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Pharmacology - Potters drugs
potters drugs for exam #4: know class, MOA, ophthalmic indications, and ADR
90
Other
Graduate
04/03/2009

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Term
Antimicrobial
Definition
chemical substance that inhibits bacteria & other microbes, stains pink
Term
Antibiotic
Definition
chemical substance produced by a microbe, which has capacity to inhibit selectively or even destroy bacteria & other microbes through an antimetabolic mechanism
Term
Antiseptic
Definition
chemical substance which when applied to living tissue, destroys or inhibits the growth of microbes primarily pathogenic microbe
Term
Bactericidal
Definition
ability of antimicrobial agent to KILL bacteria
Term
Bacteriostatic
Definition
ability of antimicrobial agent to inhibit growth &/or reproduction of bacteria; endogenous immune system must eradicate organism
Term
Beta lactamases
Definition
endogenous bacterial enzymes that deactivate geta-lactam antibiotics
Term
Narrow-Sprectrum Antibiotics
Definition
act on single or limited group of organisms
Term
Extended-Spectrum Antibiotics
Definition
effective against gm+ and gm- organisms
Term
Broad-Spectrum Antibiotics
Definition
effective against gm+, gm-, and other organisms
Term
Bacteria Structure
Definition
capsule, cell wall (peptidoglycan nag-nam), plasma(cell) membrane
Term
Gram Positive
Definition
thick cell wall, stain purple
Term
Gram Negative
Definition
Thin cell wall, have lipid A FA outer membrane, better barrier against antibiotics, harder to treat
Term
Anaerobic Organisms
Definition
usually in the gut, gram +, gram -,
Term
Atypical Bacteria
Definition
dont act like gram + or -, ex: chlamydia, mycoplasm, mycobacterium
Term
Selective Bacterial Targets
Definition
1. cell wall - humans dont have
2. DNA gyrase - humans have different type enzyme
3. Ribosomes - humans are different size
4. Plasma Cell membrane
5. Folic Acid Synthesis
Term
Complications of antibiotic Therapy
Definition
1. Hypersensitivity
2. direct organ toxicity to host
3. Alteration of normal GI flora
Term
Antimicrobial Resistance
Definition
ability of microorgansim to prevent or avoid action of antimicroial agent
Cross resistance
Term
DI: ASA and Wafarin-Coumadin
Definition
Inc wafarin blood levels
MOA; protein binding displacement
Term
DI: Azole Antifunglas (ketoconazole-nizoral) and CCB (Benzodiazepine)
Definition
Inc CCB blood levels, Inc Benzodiazepine blood levels
MOA: CYP3A4 inhibitor
Term
DI: Broad Spectrum Antibiotics and OCP
Definition
Decrease Estrogen and Progestin blood levels
MOA: dec bacterial hydrolysis of hormones therefore dec absorption
Term
DI: CAI and Lithium-Eskalith
Definition
Increase excretion of lithium
Term
DI: Clarithromycin,Erythromycin and HMG CoA Reductase Inhibitor
Definition
Dec Statin Metabolism
MOA: CYP3A4 substrates
Term
DI: Erythromycin and THeophylline
Definition
Inc Theophylline blood levels
MOA: dec theophylline metabolism
Term
DI: Ketoralac and ASA/other NSAIDS/Probencid
Definition
Serious ketoralac ADR
Term
DI: NSAID and ACE inhibitors
Definition
dec antihypertensive effect of ACEI
MOA:inc constriction of afferent arteriole in nephron
Term
DI: NSAID and Beta Adrenergic antagonist
Definition
dec antihypertensive efffect of beta blocker
Term
