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DnD- ID > Pharmacology 1/2 > Flashcards

Pharmacology 1/2 Flashcards

1
Q

MIC

A

lowest concentration of the agent to prevent visble growth

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2
Q

Bactericidal

A
  • kill bacterial cells
  • target biochemical pathways involved in cell wall assembly
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3
Q

Bacteriostatic

A
  • does not kill but slows their growth
  • reversible
    affects protein synthesis
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4
Q

Combo therapy

A
  • polymicrobial infection
  • decrease resistance
  • decrease toxicity
  • enhance inihbition/killing
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5
Q

Synergism

A
  • blockage of steps in metabolic sequence
  • inhibition of enzymatic activity
  • enhancement of antimicrobial agent uptake
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6
Q

Antagonistic

A
  • inhibition of cidal activity by static agents
  • inducing enzymative inactivation
  • competing for target site
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7
Q

Mechanism of Resistance

A
  • reduced entry of abx into pathogen
  • ehanced effluc pump activity (removal)
  • release enzymes that destroy abx
  • altering proteins that transform prodrugs
  • altering target proteins
  • develop alternative pathways to those inhibited by abx
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8
Q

Reduced entry of abx

A
  • gram neg
  • mutation, decrease, absence of porin channels in outer membrane
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9
Q

Destruction of Abx

A
  • B-lactamases inactive B-lactam abx by hydrolysis
  • aminoglycosides altered by acetylation, phosphorylation, adenylation
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10
Q

Incorporation of drug

A
  • not only resistant but using it for growth
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11
Q

Reduced affinity to target site

A
  • point mutations in target activating enzymes
  • mutation of the target
  • target modification
  • acquired resistance form naturally
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12
Q

Altered metabolic pathway

A
  • resistant strain over producing PABA = antagonizes sulfonamide
  • resistant strains produce d-ala-d-lactat instead of D-Ala-D-Ala
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13
Q

Structure of Sulfas and PABA

A

-Sulfonamides are structural analogs of PABA

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14
Q

Sulfonamides

A
  • Inhibit DiHydropteoate synthase
  • synergy with DHFR inhibitors (TMP, pyrimethamine)
  • active against Gram pos, gram neg, and enteric bacteria
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15
Q

Trimethoprim

A
  • inhibit Dihydrofolate reducatase
  • active against, respiratory pathogens, s. aureus (MRSA/MSSA)
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16
Q

Resistance for Sulfas

A
  • Overproduction of PABA
  • produce Dihydropteroate synthase that has low affinity for sulfonamides
  • impair permeability/ active efflux
  • random mutation/ transfer by plasmid
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17
Q

Resistance of TMP

A
  • reduced permeability
  • overproduction of DiHydrofolate reductase
  • produce altered reductase with reduced drug binding
  • mutation, plasmid-encoded TMP- resistant dihydrofolate reductase
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18
Q

Sulfa + TMP

Clinical uses

A
  • decline in use of sulfa due to significant resistance
  • TMP/SMX is the drug of choice for UTI, MRSA
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19
Q

Sulfonamide Drugs

A
  • sulfadiazine
  • Sulfaisoxazole
  • Sulfamethoxazole
  • Mafenide
  • Silver sulfadiazine
  • Sulfactamide sodium
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20
Q

Trimethoprim Drugs

A
  • TMP
  • TMP/SMX
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21
Q

Pyrimethamine Drugs

A
  • Pyrimethamine
  • Pyrimethamine-sulfadoxine
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22
Q

P-Kinetics

TMP

A
  • rapid absoption
  • renal excretion
  • t1/2= 11 hrs
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23
Q

P-Kinetics

Sulfonamides

A
  • absorbed, wide distribution
  • rapid excretion
  • renal excretion
  • t1/2= 5-11 hrs
  • Sulfadoxine T1/2= 4-10 days
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24
Q

