Hydroxychloroquine, 200 mg 30 pcs
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Pharmacotherapeutic group: Antimalarial
ATC code: P01BA02
Pharmacodynamics:
Hydroxychloroquine by the chemical structure and pharmacological action is similar to chloroquine (hingamine).
Hydroxychloroquine has several pharmacological effects determining its therapeutic effect: it interacts with sulph-hydryl groups, changes enzyme activity (including phospholipase NADN-cytochrome C-reductase cholinesterase proteases and stabilizes lysosomal membranes; inhibits prostaglandin formation inhibits chemotaxis and phagocytosis of polymorphonuclear cells.
Malaria
Hydroxychloroquine actively suppresses erythrocytic forms and R. vivax and R. malariae gametes that disappear from the blood almost simultaneously with sexless forms does not affect R. Falciparum gametes. Hydroxychloroquine does not prevent recurrent attacks of malaria caused by P. vivax and P. malariae because it is ineffective against exoerythrocytic forms of P. vivax R. malariae and P. ovale and also does not prevent infection with these microorganisms when used prophylactically.
At the same time it reduces the severity of attacks, stops the attacks and significantly prolongs the interval between the course of treatment and the next attack at disease caused by these pathogens. At malaria caused by P. falciparum it eliminates acute attacks and leads to a complete cure unless we are not talking about resistant variants of the parasite. The frequency of resistant to 4-aminoquinoline derivatives forms of P. falciparum depends on the geographical location most often observed in some areas of South Asia, Central and South America, East Africa, Oceania.
Rheumatoid arthritis and lupus erythematosus
Hydroxychloroquine has immunosuppressive and anti-inflammatory discoid and systemic forms) and in acute and chronic rheumatoid arthritis. The exact mechanism of action in these diseases is unknown.
Pharmacokinetics:
Being a weak base hydroxychloroquine is quickly and completely absorbed in the small intestine of the gastrointestinal tract (GIT). The rate and completeness of absorption may vary from person to person but is independent of food intake. In the blood, hydroxychloroquine is approximately 40 to 45% bound to plasma proteins (albumin and a 1-glycoprotein) with a degree of availability of about 74% (70 to 80%). After a single oral intake of 200 mg of hydroxychloroquine sulfate (1 tablet) by a healthy subject, the average peak concentration (Cmax) is 244 ng/ml (188-427 ng/ml) 2-45 hours after intake (Tmax). The drug concentration in plasma is 7-8 times lower than in whole blood.
The drug is easily distributed between the body tissues having a significant apparent volume of distribution (Vd) (550±220 L and 440±210 L when calculated for whole blood and plasma, respectively). The drug concentrates in the brain, liver, spleen, lungs and erythrocytes; its concentration in these organs is higher than in plasma. Both chloroquine and hydroxychloroquine exhibit high affinity for melanin; their highest concentrations are observed in the epidermis of the retina vasculature and ciliary body of the eyeball. Small concentrations of hydroxychloroquine (about 32 micrograms after 48 hours) were found in the breast milk of women who received 800 mg of the drug.
Hydroxychloroquine is partially metabolized in the liver. A small part of the drug (6%) is metabolized in one pass. The formation of a number of decomposition products occurs in this sequence:
- secondary amine deethylhydrochloroquine or deethylchloroquine;
- primary amine bisdeethylchloroquine;
- 4′ – aldehyde derivative a small portion is further reduced to alcohol;
- 4′ – carboxy derivative. The main product of decomposition is deethylhydrochloroquine, which also has anti-plasmodial activity. Hydroxychloroquine conjugated to glucuronic acid is found in bile.
After administration of 200 mg of hydroxychloroquine sulfate orally to adult volunteers, the half-life of the drug (t1/2) is 50 ± 16 days according to whole blood (about 32 days in plasma).
Elimination of hydroxychloroquine from the body occurs in 2 stages. About 30-60% of the drug taken into the body is metabolized in the liver. A small amount is excreted by the kidneys – 15 to 25% of the total amount, even several months after the end of treatment traces of the drug are detected in the urine. After a single use of 200 mg of hydroxychloroquine sulfate total excretion with urine of unchanged substance and its metabolites after 86 days is 16 % and 13 % of the administered dose, respectively. Unabsorbed substance (up to 15-24 %) is excreted via gastrointestinal tract.
