Mefloquine

These indications are based on manufacturer information for both originator and generic products. For product specific registered indications, please refer to product specific manufacturer information

Registered South African indications:

• Prophylaxis of Plasmodium falciparum malaria, in regions where resistance to 4-aminoquinolines occur

Due to the risk of a potentially fatal prolongation of the QTc interval, halofantrine must not be given during mefloquine therapy for prophylaxis or within 15 weeks after the last dose of mefloquine. Quinine and quinidine which are commonly required for the treatment of severe malaria, are contraindicated when mefloquine prophylaxis has been used. If acute anxiety, depression, restlessness or confusion occurs during prophylactic use, mefloquine should be discontinued and an alternative prophylactic agent should be recommended. Due to elevated plasma concentrations and increased elimination half-life of mefloquine following coadministration with ketoconazole, the risk of QTc prolongation may also be increased if ketoconazole is taken during mefloquine therapy for prophylaxis, or within 15 weeks after the last dose of mefloquine.

 

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to related compounds (e.g. quinine and quinidine)
• Pregnancy
  - As teratogenicity in animals has been shown
• Lactation
  - Mefloquine is excreted into breastmilk, with 3-4% excreted after a dose of 250mg
• Mefloquine should not be used for prophylaxis in persons with a history of psychiatric disturbances, including depression or convulsions
• Prophylactic use in young children (body weight less than 5 kg) due to lack of available data
• Renal impairment
• Hepatic impairment
• Due to the risk of a potentially fatal prolongation of the QTc interval, halofantrine must not be given during mefloquine therapy for prophylaxis or within 15 weeks after the last dose of mefloquine

Cautions

• Cardiac conduction disorders
• Epilepsy
• Prolonged use
• Drug resistance
• Congenital hyperinsulinaemic hypogylaemia
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption

Forms avail. in SA and covered in this monograph: tab

Infections caused by: Plasmodium falciparum 

Specific doses based on individual indications

Please note that the dosages below should be used in combination with regional guidelines, taking into account local antibiotic sensitivities

Prophylaxis of Plasmodium falciparum malaria
- In regions where resistance to 4-aminoquinolines occur

• >45kg: Oral (tab): 250mg, once weekly
• <45kg: Oral (tab): See paediatric dosages

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Mefloquine may be effective against malaria parasites resistant to proguanil, pyrimethamine-sulfonamide combinations

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The recommended prophylactic dose of mefloquine is approximately 5mg/kg once weekly

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The first dose should be taken at least one week before arrival in an endemic area. In certain cases, e.g. when a traveller is taking other medication, it may be desirable to start prophylaxis 2-3 weeks prior to departure, in order to ensure that the combination of drugs is well tolerated. Weekly doses should always be taken on the same day of the week. To reduce the risk of malaria after leaving an endemic area, prophylaxis must be continued for 4 additional weeks

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Directions for use
The tablets should be swallowed whole after food with plenty of fluids. The tablets may be crushed and suspended in a small amount of water, milk or other beverage for administration to small children and other persons unable to swallow them whole. Mefloquine has a bitter and slightly burning taste

Paed. forms avail. in SA and covered in this monograph: tab

Infections caused by: Plasmodium falciparum 

Specific doses based on individual indications

Please note that the dosages below should be used in combination with regional guidelines, taking into account local antibiotic sensitivities

Prophylaxis of Plasmodium falciparum malaria
- In regions where resistance to 4-aminoquinolines occur

• Infant <3months OR <5kg: Not established for use
• 5-20kg: Oral (tab): 62.5mg, once weekly
• >20-30kg: Oral (tab): 125mg, once weekly
• >30-45kg: Oral (tab): 187.5mg, once weekly
• >45kg: See adult dosages

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Mefloquine may be effective against malaria parasites resistant to proguanil, pyrimethamine-sulfonamide combinations

---

The recommended prophylactic dose of mefloquine is approximately 5mg/kg once weekly