Sulfa SE

A
  • Rashes
  • SJS
  • photosensitivity
  • GI distress
  • CNS effects
  • Hemolytic anemia in G6PH deficiency
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25
TMP SE
- Megaloblastic anemia, leukopenia, granulocytopenia - TMP/SMX - Sulfa adverse effects
26
#MOA Quinolones
- Inhibit DNA gyrase (topo 2) and topo 4 - inhibits the nicking and closing activity of gyrase - interferes with seperation of replicated DNA into daughter cells
27
Quinolone 1st group
Norfloxacin
28
# commonly used Quinolone 2nd group
**- Ciprofloxacin -Levofloxacin** - enoxacin - pefloxacin - ofloxacin
29
Quinolone 3rd group
**- Moxifloxacin** - gatifloxacin - gemifloxacin
30
Quinolone 1st Spectrum
gram negative aerobic bacteria
31
Quinolone 2nd Spectrum
- aerobic gram-neg - some atypicals - cipro: Pseudo - Levo: better for S. pneumo
32
Quinolone 3rd spectrum
- Gram pos - same as cipro for gram neg - moxi = good for anaerobes
33
Quinolone resistance
- point mutations in the quinolone bind region of target enzyme, change in permeability - Qnr proteins, protect DNA gyrase from fluroquinolones - aminoglycoside acetyltransferase that can modify cipro
34
# P-Kinetic Fluroquinolone
- high bio av, except for Norfloxacin - High tissue penetration - CYP450 metabolism - renal extretion - Divalent/trivalent cations impair absorption - Moxi = hepatic failure
35
Fluroquinolone Clinical use
- UTIs - P. aeruginosa - Bacterial diarrhea - Pseudomonas, enterobacter - Levo, gati, gemi, moxi = respiratory fluroquinolones
36
Fluroquinolone SE
- GI effects - CNS effects - skin effects - Phototoxicity - Muskuloskeletal (children) avoid during pregnancy
37
Nitrofurantoin
- urinary antiseptic - bactericidal - For simple UTIs - Super rapid excretion
38
Nitrofurantoin MOA
- activated in bacteria by reduction via flavoprotein nitrofurantoin reductase - unstable metabolites disrupt RNA, DNA
39
Nitrofurantoin SE
- GI issues - neuropathy - Pulmonary toxicity - Hemolytic anemia in G6PH
40
B-lactam classes
- penicillins - cephalosporins - monobactams - carbapenems - B-lactamase inhibitors
41
Non B-lactam cell wall inhibitors
Glycopeptides Daptomycin Fosfomycin Bacitracin Polymyxin
42
Penicillin Drugs
- Methicillin - nafcillin - oxacillin - cloxacillin - Penicillin G, V
43
Penicillin MOA
- B-lactam abx mimic D-ala-D-ala - irreversible - inhibits the activity of transpeptidase enzyme (PBP) by forming a stable metabolite
44
Penicillin Spectrum
- Gram pos - Gram neg cocci - Non B-lactamase anaerobes - (anti-staph penicillin) staph and strep
45
Penicillin resistance
- inactivation of abx by B-lactamase - Modification of target PBP - impaired penetration of drug to target PBP - Antibiotic efflux
46
Penicillin p-kinetic
- Diclox, amp, amox: acid-stable, well absorbed - Binds to plasma proteins (albumins) - Poor penetration to the eye, prostate, CNS - Excretion : renal, unchanged - Naf: only billiary
47
# Clinical use Penicillin G B-lactam
- streptococci - meningococci - enterococci - Sus Pneumococci - Non B-lactamase staph - Gram positive - syngeristic with gentamycin and tobramycin
48
# Clinical use Penicillin V
- minor infections - poor bio aval
49
# Clinical use Benzathine Pen and Procaine Pen
- treatment for b- hemolytic step pharyngitis
50
# Clinical use Anti-staph Penicillins
- Penicillinase producing staph - penicillin sus strains of strep and pneucocci
51
# Clinical use Nafcillin
- serious systemic staph infection - neutropenia
52
# Clinical use Dicloxacillin
- gram pos - sus staph - group a strep - viridans strep - strep pneumo - penicillinase producing staph
53
Extened spectrum Penicillins
- Ampi, amox - similar antibacterial spectrum
54
Ampicillin
