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113 Cards in this Set
- Front
- Back
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Cell Wall Inhibitors
B-lactams |
-contain b-lactam ring
-penicillins, cephalosporin, carbapenans, aztreonam -INHIBIT TRANSPEPTIDATION |
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Penicillin G & Penecillin V
effects, acid stability |
(G)
-hydrolyzed in the stomach -metabolized by b-lactamase -slow release (V) -hydrolyzed in stomach -acid stable |
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Penicillin G & Penecillin V
Mech of Action |
Narrow Spectrum (vs. Gram +)
Contain b-lactam ring which inhibits transpeptidation |
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B-lactamase resistant penicillins
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Nafcillin (not affected by penicillinase)
Oxacillin (can cause hepatitis) Cloxacillin (oxacillin + Cl-) Dicloxacillin (oxacillin + 2Cl-) *Methicillin -for special cases -causes major kidney problems -MRSA=methicillin resistant staph. aureus |
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Extended Spectrum Penicillin
effects, mech of action |
-More effect on Gram-
-inhibited by penicillinases -acid stable (taken orally) -have b-lactam ring that inhibits transpeptidation -not b-lactamase resistant |
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Extended Spectrum Penicillins
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Amoxicillin (amino-penicillinase)
Ampicillin (amino-penicillinase)-->causes rash in mono pts Ticarcillin Piperacillin Mezlocillin Carbenicillin |
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Penicillinase Inhibitors
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Sulbactam
Clavulanic acid -inhibit penicillinase -can bind to the b-lactam ring |
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Penicillin side effects
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-allergic hypersensitivity
-immediate IgE response-hives, anaph. shock -delayed hypersensitivity-hepatitis, rash -high IV dose-seizures |
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Cephalosporins
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-same mech. as penicillin (prevent PG cross-link)
-more complex structure -NOT metabolized by b-lactamase -there are cephalosporinases -each generation has inc. G- and dec. G+ activity, and less susceptible to b-lactamase |
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1st Generation Cephalosporins
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Cephalexin
Cefazolin |
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2nd generation Cephalosporins
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Cefaclor
Cefuroxime -both taken orally -treat H. influenzae -both can cross blood-brain barrier |
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3rd Generation Cephalosporins
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Cefixime
Ceftazidime (used vs. pseudomonias) Ceftriaxone (longer half-life, effective againse N. gonnorrhea) -can enter CNS -vs. G- bacteria |
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4th Generation Cephalosporins
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Cefepime
-given IV, IM, very broad spectrum -Treats: staph aureus pseudomonias strep. pneumonie |
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Cephalosporin Side Effects
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-some allergic cross-reactivity with penicillins
-possibility of super infection with c. dificile |
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Cell Wall Inhibitors
Carbapenams |
Imipenem (IV, G+)
Meropenem (G-) -same SE as penicillin -causes SEIZURES. especially in epilepsy patients -treats difficult, mixed infection -metabolized in kidney by dihydropeptidase (makes toxic product) -ALWAYS given w/ Cilastatin |
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Monobactams
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Aztreonam (vs AEROBIC G-)
-SE: seizures, leukopenia -Dental Prophylaxis w/ antibiotics only for pts w/ heart defects! -NOT cross reactive w/ penicillin |
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Non B-lactam cell wall inhibitors
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Vancomycin
Bacitracin Fosfomycin Cycloserine |
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Vancomycin
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-binds DIALANINE RESIDUES
- vs. G+ cells -given IV (unless infection in intestine) -enters CNS (vs. cerebral infex) -SE:nephrotoxic, ototoxic, Red Man syndrome, Red Neck Syndrome -resistance:bact. replace terminal alanine w/ lactic acid |
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Bacitracin
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- vs G+
-used topically -nephrotoxic -inhibits BACTOPRENOL carrier |
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Fosfomycin
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blocks synth. of NAM
vs G+ or G- used for uncomplicated pts (UTIs) |
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Cycloserine
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inhibits INCORPORATION OF ALANINE INTO NAM
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Antibiotics that inhibit bacterial protein synthesis
MACROLIDES |
Erythromycin
Clarithromycin Azithromycin Telithromycin |
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Antibiotics that inhibit bacterial protein synthesis
Mech of Action |
-reversibly binds 50-S
-inhibits tRNA translocation -inhibits tRNA binding to 'p' site |
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Erythromycin
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SE:-GI upset/motility
-inhibits p450 -ototoxicity -liver damage -some pregnancy risk resistance: inc transport out of cell Targets: G+:Staph/Strep G-:Legionella, Chlamydia, Mycoplasma UNSTABLE IN ACID |
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Clarithromycin
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used to target HELICOBACTER PYLORI
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Azithromycin
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Used against H. influenzae, and chlamydia
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Telithromycin
