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PHRM 865: Theraputics V > Lecture 12: Aminoglycosides, Fluoroquinolones, Macrolides > Flashcards

Lecture 12: Aminoglycosides, Fluoroquinolones, Macrolides Flashcards

Erdman's Section

1
Q

What is the Mechanism of Action for the Aminoglycosides?

A
  • Irreversibly bind to 30s [maybe 50s] and decrease protein synthesis & mesread RNA
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2
Q

What are some of the Mechanisms of Resistance for the Aminoglycosides?

A
  • Alteration in AG uptake
  • Synthesis of AG modifying enzymes
  • Alteration in binding [Rare]
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3
Q

What are the Aminoglycosides that are used?

A
  • Gentamicin, Tobramycin, Amikacin, Streptomycin, Plazomicin
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4
Q

What is the Spectrum of Activity for Gram (+) for the Aminoglycosides?

A
  • NEVER USED ALONE; always low dose with cell wall agents
  • Virdian, Entercoccis [G or S], S. Aureus

MAINLY GENTAMICIN USED
Cell Wall Agents = Beta & Vanco

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5
Q

What is the Spectrum of Activity for the Gram (-) for the Aminoglycosides?

A
  • A,P>T>G; NOT S
  • PPPEEACKSSS
  • Pseudomonas Aeruginosa [Target]

HIGH DOSES with cell wall agents
Cell Wall Agents = Beta & Vanco

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6
Q

What is important to know about Mycobacteria in Aminoglycosides?

A
  • STREPTOMYCIN active aganist it
  • Maybe Amikacin too
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7
Q

What is important to know about the Pharmacology of the Aminoglycosides?

A
  • Highly Polar Cations = decreased oral administration
  • Vd and ClCr are the main parameters
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8
Q

What in important about Absorption in Aminoglycosides?

A
  • Bad oral = Good Parenteral
  • DONT USE IM in critically ill
  • IV is Preferred
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9
Q

What is important to know about Distribution in Aminoglycosides?

A
  • In Extracellular Fluids [Ascites, Pericardial, Peritoneal, Pleural…]
  • NOT CSF[even with inflammed meninges], sputum, adipose tissue
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10
Q

When discussing Distribution characteristics alter the Vd and Cl?

A
  • IBW should be used when >130% IBW
  • Vd is important when calulating a AG dose
  • Vdnormal = 0.25; Vddehydration = 0.15-0.20; Vdedema = 0.30-0.35

Vd is HIGHER in neonates and infants

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11
Q

What is important to know about Elimination in Amioglycosides?

A
  • Kidneys; so HIGH urinary conc.
  • Half Life = 2.5 - 4h [increase with renal issues]
  • Hemodialysis removes 30-50%
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12
Q

What is important to know about the dosing [Traditional & Extended] in Aminoglycosides?

A
  • Trad: 1-2.5 mg/kg/dose [Gram (+)]
  • Ext: G/T = 5-7 mg/kg daily & A = 15-25 mg/kg daily [Gram (-)]
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13
Q

What are the Major Clinical used for the Aminoglycosides?

A
  • A, G, T: Good for Gram (-); Pseudomonas Aeruginosa
  • G, S: Gram (+); Enterococci, Viridan, Staph
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14
Q

What are some of the Adverse Effects for Aminoglycosides?

A
  • Nephrotoxicity
  • Ototoxicity: 8th Cranial damage

prolonged high tough conc., 2w of treatment, renal issue for both

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15
Q

What are the Fluoroquinolones?

A
  • Ciprofloxacin, Ofloxacin, Levofloxacin, Gatifloxacin, Moxifloxacin, Gemifloxacin
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16
Q

What is the mechanism of action for the Fluoroquinolones?

A
  • Inhibition of DNA synthesis by binding to and inhibiting Topoisomerase [Gyrase & IV]

Conc. Dependent Bactericidal Activity

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17
Q

What is the difference between Gyrase and Topo IV?

A
  • Gyrase: blocks replication fork; Gram (-)
  • Topo IV: Stops DNA replication Gram (+)
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18
Q

What is the Mechanism of resistance for the Fluoroquinolones>

A
  • Alteration in Binding Site
  • Efflux: Enhances the transfer out
  • Alteratoin of Permeability: decrease FQ in cell
19
Q

What are the older and newer repiratory Fluoroquinolones?

A
  • Old: Cipro
  • New: Levo, Moxi, Gem [Maybe Dela]

All help with Strep

20
Q

What is the Spectrum of Activity for the Gram (+) for the Fluoroquinolones?

A
  • Cipro = POOR & Levo, Moxi, Dela = GOOD
  • Group/Viridan, PRSP [NOT CIPRO], MSSA, MRSA [ONLY DELA]

Mainly ALL respiratory things
FQs NEVER used in S. Aureus

21
Q

What is the Spectrum of Activity of the Gram (-) for the Fluoroquinolones?

