APR LERRYQUIN 30 ml

M-01:

INFORMATION FOR THE USER

Chloroquine Injection

Read all of this information carefully before you start taking this medicine because it contains important information for you.
• Keep this information. You may need to read it again.
• If you have any further questions, ask your doctor, pharmacist or nurse.
• This medicine is prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours.
If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side effects not listed in this information.

1. COMPOSITION:
Eachvial contains:
Chloroquine phosphate eq. to chloroquine – 40mg

For IV use only.

2. DESCRIPTION:
Chloroquine is an anti-malarial and is used for the treatment of malaria.

3. PHARMACOLOGICAL ACTION:
The mode of action of chloroquine on plasmodia has not been fully elucidated. It binds to & alters the properties of DNA. It also binds to ferriprotoporphyrin IX & this leads to lysis of the plasmodial membrane. In suppressive treatment, it 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.
4. CLINICAL PHARMACOKINETICS:
Absorbed readily & almost completely. 55% bound to plasma proteins. Concentrated in erythrocytes, liver, spleen, kidneys, heart & brain & is strongly bound in melanin-containing cells. About 30% of dose is metabolized by the liver to monodesethyl-chloroquine &bidesethylchloroquine. About 70% of dose is excreted unchanged in urine; unabsorbed drug is excreted in feces. Small amounts of the drug may be present in urine for months after the drug is discontinued. Renal excretion is enhanced by urinary acidification.

5. INDICATIONS:
Chloroquine injection is indicated for the treatment of:
– Treatment of malaria
– Prophylaxis and suppression of malaria
– Treatment of amoebic hepatitis and abscess

6. CONTRAINDICATIONS:
– Known hypersensitivity to chloroquine or any other ingredients of the formulation
– Concomitant use with amiodarone

7. WARNINGS AND PRECAUTIONS:
When used as malaria prophylaxis official guidelines & local information on prevalence of resistance to anti-malarial drugs should be taken into consideration.
Has been shown to cause severe hypoglycaemia including loss of consciousness that could be life threatening in patients treated with & without antidiabetic medications. Patients treated with chloroquine should be warned about the risk of hypoglycaemia & the associated clinical signs and symptoms.
Prolongation of QTc interval: Has been shown to prolong the QTc interval in some patients.
Should be used with caution in patients with congenital/documented acquired QT prolongation and/or known risk factors for prolongation of the QT interval such as:
– cardiac disease e.g. heart failure, myocardial infarction,
– proarrhythmic conditions e.g bradycardia (< 50 bpm)
– a history of ventricular dysrhythmias
– uncorrected hypokalemia and/or hypomagnesemia
– during concomitant administration with QT interval prolonging agents
as this may lead to an increased risk for ventricular arrhythmias, sometimes with fatal outcome.
The magnitude of QT prolongation may increase with increasing concentrations of the drug. Therefore, the recommended dose should not be exceeded.
If signs of cardiac arrhythmia occur during treatment, treatment should be stopped & an ECG should be performed.
Cardiomyopathy: Cases of cardiomyopathy have been reported, leading to heart failure, sometimes with fatal outcome. If signs & symptoms of cardiomyopathy occur during treatment with chloroquine, treatment should be stopped.
Caution is necessary when giving to patients with impaired hepatic function, particularly when associated with cirrhosis.
Caution is also necessary in patients with porphyria. It may precipitate severe constitutional symptoms & an increase in the amount of porphyrins excreted in the urine. This reaction is especially apparent in patients with high alcohol intake.
Small number of cases of diffuse parenchymal lung disease have been identified. A response after therapy with steroids has been observed in some of these cases.
Cases of drug rash with eosinophilia & systemic symptoms syndrome have been identified alone or in combination with proguanil. Recovery after discontinuation of treatment and response after therapy with steroids has been observed.
Caution is necessary when giving to patients with renal disease.
Should be used with care in patients with a history of epilepsy. Potential risks & benefits should be carefully evaluated before use in subjects on anticonvulsant therapy or with a history of epilepsy as rare cases of convulsions have been reported.
Considerable caution is needed in the use for long-term high dosage therapy & such use should only be considered when no other drug is available. Patients on long-term therapy should also be monitored for cardiomyopathy.
Irreversible retinal damage & corneal changes may develop during long term therapy & after the drug has been discontinued. Ophthalmic examination prior to & at 3–6 monthly intervals during use is required if patients are receiving chloroquine
• at continuous high doses for longer than 12 months
• as weekly treatment for longer than 3 years
• when total consumption exceeds 1.6 g/kg (cumulative dose 100 g)
Full blood counts should be carried out regularly during extended treatment as bone marrow suppression may occur rarely.
Use in patients with psoriasis may precipitate a severe attack.
Caution is advised in patients with glucose-6-phosphate dehydrogenase deficiency, as there may be a risk of haemolysis.
Acute extrapyramidal disorders have been reported usually disappearing on discontinuation of treatment and /or on symptomatic treatment.
8. ADVERSE EFFECTS:
Side effects include: Changes in liver function, Cardiomyopathy, Hallucinations, GI disturbances, Pruritis, Visual disturbances, Hypotension, ECG changes, AV block, Headache

DRUG INTERACTIONS:
Should be used with caution in patients receiving drugs known to prolong the QT interval e.g. Class IA & III antiarrhythmics, tricyclic antidepressants, antipsychotics, some anti-infectives due to increased risk of ventricular arrhythmia. Halofantrine should not be administered with chloroquine. Amiodarone should not be used and its use is contraindicated. Antacids (aluminium, calcium & magnesium salts) & adsorbents (e.g. kaolin) may reduce the absorption of chloroquine, so should be taken well separated (at least 4 hrs apart).
If the patient is taking ciclosporin then chloroquine may cause an increase in ciclosporin levels.
Significantly reduces levels of praziquantel. Caution is therefore advised during co-administration.
Other antimalarials: Increased risk of convulsion with mefloquine.
Cardiac glycosides: Increase plasma conc. of digoxin.
Parasympathomimetics: Have potential to increase symptoms of myasthenia gravis & thus diminish effect of neostigmine &pyridostigmine.
Ulcer healing drugs: Cimetidine inhibits metabolism of chloroquine (increased plasma conc).

Concomitant use of drugs such as multidrug & toxin extrusion protein (MATE1) inhibitors (e.g., ciprofloxacin, cimetidine, omeprazole, pyrimethamine) may impact the renal clearance, which could theoretically lead to increased levels of chloroquine & potentially overdosage.
May lower the convulsive threshold & 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.
Risk of inhibition of intra-cellular α-galactosidase activity when chloroquine is co-administered with agalsidase.
9. DOSAGE:The recommended dose is500-1,000mg initially & then 500mg every 6-8 hours or as prescribed by the physician.

10. ADMINISTRATION:
For IV only.
Administration to be done by a registered medical practitioner/nurse in a proper sterile & hospital setting only.
11. STORAGE:
Do not store above 25°C. Store in the original package. Keep away from children. Do not expose to direct sunlight.

12. MANUFACTURED BY:

13. MARKETED BY:

Last revised on August 2020.