Chloroquine

Brands Names of Chloroquine in Kenya

Cosmoquin , Cosmos Limited


Chloroquine in Kenya: Brands, Uses, Usage in Covid 19, Prices
Chloroquine Chemical Structure

MODE OF ACTION

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.

INDICATIONS

a) Treatment of malaria.

b) Prophylaxis and suppression of malaria.

c) Treatment of amoebic hepatitis and abscess.

d) Treatment of discoid and systemic lupus erythematosus.

e) Treatment of rheumatoid arthritis.

DOSAGE AND ADMINISTRATION

a) Treatment of malaria

i) P. falciparum and P. malariae infections

Adults: A single dose of four tablets, followed by two tablets six hours later and then two tablets a day for two days.

Children: A single dose of 10mg base/kg, followed by 5mg base/kg six hours later and then 5mg base/kg a day for two days.

Age (years)Initial doseSecond dose 6 hours after firstDose on each of the two subsequent days
1 – 41 Tablet½ Tablet½Tablet
5 – 82 Tablets1 Tablet1 Tablet
9 -143 Tablets1½ Tablets1½ Tablets

ii) P. vivax and P. ovale infections

Adults: A single dose of four tablets, followed by two tablets six hours later and then two tablets a day for two days. Follow with a course of treatment with primaquine if a radical cure is required.

Children: A single dose of 10mg base/kg, followed by 5mg base/kg six hours later and then 5mg base/kg a day for two days. Follow with a course of treatment with primaquine if a radical cure is required.

Elderly Patients: 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.

Hepatic or Renally Impaired Patients: Caution is necessary when giving Avloclor to patients with renal disease or hepatic disease.

b) Prophylaxis and suppression of malaria

Adults: Two tablets taken once a week, on the same day each week. Start one week before exposure to risk and continue until four weeks after leaving the malarious area.

Children: A single dose of 5mg chloroquine base/kg per week on the same day each week. Start one week before exposure to risk and continue until four weeks after leaving the malarious area.

For practical purposes, children aged over 14 years may be treated as adults. The dose given to infants and children should be calculated on their body weight and must not exceed the adult dose regardless of weight.

1 – 4 years ½ tablet

5 – 8 years 1 tablet

9 – 14 years 1½ tablets

Elderly Patients: 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.

Hepatic or Renally Impaired Patients: Caution is necessary when giving Avloclor to patients with renal disease or hepatic disease.

c) Amoebic hepatitis

Adults: Four tablets daily for two days followed by one tablet twice daily for two or three weeks.

Elderly Patients: 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.

Hepatic or Renally Impaired Patients: Caution is necessary when giving Avloclor to patients with renal disease or hepatic disease.

d) Lupus erythematosus

Adults: One tablet twice daily for one to two weeks followed by a maintenance dosage of one tablet daily.

Elderly Patients: 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.

Hepatic or Renally Impaired Patients: Caution is necessary when giving Avloclor to patients with renal disease or hepatic disease.

e) Rheumatoid arthritis

Adults: The usual dosage is one tablet daily.

Elderly Patients: 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.

Hepatic or Renally Impaired Patients: Caution is necessary when giving Avloclor to patients with renal disease or hepatic disease.

CONTRAINDICATIONS

Known hypersensitivity to chloroquine or any other ingredients of the formulation.

Concomitant use with amiodarone.

DRUG INTERACTIONS

Chloroquine should be used with caution in patients receiving drugs known to prolong the QT interval e.g. Class IA and III antiarrhythmics, tricyclic antidepressants, antipsychotics, some anti-infectives due to increased risk of ventricular arrhythmia

Halofantrine should not be administered with chloroquine.

In particular, amiodarone should not be used and its use is contraindicated.

Antacids (aluminium, calcium and magnesium salts) and adsorbents (e.g. kaolin) may reduce the absorption of chloroquine, so should be taken well separated from Chloroquine (at least four hours apart).

If the patient is taking ciclosporin then chloroquine may cause an increase in ciclosporin levels.

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.

Chloroquine significantly reduces levels of praziquantel. Caution is therefore advised during co-administration. Prescribers may consider increasing the dose of praziquantel if the patient does not respond to the initial dose.

Other antimalarials:
increased risk of convulsion with mefloquine.

Cardiac glycosides:
hydroxychloroquine and possibly chloroquine increase plasma concentration of digoxin.

Parasympathomimetics:
chloroquine and hydroxychloroquine have potential to increase symptoms of myasthenia gravis and thus diminish effect of neostigmine and pyridostigmine.

Ulcer healing drugs:
cimetidine inhibits metabolism of chloroquine (increased plasma concentration).

