Pharmacology Ii - Antimicrobial Drugs

Front 1

Name 5 groups of B-Lactams:

Back 1

1.Penicillin
2. Cephalosporin C – (Cephalosporium acremonium)
3. Cephamycin
4. Carbapenems - pseudo
5. Monobactams - pseudo

Front 2

TQ. What is the only second generation cephalosporin that can adequately penetrate into cerebrospinal fluid?

Back 2

cefuroxime

fur (for) ROX in the brain

Front 3

When combining bacterioSTATic agents you can expect what kind of effect?

Back 3

Additive effect

hint: ADD :: STATS

Front 4

Penicillinase-resistant penicillins (isOXazolyl penicillins) are most often used to treat/prevent what disease?

Back 4

Bovine staphylococcal mastitis
(can be given orally like Pen.V; unlike other Penicillins)

Front 5

What antibiotics have the action of interfering with the cell membrane?

Back 5

Polymyxin B
Colistin
(Bacitracin does not it interferes with cell wall)

Front 6

Beta lactams (penicillins and cephalosporins), bactracin, vancomycin, and cycloserine are all examples of which type of antimicrobials?

Back 6

interfere with cell wall synthesis

Front 7

What increases the half-life of sulfonamides?

Back 7

Low urine pH

Front 8

Which penicillin is excreted mainly by bile?

Back 8

Naficillin

Front 9

What cephalosporin excreted in bile?
How about the rest of them (most)?

Back 9

Ceftriaxone and cefoperazone are excreted mainly in bile, but most cephalosporins excreted by kidney and prox.tubular secretion
- end with -one
- C "own" bile
-TriA(nd)X Bile OPERA.zone
- Try One Operation Zone Bi LE

Front 10

When combining bactericidal agents you can expect what kind of effect?

Back 10

Synergistic effect

Drug synergy occurs when drugs can interact in ways that enhance or magnify one or more effects, or side-effects, of those drugs.
SIN:KILL
SYN:CIDE

Front 11

What is the major pathway of sulfonamide metabolism? Where?

Back 11

Acetylation in the liver and some in the lung

Front 12

What type of bacterial resistance develops slowly to sulfonamides?

Back 12

Chromosomal mediated resistance

Front 13

Which group of penicillins is more effective against gram-negative aerobic and anaerobic bacteria?

Back 13

Extended spectrum/anti-pseudomonal penicillins (carboxypenicillins)
(there are 5: C.MAT.P. )
~aren't natural penicillins decent against anarobes? but not pseudo.?

Front 14

Which bacteria's cell wall is not permeable to beta-lactam antibiotics?

Back 14

Gram negative bacteria

Front 15

What antibiotics were developed from the microorganism Bacillus? (2)

Back 15

Polypeptide antibiotics (polymyxin and bacitracin)

Front 16

Which animals are sensitive to procaine penicillin, producing anaphylaxis and CNS disorders?

Back 16

Guinea pigs
Chinchillas
Birds
Snakes
Turtles

Front 17

What antibiotics were developed from the microorganism Actinomycetes (Streptomyces)? (3 groups & 3 drugs)
>It is a Gram + bacteria.

Back 17

1. Tetracyclines
2. Aminoglycosoides
3. Macrolides
4. Chloramphenicol
5. Ivermectin
6. Rifamycin

Front 18

What antibiotics have the action of interfering with protein synthesis 30S ribosomal sub-unit?

Back 18

Tetracyclines
Aminoglycosides

Front 19

What antibiotics have the action of interfering with cell wall synthesis? (1 grp., 3 drugs)

Back 19

Beta lactams
Bacitracin
Vancomycin
Cycloserine

Front 20

What antibiotics have the action of interfering with the protein synthesis 50S ribosomal sub-unit?
(1 group, 2 drugs)

Back 20

Chloramphenicol
Macrolides
Lincomycin
(50s higher than 30 and macro means big)

Front 21

What antibiotics have the action of interfering with nucleic acids?
(1 grp., 2 drugs)

Back 21

Fluoroquinolones
Rifampin
Metronidazole
forget making RNA

Front 22

What antibiotics have the action of interfering with folate acid synthesis?

