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Pharmacology: Exam 1 > Unit 1. Lec 8,9,10-Antimicrobials I > Flashcards

Unit 1. Lec 8,9,10-Antimicrobials I Flashcards

1
Q

What are antimicrobials (antibiotics)?

A

Chemicals produced by microorganisms that inhibit or kill other microorganisms (BACTERIA only)

Include natural products as well as synthetic drugs

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2
Q

List Determinants (4) of bacterial responses

A
  • Synergism
  • Clearance
  • Age
  • Pregnancy
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3
Q

What is the goal of antibiotics?

A

Selectivity Toxicity: Kill or damage a microbe w/out damage to the host

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4
Q

Explain the Ideal Antibotic

A

Will kill pathogenic microbes w/out side effects for the patient

e.g. penicillin G

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5
Q

How does antibiotics obtain selectivity toxicity?

A
  • Antibiotics target cellular differences btw the host & the pathogenic microbe
  • E.g., penicillin inhibits the cell wall which is not in the mammalian cells
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6
Q

Explain the Therapeutic ratio (index)

Selective Toxicity

A
  • Ratio of the toxic dose to the effective dose of the drug, e.g., TI=LD50/ED50 (high LD, low ED)
  • Differs for each antimicrobial agent, i.e., some more toxic than others
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7
Q

What are the human body natural defenses against bacteria?

A
  1. Barriers:e.g skin & mucous membranes
  2. Immune Responses: Antibodies, complement systems, etc
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8
Q

Why are antimicrobials used with the bodies natural defenses?

A

Human body naturally kill pathogenic microbes. However, antimicrobial are used when the natural defenses are overwhelmed or damaged

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9
Q

What are the two effects of microbials?

A
  • Bactericidial
  • Bacteriostatic
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10
Q

Define BacteriCIDAL

A

Kills bacteria (lysis of cell wall to cause death)

Penicillins, Aminoglycans, Cephalosporins (PACS a punch)

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11
Q

Define BacterioSTATIC

A

Inhibit bacterial cell replication

Tetracylines, Erythromycins, Chloramphenicol (TEC)

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12
Q

Describe the cell walls of Gram + bacteria

A
  • Lactamase outside
  • Thicker peptidoclycan wall
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13
Q

Describe Gram - cell wall

A
  • Outer membrane with porin channel
  • Thin peptidoglycan layer
  • Lactamase inside
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14
Q

Describe the mechanism of cell wall cross-linking

A
  • NAG (N-acetyl-glucosamine) uses Pyruvyl transferase + D-Ala-D-Ala to become NAM (N-Acetyl-muramic acid)
  • Peptidoglycan than cross-links the NAM and NAGs to make the cell wall
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15
Q

What drugs should you not give d/t age and the side effects?

A

Neonates

  • Chloramphenicol–>Gray Baby syndrome [lower dose]
  • Sulfonamides–>Kernicterus or Toxic Encephalopathy [Contraindication]

Children

  • Tetracycline–>Bone growth/Teeth discoloration

CHF (Congestive Heart Failure)

  • Ticarcillin disodium/Clavulanate potassium–> Edema/Arrythmia
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16
Q

What drug do we increase to infants and young children?Why?

A
  • Gentamicin becasue volume of distribution
  • As we age, we increase lipid profile and younger pts are more aqueous
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17
Q

What type of drugs are Penicllins?

A

All β-lactams (Cell wall synthesis inhibitor)

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18
Q

List Pregnacy Contraindication (5)

DO NOT GIVE when pregnant

A
  • Metronidazole (Mutagenic)
  • Sulfonamides (Breast milk, Kernicterus (incr. bilirubin, displaced from albumin)
  • Antifolate drugs (decr. conc. of folic acid in pregnant women-can lead to spina bifida)
  • Fluoroquinolones (Afffect cartilage growth)
  • Tetracyclines (Inhibit bone growth, tooth enamel dysplasia)
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19
Q

List Penicllin drugs

A
  • Penicillin G
  • Ampicillin
  • Penicillin V
  • Dicloxacillin
  • Ticarcillin
  • Piperacillin
  • Amoxicillin
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20
Q

