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Multi-Systems: ABX Flashcards

1
Q

(3) Mechanisms of ABX that inhibit Cell Wall Biosynthesis?

A
  • Inhibit Peptidoglycan Cross-linking
  • Inhibit Peptidoglycan Polymerization
  • Inhibit Cell wall Synthesis by Binding PBP3
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2
Q

ABX that inhibit Membrane Potential?

A
  • Lipopeptides
    • ​Daptomycin
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3
Q

(1) ABX that cause Cell Membrane Disruption?

A
  • Polymyxins
    • ​Polymyxin A
    • Polymyxin B
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4
Q

(10) ABX that inhibit Protein Synthesis?

A
  • Oxazoladinones
  • Tetracyclines
  • Aminoglycosides
  • Glycylcycline
  • Chloramphenicol
  • Clindamycin
  • Lincosamines
  • Macrolides
  • Streptogramins
  • Trimethoprim
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5
Q

(2) ABX that inhibit Folic Acid Synthesis?

(DNA Methylation)

A
  • Sulfonamides
  • Trimethoprim
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6
Q

(3) ABX that inhibit DNA Replication or Transplatation?

A
  • Fluoroquinolones (DNA Topoisomerase)
    • ​Ciprofloxacin
    • Levofloxacin
  • Nitroimidazole
  • Rifamycin (mRNA synthesis - RNA Polymerization)
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7
Q

(2) ABX that acts on the Transglycosylase enzyme
of the Cell Wall Biosynthesis?

A
  • Vancomycin
    • ​D-ala D-ala portion of cell wall precursor
  • Teicoplanin
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8
Q

(5) Sub-types of ABX that acts on the Transpeptidase
of the Cell Wall Biosynthesis?

(Inhibiting Peptidoglycan Cross-linking)

A
  • Beta-Lactams
    • Penicillins (Sensitive, Resistant)
    • Cephalosporins (I, II, III, IV)
    • Carbecephams
    • Carbepenems
    • Monobactams
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9
Q

(5) Penicillinase-Resistant Penicillins?

“MEt NAsty OX -OX -OX”

A
  • Methicillin
  • Nafcillin
  • Oxacillin
  • Cloxacillin
  • Dicloxacillin
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10
Q

(2) Extended Range Penicillins?

“AM extended”

A
  • Ampicillin
  • Amoxicillin
  • Penicillinase Sensitive
  • Combine w/ Clavulanic Acid
  • -> protect against β-lactamase
  • “AMinoPenicillins are AMPed-up Penicillin”
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11
Q

Anti-Pseudomonal Penicillins?

“Pseudo-cars (2x), Never are more popular”

A
  • Carboxylated derivatives extend range of Ampicillin to
  • P. aeruginosa*; Indole-positive Proteus and Enterobacter
    • Carbenicillin
    • Ticarcillin
  • N-acyl derivatives
    • Azlocillin
    • Mezlocillin
    • Piperacillin
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12
Q

(3) Prophylaxis during intra-abdominal surgery?

A
  • Cefotetan (2nd)
  • Cefoxitin (2nd)
  • Neomycin (Bowel surgery) (Aminoglycoside)
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13
Q

(4) Surgery prophylaxis?

A
  • First Generation
    • Cephalexin
    • Cephadrine
    • Cefadroxil
    • Cefazolin
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14
Q

(1) Used to treat Community-acquired Pneumonia?

(H. influenzae and K. pneumoniae)

A
  • Cefuroxime
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15
Q

(1) Used to treat Diabetic Foot Infections?

A
  • Cephalexin
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16
Q

Drugs of choice for treating?

(1) N. gonorrhea
(2) Meningitis (Adult, Children)
(1) B. burgdorferi

A
  • N. gonorrhea
    • ​Ceftriaxone
  • Meningitis
    • ​Ciprofloxacin (1st)
    • Rifampin (children)
  • B. burgdorferi
    • ​Tetracyclines
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17
Q

(2) ABX for Multidrug-resistant Gram-negative Infections, especially those caused by P. aeruginosa?

A
  • Ceftazidime
  • Cefoperazone
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18
Q

First β-lactam approved for MRSA?

Better drug Rx for MRSA?

A
  • Ceftaroline fosamil (IV) (1st)
  • Vancomycin (Better)
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19
Q

(3) Glycopeptide ABX?

