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Pharmacology > Antiparasitic drugs > Flashcards

Antiparasitic drugs Flashcards

1
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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2
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)
Balantidiasis
Enterocolitis
Rosacea (acne rosacea)
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3
Q

Metronidazole and Tinidazole - Contraindications

A

Contraindicated during first trimester of pregnancy

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4
Q

Metronidazole and Tinidazole - Adverse effects

A

Metallic taste
Transient leukopenia
Thrombocytopenia

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5
Q

Metronidazole and Tinidazole - Interactions

A

Increase effect of warfarin.

Ethanol: disulfiram-like reaction

Serum levels affected by drugs inhibiting/inducing CYP3A4.

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6
Q

Tinidazole - Clinical use

A

Entamoeba histolytica
Giardia intestinalis (Giardia lamblia)
Trichonomas vaginalis

Anaerobic bacteria:
Bacteroides fragilis
Helicobacter pylori
Clostridium difficle

Giardiasis
Trichonomiasis
Amebiasis
Amebic liver abscess
Bacterical vaginosis
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7
Q

Iodoquinol, Paromomycin, Diloxanide - Clinical use

A

Used alone to treat asymptomatic carriers of E. histolytica, but it must be used in combination with a tissue amebicide to treat patients with symptomatic disease, including amebic dysentery and liver abcess

Dientamoeba fragilis (Idoquinolol)

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8
Q

Nitazoxanide - MoA

A

Noncompetative inhibitor of pyruvate-ferredoxin oxidoreductase

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9
Q

Nitazoxanide - Clinical use

A

Cryptosporidium parvum
Giardia lamblia
Entamoeba histolytica

Cryptosporidiosis, giardiasis in immunocompetent persons

Ascariasis

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10
Q

Quinine, Chloroquine, Mefloquinine - MoA

A

Inhibits nucleic acid synthesis/function during erythrocytic schizogony

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11
Q

Chloroquine, Quinine - Clinical use

A

Chloroquinine
P. falciparum, prevention and treatment

Combination with primaquine to eradicate P. vivax or P. ovale

Quinine: Alternative to artesunate for severe malaria

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12
Q

Chloroquine - Contraindications

A

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

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13
Q

Chloroquine - Adverse effects

Quinine - Adverse effects

A

Toxic overdose: Retinal damage and blindness
Exacerbation of psoriasis and pruritus

Cinchonizm

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14
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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15
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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16
Q

Primaquine - MoA

A

Form quinones that oxidize and destroy schizont membranes

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17
Q

Primaquine - Clinical use

A

Exoerythrocytic tissue stage of P. vivax and P. ovale in combination with chloroquine or other drugs

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18
Q

Primaquine - Adverse effects and Contraindications

A

Hemolytic anemia in G6PD deficiency

G6PD deficiency

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19
Q

Artesunate, Artemether - MoA

A

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

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20
Q

Artesunate - Clinical use

A

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

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21
Q

Artemether - Clinical use

A

P. falciparum malaria

P. vivax

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22
Q

Which drugs has the most rapid action of the current drugs against falciparum?

A

Artesunate and Artemether

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23
Q

Atovaquone - MoA

A

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

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24
Q

Atovaquone - Clinical use

A

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

Alone: pneumocystitis jiroveci infections

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25
Q

Atovaquone - Special considerations

A

Always in combo with proguanil or doxycycline for malaria.

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26
Q

Proguanil - MoA

A

Inh synthesis of pyrimidines and nucleic acid synthesis by inhibiting dihydrofolate reductase

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27
Q

Proguanil - Clinical use

A

Prophylaxis and treatment of Chloroquine-resistant falciparum malaria in combination with atovaquone

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28
Q

Pyrimethamine, Sulfadoxine - MoA

A

Pyrimethamine:
Inh folic acid synthesis in plasmodia by blocking dihydrofolate reductase.

Sulfadoxine:
Inh folic acid synthesis in plasmodia by inhibiting dihydrofolate synthesis

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29
Q

Pyrimethamine, Sulfadoxine - Clinical use

A

Malaria

Toxoplasmosis (in combination)

30
Q

Pyrimethamine, Sulfadoxine - Adverse effects

A

Skin rashes
Megaloblastic anemia and other hematologic reactions
Folate deficiency
Severe hematologic abnormalities

31
Q

Drugs for toxoplasmosis

A

Pyrimethamine + sulfadiazine

Spiramycin

32
Q

Drugs for toxoplasmosis - Clinical use

A

Pyrimethamine + sulfadiazine: Toxoplasmosis in AIDS Spiramycin: Fetal toxoplasmosis

33
Q

Which drug is used for pregnant women with toxoplasmosis?

A

Spiramycin

34
Q

Drugs for pneumocystic jiroveci infection

A 
Trimethoprim-sulfamethoxazole 
Atovaquone
Pentamidine
Dapsone
Prednisone
35
Q

Which drug is preferred for acutely ill patients with pneumocystis jiroveci infections?

