• HYDROXYCHLOROQUINE (generic Plaquenil) tablets

Buy Hydroxychloroquine 200mg 30 tablets

      Active ingredient: hydroxychloroquine

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Warning: Please note that if the labeling for the drug is not in English, that means that this drug is not intended for the U.S. market. So, if you live in the United States and want to buy HYDROXYCHLOROQUINE you should contact FDA first to know if you can purchase Hydroxychloroquine and bring it in the USA.


Indications

Malaria (with the exception of chloroquine-resistant P. falciparum strains): prevention and relief of acute attacks of malaria caused by Plasmodium vivax, P. ovale and P. ma-lariae, as well as susceptible strains of P. falciparum; radical treatment of malaria caused by susceptible strains of P. falciparum; rheumatoid arthritis; juvenile rheumatoid arthritis; lupus erythematosus (systemic and discoid); photodermatitis.


Pharmacodynamics

Hydroxychloroquine has antimalarial properties, and also has anti-inflammatory and immunosuppressive effects in chronic discoid or systemic lupus erythematosus (SLE), acute and chronic rheumatoid arthritis (RA). Its mechanism of action in malaria, lupus erythematosus and rheumatoid arthritis is not fully understood.

Hydroxychloroquine has the properties of a moderate immunosuppressive agent, suppressing the synthesis of rheumatoid factor and components of the acute phase reaction. It also accumulates in leukocytes, stabilizing lysosomal membranes, and inhibits the activity of many enzymes, including collagenase and proteases, that cause cartilage breakdown.

Efficacy in SLE and RA is associated with the following anti-inflammatory and immunomodulatory effects of hydroxychloroquine:

- an increase in intracellular pH leads to a slowdown in the antigenic response and decreases the binding of peptides to the receptors of the major histocompatibility complex (MHC). Fewer antigen-MHC receptors reach the cell surface, which leads to a decrease in the autoimmune response;

- a decrease in the activity of phospholipase A2 at high concentrations of lysosomal enzymes;

- a decrease in the concentrations of the cytokines IL-1 and IL-6, leading to a decrease in clinical and laboratory parameters of the autoimmune response. Since there is no violation of the synthesis of interferon gamma, these effects may be associated with a selective effect on cytokines;

- inhibition of pre- and / or post-transcription of DNA and RNA.

The drug actively suppresses asexual erythrocyte forms, as well as the gametes P. vivax and P. malariae, which disappear from the blood almost simultaneously with asexual forms. Hydroxychloroquine has no effect on P. falciparum gametes. Hydroxychloroquine is ineffective against chloroquine-resistant P. falciparum strains, and is also inactive against extra-erythrocyte forms of P. vivax, P. malariae and P. ovale and therefore cannot prevent infection by these microorganisms when administered for prophylactic purposes, and also cannot prevent recurrence of the disease caused by these pathogens.


Pharmokinetics

After oral administration, hydroxychloroquine is rapidly and almost completely absorbed. In healthy volunteers after a single dose of 400 mg, the maximum plasma concentration of hydroxychloroquine was reached after 1.83 hours and ranged from 53 to 208 ng / ml. The connection with plasma proteins is 45%. The mean value of the plasma half-life varies depending on the time elapsed after taking the drug as follows: 5.9 hours (from reaching the maximum plasma concentration (Cmax) to 10 hours) 26.1 hours (from 10 to 48 hours ) and 299 hours (48 to 504 hours). In the liver, it is partially converted into active ethylated metabolites. The unchanged drug and its metabolites are well distributed in the body. The volume of distribution is 5-10 l / kg. The drug accumulates in tissues with a high level of metabolism (in the liver, kidneys, lungs, spleen - in these organs the concentration exceeds the plasma concentration by 200-700 times; central nervous system, erythrocytes, leukocytes), as well as in the retina and tissues rich in melanin. Hydroxychloroquine and its metabolites are excreted mainly in the urine and to a lesser extent in the bile. The release of the drug is slow, the terminal half-life is about 50 days (from whole blood) and 32 days (from plasma). Within 24 hours, 3% of the administered dose of the drug is excreted in the urine.