- not good for nosocomial infections - active for gram-positive ans some gram negative - Respiratory infection, endocarditis, UTI, GI infection, bacterial meningitis - SE: pseudomembranous colitis, vaginal candidiasis
55
Amoxicillin
- gram-positive and some gram-neg - UTI, otitis, sinusitis, lower respiratory infection
56
# Extended Spectrum Penicillin : carboxy Ticarcillin
- active: pseudomonas, enterobacter, proteus - not used for gram positive cocci and listeria - used for serious infections only
57
# Extended spec Penicillin: Ureidopenicillins Piperacillin
- anti-pseudomonas penicillin - Pseudomonas, Klebsiella, and other gram-negative - can be used with B-lactamase inhibitors to decrease resistance
58
Penicillins SE
- Serious hypersensitivity - Anaphylaxis - Seizures (renal failure patients) - GI discomfort - skin rash - Meth: interstitial nephritis - Oxa: hepatitis
59
# Penicillins Drug interations
- Pen G, V: decrease oral contraceptives effectiveness colestipol decreases Pen absorption Probenecis increases plasma lvl - Amox: increase rash with allopurinol - serious toxicity with methotrexate (except amox)
60
#MOA Cephalosporins
- more resistant to B-lactamases - Against Gram Positive, increasing Gen decreases gram-ng and B-lactamase - Broader spectrum than Penicillins (not against Listeria, enterococci) - similar MOA and resistance mechanism as Penicillin
61
Cephalosporin Gen 1
- Cefazolin - Cephalexin - Cefadroxil
62
Cephalosporin Gen 2
- Cefoxitin - Cefuroxime
63
Cephalosporin Gen 3
- Ceftaxime - Ceftriaxone - Ceftazidime
64
Cephalosporin Gen 4
- Cefepime
65
Cephalosporin Gen 5
- Ceftaroline - Ceftolozane
66
Cephalosporin Resistance
- decreased conc. at site of action - Alterations in PBP, decreased affinity (1A, 2X) - Cephalosporinase hydrolysis by B-lactamase
67
Cephalosporin Gen 1 Activity
- Gram positive cocci ( strep, staph) + MSSA + some gram neg - PEK (proteus, E.coli, Klebsiella) - No MRSA, Pseudo, etc - Renal excretion - beware of renal impairment
68
Cephalosporin Gen 2 Activity
- Gram positive Cocci, Klebsiella - Cefuroxime: H. influenzae. Moraxella - Not used in Meningitis
69
Cephalo Gen 2 P-Kinetics
- renally cleared - dosage adjust in renal impairment - IM should be avoided
70
Cephalo Gen 3 activity
- H. influ, Neisseria, some enterobacterales, some gram positive cocci - Ceftazidime: Pseudomonas
71
Cephalo Gen 3 P-kinetics
- Distributes well in CSF (except oral) - Renal excretion - Ceftriaxone: billiary excretion - IM Ceftriaxone + azithro = gonnorhea
72
Cephalo Gen 3 Clinical use
- Serious infections - empiric treatment of sepsis - Not for enterobacter infection - Ceftriaxone, cefotaxime: meningitis
73
Cefepime
- Against: Pseudo, enterobacter, Staph, strep, Haemophilus, Neisseria - IV - Penetrates CSF
74
Ceftaroline
- IV - Only against MRSA - retains binding to PBP2a - Not active against AmpC or extended spectrum B-lactamase organisms
75
Cephalo + B-lactamase inhibitor
- Ceftazidime + Avibactam - Ceftolozane + tazobactam
76
Cephalo SE
- Allergy (hyper, crossreaction) - renal toxicity - Methythiotetrazole: bleeding discorder, hypoprothrombinemia , disulfiram reactions
77
Monobactams (Azetreonam)
- Monocyclic B-lactam ring - Binds to PBP-3 and PBP1A
78
Azetreonam
- Aerobic gram-negative bacilli + Pseudo - Resistant to B-lactamases - Distribute to CSF - Used for serious infections
79
Carbapenems Activity
- Broad, gram-negative cocci (Pseudo), Gram-positive, anaerobes - Resistant to B-lactamases - IV - Renal excretion - Good distribution, CSF
80
Imipenem + Cilastatin
- given together to prevent breakdown of Imipenem - Imipenem is inavtivated by dehydropeptidase in renal = low urinary conc.
