CH 14

Fundamentals of Pharmacology for Veterinary Technicians Chapter 14
Lysosome
Ribosomes
Cytoplasm
Centrioles
A Golgi apparatus Chromosomes Rough endoplasmic reticulum
Nucleus
Nucleolus
Cell wall
Smooth endoplasmic
reticulum
Mitochondria
Cell or plasma
membrane
Vacuole
Figure 14-1A
Copyright 2011 Delmar, Cengage Learning
Figure 14-1B
Ribosomes
Pilus
Flagellum
Plasmid (DNA) Cytoplasm
Cell membrane
Cell wall
Capsule
Nucleoid (DNA)
B
Figure 14-2
Step Procedure ResuIt
1
2
3
4
Primary stain: Apply crystal
violet stain (purple)
Mordant: Apply Gram's iodine
Rinse slide
Decolorize: Apply acid-alcohol or acetone
Counterstain: Apply safranin
stain (red)
Rinse slide
Rinse slide
Rinse slide
All bacteria stain purple
All bacteria remain purple
Purple stain is removed from
gram-negative cells
Gram-negative cells appear
pink-red; gram-positive cells
appear purple
Figure 14-3
Figure 14-4
0.1 0.5 1.0
+g of antibiotic per mL of broth
5.0 10.0
Figure 14-5
Blocking the use
of needed nutrients
Ribosomes
Protein synthesis
inhibition
Pilus
Flagellum
Cell membrane
Cell membrane
disruption
Cell wall
Cell wall
disruption
Capsule
Nucleoid (DNA)
Nucleic acid
synthesis alteration
Figure 14-6
Cephalosporins
N
R
2
-N
R
1
COOH
S
C C
N
O
`-Lactam
C C
C
O
C
Penicillins
N
N
CH
3
CH
3
R
COOH
S
C C
O
C
Figure 14-7
Blocking the use
of needed nutrients
Ribosomes
Sulfonamides
Protein synthesis
inhibition
Aminoglycosides
Tetracyclines
Macrolides
Chloramphenicol
Florfenicol
Lincosamides
Aminocoumarins
Diterpines
Pilus
Flagellum
Cell membrane
Polymyxin B
Cell membrane
disruption
Nitrofurans
Nitroimidazoles
Rifampin
Miscellaneous
Cell wall
Cell wall
disruption
Penicillins
Cephalosporins
Bacitracin
Vancomycin
Carbapenems
Monobactams
Capsule or slime layer
Nucleoid (DNA)
Nucleic acid
synthesis alteration
Fluoroquinolones
Figure 14-8
Figure 14-9A
Figure 14-9B
Figure 14-10
Lysosome
Ribosomes
Cytoplasm
Centrioles
A Golgi apparatus Chromosomes Rough endoplasmic reticulum
Nucleus
Nucleolus
Cell wall
Smooth endoplasmic
reticulum
Mitochondria
flucytosine
NucIeic acid synthesis
aIteration
griseofulvin
CeII division
aIteration
Cell or plasma
membrane
Polyenes
(nystatin,
amphotericine)
Imidazoles
(ketoconazole,
miconazole,
itraconazole,
fluconazole,
voricanazole)
Allylamine
(terbinafine)
CeII membrane
disruption
Vacuole
Figure 14-11
Virus
RNA or DNA
Entry
Uncoating
Nucleic acid synthesis
(viral enzyme directed)
Interferes with
nucIeic acid synthesis
acyclovir
Eukaryotic
host cell
Viral particle
production
Exit
Figure 14-12A
Figure 14-12B
Figure 14-13A
Figure 14-13B
Figure 14-14
CI
CI OH
hexachlorophene
B)
C)
D) E)
F)
G)
H)
A)
phenol ortho-phenylphenol
Chemical structure of select disinfectants
PhenoIs and phenoIics
CI CI
HO
CH
3
CH
3
benzalkonium chloride
CH
2
O
formaldehyde
ethylene oxide
glutaraldehyde
Quaternary ammonium compounds
CH
2
N
+
Long hydrocarbon chain
AIdehydes
EthyIene oxide AIcohoIs
HaIogens
Na
+
[OCI]
-
sodium hypochlorite povidone iodine
HC
O
O
N I
2
O CH CH O
O
CH
2
CH
2
CH
3
CH
2
OH
ethyl alcohol
isopropyl alcohol
CH
3
CH
3
CH OH
CH
2
CH
2
CH
2
CI
CI HO OH
CI
H
3
C O
O
O H
O H
H O
CI NHCNHCNH(CH
2
)
6
NHCNHCNH
NH NH NH NH
Biguanide
Oxidizing agents
peracetic acid hydrogen peroxide
chlorhexidine
C
H
H
Table 14-1
Table 14-1 Mechanisms of Action of Antibiotic Drugs
s e l p m a x E g u r D t c e f f E n o i t c A
Inhibition of cell wall
synthesis
Bactericidal effect by inhibition of an enzyme penicillins, cephalosporins, bacitracin,
vancomycin, carbapenems, monobactams,
aminocoumarins
Alteration in cell membrane
permeability
Bacteriostatic or bactericidal effect; as the
membrane permeability is increased, the loss
of cellular substances causes cell lysis
