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Anti-biotics that have beta-lactam rings
Pennicillins, Cephalosporins, Carbapenems, Monobactams
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Anti-biotics that inhibit bacterial cell wall synthesis
Penicillins, Cephalosporins, Carbapenems, Monobactams, Vancomycin, Telavancin, Fosfomycin
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Protein syntehsis inhibitor anti-biotics
Tetracyclines, Macrolides, Lincosamides, Streptogramins, Aminoglycosides, Linezolids
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Cell membrane disrupters
Polymyxin, Daptomycin
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Nucleic acid synthesis inhibitors
Rifampin, Rifaximin, Fluoroquinolones, Metronidazole
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Folate synthesis inhibitors
Sulfonamides, Trimethoprim
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Anti-mycobaterials (TB, leprosy)
Isoniazid, Ethambutol
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Penicillin catagories
- Natural penicillins
- Aminopenicillins
- Antipseudomonal penicillins
- Antistaphylococcal pennicillins
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amoxicillin + clavulanate
Augment
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ampicillin + sulbactam
Unasyn
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piperacillin + tazobactam
Zosyn
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natural penicillins
- penicillin G (IV, IM)
- penicillin V (oral, IM)
- Gram +
- interstitial nephritis
- anaphylaxis
- beta-lactamase inactivation
- Take penicillin V (oral) on empty stomach
- renal elim
- high dose seizure
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MOA of penicillins
irreversible suicide-inhibition of transpepitidase enzyme
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Aminopenicillins
- ampicillin (IV, PO)
- amoxicillin (PO)
- Gram +, little more Gram -
- beta lactamase inactivation
- renal elamination
- high dose seizure
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Anti-pseudomonal penicillins
piperacillin (IV)
- Gram +, even more Gram -
- beta lactamase inhibition
- renal elimination
- high dose seizure
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Anti-staphylococcal penicillins
- nafcillin (IV)
- dicloxacillin (PO)
- staphlococcus
- poor activity against non-staph
- not staphlococcal beta-lactamase vulnerable
- hepatic elimination
- Take dicloxacillin on empty stomach
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1st generation cephalosporins
- cephalexin (PO)
- cefazolin (IV)
Gram + >> Gram -
- renal excretion
- seizure
- anaphylaxis
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2nd generation cephalosporins
- cefuroxime (IV, PO)
- cefoxitin (IV)
Gram - ~ Gram +
- renal excretion
- seizure
- anaphylaxis
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3rd generation cephalosporins
- ceftriaxone (IV) (BILIARY)
- ceftazidime (IV)
- cefdinir (PO)
- cefixime (PO)
Gram - >> Gram +
- renal excretion
- seizure
- anaphylaxis
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4th generation cephalosporins
cefepime (IV)
broad spectrum
- renal excretion
- seizure
- anaphylaxis
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5th generation cephalosporins
ceftaroline (IV)
- broad spectrum
- not susceptible to MRSA b-lactamases
- renal excretion
- seizure
- anaphylaxis
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Carbapenems
- ertapenem INVANZ
- meropenem MERREM
- imipenem/cilastatin PRIMAXIN
- broad spectrum
- not vulnerable to beta-lactamases
- inhibit lactamases, but also induce them
- poor chemical stability
- inactivated by renal dehydropeptidase 1
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renal dehydropeptidase
inactivates imipenem
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cilastatin
renal dehydropeptidase inhibitor
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Monobactams
aztreonam (IV, inh for CF)
- Gram - only
- not vulnerable to beta-lactamase
- renal elimination
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MOA of vancomycin and telavancin
- vancomycin (IV, PO - GI infect)
- telavancin (IV)
binds to terminus of growing peptidoglycan peptides
- Gram +
- not beta-lactamase inactivated (no b-lactam ring)
- renal elimination
- Maintain adequate hydration
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basic antibiotic counseling points
- complete full therapy course
- may decrease OC efficacy - use back up
- GI upset
- seizure - cephs
- anaphylaxis - cephs
- fatal colitis - cell wall inhibitors
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Name antibiotics eliminated hepatically
- dicloxacillin - anti-staph penicillin
- azithromycin, erythromycin - macrolides
- clindamycin - lincosamides
- quinupristin/dalfopristin - streptogamins
- linezolids
- rifampin, rifaximin - rifamycins
- ciprofloxacin, moxifloxacin, levofloxacin - fluoroquinolones
- metronidazole
- isoniazid
- doxycycline
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MOA of fosfomycin
fosfomycin (PO)
inhibits enolpyruvate transferase which blocks the formation of cell wall acetylmuramic acid (NAM)
- broad spectrum
- not beta-lactam susceptable (no b-lactam)
- renal elimination
- maintain adequate hydration
- powder that must be dissolved in cold water and taken immediately
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what does transpeptidase do?
