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pharm 2 mod 4: fungals/microbials > EXAM PREP > Flashcards

EXAM PREP Flashcards

1
Q

What are the uses of Metronidazole

A

Ambebiasis, giardiasis, trichomoniasis, anaerobic bacterial infections
co-administer with Paromycin (luminal agent)

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2
Q

what is the MOA for Metronidazole

A

Nitro group serves as electron acceptor, forms toxic metabolite that disrupts DNA structure -> cell death

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3
Q

what are the pharmacokinetics of Metronidazole

A

Oral
hepatic metabolism, excreted in urine

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4
Q

What are the SE/Contraindications of metronidazole

A

N/V, abdominal pain, metallic taste, seizures, neuropathy, disulfiram effect with alcohol

contra: pregnancy, breast feeding, recent use of disulfiram

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5
Q

What are the uses of Trimethoprim-sulfamethoxazone (TMP-SMX)

A

aka Bactrim
cyclospora and isopora infections
treatment of choice for P. jirovecci pneumonia

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6
Q

what is the MOA for TMP-SMX

A

combo provides sequential and synergistic blockade of folate pathway -> inhibition of thymidine synthesis

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7
Q

What are the pharmacokinetics of TMP-SMX

A

oral or IV infusion

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8
Q

what are the AE/Contraindications for TMP-SMX

A

Rash, SJS, kernicterus, bone marrow suppression, anemia, renal impairment, hepatotoxicity

Contra: renal disease, newborns and pregnancy

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9
Q

What are the uses for Albendazole

A

broadly effective against nematodes (round worms)

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10
Q

What is the MOA for Albendazole

A

binds to microtubules in worms and larvae -> impaired glucose uptake -> glycogen depletion -> degeneration of mitochondria -> release of lysosomes, depletion of ATP -> worm death

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11
Q

What are the pharmacokinetics of Albendazole

A

oral admin

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12
Q

What are the AE/contraindications of Albendazole

A

HA, elevated LFTs, liver impairment, bone marrow suppression, seizures, alopecia

Contra: pregnancy

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13
Q

What are the uses of Pyrantel pamoate

A

alternative to albendazole for infestations with hookworms or pinworms

NOT preferred, newer agents available

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14
Q

what is the MOA for pyrantel pamoate

A

causes release of Ach and inhibits cholinesterase -> depolarizing neuromuscular blocker -> spastic paralysis and release of helminths

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15
Q

What are the pharmacokinetics of pyrantel pamoate

A

oral admin

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16
Q

what are the AE/Contraindications of pyrantel pamoate

A

GI upset, dizziness, drowsiness, HA, insomnia

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17
Q

what are the uses of Praziquantel

A

flukes and cestodes (tapeworms) and is the DOC for tapeworms and schistosomiasis and other fluke infestations

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18
Q

what is the MOA of Praziquantel

A

increase cell permeability to Ca2+ in schistosomes -> strong contractions and paralysis of worms -> detachment, death

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19
Q

What are the pharmacokinetics of Praziquantel

A

Oral
extensively metabolism by CYP3A4

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20
Q

What are the AE/contraindications for Praziquantel

A

HA, abdominal discomfort, drowsiness, dizziness
patients with cerebral cystocercosis (brain worms) experience CNS AE
avoid co-admin with CYP inducers

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21
Q

what are the uses of Ivermectin

A

Onchocerciasis (major cause of blindness worldwide) and intestinal stronglyoidasis
head lice

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22
Q

What is the MOA for Ivermectin

A

binds and activates glutamate-gated Cl-channels in invertebrate nerve/muscle cells -> hyperpolarization -> death

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23
Q

What are the pharmacokinetics of Ivermectin

A

Oral or topical
does NOT cross BBB

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24
Q

What are the AE/Contraindications for Ivermectin

A

pruritus, rash, fever, lymph node tenderness, bone and joint pain, neurotoxicity

contra: pregnancy and meningitis

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25
Q

What are the Antiparacitis/anti-helmintics

A

Metronidazole
Bactrim
Albendazole
Pyrantel pamoate
Praziquantel
Ivermectin

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26
Q

What are the uses for Amphotericin B

A

widest spectrum of activity of all antifungals
treatment of severe invasive fungal infections

resistance rare, but some resistance is d/t decreased ergosterol content in cell membrane

