Atovaquone-proguanil: Difference between revisions
imported>Howard C. Berkowitz (New page: '''Atovaquone-proguanil''', made by Smith Kline Glaxo and approved by the U.S. Food and Drug Administration in 2000, is a fixed-combination antimalarial drug for [[chemoprophyl...) |
imported>Howard C. Berkowitz |
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'''Atovaquone-proguanil''', made by [[Smith Kline Glaxo]] and approved by the U.S. [[Food and Drug Administration]] in 2000, is a fixed-combination [[antimalarial]] drug for [[chemoprophylaxis]] and treatment. | {{subpages}} | ||
'''Atovaquone-proguanil''', made by [[Smith Kline Glaxo]] and approved by the U.S. [[Food and Drug Administration]] in 2000, is a fixed-combination [[antimalarial]] drug for [[chemoprophylaxis]] and treatment. It is labeled for treatment and prevention of ''[[Plasmodium falciparum]]'', especially [[chloroquine]]-resistant. Off-label uses include prevention of ''[[Plasmodium vivax]]'' and treatment of [[babesiosis]]. | |||
==Mechanism of action== | ==Mechanism of action== | ||
The two components block with two different pathways involved in the biosynthesis of [[pyrimidine]]s required for nucleic acid replication. Atovaquone is a selective inhibitor of parasite mitochondrial electron transport. Proguanil hydrochloride primarily exerts its effect by means of the metabolite cycloguanil, a [[ | The two components block with two different pathways involved in the biosynthesis of [[pyrimidine]]s required for nucleic acid replication. Atovaquone is a selective inhibitor of parasite mitochondrial electron transport. Proguanil hydrochloride primarily exerts its effect by means of the metabolite cycloguanil, a [[tetrahydrofolate dehydrogenase]] inhibitor]]. Inhibition of tetrahydrofolate dehydrogenase in ''Plasmodium sp.'' disrupts deoxythymidylate synthesis.<ref>{{citation | ||
| url = http://www.centerwatch.com/drug-information/fda-approvals/drug-details.aspx?DrugID=634 | | url = http://www.centerwatch.com/drug-information/fda-approvals/drug-details.aspx?DrugID=634 | ||
| title = Drug Name: Malarone (atovaquone; proguanil hydrochloride) Tablet | | title = Drug Name: Malarone (atovaquone; proguanil hydrochloride) Tablet | ||
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==Drug-drug interactions== | ==Drug-drug interactions== | ||
There are adverse interactions with [[tetracycline]], [[metoclopramide]] and [[rifampin]]. | There are adverse interactions with [[tetracycline]], [[metoclopramide]] and [[rifampin]]. | ||
Antimalarial agents, in general, have ans adverse reaction with [[penicillinamine]]. They increase the effect of lumefantrine in the [[artemether-lumefantrine]] combination. | |||
==References== | ==References== | ||
{{reflist}} | {{reflist}} | ||
Latest revision as of 14:29, 27 May 2010
Atovaquone-proguanil, made by Smith Kline Glaxo and approved by the U.S. Food and Drug Administration in 2000, is a fixed-combination antimalarial drug for chemoprophylaxis and treatment. It is labeled for treatment and prevention of Plasmodium falciparum, especially chloroquine-resistant. Off-label uses include prevention of Plasmodium vivax and treatment of babesiosis.
Mechanism of action
The two components block with two different pathways involved in the biosynthesis of pyrimidines required for nucleic acid replication. Atovaquone is a selective inhibitor of parasite mitochondrial electron transport. Proguanil hydrochloride primarily exerts its effect by means of the metabolite cycloguanil, a tetrahydrofolate dehydrogenase inhibitor]]. Inhibition of tetrahydrofolate dehydrogenase in Plasmodium sp. disrupts deoxythymidylate synthesis.[1]
Drug-drug interactions
There are adverse interactions with tetracycline, metoclopramide and rifampin.
Antimalarial agents, in general, have ans adverse reaction with penicillinamine. They increase the effect of lumefantrine in the artemether-lumefantrine combination.