Atovaquone

Atovaquone Brand Name– Mepron

What is Atovaquone

Atovaquone is an oral antiprotozoal agent. It is active against both Toxoplasma gondii and Pneumocystis jiroveci (formerly Pneumocystis carinii).

Atovaquone is structurally and pharmacologically related to lapinone and parvaquone, which were used as antimalarials; in combination with proguanil, atovaquone is effective for malaria.

Atovaquone has been shown less effective than oral TMP-SMX and roughly equivalent to IV pentamidine in the treatment of Pneumocystis pneumonia (PCP) in patients with AIDS.

Both of these studies, however, found that atovaquone had fewer treatment-limiting adverse effects.

These studies were conducted with atovaquone tablets.

Atovaquone was originally approved by the FDA in November 1992 for use in the treatment of PCP in patients who do not tolerate TMP-SMX. An oral suspension with improved bioavailability relative to the tablets was later approved in February 1995, and the tablets were subsequently removed from the market.

In January 1999, the FDA approved use of atovaquone for the prevention of PCP in HIV-infected patients intolerant of TMP-SMX, after two clinical trials reported equivalence of atovaquone to dapsone or aerosolized pentamidine for this purpose.

Atovaquone remains designated as an orphan drug for the prophylaxis, treatment, and suppression of Toxoplasma gondii encephalitis.

Atovaquone has not been proven to decrease the risk of T. gondii encephalitis relapse, and thus is considered an alternative to standard therapy (e.g., pyrimethamine plus sulfadiazine or clindamycin).

Indications

  1. babesiosis
  2. Plasmodium falciparum
  3. Plasmodium sp.
  4. Pneumocystis jirovecii (formerly Pneumocystis carinii)
  5. Pneumocystis pneumonia (PCP)
  6. Pneumocystis pneumonia (PCP) prophylaxis
  7. Toxoplasma gondii
  8. toxoplasmic encephalitis
  9. toxoplasmosis
  10. toxoplasmosis prophylaxis

Side Effects

  1. abdominal pain
  2. anemia
  3. angioedema
  4. anorexia
  5. anxiety
  6. asthenia
  7. bronchospasm
  8. candidiasis
  9. constipation
  10. cough
  11. diarrhea
  12. dizziness
  13. dysgeusia
  14. dyspepsia
  15. dyspnea
  16. elevated hepatic enzymes
  17. erythema multiforme
  18. fever
  19. headache
  20. hepatic failure
  21. hepatitis
  22. hyperamylasemia
  23. hyperglycemia
  24. hyperhidrosis
  25. hypoglycemia
  26. hyponatremia
  27. hypotension
  28. infection
  29. influenza
  30. insomnia
  31. keratopathy
  32. maculopapular rash
  33. methemoglobinemia
  34. myalgia
  35. nausea
  36. neutropenia
  37. pancreatitis
  38. pruritus
  39. rash
  40. rhinitis
  41. sinusitis
  42. Stevens-Johnson syndrome
  43. thrombocytopenia
  44. urticaria
  45. vomiting

Monitoring Parameters

  • CBC
  • LFTs
  • serum amylase
  • serum sodium

Contraindications

  • benzyl alcohol hypersensitivity
  • breast-feeding
  • GI disease
  • hepatic disease
  • infection
  • neonates
  • pregnancy
  • respiratory insufficiency

Interactions

  • Abacavir; Lamivudine, 3TC; Zidovudine, ZDV
  • Atazanavir
  • Atazanavir; Cobicistat
  • Bismuth Subcitrate Potassium; Metronidazole; Tetracycline
  • Bismuth Subsalicylate; Metronidazole; Tetracycline
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Indinavir
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Lamivudine, 3TC; Zidovudine, ZDV
  • Lopinavir; Ritonavir
  • Metoclopramide
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole; Amoxicillin; Rifabutin
  • Penicillamine
  • Rabies Vaccine
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Ritonavir
  • Sulfamethoxazole; Trimethoprim, SMX-TMP, Cotrimoxazole
  • Tetracycline
  • Trimethoprim
  • Zidovudine, ZDV
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