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Pharmacology > 31 Antiprotozoal drugs > Flashcards

31 Antiprotozoal drugs Flashcards

1
Q

31.01 BLOOD SCHIZONTICIDES - MALARIA

Chloroquine, quinine, mefloquine, amodiaquine - actions

A

schizonticidal drugs kill malarial parasites in red blood cells

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2
Q

31.01 BLOOD SCHIZONTICIDES - MALARIA

Chloroquine, quinine, mefloquine, amodiaquine - MOA

A

inhibit haem polymerase which would normally degrade haem
the toxic haem molecules accumulate and kill the parasite

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3
Q

31.01 BLOOD SCHIZONTICIDES - MALARIA

Chloroquine, quinine, mefloquine, amodiaquine - abs/distrib/elim

A

given orally (IV quinine is used for severe falciparum malaria)
concentrates in parasitised erythrocytes

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4
Q

31.01 BLOOD SCHIZONTICIDES - MALARIA

Chloroquine, quinine, mefloquine, amodiaquine - clinical use

A

for acute attacks of malaria depending on local resistance patterns
chloroquine and mefloquine can be used for chemoprophylaxis of malaria in specific areas
chloroquine is also used in autoimmune conditions such as lupus erythematosus

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5
Q

31.01 BLOOD SCHIZONTICIDES - MALARIA

Chloroquine, quinine, mefloquine, amodiaquine - adverse effects

A

few when used for chemoprophylaxis
the larger doses used to treat the acute attack can cause GIT disturbances, dizziness and hearing abnormalities
arrhythmias and hypotension at high doses

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6
Q

31.01 BLOOD SCHIZONTICIDES - MALARIA

Chloroquine, quinine, mefloquine, amodiaquine - special points

A

for falciparum malaria, quinine is given together with antibiotics such as doxycycline or clindamycin or pyrimethamine/sulfadoxine

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7
Q

31.02 TISSUE SCHIZONTICIDE - MALARIA

Primaquine - actions

A

kills hypnozoites in the liver
kills gametocytes

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8
Q

31.02 TISSUE SCHIZONTICIDE - MALARIA

Primaquine - MOA

A

not really known

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9
Q

31.02 TISSUE SCHIZONTICIDE - MALARIA

Primaquine - abs/distrib/elim

A

given orally, rapidly metabolised
half-life 3-6h

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10
Q

31.02 TISSUE SCHIZONTICIDE - MALARIA

Primaquine - clinical use

A

for radical cure of Plasmodium vivax and P. ovale by eliminating the exo-erythrocytic stage
given as adjunct to chloroquine treatment of the acute attack

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11
Q

31.02 TISSUE SCHIZONTICIDE - MALARIA

Primaquine - adverse effects

A

dose-related GIT disturbances and methaemoglobinaemia
causes haemolytic anaemia in patients with genetic glucose 6-phosphate dehydrogenase deficiency (G6PD)

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12
Q

31.03 FOLATE INHIBITORS - MALARIA

Proguanil, pyrimethamine - actions

A

folate inhibition
these are slow blood schizonticides that have a greater affinity for the parasite’s enzymes than the equivalent human cellular enzymes

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13
Q

31.03 FOLATE INHIBITORS - MALARIA

Proguanil, pyrimethamine - MOA

A

inhibit the malaria parasite’s dihydrofolate reductase (DHFR) and thus interfere with its thymidylate synthesis
pyrimethamine is used in a combination tablet with sulfadoxine which inhibits dihydropteroate synthetase - an earlier step in thymidylate synthesis
proguanil is often given in combination with atovaquone which inhibits the parasite’s mitochondrial electron transport

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14
Q

31.03 FOLATE INHIBITORS - MALARIA

Proguanil, pyrimethamine - abs/distrib/elim

A

given orally, usually in combination tablet formulation

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15
Q

31.03 FOLATE INHIBITORS - MALARIA

Proguanil, pyrimethamine - clinical use

A

proguanil + atovaquone or chloroquine is used for chemoprophylaxis of malaria
pyrimethamine/sulfadoxine (with quinine) or proguanil + atovaquone can be used for treatment of acute uncomplicated falciparum malaria in some regions
toxoplasmosis can be treated with pyrimethamine/sulfadoxine

