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Flashcards in PDA anti-everything else Deck (166):
1

What increases risk for TB?

socioeconic very low
TB-endemic area travel or immigration
immunocompromised

2

What are the challeges of antimycobacterial therapy?

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

3

What are the side effects of isoniazid?

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

4

What drugs are first line TB drugs?

Isoniazid
Rifampin
Ethambutol
Pyrazinamide
Streptomycin

5

What is isoniazid mechanism of action?

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

6

What is resistance to isoniazid?

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

7

What is isoniazid use?

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

8

What are the side effects of RIfampin?

Hepatotoxicity and inducer of multiple CYPs
orange-red color of body secretions

9

What is the mechanism of action of Ethambutol?

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

10

What are the side effects of ethambutol?

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

11

What is mechanism of action of pyrazinamide?

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

12

Pyrazinamide is particulary useful for TB with what involvement?

CNS involvement because of distribution

13

What are the adverse effects of Pyrazinamide?

hepatic damage, adds to hepatotoxicity of other drugs

14

What is the mechanism of streptomycin?

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

15

What are the side effects of streptomycin?

renal damage
and ototoxciity efecting both balance and hearing

16

What does tx of short-course uncomplicated TB requrie?

isoniazid plus rifampin plus pyrazinamide for the first two months

17

How does one treat disseminated TB?

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

18

Why use simultaneous 4 or more drugs?

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

19

How does one treat XDR TB?

5 or more drug treatments at once

20

What are atypical mycobacterial infections?

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

21

What does rifabutin do/ mechanism of action?

prophylaxis of MAC
similar to Rifampin but less severe side effects

22

What is clarithromycin used to treat with regards to mycobacteria?

tx of MAC in AIds patients and MAC prophylaxis

23

What is dapsone sued to treat?

leprosy and pneumocystis jiroveci in AIDs pats

24

What is the mechanism of action of Dapsone?

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

25

What are the side effects of Dapsone?

hemolytic anemia
methemoglobinemia
dose depndent

26

What is teh mechanism of Clofazimine?

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

27

What is Clofazimine used to treat?

Leprosy

28

What are the adverse side effects of Clofazimine?

well tolerated
GI problems and red-brown pigmentation of eyes and skin

29

What drugs are used to treat leprosy?

Clofazimine, Dapsone and Rifampin

30

What is amphotericin B used to treat?

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

31

What is the mechanism of action of amphotericin B?

Binds to ergosterol; very lipophilic

32

Why is hte total cumulative dose of Amphotericin important?

permanent renal toxicitiy is related to the total cumulative dose

33

What is the side effects of amphotericin?

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

34

What flucytosine (5-FC) used to treat?

serious infections of candida and crytpococcus
used in conjunction wiht amphotericin

35

What si the mechanism of action of flucytosine?

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

36

What are the side effects of flucytosine?

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

37

What are the two antifungal classes for serious infections?

imidazole and triazole

38

What are the mechanism of actions of imidazole and triazoles?

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

39

What is fluconazole used to treat?

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

40

What is itraconazole ussed to treat?

Blastomyces, histoplasma, candida esophogause and oropharynx
more albican and glabatra some krusei

41

What is voriconazole used to treat?

aspergillus with some CNS coverage
Fusarium, Scedosporium, Candida-->covers most species but not for urinary candida infections

42

What drug is superior to amphotericin for invasive aspergillus?

voriconazole

43

What azole has best CNS penetration?

fluconazole

44

What are the side effects common to -azoles?

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

45

What is the major contraindication of itraconazole?

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

46

What azole has lowest incidence of hepatotoxicity?

fluconazole

47

What unusal side effects do voriconazole have?

visual disturbance and photosensitive component to rash

48

What anti-fungals target the cell wall?

caspofungin*
micafungin
anidulafungin

49

What is Caspofungin used to treat?

aspergillus-invasive
Candida with wide coverage

50

What is mechanism of action fo capsofungin?

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

51

What are the side effects fo capsofungin?

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

52

Fluconazole is used to treat what other than serious infections?

superficial fungi; often one oral dose all thats required

53

miconazole is used to treat what?

creams/suppositories to treat vaginal infections

54

What is clotrimazole used to treat?

candida; topical use

55

Nystatin is what mechanism of action?

similar to amphotericin B

56

What is nystatin used to treat?

superficial fungi; for -azole resistant strains
topical use for candida and GI tract

57

What are the side effects fo Nystatin?