81
Carbapenem SE
- NVD - rash - Infusion site rxn - seizures (renal failure) - Penicillin cross reactivity allergy
82
B-lactamase inhibitors
- Irreversible potent inhibitors of B-lactamases - resemble B-lactam - protects penicillins and cephalosporins - Mainly for, immunocompromised patients, mixed infections
83
Glycopeptides
- bulky structure = IV - gram positive, bactericidal - synergistic with gentamicin
84
# #glycopeptide Vancomycin MOA
- inhibits the polymerazation or transglycosylase reactio by binding to D-Ala-D-Ala
85
Glycopeptide Resistance
- D-Ala-D-lactate instead of D-Ala-D-Ala - Thickened cell wall with increases D-Ala-D-Ala residues, deadend binding site
86
Glycopeptide P-Kinetics
- orally only for C. diff - IV for serious infections - renal excretion - widely distributed
87
Glycopeptide SE
- ototoxicity, nephrotoxicity - Vanco infusion reaction (histamine)
88
Dalbavancin and Oritavancin
- semisynthetic lipoglycopeptide - Orita inhibits RNA synthesis and disrupts membrane
89
Daptomycin
- cyclic lipopeptide - Against: gram-positive bacteria - concentration dependent bactericidal - Resistance: genetic changes in mprF gene (membrane charge) - Not in CAP
90
Daptomycin p-Kinetics
- Only IV - Highly Protein bound - renal excretion
91
Daptomycin SE
- damage to musculoskeletal system - Rhabdomyolysis - nephrotox - hepatotox
92
Fosfomycin
- Analog of phosphoenolpyruvate - Broad, bactericidal - Both gram + and gram - - synergy with B-lactam antibiotics, aminoglycosides, fluroquinolones - Simple UTIs - SE: anaphylaxis, C. diff diarrhea
93
Bacitracin
- cyclic peptide - Prevents dephosphorylation in cycling of the lipid carrier that carries peptidoglycan - Highly nephrotoxic, topical - for lesions of the skin, wounds, membranes - + neomycin/ polymyxin + hydrocodone
94
Polymyxin
- surfactant active amphipathic agents - Gram-negative - Interact with phospholipids and disrupt cell membrane - Resistance: prevent access of drug to cell membrane - given parental, renal excretion
95
Fidaxomicin
- macrolide - bactericidal - Treats C diff diarrhea - inhibits RNA synthesis by RNA polymerases - Resistance: Mutation in bacterial RNA polymerase
96
Protein synthesis Inhibitor drugs
- tetracyclines, glyclcyclines - macrolides - lincosamides - streptogramins - chloramphenicol - oxazolidinones - aminoglycosides
97
Protein synthesis inhibitor bactericidal
- streptogramins - aminoglycosides - sometimes oxasolidinones
98
# Protein synthesis Inhibitors S30
- aminoglycosides - tetracyclines + glycylcyclines
99
# Protein synthesis Inhibitors S50
- macrolides - lincosamides - streptogramins - chloramphenicol - oxazolidiniones
100
Tetracycline MOA
- broad spectrum, bacteriostatic - Passive diffusion - binds reversibly to 30S subunit of bacterial ribosome - Blocks the binding of aminoacyl-tRNA to the accepter site
101
Tetracycline spectrum
- broad spectrum, - active against gram positive and negative, certain anaerobes - Tet-resistant strains are susceptible to doxy, mino, tige - Resistant: enterobacter, Pseudo, N, gonorrhea
102
Tetracycline Resistance
- decrease abx influx - produce ribosomal protection protein that displaces tetracycline from target - enzymatic inactivation of tetracyclines
103
Tetracycline P-kinetic
- oral absorption = incomplete - only parenteral - absorption impaired by divalent and trivalent cations - damages growing bone and teeth
104
Tetracycline Clinical use
- drug of choice for rickettsia, borrelia, M. pneumonia, chlamydia
105
Tigecycline
- bacteriostatic - gram neg and positive - active against vanco resistant bacteria - IV, biliary excretion
106
Tetracycline SE