Back 22

Sulfonamides
Diaminopyrimidines

Front 23

Which antibiotics are classified as broad spectrum? (6 grps,)

Back 23

Tetracyclines
Chloramphenicol and derivatives
Macrolides and linomycins
Fluoroquinolones
Sulfonamides
TLC Fr M S

Front 24

Which antibiotics are classified as narrow spectrum?
(2grps, 3 drugs)

Back 24

Beta-lactams
Aminoglycosides
Polymyxin B and colistin
Rifampin
N-A-B-P-R
narrow antibiotics poor range

Front 25

What are the three ways that transfer of resistance genes between bacteria occur?

Back 25

Conjugation
Transduction
Transformation

Front 26

What are the four biochemical mechanisms of antimicrobial resistance?

Back 26

Antimicrobial inactivation
Alteration of drug-sensitive site or drug binding site
Decreased drug accumulation in the bacterium
Development of an alternate metabolic pathway

Front 27

Sulfonamides are structural analogs of what structure in bacterial organisms? Why important?

Back 27

PABA; competitvely inhibits enz. step in Folic Acid synth.

Front 28

What antimicrobials!! are inhibited by sulfonamides? What are not inhibited?

Back 28

Inhibits Gram+, Gram-, and protozoa
Does not inhibit obligate anaerobes

Front 29

What can sulfonamides be combined with to increase their spectrum of activity?

Back 29

Diaminopyrimidine

Front 30

Which sulfonamides are indicated for ophthalmic use?

Which cephalosp. are indicated for ophthalmic use?

Back 30

those with neutral or near neutral pHs (sulfacetamide)

note: cephalosporin suck penetrating vitreous humor

Front 31

What is the major pathway of sulfonamide metabolism?

Back 31

Acetylation in the liver and some in the LUNG

SULF -> LUNG

Front 32

Which animals are unable to acetylate sulfonamides?

Back 32

Dogs

Front 33

What are the two classifications of sulfonamide toxicity?
1+1
1+4

Back 33

Immunologic (keratoconjunctivitis sicca)
Non-immunologic (crystalluria, hypoprothrombinemia, aplasic anemia, and thrombocytopenia)

Front 34

What increases the half-life of sulfonamides?

Back 34

Low urine pH

sulfonamides = weak organic acid
pka = 4.7 (sulfizoxazole) to 10.4 (sulfanilamide)

Front 35

What breed of dogs reacts to sulfonamides with polyarthritis, fever, cutaneous eruptions, and hepatitis?

Back 35

Doberman Pinschers - hate sulfonamides

Front 36

What animals react to sulfonamides with hypoglycemia? (2)

Back 36

Ducks
Dogs

Front 37

What type of bacterial resistance develops slowly to sulfonamides?

Back 37

Chromosomal mediated resistance

Front 38

What type of bacterial resistance develops rapidly to sulfonamides?

Back 38

Plasmid mediated resistance

Front 39

What are the most commonly used diaminopyrimidines (combined w/sulfonamides) used in veterinary practice? (3)

Back 39

Ormetoprim
Pyrimethamine
Trimethoprim
(have 'prim' or 'pyrim')
Prim POT

Front 40

What class of drugs is a lipid-soluble organic base, bacteriostatic, reversibly binds and inhibits dihydrofolate reductase, and has a low affinity towards mammalian dihydrofolate reductase?

Back 40

Diaminopyrimidines

Front 41

Which diaminopyrimidines is not degraded in rumen and can be given orally to ruminants?

Back 41

Ormethoprim
OR = oral rumen

Front 42

How are diaminopyrimidines metabolized?

Back 42

Oxidation and conjugation in the liver

Front 43

Which class of drugs combines two bacteriostatic drugs to create a bactericidal drug?

Back 43

Potentiated Sulfonamides (Sulfonamides + Diaminopyrimidines)

Front 44

Which bacteria is not susceptible to potentiated sulfonamides?

Back 44

Pseudomonas aeruginosa

Front 45

How are potentiated sulfonamides metabolized?

Back 45

Sulfonamides acetylated and conjugated with glucoronic acid in the liver
Diaminopyrimidines are metabolized to oxide and hydroxylated metabolites in the liver

Front 46

Which drugs interfere with the transpeptidase enzyme by binding to a PBP leading to the formation of defective cell walls that are osmotically unstable?

