| 
 Chloroquine
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
hydroxyl chloroquin have disease-modifying effect.
Indications & Dosage:
Oral - Malarial – Acute Attack
initially 600mg base followed by 300 mg base after 6-8 hours on
day 1. On days 2 and 3, single doses of 300mg base/day.
Children – Initially 10 mg base/kg(max 600mg base) followed
by 5mg base/kg(max 300mg base) after 6 hours. Ingle doses of 5mg
base/kg on days 2 & 3.
Adults – 300 mg base weekly continue for 8 weeks after leaving
endemic area.
IV – Falciparum Malaria in seriously ill Patients: 10mg base/kg
infused over 8 hours followed by 15 mg base/kg over 24 hours.
IM - Falciparum Malaria in seriously ill Patients: 3.5mg base/kg
6 hourly, max 25mg base/kg. Change to oral therapy ehrn patient
takes oral medication.
Composition:
Each Capsule Contains:
Chloroquine Phosphate B.P. 500mg
Safety Alert:
CL: Hypersens,
known or suspected resistant P.falciparum infection, prophyria,
retinal damage, concurrent hepatotoxic drugs.
SP: Psoriasis, diseases of haematopoietic or CNS
systems, hepatic or renal impairment, G-6PD deficiency, pregnancy,
epilepsy, children, lactation.
INT POT-HAZ: Antacids reduce systemic availability
of chloroquine hence administration should be separated by 4 hours.
Especially relevant for chemoprophylaxis. Rarely Steven-Johnson
syndrome, when administered with pyrimethamine/sulphadoxin. Increased
toxicity with quinacrine.
Others: Concomitant therapy with phenylbutazone predisposes to dermatitis,
antagonizes effect of neostigmine , and reduces bioavailability
of ampicillin. Cimetidine inhibits metabolism of chloroquine raising
plasma levels.
ADR POT-LT: Especially in children. Depressant
effect on CVS leading to hyptension, heart block & arrest.Fatal
poisonin can occur in adults with a dosage os3-6g taken at once.
Sulphadoxine
+ Pyrimethamine
The two drugs cause a sequential
blockade of 2 enzymes involved in the biosynthesis of folinic acid
by the paracytes. Both have prolonged half-lives enabling single
dose administration.
Indications &
Dosage:
Oral – Treatment of Chloroquin
resistant Falciparum malaria acute attack: Pyrimethamine 25mg +
Suplhadoxine 500mg (Tablet).
Adults – 3 tabs single dose.
Children – 9-14 years : 2 tabs single dose
4-8 years : 1 tab single dose
Under 4 years : ½ tab single dose.
Composition:
Each Tablet Contains:
Sulfadoxine U.S.P. 500mg
Pyrimethamine U.S.P. 25mg
Safety Alert:
CL: Severe renal impairment, severe
liver parenchymal damage, blood dyscrasias, hypersensitivity to
components, megaloblastic anaemia due to folate deficiency, pregnancy
at term and during lactation, infants less than 2 months old.
SP: Impaired renal or hepatic function, folate
deficiency, severe allegy or bronchial astma, G6PD deficiency, pregnancy.
INT POT-HAZ: increased effects of warfarin and
thiopentone. Pulmonary eosinophilia and agranulocytosis in combination
with daspone. Others – Increased toxicity of quinine, methotrexate.
ADR POT-LT: Severe cutaneous eruptions, disseminated
intravascular coagulation, blood dyscrasias, anaphylactoid reactions.
Others – Nausea, Vomiting, abdominal pain, vertigo, liver
damage, headache & convulsions.
|
|
