Mefloquine oral
- Drugs List
- Therapeutic Indications
- Dosage
- Contraindications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
- Monograph
Presentation
Tablets containing mefloquine.
Drugs List
Therapeutic Indications
Uses
Malaria - prophylaxis
Malaria - treatment
Treatment of malaria:
Mefloquine is especially indicated for treatment of Plasmodium falciparum malaria in which the pathogen is resistant to other antimalarial agents.
Mefloquine is recommended for inclusion in artemisinin combination therapy (ACT).
Prophylaxis of malaria:
Prophylaxis with mefloquine is especially recommended for travellers to areas where multiple resistant P. falciparum strains occur.
For up to date advice on geographical resistance patterns and appropriate prophylaxis, current guidelines should be consulted.
Guidelines for Malaria Prevention from Public Health England specifically developed for travellers from the United Kingdom may be obtained from:
https://www.gov.uk/government/publications/malaria-prevention-guidelines-for-travellers-from-the-uk
Dosage
Adults
Malaria Treatment:
20mg/kg to 25mg/kg.
The total curative dose may be split into two or three doses taken 6 to 8 hours apart in order to reduce the risk or severity of adverse effects. Below are the recommended therapeutic dosages of mefloquine relative to body weight:
Body weight over 60kg: six 250mg tablets (1.5g)
Body weight over 45kg to 60kg: four to five 250mg tablets (1g to 1.25g)
Body weight over 30kg to 45 kg: three to four 250mg tablets (750mg to 1g)
Body weight 20kg to 30 kg: two to three 250mg tablets (500mg to 750mg)
There is no experience of doses greater than six 250mg tablets (1.5g) in very heavy patients.
If treatment course yields no improvement with 48 to 72 hours, consider alternative treatment.
Malaria Prophylaxis:
Prophylaxis of malaria with mefloquine should be initiated at least 10 days or up to 3 weeks prior to arrival in a malarious area. The tablets should be taken once weekly on the same day of the week, and continued for 4 weeks after leaving the malarious area. The minimum duration of treatment is 6 weeks and the maximum is 12 months.
The dose for prophylaxis approximately equates to 5mg/kg once weekly.
Body weight over 45kg: one 250mg tablet once weekly
Body weight 31kg to 45kg: three quarters of a 250mg tablet (187.5mg) once weekly
Body weight 20kg to 30kg: half a 250mg tablet (125mg) once weekly
Body weight 5kg to 19kg: one quarter of a 250mg tablet (62.5mg) once weekly
Children
Experience with mefloquine in infants less than 3 months old or weighing less than 5kg is limited.
Malaria Treatment:
20mg/kg to 25mg/kg.
The total curative dose may be split into two or three doses taken 6 to 8 hours apart in order to reduce the risk or severity of adverse effects. Below are the suggested therapeutic dosages of mefloquine relative to body weight:
Body weight over 60kg: six 250mg tablets (1.5g)
Body weight over 45kg to 60kg: four to five 250mg tablets (1g to 1.25g)
Body weight over 30kg to 45kg: three to four 250mg tablets (750mg to 1g)
Body weight 20 to 30kg: two to three 250mg tablets (500mg to 750mg)
Body weight less than 20kg: one quarter of a 250mg tablet (62.5mg) per every 2.5kg to 3kg. One 250mg tablet per every 10kg to 12kg.
There is no experience of doses greater than six 250mg tablets (1.5g) in very heavy patients.
If treatment course yields no improvement with 48 to 72 hours, consider alternative treatment.
Malaria Prophylaxis:
The dose for prophylaxis approximately equates to 5 mg/kg once weekly.
