It is completely absorbed from the GIT, and reaches an effective plasma level in 2-3hrs time.health and fitness Updated: Mar 03, 2004 17:06 IST
Chloroquine is completely absorbed from the GIT, and reaches an effective plasma level in 2-3hrs time. It is metabolised by Hepatic Microsomal enzymes and is excreted via urine. Acidification increases renal excretion of chloroquine.It is concentrated in the liver,spleen,kidney,lungs,skin,leukocytes and other tissues.Its selective accumulation in retina is responsible for ocular toxicity on prolonged use.Absorbtion after I.M & S.C injections is also good.
Chloroquine belongs to the 4-aminoquinolines, and is prepared as diphosphate salt. It is used against asexual erythrocytic forms of P.vivax, P.falciparum and against gametocytes of P.vivax, P.ovale and P.malariae.It is also used an extraintestinal amoebicidal agent and as disease modifying agent in rheumatoid arthritis.
Routes of Administration and Dosage
For oral dosage- For treatment of malaria in Adults: 600 mgs stat followed by 300 mgs after 8 hours.Then 300 mgs daily for next two days. Children: Initially 10 mgs base per kilogram[ maximum 600 mgs base] followed by 5 mgs base per kilogram [ maximum 300 mgs base] after 6 hours.Single doses of 5 mgs base per kilogram on second and third day. For injection dosage form-I.M:
For treatment of falciparum malaria in seriously ill patients 3.5 mgs base per kilogram 6 hourly[ maximum 25 mgs base per kilogram].For suppressive prophylaxis -300mgs(base) weekly for adults ;50 mg for infants ; 100 mgs for children 1 to 5 yrs ; 200 mgs for children 5 to 10 yrs.
For treatment of extra intestinal amoebiasis --- For amoebic liver abcess 600 mg ( base) for two days followed by 300 mgs daily for 2 to 3 weeks.It is now employed only when metronidazole is not effective or not tolerated. For treatment of Rheumatiod arthritis ; hydroxy chloroquine 400 mgs /day initially followed by 200 to 400 mgs for maintanance.
Chloroquine is contraindicated in hypersensitivity, Chloroquine resistant falciparum infection, G6PD deficiency, renal and hepatic impairment, epilepsy and in psoriasis.
Chloroquine doses used in malaria produce side effects like nausea, vomiting, itching, difficulty in accommodation and headache. Chloroquine may cause blood disorders like pancytopenia and agranulocytosis. Chloroquine may affect the eyes causing retinopathy, diplopia and blurring of vision.
Chloroquine may cause serious blood disorders in patients with Glucose-6-phosphate dehydrogenase (G6PD) deficiency. Liver disease may decrease the metabolism of Chloroquine. Chloroquine may cause muscle weakness and, in high doses, seizures .It may cause episodes of porphyria to occur more frequently. Chloroquine may bring on severe attacks of psoriasis.Parenteral administration can cause hypotention,cardiac depression and arrhythmias.Chloroquine can be used in malaria in pregnancy safely.
Antacid can reduce the systemic level of chloroquine .Steven-Johnson syndrome can occur when it is given along with pyrimethamine/sulphadoxine combination.Chloroquine antagonises the action of neostigmine and pyridostigmine.Cimitidine raises Chloroquine level in the blood by inhibiting its metabolism.
Alpiquin(Alpine), Amloquin(Brown & Burk), Bitaquin DS TABS(Bombay Tablets), Bitaquin INJ(Bombay Tablets), Cadiquin(Cadila Healthcare), Chloromet(BDH), Cloquin(Indoco), Emquin (Merck), Idiquin (IDPL), La-Quin(Stadmed), Lariago (IPCA), Larover(Aglomed), Malaclor- EC(Unicure), Malaquin (PCI), Melubrin (Ranbaxy), Nivaquine-P(Rhone-Poulenc), Quinross(Tata Pharma), Resochin(Bayer), Rimoquin(Anglo French).
First Published: Mar 03, 2004 17:06 IST