(Inhibits Peptidoglycan Syn. –> Cell Wall Synthesis)

A
  • Vancomycin
  • Bacitracin
  • Teicoplanin
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20
Q

Pathogenic spectrum of Vancomycin?

A
  • G+ only
  • Bacteriostatic against Gram-positive Cocci
  • Bactericidal for Gram-positive Rods
    • Serious Penicillinase producers
    • MRSA
    • Enterococci
  • NOT Effective against Gram negatives
  • Last Resort for Pseudomembranous colitis cause by
  • C. difficile* (Oral Vancomycin)
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21
Q

Where does Vancomycin work?

A
  • Binds to D-Ala-D-Ala terminus of Murein Monomer
  • -> D-Ala-D-Lactate. Same mode of VRE
  • Inhibits Murein Polymer synthesis
  • -> Inhibits Peptidoglycan formation
  • Blocks attachment of Disaccharide subunits to pre-existing Cell Wall
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22
Q

SE of Vancomycin?

“NOT”

A
  • Hypersensitivity Rxn - Skin flushing or Rash
    • “Red man syndrome” - rapid infusion due to Histamine release (slow infusion and pretreatment w/ antihistamines)
  • Nephrotoxicity
  • Ototoxicity
  • Thrombophlebitis
  • Neutropenia
  • Tissue necrosis if given IM
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23
Q

Pathogen spectrum of Lipopeptide ABX?

A
  • Gram positive Aerobic organisms
    • Complicated skin infections
    • Endocarditis
  • Bactericidal against VRE?
  • Bacteriostatic against
    • S. pneumoniae
    • S. aureus
  • Retains activity against Gram-positive bacteria
  • Synergizes w/ Oxacillin against MRSA
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24
Q

Where does Lipopeptide ABX work?

