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Block7 > PDA anti-everything else > Flashcards

PDA anti-everything else Flashcards

1
Q

What increases risk for TB?

A

socioeconic very low
TB-endemic area travel or immigration
immunocompromised

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2
Q

What are the challeges of antimycobacterial therapy?

A

difficult to kill
vunerable to -cidal drugs only when metabolically active
small population semi-dormant
slow growth-hampers identification/susceptibility
lengthy therapy
intracellular forms
chronic disease
spontaneous resistance requires multi-drug therapy

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3
Q

What are the side effects of isoniazid?

A

hepatotoxicity
neurotoxicity-peripheral neuritits
improved with pyridoxine and vitamin B6 admin

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4
Q

What drugs are first line TB drugs?

A 
Isoniazid
Rifampin
Ethambutol
Pyrazinamide
Streptomycin
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5
Q

What is isoniazid mechanism of action?

A

inhibits synthesis of mycolic acid by targeting the enoyl acyl carrier protein reductase
activated by catalse peroxidase
cidal for actively growin bacilli

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6
Q

What is resistance to isoniazid?

A

very high up to 25% in some cities, spontaneous resistance

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7
Q

What is isoniazid use?

A

primary TB drug most important; given in combination
Tx active TB given in combination
can be given alone for latent TB

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8
Q

What are the side effects of RIfampin?

A

Hepatotoxicity and inducer of multiple CYPs

orange-red color of body secretions

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9
Q

What is the mechanism of action of Ethambutol?

A

interferes with arabinosyl transferase blocking cell wall syntehsis
Tuberculostatic and enhances the permeability for drugs

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10
Q

What are the side effects of ethambutol?

A

well-distributed generally well tolerated but causes optic neuritis
decreased visual acuity or loss of ability to differentiate red-green

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11
Q

What is mechanism of action of pyrazinamide?

A

blocks mycolic acid syntehsis by inhibiting fatty acid synthase I, -cidal

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12
Q

Pyrazinamide is particulary useful for TB with what involvement?

A

CNS involvement because of distribution

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13
Q

What are the adverse effects of Pyrazinamide?

A

hepatic damage, adds to hepatotoxicity of other drugs

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14
Q

What is the mechanism of streptomycin?

A

aminoglycoside, binds to several ribisomal sites and cause mRNA misreading
usually reserved for most serious forms of TB

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15
Q

What are the side effects of streptomycin?

A

renal damage

and ototoxciity efecting both balance and hearing

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16
Q

What does tx of short-course uncomplicated TB requrie?

A

isoniazid plus rifampin plus pyrazinamide for the first two months

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17
Q

How does one treat disseminated TB?

A

isoniazid plus rifampin for 9 mos-2yrs and others for first two months

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18
Q

Why use simultaneous 4 or more drugs?

A

disseminated disease, meningitis, known exposures to drug-resistant strains, severe pulmonary disease

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19
Q

How does one treat XDR TB?

A

5 or more drug treatments at once

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20
Q

What are atypical mycobacterial infections?

A

MAC= m. avium intracellulare complex
among most frequent opportunistic infections in AIDS
less fatal than TB

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21
Q

What does rifabutin do/ mechanism of action?

A

prophylaxis of MAC

similar to Rifampin but less severe side effects

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22
Q

What is clarithromycin used to treat with regards to mycobacteria?

A

tx of MAC in AIds patients and MAC prophylaxis

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23
Q

What is dapsone sued to treat?

A

leprosy and pneumocystis jiroveci in AIDs pats

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24
Q

What is the mechanism of action of Dapsone?

A

structural analog of para-aminobenzoic acid; inhibits syntehsis of folic acid

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25
Q

What are the side effects of Dapsone?

A

hemolytic anemia
methemoglobinemia
dose depndent

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26
Q

What is teh mechanism of Clofazimine?

A

mechanism poorly understood; somehow binds to DNA and interferest with growth

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27
Q

What is Clofazimine used to treat?

A

Leprosy

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28
Q

What are the adverse side effects of Clofazimine?

A

well tolerated

GI problems and red-brown pigmentation of eyes and skin

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29
Q

What drugs are used to treat leprosy?

A

Clofazimine, Dapsone and Rifampin

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30
Q

What is amphotericin B used to treat?