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27
Q

what is the MOA for Amphotericin B

A

lipophilic rod-like molecule binds to ergosterol -> forms pores in membrane -> K+ leaks out of cell causing death

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28
Q

What are the pharmacokinetics of Amphotericin B

A

IV infusion
6-8 weeks of treatment, but can be as long as 3-4mo
onset of action is rapid
low TRUTH IS
little CSF penetration

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29
Q

what needs to be monitored with someone on Amphotericin B

A

K+ and Mg2+

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30
Q

What are the AE/Contraindications for amphotericin B

A

infusion reactions, nephrotoxicity, bone marrow suppression, N/V, anemia, phlebitis

contra: renal insufficiency, combo with other nephrotoxic agents

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31
Q

How can nephrotoxicity be reduced with Amphotericin B

A

Saline loading and increased infusion time

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32
Q

What are the uses of Nystatin

A

candida infections of skin, mouth, esophagus, intestines, vagina

too toxic for systemic use

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33
Q

What is the MOA of Nystatin

A

lipophilic rod-like molecule binds to ergosterol -> forms pores in membrane -> K+ leaks out of cell causing death

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34
Q

What are the pharmacokinetics of Nystatin

A

Powder, Ointment, Cream or Suspension administration

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35
Q

What are the AE/Contraindications of Nystain

A

topical: local irritation

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36
Q

What are the uses for Flucytosine

A

systemic mycosis and meningitis caused by candida and cryptococcus
combo with itraconazole for treatment of chromoblastomysocis
combo with ampB - NOT used alone due to resistance

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37
Q

why does Flucytosine have high resistance levels

A

caused by fungi decreased levels of targeted enzymes

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38
Q

What are the pharmacokinetics of Flucytosine

A

oral
can cross BBB
dose adjust in renal impaired

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39
Q

what are the AE/Contraindications of Flucytosine

A

reversible neutropenia, thrombocytopenia and hepatic dysfunction
dose-related bone marrow suppression
More common: N/V/D

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40
Q

What are the uses of Ketoconazole

A

systemic and superficial mycoses
candida, histoplasma, blastomyces, coccidiioides NOT aspergillius
DO NOT use in combo with ampB

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41
Q

what causes the resistance to Ketoconazole

A

mutations in C-14 alpha-demethlyase gene -> decreased binding of drug
stains can pump drug out of cells

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42
Q

what is the MOA for Ketoconazole

A

inhibits C-14alpha-demethylase -> blocks demethylation of lanosterol to ergosterol -> disrupts membrane synthesis

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43
Q

What are the pharmacokinetics of Ketoconazole

A

oral or topical
requires gastric acid for dissolution and absorption
does NOT penetrate CSF
Hepatic metabolism

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44
Q

What are the AE/contraindications of Ketoconazole

A

N/V, hepatic necrosis
endocrine effects: gynecomastia, decreased libido, menstrual irregularities
may increase toxicities of drugs metabolized by CPY450

contra: pregnancy

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45
Q

What are the uses of clotrimazole

A

superficial mycoses, too toxic for systemic use
ringworm, candida

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46
Q

what is the MOA for clotrimazole

A

inhibits C-14alpha-demethylase -> blocks demethylation of lanosterol to ergosterol -> disrupts membrane synthesis

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47
Q

What are the pharmacokinetics of clotrimazole

A

topical

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48
Q

what are the AE/contraindications of Clortimazole

A

contact dermatitis, vulvar irritation, edema

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49
Q

What are the uses of Fluconazole

A

systemic and superficial mycoses
candida, cryptococcus, coccidioides
NO activity against aspergillus

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50
Q

what is the MOA for fluconazole

A

inhibits C-14alpha-methylase -> blocks demethylation of lanosterol to ergosterol -> disrupts membrane synthesis

