Pharmocology Flashcards
Well absorb drugs (oral)
Anti-folate
FQ
Nitrofurantoin
Metronidazole
Tetracycline
Lincosamide
Linezolid
Poor absorption oral
Carbapenams
Monobactam
Glycopeptide
Not absorb orally
Daptomycin
Polymyxin
Aminoglycoside
Penicillin oral absorption
Penicillin V 60%
Amoxicillin 75%
Cloxacillin 50%
Cephalosporin oral absorption
Cephalexin 90%
Cefuroxime 52%
Tetracycline and doxycycline oral absorption
Tetra 60-80%
Doxy 90-100%
Macrolide oral absorption
Azithromycin 40%
Clarithromyxin 50%
Erythromycin 15-45%
Good CSF penetration
Gen 3&4 cephalosporins and cefuroxime
Meropenem
Imipenem
Anti-folate
Metronidazole
FQ(m>I>c)
Abscess distribution
Glycopeptide
Lincosamide
Bile distribution
Tetracycline
Lincosamide
Metabolism liver
Tetracycline Tigecycline (minimal) Macrolide Lincosamide Linezolid (not cyp 450) Anti folate Macrolide (partly; inhibit liver also) Metronidazole
Not metabolize in liver
Penicillin Cephalosporin Carbapenams Monobactam Glycopeptide
Excrete in kidney
Penicillin anti staphy (bile and renal) Cephalosporin (except ceftriaxone)
Carbapenans
Monobactam
Glycopeptide
Daptomycin
Polymyxin(?) Aminoglycoside Tetracycline (and bile) Tigercycline (mainly bile) Macrolide (4-30%) Lincosamide (and bile) Linezolid (and non renal)
Anti folate
Nitrofurantoin
Metronidazole
FQ (except mo and nalidixic )
Excreted in bile
Nafcillin
Antistaph
Ceftriaxone
Tetracycline
Tigecycline
Lincosamide
Time dependent killings
Penicillin (40-50%) Cephalosporin (40-50%) Carbapenams (40-50%) Monobactam (50-60%) Glycopeptide Tetracycline Lincosamide Linezolid
Concentration killing
Daptomycin Polymyxin Aminoglycoside FQ Metronidazole
Daptomycin should not be use to treat
Pneumonia
Vancomycin is not as effective as _______________ for treatment of serious infections such as endocarditis caused by MSS strain.
Anti staphylococcus penicillin
MSSA choices of drugs
1st
Nafcillin
2nd
Cefazolin (1gen)
Vancomycin (if allergic to pcn)
Oral
Dicloxacillin
Cephalexin (1gen)
FQ
CONS DOC
Nafcillin
Vancomycin
Daptomycin
Carbapenams
Strep grp a / b DOC
Pcn g + clindamycin
Any BL
Vancomycin (pcn allergy)
Clindamycin
Amoxicillin
Tmp/smx
Viridans strep doc
Pcn g
Ceftriaxone
Vancomycin
Amoxicillin
Faecalis doc
Ampicillin
Pcn g
vancomycin
Amoxicillin
Pseudomonal aeruginosa is resistant to
Tetracycline inc tigecycline
And
Sulfonamide
Static or cidal
Beta lactam AG Tetracycline Macrolide Linezolid
Cidal
Cidal
Cidal at high conc
Static but cidal against streptococci
Macrolide activity is enhanced at
Alkaline ph
Sulphonamide may ppt in Urine esp at _______ producing crystalluria, hematuria or even obstruction
Neutral or acid pH
Sulphonamide
Trimethoprim
Co trimoxazole
Cidal or static
Static
Static
Cidal
Co-trimoxazole ratio
Trimethoprim :
Sulfamethoxazole 1:5
FQ cidal or static
Cidal (broad spectrum)
FQ block DNA synthesis by _______
Inhibiting bacterial. Topoisomerase II (DNA gyrase)
And topoisomerase IV.
Nitrofurantoin is cidal or static
Cidal at right dose
Nitrofurantoin antagonizes action of ____
Nalidixic acid
It is desirable to keep urine ph __________ when using nitrofurantoin to treat Chronic UTI
Below 5.5
Metronidazole Moa
Non enzymatically reduced by reacting with reduced ferrodoxin.
This result in production of toxic product.
Fosfomyxin MOA
An analogue of phosphoenolopyruvate.
It inhibits the cytoplasmic enzyme enolpyruvate transferase by covalently binding to the cysteine residue of the active site and blocking the addition of phosphoenolpyruvate to UDP-N-acetylglucosamine.
Uptake of fosfomycin require
___
Glycerophosphate or glucose 6 phosphate transport system.
