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Pharmacology - Midterm 2 > Antiparasitics > Flashcards

Antiparasitics Flashcards

(107 cards)

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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
Clinical applications of Chloroquine
Used in combination with Metronidazole and Diloxanide Furoate
26
MOA of Chloroquine
Eliminates trophozoites in liver abscesses
27
MOA of Emetine and Dehydroemetine
Block ribosomal movement along mRNA to inhibit protein synthesis
28
Indications of Dehydroemetine and Emetine
Backup drugs for treatment of severe intestinal or hepatic amebiasis
29
Clinical applications of Dehydroemetine and Emetine
Used in combination with luminal agent
30
PK of Dehydroemetine and Emetine
Concentrate in liver --> persist for 1 month; slow metabolism and elimination
31
AE of Dehydroemetine and Emetine
Pain at injection site, Cardiotoxicity, neuromuscular weakness, rash
32
Antihelminthics
Albendazole, Mebendazole, Thiabendazole, Ivermectin, Piperazine, Pyrantel pamoate, Diethylcarbamazine, Doxycycline, Praziquantel, Bithionol, and Niclosamide
33
Benzimidazole Antihelminthics
Albendazole, Mebendazole, and Thiabendazole
34
GABA Agonist Antihelminthics
Ivermectin and Piperazine
35
MOA Albendazole and Mebendazole
Inhibit microtubule synthesis and glucose uptake --> decreased ATP causes worm immobilization and death
36
Indications for Albendazole
Cestodal infections (cysticercosis), Taenia solium, Echinococcus granulosus (hydatid
37
PK of Albendazole
Oral; absorption enhanced by fatty meal; Extensive first-pass metabolism --> rapid sulfoxidation to active metabolite
38
AE of Albendazole
Hepatotoxicity, agranulocytosis, or pancytopenia with long-term treatment (3 months for Echinococcus)
39
Which Benzimidazole is associated with inflammatory responses to dying parasites in the CNS?
Albendazole; convulsions, hyperthermia, headache, mental changes
40
Contraindications of Albendazole
Pregnancy (Cat. C) and children < 2 yoa
41
PK of Mebendazole
Oral; insoluble in aqueous solution; absorption increases with fatty meals; 1st pass metabolism causes inactive compounds
42
How are parasites treated with Mebendazole excreted?
In the feces
43
Contraindications of Mebendazole
Pregnancy (Cat. C) and patients with cirrhosis, and children < 2 yoa
44
AE of Mebendazole
abdominal pain, headache, diarrhea, and dizziness
45
MOA of Thiabendazole
Inhibits microtubule aggregation
46
Indications of Thiabendazole
Strongyloides stercalis (threadworm), cutaneous larva migrant, and early stage of trichinosis
47
PK of Thiabendazole
Oral; insoluble in water
48
Contraindications of Thiabendazole
Pregnancy (Cat. C), liver or kidney disease
49
AE of Thiabendazole
CNS disturbances (dizziness and seizures), Stevens-Johnson syndrome, Erythema multiforme
50
Most toxic of Benzimidazoles
Thiabendazole
51
DOC for Strongyloides, Onchocerciasis, and Cutaneous Larva Migrans
Ivermectin
52
MOA of Ivermectin
GABA agonist; Cl- influx causes hyper polarization of nerve/muscle cell --> paralysis of parasite causes death
53
PK of Ivermectin
Oral; does not cross BBB
54
Mazzotti-like Rxn is associated with which GABA agonist ?
Ivermectin
55
Contraindications of Ivermectin
Pregnancy (Cat. C), Meningitis (may cross BBB), and concomitant use with other GABAergic drugs (benzodiazepines and barbituates)
56
Contraindications of Piperazine
Patients with seizure disorders
57
MOA of Piperazine
GABA agonist
58
Indications of Piperazine
Alternative treatment for pinworm and round worm infections
59
PK of Piperazine
Expulsion of worm via peristalsis
60
Indications of Pyrantel pamoate
Roundworm, pinworm, and hookworm infections
61
MOA of Pyrantel pamoate
Acts as a depolarizing neuromuscular blockade --> Act release and inhibition of Achesterase causes persistent activation of parasite's nicotinic receptors
62
PK of Pyrantel pamoate
Poor oral absorption --> exerts effects in intestinal tract
63
AE of Pyrantel pamoate
