Atovaquone Proguanil

Atovaquone Proguanil Brand Names- Malarone | Malarone Pediatric

What is Atovaquone Proguanil

Atovaquone proguanil is an oral antimalarial combination. Plasmodium falciparum exhibits a high incidence of resistance to both atovaquone and proguanil as single agents for the treatment of malaria.

The combination, however, has potent synergistic antimalarial activity.

Atovaquone is structurally and pharmacologically related to older antimalarials, lapinone and parvaquone.

Proguanil is a synthetic biguanide derivative of pyrimidine and is actually a prodrug for the active drug cycloguanil.

In certain populations which are poor metabolizers (e.g., Asian and African populations), the conversion of proguanil to cycloguanil is inadequate and therapeutic concentrations of the active compound are not achieved.

Malarone was approved by FDA July 14, 2000 for the prevention and treatment of malaria.

Indications

  • malaria
  • malaria prophylaxis
  • Plasmodium falciparum
  • Plasmodium sp.

Side Effects

  1. abdominal pain
  2. anaphylactoid reactions
  3. anemia
  4. angioedema
  5. anorexia
  6. anxiety
  7. asthenia
  8. back pain
  9. cholestasis
  10. cough
  11. depression
  12. diarrhea
  13. dizziness
  14. dyspepsia
  15. elevated hepatic enzymes
  16. erythema multiforme
  17. fever
  18. gastritis
  19. hallucinations
  20. headache
  21. hepatic failure
  22. hepatitis
  23. infection
  24. influenza
  25. insomnia
  26. myalgia
  27. nausea
  28. neutropenia
  29. oral ulceration
  30. pancytopenia
  31. photosensitivity
  32. pruritus
  33. rash
  34. seizures
  35. Stevens-Johnson syndrome
  36. stomatitis
  37. urticaria
  38. vasculitis
  39. vomiting

Monitoring Parameters

  • CBC
  • LFTs
  • serum amylase
  • serum creatinine/BUN
  • serum sodium

Contraindications

  • Asian patients
  • Black patients
  • breast-feeding
  • children
  • diarrhea
  • driving or operating machinery
  • geriatric
  • GI disease
  • hepatic disease
  • infants
  • pregnancy
  • pulmonary edema
  • renal failure
  • renal impairment
  • sunlight (UV) exposure
  • vomiting

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
  • Esomeprazole
  • Esomeprazole; Naproxen
  • Fedratinib
  • Indinavir
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Lamivudine, 3TC; Zidovudine, ZDV
  • Lopinavir; Ritonavir
  • Luliconazole
  • Metoclopramide
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole; Amoxicillin; Rifabutin
  • Oritavancin
  • Penicillamine
  • Phentermine; Topiramate
  • Rabies Vaccine
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Ritonavir
  • Sulfamethoxazole; Trimethoprim, SMX-TMP, Cotrimoxazole
  • Tetracycline
  • Topiramate
  • Trimethoprim
  • Typhoid Vaccine
  • Voriconazole
  • Warfarin
  • Zidovudine, ZDV