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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
what are the 5 ways to Absorb drugs?
"TAP IT"
Topical
Alimentary
Parenteral
Inhalation
Transdermal
Inhalation
pulmonary drugs
Topical
localized disease
Transdermal
sustained release
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
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
2 ways to distribute drugs in the body.
Diffusion: high ⇨ low conc, may be facilitated
Active transport: against concentration gradient, ATP ⇨ ADP
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
Phase I rxn: location and MOA
Liver ER: redox and hydrolysis =>polar groups
Phase II rxn
Liver cytosol: conjugation => add glutathione, acetic acid, sulfate
Biotransformation factors: give 5 examples
Genetics, age, gender, liver disease, P45O
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
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
2 ways to remove the drug from the body:
Excretion
Secretion
Excretion
removal of drug from body via urine, feces, respiration, skin, breast milk
Secretion
transport drug to another compartment
Pharmacodynamics
what drugs do to the body
4 types Receptor interactions and examples
>Transmembrane (Ex: Insulin)
>Ligand-gated ion channels (Ex: BZ, ACh)
>Transcription factors (Ex: Steroid hormone receptors)
>Second-messengers: (Ex: cAMP, cGMP, IP3)
Agonist
activates receptors
Antagonist
inhibits receptors
t1/2= formula
(.693)(Vd) /clearance
Vd
equation
what does a large Vd mean?
total drug / plasma conc
(large Vd => most of drug is sequestered)
Loading dose:
(desired plasma conc)(Vd)
Maintenance dose:
(desired plasma conc)(clearance)
Steady-state plasma conc (Css)
how many half lives does it take?
availability rate = elimination rate
takes 4.5 halflives
Clearance
volume of plasma cleared of drug
calculate the Excretion rate:
(clearance)(plasma conc) - rate of elimination
TI= formula
what does high TI mean?
(toxic dose)/(therapeutic dose)
(High TI => safe drug) = LD50, ED50
Peak level
what if the peak level is high? management
4 hrs after dose
(too high=> decrease dose)
Trough level
management if the trough level is high?
2 hrs before dose
(too high => give less often)
Bacteriostatic:
protein synthesis inhibitors
(except aminoglycosides)
Bacteriocidal
all the rest
p450-dependant drugs:
levels rise if you inhibit p450
"Women's DEPT"
Warfarin
Digoxin
Estrogen
Phenytoin
Theophylline
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
Staph Drugs: (7)
(at least one)
• Amoxicillin + Clavulanate
• Ampicillin + Sulbactam
• Methicillin
• Naficillin
• Cephalosporins
• Vancomycin
• Macrolide
Inhibit p450:
"Frequently I Do SMACK Grapefriut juice"
Fluoroquinolones
INH
Diltiazem
Sulfa drugs
Macrolides
Amiodorone
Cimetidine
Ketoconazole
Grapefruit juice
Pseudo Drugs: name all 8
(at least two)
• Ticarcillin + Clavulinic
• Piperacillin +Tazobactam
• Carbenacillin
• Ceftazidime or Cefepime
• Vancomycin
• Fluoroquinolones
• Aminoglycosides
what should be started with pseudo drug when fever is >48 hrs.
Start anti-fungal if fever >48hr
p450 Inducers:
"Queen Barb StealS Phen-Phen And Then Refuses Greasy Carbs"
Quinidine
Barbiturates
St. John's wort/spirololactone
Phenytoin
Alcohol
Tetracyclines
Rifampin
Griseofulvin
Carbamazepine
Cystic Fibrosis acute exacerbation of the lung tx
Tx: penicillin/cephalosporin + aminoglycoside
ie. ceftazidime and gentamycin
DNA Synthesis Inhibitors:
Fluoroquinolones
RNA Polymerase Inhibitors
Sulfa Drugs
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
what are the fluoroquinolone drugs?
