Hydroxychloroquine, sold under the brand name Plaquenil among others, is a medication used to prevent and treat malaria in areas where malaria remains sensitive to chloroquine.
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Brand names of hydroxychloroquine include:
Plaquenil, Hydroquin, Axemal (in India), Dolquine, Quensyl, Quinoric.
What is Hydroxychloroquine (Plaquenil) ?
Antimalarial agent. Causes the death of red blood cell forms of all types of plasmodium. Also, hydroxychloroquine has a therapeutic effect in some diffuse connective tissue diseases. The mechanism of action is not fully understood. It is believed that the effectiveness of hydroxychloroquine is associated with its ability to change the activity of several enzymes (including phospholipase, NADP-cytochrome C reductase, cholinesterase, protease, hydrolase), to stabilize the membranes of lysosomes, to inhibit the formation of prostaglandins, to inhibit chemotaxis and phagocytosis, to influence the production of interleukin-1. It has immunosuppressive and some anti-inflammatory activity.
Composition and form of release Hydroxychloroquine 200mg 30 pcs. film-coated tablets. Tablets - 1 tab.:
- Active substance: hydroxychloroquine sulfate 200 mg.
- Excipients: calcium hydrophosphate dihydrate-99.86 mg, prosolv (microcrystalline cellulose 98%, silicon dioxide colloidal 2%) - 126.79 mg, hypromellose-24.25 mg, croscarmellose sodium-19.4 mg, silicon dioxide colloidal-4.85 mg, magnesium stearate-4.85 mg.
- The composition of the film shell: hypromellose (hydroxypropylmethylcellulose) - 2.972 mg, titanium dioxide (E171) - 1.363 mg, macrogol (polyethylene glycol) (E1521) - 0.665 mg. 10 pcs. - cell contour packages (3) - cardboard packs.
Description of the dosage form
Plaquenil tablets covered with a white film shell, round, biconvex; slight surface roughness is allowed; the color of the tablets on the break is white or white with a yellowish tinge.
With caution, it is used for violations of liver and kidney function, gastrointestinal diseases, neurological disorders, hematopoietic disorders, psoriasis, glucose-6-phosphate dehydrogenase deficiency, hypersensitivity to quinine.
Before starting therapy, as well as in the process of system administration, it is necessary to conduct an ophthalmological examination at least once every 6 months.
Caution is necessary when using concomitantly with drugs, the side effect of which is associated with the effect on the organ of vision and skin.
Side effects Hydroxychloroquine 200mg 30 pcs. film-coated tablets.
- From the digestive system: nausea, vomiting, diarrhea, anorexia, abdominal pain.
- From the central nervous system and peripheral system: headache, weakness, nervousness, neuromuscular blockade, toxic psychosis, decreased visual acuity, a feeling of flashing in the eyes, photophobia.
- From the hematopoietic system: anemia, agranulocytosis, thrombocytopenia, neutropenia.
- Dermatological reactions: dermatitis, depigmentation of the skin and mucous membranes, hair loss.
- Other: deposition of pigment in the cornea.
Overdose of 4-aminoquinolines is especially dangerous in children, even 1-2 g of the drug can lead to death.
Symptoms of overdose include headache, visual disturbances, collapse, convulsions, hypokalemia, rhythm, and conduction disturbances, followed by cardiac and respiratory arrest.
Since overdose symptoms can develop very quickly after taking a large dose of the drug, in these cases, appropriate measures should be taken immediately. Artificial vomiting or gastric lavage through a probe should be performed immediately. Activated charcoal can slow down the absorption at a dose at least 5 times higher than the accepted dose of the drug. Parenteral administration of diazepam is advisable, which will reduce the cardiotoxicity of chloroquine. If necessary, artificial ventilation and anti-shock therapy should be performed.
After the symptoms of overdose are relieved, it is necessary to continue constant medical supervision for at least 6 hours.
Hydroxychloroquine in the treatment of patients with COVID-19
Chloroquine and hydroxychloroquine are antimalarial drugs approved for the treatment of COVID-19. Taking these drugs can be accompanied by rare, but quite serious side effects, such as hypoglycemia. Besides, their toxic effect on the heart and retina is known.
To assess the toxicity of chloroquine and hydroxychloroquine to different organs, Chinese scientists studied the proliferation of cells of different types in culture for 72 hours when exposed to the drugs. They used eight cell lines: five human (pulmonary fibroblasts, pulmonary carcinoma, retinal cells, hepatocellular carcinoma, embryonic kidney cells), two rats (cardiomyocytes and intestinal epithelium), and a Vero cell line of green monkey renal epithelium. The toxicity of the compounds was quantified using two parameters: the cytotoxic concentration CC50, at which 50% of the cells die, and the RTTCC parameter, which predicted the toxicity of the drugs to the corresponding tissues. In other words, the authors constructed a physiological pharmacokinetic model describing the toxicity of chloroquine and generic Plaquenil for various tissue types.
For both chloroquine and Plaquenil, the CC50 values decreased over time, indicating cumulative cytotoxicity of both drugs. Chloroquine was found to be most toxic to hepatocellular carcinoma cells and intestinal epithelium, while hydroxychloroquine was most toxic to intestinal epithelial and lung cells. In general, hydroxychloroquine was shown to be less toxic than chloroquine for all the cells studied, except cardiomyocytes.
According to the authors, the toxicity of hydroxychloroquine to the tissues of the lungs, kidneys, heart, and liver should be significantly (6-87 times) lower than that of chloroquine. The authors conclude that both drugs exhibit cytotoxicity, but in general, Plaquenil is less toxic for most cell types.
Reviews of Hydroxychloroquine
There are quite a lot of reviews about the drug on the Internet. They are left by patients with rheumatic diseases and people who have suffered from malaria.
Most consumers note the high effectiveness of the drug. It helps to cope with infection and manifestations of rheumatic pathology. However, some patients are dissatisfied with the long-term development of the effect and the appearance of various adverse reactions. Moreover, undesirable manifestations may occur after taking the first pill, but the therapeutic effect is at least a few days later.
- COVID-19: Could Hydroxychloroquine Really Be The Answer? - Medscape - March 18, 2020. https://www.medscape.com/
- Xuet Yao et al. In Vitro antiviral activity and projection of an Optimized Hydroxychloroquine dosing Design for the treatment of severe acute respiratory syndrome Coronavirus 2 (SARS-CoV-2), Clinical infectious Diseases,, ciaa237, https://doi.org/10.1093/cid/ciaa237 https://academic.oup.com/