Some GI side effects but topical well toleratied

58

What is natamycin used for?

opthalmic infections by fungal infectionss

59

What is mechanism of action of natamycin?

similar to amphotericin B; too toxic for systemic

60

What are used for topical treatment of dermatophytes?

miconazole, clotrimazole
tolnaftate-
terbinafine
ciclopirox

61

What is mechanism of action of tolnaftate?

likely inhibits fungal ergosterol syntehsis
few toxic reactions topical only

62

What is ciclopriox used for?

approved topical tx for mild to moderate fungal nail infections

63

What is the ciclopirox mechanism of action?

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

64

What are the oral preapartions of dermatophyte used for?

severe dermatophyte infections
those that are resistant

65

What is terbinafine used for?

12-week thereapy for nail infections
shorter for other dermatophytic infections

66

What is the mechanism of action of terbinafine?

deposits in skin and nails leadign to prolonged effect
blocks ergosterol syntehsis and causes accumulation of squame which is toxic to fungi

67

What are the side effects of terbinafine?

diarrhea dyspepia, GI
well tolerated in general

68

What is griseofulvin tx?

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

69

What is the mechanism of aciton of griseofulvin?

interferes wtih microtubule function

70

What are the side effects of griseofulvin?

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

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

dermatophytes, superficial

72

Inner city children are more likely to have what parasite?

roundworms

73

What does mebendazole treat?

many of the roundworm species
kill some ova

74

Why does mebendazole have few systemic side effects?

poorly absorbed

75

What does albendazole treat?

Echinococcus
cutaneous larval migrans

76

What rae hte problems with albendazole metabolism?

Well distributed and causes elevated hepatic enzme
abdominal pain vomitting

77

What does Thiabendazole used to treat?

stronglyoides, cutaneous larva migrans

78

What is the mechanism of thiabendazole?

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

79

What is mechanism of action of mebendazole?

immobilizes and kills parasites by selective microtubule damage

80

What is the mechanism of action of pyrantel pamoate?

depolarizing neuromucular blocker

81

What is pyrantel pamoate used for?

hookworm, pinworm and roundworm
OTC for pinworm

82

Why does pyrantel pamoate have few side effects?

poorly absorbed resulting in only mild GI side effeccts

83

What is praziquantel mechansim of action?

increase calcium permeability causing spastic paralysis

84

What is praziquantel side effects?

abdominal discomfor and nausea

85

What is praziquantel used for?

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

86

What is praziquantel used for besides flukes?

off label for many cestodes(tapeworms)
for Taneia solium b/c also kill egss thereby avoiding cysticerosis

87

What is albendazole used to treat besides roundworms?

neurocysticerosis

88

What is paromomycin sulfate used for?

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

89

What are antimalarial drugs used for?

none prevent infections; only prevent progression to symptomatic infection

90

What is chloroquine used for?

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

91

What is the mechanism of action of chloroquine?

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

What malaria is mostly resistant to chloroquine?

P. falciparum

93

What ar ethe side effects of chloroquine?

visual impairment with extended use but generally well tolerated

94

What is mfeloquine mechanism?

similar to chloroquine

95

What does mefloquine treat?

P. falciparum and P. vivaz
tx or prevention of malaria

96

What side effect does meloquine cause?

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

97

What is the Atovquone and proguanil used to treat?

block schizonticides
block and tx of chloroquine resistant P. falciparum

98

What is the mech of action of Atovaquone and Proguanil?

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

99

What are the side effects of Atovquone and proguanil>

nausea, diarrhea, vomiting and rash

100

What is quinine?

bark of cinchona tree

101

What is mechanism of quinine?

mechanims similar to chloroquine

102

What is quinine used to treat?

blood schizonticide all four malarial parasites
severe malarial attack

103

What is quinine side effects?

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

104

What is doxycycline used in addition to antibacterial?

decreases malarial syntehsis
depresses dihydroorate synthesis
combats malari

105

What is primaquine used to treat?

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

106

What is primaquine side effects?

hemolytic reactions in those wiht G6P dehydrogenase deficiency

107

What is the treatment for amebic dysentery?

metronidazole pluse either idoquinol or paromomycil sulfate

108

What is used to treat Giardia and Tirchomonas vaginals?

metronidazole

109

What is used to treat nitrazoxanide?

giardia and cryptosporidium parvum

110

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

Atovaquone

111

What is amantadine used to treat?

