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Pharmacology - Midterm 2 > Antiparasitics > Flashcards

Antiparasitics Flashcards

1
Q

What are the Antiamebics?

A

Metronidazole, Tinidazole, Diloxanide Furoate, Iodoquinol, Paramomycin, Chloroquine, Dehydroemetine, Emetine

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2
Q

Mixed Luminal and Systemic Antiamebics

A

Metronidazole and Tinidazole

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3
Q

DOC for invasive amebiasis

A

Metronidazole; follow with Luminal Agent

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4
Q

MOA of Metronidazole

A

Non-ezymatic reduction by Ferredoxin produces cytotoxic compounds that bind to proteins and DNA, causing cell death

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5
Q

Clinical applications of Metronidazole

A

Part of combination therapy against H. pylori, Giardia lamblia, Trichomonas vaginalis, Anaerobic cocci, Anaerobic Gram negative bacilli

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6
Q

PK of Metronidazole

A

Oral; well distributed (including vaginal and seminal fluids, CSF, breast milk, and saliva); hepatic oxidation and glucuronidation via CYP450 enzymes

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7
Q

AE of Metronidazole

A

Disulfiram-like reaction, dark urine, metallic taste, oral monoliasis, ataxia

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8
Q

Is Metronidazole safe for use during pregnancy?

A

Unknown

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9
Q

2nd generation Nitroimidazole better tolerated than Metronidazole

A

Tinidazole

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10
Q

Clincal applications of Tinidazole

A

Amebiasis, Amebic liver abscess, Giardiasis, and Trichomoniasis

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11
Q

AE of Tinidazole

A

Same as Metronidazole but shorter duration; dark urine, metallic taste, Disulfiram-like reaction, oral monoliasis, ataxia

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12
Q

Luminal Antiamebics

A

Diloxanide Furoate, Iodoquinol, Paramomycin

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13
Q

DOC for asymptomatic amebiasis

A

Diloxanide Furoate

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14
Q

MOA of Diloxanide Furoate

A

Converted to Diloxanide freebase active form in gut

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15
Q

AE of Diloxanide Furoate

A

Mild GI distress

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16
Q

Used as alternative to Diloxanide Furoate for mild to severe amebic infections

A

Iodoquinol

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17
Q

MOA of Iodoquinol

A

Orally active against luminal trophozoite AND cyst forms of E. histolytica

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18
Q

AE of Iodoquinol

A

Optic neuritis with long-term use; rash, diarrhea, peripheral neuropathy

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19
Q

Aminoglycoside antibiotic active against luminal forms of E.histolytica and tapeworm

A

Paramomycin

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20
Q

Clinical applications of Paramomycin

A

Alternative for Cryptosporidiosis in AIDS patient

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21
Q

MOA of Paramomycin

A

Amebicidal; binds to 30S ribosomal subunit to inhibit bacterial protein synthesis; reduces intestinal flora

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22
Q

AE of Paramomycin

A

Arthralgia, GI effects and diarrhea, headaches

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23
Q

Systemic Antiamebics

A

Chloroquine, Emetine, Dehydroemetine

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24
Q

Indications for Systemic Antiamebics

A

Treating liver abscesses or intestinal wall infections

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25
Q

Clinical applications of Chloroquine

A

Used in combination with Metronidazole and Diloxanide Furoate

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26
Q

MOA of Chloroquine

A

Eliminates trophozoites in liver abscesses

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27
Q

MOA of Emetine and Dehydroemetine

A

Block ribosomal movement along mRNA to inhibit protein synthesis

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28
Q

Indications of Dehydroemetine and Emetine

A

Backup drugs for treatment of severe intestinal or hepatic amebiasis

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29
Q

Clinical applications of Dehydroemetine and Emetine

A

Used in combination with luminal agent

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30
Q

PK of Dehydroemetine and Emetine

A

Concentrate in liver –> persist for 1 month; slow metabolism and elimination

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31
Q

AE of Dehydroemetine and Emetine

A

Pain at injection site, Cardiotoxicity, neuromuscular weakness, rash

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32
Q

Antihelminthics

A

Albendazole, Mebendazole, Thiabendazole, Ivermectin, Piperazine, Pyrantel pamoate, Diethylcarbamazine, Doxycycline, Praziquantel, Bithionol, and Niclosamide

