Atovaquone and proguanil

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The fixed combination of atovaquone and proguanil is a drug that is used both for the prevention and treatment of acute, uncomplicated tropic malaria .

Proguanil is metabolized in the liver to the active cycloguanil, which inhibits the life cycle of Plasmodium falciparum by inhibiting the enzyme dihydrofolate reductase . Atovaquone slows down certain vital metabolic processes in the plasmodia.

Comparative studies show a significantly better tolerance for prophylactic use compared to mefloquine and chloroquine plus proguanil. Very common side effects include a. Stomach pain, headache, nausea, vomiting, and diarrhea. The medical research literature also reports on Stevens-Johnson syndrome and acute hepatitis after taking atovaquone / proguanil.

It is contraindicated in severe kidney disorders. There may be interactions with metoclopramide , tetracycline , rifampicin , rifabutin , warfarin and etoposide .

The prophylactic use of atovaquone / proguanil was limited to a period of 28 days until 2012. This restriction on use was lifted in August 2012. Since then, the duration of taking Atovaquon / Proguanil (Malarone) for malaria prophylaxis has not been limited in time.

Malaria prophylaxis and therapy must also be carried out during pregnancy and be based on the resistance situation. As there is only limited experience with the safety of using atovaquone during pregnancy, the combination atovaquone / proguanil is a reserve drug if other therapies cannot be used.

Finished preparations

Malarone ( GlaxoSmithKline ), various generics.

The combination preparation is available in two strengths:

  • 250 mg atoquavone / 100 mg proguanil hydrochloride for the treatment of patients weighing 11 kg or more and for prophylaxis for patients weighing 40 kg or more
  • 62.5 mg atoquavone / 25 mg proguanil hydrochloride for the treatment of patients with a body weight of 5 to 11 kg and for prophylaxis for patients from 11 to 40 kg

The drugs are subject to a medical prescription within the EU , Switzerland , the Principality of Liechtenstein and Norway .

Individual evidence

  1. ↑ P. Schlagenhauf, A. Tschopp, R. Johnson, HD Nothdurft, B. Beck, E. Schwartz, M. Herold, B. Krebs, O. Veit, R. Allwinn, R. Steffen: Tolerability of malaria chemoprophylaxis in non -immune travelers to sub-Saharan Africa: multicentre, randomized, double blind, four arm study. In: BMJ . 327 (7423), Nov. 8, 2003, p. 1078. PMID 14604928 .
  2. ↑ B. Hogh, PD Clarke, D. Camus, HD Nothdurft, D. Overbosch, M. Gunther, I. Joubert, KC Kain, D. Shaw, NS Roskell, JD Chulay: Atovaquone-proguanil versus chloroquine-proguanil for malaria prophylaxis in non-immune travelers: a randomized, double-blind study . Malarone International Study Team. In: The Lancet . 356 (9245), Dec 2, 2000, pp. 1888-1894. PMID 11130385 .
  3. ↑ D. Overbosch, H. Schilthuis, U. Bienzle, RH Behrens, KC Kain, PD Clarke, S. Toovey, J. Knobloch, HD Nothdurft, D. Shaw, NS Roskell, JD Chulay: Atovaquone-proguanil versus mefloquine for malaria prophylaxis in nonimmune travelers: results from a randomized, double-blind study. ( Memento of the original from October 16, 2013 in the Internet Archive ) Info: The archive link was inserted automatically and has not yet been checked. Please check the original and archive link according to the instructions and then remove this notice. (PDF file; 1.1 MB). In: Clin Infect Dis . 33 (7), October 1, 2001, pp. 1015-1021. @1@ 2Template: Webachiv / IABot / www.lariaminfo.org
  4. ↑ MM van Riemsdijk, MC Sturkenboom, JM Ditters, RJ Ligthelm, D. Overbosch, BH Stricker: Atovaquone plus chloroguanide versus mefloquine for malaria prophylaxis: a focus on neuropsychiatric adverse events. In: Clin Pharmacol Ther . 72 (3), Sep 2002, pp. 294-301. PMID 12235450 .
  5. ↑ D. Camus, F. Djossou, HJ Schilthuis, B. Hogh, E. Dutoit, D. Malvy, NS Roskell, C. Hedgley, EH De Boever, GB Miller: Atovaquone-Proguanil versus Chloroquine-Proguanil for Malaria Prophylaxis in Nonimmune Pediatric Travelers: Results of an International, Randomized. Open-Label Study , International Malarone Study Team. In: Clin Infect Dis. 38 (12), Jun 15, 2004, pp. 1716-1723.
  6. ↑ H. Nakato, R. Vivancos, PR Hunter: A systematic review and meta-analysis of the effectiveness and safety of atovaquone proguanil (Malarone) for chemoprophylaxis against malaria. In: J Antimicrob Chemother . September 10, 2007. PMID 17848375 .
  7. ↑ FA Jacquerioz, AM Croft: Drugs for preventing malaria in travelers. In: Cochrane Database Syst Rev. (4), Oct 7, 2009, Art. No. CD006491. PMID 19821371 .
  8. ↑ a b c Package insert Malarone film-coated tablets , GlaxoSmithKline, Munich. As of June 2017.
  9. ↑ M. Emberger, AM Lechner, B. Zelger: Stevens-Johnson syndrome associated with Malarone antimalarial prophylaxis. In: Clin Infect Dis. 37 (1), Jul 1, 2003, pp. E5 – e7. PMID 12830430 .
  10. ↑ M. Grieshaber, J. Lammli, L. Marcus: Acute hepatitis and atovaquone / proguanil. In: J Travel Med. 12 (5), Sep-Oct 2005, pp. 289-290. PMID 16256055 .
  11. ↑ db: Malaria: Malarone now also for long-term prophylaxis. In: Pharmaceutical newspaper . October 9, 2012.
  12. ↑ Atovaquon , www.embryotox.de, accessed on July 16, 2020.
  13. ↑ Package insert Malarone Junior film-coated tablets , GlaxoSmithKline, Munich. As of June 2017.