Hydroxychloroquine


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Discoid and systemic lupus erythematosus; Rheumatoid arthritis Initial: 400 mg/day as single or in 2 divided doses. Maintenance: 200-400 mg/day. Max: 6.5 mg/kg/day or 400 mg/day whichever is lower. Prophylaxis of malaria Initial: 400 mg once wkly, 2 wk before exposure and continued until 8 wk after exposure; if 2-wk lead-in period is not possible, 800 mg as loading dose in 2 divided doses 6 hr apart, then 400 mg once wkly, continued until 8 wk after exposure. All doses should be taken on same day of each wk. Acute malaria Initial: 800 mg, then 400 mg after 6-8 hr, and a further 400 mg once daily for 2 succeeding days; or 800 mg as single dose.
Dosage Details
Oral
Acute malaria
Adult: Initially, 800 mg, then 400 mg after 6-8 hr and a further 400 mg once daily for 2 succeeding days. Alternatively, 800 mg as single dose.
Child: Initially, 13 mg/kg as single dose then 6.5 mg/kg after 6, 24 and 48 hr.

Oral
Discoid and systemic lupus erythematosus, RA (rheumatoid arthritis)
Adult: Initially, 400 mg daily as single or in 2 divided doses. Maintenance: 200-400 mg daily, according to response. Max: 6.5 mg/kg/day or 400 mg daily, whichever is lower.
Child: Up to 6.5 mg/kg daily or 400 mg daily, whichever is lower.

