Plafvenil: instructions for use, price, analogs, reviews, composition

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Plaquenil is used in the treatment and prevention of malaria, as well as with systemic ailments and diffuse connective tissue diseases. The drug belongs to the vital

Plakvenil - the most famous of the existing antimalarial drugs, which is on the list of vital and essential drugs. This is due to the fact that plakvenil quickly destroys the pathogens of malaria, and with what has other effects: suppresses the excessive immune reaction.

Features of the preparation

Plakvenil - Plaquenil¸ or sulfate hydroxychlorine, a derivative of 4-aminoquinoline. Its main medicinal effect is the ability to suppress all erythrocyte forms of plasmodia. The drug suppresses pathogens of three-day malaria, a four-day, oval and some tropical species.

However, only this action of plaquenyl is not exhausted: it has a specific and nonspecific anti-inflammatory effect, which has widened the scope of its application.

Hydroxychlorine has the following properties:

• has an antiprotozoal effect - the drug suppresses the activity of protozoa that act as pathogens of various infections;
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• has a moderate immunosuppressive effect - in autoimmune diseases - systemic lupus, discoid, some tissue sites are attacked by the body's immune system, as mistakenly mistaken for foreign ones. Plaquenil suppresses this excessive reaction;
• anti-inflammatory effect is more widely used - hence the use of the drug in many types of joint pain, where conventional non-steroidal agents are weak.

Plaquenil( photo)

Medicinal forms

Plaquenil is available only in the form of tablets - biconvex, white, film membrane. On one side of the tablet there is an inscription HCQ, on the other - 200.

In a blister 10 pieces, in a standard carton box - 6 blisters. It is intended only for oral administration strictly according to the doctor's prescription.

Composition

The preparation has only one form of release with a specified composition:

• active ingredient - 200 mg of hydroxychlorinate sulfate in each tablet;
• excipients - Macrogol 4000, corn starch, lactose monohydrate, magnesium stearate, titanium dioxide.

Price of Plaquenel

The cost of 1 medicine package varies from 1076 to 2313 r.

Pharmacological action of

The pharmacological effect of plaquenew is based on the possibility of inhibiting the erythrocyte forms of practically all plasmodia. Strange as it may seem, the precise mechanism of its effect has not been determined so far, although the preparation regularly performs its function. It is assumed that hydroxychlorine reduces the activity of certain enzymes - phospholipase, cholinesterase, and thereby stabilizes the lysosome membranes. In addition, the substance inhibits the formation of prostaglandins, which reduces pain.

Farmakodinamika

Hydroxychloride sulphate inhibits gametes and erythrocyte forms - asexual, pathogens of malaria. Under its action gametes from the blood disappear completely. Thus, the drug prevents malaria attacks and treats if the pathogens of the disease are strains sensitive to the action of chlorine. Also, the drug is used if the disease is caused by chlorine-resistant strains of Plasmodium falciparum.

Relative to chlorine-resistant strains, the drug, alas, is powerless. In addition, plakvenil does not affect non-erythrocyte forms and in such cases can not be prescribed as a means for prevention.

The use of the drug for other ailments is due to the following abilities of the drug:

• suppresses the synthesis and work of enzymes that provoke the disintegration of cartilaginous tissue. Hence its use as a medicine for arthritis;
• suppresses the production of cytokines - the latter activate the immune system, which leads to the appearance of autoimmune processes, that is, damage to one's own tissues;
• inhibits the synthesis of prostaglandins - these substances are actively produced by inflammation and intensify painful sensations;
• A very important feature of plaquenyl is the ability to suppress rheumatoid factors - the synthesis of immunoglobulins. The latter are perceived by the body as alien and provoke the production of antigens;The
• drug inhibits the activity of lymphocytes, also involved in immune responses.

Pharmacokinetics

Hydroxyschlorine is absorbed almost completely by the gastrointestinal tract and at a high rate. When taking the medicine - 400 mg, the maximum concentration of the substance in the blood was reached by a healthy person after 1.8 hours.

In the liver, the substance is converted to ethylated metabolites. Distributed gidroksichlorin and its decay products across all tissues, accumulates in the kidneys, liver, lungs and melanin-containing cells of the skin and eyes. This feature determines the effect of the drug on vision.

The bioavailability of the drug is 45%.The average value in plasma is maintained depending on the time of reception:

• 5.9 hours - after reaching a maximum concentration of up to 10 hours;
• 26.1 hours - when the maximum is reached from 10 to 48 hours;
• 299 - from 48 to 509 hours.

The drug in an unchanged form, like the products of disintegration, is excreted in the urine and in some quantity with bile. Output is slow - for a day the withdrawal is 3% of the dose. For complete withdrawal of the drug from the blood takes up to 50 days, from the plasma - up to 30 days.

Indications

Plaquenyl is prescribed for a number of skin and autoimmune diseases, as the substance inhibits the activity of the immune system.