Back 46

Beta-lactam antibiotics - interfer w/cell walls & bactericidal

Front 47

Penicillinase-resistant penicillins (isoxazolyl penicillins) are most often used to treat/prevent what disease?

Back 47

Bovine staphylococcal mastitis

Front 48

What drugs are considered broad-spectrum penicillins (Aminopenicillins)?

Back 48

Amoxicillin
Ampicillin

Front 49

What bacteria are susceptible to broad-spectrum penicillins (Aminopenicillins)?

Back 49

Those susceptible to natural penicillins (Active against Gram positive and Gram negative anaerobic?)
Enterobacteriaceae (E. coli, Proteus mirabilis, and Salmonella)
~e.g. Amoxicillin susceptible to B-lactamase?

Front 50

What drugs are considered extended spectrum/anti-pseudomonal penicillins (carboxypenicillins)? (5)

Back 50

Carbenicillin
Mezlocillin
Azlocillin
Ticarcillin
Piperacillin
C-MAT-P

Front 51

Which group of penicillins is more effective against gram-negative aerobic and anaerobic bacteria?

Back 51

Extended spectrum/anti-pseudomonal penicillins (carboxypenicillins)

Front 52

Which penicillin should NOT be be administered via IV, because it will affect the cardiac conduction system?

Back 52

Procaine penicillin G
(also tilmicosin)

PPT

Front 53

Which penicillin is a repository salt and absorption can be prolonged for 7 or more days? (give full name)

Back 53

Benzathine penicillin G

Front 54

Naficillin is what kind of antibiotic? What's unusual about it?

Back 54

it's a penicillin; excreted in bile

Front 55

What is used when animals to be treated do not exhibit signs of disease but are in close contact with diseased animals?

Back 55

metaphylactic

Front 56

What is used for treating a clinical disease?

Back 56

therapeutic

Front 57

What is used to prevent the disease when its occurrence can be predicted?

Back 57

prophylactic

Front 58

Polymyxin B and colistin are examples of what type of antimicrobials?

Back 58

antimicrobials interfering with cell membrane
-also i think they're bactericidal

Front 59

What has been reported in dogs and leghorn chickens receiving sulfaquinoxaline, which is due to the inhibition of vitamin K epoxide reductase?

Back 59

sulfaquinoxaline + (dogs,chickens) = hypoprothrombinemia

Front 60

Sulf. induced toxicity can be classified as ____, causing crystalluria, hypothrombinemia, aplastic anemia, and thrombocytopenia

Back 60

non-immunogenic <- crystalluria, hypothrombinemia, aplastic anemia, and thrombocytopenia

Front 61

diaminopyrimidines are metabolized to what (general chemical/product structure)? (2)

Back 61

oxide and hydroxylated metabolites

Front 62

What is the most common route of administration with penicillins?

Back 62

IM injection

Front 63

Isoxazolyl penicillins and V penicillin for administration via what route? Why?

Back 63

indicated for oral use because of good absorption (Isoxazolyl penicillins and V penicillin)

Front 64

How are penicillins classified?
1(+2 subgroups)
1
Admin?

Back 64

natural penicillin (G & V) and semi synthetic

G- please Give IM
V- victory Over (oral)

Front 65

How must penicillin G be administered?

Back 65

only parenteral administration

Front 66

Cephalosporins are well absorbed following what administration?

Back 66

IM or SC

Front 67

Are amoxicillin & ampicillin broad or extended spectrum penicillin?

Back 67

broad spectrum

Front 68

What is it called when DNA is acq. directly from environment and incorp. within genome thr. normal cross-over mechanism?

Back 68

transformation

Front 69

What inactivates chlorampehnicol?

Back 69

chloramphenicol acetyl transferase produced by gram positive and gram neg bacteria
(CAT anti-chlor)

Front 70

What causes decreased permeability through the cell membrane of gram negative organisms?

Back 70

ampicillin

Front 71

What drugs sensitive to bacterial resistance via energy dependent active efflux of drug (Impaired uptake of drug)?

efflux = mechanism responsible for extrusion of toxic substances and antibiotics outside the cell

Back 71

tetracyclines and fluoroquinolones

ET F.one

Front 72

How do bacteria synthesize their folic acid?

