Pharmacology (1-24) Flashcards
1
Q
what does rINN stand for
A
recognised international non-prprietary name
2
Q
what does BAN stand for
A
British Approved Name
3
Q
what does USAN stand for
A
United States Approved Name
4
Q
this determines what the body does to the drug (Absorption, Distrbution, Metabolism, Excretion)
A
pharmacokinetics
5
Q
name the 4 parts of pharmacokinetics
A
- Absorption
- Distribution
- Metabolism
- Excretion
6
Q
this is defined as what the drug does to the body / the relationship to drug concentration at the effect site
A
pharmacodynamics
7
Q
name the pharmacokinetic model
helps understanding but is not directly relevant for clinical practice
A
one-compartment model
8
Q
name the pharmacokinetic model
describes movement between compartments; drug is only removed from central compartment
A
two-compartment model
9
Q
name the pharmacokinetic model
most commonly used to describe clinical scenarios
A
three-compartment model
10
Q
name the pharmacokinetic model
drug is eliminated from the body, elimination occurs from central compartment
A
open model
11
Q
name the pharmacokinetic model
drug is recirculated / drug is released into GIT via bile and then reabsorbed into plasma (enterohepatic recirculation)
A
closed model
12
Q
reaction order?
rate at which drug concentration changes is constant and independent of drug concentration; rate of elimination is constant
A
zero order kinetics: 𝚫C/𝚫t = -K0
13
Q
reaction order?
rate of drug elimination changes and is proportional to drug concentration; drug concentration decays exponentially; applies to most commonly used drugs
A
first order kinetics: 𝚫C/𝚫t = -KC
14
Q
name 4 pH environments that may lead to ion trapping effect with drugs
A
- gastric pH
- fetal pH
- milk pH
- urine pH
15
Q
what is the Henderson Hasselbach equation for acids
A
pH - pKa = log(ionized/nonionized)
16
Q
what is the Henderson Hasselbach equation for bases
A
pH - pKa = log (nonionized/ionized)
17
Q
how to find the pKa of a drug
A
pH at which 50% of the drug is ionized
18
Q
this is the passage of a drug from site of administration to blood stream; influenced by solubility, physiochemical properties, site of administration, and bioavailability
A
absorption
19
Q
name the 3 types of parenteral administration
A
- intravenous
- intramuscular
- subcutaneous
20
Q
name the route of administration
most rapid onset of action, rate of administration usually slow
A
intravenous
21
Q
name the route of administration
bypasses GIT, achieves sytemic levels more rapidly, advantageous when animal is inappetant or vomiting
A
parenteral
22
Q
name the route of administration
often the only option for owners, influenced by speed of gastric emptying and presence of food
A
oral
23
Q
this refers to the removal of a percentage of the drug as it passes through the liver via the portal vein before it reaches the systemic circulation and effect site
A
first pass effect
24
Q
what effect does vasoconstriction have on absorption of agent from a site
A
reduces it
25
this is an indication of total exposure to the drug, used to define bioavailability, and used to calculate clearance
area under the curve (AUC)
26
this defines the extent to which an administered does of a drug enters the systemic circulation intact; referred to as F
bioavailability
27
what is the bioavailability of intravenous drugs
100%
28
this feature of pharmacokinetics is influenced by movement across membranes, blood flow to different organs, lipid solubility, and plasma protein binding
distribution
29
this is the main plasma protein drugs bind to
albumin
30
what is the equation for volume of distribution for a drug
Vd = Dose / C0
31
this is the peak plasma concentration after equilibrium is achieved and before elemination has begun
C0
32
this enhances drug access to sites of metabolism
lipid solubility
33
this enchances possibility of renal excretion of drug
water solubility
34
this part of drug elimination occurs mainly in the liver (but also in plasma, kidney, gut and lung); in phase 1 or phase 2 reactions
biotransformation
35
what are the 3 types of phase 1 biotransformation reactions?