Mechanisms of Action for Penicillin

A
  • Inhibit peptidoglycan transpeptidase (cross-linking of the glycopeptide polymers)
  • Pencillin binding proteins (PBP)-lethal effects
  • Trigger autolysis

PBP-requied for maintance of rod shape

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21
Q

Explain the Pharmocokinetics of Penicillins

A
  • Majority undergo renal clearance
  • Distribute widely throughout body spaces
  • Passage into cerebrospinal, joint, & occular fluids, poor in the absense of imflammation
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22
Q

Side Effects of Peniciilins

A
  • PO: gastric distress, diarrhea (NVD)
  • Superinfection of GI tract: C. diff
  • Penicilin Allergy
  • Neurotoxixity, ie sexiures, penicillin G, inhibit GABA
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23
Q

Mechanism (4) of Resistance of Penicillin

HIGH yield

Same for all β-lactams

A
  • Changes in PBP
  • Tolerance: deficiency in autolytic enzymes
  • Changes in the porins (Gram -)
  • β-lactamase
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24
Q

List the therapeutic uses of Penicillin G,V

  • Spectrum
  • Sensitive/Resistant
  • Pathogens

Penicillins

A
  • Narrow Spectrum
  • Penicillinase-sensitive
  • S. pneumoniae, P. magnus, T. pallifum, S. pygones (Necrotizing fasciitis)

*Strep, Pepto, Trep, Necrotize

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25
Q

List the therapeutic uses of Dicloxacillin

  • Spectrum
  • Sensitive/Resistant
  • Pathogens

Pencillins

A
  • Narrow Spectrum
  • Pencillinase-Resistant
  • MSSA, MSSE, Skin/soft tissue (little infection)

MSSA: Methicillin-sensitive Staphylococcus aureus, MSSE: Methicillin-sensitive Staphylococcus epidermidis

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26
Q

List the therapeutic uses of Amoxicillin, Ampilcillin

  • Spectrum
  • Sensitive/Resistant
  • Pathogens

Penicillins

A
  • Broad Spectrum
  • Pencillinase-sensitive
  • H. influenzae, E. coli, L. monocytogenes, Community-acquired-ear/URTI

URTI: upper respiratory tract infections

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27
Q

List the therapeutic uses of Ticarcillin

  • Spectrum
  • Sensitive/Resistant
  • Pathogens

Penicillin

A
  • Broad Spectrum
  • Pencillinase-sensitive
  • P. aeruginosa,E. cloacae, S. marcenscens, G-nocosomial (hospital acquired), also amoxicillan pathogens

Pseudo aeru+ G-nocosomial (hospital acquired)

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28
Q

List the therapeutic uses of Piperacillin

  • Spectrum
  • Sensitive/Resistant
  • Pathogens

Pencillin

A
  • Extended Spectrum
  • Pencillianase-sensitive
  • K. pneumoniae, G-nosocomial infections, also ticarcillin pathogens
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29
Q

What type of drugs are Cephalosporins?

A

β-lactam (Cell wall synthesis inhibitor)

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30
Q

List Cephalosporin drugs

All begin w/ Cef- (5 gens)

A
  • Cefazolin 1st gen
  • Cefoxitin 2nd gen
  • Ceftriaxone 3rd gen
  • Cefepime 4th gen
  • Ceftaroline 5th gen
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31
Q

Mechanism of Action of Cephalosporins

Same as Penicillin

A
  • Inhibit peptidoglycan transpeptidase (cross-linking)
  • Pencillin binding proteins (PBP)-lethal effects
  • Trigger autolysis

DO NOT give to patients w/ history of severe penicillin reaction

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32
Q

Pharmacokinectics of Cephalosporins

A
  • Renal Elimination

Ceftriaxone-Treatment of Mengitis

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33
Q

Side Effects of Cephalosporins

A
  • Less immunogenic than pencillins (DO NOT give to pts w/ severe pencillin reations)
  • Hypersensitivity reactions
  • Local reactions, e.g. pain at intramuscular site
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34
Q

Mechanisms (4) of Resistance to Cephalosporins

Similar to Pencillin

A
  • Changes in PBP
  • Tolerance: Deficiency in autolytic enzymes
  • Changes in the porins
  • β-lactamase
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35
Q