In vitro work has shown that the concomitant use of drugs such as multidrug and toxin extrusion protein (MATE1) inhibitors (e.g., ciprofloxacin, cimetidine, omeprazole, pyrimethamine) may impact the renal clearance of chloroquine, which could theoretically lead to increased levels of chloroquine and potentially overdosage. In addition, care should be taken when alkalinization of urine occurs as this may reduce chloroquine renal excretion.

Chloroquine may lower the convulsive threshold and thus antagonise the actions of antiepileptics.

Thyroid medication: increased Thyroid Stimulating Hormone levels have been observed with the concomitant use of levothyroxine, dosage adjustment of thyroid medication may be necessary.

There is a theoretical risk of inhibition of intra-cellular α-galactosidase activity when chloroquine is co-administered with agalsidase.

ADVERSE EFFECTS

Ocular disorders: Maculopathy and macular degeneration have been reported and may be irreversible. Irreversible retinopathy with retinal pigmentation changes (bull’s eye appearance) and visual field defects (paracentral scotomas) in patients receiving long-term or high-dosage 4-aminoquinoline therapy have been reported . Visual disturbances (blurring of vision and difficulty of focusing or accommodation); nyctalopia; scotomatous vision with field defects of paracentral, pericentral ring types, and typically temporal scotomas (e.g., difficulty in reading with words tending to disappear, seeing half an object, misty vision, and fog before the eyes) have been reported. Reversible corneal opacities have also been reported.

Immune system disorders: Urticaria, anaphylactic reaction including angioedema.

Ear and labyrinth disorders: Nerve type deafness; tinnitus, reduced hearing in patients with preexisting auditory damage.

Musculoskeletal and connective tissue-disorders: Sensorimotor disorders, skeletal muscle myopathy or neuromyopathy leading to progressive weakness and atrophy of proximal muscle groups, depression of tendon reflexes and abnormal nerve conduction.

Gastrointestinal disorders: Hepatitis, increased liver enzymes, anorexia, nausea, vomiting, diarrhea, abdominal cramps.

Skin and subcutaneous tissue disorders: Erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, exfoliative dermatitis. Pleomorphic skin eruptions, skin and mucosal pigmentary changes; lichen planus-like eruptions, pruritus,; drug rash with eosinophilia and systemic symptoms (DRESS syndrome); photosensitivity and hair loss and bleaching of hair pigment.

Blood and lymphatic system disorders: Pancytopenia, aplastic anemia, reversible agranulocytosis, thrombocytopenia and neutropenia. Hemolytic anemia in G6PD deficient patients.

Nervous system disorders: Convulsions, mild and transient headache, polyneuropathy, acute extrapyramidal disorders (such as dystonia, dyskinesia, tongue protrusion, torticollis).

Neuropsychiatric disorders: Neuropsychiatric changes including psychosis, delirium, anxiety, agitation, insomnia, confusion, hallucinations, personality changes, depression, and suicidal behavior.

Cardiac disorders: Hypotension, electrocardiographic changes (particularly, inversion or depression of the T-wave with widening of the QRS complex), and cardiomyopathy (which may result in cardiac
failure and in some cases a fatal outcome).
Cardiac arrhythmias, conduction disorders such as bundle branch block / atrio-ventricular block, QT interval prolongation, torsade de pointes, ventricular tachycardia and ventricular fibrillation have been reported with therapeutic doses of chloroquine as well as with overdose. The risk is greater if chloroquine is administered at high doses. Fatal cases have been reported.

Metabolic and Nutritional disorders: Hypoglycemia .

Reporting of suspected adverse reactions:

The PPB Department of Pharmacovigilance was set up with a vision to develop, implement and continuously upgrade an appropriate system for detecting, reporting, and monitoring adverse drug reactions (ADRs) and other relevant problems with medicines in Kenya. The department strives to ensure the safety and efficacy of pharmaceutical products in Kenya.
Reporting suspected adverse reactions after authorization of the medicinal product are important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals/ Patients are encouraged to report any suspected adverse reactions via Pharmacovigilance Yellow Form, pv@pharmacyboardkenya.org or clicking below button:


Chloroquine in Kenya
Chloroquine in Kenya
Chloroquine in Kenya
Chloroquine in Kenya
Chloroquine in Kenya
Chloroquine in Kenya
COVID 19

Clinical | Pharmacokinetic data


Pregnancy Category: N (Not classified yet
Routes of Administration: Intravenous | Oral
Bioavailability: Not Available
Protein Binding: 46-74%
Metabolosim: Liver
Onset of Action: N/A
Elimination Half life: 1-2 months
Excretion: Chloroquine is predominantly eliminated in the urine

Legal Status | Dosage forms & Strengths


Prescription Category:
Prescription only Medicine (POM) , ℞-only
Narcotic Drugs and Psychotropic Substances (Control ) Act Schedule:
This drug is not a controlled substance under Narcotic Drugs and Psychotropic Substances (Control ) Act
Dosage Forms | Strengths:


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References/ Citation:




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