1. hydrolysis
2. reduction
3. oxidation
36
what are the 3 types of phase 2 biotransformation reactions
1. acetylation
2. glucoronidation
3. conjugation to amino acids
37
what is the main organ for drug excretion?
kidney
38
what are the 3 main factors for drug excretion by the kidney
1. water solubility
2. GFR
3. Active Transport
39
what are the 2 factors for reabsorption of a drug
1. lipid solubility
2. ionisation (ion trapping)
40
what are the 3 less common routes of drug elimination?
1. biliary
2. skin
3. pulmonary
41
this is the time taken for the plasma drug concentration to fall by 50%
half-life of elimination
42
what is the equation for half-life in terms of K (slope of the PDC/time curve)
t 1/2 = 0.693 / K
43
name 3 factors affecting half-life of a drug
1. access to sites of biotransformation or elimination
2. interaction with other drugs
3. physiologica/pthological states
44
what is the equation for the relationship between half-life and clearance?
t 1/2 = 0.693 x Vd / Cl_B
45
this is defined as the volume of blood cleared of the drug by all elimination processes per unit of time (mL/min) - encompasses biotransformation and excretion processes
clearance
46
this is where the levels of drug remain stable or consistent from dose to dose
steady state
47
how many half-lives does it take to reach 95% steady state
5
48
how many half-lives does it take to reach 99% steady state
7
49
name the 3 ways steady state can be achieved
1. intravenous continuous infusion
2. loading dose followed by a regular dose at fixed intervals
3. fixed interval of a regular does
50
what is the fluctuation within steady state if the dose interval is the same as the half-life
50%
51
what is the fluctuation within steady state if the dose interval is twice the half-life
75%
52
name the formula for acids
| (pharmacology summary of Formulae)
pH - PKa = log[ionized/non-ionized]
53
name the formula for bases
| (pharmacology summary of Formulae)
pH - PKa = log[non-ionized/ionized]
54
name the formula for bioavailability
| (pharmacology summary of Formulae)
F = AUC oral / AUC IV
55
name the formula for volume of distribution
| (pharmacology summary of Formulae)
Vd = dose/C_0
| (where C_0 = concentration at time 0)
56
name the formulas for half-life
| (pharmacology summary of Formulae)
t 1/2 = 0.693/K
t 1/2 = 0.693 x Vd/Cl
57
name the formula for clearance
| (pharmacology summary of Formulae)
Cl = Vd x K
58
name the formula for dose
| (pharmacology summary of Formulae)
Dose = [Cmax] x Vd
59
this is a macromolecular structure with which the drug reacts; may be a protein, enzyme, nucleic acid, or less specific
drug receptor
60
this is a drug that binds to a physiological receptor and mimics the effect of the endogenous ligand
agonist
61
this type of agonist can achieve maximal response even if not all the receptors are occupied
full agonist
62
this type of agonist is incapable of achieving maximal response even if all the receptors are occupied
partial agonist
63
this is the tendency of the ligand (drug) to bind to the receptor
affinity
64
this is a term used to describe how good the drug is at eliciting a response
efficacy
65
this is a relative term that is often used to compare two drugs - comparing the concentration required to elicit the same response
potency
66
this is the concentration of the drug required to produce 50% of maximal response
EC 50
67
these drugs habe affinity but have no instrinsic activity & block the effect of the agonist
antagonist
68
# name the type of antagonist
most important, effects are reversible/surmpuntable by increasing amount of agonist
competitive antagonist
69
# name the type of antagonist
cannot be overcome by increasing amount of agonist; ex: Aspirin
non-competitive antagonist
70
at equilibrium, the number of receptors occupied by the drug is related to the concentration of the drug & described by this equation
Hill-Langmuir equation
71
this defines the capacity of a drug to preferentially produce one particular effect
selectivity
72
this is an absolute term; a drug with this tends to only act on one particular receptor type
specificity
73
this is the ratio of the dose giving an undesirable effect over the dose required to give the desired effect
therapeutic index
74
name 4 types of drug receptors
1. ion chanell cell surface transmembrane receptor
2. G protin couple receptor
3. protein kinase
4. cytosolic receptor
75
this type of drug receptor mediates action of a variety of proteins such as insulin
protein kinases
76
this is when a receptor is exposed to a ligand and the response reaches a peak then begins to fall off (despit the continued presence of ligand)
receptor desensitization
77
this is when receptors become internalized and degraded within the cell
receptor down-regulation
78
this is a term used to denote the rapid loss of responsiveness to a drug following intial dosing
tachyphylaxis
79
what are drug dosing regimens based on?