List the therapeutic uses of Cefazolin, Cephalexin, 1st

  • Pathogens
  • Treatment

Cephalosporins

PEKS

A
  • MSSA, P. mirabilis, E.coli, K. pneumoniae, S. pneumoniae (PEKS)
  • Prevention or treatment of Staph or Steph infections
  • Surgical prophylaxis
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36
Q

List the therapeutic uses of Cefoxitin, Cefaclor, Cefuroxime 2nd

  • Pathogens
  • Treatment

Cephalosporins

HEN PEKS

A
  • H. influenzae, E. aerogenes, N. gonorrhoeae + 1st gen pathogens (P. mirabilis, E.coli, K. pneumoniae, S. pneumoniae)
  • <G+ coverage, Prophylaxis during surgery
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37
Q

List the therapeutic uses of Ceftriaxone, Cefotaxime, Ceftazidime 3rd

  • Pathogens
  • Treatments

Cephalosporins HIGH yield

ACES

A
  • A. calcoaceticus, C. diversus, E. cloacae, S. marcescens
  • Serious G- infections, Meningitis
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38
Q

List the therapeutic uses of Cefepime 4th

  • Pathogens
  • Treatment

Cephalosporins

A
  • MSSA, S. pyogenes, P. aeruginosa, C. freundii + 3rd gen pathogens (ACES-A. calcoaceticus, C. diversus, E. cloacae, S. marcescens )
  • > β-lactamase resistance, Serious G-nosocomial infections
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39
Q

List the therapeutic uses of Ceftaroline 5th

  • Pathogens
  • Treatment

HIGH yield

Cephalosporins

A
  • MRSA + 4th gen pathogens -(MSSA, S. pyogenes, C. freundii; except P. aeruginoisa)
  • Acute bacterial skin+skin structures infections, community acquired pneumonia
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40
Q

What type of drugs are Carbapenems?

A

β-lactam (Cell wall inhibitor)

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41
Q

List Carbapenem drugs

End witn -nem
“I Must Eat Dinner”

A
  • Imipenem
  • Meropenem
  • Ertapenem
  • Doripenem
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42
Q

Mechanism of Action of Carbapenems

Same as Penicillin
End witn -nem

A
  • Inhibit peptidoglycan transpeptidase (cross-linking)
  • Pencillin binding proteins (PBP)-lethal effects
  • Trigger autolysis
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43
Q

Pharmacokinetics of Carbapenems

End witn -nem

A
  • Primarly renally cleared
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44
Q

Side Effects of Carbapenems

End witn -nem

A
  • Seizures
  • Hypersensitvity reactions
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45
Q

Mechanism of Resistance to Carbapenems

Similar to Pencillin
End witn -nem

A
  • β-lactamase
  • Changes in PBP
  • Changes in porin (Gram -)
  • Autolysins
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46
Q

List the therapeutic uses of Carbapenems

  • Pathogens

End witn -nem

G-, pseudo, mono

A
  • Most G- rods (A. calcoaceticus, C, freundii, H. influenzae, E.coli), P. auruginosa,L. monocytogenes, etc
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47
Q

What type of drugs are Monobactam?

A

β-Lactam (Cell Wall Synthesis)

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48
Q

Example of Monobactam drug

A

Aztreonam

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49
Q

Mechanism of Action of Azteronam

Monobactam

A
  • Inhibit peptidoglycan transpeptidase (cross-linking of the glycopeptide polymers)
  • Pencillin binding proteins (PBP)-lethal effects
  • Trigger autolysis
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50
Q

Pharmacokinetics of Monobactam

Aztreonam

A
  • Primarly renally cleared
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51
Q

Side Effects of Monobactam

Aztreonam

A
  • GI upset
  • Hypersensitivity rxns, <1% of β-lactam allergic patients, cross reactivity
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52
Q

Mechanism of Resistance to Monobactam

Aztreonam

Similar to penicillin

A
  • Changes in PBP
  • Tolerance: deficiency in autolytic enzymes
  • Changes in the porins (Gram -)
  • β-lactamase
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53
Q

Therapeutic use of Aztreonam

Monobactam

A
  • GIVE IF ALLERGIC TO PENCILLIN
  • Mostly G- rods
  • P. aeruginosa
  • Others: N. gonorrhoeae
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54
Q

What type of drugs are Tricyclic glycopeptide?