DI: NSAIDS and Furisemide-Lasix
Definition
dec pharmacologic effect of furosemide
Term
DI: NSAIDS and Phenytoin
Definition
Inc Phenytoin plasma levels
MOA: dec phenytoin metabolism
Term
Quinolones and Antacids/Iron
Definition
dec GI absorption of quinolones
Term
DI: Quinolones and Theophylline
Definition
dec pharmacologic effect of theophylline
MOA: dec thephylline metabolism
Term
DI: Sulfamethoxazole/PNC/Cehpalosporins and WAfarin-Coumadin
Definition
inc wafarin blood levels
MOA: displace plasma protein binding, removing vit K producing bacteria from gut
Term
DI: Tetracycline and Antacids/Iron/Digoxin-lanoxin
Definition
dec GI absorption of tetracycline, Inc digoxin blood levels
MOA: dec digoxin metabolism
Term
PNC and Cephalosporin MOA
Definition
1. inactivate PBP (PBP involve in synthesis of cell membrane)
2. Inhibit bacterial Cell WAll Synthesis - inhibit TRANSPEPTIDATION by PBP, (PEP cross linking), bacterial lysis by intracellular build up of osmotic pressure cell lysis
Bactericidal action: polymerization, nag-nam formation
Term
MRSA
Definition
more respiratory
nosocomial infections often spread among health care workers
REsistant to most PNC, cephalosporins, aminoglycosides, and macrolides
Vancomycin restance happening - VRSA
Linezolid-zyvox reserved for resistant strains
Term
CA-MRSA
Definition
skin infections-pimple and boils
can be big problems with diabetic foot infections and insect bites
resistance is increasing
Term
ADR/Toxicity/CI of PNC and Cephalosporins
Definition
Hypersensitivity - PNS(2-5%), ceph(1-2%)
Immediate: <72 hrs, uticaria, laryngeal edema, bronchospasm, hypotension, anaphylaxis
Late: >72hrs diffuse maculopathy rash, serum sickness, drug fever
Cross rxn w/ other B lactam antibiotics: occurs 5-15%,
Term
Penicillin VK
Definition
Natural and Semi-Synthetic PNCs (oral)
Gr + and Gr -
resetance is there
gets destroyed by Beta lactamases easily
Term
Amoxicillin-Amoxil
Definition
Natural and Semi-Synthetic PNCs (oral)
gr + and Gr-
Term
Dicloxacillin-Dynapen
Definition
Penicillinase Resistant PNCs (oral)
Gram +
Internal Hordeolum
Term
Amoxicillin/Clavulanic Acid-Augmentin
Definition
PNC + Beta Lactamase Inhibitor combo (oral)
Preceptal Cellulitis
Gr + and Gr -
ADR: >10% diarrhea
Term
Ticarcillin-Ticar
Definition
Anti-Psuedomonal PNC (IV)
IND: corneal ulcers due to psudomonas
Gr-
Term
Cephalexin-Keflex
Definition
Cephalosporins - 1st Generation (oral)
Internal Hordeolum
Gr+ > Gr-
Term
Cefadroxil-Duricef
Definition
Cephalosporins - 1st Generation (oral)
Internal Hordeolum
Gr+ > Gr-
Term
Cefaclor-Ceclor
Definition
Cephalosporin-2nd Generation (oral)
Gr- > Gr+
ADR: <1% Serum Sickness
Term
Loracarbef-Lorabid
Definition
Cephalosporin-2nd Generation (oral)
Gr- > Gr+
Term
Cefprozil-Cefzil
Definition
Cephalosporin-2nd Generation (IV)
Gr- > Gr+
Term
Cefdinir-Omnicef
Definition
Cephalosporin-3rd Generation (oral)
Orbital Cellulitis
GR- >>>Gr+
Term
Cefpodoxime-Vantin
Definition
Cephalosporin-3rd Generation (oral)
Orbital Cellulitis
GR- >>>Gr+
Term
Ceftriaxone-Rocephin IV
Definition
Cephalosporin-3rd Generation (IV)
Orbital Cellulitis
GR- >>>Gr+
Term
Vancomycin
Definition
Oral and IV acts on cell wall but NOT beta lactam antibiotic
MOA: Inhibits Polymerization of Nag-Nam by Blocking Transglycosidase
Gr + ONLY
MRSA, has use in resistance bacteria but resistence is growing!