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51
Q

what are the pharmacokinetics of fluconazole

A

oral or IV admin, not dependent on gastric acid
good CSF penetration
dose adjust in renal impairment

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52
Q

what are the AE/contraindications for Fluconazole

A

Nausea, HA, rashes, alopecia, SJS
Hepatitis rare

contra: pregnancy

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53
Q

what are the uses of Itraconazole

A

systemic and superficial ycoses
DOC for blastomycosis, histoplasmosis, and sporotrichosis

alternative to ampB for aspergillosis, candidiasis, and coccidioidomycosis

54
Q

what is the MOA for Itraconazole

A

inhibit C-14alpha-methylase -> blocks C-14alpha-demethylation of ianosterol to ergosterol -> disrupts membrane synthesis

55
Q

what are the pharmacokinetics of Itraconazole

A

oral admin, requires gastric acid for absoprtion
hepatic metabolism
no dose-adjustment in renal impairment
poor CSF penetration

56
Q

what are the pharmacokinetics of Itraconazole

A

oral admin, requires gastric acid for absorption
hepatic metabolism
no dose-adjustment in renal impairment
poor CSF penetration

57
Q

What are the AE/contraindications for Itraconazole

A

GI upset, rash, HA, alopecia, abd pain, edema, HTn, hypokalemia, hepatitis rare
serious: Cardiac suppression and liver injury
inhibits CYP3A4-> increase levels of many other drugs

contra: pregnancy, CHF

58
Q

What are the uses of Capsofungin

A

systemic mycoses, second line to vericonazole
aspergillus, candida
better tolerated than ampB
NOT active against zygomycetes and crytococcus neoformans

59
Q

what is the MOA of Capsofungin

A

inhibits synthesis of beta-1,3-d-glucan and disrupts fungal cell wall

60
Q

what are the pharmacokinetics of Capsofungin

A

IV
half life of 9-11 hours
CNS penetration is poor

61
Q

What are the AE/contraindications of Capsofungin

A

well tolerated
histamine reaction with infusion
drug interactions with cyclosporine, tacrolimus, rifampin

62
Q

how do you avoid histamine reaction with capsofungin

A

pretreat with diphenhydramine (benadryl)

63
Q

What are the uses of Griseofulvin

A

superficial mycoses
dermatophytic infections of the skin, hair and nails
accumulates in keratin-containing tissue

64
Q

what is the MOA for Griseofulvin

A

binds to components of microtubules -> inhibits mitosis

65
Q

what are the pharmacokinetics of Griseofulvin

A

oral
treatment may be required for 6-12 months

66
Q

what are the AE/contraindications with Griseofulvin

A

avoid alcohol
induces CYP enzymes

contra: pregnancy and patients with porphyria

67
Q

what are the uses of Terbinafine

A

superficial mycoses
highly active against dermatophytes and less active against candida species

DOC for onychomycosis

68
Q

What is the MOA of Terbinafine

A

inhibits squalene epoxidase with resultant inhibition of ergosterol synthesis -> inhibits cell wall synthesis

69
Q

what are the pharmacokinetics of Terbinafine

A

oral and topical
6-12 weeks of treatment

70
Q

What needs to be monitored with Terbinafine treatment

A

LFTs

71
Q

what are the AE/Contraindications of terbinafine

A

diarrhea, dyspepsia, nausea, HA, rash, hepatotoxicity

Contra: lactating women

72
Q

What are the antifungal medications

A

Amphotericin B
Nystatin
Flucytosine
Ketoconazole
Clotrimazole
Fluconazole
Intraconazole
Capsofungin
Griseofulvin
terbinafine

73
Q

What are the uses of Oseltamivir

A

aka Tamiflu
influenza A and B, decrease course of dz and can be used for prophylaxis
treat patients with higher risk; children <3, adults >65yo, pregnant, pts with comorbidities, morbidly obese, nursing homes

74
Q

What is the MOA for Oseltamivir

A

Inhibits neuroamidase, enzyme essential for cleaving virus from its host cell

75
Q

What are the pharmacokinetics of Oseltamivir

A

oral - prodrug that is hydrolyzed by the liver to active form
must be admin within 24 -48 hours of symptom onset
dose-adjust in renal impairment