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-SEVERE LIVER TOXICITY
-WORSENS MYASTHENIA GRAVIS -does not readily become resistant (not readily pumped out) |
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Aminoglycosides
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Streptomycin
Gentamycin Neomycin Amikacin Tobramycin Kanamycin Netilmicin |
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Aminoglycosides
Mechanism |
IRREVERSIBLY binds 30-S (cidal)
Inhibits/alters tRNA binding on mRNA Highly basic, become ionized (enter CNS) Used with b-lactamase |
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Streptomycin
Side Effects |
Ototoxicity: hearing loss, impaired balance
Nephrotoxicity: Kidneys excrete, induced renal failure *most common cause of drug induced renal failure Decrease Ach receptors (neuromuscular block) Fetal Damage (category D) -most POTENT antibiotic |
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Streptomycin
Resistance & Targets |
Resistance
- decreases uptake - increases metabolism -MOST POTENT ANTIBIOTIC Targets - Aerobic G- bacteria - TB - works only w/ Aerobic species |
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Gentamycin
SE |
High dose:irreversible effects on balance
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Neomycin
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-severe nephrotoxin
-used topically (orally for gut infections) |
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Amikacin
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Not readily metabolized by bacteria
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Tetracyclines
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Tetracyclin
Doxycycline Minocycline Tigecycline |
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Tetracycline
Mechanism |
REVERSIBLY binds to 30-S (static)
inhibits binding at 'a' site oral or injection administration can pass the placenta |
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Tetracycline
SE |
Binds cations: Ca2+, Fe2+, Al3+
Ca2+ binding in teeth:permanent mottling Category D fetal damage -bone deformation -renal/hepatic toxicity -GI upset -Allergic photosensitivity |
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Tetracycline
Resistance & Targets |
Resistance: decrease uptake & increase efflux
Targets: G+ and some G- Rickettsia Spirochetes (lyme disease) Syphilis Helicobacter pylori (ulcers) Mycoplasma |
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Doxycycline administration
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IV
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Minocycline
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Gets into CNS better
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Tigecycline
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Broad spectrum
Minocycline derivative |
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Miscellaneous protein synthesis inhibitor?
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Chloramphenicol
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Chloramphenicol
Mechanism |
inhibits PEPTIDYL TRANSFERASE (associated w/ 50s)
cidal or static action gets into CNS |
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Chloramphenicol
Side Effects |
inhibits p450
aplastic anemia not well absorbed in newborns (liver metabolism) -inc conc., vasomotor collapse Hemolytic Anemia in pts with G6PDH deficiency Pregnancy category C |
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Chloramphenicol
Resistance & Targets |
Resistance: increases metabolism
Targets: -salmonella -used in poor countries |
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Lincosamides
& Mechanism, target, DOC? |
Clindamycin
Licomycin -binds 50s -inhibits tRNA translocation inhibits tRNA binding to 'p' site target site modified cation DOC: severe anaerobic infections G+ & G- dental prophylaxis |
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Streptogramins
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Quinupristin+ Dalfopristin
-binds 'a' & 'p' sites -cidal action SE: inhibits p450, causes joint/muscle pain Targets: G+, esp VANCOMYCIN RESISTANT STAPH & STREP |
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Oxazolidinones
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Linezolid
-binds 50s -inhibits binding of Fmet tRNA to 'p' site SE: anemia, thrombocytopenia -targets: altered targets G+ vs staph: static vs strep: cidal MRSA & vancomycin resistant enterococcus infections |
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Daptomycin
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Lipopeptide- makes pores in bacterial cell membrane
Depolarization: decreases DNA, RNA, protein synthesis SE:possible SE on muscle Targets: Aerobic G+ -used in skin and soft tissue infections -given IV |
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Fluoroquinolines (-floxacins)
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Ciprofloxacin
Ofloxacin Gatifloxacin Mofloxacin Levofloxacin Gemifloxacin Norfloxacin Lomefloxacin |
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Ciprofloxacin
Mechanism |
Mech
-inhibits bacterial topoimerase Topoimerase II: DNA Gyrase Topoimerase IV: separates daughter strands after DNA replication cidal |
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Ciprofloxacin
SE, Resistance, Targets |
SE:
-developing cartilage damage -tendonitis, achilles rupture - generally dont use in pregnant Resistance: altered enzyme target increase efflux Broad Spectrum, G+,G-, Acid fast bacteria |
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Anti-metabolites
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Sulfisoxazole
Sulfacetamide Sulfadizine Trimethoprim |
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Sulfonamides
Mech |
Mech: inhibits DIHYDROPTERATE SYNTHETASE
static |
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Sulfonamides
SE, Resistance, Target |
SE:
-Allergic Rash (Stevens-Johnson Syndrome) -Hemolytic Anemia in G6PDH def -Category C pregnancy Resistance:Alteration of target enzyme -broad spectrum -primarily treats UTI |
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Trimethoprim
Mech |
Mech:
-inhibits DIHYDROFOLATE REDUCTASE -specific bacterial enzyme -combo w/ sulfa: trimethoprim + sulfamethoxazola= COTRIMAZOLE |
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Trimethoprim
SE, Targets |
SE:
Megaloblastic anemia Leukopenia Granulocytopenia (prevented by folic acid use) Target: G+ -treats UTI bc they concentrate in prostate & vagina |
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Systemic Antimicrobials
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Metronidazole
Nitrofurantoin |
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Metronidazole
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Mech:
-binds many different molecules -prodrug converted to free radical by anaerobic bacterica High dose: seizures Given IV for ANUG |
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Nitrofurantoin
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Prodrug-converted by bacteria and concentrates in urine
SE: cough, chest pain, brown pee, hemolytic anemia Treats UTI of staph aureus & e. coli origin |
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Agents used only topically
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Polymixin B
Gramicidin Neomycin Mupirocin Retapamulin |
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Polymixin B
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Binds to LPS sites & increases cell membrane permeability
Neurotoxic, Nephrotoxic, Neuromuscular block Gram - targets |
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Gramicidin
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Forms ion channels in bacterial cell membrane
-mix of 3 peptide antibiotics Gram + target |
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Mupirocin
Retapamulin |
-inhibit PROTEIN SYNTHESIS
Mupirocin--> Staph/Strep Retapamulin--> G+ |
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Neosporin mix
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neomycin
polymixin gramicidin |
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polysporin mix
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polymixin
Bacitracin |
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polytrim mix
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trimethoprim
polymixin |
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Antimycobacterial Agents
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Isoniazid
Rifampin Pyrazinamide Ethamutol Dapsone |
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Isoniazid
mech |
Prodrug- activated into mycolic acid derivative
-cidal in growing cells -static in dormant cells |
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Isoniazid
SE |
-inc vitamin B6 excretion-->niacin def
-pellagra -optic neuritis -hepatotoxicity -works against TB 2 or more agents always used to prevent resistance metabolized by acetylation (slow acetylator=more SE) tx time: 6mo-2yr |
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Rifampin
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Inhibits DNA dependent RNA polymerase
-cidal SE: hepatotoxicity red color in all body fluids INDUCES p450 works against TB |
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Pyrazinamide
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Converted in macrophage lysosomes to MYCOLIC ACID SYNTHESIS INHIBITOR
SE: hepatitis works against TB |
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Ethamutol
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Inhibits ARABINOSYL TRANSFERASE (need for synth of cell wall)
SE: optic neuritis, altered color vision works against TB |
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Dapsone
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INHIBITS FOLATE SYNTHESIS (like sulfamides)
SE: rash, Hemolytic anemia Targets: mycobacteria leprae (leprosy, Hansens disease) |
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ANTIFUNGALS
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ANTIFUNGALS
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Polyene Antibiotics
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Nystatin (not readily absorbed; not systemic
Amphotericin B (used systemically) Natamycin (primarily used in eye) -Binds to ERGOSTEROL in cell wall (causes membrane leakage) -topical use -kidneys most affected (too potent for parenteral dosing |
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For Ringworm
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Tolnaftate (for athletes foot)
Ciclopirox Terbinafine** (used systemicaly) |
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For Candida & Ringworm
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Miconazole & other -azoles
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Griseofulvin
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Taken up by growing skin and concentrates in keratin layer
Works by binding to fungal MICROTUBULES, INHIBITING MITOSIS Rash-derived from penicillin INDUCES p450 |
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Terbinafine
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INHIBITS ERGOSTEROL SYNTHESIS
INHIBITS SQUALENE EPOXIDASE (causes toxic squalene buildup) inhibits p450 some effects on liver systemically used for skin infections |
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Systemic Mycoses
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Tx fungal infections of body other than skin
Pathologic: Histoplasmosis Blastomycosis Coccidomycoses Opportunistic: IV, immunocompromised, intubations -fungi can grow into open spaces and occlude airways, ureters, vessels |
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Amphotericin B
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-Binds ergosterol, causes membrane leakag
-insoluble in H20 (used as detergent) >80% impaired renal >50% fever, convulsion, vomit, headache anemia |
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IMIDAZOLES
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Ketoconazole
-inhibits human/fungal p450 Lanosterol demethylase=p450 decreases adrenal and gonadal steroids in humans |
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TRIAZOLES
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Fluconazole generic
Itraconazole generic: -strong p450 inhibitor -broad fungi spectrum -causes heart problems Posaconazole Voriconazole |