A

NOT a β-lactam (Cell Wall Synthesis Inhibitor)

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55
Q

List examples of Tricyclic glycopeptide drugs

A

Vancomyin

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56
Q

Mechanism of Action of Vancomyin

Tricyclic glycopeptide

A
  • Inhibitor of peptidoglycan synthase (Attaches to NAG and NAM), Binds to D-Ala-D-Ala
  • Inhibitor of pentapeptide precursor & membrane carrier
57
Q

Pharmacokinetics of Vancomycin

Tricyclic glycopeptide

A
  • Renally cleared
  • Can enter CSF w/ inflamed meninges
58
Q

Side of Effects of Vancomycin

Tricyclic glycopeptide

A
  • Otoxicity: rare
  • Nephrotoxicity: uncommon
  • Infused related flushing: Histamine release
59
Q

Mechanism of Resistance to Vancomycin

Tricyclic glycopeptide

A
  • D-Ala-D-Ala—>D-Ala-D-Lactate (1000x less affinity)
  • VRE (Vancomyin resistant enterococci)
  • VISA= Vancomycin intermediate Staph. Aur. OVER produced D-Ala-D-Ala to have false binding sites
60
Q

Therapeutic uses of Vancomyin

Tricyclic glycopeptide

A
  • Primarily G+, MRSA, MRSE
  • Serious multi-drug resistant infections
  • Other: C. difficile (PO)
61
Q

What type of drug are Cyclic Lipopeptide

A

Cell Wall/Membrane Synthesis Inhibitor

62
Q

List examples of Cyclic lipopeptide drugs

DAP the wall=PUNCHES HOLES

A

Daptomycin

63
Q

Mechanism of Action of Daptomycin

Cyclic lipopeptide

A
  • Binds to cell membrane
  • Forms pores–>Depolarization (⬇ K+)
  • Rapid cell death (⬇DNA, RNA, Protein synthesis)
64
Q

Pharmacokinetics of Daptomycin

Cyclic lipopeptide

A
  • Renally cleared
  • Pulmonary surfactant inactivates it (CANNOT use for lung infection like pneumonia)
65
Q

Side Effects of Daptomycin

Cyclic lipopeptide

A
  • Myopathy, Rhabdomyolysis
  • Allergic pneumonitis, If used > 2 weeks
66
Q

Mechanism of Resistance to Daptomycin

A
  • Treatment failure→⬆MIC (Minimun inhibitorry concentration)
67
Q

What is the main difference btw eukaryotic ribsomes and bacterial ribosomes?

A
  • Eukaryotic=80S
  • Bacterial=70S
68
Q

What subunits and what sites on the bacterial ribosomes do the antimicrobals bind to?

A
  • 30S (Tetracyclines, Glycylcyclines, Aminoglycosides)
  • 50S (Macrolides, Chloramphenical, Lincosamides, Streptogramins, Oxazolides)
  • P Site: Majority bind
  • A Site: Tetracyclines & Aminoglycoside
69
Q

What type of drugs are Tetracylcines

A
  • Protein Synthesis Inhibitors
  • 30S, A site
70
Q

List examples of Tetracyclines drugs

A
  • Tetracycline
  • Doxycycline
  • Minocycline
  • Demeclocycline
71
Q

Mechanism of Action of Tetracyclines

A
  • Inhibit protei synthesis
  • Bind to bacterail 30S ribosomal subunit, A site
  • Prevent attachement of aminoacyl-tRNA
  • Bacteriostatic
72
Q

Pharmacokinectics of Tetracylclines

A
  • Doxycyline 1° Fecally elimated–>OK w/ renal failure
73
Q

Side Effects of Tetracyclines

A
  • Contraindicated during pregnancy
  • N/V
  • Discoloration of teeth & inhibit bone growth in children
  • Photosensitivity
  • Superinfection–>C. difficle, C.albicans (causes not tx)
74
Q

Mechanism of Resistance to Tetracyclines

A
  • Plasmid-determined resistance: ↓ influx & ↑efflux
  • Ribosomal change
75
Q

