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Pharmacology > Antiparasitic/Antifungal > Flashcards

Antiparasitic/Antifungal Flashcards

1
Q

metronidazole (Flagyl)

A
  • antiparasitic
  • MOA: activated by pyruvate:ferrodoxin oxidoreductase (PFOR)–> bind and disrupt protein and DNA structure/function
  • activated under anaerobic conditions
  • use: trichomoniasis (partners treated simultaneously), giardiasis, amebiasis
  • effective against trophozoite form NOT cyst form
  • adverse effects: headache, dry mouth, metallic taste, vomiting, diarrhea, disulfiram-like effect (avoid alcohol
  • safe during pregancy
  • resistance: RARE, some decreased PFOR activity
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2
Q

idoquinol

A
  • antiparasitic
  • MOA: unknown
  • use: eliminate trophozoite AND cyst form of E.histolytica in lumen of intestines (poorly absorbed)
  • used in combo with metronidazole
  • adverse effects: GI discomfort (take w/ food), optic atrophy, permanent vision loss (long term use)
  • resistance: no information
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3
Q

paromomycin

A
  • antiparasitic
  • MOA: aminoglycoside antibiotic–>inhibit protein synthesis in bacteria
  • use: eliminate trophozoite and cyst form of E. histolytica from lumen of intestine NOT tissue
  • combo w/ metronidazole
  • adverse effects: abdominal discomfort, less toxic than iodoquinol
  • resistance: unknown
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4
Q

nitazoxanide

A
  • antiparasitic
  • MOA: interference with PFOR–>disrupt anaerobic energy metabolism
  • use: Cryptosporidium parvum, Giardia lamblia for >1yo
  • resistance: unknown
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5
Q

pyrimethamine-sulfadiazine

trimethoprim-sulfamethoxazole (TMP-SMX)

A
  • antiparasitic
  • MOA: sulfonamides–> inhibit production of pteroic acid from PABA by dihydropteroate synthase; diaminopyrimidines–>inhibit DHFR enzyme–> prevent tetrahydrofolate formation
  • pyrimethamine-sulfadiazine: toxoplasmosis, ineffective against tissue cyst
  • TMP-SMX: Pneumocystis jirovecii
  • synergistic effect when in combo
  • adverse effects: rash, GI intolerance
  • can induce folate deficiency–> leucovorin co-administered
  • resistance: aa substitutions in targeted enzymes
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6
Q

chloroquine

A
  • antimalarials
  • MOA: interfere w/ parasite ability to detoxify compound from degradation of hemoglobin
  • use: asexual erythrocytic stage of all Plasmodium, prophylaxis and clinical disease
  • adverse effects: headache, nausea, vomiting, blurred vision, dizziness, fatigue, confusion
    resistance: BIG TIME, rapid export, pump?
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7
Q

quinine

A
  • antimalarial
  • MOA: digestive vacuoles–>interfere with hemoglobin degradation or detoxification of metabolic products; complex with DNA–>interfere w/ transcription and replication
  • use: eliminate asexual erythrocytic stage of Plasmodium clinical disease, IV admin
  • adverse effects: WORST, cinchonism, hypoglycemia
  • resistance: beginning in Asia
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8
Q

mefloquine

A
  • antimalarial
  • MOA: similar to quinine?
  • use: intraerythromcytic form of Plasmodium, prophylaxis and treatment
  • adverse effects: some neuropsychiatric reactions
  • resistance: none
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9
Q

primaquine

A
  • antimalarial
  • MOA: activation by host–> interfere w/ mitochondrial ETC and pyrimidine synthesis
  • use: dormant liver (hypnozoite) form of P. vivax and P. ovale
  • adverse effects: hemolysis in G6PD pts
  • resistance: some
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10
Q

malarone

A
  • antimalarial
  • atovaquone: MOA unknown
  • proguanil: MOA–>inhibits DHFR–> inhibit folate synthesis
  • use: treament of P. falciparum, prophylaxis
  • resistance: none reported
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11
Q

