PHARMA P3

chemotherapy

a branh of pharmacology dealing with drugs that selectively inhibit or destroy specific agents or diseases

chemotherapeutic agents

have selective toxicity, the porperty of a substance that makes it more harmful to certain living organisms while beingless harmful to others.

anti-microbial

a natural or synthetic drug that acts against one or more kinds of microorganisms

antibiotics

a substance produced by various species or microorganisms which inhibits the growth of another microorganism

sulfonamides

first antimicrobial agent

penicillin

first antibiotic discovered by Alexander Fleming in 1928

Minimum Inhibition Concentration

the lowest drug concentration that INHIBITS visible bacterial growth after 12-24 hours

Minimum Bacterial Concentration

the lowest drug concentration that sterilizes the medium or reduces the bacterial count by 99.9%

Post Antibiotic Effect

the continued suppression of bacterial growth even after the antibiotic levels drop below MIC

Breakpoint

the plasma concentration where an antibiotic may become toxic to the host.

Antibacterials

Also called Antibiotics. Drugs/compounds used to kill or inhibit growth of bacteria in cases of infection. Most agents are of bacterial origin

actinomycetes

where most antibacterial agents are derived from.

narrow spectrum

either gram positive or negative

broad spectrum

both gram positive or negative.

bactericidal

kills bacteria at MIC

bacteriostatic

inhibits bacterial growth

bacteriolytic

causes dissolution of bacterial cells.

Betalactams

inhibits cell wall synthesis by inhibiting transpeptidases, leading to cell lysis.

Penicillins

betalactam antibiotic that is effective against gram POSITIVE aerobes and anaerobes.
consists of a betalactam ring and a thiazolidine ring that is linked to an amide bond side chain

Penicillum notatum

where penicillin is derived from

Methicillin, oxacillin and cloxacillin

penicillinase resistant that used mainly for penicillinase- producing bacteria, less effective against other gram positive bacteria than Pen G

Penicillin G or Benzylpenicillin

used for gram positive, non- pencillinase producing infection and is the MOST POTENT for the pathogens

transpeptidases

essential for peptidoglycan cross linking which is the final step in cell wall synthesis

Penicillinase

a type of betalactamase and an enzyme produced by certain bacteria that breaksdown penicillin, rendering it inactive. Also common in methicillin- resistant staph aureus or MRSA

Aminopenicillin, Carboxypenicillin, Ureidopeniciilin

broad spectrum penicillin

TRUE

T/F : penicilliins are excreted unchanged by renal mechanism

aminopenicillin

Amox and Ampi: active against many gram negative

Amoxicillin

DOC for infections

Ampicillin

DOC for leptospirosis

LEPTOSPIREMIA because doxy is bacteriostatic and rapid bacterial clearance is needed

Carboxypenicillin

Carbencillin and Ticarcillin: specifically active against Pseudomonas. Can be combined with Tobramycin and Gentamicin

Ureidopenicillin

Piperacillin and Azlocillin: very broad spectrum of activity including Pseudomonas, Enterobacter and Klebsiella

Cephalosporins

Often used for antibiotic prophylaxis due to their tissue prnetration and are a primary alternative to penicillins for gram positive infections

Cephalosporium acremonium

where cephalosporins are derived from

Giuseppe Brotzu

Discovered cephalosporins

1st Generation Cephalosporins

used for prophylaxis and treating bone and soft tissue infections but are ineffective against anaerobes and susceptible to cephalosporinase from gram negative bacteria
FIRST ALTERNATIVE TO PENICILLINS

2nd Generation Cephalosporins

broader than the first gen, covering gram negative pathogens like klebsiella. proteus, providencia and enterobacter. However, enteroccoci, psuedomonas and actinobacteria are resistant
MORE RESISTANT TO BETALACTAMASE and effective against species resistant to 1st gen

