Piperaquine tetraphosphate with artenimol oral
- Drugs List
- Therapeutic Indications
- Dosage
- Contraindications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
- Monograph
Presentation
Oral formulations containing piperaquine tetraphosphate (as the tetrahydrate) and artenimol.
Drugs List
Therapeutic Indications
Uses
Treatment of falciparum malaria
Treatment of uncomplicated P. falciparum malaria in adults, children and infants 6 months and over, weighing 5kg or more.
For up to date advice on geographical resistance patterns and appropriate prophylaxis, current guidelines should be consulted.
Guidelines for Malaria Prevention from the Health Protection Agency specifically developed for travellers from the United Kingdom may be obtained on the HPA website: https://www.gov.uk/government/organisations/public-health-england
Dosage
Adults
Administer over three consecutive days, for a total of three doses. Doses should be taken at the same time each day.
Dosing should be based on body weight (kg) as follows:
5kg to 7kg body weight: 80mg piperaquine and 10mg artenimol (equivalent to a quarter of a 320mg/40mg tablet)
7kg to less than 13kg body weight: 160mg piperaquine and 20mg artenimol (half a 320mg/40mg tablet)
13kg to less than 24kg body weight: 320mg piperaquine and 40mg artenimol (one 320mg/40mg tablet)
24kg to less than 36kg body weight: 640mg piperaquine and 80mg artenimol (two 320mg/40mg tablets)
36kg to less than 75kg body weight: 960mg piperaquine and 120mg artenimol (three 320mg/40mg tablets)
75kg to less than 100kg body weight: 1280mg piperaquine and 160mg artenimol (four 320mg/40mg tablets)
More than 100kg body weight: There are no data available to recommend doses in these patients
This formulation is not suitable for patients weighing less than 5kg.
Children
(See Dosage; Adult)
Additional Dosage Information
If a patients vomits up to 30 minutes after taking a dose, the whole dose should be re-administered.
If a patients vomits 30 to 60 minutes after taking a dose, half the dose should be re-administered.
Re-dosing should not be attempted more than once. If the second dose is vomited, alternative antimalarial therapy should be instituted.
If a dose is missed, it should be taken as soon as realised and the recommended regimen continued until the full course of treatment has been completed.
A second course should not be given within two months after the first course due to the long elimination half-life of piperaquine. No more than two courses may be given within a 12 month period due to a lack of clinical experience, at the time of writing, on repeated courses of treatment.
Contraindications
Children under 6 months
Children weighing less than 5kg
Family history of long QT syndrome
Family history of sudden death
Breastfeeding
Congestive cardiac failure with reduced left ventricular ejection fraction
History of cardiac arrhythmias
History of left ventricular hypertrophy
Hypertrophic cardiomyopathy
Hypocalcaemia
Hypokalaemia
Hypomagnesaemia
Long QT syndrome
Pregnancy
Severe bradycardia
Severe hypertension
Torsade de pointes
Precautions and Warnings
Elderly
Electrolyte imbalance
History of torsade de pointes
Moderate hepatic impairment
Moderate renal impairment
Correct electrolyte disorders before treatment
Consider prevalence of resistance when prescribing
Consult national/regional policy on the use of anti-infectives
No experience of exposure to second or subsequent treatment courses
Advise no food for 3 hours pre- and post dose
Perform ECG before and during treatment
If QTc>500msec during therapy, continuous cardiac monitoring is required
Monitor serum electrolytes
Predisposition QT prolongation: Counsel patient on symptoms of arrhythmias
Discontinue treatment if QTc exceeds 500msec
Advise patient not to take St John's wort concurrently
Advise patient grapefruit products may increase plasma level
Prescriber should note the long half-life of piperaquine, about 22 days, in the event that another anti-malarial agent is started due to treatment failure or a new malaria infection.
The risk of QTc interval prolongation may be greatest during the period before the last dose and 4 to 6 hours after the last dose. When clinically appropriate, consideration should be given to obtaining an ECG from all patients before the last of the three daily doses is taken and approximately 4 to 6 hours after the last dose. QTc intervals of more than 500 ms are associated with an increased risk for potentially life-threatening ventricular tachyarrhythmias including torsades de pointes. ECG monitoring during the following 24 to 48 hours is necessary in patients found to have a prolongation to this extent. No further doses of piperaquine tetraphosphate and artenimol should be given.
Female and elderly patients have longer QTc intervals than adult males. These patients may therefore be more sensitive to the effects of QTc-prolonging medications such as piperaquine tetraphosphate and artenimol. Special caution is required.
Caution is advised in young children when vomiting, as they are likely to develop electrolyte disturbances. These may increase QTc-prolonging effect of piperaquine tetraphosphate and artenimol.
Absorption of piperaquine is increased in the presence of fatty food which may increase its effect on QTc interval. Tablets should be taken with water only.
Pregnancy and Lactation
Pregnancy
Piperaquine with artenimol is contraindicated during pregnancy.
The manufacturer recommends piperaquine tetraphosphate and artenimol should not be used during pregnancy in situations where other suitable and effective anti-malarials are available. Animal data suggests piperaquine tetraphosphate and artenimol would cause serious birth defects when administered during the first trimester of pregnancy. At the time of writing, there are insufficient data on the use of piperaquine tetraphosphate and artenimol during human pregnancy. Reproductive studies with artemisinin derivatives have demonstrated teratogenic potential with an increased risk during early gestation.
Lactation
Piperaquine with artenimol is contraindicated during breastfeeding.
The manufacturer recommends women taking piperaquine with artenimol should not breastfeed during their treatment. Animal data suggest piperaquine is excreted into breast milk. At the time writing, there are insufficient data on the use of piperaquine with artenimol during breastfeeding. The effects on exposed infants are unknown.
Side Effects
Abdominal pain
Acanthosis nigricans
Altered liver function tests
Anaemia
Anorexia
Arthralgia
Asthenia
Bradycardia
Cardiac conduction disturbances
Conjunctivitis
Convulsions
Cough
Decrease in haemoglobin and haematocrit
Decreased appetite
Dermatitis
Diarrhoea
Dizziness
Ear infection
Eosinophilia
Epistaxis
Headache
Heart murmur
Hepatitis
Hepatomegaly
Hypochromic anaemia
Influenza
Jaundice
Leucopenia
Lymphadenopathy
Myalgia
Nausea
Neutropenia
Prolongation of QT interval
Pruritus
Pyrexia
Rash
Respiratory tract infection
Rhinorrhoea
Sinus arrhythmia
Sinus tachycardia
Splenomegaly
Stomatitis
Tachycardia
Thrombocythaemia
Thrombocytopenia
Variation in heart rate
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: August 2019
Reference Sources
NICE Evidence Services Available at: www.nice.org.uk Last accessed: 06 August 2019
Summary of Product Characteristics: Eurartesim 320mg/40mg film-coated tablets. Logixx Pharma Solutions Ltd. Revised September 2016.
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