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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
List the therapeutic uses of Dicloxacillin * Spectrum * Sensitive/Resistant * Pathogens ## Footnote Pencillins
* Narrow Spectrum * Pencillinase-Resistant * MSSA, MSSE, Skin/soft tissue (little infection) ## Footnote MSSA: Methicillin-sensitive Staphylococcus aureus, MSSE: Methicillin-sensitive Staphylococcus epidermidis
26
List the therapeutic uses of **Amoxicillin**, Ampilcillin * Spectrum * Sensitive/Resistant * Pathogens ## Footnote Penicillins
* Broad Spectrum * Pencillinase-sensitive * H. influenzae, E. coli, L. monocytogenes, Community-acquired-ear/URTI ## Footnote URTI: upper respiratory tract infections
27
List the therapeutic uses of Ticarcillin * Spectrum * Sensitive/Resistant * Pathogens ## Footnote Penicillin
* Broad Spectrum * Pencillinase-sensitive * P. aeruginosa,E. cloacae, S. marcenscens, G-nocosomial (hospital acquired), also amoxicillan pathogens ## Footnote Pseudo aeru+ G-nocosomial (hospital acquired)
28
List the therapeutic uses of Piperacillin * Spectrum * Sensitive/Resistant * Pathogens ## Footnote Pencillin
* Extended Spectrum * Pencillianase-sensitive * K. pneumoniae, G-nosocomial infections, also ticarcillin pathogens
29
What type of drugs are Cephalosporins?
β-lactam (Cell wall synthesis inhibitor)
30
List Cephalosporin drugs ## Footnote All begin w/ Cef- (5 gens)
* Cefazolin 1st gen * Cefoxitin 2nd gen * **Ceftriaxone** 3rd gen * Cefepime 4th gen * **Ceftaroline** 5th gen
31
Mechanism of Action of Cephalosporins ## Footnote Same as Penicillin
* Inhibit **peptidoglycan transpeptidase (cross-linking)** * Pencillin binding proteins (PBP)-lethal effects * Trigger autolysis ## Footnote DO NOT give to patients w/ history of severe penicillin reaction
32
Pharmacokinectics of Cephalosporins
* Renal Elimination ## Footnote Ceftriaxone-Treatment of Mengitis
33
Side Effects of Cephalosporins
* Less immunogenic than pencillins (DO NOT give to pts w/ severe pencillin reations) * Hypersensitivity reactions * Local reactions, e.g. pain at intramuscular site
34
Mechanisms (4) of Resistance to Cephalosporins ## Footnote Similar to Pencillin
* Changes in PBP * Tolerance: Deficiency in autolytic enzymes * Changes in the porins * β-lactamase
35
List the therapeutic uses of **Cefazolin**, Cephalexin, 1st * Pathogens * Treatment | Cephalosporins ## Footnote PEKS
* MSSA, P. mirabilis, E.coli, K. pneumoniae, S. pneumoniae (PEKS) * Prevention or treatment of Staph or Steph infections * Surgical prophylaxis
36
List the therapeutic uses of **Cefoxitin**, Cefaclor, Cefuroxime 2nd * Pathogens * Treatment | Cephalosporins ## Footnote HEN PEKS
* H. influenzae, E. aerogenes, N. gonorrhoeae + 1st gen pathogens (P. mirabilis, E.coli, K. pneumoniae, S. pneumoniae) *
37
List the therapeutic uses of **Ceftriaxone**, Cefotaxime, Ceftazidime 3rd * Pathogens * Treatments | Cephalosporins HIGH yield ## Footnote ACES
* A. calcoaceticus, C. diversus, E. cloacae, S. marcescens * Serious G- infections, Meningitis
38
List the therapeutic uses of **Cefepime** 4th * Pathogens * Treatment ## Footnote Cephalosporins
* 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
39
List the therapeutic uses of **Ceftaroline** 5th * Pathogens * Treatment | HIGH yield ## Footnote Cephalosporins
* MRSA + 4th gen pathogens -(MSSA, S. pyogenes, C. freundii; except P. aeruginoisa) * Acute bacterial skin+skin structures infections, community acquired pneumonia
40
What type of drugs are Carbapenems?