A
  • Binds to Bacterial Membranes
  • Forms membrane channels in a Calcium-dependent manner leading to a rapid membrane depolarization thus inhibiting protein
  • DNA and RNA synthesis
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25
SE of Lipopeptide ABX?
* Irritation at site of Injection * Skeletal muscle Pain and Weakness (Myopathy) * Increase in CPK (creatine phosphokinase) * Renal Failure
26
Where does Polymyxins ABX work?
* **Cationic detergents** (positive potential) disrupt the **membranes** of **Gram-negative Bacteria**
27
Pathogen spectrum of Polymyxins?
* Topical: **OTC ointments** * IV: Last resort for **Gram-negative infections** * **Ophthalmic drops** * **Otic drops**
28
SE of Polymyxins?
* **(IV) EXTREME Nephrotoxicity** and **Neurotoxic** * Sometimes used Internally for Multidrug resistant Strains * **Acinetobactor from the Middle East**
29
(2) ABX that **Inhibit Peptidoglycan Polymerization Synthesis**? (**Glycopeptides**)
* **Bactericidal** * Vancomycin * Bacitracin
30
(1) ABX that **Inhibits Cell Wall Synthesis** by Binding **PBP-3**? (Monbactam - monocyclic β-lactam)
* **Bactericidal** * **​**Aztreonam * Penicillin-binding-protein 3 (PBP-3)
31
(1) ABX that **Disrupt Outer Membrane** in * *Gram-negative Bacteria**?
* **Bactericidal** * **​**Polymyxins
32
ABX that inhibits Synthesis, **Para-aminobenzoic acid (PABA) inhibit Dihydropteroate Synthetase** in Nucleotide Synthesis? 1x - Bacteriostatic
* **Bacteriostatic** * **​**Sulfonamides
33
ABX that **Inhibit Dihydrofolate Reductase** for Nucleotide Synthesis? 2x - Bactericidal 2x - Bacteriostatic
* **Bactericidal** * **​**Trimethoprim (Dihydrofolate reductase) * Sulfamethoxazole (inhibit Folate synthesis) * **Bacteriostatic** * **​**Trimethoprim (Dihydrofolate reductase) * Pyrimethamine
34
ABX that Inhibit DNA gyrase - Type II and TYpe IV Topoisomerase? 1x - Bactericidal
* **Bactericidal** * Fluoroquinolones (must be taken w/ antacids)
35
ABX that Inhibit mRNA Synthesis? 1x - Bactericidal
* **Bactericidal** * **​**Rifampin (DNA-dependent RNA polymerase)
36
ABX that **Binds 23S, Blocks initiation of Complex formation of 50S Ribosomal subunit**? 1x - Bacteriostatic
* **Bacteriostatic** * Linezolid (Binds to 23S RNA)
37
ABX that Blocks release of Nascent Peptides from the Ribosome at 50S Ribosomal subunit? 1x - Bactericidal 1x - Bacteriostatic
* **Bactericidal** * **​**Quinupristin/Dalfopristin**​** * **Bacteriostatic** * **​**Macrolides (Erythromycin) (Methylation 23S rRNA)
38
ABX that Block peptide transfer (translocation) at 50S Ribosomal subunit? 1x - Bacteriostatic
* **Bacteriostatic** * Clindamycin
39
ABX that inhibits **Peptidyltransferase at 50S Ribosomal subunit**? 1x - Bacteriostatic
* **Bacteriostatic** * Chloramphenicol
40
ABX that **Inhibit formation of Initiation complesx** cause **miscoding** (misreading) of **mRNA** and **incorrect Amino acid** linking for Peptide formation? Blocking normal Protein Synthesis at 30S Ribosomal subunit? 1x - Bactericidal
* **Bactericidal** * **​**Aminoglycosides (Gentamicin)
41
ABX that Block binding of **aminoacyl-tRNA** and **Addition of Amino Acids** to the Peptide chain of **30S Ribosomal subunit**? 1x - Bacteriostatic
* **Bacteriostatic** * Tetracyclines
42
(1) ABX that works on **Dihydropteroate Synthetase** Enzyme that converts **PABA --\> Dihydrofolate**? (Inhibits Folate Synthesis)
* Sulfonamides
43
2x ABX that works on **Dihydrofolate reductase** enzyme for **Dihydrofolate --\> THF**?
* Trimethoprim * Pyrimethamine
44
(1) ABX that inhibits **DNA gyrase Topoisomerase II** and **Topoisomerase IV** activity?
* Fluoroquinolones
45
(1) ABX that **inhibits the formation of mRNA** from Nucleotides through blocking **DNA-dependent RNA Polymerase**?
* Rifampin
46
(2) ABX that works on **Translocase** enzyme for * *Peptide bond formation --\> Translocation**?
* Macrolides (23S subunit of 50S) * Clindamycin (50S)
47
(1) ABX that works on **Peptidyltransferase** at **50S Ribosomal subunit** enzyme for **Attach of AA-tRNA to Ribosome --\> Peptide bond formation**?
