Index of drugs

Dabs: prevention and treatment of acute attacks and maintenance treatment for malaria caused byPlasmodium vivax, Plasmodium malariae, Plasmodium ovaleand chloroquine-sensitive strainsPlasmodium falciparum. Amoebiasis and liver abscess caused byEntamoeba histolytica, usually in combination with anti-sedatives working in the intestinal lumen; Chloroquine is used as a second-line drug if Metronidazole has failed or is unavailable. Different forms of lupus erythematosus, systemic form (SLE), chronic lupus and discoid lupus erythematosus (DLE). Rheumatoid arthritis.

1 tabl contains 250 mg of chloroquine phosphate.

A drug from the group of 4-aminoquinolones with antiprotozoal and anti-inflammatory properties. It is used in dabs caused by 4 speciesPlasmodium: P. vivax, P. ovale, P. malariae and by sensitive strainsP. falciparum. Chloroquine is a weak base, it works by increasing the pH in protozoan organisms that cause diarrhea. It induces rapid agglutination of hemoglobin (originating from human erythrocytes affected) in protozoan aquatic lice. Digesting host (human) hemoglobin inside the gastrointestinal tractPlasmodium releases heme which has lytic properties in relation to protozoan cell membranes. Hem may be inactivated by the enzyme - polymerasePlasmodium for the non-toxic dye of hemazoline. Chloroquine inhibits the activity of this polymerase and therefore, in the presence of chloroquine, the concentration of heme toxic toPlasmodium. SensitivityPlasmodium for chloroquine depends on the ability of protozoa to accumulate the drug in Aquatic Warblers. Chloroquine acts directly toxic to protozoa of the genusEntamoeba histolytica, the fact that chloroquine accumulates in the liver is also used. Chloroquine is used in dermatology and rheumatology as an anti-inflammatory in collagenoses and diseases with hypersensitivity to light. The mechanism of action of chloroquine in these diseases is probably: inhibition of phospholipase A2, action on lysosomes, inhibition of phagocytosis, inhibition of peroxide synthesis, increase of intracellular pH in Aquatic Warblers, which leads to reduction of CD4 cell stimulation, inhibition of cytokine release from monocytes, inhibition of antibody production. Chloroquine combines with porphyrins and facilitates their excretion in the urine. It also has an affinity for melanin and other dyes, which may be the reason for retinopathy that occurs during long-term drug administration. It reduces Na filtration and retention⁺ and Cl^- and increase in aldosterone. Chloroquine is well absorbed after oral administration, with plasma proteins associated in about 50%. The highest concentration in the blood occurs 3-6 h after administration. Administration of the drug together with the food increases absorption and bioavailability. Bioavailability after oral administration is 89%. Chloroquine accumulates in tissues, mainly in the liver, spleen, kidneys, lungs, in tissues containing melanin, and to a lesser extent in the brain and spinal cord. The placement of the drug depends on age and body weight. It is metabolized mainly in the liver (to a small extent in the kidneys) to deethylchlorochin, which reaches a plasma concentration of 20-30% of chloroquine concentration. The drug is very slowly excreted from the body, mainly through the kidneys (in 50-60%), of which 70% in unchanged form, 25% in the form of deethylchlorochin and in 5% as other metabolites. The acid reaction of urine accelerates excretion. T_0,5 drug in full renal function is variable and is usually 10-60 days (T._0,5 deethylchlorochin is about 15 days). The drug can be detected in the urine even after a few months after the end of treatment. Chloroquine penetrates the placental barrier and into breast milk, in which about 2-4% of the administered dose is secreted. Chloroquine after oral administration is also detected in semen.

Hypersensitivity to chloroquine phosphate, derivatives of 4-aminoquinoline or to any of the excipients. Changes in the retina or field of view caused by 4-aminoquinoline derivatives.

The drug should be used with caution in patients with impaired liver function (especially in the course of ACUTE, alcoholic liver damage) or kidneys, in people with alcoholism. Avoid using the drug in people with retinal disorders (except acute phase of diarrhea), in patients with impaired blood picture, as well as in patients with G-6-PD deficiency (hemolytic anemia, Favism) and in severe disorders of the stomach and intestines. Chloroquine can exacerbate the course of psoriasis, porphyria and myasthenia gravis. During long-term use, a full eye examination should be performed periodically every 3 months (examination of visual acuity, fundus, field of view, retinal and corneal assessment) due to the risk of retinopathy. If abnormalities are found, treatment should be discontinued immediately and the patient should be observed, as it is possible to undergo medical changes even after discontinuation of therapy. During chronic treatment with high doses of chloroquine, irreversible retinopathy may occur. When using the drug in patients with a history of epilepsy, be careful. Patients who are taking anticonvulsant or epilepsy therapy should be considered for their potential benefit over risk because rare cases of seizures have been reported with chloroquine. In all patients treated for long periods of time, reflex tests and other neurological tests should be performed every 3 to 6 months to detect muscle weakness early. If irregularities are found, the drug should be discontinued. In long-term patients, the blood picture should be monitored because bone marrow depression may occur in rare cases. Caution should be exercised when chloroquine is used together with medicines that cause blood disorders. If there are disorders not related to the disease process, treatment should be discontinued. Long-term treatment should avoid sun exposure and UV irradiation. Patients should be closely monitored during long-term use of chloroquine due to the risk of cardiomyopathy. It has been shown that chloroquine can cause severe hypoglycaemia, including loss of consciousness, which may be life-threatening for patients who are treated with or without antidiabetic agents. The patient being treated with chloroquine should be informed about the risk of hypoglycaemia and related clinical symptoms. If clinical signs of hypoglycaemia occur during treatment with chloroquine, the patient should be monitored for blood Glucose and, if necessary, revised treatment. In any case, it should be considered whether contagion to the body is a greater risk than the side effects that may occur when using chloroquine. The drug is not intended for use in children under 14 years of age.