normal healthy individuals
80
name 4 things that may cause a dosing regimen to need individualization
1. age
2. species
3. health status
4. concurrent treatment
81
certain states of the animal may cause drug dose regimens to need individualization bc they may result in these 3 changes
1. changes in Vd
2. changes in plasma protein binding
3. changes in metabolism
82
name 4 routes of ectotoxicity for ectoparasiticides
1. incorrect disposal
2. leakage from fish farms
3. excretion in feces or urine
4. topical products washed off
83
name the 5 points of the BSAVA/BVA/BVZA 5-point plan for responsible ectoparasiticide use
1. educate clients to check & prevent parasites
2. understand the risks
3. risk-based prescribing
4. ensure appropriate use & disposa
5. record & monitor use
84
what is the mode of action for systemic macrocytic lactones?
| (ectoparasiticide)
bind to glutamate & GABA-activated chloride channels
| (leading to paralysis and death)
85
do systemic macrocytic lactones have repellent or knock-down activity?
no
86
name the two main groups of systemic macrocytic lactones
1. Avermectins
2. Milbemycins
87
what are the 2 main parasites that systemic macrocytic lactones act against
1. Mites (Sarcoptiforms & Demodex & other)
2. Fleas
(NOT ticks)
88
what species are systemic macrocytic lactones used clinically for?
range of species
89
these are licensed for flea control in dogs and cats in the US; derived from Saccharopolyspora spinosa; selective for insects
Spinosyn macrocytic lactones
| (Spinosad and Spinetoram)
90
what type of pyrethroid is Permethrin
type 1 (non alpha-cyano)
91
what type of pyrethroid is Cypermethrin, Deltamethrin, and Flumethrin?
type 2 (alpha-cyano)
92
what is the mode of action of Pyrethrins & Pyrethroids?
| (ectoparasiticides)
affect voltage-gated sodium channels
| (causing hyper-exciitability and death)
93
what species are Pyrethrins & Pyrethroids used clinically on?
dogs, small mammals, horses, farm animals, poultry
93
do Pyrethrins & Pyrethroids have repellent or knock-down activity?
yes, good
94
what adverse effects can type 1 Pyrethroids have?
1. excitation
2. tremors
3. hyperthermia
95
what adverse effects can type 2 Pyrethroids have?
1. salivation
2. extensor tone
3. incoordination
4. seizures
5. apnea
96
what is the mode of action for oxadiazines?
blocks neuronal sodium channels
| (causing paralysis and death)
97
do oxadiazines have repellent or knowck-down activity?
no
97
what species are oxadiazines used for clinically?
dogs and cats
98
what is the mode of action for phenylpyrazoles?
| (ectoparasiticide)
bind to GABA & glutamate-activated chloride channels
| (leading to hyper-excitability and death)
99
name two types of phenylpyrazoles
| (ectoparasiticide)
1. fipronil
2. pyriprole
100
what species are phenylpyrazoles used for clinically?
dogs and cats
101
does phenylpyrazoles have repellent or knowck-down activity?
no
102
which ectoparasiticide is topical and spreads in sebum?
phenylpyrazoles
103
what two species are phenylpyrazoles highly toxic to?
rabbits and fish
104
what is the mode of action for neonicotinoids?
| (ectoparasiticide)
bind to nicotinic acetylcholine receptors
| (leading to hyper-excitability, paralysis and death)
105
do neonicotinoids have repellent or knock-down activity?
no (except nitenpyram has knock-down effect)
105
what species are neonicotinoids used for clinically?
dogs, cats, small mammals
106
name 3 types of neonicotinoids
1. nitenpyram
2. imidacloprid
3. dinotefuran
107
what is the mode of action for isoxazolines?
| (ectoparasiticide)
bind to GABA and glutamate-activated chloride channels
| (causing hyper-excitability and death)
108
what parasites are isoxazolines efficient on
1. fleas and other insects
2. Sarcoptes, Demodex & other mites
3. ticks
108
do isoxazolines have repellent or knock-down activity?
