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131 Cards in this Set
- Front
- Back
what is pharmacokinetics?
what are 4 steps that the body does to the drug? |
what the body does to drug:
1) Absorbed 2) Distributed 3) Metabolized 4) Excreted |
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what are the 5 ways to Absorb drugs?
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"TAP IT"
Topical Alimentary Parenteral Inhalation Transdermal |
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Inhalation
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pulmonary drugs
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Topical
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localized disease
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Transdermal
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sustained release
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what are the 4 different alimentary ways of absorbing drugs?
which ones bypasses the liver which one goes straight to the venous circulation? which one uses the small intestine for absorption? |
>Oral- uses small intestine (large surface area)
>Buccal- goes into venous circulation >Sublingual- goes into SVC (bypass liver) >Rectal - 50% bypass liver |
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what are the 4 different ways parenteral of absorbing drugs?
which one goes 100% to circulation? which one goes to subarachnoid space? |
• IV- 100% goes into circulation
• IM • Subcutaneous • Intrathecal- into subarachnoid space |
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2 ways to distribute drugs in the body.
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Diffusion: high ⇨ low conc, may be facilitated
Active transport: against concentration gradient, ATP ⇨ ADP |
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what are the 5 different ways to metabolize drugs?
define Metabolism. polar/fat soluble is eliminated quicker? |
Metabolism is when lipids pass through cell membrane
polar eliminates quicker. >Phase I rxn >Phase II rxn >Biotransformation factors >Zero-order Kinetics >1st-order Kinetics |
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Phase I rxn: location and MOA
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Liver ER: redox and hydrolysis =>polar groups
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Phase II rxn
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Liver cytosol: conjugation => add glutathione, acetic acid, sulfate
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Biotransformation factors: give 5 examples
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Genetics, age, gender, liver disease, P45O
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Zero-order Kinetics
define give 3 examples EtOH (100mg/dL/hr): what is this equivalent to? |
metabolism independent of concentration
Ex: EtOH, Phenytoin, Chemo drugs EtOH (100mg/dL/hr): 1 glass wine, 1 shot whiskey, 2 cans of beer |
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define 1st order Kinetics
Ex: 10% of drug (conc=100mg/dL) eliminated every 2 hours: • T=O hrs: [D]= • T=2 hrs: [D]= • T=4 hrs: [D]= |
constant drug percentage metabolism over time:
Ex: 10% of drug (conc=100mg/dL) eliminated every 2 hours: • T=O hrs: [D]=100mg/dL • T=2 hrs: [D]=90 mg/dL • T=4 hrs: [D]=81 mg/dL |
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2 ways to remove the drug from the body:
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Excretion
Secretion |
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Excretion
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removal of drug from body via urine, feces, respiration, skin, breast milk
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Secretion
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transport drug to another compartment
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Pharmacodynamics
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what drugs do to the body
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4 types Receptor interactions and examples
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>Transmembrane (Ex: Insulin)
>Ligand-gated ion channels (Ex: BZ, ACh) >Transcription factors (Ex: Steroid hormone receptors) >Second-messengers: (Ex: cAMP, cGMP, IP3) |
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Agonist
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activates receptors
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Antagonist
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inhibits receptors
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t1/2= formula
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(.693)(Vd) /clearance
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Vd
equation what does a large Vd mean? |
total drug / plasma conc
(large Vd => most of drug is sequestered) |
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Loading dose:
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(desired plasma conc)(Vd)
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Maintenance dose:
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(desired plasma conc)(clearance)
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Steady-state plasma conc (Css)
how many half lives does it take? |
availability rate = elimination rate
takes 4.5 halflives |
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Clearance
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volume of plasma cleared of drug
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calculate the Excretion rate:
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(clearance)(plasma conc) - rate of elimination
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TI= formula
what does high TI mean? |
(toxic dose)/(therapeutic dose)
(High TI => safe drug) = LD50, ED50 |
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Peak level
what if the peak level is high? management |
4 hrs after dose
(too high=> decrease dose) |
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Trough level
management if the trough level is high? |
2 hrs before dose
(too high => give less often) |
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Bacteriostatic:
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protein synthesis inhibitors
(except aminoglycosides) |
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Bacteriocidal
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all the rest
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p450-dependant drugs:
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levels rise if you inhibit p450
"Women's DEPT" Warfarin Digoxin Estrogen Phenytoin Theophylline |
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Hospital Abscesses:
Day 1-3: Day 4-7: >7: |
Hospital Abscesses:
Day 1-3: Staph aureus - lots of 02 Day 4-7: Strep viridans- no enzymes >7: Anaerobes - PMNs |
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Staph Drugs: (7)
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(at least one)
• Amoxicillin + Clavulanate • Ampicillin + Sulbactam • Methicillin • Naficillin • Cephalosporins • Vancomycin • Macrolide |
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Inhibit p450:
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"Frequently I Do SMACK Grapefriut juice"
Fluoroquinolones INH Diltiazem Sulfa drugs Macrolides Amiodorone Cimetidine Ketoconazole Grapefruit juice |
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Pseudo Drugs: name all 8
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(at least two)
• Ticarcillin + Clavulinic • Piperacillin +Tazobactam • Carbenacillin • Ceftazidime or Cefepime • Vancomycin • Fluoroquinolones • Aminoglycosides |
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what should be started with pseudo drug when fever is >48 hrs.
