IMMARD
Active material: Gidroksixloroxin
When ATH: P01BA02
CCF: The 4-aminoquinoline. Antimalarial drug and amebitsidny. Immunosuppressant
ICD-10 codes (testimony): B50, B51, B52, J45, L56.2, L93.0, M05, M32, M35.0
When CSF: 05.02.03
Manufacturer: IPCA LABORATORIES Ltd. (India)
Pharmaceutical form, composition and packaging
Pills, Film-coated white or nearly white, round, lenticular, Engraved “HCQS” on one side.
| 1 tab. | |
| hydroxychloroquine sulfate | 200 mg |
Excipients: corn starch, calcium hydrogen phosphate, talc, colloidal silicon dioxide, polysorbate 80, magnesium stearate.
The composition of the shell: Titanium dioxide, macrogol, gipromelloza, talc.
10 PC. – blisters (1) – packs cardboard.
10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (6) – packs cardboard.
Pharmacological action
The antimalarial, actively suppresses human erythrocyte shape (gematoshizotropnyj drug). Plumping lizosomaiona membranes and hampers Lysosomal enzymes, violates reduplicatia DNA, RNA synthesis and recycling hemoglobin eritrocitariani forms of Plasmodium.
Also has an immunosuppressive and anti-inflammatory effect, Suppresses processes, in which free radicals are formed, weakens Active proteolytic enzymes (protease and collagenase), leukocytes, chemotaxis of lymphocytes.
Pharmacokinetics
Absorption
Drug absorption variabelna. Period of poluabsorbcii – 3.6 no (1.9-5.5 no). Bioavailability – 74%.
Tmax plasma – 3.2 no (2-4.5 no). After taking the drug orally at a dose 155 mg Cmax in plasma is 948 ng / ml, dose 310 mg – 1895 ng / ml.
Distribution
Plasma protein binding – 45%. It accumulates in tissues with a high level exchange (liver, kidney, light, spleen – in these organs in a plasma concentration of greater than 200-700 time; CNS, erythrocytes, leukocytes) and in tissues, rich melanin. In very low concentrations detected in the walls of the DIGESTIVE TRACT. It penetrates through the placental barrier, in small quantities determined in breast milk. Vd in blood – 5 522 l, plasma – 44 257 l.
Metabolism
Partially metabolized in the liver with the formation of active metabolites dezjetilirovannyh.
Deduction
T1/2 – 50 days, plasma – 32 day. Report the news (23-25% in unchanged form) and the bile (less 10%). Prints very slowly and can be measured in the urine for a long time after the end of treatment.
Testimony
— malaria: treatment of acute attacks and overwhelming malaria therapy, caused by Plasmodium vivax , Plasmodium ovale and Plasmodium malariae (excluding hydroxychloroquine-resistant cases) and susceptible strains of Plasmodium falciparum; radical treatment of malaria, caused by susceptible strains of Plasmodium falciparum;
- Rheumatoid arthritis;
- Systemic lupus erythematosus, discoid lupus erythematosus;
is a photodermatosis;
- Bronchial asthma;
is Sjogren's syndrome.
Dosage regimen
Is inwards during eating or drinking a glass of milk.
200 mg gidroksihlorohina sulfate equivalent 155 mg gidroksihlorohina Foundation.
At malaria as a suppressive therapy adult administered at a dose of 400 mg/day each 7 day; children – 6.5 mg/kg downloads, But regardless of body weight dose for children should not exceed the dosage for adults (400 mg). If conditions allow, most therapy is prescribed for 2 Sun. before the possible infection. Otherwise, you can assign the initial double dose: adult – 800 mg, children – 12.9 mg / kg (but not more 800 mg), dividing the dose 2 receiving intervals 6 no. Most therapy should continue for 8 Sun. Once abandoned endemic area.
Treatment of acute attack of malaria: to Adult the initial dose – 800 mg, then through 6-8 no – 400 mg and 400 mg 2 and 3 days of treatment (a total of – 2 g gidroksihlorohina sulfate). As an alternative method may be effective dose 800 mg – single.
To children the total dose is 32 mg / kg (but not more 2 g) and shall be appointed within 3 days: the first dose – 12.9 mg / kg (but no more than a single dose 800 mg), the second dose – 6.5 mg / kg (but not more 400 mg) through 6 hours after the first, third dose – 6.5 mg / kg (but not more 400 mg) through 18 hours after the second dose, the fourth dose – 6.5 mg / kg (but not more 400 mg) through 24 hours after the third dose.
Dose for adults can be calculated on the 1 kg body weight, as well as for children.
Rheumatoid arthritis: to Adult the initial dose – 400-600 mg / day, supports – 200-400 mg / day.
