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Antimalarial


QST

Composition

TABLETS
QST EC 100
Each enteric coated tablet contains :
Quinine Sulphate I.P. 100 mg

QST EC 300
Each enteric coated tablet contains :
Quinine Sulphate I.P. 300 mg

QST EC 600
Each enteric coated tablet contains :
Quinine Sulphate I.P. 600 mg

QST SUSPENSION
Each 5ml contains Quinine
Sulphate I.P. 150 mg. Orange flavoured

QST INJECTION
1ml and 2ml ampoules
Each ml contains
Quinine dihydrochloride I.P.300 mg

Description
Quinine is the chief alkaloid of cinchona, the bark of the
cinchona tree. This is the first ever chemotherapeutic agent to
be identified and used against the malarial parasite.
It has been in use from almost 1633 and still is one of the most effective drugs for the treatment of malaria.

When swallowed, quinine is absorbed readily from the upper small intestine. In plasma it is bound to the plasma protein and in severe malaria when given in therapeutic doses increased protein binding prevents any possible quinine toxicity.

Quinine acts primarily as a blood schizontocide with activity against Plasmodium falciparum, P.vivax, P.ovale and P.malariae

Indications
Treatment of malaria In areas where Chloroquine resistance is wide spread When paracitemia is greater than 2% When no clinical improvement occurs in 24 hours or earlier following treatment with other antimalarials In sever infection broken through Chloroquine prophylaxis

Dosage and Administration
Uncomplicated falciparum malaria 10mg per kg body weight ( orally ) 8 hourly for 7 to 10 days

In Cerebral Malaria
Quinine dihydrochloride 20 mg salt/kg of body weight (loading dose) by infusion over 4 hours, in 5% dextrose saline (5-10 ml/kg of body weight depending on the patient’s overall fluid balance).

Quinine dihydrochloride 20 mg salt/kg of body weight (loading dose) by infusion over 4 hours, in 5% dextrose saline (5-10 ml/kg of body weight depending on the patient’s overall fluid balance).

1. In patients requiring more than 48 hours of parenteral therapy, reduce the quinine maintenance dose by one-third to one-half (i.e. 5-7 mg salt/kg of body weight every 8 hours). 2. Total daily doses of intravenous quinine are as follows : day 0 (first day of treatment): 30-40 mg/kg of body weight. day 1 : 30 mg/kg of body weight. day 2 and subsequent days : 15 mg/kg of body weight. It is unusual to have to continue intravenous infusions of quinine for more than 4-5 days. If it is more convenient, Quinine may be given by continuous infusion. (Infusion rates should not exceed 5 mg pre kg of body weight per hour). 3. A loading dose should not be used if the patient received quinine within the preceding 7 days. 4. If for some reason quinine cannot be administered by infusion, quinine dihydrochloride can be given in the same dosage by intramuscular injection in the anterior thigh. The dose of quinine should be divided between two sites – half the dose in each anterior thigh. If possible, for intramuscular use, quinine should be diluted in normal saline to a concentration of 60 mg/ml.

In unconscious patients, the blood glucose value should be measured every 4 to 6 h; if the blood glucose value falls below 2.2 mmol/L (40 mg/dl), the patient should receive intravenous dextrose (0.3 g/kg). All patients given intravenous quinine should receive a continuous infusion of 5% to 10% dextrose. The parasite count and haematocrit should be measured every 12 h. If the haematocrit falls below 15 to 20 percent, then whole blood (preferably fresh) or packed cells should be transfused slowly, with careful attention to circulatory status; judicious use of diuretics may be required to prevent fluid overload. Renal function should be assessed daily. Management of fluid balance is difficult in severe malaria because there is a thin dividing line between over hydration, which can contribute to renal impairment. If necessary, pulmonary arterial wedge pressure should be measured and maintained in the low to normal range. As soon as the patient can take fluids, oral anti-malarial should be substituted.

Contraindication
Hypersensitivity to quinine, Glucose-6-phosphate dehydrogenase (G-6-PD) deficiency, optic neuritis, tinnitus

Drug Interactions
Aluminium containing antacids may delay or decrease absorption of concurrent quinine.

Oral anticoagulants
quinine may depress the hepatic enzyme system that synthesizes the vitamin K dependent clotting factors and thus may enhance the action of warfarin and other oral anticoagulants.

Cimetidine: May reduce quinine’s oral clearance and increase its elimination half-life.

Rifampicin : The concurrent use of quinine and enzyme-inducers such as Rifampicin may lead to increased metabolism of quinine and thereby hamper the achievement of effective levels.

Digoxin : Serum concentrations may be increased by concurrent quinine.

Mefloquine : Should not be used concurrently with quinine. If the two drugs have to be used in the initial treatment of sever malaria, mefloquine administration should be delayed by at least 12 hours after the last dose of quinine. Co-administration increases risk of ECG abnormalities, cardiac arrest and convulsions.

Neuromuscular blocking agents : the neuromuscular blockade may be potentiated by quinine and may result in respiratory difficulties. Urinary alkalinizers eg. Acetazolamide and sodium bicarbonate administered concurrently with quinine may increase quinine blood levels with potential for toxicity.

Warnings / precautions
Pregnancy Quinine medication in pregnant women is likely to provoke marked hypoglycaemia. This calls for regular monitoring of blood glucose levels.
Nursing mothers: Quinine is secreted in breast milk in small amounts. Although no adverse effects have been reported in the nursing infants, patients at risk for G-6-PD deficiency should be ruled out for before breast-feeding.

Elderly : The potential special risks of quinine in the elderly stem from its interaction with cardiovascular drugs.

Others Cinchonism : Repeated doses or over dosage of quinine may precipitate cinchonism. The mildest symptoms include tinnitus, headache, nausea and slightly disturbed vision, which usually subside rapidly upon discontinuation of the drug. When quinine is continued or after large single doses, symptoms also involve the GI tract, the nervous and cardiovascular systems and the skin.

Haemolysis has been associated with a G-6-PD deficiency in patients taking quinine and therapy should be stopped immediately if haemolysis appears. Cardiac disease. The drug should be used with caution in cardiac arrhythmias, quinine has quinidine-like activity.

Side Effects Cinchonism may occur at therapeutic doses.

Haematologic : acute haemolysis, haemolytic anaemia.

Opthalmic : Visual disturbances.

CNS : Tinnitus, vertigo, headache, fever, apprehension, restlessness, confusion, syncope, excitement, delirium, convulsions, hypothermia. GI: Nausea, vomiting, epigastric pain, hepatitis.

Over dosage
The more common signs and symptoms of over dosage are tinnitus, dizziness, skin rash and GI disturbances. With higher doses cardiovascular and CNS effects may occur including headache, fever, vomiting, apprehension, confusion and convulsions. Over dosage can be treated by employing gastric lavage or inducing emesis. Urinary acidification will promote renal excretion of quinine. Quinine should be readily dialyzable by haemodialysis or haemoperfusion.

Presentation


QST EC 100
Strip of 10 tablets, box of 10 Strips
.
QST EC 300
Strip of 10 tablets, box of 6 Strips.

QST EC 600
Blister of 10 tablets, box of 5 Strips.

QST SUSPENSION
Bottle of 60 ml

QST INJECTION
1ml and 2ml 5 ampoules in tray , 5 trays in a box



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