- GI discomfort - Photosensitivity - hepatotox - nephrotox - Fanconi syndrome - Discoloration of teeth
107
Macrolides Drug names
- Erythromycin - Clarithromycin - Azithromycin
108
Macrolide Activity
- broad - Gram neg and pos - bacteriostatic - binds to 50S - Inhibits the translocation step
109
Macrolide resistance
- reduced permeability of the cell membrane/efflux - production of esterases that hydrolyze macrolides - MLS type B resistance (modification of ribosome binding site)
110
Macrolide SE
- Cardiac toxicity - GI discomfort - Hepatotox
111
Clarithromycin
- improved acid stability than Erythro - similar spectrum (better against mycobacterium and H Influ)
112
Azithromycin
- Against chlamydia, H. Influ - Excellent tissue distribution - No DDI as Erythro and clari - SE: arrythmia, cardiac death
113
# Lincosamide Clindamycin
- Against strep, staph, pneumo. anaerobes - Gram neg and pos - Same MOA as macrolides - Resistance: mutation, modification by methylase, enzyme inactivation
114
Clindamycin SE
- GI distress - Skin rash - Pseudomembranous colitis - Neuromuscular block
115
Streptogramins Quinupristin/Dalfopristin
- bactericidal (concentration), gram positive cocci - binds to 50S ribosome - Quinu bind at same site as macrolides - Dalfo binds nearby. synergistic enhancing the binding of quinu - Dalfo interferes with polypeptide chaine formation
116
Streptogramins Resistance
- modification of quinu binding site - enzymatic inactivation of dalfo - increased effluc
117
Chloramphenicol
- reversible, 50S - Bacteriostatic - aerobic, anaerobic, gram pos and neg - Resistance: choramphenicol acetyltransferase - decrease entry
118
Chloramphenicol p-kinetic
- prodrug - Liver metabolism - good distribution, CSF, brain - adjust for hepatic failure
119
Chloramphicol SE
- GI discomfort - Aplastic anemia - gray baby syndrom - inhibit CYP
120
Chloramphenicol Clinical use
- serious rickettsia infection - bacterial meningitis - topical eye infection
121
Oxasolidinones
Linezolid
122
Linezolid
- Binds to 23s of 50S - prevents formation that initiates protein synthesis - bacteriostatic - Gram positive - Resistance: mutation on 23S binding site
123
Linezolid SE
- GI discomfort - skin reaction - throbocytopenia - optic neuritis, peripheral neuropathy
124
Aminoglycosides drugs
- streptomycin - neomycin (very toxic) - kanamycin - amikacin - gentamycin - tobramycin - sisomicin - netilmicin
125
Aminoglycoside MOA
- Blocks initiation of protein synthesis - incorporate incorrect amino acid - Break polysomes into nonfunctional monosomes
126
Aminoglycosides
- irreversible, bactericidal - concentration dependent - binds to 30S (16S of ribosome)
127
Aminoglycoside Resistance
- Enzymes inactivate aminoglycoside by AMPylation, acetylation, phosphorylation - impaired entry of aminoglycosides into the cell - receptor protein on 30S is deleted or altered due to mutation
128
Aminoglycoside spectrum
- tobra, amika, netil, genta -- widest spectrum - active against aerobic gram negative, MSSA - nosocomial infection - synergy with B-lactams
129
Aminoglycosides P-Kinetics
- IV or IM - highly polar, low distribution in brain and CSF - Intrathecal/intraventricular injection to reach high levels in CSF - urinary excretion
130
Aminoglycosides SE
- Ototoxicity - Nephrotox - should not be used during pregnacy - potential neuromuscular blockage
131
Mupirocin
- Bactericidal - gram pos, some gran neg - reversible binding and inhibition of isoleucul tRNA synthase - AE: irritation at site, nasal irritation
132
Retapamulin
- semisynthetic pleromutilin deriv - tx for uncompliacted superficial skin infection - Selective inhibition on 50S

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