the "ofloxacin" drugs
Levofloxacin
Ciprofloxacin
Norfloxacin
Trovafloxacin
Ofloxacin
Gatifloxacin
Ciprofloxacin
best Pseudomonas coverage
Norfloxacin
tx UTI only
Trovafloxacin
taken off market due to hepatic necrosis
Ofloxacin
tx Gonorrhea (1-dose), increasing resistance
Gatifloxacin
tx Gonorrhea (1-dose), increasing resistance
drugs that cause Myositis:
"RIPS"
• Rifampin
• INH
• Prednisone (any steroid)
• Statins
what drugs cause disulfiram Rxns:
• Metronidazole
• Cephalosporins
• Procarbazine
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)
Sulfa Drugs:
MOA
bugTx (2)
SE: (3)
MOA: inhibit folate synthesis/PABA
bug Tx: Gram+, simple Gram -
SE: G-6PD hemolytic anemia, porphyria, MetHb
what are the sulfa drugs
Sulfamethoxazole
• Sulfadiazine
• Sulfacetamide
• Sulfasalazine
• Sulfapyrazone
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
Sulfadiazine
tx burn pts (cream)
Sulfasalazine
tx UC
Sulfapyrazone
tx UC
Sulfacetamide
tx
tx Chlamydia eye infections
prevent neonatal blindness in 3rd world
Polymixins class
MOA
bug Tx
Cell membrane disrupter
cationic detergents
Tx: Gram ( - )
Metronidazole MOA
02 free radicals
metronidazole tx
''GGETon the Metro"=>
Tx: Giardia, Gardnerella, Entamoeba, Trichomonas, all anaerobes
why does metronidazole cause disulfiram rxn.
>Inhibits acetaldehyde dehydrogenase => hemolytic anemia due to oxidation
>disulfiram rxn (N/V /D w/ EtOH)
drugs that cause dysgeusia:
Clarithromycin
Li
metronidazole
Protein Synthesis Inhibitors:
30S Inhibitors:
"buy' AT 30, CEL at 50"
Aminoglycosides
Tetracyclines
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
name the aminoglycosides
Gentamicin
Neomycin
Amikacin
Tobramycin
Streptomycin
Spectinomycin
Gentamicin
SE
neuropathy
Neomycin
SE
function
topical (including gut surface) => rash
kills NH4-producing bacteria
Amikacin
1/2 life
excretion
hepatic excretion=> OK for kidneys, long t1/2
Tobramycin
tx CF pts
Spectinomycin
former gonorrhea
"now just a spectator"
Streptomycin
treatment for what two diseases
tx TB pts, tx tularemia
Tetracyclines
MOA
bug TX
MOA: block tRNA
Tx: all Gram+ , simple Gram-, Atypicals (not Staph aureus), Rickettsia
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
Tetracyclines name all
Minocycline
Doxycycline
Demecocycline
Oxytetracycline
Minocycline
tx acne "mean-o-teenagers have acne"
Doxycycline
how is it excreted?
hepatic excretion
Demecocycline: MOA
SE
blocks ADHr =>nephrogenic DI (like Li)
Triple Antibiotic:
"Brand New Patient"
Bacitracin
Neomycin,
Polymyxin D
50S Inhibitors:
Lincosamides
Macrolides
Chloramphenicol
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
Macrolides
MOA
Tx: (3)
SE: (2)
MOA: block translocation
• Tx: all Gram +, simple Gram (-), Atypicals
• SE: inhibit P450, Torsade w / 3rd generation anti-histamines
Macrolides name all
Clarithromycin
Erythromycin
Azithromycin
Clarithromycin:
class
MOA
SE
MacroLide
transLocase on the 50S subunit
dysguisia (metallic taste)
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
Erythromycin:
class and MOA
SE
tx
Macrolide: Inhibits transLocase on the 50S subunit
GI upset
tx Legionella pneumonia
Lincosamides
MOA
Tx
SE
MOA: block translocation (tranlocation on 50S subunit)
• Tx: all Gram +, simple Gram- , all Anaerobes
• SE: pseudomembranous Colitis
Lincosamides
which one is not used now?
