What Is Hydroxychloroquine Sulfate?

Hydrochloroquine sulfate tablets are indicated for rheumatoid arthritis, juvenile chronic arthritis, discoid and systemic lupus erythematosus, and skin lesions caused or exacerbated by sunlight.

Whether prescription drugs: prescription
Drug Name: Hydroxychloroquine sulfate tablets

Drug type: Prescription drugs, medicines for medical workers' injuries
Use classification: Other antipyretic, analgesic and anti-inflammatory drugs

Ingredients of hydroxychloroquine sulfate tablets

The main ingredient of this product is hydroxychloroquine sulfate.
Chemical name: 2-[[4-[(7-chloro-4-quinolinyl) amino] pentyl] ethylamino] -ethanol sulfate.
Chemical Structure:

Molecular formula: C ₁₈ H ₂₆ ClN ₃ O · H ₂ SO ₄
Molecular weight: 434.0

Hydroxychloroquine sulfate tablets

This product is a white film-coated tablet that appears white after removal of the coating.
HCQ is engraved on one side and 200 words on the other.

Indications of hydroxychloroquine sulfate tablets

Rheumatoid arthritis, juvenile chronic arthritis, discoid and systemic lupus erythematosus, and skin lesions caused or exacerbated by sunlight.

Specification of hydroxychloroquine sulfate tablets

0.2g (based on hydroxychloroquine sulfate)

Dosage of hydroxychloroquine sulfate tablets

The tablets are administered orally.
Adults (including seniors)
The first dose was 400 mg daily and was taken in divided doses. When the efficacy does not improve further, the dose can be reduced to 200 mg to maintain. If the response to treatment weakens, the maintenance dose should be increased to 400 mg daily. The minimum effective dose should be used, which should not exceed 6.5 mg / kg / day (calculated from the ideal weight rather than the actual weight) or 400 mg / day or even less.
Children should use the minimum effective dose, which should not exceed 6.5 mg / kg / day (based on the ideal weight) or 400 mg / day or even less. Children younger than 6 years old are contraindicated and 200mg tablets are not suitable for children weighing less than 35kg.
Eat or drink milk at the same time with each dose.
Hydroxychloroquine has a cumulative effect and takes several weeks to exert its beneficial effects, while minor adverse reactions may occur relatively early. If rheumatic disease does not improve after 6 months of treatment, treatment should be discontinued. In the case of light-sensitive diseases, treatment should only be given to the maximum exposure to sunlight.

Adverse reactions of hydroxychloroquine sulfate tablets

Visual effects < br Retina changes:
Changes in retinal pigmentation and visual field defects can occur, which are rarely reported. These lesions are reversible after early discontinuation of this product. If it is further developed, there is still an increased danger even after this product is stopped. Cases of macular degeneration and macular degeneration are reported and may be irreversible.
Patients with retinopathy may be asymptomatic in the early stages, or may be accompanied by paracenter or central circular dark spots, temporary blind spots, temporal visual field defects, and abnormal color vision.
Corneal changes:
Reports of corneal changes include corneal edema and opacities, which can be unconscious symptoms or can cause halos, blurred vision, or photophobia. These symptoms may be temporary or reversed after withdrawal.
Blurred vision due to abnormal regulatory function is dose-dependent and may be reversible.
Skin effects < br Sometimes rashes can occur: pruritus, changes in skin and mucous membrane pigmentation, whitening of hair, and hair loss. These symptoms are usually easy to recover after withdrawal.
Has herpes including very rare erythema polymorpha and Steven-Johnson syndrome, toxic epidermal necrolysis, drug eruptions with eosinophilia and systemic symptoms (DRESS syndrome), light sensitivity and exfoliative dermatitis Report. Very rare cases of acute generalized eruptive impetigo (AGEP) must be distinguished from psoriasis, although hydroxychloroquine may contribute to the onset of psoriasis. Fever and leukocytosis may be related to hydroxychloroquine. Results usually improve after withdrawal.

Gastrointestinal effects < br Gastrointestinal disorders such as nausea, diarrhea, anorexia, abdominal pain and rare vomiting can occur. These symptoms usually disappear immediately after reducing the dose or stopping treatment.

Central nervous system effects < br Rarely, adverse reactions such as dizziness, dizziness, tinnitus, hearing loss, headache, neurosis and emotional instability, psychosis, and convulsions have been reported, but these have been reported.
Neuromuscular effects < br Sensory motor neuron disease can occur. Skeletal muscle disease or neuromuscular disease with progressive weakness and proximal muscle group atrophy has been reported. Myopathy may recover after discontinuation, but recovery takes multiple months.
Slight sensory changes, inhibition of tendon reflexes, and abnormal nerve conduction may be observed.