* Chloramphenicol (50S)
48
(1) ABX that binds to **30S**, blocks **Initiation Complex Formation --\> Attachment of aminoacyl-tRNA to Ribosome**?
* Tetracyclines (30S)
49
(2) ABXs that inhibit **Protein synthesis - -\> Initiation of Complex formation**?
* Aminoglycosides (30S) * Linezolid (23S subunit of 50S)
50
(3) Different ways Bacteria protect themselves from β-lactam drugs?
1. **Inactivation via β-lactamase** * Cleaving C-N ring 2. Changes in Drug target through **mutation of Binding site** * Transpeptidase changes 3. Decreased permeability, and **Efflux pumps (G- only)** * Restricting drug entry
51
SEs of Penicillin?
* **Hypersensitivity** * Urticaria, Pruritus, Fever, Anaphylaxis, Joint swelling * **Rash** * **Hemolytic anemia** * Coombs-positive
52
Clinical use of Penicillin?
* **Gram-positive** Bacteria * *S. pneumoniae* * *S. pyogenes* * *Actinomyces* * **Fastidious Gram-negative** Bacteria * *Neisseria meningitidis* * *T. pallidum* * **Gram-positive (Bactericidal)** * **​***Clostridia, Listeria, Bacillus* * Most anaerobes EXCEPT *B fragilis* group * **Spirochetes: Drug of choice for Syphilis** (Penicillin G)
53
Clinical uses of **Ampicillin** and **Amoxicillin** (Aminopenicillins)? "HELPS Slaughter Enterococcus" Am**O**xicillin is an **O**ral form of Ampicillin
* **Gram-positive** (moderate) * **Gram-negative** (moderate) * **UTI**s * **Neonatal infections (+ Gentamicin)** * **_HELPS_ **_S_**laughter **_E_**nterococcus** * ***_Haemophilus influenza_, _E coli_, Listeria, _Proteus mirabilis_, _Salmonella_, _Shigella_, Enterococcus*** * Used w/ **_Clavulanic acid_** --\> Extends coverage by protecting against β-lactamase * Gram-negative rods * *H influenzae, E coli, P mirabilis, Salmonella, Shigella* * 2nd Line Tx for **Lyme Disease**
54
SE of Ampicillin and Amoxicillin?
* **Hypersensitivity** * **Rash** * If they have mononucleolus and you give Ampicillin - -\> Full body Rash, Head to Toe (non-allergic rxn) * **Pseudomembranous colitis** (Colon colitis, C. dificille)
55
Clinical use of **Ticarcillin**, Carbenicillin, Piperacillin?
* Extended spectrum for **Gram-negative rods** including **Pseudomonas** * Synergistic w/ **Aminoglycosides** against **Pseudomonas** (both are Bactericidal)
56
SEs of **Ticarcillin**, Carbenillin, Piperacillin?
* **Hypersensitivity**; interference w/ _Platelet function_ --\> Bleeding * Used w/ **β-lactamase inhibitors** * **​**Ticarcillin + Clavulanic acid * Piperacillin + Tazobactam
57
What does **Clavulanic Acid**, **Sulbactam**, and **Tazobactam** do for β-lactam ABX? "**CaST**"
* Binds to β-lactamase and Prevents its Binding and Destruction of the β-lactam ring on suceptible Penicillins * Expands the spectrum of activity of β-lactam ABX * Used in combination w/ * Penicillin, Ampicillin, Piperacillin, Ticarcillin * Expands activity against: * Gram-positive Cocci --\> *S aureus* * Gram-negative Rods --\> *H influenza, Klebsiella* * Anaerobes --\> *B fragilis*
58
(2) First-generation **Cephalosporins** (β-lactam)?
* Cefazolin --\> surgical prophylaxis for *S. aureus* * Cephalexin
59
(5) Second-generation Cephalosporins (β-lactam)?
* Cefotetan * Cefuroxime * **Cefaclor** * **Cefprozil** * **Cefoxitin**
60
(4) Third-generation Cephalosporins (β-lactam)?
* Cefoperazone * **Ceftriaxone** --\> excreted in Bile, Renal Failure pts. * **Ceftazidime** --\> *Pseudomonas* * **Ceftriaxone** --\> Meningitis and *gonorrhea*
61
Clinical use of First-generation Cephalosporins (β-lactam)? "PEcK"
* **Gram-positive cocci** * URIs * **Gram-negative** * *P mirabilis* * *E coli* (G-neg) * *K pneumoniae* * β-lactamase sensitive
62
Clinical use of Second-generation Cephalosporins (β-lactam)? "+ and - HEN PEc**_K_**S
* **Gram-positive Cocci** * **Extended Gram-negative coverage** * *H influenzae* (G-neg) * *Enterobacter* * *Neiseria* (G-neg) * *P mirabilis* * *E coli* (G-neg) * *Klebsiella* (G-neg) * *S marcescens* * Mosderate (β-lactamase resistance
63
Clinical use of Third-generation Cephalosporins (β-lactam)?
