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What is penicillin converted into by beta lactamase?
Penicilloci acid-inactive and allergenic.
What is the mech of action of narrow spectrum penicllins?
bind to penicillin binding protein, inhibit cross linking of peptidoglycan, causes autolysis and altered shape.
What bugs do narrow spectrum antibiotics hit?
Gram pos cocci-streptococci
gram negative cocci-meningococci
Gram pos bacilli-Clostridia
spirochetes-t. pallidum
What are the therapeutic uses of penicillin G?
Endocarditis (streptococci), pneumococcal pneumonia, meningococcal meningitis, gas gangrene, syphilis
Pharmokinetics of penicillin G?
How is it excreted?
degraded by stomach acids-usually given parenterally, IV, giving them IM can prolong there use in body for 2-3 weeks
Renal tubular secretion blocked by PROBENECID
What is penicillin V used for?
Oral-used for minor outpatient infections pharyngitis.
What are the adverse affects?
Skin rash, anemia, hepatitis, nephritis
What are the Anti-Staph penicillins?
Methicillin, Nafcillin, Oxacillin, dicloxacillin
What do you use if bug is resistant to Methicillin and all anti-staph penicillins?
What do you use nafcillin and oxacillin for?
Methicillin resistant Staph, endocarditis, OSTERMYELITIS, pneumonia, toxic shock, skin and soft tissue inf.
How are naf and oxa cillin given?
Adverse effects of Methicillin
Nafcillin is preferred
Anti bug activity of amoxicillin?
Gram pos cocci (pneumococci, streptococci, staphylococci (amox+clavulanate)
Use of amoxicillin?
Resp. tract infections, prophylaxis of bacterial endocarditis, lyme disease, skin and soft tissue inf. UTI
What is best for a boy bitten by a dog?
Pasteurella-Amox + Clavulanate
What is ampicillin used for?
Listeria-food in fridge long time.
Gram negative bacilli-e. coli, p. multocida, bacteroides
What is the therapeutic use?
Meningitis, Diabetic skin ulcers and bite wounds with SULBACTAM, endocarditis with GENTAMYCIN, lyme disease
How is ampicillin given?
Oral or parenteral and combined with sulbactam
What adverse effects does ampicillin have?
maculopapular rash with viral infections
What gram negative bacilli do ticarcillin and pipercilin act on?
pseudomonas aeruginosa, e. coli, bacteroides fragilis
How are ticarcillin and pipercillin administered?
IV and combined with clavulanate or tazobactam.
Why are the carbampenems more stable than the penicillins?
The sulfur atom is replaced with a carbon atom
What is the antimicrobial activity of the carbapenems?
Bactericidal, broad spectrum, drug resistant gram negative bacilli, gram (+), anerobes
Therapeutic use of carbapenems?
Serious infections in hospitilized patients due to drug resistant gram (-) rods, POLYMICROBIAL RODS
How are the carbapenems administerd and what are adverse effects?
Seizures with high doses,
What is special about aministration of imipenem?
Combined with cilastatin-inhibits metabolism by renal dehydropeptidase
What is the only monocyclic beta lactam?
Aztreonam-used for infections due to aerobic gram negative rods, and people allergic to penicillins or cephalasporins.
Compare cephalasporins to penicillins
Cephalasporins-two or three R groups, greater structural diversity and stability, more stable to beta-lactamase, less allergenic
What is spectrum of action of 1st gen cephalasporins?
Gram positive cocci except enterococci, a few gram negative bacilli,
Use-skin/soft tissue, UTI, and surgical prophylaxis.
What is the difference in activity of 2nd gen cephalasporins compared to first?
More active against gram negative bacteria- USE otitis media and sinusitis (Oral drugs) PELVIC AND INTRAABDOMINAL INFECTIONS (cefotetan)
3rd generation cephalasporins?
Streptococci, wide range of gram negative bacteria
What is ceftazidime used to treat?
What are therapeutic uses of 3rd generation?
Gonorrhea, chancroid, pneumonia, meningitis, urinary tract, lyme disease, URI
4th generation?
Gram negative bacilli
What is the thera use of Ceftriaxone and cefotaxins?
