Chloroquine Sulphate

These indications are based on manufacturer information for both originator and generic products. For product specific registered indications, please refer to product specific manufacturer information

Registered South African indications: 

• Malaria prophylaxis, in areas where there is no chloroquine resistance
• Malaria treatment, provided malaria was not contracted in a chloroquine-resistant area and chloroquine prophylaxis was not taken
• Adjuvant management of rheumatoid arthritis and discoid and systemic lupus erythematosus

---

See additional prescribing points regarding comments about use during the COVID-19 pandemic 

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Coadministration with amiodarone
• Porphyria

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment
• Hepatic impairment
  - Cirrhosis
• Elderly
• Diabetes mellitus
• Congenital or documented acquired QT interval prolongation
• Known risk factors for QT interval prolongation:
  - Cardiac disease, e.g. heart failure, myocardial infarction
  - Proarrhythmic conditions, e.g. bradycardia
  - History of ventricular dysrhythmias
  - Uncorrected hypokalemia and/or hypomagnesemia
  - Coadministration with QT interval prolonging agents
• Long-term high dose therapy
• High alcohol intake
• History of epilepsy, convulsions and other neurological disorders
• Psoriasis
• Coadministration with agents known to induce blood disorders
• Glucose-6-phosphate dehydrogenase deficiency
• Fructose intolerance (syr)
• Glucose-galactose malabsorption (syr)
• Sucrase-isomaltase insufficiency (syr)
• May impair ability to drive or operate machinery

Forms avail. in SA and covered in this monograph: cap, tab

Adult dosages below include:

• South African Standard Treatment Guidelines indications and dosages
• South African registered indications and dosages
• Indications and dosages registered in other jurisdictions

Infections caused by: Plasmodium falciparum; Plasmodium malariae; Plasmodium vivax; Plasmodium ovale

---

Note: 

200mg chloroquine sulphate is equivalent to 150mg chloroquine base

200mg chloroquine sulphate monohydrate is equivalent to 146,7mg chloroquine base

---

Specific doses based on individual indications

Please note that the dosages below should be used in combination with regional guidelines, taking into account local antibiotic sensitivities

South African Standard Treatment Guidelines indications and dosages

Rheumatoid arthritis (Additional agent(s) may be required)

• Oral (tab): 200mg chloroquine sulphate (i.e 150mg chloroquine base), dly, 5 days per week
  (STG, Adult 2019)

Systemic lupus erythematosus (SLE)
- To suppress disease activity

• Oral (tab): 200mg chloroquine sulphate (i.e 150mg chloroquine base), dly, 5 days per week
  (STG, Adult 2019)

---

South African registered indications and dosages

Prevention of malaria

• Oral (tab,cap); 400mg chloroquine salt (i.e. 300mg chloroquine base (tab) or 295.6mg chloroquine base (cap)), weekly  

---

The above dose should be taken on the same day each week, with food. It is advisable to start taking it 1-2 weeks (if not possible, at least 24hrs) before entering an endemic area and to continue for at least 4-6 weeks after leaving

---

Treatment of malaria 

• Oral (tab, cap): Initial: 800mg chloroquine salt (i.e. 600mg chloroquine base (tab) or 586,8mg chloroquine base (cap)); Then: 400mg chloroquine salt (i.e. 300mg chloroquine base (tab) or 295.6mg chloroquine base (cap)), 6-8 hours after initial dose; Then 400mg chloroquine salt (i.e. 300mg chloroquine base (tab) or 295.6mg chloroquine base (cap), dly, for 2 days

---

Treatment should be adjusted to the severity of the infection, the condition, and the age and weight of the patient

---

Rheumatoid arthritis

• Oral (tab): 200mg chloroquine salt (i.e. 150mg chloroquine base), dly

Discoid and systemic lupus erythematosus

• Oral (tab): 200-400mg chloroquine salt (i.e. 150-300mg chloroquine base), dly; Titrate dose down gradually once symptoms controlled