* **Broad spectrum Gram-negative coverage** * Most **cross BBB** and are commonly used for **Meningitis** and **Sepsis****​** * ​E. coli * Proteu morabilis * Klebsiella * Enterobacter * Serratia * Citrobacter * Neisseria * H. Influenza * Strep. pneuonaie
64
Cephalosporin Rx for *Pseudomonas*?
Ceftazidime | (3rd generation)
65
Cephalosporin Rx for Gonorrheal infections?
Ceftriaxone | (3rd generation)
66
(1) Fourth-generation Cephalosporins (β-lactam)?
* Cefepime * Increased activity against ***Pseudomonas*** and **Gram-positive Cocci** due to increased resistance to β-lactamase
67
SEs of Cephalosporins?
* **Hypersensitivity** * **Increased Aminoglycoside nephrotoxicity** * **Methylthiotetrazole group (Cefotetan, Cefoperazone)** * can cause **_Disulfiram-like Rxn_ w/ _Ethanol_** and increased risk of Bleeding * **Cefaclor (2nd)** and **Cephalexin (1st)** can cause * *Serum sickness-like** reaction * **Vit. K deficiency**
68
Clinical use of Monobactams (Aztreonam) (β-lactam)?
* **Gram-negative rods ONLY** * ***Pseudomonas*** * **NO activity** against **_Gram-positive_** organsism or anaerobes * **NO Renal Involvement** * β-lactamase-resistant * Pts. who cannot tolerate Penicillins or Aminoglycosides * **SAFE IN PREGNANCY** * **No penicillin cross-reactivity**
69
SEs of Aztreonam (Monobactam)?
* **Nontoxic** * **No cross-sensitivity w/ Penicillins** * Occasional rash * GI distress * Fever * Phlebitis
70
Clinical use of Carbapenems?
* Impenem / Cilastatin * Meropenem decreased risk of seizures and is stable to dehydropeptidase I * Broad spectrum against - Broadest β-lactam available * **Gram-positive cocci** * **Gram-negative rods** * **Anaerobes** * **Pseudomonas** * **DOES NOT cover MRSA, VRE, Rickettsia, Chlamydia** * **Impenem + Cilastatin** --\> a Renal dehydropeptidase inhibitor prevents metabolism of Impenem by Kidneys
71
SEs of Imipenem / Cilastatin, Meropenem (Carbapenem)?
* Hypersensitivity * **Rash** * **GI distress** * Drug Fever * **Seizures at High Plasma lvls** (CNS toxicity w/ Imipenem) * Cross-reactivity w/ Penicillin * **Meropenem** is not degraded by Renal Dehydropeptidase and presents a Reduced risk of Seizures
72
How does Bacitracin work?
* Inhibits Peptidoglycan precursors from being transported across the Bacterial Cell Membrane
73
Clinical use of Bacitracin?
* Topical ABX for wound irrigation * Covers Gram-positive bacteria
74
SEs of Bacitracin?
* Nephrotoxicity prevents systemic use
75
How do Polymyxin work?
* Basic proteins that act like **Detergents** * They bind to and **disrupt the Cell membrane** of * *Gram-negative Bacteria** * "**MYX**ins **MIX** up Cell **M**embranes"
76
Clinical use of Polymyxin?
* Resistant Gram-negative infections * Resistant *Pseudomonas* in Cystic Fibrosis
77
SEs of Polymyxins?
* When given systemically; **Nephrotoxicity** (Acute tubular necrosis) and **Neurotoxicity**
78
How do Sulfonamides work?
* Bacteriostatic - Inhibits Folate Synthesis * Inhibits **Dihydropteroate synthetase** * Enzyme essential for conversion of * *PABA + Pteridine** --\> **Dihydrofolic acid** * Synthesis of **Purines, Thymidine** and **AAs** is impaired * Synergistic w/ Trimethoprim and Pyrimethamine
79
Clinical use of Sulfonamides?
* **Gram-positive** * **Gram-negative** * *_Nocardia_* (Tx in combination) * Chlamydia * *Toxoplasma* * Used w/ **Trimethoprim (TMP-SMX)** for **UTIs** * TMP - treats marrow poorly * *Salmonella* * *Shigella* * *Serratia* * *P jiroveci (PCP)* * Sulfadiazine - silver ointment for Burn infection
80
SEs of Sulfonamides?
* **Hemolytic anemia in G6PD deficiency** * **Kernicterus** in Neonates (hyperbilirubinemia brain dys.) * **Hypersensitivity** (including Stevens-Johnson syndrome) * **Photosensitivity** * **Interstitial Nephritis** * Nephrotoxicity (tubulointerstitial nephritis) * **Displace** other **Drugs** from Albumin * Warfarin
81
How does Trimethoprim and Pyrimethamine work?
* Bacteriostatic * Synergistic w/ Sulfonamides * Folic acid analog that inhibits **Dihydrofolate reductase (DHFR) Dihydrofolic acid -|-\> Tetrahydrofolic acid (THF)** * **Decreases** Sythesis of Purines, Thymine, and AAs Methionine and Glycine
