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Drug Information
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.
Oral
MALARIA. ACUTE ATTACK: Initially 600mg base followed by 300mg base after 6-8 hours on day 1. On days 2 and 3, single doses of 300mg base/day. Children: Initially 1mg base/kg (max 600mg base) followed by 5mg base/kg (max 300mg base) after 6 hours. Single doses of 5mg base/kg on days 2 and 3 MALARIA PROPHYLAXIS: Adults: 300mg base weekly. CHildren: 5mg base/kg weekly. Continue for 8 weeks after leaving endemic area.
IV
FALCIPARUM MALARIA IN SERIOUSLY ILL PATIENTS: 3.5mg base/kg 6 hourly, max 25mg base/kg. Change to oral therapy when patient takes oral medication
IM
FALCIPARUM MALARIA IN SERIOUSLY ILL PATIENTS: 3.5mg base/kg 6 hourly, max 25mg base/kg. Change to oral therapy when patient takes oral medicatons.
Action
Used for malarial prophylaxis (as a suppressive) and in managing acute
attacks of malaria. Highly active against erythrocytic forms of P. vivax,
P.malariae and P.falciparum. Also effective in extra intestinal
amoebiasis. In Rh Arthritis chloroquin and more effectively
hydroxy chloreoquin have a disease-modifying effect.
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.
Adverse
Effect & Precaution
Nausea, epigastric distress,
vomiting, itching and headache. Chronic therapy may cause loss of vision
due to retinal damage. COrneal opacities may occur but are reversible.
Skin rash, photoallergy, myopathy, loss o hearing and graying of hair.
Parenteral administration may lead to hypotension and cardiac depression
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.
Pregnancy: Use with caution.
Breast Feeding: Safety not established.