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116 Cards in this Set
- Front
- Back
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REVIEW:
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If 75% of the drug is eliminated from the body, how many half-lifes have occured?
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2 half-lifes
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How is half-life calculated?
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T1/2 = (Vd/Cl) x .7
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How is Loading Dose calculated?
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LD = (Css x Vd) / f
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How is Maintenance Dose calculated?
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MD = (Css x Cl) / f
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What is the function of a Maintenance Dose?
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To replace the amount of drug that has been eliminated
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3 Drugs that undergo 1st order elimination:
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"All drugs except:
Ethanol Phenytoin Aspirin (high dose) |
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What direction does a noncompetitive antagonist shift the potency curve (right, left, up, or down)?
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"It doesn't: potency (Km) is not affected (the drug is just as potent as before, but some receptors are turned off).
However, efficacy (Vmax) is decreased and therefore the EFFICACY is shifted downward. |
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What question is answered by Phase II drug development?
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Does it work?
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Which phase do we calculate Therapeutic Index?
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Phase II
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How do we calculate Therapeutic Index?
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"*TILE
TI = LD50/ED50 |
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What are the peptidoglycan synthesis inhibitor?
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"Bacitracin
Vancomycin Cycloserine |
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What are the 50s Inhib's?
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"*CCELLS (Buys AT 30 CCELLS at 50)
Chloramphenical Clindamycin Erythromycin Lincomycin Linizolid Streptrogrammins |
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What are the Macrolides?
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*ACE
Azythromycin Clarithromycin Erythronycin |
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What are the Streptogramins?
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Dalfopristin
Quinopristin |
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What are the 30s Inhib's?
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*AT (Buys AT 30 CCELLS at 50)
AMG's Tetracyclines |
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What are the AMG's?
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*STANG
Streptomycin Tobramycin Amikacin Neomycin Gentamicin |
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What are the Nucleotide Synthesis Inhib's?
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Sulfonamides
Trimethoprim Pyrimethamine Methotrexate |
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What is the MOA of Sulfonamides?
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Inhibition of Dihydropterate Synthase
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What is the MOA of Trimethoprim?
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Inhibition of DHF Reductase
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What is the MOA of Methotrexate?
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Inhibition of DHF Reductase
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What is the MOA of Pyromethamine?
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Inhibition of DHF Reductase
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What Blocks Topoisomerase II?
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Quinilones
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What Blocks DNA Gyrase?
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Quinilones
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What inhibits mRNA synthesis?
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Rifampin
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How does Rifampin inhibit mRNA synthesis?
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Inhibition of DNA-Dependent RNA Polymerase
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What is the c/u for Penicillins?
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G+ cocci & rods
G- cocci Spirochetes |
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What is the toxicity of Penicillins?
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Hypersensitivity
Hemolytic anemia |
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Hemolytic anemia"
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What is the toxicity of Methicillin?
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Interstitial Nephritis
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What is the c/u for Methicillin?
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S. Aureus
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What are the anti-Staph Penicillins?
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*CONDM
Cloxacillin Oxacillin Nafcillin Dicloxacillin Methicillin |
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What are the anti-Pseudomonas Penicillins? (4th Gen PCN)
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*PTC of Pseudomonas in the AM
Piperacillin Ticarcillin Carbenicilin Azlocillin Mezlocillin |
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What is the c/u of Ampicillin/Amoxicillin?
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*HELPS Enterococci
H. Influenza E. Coli Listeria Proteus Salmonella Enterococci |
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What is the toxicitiy of Ampicillin/Amoxicillin?
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Hypersensitvity
Ampicillin rash Pseudomembranous colitis |
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What drugs cause Pseudomembranous Colitis?
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Ampicillin/Amoxicilin & Clindamycin
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What is the MOA of Clindamycin?
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Inhibits peptide bond formation b/w nucleotides at the P site
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What is the c/u of Clindamycin?
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Anaerobes above the diaphram
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What is the tx for Pseudomembranous Colitis secondary to C. Difficile?
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Vancomycin
Metronidazole |
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What is the MOA of Vancomycin?
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Inhibits D-ala D-ala (t/f can't make peptidoglycan)
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What is the c/u for Vancomycin?
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MRSA
C. Difficile (Pseudomembranous Colitis) Nosocomial infections (presumeably drug-resistent infxns) |
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What is the c/u for 2nd Gen Ceph's?
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*HEN PEcKS (c = cocci)
H. Influenza Enterobacter Neisseria Proteus E. Coli Klepsiella Serratia G+ cocci |
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What is a 3rd Gen Ceph used for the tx of Pseudomona?