β-lactam (Cell wall inhibitor)
41
List Carbapenem drugs ## Footnote End witn -nem "I Must Eat Dinner"
* Imipenem * Meropenem * Ertapenem * Doripenem
42
Mechanism of Action of Carbapenems ## Footnote Same as Penicillin End witn -nem
* Inhibit **peptidoglycan transpeptidase (cross-linking)** * Pencillin binding proteins (PBP)-lethal effects * Trigger autolysis
43
Pharmacokinetics of Carbapenems ## Footnote End witn -nem
* Primarly renally cleared
44
Side Effects of Carbapenems ## Footnote End witn -nem
* Seizures * Hypersensitvity reactions
45
Mechanism of Resistance to Carbapenems ## Footnote Similar to Pencillin End witn -nem
* β-lactamase * Changes in PBP * Changes in porin (Gram -) * Autolysins
46
List the therapeutic uses of Carbapenems * Pathogens | End witn -nem ## Footnote G-, pseudo, mono
* **Most G- rods** (A. calcoaceticus, C, freundii, H. influenzae, E.coli), **P. auruginosa**,**L. monocytogenes**, etc
47
What type of drugs are Monobactam?
β-Lactam (Cell Wall Synthesis)
48
Example of Monobactam drug
Aztreonam
49
Mechanism of Action of Azteronam ## Footnote Monobactam
* Inhibit **peptidoglycan transpeptidase (cross-linking of the glycopeptide polymers)** * Pencillin binding proteins (PBP)-lethal effects * Trigger autolysis
50
Pharmacokinetics of Monobactam ## Footnote Aztreonam
* Primarly renally cleared
51
Side Effects of Monobactam ## Footnote Aztreonam
* GI upset * Hypersensitivity rxns, <1% of β-lactam allergic patients, cross reactivity
52
Mechanism of Resistance to Monobactam | Aztreonam ## Footnote Similar to penicillin
* Changes in PBP * Tolerance: deficiency in autolytic enzymes * Changes in the porins (Gram -) * β-lactamase
53
Therapeutic use of Aztreonam ## Footnote Monobactam
* GIVE IF ALLERGIC TO PENCILLIN * Mostly G- rods * P. aeruginosa * Others: N. gonorrhoeae
54
What type of drugs are Tricyclic glycopeptide?
NOT a β-lactam (Cell Wall Synthesis Inhibitor)
55
List examples of Tricyclic glycopeptide drugs
Vancomyin
56
Mechanism of Action of Vancomyin ## Footnote Tricyclic glycopeptide
* Inhibitor of peptidoglycan synthase (Attaches to NAG and NAM), Binds to **D-Ala-D-Ala** * Inhibitor of pentapeptide precursor & membrane carrier
57
Pharmacokinetics of Vancomycin ## Footnote Tricyclic glycopeptide
* Renally cleared * Can enter CSF w/ inflamed meninges
58
Side of Effects of Vancomycin ## Footnote Tricyclic glycopeptide
* Otoxicity: rare * Nephrotoxicity: uncommon * Infused related flushing: Histamine release
59
Mechanism of Resistance to Vancomycin ## Footnote Tricyclic glycopeptide
* 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
Therapeutic uses of Vancomyin ## Footnote Tricyclic glycopeptide
* Primarily G+, MRSA, MRSE * Serious multi-drug resistant infections * Other: **C. difficile (PO)**
61
What type of drug are Cyclic Lipopeptide
Cell Wall/Membrane Synthesis Inhibitor
62
List examples of Cyclic lipopeptide drugs ## Footnote DAP the wall=PUNCHES HOLES
Daptomycin
63
Mechanism of Action of Daptomycin ## Footnote Cyclic lipopeptide
* Binds to cell membrane * Forms pores-->Depolarization (⬇ K+) * Rapid cell death (⬇DNA, RNA, Protein synthesis)
64
Pharmacokinetics of Daptomycin ## Footnote Cyclic lipopeptide
* Renally cleared * Pulmonary surfactant inactivates it (CANNOT use for lung infection like pneumonia)
65
Side Effects of Daptomycin ## Footnote Cyclic lipopeptide
* Myopathy, Rhabdomyolysis * Allergic pneumonitis, If used > 2 weeks
66
Mechanism of Resistance to Daptomycin
* Treatment failure→⬆MIC (Minimun inhibitorry concentration)
67
What is the main difference btw eukaryotic ribsomes and bacterial ribosomes?
