Note: All doses are for hydroxychloroquine sulfate, and are not equivalent to base.

Inside, during meals or with a glass of milk.

RA treatment. Hydroxychloroquine has cumulative activity. For the manifestation of its therapeutic effect, several weeks of taking the drug are required, while side effects can appear relatively early. The required therapeutic effect develops after several months of taking the drug. If there is no objective improvement in the patient's condition within 6 months of taking hydroxychloroquine, the drug should be discontinued.

Adults (including the elderly) should take the minimum effective dose. They should not exceed 6.5 mg / kg / day (calculated according to the "ideal" body weight, not real body weight) and can be either 200 or 400 mg / day.

In patients capable of taking 400 mg daily

Initially - 400 mg daily, in divided doses. When an obvious improvement is achieved, the dose can be reduced to 200 mg. With a decrease in the effect, the maintenance dose can be increased to 400 mg.

Children. The minimum effective dose should be used. The dose should not exceed 6.5 mg / kg (based on the "ideal" body weight). Therefore, 200 mg tablets are not suitable for children with an “ideal” body weight less than 31 kg.

Use of Plaquenil for combination therapy of RA. Plaquenil can be used safely in combination with GCS, salicylates, NSAIDs, methotrexate and other second-line therapeutic agents. After several weeks of using the drug Plaquenil, the doses of corticosteroids and salicylates may be reduced or these drugs may be discontinued. Doses of GCS should be reduced gradually every 4-5 days: the dose of cortisone - no more than 5-15 mg, the dose of hydrocortisone - no more than 5-10 mg, the dose of prednisolone and prednisone - no more than 1-2.5 mg , the dose of methylprednisolone and triamcinolone - no more than 1–2 mg and dexamethasone - no more than 0.25–0.5 mg.

SLE treatment. The initial average dose in adults is 400 mg 1 or 2 times a day. It should be administered over several weeks or months, depending on the patient's response. For long-term maintenance therapy, it is sufficient to use the drug in a lower dose - from 200 to 400 mg.

Malaria treatment

Prevention of acute attacks of malaria caused by P. malariae and susceptible strains of Plasmodium falciparum

Adults - 400 mg weekly on the same day of the week.

For children, the weekly dose is 6.5 mg / kg (the "ideal" body weight is taken for the calculation), however, regardless of body weight, it should not exceed the adult dose.

If conditions permit, then preventive therapy should be started 2 weeks before entering the endemic area. If this is not possible, then an initial double (loading) dose can be prescribed: adults - 800 mg, children - 12.9 mg / kg of "ideal" body weight (but not more than 800 mg), divided into two doses with a 6-hour interval. Prophylactic treatment should be continued for 8 weeks after leaving the endemic area.

Treatment of acute attacks of malaria

For adults, an initial dose of 800 mg is followed by a dose of 400 mg every 6 or 8 hours, and then 400 mg every 2 consecutive days (a total of 2 g of hydroxychloroquine sulfate).

Alternative treatment: A single dose of 800 mg has also been proven to be effective.

Doses for adults can also be calculated based on “ideal” body weight, similar to calculating doses for children (see below).

For children, a total dose of 32 mg / kg of "ideal" body weight (but not higher than 2 g) is prescribed for 3 days as follows:

first dose - 12.9 mg / kg (single dose not more than 800 mg); the second dose is 6.5 mg / kg (no more than 400 mg) 6 hours after the first; the third dose is 6.5 mg / kg (not more than 400 mg) 18 hours after the second dose; the fourth dose is 6.5 mg / kg (not more than 400 mg) 24 hours after the third dose.

Radical treatment of Plasmodium malariae and Plasmodium vivax malaria

For the radical treatment of malaria caused by Plasmodium malariae and Plasmodium vivax, the simultaneous administration of 8-aminoquinolone derivatives is necessary.

Contraindications

hypersensitivity to 4-aminoquinoline derivatives;

retinopathy;

pregnancy (see "Application during pregnancy and lactation");

hereditary lactose intolerance, lactase deficiency, galactosemia or glucose / galactose malabsorption syndrome (due to the presence of lactose in the preparation).

children's age, if long-term therapy is necessary (children have an increased risk of developing toxic effects);

children under 6 years of age (200 mg tablets are not intended for children with "ideal" body weight less than 31 kg).

Carefully:

visual disturbances (decreased visual acuity, impaired color vision, narrowing of the visual fields), the simultaneous administration of drugs that can cause adverse ophthalmic reactions (risk of progression of retinopathy and visual disturbances);

hematological diseases (including a history);

severe neurological diseases, psychosis (including a history);

late cutaneous porphyria (risk of exacerbation), psoriasis (risk of increased skin manifestations of the disease), concomitant use of drugs that can cause skin reactions;

renal failure and / or hepatic failure, hepatitis, concomitant use of drugs that can adversely affect liver and / or kidney function (in severe renal or hepatic impairment, the dose should be selected under the control of plasma concentrations of hydroxychloroquine);

deficiency of glucose-6-phosphate dehydrogenase;

severe gastrointestinal diseases;

hypersensitivity to quinine (the possibility of cross-allergic reactions).

Application during pregnancy and lactation

Hydroxychloroquine crosses the placenta. Limited data are available for its use in pregnancy. It should be noted that 4-aminoquinolines in therapeutic doses can cause intrauterine damage to the central nervous system, incl. the auditory nerve (hearing and vestibular disorders, congenital deafness), retinal hemorrhages and abnormal retinal pigmentation. Therefore, the use of hydroxychloroquine during pregnancy should be avoided, unless the potential benefit to the mother outweighs the risk to the fetus.