Juvenile arthritis: the maximum dose – 6.5 mg / kg or 400 mg / day (You should choose the lowest dose).
Systemic Lupus Erythematosus and Discoid Lupus Erythematosus: to Adult the initial dose – 400-800 mg / day, supports – 200-400 mg / day.
Photodermatosis: to 400 mg / day. Treatment should be restricted to periods of maximum solar exposure.
Side effect
On the part of the musculoskeletal system: myopathy or nejromiopatija, lead to increasing myasthenia and atrophy of the proximal muscle groups.
From the central and peripheral nervous system: sensory violation, reduction of tendon reflexes, abnormal nervous conductivity; headache, dizziness, nervousness, psychosis, emotional lability, convulsions.
From the senses: noise in ears, hearing loss, photophobia, violation of visual acuity, ccomodation, swelling and clouding of the cornea, scotoma; long-term use in high doses – retinopathy (incl. with violation of pigmentation and fields of vision defects), optic atrophy, keratopathy, the ciliary muscle dysfunction.
With the circulatory system: with long-term therapy the drug at high doses – miokardiodistrofija, cardiomyopathy, AV блокада, reducing sokratimosti attack, myocardial hypertrophy.
From the digestive system: nausea, vomiting (rarely), decreased appetite, abdominal pain, spastic nature, diarrhea, gepatotoksichnostь (abnormal liver function, hepatic failure).
From the hematopoietic system: neutropenia, aplasticheskaya anemia, agranulocytosis, thrombocytopenia, gemoliticheskaya anemia (in patients with deficiency of glucose-6-phosphate dehydrogenase).
Metabolism: weight loss, worsening porfirii flow.
Dermatological reactions: skin rash (incl. Bullous and generalized pustuleznaja), itch, pigmentation of skin and mucous membranes, Hair discoloration, alopecia, photosensitivity, Stevens-Johnson syndrome (erythema multiforme exudative), exacerbation of psoriasis (incl. with fever and giperlejkocitozom).
Contraindications
- Pregnancy;
- Lactation;
- Children up to age 3 years;
-prolonged therapy in childhood;
- Hypersensitivity to the drug.
FROM caution should be used in patients with retinopathy (incl. history of makulopatiej), kostnomozgovy blood disorders, diseases of the CENTRAL NERVOUS SYSTEM and cardiovascular system, When psychosis (incl. history), porfirii, psoriaze, definition, glucose-6-fosfatdegidrogenazы, with hepatic and / or renal insufficiency.
Pregnancy and lactation
The drug is contraindicated in pregnancy and lactation (breast-feeding).
Cautions
Before and during therapy, it was necessary to conduct ophthalmologic examination not less 1 times a 6 month.
During therapy requires constant monitoring of cellular blood, State of skeletal muscles (incl. tendon reflexes).
Effects on ability to drive vehicles and management mechanisms
During treatment, it is necessary to be careful when driving vehicles and other potentially hazardous activities, require high concentration and speed of psychomotor reactions.
Overdose
Symptoms: cardiotoxicity (violation of conductivity to lift Guisa; in chronic intoxication – myocardial hypertrophy of both ventricles), decrease in blood pressure, neurotoxicity (dizziness, headache, hypererethism, convulsions, coma), blurred vision, respiratory arrest and heart.
Overdose is especially dangerous in young children, even the reception 1-2 grams of the drug can be fatal.
Treatment: gastric lavage, appointment of activated carbon (dose, in 5 times higher than the dose of the drug), forced diuresis and alkalinization of urine (eg, ammonium chloride to the pH of the urine – 5.5-6.5) increase excretion in urine 4-aminohinolina, simptomaticheskaya therapy (including the appointment of cramps – diazepama, antishock therapy). Needed to be monitored concentrations of sodium in blood serum and constant medical supervision at least 6 hours after the edema symptoms.
Drug Interactions
While applying hydroxychloroquine raises the concentration of Digoxin in plasma, aminoglikozida increase the blocking effect on neuromuscular conductivity.
Hydroxychloroquine magnifies the effect of hypoglycemic drugs (you want to reduce the dose of the past).
Together with the application antatidami reduced absorption gidroksihlorohina (the interval between admission and antacida drug Immard should be not less than 4 no).
Alkaline and alkaline drink accelerate excretion from the body gidroksihlorohina.
Hydroxychloroquine raises the plasma concentrations of penicillamine for and increases the risk of side-effects of the blood, urinary tract and skin reactions.
Hydroxychloroquine do side effects of CORTICOSTEROIDS, salitsilatov, antyarrhythmic preparations class IA, gemato-, scarp- and neurotoxic agents.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored out of reach of children, dry, dark place at a temperature no higher than 25 ° C. Shelf life - 2 year.