An unspecified amount is deposited in epithelium cells and excreted during their exfoliation. Some portion of the dose taken is eliminated by hepatic metabolism with subsequent excretion in the bile and in the renewal of pigmented epithelial tissues such as the skin. A number of studies indicate that 21 to 47% of the drug is excreted unchanged.
Indications
Malaria – for relief of acute attacks and prevention of malaria caused by Plasmodium vivax P. ovale and P. malariae and sensitive strains of P. falciparum; for radical treatment of malaria caused by sensitive strains of P. falciparum.
– Rheumatoid arthritis chronic juvenile arthritis.
– Dermatological diseases – lupus erythematosus (systemic and discoid) dermatological diseases caused or exacerbated by exposure to sunlight (photodermatosis).
Active ingredient
Hydroxychloroquine
Composition
1 film-coated tablet contains:
active ingredient:
Hydroxychloroquine sulfate – 200 mg;
excipients:
croscarmellose sodium – 3.0 mg,
magnesium stearate – 4.0 mg,
Colloidal silica – 0,5 mg,
Microcrystalline cellulose (PH 102) – 92,5 mg;
film coating: Hyprolose (hydroxypropyl cellulose), LF – 2.4 mg, hypromelose 2910 (hydroxypropyl methylcellulose) – 0.6 mg, macrogol (polyethylene glycol) 8000 – 1.8 mg, titanium dioxide (E 171) – 2.4 mg.
How to take, the dosage
It is prescribed orally. Tablets are taken with a meal or with a glass of milk. All doses are given for hydroxychloroquine sulfate and are not equivalent to doses of hydroxychloroquine base!
Malaria
Malaria suppression: for adults: 400 mg every seventh day.
For children over 6 years of age, the weekly dose is 65 mg/kg, but regardless of body weight, it should not exceed the dose for adults. If conditions allow, prophylactic treatment should be started 2 weeks before the trip to the endemic zone. If this is not possible for adults, an initial double dose of 800 mg in children – 129 mg/kg (but no more than 800 mg) divided into two doses with an interval of 6 hours.
Prophylactic treatment should be continued for 8 weeks after departure from the endemic zone.
Treatment in acute malaria attacks: the initial dose for adults is 800 mg followed by 400 mg after 6 or 8 hours and 400 mg for the next two days (2 g of hydroxychloroquine in total). A single dose of 800 mg is available as an alternative method. The dose for adults as well as for children can be calculated taking into account the body weight (see below).
For children over 6 years of age, a total dose of 32 mg/kg (but not exceeding 2 g) is administered over three days as follows:
– first dose is 129 mg/kg (but no more than 800 mg per dose);
– second dose is 65 mg/kg (but no more than 400 mg) 6 hours after the 1st dose;
– The third dose – 65 mg/kg (but not more than 400 mg) 18 hours after the 2nd dose;
– The fourth dose – 65 mg/kg (but not more than 400 mg) 24 hours after the 3rd dose.
Rheumatoid diseases
The drug has a cumulative effect and it takes several weeks to achieve its therapeutic effect while side effects may appear relatively early. If the patient’s condition doesn’t improve within 6 months the drug is discontinued.
The initial dose for adults is 400 – 600 mg/day the maintenance dose – 200 – 400 mg/day.
Systemic and discoidal lupus erythematosus
Doses should not exceed 65 mg/kg body weight (calculated by “ideal body weight”) or 400 mg/day the minimum effective dose or 200-400 mg/day should be prescribed.
In light sensitive dermatologic diseases, treatment should be limited to periods of maximum light exposure. For adults, a dose of 400 mg/day may be sufficient.
Interaction
Increases the side effects of glucocorticoids salicylates quinidine good antiarrhythmics hematopoietic and neurotoxic drugs.
Simultaneous use of hydroxychloroquine and digoxin may cause increased serum digoxin levels, so patients receiving the combined therapy should regularly monitor serum digoxin levels if necessary reduce the digoxin dose.
