Pharm antibiotics part 2 Flashcards
Antimicrobial agents- MOA
Part 1: cell wall synthesis and cytoplasmic membrane structure
* betalactams= Penicillins, Cephalosporins, Carbapenems, Monobactam
* glycopeptides= Vancomycin
* cyclic lipopeptide= Daptomycin
Part 1: target DNA or DNA replication
Antimetabolites: sulfonamides and trimethoprim
Fluoroquinolones: Ciprofloxacin, Levofloxacin, Ofloxacin
Now= block production of new proteins= bacterial ribosome
Aminoglycosides: neomycin, Gentamicin, Tobramycin, and amikacin, strptomycin
Tetracyclines: tetracycline, doxycycline, minocycline
Macrolides: Erythromycin, Clarithromycin, Azithromycin
Clindamycin
Linezolid
Chloramphenicol
Aminoglycosides types
- Gentamicin
- Tobramycin
- Amikacin
- Plazomicin
- Streptomycin
- Neomycin
- Paromomycin
Aminoglycosides MOA
- cause addition of incorrect aa resulting in synth of abn proteins
- cause misreading of mRNA and terminate protein synth
- Bind to 30S ribosomes and block the initiation of protein synth
Pharmacodyn and kinetic prop of Aminoglycosides
- Favorable target: Aerobic Gram - rods and mycobacteria
- Postantibiotic effect PAE= persistent suppression of growth after drug done
- Conc dependent killing characteristics-> higher conc induce more rapid killing
- Synergistic effect= in combo, MC cell wall active agents to help target gram positive bacteria
- Absorption= peak conc -> 30-60 min IV and 30-90 min IM
Aminoglycoside Toxicity
Nephrotoxicity
Ototoxicity
Neuromuscular blockade
Aminoglyc routes and indications
*Neomycin-> topical with Bacitracin and Polymyxin
* Gentamicin: topic, opth, systemic-> Group B streptococcus
* Tobramycin: Inhalation for CF patients with pseudomonas infections
* Streptomycin: second line drug for TB
General Aminoglycosides indications
- Septicemia
- Complicated UTI
- complicated Intraabdominal
- combo with others for drug resistant organisms
- topical drugs in conjunc for Otitis Externa
Otitis External- swimmers ear
mc: STAPH AUREUS AND PSEUDOMONAS AERUGINOSA
topical only: Fluoroquinolones ie
* ciprofloxacin
* Ofloxacin
AB with glucocorticoid: hydrocortisone, Dexamethasone, Prednisolone
* Neomycin
* Tobramycin
* Gentamycin
* allllllllll aminoglycosides
* combos: neomycin, polyyxin B, hydrocort= Cortisporin otic
* Combos: tobramycin and dexamth= Tobradex- opthalmic solution
Fluoroquinolones:
* Ciprofloxacin and Ofloxacin
* combos
ciprofloxacin and dexamethasone-Ciprodex
ciprofloxacin and hydrocortisone- Cipro HC Otic
DO NOT GIVE STEROID IN PERFORATED EAR DRUMS
Otitis External- swimmers ear
mc: STAPH AUREUS AND PSEUDOMONAS AERUGINOSA
topical only: Fluoroquinolones ie
* ciprofloxacin
* Ofloxacin
AB with glucocorticoid: hydrocortisone, Dexamethasone, Prednisolone
* Neomycin
* Tobramycin
* Gentamycin
* allllllllll aminoglycosides
* combos: neomycin, polyyxin B, hydrocort= Cortisporin otic
* Combos: tobramycin and dexamth= Tobradex- opthalmic solution
Fluoroquinolones:
* Ciprofloxacin and Ofloxacin
* combos
ciprofloxacin and dexamethasone-Ciprodex
ciprofloxacin and hydrocortisone- Cipro HC Otic
DO NOT GIVE STEROID IN PERFORATED EAR DRUMS
Tetracyclines types
- Chlortetracycline
- Minocycline
- Doxycycline
- Eravacycline
- Sarecycline
- Omadacycline
Tetracyclines MOA
- Bacteriostatic
- Passive diffusion and transporter uptake
- inhibit protein synthesis
- aerobic gram + and -
- Intracellular bacteria:
* rickettsiae
* chlamydiae
* mycoplasmas
Tetracyclines MOA
- Bacteriostatic
- Passive diffusion and transporter uptake
- inhibit protein synthesis
- aerobic gram + and -
- Intracellular bacteria:
* rickettsiae
* chlamydiae
* mycoplasmas
Pharmacokinetics Doxycycline and Minocycline
absorption, distribution, excretion, classification
Absorption
* 95-100% absorbed orally, duodenum, ALL TETRAC IMPAIRED BY MULTIVALENT CATIONS- Ca, Mg, Fe, Al
* Doxycycline and minocycline absorption NOT IMPAIRED BY FOODS
Distribution
* CROSS PLACENTA, NOT INDICATED IN PREGNANCY
* high tissue penetration except CSF
Excretion
* mainly in bile and urine
* Doxycycline: elim by nonrenal mechanisms, no dose adjustment required in renal failure
Classification:
* short acting- regular tetra: 6-8 hours
* long acting- doxy and mino: 16-18 hours
Tetracyclines- Side effects
- Photosensitivity- doxy is biggest culprit
- GI disturbances- dose related, abdominal discomfort, food decrease symptoms
- Hepatotoxicity- rare
- Audiovestibular- dizziness, vertigo, tinnitis= Doxy and mino
- Teeth and bone- calcium attaches to and deposit in bone
Doxycycline/Minocycline indications
broad uses
- Acne
- Rosacea
- URI
- Pneumonia CAP
- Chlamydia
- Syphilis
- GU
- Anthrax
- Malaria
- tick borne disease
- H. Pylori
- other= ehrlichiosis, anaplasmosis, plasmodium, mycobacteria
Helicobacter Pylori
H. Pylori
4 drug therapy:
1. Proton pump inhibitor PPI
2. Bismuth subsalicylate
3. Tetracycline
4. Metronidazole
Bismuth Quadruple Therapy for 10-14 days
Macrolides types
- Erythromycin
- Clarithromycin
- Azithromycin
Macrolides MOA
inhibit bacterial synthesis
Macrolides AE
- GI upset
- acute cholestatic hepatitis-> fever, jaundice, imparied liver fxn
- Prolonged QT interval- effect potassium ion channels
- hearing loss and exacerbation of Myasthenia Gravis