Clindamycin
Lincomycin: not used now
Lincomycin
Lincosamides that is not used now
Chlamydia 1-dose Tx:
dose to treat with GC
• Azithromycin (1g)
• Or 2g to tx GC
who is at risk of Staph /Pseudo Attack:
• DM
• CF
• Burn pts
• Neutropenic pts
3 bugs Vancomycin tx:
• MRSA
• Staph. epidermidis
• Enterococcus
Gonorrhea 1-dose Tx:
"TRI to FIX the FOX with 3 FLOX''
• Ceftriaxone
• Cefixeme
• Cefoxitin
• Ciprofloxacin
• Ofloxacin
• Gatifloxacin
Cell wall synthesis inhibitors (5)
Penicillins
Cephalosporins
Carbapenems
Monobactams
Vancomycin
Vancomycin
MOA
Tx:
SE
MOA: irreversibly blocks formation of cell wall peptide bridges
Tx: all Gram +
SE: ototoxicity, nephrotoxicity, red man syndrome
Aztreonam:
class
tx for what bug
MOA
usage
Monobactams:
Gram- rods
good for penicillin allergies
Carbapenems:
Tx for what bugs?
and 2 drugs
everything (except atypicals)
• Imipenem + Cilastatin
• Meropenem
Imipenem + Cilastatin
how does this decrease seizure incidence?
(inhibits renal enzymes to decrease seizure incidence)
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
how many generations of cephalosporins?
name all the first generations?
There are 3 generations of cephalosporins:
1stGen:
Cefazolin
Cephalothin
Cephalexin
Cefazolin
parenteral (IV)
Cephalothin
SE
class
interstitial nephritis
1st generation cephalosporin
2nd gen cephalosporins: name all drugs
"FOX FAMily are FACking FOes and wearing FUR "

Cefaclor
Cefotetan
Cefoxitin
Cefamandole
Cefuroxime
Cefaclor
class
who uses it
SE (4)
2nd gen cephalosporins
use in kids => erythema multiforme, urticaria, bone pain, serum sickness
Cefotetan
inhibits Vit K =>bleeding
Cefoxitin
excellent complete anaerobic coverage
Cefamandole
inhibits Vit K => bleeding
Cefuroxime
tx for what diesease
class
tx epiglottitis
second generation cephalosporin
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
Ceftriaxone
MOA
crosses what barrier
tx:
why cannot be used for <2mo
cross BBB
hepatic excretion (not <2m/o),
tx meningitis >2 mo
Ceftazidime
class
coverage
third generation
best Pseudo coverage ''pseudo tazo tea"
Cefoperazone
class
SE
third generation cephalosporin
dec. Vit K
Moxalactam
class
SE
third generation cephalosporin
dec. Vit K
4th Generation cephalosporin
Cefepime
4 types of Penicillins:
Simple
Extended Spectrum
Anti-Staphylococcal
Anti-Pseudomonal
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
what are the Simple penicillins
• Penicillin G
• Penicillin V
• Benzathine
• Procaine
Penicillin G
shot
Penicillin V
oral
"remember the terminal Sulcus v line in the back of the tongue?"
Benzathine
simple penicillin
long-acting
Procaine
simple penicillin
short -acting
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
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
5 Anti-Staphylococcal penicillins
which one is oral
• Methicillin
• Nafcillin
• Oxacillin
• Cloxacillin
• Dicloxacillin: oral
Methicillin
type of penicillin
route
SE
>>Anti-Staphylococcal penicillins
>>IV=> #1 PCN causing interstitial nephritis
Nafcillin
type of antibiotic
route/SE
>>Anti-Staphylococcal penicillins
>>IV-high Na load (do not use w/ Conn's, arrhythmias, HTN, seizures)
what are the three Anti-Staphylococcal penicillins that can be taken orally?
• Oxacillin
• Cloxacillin
• Dicloxacillin
4 Anti-Pseudomonal penicillins
• Ticarcillin + Clavulinic acid
• Piperacillin + Tazobactam
• Carbenacillin
• Mezlocillin
Ticarcillin + Clavulinic acid
coverage
anti-pseudomonal penicillins
(also covers S. Aureus)
Carbenacillin
class
SE
anti pseudomonal penicillins
high Na load