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(Redirected from Malarone)
'Atovaquone' (alternative spelling: 'atavaquone') is a chemical compound that belongs to the class of naphthalenes. Atovaquone is a hydroxy-1,4-naphthoquinone, an analog of ubiquinone, with antipneumocystic activity. Its average wholesale price is about $2.13 per standard 250 mg. tablet.[1] It is also manufactured in the US in the liquid form, or oral suspension, under the brand name Mepron.[2]
Atovaquone is a medication used to treat or prevent:
# Pneumocystis pneumonia (PCP), although it is not approved for treatment of severe PCP.
# Toxoplasmosis. The medication has antiparasitic and therapeutic effects.
# Malaria. It is one of the two components (along with proguanil) in the drug Malarone. Malarone has fewer side effects than mefloquine, but can be more expensive because it's taken daily.[3]
Trimethoprim-sulfamethoxazole (TMP-SMX, Bactrim) is generally considered first line therapy for PCP or toxoplasmosis. However, atovaquone may be used in patients who cannot tolerate, or are allergic to, TMP-SMX. In addition, atovaquone has the advantage of not causing myelosuppression, which is an important issue in patients who have undergone bone marrow transplantation.
Atovaquone is only available as a fixed preparation with proguanil that has been commercially available from GlaxoSmithKline since 2000 as 'Malarone'® (sometimes abbreviated 'A+P'). It can be used both to treat and to prevent malaria.
A "standard" tablet of Malarone contains 100 mg of proguanil hydrochloride and 250 mg of atovaquone. A "pediatric" tablet of Malarone contains 25 mg of proguanil hydrochloride and 62.5 mg of atovaquone.
The adult treatment dose is four "standard" tablets once a day for three days. In children, the drug is prescribed by body weight:
★ 11 to 20 kg: 1 "standard" tablet once daily for 3 days;
★ 21 to 30 kg: 2 "standard" tablets once daily for 3 days;
★ 31 to 40 kg: 3 "standard" tablets once daily for 3 days;
★ 41 kg and above: use adult dose.
Malarone is not licensed for use in children weighing 10 kg or less. The "pediatric" tablets are ''not'' used in malaria treatment.
The advice of a specialist should always be sought when starting malaria treatment. Malarone should not be used to treat severe malaria, when an injectable drug (quinine or artesunate in the UK; quinidine in the US) should be used instead.
Medical advice should always be taken before choosing a drug for malaria prevention. Because some strains of malaria are resistant, Malarone is not effective for malaria prevention in all parts of the world. It must be taken with a fatty meal or at least some milk to be absorbed adequately.
The adult dose is one "standard" tablet daily starting one or two days before traveling into a malaria-endemic area, and continuing throughout the stay and then for another 7 days after returning from the malarious area.
The child dose is prescribed according to body weight:
★ 11–20 kg: 1 "pediatric" tablet once daily;
★ 21–30 kg: 2 "pediatric" tablets once daily;
★ 31–40 kg: 3 "pediatric" tablets once daily;
★ 41 kg and above use adult dose.
The duration of treatment is the same as for adults.
Proguanil acts as a mitochondrial sensitiser and synergizes with atovaquone; also, there is a high natural frequency of cytochrome b mutants which leads to a high failure rate if atovaquone is used on its own to treat malaria. Specific mutations (Y268S, Y268C) have been shown to confer resistance ''in vivo,''[4][5][6] but there are other mechanisms of resistance that remain unknown.[7]
1. (ATN) Atovaquone (Mepron; 566C80) Approved for Pneumocystis; Drug Development, Activism Success
2. Mepron
3. Malarone: New Malaria Medication With Fewer Side-effects
4. Evidence of ''Plasmodium falciparum'' malaria resistant to atovaquone and proguoanil hydrochloride: case reports, Färnet A, Lindberg J, Gil P, ''et al.'', , , Brit Med J, 2003
5. Malarone treatment failure and in-vitro confirmation of resistance of ''Plasmodium falciparum'' isolate from Lagos, Nigeria, Fivelman QL, Butcher GA, Adagu IS, ''et al.'', , , Malaria J, 2002
6. Genetic confirmation of atovaquone-proguanil-resistant ''Plasmodium falciparum'' malaria acquired by a nonimmune traveller to east Africa, Schwartz E, Bujanover S, Kain KC, , , Clin Infect Dis, 2003
7. Malarone treatment failure not associated with previously described mutations in the cytochrome b gene, Wichmann O, Muehlen M, Gruss H, ''et al.'', , , Malaria J, 2004
★ Molecular Basis for Atovaquone Resistance in Pneumocystis jirovecii
★ Atovaquone (Meprone)
★ British National Formulary
Malarone anti-malaria tablets, as issued in the UK.