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33
Q

Benzimidazole Antihelminthics

A

Albendazole, Mebendazole, and Thiabendazole

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34
Q

GABA Agonist Antihelminthics

A

Ivermectin and Piperazine

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35
Q

MOA Albendazole and Mebendazole

A

Inhibit microtubule synthesis and glucose uptake –> decreased ATP causes worm immobilization and death

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36
Q

Indications for Albendazole

A

Cestodal infections (cysticercosis), Taenia solium, Echinococcus granulosus (hydatid

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37
Q

PK of Albendazole

A

Oral; absorption enhanced by fatty meal;

Extensive first-pass metabolism –> rapid sulfoxidation to active metabolite

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38
Q

AE of Albendazole

A

Hepatotoxicity, agranulocytosis, or pancytopenia with long-term treatment (3 months for Echinococcus)

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39
Q

Which Benzimidazole is associated with inflammatory responses to dying parasites in the CNS?

A

Albendazole; convulsions, hyperthermia, headache, mental changes

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40
Q

Contraindications of Albendazole

A

Pregnancy (Cat. C) and children < 2 yoa

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41
Q

PK of Mebendazole

A

Oral; insoluble in aqueous solution; absorption increases with fatty meals; 1st pass metabolism causes inactive compounds

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42
Q

How are parasites treated with Mebendazole excreted?

A

In the feces

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43
Q

Contraindications of Mebendazole

A

Pregnancy (Cat. C) and patients with cirrhosis, and children < 2 yoa

44
Q

AE of Mebendazole

A

abdominal pain, headache, diarrhea, and dizziness

45
Q

MOA of Thiabendazole

A

Inhibits microtubule aggregation

46
Q

Indications of Thiabendazole

A

Strongyloides stercalis (threadworm), cutaneous larva migrant, and early stage of trichinosis

47
Q

PK of Thiabendazole

A

Oral; insoluble in water

48
Q

Contraindications of Thiabendazole

A

Pregnancy (Cat. C), liver or kidney disease

49
Q

AE of Thiabendazole

A

CNS disturbances (dizziness and seizures), Stevens-Johnson syndrome, Erythema multiforme

50
Q

Most toxic of Benzimidazoles

A

Thiabendazole

51
Q

DOC for Strongyloides, Onchocerciasis, and Cutaneous Larva Migrans

A

Ivermectin

52
Q

MOA of Ivermectin

A

GABA agonist; Cl- influx causes hyper polarization of nerve/muscle cell –> paralysis of parasite causes death

53
Q

PK of Ivermectin

A

Oral; does not cross BBB

54
Q

Mazzotti-like Rxn is associated with which GABA agonist ?

A

Ivermectin

55
Q

Contraindications of Ivermectin

A

Pregnancy (Cat. C), Meningitis (may cross BBB), and concomitant use with other GABAergic drugs (benzodiazepines and barbituates)

56
Q

Contraindications of Piperazine

A

Patients with seizure disorders

57
Q

MOA of Piperazine

A

GABA agonist

58
Q

Indications of Piperazine

A

Alternative treatment for pinworm and round worm infections

59
Q

PK of Piperazine

A

Expulsion of worm via peristalsis

60
Q

Indications of Pyrantel pamoate

A

Roundworm, pinworm, and hookworm infections

61
Q

MOA of Pyrantel pamoate

A

Acts as a depolarizing neuromuscular blockade –> Act release and inhibition of Achesterase causes persistent activation of parasite’s nicotinic receptors

62
Q

PK of Pyrantel pamoate

A

Poor oral absorption –> exerts effects in intestinal tract

63
Q

AE of Pyrantel pamoate

A

N/V/D

64
Q

MOA of Diethylcarbamazine

A

Immobilizes microfilariae, making them susceptible to host defenses

65
Q

DOC for Loiasis, Tropical Eosinophilia, and Lymphatic filiarisis

A

Diethylcarbamazine

66
Q

May administer Antihistamines or Steroids with this Antihelminthic agent to decrease AE

A

Diethylcarbamazine

67
Q

AE of Diethylcarbamazine

A

Thought to be due to host responses after damage to/death of parasite: leukocytosis, myalgia, fever, rash, etc.

68
Q

Tetracycline antibiotic that also is active against Wucheria bancrofti (macrofilaricidal) and Onchocerca volvulus (onchocerciasis)

A

Doxycycline

69
Q

MOA of Doxycycline

A

Acts indirectly by killing Wolbachia, intracellular bacterial symbiont of filarial parasites

70
Q

Which Antihelminthic drug has the same efficacy as Albendazole when treating Cysticercosis?