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Ceftazidime
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What is a 3rd Gen Ceph used for the tx of Gonorrhea?
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Ceftriaxone
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What are the Ceph's used for the tx of Gonorrhea?
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*TRI to FIX a FOX
Ceftriaxone Cefixitine Cefoxitime |
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What is the one-dose tx for Gonorrhea?
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Azithromycin
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What Ceph's cause a disulfram-like reaction with alcohol?
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*Pair of FAMily ""TETS""
Cefaparazone Cefamandole Cefotetan |
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What are the anti-Penicillinase's?
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"*CONDM + Ampicillin/Amoxicillin w/Clavulonic Acid + all Cephalosporins
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What are the Penicillinase/B-Lactimase inhibitors
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*AIM
Aztreonam Imipenem/Cilistatin Meropenem |
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"
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How can any drug be altered to become Penicillinase-Resistent?
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Add Clavulonic Acid
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What is the MOA of Aztreonam?
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*AzTHREEonam
Binds to PBP #3 |
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What is the c/u of Aztreonam?
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G- Rods
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What pt's is Aztreonam used to tx?
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Pt's who cannot tolerate AMG's (1st line for any G-)
OR Pt's who are allergic to Penicillin OR Pt's in Renal Failure |
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With what is imipenem co-administered? Why?
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Cilistatin
Prevents breakdown of imipenem by inhibiting renal dihydropeptidase-1 |
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What is the c/u of imipenem/cilistatin?
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Enterobacter (DOC)
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What are the Ototoxicity-causing drugs?
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AMG's
Loops Vancomycin Quinidine Chloroquin |
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What is the MOA of AMG's?
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Inhibits initiation complex of N-Acetyl formation causing misreading of mRNA
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What is the MOA of Tetracyclines?
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"Inhibition of tRNA charging by preventing attachement of amino acyl tRNA, thereby inhibiting protein synthesis
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What is the MOA of Macrolides?
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"Blocking translocation from the A --> P site by binding the 23s subunit of the 50s ribosome
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What is the MOA of Chloramphenicol?
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"Inhibits Peptidyltransferase, the enzyme responsible for transferring nucleotides from A --> P site
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What is the MOA of Clindamycin?
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Inhibits peptide bond formation b/w nucleotides at the P site
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What is the c/u for Macrolides?
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*UPS Lost My Brand New Car
URI's (caused by G+ cocci) Pneumonia (caused by G+ cocci) STD's (caused by G+ cocci) Legionella Mycoplasma bordatella Neisseria Chlamydia |
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What is the clinical use for AMG's?
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Any G- rod
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What drug is used if a pt cannot tolerate AMG's?
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Aztreonam
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What is the c/u for Tetracyclines?
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*VACUuM THe BR
Vibrio Acne (Propionbacterium Acnes) Chlamydia Ureaplasm Urealytica Mycoplasm Tularemia H. Pylori Borellia Rickettsia |
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What is the toxicity of Tetracyclines?
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Discoloration of teeth (kids)
Abnormal bone growth (kids Potosensitivity Drug-induced pancreatitis Fanconi Syndrome (old Tetracyclines) |
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What is the toxicity of Macrolides?
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Acute cholestatic hepetatis
Eosinophilia |
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What is the MOA of Macrolides?
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"Blocking translocation from the A --> P site by binding the 23s subunit of the 50s ribosome
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What are the Macrolides?
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*ACE
Azithromycin Clarithromycin Erythromycin |
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What is an alternative MOA of Erythromycin?
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Binds to motilin receptors, causing hypermotility motility --> GI upset
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What class of drug is Dimiclocycline?
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Tetracycline
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What is the MOA of Tetracyclines?
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Inhibition of tRNA charging by preventing attachement of amino acyl tRNA
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What is the primary MOA of Dimiclocycline?
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Prevents attachment of amino acyl tRNA
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What is an alternative MOA of Dimiclocycline?
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Blocks ADH receptors
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What drugs block ADH receptors?
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Dimiclocycline
Lithium |
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What is the c/u for Chloramphenicol?
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Bacterial meningitis
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What is the MOA of Sulfonamides?
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Inhibition of Dihydropterate Synthase
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What is the MOA of Trimethoprim?
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Inhibition of DHF Reductase
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What drugs inhibit DHF Reductase?
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Trimethoprim
Pyromethamine Methotrexate |
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Day 2:
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What is the c/u for Sulfonamides?
