Hydroxychloroquine (Plaquenil) is an antimalarial drug derived from 4-aminoquinoline. It also has a moderate immunosuppressive , specific and non - specific anti - inflammatory effect in autoimmune diseases .
| Hydroxychloroquine | |
|---|---|
| Chemical compound | |
| IUPAC | ( RS ) -2 - [{4 - [(7-chloroquinolin-4-yl) amino] pentyl} (ethyl) amino] ethanol |
| Gross formula | C 18 H 26 ClN 3 O |
| Molar mass | 335.872 g / mol |
| Cas | |
| PubChem | |
| Drugbank | |
| ATX | |
| Pharmacokinetics | |
| Bioavailable | 74% |
| Metabolism | liver |
| The half-life. | 32-50 days |
| Excretion | kidneys , bile , feces |
| Other names | |
| Plaquenil, Immard | |
Hydroxychloroquine is included in the list of vital and essential drugs .
Content
- 1 Pharmacological action
- 2 Pharmacokinetics
- 3 Indications
- 4 Contraindications
- 5 Side effects
- 6 dosage
- 7 Drug Interactions
- 8 Special instructions
- 9 References
Pharmacological action
It causes the death of erythrocyte forms of all types of plasmodia. In addition, 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 alter the activity of a number of enzymes (phospholipase, NADP-cytochrome C reductase, cholinesterase, protease, hydrolase), stabilize lysosome membranes, inhibit the formation of prostaglandins, inhibit chemotaxis and phagocytosis, and affect the production of interleukin-1 . It has immunosuppressive and some anti-inflammatory activity.
Pharmacokinetics
After ingestion, hydroxychloroquine is rapidly and almost completely absorbed from the digestive tract. After i / m or s / c administration, it is also rapidly absorbed from the injection site. It is distributed in the tissues of the body. It accumulates in high concentrations in the kidneys, liver, lungs, spleen, as well as in melanin-containing cells of the eyes and skin. It is metabolized in the liver with the formation of active and inactive metabolites. It is very slowly excreted in the urine from the body.
Indications
Rheumatoid arthritis, juvenile chronic arthritis, discoid and systemic lupus erythematosus, skin diseases caused or exacerbated by sunlight, malaria.
Contraindications
Retinopathy, keratopathy, visual impairment, hypersensitivity to hydroxychloroquine.
- Pregnancy and lactation
The use of hydroxychloroquine during pregnancy is possible only when the intended benefits to the mother outweigh the potential risk to the fetus. If necessary, use during lactation should decide on the termination of breastfeeding. Hydroxychloroquine crosses the placental barrier, excreted in breast milk.
Side effect
From the digestive system: nausea, vomiting, diarrhea, anorexia, abdominal pain. From the side of the central nervous system and peripheral system: headache, weakness, nervousness, neuromuscular blockade, toxic psychosis, decreased visual acuity, flickering in the eyes, photophobia. From the hemopoietic system: anemia, agranulocytosis, thrombocytopenia, neutropenia. Dermatological reactions: dermatitis, depigmentation of the skin and mucous membranes, hair loss. Other: deposition of pigment in the cornea.
Dosage
When taken orally by adults, the course is 2 g according to the following scheme: on the 1st day, for the first intake, 800 mg, then after 6-8 hours - 400 mg; on the 2nd and 3rd days - 400 mg in one dose. Depending on the etiology of the disease, it is possible to use a daily dose of 400-600 mg in several doses, in the future the doses can be reduced. For children, the daily dose is 6.5 mg / kg.
Drug Interactions
With simultaneous use with digoxin, an increase in the concentration of digoxin in the blood plasma is noted. Aminoglycoside antibiotics potentiate the blocking effect of hydroxychloroquine on neuromuscular transmission.
Special instructions
It is used with caution in cases of impaired liver and kidney function, gastrointestinal diseases, neurological disorders, in cases of hematopoiesis, psoriasis, glucose-6-phosphate dehydrogenase deficiency, and hypersensitivity to quinine. Before starting therapy, as well as in the process of systematic administration, it is necessary to conduct an ophthalmological examination at least 1 time in 6 months. Caution is necessary when used simultaneously with drugs whose side effect is associated with an effect on the organ of vision and skin. Hydroxychloroquine in the form of tablets is included in the List of Vital and Essential Drugs.
Links
- Hydroxychloroquine . Encyclopedia of medicines and pharmaceutical products . Radar Patent. - Instruction, application and formula.