A

effecctive broad spectrum anti-fingal for most systemic myoces; esp those that are life-threatening
Gold-standard for anti-fungal effectiveness

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31
Q

What is the mechanism of action of amphotericin B?

A

Binds to ergosterol; very lipophilic

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32
Q

Why is hte total cumulative dose of Amphotericin important?

A

permanent renal toxicitiy is related to the total cumulative dose

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33
Q

What is the side effects of amphotericin?

A

fever, nausea, vomiting, headache, chills
hypotension, hypokalemia, tachypnea
90% will show non-permanent renal toxicity
reversble hypochromic, normocytic anemia
cnS side effects

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34
Q

What flucytosine (5-FC) used to treat?

A

serious infections of candida and crytpococcus

used in conjunction wiht amphotericin

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35
Q

What si the mechanism of action of flucytosine?

A

inhibits thymidylate synthetase and thus DNA syntehsis
incorporated in RNA in place of Uracil
fungal cytosine deaminase activates it

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36
Q

What are the side effects of flucytosine?

A

GI
leukopenia, thrombocytopenia
may accumulate in renal insufficiency and dangerous in bone marrow suppresion
elevated hepatic enzymes

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37
Q

What are the two antifungal classes for serious infections?

A

imidazole and triazole

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38
Q

What are the mechanism of actions of imidazole and triazoles?

A

inhibits 14-alpha-sterol demethylase a fungal cytochrom p450 that conferst lanosterol to ergosterol
inhibits ergosterol syntehsis
SLOW onset of action

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39
Q

What is fluconazole used to treat?

A

cryptococcus meningits
Candida many sites including CNS and urinary; some albican and glabrata but not krusei
excreted in urine so good for urinary

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40
Q

What is itraconazole ussed to treat?

A

Blastomyces, histoplasma, candida esophogause and oropharynx

more albican and glabatra some krusei

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41
Q

What is voriconazole used to treat?

A

aspergillus with some CNS coverage

Fusarium, Scedosporium, Candida–>covers most species but not for urinary candida infections

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42
Q

What drug is superior to amphotericin for invasive aspergillus?

A

voriconazole

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43
Q

What azole has best CNS penetration?

A

fluconazole

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44
Q

What are the side effects common to -azoles?

A

mild hepatotoxicity; discontinue with onset of liver dysfunciton
GI, headache
CYP3A and 2C inhibitors

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45
Q

What is the major contraindication of itraconazole?

A

other drugs that are metabolized by CYP3A4; and potential for serious CV events

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46
Q

What azole has lowest incidence of hepatotoxicity?

A

fluconazole

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47
Q

What unusal side effects do voriconazole have?

A

visual disturbance and photosensitive component to rash

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48
Q

What anti-fungals target the cell wall?

A

caspofungin*
micafungin
anidulafungin

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49
Q

What is Caspofungin used to treat?

A

aspergillus-invasive

Candida with wide coverage

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50
Q

What is mechanism of action fo capsofungin?

A

inhibits fungal cell wall ysntehsis by noncompetively blocking syntehsis of Beta-D-glucan in filamentous fungi
No cross resistance mechanisms

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51
Q

What are the side effects fo capsofungin?

A

phlebitis at injection site
GI effects
some pulm edema but generally well tolerated

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52
Q

Fluconazole is used to treat what other than serious infections?

A

superficial fungi; often one oral dose all thats required

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53
Q

miconazole is used to treat what?

A

creams/suppositories to treat vaginal infections

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54
Q

What is clotrimazole used to treat?

A

candida; topical use

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55
Q

Nystatin is what mechanism of action?

A

similar to amphotericin B

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56
Q

What is nystatin used to treat?

A

superficial fungi; for -azole resistant strains

topical use for candida and GI tract

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57
Q

What are the side effects fo Nystatin?

A

Some GI side effects but topical well toleratied

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58
Q

What is natamycin used for?

A

opthalmic infections by fungal infectionss

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59
Q

What is mechanism of action of natamycin?

A

similar to amphotericin B; too toxic for systemic

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60
Q

What are used for topical treatment of dermatophytes?

A

miconazole, clotrimazole
tolnaftate-
terbinafine
ciclopirox

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61
Q

What is mechanism of action of tolnaftate?

A

likely inhibits fungal ergosterol syntehsis

few toxic reactions topical only

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62
Q

What is ciclopriox used for?

A

approved topical tx for mild to moderate fungal nail infections

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63
Q

What is the ciclopirox mechanism of action?

