Immard

Imard is an antimalarial drug.

Indications Immarda

It is indicated for the treatment of rheumatoid arthritis (also juvenile type), SLE and DLE, as well as dermatitis that develops under the influence of sunlight (or when the symptoms of the disease worsen).

In suppression or treatment of acute malarial attacks caused by Plasmodium vivax, Plasmodium ovale and P.malariae, as well as sensitive strains of Plasmodium falciparum bacteria. Also in radical therapy of malaria caused by sensitive strains of Plasmodium falciparum bacteria.

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Release form

Available in tablets - 10 pieces on a blister plate. One pack contains 3 blisters.

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Pharmacodynamics

Antimalarial components (chloroquine and hydroxychloroquine) have several pharmacological effects that determine their medicinal effect in the process of eliminating rheumatic pathologies (however, the role of these mechanisms remains unclear).

Among the effects provided are interaction with thiol groups, changes in the manifestations of enzyme activity (including phospholipase, protease, NADH-hemoprotein C reductase, and also hydrolase with cholinesterases), DNA synthesis. In addition, normalization of lysosome membranes, slowing down the processes of PG formation, and also phagocytosis with chemotaxis of polymorphonuclear cells. At the same time, they are able to interfere with the process of binding IL-1 monocytes and slowing down the processes of superoxide release with the help of neutrophils.

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Pharmacokinetics

The pharmacokinetic properties, mechanism of action, and metabolism process of hydroxychloroquine are similar to those of chloroquine. After taking the drug, hydroxychloroquine is absorbed quite quickly and almost completely. During testing on volunteers who took a single dose of the drug (400 mg), it was found that the peak level of the substance was within 53-208 ng / ml, and the average value was 105 ng / ml. The average period of time required to obtain the maximum plasma indicator is 1.83 hours.

The half-life varies depending on the time elapsed since consumption, respectively: 5.9 hours (peak value - 10 hours), 26.1 hours (peak value - 10-48 hours), and 299 hours (peak level - 48-504 hours).

Related compounds with decay products are distributed throughout all tissues of the body and excreted mainly in urine. There is testing that showed that after 24 hours from the moment of taking the drug, only 3% of the dosage was excreted.

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Dosing and administration

The medicine should be taken orally. Adults, and at the same time elderly people, need a minimum dosage that gives a medicinal effect (it is not allowed to be higher than 6.5 mg / kg (calculation is based on the ideal, not the actual weight) per day and is usually equal to 200 or 400 mg).

People who are allowed to take 400 mg of the drug per day - at the initial stage, this dosage must be divided into 2 separate doses. If there are no noticeable signs of improvement, it is allowed to reduce it to 200 mg. If the drug is effective, the daily maintenance dosage can be increased to 400 mg.

Children are prescribed the minimum effective daily dosage (no more than 6.5 mg/kg of ideal weight). This is why it is prohibited to prescribe the medicine in 200 mg tablets to children whose ideal weight is less than 31 kg.

During the elimination of malaria attacks - for adults, the dosage is 400 mg on the same days of the week. In childhood (children with a weight of 31+ kg) - the weekly dosage for suppressing an attack is 6.5 mg / kg, but at the same time, regardless of weight, it cannot exceed the dosage recommended for adults.

If circumstances permit, suppressive treatment should be started 2 weeks before travel to an endemic area. If this is not possible, a loading double dose (800 mg) is prescribed for adults and 12.9 mg/kg of body weight (but not more than 800 mg) is prescribed for children, divided into 2 separate doses 6 hours apart. Suppressive therapy should be continued for 8 weeks after leaving the endemic area.

Treatment in case of acute malarial attacks. The initial adult dosage is 800 mg, then 400 mg every 6-8 hours for the next 2 days (in total, 2 g of the active ingredient of the drug). As an effective alternative, a single dose of 800 mg can be used. It can be calculated taking into account the weight (as for a child).