• Lupus erythematosus - systemic and discoid, in which connective tissue and its derivatives, as well as vessels, are affected.
• Rheumatoid arthritis - including associated with advanced age, a systemic ailment of connective tissue with a similar autoimmune disease mechanism.
• Rheumatism of the heart.
• Systemic scleroderma.
• Malaria - excluding those forms of the disease, where the pathogens are resistant to the action of chlorines strains. It is used both as a therapeutic and as a preventive agent.
• Skin diseases - in particular those caused or exacerbated by exposure to the sun. These are all kinds of photodermatisms: sunlight pruritus, photophytodermatitis, solar urticaria, light eczema, phototoxic dermatitis and so on. They are related to the excessive sensitivity of the skin to the action of ultraviolet. Instead of the usual mechanism of melanin production under the action of sunlight, with such ailments, a variety of unexpected and unexpected chemical reactions occur, leading to skin damage.

Instruction for use

The drug is prescribed only by the attending physician and only after a thorough examination. Hydroxychlorine has a number of serious side effects and affects the patient's condition during the course of treatment. Self-diagnosis and dose determination in this case are fraught with extreme complications.

Adult

Plaquenyl for the therapeutic effect should accumulate, so the therapeutic effect of the drug manifests itself only after a few weeks - up to 4. Side effects can affect faster, so the optimal dosage is chosen by the attending physician. If the therapeutic effect has not been achieved within half a year, the medicine is canceled.

• The purpose of determining the dosage is to select the minimum dose that has a therapeutic effect. For adults and elderly patients, the dose is calculated based on the ideal body weight, not the actual weight. The maximum allowable per day is 6.5 mg per kg of body weight, that is, the dose can be 200 and 400 mg per day.

• With an acute attack of malaria, the initial dose is also 800 mg. After 6 or 8 hours 400 mg are administered, and in the next 2 days 400 mg. For the radical treatment of some forms of malaria, the use of 8-aminoquinoline derivatives is also required.
• For prophylaxis and prescribe 400 mg adults weekly, always on the same day of the week. Therapy starts 2 weeks before entering the danger zone and continues after 8 more weeks after the departure. If you do not have the opportunity to prepare beforehand, you will be given a double dose of 800 mg, which is taken in 2 stages with a 6-hour interval, and then drink according to the scheme described above.
• In the treatment of lupus erythematosus, the initial dose reaches 400 mg 1 or 2 times a day. Depending on the reaction of the body, this dose can be used from several weeks to months. With maintenance therapy, the daily dose is 400 or 200 mg.

Plakvenil taken with food. It is recommended to drink the medicine with 200 ml of milk. It is possible to administer hydroxychlorine intravenously or intramuscularly, but this method is rarely used.

For children, newborns

As a rule, plaquenyl is prescribed for children in the prevention of malaria or its treatment. However, the drug is allowed to use in the treatment of skin diseases and systemic ailments.

• It is important to determine the minimum effective therapeutic dose. Calculate it based on the ideal, not the actual body weight. The daily amount can not exceed 6.5 mg per kg of weight, that is, children weighing up to 31 kg tablets in 200 mg are not suitable.
• In the prevention of malaria, a weekly dose for a child is 6.5 mg / kg of body weight based on ideal weight. Begin prevention 2 weeks before entering the endemic zone. If this is not possible, a shock dose of 12.9 mg / kg, but not more than 800 mg per day, is prescribed. Prophylactic reception is continued 8 weeks after leaving the zone.
• In acute malaria, the total dose of 32 mg / kg - but not exceeding 2 g, is taken according to the scheme:
  • 12.9 mg / kg - the initial dose, but not more than 800 mg;
  • after 6 hours take the medicine at a rate of 6.5 mg / kg, but not more than 400 mg;
  • third reception, calculated in the same way, after 18 hours;
  • the fourth dose is 6.5 mg / kg, but no more than 400 mg is taken 24 hours later.

In pregnancy and lactation

Hydroxychloric sulphate passes through the placenta and is found in small amounts in breast milk. Unfortunately, the toxic effect of 4-aminoquinoline is high, so if you need treatment for breast-feeding, you need to opt out.

Data on the effects of the substance on the fetus are limited. It is known that hydroxychlorine is capable of provoking damage to the auditory nerve, vestibular apparatus, causing hemorrhage in the retina, a violation in the pigmentation of the iris, and so on. In pregnancy, the use of the drug is justified only when the benefits of its use exceed the danger.

Contraindications

Plaquenyl has a lot of contraindications, as it creates a significant burden on the kidneys and liver. In addition, hydroxychlorine causes and significantly enhances visual disorders.

The main direct contraindications include:

• pregnancy - it is allowed to be used only for acute need;
• excessive sensitivity to 4-aminochlorins and its derivatives;
• hereditary lactose intolerance, as well as deficiency of this enzyme, galactosemia and others. The restriction is due to lactose in the composition of the drug;
• insufficient weight - for children weighing less than 31 kg, that is, almost up to 6 years, the drug is not prescribed;
• retinopathy - affection of the retina;
• children's age - is a contraindication, if long-term therapy is needed, since the risk of toxic effects is too high.