A

inhibits metal-depndent fungal enzymes by metal chelation is the believed mechanism

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64
Q

What are the oral preapartions of dermatophyte used for?

A

severe dermatophyte infections

those that are resistant

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65
Q

What is terbinafine used for?

A

12-week thereapy for nail infections

shorter for other dermatophytic infections

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66
Q

What is the mechanism of action of terbinafine?

A

deposits in skin and nails leadign to prolonged effect

blocks ergosterol syntehsis and causes accumulation of squame which is toxic to fungi

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67
Q

What are the side effects of terbinafine?

A

diarrhea dyspepia, GI

well tolerated in general

68
Q

What is griseofulvin tx?

A

for recalcitrant dermatophytic infections of skin, hair, nails
tx for children esp tinea capitis

69
Q

What is the mechanism of aciton of griseofulvin?

A

interferes wtih microtubule function

70
Q

What are the side effects of griseofulvin?

A

well tolerated
contraindicated in those with porphyria and advanced liver disease
increased metabolism by CYP inducer
used in caution in those with penicillin allergies

71
Q

Itraconazole is used to treat what in addition to systemic fuunals?

A

dermatophytes, superficial

72
Q

Inner city children are more likely to have what parasite?

A

roundworms

73
Q

What does mebendazole treat?

A

many of the roundworm species

kill some ova

74
Q

Why does mebendazole have few systemic side effects?

A

poorly absorbed

75
Q

What does albendazole treat?

A

Echinococcus

cutaneous larval migrans

76
Q

What rae hte problems with albendazole metabolism?

A

Well distributed and causes elevated hepatic enzme

abdominal pain vomitting

77
Q

What does Thiabendazole used to treat?

A

stronglyoides, cutaneous larva migrans

78
Q

What is the mechanism of thiabendazole?

A

hook worm inhibits energy metabolism, mitochondrial fumarate reductase
strongyloides blocks microtubule assembly

79
Q

What is mechanism of action of mebendazole?

A

immobilizes and kills parasites by selective microtubule damage

80
Q

What is the mechanism of action of pyrantel pamoate?

A

depolarizing neuromucular blocker

81
Q

What is pyrantel pamoate used for?

A

hookworm, pinworm and roundworm

OTC for pinworm

82
Q

Why does pyrantel pamoate have few side effects?

A

poorly absorbed resulting in only mild GI side effeccts

83
Q

What is praziquantel mechansim of action?

A

increase calcium permeability causing spastic paralysis

84
Q

What is praziquantel side effects?

A

abdominal discomfor and nausea

85
Q

What is praziquantel used for?

A

flukes; drug of choice for shicstosoma and some activity against other trematodes

86
Q

What is praziquantel used for besides flukes?

A

off label for many cestodes(tapeworms)

for Taneia solium b/c also kill egss thereby avoiding cysticerosis

87
Q

What is albendazole used to treat besides roundworms?

A

neurocysticerosis

88
Q

What is paromomycin sulfate used for?

A

3rd choice for those who can’t handle other drugs for tapeworms

89
Q

What are antimalarial drugs used for?

A

none prevent infections; only prevent progression to symptomatic infection

90
Q

What is chloroquine used for?

A

anti-malarial
malarial prophylaxis
effective for all 4 species; not effective for chloroqine sensitive strains;

91
Q

What is the mechanism of action of chloroquine?

A

blood schizonticide
parasitic erythrocytes concetnrates teh drug 25 fold by pH dependent mechanism intoo acidic vacuoles; inhibitis heme polymerization allowing heme to accumulate to toxic levels for parasites

92
Q

What malaria is mostly resistant to chloroquine?

A

P. falciparum

93
Q

What ar ethe side effects of chloroquine?

A

visual impairment with extended use but generally well tolerated

94
Q

What is mfeloquine mechanism?

A

similar to chloroquine

95
Q

What does mefloquine treat?

A

P. falciparum and P. vivaz

tx or prevention of malaria

96
Q

What side effect does meloquine cause?

A

contraindicated in ppl with epilepsy or psychiatric disorders
psychiatric effects
-8% of men
vestibular effects

97
Q

What is the Atovquone and proguanil used to treat?

A

block schizonticides

block and tx of chloroquine resistant P. falciparum

98
Q

What is the mech of action of Atovaquone and Proguanil?