Emipiric therapy of adult meningitis and Late Lyme disease (arthritis, carditis, neurologic, and pediatric
which cephalapsorin is excreted in the bile?
ceftriaxone-much longer half life used to treat gonorhea
What are the adverse effects of cephalasporins?
hypersensitivity reaction less than with penicillin, DO NOT GIVE TO PEOPLE who have had ANAPHYLAXIS
Describe vancomycin?
mech of absorption
glycopeptide antibiotic (not a beta lactam)
binds d-alanyl-d-alanine of cell wall precursor, prevents peptidoglycan synthesis
Use of vancomycin?
How is resistance made to vancomycin?
Alteration of d-alanyl-d-alanine group in enterococci
What is the drug of choice for antibiotic associated colitis due to C. dificle?
Metronidazole, can use oral vancomycin
How is vancomycin given?
IV administration, can cause flushing, hypotension, skin rash, chills drug fever.
What is bacitracin?
Peptide antibiotic, inhibits incorporation of mucopeptides.
Use and antimicrobial activitiy?
Gram positive cocci and bacilli, topical treatment of superficial infections.
Absorbed and adverse effects of bacitracin?
poorly absorbed from mucous membranes, skin, or gut.
Renal Failure
Phosponic acid derivative, inhibits early step in cell wall synthesis
USE-enterococci, gram negative rods
What is thera use of fosfomycin?
Acute uncomplicated UTI, a SINGLE DOSE
Oral admin, and high concentrations in urine
Which drugs bind to the 30s ribosomal subunit?
tetracyclines, aminoglycosides
Which drugs bind to the 50s ribosomal subunit?
macrolides, ketolide, chloramphenicol, clindamycin
What is the mech of action of linezolid?
binds to 23s RNA of 50s ribosomal subunit, prevents formation of functional 70s complex for initiation of protein synthesis.
What does mupirocin do?
competes with isoleucine for binding to isoleucyl trna synshesis
Why aren't the aminglycoside antibiotics absorbed from the gut?
they are positively charged in body fluids, not absorbed from gut
What is the most widely used aminoglycosides?
ocular infections, pseudomonas aeruginosa
TB plague, tularemia
What is gentamycin used for?
aerobic gram negative bacilli
synergistic with cell wall inhibitors against gram positive cocci
What charge are the aminglycosides and how does this affect absorption?
Positive charge in fluid, no absorption in gut
What is gentamycin used for and how often is it used?
most used, AEROBIC GRAM NEGATIVE BACILLI -psuedomonas, e. coli, proteus, and serratia. GRAM POST COCCI-staph, strep, enterococci
What is thera use of aminoglycosides?
Why can't gentamycin be used for anaerobes?
requires oxygen to be taken up into cells
What are some other uses of gentamycin?
Enteroccol endocarditis and streptococcal endocarditis-penicillin or vancomycin with add of gentamycin
What is use of streptomycin?
TB, plague, and tularemia
What is pharmokinetic of aminoglycosides?
poor penetraion of csf, excreted unchanged by the kidneys, toxic in kidney failure
What is administration of aminoglycoside dosing?
Give every 8 hours, single dose may increase bacterial killing while reducing toxicity.
What are the adverse effects of aminoglycosides?
What is the spectrum of action of antimicrobial activity? Tetracyclines
broadspectrum, bacteriostatic activity, chlamydia, ricketssia, mycoplasma and erhlichia
What is the thera use of the tetracyclines?
rocky mountain spotted fever, cervicitis, PID, ATYPICAL PNEUMONIA, acne vulgaris, h. pylori, lyme disease, syphilis and bite wounds, brucellosis, cholera, ehrlichiosis
What is advantage of elimination of doxycycline?
eliminated by non-renal route, don't need to adjust in renal failure pooped out
What reduces bioavailability of tetracyclines?
Dairy products, antacids, iron reduce bioavailability-due to binding cations
What are adverse effects of tetracycline?
What are the macrolide antibiotics?
Eryhthromycin-azithromycin and clarithromycin are semi derivatives
What is the activity of the macrolide antibiotics?
strep, and pneumococci-mycoplasma, chlamydia, legionella, h. ducreyi
What drugs work against h. influenza and m. catarrhalis?
Azithromycin and 2nd gen cephalasporins
What treats c. diptheria and bordella pertussis?
What is the thera use of macrolides?
pharyngitis, sinusitis, bronchitis, otitis media, impetigo, community aquired pneumonia,
What is the singly dose treatment for chlamydia?
What treats peptic ulcer?
What is the diff in bioavailibilty of erythromycin and the semis?