Children with an ideal weight of 31+ kg - the total dosage is 32 mg/kg (but maximum 2 g), it should be taken for 3 days, taking into account the additions described below:

• initial – 12.9 mg/kg (but a single dose is no more than 800 mg);
• 2nd – 6.5 mg/kg (but maximum 400 mg) 6 hours after taking the initial dose;
• 3rd – 6.5 mg/kg (maximum 400 mg) 18 hours after taking the 2nd dose;
• 4th – 6.5 mg/kg (maximum dose 400 mg) 24 hours after taking the 3rd dose.

All tablets must be taken with food or with milk (1 glass).

Hydroxychloroquine can accumulate in the body, which is why it takes several weeks to achieve the medicinal effect, but weak negative reactions can appear quite early. In cases where there is no improvement in the patient's condition during the treatment of rheumatic pathologies for six months, it is recommended to stop the course.

When treating pathologies associated with light intolerance, it is necessary to limit therapeutic courses exclusively to periods of constant exposure to light.

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Use Immarda during pregnancy

It is prohibited to prescribe to pregnant and lactating women.

Contraindications

Among the contraindications:

• intolerance to 4-aminoquinoline derivatives;
• history of retinopathy, liver or kidney pathologies, maculopathy, blood or CNS diseases, and also porphyria;
• people with rare congenital disorders (including galactose sensitivity, lactase deficiency, or glucose-galactose malabsorption);
• children weighing less than 31 kg;
• long-term use in children;
• if the patient has porphyria at the time of treatment.

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Side effects Immarda

Taking pills can cause the development of the following side effects:

• Visual organs: development of nystagmus. Sometimes retinopathy develops together with defects in the visual field, and also with changes in pigmentation, although such symptoms are rare when the required dosages are observed. At the early stage of retinopathy, the process of its development is reversible after stopping the drug. But if this is not done in time, there is a risk that the disease will progress after late cancellation. Changes in the retina may occur, which are initially asymptomatic or manifest as a disorder of color perception or temporal, pericentral or paracentral forms of scotoma. Problems with the cornea (such as clouding or edema) may develop. These disorders are sometimes asymptomatic, but sometimes contribute to the development of blurred vision, as well as the appearance of photophobia or halos. Such disorders may be transient and reversible if therapy is stopped. Loss of visual acuity occurs due to accommodation disorder and depends on the dosage. This disorder is reversible;
• Skin: itching occasionally appears, and in addition to this, skin rashes, skin pigmentation changes along with the pigmentation of the mucous membranes, alopecia occurs, hair becomes discolored, porphyria develops. Such disorders often disappear when the drug is discontinued. A bullous rash may appear with isolated observations of the development of erythema multiforme and malignant exudative erythema, as well as photophobia. In the cases described separately, Ritter's dermatitis appeared. Rarely, a pustular rash (generalized exanthematous form) of an acute type develops - it should be differentiated from psoriasis, although the active substance of the drug can provoke an exacerbation of this pathology. It is possible that this is due to leukocytosis and an increase in temperature. When the drug is discontinued, the disorders are often reversible;
• Digestive system organs: diarrhea, severe nausea, and also abdominal pain and anorexia; vomiting is occasionally observed. These symptoms disappear after reducing the dosage or stopping the drug;
• organs of the nervous system: the appearance of noises in the ears, severe dizziness, sharp headaches, feelings of nervousness, emotional instability. In addition, hearing loss, convulsions, ataxia, toxic psychoses, the occurrence of nightmares and suicidal behavior;
• Musculature and skeleton: the appearance of progressive muscular dystrophy or neuromyopathy, which cause the development of weakness and subsequent atrophy of the proximal muscles. This pathology is reversible when the drug is discontinued, but full recovery may occur only after several months. The development of moderate sensory disturbances, pain in the shins, suppression of tendon reflexes, and in addition to this, abnormal nerve conduction is possible;
• CVS organs: cardiomyopathy occurs sporadically. If problems with conduction arise (the so-called bundle branch block) or hypertrophy of each ventricle begins, chronic poisoning may have begun. If the drug is discontinued, conduction may be restored;
• organs of the hematopoietic system: bone marrow function is occasionally suppressed; anemia (or its aplastic form), thrombocytopenia or leukopenia, and also hemolysis in people with G6PD deficiency develop occasionally. The active component of the drug can contribute to the exacerbation of porphyria or worsening of the course of this disease;
• hepatobiliary disorders: changes in the values of functional liver tests; there is information about the development of fulminant liver failure;
• intolerance reactions: allergic reactions, including Quincke's edema, urticaria, bronchospasm. In addition, skin itching and redness;
• Other: weight loss.