'Atovaquone' (alternative spelling: 'atavaquone') is a chemical compound that belongs to the class of naphthalenes. Atovaquone is a hydroxy-1,4-naphthoquinone, an analog of ubiquinone, with antipneumocystic activity. Its average wholesale price is about $2.13 per standard 250 mg. tablet.[1] It is also manufactured in the US in the liquid form, or oral suspension, under the brand name Mepron.[2]
Atovaquone is a medication used to treat or prevent:
# Pneumocystis pneumonia (PCP), although it is not approved for treatment of severe PCP.
# Toxoplasmosis. The medication has antiparasitic and therapeutic effects.
# Malaria. It is one of the two components (along with proguanil) in the drug Malarone. Malarone has fewer side effects than mefloquine, but can be more expensive because it's taken daily.[3]
Trimethoprim-sulfamethoxazole (TMP-SMX, Bactrim) is generally considered first line therapy for PCP or toxoplasmosis. However, atovaquone may be used in patients who cannot tolerate, or are allergic to, TMP-SMX. In addition, atovaquone has the advantage of not causing myelosuppression, which is an important issue in patients who have undergone bone marrow transplantation.
| Contents |
| Malaria |
| Treatment |
| Prevention |
| Resistance |
| References |
| External links |
Malaria
Atovaquone is only available as a fixed preparation with proguanil that has been commercially available from GlaxoSmithKline since 2000 as 'Malarone'® (sometimes abbreviated 'A+P'). It can be used both to treat and to prevent malaria.
A "standard" tablet of Malarone contains 100 mg of proguanil hydrochloride and 250 mg of atovaquone. A "pediatric" tablet of Malarone contains 25 mg of proguanil hydrochloride and 62.5 mg of atovaquone.
Treatment
The adult treatment dose is four "standard" tablets once a day for three days. In children, the drug is prescribed by body weight:
★ 11 to 20 kg: 1 "standard" tablet once daily for 3 days;
★ 21 to 30 kg: 2 "standard" tablets once daily for 3 days;
★ 31 to 40 kg: 3 "standard" tablets once daily for 3 days;
★ 41 kg and above: use adult dose.
Malarone is not licensed for use in children weighing 10 kg or less. The "pediatric" tablets are ''not'' used in malaria treatment.
The advice of a specialist should always be sought when starting malaria treatment. Malarone should not be used to treat severe malaria, when an injectable drug (quinine or artesunate in the UK; quinidine in the US) should be used instead.
Prevention
Medical advice should always be taken before choosing a drug for malaria prevention. Because some strains of malaria are resistant, Malarone is not effective for malaria prevention in all parts of the world. It must be taken with a fatty meal or at least some milk to be absorbed adequately.
The adult dose is one "standard" tablet daily starting one or two days before traveling into a malaria-endemic area, and continuing throughout the stay and then for another 7 days after returning from the malarious area.
The child dose is prescribed according to body weight:
★ 11–20 kg: 1 "pediatric" tablet once daily;
★ 21–30 kg: 2 "pediatric" tablets once daily;
★ 31–40 kg: 3 "pediatric" tablets once daily;
★ 41 kg and above use adult dose.
The duration of treatment is the same as for adults.
Resistance
Proguanil acts as a mitochondrial sensitiser and synergizes with atovaquone; also, there is a high natural frequency of cytochrome b mutants which leads to a high failure rate if atovaquone is used on its own to treat malaria. Specific mutations (Y268S, Y268C) have been shown to confer resistance ''in vivo,''[4][5][6] but there are other mechanisms of resistance that remain unknown.[7]
References
1. (ATN) Atovaquone (Mepron; 566C80) Approved for Pneumocystis; Drug Development, Activism Success
2. Mepron
3. Malarone: New Malaria Medication With Fewer Side-effects
4. Evidence of ''Plasmodium falciparum'' malaria resistant to atovaquone and proguoanil hydrochloride: case reports, Färnet A, Lindberg J, Gil P, ''et al.'', , , Brit Med J, 2003
5. Malarone treatment failure and in-vitro confirmation of resistance of ''Plasmodium falciparum'' isolate from Lagos, Nigeria, Fivelman QL, Butcher GA, Adagu IS, ''et al.'', , , Malaria J, 2002
6. Genetic confirmation of atovaquone-proguanil-resistant ''Plasmodium falciparum'' malaria acquired by a nonimmune traveller to east Africa, Schwartz E, Bujanover S, Kain KC, , , Clin Infect Dis, 2003
7. Malarone treatment failure not associated with previously described mutations in the cytochrome b gene, Wichmann O, Muehlen M, Gruss H, ''et al.'', , , Malaria J, 2004
External links
★ Molecular Basis for Atovaquone Resistance in Pneumocystis jirovecii
★ Atovaquone (Meprone)
★ British National Formulary
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