NO
109
what species are isoxazolines used to treat clinically?
dogs, cats, poultry
110
what percent are isoxazolines passed out unchanged in feces?
80-90%
111
what is the mode of action for formamidines?
| (ectoparasiticide)
1. monoamine oxidase inhibitor
2. octopamine receptor agonist
3. Alpha2 receptor agonist
| (causing increased nerve activity and death)
112
what parasties are formamidines effictive against?
1. Sarcoptes, Demodex & other mites
2. ticks
113
do formamidines have repellent or knock-down activity?
yes, good
114
what species are formamidines used to treat clinically?
small animals, farm animals
115
what 3 animals are formamidines contraindicated for?
1. cats
2. horses
3. chihuahuas
116
what is the mode of action for carbamates and organophosphates?
form complexes with acetylcholinesterases
117
do carbamates and organophosphates have repellent or knock-down activity?
yes, rapid
118
name 5 adverse effects of muscarinic overstimulation from organophosphate poisoning
1. Salivation
2. Lacrimation
3. Urination
4. Defecation
5. GI cramps
6. Emesis
| (SLUDGE)
119
name 4 adverse effects of nicotinic overstimulation from organophosphate poisoning
1. Mydriasia Tachycardia
2. muscle Weakness
3. Twitching
4. Fasciculation
(high BP, paralysis)
| (MT WTF)
120
which ectoparasiticide can cause irreversible chronic neurotoxicity from long term sub-clinical exposure (ataxia, paresis, paralysis)
carbamates and organophosphates
121
what species are calcium polysulfides and thiosulphates (lime sulphur) used to treat clinically
cats, horses, SA camelids
122
what parasites are calcium polysulfides and thiosulphates (lime sulphur) effective against in cats?
1. Demodex gatoi
2. Lynxacarus
3. Notoedres
4. Cheyletiella
5. Trombicula
6. lice
123
what parasites are calcium polysulfides and thiosulphates (lime sulphur) effective against in horses?
1. Chorioptes
2. lice
124
what parasites are calcium polysulfides and thiosulphates (lime sulphur) effective against in SA camelids?
1. Chorioptes
2. Sarcoptes
125
do calcium polysulfides and thiosulphates (lime sulphur) have repellent or knock-down effects?
NO
126
name 4 adverse effects of calcium polysulfides and thiosulphates (lime sulphur)
1. skin irritatio
2. malodorous
3. yellow stains
4. oral ulcers if ingested
127
# name the topical ectoparasiticide formulation
hydrophobic polymers (resist wetting and degradation);
silicons oils and fatty acids (gradual release and diffusion);
can cause physical injury or skin irritation
collars
128
# name the topical ectoparasiticide formulation
raid systemic absorption/diffusion through skin and coat; sebum may be important for diffusion;
can have aversion or irritation, effects on furniture and surfaces, and environmental impacts
spot-on or pour-on
129
# name the topical ectoparasiticide formulation
good application and distribution, but more difficult to apply;
vulnerable to wetting and bathing;
disliked by animals;
increased risk of eye exposure, inhalation, and ingestion as well as human exposure
sprays and dips
130
this is an agent that kills microbes or inhibits their growth without damaging the host
antimicrobials
131
these are microbial products that kill or inhibit other micro-organisms
antibiotic
132
these are synthetic agents with activity against bacterial
antibacterial
133
# name the type of resistance
lack of acticity due to inherent phenotype (e.g. lack of target, failure to penetrate cell wall, etc.)