Therapeutic uses of Tetracyclines

A
  • M. pneumoniae
  • Cutibacterium acnes
76
Q

What type of drugs are Glycylcyclines

A
  • Protein synthesis inhibitor
  • 30S
  • Bacteriostatic
77
Q

List Glycylcylines drug examples

A
  • Tigecycline (Reserved for: Difficult to treat infection)
78
Q

Mechanism of Action of Glycylclines

Tigecycline

A
  • Bind to bacterial 30S ribosomal subunit
  • Bacteriostatic
79
Q

Side Effects of Glycylcyclines

Tigecycline

A
  • ↑ Mortality risk (0.6%), limit use for multi-resistance
  • Contraindicated in pregnancy, Superinfection
80
Q

Therapeutic use of Glycylcylines

Tigecyclines

A
  • Broad spectrum, Many G+ and G- anaerobes
  • MRSA, VRE, PRSP
  • Complicated skin, skin structure, intra-abdominal infections
81
Q

What type of drugs are Macrolides?

A
  • Protein synthesis inhibitor
82
Q

List example Macrolide drugs

A
  • Erythromycin
  • Azithromycin
  • Clarithromycin
83
Q

Mechanism of Action of Macrolides

Erythromycin, Azithromycin

A
  • Inhibit protein synthesis
  • Binds to the peptidyl-tRNA binding region (P site) on the 50S ribosome subunit
  • Bacteriostatic
84
Q

Side of Effects of Macrolides

Erythromycin, Azithromycin

A
  • Prolong the QTc interval
  • N/V/D Rash
  • Cholestatic hepatitis
85
Q

Mechamism of Resistance to Macrolides

Erythromycin, Azithromycin

A
  • Methylation of the 23 rRNA-binding site, Prevents binding
86
Q

Drug Interaction of Macrolides

Erythromycin, Azithromycin

A
  • Erythromycin»clarithromycin, Inhibit CYP3A4
87
Q

Therapeutic use of Macrolides

Erythromycin, Azithromycin

A
  • C. pneumoniae, H. influenza, M. catarrhalis, Chlamydia
  • Community accquired: UTRI, Pneumonia, Otitis media
88
Q

What type of drug is Chloramphenicol? Mechanism of Action?

A
  • Protein Synthesis inhibitor
  • Binds to the 50S subunit
  • Bacteriostatic-inhibits peptide bond formation
  • Bactericidal for Meningitis tx
89
Q

Side Effects of Chloramphenicol

A
  • Amenia (dose-related)
  • Aplatic anemia (dose-independent)
  • Gray baby syndrome (premature infants, ↓ UGT)
90
Q

Therapeutic uses of Chloramphenicol

A
  • H. influenzae, N. meningitidis, S. pneumoniae, R. rickettsii
91
Q

What type of drug are Lincosamides

A

Protein synthesis Inhibitors

92
Q

List example Lincosamides drugs

“CCC”

A
  • Clindamycin
  • Camrsa
  • CDAD
93
Q

Mechanism of Action of Lincosamides

Clindamycin

A
  • Binds to 50S ribosome subunit
  • Bacteriostatic
94
Q

Side Effects of Lincosamides

Clindamycin

A
  • CDAD
  • Rash
  • Diarrhea
  • Fever
  • Neutropenia (rare)
95
Q

Mechanism of Resistance to Lincosamides

Clindamycin

A
  • Methylation of the 23 rRNA binding site, prevents binding
96
Q

Therapeutic uses of Lincosamides

A
  • CA-MRSA, S. pneumoniae
  • Lung abscess
  • BLA ( β-lactam allergy)
97
Q

What type of drug are Streptogramins

A

Protein synthesis inhibitor

98
Q

List example drugs of Streptogramins

A
  • Quinopristin+Dalfopristin (In the same dose)

Synergy

99
Q

Mechanism of Action of Streptogramins

Quinopristin+Dalfopristin

A
  • Binds to 50S ribosome subunit
  • Bactericidal
100
Q

Side Effects of Streptogramins

Quinopristin+Dalfopristin

A
  • Pain, phlebitis at infusion site
  • Arthralgias
  • Myalgias
101
Q

Mechanism of Resistance to Streptogramins

Quinopristin+Dalfopristin

A
  • Ribosomal methylase (Q)
  • Acetyltransferase (D)
102
Q

Therapeutic uses of Lincosamides

Quinopristin+Dalfopristin

A
  • 1° G+
  • E. faecium (VRE), MRSA, S. pyogenes, PRSP, Osteomyelitis, Endocarditis
103
Q

