Chloroquine ([7-chloro-4- (4-diethylamino-1-methylbutylamino) quinoline, CHQ] is a derivative of 4-aminoquinoline, synthesized for the first time in Germany. the US Food and Drug Administration (FDA) to treat malaria and parenteral amoebiasis (amoebiasis).
Action of chloroquine
Chloroquine is categorized as:
- drugs with anti-malarial (anti-cold) properties,
- anti-rheumatic drugs,
- antiviral drugs
- anti-inflammatory drugs.
The process of antimalarial action is to inhibit the development of all types of malaria caused by susceptible strainsPlasmodium falciparum ,P. ovale ,P. vivaxiP. malariae . The mechanism of the antiviral effect of chloroquine is related to its physicochemical properties and pharmacokinetic parameters.
The drug contributes to the inhibition of the intracellular pH-dependent stages of fusion of certain virus particles, including retroviruses and coronaviruses, with the host cell membrane. It inhibits the glycosylation of cellular SARS-CoV receptors.
It also affects the immune system by inhibiting the proliferation of lymphocytes or by preventing the formation and release of selected elements of the inflammatory response, including tumor necrosis factor alpha (TNF-alpha), interleukin 1 (IL-1, interleukin 1 ), interleukin 6 (IL-6, interleukin 6).
In addition, it can directly affect phospholipase A2, the presentation of antigens to cells of the immune system, the secretion of certain enzymes from cell lysosomes, and the release of toxic reactive oxygen species from macrophage cells.
Chloroquine has the ability to inhibit virion formation in structures similar to the endoplasmic reticulum, the Golgi compartment (ERGIC). Chloroquine reduces the exacerbation of pneumonia. The anti-inflammatory action of chloroquine is based on the inhibition of the release of pro-inflammatory cytokines into the human body and the production of antibodies.
Use of chloroquine
Chloroquine has been used in the treatment of severe ailments related to pneumoniacaused by a beta coronavirus strain such as SARS-CoV. The drug is used as an antimalarial agent to prevent acute attacks of malaria.
Chloroquine is used to treat dysentery amoebiasis and liver abscesses caused byEntamoeba histolytica , usually together with intestinal anti-amoebiasis medications. It also has anti-inflammatory effects in the treatment of rheumatoid arthritis or in the treatment of discoidal lupus erythematosus.
Indications for the use of chloroquine
Chloroquine is recommended in the treatment of malaria and as a preventive measure for people planning a trip to the endemic zone. Chloroquine is also used in the treatment of rheumatic diseases, in anti-inflammatory treatment, in dermatology, in collagenosis and in diseases related to photosensitivity. The indication for the use of the drug is also viral infection (SARS-CoV, MERS-CoV, SARS-CoV-2, HIV).
Dosage of chloroquine
The drug should be used as described in the patient information leaflet or according to specific guidelines and recommendations of a doctor or pharmacist. Check with your doctor or pharmacist if you are unsure. Chloroquine is administered orally or parenterally. The dose depends largely on the disease, age, weight, and co-morbid conditions such as renal or hepatic failure.
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Contraindications to the use of chloroquine
Contraindications to the use of chloroquine are hearing or vision defects (in the retina or in the field of vision) caused by 4-aminoquinoline derivatives. The contraindications also include:
- end stage renal failure,
- epilepsy,
- changes in the blood picture or the skin (psoriasis, urticaria).
Chlorohemine is not given to people allergic to this ingredient and to children and adolescents under 14 years of age.
Precautions when using chloroquine
Chloroquine should not be administered in severe stomach and intestinal disorders, retinal disorders, abnormalities in the blood picture, as well as in people with glucose-6-phosphate dehydrogenase deficiency. Chloroquine should be used with caution in patients with renal or hepatic insufficiency.
The drug may aggravate the course of porphyria, psoriasis, myasthenia gravis and epilepsy by intensifying convulsions. Long-term use of the drug (lasting more than 3 months) should be monitored by a doctor through regular examinations:
- ophthalmic due to the risk of irreversible occurrenceretinopathy,
- blood, as there is a risk of bone marrow suppression,
- neurological due to neurotoxic effects (polyneuritis, dystonia, dyskinesia).
Exposure to UV radiation should be avoided during treatment.
Chloroquine side effects
Treatment with chloroquine may lead to life-threatening severe hypoglycaemia. Symptoms of hypoglycaemia include, but are not limited to, hand tremors, excessive sweating, palpitations, impaired concentration, anxiety, sleepiness, nausea and vomiting.
If a patient develops symptoms of hypoglycaemia during therapy, treatment should be changed. A very serious side effect of chloroquine is macular retinopathy, the effect of which depends on the cumulative dose, not a single administration.
Side effects also include allergic reactions and a lack of appetite or a drop in blood pressure.
Interactions of chloroquine with other drugs and diseases
Before using the active substance, inform your doctor about taking other medications. Concomitant use of chloroquine with antidiabetic, anti-malaria or anti-epileptic drugs may worsen the symptoms of these diseases, reduce their effects or cause seizures.
Chloroquine should not be administered together with penicillamine, because it will increase the concentration of this drug in the blood, risk of severe side effects affecting the hematopoietic system and kidneys, and the development of skin allergic reactions. The combined use of chloroquine with amiodarone is contraindicated as it increases the disturbance of the heart rhythm and causes damage to peripheral nerves and the appearance of related ailments (tingling, pain and numbness in the limbs).
Chloroquine may also increase blood levels of cyclosporine.
Chloroquine use and pregnancy and breastfeeding
Before taking the drug, inform your doctor if you are pregnant or breastfeeding. It should not be used during pregnancy unless the doctor considers that the benefits of treating the mother outweigh the risks to the fetus. Breastfeeding is contraindicated during long-term administration of high doses of chloroquine.
Chloroquine storage
The drug should be stored in a suitable place that is invisible and inaccessible to children. Store in a dry place, away from direct sunlight at a temperature below 25 ° C, in the original packaging. The drug should not be used after the expiry date stated on the package. The expiry date means the last oneday of the month.