82
Clinical use of Trimethoprim and Pyrimethamine?
* Trimethoprim used w/ Sulfonamides * UTIs * *Shigella, Salmonella, Pneumcystitis jirovecii* * Pyrimethamine + Sulfadiazine --\> Toxoplasmosis
83
SEs of Trimethoprim and Pyrimethamine?
* Bone Marrow Suppression * **Megaloblastic anemia** * **Leukopenia** * **Granulocytopenia** * GI Distress * Pruritus * Rash * Aleviated w/ supplemental **Folinic acid**
84
What are the Fluoroquinolones? "--Floxacin"
* **Cipro**-Floxacin * **Nor**-Floxacin * **Levo**-Floxacin * **O**-Floxacin * **Gati**-Floxacin * **Moxi**-Floxacin
85
How do Fluoroquinolones work?
* Bactericidal * Inhibit **DNA gyrase (Topoisomerase II)** and **Topoisomerase IV** * Bacterial enzymes that unwind, sever, and reanneal DNA during replication and transcription * **MUST NOT be taken w/ antacids** --\> Inhibit absorption
86
Clinical use of Fluoroquinolones?
* **Gram-negative Rods** that cause **UTI**s and **Gastroenteritis** * ***Pseudomonas*** * ***Neisseria gonorrhoeae*** * **Mycobacteria** * Atypicals such as *Mycoplasma* and *Legionella* * **Drug of choice for Anthrax** * **Some Gram-positive**
87
SEs of Fluoroquinolones?
* GI distress * Rash * Superinfections * CNS effects * Photosensitivity * **Prolonged QT interval** * **Contraindicated in Pregnant and Kids** --\> Cartilage Dmg * Leg cramps and Myalgias * Tendinitis and **Tendon rupture** (adults)
88
How does Chloramphenicol work?
* Bacteriostatic * **Binds** to **Peptidyltransferase** at **50S Ribosomal subunit** and **blocks** the Proper positioning of **tRNA** and the addition of **New AA** to the **Polypeptide chain**
89
Clinical use of Chloramphenicol?
* **Meningitis** * *Neisseria Meningitidis* * Streptococcus pneumoniae * *H influenzae* (penicillin allergy) * Rocky Mountain Spotted Fever (*Rickettsia rickettsii*) * Used topically for **Eye Infections**
90
SEs of Chloramphenicol?
* **Anemia** * Dose dependent * Idiosyncratic **Aplastic Anemia** (1/30,000 doses) * Dose independent * Reversible Bone marrow suppression * **Gray Baby Syndrome** * ​Lack of Hepatic **UDP-glucuronyl transferase** * Crosses the BBB and Placenta * Severe toxicities for multiple uses
91
What are the (3) Macrolides?
* Erythromycin * Azithromycin (Safe to use in Pregnancy) * Clarithromycin
92
How do Macrolides work?
* **Bacteriostatic** * Binds reversibly to the **23S rRNA** of the 50S Ribosomal subunit and **Blocks** the **Translocation step**
93
Clinical Use of Macrolides?
* Broad spectrum of Action * **STIs** * *Chlamydia* * *N gonorrhea*) * **Pneumonia** * Mycoplasma * Chlamydia * Legionella * **Streptococcal infection** in Pts. allergic to Penicillin * *C diphtheriae* * Nontuberculous Mycobacteria
94
SEs of Macrolides? "MACRO"
* Prolonged QT Interval * Esp. Erythromycin * Gastrointestinal **M**otility issues * **A**rrhythmia by prolonged QT * Acute **C**holestatic Hepatitis * **R**ashes * e**O**sinophilia (increases serum Theophyllines) * Allergy --\> Fever * **P450 inhibition** (Increases lvls of **Warfarin**)
95
How does Clindamycin and Lincomycin work?
* **Bacteriostatic** * Binds to **50S Ribosomal** subunit and Inhibits the **Aminoacl translocation step** by Blocking the Growth and Release of the Growing Peptide chain
96
Clincial use of Clindamycin and Lincomycin?
* Narrow spectrum, **Anaerobes** in mixed **infections** * **​*Bacteroides spp*** * ***Chlostridium perfringens*** * Aspiration pneumonia * Causative agent in Pseudomembranous colitis due to *C difficile* infection * Lung abscesses * Oral infections * **Safe in Pregnancy**
97
SEs of Clindamycin and Lincomycin?
* Pseudomembranous colitis (*C difficile* Superinfection) * GI distress (diarrhea) * Fever
98
What does **"buy AT 30, CELL at 50"**?
* **Protein Synthesis Inhibitors - specifically target smaller bacterial ribosome (30S + 50S = 70S)** * **A**minoglycosides and **T**etracyclines inhibit the **30S** Ribosomal subunit * **C**hloramphenicol, **E**rythromycin, **L**inezolid, and c**L**indamycin inhibit the **50S** Ribosomal subunit
99
How does Linezolid work?
