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What is MOA of penicillins, cephalosporins, aztreonam and imipenem?

Block cell wall synthesis by inhibiting crossing linking of peptidoglycan (binding transpeptidases)

1

What is MOA of bacitracin and vancomycin

Block peptidoglycan synthesis

2

What is MOA of sulfonamides/trimethoprim?

Block nucleotide synthesis by inhibiting folic acid synthesis

3

What is th MOA of fluoroquinolnes?

Block DNA topoisomerases

4

What is the MOA of rifampin?

Blocks mRNA synthesis

5

What is th MOA of metronidazole?

Damages DNA

6

What is the MOA of chloramphenicol , macrolides, clindamycin, streptogramins, linezolid?

Inhibits protein synthesis at 50S subunit

7

What is the MOA of amino glycosides and tetracyclines?

Block protein synthesis at 30S ribosomal unit

8

What is the MOA of penicillin?

Bind penicillin binding proteins, transpeptidases, and inhibits cross-linking of the peptidoglycan wall
Activates autolytic enzymes

9

What is the penicillin used for?

Gram positive orgs: s. pneumo, s.pyogenes, actinomyces
Neisseria meningitidis, syphilis

10

Is penicillin bacteriacidal or bacteriostatic?

Cidal

11

What are the side effects of penicillin?

Hypersensitivity reactions
Hemolytic anemia

12

What is the mechanism of resistance to penicillin?

Production of B-lactamases

13

What are the penicillinase-resistant penicillins?

Oxacillin, nafcillin, dicloxacillin

14

What organism are the penicillinase-resistant penicillins used for?

S. aureus

15

What are the side effects of oxacillin, dicloxacillin, nafcillin?

Hypersensitivity
Interstitial nephritis

16

What are the amino penicillins?

Ampicillin
Amoxicillin

17

What are the uses for amino penicillins?

Broader spectrum: H. Flu, Listeria, Proteus, E. coli, Salmonella, Shigella, enterococcus

18

What is the mneumonic for the amino penicillins?

HELPSS:
H.flu
E.coli
Listeria
Proteus
Salmonella
Shigella

19

What are the side effects of amino penicillins?

Hypersensitivity
Rash
Pseudo membranous colitis

20

What is the mech of resistance to amino penicillins?

Production of beta lactamases

21

What is in amoxicillin?

Clavulanic acid - prevents from beta-lactamases

22

What are the anti pseudomonal penicillins?

Ticarcillim, piperacillin

23

What are the anti pseudomonals used for?

Pseudomonas
Gram negative rods

24

What is the side effect of anti-pseudomonals?

Hypersensitivity

25

What are the B-lactamase inhibitors?

CAST:
Clavulanic Acid
Sulfabtam
Tazobactam

26

Why can't you use penicillinase-resistant penicillins against MRSA?

MRSA is resistant because it has an altered penicillin-binding site

27

What are the organisms that are not covered by cephalosporins?

LAME:
Listeria
Atypicals: chlamydia, mycoplasma
MRSA
Enterococci

28

Which cephalosporin can be used for MRSA ?

Ceftaroline

29

What is the advantage of cephalosporin over penicillin?

Less susceptible to b-lactamase

30

Are cephalosporins bacteriostatic or cidal?

Cidal

31

What are the first generation cephalosporins?

Cefazolin
Cephalexin

32

What are the first generation cephalosporins used for?

Gram positives
Proteus
E. coli
Klebsiella

33

What is cefazolin used for?

Used prior to surgery to prevent staph wound infections

34

What are the second generation cephs?

Cefoxitin
Cefaclor
Cefuroxime

35

What are the second generation cephs used for?

Gram positive cocci
HEN PEKS:
H. Flu
Enterobacter
Neisseria
Proteus
E.coli
Klebsiella
Serratia

36

What are the third generation cephalosporins?

Ceftriaxone
Cefoxatime
Ceftazidime

37

What are the third gen cephs used for?

Serious gram negatives that are resistant to other beta-lactams
Neisseria
Pseudomonas

38

What is the 4th gen ceph?

Cefepime

39

What is the 4th gene ceph used for?

Pseudomonas and gram positives.

40

What is the mech of resistance of cephalosporins?

Change in protein structure of the penicillin binding sites

41

What are the side effects of cephalosporins?

Hypersensitivity
Vit K def

42

What is the MOA for aztreonam?

Prevents peptidoglycan cross-linking by binding to PBP3

43

What is aztreonam used for?

Only gram negative rods

44

When is aztreonam used?

When a patient is allergic to penicillin
When a patient has renal insufficiency and can't tolerate amino glycosides

45

What are the side effects of aztreonam?