A

atovaquone selectively inhibits malarial electron transport and disrupts pyrimidine synthesis
proguanil disrupts folate syntehsiss preventidng pyramidine synthesis

99
Q

What are the side effects of Atovquone and proguanil>

A

nausea, diarrhea, vomiting and rash

100
Q

What is quinine?

A

bark of cinchona tree

101
Q

What is mechanism of quinine?

A

mechanims similar to chloroquine

102
Q

What is quinine used to treat?

A

blood schizonticide all four malarial parasites

severe malarial attack

103
Q

What is quinine side effects?

A

cinchonism-headache, visual distrubance, dizziness, tinnitues
cardiac effects similar to quinidine
Gastric irritation

104
Q

What is doxycycline used in addition to antibacterial?

A

decreases malarial syntehsis
depresses dihydroorate synthesis
combats malari

105
Q

What is primaquine used to treat?

A

kill liver hypnozoites
radical cure/terminal prophylaxis of P. vivax and ovale
Pneumocystis jiroveci pneumonia in AIDs in combination with an antibacteria

106
Q

What is primaquine side effects?

A

hemolytic reactions in those wiht G6P dehydrogenase deficiency

107
Q

What is the treatment for amebic dysentery?

A

metronidazole pluse either idoquinol or paromomycil sulfate

108
Q

What is used to treat Giardia and Tirchomonas vaginals?

A

metronidazole

109
Q

What is used to treat nitrazoxanide?

A

giardia and cryptosporidium parvum

110
Q

What is used to treat pneumocystis jiroveci as a prophylaxis or treamnet as an alternative for intolerance of TMP/SMX?

A

Atovaquone

111
Q

What is amantadine used to treat?

A

Influenza A; reduces fever by 50%

112
Q

What is the mechanism of action of Amantadine?

A

blocks viral uncoating by interfering with viral uncoating by interefering M2 protein the ion channel

113
Q

What are the amantadine side effects?

A

CNS effects; confusion, slurred speach, depression, headache, hallucinations

114
Q

WHat is the mechanism of action of oseltamivir?

A

inactive pprodrug converted to oseltamivir carobxylate competiviely inhibits neuramidiases interferres with viral release and viral pen

115
Q

What is the approved use of oseltamivir?

A

treatment of influenza A and B; only effective if given within 48 hours of onset

116
Q

What are the side effects of oseltamivir?

A

nausea, vomiting and diarreha
bronchitis and cough
well tolerated

117
Q

What is mechanism of action of trifluridine?

A

thymidine analog interferes with DNA synthesis

118
Q

What is trifluridine used for?

A

opthalmic use only treatment of herpes simplex type 1 and 2

119
Q

Acyclovir has what mechanism of action?

A

inhibits herpes DNA polymerase 10-30 times more effectively than host cell DNA polymerase
occurs after it is phosphorylated

120
Q

What is the intravenous acyclovir used for?

A

serious systemic herpes virus

HSV encephalitis

121
Q

What is acyclovir orally used for?

A

primary genital herpes

primary herpes in the mouth or face region for

122
Q

What is topical acyclovir used for?

A

mild herpes

123
Q

What are the side effects of acyclovir?

A

well tolerated
rash, itching
GI upset

124
Q

What is the mechanism of action of Famciclovir?

A

Prodrug activated by complex with multiple intermediates

herpes thymidine similar to acyclovir after activated

125
Q

What is the use of famciclovir?

A

acute herpes zoster (shingles) (latent chickenpox virus)

tx and suppression of current genital herpes

126
Q

What is the mechanism of penciclovir?

A

activated for of famciclovir but can be given straight but only topically
very similar to acyclovir

127
Q

What is the use of penciclovir?

A

recurrent herpes of the lips and face

topical Administration

128
Q

What is the importance of CMV in pts with HIV?

A

retinitis can be caused by it or GI, CNS, respiratory, adrenal

129
Q

What is the mechanism of ganciclovir??

A

mechanism similar to acyclovir, except mono-phos. by CMV protein kinase

130
Q

What is the use of ganciclovir?

A

CMV retinitis in AIDS pts

CMV prophylaxis for transplant pts

131
Q

What are the side effects of Ganciclovir?

A

bone marrow suppression

-

132
Q

What is foscarnet mechanism of action?/

A

inhibits CMV DNA polymerase by binding to its pyrophosphate site
doesn’t requrie activation

133
Q

What is Foscarrnet used for?

