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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
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

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