polymyxin B
Inhibition of protein
interference
Bacteriostatic or bactericidal effects due to
interference with bacterial protein synthesis,
but not animal cell protein synthesis or
inhibition of the steps of protein synthesis
aminoglycosides, tetracyclines,
chloramphenicol, orfenicol, macrolides,
lincomycins, aminocoumarins, diterpines
Interference with metabolism Bacteriostatic effects due to the deprivation of
essential material for bacterial metabolism
sulfonamides
Nucleic acid impairment Bactericidal effects due to inhibition of nucleic
acid enzymes
quinolones, uoroquinolones
Table 14-2
Table 14-2 Classes of Antibiotics and Their Effectiveness
Class of
Antibiotic
Action of
Antibiotic
Considerations Examples
penicillins Inhibit cell wall synthesis
Bactericidal
Mainly work on gram+
bacteria; some gram with
amoxicillin, ampicillin,
ticarcillin, and carbenicillin
Carbenicillin, ticarcillin, and
piperacillin are effective
against Pseudomonas
bacteria
Oral and injectable forms
Given orally, most
absorption occurs in
stomach and small intestine
Rapidly distributed
Give 12 hours before
eating
penicillin V (V-Cillin K
), penicillin G
procaine (Crystacillin
), penicillin G
benzathine with penicillin G procaine
(Dual Pen
)
amoxicillin (Amoxi-tabs
, Amoxi-drops
,
Biomox
, Robamox-V
)
ampicillin (Polyex
, Omnipen
)
ampicillin with sulbactam (Unasyn
)
amoxicillin with clavulinic acid
(Clavamox
)
ticarcillin (Ticar
)
carbenicillin (Pyopen
, Geocillin
)
cloxacillin (Dari-Clox
, Orbenin-DC
)
dicloxicillin (Dynapen
, Pathocil
)
oxacillin (Add-Vantage
)
piperacillin (Pipracil
)
piperacillin with tazobactam (Zosyn
)
ticarcillin with clavulanate (Timentin
)
hetacillin (Hetacin-K
)
nafcillin (Nafcil
)
cephalosporins Inhibit cell wall synthesis
Bactericidal
First generation mainly
work on gram+ bacteria,
second through fourth
generation work on gram+
and gram bacteria with
fourth generation having
the broadest spectrum
(including Pseudomonas)
Can cross placenta
GI absorption not good;
usually administered
parenterally
Well distributed to tissues,
except CNS
Vomiting and diarrhea may
occur when given on empty
stomach
If animal is allergic to
penicillin, it may be allergic
to cephalosporin
First generation: cephapirin (Cefa-Dri
,
Cefa-lak
), cefadroxil (Cefa-drops
, Cefa-
tabs
), cefazolin (Kefzol
), cephalexin
(Keex
)
Second generation: cefoxitin (Mefoxin
),
cefaclor (Ceclor
), cefotetan (Cefotan
),
cefuroxime (Ceftin
)
Third generation: ceftiofur (Naxcel
,
Spectramast
, Excenel
), cefovecin
(Convenia
), cefoperazone (Cefobid
),
cefotaxine (Claforan
), cefpodoxine
(Simplicef
), ceftriaxone (Rocephin
)
Fourth generation: cefepime
(Maxipime
)
polypeptides Inhibit either cell wall or
cell membrane synthesis
Bactericidal
Absorption is poor; used for
topical infections or wound
lavage
polymyxcin B (found in Optiprime

ophthalmic ointment)
bacitracin (found in Mycitracin
and
Trioptic
ophthalmic ointment)
glycopeptides Inhibit cell wall synthesis
Bactericidal
Treats drug-resistant
Staphylococcus spp
Injectable form used in
veterinary medicine
vancomycin (Vancocin
)
(Continued )
Table 14-2 continued
Class of
Antibiotic
Action of
Antibiotic
carbapenems Inhibit cell wall synthesis
Bactericidal
Injectable form only
Broadest spectrum
beta-lactam antibiotic
Used to treat resistant
bacteria
imipenem-cilastatin (Primaxin
)
meropenem (Merrem
)
monobactams Inhibit cell wall synthesis
Bactericidal
Injectable form only
Gram-negative spectrum of
activity
aztreonam (Azactam
)
aminoglycosides Inhibit protein
synthesis[en]
Bactericidal (concentration
dependent)
Work mainly on gram
bacteria
Can cross placenta
Injectable form only (except
neomycin which is topical)