N/V/D
64
MOA of Diethylcarbamazine
Immobilizes microfilariae, making them susceptible to host defenses
65
DOC for Loiasis, Tropical Eosinophilia, and Lymphatic filiarisis
Diethylcarbamazine
66
May administer Antihistamines or Steroids with this Antihelminthic agent to decrease AE
Diethylcarbamazine
67
AE of Diethylcarbamazine
Thought to be due to host responses after damage to/death of parasite: leukocytosis, myalgia, fever, rash, etc.
68
Tetracycline antibiotic that also is active against Wucheria bancrofti (macrofilaricidal) and Onchocerca volvulus (onchocerciasis)
Doxycycline
69
MOA of Doxycycline
Acts indirectly by killing Wolbachia, intracellular bacterial symbiont of filarial parasites
70
Which Antihelminthic drug has the same efficacy as Albendazole when treating Cysticercosis?
Praziquantel
71
DOC for Schistosomiasis and most Trematode and Cestode infections
Praziquantel
72
MOA of Praziquantel
Increases cell membrane permeability to Ca ==> contracture and paralysis of worm musculature ==> detachment of suckers from blood vessel walls
73
PK of Praziquantel
Oral; extensive first-pass metabolism via CYPs
74
Excretion of Praziquantel
Inactive metabolites excreted in bile and urine
75
Drug interactions with Praziquantel are due to?
CYP450 enzymes
76
Contraindications of Praziquantel
Pregnancy (Cat. B), nursing mothers, treatment of Ocular Cysticercosis (destruction of organism may damage the eye!)
77
AE of Praziquantel
GI upsets, anorexia, drowsiness
78
DOC for Fasciolis (sheep liver fluke)
Bithionol
79
Alternative treatment for Pulmonary Paragonimiasis
Bithionol
80
MOA of Bithionol
Inhibits parasite's ETC
81
2nd line drug for most Cestode infections; however, it is uncommonly used due to efficacy of Praziquantel
Niclosamide
82
MOA of Niclosamide
Inhibits mitochondrial phosphorylation of ADP and possibly inhibits anaerobic metabolism
83
How does Niclosamide affect Cestodes?
Lethal to Cestode scolex and segments of Cestode but not to ova
84
PK of Niclosamide
Oral; Laxative should be administered prior to Niclosamide purge all dead segments and ova, which may lead to Cysticerosis
85
What must be avoided within 1 day of dose of Niclosamide
Alcohol
86
Is Niclosamide safe for use in pregnancy and children < 2 yoa?
Unknown
87
DOC for Ascariasis (roundworm)
Albendazole, Pyrantel pamoate, or Mebendazole
88
DOC for Enterobiasis (pinworm)
Mebendeazole or Pyrantel pamoate
89
DOC for Trichuriasis (whipworm)
Mebendazole or Albendazole
90
DOC for Hookworm (N. americanus or A. duodenale)
Pyrantel pamoate, Mebendazole, or Albendazole
91
DOC for Onchocerciasis (River Blindness)
Ivermectin
92
Cutaneous larva migrans (Creeping eruption, dog, and cat hookworm) Ancylostoma sp
Albendazole or Ivermectin
93
DOC for Fasciola hepatica (liver fluke)
Bithionol
94
DOC for Schistosomiasis
Praziquantel
95
DOC for Clonorchis sinensis (Oriental liver fluke)
Praziquantel
96
DOC for Paragonimus westermani (lung fluke)
Praziquantel
97
DOC for Echinococcosis - Echinococcus granulosis (dog tapeworm)
Albendazole
98
DOC for Taeniasis - Taenia solium (pork tapeworm)
Praziquantel or Niclosamide
99
DOC for Taeniasis - Taenia saginata (beef tapeworm)
Praziquantel or Niclosamide
100
Cysticercosis (Taenia solium larvae)
Albendazole or Praziquantel
101
DOC for Dyphyllobothriasis - Dyphyllobothrium latum (fish tapeworm)
Praziquantel or Niclosamide
102
DOC for Giardia lamblia and Trichomonas vaginalis
Metronidazole
103
Trypanosomiasis (African sleeping sickness)
Melarsoprol or Suramin
104
Treatment of hemolymphatic stage of trypanosomiasis and for Pneumocystis jiroveci
Pentamidine
105
DOC Toxoplasmosis (toxoplasmic encephalitis)
Pyramethamine + Clindamycin or Sulfadiazine or Folinic acid (Leucovorin)
106
Treatment of Leishmaniasis (all stages)
Sodium stibogluconate/Amphotercin B
107
DOC for Pneumocystis jiroveci
Trimethoprim-Sulfamethoxazole (Cotrimoxazole)

Pharmacology - Midterm 2 (16 decks)

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