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antimicrobials
drugs that kill or inhibit growth of microorganisms such as bacteria, protozoa, viruses, and fungi
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suffix 'cidal'
kills microorganism
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suffix 'static'
inhibits growth of microorganism
(basically starving the microorganism to death)
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antibiotics
antimicrobials produced by a microorganism
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antibacterials
synthetic, toxic to bacteria
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primary goal of antimicrobial therapy
kill microorganism without killing patient
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MIC
- Minimum Inhibitory Concentration
- lowest concentration at which growth of the bacterium is inhibited
(how susceptible is a bacterial strain?^)
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MIC low vs. high #
- low #-strong antibiotic
- high #-weak antibiotic
(ex:MIC for Penicillin may be higher than MIC for Amoxicillin. the MIC changes as time goes on and the bacteria become more and more resistant to the antibiotic)
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iatrogenically induced bacterial resistant practices
- antibiotics in feed over long periods (ex: Strongid T)
- failure to admin for appropriate period of time (never use antibiotics less than 5 days)
- failure to consider pharmacokinetics of drug (ex: renal infections, drug have to be admin for extended periods of time)
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ways antimicrobials kill bacteria
- cell wall- lyse wall&kill bacteria. effective only in growing bacteria
- cell membrane permeability-penetrates cell wall and membrane by bringing about death inside the cell once entered (but does not destroy cell wall)
- ribosomes-block protein synthesis by interfering with sequence of amino acids and thus protein development
- critical enzymes- drug attach to enzymes needed in the conversion of food&growth products thus starving to death (ex:bacteriostatic)
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most recent method of killing bacteria
- nucleic acids
- these drugs damage the nucleic acid production of a bacteria, preventing it from normal division
- these drugs usually take longer to work/kill
- ex: antiprotozoan/antifungal products
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Penicillin synthetic derivatives
- penVK
- ampicillin
- amoxicillin
- hetacillin
- cloxacillin
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how does Penicillin work?
- cell wall lysis
- effective against gram + bacteria (not beta-lactamase)
- procaine&benzathine- vehicles
- broad&narrow spectrum
- belongs to group B-Lactam Drugs
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vehicle
either intensify or lengthen effect of drug
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broad spectrum
kills gram+ and -
(narrow kills one or the other)
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B-Lactam drugs
act by disrupting bacterial cell wall synthesis
inclues penicillins, cephalosporins, etc.
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B-lactamase enzymes
most common mechanism of bacterial resistance to B-lactams is production of B-lactamase enzymes which damages the B-lactam ring of these compounds and renders them ineffective.
these organisms are classified as methicillin-resistant types and compromise a majority of nosocomial isolates from human&some animal hospitals
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nosocomial infection
infections inside an otherwise sterile area
(infection at hospital)
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increases bacteria's resistance by converting penicillin to inactive penicillic acid
beta-lactamase (penicillinase)
beta-lactamase-resistant/penicillinase resistant penicillins: some penicillins are more resistant to beta-lactamase-hydrolysis
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penicillins are usually very effective against
gram-positive bacteria
but gram-negative bacteria have an outer membrane around the cell wall that limits permeability (ex: methicillin, cloxacillin, dicloxacillin, oxacillin)
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narrow spectrum penicillins (common gram positives)
- Penicillin G sodium
- Penicillin G potassium
- Penicillin G procaine
- Penicillin G benzathine
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narrow spectrum acid-resistant penicillins
Penicillin V
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beta-lactamase resistant penicillins
- Methicillin
- Cloxacillin
- Dicloxacillin
- Oxacillin
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broad spectrum penicillins
- Ampicillin
- Hetacillin
- Amoxicillin
- Carbenicillin
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potentiated penicillins
Amoxicillin
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antagonists for narrow spectrum penicillins (Penicillin G sodium,potassium,procaine,benzathine)
tetracyclines & chloramphenicol
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antagonists for penicillin V
tetracylines & chloramphenicol
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antagonists for beta-lactamase resistant penicillins
methicillin, cloxacillin, dicloxacillin- tetracyclines& chloramphenicol
oxacillin- sulfonamides
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antagonist of ampicillin and hetacillin
chloramphenicol, erythromycin, tetracyclines, cephalosporins
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antagonist of amoxicillin
chloramphenicol, erythromycin, tetracyclines, cephalosporins
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antagonist of carbenicillin
chloramphenicol, erythromycin, tetracyclines, cephalosporins
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most of absorption of penicillins takes place in stomach&upper small intestines, therefore, immediate allergic reactions can be treated with
anti-emetics like apomorphine or syrup of ipeca
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primary organ for excretion
kidney
therefore, kidneys BUN and Creatinine must be checked in geriatric animals
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why must withdrawal times be computed when treating mastitis in dairy animals?