76
Q

what are the AE/contraindications of Oseltamivir

A

N/V
take with food to minimize GI effects

77
Q

what are the uses of amantadine

A

currently ineffective for viral infections due to rate of resistance
used in PD

78
Q

what is the MOA for amantadine

A

inhibits M2 protein

79
Q

what are the anti-viral flu medications

A

Oseltamivir (tamiflu)
amantadine (high rate resistance)

80
Q

What are the uses of Acyclovir

A

HSV-1, HSV-2, VZV
NO activity against CMV
resistance is building especially in immunocompromised patients

81
Q

what causes the resistance to Acyclovir

A

mutation or loss of viral thymidine kinase

82
Q

What is the MOA of Acyclovir

A

guanosine analogue that inhibits viral DNA polymerase by chain termination - > inhibits transcription
activated by viral thymidine kinase in infected cells

83
Q

what are the pharmacokinetics of acyclovir

A

oral, topical, or IV admin
oral bioavailability low, requires frequent dosing
dose adjust in renal impairment

84
Q

what are the AE/contraindications of Acyclovir

A

oral: N/V/D, Ha, vertigo
Topical: local burning sensation
IV: renal failure - can crystalize in renal tubules, neurotoxicity

85
Q

what are the uses of Valacyclovir

A

HSV-1, HSV-2, VZV
NO activity against CMV
5x more expensive than Acyclovir

86
Q

what is the MOA of Valacyclovir

A

guanosine analogue that inhibits viral DNA polymerase by chan termination -> inhibits transcription
activated by viral thymidine kinase in infected cells

87
Q

what are the pharmacokinetics of Valacyclovir

A

prodrug, hydrolyzed to acyclovir in intestines and liver
oral admin
higher bioavailability
3x/day admin

88
Q

what are the AE/contraindications of Valacyclovir

A

N/V/D, HA, vertigo
HA more common than acyclovir

89
Q

what are the uses of Famciclovir

A

HSV-1, HSV-2 and VZV
No activity against CMV

90
Q

what is the MOA for Famciclovir

A

selectively inhibits viral DNA plymerase by chain termination -> inhibits transcription
activated by viral thymidine kinase in infected cells

91
Q

what are the pharmacokinetics of Famciclovir

A

prodrug of penciclovir, undergoes intracellular conversion to penciclovir triphosphate

92
Q

what are the AE/contraindications of Famciclovir

A

N/V, HA

93
Q

what are the uses of Foscarnet

A

CMV retinitis and acyclovir-resistant mucocutatneous HSV and VVZV infection in immunocompromised

94
Q

what is the MOA of Foscarnet

A

reversibly blocks pyrophosphate binding site of viral DNA polymerase -> inhibits transcription

95
Q

what are the pharmacokinetics of Foscarnet

A

IV admin only
active as administered
dose adjust in renal impairment

96
Q

what are the AE/contraindications of Foscarnet

A

Fever, N/V/D, anemia, HA, fatigue, tremor, irritability, elevated liver enzymes
nephrotoxicity, electrolyte/mineral imbalances, seizures, blood disorders, QT prolongation, dysrhythmias

97
Q

What are the medications against herpes viruses

A

acyclovir
valcyclovir
famciclovir
foscarnet

98
Q

what are the uses of interferons

A

treatment of HBC and HCV, usually as part of a combination
rarely first line treatment
many other potential uses

99
Q

what is the MOA for interferons

A

thought to induce gene transcription of host cell enzymes that inhibit viral RNA
increase phagocytic activity of macrophages
increase cytotoxicity of lymphocytes for target cells

100
Q

what are the pharmacokinetics of interferons

A

IV or SubQ
never oral
dose adjust in severe renal disease

101
Q

what are the AE/contraindications of Interferons

A

flu-like sx after admin
mood disorders, depression, somnolence, confusion, profound fatigue, weight loss, seizures, myelosuppression, rash, cough, myalgia, alopecia, tinnitus, reversible hearing loss, retinopathy, pneumonitis, cardiotoxicity, autoimmune reaction

