Bactericidal inhibitors of bacterial protein synthesis Flashcards
Aminoglycosides types
- gentamicin
- tobramicin
- bactericidal inhibitors of protein synthesis–> concentration dependent agents (require a certain concentration to be reached in order to have full effect)
aminoglycosides uses
1) GRAM - (CRE)
2) severe gram - infections (multi drug resistant organisms)
3) some pre op
- Gram + and Gram -
aminoglycosides US boxed warnings
1) nephrotoxicity- irreversible
2) ototoxicity - typically irreversible (ppl with renal dysfunction are more susceptible to this)
3) pregnancy- fetal harm
- these kind of limit use
MOA of aminoglycosides
inhibits bacterial protein synthesis
bactericidal
Routes of aminoglycosides
IV (can use IV formulation for inhalation for tobramycin- cystic fibrosis patients)
Metabolism/ excretion of aminoglycosides
pharmacy to dose- peaks for concentration dependent killing, troughs to minimize toxicity
Rare affect of aminoglycosides
aminoglycoside induced neuromuscular blockade –> paralyzes patients
Antimetabolites (2)
1) sulfonamides
2) trimethoprim
Sulfonamides (1)
sulfamethoxazole / trimethoprim (bactrim)
- inhibit folic acid synthesis
-antimetabolites
sulfonamide uses
cellulitis, uti, Gram +, good MRSA coverage
MRSA, MSSA, Gram +
sulfonamide MOA
inhibit folic acid synthesis
- trimethoprim combined with this inihibits folic acid synthesis via a different pathway
sulfonamide Contradindications
history of drug induced immune thrombocytopenia
ADR of sulfonamide
1) hyperkalemia (blocks Na channels in the distal nephron, inhibits potassium secretion, potentially fatal)
2) hypersensitivity reaction - delayed and immediate
- immediate- typical rash, angioedema, anaphylaxis
- delayed - stevens johnson syndrome , toxic epidermal necrolysis (severe forms of rashes)
metabolism/excretion sulfonamide
Renal adjusment needed
Sulfacetamide
topical for acne, bacterial infections, scaling dermatoses, ophthalmic infections
Silvadene
silver sulfadiazine - topical for burn treatment- prevention and treatment of wound sepsis
sulfadizine
toxoplasmosis treatment - first line
Fluoroquinolones indications
- broad spectrum –> cover GRAM + and atypical organisms
- MOXIFLOXACIN (BROADEST) –> ANAEROBES
- do not cover MRSA
- Levofloxacin (levaquin)/ moxifloxican –> respiratory Fluoroquinolones
- Ciprofloxacin (CIPRO) –> non-respiratory Fluoroquinolones (belly button down)
-gram +, gram -, pseudomonas, atypicals and moxifloxacin does anaerobes, some MSSA
US box warnings Fluoroquinolones
1) serious adverse reactions –> tendinitis and tendon rupture, peripheral neuropathy, CNS effects
2) Exacerbation of myasthenia gravis –> avoid in patients with MG
MOA Fluoroquinolones
Promotes DNA strand breakage via inhibition of topoisomerase
Routes of Fluoroquinolones
Oral (xr tablets/ solution)
IV
ophthalmic/otic
Metabolism/excretion Fluoroquinolones
- require renal adjustment
- absorption decreased by POSITIVE CATIONS (2 hours before or 6 hours after)
Fluoroquinolones ADRs (severe)
1) CNS effect/neuroexcitation
2) QT interval prolongation
3) tendon rupture/ tendinopathy
4) phototoxicity
Metroidazole (flagyl) Indications
Anaerobic bacterial infections (bacterial vaginosis), trichomoniasis, surgical prophylaxis
- THE BEST ANAEROBIC AGENT