A

CMV retinitis

acyclovir-resistant herpes simplex

134
Q

What are the side effects of Foscarnet?

A

some side effects

  • renal damage
  • electrolyte imbalance
  • seizures
  • higher % of side effects
135
Q

What is the mechanism of action of Lamivudine?

A

inhibits the reverse transcriptase domain of hte hepatitis B DNA polymerase
Nucleoside analg phosphorylated by cell enzymes to active form

136
Q

What is Lamivudine used to treat?

A

HIV and hepatitis B

137
Q

What are the side effects of Lamivudine?

A

GI effects pretty common;

otherwise well tolerated

138
Q

What is the mechanism of action of Tenofovir?

A

adenosine monophosphate analog

139
Q

What si tenofovir used to treat?

A

hepatitis BW

140
Q

What is the mechanism of Ribavirin?

A

nucleoside analog
interferes with viral mRNA synthesis
Moono-P form inhibits inosine-5’ dehydrogenase and therefore GTP syntehsis
Tri-P form inhibits GTP dependent capping

141
Q

What is the use of aerosol use of Ribavirin?

A

severe RSV infections in young children; no longer used

142
Q

What are the oral capsules of Ribavirin used for?

A

hepatitis C in combination with PEG-interferon-alpha

143
Q

What are the side effects of RIbavirin?

A

drug may precipitate in and clog respiratory equipment
pulmonary function deterioration
IV or oral
anemia, bone marrow suppression

144
Q

What are hte alpha interferons used for?

A

condyloma acuminata

hep B and C; used in combination with ribavarina nd boceprevir for hep C

145
Q

What is the side effects fo interferon alpha?

A

flu-like syndrome
leukopenia, bone marrow suppresion
neurotoxicity, myalgia

146
Q

What is hte mechanism of Boceprevir?

A

reversible inhibitor of NS3 protease of hepatitis C, blocks formation of infectious virus

147
Q

What is Boceprevir used for?

A

Hep C genotype 1

148
Q

What combination of drugs i the most efefctive tx for hep C genotype 1?

A

interferon alpha, boceprevir, ribavirin

149
Q

What are the side effects of boceprevir?

A

bone marrow suppression

CYP3A4 inhibitor

150
Q

What is zidovudine?

A

first anti-HIV drug

151
Q

What is the mechanism of action of zidovudine?

A

thymidine analog;

152
Q

What are the side effects of Zidovudine?

A

bone marrow suppression
neutropenia, anemia
avoid drugs which inhibit glucuronyl transferase
myopathy

153
Q

What are the mechanism of action of other NRTIs

A

nucleoside analogs that must be phosphorylated

154
Q

What is used to treat HIV that is an analog of lamivudine?

A

Emtricitabine

155
Q

What is the mechanism of abacavir?

A

nucleoside analog inhibitor of RT

156
Q

What are the side effects of abacavir?

A

hypersensitivity

157
Q

What are the side effects associated with NRTI’s?

A

lactic acidosis

hepatic steatosis

158
Q

What is the mechanism of efavirenz?

A

non-nucleoside reverse transcriptase inhibitor;

binds RT and disrupts teh active site

159
Q

What are the side effects of Efavirenz?

A

CNS/ psychiatric symptoms, nightmares

GI upset

160
Q

What are hte toxicities common to protease inhibitors?

A 
diabetes
alterations in lipid metabolism
fat redistriution
alters metabolism of many other drugs
CYP3A inhibitors
161
Q

What is Ritonavir used for?

A

used to boost levels of other protease inhibitors bc blocks their metabolism by CYP3A
potent inhibitor

162
Q

What is the mechanism of action of enfuviritide?

A

binds to gp41 subunit of HIV glycoprotein; blocks conformational changes required for membrane fusion to CD4 cells

163
Q

What are the side effects of Enfuvirtide?

A

local injection site reactions

GI upset

164
Q

What is the mechanism of Maraviroc?

A

CCR5 antagonist; tx of HIV-1

effective in strains resistant to other drugs

165
Q

What is raltegravir used for?

A

tx of HIV-1 and works on virust that is resistant to other drugs

166
Q

Whatis mechanism of raltegrivir?

A

inhibits HIV-1 integrase activity

preventing integration of HIV-1 in new and tx expereinced pts

Block7 (10 decks)

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