---

Indications and dosages registered in other jurisdictions

Treatment of malaria
- Non-immune

• Oral (tab): Initial: 1g chloroquine salt (i.e. 620mg chloroquine base), as a single dose; Then: 500mg chloroquine salt (i.e. 310mg chloroquine base), 6hrs after initial dose; Then: 500mg chloroquine salt (i.e. 310mg chloroquine base), dly, for 2 days

---

For P.vivax and P.ovale infections, follow chloroquine treatment with a course of treatment with primaquine if a radical cure is required

---

OR

• Oral (syr): Initial: 960mg chloroquine salt (i.e. 600mg chloroquine base), as a single dose; Then: 480mg chloroquine salt (i.e. 300mg chloroquine base), 6 hours after initial dose; Then: 480mg chloroquine salt (i.e. 300mg chloroquine base), dly; Treatment duration: 2 days

- Partially-immune

• Oral (syr): 960mg chloroquine salt (i.e. 600mg chloroquine base), as a single dose

Prophylaxis and suppression of malaria
- Non-immune

• Oral (tab): 500mg chloroquine salt (i.e. 310mg chloroquine base), weekly, on the same day each week

OR

• Oral (syr): 480mg chloroquine salt (i.e. 300mg chloroquine base), weekly, on the same day each week

---

Start 7 days before exposure to risk and continue until 4 weeks after leaving the malarious area

---

- Partially-immune

• Oral (syr): 240mg chloroquine salt (i.e. 150mg chloroquine base), every two weeks

Amoebic hepatitis

• Oral (tab): Initial: 1g chloroquine salt (i.e. 620mg chloroquine base), dly, for 2 days; Then: 250mg chloroquine salt (i.e. 155mg chloroquine base), 12hrly, for 2-3 weeks

Lupus erythematosus

• Oral (tab): Initial: 250mg chloroquine salt (i.e. 155mg chloroquine base), 12hrly, for 1-2 weeks; Maintenance: 250mg chloroquine salt (i.e. 155mg chloroquine base), dly

Rheumatoid Arthritis

• Oral (tab): 250mg chloroquine salt (i.e. 155mg chloroquine base), dly

Paed. forms avail. in SA and covered in this monograph: cap, tab, syr

Paed. dosages below include:

• South African Standard Treatment Guidelines indications and dosages
• South African registered indications and dosages
• Indications and dosages registered in other jurisdictions

Infections caused by: Plasmodium falciparum; Plasmodium malariae; Plasmodium vivax; Plasmodium ovale

---

Note:

Each 5ml contains: Chloroquine sulphate 68mg equivalent to 50mg chloroquine base

200mg Chloroquine sulphate is equivalent to 150mg chloroquine base

200mg Chloroquine sulphate monohydrate is equivalent to 146,7mg chloroquine base

---

Specific doses based on individual indications

Please note that the dosages below should be used in combination with regional guidelines, taking into account local antibiotic sensitivities

South African Standard Treatment Guidelines indications and dosages

Treatment of P. Malariae
Treatment of P. Ovale and P. Vivax  (Additional agent required)

• Oral (tab, syr): Initial: 10mg/kg chloroquine base; Then: 5mg/kg chloroquine base given 6hrs, 24hrs and 48hrs after first dose
  (STG, Paed. 2017)

Systemic lupus erythematosus

• Oral (tab, syr): 5mg/kg chloroquine base, dly; Max: 150mg/24hrs
  (STG, Paed. 2017)

---

South African registered indications and dosages

Treatment of malaria

Oral (tab)

• Younger than 12 years: Initial: 10mg/kg chloroquine base; Then: 5mg/kg chloroquine base 6-8hrs after initial dose; Then: 5mg/kg chloroquine base, dly, for 2 days
•  12 years and older: See adult dosage

Oral (cap)

• Younger than 6 years: No information available
• Between 6-12 years: 294mg chloroquine base, as a single dose; Then: 147mg chloroquine base after 6hrs; Then: 147mg chloroquine base, dly: Treatment duration: 2 days
• Older than 12 years: See adult dosage

Oral (syr)

