antiparasitics Flashcards

1
Q

metronidazole- MOA

A

•Pro-drug targets enzyme unique to the parasite. Active form is free radical that damages DNA and causes oxidative stress that kills parasite.

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2
Q

metronidazole uses

A

GET GAP: giardia, entamoeba, trichomonas, gardnerella vaginalis, anaerobes (bacteroides, C. diff), H. Pylori. It doesn’t reach lumen so better for systemic dz. Can use with lumenal amebicide (paromomycin/ diloxanide) for amebiasis.

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3
Q

Metronidazole adverse rxns/ contraindications

A

disulfiram like rxn with alcohol (flushing, tachycardia, hypotension), headache, metallic taste. Contraindicated in hepatic dz, renal dz, CNS abnormalities

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4
Q

Paromomycin- MOA, uses

A

aminoglycoside Abx (inhibits 30S).Concentrates in parasite in the gut. Little systemic absorption. Uses: asymptomatic lumenal amebiasis, cryptosporidiosis (AIDS), visceral and cutaneous Leishmanias.

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5
Q

Toxoplasmosis treatment

A

Pyrimethamine + sulfadiazine (or clindamycin if sulfa allergy). Pyrimethamine targets dihydrofolate reductase and sulfadiazine targets dihydropteroic synthase, blocking folic acid synthesis and thus nucleic acid and protein synthesis

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6
Q

Pneumocystis jirovecii treatment

A

TMP-SMX

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7
Q

Pentamide MOA

A

disrupts DNA structure/ function (inhibits SAM decarboxylase), inhibits protein synthesis (binds minor groove of DNA), inhibits DNA replication (type II topoisomerase)

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8
Q

Pentamide uses

A

PCP pneumonia alternative to TMP-SMX, West African Trypanosomiasis (T. brucei gambiense), Visceral Leishmanias

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9
Q

Pentamide adverse rxns

A

histamine release (dying orgnaisms), drop in BP, hypoglycemia, elevates LFTS, impaired renal function. Few side effects when inhaled for PCP

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10
Q

Benzimidazoles MOA

A

inhibit microtubule formation - selectively binds to parasite tubulin.

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11
Q

Benzimidazoles uses

A

Mebendazole: nematodes - enterobiasis (pinworm), ascariasis, trichuriasis (whipworm), hookworm. Albendazole: nematodes- ascariasis, enterobiasis, hookworm. Invasive cestodes- cystic hydatid dz, cysticercosis (pork tapeworm).

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12
Q

mebendazole vs albendazole

A

mebendazole: poor absorption, excreted in bile, uncomplicated nematode infections. Albendazole better absorption, excreted in urine, cysticercosis, used in kids >4yrs. Both are teratogens

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13
Q

Pyrantel Pamoate MOA

A

concentrates in parasite- Ach receptor agonists cuases complete spastic paralysis of worm.

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14
Q

Pyrantel Pamoate uses

A

ascariasis (roundworm), enterobiasis (pinworm) DOC, hookworms

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15
Q

Pyrantel Pamoate contraindications

A

liver dysfunction.

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16
Q

Praziquantel MOA

A

Ca2+ ionophore - induces paralysis, detachment, excretion. Induces tegmental damage - activates immune system

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17
Q

Praziquantel uses

A

Cestodes (tapeworms), and trematodes (flukes) EXCEPT: pork tapeworm cysticercosis, cystic hydatid dz, and sheep liver fluke

18
Q

Praziquantel adverse rxns

A

If neurocysercicosis is present: meningismus, seizures, CSF pleocytosis

19
Q

treatment of Leishmanias

A

sodium stibogluconate

20
Q

treatment of African trypanosomiasis

A

Hemolymphatic stage: suramin, pentamidine. Late stage with CNS involvement: melasporol, eflornithine (west)

21
Q

Chloroquine MOA

A

Concentrates in food vacuoles. Inhibits heme polymerization, causing heme accumulation which is toxic to plasmodium. Inhibits peroxidase and catalase activity, generates oxidative stress.

22
Q

Chloroquine uses

A

Plasmodium vivax, ovale and malariae. P. falciparum is mostly resistant.

23
Q

Chloroquine adverse rxns

A

retinopathy, pruritis. Also hypotension, cardiac arrest, confusion, coma with IV. May cause hemolysis in G6PD deficiency.

24
Q

Quinine MOA

A

inhibits parasite feeding mechanism, generates oxidative stress

25
Q

Quinine uses

A

treat/ cure of erythrocytic stages of
chloroquine resistant and MDR P. falciparum malaria treat/ cure of erythrocytic stages of
chloroquine resistant and MDR P. falciparum malaria

26
Q

multi drug resistant malaria treatment

A

quinine plus Pryimethamine-sulfadoxine, TMP-SMX, clindamycin, doxycycline or tetracycline

27
Q

Quinine adverse rxns

A

Cinchonism- visual defects, auditory defects (tinnitus, deafness), GI (nausea, vomiting). Stimulates pancreatic beta cells (hyperinsulinemia), hypotension, hemolysis in G6PD deficiency.

28
Q

quinine drug interactions

A

may raise plasma levels of anti-coagulants (warfarin) and cardiac glycosides (digitoxin)

29
Q

Mefloquine MOA

A

generates oxidative stress

30
Q

Mefloquine MOA

A

Alternative for treatment of erythrocytic
stages of chloroquine resistant and
MDR P. falciparum. BUT…it is a court martial offence to prescribe nowAlternative for treatment of erythrocytic
stages of chloroquine resistant and
MDR P. falciparum. BUT…it is a court martial offence to prescribe now

31
Q

Mefloquine adverse rxns

A

CNS toxicity inn 50% (ataxia, visual/auditory disturbances), neuropsychiatric disturbances

32
Q

Malarone components

A

Proguanil with Atovaquone

33
Q

Malarone uses

A

Malaria caused by P. falciparum (safe for children), PCP (alternative to TMP-SMX), Toxoplasma gondii

34
Q

malarone adverse rxns

A

rash. Interacts with rifampin

35
Q

Malarone MOA

A

•DHFR Inhibitor. Increases efficacy of Atovaquone to collapse proton gradient

36
Q

Primaquine MOA and uses

A

MOA unknown. Latent forms of P. vivax and P. ovale. Only drug active against latent hepatic forms

37
Q

primaquine adverse rxns

A

hemolytic anemia in G6PD deficiency

38
Q

Artemisinin

A

Component of Chinese herbal remedies. Used in conjunction with lumefantrine (chloroquine analogue), sulfadoxine-pryimethamine for MDR P. falciparum. Generates ROS by interacting with heme.

39
Q

list drugs used for sensitive P. falciparum, P. vivax, P. malaria and P. Ovale

A

Chloroquine plus primaquine (for vivax and ovale)

40
Q

List drugs used for treatment of MDR P. falciparum and P. vivax

A

mefloquine prophylaxis (use doxycyclie now). Mefloquine plus primaquine OR artemisinin plus lumefantrine OR quinidine. Plus tetracyline OR pyrimethamine-sulfadoxine OR clindamycin