Influenza A; reduces fever by 50%

112

What is the mechanism of action of Amantadine?

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

113

What are the amantadine side effects?

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

114

WHat is the mechanism of action of oseltamivir?

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

115

What is the approved use of oseltamivir?

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

116

What are the side effects of oseltamivir?

nausea, vomiting and diarreha
bronchitis and cough
well tolerated

117

What is mechanism of action of trifluridine?

thymidine analog interferes with DNA synthesis

118

What is trifluridine used for?

opthalmic use only treatment of herpes simplex type 1 and 2

119

Acyclovir has what mechanism of action?

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

120

What is the intravenous acyclovir used for?

serious systemic herpes virus
HSV encephalitis

121

What is acyclovir orally used for?

primary genital herpes
primary herpes in the mouth or face region for

122

What is topical acyclovir used for?

mild herpes

123

What are the side effects of acyclovir?

well tolerated
rash, itching
GI upset

124

What is the mechanism of action of Famciclovir?

Prodrug activated by complex with multiple intermediates
herpes thymidine similar to acyclovir after activated

125

What is the use of famciclovir?

acute herpes zoster (shingles) (latent chickenpox virus)
tx and suppression of current genital herpes

126

What is the mechanism of penciclovir?

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

127

What is the use of penciclovir?

recurrent herpes of the lips and face
topical Administration

128

What is the importance of CMV in pts with HIV?

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

129

What is the mechanism of ganciclovir??

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

130

What is the use of ganciclovir?

CMV retinitis in AIDS pts
CMV prophylaxis for transplant pts

131

What are the side effects of Ganciclovir?

bone marrow suppression
-

132

What is foscarnet mechanism of action?/

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

133

What is Foscarrnet used for?

CMV retinitis
acyclovir-resistant herpes simplex

134

What are the side effects of Foscarnet?

some side effects
-renal damage
-electrolyte imbalance
-seizures
-higher % of side effects

135

What is the mechanism of action of Lamivudine?

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

136

What is Lamivudine used to treat?

HIV and hepatitis B

137

What are the side effects of Lamivudine?

GI effects pretty common;
otherwise well tolerated

138

What is the mechanism of action of Tenofovir?

adenosine monophosphate analog

139

What si tenofovir used to treat?

hepatitis BW

140

What is the mechanism of Ribavirin?

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

What is the use of aerosol use of Ribavirin?

severe RSV infections in young children; no longer used

142

What are the oral capsules of Ribavirin used for?

hepatitis C in combination with PEG-interferon-alpha

143

What are the side effects of RIbavirin?

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

144

What are hte alpha interferons used for?

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

145

What is the side effects fo interferon alpha?

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

146

What is hte mechanism of Boceprevir?

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

147

What is Boceprevir used for?

Hep C genotype 1

148

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

interferon alpha, boceprevir, ribavirin

149

What are the side effects of boceprevir?

bone marrow suppression

CYP3A4 inhibitor

150

What is zidovudine?

first anti-HIV drug

151

What is the mechanism of action of zidovudine?

thymidine analog;

152

What are the side effects of Zidovudine?

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

153

What are the mechanism of action of other NRTIs

nucleoside analogs that must be phosphorylated

154

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

Emtricitabine

155

What is the mechanism of abacavir?

nucleoside analog inhibitor of RT

156

What are the side effects of abacavir?

hypersensitivity

157

What are the side effects associated with NRTI's?

lactic acidosis
hepatic steatosis

158

What is the mechanism of efavirenz?

non-nucleoside reverse transcriptase inhibitor;
binds RT and disrupts teh active site

159

What are the side effects of Efavirenz?

CNS/ psychiatric symptoms, nightmares
GI upset

160

What are hte toxicities common to protease inhibitors?

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

161

What is Ritonavir used for?

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

162

What is the mechanism of action of enfuviritide?

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

163

What are the side effects of Enfuvirtide?

local injection site reactions
GI upset

164

What is the mechanism of Maraviroc?

CCR5 antagonist; tx of HIV-1
effective in strains resistant to other drugs

165

What is raltegravir used for?

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

166

Whatis mechanism of raltegrivir?

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