MEFLOQUINE

(Antiprotozoal)

Ma. Jessabeth N. Aluba

BSMT-3A

I. Introduction

• Mefloquine (Lariam, Mephaquin or Mefliam) is a synthetic 4-quinoline methanol derivative, chemically related to Quinine.

• Chemical formula of C17H16F6N2O with a molecular mass of 378.312 g/mol

• It is an effective orally administered medication used in the prevention and treatment of Plasmodium falciparum and against other malarial parasites such as Plasmodium vivax, Plasmodium ovale and Plasmodium malariae.

• Rare but serious neuropsychiatric problems have been associated with its use.

• May increase the risk of convulsion in epileptic patients.

• Also a risk of fatal arryhythmias if given together with Halofantrine.

II. Mechanism of action

• The exact mechanism of action is uncertain or is unknown.

• However, it is proposed to share a similar mechanism of action with Chloroquine, which is inhibition of heme polymerase.

III. Indications

Treatment of Acute Malaria Infections:

Mefloquine is indicated for the treatment of mild to moderate acute malaria caused by mefloquine-susceptible strains of P. falciparum (both chloroquine-susceptible and resistant strains) or by Plasmodium vivax. There are insufficient clinical data to document the effect of mefloquine in malaria caused by P. ovale or P. malariae.

Malaria prevention:

Mefloquine is useful for the prevention of malaria in all areas except for those where parasites may have resistance to multiple drugs. It is typically taken for one to two weeks before entering an area with malaria.Doxycycline and atovaquone/proguanil provide protection within one to two days and may be better tolerated. If a person becomes ill with malaria despite prophylaxis with mefloquine, the use of halofantrine and quinine for treatment may be ineffective.

IV. Contraindications

• Contraindicated in patients hypersensitive to mefloquine or related compounds.

• Contraindicated for prevention of malaria in patients with a history of seizures or an active or recent history of depression, generalized anxiety disorder, psychosis, schizophrenia, or other major psychiatric disorders.

V. Adverse effects

• CNS

fever, dizziness, syncope, headache, psychotic changes, hallucinations, confusion, anxiety, fatigue, vertigo, depression, seizures, tremor, ataxia, mood changes, panic attacks

• CV

chest pain, edema• EENT

tinnitus, visual disturbances

• GI

Anorexia, vomiting, nausea, loose stools, diarrhea, abdominal discomfort or pain, dyspepsia

• Hematologic

leukopenia, thrombocytopenia• Musculoskeletal

myalgia• Skin

rash

• Other

chills, itching, weight loss, unusual aches and pains, jaundice

VI. Responsibilities

• Take dose immediately before or after a meal on the same day each week, to improve compliance.

• Patient should not take drug on an empty stomach and always to take it with at least 8 ounces of water.

• Patient should be careful when performing activities that require alertness and coordination because dizziness, disturbed sense of balance, and neuropsychiatric reactions may occur.

• Patient should notify prescriber if signs and symptoms of impending toxicity occur.

• Women of childbearing age should use reliable contraception during treatment.

• Call your doctor immediately if you are experiencing some uncommon side effects like tingling in your fingers or toes, difficulty in walking, dark colored urine, shaking of arms or legs that you cannot control, etc.

THANKYOU!!