inherent
134
# name the type of resistance
mutations that confer resistance
chromosomal
135
# name the type of resistance
resistance genes on mobile genetic elements (e.g. plasmids)
transferable
136
what are mycoplasmas resistant to?
beta-lactams
137
what are anaerobes resistant to?
aminoglycosides
138
what are aerobes resistant to?
metronidazole
139
this is the biggest driver of antimicrobial resistance
antimicrobial use
140
name 3 methicillin resistant staphylocci (MRS) organisms of concern
1. S. pseudointermedius (MRSP)
2. S. schleiferi (MRSS)
3. S. aureus (MRSA)
141
name 2 multidrug resistant (MDR) cocci organisms of concern
1. Streptococcus
2. Enterococcus
142
name 2 other multidrug resistant (MDR) organisms of concern
1. Pseudomonas
2. Salmonella
143
what does nosocomial mean?
healthcare-acquired
144
name the 3 most common problems of vet-visiting dogs, cats and horses that tend do get antimicrobials but do not always require systemic antimicrobial treatment
1. pruritis
2. diarrhea
3. respiratory conditions
145
name the 3 most important drivers for antimicrobial use in practice which should be addressed to change the practice culture and improve antimicrobial stewardship (AMS)
1. vet prescribing behaviors
2. interactions with clients
3. practice norms
146
this describes the drug-host interaction
(bioavailability, penetration and clearance)
pharmacokinetics (PK)
147
this describes the drug-target interaction
(mode of action)
Pharmacodynamics
148
name 6 factors affecting PK/PD drug models
1. poor bioavailability
2. hypovolemic shock/poor perfusion
3. renal/liver failure
4. increased minimum inhibitory concentration (MIC)
5. biofilm
6. pus, debris, foreign material
149
this type of drugs are largely restricted to extracellular fluid (ECF);
fluid retention, IV fluid therapy, and/or increased renal clearance may necessitate higher doses to ensure therapeutic concentrations at the site of infection
hydrophilic (water soluble)
150
this type of drug penetrates tissues effectively and are less affected by changes in fluid dynamics and clearance
lipophilic (fat-soluble)
151
# excellent, good, or poor tissue penetration?
Chloramphenicols
Fluoroquinolones
Minocycline
Doxycycline
Metronidazole
Rifampin
excellent
152
# excellent, good, or poor tissue penetration?
Trimethoprim-sulfonamides
Lincosamides
Macrolides
Tetracyclines
good
153
# excellent, good, or poor tissue penetration?
Beta-lactamase inhibitors
Penicillins
Cephalosporins
Aminoglycosides & aminocyclitols
poor
154
name 3 concentration dependent antimicrobials
1. most fluoroquinolones
2. aminoglycosides
3. metronidazole
155
name 2 time dependent antimicrobials
1. penicillins
2. cephalosporans
156
name 3 antimicrobials with mixed effects for mode of action
1. some fluoroquinolones
2. lincosamides
3. tetracyclines
157
what is the efficacy of concentration dependent antimicrobials
ratio peak concentration (Cmax) to MIC
158
what is the efficacy of time dependent antimicrobials
time above MIC
159
what is the efficacy of antimicrobials with mixed effects
total 24h exposure (area under curve)
