Reludrine Tablet Composition, Side Effect, Use, Dose

The Reludrine tablet is for prevention of malaria. It contains proguanil. It is suitable for both adults and children. It is the best drug of choice for preventing malaria in sickle cell patients.

Reludrine

Reludrine is made by McW healthcare and exported by Aquatic remedies ltd both in India. Marketing is done in Nigeria by Reals pharmaceuticals ltd.

Composition Of Reludrine Tablet

Each uncoated tablet contains:

Proguanil Hydrochloride BP 100 mg

Excipients q.s.

Pharmacological Action

Pharmacodynamics

Proguanil is effective against the exoerythrocytic forms of some strains of P. falciparum but it has little or no activity against the exoerythrocytic forms of P. Vivax. The mechanism of action is probably due to inhibition of dihydrofolate reductase. The effect of this action is to prevent schizogony and its main effect is against the developing primary tissue schizonts.

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Pharmacokinetics

Absorption: Rapid, reaching a peak at 3 to 4 hours. The active metabolite (cycloguanil) peaks somewhat later (4 to 9 hours).

Half-life: The half-life of proguanil is 14 to 20 hours, whilst cycloguanil has a half-life of the order of 20 hours. Accumulation during repeated dosing is therefore limited, steady-state being reached within approximately 3 days.

Metabolism: Transformation of proguanil into cycloguanil is associated with cytochrome P450, CYP2C19, activity. A smaller part of the transformation of proguanil into cycloguanil is probably catalyzed by CYP3A4.

Elimination: Elimination occurs both in the faces and, principally, in the urine.

In the event of a daily dose being missed, the blood levels fall rapidly but total disappearance of the drug only occurs 3 to 5 days after stopping treatment.

Indications And Use Of Reludrine

Proguanil is an effective antimalarial agent. It is recommended for the prevention and suppression of malaria.

Dosage Of Reludrine Tablet

Adults: Two tablets (200 mg) daily.

Children: Under 1 year: 1/4 tablet (25 mg) daily

1 to 4 years: 1/2 tablet (50 mg) 

5 to 8 years: 1 tablet (100 mg) dally

9 to 14 years: 1 1/2 tablets (150 mg) daily

Over 14 years: Adult dose daily

The daily dose is best taken with water, after food, at the same time each day.

Elderly patients: There are no special dosage recommendations for the elderly, but it may be advisable to monitor elderly patients so that optimum dosage can be individually determined.

Renal Impairment: Based on a theoretical model derived from a single dose pharmacokinetic study, the following guidance is given for adults with renal impairment.

Creatinine clearance (ml/min 1.73 m') ≥ 60: dosage 200 mg once daily (standard dose)

Creatinine clearance (ml/min 1.73 m') 20 to 59: dosage 100 mg once daily

Creatinine clearance (ml/min 1.73 m') 10 to 19: dosage 50 mg every second

Creatinine clearance (ml/min 1.73 m') < 10: dosage 50 mg once weekly

The grade of renal impairment and/or the serum creatinine concentration may be approximately equated to creatinine clearance levels as indicated below.

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clearance (ml/min/1.73 m²) ≥60: Approx serum creatinine (micromol/1) nil: Renal Impairment Grade (arbitrarily divided for dosage purposes) nil

clearance (ml/min/1.73 m²) 20 to 59: Approx serum creatinine (micromol/1) 150 to 300: Renal Impairment Grade (arbitrarily divided for dosage purposes) mild

clearance (ml/min/1.73 m²) 10-19: Approx serum creatinine (micromol/1) 300 to 700: Renal Impairment Grade (arbitrarily divided for dosage purposes) moderate

clearance (ml/min/1.73 m²) ≥60: Approx serum creatinine (micromol/1) >700: Renal Impairment Grade (arbitrarily divided for dosage purposes) severe

*Serum creatinine concentration is only an approximate guide to renal function unless corrected for age, weight and sex.

Contraindications Of Reludrine

Proguanil should be used with caution in patients with severe renal impairment.

Drug Interaction

Antacids may reduce the absorption of proguanil, so should be taking at least 2 - 3 hours apart.

Anticoagulants

Proguanill can potentiate the anticoagulant effect of warfarin and related anticoagulants through a possible interference with their metabolic pathways. Caution is advised when initiating or withdrawing malaria prophylaxis with Paludrine in patients on continuous treatment with anticoagulants.

Live Oral Typhoid Vaccination (Ty21a Strain)

Proguanil should be stopped 3 days before and should not be started until 3 days after receiving live oral typhoid vaccination (Ty21a strain).

Boosted Protease-inhibitors

When given with boosted protease-inhibitors, reduction in proguanil exposure has been observed. This combination should be avoided when possible.

Warnings And Precautions

Proguanil should be used with caution in patients with severe renal impairment. There have been rare reports of hematological changes in such patients. In any locality where drug-resistant malaria is known or suspected, it is essential to take local medical advice on what prophylactic regimen is appropriate. Prophylactic use of Proguanil alone may not be sufficient.

Pregnancy And Lactation

Pregnancy- Proguanil has been widely used for over 40 years and a causal connection between its use and any adverse effect on mother or fetus has not been established.

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However, Proguanil should not be used during pregnancy unless, in the judgment of the physician, potential benefit outweighs the risk. Malaria in pregnant women increases the risk of maternal death, miscarriage, still-birth and low birth weight with the associated risk of neonatal death. Although travel to malarious areas should be avoided during pregnancy, if this is unavoidable effective prophylaxis is therefore strongly advised in pregnant women.

Lactation- Although Proguanil is excreted in breast milk, the amount is insufficient to confer any benefit on the infant. Separate chemoprophylaxis for the infant is required.

Effects On Ability To Drive And Use Machines

There is no evidence to suggest that Proguanil causes sedation or is likely to affect concentration.

Side Effects Of Reludrine Tablet

Side effects which may occur in adult patients include, but are not limited to abdominal Pain, nausea, vomiting, headache, diarrhea, asthenia, dizziness, anorexia.

Known Symptoms Of Overdosage And Particulars Of Its Treatment

The following effects have been reported in cases of overdosage: Haematuria, renal irritation, epigastric discomfort and vomiting There is no specific antidote and symptoms should be treated as they arise.