Body weight over 45kg: one 250mg tablet once weekly
Body weight 31kg to 45kg: three quarters of a 250mg tablet (187.5mg) once weekly
Body weight 20kg to 30kg: half a 250mg tablet (125mg) once weekly
Body weight 5kg to 19kg: one quarter of a 250mg tablet (62.5mg) once weekly
The following alternate dosing schedule may also be suitable:
Children with body weight over 45kg: 250mg once weekly
Children with body weight 25kg to 44kg: 187.5mg once weekly
Children with body weight 16kg to 24kg: 125mg once weekly
Children with body weight 5kg to 15kg: 62.5mg once weekly
Additional Dosage Information
If the patient vomits less than 30 minutes after receiving the drug, a second full dose should be given. If the patient vomits between 30 to 60 minutes after a dose, a further half dose should be given.
For severe acute malaria, mefloquine may be administered following an initial course of intravenous quinine lasting at least 2 to 3 days. To prevent interactions leading to adverse effects, an interval of 12 hours should elapse between quinine and mefloquine doses.
Contraindications
Epilepsy - unless for malaria treatment
Galactosaemia
History of psychiatric disorder - if used for malaria prophylaxis
Long QT syndrome
Severe hepatic impairment - if used for malaria prophylaxis
Torsade de pointes
Precautions and Warnings
Children under 3 months
Children weighing less than 5kg
Family history of long QT syndrome
Breastfeeding
Cardiac conduction defects
Electrolyte imbalance
Glucose-galactose malabsorption syndrome
History of torsade de pointes
Lactose intolerance
Pregnancy
Renal impairment - glomerular filtration rate below 10ml/minute
Correct electrolyte disorders before treatment
Advice available from specialist unit for the use of this drug
Advise ability to drive/operate machinery may be affected by side effects
Avoid within 12 hours of oral typhoid vaccine
Consult national/regional policy on the use of anti-infectives
Drugs for malaria prophylaxis are not prescribable on the NHS
Use different drug for treatment if this agent was used for prophylaxis
Contains lactose
Consider monitoring ECG in patients at risk of QT prolongation
If visual disturbances occur, perform ophthalmic evaluation
Monitor serum electrolytes
Advise patient or carer to report any neuropsychiatric event
Advise patient to report signs of neuropathy
Discontinue if psychiatric disturbances develop
May exacerbate epilepsy - use for curative treatment of malaria only
Treatment: if no improvement within 72 hours consider alternative therapy
Advise patient not to take St John's wort concurrently
Male & female: Contraception required during & for 3 months after treatment
Advise of importance of avoiding mosquito bites
Advise patients on the importance of taking treatment regularly
Consult Dr. if illness occurs within 1 year of return from malarious area
There is a possibility of re-infection or recrudescence after successful antimalarial treatment and the patient should be made aware of this.
Pregnancy and Lactation
Pregnancy
Use mefloquine with caution during pregnancy.
The manufacturer suggests prophylactic treatment with mefloquine in pregnancy may be considered as long as strict respect to the indications are followed. Use of mefloquine as a curative treatment in pregnancy is limited to the treatment of acute uncomplicated malaria when quinine is contraindicated or in case of Plasmodium falciparum resistance to quinine. In case of unplanned pregnancy, malaria chemoprophylaxis with mefloquine is not considered as an indication for pregnancy termination. Relevant guidelines should be consulted.
Clinical experience with mefloquine in pregnancy has not revealed embryotoxic or teratogenic effect. Data from a limited number of exposed pregnancies, at the time of writing, indicate no adverse effects of mefloquine on pregnancy or on the health of the foetus/newborn child. Teratogenicity has been observed in mice and rats and embryotoxicity has been seen in rabbits.
Lactation
Use mefloquine with caution during breastfeeding.
The manufacturer does not recommend using mefloquine during breastfeeding.
Administration of mefloquine to the infant should be considered separately from administration to the mother. The effect of the small amounts of mefloquine excreted in breast milk on the infant are unknown. Relevant guidelines should be consulted. Mefloquine is excreted into breast milk at low levels (approximately 4% of maternal dose). Mefloquine has the potential for neurotoxicity. However, there is insufficient information to assess the neurotoxic potential of mefloquine in a breastfeeding infant.