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16
Q

31.03 FOLATE INHIBITORS - MALARIA

Proguanil, pyrimethamine - adverse effects

A

GIT disturbances, rash, marrow suppression (with pyrimethamine)

17
Q

31.04 ARTEMISININ DERIVATIVES - MALARIA

Artemether, artesunate, artemisinin - actions

A

a blood schizonticide combination

18
Q

31.04 ARTEMISININ DERIVATIVES - MALARIA

Artemether, artesunate, artemisinin - MOA

A

artemisinin compounds become concentrated in parasitised red cells and give rise to highly reactive compounds that damage parasite proteins and membranes
artemether is usually combined with lumefantrine which prevents parasite detoxification of haem

19
Q

31.04 ARTEMISININ DERIVATIVES - MALARIA

Artemether, artesunate, artemisinin - abs/distrib/elim

A

artesunate is a water-soluble version that can be IV, whereas artemether and artemisinin are given orally or IM
they are metabolised in the liver to the active compound dihydroartemisinin

20
Q

31.04 ARTEMISININ DERIVATIVES - MALARIA

Artemether, artesunate, artemisinin - clinical use

A

fast-acting blood schizonticidal action against falciparum and non-falciparum malaria

21
Q

31.04 ARTEMISININ DERIVATIVES - MALARIA

Artemether, artesunate, artemisinin - adverse effects

A

transient heart block, fever, decreased neutrophil count

22
Q

31.05 TREATMENT OF AMOEBIASIS

Amoebicides: metronidazole, tinidazole, diloxanide - actions

A

metronidazole and tinidazole are active against the invasive motile forms of Entamoeba histolytica in the gut and liver
diloxanide acts against the non-invasive cysts in the gut lumen

23
Q

31.05 TREATMENT OF AMOEBIASIS

Amoebicides: metronidazole, tinidazole, diloxanide - MOA

A

metronidazole and tinidazole are activated by anaerobic organisms to form free radicals that damage the DNA
the mechanism of diloxanide is not known but thought to affect protein synthesis

24
Q

31.05 TREATMENT OF AMOEBIASIS

Amoebicides: metronidazole, tinidazole, diloxanide - abs/distrib/elim

A

given orally, can be given IV and rectally
tinidazole has longer action
diloxanide is given orally

25
Q

31.05 TREATMENT OF AMOEBIASIS

Amoebicides: metronidazole, tinidazole, diloxanide - clinical use

A

metronidazole and tinidazole are used for amoebic liver abscess and amoebic dysentery (followed by eradication of cysts using diloxanide), trichomoniasis and giardiasis

26
Q

31.05 TREATMENT OF AMOEBIASIS

Amoebicides: metronidazole, tinidazole, diloxanide - adverse effects

A

GIT disturbances, anorexia, dizziness
metronidazole and tinidazole can cause disulfiram reactions after alcohol

27
Q

31.06 OTHER ANTIPROTOZOAL DRUGS

Suramin for human African trypanosomiasis

A

given by slow IV injection
inhibits key parasite enzymes, leading to gradual destruction of organelles
wide range of serious adverse effects in humans, including renal failure, agranulocytosis and shock

28
Q

31.06 OTHER ANTIPROTOZOAL DRUGS

Pentamidine for trypanosomiasis, pneumocystis pneumonia, leishmaniasis

A

given by IV or deep IM injection with direct trypanocidal action
inhaled pentamidine for prophylaxis of pneumocystis pneumonia
hypotension, cardiac arrhythmias, dyspnoea, renal failure and hypoglycaemia are serious toxicities

29
Q

31.06 OTHER ANTIPROTOZOAL DRUGS

Sodium stibogluconate for leishmaniasis

A

given by slow IV or IM injection
increased production of free oxygen radicals may lead to killing of parasite

Pharmacology (34 decks)

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