Erythromycin-low and variable, higher and predictable
Azithromycin-longer half life and higher tissue levels
What are the drug interactions of the macrolide antibiotics?
erythromycin and clrithromycin inhibit p450 metabolism-increase theophylline, carbamazepine, warfarin, and lovastatin
what is up with ketolide (telithromycin)
Similar to the macrolides, binds to the 50s ribosomal subunit,
Less susceptible to bacterial export pumps
Ketone and methoxy groups make it more stable to stomach acid and increases ribosomal binding affinity
What is ketolide used for?
Active against community acquired resp pathogens, including MULTI DRUG RESISTANT STRAINS OF STREP, LEGIONELLA, AND CHLAMYDIA MAINLY RESP. PROBLEMS
What is unique about clindamycin?
it is a unique aminosugar antibiotic derived from lincomycin
What is clindamycin used for?
anaerobic infections, lung abcesses, sking and soft tissue inf, infections due to gram positive cocci and anaerobes
What do you use for necrotizing fascitis?
Penicillin and clindamycin
What are adverse effects of clindamycin?
incidence of diarhea and colitis-due to c. dificile
what is mech of action of quinupristin and dalfopristin?
binds to 50s subunit and prevents peptide degradation
What is quinupristin and dalfopristin used for?
How is quinupristin and dalfopristin given?
IV can get phlebitis from injection site
What is up with linezolid?
first member of the oxazolidinone group, no cross resistance, binds to 23s subunit on 50s subunit, prevents formation of 70s subunit
What is linezolid used for?
drug resistant staph and vancomycin resistant enterococci
What is bioavailable of linezolid and adverse effects?
100% oral bioavailability and thrombocytopenia
What is chorophenicol?
unique nitrobenzene activity, old drug used for meningitis
What is the therapeutic use of chloramphenicol?
INfections in which benefits outweigh risks-meningitis......VERY HIGH LEVELS IN CSF OF DRUG
What are the adverse affects of chloramphenicol/
aplastic anemia, reversible microcytic anemia
gray baby syndrome
What is mech of action of mupirocin?
Unique pseudomonal derivative, prevents formation of tRNA, gram pos cocci
How is mupirocin given?
Topical only
What is the thera use of mupirocin?
impetigo, nasal colinization of meth resistant staph, infected skin lesions. ADVERSE AFFECTS-SKIN irritation
What are the two antibacterial folate inhibitors?
sulfonamides and trimethroprim
What is the mech of action of the sulfonamides?
Inhibit bacterial foalte synthesis by blocking step that produces dihydrofolate
What is the mech of action of trimethoprim?
It inhibits bacteral folate reductase-works together with sulfonamides
What is the antimicrobial activity of sulfonamides and trimethropim?
E. coli, salmonella and shigella, nocardia, pneumocystis jiroveci, toxoplasma, staph aureus
What is the thera use of sulfonamides and trimethropim?
UTI, pneumonia (AIDS), Salmonella and shigella, burn wounds, ocular infections, meth resistant staph inf.
What is one of the major thera use of nocardia pneumonia?
immunocompromised, pulmonary abcess give TMP-SMX for 6-12 months-Norcardia pneumonia
Is there resistance to TMP-SMX
yes, in e. coli, can't give in some areas
What is the pharmokinetics of TMP-SMX?
Oral, parenteral, metabolized by acetylation, excreted in urine
What are the adverse affect sof sulfonamides and TMP?
GI irritation, jaundice, kernicterus, CRYSTALLURIA, sking rash, G6PD DEFICEINCY, macrocytic anemia
What drugs are in first gen. flouroquinolones?
Ciprofloxacin and ofloxacin-used for UTI, gonorrhea and anthrax
What drugs are in 2nd gen flouroquinolones?
Levofloxacin, gatifloxicin, moxifloxacin, gemifloxacin, Used for community acquired pneumonia
What is the mech of action of flouros?
Inhibit DNA topoisomerases Type 2 and type 4
How does DNA gyrase work?
introduces negative supercoils into double stranded bacterial DNA, eliminate the pos. supercoils that occur ahead of the DNA replication fork, produces supercoiling by breaking double stranded DNA, movings strands through the break and resealing the broken strands PRIMARY GRAM NEG.
Where do flouros bind?
the A subunit of DNA gyrase containing the active site and inhibit the reaction
What does type iv topomerase do?
resp. for separating daughter chromosomes after DNA replication, PRIMARY GRAM POS
What is the only use of norfloxacin?