* **Bacteriostatic** * Binds to the **23S** of the **50S** Ribosomal subunit and _inhibits_ **Initiation Complex formation**
100
Clinical use of Linezolid?
* MRSA * VRE * Oral medication for outpatient basis for these two bacteria
101
SEs of Linezolid?
* **Pseudomembranous colitis** (*C difficile* Superinfection) * **GI distress** * **Bone marrow suppression** may be treatment-limiting * **Ocular** and **Peripheral neuritis**
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How does Quinupristin / Dalforpristin work?
* **Bactericidal** * Combination of Streptogramin ABX binds to the **50S** Ribosomal subunit and inhibits Protein synthesis at (2) successive steps
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Clinical use of Quinupristin / Dalfopristin?
* MRSA * VRE
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SEs of Quinupristin / Dalfopristin?
* Phlebitis * Hyperbilirubinemia
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What are the Aminoglycoside drugs? "GNATS"
* **G**entamicin * **N**eomycin * **A**mikacin * **T**obramycin * **S**treptomycin
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How do Aminoglycosides work?
* Enter the Bacteria via an **O2-dependent transporter** * _Ineffective against Anaerobes_, since O2 is needed for drug uptake * **Inhibits formation** of the **30S** I**nitiaion complex** * **_Misreading_** of **mRNA --\> Aberrant proteins** * Prevents all Protein syn. at High concentrations * **Breakup of Polysomes**
107
Clinical use of Aminoglycosides?
* **Serious Gram-negative Rod** * **used in combination w/ β-lactam** for serious Gram-positive infections * **Neomycin** - given in the setting of **Bowel surgery** and **Hepatic encephalopathy** * Streptomycin - Mycobacteria * Spectinomycin - 2nd line Rx for *Gonorrhea*
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SEs of Aminoglycosides?
* "_mean_ **GNATS** ca**NNOT** kill anaerobes" * Contraindicated in Renal Insufficiency due to Reversible **Nephrotoxicity** (esp. w/ Cephaosporins) * **Neuromuscular blockade** * Hearing loss - Irreversible **Ototoxicity** * Esp. w/ Loop diuretics * "A Mean guy punched a baby in the ear" * NOT USED in Pregnancy --\> **Teratogenicity** * Fanconi Syndrome (Dys. of Renal electrolyte reabsorp.) * Neomycin - GI malabsorption and Superinfection
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What are the (4) Tetracycline Drugs?
1. Tetracyline 2. Doxycycline 3. Minocycline 4. Demeclocycline
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What is the (1x) Glycylcycline drug?
* Tigecycline
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How do Tetracyclines and Glycylcycline drugs work?
* Bacteriostatic * Inhibit the **30S** Ribosomal subunit by preventing the attachment of the **Aminoacyl-tRNA** to the **Ribosome** * Must be imported through the **Inner cytoplasmic membrane** via an energy-dependent Active Transport system only in Bacteria * **MUST NOT be taken w/ MILK, ANTACIDS, IRON-containing agents** * **​**Divalent cations inhibits proper absorption in the Gut * Limited CNS penetration
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Clinical use of Tetracyclines and Glycylcycline?
* Broad-spectrum * "VACUUM your BedRooM Tonight" * Tigecycline is a new drug used to treag Gram-negative infections resistant to other agents * 2nd Line after Penicilin for Syphilis
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Organisms covered by Tetracyclines? "VACUUM your BedRooMM Tonight"
* **V**ibrio cholerae * **A**cne * **C**hlamydia * **U**reaplasma **U**realyticum * **M**ycoplasma pneumoniae * **B**orrelia burgdorferi * **R**ickettsia * **M**ultidrig-resistant **M**alaria (*Plasmodium falciparum*) * **T**ularemia
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SEs of Tetracyclines and Glycylcyclines?
* GI distress * Tooth discoloration * Bone growth abnormalities in Young children * Photosensitivity * Fatty Liver disease in Women * Drugs past expiration date can cause Fanconi Syndrome * Minocycline - reversible vestibular toxicity * Demeclocycline - used to treat syndrome of Inappropriate antidiuretic hormone (SIADH) because it causes nephrogenic Diabetes Insipidus as an ADH antagonist