cross links polypeptide chains in peptidoglycan cell walls for structure to keep the cell from lysing
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what makes MRSA resistant to anti-biotics
methacillin resistant staph aureus has a MecA gene that encodes a form of transpeptidase that is poorly inhibited by beta-lactams
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beta-lactamase
is a resistance form where the bacteria has produced an enzyme to break down drugs with a beta-lactam ring. the beta-lactamase can use water to regenerate itself and release the drug with an inactivated open beta lactam ring
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Name 3 beta-lactamase inhibitors
- clavulanate
- tazobactam
- sulbactam
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Drugs INHIBIT enzymes. Enzymes INACTIVATE drugs.
bacteria and drugs can be VULNERABLE or RESISTANT to each other.
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Classes of drugs that have beta-lactam rings
- penicillins
- cephalosporins
- carbapenems
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MOA of folate synthesis inhibitors
block dihydropteroate synthetase (sulfonamide) or dihydropteroate reductase (trimethoprim) which blocks the production of tetrahydrofolic acid, purines, and ultimately the production of DNA, and RNA
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MOA of rifamycins
binds and inhibits RNA polymerase
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MOA of fluoroquinolones
Inhibits DNA gyrase and blocks mRNA production
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MOA of metronidazole
breaks apart DNA
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MOA of polymyxin
Cell membrane disrupter
detergent disruption of OUTER then INNER membrane, causes cell lysis
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MOA of daptomycin
calcium dependent detergent disruption of INNER membrane causing cell lysis
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Gram positive cocci
- Staphlococcus aureus
- Staphlococcus epidermidis
Anaerobes: Peptococcus, Peptostreptococcus
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Gram positive diplococci (pairs)
Streptococcus pneumoniae
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Gram positive cocci chains
- Streptocuccus pyogenes
- Group B Strept
- Viridans Streptococcus
- Enterococcus
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Gram positive bacilli
- small: Listeria
- Large and anaerobic: Clostridium
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Gram negative cocci
- Neisseria meningititis
- Neisseria gonorrhoeae
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Gram negative bacilli
- Escherichia coli
- Klebsiella
- Proteus
- Serratia
- Pseudomonas
- Acinetobacter
- Citrobacter
- Enterobacter
Anaerobe: Bacteroides
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Gram negative coccobacilli (respiriatory GNB)
- Haemophilus influenzae
- Moraxella catarrhalis
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Coagulase positive Staphlococcus
- MSSA Methacillin sensitive Staph aureus
- MRSA Methicillin resistant Staph aureus
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Coagulase negative Staphlococcus
- Staph epidermidis (plastic)
- Staph saprophyticus
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SPACE
- Serratia
- Pseudomonas
- Acinetobacter
- Citrobacter
- Enterobacter
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Name anti-biotic drug classes that inhibit synthsis of proteins
- tetracyclines
- macrolides
- lincosamides
- streptogramins
- aminoglycosides
- linezolid
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MOA of tetracyclines
- tetracycline (PO, IV)
- doxycycline (PO, IV)
binds reversibly to 30S subunit of bacterial ribosome and blocks tRNA from docking -> inhibits protein synthesis
- broad spectrum
- avoid dairy, Fe, or Ca
- photosensitivity
- take with full glass of water
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MOA of macrolides
- erythromycin (PO, IV)
- azithromycin (PO, IV)
binds to 50S subunit of bacterial ribosome and blocks formation of elongation complex -> inhibits protein synthesis
- Gram +, Gram -
- Take with food if GI upset
- hepatic elimination
- QT prolongation
- inhibits CYP3A4
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MOA to lincosamides