NOT WIDELY USED IN VET MED

3rd Generation Cephalosporins

have extended spectrum against gram negative organisms, betalactamase resistant, ABLE TO PENETRATE BBB and are indicated in GRAM NEGATIVE MENINGITIS

Ceftriofur

3rd gen cephalosporins used in respiratory diseases in cattle, horses, sheep and swine and mastitis in cattile. Also used in UTI and soft tissue infections in dog and cats

4th Generation Cephalosporins

have increased activity against Pseudomonas and other bacteria resistant to cephalosporins

most cephalosporins are unstable in gastric acid and must be given PARENTERALLY

among the SAFEST antibiotics in use but prolonged use or high doses may cause hemopoietic effects

MAY CAUSE ANEMIA OR BONE MARROW DEPRESSION

Carbapenems

one of the widest pectrum antibiotics and is included in the LAST LINE antibiotics. Should only be considered as the LAST RESORT when other antimicrobial treatment options have been ruled out
oral administration isnt possible because of acid hydrolysis and poor absorption

Thiemamycin (Thienpenem)

a carbapenem which is the first representative of this drug class discovered in 1976

served as the PARENT COMPOUND of all carbapenems available for use today

VERY UNSTABLE

Imipenem

the first carbapenem that was developed and approved for HUMAN use

Monobactams

used as a reserve antibiotic in vetmed to treat severe gram negative infections

Streptomyces cattleya

where the majority of carbapenems come from

Chromobacterium violaceum

monobactams are derived from this

Aztreonam

used in humans as an alternative to amoniglycosides which are more toxic when combined with macrolides and lincosamides

Betalactamase Inhibitors

when added with penicillin, becomes potentiated penicillins

potentiated penicillins

betalactamase inhibitors + penicillin

used in small animals for extended spectrum and antibiotic actions

Clavulanic Acid

when combined with amox, becomes COAMOX

Has limited antibacterial activity but inhibits many betalactamase produced by penicillin resistant organisms

Sulbactam

a betalactalamse inhibitor that has similar actions with clauvulanic acid and is combined with ampicillin

Tazobactam

A betalactamse inhibitor that has similar action as sulbactam and is used in cobination with piperacillin or ceftolozane

Polymixins

binds to LPS molecules in the outer membrane of gram negative bacteria and alter the permeability of outer and inner membranes to K+ and Na+ ions leading to cell lysis

bactericidal and has a narrow pectrum activity against gram negative organisms but Proteus and Serratia are resistant

TX FOR E COLI AND SALMONELLA DIARRHEA

LOCAL TX FOR PSUDOMONAS INFECTIONS LIKE OTITIS EXTERNA AND SUPERFICIAL LIP INFECTIONS

Polymyxin B

a polymyxin that is derived from Paenibacillus polymyxa

Polymyxin E AKA Colistin

derrived from Paenibacillus polymyxa var colistinus

Aminoglycosides

Binds to the 30S ribosomal subunit, causing misreading of mRNA, impairing protein synthesis leading to cell death

Not absorbed from the GIT because of their high polar nature

ACCUMULATES IN THE RENAL CORTEX AND OTIC ENDOLYMPH which predisposes these tissued to their toxicity

Can cause NEUROMUSULAR BLOCKADE leading to muscle paralysis and apnea and is treated with CALCIUM GLUCONATE

30S Ribosomal subunit

reads the genetic instructions from the mRNA which contains the code for building proteins

Streptomyces, Micromonaspora and Bacillus species

Where Aminoglycosides are derived from

TRUE

T/F: aminoglycosides are relatively more nephrotoxic and ototoxic class of antibiotics

TRUE

T/F: the prolonged residues values in kidney severely limits the use of aminoglycosides in production animals to label use only

Streptomycin and Dihydrostreptomycin

Narrow spectrum aminoglycosides that are active against aerobic gram negative bacteria

Oldest members of this class

used for eliminating kidney carrier state of leptospirosis in swine, used concurrently with the MINOCYCLINE to treat brucellosis and is also used to treat TUBERCULOSIS

