Full Prescribing Info
Hydroxychloroquine sulfate.
Each film-coated tablet contains: Hydroxychloroquine Sulfate 200 mg.
Pharmacology: Pharmacokinetics: Hydroxychloroquine has action, pharmacokinetics and metabolism similar to Chloroquine. After oral administration, Hydroxychloroquine is absorbed rapidly and almost entirely.
Treatment of systemic lupus erythematosus.
Dosage/Direction for Use
Adult (including elderly): The minimum effective dose must be given. The dosage should not exceed 6.5 mg/kg/day (calculated based on ideal body weight and not actual weight) and between 200 mg or 400 mg per day. The dosage above 400 mg are not recommended.
Patients who can receive 400 mg per day: The initial dose is 400 mg in divided doses. The dosage can be reduced to 200 mg if there is no improvement. The maintenance dose must be increased to 400 mg per day if the response is not adequate.
Children: The minimum effective dose should be given and should not exceed 6.5 mg/kg/day based on ideal body weight. Therefore, the dosage of 200 mg is not appropriate for use in children with an ideal body weight of less than 31 kg.
This drug must be taken with food or a glass of milk.
The therapeutic effect of Hydroxychloroquine is only seen after using within a few weeks when mild side effects occur early. In patients with conditions sensitive to light, treatment must be given only when the patient gets maximum exposure to light.
Overdosage of 4-aminoquinolone is especially dangerous for the fetus, although only 1-2 g is proven to be fatal. Symptoms of overdosage include headaches, visual disturbances, heart failure and seizures, hypokalemia, disorder of heart rhythm and conduction, including QT prolongation, torsade de pointes, ventricular tachycardia and ventricular fibrillation, followed by sudden cessation of heart beat and breathing. The possibility of these symptoms appear after the administration of large doses. The treatment must be done immediately and symptomatic. Gastric emptying must be performed immediately, either by vomiting or gastric drainage. Activated carbon with five times dosage of the taken dosage (overdose) minimally can inhibit further absorption if inserted into the stomach through a nasogastric tube followed by gastric drainage in 30 minutes after overdosage.
Parenteral administration of Diazepam should be considered in cases of overdosage, because it has been shown to improve Chloroquine cardiotoxicity.
Rescue breathing may be needed and the need of intubation or tracheostomy management can be considered. The condition of shock must be treated by administering fluids (plasma solution expanders if needed) and monitoring central venous pressure. In severe cases, administration of Dopamine must be considered.
Patients who survive from acute and asymptomatic phase must be observed for at least 6 hours.
Fluid administration may have to be forced and a certain amount of Ammonium Chloride (8 g daily in divided doses in adult patients) may have to be administered for several days to acidify urine. This action triggers urine excretion in cases of overdosage or sensitivity. However, caution must be taken in patients with impaired kidney function or metabolic acidosis.
Hypersensitivity to 4-aminoquinolone compounds.
Patients with eye maculopathy.
Pregnant women (see Use in Pregnancy & Lactation).
Children under 6 years old (200 mg tablets not allowed for body weight < 31 kgs).
Special Precautions
General: Retinopathy is very rare if the recommended daily dose is not exceeded. Dosing above the maximum dose can increase the risk of retinopathy and speed up its onset.
All patients must undergo an ophthalmological examination prior to Hydroxychloroquine treatment. After that, the ophthalmological examination must be repeated at least once every 12 months.
Children are very sensitive to the toxic effects of the 4-aminoquinolone compound; therefore parents should be warned that hydroxychloroquine must not be within the reach of children. Testing should include examining visual acuity, ophthalmoscopy, funduscopy, central visual field testing with red targets and color vision.
This examination should be more frequent and adjusted to the following patient: Daily dose exceeds 6.5 mg/kg body weight. Absolute body weight used as a guide for dosing can cause overdose for patients with obesity; Impaired kidney function; Visual acuity below 6/8; Age over 65 years; Cumulative doses of more than 200 g.
Hydroxychloroquine must be stopped immediately in patients who experience pigment abnormalities, vision problems, or other abnormalities that cannot be explained due to corneal opacification. Patients must be observed regularly.
Patients are advised to stop treatment immediately and seek medical help from a doctor if there are visual impairments, including abnormal color vision.
The concomitant drugs that can induce retinal toxicity, such as Tamoxifen is not recommended.
Hypoglycemia: Hydroxychloroquine has been shown to cause severe hypoglycemia including loss of life-threatening awareness in patients treated concomitantly or without antidiabetic drugs (see INTERACTIONS and ADVERSE REACTIONS). Patients treated with Hydroxychloroquine should be warned about the risk of hypoglycemia, associated clinical signs and symptoms. Patients who experience clinical symptoms of hypoglycemia should have their blood glucose levels checked and monitored during treatment with Hydroxychloroquine. Extrapyramidal disorders can occur if following by Hydroxychloroquine therapy (see ADVERSE REACTIONS).