Very carefully, plaquenil should be prescribed for eye disorders:

• reduction in severity;
• violation of light perception;
• narrowing of the visual field;
• when using drugs that also provoke ophthalmic manifestations.

There are a number of pathologies in which the use of the drug may not be appropriate. In each such case, the physician should evaluate the actual risks and benefits of using hydroxylchlorine:

• severe disorders of the gastrointestinal system;
• skin porphyria - there is a risk of exacerbation;
• renal or hepatic insufficiency, including on the background of taking nephrotoxic drugs. If necessary, the dose is selected by monitoring the concentration of hydroxychlorin in the plasma;
• hematologic diseases, including anemia;
• lack of glucose-6-phosphate dehydrogenase;
• high overall sensitivity to quinine;
• is not prescribed for strong psychiatric disorders - psychoses, for example;
• psoriasis - skin manifestations can be significantly intensified. Also, use caution when taking a medication that can cause skin rashes.

Side effects of

The latter may appear much earlier than the therapeutic effect of the drug, which, of course, causes distrust of the drug. But if the side effects are not pronounced and do not pose a danger, they should be neglected for the sake of curing from much more serious illnesses.

• The greatest concern is the change in the organs of vision: some of them pass asymptomatically. If the transformation has not crossed a certain border, they disappear after the end of the course of treatment. However, the risk of visual defects progress remains. There is a clouding of the cornea, swelling, falls visual acuity, there are halos and a fear of light. Most often, the changes are reversible.
• Skin rashes, itching, discoloration, discoloration of the hair are possible. These symptoms disappear after the course is over. In rare cases, an acute exanthematous pustulosis is observed, which must be distinguished from psoriasis, since the manifestations of the latter also increase.
• From the digestive tract may manifest anorexia, diarrhea, pain, sometimes vomiting. With a reduction in dose or withdrawal symptoms go away.
• Infrequent dizziness, hearing loss, tinnitus, headaches. There may be weakness, atrophy of muscle groups, suppression of tendon reflexes. All changes are reversible.
• Changes in the cardiovascular system - cardiomyopathy, conduction disturbance, and possibly oppression of hematopoiesis are much less frequent. The cases of development of anemia, leukopenia, thrombocytopenia have been recorded.

Special instructions for

Most side effects with taking medication are reversible. However, if any of them threatens the state of health, it is necessary to evaluate the effectiveness of treatment and, possibly, change the dosage or choose another drug.

Overdose is extremely dangerous, especially in children.1-2 g at one-time reception can lead to a fatal outcome. Signs of an overdose are similar to the manifestation of side effects, but much brighter and faster. This is a sharp headache, convulsions, impaired vision, a violation of the rhythm of the heart, followed by his stop and stop breathing.

1. If these signs appear, the stomach should be washed immediately - induce vomiting or use a probe. The use of large doses of absorbents, for example, activated carbon, in an amount 5 times higher than the accepted dose of plakvenyl. As a rule, diazepam is administered to reduce the toxicity of the drug.
2. If necessary, forced ventilation and anti-shock therapy.
3. After relief of symptoms, follow-up is necessary for at least 6 hours.

The drug has an effect on the state of vision, so driving or working on complex technical devices during therapy is contraindicated.

Interaction with other medications

Hydroxychlorin interacts with a number of drugs. With the appointment of treatment it is necessary to take this into account.

• Digoxin - increases the digoxin content in the blood plasma, which can lead to intoxication. If the need for simultaneous administration of drugs, the dose of digoxin is appropriately reduced.
• Hydroxychlorin enhances the action of insulin. In the treatment of patients with diabetes, the dose of insulin before taking medication is reduced.
• Antacids reduce the digestibility of the substance, so between taking these medications should be a time interval of 4 hours.
• Aimnoglycosides have the potential to affect the rate of nerve impulse transmission. Plakvenil strengthens this effect.
• Citadin suppresses the processing of antimalarial drugs. Under its action, the concentration of the substance in the plasma can dangerously rise, which will lead to an overdose.
• Neostigmine and pyridostigmine are antagonists of plaquenyl and not co-administered.
• Any rabies vaccine is incompatible with hydroxychloride.

Reviews

Plaknevit is an effective antimalarial drug with additional beneficial properties. This makes it possible to actively apply it in the treatment of systemic ailments and diffuse connective tissue diseases. The medicine is on the list of vital.

The effectiveness of its action in systemic diseases can be assessed only after a few weeks, which, of course, irritates patients. In addition, side effects occur much earlier than the curative effect, which causes censure.

Analogues

Analogues of plaquenyl are preparations in which one of the 4-aminoquinoline derivatives acts as the active substance. These include:

• quinocide;
• has been assigned;
• plasmacid;
• is an immar.

Plaquenyl is a potent antimalarial agent with a pronounced immunosuppressive effect. The drug is used only as prescribed by the doctor, and strictly following the recommended dosage.

Plaquenil is an analogue of Delagil, but it also has significant differences from it, for example, lack of pills like nausea and stomach pain, while Plakvenil costs 5-6 times more.