BOTH EXTREMELY OTOTOXIC TO CATS

Neomycin

A broad spectrum aminoglycoside which is used ORALLY for tx of enteric infections to suppress GI microflora and TOPICALLY for tx skin, ear and eye infections

Used pre-op for large bowel surgery

can cause MALABSORPTION syndrome or GI superinfection

Gentamicin

a broad spectrum aminoglycoside which is MOST ACTIVE and has the broadest spectrum in the class used in all species for tx SEPTICEMIA.

very nephrotoxic

mostly available in opthalmic and tic preps and for intra-uterine infusion in mares

Amikasin

used for gentamicin- resistant gram negative infections

also used as intra- uterine infusion for mares

Kanamycin

broad spectrum aminoglycoside that has similar gentamicin except it is not effective against pseudomonas spp

used in vetmed to treat bacterial enteritis and relieve diarrhea in dogs

Tobramycin

A broad spectrum aminoglycoside that has similar spectrum with gentamicin but MORE POTENT pseudomonal activity

Reduced toxicity compared to gentamicin and enhanced antibacterial activity compared to kanamycin. Available in combination with Dexa (TobraDex)

Tertacyclines

inhibits protein synthesis by binding to 30S ribosomal subunit, blocking amino acid addition and preventing bacterial growth

they are broad spectrum and can become bactericidal if bacterial membranes lose integrity

NOT RECOMMENDED FOR YOUNG ANIMALS AS IT CAUSES PERMANENT STAINING OF UNINTERRUPTED TEETH

Tetracyclines (oral)

should not be used with herbivores because of serious effects on ruminant digestion

Naturally Occuring Tetracyclines

mainly used as feed additives and growth promoters by reducing harmful gut bactera, leading to a healthier gut microbiota that improves nutrient absorption and digestion

OXYTETRACYCLINE and CHLORTETRACYCLINE are mainly used in large animals for treatment of local and systemic bacterial, chlamydial, rickettsial and protozoal infections

Semi-synthetic Tetracyclines

Useful in patients with renal impairment especially in cases of lepto and it can penentrate the BBB

Doxycycline

a semi- synthetic tetralcycline that is unique in that intestinal excretion is the major route of elimination (75%)

for leptospiruria because ampicillin does not penetrate the kidneys but it is mainly excreted there

Macrolides

inhibit protein synthesis by binding to the 50S ribosomal subunit, inhibiting the ribosome from moving along the mRNA, preventing the addition of NEW AMINO ACIDS into the peptide chain

BROAD SPECTRUM, BACTERIOSTATIC AND can become BACTERICIAL if bacterial membranes lose integrity

Tetracycline, Doxycycline and Minocycline

semi-synthetic tetracyclines that are mainly used in SMALL ANIMALS, respi and urinary tract infections in dogs and cats

used as specirfic therapy for BORRELIA (LYME DISEASE), Brucella, haemobartonella and ehrlichia infections.

also effective in the treatment of PSITTACOSIS in birds

Psittacosis or avian chlamydiosis

zoonotic disease caused by chlamydia psittaci

parrot fever in psittacine birds and ornithosis in other avian species

Streptomyces aureofasciens

Where tetracyclines are derived from

Streptomyces erythreus

where macrolides are derrived from

Lincosamides and Chloramphenicols

not recommended for combination therapy with macrolides due to same binding sites

50S Ribosomal subunit

helps link amino acids together to form proteins wich are essential for the bacteria to grow and function

erythromycin

a macrolide that is an ALTERANTIVE TO PENICILLIN for gram positive infections.

often used as tx for ENTERITIS caused by campylobacter jejuni in dogs and foals and for rhodococcus equi pneumonia in foals

tylosin

a macrolide that is used in dogs and cats for the treatment of CHRONIC COLITIS

also used in cattle, sheep and swine for the tx of local and systemic infections caused by mycoplasma and gram negative bacteria