What is the thera use of flourquinolones? (cipro and oflo)
UTI, gonorhea and chlamydia, travelers diarhea, shigellosis, typhoid fever, anthrax, ocular inf, bone and joint inf, and otitis externa
What is the use of levo, moxi, gatif, and gemi floxacin?
UTI, prostatitis, bronchitis and community acquired pneumonia
What are adverse affects of flouros?
arthropathy and tendonopathy-avoid in juveniles, CNS excitation
They inhibit caffeine and theophylline metabolism-can lead to seizures
What is nitrofurantion used for?
Active against E. coli, staph saprophyticus UTI, MACROCRYSTALLINE FORM CAUSES less GI UPSET.
What are side effects of nitrofurantion?
GI distress, neutropenia
What is polymoxin used for?
gram negative bacilli, can be given with bacitracin, used for skin and ocular infections
What is daptomycin?
new cyclic lipopeptide, disrupts bacterial plasma membrane, active against vanco and meth resistant staph and enterococci
What is daptomycin used for?
skin, soft tissue, diabetic foot ulcers and burn infections
What drugs are used for vanco and meth resistant staph and enterococci?
Daptomycin, linezolid, tigecycline, quinupristin-dalfopristin
What is the main use of rifamaxin?
travelers diarhea in people 12 and older
Who should rifazimin not be given to?
people with fever, blood in stools, or camp jejuni infection
What are the primary TB drugs?
Isoniazid, rifampin, pyrazinamide and ethambutol
How does isoniazide work?
activated by catalase perfoxidase and inhibits long chain fatty acid reductase involved in mycolic acid synthesis
What is cool about isoniazed distribution?
penetrates cells and lesions, absorbed from the gut
What is the toxic metabolite of isoniazid?
What is isoniazid used for?
TB, and m. kansasii
What cuases resistance to isoniazid?
mutations of katG gene
What are adverse affects of isoniazid?
Hepatitis, peripheral neuritis-due to a B6 deficiency
What is ethambutol used to treat?
TB, m. avium intracellular
When is ethambutol indicated?
resistance to other drugs
What are the adverse affects of ethambutol?
Optic neuritis-can't tell red from greeen
What is up with pyrazinamide?
adverse affects
metabolized to pyrazinocic acid by susceptibele mycobacteria-lowers ph to level at which organisms can no longer grow
given first two months of treatment
can cause hyperuricemia and gout due to competition of acid with uric acid excretion
What is the mech of action of rifampin?
inhibits RNA synthesis and causes decreased affinity of RNA polymerase
What is rifmpin used for?
most mycobacteria
STaph and Legionella
Prophylaxis of meningococcal and H. flu
When is rifampin used alone?
What are adverse affects of rifampin?
Hepatitis, hypersensitivity reactions, and discoloration of tears, saliva and urine
What does rifampin do to the p450 enzymes,
Induces them, causes decreased levels of HIV drugs, warfarin adn many others
What drugs are used to treat m. avian-intracellulare?
Rifabutin, azithromycin and clarithromycin ethambutol and ciprofloxacin
What is used in prophylaxis of M. avian intracellulare?
Azithro weekly or clarithromycin twice daily
What is used in treatment of m. avian intracellulare?
clarithromycin or azithromycin plue ethambutol and rifabutin----add cipro or amikacin if neede
What do you use for sever leprosy?
Sulfones like dapsone-inhibit folic acid synthesis, rifampin, clofazimine and thalidomide
What is mech of action of clofazimine
antibacterial, aniinflammatory and immunologic effects
What is clofazimine?
a synthetic phenazine dye, active against TB, leprae, and avium intracellular
It enhances phago activity of neurtrophils and macrophages
What is clofazimine used to treat?
It is used to treat erythema nodosum leprosum-a type 2 hypersensitivity reaction, characterized by tender erythematous skin nodules that occur with inflammation of subcutaneous fat and acute vasculitis
what is mech of action of thalidomide?
It stimulates t cells, particularyly CD8 subset,
it is an orphan drug for TB, leprosy and ENL
What is the adverse effect thalidomide?
may cause phocomelia -abnormalities of the limb,
Waht is the therapy for isoniazid resistant TB?
Isoniazid, rifampin, pyrazinamide and ethambutol for 6 months (UP TO NINE MONTHS FOR HIV POSITIVE)

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