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Start anti-fungal if fever >48hr
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p450 Inducers:
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"Queen Barb StealS Phen-Phen And Then Refuses Greasy Carbs"
Quinidine Barbiturates St. John's wort/spirololactone Phenytoin Alcohol Tetracyclines Rifampin Griseofulvin Carbamazepine |
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Cystic Fibrosis acute exacerbation of the lung tx
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Tx: penicillin/cephalosporin + aminoglycoside
ie. ceftazidime and gentamycin |
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DNA Synthesis Inhibitors:
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Fluoroquinolones
RNA Polymerase Inhibitors Sulfa Drugs |
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Fluoroquinolones
MOA do not mix with what drug? bug tx SE CI |
MOA: inhibit Topo II (DNA gyrase), decreased w/ antacids
Tx: Gram +/- , Atypicals (not anaerobes) SE: Inhibit rapidly dividing cells => anemia, UTI, dry skin, fetal growth retardation CI: Pregnancy, Kids |
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what are the fluoroquinolone drugs?
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the "ofloxacin" drugs
Levofloxacin Ciprofloxacin Norfloxacin Trovafloxacin Ofloxacin Gatifloxacin |
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Ciprofloxacin
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best Pseudomonas coverage
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Norfloxacin
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tx UTI only
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Trovafloxacin
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taken off market due to hepatic necrosis
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Ofloxacin
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tx Gonorrhea (1-dose), increasing resistance
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Gatifloxacin
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tx Gonorrhea (1-dose), increasing resistance
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drugs that cause Myositis:
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"RIPS"
• Rifampin • INH • Prednisone (any steroid) • Statins |
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what drugs cause disulfiram Rxns:
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• Metronidazole
• Cephalosporins • Procarbazine |
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RNA Polymerase Inhibitors:
SE (2) Tx MOA |
'The 5 R 's of Rifampin"
SE: Revs up P450, Red-orange secretions, Resistance if used alone SE: Fat soluble=> myositis (rips up muscle), hepatitis Tx: TB, N. Meningitidis and HI-B prophylaxis (give to close contacts) • Rifampin (inhibits beta subunit of RNA Pol) |
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Sulfa Drugs:
MOA bugTx (2) SE: (3) |
MOA: inhibit folate synthesis/PABA
bug Tx: Gram+, simple Gram - SE: G-6PD hemolytic anemia, porphyria, MetHb |
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what are the sulfa drugs
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Sulfamethoxazole
• Sulfadiazine • Sulfacetamide • Sulfasalazine • Sulfapyrazone |
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Trimethoprim Sulfamethoxazole
what does Sulfamethoxazole inhibit? used for who? what does Trimethoprim inhibit SE |
Sulfamethoxazole - inhibits DHP synthetase, used for kids
Trimethoprim- inhibits DHF reductase SE: kernicterus, renal failure, no sulfur |
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Sulfadiazine
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tx burn pts (cream)
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Sulfasalazine
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tx UC
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Sulfapyrazone
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tx UC
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Sulfacetamide
tx |
tx Chlamydia eye infections
prevent neonatal blindness in 3rd world |
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Polymixins class
MOA bug Tx |
Cell membrane disrupter
cationic detergents Tx: Gram ( - ) |
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Metronidazole MOA
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02 free radicals
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metronidazole tx
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''GGETon the Metro"=>
Tx: Giardia, Gardnerella, Entamoeba, Trichomonas, all anaerobes |
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why does metronidazole cause disulfiram rxn.