Cardiovascular: Cases of cardiomyopathy that cause heart failure and in some cases cause fatality, have been reported in patients treated with Hydroxychloroquine (see OVERDOSAGE and ADVERSE REACTIONS). Clinical monitoring of cardiomyopathy signs and symptoms is recommended. Hydroxychloroquine must be stopped if cardiomyopathy occurs. Chronic toxicity must be considered when conduction disorders including biventricular hypertrophy are found (see ADVERSE REACTIONS).
Hydroxychloroquine can induce cardiac arrhythmias: Hydroxychloroquine extends QT interval. Ventricular arrhythmias and torsades de pointes have been reported in patients using Hydroxychloroquine. Therefore, Hydroxychloroquine should not be used with other drugs that have the potential to extend QT interval.
Hydroxychloroquine must be used with caution for individuals who are known to have heart disease or patients with families who have a history of unexpected death with cardiac arrhythmias and factor in the extension of QT/QTc.
Other monitoring of long-term treatment: Hydroxychloroquine must be used with caution in patients taking drugs that can cause adverse reactions on eye or skin. Caution on usage in: Patients with liver or kidney disease, and in patients using drugs that are known to affect these organs.
Estimated Hydroxychloroquine plasma levels should be considered in patients with impaired kidney and liver function for dose adjustments.
Patients with gastrointestinal, neurological or blood disorders.
Although the risk of bone marrow depression is low, periodic blood tests are recommended because the incidence of aplastic anemia, agranulocytosis, decreased white blood cells, and thrombocytopenia have been reported. Hydroxychloroquine must be stopped if abnormalities occur.
Caution is also recommended in patients with allergies to Quinine, glucose-6-phosphate dehydrogenase deficiency, and porphyria cutanea tarda which can be aggravated by Hydroxychloroquine and in patients with psoriasis which can increase the risk of skin reactions.
Patients with rare hereditary problems namely galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption should not use this drug.
All patients on long-term therapy must undergo regular check-up of skeletal muscle function and tendon reflexes. If the muscles become weak, treatment must be stopped.
Potential carcinogen risk: An experimental data indicate a potential risk of inducing gene mutations. Animal carcinogenicity data are only available for one species for Chloroquine and the results are negative. There are not enough evidence to rule out an increased risk of cancer in patients receiving long-term treatment in humans. Long-term studies in animals have not been established to evaluate the carcinogenic potential of Hydroxychloroquine. The mutagenic potential of Hydroxychloroquine was not evaluated. However, Chloroquine has been proven as a catalytic inhibitor of DNA repair enzymes (topoisomerase II) and to produce weak genotoxic effects through this action.
Effects in driving and operating machines: Visual accommodation disturbances immediately after the start of treatment have been reported and patients should be warned about driving or operating machines. This can be overcome by reducing the dose or stopping treatment.
Use in Pregnancy and Lactation: A related chemical compound, Chloroquine Phosphate, has been found to cause damage to the fetal and retinal cochlea when consumed in high doses during pregnancy, therefore Hydroxychloroquine should not be consumed during pregnancy. Careful consideration must be given when using Hydroxychloroquine during breast-feeding, because it has been shown to be excreted in small amounts through breast milk, and it is known that babies are very sensitive to the toxic effects of 4-aminoquinolones.
Use In Pregnancy & Lactation
A related chemical compound, Chloroquine Phosphate, has been found to cause damage to the fetal and retinal cochlea when consumed in high doses during pregnancy, therefore Hydroxychloroquine should not be consumed during pregnancy. Careful consideration must be given when using Hydroxychloroquine during breast-feeding, because it has been shown to be excreted in small amounts through breast milk, and it is known that babies are very sensitive to the toxic effects of 4-aminoquinolones.
Adverse Reactions
Eye disorders: Retinopathy with changes in pigmentation and visual disturbances can occur (bull's eye appearance), but it is very rare if the recommended daily dose is not exceeded. Initially it appears reversible on Hydroxychloroquine discontinuation, but if it left unchecked there will be a risk of progression even after discontinue the drug. Patients with retinal changes may be asymptomatic initially, or may have vision of scotoma with the type of paracetamol, pericentral ring, temporal scotoma and abnormal color vision at first; Visibility disorders (visual field defect/paracentral scotomas); Impaired vision (visual activity); Decreased adaptation to dark; Abnormal color vision; Blurred vision due to accommodation disorders that are dose dependent and reversible; Corneal changes including edema and unclear vision were reported. It does not cause symptoms or can cause disturbances such as halo, blurred vision or photophobia. It may be temporary and reversible at discontinuation of treatment; Cases of maculopathy and macular degeneration have been reported and may not be recovered.