USED PRIMARILY IN FOOD ANIMAL MEDICINE INCLUDING POULTRY AS FEED ADDITIVE

spiramycin

a macrolide that is the DOC for CRYPTOSPORIODOSIS but is less active than erythromycin

Tilmicosin

a macrolide that is used in cattle for the tx of respiratory disease caused by PASTEURELLA

has a potential fatal toxic effect in horses and humans

Azithromycin

a macrolide is used in dogs, cats, and horses and is effective against staph, strep and mycoplasma

used as an ALTERNATIVE TO ERYTHROMYCIN for R. equi pneumonia in foals

Tulathromycin

a macrolide that is effective against manheimia, mycoplasma and haeomophilus.

it is concentrated in the LEUKOCYTES and LUNG TISSUES

used for the treatment of bovine and swine respiratory disease

Clarithromycin

a macrolide used in dogs, cats and foals to treat mycobacterial infection like CANINE LEPROID GRANULOMA, FELINE LEPROSY, helicobacter spp and R equi infections

Lincosamides

inhibits protein synthesis by binding to 50S ribosomal subunits and blocking the formation of peptide bonds preventing the elongation of the growing peptide chain

BROAD SPECTRUM, BACTERIOSTATIC and can be BACTERICIAL if bacterial membrane lose integrity

Streptomyces lincolnensis

where lincosamides are derived from

Lincomycin

a lincosamide used in swine for the control and tx of SWINE DYSENTERY and the tx of staph, strep and mycoplasmal infection

CONTRAINDICATED in horses, rabbits, hamsters and guinea pigs beuse it may produce a severe, often fatal, diarrhea due to altered GI flora

pseudomembraneous colitis or antibiotic associated colitis

inflammation of the colon associated with an overgrowth of bacterium CLOSTRIDIOIDES DIFFICILE

Clindamycin

a lincosamide that has greter activity against anaerobes than lincomycin

used in dogs and cats to treat PERIODONTAL DISEASE, osteomyelitis, dermatitis and deep soft tissue infections caused by gram positive bacteria as well as toxoplasmosis and neosporosis in dogs

Fluoroquinolones

inhibits bacterial DNA gyrase and topoisomerase IV preventing the bacteria from properly copying their DNA leading to DNA damage and cell death

anaerobes tend to be resistant to this class

causes EROSION of ARTICULAR CARTILAGE in young dogs and foal particulary if they are used at high doses for longer than 14 days in rapid growth phase

RETINAL DEGENERATION has been reported due to acute and diffuse retinal damage in cats

DNA gyrase

enzymes that are only found in bacteria

marb

a fluoroquinolone that is used in the tx of dermal,respi and urinary tract infections INCLUDING PROSTATITIS in dogs, cats and birds and repsi infections cattle

ALTERANTIVE TO CLINDAMYCIN IN DCM (doxy, clinda, metro) therapy for canine babesiosis

has been reported to produce seizures in dogs on phenobarb for epilepsy

Danofloxacin

a fluoroquinolone that is used to treat BOVINE RESPIRATORY INFECTIONS including manheimia species

Ciprofloxacin

a fluoroquinolone most often used as OFF LABEL to treat UTI or skin infections in dogs and cats

Orbifloxacin and Marbofloxacin

a fluoroquinolone used for dermal, respi and urinary infection of dogs and cats

Orbifloxacin

ussed for susceptible gram negative infections in horses

Sulfonamides

inhibits the bacterial enzyme DIHYDROPTEROATE SYNTHASE which is involved in the synthesis of folic acid

folic acid

required for purinie and DNA synthesis and thus bacterial growth is inhibited

Sulfamethazine

a sulfonamide used in cattle, sheep and swine for the tx of respi infections and as GROWTH PROMOTER in swine

Sulfadimethoxine

a sulfonamide which is LONG ACTING and commonly used in all species for the tx of systemic and soft tissue infection and coccidiosis