Protein binding penicillin
Penicillin 80%
Amoxicillin 25%
Cloxacillin 95%
Protein binding cephalosporins
Cefepime 20%
Ceftriaxone 90%
Protein binding carbapenams
Meropenem 2%
Ertapenam 95%
Monobactam protein binding
56%
Vancomycin
Teicoplanin
Protein binding
Vanco 30-55%
Teicoplanin 90%
Daptomycin protein binding
90%
Polymyxin protein binding
80-90%
Aminoglycoside protein binding
10%
Tetracycline BP
T: 20-67%
D: 82-93%
Tigecycline BP
79-81%
Macrolide BP
A 7-50%
C 65%
E 70%
Lincosamide BP
85-94%
Linezolid BP
13%
SMZ binding protein
70%
TMP BP
44-62%
FQ BP
Low 30-50%
Metronidazole BP
<20%
Penicillin half life
30-90min short
Cephalosporin half life
1-2hr
Ceftriaxone 8hr
Carbapenams half life
1hr
Ertapenem 4hr
Monobactam half life
2hr
Vancomycin half life
4-12hr
Teicoplanin half life
83-168hr
Daptomycin half life
7-9hr
Polymyxin Bhalf life
4-6hr
AG halflife
1.5 -3.5hr
Tetracycline half life
6-12hr
Doxycycline halflife
15-48hr
Tigecycline halflife
24-42hr
Macrolide half life
A: 68hr
C: 5-7hr
E: 2-4hr
Lincosamide halflife
2.5hr
Linezolid half life
4-5hr
Tmp half life
11hr
SMZ halflife
9hr
FQ half life
M: 9.5hr
L: 6-8hr
C: 4hr
Nitrofurantoin halflife
0.3-1hr
Metronidazole half life
6-14hr
MRSQ doc
Vancomycin Teicoplanin Linezolid TMP/SMZ Clindamycin Doxycycline Rifampin
Cefazoline
1st gen cephalosporins
Cefadroxil
1st
Cephalexin
1st
Cephalothin
1st
Cephapirin
1st
Cephradine
1st
Cefazoline ROA
Parenteral
Cefaclor
2nd
Cefamandole
2nd
Cefonicid
2nd
Cefuroxime
2nd
Cefprozil
2nd
Loracarbef
2nd gen cephalosporins
Ceforanide
2nd
Cefoxitin
2nd
Cephamyxin
2nd
Cefmetazole
2nd
Cefotetan
2nd
Cefoperazone
3rd
Cefotaxime
3rd
Ceftazidime
3rd
Ceftizoxime
3rd
Ceftriaxone
3rd
Cefixime
3rd
Cefpodoxime
3rd
Cefdinir
3rd
Cefditoren
3rd
Ceftibuten
3rd
Cefepime
4th
Ceftaroline
5
Ceftobiprole
5th
Moxifloxacin
4th FQ
Levofloxacin
3rd FQ
Ciprofloxacin
2nd FQ
Norfloxacin
2nd FQ
Ofloxacin
2nd FQ
Nalidixic acid
1st FQ
Clinical use of daptomycin
Complicated skin and soft tissue infections and bacteremia.
Right sided endocarditis.
Less in cap
Polymyxin Clincial uses.
Infection of skins, mucous membrane, eye, ear.
Salvage therapy for treatment of infection caused by multi drug resistance organism.
MOA AG
Changes the shape of 30S portion causes code on mRNA to be read incorrectly.
MOA tetracycline
Interfere with attachment of tRNA to mRNA ribosome complex.
50s inhibitors MOA
Block peptide bond formation
Azithromycin covers
Mycobacterial avium
Compare macrolide with erythromycin
Azithromycin is 2-4fold less active against streptococcus and staphylococcus than erythromycin
Clarithromycin is 2-4 fold more active against streptococcus and staphylococcus than erythromycin
Oxazolidione MOA
Inhibits protein synthesis by binding to 50S ribosomal subunit near to surface interface of 23S ribosomal RNA
Sfx and TMP MOA
Sulfonamide susceptible organism unlike mammals cannot use exogenous folate but must synthesize it from PABA.
This pathway is essential for production of purines and NA synthesis.
As structural analog of PABA, sulphonamide inhibits
Dihydropteroate synthase and folate production.
Trimethoprim inhibit dihydrofolate reductasd.
PABA
P aminobenzoic acid.
Antifolate cidal or static
Static
Unless together then is cidal
Nitrofurantoin cidal or static
Static
FQ static or cidal
Cidal
Fosfomycin MOA
Inhibits enolpyruvate transferases by covalently binding to the cysteine residue of the active site.
Blocking the addition of phosphoenoloyruvate to UDP-N-acetylglucosamine
Metronidazole MOA
Enzyme nitroreductase
Reduces the nitro group in metronidazole to cytotoxic metabolite which bind to DNA to cause strand breakage and loss of helical structure
This interfering with nucleic synthesis
Aerobic microbes do not have the enzyme to activate this drug