Term
Bacitracin
Definition
Ocular Ointment: bacitracin; bacitracin+Polymyxin B-Polysporin
Dermatologic ointment: Bacitracin; bacitracin+Neomycin+polymyxin-Cortisporin
act on cell wall but NOT a beta lactam antibiotic
Inhibits Polymerization of Nag-Nam by Blocking Bactoprenol
Gram + ONLY
ADR: topical admin-nephrotoxicity
Term
Polymyxin B
Definition
Ocular ointment: bacitracin+polymyxin B-Polysporin
Dermatologic ointment: bacitracin+Neomycin+polymyxin-Cortisporin
Act on cell wall but NOT beta lactam antibiotic
MOA: CAtionic detergent that interrupt lipopolysaccharides in outer cell membrane, INCREASES cell wall permeability due to inc osmotic pressure inside bacteria
GR-, including psuedomonas
Term
Tetracycline-Sumycin
Definition
Protein Synthesis Inhibitor-tetracycline
Blepharitis, Meibomian Gland Infections, Acne Rosacae
MOA: binds irreversibly to 30s subunit of Bact, blocks AA-tRNA docking to mRNA-ribosome complexat the A (acceptor) site
GR+ and Gr-
ADR/Toxic/CI: CI in prego, breast feed, kids-fetal bone and teeth problems, tooth discoloration
CI in REnal failure
Avoid cations-milk, ca2+, antacids
photoxicity: severe sunburn
Rare-psuedotumor cerebri
DI: OCP, pregnancy can develop
Term
Doxycycline-Vibramycin
Definition
Protein Synthesis Inhibitor-Tetracycline
Blepharitis, Meibomian Gland Infections, Acne Rosacae
MOA: binds irreversibly to 30s subunit of Bact, blocks AA-tRNA docking to mRNA-ribosome complexat the A (acceptor) site
GR+ and Gr-
ADR/Toxic/CI: CI in prego, breast feed, kids-fetal bone and teeth problems, tooth discoloration
CI in REnal failure
Avoid cations-milk, ca2+, antacids (less severe)
photoxicity: severe sunburn
Rare-psuedotumor cerebri
DI: OCP, pregnancy can develop
Term
Minocycline-Minocine
Definition
Protein Synthesis Inhibitor-Tetracycline
Blepharitis, Meibomian Gland Infections, Acne Rosacae
MOA: binds irreversibly to 30s subunit of Bact, blocks AA-tRNA docking to mRNA-ribosome complexat the A (acceptor) site
GR+ and Gr-
ADR/Toxic/CI: CI in prego, breast feed, kids-fetal bone and teeth problems, tooth discoloration
CI in REnal failure
Avoid cations-milk, ca2+, antacids (less severe)
photoxicity: severe sunburn
Rare-psuedotumor cerebri
DI: OCP, pregnancy can develop
Term
Gentamycin-Gentak
Definition
Protein Synthesis Inhig-Aminoglycoside(IV)
MOA: bind to 30s subunit of bact altering triplet codon of mRNA causing the wrong AA-tRNA insertion
Gr+ and Gr-
ADR/Toxic/CI: Nephrotoxicity (10-15%, maybe reversible)
ototoxicity (1-5%, maybe reversible)
Ocular: epi breakdown, weepy erethema, and edema or eyelids
Systemic gentamycin, psuedotumor cerebri w/ secondary papilledema
Term
Tobramycin-Nebcin
Definition
Protein Synthesis Inhib-Aminoglycoside(IV)
MOA: bind to 30s subunit of bact altering triplet codon of mRNA causing the wrong AA-tRNA insertion
Gr+ and Gr-
ADR/Toxic/CI: Nephrotoxicity (10-15%, maybe reversible)
ototoxicity (1-5%, maybe reversible)
Ocular: epi breakdown, weepy erethema, and edema or eyelids
Systemic gentamycin, psuedotumor cerebri w/ secondary papilledema
Term
Amikacin-Amikan
Definition
Protein Synthesis Inhib-Aminoglycoside(IV)
MOA: bind to 30s subunit of bact altering triplet codon of mRNA causing the wrong AA-tRNA insertion
Gr+ and Gr-
ADR/Toxic/CI: Nephrotoxicity (10-15%, maybe reversible)
ototoxicity (1-5%, maybe reversible)
Ocular: epi breakdown, weepy erethema, and edema or eyelids
Systemic gentamycin, psuedotumor cerebri w/ secondary papilledema
Term
Neomycin/Polymyxin B/bacitracin-Neosporin
Definition
Topical Ointment
Protein Synthesis Inhib-Aminoglycoside
MOA: bind to 30s subunit of bact altering triplet codon of mRNA causing the wrong AA-tRNA insertion