Cardiovascular system effects < br Cardiomyopathy (which may lead to heart failure), some cases have reported death.
Chronic toxicity of the drug should be suspected when cardiac conduction abnormalities (bundle branch block / atrioventricular block) and bilateral ventricular hypertrophy are found. May recover after discontinuation.
Hematological effects < br Reports of bone marrow suppression are rare. Hematological abnormalities such as anemia, aplastic anemia, agranulocytosis, leukopenia, and thrombocytopenia have been reported.
Hydroxychloroquine may cause or aggravate porphyria.
· Liver effects:
There have been reports of abnormal liver function tests and some cases of fulminant liver failure.
-Allergic reactions < br Urticaria, angioedema and bronchospasm have been reported.
Metabolic and nutritional system effects may occur with hypoglycemia at an unknown frequency.

Hydrochloroquine sulfate tablets contraindications

-Patients known to be allergic to 4-chloroquinoline compounds-Patients with previous macular degeneration-Children under 6 years of age (200mg tablets are not suitable for children weighing less than 35kg)

Precautions for hydroxychloroquine sulfate tablets

· Before starting treatment with this product, all patients should undergo ophthalmological examinations, including visual acuity sensitivity, ophthalmic microscopy, central visual field, color vision, and fundus examination. Thereafter, it should be checked at least once a year.
Retinopathy is highly correlated with drug doses. The risk of retinal damage is low when the maximum daily dose does not exceed 6.5 mg / kg body weight. But exceeding the recommended daily dose will greatly increase the risk of retinal toxicity.
The frequency of eye examinations should be increased in patients with:
-The daily dose exceeds the ideal body weight of 6.5 mg / kg. Abdominal patients will be overdose based on absolute weight as a guide for dosing.
-Renal insufficiency;
Cumulative dose exceeds 200g;
-The elderly;
-Impaired visual acuity;
If visual impairment (visual acuity, color vision, etc.) occurs, the drug should be stopped immediately and the progress of the abnormal condition of the patient should be closely monitored. Retinopathy (and visual impairment) may progress even after stopping treatment. (See section "Adverse reactions")
Studies have shown that hydroxychloroquine can cause severe hypoglycemia, including loss of consciousness, which may endanger the lives of patients who have received or not received anti-diabetic medication. Patients receiving hydroxychloroquine should be warned of the risk of hypoglycemia and related clinical signs and symptoms. During the course of treatment with hydroxychloroquine, if symptoms of hypoglycemia occur, blood glucose levels should be checked and treatment re-evaluated if necessary.
In patients treated with hydroxychloroquine sulfate, suicide is reported in rare cases.
Patients treated with this product have reported cases of cardiomyopathy leading to heart failure, and some of them have reported deaths. Clinical monitoring of the signs and symptoms of cardiomyopathy is recommended. This product should be discontinued in the presence of cardiomyopathy. When abnormal cardiac conduction (bundle branch block / atrioventricular block) and bilateral ventricular hypertrophy are found, the chronic toxicity of the drug should be considered.
Patients who are taking drugs that may cause eye or skin adverse reactions should use this product with caution. This product should also be used with caution in patients with liver or kidney disease, or those who are taking medications known to affect these organs, as well as patients with severe gastrointestinal, neurological, and hematological disorders. Patients with severely impaired liver and kidney function should be assessed for plasma chlorochloroquine levels in order to adjust the dose used.
Although the risk of bone marrow suppression is low, anemia, aplastic anemia, agranulocytosis, leukopenia, and thrombocytopenia have been reported. Regular blood counts are recommended, and this product should be discontinued if abnormalities occur.
Patients who are sensitive to quinine, those who are deficient in glucose-6-phosphate dehydrogenase, those who take hydroxychloroquine can exacerbate late-onset skin porphyria, and psoriasis patients who seem to be able to increase skin adverse reactions by taking this product Risks, this product should also be used with caution.
Patients with rare genetic diseases of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption should not take this product.
Children are particularly sensitive to the toxic effects of 4-aminoquinoline; patients are therefore warned to keep this product out of reach of children.
All patients undergoing long-term treatment should be checked regularly for skeletal muscle function and tendon reflexes. If there is a decrease in skeletal muscle function and tendon reflexes, the drug should be discontinued.
Impaired vision regulation has been reported shortly after starting treatment. The persons involved in driving and operating the machine should be reminded. If symptoms cannot be self-limited, the dose should be reduced or treatment discontinued.
Malaria: Plasmodium falciparum, which is resistant to chloroquine, is ineffective in treatment with hydroxychloroquine, and it is also ineffective against Plasmodium vivax, Plasmodium ovale, and Plasmodium malariae outside the red blood cells, so it cannot prevent its infection and prevent recurrence.

Hydroxychloroquine sulfate tablets for pregnant and lactating women

Hydroxychloroquine can pass through the placenta. There is limited information on the use of hydroxychloroquine during pregnancy. It should be noted that 4-aminoquinoline in therapeutic doses is associated with central nervous system damage, including ototoxicity (auditory and vestibular toxicity, congenital deafness), retinal hemorrhage, and retinal pigmentation. Therefore, hydroxychloroquine should be avoided in pregnant women unless the potential therapeutic benefit outweighs the potential risk based on a doctor's assessment.
Hydroxychloroquine should be used with caution in breast-feeding women because a small amount of hydroxychloroquine is secreted in breast milk, and infants are known to be very sensitive to the toxic effects of 4-aminoquinoline.