---

The first dose should be taken at least one week before arrival in an endemic area. In certain cases, e.g. when a traveller is taking other medication, it may be desirable to start prophylaxis 2-3 weeks prior to departure, in order to ensure that the combination of drugs is well tolerated. Weekly doses should always be taken on the same day of the week. To reduce the risk of malaria after leaving an endemic area, prophylaxis must be continued for 4 additional weeks

---

Directions for use
The tablets should be swallowed whole after food with plenty of fluids. The tablets may be crushed and suspended in a small amount of water, milk or other beverage for administration to small children and other persons unable to swallow them whole. Mefloquine has a bitter and slightly burning taste

Pregnancy

• Contraindicated

Breastfeeding

• Contraindicated

Renal Impairment

• Contraindicated

Hepatic Impairment 

• Contraindicated

Elderly

• No dose adjustment recommended

Porphyria Information

• Possibly porphyrinogenic (PSP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Dizziness 
• Headache
• Encephalopathy 
• Cranial nerve paralysis
• Seizures
• Amnesia
• Syncope 
• Speech disorder 
• Memory impairment 
• Balance disorder
• Gait disturbance 
• Peripheral motor neuropathy
• Peripheral sensory neuropathy 
• Somnolence
• Abnormal dreams
• Insomnia
• Depression
• Anxiety
• Suicide
• Attempted suicide
• Suicidal ideation 
• Self-endangering behavior 
• Bipolar disorder
• Psychotic disorder
• Depersonalization 
• Mania
• Schizophrenia
• Schizophreniform disorder
• Paranoia
• Panic attacks 
• Confusion
• Hallucinations
• Aggression
• Agitation
• Restlessness 
• Mood swings 
• Disturbance in attention

Cardiovascular Disorders

• Atrio-ventricular block
• Tachycardia 
• Palpitation 
• Bradycardia
• Irregular heart rate
• Extrasystoles 
• Transient conduction disorder
• Hypotension 
• Hypertension 
• Flushing

Respiratory Disorders

• Pneumonia
• Pneumonitis
• Dyspnoea

Gastrointestinal Disorders

• Nausea and vomiting 
• Diarrhoea
• Abdominal pain
• Pancreatitis
• Dyspepsia

Hepatobiliary disorders

• Hepatic failure
• Hepatitis
• Jaundice
• Increased transaminases

Genitourinary Disorders

• Acute renal failure
• Nephritis 
• Increased blood creatinine

Endocrine and Metabolism Disorders

• Decreased appetite 

Musculoskeletal Disorders

• Muscular weakness
• Muscle spasms
• Myalgia
• Arthralgia

Skin and Subcutaneous Tissue Disorders

• Pruritus
• Stevens-Johnson syndrome
• Erythema multiforme
• Rash
• Erythema
• Urticaria
• Alopecia
• Hyperhidrosis

Immune, Blood and Lymphatic System Disorders

• Agranulocytosis
• Aplastic anaemia
• Leukopenia
• Leukocytosis
• Thrombocytopenia
• Hypersensitivity

Sensory Disorders

• Visual impairment
• Cataract
• Retinal disorders
• Optic neuropathy
• Vision blurred
• Vertigo
• Tinnitus
• Partial deafness 
• Impaired hearing 
• Hyperacusis

• Halofantrine
• Quinine
• Quinidine
• Ketoconazole
• QT prolonging agents
• Anticonvulsants
• Agents that lower seizure threshold
• CYP3A4 inhibitors
• CYP3A4 inducers
• Oral live typhoid vaccine

None routine. Specific cases may require:

• Hepatic function 
• Ophthalmic examination

Mefloquine produces swelling of the Plasmodium falciparum food vacuoles. It acts by forming toxic complexes with free heme which damage membranes and interact with other plasmodial components.

Spectrum of activity: Plasmodium falciparum 

Tablet 250mg

• Lariam (Roche) originator
• Mefliam (Cipla)