Well tolerated - occasional GI upset

46

What is imipenem?

Broad spectrum, b-lactamase resistant carbapenem - inhibits cell wall synthesis

47

What is imipenem inactivated by?

Dihydropeptidases in the renal tubules

48

What is cilastatin?

Inhibits dihydropeptidases in renal tubules

49

What is imipenem the DOC for?

Enterobacter

50

What are the other clinical uses of imipenem?

Gram positive cocci
Gram negative rods
Anaerobes

51

What is the advantage or meropenem?

Reduced risk of seizures
Stables in dihydropeptidases

52

What are the side effects of imipenem?

GI
Skin rash
CNS tox - seizures

53

When is imipenem used and why?

In life threatening situations when nothing else has worked because of its side effects

54

What is the MOA of vancomycin?

Inhibits bac wall synthesis by binding to the d-ALA, d-ALA portion of the cell wall precursors

55

Is vancomycin bacteriocidal or bacteriostatic?

Cidal

56

What is vancomycin used for?

Gram positive only: serious multi-drug resistant orgs:
MRSA
enterococcus
C. Difficile

57

What are the side effects of vanc?

Nephrotoxicity
Ototoxicity
Thrombophlebitis
Red man syndrome - prevented with antihistamines and slow infusion rate

58

What is the mech of resistance to vanc?

Change of D-ALA D-ALA to D-ALA D-LAC

59

What are the amino glycosides?

Gentamicin
Neomycin
Amikacin
Tobramycin
Streptomycin

60

Are aminoglycosides bacteriocidal or bacteriostatic?

Cidal

61

What's the MOA of aminoglycosides?

Inhibit formation of the initiation complex causing misreading of mRNA
Block translocation

62

What is required for aminoglycoside uptake?

O2
So not effective against anaerobes

63

What are aminoglycosides used for?

Severe gram negative rod infections:
Chronic UTI
P. aeroginosa
Enterococcus endocarditis

64

What aminoglycoside is used for bowel surgery?

Neomycin

65

What drugs are aminoglycosides synergistic with

B-lactams

66

What is the toxicity of aminoglycosides?

Nephrotoxicity
Ototoxicity
Teratogenicity
Neuromuscular blockade

67

What is the mech of resistance?

Plasmid dependent - carries enzymes that inactivate the aminoglycosides by acetylation, phosphorylation, adenylation

68

Are tetracyclines bacteriocidal or static?

Static

69

What is the MOA of tetracyclines?

Bind to 30s and prevent attachment of aminoacyl-tRNA - inhibits addition of amino acids to growing chains

70

What are tetracyclines used for?

Borrelia
Mycobacterium
Rickettsia
Chlamydia

71

What are the side effects of TC?

GI
Discoloration of teeth
Inhibition of bone growth
Photosensitivity
Teratogenicity

72

What is the mech of resistance against a TC?

Decreased uptake
Or increased efflux by plasmid-encoded transport pumps

73

What is the MOA of macrolides?

Inhibits protein synthesis by blocking translocations
Bind to 23S rRNA and 50S ribsosomal subunit

74

What are the macrolides?

Azithromycin
Clarithromycin
Erythromycin

75

Are macrolides cidal or static?

Static

76

What are the uses of macrolides?

Atypical pneumonia
Chlamydia
Gram positive cocci

77

What are the side effects of macrolides?

Motility issues
Arrhythmia - prolonged QT
Acute cholestatic hepatitis
Rash
Eosinophilia
Increased conc. of theophylline, anticoagulants

78

What is the mech of resistance to a macrolides?

Methylation of 23S rRNA binding site
Transmembranous efflux pumps

79

What is the MOA of chloramphenicol?

Blocks peptidyltransferase at 50S ribosomal subunit

80

Is chloramphenicol bacteriocidal or static?

Static

81

What is chloramphenicol used for?

Meningitis

82

What are the side effects of chloramphenicol?

Anemia
Aplastic anemia
Gray baby syndrome

83

Why do babies get gray baby syndrome?

Because they lack UDP-glucuronyl transferase

84

What is the mech of resistance of chloramphenicol?

Plasmid-encoded acetyl transferase that inactivates it

85

What is the MOA of clindamycin?

Blocks peptide transfer at 50S subunit

86

Is clindamycin bacteriocidal or static?

Static

87

What is clindamycin used for?

Anaerobic infections:
B. gracilis in abscesses
C. Perfringens
Treats anaerobics ABOVE the diaphragm

88

What is the toxicity of clindamycin?

