Immard

General characteristics. Structure:

Active agent: hydroxychloroquine of 200 mg

Excipients: starch corn, calcium hydrophosphate, talc, silicon dioxide colloid, polysorbate-80, magnesium stearate.
The cover contains: titanium dioxide, macrogoal, gipromelloza, talc.

Pharmacological properties:

Pharmacodynamics. Antimalarial drug, actively suppresses erythrocyte forms (gematoshizotropny drug). Condenses lizosomalny membranes and interferes with an exit of lizosomalny enzymes, breaks DNA reduplication, synthesis of RNA and utilization of Hb erythrocyte forms of a plasmodium.
Has also immunodepressive and antiinflammatory effect, suppresses free radical processes, weakens activity of proteolytic enzymes (protease and a collagenase), leukocytes, a chemotaxis of lymphocytes.

Pharmacokinetics. Absorption - is variable. The semi-absorption period - 3.6 h (1.9-5.5 h). Bioavailability - 74%. Communication with proteins of plasma - 45%. Time of achievement of the maximum concentration of drug in blood (Tcmax) - 3.2 h (2-4.5 h), the maximum concentration makes (Cmax) after intake of 155 mg - 948 ng/ml, after intake of 310 mg-1895 ng/ml. Collects in fabrics with the high level of exchange (a liver, kidneys, lungs, a spleen - in these bodies concentration exceeds plasma by 200-700 times; in the central nervous system, erythrocytes, leukocytes) and in the fabrics rich with melanin.
In very low concentration it is found in digestive tract walls.
Gets through a placental barrier, in insignificant quantities is defined in breast milk. Distribution volume: measured in blood - 5.522 l, in plasma - 44.257 l.
It is metabolized partially in a liver with formation of active dezetilirovanny metabolites. An elimination half-life from blood (Т½) - 50 days, from plasma - 32 days.
It is removed by kidneys (23-25% in not changed look) and with bile (less than 10%). Removal very slowly also can is long to be defined in urine after the treatment termination.

Indications to use:

Malaria: treatment of bad attacks and overwhelming therapy of the malaria caused by Plasmodium vivax, Plasmodium ovale and Plasmodium malariae (excepting hydroxychloroquine - resistant cases) and sensitive strains of Plasmodium falciparum; radical treatment of the malaria caused by sensitive strains of Plasmodium falciparum; pseudorheumatism; lupus erythematosus (system and diskoidny); photodermatitis; bronchial asthma, Shegren's syndrome.

Route of administration and doses:

Inside, during meal or washing down with a glass of milk. 200 mg of hydroxychloroquine of sulfate are equivalent to 155 mg of hydroxychloroquine of the basis.
Pseudorheumatism: an initial dose at adults - 400-600 mg/days, supporting-200-400 mg/days.
Juvenile arthritis: the dose should not exceed 6.5 mg/kg or 400 mg/days (the smallest dose is chosen).
Diskoidny and system lupus erythematosus: an initial dose for adults - 400-800 mg/days, supporting - 200-400 mg/days.
Photo dermatosis: to 400 mg/days. Treatment has to be limited to the periods of the maximum solar exposure.
Malaria: overwhelming therapy adults - to 400 mg/days have each 7 day; children have a weekly overwhelming dose - 6.5 mg/kg, but irrespective of body weight, should not exceed a dose for adults (400 mg). If conditions allow, appoint overwhelming therapy for 2 weeks before influence, otherwise, it is possible to appoint an initial double dose: 800 mg - the adult and 12.9 mg/kg (but not exceeding 800 mg) - to children, having divided into 2 inclusion with an interval in 6 h. Overwhelming therapy should be continued during 8 weeks.
After the endemic zone is left.
Treatment of a bad attack of malaria: an initial dose for adults - 800 mg, then in 6-8 h - 400 mg and on 400 mg for the 2 and 3 days of treatment (in total 2 g of hydroxychloroquine of sulfate). As an alternative method there can be effective a dose of 800 mg once.
For children the general dose - 32 mg/kg (but not exceeding 2 g) are appointed within 3 days: the first dose - 12.9 mkg/kg (but not exceeding a single dose of 800 mg), the second dose - 6.5 mg/kg (but not exceeding 400 mg) in 6 h after the first, third dose - 6.5 mg/kg (but not exceeding 400 mg) in 18 h after the second dose, the fourth dose - 6.5 mg/kg (but not exceeding 400 mg) in 24 h after the third dose.
The dose for adults can be expected 1 kg of body weight, as well as for children.