102
Q

what are the uses of Lamivudine

A

HBV
can be used in HIV-HBV co-infection
growing resistance

103
Q

what is the MOA of Lamivudine

A

cytosine analog that inhibits HBV DNA polymerase and works against HIV reverse transcriptase -> inhibits viral DNA synthesis

104
Q

What are the pharmacokinetics of Lamivudine

A

oral admin, good absorption
dose adjust in renal impairment

105
Q

what are the AE/contraindications of Lamivudine

A

HA, dizziness, pancreatitis
rare: lactic acidosis and hepatomegaly

106
Q

what are the uses of Entecavir

A

HBV
weakly active against HIV
typically second-line, not preferred for lamivudine-resistance strains

107
Q

what is the MOA of Entecavir

A

phosphorylated to guanosine triphosphase; competes as substrate for HBV DNA polymerase thereby inhibiting the enzyme -> inhibits viral DNA synthesis

108
Q

what are the pharmacokinetics of Entecavir

A

oral
dose adjust in renal impairment

109
Q

what are the AE/contraindications of entecavir

A

may cause increase ALT levels, mild GI upset, mild hyperglycemia, HA
Rare: lactic acidosis and hepatomegaly

110
Q

what are the uses of Tenofovir

A

HBV
typically second-line but PREFERRED for lamivudine-resistance strains

111
Q

what is the MOA of Tenofovir

A

Binds HBV DNA polymerase and works against HIV reverse transcriptase -> inhibits replication of HBV

112
Q

what are the pharmacokinetics of Tenofovir

A

2 formulations available: tenofovir disoproxil fumarate and tenofovir alafenamide
dose adjust in renal impairment

113
Q

what are the AE/contraindications of tenofovir

A

GI effects, rash, hypercholesterolemia, decreased bone mineral density
rare: lactic acidosis and hepatomegaly

114
Q

what are the uses of Ribavirin

A

HCV, usually in combo with interferons
NOT preferred treatemnt
severe pediatric RSV

115
Q

what is the MOA of Ribavirin

A

inhibits guanine nucleotide synthesis -> inhibits viral transcription and RNA replication

116
Q

what are the pharmacokinetics of Ribavirin

A

oral
aerosolized for children

117
Q

what are the AE/contraindications of Ribavirin

A

hemolytic anemia
contra: pregnancy

118
Q

what are the uses of Ledipasvir

A

direct-acting anativiral
HCV
newer and more expensive

119
Q

what is the MOA of Ledipasvir

A

inhibits NS5A protein which plays a role in both viral replication and the assembly of HCV

120
Q

what are the pharmacokinetics of Ledipasvir

A

oral
increase gastric pH levels 9more alkalotic) may decrease absorption)

121
Q

what are the AE/contraindications of Ledipasvir

A

generally well tolerated
be careful with co-admin with PPIs

122
Q

what are the uses of Sofosbuvir

A

direct-acting antiviral
HCV
newer and more expensive
commonly given in combo tablet with Ledipasvir

123
Q

what is the MOA of Sofosbuvir

A

inhibits HS5B protein which plays a role both viral replication and assembly of HCV

124
Q

what are the pharmacokinetics of Sofosbuvir

A

oral
activated by metabolism

125
Q

what are the AE/contraindications of Sofosbuvir

A

HA, fatigue, insomnia
avoid with rifampin , rifapentine, carbamazepine, phenytoin, phenobarbital, oxcarbazepine, tipranavir/ritonavir, amiodarone

126
Q

What are the antivirals against hepatoviruses

A

interferons
lamivudine
entecavir
tenofovir
ribavirin
ledipasvir
sofosbuvir

127
Q

What are nemotodes

A

round worms

128
Q

what are cestodes

A

flat forms

129
Q

what are trematodes

A

flukes

130
Q

what are rhizopods

A

amoeba

pharm 2 mod 4: fungals/microbials (3 decks)

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