Back 72

using para-aminobenzoic acid

Front 73

What 2 classes of antimicrobial compounds can inhibit the synthesis of folic acid?

Back 73

sulfonamides and diaminopyrimidines

Front 74

causing depletion of the folic acid stores in bacterial cells abd are insoluble in water?

Back 74

sulfonamides

Front 75

Succinylsulfathiazole, <sulfasalazine>, sulfaquinoxaline, sulfaguanidine, and <<phtyalylsulfathiazole>> are examples of what? How unique?

Back 75

enteric sulfonamides (e.g. phtyalylsulfathiazole); these are only sulfonamides not well absorbed orally
~slowly abs. due to poor water solub.; exerts local action in GIT!

Front 76

What acts as topical anti-inflammatory by inhibiting prostaglandin synthesis and is used to treat rheumatoid arthritis in humans and colitis in dogs?

Back 76

5-aminosalicyclic acid (1 of 2 components of sulfasalazine, an enteric sulfonamide)

Front 77

What is hydrolyzed in the bowl by the bacteria into phtalic acid and sulfathiazole?

Back 77

phtyalylsulfathiazole

Front 78

Why must sulfonamide solutions be buffered for parenteral administration?

Back 78

prevent perivascular reactions fue to the alkalinity of most sulfonamides

Front 79

What are the 2 sulfonamides that can be used topically?

Back 79

silver sulfasiazine and mafenide

Front 80

What type of sulfonamides need to be used for opthalmic use?

Back 80

on neutral or near neutral pHs sulfonamides such as sulfacetamide

Front 81

Sulfonamide plasma protein binding is higher in cows or goats?
What drug is highly protein bound?

Back 81

15% (sulfanilamide in cows) to 90% (sulfadimethoxine in goats)
sulf-DIMEth

Front 82

T or F: Sulfonamides cross placenta barrier and get into CSF, synovial fluid

Back 82

TRUE

CSF -> CPR's
cephalosporins
potentiated sulfonamides
rifampin

Front 83

Why are acetylated sulf. metabolites a problem?

Back 83

less soluble than parent compound, therefore can accum. in kidney etc. = crystal formation

Front 84

What is the primary route of excretion of sulfonamides except enteric sulfonamide?

Back 84

renal excretion
except the enteric sulfonamides

Front 85

What urine pH favors tubular reabs. of sulfonamides thereby increasing half-life?

What other drug class affected by pH?

Back 85

low urine pH favors tubular reabs. of sulfonamides (weak acids) thereby increasing half-life

Macrolide, however, ineffective at low pH

Front 86

Long acting sulfonamides have low or high pka?

Back 86

not sure; but i think high pka, that way they are NOT ionized at low pH

Front 87

Why would you NOT want to use Sulfonamides for mastitis treatment?

Back 87

Sulfonamides may be distributed into milk (low concentrations); not for mastitis b/c don't want people drinking antibiotics

Front 88

What drug when given orally, ; treats colitis in dogs (as anti-imflam. by inhibiting prostaglandin synth.) and rheumatoid arthr. in humans?

Back 88

Sulfasalazine (enteric sulfonamide)

Front 89

Why Folic Acid important to microbes?

Back 89

used for RNA, DNA, protein synthesis? (can't synth. purines and some nucleotides w/o it)

Front 90

T or F: Although Sulfonamides primarily excreted via kidney (urine), also via tears, saliva, bile, milk, and sweat..to some extent.

Back 90

True

Front 91

Enteric sulfonamides are excreted how?

Back 91

via feces mostly, some metabolites may be reabs etc

Front 92

Sulfonamide induced toxicity can be classified as immunologic, such as what?

Back 92

keratoconjunctivitis sicca (KCS)

Front 93

Sulfonamide induced toxicity can be classified as non-immunologic, such as what?

Back 93

crystalluria, hypothrombinemia, aplastic anemia, and thrombocytopenia

Front 94

What can induce hepatic necrosis and chloestatic hepatitis in humans?

Back 94

trimethoprim-sulfadiazine and trimethoprim-sulfamethoxazole

Front 95

What is the consequence of precipitation of the sulfonamide in the glomerular filtrate of the kidney?