Gr+ and Gr-
ADR/Toxic/CI: only with IV
Term
Erythromycin-E-mycin
Definition
Protein Synthesis Inhib-Macrolide
MOA: binds to 50s subunit of bact ribosome, inhibits TRanslocation (transfer from A to P site) of protein synthesis; inhibits peptide bond formation and peptidyl transferase
Gr+ and Gr-
ADR: Gi distress (erythromycin>clarithromycin>azithromycin)
Term
EES
Definition
Protein Synthesis Inhib-Macrolide
MOA: binds to 50s subunit of bact ribosome, inhibits TRanslocation (transfer from A to P site) of protein synthesis; inhibits peptide bond formation and peptidyl transferase
Gr+ and Gr-
ADR: Gi distress (erythromycin>clarithromycin>azithromycin)
Term
Ery-Tab
Definition
Protein Synthesis Inhib-Macrolide
MOA: binds to 50s subunit of bact ribosome, inhibits TRanslocation (transfer from A to P site) of protein synthesis; inhibits peptide bond formation and peptidyl transferase
Gr+ and Gr-
ADR: Gi distress (erythromycin>clarithromycin>azithromycin)
Term
Azithromycin-Zithromax
Definition
Protein Synthesis Inhib-Macrolide
Longer T1/2, less pills, inc compliance
MOA: binds to 50s subunit of bact ribosome, inhibits TRanslocation (transfer from A to P site) of protein synthesis; inhibits peptide bond formation and peptidyl transferase
Gr+ and Gr-
ADR: Gi distress (erythromycin>clarithromycin>azithromycin)
Term
Azithromycin-Zithromax
Definition
Protein Synthesis Inhib-Macrolide
Longer T1/2, less pills, inc compliance
MOA: binds to 50s subunit of bact ribosome, inhibits TRanslocation (transfer from A to P site) of protein synthesis; inhibits peptide bond formation and peptidyl transferase
Gr+ and Gr-
ADR: Gi distress (erythromycin>clarithromycin>azithromycin)
Term
Z-Pak
Definition
Protein Synthesis Inhib-Macrolide
Longer T1/2, less pills, inc compliance
MOA: binds to 50s subunit of bact ribosome, inhibits TRanslocation (transfer from A to P site) of protein synthesis; inhibits peptide bond formation and peptidyl transferase
Gr+ and Gr-
ADR: Gi distress (erythromycin>clarithromycin>azithromycin)
Term
Fluroquinolone Antibiotics-"Quinolones"
Definition
MOA: Inhibit replication of bact DNA, interfere w/ topisomerase II and IV during cell division, binds to both DNA gyrase and bact DNA to from complex that inhibits resealing step, bacterial DNA cleaves apart!
Topo II- Gr +
Topo IV- Gr-
Mammals dont have topo II
Overall DI:cations (dec effectiveness)
CI: nursing moms and kids under 18; articular erosion, tendon rupture, CT toxicity
Caution in pregnancy
Term
Ciprofloxin-Cipro
Definition
Quinolones-2nd generation, oral
prophylaxis and tx of anthrax
Gr- >> Gr+
also for atypical organisms, mycoplasm and chlamydia
Term
Norfloxacin-Noroxin
Definition
Quinolones-2nd generation, oral
Gr- >> Gr+
also for atypical organisms, mycoplasm and chlamydia
Term
Gatfloxicin-Tequin
Definition
Quinolones-3rd Generation
Gr+ and Gr-
also for atypical organisms, mycoplasm and chlamydia
Term
Levofloxacin-Levaquin
Definition
Quinolones-3rd Generation
Gr+ and Gr-
also for atypical organisms, mycoplasm and chlamydia
Term
Folic Acid Antagonists
Definition
MOA: sulfonamides are analogs of PABA and bind w/ dihydropteroate (only on bact) synthetase and inactivates it, dec folic acid
Trimethoprim inhib dihydrofolate reductase, dec production of tetrahydrofolate acid(both human and bact, more toxic)
Bacteriostatic
ADR/Toxic/CI: Crytalluria (need to dirnk lots of water w drug); Hypersensitivity (SJS); neonatal kernicterus(dont use in 3rd trimester, excess bilirubin crosses BBB); Myopia w/ systemic sulfonamides (reversible)
Term
Sulfamethoxazole-Septra
Definition