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Norcardia
Simple UTI's Chlamydia G+ & G- |
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What is the toxicity of Sulfonamides?
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Displaces drugs from albumin (e.g. Warfarin)
Hemolytic Anemia (G6PD Def Pt's) Hypersensitivity Kernicteris (kids) Tubulointerstitial Nephritis Photosensitivity |
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What is the c/u for Trimethoprim?
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Norcardia
UTI PCP Salmonella Shigella |
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What is the toxicity of Trimethoprim?
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Megaloblastic Anemia
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What drug class is Enoxacin?
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Non-Fluoroquinolone
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What is the MOA of Enoxacin?
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Inhibits Topoisomerase II/DNA Gyrase (i.e. the same as Quinolones)
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What is the c/u for Quinolones?
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G- rods in GI/GU track
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What is the toxicity of Quinolones?
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Tendonitis (adults)
Cartilage rupture (kids) |
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What is an additional SE of Moxifloxicin?
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Screws with K+ leading to Torsades de Pointes (aka Prolonged QT Syndrome)
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What is the c/u for Metronidazole?
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*GET GAP
Giardia Entomeba Trichamonas Gardnerella Anaerobes H. Pylori |
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What is the MOA of Metronidazole?
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Form toxic metabolites in the bacterial cell wall that damage DNA
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What is the toxicity of Metronidazole?
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Disulfram-like reaction with alcohol
Dysguzia Drug-induced pancratitis Teatogenic |
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What is the tx for bacterial vaginosis for pregnant pt's?
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Metro cream
Clindamycin cream |
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What other drug is used to tx Giardia & Gardnerella in order to avoid the SE's of Metronidazole?
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Tinidazole
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What is the MOA of Polymyxins?
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Disruption of fungal membranes (like a detergent)
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What is the c/u for Polymyxins?
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G- rods
Fungal Infections |
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What is the toxicity of Polymyxins?
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ATN (acute tubular necrosis)
Neurotoxicity |
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If a pt has a positive PPD test but negative CXR, what is the next step mgmt?
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INH for 6 - 9 months
& Vit. B6 (b/c INH depletes B6) |
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What is the MOA of INH?
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Decreases synthesis of mycolic acid
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What is the toxicity of INH?
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Drug-induced SLE
Neurotoxicity (that's why we give concomittant Vit. B6) Hepatotoxicity Hemolytic anemia (G6PD pt's) |
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What drugs cause drug-induced SLE?
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*HIPPPE
Hydralazine INH Procainamide Phenytoin Penicillimine Ethosuximide |
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When do you proceed with a CXR in the following pt's:
a. PPD+ and has active TB (ie. TB-defining lesion) b. Lives in a prison yard c. Works in a hospital d. General population |
When induration is:
a. >5mm b. >10mm c. >10mm d. >15mm |
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If a pt meets the risk criteria for TB warranting a CXR, what is the next step (if any) in management if the CXR is negative?
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INH & Vitamin B6 for 9 months
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If a pt meets the risk criteria for TB warranting a CXR, what is the next step (if any) in management if the CXR is positive?
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*RIPES
Rifampin INH Pyrazinamide Ethambutol Streptomycin (added if necessary) |
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What is the 2nd line tx of TB?
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Cycloserine
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What is the MOA of Cycloserine?
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Inhibition of peptidoglycan synthesis
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What are the peptidoglycan synthesis inhibitors?
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Bacitracin
Vancomycin Cycloserine |
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What is the MOA of Ethambutol?
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Inhibits Arabinosyl Tranferase
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What is the toxicity of Ethambutol?
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Optic Neuritis
Central Scotoma |
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What is the MOA of Rifampin?
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Blocks mRNA synthesis by inhibiting DNA-Dependent RNA Polymerase
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What is the c/u of Rifampin?
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TB
Meningiococcal Prophylaxis Close contacts of Pt's with Hib Delays Dapsone resistence in the tx of Leprosy |
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What is the MOA of Dapsone?
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Inhibition of bacterial DHF synthesis by binding Dihydropteroate Synthetase
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What is an alternative MOA of Dapsone? For what disease is this alternative MOA the basis for treatment?
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"Blocks Myeloperoxidase (MPO) --> Dermatitis Hepatiformis
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What is the c/u of Dapsone?
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Leprosy
Dermatitis Hepatoformis (Celiac Sprue) Delays Rifampin resistence in the tx of TB 3rd-line tx for PCP |
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What is the toxicity of Dapsone?
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*HAM
Hemolytic Anemia Agranulocytosis Methemoglobinemia |