Back 95

crystalluria, hematuria, and renal tubular blockage

Front 96

How can aciduria be minimized?

Back 96

by keeping patient well hydrated during therapy and alkalinizing the urine
(high pH will favor elimination of Sulfonamide drug)

Front 97

What has been reported in dogs and leghorn chickens receiving sulfaquinoxaline, which is due to the inhibition of vitamin K epoxide reductase?

Back 97

hypoprothrombinemia; blood disorder in which a deficiency of prothrombin (Factor II) results in impaired blood clotting

Front 98

What can interfere with thyroid hormone synthesis?

Back 98

sulfonamides

Front 99

First generation cephalosporing have the highest activity of the cephalosporins against what?

Back 99

gram-positive bacteria

Front 100

Beta-lactamase enz. made by what bacteria?

Back 100

gram negative bacteria

BL + N = BNL

Front 101

Second generation cephalosporins are more effective than 1st generation in the treatment of what?

Back 101

infections caused by gram negative bacteria

Front 102

What cephalosporin drug is "new generation", has broader gram+ activity, active against beta-lactamase-producing strains as well as anerobes?

Back 102

ceftiofur

FUR ACTIVE

Front 103

Ceftiofur is indicated for the treatment of respiratory tract infections in ____ and ____, for urinary tract infections in ____, pleuritis and peritonitis in ____, and E. coli infections in ____.

Back 103

resp. tract in cattle and pigs, urinary in dogs, perit. in horses, and E.coli in poultry

Front 104

Most cephalosporins are excreted entirely by what?

Back 104

the kidneys by glomerular filtration and proximal tubular secretion
CPT

Front 105

Penicillin sensitive individuals are also sensitive to what?

Back 105

cephaloporins

Front 106

what beta-lactamase inhibitor acts as competitive inhibitor (preventing B-lactamase from bothering penicillin)?

Back 106

Clavulanic acid

Front 107

What are examples of penicillin G? 2+2

Back 107

sodium salt, potassium salt (benzathine, procaine)

Front 108

What form of penicillin G or ampicillin should be given when intravenous administration is indicated?

Back 108

Sodium salt

Front 109

What drug has higher bioavailibity in dog: amoxicillin or ampicillin?

Back 109

Amoxicillin

Front 110

What penicillin causes acute toxicity given IV and generally sux at life?

Back 110

Procaine

Front 111

What are examples of penicillin G?

Back 111

sodium salt, potassium salt (benzathine, procaine)

Front 112

2 CEPHLOSPORINS which have good oral absorption (most IM/SC):

Back 112

Cephalexin and cefaclor – high oral absorption

Front 113

What do these have in common?
2nd generation cephalosporin – cefuroxime
3rd generation of cephalosporin - ceftriaxone, cefotaxime, ceftazidime, ceftizoxime

Back 113

All cross BBB to CSF

notice all have x or z in them!

Front 114

Metabolism of cephalosporins?

Back 114

LIVER – to form deacetyl derivatives

Front 115

Deacetylated metabolite of _____– longer half-life than parent compound?

Back 115

CefoTAXIME (has metabolite with long HL)

~Death and taxes

Front 116

What cephalosporins have very ACTIVE METABOLITE?

What is it?

Back 116

Ceftiofur

Desfuroyl-ceftiofur

Front 117

Cefoperazone, cefamandole, moxalactam inhibits vitamin K dependent pathway for the synthesis of clotting factors, this leads to what?

Back 117

hypoprothrombinemia and coagulopathy

Front 118

What beta-lactamase inhibitor is a penicillanic acid sulfone, increases the activity of beta lactam antibiotic, and can only be administered IV?

Back 118

sulbactam

Sulb.IV (AMP SS)

Front 119

What are examples of sulbactam?

Back 119

sodium sulbactam and ampicillin

Front 120

What beta-lactam drug group is useful for serious infections, can be administered with cilastatin, and has broad spectrum action against Gram- aerobic and anaerobic bacteria?

Back 120

CARBAPENEMS - good against pseudomonas like monobactams

CARBoNO

Front 121

What B-lactam drug group have one ring, active against gram negative bacteria like Pseudomonas, stable against B-lactamase, and used in penicillin allergic patients?

Back 121

Monobactams (aztreonam)

stable against B-lactamase