A

Praziquantel

71
Q

DOC for Schistosomiasis and most Trematode and Cestode infections

A

Praziquantel

72
Q

MOA of Praziquantel

A

Increases cell membrane permeability to Ca ==> contracture and paralysis of worm musculature ==> detachment of suckers from blood vessel walls

73
Q

PK of Praziquantel

A

Oral; extensive first-pass metabolism via CYPs

74
Q

Excretion of Praziquantel

A

Inactive metabolites excreted in bile and urine

75
Q

Drug interactions with Praziquantel are due to?

A

CYP450 enzymes

76
Q

Contraindications of Praziquantel

A

Pregnancy (Cat. B), nursing mothers, treatment of Ocular Cysticercosis (destruction of organism may damage the eye!)

77
Q

AE of Praziquantel

A

GI upsets, anorexia, drowsiness

78
Q

DOC for Fasciolis (sheep liver fluke)

A

Bithionol

79
Q

Alternative treatment for Pulmonary Paragonimiasis

A

Bithionol

80
Q

MOA of Bithionol

A

Inhibits parasite’s ETC

81
Q

2nd line drug for most Cestode infections; however, it is uncommonly used due to efficacy of Praziquantel

A

Niclosamide

82
Q

MOA of Niclosamide

A

Inhibits mitochondrial phosphorylation of ADP and possibly inhibits anaerobic metabolism

83
Q

How does Niclosamide affect Cestodes?

A

Lethal to Cestode scolex and segments of Cestode but not to ova

84
Q

PK of Niclosamide

A

Oral; Laxative should be administered prior to Niclosamide purge all dead segments and ova, which may lead to Cysticerosis

85
Q

What must be avoided within 1 day of dose of Niclosamide

A

Alcohol

86
Q

Is Niclosamide safe for use in pregnancy and children < 2 yoa?

A

Unknown

87
Q

DOC for Ascariasis (roundworm)

A

Albendazole, Pyrantel pamoate, or Mebendazole

88
Q

DOC for Enterobiasis (pinworm)

A

Mebendeazole or Pyrantel pamoate

89
Q

DOC for Trichuriasis (whipworm)

A

Mebendazole or Albendazole

90
Q

DOC for Hookworm (N. americanus or A. duodenale)

A

Pyrantel pamoate, Mebendazole, or Albendazole

91
Q

DOC for Onchocerciasis (River Blindness)

A

Ivermectin

92
Q

Cutaneous larva migrans (Creeping eruption, dog, and cat hookworm) Ancylostoma sp

A

Albendazole or Ivermectin

93
Q

DOC for Fasciola hepatica (liver fluke)

A

Bithionol

94
Q

DOC for Schistosomiasis

A

Praziquantel

95
Q

DOC for Clonorchis sinensis (Oriental liver fluke)

A

Praziquantel

96
Q

DOC for Paragonimus westermani (lung fluke)

A

Praziquantel

97
Q

DOC for Echinococcosis - Echinococcus granulosis (dog tapeworm)

A

Albendazole

98
Q

DOC for Taeniasis - Taenia solium (pork tapeworm)

A

Praziquantel or Niclosamide

99
Q

DOC for Taeniasis - Taenia saginata (beef tapeworm)

A

Praziquantel or Niclosamide

100
Q

Cysticercosis (Taenia solium larvae)

A

Albendazole or Praziquantel

101
Q

DOC for Dyphyllobothriasis - Dyphyllobothrium latum (fish tapeworm)

A

Praziquantel or Niclosamide

102
Q

DOC for Giardia lamblia and Trichomonas vaginalis

A

Metronidazole

103
Q

Trypanosomiasis (African sleeping sickness)

A

Melarsoprol or Suramin

104
Q

Treatment of hemolymphatic stage of trypanosomiasis and for Pneumocystis jiroveci

A

Pentamidine

105
Q

DOC Toxoplasmosis (toxoplasmic encephalitis)

A

Pyramethamine + Clindamycin or Sulfadiazine or Folinic acid (Leucovorin)

106
Q

Treatment of Leishmaniasis (all stages)

A

Sodium stibogluconate/Amphotercin B

107
Q

DOC for Pneumocystis jiroveci

A

Trimethoprim-Sulfamethoxazole (Cotrimoxazole)

Pharmacology - Midterm 2 (16 decks)

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