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Atovaquone

 

 
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Atovaquone
 
 
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Atovaquone (alternative spelling: atavaquone) is a chemical compound that belongs to the class of naphthaleneNaphthalene

Naphthalene is a crystalline, aromatic, white, solid hydrocarbon, best known as the primary ingredient of mothballs....
s. Atovaquone is a hydroxy-1,4-naphthoquinone, an analog of ubiquinone, with antipneumocystic activity. Its average wholesale priceAverage Wholesale Price

The average wholesale price is a prescription drugs term referring to the average price at which wholesalers sell drugs to ...
 is about $2.13 per standard 250 mg. tablet. It is also manufactured in the US in the liquid form, or oral suspension, under the brand name Mepron.

Atovaquone is a medication used to treat or prevent:
  1. Pneumocystis pneumoniaPneumocystis pneumonia

    Pneumocystis pneumonia is a form of pneumonia caused by the yeast-like fungus, Pneumocystis jirovecii ....
     (PCP), although it is not approved for treatment of severe PCP.
  2. ToxoplasmosisToxoplasmosis

    Toxoplasmosis is a parasitic disease caused by the protozoan Toxoplasma gondii....
    . The medication has antiparasitic and therapeutic effects.
  3. MalariaMalaria

    Malaria is an infectious disease that is widespread in many tropical and subtropical regions....
    . It is one of the two components (along with proguanilProguanil

    Proguanil is a prophylactic antimalarial drug, which works by stopping the malaria parasite, Plasmodium falciparum, from...
    ) in the drug Malarone. Malarone has fewer side effects than mefloquineMefloquine

    Mefloquine is an orally administered antimalarial drug used as a prophylaxis against and treatment for malaria....
    , but can be more expensive because it's taken daily.


Trimethoprim-sulfamethoxazoleCo-trimoxazole

Co-trimoxazole is an antibiotic combination of trimethoprim and sulfamethoxazole, in the ratio of 1 to 5, used in the treatm...
 (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.

Malaria

Atovaquone is only available as a fixed preparation with proguanilProguanil

Proguanil is a prophylactic antimalarial drug, which works by stopping the malaria parasite, Plasmodium falciparum, from...
 that has been commercially available from GlaxoSmithKlineGlaxoSmithKline Summary

GlaxoSmithKline plc is a British based pharmaceutical, biologicals, and healthcare company....
 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 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 mitochondrialMitochondrion

In cell biology, a mitochondrion is an organelle, variants of which are found in most eukaryotic cells....
 sensitiser and synergizes with atovaquone; also, there is a high natural frequency of cytochrome BFacts About Cytochrome b

Cytochrome b/b6 is main subunit of transmembrane cytochrome bc1 and b6f complexes....
 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, but there are other mechanisms of resistance that remain unknown.

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