Penicillins are excreted through the milk in small amounts
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more specific name for mastitis
Staphlococcus agalactiae
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this should be ready to admin at all times for sensitivity reactions (hives, respiratory distress) to penicillin or procaine
Epinephrine 1:10,000 IV
comes 1,000 mg per mL--reconstitute to 1 mL of epi per 10 mL water (will kill by IV if not)
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is Penicillin G long or short acting?
long acting (48-72 hrs)
not normally approved for use in dairy animals
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dosage forms for penicillin
- polyflex (ampicillin injection)
- penicillin G procaine or benzithine injection
- ambi-pen injection
- amoxi-tabs&clavamox tabs for dogs&cats
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Cephalosporins
- ceph/cef prefix
- similar to penicillins
- bacteriocidal
- susceptible to beta-lactam
- broad spectrum, more effective against gram+ bacteria
- classified by generations
higher the generation=more gram neg. effectiveness
- major risk- allergy to penicillin also allergic
- minor risk- nephrotoxic
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first generation cephalosporin
Cephalexin (Keflex)
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second generation cephalosporin
Cefaclor (Ceclor)
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third generation cephalosporin
Cefixime (Suprax)
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antipseudomonal third generation cephalosporin
Ceftazidime (Fortaz)
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fourth generation cephalosporin
Cefepime (Maxipime)
*IV only*
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only antagonist for cephalosporins
any product containing gentamicin
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what should never be given with penicillin?
tetracycline
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dosage forms for cephalosporin
- cefa-drops
- cefa-tabs
- cefa-lak (mastitis treatment)
- naxcel powder for injection
- excenel injectable suspension
adverse side effects: nausea, vomiting, diarrhea, lethargy
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name some gram-neg bacterias
- proteus
- pseudomonas (most resistant-use polymyxin B, Gentamicin)
- pastuerella
- klebsiella
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effective against the very resistant, gram negative bacteria, pseudomonas
Polymyxin B
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Bacitracin
- antimicrobial effective against gram+ bacteria
- topical--dissolves well into dermis
- often combined with other antibiotics for broad spectrum effect (ex: triple antibiotic ointment contains bacitracin, polymyxin B, neomycin)OTC
bacteriostatic unlike penicillin&cephalosporin
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Aminoglycosides
- developed from gram neg bacteria
- broad spectrum
- bacteriocidal
- includes: gentamicin, amikacin, neomycin, streptomycin, dihydrostrep, apramycin, kanamycin, tobramycin
- nephrotoxic&ototoxic in felines
- to prevent nephrotoxicity in animals other than feline, IV fluids must be admin simultaneously
- combine with ribosomes interfering with amino acid sequence
- be careful with--very toxic!
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Oxacillin antagonist
sulfonamides
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amoxicillin antagonist
- erythromycin
- tetracycline
- cephalosporins
- chloramphenicol
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why are aminoglycosides administered parenterally (except neomycin)?
because they are not readily absorbed through GI tract
neomycin administered orally bc it is not absorbed at all. thus, can be accurately administered by weight for infections of GI tract&be assured that 0% is lost in the tissues surrounding the tract (ex: Neo-pectalin--oral absorbant)
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Tetracyclines
- bacteriostatic
- one of oldest antibiotics
- binds to ribosomes disturbing amino acid
- first antibiotic broad spectrum (gram+&-, as well as mycoplasmas, spirochetes, chlamydia)
- precautions: chelates with minerals of developing tooth enamel&bones imparting a yellow discoloration, use cautiously with impaired liver function
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adverse side effects of tetracyclines
- permanent staining of teeth if received in utero or as juvenile
- drug is also deposited in growing bones, slowing their development
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absorption of tetracyclines by GI tract is dramatically decreased by
presence of food, milk products, antacids
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list tetracyclines
- Oxytetracycline
- Chlortetracycline
- Doxycycline
- Minocycline
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antagonist of Oxytetracycline
diuretics, antacids, milk, penicillins (DAMP)
(shock&diarrhea can occur if given IV in horses)
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antagonist of Chloretetracycline
diuretics, antacids, milk, penicillins (DAMP)
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antagonist of Doxycycline
- diuretics, antacids, milk, penicillins (DAMP)
- same as barbituates
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antagonist of Minocycline
diuretics, antacids, milk, penicillins (DAMP)
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Chloramphenicol
- bacteriostatic in low doses
- bacteriocidal in high doses (unique)
penetrates CNS (blood-brain barrier), prostate gland, globe of eye, etc due to the fact that in high doses it exceeds the MIC
- precautions: anorexia in cats
- banned in food animals
- gray babies in humans
- vehicle with barbituates
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adverse side effects of Chloramphenicol
blood dyscrasias in cats after prolonged treatment
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antagonists of chloramphenicol
- penicillin
- streptomycin
- cephalosporins
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synergistic with sulfur
chloramphenicol
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what type of bacteria are lincosamides effective against?