Fever, diarrhea, pseudo membranous colitis

89

What is the MOA of sulfonamides?

Inhibit dihydroteroate reductase

90

Are sulfonamides cidal or static?

Static

91

What are sulfonamides used for?

Gram pos
Gram neg
Chlamydia
Nocardia

92

What are the side effects of sulfonamides?

Hypersensitivity
Hemolysis in g6PD def
Nephrotoxicity
Photosensitivity
Kernicterus
Displaces drugs from albumin - warfarin

93

What is the mech of resistance of sulfonamides?

Altered dihydropteroate synthase
Decreased uptake
Increased PABA

94

What is the MOA of trimethoprim?

Inhibits dihydrofolate reductase

95

What is the MOA of TMP-SMX?

Blockade of folic acid synthesis

96

What is TMP-SMX used for?

UTIs
Pneumocystis

97

What are the side effects of TMP?

Megaloblastic anemia
Leukopenia
Granulocytopenia

98

What is the MOA of fluoroquinolones?

Blocks DNA gyrase (topo II) and topo IV

99

Are quinolones cidal or static?

Cidal

100

What are quinolones used for?

Gram neg rods of GU and GI tract
Some gram positives

101

What are the toxicities of fluoroquinolones?

GI
Dizziness
Super infections (c. Difficile)
Headache
Skin rash
Tendinitis
Tendon rupture
Cartilage damage (teratogen)
Prolonged QT

102

What is the mech of resistance to fluoroquinolones?

Mutation in DNA gyrase
Plasmid resistance
Efflux pumps

103

What decreases the absorption of fluoroquinolones

Antacids

104

What decreases the absorption of TCs?

Milk, antacids, iron containing preps
(Divalent cations)

105

What is the MOA of metronidazole?

Forms free radical toxic metabolites that damage the bac cell DNA

106

Is metro cidal or static?

Cidal and antiprotozoal

107

What is metro used for?

GET GAP
Giardia
Entamoeba
Trichomonas
Gardnerella
Anaerobes (below diaphragm)
H. Pylori

108

What is the tox?

Disulfiram like reaction with alcohol
Headache
Metallic taste

109

What is the tx for mycobacterium TB?

RIPE
Rifampin
Isoniazid
Pyrazinamide
Ethambutol

110

What is the prophylaxis for mycobacterium TB?

Isoniazid

111

What is the prophylaxis for M. Avium-intracellulare?

Azithromycin

112


What is the tx for m.avium TB?

EARS:
Ethambutol
Azithromycin
Rifampin
Streptomycin

113

What is the tx for M. Leprae?

Long- term tx with dapsone and rifampin for tuberculoid form
Dapsone+rifampin+clofazimine for lepromatous form

114

What is the MOA of isoniazid?

Decreases synthesis of mycolic acid

115

What is needed for isoniazid to be converted to active metabolite?

Bacterial catalase peroxidase

116

What is the toxicity of isoniazid?

Neurotoxicity
Hepatotoxicity

117

What can be used for prevent neurotoxicity caused by isoniazid?

Vit b6

118

What is the MOA of rifampin?

Inhibits DNA-dependent RNA pol

119

What is rifampin used for?

Prophylaxis for meningococcal meningitis
Chemoprophylaxis in children exposed to H. Flu type B
Delays resistance to dapsone
M. TB

120

What are the side effects?

Red/orange body fluids
Minor hepatotoxicity
Induces P450
Rapid resistance if used alone

121

What is the MOA of pyrazinamide?

Acidify intracellular environment via conversion to pyrazinoic acid,

122

What are the side effects of pyrazinamide?

Hyperuricemia
Hepatotoxicity

123

What is the MOA of ethambutol?

Decreased carb polymerization of mycobacterium cell wall by blocking arabinosyltransferase

124

What is the side effect of ethambutol?

Optic neuropathy - red/green color blindness

125

What do you use to treat VRE?

Linezolid and streptogramins

126

What is the MOA of amphotericin B and nystatin?

Binds ergosterol and forms pores in the membrane

127

What are the side effects of amphotericin B?

Fever
Chills
Hypotension
Nephrotoxicity
Arrythmia anemia
IV phlebitis

128

What are the uses of amphotericin B?

Cryptococcal meningitis
Systemic fungal infections: histo, blasts, coccidiosis. Candida

129

What needs to be supplemented when giving amphotericin B?

K and Mg because of altered renal tubule permeability

130

What are the uses of nystatin?

Only topical
Swish and swallow for oral thrush
Topical for diaper rash, vaginal candidiasis

131

What is MOA of Azoles?