clindamycin (PO, IV)
binds to bacterial ribosome 50S and blocks protein elongation
- Gram +
- diarrhea
- take with full glass of water
- hepatic elination
- [severe fatal colitis]
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MOA of streptogramins
- quinupristin (IV)
- dalfopristin (IV)
- quinupristin + dalfopristin SYNERCID
dalfopristin increases binding of quinupristin to the bacterial 50S ribosomal subunit and blocks elongation
- Gram +
- myalgia and flu-like symptoms
- hepatic elimination (t50 = 0.85hr)
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MOA of aminoglycosides
- gentamicin
- tobramycin
- amikacin
- neomycin
- bind to ribosome and blocks proof reading -> incorporation of wrong AAs
- must be activily transported into cells
- Gram - (enteric)
- HA, dizzines, tinnitis
- Ototoxic (irrevers)
- Neprhotoxic (revers)
- Cell wall inhibitors increase penetration
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MOA of oxazolidinones
linezolid (PO)
binds to unique site on bacterial ribosome 50S and inhibits the formation of initiation complex -> inhibits protein synthesis
- Gram +
- hepatic elimination
- lots of GI upset
- Gently mix oral solution before admin
- No MAOIs within 2 weeks
- Avoid tyramine foods
- Bone marrow suppression
- Serotonin Syndrome
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MOA of polymyxins
- polymixin B
- polymixin E
- (top, Otic, Opth, IM, IV)
detergent disruption to OUTER then inner cell membrane -> causes lysis
- Gram -
- renal excretion
- Opth - redness, itching
- Otic - accumulation (use spariningly)
- Muscle pain, [nephrotoxicity], [IM/IT/IV hospital use only], [pregnant]
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MOA of daptomycin
daptomycin (IV)
calcium-dependent detergent disruption to INNER cell membrane
- Gram + only
- renal elimination
- rhabdomyolysis (CPK monitoring)
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MOA of rifamycins
- rifampin (PO, IV)
- rifaximin (unabsorbed PO form)
inhibits bacterial RNA polymerase -> blocks RNA synthesis
- Gram +, mycobacteria
- hepatic elimination
- take on empty stomach with full glass of water
- avoid alcohol
- Orange body fluids (stains contacts)
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MOA of fluoroquinolones
- ciprofloxacin (PO, IV)
- moxifloxacin (PO, IV)
- levofloxacin (PO, IV)
inhibits bacterial DNA gyrase/topoisomerase and prevents relaxation of supercoiled DNA -> blocks DNA replication and protein synthesis
- Gram +, Gram - (broad spectrum)
- hepatic, renal elimination
- photosensitivity
- hypo/hyperglycemia diabetics
- QT prolongation
- [Tendon inflammation/rupture]
- damages growing cartilage
- CNS effects
- no dairy, Fe, Ca
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MOA of metronidazole
metronizadole (PO, IV)
fragments DNA and blocks DNA synthesis and protein synthesis
- Gram -
- hepatic elimination
- N, HA, taste disturbance
- alcohol within 3 days (disulfiram like reaction)
- GI upset - take with food, milk
- contact MD c numbness/tingling [peripheral neuropathy]
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MOA of sulfonamides
sulfamethoxazole (PO, IV)
- Broad spectrum, Gram +, Gram -
- renal elimination -> active metabolites UTIs
- Sulfa allergies
- photosensitivity
- maintain adequate hydration
- jaundice, haemolytic anemia
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anti-biotic basic counseling points
- GI upset
- OC backup
- complete whole therapy
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MOA of isoniazid
isoniazid (PO)
inhibits mycobacterial fatt acid synthesis, blocks cell wall synthesis
mycobacteria
- hepatic elimination
- take on empty stomach 1-2 hours after meal
- avoid tyramine foods
- avoid alcohol, acetaminophne
- peripheral neuropathy = take VitB6
fatal hepatitis
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MOA of ethambutol
ethambutol (PO)
inhibits mycobacterial fatt acid synthesis, blocks cell wall synthesis
mycobacteria
renal elimination
- take with food
- dizziness, disorientation, drowsiness
- optic neuritis = need eye exams
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MOA of pyrazinamide
pyrazinamide (PO)
MOA unknown
TB active only
- hepatic elimination
- need regular medical followups
- nausea, loss of appetite
- hepatitis
- gout exacerbations
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