Pharmacology Flashcards
Penicillin/Aminoglycosides
Increases the penetration of aminoglycosides since penicillin will break down cell walls
Postantibiotic Effect
Persistent effect of antibiotic effect on growth after only brief exposure to the drug
*Exhibited by aminoglycosides and fluoroquinolones
Prevents the cross linking of peptidoglycan by inhibiting transpeptidases
Penicillin / Cephalosporins / Carbapenems / Aztreonam
Inhibitor of peptidoglycan synthetase
Vancomycin
Inhibitors of 30s ribosome
Aminoglycosides
Inhibitors of peptidyl transferase
Chloramphenicols
*Decreased peptide bond formation
Inhibitors of 50s ribosome
Erythromycin / Clindamycin / Linomycin
“Macrolides”
Inhibits binding of aminoacyl tRNA to ribosome
Tetracyclines
Binds the 23s ribosome
Linezolid / Streptogramins
Cationic Detergents (Interference w/ cell membrane)
Polymixin B / Colistin
Inhibits DNAP
Rifampin
Inhibits action of DNA gyrase
Fluoroquinolones
*Inhibits the negative supercoiling of bacterial DNA
Inhibitors of lipid synthesis
Isoniazid
Inhibitors of folic acid synthesis
Sulfonamides / Trimethoprim
Reasons why you might start empiric coverage
- Site of infection is difficult to culture
- Brain abscess, pneumonia, middle ear infxn - Serious or life-threatening condition
- Empiric therapy- given as a broad treatment
Drugs that interfere w/ Warfarin
Bactrim & Erythromycin
Drugs that interfere w/ Theophylline
Ciprofloxacin
Drugs that interfere w/ SSRIs
Linezolid
What antibiotics do antacids interfere with?
FQNs and Tetracycline
Bactrim
Trimethoprim + Sulfamethoxazole
Treats Gram + (minus MRSA & VRE), ^PEK and CE, and Chlamydia, Cloroquine (R) malaria, Toxoplasmosis, and Pneumocystis carinii
Interactions: Warfarin => Potentiates effects causing excess clotting
Methotrexate => Increases free methotrexate in the blood
Which drugs inadequately reach the lungs?
Aminoglycosides
Abscesses and antibiotics
Must be drained before antibiotics can adequately do their job
“Piddly” Gram neg organisms
Haemophilus, Morganella, Moraxella, Shigella, Salmonella
Neisseria, Providencia
“Fence” Gram neg organisms
Proteus, E. Coli, Klebsiella
SPACE Gram neg organisms
Serratia
Pseudomonas
Acinetobacter
Citrobacter
Enterobacter
“Atypical” Orgs
Legionella
Mycoplasma
Chlamydia
Anerobic Gram neg organisms
Bacteroides
Clostridium
Peptostreptococcus
SPACE bug antibiotic coverage
Cell Wall Inhibitor + FQN OR Aminoglycoside
(Penicillin/Cephalosporin/Carbapenem)+ (Ciprofloxacin/Levofloxacin) OR (Gentramycin/Topramycin)
*Ace in the hole = Aztreonam
Penicillin General Structure
- Thiazolodine Ring (House)
- B-lactam ring (Garage)
- Acyl side group (chimney)
Targets of B-lactam antibiotics
PBPs
Cockroft-Gault Equation
(140-age)(Weight in kg)/([Creatinine])(72)
- Must account for renal insufficiencies
- If female, multiply by .85
Used to calculate renal excretion
Poor areas of penicillin distribution
Insoluble in lipid
=>CNS, Brain, Prostate
Adverse effects of penicillin
Allergic rxn =>Maculopapular rash
Interstitial nephritis (especially w/ methicillin)
Pseudomembranous colitis
Anti-staphylococcal penicillins
Methicillin, Oxacillin, Nafcillin
Aminopenicillins
Ampicillin / Amoxicillin
- Amino group allows for penetration into cell walls
- Treats strep, proteus, entero, salmonella, shigella, haemophilus
- Drug of choice for Enterococcus
Carboxypenicillins
Carbenicillin / Ticaricillin
- Has increased permeability to cell walls
- Works against PIDDLYs, SPACE, and Strep
- Can be causes dysfunctional platelets; Ticarcillin has high Na+ content
Ticarcillin hazards
Dangerous for CHF patients due to the high Na+ content
- Can also cause platelet dysfunction
- Replace w/ piperacillin
Augmentin
Amoxicillin + Clavulonic Acid
=>B-lactamase inhibitor adds Staphylococcus and anaerobe coverage
Timentin
Ticarcillin + Clavulonic Acid
=>B-lactamase inhibitor adds Staph and anaerobes to the spectrum
Cephalosporin Structure
- Dihydrothiazine ring (House)
- B-lactam ring (Garage)
- Acyl Side Chain (Chimney)
* Cephalosporins have TWO R-groups; one on the acyl side chain and one on the dihydrothiazine ring
R1= Spectrum of Activity
R2= Stabilizer; increases t^1/2
Cephalosporin Distribution
Well-distributed; oral form is completely absorbed by the GI tract
- CSF penetration is extra efficacious w/ inflammation
- Usually use 4x Ceftriaxone
Elimination of Cephalosporins
Hepatic => Ceftriaxone, Cefoperazone
Renal => Everything else`
Adverse effects of Cephalosporins
*Presence of NMTT side chain on certain drugs can interfere w/ Vitamin K dependent clotting factors => bleeding
(Cefamandole, Cefoperazone)
- Presence of NMTT along w/ alcohol consumption => severe sickness
- 10% cross reactivity w/ penicillin => Possible allergies
1st Generation Cephalosporins
Cefazolin
Good for treating Gram + and Piddly Gram -
2nd Generation Cephalosporins
Cefuroxime
Good for treating Gram + and Gram - H. flu and PEK (fence)
2nd Generation Cephalosporins (Cephamycins)
Cefoxitine and Cefotetan
Good against Gram +, H. flu and PEK, AND ANAEROBES
Third Generation Cephalosporins
Ceftriaxone and Cefotaxime
Covers Strep and up to SACE gram negs
Third Generation Cephalosporins (antipseudonomal)
Ceftazidime and Cefoperazone
Covers SPACE
Fourth Generation Cephalosporins
Cefapime
Gram + and SPACE
5th Generation Cephalosporin
Ceftarazine
Staph, Strep, and Enterococcus and SCE
Drugs used for surgical prophylaxis
Cefazolin
-Will cover Staph aureus infxns that can occur when penetrating the skin
Imipenem
Treats all bacteria except for the atypicals
Undergoes extensive renal metabolism; add cilastatin to prevent
*Toxicity => Seizures, possible hematologic disorders
Ertapenem
Weaker version of imipenem/meropenem that doesn’t cover enterococcus or psedomonas
*Requires less doses
Aztreonam
Good against all gram neg organisms but saved for severe, life-threatening conditions
Monobactam antibiotic: structured much like penicillin
*Can also be used if penicillin allergy present
Problems with Aminoglycoside Distribution
Poor concentrations to the lungs and CSF w/ inflammation
*Also has poor absorption in the gut
Adverse Effects of Aminoglycosides (Neomycin)
Nephrotoxicity- occurs when the trough levels are too high
Ototoxicity- occurs when the peak levels are too high
Treatment of TB
Streptomycin
Indications for use of neomycin
- Surgical prophylactic for colorectal surgery- suppresses growth of intestinal flora
- Hepatic coma- decreases number of NH4 forming flora
- Hyperlipidemia- decreased flora => decreased cholesterol absorption