Proguanilum

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

Introduction

Proguanilum 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. Proguanilum was approved by the US Food and Drug Administration in 1952 and has been in use for over 50 years.

Uses

Proguanilum 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

Proguanilum 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, Proguanilum 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, Proguanilum starts to work immediately. However, for those already infected with malaria, it may take several days for the drug to show its effects.

Absorption

Proguanilum 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

Proguanilum 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 Proguanilum 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

Proguanilum 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 Proguanilum 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

Proguanilum 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 Proguanilum 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 Proguanilum 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

Proguanilum 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 Proguanilum.

Disease Interaction

Proguanilum 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

Proguanilum 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 Proguanilum. Patients should inform their doctor of any other medications they are taking before starting Proguanilum.

Food Interactions

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

Pregnancy Use

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

Lactation Use

Proguanilum 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 Proguanilum 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

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

Use Directions

Proguanilum 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

Proguanilum 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 Proguanilum is approximately 0.24 L/kg.

Half Life

Proguanilum has a half-life of approximately 9.1 hours.

Clearance

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

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