Chlorokhin (Chloroquinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Other synthetic antibacterial agents

Immunosuppressive drugs

Included in the formulation
  • Delagil
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    Meda Pharma GmbH & Co. KG     Germany
    • АТХ:

    P.01.B.A.01   Chlorokhin

    Pharmacodynamics:

    The 4-aminoquinoline derivative interacts with ferriprotoporphyrin IX, a specific degradation product of parasites within the erythrocytes. Has selective toxicity with respect to plasmodium infection in the erythrocyte phase. It binds to nucleic acids, interrupting the synthesis of DNA, which leads to the death of parasites that cause malaria, as well as tissue forms of amoebae.

    Has immunosuppressive and anti-inflammatory action in autoimmune processes. Reducing the excitability of the myocardium, has antiarrhythmic effect.

    Pharmacokinetics:

    After oral administration, up to 98% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached in 1-6 hours. The connection with plasma proteins is 55%.

    Penetrates through the blood-brain and placental barrier, is found in breast milk. Metabolism in the liver.

    The half-life is 6-7 days. Elimination by the kidneys, up to 70% unchanged.

    Indications:

    It is used for the prevention and treatment of malaria, systemic lupus erythematosus, porphyria, amoebiasis. It is part of the combined therapy of systemic lupus erythematosus, scleroderma, rheumatoid arthritis and photodermatosis.

    ICD-10

    I.A00-A09.A06.4   Amoebic liver abscess

    I.A00-A09.A06   Amebiasis

    I.B50-B64.B54   Malaria, unspecified

    IV.E70-E90.E80   Disorders of porphyrin and bilirubin metabolism

    XII.L55-L59.L56   Other acute skin changes caused by ultraviolet radiation

    XIII.M05-M14.M06.9   Rheumatoid arthritis, unspecified

    XIII.M30-M36.M32   Systemic lupus erythematosus

    XIII.M30-M36.M34   Systemic sclerosis

    Contraindications:

    Inhibition of cerebral circulation, renal and hepatic insufficiency, psoriasis, neutropenia, cardiac rhythm disturbances, individual intolerance, children under 12 months.

    Carefully:

    Epilepsy, deficiency of glucose-6-phosphate dehydrogenase, retinopathy, myasthenia gravis, diseases of the gastrointestinal tract, hypersensitivity.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. It is used with caution during pregnancy and lactation in cases where the intended benefit exceeds the risk to the fetus and newborn.

    Dosing and Administration:

    Use in children

    Inside, depending on age:

    1-6 years: 1st day - 125 mg, 2-3 days - 50 mg;

    6-10 years: 1st day - 250 mg, 2-3 days - for 125 mg;

    10-15 years: 1st day - 500 mg, 2-3 days - 250 mg each.

    For treatment of extraintestinal amoebiasis: 6 mg / kg per day for 2 weeks, followed by a lower dose twice.

    Adults

    Inside, for the prevention of malaria - 500 mg 2 times a week, then 500 mg 1 time on the same day of the week.

    For the treatment of malaria - 1 g in the first day once, then after 6-8 hours - 500 mg, on the 2 nd and 3 rd day 750 mg at a time.

    In the treatment of amoebiasis: inside, 500 mg 3 times a day for a week, then 250 mg 3 times a day for the second week, then 750 mg twice a week for 2-6 months.

    With rheumatoid arthritis: 259 mg twice a day for a week. Then every day for 250 mg for 12 months.

    With systemic lupus erythematosus: 250-500 mg once a day.

    For the treatment of photodermatosis: 250 mg per day for a week, then 500-750 mg per week.

    The highest daily dose: 1.5 g.

    The highest single dose: 1 g.

    Side effects:

    Central and peripheral nervous system: dizziness, headache, convulsive attacks, sleep disorders, acute psychosis.

    Hemopoietic system: thrombocytopenia, agranulocytosis, leukopenia.

    The cardiovascular system: arterial hypotension, toxic myocarditis.

    Digestive system: anorexia, gastralgia, nausea, vomiting.

    Musculoskeletal system: arthralgia, muscle weakness, myalgia, muscle spasms.

    Dermatological reactions: itching, hyperpigmentation of mucous membranes and skin, dermatitis, hair color change (depigmentation).

    Sense organs: ringing in the ears, hearing impairment, retinal damage, corneal opacity, visual impairment.

    Allergic reactions.

    Overdose:

    Nausea and vomiting, a sharp drop in blood pressure, quickly turning into a coma and apnea.

    Treatment is symptomatic.

    Interaction:

    Increases glycoside intoxication of cardiac glycosides.

    With simultaneous use with penicillamine, gold preparations, levamisole, phenylbutazone and cytostatics, neurotoxicity increases.

    Ethanol increases hepatotoxicity.

    When used simultaneously with glucocorticoids, the risk increases development of cardiomyopathy and myopathy.

    Cimetidine increases the concentration of chloroquine in the blood plasma.

    Antacids reduce absorption.

    Monoamine oxidase inhibitors increase toxicity.

    Special instructions:

    Monitoring the cellular composition of the blood.

    In the treatment it is necessary to observe patients with an oculist.

    In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

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