doxycylcine

A
  • antimalarial, tetracycline antibiotic
  • MOA: inhibit protein synthesis
  • use: prophylaxis or treatment in combo
  • adverse effects: photosensitivity dermatitis, staining of teeth in children (contraindicated in children and pregnancy)
  • resistance: little evidence
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12
Q

artemisinin

A
  • antimalarial, extracted from Chinese wormwood
  • MOA: interact with iron–> radicals damage membranes?
  • use: all Plasmodium
  • adverse effects: minor nausea and diarrhea
  • resistance: declining susceptibility
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13
Q

albendazole

A
  • anthelminitic-benzimidazole
  • MOA: inhibit mitosis, cause muscle paralysis of parasite
  • poorly soluble
  • empty stomach for luminal nematodes, fatty meal for tissue dwelling
  • use: acariasis, pinworms, hookworm, whipworm
  • adverse effects: primarily GI
  • contraindicated in pregnancy and possible
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14
Q

mebendazole

A
  • anthelminitic-benzimidazole
  • MOA: inhibit mitosis, cause muscle paralysis of parasite
  • poorly soluble
  • empty stomach for luminal nematodes, fatty meal for tissue dwelling
  • use: acariasis, pinworms, hookworm, whipworm
  • adverse effects: primarily GI
  • contraindicated in pregnancy and possible
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15
Q

thiabendazole

A
  • anthelminitic-benzimidazole
  • MOA: inhibit mitosis, cause muscle paralysis of parasite
  • absorbed–>greater toxicity
  • empty stomach for luminal nematodes, fatty meal for tissue dwelling
  • use: 2nd line strongyloidiasis, cutaneous larval migrans
  • adverse effects: anorexia, nausea, vomiting, delirium, hallucinations
  • contraindicated in pregnancy and possible
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16
Q

ivermectin

A
  • anthelmintics
  • MOA: increase Cl- permeability–> hyperpolarization–> muscle paralysis
  • use: strongyloidiasis (intestinal and extraintestinal), tissue dwelling nematodes
  • resistance: none
17
Q

pyrantel pamoate

A
  • anthelminitic
  • MOA: activate cholinergic nicotinic receptors in somatic muscles–>depolarizing neuromuscular blockade
  • poorly absorbed–>luminal nematodes
  • use: pinworms, treat ENTIRE family, secondary drug for Ascaris and hookworm
  • resistance: none
18
Q

praziquantel

A
  • Against cestodes (tapeworms) and trematodes (flukes)
  • MOA: increase Ca2+ permeability–> depolarization; increased immune detection; induce spastic paralysis in trematodes
  • adverse effects: immune response to dying worm (fever, rash, myalgia), headache, abdominal discomfort
  • use: flukes, tapeworms, cysticerosis
    resistance: some Schistosomes
19
Q

amphotericin B

A
  • systemically active drugs for systemic infections
  • polyenes
  • MOA: bind ergosterol in cell membrane–> forms pore–> fungicidal
  • use: systemic yeast (Candida, Cryptococcus), systemic molds (Aspergillus, Histoplasma, Coccidioides, Blastomyces, Sporothrix, mucormycoses)
  • resistance: decrease ergosterol, seen in Candida and Aspergillus
  • does NOT penetrate CNS
  • adverse effects: fever, chills, hypertension, vomiting, nephrotoxicity (decreased renal perfusion)
  • liposomal packaged–>less toxic
20
Q

ketoconazole
miconazole
clotrimazole

A
  • azole, imidazole
  • MOA: bind enzyme responsible for converting lanosterol to ergosterol–> leaky cell membrane
  • use: pathogenic yeast, systemic mycoses, dermatophytes
  • systemic activity (ketoconazole), topical use for others
  • adverse effect: inhibits liver cytochrome P450 enzymes
  • less selective toward fungi–> not used as often
  • resistance: efflux pumps, mutations in target enzyme, decreased ergosterol content
21
Q