* Eukaryotic=80S * Bacterial=70S
68
What subunits and what sites on the bacterial ribosomes do the antimicrobals bind to?
* 30S (Tetracyclines, Glycylcyclines, Aminoglycosides) * 50S (Macrolides, Chloramphenical, Lincosamides, Streptogramins, Oxazolides) * P Site: Majority bind * A Site: Tetracyclines & Aminoglycoside
69
What type of drugs are Tetracylcines
* Protein Synthesis Inhibitors * 30S, A site
70
List examples of Tetracyclines drugs
* **Tetracycline** * **Doxycycline** * Minocycline * Demeclocycline
71
Mechanism of Action of Tetracyclines
* Inhibit protei synthesis * Bind to bacterail 30S ribosomal subunit, A site * Prevent attachement of aminoacyl-tRNA * Bacteriostatic
72
Pharmacokinectics of Tetracylclines
* Doxycyline 1° Fecally elimated-->OK w/ renal failure
73
Side Effects of Tetracyclines
* Contraindicated during pregnancy * N/V * Discoloration of teeth & inhibit bone growth in children * Photosensitivity * Superinfection-->C. difficle, C.albicans (causes not tx)
74
Mechanism of Resistance to Tetracyclines
* Plasmid-determined resistance: ↓ influx & ↑efflux * Ribosomal change
75
Therapeutic uses of Tetracyclines
* M. pneumoniae * Cutibacterium acnes
76
What type of drugs are Glycylcyclines
* Protein synthesis inhibitor * 30S * Bacteriostatic
77
List Glycylcylines drug examples
* Tigecycline (Reserved for: Difficult to treat infection)
78
Mechanism of Action of Glycylclines ## Footnote Tigecycline
* Bind to bacterial 30S ribosomal subunit * Bacteriostatic
79
Side Effects of Glycylcyclines ## Footnote Tigecycline
* ↑ Mortality risk (0.6%), limit use for multi-resistance * Contraindicated in pregnancy, Superinfection
80
Therapeutic use of Glycylcylines ## Footnote Tigecyclines
* Broad spectrum, Many G+ and G- anaerobes * MRSA, VRE, PRSP * Complicated skin, skin structure, intra-abdominal infections
81
What type of drugs are Macrolides?
* Protein synthesis inhibitor
82
List example Macrolide drugs
* **Erythromycin** * **Azithromycin** * Clarithromycin
83
Mechanism of Action of Macrolides ## Footnote Erythromycin, Azithromycin
* Inhibit protein synthesis * Binds to the peptidyl-tRNA binding region (P site) on the 50S ribosome subunit * Bacteriostatic
84
Side of Effects of Macrolides ## Footnote Erythromycin, Azithromycin
* **Prolong the QTc interval** * N/V/D Rash * Cholestatic hepatitis
85
Mechamism of Resistance to Macrolides ## Footnote Erythromycin, Azithromycin
* Methylation of the 23 rRNA-binding site, Prevents binding
86
Drug Interaction of Macrolides ## Footnote Erythromycin, Azithromycin
* Erythromycin>>clarithromycin, **Inhibit CYP3A4**
87
Therapeutic use of Macrolides ## Footnote Erythromycin, Azithromycin
* C. pneumoniae, H. influenza, M. catarrhalis, Chlamydia * Community accquired: UTRI, Pneumonia, Otitis media
88
What type of drug is Chloramphenicol? Mechanism of Action?