What type of drug are Oxazolidinones

A

Protein synthesis Inhibitor

104
Q

List drug examples of Oxazolidinones

end w/ -zolid

A
  • Linezolid
  • Tedizolid
105
Q

Mechanism of Action of Oxazolidinones

Linezolid, Tedizolid

A
  • Bind to 50S ribosome subunit
  • Bacterostatic
106
Q

Side Effects of Oxazolidinones

Linezolid, Tedizolid

A
  • Myelosupression
  • MAOI: Monoamine oxidase inhibitor
  • Rash
  • Perpiheral neuropathy
107
Q

Mechanism of Resistance of Oxazalidinones

Linezolid, Tedizolid

A
  • Ribosomal binding site mutation
108
Q

Therapeutic uses of Oxazolidinones

Linezolid, Tedizolid

A
  • E. faecium (L) & E. faecalis (VRE), MRSA, MRSE (L), PRSP (L), Skin infections, Pneumonia (L), Bacteremia (L)
109
Q

What type of drug are Aminoglycosides

A

Protein synthesis inhibitors

110
Q

List example drugs of Aminoglycosides

A
  • Gentamicin
  • Tobramycin
  • Amikacin
  • Streptomycin
  • Paromomycin
  • Neomycin
111
Q

Mechanism of Action of Aminoglycosides

Gentamicin, Tobramycin

A
  • Inhibit protein synthesis
  • Bind to the 30s ribosomal subunit
  • Bactericidal
  • Concentration-dependent killing, Post-antibiotic effect
  • Synergistic with β-lactams
112
Q

Pharmacokinetics of Aminoglycosides

Gentamacin, Tobramycin

A
  • 1° renally cleared
  • Polar → ↓ distribution (CNS, lungs)
113
Q

Side Effects of Aminoglycosides

Gentamicin, Tobramycin

A
  • Nephrotoxicity
  • Ototoxicity
  • Neuromuscular blockade
  • Teratogen (8th CN)
  • Myelosuppression (rare)
114
Q

Mechanism of Resistance to Aminoglycosides

Gentamicin, Tobramycin

A
  • ↓ porin permeation
  • ↓ ribosomal binding
  • Enzymatic inactivation: acetyltransferase, phosphotransferase
115
Q

Therapeutic uses of Aminoglycosides

Gentamicins, Tobramycins

A
  • 1° for aerobic G-, (G,T,A)
  • P. aeruginosa (T > G), E. cloacae, S. marcescens (G > T), P. vulgaris, K. pneumoniae, E. faecalis (S), L. monocytogenes (S)
  • Serious G- nosocomial infections,
116
Q

What type of drug are Macrocylic antibiotic

A

Protein synthesis Inhibitor

117
Q

List example drugs of Macrocyclic antibiotic

A

Fidaxomicin

118
Q

Mechanism of Action of Fidaxomicin

Macrocylic antibiotic

A
  • Binds to the sigma unit of RNA polymerase
  • Inhibits protein synthesis
119
Q

Pharmcokinectics of Fidaxomicin

Macrocylic antibiotic

A

PO: very little systemic absorption, High fecal concentration

120
Q

Side Effects of Fidaxomicin

Macrocylic antibiotic

A
  • N/V
  • Abdominal pain
  • GI hemorrhage
  • BMS (2%)
121
Q

Therapeutic use of Fidaxomicin

Macrocylic antibiotic

A
  • C. difficile
  • CDAD

Only Fidaxomicin & Vancomycin tx C. diffcile

122
Q

What type of drug are Sulfomamides

A

Folic Acid Inhibitors

123
Q

List example drugs of Sulfonamides

A
  • Sulfamethoxazole
  • Sulfisoxazole
  • Sulfadiazine
  • Mafenide
  • Sulfacetamide
124
Q