A
  • HENPECKSSS
  • Pseudomonoas Aeruginosa [Cipro>Levo>Dela; NOT Moxi or Gemi] Target
22
Q

How does the Fluoroquinolones act toward the Atypical Bacteria?

A
  • Extremly active to Legionella
  • One of the claim to fames
23
Q

What are some important things to note about the Pharmacology of Fluoroquinolone?

A
  • Rapid, Conc. Dependent
  • AUC/MIC
  • Has PAE

AUC/MIC: 30-50 S. Pneumoniae; 100-125 for Gram (-)

24
Q

What is important to know about the Absorption for the Fluoroquinolones?

A
  • ORALLY absorbed
  • Bioavailability: 70-75% for Cipro and >90% for Levo/Moxi
25
Q

What is important to know about the Distribution fo the Fluoroquinolones?

A
  • Good Tissue Penetration [because of F-]: Prostate, Lung, Bronchial, Sputum, Bone
  • High Urine Conc. [NOT Moxi & Gemi]
  • Minimal CSF penetration
26
Q

What is important to know about the Elimination of the Fluoroquinolones?

A
  • Renal [Levo, Oflox, Gati]: Dosage Adjustments are necessary
  • Hepatic [Trova, Moxi]
  • Renal & Hepatic [Cipro & Dela]
  • NONE ARE REMOVED DURING HEMO
27
Q

What are some of the clinical uses of the Fluoroquinolones?

A
  • CAP: all respiratorys
  • Bronchitis/Sinusitis
  • HAP
  • UTI
  • Prostatitis
  • Skin Infections
28
Q

What are some of the adverse effects of the Fluoroquinolones?

A
  • GI, Neurologic
  • Hepatotoxic
  • OTc Prolongation
  • Articular Damage: AVOID IN PREGNANCY/BREAST FEEDING
  • Tendonitis
29
Q

What are some of the drug interactions for the Fluoroquinolones?

A
  • Divalent and Trivalent cations: Impair ANY absorption
  • Warfarin
30
Q

What is the differences in the chemical structures between Erythromycin, Azithromycin, and Clarithromycin?

A
  • Clarith: Methoxy group on C-6
  • Azithro: 15-membered ring with an Azalide
31
Q

How does the structural difference between Clarithromycin and Azithromycin have advantages over Erythromycin?

A
  • They will improve oral bioavailability, antibacterial activity, tissue penetration, prolong half life
32
Q

What are the Macrolides that are used?

A
  • Erythromycin, Clarithromycin, Azithromycin
33
Q

What is the mechanism of action for the Macrolides?

A
  • Binds to 50s during synthesis and suppresses bacterial growth
34
Q

What is the Mechansim of resistacne for the Macrolides?

A
  • Efflux Pumps: Low level resistances
  • Alteration of Binding: High Level of resistance AND others that bind to 50s
  • Cross reactivity among MACs

Time Dependent & Bacteriostatic

35
Q

What is the Spectrum of Activity of the Gram (+) for the Macrolides?

A
  • C>E>A [Clarith is da best]
  • Group/Viridan Strep, PSSP, MSSA, Bacillus, Corynebacterium
36
Q

What is the Spectrum of Activity of the Gram (-) for the Macrolides?

A
  • A>C>E [Azith is da best; NOT enterbacteriacea
  • H. Influenzae, M. Catarrhalis, Neisseria
37
Q

What is the Spectrum of Activity for the Other Organism for Macrolides?

A
  • Legionella & Mycoplasma [Azith & Clarith]
38
Q

What is important to know about the Absorption of the Macrolides?

A
  • Eryth: Bioavailability 15-45%; Some have EC so they get absorbed
  • Clarith: Stable in GI
  • Azith: Stable in GI
39
Q

What is important to know about the Distribution of the Macrolides?

A
  • Tissues and Cells [Except the CSF]
40
Q

What is important to know about the Elimination of the Macrolides?

A
  • Eryth: From Bile; Half Life = 1.4h; NO dosage adjustment
  • Clarith: From Urine; Half Life = 3-7h; Dosage adjustment when CrCl < 30
  • Azith: From Bile; Half Llife = 68h
41
Q

What are some of the main clinical uses for the Macrolides?

A
  • Repiratory Tract Infection [CAP, H. Flu, Strep Pneumo]
  • STI [1g of Azith for Chalmydia]
  • Mycobacterium avium Complex Infections [MACs for MAC]
42
Q

What are some of the Adverse Reactions for the Macrolides?

A
  • GI [MOST COMMON; cant take with food to help]
  • Thrombophlebitis
  • QT Prolongation
43
Q

What are some of the drug interaction for the Macrolides?

A
  • Eryth & Clarith inhibit P450, increases conc of the follow:
  • Theophylline, Carbamazepine, valproate, Cyclosporine, Digoxin, Phenytoin, Warfarin

PHRM 865: Theraputics V (42 decks)

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