Dihydroartemisinin

Products No drugs containing dihydroartemisinin are currently approved in many countries. However, the prodrug artemether (Riamet, with lumefantrine), which is metabolized in the body to dihydroartemisinin, is available. It is also combined fixed with piperaquine; see Piperaquine and Dihydroartemisinin. Structure and properties Dihydroartemisinin (C15H24O5, Mr = 284.3 g/mol) is derived from artemisinin from annual mugwort … Dihydroartemisinin

Halofantrine

Products Halofantrine was approved in 1988 and is now no longer available as a finished drug in many countries and many more. Halfan tablets (GlaxoSmithKline AG, 250 mg) are off the market. Structure and properties Halofantrine (C26H30Cl2F3NO, Mr = 500.4 g/mol) is a racemate and a halogenated phenanthrene derivative. It is also known as phenanthrene … Halofantrine

Mefloquine

Products Mefloquine is commercially available in the form of film-coated tablets (generic: mephaquine). The active ingredient was approved in many countries in 1984. Distribution of the original Lariam (Roche) was discontinued in 2014 for commercial reasons. Structure and properties Mefloquine (C17H16F6N2O, Mr = 378.3 g/mol) is a fluorinated quinoline and piperidine derivative and an analog … Mefloquine

Proguanil

Products Proguanil is commercially available in the form of film-coated tablets and exclusively as a fixed combination with atovaquone (Malarone, generic). It has been approved in many countries since 1997. Generics went on sale in 2013. Structure and properties Proguanil (C11H16ClN5, Mr = 253.7 g/mol) is an active ingredient of the biguanide group. It exists … Proguanil

Primaquine

Products No medicines containing primaquine are currently registered in many countries. Structure and properties Primaquine (C15H21N3O, Mr = 259.3 g/mol) is an 8-aminoquinoline derivative and a racetate. It is present in drugs as primaquine bishydrogen phosphate, an orange crystalline powder that is soluble in water. Primaquine is derived from plasmoquine. It was developed in the … Primaquine

Chloroquine

Products Chloroquine was commercially available in tablet form (Nivaquine). It was approved in many countries since 1953. Its distribution was discontinued in 2019. It was first synthesized in 1934 by Hans Andersag at Bayer in Elberfeld (I.G. Farbenindustrie). Currently, medicines containing chloroquine are no longer available in many countries. Magisterial formulations can be made in … Chloroquine

Mepacrine

Products Mepacrine is no longer commercially available in many countries. At best, mepacrine capsules could be prepared as a magisterial formulation in a well-equipped pharmacy. Alternatively, other antimalarials such as chloroquine or quinine could be used. Structure and properties Mepacrine (C23H30ClN3O, Mr = 399.96 g/mol) is a pale yellow crystalline powder that is soluble in … Mepacrine

Lumefantrine

Products Lumefantrine is commercially available in tablet form as a fixed combination with artemether (Riamet). It has been approved in many countries since 1999. Structure and properties Lumefantrine (C30H32Cl3NO, Mr = 528.9 g/mol) is a racemate. It exists as a yellow crystalline powder that is insoluble in water. Effects Lumefantrine (ATC P01BF01) has antiparasitic properties. … Lumefantrine

Antimalarials

Effects Antiparasitic against plasmodia. Indications Malaria Malaria prophylaxis Also for the treatment of rheumatic diseases, lupus erythematosus. Off-label: some antimalarials such as quinine and chloroquine are used off-label to treat calf cramps. Active ingredients Aminoquinolines: Amodiaquine Chloroquine (Nivaquine, out of commerce). Hydroxychloroquine (Plaquenil) Mepacrine Pamaquin Piperaquine Primaquine Tafenoquin (crinoline) Biguanides: Proguanil (Malarone + Atovaquone). Cycloguanilembonate … Antimalarials