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>Inhibits acetaldehyde dehydrogenase => hemolytic anemia due to oxidation
>disulfiram rxn (N/V /D w/ EtOH) |
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drugs that cause dysgeusia:
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Clarithromycin
Li metronidazole |
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Protein Synthesis Inhibitors:
30S Inhibitors: |
"buy' AT 30, CEL at 50"
Aminoglycosides Tetracyclines |
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Aminoglycosides:
MOA bacteriostatic/bacteriocidal SE bug Tx CI with what disease? |
MOA: inhibit IF2; bacteriocidal
Tx: All Gram ( - ) SE: ototoxicity, nephrotoxicity, neurotoxicity (inhibits presynaptic Ca influx) =>can't use w/ NM |
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name the aminoglycosides
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Gentamicin
Neomycin Amikacin Tobramycin Streptomycin Spectinomycin |
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Gentamicin
SE |
neuropathy
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Neomycin
SE function |
topical (including gut surface) => rash
kills NH4-producing bacteria |
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Amikacin
1/2 life excretion |
hepatic excretion=> OK for kidneys, long t1/2
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Tobramycin
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tx CF pts
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Spectinomycin
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former gonorrhea
"now just a spectator" |
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Streptomycin
treatment for what two diseases |
tx TB pts, tx tularemia
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Tetracyclines
MOA bug TX |
MOA: block tRNA
Tx: all Gram+ , simple Gram-, Atypicals (not Staph aureus), Rickettsia |
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Tetracyclines
SE (6) should not mix with what drugs? CI (2) |
SE: photosensitivity (wear SPF15), errosive esophagitis,
permanent grey teeth, revs up P450, Fanconi's (if old drug), negates Oral contraceptives binds Ca2+=> don't use w/ Tums or milk CI: Pregnancy, kids |
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Tetracyclines name all
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Minocycline
Doxycycline Demecocycline Oxytetracycline |
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Minocycline
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tx acne "mean-o-teenagers have acne"
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Doxycycline
how is it excreted? |
hepatic excretion
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Demecocycline: MOA
SE |
blocks ADHr =>nephrogenic DI (like Li)
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Triple Antibiotic:
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"Brand New Patient"
Bacitracin Neomycin, Polymyxin D |
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50S Inhibitors:
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Lincosamides
Macrolides Chloramphenicol |
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Chloramphenicol
MOA Tx bugs: (2) SE: (3) |
"CAM" - blocks peptidyl transferase
• Tx: all Gram +, Rickettsia • SE: aplastic anemia, inhibits ETC complex IV, grey-baby syndrome |
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Macrolides
MOA Tx: (3) SE: (2) |
MOA: block translocation
• Tx: all Gram +, simple Gram (-), Atypicals • SE: inhibit P450, Torsade w / 3rd generation anti-histamines |
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Macrolides name all
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Clarithromycin
Erythromycin Azithromycin |
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Clarithromycin:
class MOA SE |
MacroLide
transLocase on the 50S subunit dysguisia (metallic taste) |
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Azithromycin:
class and MOA t1/2 tx for what bug good for what patients |
Macrolide: Inhibits transLocase on the 50S subunit
longest t1/2, tx MAI (AIDS pts) good for pregnant women |
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Erythromycin:
class and MOA SE tx |
Macrolide: Inhibits transLocase on the 50S subunit
GI upset tx Legionella pneumonia |
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Lincosamides
MOA Tx SE |
MOA: block translocation (tranlocation on 50S subunit)
• Tx: all Gram +, simple Gram- , all Anaerobes • SE: pseudomembranous Colitis |
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Lincosamides
which one is not used now? |
Clindamycin
Lincomycin: not used now |
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Lincomycin
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Lincosamides that is not used now
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Chlamydia 1-dose Tx:
dose to treat with GC |
• Azithromycin (1g)
• Or 2g to tx GC |
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who is at risk of Staph /Pseudo Attack:
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• DM
• CF • Burn pts • Neutropenic pts |
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3 bugs Vancomycin tx:
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• MRSA
• Staph. epidermidis • Enterococcus |
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Gonorrhea 1-dose Tx:
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"TRI to FIX the FOX with 3 FLOX''
• Ceftriaxone • Cefixeme • Cefoxitin • Ciprofloxacin • Ofloxacin • Gatifloxacin |
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Cell wall synthesis inhibitors (5)
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Penicillins
Cephalosporins Carbapenems Monobactams Vancomycin |
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Vancomycin
MOA Tx: SE |
MOA: irreversibly blocks formation of cell wall peptide bridges
Tx: all Gram + SE: ototoxicity, nephrotoxicity, red man syndrome |
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Aztreonam:
class tx for what bug MOA usage |
Monobactams:
Gram- rods good for penicillin allergies |
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Carbapenems:
Tx for what bugs? and 2 drugs |
everything (except atypicals)
• Imipenem + Cilastatin • Meropenem |
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Imipenem + Cilastatin
how does this decrease seizure incidence? |
(inhibits renal enzymes to decrease seizure incidence)
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Cephalosporins:
Tx: SE: same as what drug? crossover gram - coverage |
Tx: all Gram+, simple Gram-, simple anaerobes
SE: same as penicillins (15% crossover with penicillins for anaphylaxis) More Gram - coverage as you progress through generations |
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how many generations of cephalosporins?