Not absorbed readily from
GI tract; usually given
parenterally
Nephrotoxicity and
ototoxicity concerns
Do not mix with penicillin
in the same syringe (makes
penicillin inactive)
gentamicin (Gentocin
, Garacin
)
neomycin (Biosol
, Mycifradin
)
amikacin (Amiglyde-V
, Amikin
)
tobramycin (Nebcin
)
dihydrostreptomycin (Ethamycin
)
spectinomycin (Adspec
, Spectam
)
tetracyclines Inhibit protein synthesis
Bacteriostatic
Work on gram+ and
gram bacteria, as well
as rickettsial bacteria,
spirochetes, and some
protozoa
Once given, quickly
distributed, sometimes to
CNS
Very little metabolism
Bind to calcium, causing
side effects (do not give
with dairy products or
antacids/antidiarrheal drugs)
Can cause yellow
discoloration of teeth due to
calcium binding
tetracycline (Panmycin Aquadrops
,
Oxy-Tet 100
injectable, Tetracycline
HCl
soluble powder)
oxytetracycline (Terramycin
,
Liquamycin
)
chlortetracycline (Aureomycin
)
doxycycline (Vibramycin
, Doxirobe
Gel)
minocycline (Minocin
)
demeclocycline (Declomycin
)
chloramphenicol Inhibits protein synthesis
Bacteriostatic
Works on gram+ and
gram bacteria as well as
rickettsial bacteria
Oral, injectable, and
ointment forms
Readily absorbed into tissues
Side effect of bone marrow
suppression makes use not
recommended
chloramphenicol (Chloromycetin
,
Viceton
, Amphicol
)
orfenicol Inhibits protein synthesis
Bacteriostatic
Injectable form
Well distributed in body; can
achieve therapeutic levels in
the CNS
orfenicol (Nuor
)
macrolides Inhibit protein synthesis
Bactericidal or
bacteriostatic
Well distributed to most
body tissues, but not the
CNS
tilmicosin (Micotil
)
tylosin (Tylan
)
erythromycin (Erythro-100
,
Erythro-Dry
)
azithromycin (Zithromax
)
tulathromycin (Draxxin
)
(Continued )
Table 14-2 (Continued )
Class of
Antibiotic
Action of
Antibiotic
lincosamides Inhibit protein synthesis
Bactericidal or
bacteriostatic
Recommended for
abscesses and dental
infections
clindamycin (Antirobe
)
pirlimycin (Pirsue
)
lincomycin (Lincocin
)
aminocoumarins Inhibit protein and nucleic
acid synthesis; also
interferes with cell wall
synthesis
Bactericidal
Works mainly on
gram+ bacteria
Used as a combination
product in dogs
Used as a mastitis
treatment in dry dairy cattle
novobiocin/tetracycline/prednisolone
(Delta Albaplex
)
novobiocin/penicillin G procaine (Albadry
Plus
)
novobiocin (Biodry
)
diterpines Inhibit protein synthesis
Bacteriostatic
Works on gram+ cocci
and limited gram
bacteria
Premix, solution, and
powder formulations
Used to treat pneumonia in
swine
tiamulin (Denagard
)
sulfonamides Inhibit folic acid synthesis
Sulfonamides are
bacteriostatic
Trimethoprim and ormetro-
prim are bactericidal and
used to potentiate sulfas
Potentiated sulfas are
bactericidal
Can have anti-inammatory
effects
Well distributed through the
body, including eye and CNS
and synovial uid
Can cause increased
salivation in cats
sulfadiazine/trimethoprim (Tribrissen
)
sulfadimethoxine (Albon
)
sulfadimethoxine/ormetroprim (Primor
)
sulfasalazine (Azuldine
)
sulfamethoxazole with trimethoprim
(Bactrim
)
uoroquinolones Inhibit DNA function
Bactericidal
Readily absorbed into
tissues and body uids
after oral and parenteral
administration
enrooxacin (Baytril
)
orbioxacin (Orbax
)
dioxacin (Dicural
)
marbooxacin (Zeniquin
)
saraoxacin (SaraFlox
)
ciprooxacin (Cipro
)
danooxacin (Advocin
)
nitrofurans Inhibit bacterial enzyme
systems
Bactericidal
Eliminated from body
quickly; usually used in
urinary tract infections
Banned for use in food-
producing animals
nitrofurazone (Furazone
, NFZ Puffer
)
nitrofurantoin (Macrodantin
)
furazolidone (Topazon
, Furox
)
nitroimidazoles Disrupt DNA and nucleic
acid synthesis
Bactericidal