Hydroxychloroquine crosses the placental barrier and is found in small amounts in breast milk.


Contraindications

Hypersensitivity to hydroxychloroquine and 4-aminoquinoline derivatives or to other components of the drug.

  • - Retinopathy (including a history of maculopathy).
  • - 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 an "ideal" body weight less than 31 kg).
  • - Pregnancy (see "Pregnancy and lactation").


Carefully

  • - In case of visual disturbances (decreased visual acuity, impaired color vision, narrowing of the visual fields), while taking medications that can cause adverse ophthalmic reactions (risk of progression of retinopathy and visual disorders).
  • - With hematological diseases (including history).
  • - With neurological diseases, psychosis (including a history).
  • - With tardive cutaneous porphyria (risk of exacerbation), psoriasis (risk of increased skin manifestations of the disease), while taking drugs that can cause skin reactions.
  • - In case of renal failure and / or liver failure, hepatitis, simultaneous administration of drugs that can adversely affect the function of the liver and / or kidneys (in severe renal or hepatic impairment, the dose should be adjusted under the control of plasma concentrations of hydroxychloroquine).
  • - With a deficiency of glucose-6-phosphate dehydrogenase.
  • - With gastrointestinal diseases.
  • - In case of hypersensitivity to quinine (the possibility of cross-allergic reactions).
  • - In case of violation of the conduction of the heart (blockade of the legs of the bundle of Gis / atrioventricular block) and with hypertrophy of both ventricles.
  • - With cardiomyopathy.
  • - Due to the risk of developing hypoglycemia, the drug should be prescribed with caution to patients who are taking and not taking hypoglycemic drugs (see the sections "Side effects", "Interaction with other drugs", "Special instructions").


Application during pregnancy and during breastfeeding

Hydroxychloroquine crosses the placenta. There are limited data regarding its use during pregnancy. It should be noted that 4-aminoquinolines in therapeutic doses can cause intrauterine damage to the central nervous system, including the auditory nerve (hearing and vestibular disorders, congenital deafness), retinal hemorrhages, and abnormal retinal pigmentation.

The need to use the drug during breastfeeding should be carefully weighed, since it has been shown that it is excreted in small quantities in breast milk, and small children are especially sensitive to toxic effects 4-aminoquinolines.


Overdose

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

Symptoms

Overdose symptoms include headache, visual disturbances, collapse, seizures, hypokalemia, rhythm and conduction disturbances, followed by cardiac arrest and respiratory arrest.

Treatment

Since overdose symptoms can develop very quickly after taking a large dose of the drug, in these cases, appropriate measures should be taken immediately. An artificial induction of vomiting or gastric lavage through a tube should be performed immediately. Absorption can be slowed down by activated carbon in a dose of at least 5 times the dose of the drug taken. It is advisable to parenteral administration of diazepam, which will reduce the cardiotoxicity of chloroquine. If necessary, artificial ventilation and anti-shock therapy should be performed.

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


Side effects

The frequency of adverse reactions is presented in accordance with the classification of the World Health Organization (WHO): very often (> 1/10), often (≥ 1/100 and <1/10), infrequently (≥ 1/1000 and <1/100), rarely (≥ 1/10000 and <1/1000), very rarely (<1/10000), the frequency is unknown (it is not possible to determine the frequency of occurrence of an adverse reaction).

Disorders from the blood and lymphatic system: the frequency is unknown - inhibition of bone marrow hematopoiesis, anemia, aplastic anemia, agranulocytosis, leukopenia, thrombocytopenia.

Immune system disorders: frequency unknown - urticaria, angioedema, bronchospasm.

Metabolic and nutritional disorders: often - anorexia; frequency unknown - hypoglycemia, the possibility of exacerbation of porphyria.

Mental disorders: often - affective lability; infrequently - nervousness; frequency unknown - psychosis, suicidal behavior.

Nervous system disorders: often - headache; infrequently - dizziness; frequency unknown - seizures, extrapyramidal disorders such as muscular dystonia, dyskinesia and tremor.

