwhelming therapy is prescribed for 2 weeks. before possible infection. Otherwise, an initial double dose can be given: adults - 800 mg, children - 12.9 mg / kg (but not more than 800 mg), dividing the dose into 2 divided doses with an interval of 6 hours. Suppressive therapy should be continued for 8 weeks. After the endemic zone is abandoned.
Treatment of an acute attack of malaria: for adults, the initial dose is 800 mg, then after 6-8 hours - 400 mg and 400 mg on the 2nd and 3rd days of treatment (a total of 2 g of hydroxychloroquine sulphate). As an alternative, an effective dose of 800 mg may be effective once.
For children, the total dose is 32 mg / kg (but not more than 2 g) and is prescribed for 3 days: the first dose is 12.9 Ојg / kg (but no more than a single dose of 800 mg), the second dose is 6.5 mg / kg (but not more than 400 mg) 6 hours after the first, the third dose is 6.5 mg / kg (but not more than 400 mg) 18 hours after the second dose, the fourth dose is 6.5 mg / kg (but not more than 400 mg) 24 hours after the third dose.
The dose for adults can be calculated for 1 kg of body weight, as well as for children.
Rheumatoid arthritis: for adults, the initial dose is 400-600 mg / day, supporting - 200-400 mg / day.
Juvenile arthritis: the maximum dose is 6.5 mg / kg or 400 mg / day (the lowest dose should be chosen).
Systemic lupus erythematosus and discoid lupus erythematosus: for adults, the initial dose is 400-800 mg / day, supporting - 200-400 mg / day.
Photodermatosis: up to 400 mg / day. Treatment should be limited to periods of maximum solar exposure.
From the side of the musculoskeletal system: myopathy or neuromyopathy, leading to increased myasthenia and atrophy of proximal muscle groups.
From the side of the central nervous system and the peripheral nervous system: sensory disorders, decrease of tendon reflexes, abnormal nerve conduction; headache, dizziness, nervousness, psychosis, emotional lability, convulsions.
From the senses: tinnitus, hearing loss, photophobia, visual acuity, accommodation disorder, edema and opacity of the cornea, scotoma; with prolonged use in high doses - retinopathy (including with a violation of pigmentation and visual field defects), atrophy of the optic nerve, keratopathy, dysfunction of the ciliary muscle.
On the part of the cardiovascular system: with prolonged therapy with the drug in high doses - myocardial dystrophy, cardiomyopathy, AV blockade, decreased myocardial contractility, myocardial hypertrophy.
On the part of the digestive system: nausea, vomiting (rarely), decreased appetite, abdominal pain of a spastic nature, diarrhea, hepatotoxicity (impaired liver function, liver failure).
From the hemopoietic system: neutropenia, aplastic anemia, agranulocytosis, thrombocytopenia, hemolytic anemia (in patients with deficiency of glucose-6-phosphate dehydrogenase).
From the side of metabolism: a decrease in body weight, aggravation of the flow of porphyria.
Dermatological reactions: skin rash (including bullous and generalized pustular), itching, skin and mucosal skin pigmentation disorder, hair loss, alopecia, photosensitivity, Stevens-Johnson syndrome (exudative erythema multiforme), exacerbation of psoriasis (including with fever and hyperleukocytosis).
- lactation period;
- children's age till 3 years;
- long-term therapy in childhood;
- Hypersensitivity to the components of the drug.
It should be used with caution in patients with retinopathy (including maculopathy in the anamnesis), disorders of bone marrow hematopoiesis, diseases of the central nervous system and cardiovascular system, with psychosis (including in anamnesis), porphyria, psoriasis, glucose- 6-phosphate dehydrogenase, with hepatic and / or renal insufficiency.
PREGNANCY AND LACTATION
The drug is contraindicated in pregnancy and lactation (breastfeeding).
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution should be used in cases of hepatic and / or renal insufficiency.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should be used in cases of hepatic and / or renal insufficiency.
APPLICATION FOR CHILDREN
Contraindicated in children under 3 years of age, as well as for long-term therapy in children of any age.
Before and during therapy, an ophthalmic examination should be performed at least once every 6 months.
During therapy, continuous monitoring of the cellular composition of the blood, the state of skeletal muscles (including tendon reflexes) is necessary.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, care must be taken when driving vehicles and other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.
Symptoms: cardiotoxicity (impaired conduction in the bundle of the Gis, with chronic intoxication - myocardial hypertrophy of both ventricles), decreased blood pressure, neurotoxicity (dizziness, headache, increased excitability, convulsions, coma), visual impairment, respiratory and cardiac arrest.
Overdose is especially dangerous in young children, even taking 1-2 g of the drug can lead to death.
Treatment: gastric lavage, administration of activated charcoal (at a dose 5 times the dose of the drug), forced diuresis and alkalinization of urine (for example, ammonium chloride to urine pH 5.5-6.5) increase excretion of urinary 4-aminoquinoline, symptomatic therapy appointment in convulsions - diazepam, antishock therapy). It is necessary to monitor the concentration of sodium in the blood serum and constant medical control for at least 6 hours after the relief of symptoms.
With the simultaneous use of hydroxychloroquine increases the concentration of digoxin in the plasma, aminoglycosides increase the blocking effect on neuromuscular conduction.
Hydroxychloroquine enhances the effect of hypoglycemic drugs (a dose reduction of the latter is required).
With simultaneous use with antacids, the absorption of hydroxychloroquine decreases (the interval between taking an antacid and Immard should be at least 4 hours).
Alkaline drink and alkalis accelerate the excretion of hydroxychloroquine from the body.
Hydroxychloroquine increases plasma concentrations of penicillamine and increases the risk of side effects from the hematopoiesis system, urinary system and skin reactions.
Hydroxychloroquine enhances the side effects of GCS, salicylates, class IA antiarrhythmic drugs, hemato-, hepato- and neurotoxic agents.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored out of reach of children, dry, protected from light at a temperature of no higher than 25 В° C. Shelf life - 2 years.