Increases plasma concentrations of penicillamine and the risk of its adverse effects on the blood forming organs, urinary system and skin reactions.
May increase the effect of hypoglycemic agents, which may require reducing the dose of insulin and antidiabetic drugs.
Hydroxychloroquine may enter into some of the known chloroquine interactions i.e. possible enhancement of:
– blocking action of aminoglycoside antibiotics on neuromuscular transmission; inhibition of its metabolism by cimetidine that may increase the drug concentration in plasma;
– antagonism of neostigmine and pyridostigmine action;
– reduction of antibody formation in response to primary immunization with diploid cell rabies vaccine.
At simultaneous use of hydroxychloroquine and antacids the interval between the intake should be at least 4 hours (reduced absorption).
Alkaline drinking and alkalis accelerate excretion of hydroxychloroquine from the body.
Special Instructions
Before and during therapy it is necessary to perform ophthalmologic examination at least once every 6 months (use of daily doses more than 65 mg/kg increases the risk of retinal damage).In case of adverse reactions on the visual side (decrease in visual acuity, change in color perception, etc.) the drug should be stopped immediately (changes in the retina may progress even after cancellation of the drug.
Exceeding the recommended daily dose increases the risk of retinal damage and accelerates this process. Before starting a course of treatment with the drug an ophthalmoscopy of both eyes should be performed to study visual acuity of color vision and optical field. Subsequently such examination should be repeated at least annually.
If the vision deteriorates (visual acuity color vision, etc.) the drug should be immediately withdrawn. Patients should be monitored since retinal changes and visual impairment may progress even after the cancellation of treatment.
Use during pregnancy is possible only on vital indications (in therapeutic doses may cause CNS damage in the fetus or infant (including ototoxicity of hearing).including ototoxicity auditory and vestibular up to deafness) retinal bleeding and abnormal retinal pigmentation (infants are especially sensitive to the toxic effects of 4-aminocholines).
Caution is recommended when treating patients with liver and kidney diseases. It may be necessary to reduce the dose of the drug to reduce its toxic effects on these organs.
Caution is exercised when treating patients with gastrointestinal neurological or hematological diseases; patients sensitive to quinine and suffering from glucose-6-phosphate dehydrogenase deficiency porphyria and psoriasis. Patients who have been taking the drug for a long time should periodically perform a detailed blood test. In case of detection of deviations from the norm the drug is suspended.
Patients taking the drug for a long time should have periodic examination of the skeletal muscle function and tendon reflexes. If muscle weakness occurs while taking the drug the drug should be discontinued.
Examination should be more frequent and in such situations: daily dose of the drug exceeds 65 mg/kg of ideal (not increased) body weight; the real weight used to set the dose for obese patients may lead to overdose; renal failure; total dose exceeds 200 mg; elderly patients (over 65 years); reduced visual acuity.
Influence on ability to drive motor transport and vehicles: During the treatment period it is necessary to be careful when driving vehicles and engaging in other potentially dangerous activities that require high concentration and quick psychomotor reactions.
Contraindications
– Hypersensitivity to 4-aminoquinoline derivatives or any other drug component
– Maculopathy
– Previous maculopathy
– Children under 6 years of age (200 mg tablets are not adapted for use in children with body weight less than 31 kg).
– Childhood age when prolonged therapy is necessary (increased risk of toxic effects)
– Pregnancy (can be used for vital indications).
– Lactation
– Congenital anomalies such as galactose intolerance, lactase deficiency or glucose/galactose malabsorption syndrome.
With caution: With retinopathy visual disorders (visual field changes, decreased visual acuity) while taking medications that can cause visual disorders suppression of the bone marrow hematopoiesis psychosis (including history porphyria psoriasis concomitant use of drugs that may cause skin reactions deficiency of glucose-6-phosphate dehydrogenase in renal or hepatic failure (if necessary, doses of hydroxychloroquine are adjusted when monitoring plasma concentrations) hepatitis severe gastrointestinal diseases.