Hydrochloroquine sulfate tablets for children

The minimum effective dose should be used and should not exceed 6.5 mg / Kg / d (calculated based on the ideal body weight) or 400 mg / day, or even less. Children younger than 6 years old are contraindicated and 200mg tablets are not suitable for children weighing less than 35kg.

Hydroxychloroquine sulfate tablets for elderly

No related information.

Hydroxychloroquine sulfate tablets drug interactions

There are reports of hydroxychloroquine sulfate increasing plasma digoxin levels: Patients receiving combination therapy should closely monitor their serum digoxin levels.
Although not specifically reported, hydroxychloroquine sulfate may also have several drug interactions with chloroquine. Including aminoglycoside antibiotics can enhance its direct block of neuromuscular junctions; cimetidine inhibits its metabolism to increase plasma concentrations of antimalarial drugs; antagonizes the effects of neostigmine and pyridostigmine; weakens the body's skin Primary Immunoantibody Response to an Injected Human Diploid Cell Rabies Vaccine
Similar to chloroquine therapy, antacids may reduce the absorption of hydroxychloroquine. Therefore, it is recommended that this product and antacids be used at an interval of 4 hours.
Hydroxychloroquine may enhance the effect of hypoglycemic drugs, so the combination of insulin and hypoglycemic drugs may need to be reduced when used in combination.
Halfentraline can prolong the QT interval and should not be used in combination with other drugs that may cause arrhythmias, including hydroxychloroquine. In addition, the combination of hydroxychloroquine with other arrhythmogenic drugs (eg, amiodarone and moxifloxacin) may increase the risk of inducing ventricular arrhythmias.
Elevated plasma cyclosporine levels have been reported in combination with cyclosporine and hydroxychloroquine.
Hydroxychloroquine reduces the convulsive threshold. The combination of hydroxychloroquine with other antimalarial drugs (eg, mefloquine) known to lower the convulsive threshold may increase the risk of convulsions.
In addition, when combined with hydroxychloroquine, the activity of antiepileptic drugs may be impaired.

Hydrochloroquine sulfate tablets overdose

4-aminoquinoline overdose in infants is very dangerous, and 1-2g can prove fatal.
Symptoms of overdose may include headaches, visual disturbances, cardiovascular failure, convulsions, hypokalemia, rhythm, and conduction disorders, including prolonged QT interval, apex torsional ventricular tachycardia, ventricular tachycardia, and ventricular fibrillation Or even sudden, potentially fatal breathing and cardiac arrest. Because these effects may occur immediately after an overdose, immediate medical intervention is required. The contents of the stomach should be emptied quickly by vomiting or gastric lavage. Within 30 minutes after taking the drug, after the gastric lavage, at least 5 times the dosage of activated carbon powder is introduced through the gastric tube to inhibit further absorption.
Stabilization should be considered parenterally in excess; it has been shown to be beneficial in reversing the cardiotoxicity of chloroquine.
If necessary, take respiratory support and shock treatment plan.
Patients who survive the acute phase should be closely observed for at least 6 hours, even if they have no symptoms.

Hydroxychloroquine sulfate tablets pharmacology and toxicology

Antimalarial drugs such as chloroquine and hydroxychloroquine have several pharmacological effects, including the therapeutic effects involved in treating rheumatic diseases, but the role of each effect is unknown. These include interactions with sulfhydryl groups, interference with enzyme activities (including phospholipase, NADH-cytochrome C reductase, cholinesterase, protease, and hydrolase), binding to DNA, stabilization of lysosomal membranes, and inhibition of prostaglandins Formation, inhibition of chemotaxis and phagocytosis of polymorphonuclear cells, may interfere with the formation of monocyte interleukin-1 and inhibit the release of neutrophil superoxide.

Pharmacokinetics of hydroxychloroquine sulfate tablets

Hydroxychloroquine has similar pharmacological effects, pharmacokinetics and metabolic processes in vivo as chloroquine. After oral administration, hydroxychloroquine is quickly and almost completely absorbed. In one study, after a single dose of 400 mg of hydroxychloroquine was administered to healthy volunteers, the average peak plasma concentration was in the range of 53-208 ng / ml and the average level was 105 ng / ml. The average time to peak plasma concentration was 1.83 hours. According to the time after administration, the mean plasma elimination half-life changes are as follows: -10 hours, 10-48, and 48-504 hours after peak plasma concentrations are 5.9 hours, 26.1 hours, and 299 hours, respectively. The parent compounds and metabolites are widely distributed in the body, and elimination is mainly through urine. In one study, 3% of the administered dose was observed over 24 hours.

Hydroxychloroquine sulfate tablets storage

Sealed and stored below 25 ° C.

Packing of hydroxychloroquine sulfate tablets :

Aluminum plastic packaging, 10 pieces / box, 56 pieces / box, 60 pieces / box.

Validity of hydroxychloroquine sulfate tablets :

24 months

Implementation of hydroxychloroquine sulfate tablets

JX20030205