Violations of the organ of vision: often - blurred vision associated with a violation of accommodation, which is dose-dependent and reversible; infrequently - retinopathy with changes in pigmentation and visual field defects. In case of timely withdrawal of the drug, these phenomena are reversible. If the condition remains undiagnosed and retinal lesions continue to develop, then the risk of their progression is possible even after the drug is discontinued. 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 impairments such as halos, blurred vision, or photophobia. These changes may be temporary or reversible. Frequency unknown - maculopathy and macular degeneration, which may be irreversible.

Hearing disorders and labyrinthine disorders: infrequently - vertigo, tinnitus; frequency unknown - hearing loss.

Cardiovascular disorders: frequency unknown - cardiomyopathy, which can lead to heart failure and, in some cases, death. Detection of cardiac conduction abnormalities (such as bundle-branch blocks / AV conduction abnormalities) and hypertrophy of both ventricles may indicate chronic cardiac toxicity. When the drug is discontinued, these changes may reverse.

Disturbances from the gastrointestinal tract: very often - abdominal pain, nausea; often - diarrhea, vomiting. These symptoms usually resolve immediately after dose reduction or drug withdrawal.

Violations of the liver and biliary tract: infrequently - deviations from the norm of functional "liver" tests; frequency unknown - fulminant hepatic failure.

Skin disorders of subcutaneous tissues: often - skin rash, itching; infrequently: changes in pigmentation of the skin and mucous membranes, hair discoloration and alopecia (these changes usually quickly disappear after stopping treatment); frequency unknown - bullous rash including erythema multiforme; Stevens-Johnson syndrome; toxic epidermal necrolysis; photosensitivity; exfoliative dermatitis; drug skin reaction accompanied by eosinophilia and systemic manifestations (DRESS syndrome); acute generalized exanthematous pustulosis (OGEP). OGEP must be distinguished from psoriasis, although hydroxychloroquine can exacerbate psoriasis. OGEB may be accompanied by fever and hyperleukocytosis. After discontinuation of the drug, the outcome is usually favorable.

Musculoskeletal and connective tissue disorders: infrequently - sensory-motor disorders; the frequency is unknown - skeletal muscle myopathy or neuromyopathy, leading to progressive weakness and atrophy of the proximal muscle groups (myopathy can be reversible after drug withdrawal, but it may take several months to fully recover), suppression of tendon reflexes and decreased nerve conduction.


Special conditions

General

The toxic effect on the retina is highly dose-dependent. The incidence of retinopathy with doses up to 6.5 mg / kg of “ideal” body weight is low. Exceeding the recommended daily dose dramatically increases the risk of developing retinopathy.

Before starting a long course of treatment with the drug, a thorough examination of both eyes should be carried out. The examination should include the determination of visual acuity, examination of the fundus, assessment of color vision and visual fields. During therapy, such an examination should be carried out at least once every 6 months.

The examination should be more frequent in the following situations:

- at a daily dose exceeding 6.5 mg / kg of "ideal" body weight (in patients with increased body weight, the use of absolute body weight to calculate the dose may lead to overdose);

- with renal failure;

- with a total dose of over 200 g;

- in the elderly;

- if the patient has a decrease in visual acuity of any severity before the start of treatment.

In the event of any visual disturbances (decreased visual acuity, changes in color vision), the drug should be discontinued immediately and the patient's visual condition should be closely monitored, since changes in the retina (and visual disturbances) can progress even after the drug is discontinued (see . section "Side effects").

In patients taking the drug Hydroxychloroquine, cases of cardiomyopathy, leading to heart failure, have been observed (see the section "Side effects").

It has been shown that hydroxychloroquine can cause the development of severe hypoglycemia (including loss of consciousness), which can threaten the lives of patients, both taking and not taking hypoglycemic drugs. Patients taking hydroxychloroquine should be warned about the risk of hypoglycemia and the associated clinical signs and symptoms. In patients who, during treatment with hydroxychloroquine, have clinical symptoms indicating the development of hypoglycemia, the blood glucose concentration should be determined and, if necessary, the therapy should be revised.