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Flucytosine
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Pyrimidine analog
Gets into CSF-->converted to 5-Fluoracil by fungi (converted by bacteria in human gut) INHIBITS THYMIDINE SYNTHESIS GI upset Bone marrow depression |
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Terbinafine
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Allylamine
Liver damage |
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Echinocandins (-fungin)
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Capsofungin
Micafungin Anidulafungin INHIBIT SYNTHESIS OF POLYSACCHARIES NEEDED FOR FUNGAL CELL WALL |
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ANTIVIRAL
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ANTIVIRAL
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Herpes Treatment
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Acyclovir
Valacyclovir Famcyclovir Ganciclovir Valganciclovir Cidofovir Foscarnet Fomivirsen |
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Acyclovir
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Inhibits viral DNA Polymerase
Renal Damage CNS-delirium Prodrug: phosphorylated by VIRAL THYMIDINE KINASE Treats herpes simplex, herpes zoster |
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Valacyclovir
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Inhibits viral DNA Polymerase
Prodrug converted to acyclovir -better oral availability Treats herpes simples, herpes zoster |
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Famciclovir
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Inhibits viral DNA Polymerase
Prodrug converted to acyclovir analog Treats herpes simplex, herpes zoster |
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Ganciclovir
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Inhibits viral DNA Polymerase
Treats Cytomegalovirus Prodrug converted by VIRAL KINASE Neutropenia Thrombocytopenia Teratogens |
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Valganciclovir
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Inhibits viral DNA Polymerase
Treats Cytomegalovirus Prodrug converted to Ganciclovir |
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Cidofovir
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Inhibits viral DNA Polymerase
Treats Cytomegalovirus Prodrug converted by VIRAL KINASE Nephrotoxic |
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Foscarnet
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Directly inhibits viral DNA polymerase
Treats Cytomegalovirus SE: Blindness ANTISENSE Molecule IV dose 3x/day |
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Fomivirsen
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Binds CMV mRNA
Treats Cytomegalovirus in Eye |
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Hepatitis B Treatment
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Inhibits Hep B DNA Polymerase
Adefovir (renal damage, liver problems Entecavir (liver problems, lactic acidosis) |
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Respiratory Syncitial Virus Treatment
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Ribavarin
Inhibits RNA dependent RNA Polymerase Prodrug- Guanosine analog phosphorylated in cell Treats severe lower Resp. Tract Infections Pregnancy Category X Hemolytic Anemia Depresses Pulmonary Function Cardiac Problems |
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Influenza Virus A Treatment
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Amantadine (also used in Parkinsons; increases DA uptake)
Rimantadine (fewer SE) Block uncoating of virus inside host cell Renal Failure Teratogenesis CNS: dizzy, slurred speech, confusion given orally |
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Influenza A & B Treatment
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Zanamivir (dry powder)
Oseltamivir INHIBIT NEUROAMINIDASE, which inhibits release of new virus cells from cell |
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Hepatatis Virus Treatment
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Recombinant interferon alpha
Inhibits viral mRNA replication Tx: Hep B and Hep C Enhances normal immune cell function |
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HIV
Nucleoside Analog Reverse Transcriptase Inhibitors |
Didanosine
Abacavir Zidovudine Zalcitabine Lamivudine Emtricitibine Stavudine Telbivudine |
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HIV
Nucleoside Analog Reverse Transcriptase Inhibitors Properties |
Inhibit Reverse Transcriptase
SE of all: Anemia Neutropenia Muscle Pain/Damage SE of some: Pancreatitis Lactic Acidosis -phosphorylated in the cell |
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HIV
NON-Nucleoside Analog Reverse Transcriptase Inhibitors |
Nevirapine
Delavirdine Efavirenz |
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Nevirapine
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Inhibits reverse transcriptase
Associated with Stevens-Johnson Syndrome Not Phosphorylated |
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Delavirdine
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Associated with Stevens-Johnson Syndrome
Metabolized by p450 |
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Efavirenz
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CNS Toxicity
Hallucination |
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HIV
Protease inhibitors |
Saquinavir
Ritonavir Amprenavir |
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Saquinavir
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Inhibit post-synthetic processing of proteins by inhibiting proteosomes
SE: Nausea, Vomiting Inhibit p450 Alters fat distribution Poor Oral Absorption (4%--> 18 capsules/day) |
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Ritonavir
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Most potent known p450 inhibitor
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Amprenevir
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Allergic Response (contains sulfur)
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Enfuvirtide
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Inhibits binding of HIV to CD4 target cell
2x/day injection ($20K/yr) |