Side effects
Organs of vision: rare – retinopathy with changes in pigmentation and visual field defects. In the early stage it is reversible after drug withdrawal. If the drug is not withdrawn in time, there is a risk of progression of retinopathy even after drug withdrawal. Changes to the retina may initially be asymptomatic or may appear as a paracentral pericentral or transient scotoma and color vision disturbances.Corneal changes including edema and clouding are possible. They may be asymptomatic or cause abnormalities such as halos of blurred vision or photophobia. These changes may be temporary or reversible when treatment is discontinued. Blurred vision is caused by impaired accommodation, is dose-dependent and reversible. Atrophy of the optic nerve keratopathy, ciliary muscle dysfunction may occur with prolonged use of high doses.
Hearing: tinnitus, hearing loss.
Skin: rare – skin rash itching pigmentation changes in the skin and mucous membranes hair discoloration and alopecia. These changes usually disappear quickly after discontinuation of treatment. Bullous rash is possible, including very rare cases of erythema multiforme and Stevens-Johnson syndrome photosensitivity and isolated cases of exfoliative dermatitis. Very rare – acute generalized exanthematous pustular rashes that should be distinguished from psoriasis, although the drug may cause exacerbation of psoriasis. It may be associated with fever and leukocytosis. After discontinuation of the drug the prognosis is usually favorable.
Central nervous system: dizziness headache nervousness emotional lability psychosis seizures ataxia irritability occasionally noted.
Cardio-vascular system: cardiomyopathy (rarely) atrioventricular block (AV-blockade) decreased myocardial contractility myocardial hypertrophy; with prolonged high-dose therapy – myocardiodystrophy. If conduction abnormalities (AV-blockade Giss bundle block) and hypertrophy of both ventricles are detected, chronic intoxication should be suspected.
Blood organs: rare – inhibition of medullary aplastic anemia agranulocytosis thrombocytopenia hemolytic anemia (in patients with glucose-6-phosphate dehyde oxygenase deficiency) aggravation of porphyria.
Musculoskeletal and nervous system disorders: skeletal muscle myopathy or neuromyopathy leading to progressive weakness and atrophy of proximal muscle groups are possible. Myopathy is usually reversible after drug withdrawal, but full recovery may take several months. Mild sensory changes, inhibition of tendon reflexes and abnormal nerve conduction may be noted. After discontinuation of the drug conduction usually recovers.
Digestive system disorders: nausea vomiting (rarely) decreased appetite spastic abdominal pain diarrhea.
Liver: hepatotoxicity (liver dysfunction liver failure). In individual cases there may be observed changes in the parameters of functional liver function tests reported on several cases of sudden liver failure.
Other: weight loss.
Overdose
Overdose is especially dangerous in young children, even taking 1-2 g of the drug can be fatal!
Symptoms: headache sleepiness stupor coma ataxia insomnia agitation hyperreflexia muscle rigidity choreoathetosis seizures BP decrease tachycardia arrhythmia intraventricular AV blockade heart failure cyanosis body temperature increase mydriasis oliguria respiratory center depression respiratory arrest. The symptoms develop 4 hours after overdose and reach their maximum in 24 hours and last for 4-6 days.
Treatment: gastric lavage (until clear lavage water); administration of activated charcoal (in dose five times the dose of the drug); forced diuresis and urine alkalinization (e.g. with ammonium chloride to pH 55-65) increase urinary excretion of 4-aminoquinoline; symptomatic therapy (including administration of diazepam for convulsions; antishock therapy). Control of serum sodium concentration and constant medical monitoring for at least 6 hours after relief of symptoms are necessary. Monitoring of cardiovascular activity (ECG) for 5 days is indicated as relapse may occur after 48 h and later.
Injection of physostigmine is contraindicated due to increased risk of seizures. Hemodialysis and forced diuresis are ineffective.
Similarities
Plakvenil
Weight | 0.026 kg |
---|---|
Shelf life | 3 years. Do not use after the expiration date printed on the package. |
Conditions of storage | Store in a dry place protected from light at a temperature of 15 to 30 ° C Keep out of reach of children. |
Manufacturer | Vector-Medica JSC, Russia |
Medication form | pills |
Brand | Vector-Medica JSC |
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