Inhibit P450 enzymes - no ergosterol synthesis

132

What are Azoles used for?

Local less serious systemic mycoses

133

What is fluconazole used for?

Chronic suppression of cryptococcal meningitis in AIDS
Candidiasis infection

134

What is intraconazole used for?

Blasto
Histo
Coccidiosis

135

What is clotrimazole and miconazole used for?

Topical fungal infections

136

What are the side effects of Azoles?

Testosterone synthesis inhibition - gynecomastia
Liver dysfunction

137

What is the MOA of flucytosine?

Inhibits DNA and RNA synthesis by converting to 5-fluorouracil by cytosine deaminase

138

What is the clinical use of of flucytosine?

Systemic fungal infections - meningitis by cryptococcal in combo with amphotericin B

139

What is the toxicity of flucytosine?

Bone marrow suppression

140

What is the MOA of caspofungin, mica fungin?

Inhibiting cell wall synthesis by inhibiting synthesis of beta-glucan

141

What are the fungins used for?

Invasive aspergillosis and candida

142

What is the toxicity of the fungins?

GI upset
Flushing

143

What is the MOA of terbinafine?

Inhibits fungal enzyme squalene epoxidase

144

What is terbinafine used for?

Dermatophytoses - onycho

145

What are the side effects of terbinafine?

Abnormals LFTs
Visual disturbances

146

What is the MOA of griseofulvin?

Interferes with MT function - disrupts mitosis

147

What is griseofulvin used for?

Oral tx of superficial infections
Inhibits growth of dermatophytes

148

What is the tox of griseofulvin?

Teratogenic
Carcinogenic
Confusion
Headaches
Induces P450 and warfarin metabolism

149

What is the MOA for chloroquine?

Blocks detox of heme into hemozoin --> heme builds up and is toxic to plasmodia

150

What is chloroquine uses for?

Plasmodia except falciparum

151

What is the toxicity of chloroquine?

Retinopathy

152

What is the mech of resistance employed by falciparum?

Efflux pump

153

What do you tx falciparum with?

Artemether/lumifantrine
Atorvaquone/proguanil

154

What do you use for life threatening malaria?

Quinidine or artisunate

155

What are the antiprotozoal therapies?

Pyrimethamine - toxoplasmosis
Suramin and melarsopol - T. Brucei
Nifurtimox - T. Cruzi
Sodium stibogluconate- leishmaniasis

156

What are the antihelminthic therapies?

Mebendazole
Pyrantel pamoate
Ivermectin
Diethylcarbamazine
Praziquantel - flukes

157

What is the MOA of zanamivir, oseltamivir?

Inhibit neuroaminidase - decrease release of progeny

158

What is zanamivir used for?

Tx and prevention of flu A and B

159

What is the MOA of ribavirin?

Inhibits synthesis of guanine nucleotides by competitively inhibiting IMP dehydrogenase

160

What is ribavirin used for?

RSV
HEP C

161

What is the toxicity of ribavirin?

Hemolytic anemia
Severe teratogen

162

What is the MOA of acyclovir and ganciclovir?

Guanosine analog - inhibits viral DNA pol by chain termination

163

What is acyclovir used for?

HSV
VZV
Genital and mucho cutaneous lesions and encephalitis

164

What is acyclovir ineffective against?

Weak for EBV
No effect on CMV or latent infection of HSV/VZV

165

Which cyclovir has better bioavailability?

Valacyclovir and valganciclovir

166

What do you use for VZV?

Famiciclovir

167

What is the mech of resistance to cyclovir?

Mutated viral thymidine kinase
Normal thymidine kinase monophosphorylates the acyclovir for incorporation into DNA

168

What is ganciclovir used for?

CMV

169

What is the toxicity of ganciclovir?

Pancytopenia
Renal toxicity

170

What is the mech of resistance to ganciclovir?

Mutated CMV DNA pol
Lack of viral kinase

171

What is the MOA of foscarnet and cidofovir?

Bind to pyro phosphate binding site of viral DNA pol
Inhibits viral DNA pol

172

What Are foscarnet and cidofovir used for?

CMV retinitis
Acyclovir resistant HSV

173

What is the toxicity of foscarnet and cidofovir?

Nephrotoxicity

174

What is the mech of resistance to foscarnet?

Mutated DNA pol

175

What does HAART include?

2 nucleoside reverse transcriptase inhibitors
1 non-nucleoside reverse transcriptase inhibitors OR
1 protease inhibitors OR 1 integrate inhibitor

176

What is the MOA of protease inhibitors?

Prevent maturation of new viruses by preventing HIV protease from cleaving HIV mRNA into new products.

