Product Information
Registration Status: ActiveCHLOROQUINE TABLET 250mg is approved to be sold in Singapore with effective from 1988-05-26. It is marketed by BEACONS PHARMACEUTICALS PTE LTD, with the registration number of SIN01559P.
This product contains Chloroquine 250mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by BEACONS PHARMACEUTICALS PTE LTD in SINGAPORE.
It is a Pharmacy Only Medicine that can be obtained from a pharmacist at a retail pharmacy.
Description
The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.
Indication
For the suppressive treatment and for acute attacks of malaria due to P. vivax, P.malariae, P. ovale, and susceptible strains of P. falciparum, Second-line agent in treatment of Rheumatoid Arthritis
Mechanism of Action
The mechanism of plasmodicidal action of chloroquine is not completely certain. Like other quinoline derivatives, it is thought to inhibit heme polymerase activity. This results in accumulation of free heme, which is toxic to the parasites. nside red blood cells, the malarial parasite must degrade hemoglobin to acquire essential amino acids, which the parasite requires to construct its own protein and for energy metabolism. Digestion is carried out in a vacuole of the parasite cell. During this process, the parasite produces the toxic and soluble molecule heme. The heme moiety consists of a porphyrin ring called Fe(II)-protoporphyrin IX (FP). To avoid destruction by this molecule, the parasite biocrystallizes heme to form hemozoin, a non-toxic molecule. Hemozoin collects in the digestive vacuole as insoluble crystals. Chloroquine enters the red blood cell, inhabiting parasite cell, and digestive vacuole by simple diffusion. Chloroquine then becomes protonated (to CQ2+), as the digestive vacuole is known to be acidic (pH 4.7); chloroquine then cannot leave by diffusion. Chloroquine caps hemozoin molecules to prevent further biocrystallization of heme, thus leading to heme buildup. Chloroquine binds to heme (or FP) to form what is known as the FP-Chloroquine complex; this complex is highly toxic to the cell and disrupts membrane function. Action of the toxic FP-Chloroquine and FP results in cell lysis and ultimately parasite cell autodigestion. In essence, the parasite cell drowns in its own metabolic products.
Pharmacokinetics
- Absorption
- Completely absorbed from gastrointestinal tract
- Distribution
- Metabolism
- Hepatic (partially)
- Elimination
Active Ingredient/Synonyms
Chloraquine | Chlorochin | Chloroquina | Chloroquine | Chloroquinium | Chloroquinum | Cloroquina | N4-(7-chloro-4-quinolinyl)-N1,N1-diethyl-1,4-pentanediamine | Chloroquine |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.