• 10 years and younger: Initial: 10mg/kg chloroquine base; Then: 5mg/kg chloroquine base 6-8hrs after initial dose; Then: 5mg/kg chloroquine base, dly, for 2 days; Max: 25mg/kg chloroquine base/72hrs
• Older than 10 years: No information available

OR

• 10 years and younger: Initial: 10mg/kg chloroquine base, dly for the first 2 days; Then: 5mg/kg chloroquine base on day 3; Max: 25mg/kg chloroquine base/72hrs 
• Older than 10 years: No information available

---

Use of the syrup formulation is recommended for children ≤10 years

---

Prevention of malaria

Oral (syr, tab)

• Younger than 12 years: 5mg/kg chloroquine base, weekly, on the same day each week
• Older than 12 years: See adult dosage

---

Tablets should be taken with food 

---

Oral (cap)

• Younger than 6 years: No information available
• Between 6-12 years: 146.7mg chloroquine base, weekly
• Older than 12 years: See adult dosage

---

 It is advisable to start taking chloroquine 1-2 weeks (if not possible, at least 24hrs) before entering an endemic area and to continue for at least 4-6 weeks after leaving the malarious area

---

No specific dosages for children provided in South African manufacturer recommendations for rheumatoid arthritis and discoid and systemic lupus erythematosus

---

Indications and dosages registered in other jurisdictions

Treatment of malaria

Oral (tab)

• Younger than 1 year: No information available
• Between 1-14 years: Initial: 10mg/kg chloroquine base, as a single dose; Then: 5mg/kg chloroquine base 6hrs after initial dose; Then: 5mg/kg chloroquine base for 2 days
• Older than 14 years: See adult dosage

---

For P.vivax and P.ovale infections, follow chloroquine treatment with a course of treatment with primaquine if a radical cure is required

---

- Non-immune

Oral (syr)

• 1 year and younger: 50-100mg chloroquine base, as a single dose; Then: 25-50mg chloroquine base 6hrs later; Then: 25-50mg chloroquine base, dly, for 2 days
• Between 1-3 years: 150-200mg chloroquine base, as a single dose; Then: 75-100mg chloroquine base 6hrs later; Then: 75-100mg chloroquine base, dly, for 2 days
• Between 3-6 years: 200-300mg chloroquine base, as a single dose; Then: 100-150mg chloroquine base 6hrs later; Then: 100-150mg chloroquine base, dly, for 2 days
• Between 6-9 years: 300-450mg chloroquine base, as a single dose; Then: 150-225mg chloroquine base 6hrs later; Then: 150-225mg chloroquine base, dly, for 2 days
• Between 9-12 years: 450-600mg chloroquine base, as a single dose; Then: 225-300mg chloroquine base 6hrs later; Then: 225-300mg chloroquine base, dly, for 2 days
• Older than 12 years: See adult dosage

-Partially immune

Oral (syr)

• Younger than 1 year: 50-100mg chloroquine base, as a single dose
• Between 1-3 years: 150-200mg chloroquine base, as a single dose
• Between 3-6 years: 200-300mg chloroquine base, as a single dose
• Between 6-9 years: 300-450mg chloroquine base, as a single dose
• Between 9-12 years: 450-600mg chloroquine base, as a single dose
• Older than 12 years: See adult dosage

Prophylaxis of malaria

Oral (tab)

• Younger than 1 year: No information available
• Between 1-14 years: 5mg/kg chloroquine base, weekly, on the same day each week
• Older than 14 years: See adult dosage

---

Start 7 days before exposure to risk and continue until 4 weeks after leaving the malarious area

---

- Non-immune

Oral (syr)

• Younger than 1 year: 25-50mg chloroquine base, weekly
• Between 1-3 years: 75-100mg chloroquine base, weekly
• Between 3-6 years: 100-150mg chloroquine base, weekly
• Between 6-9 years: 150-225mg chloroquine base, weekly
• Between 9-12 years: 225-300mg chloroquine base, weekly
• Older than 12 years: See adult dosage

---

Start 7 days before exposure to risk and continue until 4 weeks after leaving the malarious area