A

Prednisone

36
Q

Dapsone - Special considerations

A

In combination with trimethoprim/pyrimethamine

37
Q

Pyrimethamine + sulfadiazine- Interactions

A

Lecovorin (folic acid) can be added to reduce hematologic effects.

38
Q

Pentamidine - Adverse effects

A 
Hematologic toxicity
Ventricular tachycardia
Edema
Pancreatitis
Bronchospasm 
Stevens-Johnsons syndrome
39
Q

Pentamidine and Suramin - Clinical use

A

Early African trypanosomiasis (sleeping sickness),

Trypanosoma brucei

40
Q

Melarsoprol and Eflornithine - Clinical use

A

Late African trypanosomiasis (sleeping sickness) against CNS manifestations

41
Q

Nifurtimox - Clinical use

A

American trypanosomiasis (Chagas disease), Trypanosoma cruzi

42
Q

Nifurtimox - Special considerations

A

Often combined with interferon-γ

43
Q

Miltefosine - MoA

A

Inhibits enzymes for glycolipid metabolism of the surface of leishmania species

44
Q

Miltefosine - Clinical use

A

Cutaneous and visceral leishmaniasis (kala-azar)

45
Q

Miltefosine - Adverse effect

A

Reversible hepatic and renal toxicity

46
Q

Albendazole and mebendazole - Classification

A

Benzimidazole compounds

47
Q

Albendazole and mebendazole- MoA

A

Binds b-tubulin and inhibit its polymerization to form microtubules in the parasites. Makes it impossible for them to obtain glucose

48
Q

Albendazole and Mebendazole- Clinical use

A 
Both:
Intestinal nematode infections: 
Ascariasis
Capillariasis
Hookworm (Ancylostoma and Necator)
Pinworm (Enterobius vermicularis)
Whiphworm (Trichuris trichuria)

Trichinosis (combined with corticosteroid to relieve inflammation)

Albendazole:
Cysticercosis (Pork tapeworm, Taenia solium)
Echinococcosis
Microsporidiosis

49
Q

Albendazole and mebendazole - Contraindications

A

Contraindicated during pregnancy

50
Q

Pyrantel - Classification

A

Pyrimidine derivative

51
Q

Pyrantel - MoA and Clinical use

A

Activates nicotinic ACh receptors in somatic muscles of nematodes. Causes depolarizing neuromuscular blockade.

Hookworm and pinworm infection

52
Q

Ivermectin - Classification

A

Broad-spectrum anthelmintic drug

53
Q

Ivermectin - MoA

A

Increases Chloride permeability of intervertebrate muscle cells. Cause hyperpolarization of the cell membrane and paralysis of pharyngeal muscles in helminths

54
Q

Ivermectin - Clinical use

A 
Active against nematodes
Strongyloidiasis
Onchocerciasis (River blindness)
Cutaneous larva migrans (Hookworm)
Loa loa (loiasis)
Lymphatic filariasis (brugia malayi, Wuchereria bancrofti)
Scabies
55
Q

Diethylcarbamazine (DEC) - Classification

A

Piperazine derivative

56
Q

Diethylcarbamazine (DEC) - MoA

A

Inhibits prostacyclin and prostaglandin E2 and I2 in both host cell and filariae. Blood vessel constriction and aggregation of host granulocytes.

57
Q

Diethylcarbamazine (DEC) - Clinical use

A

Elephantiasis (Wuchereria bancrofti, Brugia malayi)

58
Q

Diethylcarbamazine (DEC) - Adverse effects

A

Severe hypersensitivity reaction

59
Q

Praziquantel - Classification

A

Isoquinoline derivative

60
Q

Praziquantel - MoA

A

Increased calcium permeability of the tegument, and cause depolarization

61
Q

Praziquantel - Clinical use

A 
Schistosomiasis 
Tissue flukes: 
Chinese liver fluke (Clonorchis sinesis)
Lung fluke (Paragonimus westermani) 
Tapeworms (cysticerosis).
62
Q

Triclabendazole - Clinical use

A

Sheep liver fluke (Flasciola hepatica)

63
Q

Bithionol - Clinical use

A

Alternative for sheep liver fluke and lung fluke (Paragonimus westermani)

64
Q

Oxamniquine - Clinical use

A

Alternative to praziquantel for Schistosoma mansoni infections

65
Q

Niclosamide - Clinical use

A

Alternative to praziquantel for cestode infections

66
Q

Permethrin - Classification

A

Synthetic pyrethrin-like compound

67
Q

Permethrin - MoA

A

Block sodium currents in neurons of parasites. Paralysis of the organism

68
Q

Permethrin - Clinical use

A

Pediculosis (lice)

Scabies (mites)

69
Q

Spinosad - MoA

A

Activate nicotinic ACh receptors, causing muscle contraction and paralysis

70
Q

Spinosad - Clinical use

A

Head lice (pt over 4 years)

Pharmacology (55 decks)

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