Proguanile

Proguanile Uses, Dosage, Side Effects, Mechanism of Action, How Long Does it Take to Work? Proguanile is a brand name. Its generic name is Proguanil.

Introduction

Proguanile is a type of antimalarial medication, used together with an antimalarial drug such as atovaquone in the prevention of malaria or the treatment of drug-sensitive, vivax and ovale malaria. Proguanile was approved by the US Food and Drug Administration in 1952 and has been in use for over 50 years.

Uses

Proguanile is primarily used to prevent or treat malaria, as well as in the treatment of some autoimmune diseases and systemic lupus erythematosus (SLE). It is also used as an adjuvant to enhance the effectiveness of cholera vaccines.

Mechanism of Action

Proguanile acts by preventing the development of malaria parasites in the body. It does this by inhibiting the enzyme dihydrofolate reductase (DHFR) which is involved in folate metabolism. By blocking the enzyme, Proguanile prevents the parasites from synthesizing and incorporating folates into their cell walls. This results in the death of the parasite.

How Long Does It Take to Work?

When taken as a prophylactic, Proguanile starts to work immediately. However, for those already infected with malaria, it may take several days for the drug to show its effects.

Absorption

Proguanile is rapidly and almost completely absorbed from the gastrointestinal tract. Its absolute bioavailability of around 1% following oral administration increases to over 80% when administered intramuscularly.

Route of Elimination

Proguanile is eliminated primarily through the kidneys, with approximately 90% of an administered dose being excreted unchanged in the urine. The remainder is metabolized in the liver and eliminated as metabolites.

Dosage

The recommended dose of Proguanile depends on the type of malaria being treated. For prophylaxis against certain types of malaria, the recommended dose is 200mg (1 tablet) once daily for adults, and 1.5mg/kg (maximum 200mg dose) once daily for children. For the treatment of malaria, the recommended dose is 400mg (2 tablets) once daily for adults, and 2.5mg/kg (maximum 400mg dose) once daily for children.

Administration

Proguanile can be administered orally or intramuscularly. It is available in tablet, capsule, or oral solution form as well as intramuscular injection form.

Side Effects

The most common side effects of Proguanile include abdominal pain, headaches, nausea, vomiting, diarrhea, loss of appetite, dizziness, fatigue, and rash. Other more serious side effects that occur infrequently include anemia, heart attack, kidney damage, liver damage, and seizures.

Toxicity

Proguanile is an extremely safe drug, with no known toxic reaction. It has a wide therapeutic index (the ratio between the therapeutic dose and the toxic dose) and is considered to be safe in pregnancy and breastfeeding.

Precautions

Patients taking Proguanile should check with their doctor before taking antacids (such as Mylanta or Maalox) that contain magnesium or aluminum. Taking antacids at the same time as Proguanile can reduce its effectiveness. Patients should also monitor their liver enzymes, and inform their doctor if they experience any signs of liver damage (such as yellowing of the eyes or skin, dark urine, increased pain).

Interactions

Proguanile can interact with many other drugs, including certain antacids, antibiotics, anticonvulsants, antifungals, or drugs taken for depression, allergies, or HIV infection. Patients should always inform their doctor of any medications they are taking before starting Proguanile.

Disease Interaction

Proguanile should be used with caution in patients with severe anemia, kidney or liver disease, or decreased levels of folate, or those receiving concomitant methotrexate therapy.

Drug Interaction

Proguanile can interact with many other drugs, such as antibiotics, anticonvulsants, antifungals, or drugs taken for depression, allergies, or HIV infection. It can also interact with antacids that contain magnesium or aluminum, as this can reduce the effectiveness of Proguanile. Patients should inform their doctor of any other medications they are taking before starting Proguanile.

Food Interactions

Proguanile can be taken with or without food. It is best to take Proguanile with food as it may help the body absorb the drug better.

Pregnancy Use

Proguanile should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Studies in animals suggest that Proguanile may cause fetal harm when administered during gestation.

Lactation Use

Proguanile should not be used during breastfeeding as it is found in breastmilk in low concentrations and could potentially be harmful to an infant.

Acute Overdose

An acute overdose of Proguanile can cause nausea, vomiting, loss of appetite, and abdominal pain. Rarely, an overdose can lead to unconsciousness, respiratory depression, cardiac arrest, arrhythmia, and hypotension.

Contraindication

Proguanile should not be used in patients with known allergies or hypersensitivity to the drug.

Use Directions

Proguanile should always be taken exactly as prescribed by the doctor, following the instructions on the patient information leaflet. It is best taken with food and should not be cut, chewed, or crushed.

Storage Conditions

Proguanile should be stored at room temperature, away from moisture and heat. It should be kept out of reach of children and pets.

Volume of Distribution

The volume of distribution of Proguanile is approximately 0.24 L/kg.

Half Life

Proguanile has a half-life of approximately 9.1 hours.

Clearance

Proguanile is cleared from the body by the kidneys and has a renal clearance rate of approximately 10 mL/min/kg.

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