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clindamycin is especially noted for use in
dentals (ex: Antarobe)
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primary macrolides
- Erythromycin
- Tylosin (Tylan)
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how do macrolides work?
- binds to ribosomes with no aa sequencing
- will penetrate many tissues but not CNS
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drug of choice for prostate infections
Erythromycin
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very first anti-infective drug used in both human and veterinary medicine
sulfanomides
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how do sulfonamides work
interfere with formation of folic acid, so effective against bacteria that form their own folic acid
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sulfonamides effective against
- gram-positive
- gram-negative
- coccidia
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do sulfonamides penetrate CNS?
yes
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what must you make sure of if using sulfonamides?
animal has ample amounts of water bc will precipitate out in kidneys and cause dryness of cornea and keratoconjunctivitis
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"BIG BOYS"
Fluoroquinolones
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how do flouroquinolones kill bacteria(work/action of)?
damage nucleic acid production of bacteria preventing bacterium from normal division
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most popular type of antibiotics in outpatient clinic
Fluoroquinolones
(especially in gram-positive rods in dogs,cats,fowl,cattle--not horse)
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examples of fluoroquinolones
- Enrofloxacin (Baytril)
- Orbifloxacin (Orabax)
- Ciprofloxacin (Cipro)-for anthrax ppl only
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fluoroquinolones effective against
- gram-positive
- gram-negative
- pseudomonias (gn)
- aeromonas
- beta-lactam bacteria
(good broad spectrum)
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used for a lot for middle ear infections
fluoroquinolones
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non-proprietary name for Baytril
enrofloxacin
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fluoroquinolones commonly used today
- ciprofloxacin
- enrofloxacin
- difloxacin hydrochloride
- orbifloxacin
- sarafloxacin
- marbofloxacin
- norfloxacin
- pradofloxacin
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non-proprietary name for Cipro
ciprofloxain
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non-proprietary name for Dicural
difloxacin
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non-proprietary name for Zeniquin/Marbocyl
Marbofloxacin
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non-proprietary name for Noroxin
norfloxacin
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non-proprietary name for Veraflox
pradofloxacin
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fluoroquinolone oral suspension for cats only
Veraflox (pradofloxacin)
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adverse side effect of quinolones
formation of lesions in joint articular cartilage during rapid growth phase of dogs
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#1 antibiotic prescribed for cats
Metronidazole
(commonly prescribed with corticosteroids for IBD and periodontal disease)
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"Flagyl" in human medicine
Metronidazole
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Metronidazole is
an antibacterial/antiprotozoal agent commonly used to treat protozoal infections and anaerobic bacterial infections. also has marked antiinflammatory effect on bowel.
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two types of fungal infections
- topical (superficial)- affecting skin and mm
- systemic- affecting blood, lungs, or CNS
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non-proprietary name for Fungizone
Amphotericin B
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Amphotericin B
- antifungal drug
- fungistatic or fungicidal
- mixed with D5W to decrease nephrotoxicity
- IV
- breaks down membrane wall for early death
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Ketoconazole&Miconazole
- used for yeast to systemic funguses
- can effect testosterone production in male
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Miconazole Nitrate
topical application to treat dermatophytes and yeast
- low dose-fungistatic
- high-cidal
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Sulconazole Nitrate
- "Exelderm"
- better than miconazole
- effective topically against ringworm (Microsporum canis)
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Nystatin
- oral&topical
- most commonly used for Candidas albicans infections of the skin
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Griseofulvin
- oral
- antifungal effective against dermatophytes
- easily absorbed in skin/nails especially with oils/fats in diet
- should never be given to pregnant-monsters and cleft palates can result
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antiviral drugs
more of "immuno stimulants"
include: amantadine, ganciclovir, idoxuridine, azidothymidine
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