Overdose

An overdose of 4-aminoquinolines is very dangerous for infants, because even 1-2 g of this substance can cause death.

Manifestations include: visual disturbances, severe headaches, seizures, cardiac conduction disturbances and, with them, rhythm disturbances (including prolongation of the QT interval), cardiovascular collapse, development of hypokalemia, ventricular fibrillation and ventricular tachycardia. Sudden (sometimes fatal) cardiac arrest with breathing may also occur.

Since such a reaction may occur immediately after taking a large dose of the drug, it is necessary to immediately perform therapy aimed at eliminating the signs of the disorder. Gastric lavage and induction of vomiting will be required. Taking activated carbon in an amount that is no less than 5 times greater than the amount of the drug taken can prevent its subsequent absorption (when administering activated carbon into the stomach via a probe immediately after the lavage procedure, no later than half an hour after taking the drug).

In case of overdose, the option of administering diazepam parenterally may be considered. There is evidence that this drug is capable of reducing the symptoms of cardiotoxicity caused by chloroquine.

If necessary, procedures are carried out to maintain respiratory function, and anti-shock treatment is also performed.

Interactions with other drugs

Hydroxychloroquine sulfate can increase plasma digoxin levels, which is why people taking these drugs concomitantly need to constantly monitor serum digoxin levels.

Hydroxychloroquine sulfate can also interact with the substance chloroquine. When combined, the following effects are possible: increased blocking properties of aminoglycosides relative to the myoneural synapse; slowing down of substance metabolism under the influence of cimetidine, due to which the level of antimalarial drugs in the plasma increases; antagonism relative to the properties of pyridostigmine with neostigmine; a decrease in the number of antibodies formed (as a reaction to the implementation of primary immunization - intradermal human vaccine (diploid cell) against rabies).

Antacids also have a similar effect to chloroquine – they weaken the absorption of hydroxychloroquine. Because of this, when combining such drugs, it is necessary to observe at least a 4-hour interval between their administrations.

Since hydroxychloroquine can enhance the properties of antidiabetic drugs, when they are combined, it may be necessary to reduce the dosage of insulin or hypoglycemic drugs.

Halofantrine prolongs the QT interval, so it cannot be combined with other drugs that can provoke cardiac arrhythmia (this list includes hydroxychloroquine). In addition, the likelihood of developing ventricular arrhythmia increases with the combined use of the drug with other arrhythmogenic drugs (including moxifloxacin with amiodarone).

The combination of Immard with cyclosporine causes an increase in its plasma levels.

Hydroxychloroquine is able to lower the seizure threshold. When combined with other antimalarial drugs that also lower the seizure threshold (such as mefloquine), the likelihood of seizures increases.

Combination with anticonvulsants may lead to a decrease in their effectiveness.

Studies conducted to study the interaction of single-dose combinations of chloroquine and praziquantel have demonstrated a decrease in the bioavailability of the latter. There is no information on whether the same effect could develop if hydroxychloroquine were combined with praziquantel. If we extrapolate this information, given that the pharmacokinetics and structure of chloroquine and hydroxychloroquine are very similar, we can conclude that the development of such an effect should be expected.

Combined administration with agalsidase may theoretically provoke a slowdown in the activity of α-galactosidase inside cells.

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Storage conditions

The medicine is stored under standard conditions for medicines, inaccessible to children. Temperature values are no more than 25°C.

Shelf life

Imard is permitted to be used for 2 years from the date of release of the drug.