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How does Metronidazole work?
* **Bactericidal** * **Anti-Protozoal** * Bioactivation of the Drug in Anaerobic environments produces **toxic metaboites** that react w/ **Bacterial DNA**, Protein, and Bacterial and Protozoal cell membrane
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Clinical use of Metronidazole? "GET GAP w/ Metronidazole"
* Drug of choice for **Pseudomembranous colitis** (due to *C difficle) - "*GET GAP" * **Anaerobic infections below the Diaphragm** * **Antiprotozoal**: * ***G**iardia* * ***E**ntamoeba* * ***T**richomonas* * ***G**ardnerella vaginalis* * **A**naerobes (*Bacteroides, C. difficile*) * *H. **P**ylori* * Used w/ **Bismuth** and **Amoxicillin** (or Tetracycline) for *H pylori* "Triple therapy"
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Use these (3) drugs go get rid of *H pylori*? **BAM!**
1. **B**ismuth 2. **A**moxicillin 3. **M**etronidazole
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Antiproozoal Coverage w/ Metronidazole? "GET GAP on the metro(nidazole)"
* ***G**iardia* * ***E**ntamoeba* * ***T**richomonas* * ***G**ardnerella vaginalis* * **A**naerobes * *Bacteroides* * *Clostridium* * *H **P**ylori* (used w/ Bismuth and Amoxicillin or Tetracycline for Triple Therapy)
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SEs of Metronidazole?
* **Hypotension** * **Tachycardia** * **Flushing** * Headache * Nausea * **Dysguesia** - Metallic taste in Mouth * **Disulfiram-like Rxns w/ Ethanol** * **Teratogen** * DO NOT drink Alcohol w/ Metronidazole
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ABX Contraindicated in Pregnancy? "SAFe Moms Take Really Good Care"
* **Sulfonamides** --\> Kernicterus * **Aminoglycosides** --\> Ototoxicity * **Fluoroquinolones** --\> Cartilage damage * **Metronidazole** --\> Teratogenic * **Tetracyclines** --\> Fatty Liver in Mother, Impaired bone growth and Tooth discoloration in Baby * **Ribavirin** (antiviral) --\> Teratogenic * **Griseofulvin** (antifungal) --\> Teratogenic * **Chloramphenicol** --\> Gray Baby Syndrome * UDP-glucuronyl transferase
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Rx used for **Endocarditis w/ Surgical or Dental Procedures**?
Penicillins
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Rx used for **Gonorrhea**?
Ceftriaxone
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Rx for **History of Recurrent UTIs?**
TMP-SMX
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Rx for **Meningococcal infection**?
Ciprofloxacin (drug of choice for Adults) Rifampin (Children)
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Rx for **Pregnant woman carrying Group B Strep**?
Ampicillin (During Labor)
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Rx for **Prevention of Gonococcal or Chlamydial Conjunctivitis in Newborn?**
Erythromycin Ointmen in the eyes of all newborns
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Rx used for **Prevention of Postsurgcal infection due to *S. aureus***?
Cefazolin
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Rx for **Prophylaxis of Strep pharyngitis in Child w/ prior Rheumatic Fevor**?
Oral Penicillin
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Rx for **Syphilis**?
Benzathine Penicillin G
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Rx for **Pneumocystitis jirovecii**?
TMP-SMX
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Rx for **Exposure to *H. Influenza Type B meningitis****?*
Rifampin
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Rx for exposure to **Anthrax**?
Ciprofloxacin
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(7) Rx for **Pseudomonas**?
* Fluoroquinolones * Extended spectrum Penicillins * Polymixin * 3rd gen. Cephalosporins * Cefepime * Aztreonam * Aminoglycosides

Pharmacology (29 decks)

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