Do not use the drug during pregnancy unless the doctor believes that the potential benefit to the mother outweighs the risk to the fetus.Short-term prevention of diarrhea. Infection with dab in pregnant women increases the risk of maternal death, miscarriage, stillbirth and birth of a newborn infant with a low birth weight, which poses a risk of death. During pregnancy, avoid traveling to countries with an increased risk of dermatitis, and if this is not possible, use chloroquine in prophylactic doses.Long-term use of high doses During pregnancy, chloroquids can cause damage to the eyes and hearing of the fetus. Chloroquine is excreted in human milk. If it is used in the prevention of diarrhea, the amount is too small to harm the child, but also insufficient for effective prophylaxis. Therefore, separate preventive measures are necessary for the child. You should not breast-feed during long-term use of high doses of chloroquine in rheumatic disease.

The following may occur: aplastic anemia, agranulocytosis, leukopenia, thrombocytopenia, neutropenia, bone marrow suppression, haemolysis in patients deficient in G-6-PD dehydrogenase, hypersensitivity to light, allergic and anaphylactic reactions, including urticaria or itchy rash, angioneurotic edema, breathing difficulties. convulsions, epileptic seizures, psychosis, anxiety, headache, psychomotor agitation, suicidal thoughts, cases of mania, eye disorders of ciliary body (accommodation disorder, blurred vision - dose-dependent symptoms, transient after treatment), corneal disorder (edema) , punctate or linear turbidity,reduced sensitivity to stimuli, corneal deposits, blurred vision, halo (glow) around light sources, photophobia), eye disorders of the retina (edema, atrophy, pigmentation of the macula and other parts of the retina, changes in the arterioles, retinopathy), field disorders vision, partial or complete loss of vision, double vision, deafness (nerve type), hearing loss in patients with previously existing damage to the hearing system, tinnitus, decreases in blood pressure, changes in the ECG in the form of QRS and T-wave widening, cardiomyopathy, stomach disorders and bowel movements, anorexia, nausea, vomiting, diarrhea, colic, hepatic dysfunction, hepatitis, abnormal liver function tests, hypoglycaemia, graying, alopecia, pruritus, urticaria, rash, skin discoloration, mucous membranes, nails, cutaneous allergic reactions, type changes of lichen planus, psoriasis, rum ń multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, neuromyopathy and myopathy.

Orally. Adults and children over 14 years old.DabPreventive treatment one week before going to the endemic zone, during the period of stay in this zone and for 4 weeks after returning: 500 mg 1 time in a week on the same day of the week. Healing (dermatitis): infectionPlasmodium vivax andPlasmodium ovale: first dose of 1000 mg, after 6 hours 500 mg, on the second day 500 mg, on the third day 500 mg. InfectionPlasmodium falciparum andPlasmodium malariae: first day: first dose 1000 mg, after 6-8 hours 500 mg, on the second day 500 mg, on the third day 500 mg.Amoebiasis and liver abscess: 1000 mg daily (2 times 500 mg) for 2 days, then 500 mg daily (2 times 250 mg) for 2-3 weeks. If necessary, the dosage may be reduced or increased and the treatment repeated.Lupus erythematosus: initially 250 mg 2 times a day for 1-2 weeks, followed by a maintenance dose, usually 250 mg per day.Rheumatoid arthritis: usually 250 mg a day for several weeks. To achieve the maximum effect, several months of treatment are required. If there is no improvement after 6 months of use, the drug should be discontinued. When the medicine is discontinued, the disease may recur. It is advisable to resume chloroquine treatment if there are no ophthalmological counter-indications. Patients with renal insufficiency: in diarrhea in patients with creatinine clearance> 50 ml / min and 10-50 ml / min, the dosage does not change. When the creatinine clearance is> 10 ml / min the dose is reduced by 50%, i.e. the first 500 mg dose, after 6 hours 250 mg, the second day 250 mg, the third day 250 mg. Chloramine should not be used in the prevention of diarrhea in patients with end-stage renal failure. Special dosages are not recommended in elderly patients, but it may be advisable to monitor the patient's health status to determine the optimal therapeutic dose. The drug should be taken after meals. The tablets should not be divided.