177

What are the protease inhibitors?

The -inavirs

178

What is the toxicity of protease inhibitors?

Hyperglycemia
GI
Lipodystrophy
Nephropathy
Hematuria (indinavir)

179

Which protease Inhibitor inhibits P450?

Ritonavir

180

What is the MOA of NRTIs?

Nucleoside analogs that competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain because they lack the 3' OH group

All must be activated by phosphorylation except tenofovir

181

What are the NRTIs?

-vudine
Tenofovir
Emtricitabine
Abacivir
Didanosine

182

Which NRTIs are used for prophylaxis and to reduce transmission during pregnancy?

Zidovudine

183

What are the toxicities of NRTIs?

Bone marrow suppression (reverse with G-CSF and EPO)
Peripheral neuropathy
Lactic acidosis
Rash
Anemia (ZDZ)

184

What are the NNRTIs?

Nevirapine
Efavirenz
Delaverdine

185

What is the MOA of NNRTIs?

Bind the reverse transcriptase at a different site than NRTI
Don't require phosphorylation

186

What are the side effects of NNRTIs?

Bone marrow suppression (reverse with G-CSF and EPO)
Peripheral neuropathy
Lactic acidosis
Rash
Anemia

187

What is the integrate inhibitor?

Raltegravir

188

What is the MOA of raltegravir?

Inhibits HIV genome integration into host cell

189

What is the toxicity of raltegravir?

Hypercholesterolemia

190

What is the MOA of INFs?

Block replication of RNA and DNA viruses

191

What are INFs used for?

Alpha - chronic hep B and C, Kaposi's
Beta- multiple sclerosis
Gamma - chronic granulomatous disease

192

What is the toxicity of IFN?

Neutropenia
Myopathy

193

What are the antibiotics to avoid in pregnancy?

SAFe Children Take Really Good Care
Sulfonamides
Aminoglycosides
Fluoroquinolones
Clarithromycin
Tetracyclines
Ribavirin
Griseofulvin
Chloramphenicol

194

What is the mech of resistance to isoniazid?

Decreased levels of catalase peroxidase

195

What is needed for isoniazid to become active?

Catalase peroxidase in the mycobacterium

196

What is the mech of resistance to streptomycin?

Altered 30S ribosomal protein structure so antibiotic cant bind

197

What is needed for pyrazinamide to work?

Bacterial pyrazinamidase

198

What is the tx of choice for malaria?

Chloroquine

199

What is the tx for life threatening malaria?

IV quinidine

200

What is added for tx of plasmodium vivax and ovale?

Primaquine to kill the hypnozoite in the liver

201

What is used to treat African sleeping sickness?

Pentamidine

202

What is the tx for leishmaniasis?

Pentamidine

203

What is the tx for p. jirovecii?

Pentamidine
TMP

204

What is used to tx Chaga's?

Nifurtimox

205

What is the MOA of isopropanol as a disinfectant?

Disruption of cell membranes
Degradation of proteins

206

What is the MOA of chlorhexidine as an disinfectant?

Disruption of cell membranes
Coagulation of cytoplasm

207

What is the MOA of hydrogen peroxide as a disinfectant?

Produces destructive free radicals that oxidize cellular components
Also sporicidal

208

What is MOA of iodine as an disnfectant?

Halogenation of proteins and nucleic acids
Sporicidal

209

When is chlorhexidine used?

Surgeries and percutaneous procedures

210

What surgeries is chlorhexidine contraindicated in?

Neurologic, otologic, and ophthalmic procedures

211

What is the MOA of formaldehyde as a disinfectant?

Alkylation and cross-linking of DNA and proteins

212

What is formaldehyde used for?

Cleaning hospital instruments that cannot withstand autoclaving

213

What is the MOA of daptomycin?

Depol of cell membrane used in MRSA

214

What are the side effects of daptomycin?

Myopathy and CPK elevation

215

What is daptomycin inhibited by?

Pulmonary surfactant

216

What is the MOA of linezolid?

Inhibits bac synthesis by binding to 50S subunit

217

What are the side effects of linezolid?

TCP
Optic neuritis
Serotonin syndrome

218

What is daptomycin used for?

Treating skin infections
Bacteremia due to S. aureus

219

What is daptomycin ineffective against?

Gram negatives

220

Which drugs are well known for inhibiting warfarin metabolism?

TMP
Metronidazole
Macrolides
Azoles

221

What is ricin?

A potent toxin for the castor oil plant that inhibits protein synthesis by cleaving the rRNA component of the eukaryotic 60S subunit