Mechanism of Action of Sulfonamides

Sulfamethoxazole

A
  • Inhibition of dihydropteroate synthase which inhibits the biosynthesis of folic acid
  • PABA antagonists, Therefore, ↓ biosynthesis of DNA, RNA, AA,
  • Bacteriostatic
125
Q

Pharmacokinetics of Sulfonamides

Sulfamethoxazole

A
  • Renally cleared
  • NAT (1°) & UGT substrate, Metabolites less active
  • Inhibit CYP2C9 → ↑ Warfarin AUC
126
Q

Mechanism of Resistance to Sulfonamides

Sulfamethoxazole

A
  • Do not biosynthesize folic acid
  • ↑ PABA production
  • Dihydropteroate synthase, Low affinity for Sulfa
  • ↓ Sulfa permeability
127
Q

Side Effects of Sulfonamides

Sulfamethoxazole

A
  • Rash: Sulfa allergy, SJS, TEN
  • Ppt in the kidneys: crystalluria, hematuria, obstruction
  • Aplastic anemia, Hemolytic anemia (↓G6PD)
  • Kernicterus: Newborn Encephalopathy, Bilirubin deposits in brain, Sulfa displacement on albumin
128
Q

Therapeutic Use of Sulfonomides

Sulfamethoxazole

A
  • Ophthalmic, Sulfacetamide, Tx of conjunctivitis, trachoma
  • Burns, Ag Sulfadiazine (Top, Synergistic), Mafenide
129
Q

What is the mechanism of action for Trimethoprim+Sulfamethoxazole

A
  • Folic Acid Inhibitor
  • DHFRI- dihydropteroate reductase inhibitor (Trimethoprim)
  • DHPSI- dihydropteroate synthase inhibitor (Sulfamethoxazole)
  • Synergism
  • Bacteriostatic
  • Can be Bactericidal in blood, urine
130
Q

Mechanism of Resistance to Trimethoprim

A
  • ↓ DHFR affinity
  • ↓ cell permeation
  • DHFR overproduction
131
Q

Side Effects of Trimethoprim+Sulfamethoxazole

A
  • BMS
  • Rash
  • Hemolytic anemia (↓G6PD)
132
Q

Therapeutic uses of Trimethoprim+Sulfamethoxazole

A
  • MRSA, S. pneumoniae, H. influenzae, M.catarrhalis, K. pneumoniae, E coli, S. dysenteriae, S. typhi
  • UTI
  • Prostatitis
133
Q

What type of drug are Quinolones

A

DNA Replication Inhibitor

134
Q

List example drugs of Quinolones

A
  • Ciprofloxacin
  • Levofloxacin
  • Moxifloxacin
  • Ofloxacin
  • Gemfloxacin
  • Enoxacin
135
Q

Mechanism of Quinolones

Ciprofloxacin, Levofloxacin

A
  • Inhibit Topoismerase II (bacterial DNA gyrase, DNA supercoil),
  • Inhibit DNA replication
  • Topisomerase IV (DNA relax)
  • Bactericidal
136
Q

Side Effects of Quinolones

Ciprofloxacin, Levofloxacin

A
  • Tendonitis, Tendon rupture (↑ risk > 60 y/o, Glucocorticoids, & Kidney, Heart, Lung transplant, Contraindicated, Pregnancy, Nursing, Children < 18 y/o, Except for life-threatening infections)
  • Myasthenia gravis (May exacerbate muscle weakness)
  • GI (N/V/D)
  • Neurotoxicity (Seizures, Hallucinations, Depression, Peripheral neuropathy)
  • Skin reactions (Hypersensitivity reactions (rashes), phototoxicity (sunburn))
137
Q

Drug Interactions of Quinolones

Ciprofloxacin, Levofloxacin

A
  • Chelation, Al, Mg, Fe, Ca , ↓ PO absorption, 4-6 hours
  • Inhibit CYP1A2, ↑ caffeine, theophylline AUC, Enoxacin > Ciprofloxacin» others
138
Q

Mechanisms of Resistance of Quinolones

Ciprofloxacin, Levofloxacin

A
  • Mutations in Topoismerase II or IV, ↓ Binding
  • ↑ Efflux
  • ↓ Influx

Pharmacology: Exam 1 (9 decks)

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