---

- Partially immune

Oral (syr)

• Younger than 1 year: 12.5-25mg chloroquine base, every two weeks
• Between 1-3 years: 37.5-50mg chloroquine base, every two weeks
• Between 3-6 years: 50-75mg chloroquine base, every two weeks
• Between 6-9 years: 75-112.5mg chloroquine base, every two weeks  
• Between 9-12 years: 112.5-150mg chloroquine base, every two weeks
• Older than 12 years: See adult dosage

Pregnancy

• Caution
• Chloroquine should not be used during pregnancy unless, in the judgement of the physician, the potential benefit outweighs the risk
• Short-term malaria prophylaxis: Malaria in pregnant women increases the risk of maternal death, miscarriage, stillbirth and low birth weight with the associated risk of neonatal death. Travel to malarious areas should be avoided during pregnancy, but, if this is not possible, women should receive effective prophylaxis
• Long-term high dose: There is evidence to suggest that chloroquine given to women in high doses throughout pregnancy can give rise to foetal abnormalities including visual loss, ototoxicity and cochlear-vestibular dysfunction

Breastfeeding

• Malaria prophylaxis: Caution
  Rheumatoid arthritis: Caution; not recommended
• Chloroquine is excreted in breastmilk, although amounts are probably too small to be harmful when used for malaria prophylaxis as a consequence they are insufficient to protect the infant. Separate chemoprophylaxis for the infant is required. However, when long-term high doses are used for rheumatoid disease, breastfeeding is not recommended

Renal Impairment

• Caution; no dose adjustment recommended

Hepatic Impairment

• Caution; no dose adjustment recommended

Elderly

• Caution; no dose adjustment recommended
  There are no special dosage recommendations for the elderly, but it may be advisable to monitor elderly patients so that optimum dosage can be individually determined

Porphyria Information

• Possibly porphyrinogenic (PSP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Hallucinations
• Psychotic disorder
  - Anxiety
  - Personality change
• Insomnia
• Confusion
• Depression
• Seizures
• Visual field defects
• Headache
• Neuromyopathy
• Acute extrapyramidal disorders
  - Dystonia
  - Dyskinesia
  - Tongue protrusion
  - Torticollis

Cardiovascular Disorders

• Cardiomyopathy
• Atrioventricular block
• QT prolongation
• Hypotension
• ECG changes

Respiratory Disorders

• Diffuse parenchymal lung disease

Gastrointestinal Disorders

• Nausea and vomiting
• Diarrhoea
• Abdominal pain

Hepatobiliary Disorders

• Changes in hepatic function
• Hepatitis  
• Abnormal hepatic function tests

Endocrine and Metabolic Disorders

• Hypoglycaemia

Musculoskeletal Disorders

• Myopathy

Skin and Subcutaneous Tissue Disorders

• Macular, urticarial and purpuric skin eruptions
• Alopecia
• Erythema multiforme
• Drug reaction with eosinophilia and systemic symptoms syndrome
• Stevens-Johnson syndrome  
• Toxic epidermal necrolysis  
• Precipitation of psoriasis
• Pruritus
• Photosensitivity reaction
• Lichenoid keratosis
• Pigmentation disorder (long term use)
• Exfoliative dermatitis
• Acute generalised exanthematous pustulosis  

Immune, Blood and Lymphatic System Disorders

• Bone marrow failure
• Aplastic anaemia
• Agranulocytosis
• Thrombocytopenia
• Neutropenia
• Pancytopenia
• Hypersensitivity and anaphylactic reactions
  - Urticaria
  - Angioedema
  - Vasculitis

Sensory Disorders

• Retinal degeneration
• Macular defects of colour vision
• Pigmentation
• Optic atrophy scotomas
• Blindness
• Corneal opacity and pigmented deposits
• Blurred vision
• Accommodation disorder
• Diplopia
• Tinnitus
• Hypoacusis
• Neurosensory deafness