* Protein Synthesis inhibitor * Binds to the 50S subunit * Bacteriostatic-inhibits peptide bond formation * Bactericidal for Meningitis tx
89
Side Effects of Chloramphenicol
* Amenia (dose-related) * Aplatic anemia (dose-independent) * **Gray baby syndrome (premature infants, ↓ UGT)**
90
Therapeutic uses of Chloramphenicol
* H. influenzae, N. meningitidis, S. pneumoniae, R. rickettsii
91
What type of drug are Lincosamides
Protein synthesis Inhibitors
92
List example Lincosamides drugs ## Footnote "CCC"
* **Clindamycin** * Camrsa * CDAD
93
Mechanism of Action of Lincosamides ## Footnote Clindamycin
* Binds to 50S ribosome subunit * Bacteriostatic
94
Side Effects of Lincosamides ## Footnote Clindamycin
* CDAD * Rash * Diarrhea * Fever * Neutropenia (rare)
95
Mechanism of Resistance to Lincosamides ## Footnote Clindamycin
* Methylation of the 23 rRNA binding site, prevents binding
96
Therapeutic uses of Lincosamides
* CA-MRSA, S. pneumoniae * Lung abscess * BLA ( β-lactam allergy)
97
What type of drug are Streptogramins
Protein synthesis inhibitor
98
List example drugs of Streptogramins
* Quinopristin+Dalfopristin (In the same dose) ## Footnote Synergy
99
Mechanism of Action of Streptogramins ## Footnote Quinopristin+Dalfopristin
* Binds to 50S ribosome subunit * Bactericidal
100
Side Effects of Streptogramins ## Footnote Quinopristin+Dalfopristin
* Pain, phlebitis at infusion site * Arthralgias * Myalgias
101
Mechanism of Resistance to Streptogramins ## Footnote Quinopristin+Dalfopristin
* Ribosomal methylase (Q) * Acetyltransferase (D)
102
Therapeutic uses of Lincosamides ## Footnote Quinopristin+Dalfopristin
* 1° G+ * E. faecium (VRE), MRSA, S. pyogenes, PRSP, Osteomyelitis, Endocarditis
103
What type of drug are Oxazolidinones
Protein synthesis Inhibitor
104
List drug examples of Oxazolidinones ## Footnote end w/ -zolid
* Linezolid * Tedizolid
105
Mechanism of Action of Oxazolidinones ## Footnote Linezolid, Tedizolid
* Bind to 50S ribosome subunit * Bacterostatic
106
Side Effects of Oxazolidinones ## Footnote Linezolid, Tedizolid
* Myelosupression * MAOI: Monoamine oxidase inhibitor * Rash * Perpiheral neuropathy
107
Mechanism of Resistance of Oxazalidinones ## Footnote Linezolid, Tedizolid
* Ribosomal binding site mutation
108
Therapeutic uses of Oxazolidinones ## Footnote Linezolid, Tedizolid
* E. faecium (L) & E. faecalis (VRE), MRSA, MRSE (L), PRSP (L), Skin infections, Pneumonia (L), Bacteremia (L)
109
What type of drug are Aminoglycosides
Protein synthesis inhibitors
110
List example drugs of Aminoglycosides
* **Gentamicin** * **Tobramycin** * Amikacin * Streptomycin * Paromomycin * Neomycin
111
Mechanism of Action of Aminoglycosides ## Footnote Gentamicin, Tobramycin
* Inhibit protein synthesis * Bind to the 30s ribosomal subunit * Bactericidal * Concentration-dependent killing, Post-antibiotic effect * Synergistic with β-lactams
112
Pharmacokinetics of Aminoglycosides ## Footnote Gentamacin, Tobramycin
* 1° renally cleared * Polar → ↓ distribution (CNS, lungs)
113
Side Effects of Aminoglycosides ## Footnote Gentamicin, Tobramycin
* Nephrotoxicity * Ototoxicity * Neuromuscular blockade * Teratogen (8th CN) * Myelosuppression (rare)
114
Mechanism of Resistance to Aminoglycosides ## Footnote Gentamicin, Tobramycin
* ↓ porin permeation * ↓ ribosomal binding * Enzymatic inactivation: acetyltransferase, phosphotransferase
115
Therapeutic uses of Aminoglycosides ## Footnote Gentamicins, Tobramycins