fluconazole

A
  • azole, triazole
  • MOA: bind enzyme responsible for converting lanosterol to ergosterol–> leaky cell membrane
  • use: 1st choice candidiasis, cryptococcosis, and coccidiomycosis; 2nd choice histoplasmosis, blastomycosis, sporotrichosis
  • systemic activity, CNS penetration
  • adverse effect: lowest level of inhibition of liver cytochrome P450 enzymes
  • resistance: efflux pumps, mutations in target enzyme, decreased ergosterol content
22
Q

itraconazole

A
  • azole, triazole
  • MOA: bind enzyme responsible for converting lanosterol to ergosterol–> leaky cell membrane
  • use: blastomycosis, coccidiomycosis, histoplasmosis, sporotrichosis, Aspergillus, Candida, dermatophyte, onychomycosis
  • systemic activity
  • requires low pH for absorption (impaired by antacids)
  • adverse effect: inhibition of liver cytochrome P450 enzymes
  • resistance: efflux pumps, mutations in target enzyme, decreased ergosterol content
23
Q

voriconazole

A
  • azole, triazole
  • MOA: bind enzyme responsible for converting lanosterol to ergosterol–> leaky cell membrane
  • use: Candida, dimorphic fungi, aspergillosis (treatment of choice)
  • systemic activity
  • adverse effect: inhibition of liver cytochrome P450 enzymes, blurred vision, photophobia, altered perception of color
  • resistance: efflux pumps, mutations in target enzyme, decreased ergosterol content
24
Q

posaconazole

A
  • azole, triazole
  • MOA: bind enzyme responsible for converting lanosterol to ergosterol–> leaky cell membrane
  • use: Candida, dimorphic fungi, Aspergillus, mucormycoses, Cryptococcus
  • systemic activity
  • take with fatty meal
  • adverse effect: strong inhibition of liver cytochrome P450 enzymes
  • resistance: efflux pumps, mutations in target enzyme, decreased ergosterol content
25
Q

flucytosine

A
  • originally anti-neoplastic agent
  • analog of cytosine
  • MOA: converted to 5-FU–> incorporated into RNA–> disrupt protein synthesis or inhibit DNA synthesis
  • use: systemic infections, Cryptococcus, Candida
  • adverse reaction: bone marrow suppression, anemia, leukopenia, thrombocytopenia, hepatotoxicity, GI intolerance
  • resistance: altered metabolism of flucytosine
26
Q

echinocandins

A
  • lipopeptides
  • MOA: inhibit synthesis of beta-glucans–> weakened cell wall–> osmotic stress
  • use: Candida, Aspergillus, non-responsive organisms
  • IV, poor CNS penetration, $$
  • adverse effects: well tolerated, drug interactions
27
Q

griseofulvin

A
  • oral agent to treat dermatophyte infection
  • MOA: interfere with microtubule function–> interfere with mitosis
  • admin microcrystalline form, improved with fatty meals
  • concentrates in keratin precursor cells
  • replaced by newer drugs
  • side effects: headache, decreased effectiveness of oral contraceptives
28
Q

allylamines

A
  • oral systemic drugs for cutaneous and mucocutaneous infection
  • MOA: inhibit enzyme of squalene epoxidase–> inhibit ergosterol synthesis–>damaged cell membrane
  • terbinafine= topical or oral for onychomycosis and other dermatophyte infections
  • adverse effects: rare
29
Q

nystatin

A
  • topical antifungal
  • polyene
  • MOA: binds ergosterol
  • use: Candida, oropharyngeal, vaginal candidiasis
30
Q

clotrimazole

miconazole

A
  • topical azole
  • OTC drugs
  • use: vulvovaginal candidiasis, oral lozenges for thrush, tinea corporis, tinea, pedis, tinea cruris
31
Q

terbinafine

naftifine

A
  • topical allylamines

- use: tinea cruris (jock itch), tinea corporis (ringworm), pityriasis

Pharmacology (34 decks)

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