You should carefully weigh the need to use the drug during breastfeeding, because it has been shown that it is excreted in small quantities in breast milk, and young children are especially sensitive to the toxic effects of 4-aminoquinolines.

On the part of the organ of vision: may develop, although rarely, retinopathy with changes in pigmentation and defects in the visual fields. In the early form, these events are usually reversible after discontinuation of hydroxychloroquine. If the condition remains undiagnosed and retinal lesions continue to develop further, there may be a risk of their progression even after drug withdrawal.

Retinal changes may initially be asymptomatic, or manifest as paracentral or pericentral scotomas, transient scotomas, and color vision disorders.

Changes in the cornea including edema and opacity are possible. They may be asymptomatic or cause visual disturbances such as halos, blurred vision, or photophobia. When treatment is discontinued, these changes may reverse.

There may also be visual impairments associated with accommodation disorders, which are dose-dependent and reversible.

From the side of the skin: sometimes there are skin rashes; itching, changes in skin and mucous membranes pigmentation, hair discoloration and alopecia are also described. These changes usually resolve quickly after stopping treatment. The development of bullous rash has been reported, including very rare cases of erythema multiforme and Stevens-Johnson syndrome, photosensitivity, and isolated cases of exfoliative dermatitis.

Very rare cases of acute generalized exanthematous pustulosis (OGEP) must be distinguished from psoriasis, although hydroxychloroquine can also exacerbate psoriasis. OGEB can be accompanied by fever and hyperleukocytosis. After discontinuation of the drug, the outcome is usually favorable.

From the gastrointestinal tract: nausea, diarrhea, anorexia, abdominal pain and rarely vomiting. These symptoms usually resolve immediately after dose reduction or drug withdrawal.

From the side of the hepatobiliary system: with prolonged use in large doses, the development of hepatotoxic effects is possible. There are reports of isolated cases of liver dysfunction and several cases of sudden onset of liver failure.

From the side of the central nervous system: infrequently - dizziness, tinnitus, hearing loss, headache, irritability, emotional instability, psychosis, convulsions, muscle weakness, ataxia.

From the peripheral nervous system and muscles: there have been cases of skeletal muscle myopathy or neuromyopathy leading to progressive weakness and atrophy of the proximal muscle groups. Myopathy may be reversible after discontinuation of the drug, but it may take several months for full recovery. At the same time, weak sensory changes, suppression of tendon reflexes and a decrease in nerve conduction can be observed.

From the side of the cardiovascular system: there are rare reports of the development of cardiomyopathy.

Chronic cardiac toxicity may be suspected when conduction abnormalities (bundle branch block / AV conduction abnormalities) or bilateral ventricular hypertrophy are found. When the drug is discontinued, the reverse development of these changes is possible.

From the side of the hematopoietic organs: cases of inhibition of bone marrow hematopoiesis were rarely observed. Rare cases of anemia have been reported, incl. aplastic, agranulocytosis, leukopenia and thrombocytopenia.

Hydroxychloroquine can provoke or exacerbate porphyria.

From the immune system: urticaria, angioedema, bronchospasm.

Digoxin. It was reported that hydroxychloroquine is able to increase the plasma concentration of digoxin, therefore, in order to avoid the development of glycosidic intoxication while taking these drugs, it is necessary to reduce the dose of digoxin under the control of its plasma concentrations.

Medications used to treat diabetes. Because hydroxychloroquine can potentiate the effects of insulin and oral hypoglycemic agents, it may be necessary to reduce the dose of these hypoglycemic agents when starting hydroxychloroquine.

Antacids. May decrease absorption of hydroxychloroquine. Therefore, with the simultaneous use of antacids and hydroxychloroquine, the interval between their intake should be at least 4 hours.

In hydroxychloroquine, the following interactions with other drugs that have been described for chloroquine, but have not yet been observed with hydroxychloroquine, cannot be ruled out.

Aminoglycosides. Potentiation of their direct blocking action on neuromuscular transmission.

Cimetidine. Suppresses the metabolism of antimalarial drugs, which can lead to an increase in their plasma concentrations and increase the risk of developing their side effects, especially toxic ones.

Neostigmine and pyridostigmine. Antagonism of action.

Any intradermal human diploid cell rabies vaccine. Reducing antibody production in response to primary immunization with intradermal human diploid cell rabies vaccine.

An overdose of 4-aminoquinolines is especially dangerous in children, even 1–2 g of the drug can be fatal.

Symptoms: headache, visual disturbances, collapse, seizures, hypokalemia, rhythm and conduction disturbances, followed by cardiac arrest and respiratory arrest.

Treatment: because these effects can develop very quickly after taking a large dose of the drug, in these cases, appropriate measures should be taken immediately. Induction of vomiting or gastric lavage through a tube should be performed immediately. To slow down absorption - the appointment of activated charcoal in a dose at least 5 times higher than the taken dose of the drug. Parenteral administration of diazepam is advisable (a decrease in the cardiotoxicity of chloroquine against its background is described).

If necessary, artificial lung ventilation and anti-shock therapy should be carried out.

After the relief of symptoms of an overdose, continued medical supervision is required for at least 6 hours.