It is recommended to be careful when using hydroxychloroquine in patients with liver and kidney disease, who may need to reduce the dose of the drug, as well as in patients taking drugs that can cause adverse effects on these organs.

In patients taking hydroxychloroquine for a long time, a complete blood count should be performed periodically (if hematological disorders occur, hydroxychloroquine should be canceled).

Children are particularly sensitive to the toxic effects of 4-aminoquinolines, so care should be taken to keep hydroxychloroquine out of the reach of children.

All patients taking the drug for a long time should be periodically examined by a neuropathologist regarding the functions of skeletal muscles and the severity of tendon reflexes. If muscle weakness occurs, the drug should be discontinued.

In very rare cases, suicidal behavior has been reported in patients taking hydroxychloroquine. When using the drug Hydroxychloroquine, it is possible to develop extrapyramidal disorders (see the section "Side effects").

For malaria

Hydroxychloroquine is not effective against chloroquine-resistant P. falciparum strains, and is also not active against extra-erythrocytic forms of P. vivax, P. malariae and P. ovale, and therefore cannot prevent infection with these microorganisms when used for prophylactic purposes, and cannot prevent recurrence of the disease caused by these pathogens.


Drug interactions

With digoxin

It has been reported that hydroxychloroquine is able to increase the plasma concentration of digoxin, therefore, in order to avoid the development of glycosidic intoxication with the simultaneous administration of these drugs, it is necessary to reduce the dose of digoxin under the control of its plasma concentrations.

With drugs used to treat diabetes

Hydroxychloroquine may potentiate the effects of insulin and oral hypoglycemic agents and may require dose reductions when starting hydroxychloroquine.

With antacids

Antacids may decrease the 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 excluded.

With aminoglycosides

Potentiation of the direct blocking action of aminoglycosides on neuromuscular transmission.

With cymemidine

Cimetidine inhibits 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.

With neostigmine and pyridostigmine - action antagonism.

With any intradermal human diploid cell rabies vaccine

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

With halofantrine and other arrhythmogenic drugs

Halofantrine lengthens the QT interval and, in combination with hydroxychloroquine, can cause arrhythmias (this combination is not recommended). In addition, there is an increased risk of developing ventricular arrhythmias when hydroxychloroquine is used concomitantly with other arrhythmogenic drugs (such as amiodarone and moxifloxacin).

With other antimalarial drugs that lower the seizure threshold

The use of hydroxychloroquine can lead to a decrease in the seizure threshold. Co-administration of hydroxychloroquine with other known antimalarial drugs that lower the seizure threshold (for example, mefloquine) may increase the risk of seizures.

With cyclosporine

An increase in the concentration of cyclosporine in blood plasma has been reported with the combined use of cyclosporine and hydroxychloroquine.

With antiepileptic drugs

When used together with antiepileptic drugs, the effectiveness of the latter may be insufficient.

With praziquantel

In a study of the interaction of chloroquine and praziquantel, a decrease in the bioavailability of praziquantel was reported. Due to the similarity of structure and pharmacokinetic parameters between hydroxychloroquine and chloroquine, a similar effect can be expected with the combined use of hydroxychloroquine and praziquantel.

With agalsidase

There is a theoretical risk of inhibition of intracellular α-galactosidase with the combined use of hydroxychloroquine with agalsidase.

Influence on the ability to drive vehicles, mechanisms

During the period of drug treatment, care should be taken when performing potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.


Hydroxychloroquine for sale: Even if a prescription is not required, it is assumed that you have a valid prescription or doctor's recommendation. Please do not self-cure. Get expert advice before ordering. 

The drug images are for illustrative purposes only and may differ from the actual product.

The product is intended for the Russian market and can be labeled in Russian (Packaging design may vary). With detailed English printed manual. To make sure that you are buying the right product, just translate the word ГИДРОКСИХЛОРОХИН into English using Google Translate. Just copy and paste.


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HYDROXYCHLOROQUINE (generic Plaquenil) tablets

  • Product Code: HC200X30
  • Availability: In Stock
  • 42.28€

  • Ex Tax: 42.28€