160
what is the dosing for concentration dependent antimicrobials
max dose every 24h
161
what is the dosing for time dependent antimicrobials
appropriate dose every 8-12h
162
# Bacteristatic or Bactericidal?
Lincosamides
Macrolides
Chloramphenicols
Tetracyclines
Trimethoprim
Sulphonamides
bacteriostatic
163
# Bacteriostatic or Bactericidal?
Penicillins
Cephalosporins
Fluoroquinolones
Trimethoprim-sulphonamides
Aminoglycosides & aminocyclitols
Metronidazole
bactericidal
164
# Bacteriostatic or Bactericidal drugs?
may be more effective in seriously immunocompromised patients
Bactericidal drugs
165
# Bacteriostatic or Bactericidal drugs?
may result in less toxin release and toxic shock in staphylococcal and streptococcal infections
Bacteriostatic drugs
166
# Bacteriostatic or Bactericidal drugs?
minimum bactericidal concentration (MBC) is much higher than the MIC
bacteriostatic drugs
167
# Bacteriostatic or Bactericidal drugs?
minimum bactericidal concentration (MBC) is close or identical to the MIC
bactericidal drugs
168
what is the most serious adverse drug reaction (ADR)
hypersensitivity reactions
169
what breed has a bred-specific risk of adverse drug reactions to sulphonamides
Dobermans
170
# name the main route of excretion for these drugs
Fluoroquinolones
Rifampicin
Doxycycline
Chloramphenicols
hepatic (liver)
171
# name the main route of excretion for these drugs
Tetracyclines
Lincosamides
Macrolides
Fluoroquinolones
Metronidazole
mixed hepatic-renal
172
name 5 circumstances where cuture and ASTs (antimicrobial sensitivity tests) are necessary
1. deep or complex infections
2. unusual cilinal signs/cytology
3. Rod bacteria
4. if empirical treatment fails
5. if AMR is more likely
173
in these tests: the zones of inhibition around each antimicrobial disc are compared to agreed breakpoints
Kirby-Bauer disc diffusion
174
in Kirby-Bauer disc diffusion tests, what shows that the infection is susceptible
zone of inhibition (ZI) exceeds the breakpoint
175
in Kirby-Bauer disc diffusion tests, what shows that the infection is resistant
zone of inhibition (ZI) is less than the breakpoint
176
these methods determine the lowest concentration of antimicrobial that inhibits bacterial growth
MIC methods
177
if MIC is (lower or higher?) than the breakpoint the infection is considered susceptible
lower
178
if MIC is (lower or higher?) than the breakpoint the infection is considered resistant
higher
179
the capital letters ('S' or 'R' or 'I') on a bacterial AST refer to this
the exact MIC
180
how to determine which antimicrobial is most effective from an AST
compare breakpoint:MIC ratio (want >1)
181
this breakpoint:MIC ratio means that the tissue concentration is only just sufficient enough to treat the infection and there is a risk of treatment failure
1
182
this breakpoint:MIC ratio means that the efficacy is less likely to be affected by factors that alter tissue concentration
>1
183
these can be effective in surface and superficial infections & some focal deep infections
topical microbials and antibiotics
184
name some effective antimicrobials
1. chlorohexidine
2. manuka honey
3. hypochlorous acid
4. polihexanide
5. bleach
185
these antimicrobials have well established breakpoints, efficacy and saftey;
appropriate for empirical treatment
first line antimicrobials
186
these antimicrobials have a concern for AMR;
they should only be used when there is culture evidence and/or PK/PD factors suggesting that first line drugs would not be appropriate
second line antimicrobials
187
these antibiotics are critically important andd AMR is of great concern;
they may not be licensed for use in animals;
breakpoint, efficacy and sfety data may be limited;
must only be used where no first or second line antibiotics are effective and topical antimicrobial therapy is not feasible or effective
third line antibiotics
188
# what line are these antibiotics?
Penicillins
Ampicillin & amoxicillin
1st & 2nd gen. cephalosporins
Clindamycin & lincomycin
Tetracyclines
Trimethoprim-sulphonamides
Spiramycin
Metronidazole
first line antimicrobials
189
# what line are these antimicrobials?
3rd gen. cephalosporins
Fluoroquinolones
Florfenicol (in cattle)