name all the first generations? |
There are 3 generations of cephalosporins:
1stGen: Cefazolin Cephalothin Cephalexin |
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Cefazolin
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parenteral (IV)
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Cephalothin
SE class |
interstitial nephritis
1st generation cephalosporin |
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2nd gen cephalosporins: name all drugs
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"FOX FAMily are FACking FOes and wearing FUR "
Cefaclor Cefotetan Cefoxitin Cefamandole Cefuroxime |
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Cefaclor
class who uses it SE (4) |
2nd gen cephalosporins
use in kids => erythema multiforme, urticaria, bone pain, serum sickness |
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Cefotetan
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inhibits Vit K =>bleeding
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Cefoxitin
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excellent complete anaerobic coverage
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Cefamandole
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inhibits Vit K => bleeding
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Cefuroxime
tx for what diesease class |
tx epiglottitis
second generation cephalosporin |
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3rd Generation cephalosporins
which one is take orally? which one is renally excreted? and treatment for meningitis <2 y/o? |
Ceftriaxone
Cefixeme - oral Cefotaxime -renal excretion, tx meningitis <2m/o Ceftazidime Cefoperazone Moxalactam |
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Ceftriaxone
MOA crosses what barrier tx: why cannot be used for <2mo |
cross BBB
hepatic excretion (not <2m/o), tx meningitis >2 mo |
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Ceftazidime
class coverage |
third generation
best Pseudo coverage ''pseudo tazo tea" |
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Cefoperazone
class SE |
third generation cephalosporin
dec. Vit K |
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Moxalactam
class SE |
third generation cephalosporin
dec. Vit K |
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4th Generation cephalosporin
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Cefepime
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4 types of Penicillins:
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Simple
Extended Spectrum Anti-Staphylococcal Anti-Pseudomonal |
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Penicillins:
Tx for what bugs SE (6) |
Tx: Gram + (not Staph), simple anaerobes
SE: anaphylaxis, non-specific rash, drug fever SE: hemolytic anemia, interstitial nephritis, bone marrow suppression |
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what are the Simple penicillins
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• Penicillin G
• Penicillin V • Benzathine • Procaine |
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Penicillin G
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shot
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Penicillin V
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oral
"remember the terminal Sulcus v line in the back of the tongue?" |
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Benzathine
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simple penicillin
long-acting |
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Procaine
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simple penicillin
short -acting |
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Extended Spectrum:
MOA (bug coverage) name the drugs (2) |
MOA: also cover E. coli, H. influ + Staph aureus (β -lactamase inhibitors)
• Amoxicillin + Clavulinic acid • Ampicillin + Sulbactam |
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Ampicillin + Sulbactam
class SE (2) what is it used for? |
Extended Spectrum penicillins
=> J-H rxn (EBV, CMV, Syphilis), #2 interstitial nephritis, tx pregnant UTIs |
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5 Anti-Staphylococcal penicillins
which one is oral |
• Methicillin
• Nafcillin • Oxacillin • Cloxacillin • Dicloxacillin: oral |
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Methicillin
type of penicillin route SE |
>>Anti-Staphylococcal penicillins
>>IV=> #1 PCN causing interstitial nephritis |
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Nafcillin
type of antibiotic route/SE |
>>Anti-Staphylococcal penicillins
>>IV-high Na load (do not use w/ Conn's, arrhythmias, HTN, seizures) |
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what are the three Anti-Staphylococcal penicillins that can be taken orally?
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• Oxacillin
• Cloxacillin • Dicloxacillin |
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4 Anti-Pseudomonal penicillins
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• Ticarcillin + Clavulinic acid
• Piperacillin + Tazobactam • Carbenacillin • Mezlocillin |
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Ticarcillin + Clavulinic acid
coverage |
anti-pseudomonal penicillins
(also covers S. Aureus) |
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Carbenacillin
class SE |
anti pseudomonal penicillins
high Na load |