Sulfonamide-folic acid antagonist
Oral
Term
Bactrim
Definition
Sulfonamide-folic acid antagonist
Oral
Term
Sulfisoxazole-Gantrisin
Definition
Sulfonamide-folic acid antagonist
Oral
Term
Sulamethoxazole-Trimethoprim (SMZ-TMP)-Bactrim DS
Definition
Folic Acid Antagonist-oral and IV
Lower dose of trimethoprim
Gr+ and Gr-
Term
Septra DS
Definition
Folic Acid Antagonist-oral and IV
Lower dose of trimethoprim
Gr+ and Gr-
Term
Metrinidazole-Flagyl
Definition
MOA: toxic to bact DNa and RNA
Dont take w/ alcohol
spectrum: anaerobes and protozoa
Term
Nitrofurantoin-Macrodantin
Definition
Tx UTI's
MOA: Inhibits acetyl CoA, interferes w/ bact carbohydrate metabolism
some action to inhibit cell wall sythesis
Gr + and Gr-
Term
Macrobid
Definition
Tx UTI's
MOA: Inhibits acetyl CoA, interferes w/ bact carbohydrate metabolism
some action to inhibit cell wall sythesis
Gr + and Gr-
Term
SJS-Stevens Johnson Syndrome
Definition
autoimmune rxn producing mucosal lesions and mult blisters (>10% body surface)
usu 1-3 wks after drug initiated
preceded by fever, sore throat, chills
Corneal Acarring!, blindness 7-10%
Toxic Epidermal NEcrosis(TEN), worst case, 40% fatality
Term
Tuberculosis Info
Definition
13M in US latently affected; 15-10K active
S/S: wweight loss, malaise, fever, night sweats, productive cough, chest pain, cough up blood
Mycobacterium
Transmissible by respiratory
in latency bacteria are in granulomas or macs
TX: resistence emerging quickly, Tx active w/ Mult drugs for long periods of time
Tx Latent for months to years
Term
Isoniazid-Nydrazid,PO
Definition
Binds to and Inhibits production of MYCOLIC ACIDS
Use: Mycobacteria, TB
Term
Ethambutol-Myambutol, PO
Definition
Inhibits ARABINOGALACTAN so cell wall(outer membrane) does NOT form
Use: mycobacteria, TB
ADR: retrobulbar optic neuritis w/ blur, RG color blindness
Term
Rifampin-Rifaden, PO, IV
Definition
never used alone
Inhibits RNA Synthesis, blocks transcription by inhibiting DNA dependent RNA Polymerase
Blocks action of beta subunit
USE: mycobacteria, TB and Gr+ and Gr-(not first line)
ADR: red orange discloration of urine, feces, sweat, tears(colors CL)
Term
Antiviral Agents(NONretroviral) info
Definition
1. Viruses are Intracellular parasites (DNA or RNA enclosed by protein coat)
2. viral enzymes shut down host enzymes
3. ideally attack viral specific enzymes only
Term
Respiratory Infections
Definition
Viral RNA encoded viruses!
Influenza A and B
antivirals must be administered early to be effective, but even then only dec symptoms by 2 days!
Term
Amantadine-Symmetrel
Definition
Inhibits Viral uncoating, ihibits viral ion channel once its inside host cell by inhib viral M2 protein
Term
Oseltamivir-Tamiflu
Definition
Neuraminidase Inhibitors
Prevents the release(budding) of new virions from the cell into the blood stream, therefore dec the virus
Term
Acyclovir-Zovirax
Definition
Viral DNA Synthesis inhibitor
MOA in herpes: agent is phosphorylated by viral thymidine kinase and compete w/ GTP for viral DNA polymerase, the defective nucleotide is incorp into viral DNA and causes premature DNA chain termination
MOA in CMV: defective nucleotide by different path, suicude inactivation of DNA polymerase, same effect
Term
Definition
Viral DNA Synthesis inhibitor
MOA in herpes: agent is phosphorylated by viral thymidine kinase and compete w/ GTP for viral DNA polymerase, the defective nucleotide is incorp into viral DNA and causes premature DNA chain termination
MOA in CMV: defective nucleotide by different path, suicude inactivation of DNA polymerase, same effect
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