* 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
What type of drug are Macrocylic antibiotic
Protein synthesis Inhibitor
117
List example drugs of Macrocyclic antibiotic
Fidaxomicin
118
Mechanism of Action of Fidaxomicin ## Footnote Macrocylic antibiotic
* Binds to the **sigma unit of RNA polymerase** * Inhibits protein synthesis
119
Pharmcokinectics of Fidaxomicin ## Footnote Macrocylic antibiotic
PO: very little systemic absorption, High fecal concentration
120
Side Effects of Fidaxomicin ## Footnote Macrocylic antibiotic
* N/V * Abdominal pain * GI hemorrhage * BMS (2%)
121
Therapeutic use of Fidaxomicin ## Footnote Macrocylic antibiotic
* C. difficile * CDAD ## Footnote Only Fidaxomicin & Vancomycin tx C. diffcile
122
What type of drug are Sulfomamides
Folic Acid Inhibitors
123
List example drugs of Sulfonamides
* **Sulfamethoxazole** * Sulfisoxazole * Sulfadiazine * Mafenide * Sulfacetamide
124
Mechanism of Action of Sulfonamides ## Footnote Sulfamethoxazole
* Inhibition of dihydropteroate synthase which inhibits the biosynthesis of folic acid * PABA antagonists, Therefore, ↓ biosynthesis of DNA, RNA, AA, * Bacteriostatic
125
Pharmacokinetics of Sulfonamides ## Footnote Sulfamethoxazole
* Renally cleared * NAT (1°) & UGT substrate, Metabolites less active * Inhibit CYP2C9 → ↑ Warfarin AUC
126
Mechanism of Resistance to Sulfonamides ## Footnote Sulfamethoxazole
* Do not biosynthesize folic acid * ↑ PABA production * Dihydropteroate synthase, Low affinity for Sulfa * ↓ Sulfa permeability
127
Side Effects of Sulfonamides ## Footnote Sulfamethoxazole
* 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
Therapeutic Use of Sulfonomides ## Footnote Sulfamethoxazole
* Ophthalmic, Sulfacetamide, Tx of conjunctivitis, trachoma * Burns, Ag Sulfadiazine (Top, Synergistic), Mafenide
129
What is the mechanism of action for Trimethoprim+Sulfamethoxazole
* Folic Acid Inhibitor * DHFRI- dihydropteroate reductase inhibitor (Trimethoprim) * DHPSI- dihydropteroate synthase inhibitor (Sulfamethoxazole) * Synergism * Bacteriostatic * Can be Bactericidal in blood, urine
130
Mechanism of Resistance to Trimethoprim
* ↓ DHFR affinity * ↓ cell permeation * DHFR overproduction
131
Side Effects of Trimethoprim+Sulfamethoxazole
* BMS * Rash * Hemolytic anemia (↓G6PD)
132
Therapeutic uses of Trimethoprim+Sulfamethoxazole
* MRSA, S. pneumoniae, H. influenzae, M.catarrhalis, K. pneumoniae, E coli, S. dysenteriae, S. typhi * UTI * Prostatitis
133
What type of drug are Quinolones
DNA Replication Inhibitor
134
List example drugs of Quinolones
* **Ciprofloxacin** * **Levofloxacin** * Moxifloxacin * Ofloxacin * Gemfloxacin * Enoxacin
135
Mechanism of Quinolones ## Footnote Ciprofloxacin, Levofloxacin
* Inhibit Topoismerase II (bacterial DNA gyrase, DNA supercoil), * Inhibit DNA replication * Topisomerase IV (DNA relax) * Bactericidal
136
Side Effects of Quinolones ## Footnote Ciprofloxacin, Levofloxacin
* **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
Drug Interactions of Quinolones ## Footnote Ciprofloxacin, Levofloxacin
* Chelation, Al, Mg, Fe, Ca , ↓ PO absorption, 4-6 hours * Inhibit CYP1A2, ↑ caffeine, theophylline AUC, Enoxacin > Ciprofloxacin>> others
138
Mechanisms of Resistance of Quinolones ## Footnote Ciprofloxacin, Levofloxacin
* Mutations in Topoismerase II or IV, ↓ Binding * ↑ Efflux * ↓ Influx

Pharmacology: Exam 1 (9 decks)

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