• Amiodarone
• QT interval prolonging agents
• Class IA and III antiarrhythmics
• Tricyclic antidepressants
• Antipsychotics
• Moxifloxacin
• Droperidol
• Halofantrine
• Antacids (aluminium, calcium and magnesium salts) (See additional prescribing points)
• Adsorbents
• Kaolin
• Ciclosporin
• Intradermal human diploid-cell rabies vaccine (See additional prescribing points)
• Oral typhoid vaccine (See additional prescribing points)
• Praziquantel
• Mefloquine
• Digoxin
• Cimetidine
• Multidrug and toxin extrusion protein (MATE1) inhibitors
• Ciprofloxacin
• Omeprazole
• Pyrimethamine
• Urinary alkalinizers
• Antiepileptic agents
• Levothyroxine
• Agalsidase
• Neostigmine
• Pyridostigmine

None routine. Specific cases may require

• Ophthalmic examination
• Full blood count
• Hepatic function
• Renal function
• Blood glucose
• ECG

Additional observations

• Muscle strength (long term use)

Tablet 200mg, Syrup 68mg/5ml - EML (Hospital)

---

Interactions

• Antacids (such as aluminium, calcium and magnesium salts) and adsorbents (such as kaolin) may reduce the absorption of chloroquine, so should be administered at least four hours apart
• Pre-exposure intradermal human diploid-cell rabies vaccine should not be administered to patients taking chloroquine as this may suppress the antibody response. When vaccinated against rabies, that vaccine should precede the start of the antimalarial dosing, otherwise the effectiveness of the vaccine might be reduced
• Concomitant administration of chloroquine inactivates oral typhoid vaccine, so the vaccine should be completed at least three days before the first dose of chloroquine

COVID-19 potential therapeutic use

• Based upon limited in-vitro and anecdotal data, both chloroquine (sulphate and phosphate) and hydroxychloroquine citrate are currently investigated by some medical centres and organisations as a potential agent for the management of hospitalised critical clinical cases of COVID-19
• The US-based Centers for Disease Control and Prevention (CDC) says that while chloroquine and hydroxychloroquine are currently recommended for treatment against COVID-19 in some countries, they are still currently under investigation in clinical trials for use in the US. There is no currently available data “to inform clinical use, dosing, or duration of hydroxychloroquine for prophylaxis or treatment of COVID-19 infection. [https://www.cdc.gov/coronavirus/2019-ncov/hcp/therapeutic-options.html]

'Chloroquine base' contents per volume

• The dose of chloroquine sulphate must be calculated based on the 'chloroquine base' equivalent:
•  * Each capsule of Plasmaquine® contains 200mg of chloroquine sulphate (equivalent to 146.7mg chloroquine base)
• * Each tablet of Nivaquine® contains 200mg of chloroquine sulphate (equivalent to 150mg chloroquine base)
• * Each 5mL of Miraquin® syrup contains 68mg of chloroquine sulphate (equivalent to 50mg chloroquine base)

The mode of action of chloroquine on plasmodia has not been fully elucidated. Chloroquine binds to and alters the properties of DNA. Chloroquine also binds to ferriprotoporphyrin IX and this leads to lysis of the plasmodial membrane. In suppressive treatment, chloroquine inhibits the erythrocytic stage of development of plasmodia. In acute attacks of malaria, it interrupts erythrocytic schizogony of the parasite. Its ability to concentrate in parasitised erythrocytes may account for the selective toxicity against the erythrocytic stages of plasmodial infection.

Spectrum of activity: Plasmodium falciparum; Plasmodium malariae; Plasmodium vivax; Plasmodium ovale

Tablet 200mg 

• Nivaquine (Zentiva) originator - Each tablet of Nivaquine® contains 200mg of chloroquine sulphate (equivalent to 150mg chloroquine base)

Capsule 200mg 

• Plasmoquine (Medchem) originator - Each capsule of Plasmaquine® contains 200mg of chloroquine sulphate (equivalent to 146.7mg chloroquine base)

Syrup (per 5ml) 68mg 

• Mirquin (Cipla Medpro) - Each 5mL of Miraquin® syrup contains 68mg of chloroquine sulphate (equivalent to 50mg chloroquine base)