Antiparasitic drugs (Most important) Flashcards

1
Q

Metronidazole - Classification

A

Nitromidazole compound, tissue amebicide

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2
Q

Metronidazole - MoA

A

It inhibits nucleic acid synthesis by disrupting the DNA of microbial cells.

Inhibit pyruvate-ferredoxin oxidoreductase (PFOR)

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3
Q

Metronidazole - Clinical use

A

Entamoeba histolytica
Giardia intestinalis (Giardia lamblia)
Trichonomas vaginalis

Anaerobic bacteria:
Bacteroides fragilis
Helicobacter pylori
Clostridium difficle

Amebiasis
Giardiasis
Trichonomiasis

Dracunculiasis by Dracunulus medinensis (Guinea worm infection)
Enterocolitis
Rosacea (acne rosacea)

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4
Q

Metronidazole - Contraindications

A

Contraindicated during first trimester of pregnancy

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5
Q

Metronidazole - Adverse effects

A

Metallic taste
Transient leukopenia
Thrombocytopenia

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6
Q

Metronidazole - Interactions

A

Increased effect of warfarin.

Ethanol: disulfiram-like reaction

Serum levels affected by drugs inhibiting/inducing CYP3A4.

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7
Q

Drugs for malaria

A
Quinine
Chloroquine 
Mefloquinine 
Primaquine 
Artesunate
Artemether 
Atovaquone
Proguanil 
Pyrimethamine
Sulfadoxine
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8
Q

Quinine, Chloroquine, Mefloquinine - MoA

A

Inhibits nucleic acid synthesis/function during erythrocytic schizogony

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9
Q

Quinine - Clinical use

A

Alternative to artesunate for severe malaria

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10
Q

Chloroquine - Clinical use

A

P. falciparum, prevention and treatment

Combination with primaquine to eradicate P. vivax

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11
Q

Chloroquine - Contraindications

A

Should be used cautiously in pregnant women because fetal damage has been reported

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12
Q

Chloroquine - Adverse effects

A

Toxic overdose: Retinal damage and blindness

Exacerbation of psoriasis and pruritus

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13
Q

Mefloquinine - Clinical use

A

Prophylaxis and treatment of falciparum malaria, where it is known to be effective

Combination with artesunate is a first-line therapy in parts of Southeast Asia and South America

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14
Q

Mefloquinine - Adverse effects

A

Severe neuropsychiatric syndrome characterized by hallucinations, anxiety, confusion, seizures and coma

Leukopenia
Thrombocytopenia
Bradycardia and arrythmias

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15
Q

Primaquine - Classification

A

Aminoquinoline derivative

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16
Q

Primaquine - MoA

A

Form quinones that oxidize and destroy schizont membranes

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17
Q

Primaquine - Clinical use

A

P. vivax and P. ovale in combination with chloroquine or other drugs

18
Q

Primaquine - Contraindications

A

G6PD deficiency

19
Q

Primaquine - Adverse effects

A

Hemolytic anemia in G6PD deficiency

20
Q

Artesunate, Artemether - MoA

A

Form free radicals that attack heme and proteins in malarial parasites and inhibit erythocytic schizogony

21
Q

Artesunate - Clinical use

A

IV is 1st line for severe falciparum malaria (children + adults)
P. vivax

22
Q

Artemether - Clinical use

A

P. falciparum malaria

P. vivax

23
Q

Atovaquone - MoA

A

Inh synthesis of pyrimidines and nucleic acid synthesis by selective inhibition of mitochondria electron transport in plasmodia

24
Q

Atovaquone - Clinical use

A

Prophylaxis and treatment of Chloroquine-resistant falciparum malaria in combination with proguanil or doxycycline

Alone: pneumocystitis jiroveci infections

25
Proguanil - MoA
Inh synthesis of pyrimidines and nucleic acid synthesis by inhibiting folate reductase
26
Proguanil - Clinical use
Prophylaxis and treatment of Chloroquine-resistant falciparum malaria in combination with atovaquone
27
Pyrimethamine, Sulfadoxine - MoA
Inhibit folic acid synthesis
28
Pyrimethamine, Sulfadoxine - Clinical use
Malaria | Toxoplasmosis (with sulfadiazine)
29
Pyrimethamine, Sulfadoxine - Adverse effects
Skin rashes | Megaloblastic anemia and other hematologic reactions
30
Drugs for toxoplasmosis
Pyrimethamine + sulfadiazine | Spiramycin
31
Pyrimethamine + sulfadiazine - Clinical use
Toxoplasmosis in AIDS
32
Spiramycin - Classification
Macrolide
33
Spiramycin - Clinical use
Fetal toxoplasmosis
34
Pyrimethamine + sulfadiazine - Adverse effects
Folate deficiency and hematologic abnormalities
35
Pyrimethamine + sulfadiazine - Interactions
Leucovorin (folic acid) can be added to reduce the hematologic effects of these drugs
36
Albendazole - Classification
Benzimidazole compound
37
Albendazole - MoA
Binds β-tubulin and inhibit its polymerization to form microtubules in the parasites. Makes it impossible for them to obtain glucose.
38
Albendazole - Clinical use
Intestinal nematode infections (ascariasis, capillariasis, hookworm inf, pinworm inf, whiphworm inf) Trichinosis (combo with corticosteroid to relieve inflamation) Cysticercosis, echinococcosis, microsporidiosis
39
Albendazole - Contraindications
Contraindicated during pregnancy because of potential to inhibit mitosis and impair fetal development
40
Albendazole - Adverse effects
Well tolerated High doses: Hepatitis, hemtologic toxicity
41
Albendazole - Interactions
Increased absorption with high fat meal
42
Pyrimethamine - Contraindications
Folate deficiency anemia (Vitamin B9)