Oral
Prophylaxis of malaria
Adult: Initially, 400 mg once wkly, 2 wk before exposure and continued until 8 wk after exposure. Alternatively, if 2-wk lead-in period is not possible, 800 mg as loading dose in 2 divided doses 6 hr apart, then 400 mg once wkly continued until 8 wk after exposure. All doses should be taken on same day of each wk.
Child: 6.5 mg/kg once wkly, 2 wk before exposure and continued until 8 wk after exposure. Alternatively, if 2-wk lead-in period is not possible, 13 mg/kg as loading dose in 2 divided doses 6 hr apart, then once wkly treatment for 8 wk after exposure. All doses should be taken on same day of each wk.
Administration
Should be taken with food.
Contraindications
Pre-existing maculopathy of the eye.
Special Precautions
Patient w/ G6PD deficiency, DM, haematological and GI disorders, alcoholism, porphyria, psoriasis. Renal and hepatic impairment. Childn. Pregnancy and lactation.
Adverse Reactions
Significant: Cardiomyopathy (e.g. AV block, pulmonary HTN, sick sinus syndrome), myocardial toxicity, QT interval prolongation, ventricular arrhythmia, torsade de pointes; skin reactions; bone marrow suppression (e.g. agranulocytosis, anaemia, aplastic anaemia, leucopenia, thrombocytopenia); proximal myopathy or neuromyopathy leading to progressive weakness, proximal muscle atrophy, depressed tendon reflexes, abnormal nerve conduction. Rarely, suicidal behaviour; keratopathy, retinopathy.
Nervous: Ataxia, dizziness, emotional disturbance, emotional lability, headache, irritability, lassitude, nerve deafness, nervousness, nightmares, psychosis, seizures, vertigo.
GI: Anorexia, diarrhoea, nausea, stomach cramps, vomiting.
Resp: Bronchospasm.
Hepatic: Acute hepatic failure. Rarely, hepatic insufficiency.
Endocrine: Exacerbation of porphyria, wt loss.
Haematologic: Haemolysis in G6PD deficiency.
Ophthalmologic: Accommodation disturbance, corneal changes (e.g. transient oedema, punctuate to linear opacities, decreased sensitivity, deposits, visual disturbances, blurred vision, photophobia), decreased visual acuity, macular oedema, nystagmus, optic disk disorder, retinal pigment changes, retinal vascular disease, retinitis pigmentosa, scotoma, vision color changes, visual field defect.
Otic: Tinnitus.
Dermatologic: Acute generalised exanthematous pustulosis, alopecia, bleaching of hair, bullous rash, dyschromia, annulare centrifugum erythema, erythema multiforme, exacerbation of psoriasis, exfoliative dermatitis, lichenoid eruption, maculopapular rash, morbilliform rash, pruritus, skin photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria, purpuric rash.
Immunologic: Hypersensitivity reactions (e.g. angioedema).
Potentially Fatal: Cardiac failure, severe hypoglycaemia.
Patient Counseling Information
This drug may cause dizziness and blurred vision, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor for signs/symptoms of cardiac compromise; CBC, serum glucose, proximal muscle strength and reflexes, LFT, renal function. Perform baseline and periodic eye examination.
Overdosage
Symptoms: Headache, visual disturbances, CV collapse, convulsions, and hypokalaemia. Rhythm and conduction disorders, including QT prolongation, Torsades de Pointes, ventricular tachycardia and ventricular fibrillation, followed by sudden potentially fatal resp and cardiac arrest. Management: Symptomatic and supportive treatment. Perform gastric lavage or emesis immediately. Activated charcoal can be introduced into the stomach by tube following lavage w/in 30 min of ingestion, given in a dose at least 5 times of the overdose to inhibit further absorption. Administer diazepam IV to reverse cardiotoxicity. Resp support and shock management should be instituted as needed.
Drug Interactions
Hydroxychloroquine may enhance the effect of hypoglycaemic agents. May increase plasma digoxin level. Increased risk of Torsades de pointes w/ QTc-prolonging agents (e.g. disopyramide, quinidine, amiodarone, sotalol, cisapride). Increased risk of convulsion w/ mefloquine. Antacids may interfere w/ hydroxychloroquine absorption.
Action
Description: Hydroxychloroquine is a 4-aminoquinoline derivative. It interferes w/ parasite digestive vacuoles by increasing pH and interfering w/ parasite’s ability to metabolise and utilise erythrocyte Hb. The mechanism of action in the treatment of rheumatoid arthritis and lupus erythematosus has not been fully elucidated.
Pharmacokinetics:
Absorption: Rapidly and completely absorbed. Time to peak plasma concentration: 1.83 hr.
Distribution: Widely distributed in the body. Crosses the placenta and enters breast milk (small amounts). Plasma protein binding: Approx 40%, mainly to albumin.
Metabolism: Metabolised in the liver into desethylhydroxychloroquine and desethylchloroquine (major metabolites) and small amount of bisdesethylchloroquine.
Excretion: Via urine (15-25% as metabolites, ≤60% as unchanged drug). Elimination half-life: Approx 40 days.
Chemical Structure

Chemical Structure Image
Hydroxychloroquine

Source: National Center for Biotechnology Information. PubChem Database. Hydroxychloroquine, CID=3652, https://pubchem.ncbi.nlm.nih.gov/compound/Hydroxychloroquine (accessed on Jan. 23, 2020)

Storage
Store between 20-25°C. Protect form light.
ATC Classification
P01BA02 - hydroxychloroquine ; Belongs to the class of aminoquinoline antimalarials.
References
Anon. Hydroxychloroquine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 28/06/2017.

Buckingham R (ed). Hydroxychloroquine Sulfate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 28/06/2017.

Joint Formulary Committee. Hydroxychloroquine Sulfate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 28/06/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Hydroxychloroquine Sulfate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 28/06/2017.

Plaquenil 200mg Film-Coated Tablets (Winthrop Pharmaceuticals UK Limited). MHRA. https://products.mhra.gov.uk/. Accessed 28/06/2017.

Plaquenil Tablet (Concordia Pharmaceuticals Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 28/06/2017.

Plaquenil Tablet Film Coated (Sanofi-Aventis US LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 28/06/2017.

Disclaimer: This information is independently developed by MIMS based on Hydroxychloroquine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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