Mefloquine
Mechanism :
Mefloquine is an antimalarial agent which acts as a blood schizonticide. Acts on mature trophozoite stage and is gametocidal for vivax, ovale and malaria plasmodium.
Indication :
- Malaria- prophylaxis and treatment of multi drug resistant falciparum malaria
Contraindications :
Contraindicated in patients with a known hypersensitivity to Mefloquine or related compounds (e.g., quinine and quinidine), in prophylaxis of patients with active depression, a recent history of depression, generalized anxiety disorder, psychosis, or schizophrenia or other major psychiatric disorders, or with a history of convulsions.
Dosing :
Malaria prophylaxis:
5 mg/kg salt PO once a week. Max: 250 mg. To be given 1 week before entering and to continue for 4 weeks after return.
Malaria treatment:
15 mg/kg PO followed by 10 mg/kg PO 6-24 hours later. Max: 1250 mg/dose.
Adverse Effect :
Dizziness, abdominal pain, loss of appetite, fever, insomnia, difficulty concentrating, stomach pain, light-headedness, visual disturbances, myalgia, nausea, skin rash, headache, vomiting, diarrhea, chills, fatigue, and tinnitus. Rarely pruritus, bradycardia, hair loss, asthenia, emotional problems, transient emotional disturbances and telogen effluvium (loss of resting hair). Seizures have also been reported.
Interaction :
Quinine, quinidine and chloroquine: May produce electrocardiographic abnormalities and increase the risk of convulsions.
Anti-Arrhythmic or Beta-Adrenergic Blocking Agents, Calcium Channel Blockers, Antihistamines or H1-Blocking Agents, Tricyclic Antidepressants and Phenothiazines: Might also contribute to a prolongation of the QTc interval.
Valproic Acid, Carbamazepine, Phenobarbital or Phenytoin: May reduce seizure control by lowering the plasma levels of the anticonvulsant.
Oral Live Typhoid Vaccines: Attenuation of immunization cannot be excluded. Vaccinations with attenuated live bacteria should therefore be completed at least 3 days before the first dose of mefloquine.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 20-50 | Dose as in normal renal function |
| 10-20 | Dose as in normal renal function |
| <10 | Use with caution Prophylaxis: Dose as in normal renal function |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Not dialysed. Dose as in GFR<10 mL/min |
| HD | Not dialysed. Dose as in GFR<10 mL/min |
| HDF/High flux | Not dialysed. Dose as in GFR<10 mL/min |
| CAV/VVHD | Not dialysed. Dose as in GFR=10– 20 mL/min |
Hepatic Dose :
Half-life may be prolonged and plasma levels may be higher in patients with hepatic impairment; use with caution. Avoid for prophylaxis in severe liver disease.