Cardiac disorders: Cardiomyopathy can cause heart failure and fatal events in some cases (see OVERDOSAGE and PRECAUTIONS); Chronic toxicity must be considered when conduction disorders (atrioventricular heart block) and biventricular hypertrophy are found. Withdrawal of the drug can lead to recovery; Hydroxychloroquine can extend the QT interval; Ventricular arrhythmias and torsade de pointes.
Immune system disorders: Urticaria; Angioderma; Bronchospasm.
Skin and subcutaneous tissue disorders: Skin rash; Pruritus; Pigmentation disorders of the skin and mucous membranes; Bleaching hair; Alopecia; Bullous eruptions including erythema multiform, Stevens-Johnson syndrome, and toxic epidermal necrolysis, drug rash with eosinophilia and systemic symptoms (DRESS syndrome), photosensitivity, exfoliative dermatitis, acute generalized exanthematous pustulosis (AGEP). AGEP must be distinguished from psoriasis. This is related to fever and hyperleukocytosis. The expected results usually appear after drug discontinuation.
Gastrointestinal disorders: Abdominal pain; Nausea; Diarrhea; Vomiting. These symptoms are usually treated immediately by reducing the dose or discontinue the treatment.
Nervous system disorders: Headache; Dizziness; Convulsions have been reported in this class of drugs; Extrapyramidal disorders such as dystonia, dyskinesia, tremor (see PRECAUTIONS).
Psychiatric disorders:
Affect instability; Restless; Psychosis; Nightmare; Irritability; Suicidal behavior.
Ear and labyrinth disorders: Vertigo; Tinnitus; Hearing disorders.
Musculoskeletal and connective tissue disorders: Sensorimotor disorders; Skeletal muscle myopathy or neuromyopathy which leads to progressive weakness and atrophy of proximal muscle tissue. Myopathy may be reversible after drug withdrawal, but recovery can take months; Tendon reflex depression and abnormal nerve conduction study.
Blood and lymphatic system disorders: Bone marrow depression; Anemia; Aplastic anemia; Agranulocytosis; Leukopenia; Thrombocytopenia; Hemolysis was reported in individuals who have glucose-6-phosphate dehydrogenase (G-6-PD) deficiency.
Metabolic and nutritional disorders: Anorexia; Hypoglycemia; Hydroxychloroquine can worsen porphyria; Decreased appetite; Weight loss.
Hepatobiliary disorders: Abnormal liver function tests; Fulminant liver failure.
Drug Interactions
Digoxin: Hydroxychloroquine can increase serum Digoxin levels so it needs to be monitored regularly.
Insulin or antidiabetic drugs: Hydroxychloroquine can trigger hypoglycemia effects, decrease insulin doses or antidiabetic drugs may be needed.
Drugs that can extend the QT interval and arrhythmia drugs: Hydroxychloroquine can extend the QT interval therefore it should not be used concomitantly with other drugs that have the potential to induce cardiac arrhythmias. In addition, Hydroxychloroquine can increase the risk of ventricular arrhythmia if used concomitantly with arrhythmia drugs. Mefloquine and other drugs that are known to reduce convulsive threshold: Hydroxychloroquine can reduce conclusive threshold, therefore concomitant use with drugs that reduce conclusive threshold (eg: Mefloquine) can increase the risk of convulsions.
Antiepileptic: Hydroxychloroquine can reduce the seizure threshold. Concomitant use of Hydroxychloroquine with other anti-malarials known to reduce seizures (eg: Mefloquine) can increase the risk of seizures. In addition, antiepileptic drug activity can be disrupted if used concomitantly with Hydroxychloroquine.
Methotrexate: Concomitant use with Hydroxychloroquine can increase side effects.
Cyclosporine: Increased Cyclosporine levels are reported when Cyclosporine and Hydroxychloroquine are used concomitantly.
The following interactions have been observed in treatment with similar compounds to Chloroquine Phosphate and cannot be separated from Hydroxychloroquine: Praziquantel: In a study of single-dose interactions, Chloroquine has been reported to reduce the bioavailability of Praziquantel. It is not known whether there is a similar effect when Hydroxychloroquine and Praziquantel are used concomitantly. Due to the similarity in structure and pharmacokinetic parameters between Hydroxychloroquine and Chloroquine, a similar effect can occur on Hydroxychloroquine.
Antacids and Kaolin: Antacids and Kaolin can reduce absorption of Chloroquine.
Cimetidine: Cimetidine can inhibit Chloroquine metabolism and increase Chloroquine concentration in blood plasma. The concomitant use of these two drugs must be avoided.
Ampicillin: Chloroquine can significantly reduce the Ampicillin bioavailability.
Store below 30°C, away from light.
ATC Classification
P01BA02 - hydroxychloroquine ; Belongs to the class of aminoquinoline antimalarials.
FC tab 200 mg x 6 x 10's.
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