Counselling
Tablets should be swallowed whole after a meal with plenty of liquid.
Side Effects
Abdominal pain
Acute renal failure
Aggression
Agitation
Agranulocytosis
Alopecia
Amnesia
Anaphylaxis
Anxiety
Aplastic anaemia
Arthralgia
Asthenia
Ataxia
Bradycardia
Chest pain
Chills
Circulatory disturbances
Conduction disturbances
Confusion
Convulsions
Cranial nerve palsy
Decreased appetite
Depression
Diarrhoea
Dizziness
Dream abnormalities
Dyspepsia
Dyspnoea
Encephalopathy
Erythema
Erythema multiforme
Extrasystoles
Fatigue
Fever
Flushing
Hallucinations
Headache
Hearing disturbances
Hepatic failure
Hepatitis
Hypersensitivity reactions
Hypertension
Hypotension
Impaired memory
Increases in serum transaminases (transient)
Insomnia
Irregular pulse
Jaundice
Leucocytosis
Leucopenia
Loss of balance
Malaise
Mood changes
Muscle cramps
Muscle weakness
Myalgia
Nausea
Nephritis
Neuropathy
Neuropsychiatric disturbances
Oedema
Palpitations
Pancreatitis
Panic attack
Paraesthesia
Paranoia
Pneumonitis
Prolongation of QT interval
Pruritus
Psychiatric disorders
Psychosis
Rash
Restlessness
Serum creatinine increased
Sleep disturbances
Somnolence
Stevens-Johnson syndrome
Suicidal tendencies
Sweating
Syncope
Tachycardia
Thrombocytopenia
Tinnitus
Tremor
Urticaria
Vertigo
Vestibular disorders
Visual disturbances
Vomiting
Overdosage
It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.
The following number will direct the caller to the relevant local centre (0844) 892 0111
Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Further Information
Last Full Review Date: July 2020
Reference Sources
Drugs During Pregnancy and Lactation: Treatment Options and Risk Assessment, 2nd edition (2007) ed. Schaefer, C., Peters, P. and Miller, R. Elsevier, London.
Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 9th edition (2011) ed. Briggs, G., Freeman, R. and Yaffe, S. Lippincott Williams & Wilkins, Philadelphia.
Medications and Mothers' Milk, Sixteenth Edition (2014) Hale, T and Rowe, H, Hale Publishing, Plano, Texas.
Martindale: The Complete Drug Reference, 37th edition (2011) ed. Sweetman, S. Pharmaceutical Press, London.
Summary of Product Characteristics: Lariam 250mg Tablets. Roche Products Ltd. Revised April 2020.
The Renal Drug Handbook. Fifth Edition (2019) ed. Ashley, C. and Dunleavy, A. Radcliffe Publishing Ltd, London.
MHRA Drug Safety Update: Volume 7, Issue 4, November 2013 - Direct Healthcare Professional Communication on mefloquine for malaria chemoprophylaxis and the risk of neuropsychiatric adverse reactions
https://www.mhra.gov.uk/home/groups/pl-p/documents/drugsafetymessage/con333639.pdf
MHRA Drug Safety Update November 2013
Available at: https://www.mhra.gov.uk/Safetyinformation/DrugSafetyUpdate/CON336723 Last accessed: December 10, 2013 MHRA Drug Safety Update: Volume 7, Issue 4, November 2013 - Mefloquine strengthened warnings on neuropsychiatric side effects
UK Drugs in Lactation Advisory Service.
Available at: https://www.ukmicentral.nhs.uk/drugpreg/guide.htm
Last accessed: December 10, 2013
US National Library of Medicine. Toxicology Data Network. Drugs and Lactation Database (LactMed).
Available at: https://www.ncbi.nlm.nih.gov/books/NBK501922/
Mefloquine Last revised: 31 October 2018
Last accessed: 15 June 2020
NICE Evidence Services Available at: www.nice.org.uk Last accessed: 15 June 2020
Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content
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