Well absorbed after oral
administration
Use with caution in
pregnant animals
metronidazole (Flagyl
)
rifampin Disrupts RNA synthesis
Bactericidal or
bacterioistatic depending
on dose
Relatively well absorbed
from GI tract
Can cause red urine, tears,
sweat, and saliva
Usually used in combination
with other antibiotics
rifampin (Rifadin
, Rimactane
)
Table 14-3
Table 14-3 Classes of Antifungals and Their Effectiveness
Class Mechanism of
Action
polyenes Bind to fungal cell membrane Not well absorbed; fairly toxic amphotericin B (Fungizone
)
nystatin (Panalog
)
imidazoles Cause leakage of fungal cell
membrane
Less toxic; used for systemic
mycotic infections and some
dermatophyte infections
ketoconazole (Nizoral
)
miconazole (Monistat,
Conote
)
itraconazole (Sporanox
)
uconazole (Diucan
)
voriconazole (Vfend
)
antimetabolics Interfere with RNA and
protein synthesis
Used mainly in combination
with other antifungals to treat
Cryptococcus infections
ucytosine (Ancobon
)
supercials Disrupt fungal cell division Used for dermatophyte
infections
griseofulvin (Fulvicin-U/F
, Grifulvin V
)
terbinane (Lamasil
)
Table 14-4
Table 14-4 Types of Disinfectants and Antiseptics
Disinfectant
Group
Product
Examples
Use Action Comments
phenols and
phenolics
ortho-phenylphenol
(Lysol
, Amphyl
,
Tek-Trol
, 1 Stroke
Environ
)
hexachlorophene
(Phisohex
)
Laundry,
oors, walls,
equipment
Moderately
bactericidal,
virucidal, and
fungicidal
Action not affected by organic
material
Used as a 25% solution on
contaminated objects
quaternary
ammonium
compounds
didecyl dimethyl
ammonium chloride
(Roccal
-D)
benzalkonium chloride
(Zephiran
)
Instruments,
rubber,
inanimate
objects
Moderately
bactericidal,
virucidal, and
fungicidal
Action not affected by hard water
(Continued )
Disinfectant
Group
Product
Examples
Use Action Comments
aldehydes gluteraldehyde
(Cidex
, Glutarol
)
Instruments Highly bactericidal,
virucidal, and
fungicidal
material or hard water
ortho-phthalaldehyde
(Cidex-OPA
)
Instruments Highly bactericidal,
virucidal,
tuberculocidal
All items processed with aldehydes
need to be rinsed with water prior
to use
formaldehyde Tissue biopsies
and footbaths
Highly bactericidal,
virucidal,
tuberculocidal
Use in areas of good ventilation
Avoid skin and eye contact and
inhalation of vapors
alcohols 70% isopropyl Instruments Highly bactericidal,
some virucidal
action, and
action
70% solution usually used
s r e t e m o m r e h T l o h o c l a l y h t e % 0 5 Affected by organic material and
dirt
halogens chlorines: (Chlorox
) Chlorines:
oors, cages
Moderately
to highly
virucidal,
moderately to
highly fungicidal,
and some sporicidal
activity
Corrosive to surfaces;
Vapors can be irritating
Iodine tincture is about 2%
iodophors:
(Betadine
, Povidine
)
Iodophors:
presurgical
scrub,
thermometers
Iodine tincture is about 2%
biguanide chlorhexidine
(Nolvasan
,
Hibiclens
, Virosan
)
Skin wounds,
presurgical
scrub, oral
cleaning
solutions, and
cages
moderately
virucidal, and poorly
fungicidal
Residual action of about 24 hours
due to binding to skin
ethylene oxide Rubber goods,
blankets,
and lensed
instruments
virucidal, and
fungicidal
Gas sterilization for objects
that cannot withstand
heat
Carefully read MSDS prior to
handling
Keep away from ames
and sparks
oxidizing agents hydrogen peroxide
peracetic acid
(Virkon
S)
Cleaning
wounds and
oors, foot
bath
Moderately to
highly bactericidal,
virucidal, and
fungicidal
Causes oxygen release, which kills
anaerobic bacteria
matter or hard water

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Fundamentals of Pharmacology for Veterinary Technicians Chapter 14

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