Features of use:

Before the beginning and during therapy it is necessary to carry out at least 1 time in 6 months ophthalmologic inspection.
During therapy constant control of cellular composition of blood, a condition of skeletal muscles is necessary (including tendon jerks).
During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From musculoskeletal and nervous systems: the decrease in body weight, a myopathy or a neuromyopathy leading to the amplifying myasthenia and an atrophy of proximal groups of muscles; touch disturbances, decrease in tendon jerks, abnormal nerve conduction; headache, dizziness, nervousness, psychosis, emotional lability, spasms.
From sense bodys: sonitus, relative deafness, photophobia, visual acuity disturbance, accommodation disturbance, hypostasis and opacification of a cornea, scotoma; at prolonged use of high doses - a retinopathy (including with disturbance of pigmentation and defects of fields of vision), an atrophy of an optic nerve, a keratopathy, dysfunction of a tsiliarny muscle.
From cardiovascular system: at long therapy by high doses - a myocardial dystrophy, a cardiomyopathy, an atrioventricular block, decrease in contractility of a myocardium, a myocardium hypertrophy.
From the alimentary system: nausea, vomiting (seldom), loss of appetite, abdominal pain of spastic character, diarrhea; hepatotoxic (abnormal liver function, liver failure).
From bodies of a hemopoiesis: a neutropenia, aplastic anemia, an agranulocytosis, thrombocytopenia, hemolitic anemia (at patients with deficit glyukozo-6-fosfatdegidrogenazy).
From integuments: skin rash (including violent and generalized pustular), an itch, disturbance of a xanthopathy and mucous membranes, decolouration of hair, an alopecia, photosensitivity, Stephens-Johnson's syndrome (a mnogomoforny exudative erythema), an exacerbation of psoriasis (including with fever and a hyperleukocytosis), aggravation of a porphyria.

Interaction with other medicines:

Increases concentration, digoxin in plasma, aminoglycosides strengthen the blocking action on neuromuscular conductivity. Strengthens effect of hypoglycemic medicines (demands a dose decline of the last). At simultaneous use of antacids the interval between reception has to make not less than 4 h (decrease in absorption). Alkaline drink and alkalis accelerate removal from an organism. Increases plasma concentration of Penicillaminum and risk of emergence of its side effects from bodies of a hemopoiesis, an urinary system and skin reactions. Strengthens side effects of glucocorticosteroids, salicylates, antiarrhythmic drugs 1a of a class, gemato-, gepato-and neurotoxic means.

Contraindications:

Hypersensitivity to drug, pregnancy, the lactation period, children's age up to 3 years, and also long therapy at children's age.
With care - a retinopathy (including a maculopathia in the anamnesis), disturbance of a marrowy hemopoiesis, a disease of the central nervous system and cardiovascular systems, psychosis (including in the anamnesis), a porphyria, psoriasis, deficit glyukozo-6-fosfatdegidrogenazy, a liver and/or renal failure.

Overdose:

Symptoms: cardiotoxicity (disturbance of conductivity on a ventriculonector; at chronic intoxication - a hypertrophy of a myocardium of both ventricles), a lowering of arterial pressure, a neurotoxicity (dizziness, a headache, a hyperexcitability, spasms, a coma), a vision disorder, an apnoea and hearts.
The overdose is especially dangerous at small children, even reception of 1-2 g of drug can lead to a lethal outcome.

Treatment: the gastric lavage, purpose of absorbent carbon (in a dose by 5 times exceeding a drug dose), an artificial diuresis and alkalifying of urine (for example ammonium chloride to рН urine - 5.5-6.5) increase removal with aminoquinoline urine 4, symptomatic therapy (including appointment at spasms - diazepam, antishock therapy). Control of concentration of sodium in blood serum and constant medical control not less than 6 h after stopping of symptoms is necessary.

Storage conditions:

List B.
To store in the dry, protected from light place, at a temperature not above 25 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated on 200 mg.
On 10 tablets in the blister PVC Is scarlet/.
On 1, 2, 3 or 6 blisters together with the application instruction are placed in a cardboard pack.