Immard

Immar is an antimalarial drug.

[1]

Indications of the immarda

It is indicated for the elimination of rheumatoid arthritis (also of the juvenile type), SLE and DKV, and in addition to dermatitis that has developed under the action of sunlight (or with worsening manifestations of the disease).

When suppressing or treating acute malarial attacks, provoked plasmodium Vivax, Plasmodium oval and P.malariae, and in addition sensitive strains of bacteria Plasmodium falsiparum. Also with the radical therapy of malaria, which is provoked by sensitive strains of bacteria plasmodium falciparum.

[2], [3]

Release form

Produced in tablets - 10 pieces on a blister plate. In one bundle - 3 blisters.

[4], [5]

Pharmacodynamics

Antimalarial components (chloroquine, as well as hydroxychloroquine) have several pharmacological effects that cause their medicinal effect in the process of elimination of rheumatic pathologies (but the role of these mechanisms remains unclear).

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

[6], [7], [8], [9], [10], [11], [12], [13], [14], [15]

Pharmacokinetics

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

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

Related compounds with the products of decay are distributed within all tissues of the body, and excreted mainly in the urine. There is a test, which showed that after 24 hours from the time of drug administration only 3% of the dosage was withdrawn.

[16], [17], [18], [19], [20], [21], [22], [23], [24]

Dosing and administration

The medicine should be consumed orally. Adults, and together with this elderly people, need a minimum dosage, which gives a medicinal effect (it is not allowed to be above 6.5 mg / kg (the calculation is based on the ideal and not actually available weight) per day and is usually 200 or 400 mg).

People who are allowed to consume 400 mg of medicine per day - at the initial stage this dosage should be divided into 2 separate receptions. If there are no noticeable signs of improvement, it is allowed to reduce it to 200 mg. If the drug works effectively, you can increase the daily maintenance dosage to a value of 400 mg.

Children are prescribed a minimally effective daily dosage (no more than 6.5 mg / kg of ideal weight value). It is because of this that it is forbidden to prescribe medication in 200 mg tablets to children whose ideal weight is less than 31 kg.

During elimination of attacks of malaria - for adults the dosage is equal to 400 mg on the same days of the week. In childhood (children weighing 31+ kg), a weekly dosage for an attack is 6.5 mg / kg, but it can not exceed the recommended adult dosage, regardless of weight.

If circumstances permit, overwhelming treatment should be started 2 weeks before the trip to the area of endemia distribution. In the absence of such an opportunity for adults, a double loading dose is prescribed (800 mg), and for children - 12.9 mg / kg weight (but not more than 800 mg), which is divided into 2 separate doses with an interval of 6 hours. Suppressive therapy should be continued 8 weeks after the person has left the endemic area.

Treatment in case of acute malarial attacks. The size of the initial adult dosage is 800 mg, followed by 400 mg every 6-8 hours for the next 2 days (on the whole, 2 g of the active ingredient of the drug is obtained). As an effective alternative, you can use a single dose of LS at a dosage of 800 mg. You can count on it, given the weight (as for the 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 with a single dose of no more than 800 mg);
• 2 nd - 6.5 mg / kg (but with a maximum of 400 mg) 6 hours after the use of the initial dosage;
• 3rd - 6.5 mg / kg (maximum 400 mg) 18 hours after the use of the 2nd dosage;
• 4th - 6.5 mg / kg (maximum size 400 mg) 24 hours after the use of the 3rd dosage.

All tablets should be consumed with food or by washing them with milk (1 glass).

Hydroxychloroquine is able to accumulate in the body, so several weeks are needed to get the drug, but weak negative reactions can appear quite early. In the case when in the treatment of rheumatic pathologies for six months there is no improvement in the patient's condition, it is recommended to stop the course.

In the treatment of pathologies associated with intolerance to light, it is required to limit therapeutic courses exclusively to periods of constant exposure to light.

[30], [31]

Use of the immarda during pregnancy

It is forbidden to appoint pregnant and lactating women.

Contraindications

Among the contraindications:

• intolerance to 4-aminoquinoline derivatives;
• presence in the anamnesis of retinopathy, hepatic or renal pathologies, maculopathy, blood diseases or CNS, and in addition porphyria;
• people with rare congenital disorders (among them sensitivity to galactose, lactase deficiency or impaired absorption of glucose-galactose);
• children weighing less than 31 kg;
• prolonged use in children;
• with the patient's porphyria at the time of treatment.

[25], [26], [27], [28]

Side effects of the immarda

The taking of tablets can cause the development of such side effects:

• visual organs: the development of nystagmus. Sometimes the appearance of retinopathy with the development of defects in the field of vision is observed, and besides this, with a change in the pigmentation, although such symptoms are rarely observed when the required dosages are observed. At an early stage of retinopathy, the process of its development is reversible after discontinuation of drug use. But if this is not done on time, there is a risk that the disease will progress after the late cancellation. There may be changes in the retina that initially asymptomatic or manifest as a disorder of perception of flowers or temporal, pericentral or paracentral forms of cattle. Possible development of problems with the cornea (such as opacification or edema). These disorders are sometimes asymptomatic, but sometimes contribute to the development of blurred vision, and in addition to the appearance of photophobia or halos. Such violations can be transient and reversible if therapy is discontinued. The loss of visual clarity arises from the disorder of accommodation and depends on the dosage. This disorder is reversible;
• skin: occasionally there is an itch, and besides this rash on the skin, skin pigmentation changes along with the pigmentation of the mucous membranes, alopecia occurs, the hair becomes discolored, porphyria develops. Such disorders often disappear when drugs are withdrawn. There may appear a bullous type rash with single observations of the development of erythema multiforme and malignant exudative erythema, and also photophobia. In the cases described separately, Ritter dermatitis appeared. Occasionally, 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 aggravation of this pathology. It is possible that this is due to leukocytosis and an increase in temperature. When a drug is abolished, violations are often reversible;
• organs of the digestive system: diarrhea, severe nausea, and in addition abdominal pain and anorexia; occasionally there is vomiting. These manifestations occur after a reduction in dosage or withdrawal of drugs;
• organs of the National Assembly: the appearance of noise in the ears, severe dizziness, severe headaches, feelings of nervousness, instability of an emotional nature. In addition, hearing loss, seizures, ataxia, toxic psychosis, the occurrence of nightmares and suicidal behavior;
• musculature and skeleton: the emergence of progressive muscular dystrophy or neuromyopathy, which causes the development of weakness and subsequent atrophy of the proximal musculature. This pathology is reversible with the withdrawal of the medicine, but a full recovery can come only after a few months. Perhaps the development of moderate sensory disorders, pain in the legs, suppression of tendon reflexes, and in addition to this nerve conduction anomalous type;
• organs of the CCC: there is a single occurrence of cardiomyopathy. If there were problems with conduction (the so-called blockade of the legs of the bundle of the Hisnus) or the hypertrophy of each ventricle began, it is possible that chronic poisoning began. In the case of cancellation of drugs, conductivity can be restored;
• organs of the hematopoiesis system: occasionally there is a suppression of the medullar function; anemia develops (either its aplastic form), thrombocyto- or leukopenia, and in addition hemolysis in people with G6PD deficiency. The active ingredient of the drug may exacerbate porphyria or worsen the course of the disease;
• hepatobiliary disorders: a change in the values of functional hepatic samples; there is information on the development of fulminant form of liver failure;
• reactions of intolerance: allergic manifestations, including Quincke edema, urticaria, bronchial spasm. In addition, itching and redness of the skin;
• other: weight loss.

[29]

Overdose

Overdose of 4-aminoquinolines is very dangerous for babies, because for them the use of this substance even in the amount of 1-2 g can lead to death.

Among the manifestations are: visual disturbance, severe headaches, seizures, cardiac conduction disorder, and at the same time rhythm (including QT interval prolongation), cardiovascular collapse, development of hypokalemia, ventricular fibrillation and ventricular tachycardia. A sudden (sometimes fatal) cardiac arrest with breathing may also occur.

Since such a reaction may appear immediately after the use of a large dose of drugs, it is required to immediately perform therapy aimed at eliminating the signs of the disorder. It will require gastric lavage and induction of vomiting. The intake of activated carbon in a size that is not less than 5 times the amount of medicines consumed can prevent its subsequent absorption (when activated carbon is injected into the stomach via a probe immediately after the rinsing procedure, no later than half an hour after the drug is consumed).

In case of an overdose, the variant of administering a diazepam substance by the parenteral method may be considered. There is evidence that this drug can weaken the symptoms of cardiotoxicity, provoked by chloroquine.

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

Interactions with other drugs

Hydroxychloroquine sulphate is able to increase the digoxin plasma index, which means that people taking these drugs simultaneously need to constantly monitor the serum level of digoxin.

Hydroxychloroquine sulphate is also capable of interacting with chloroquine. When combined, the following effects are possible: increased blocking properties of aminoglycosides with respect to the myoneural synapse; the slowing down of the metabolism of the substance under the action of cimetidine, which increases the level of antimalarial drugs inside the plasma; antagonism with respect to the properties of pyridostigmine with neostigmine; decrease in the number of antibodies formed (as a reaction to the performance of immunization of the primary type - intradermal human vaccine (diploid cell) against rabies).

Similar to chloroquine, antacids also have an effect - they weaken the absorption of hydroxychloroquine. Because of this, when combining such drugs it is necessary to observe a minimum 4-hour interval between their methods.

Since hydroxychloroquine is capable of increasing the properties of antidiabetic drugs, a combination of them may require a decrease in the dosage of insulin or hypoglycemic drugs.

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

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

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

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

Studies conducted to study the interaction of once-combined chloroquine and praziquanthal, showed a decrease in the bioavailability of the latter. There is no information as to whether it is possible to develop the same effect in the case of combination with hydroxychloroquine with praziquanthal. If we extrapolate this information, given that the pharmacokinetics and structure of chloroquine with hydroxychloroquine are very similar, we can conclude that the development of such an impact should be expected.

Combined therapy with agalicidase can theoretically provoke a slowdown in the activity of α-galactosidase within cells.

[32], [33], [34]

Storage conditions

The medicine is stored in standard conditions for medicines, inaccessible to children. Temperature values - no more than 25 ° С.

Shelf life

Immar is allowed to use within 2 years from the date of release of the medicinal product.

[35]