2nd line antimicobials
190
# what line are these antimicrobials?
Aminoglycosides
Anti-Pseudomonas penicillins
Azithromycin & clarithromycin
3rd & 4th gen. cephalosporins
Chloramphenicol & florfenicol (in horses and small animals)
Rifampicin
Nitrofurantoin
3rd line antimicrobials
191
# name the common antimicrobial combination
high tissue perfusion;
effective against gram- anaerobes, anaerobes, staphylococci and most gram+ aerobes (except streptococci)
Fluoroquinolone & Metronidazole
192
# name the common antimicrobial combination
low tissue penetration;
effective against gram- aerobes, most anaerobes and gram+ aerobes
Aminoglycoside & Amoxicillin-clavulanate
193
# name the common antimicrobial combination
mixed tissue penetration;
effective against gram- aerobes, most anaerobes & gram+ aerobes
Aminoglycoside & Lincosamides
194
# name the common antimicrobial combination
Mixed tissue penetration;
effective against gram- aerobes, most anaerobes and gram+aerobes;
high potential for AMR
Fluroquionolone & Amoxicillin-clavulanate
195
name the 4 principles of prophylactic treatment
1. select antimicrobial appropriate to the infection risk
2. start treatment before procedure for adequate plasma and tissue levels
3. repeat treatment to maintain tissue levels
4. pot-op treatment continued only if necessary
196
this is the treatment of the whole group including infected and non-infected animals;
may be considered to prevent the spread of disease
metaphylaxis
197
what is the mode of action for penicillins
disrupt bacterial cell wall causing lysis (penicillin-binding proteins - PBP)
198
what bacteria are penicillins most active against
gram-pos bacteria
199
name 3 categories of penicillins
1. narrow spectrum penicillins
2. aminopenicillins
3. anti-staphylococcal pennicillins
200
amoxicillin is often combined with this beta-lactamase inhibitor
clavulanic acid
201
some bacterial PBPs act as beta-lactamases to cleave the beta-lactam ring and inactivate this class of antibiotics
penicillins
202
name 3 types of beta-lactamase inhibitors
1. clavulanic acid
2. sulbactam
3. tazobactam
203
# name the antibiotic class
inhibit beta-lactamases and enhance activity for penicillins susceptible to these enzymes
beta-lactamase inhibitors
204
how are cephalosporins classed?
| (antibiotic)
generations (1G, 2G, 3G, 4G)
205
what is the mode of action for cephalosporin antibiotics?
similar to penicillins (disrupt the bacterial cell wall causing lysis)
206
what bacteria type are Cephalosporins NOT active against
enterococci (limited against anaerobes)
207
what is the mode of action for lincosamides and macrolides?
| (antibiotics)
bind to 50S ribosome subunit to prevent protein synthesis
208
name 2 types of lincosamides
| (antibiotics)
1. clindamycin
2. lincomycin
209
what type of bacteria are lincosamides and macrolides most effective against?
gram-positive bacteria
210
what type of bacteria are lincosamides and macrolides NOT effective against?
gram-negative bacteria
211
name 3 things resistance to lincosamides and macrolides is associated with
1. modified ribosome binding site (erm genes)
2. efflux pumps
3. bacteria drug modification
212
what is the mode of action for Trimethoprim-sulphonamide ?
| (antibiotics)
block folic acid synthesis (required for purine and pyrimidine synthesis)
213
name an adverse effect of trimethoprim-sulphonamide
very bitter - salivation and foaming (cats)
214
what type of bacteria are trimethoprim-sulphonamides most effective against (moderate activity)
gram-positive bacteria
215
what is the mode of action for fluorquinolones?
| (antibiotics)
inhibit topoisomoerase II (DNA gyrase) in gram-neg bacteria
| (disrupts DNA cleavage, reunion and super-coiling)
216
what 3 things is resistance to fluoroquinolones associated with
| (antibiotics)
1. decreased cell permeability
2. efflux pumps
3. altered topoisomerases
217
what is the mode of action for aminoglycosides
| (antibiotics)
block protein synthesis at 30S ribosome subunit
218
what type of bacteria are aminoglycosides most effective against
gram-neg bacteria
219
list the 6 aminoglycosides in order of most to least efficacy
| (antibiotics)
amikacin > tobramycin > gentamycin > neomycin = kanamycin > streptomycin
| aktgnks
220
what 2 things is resistance to aminoglycosides associated with
| (antibiotics)
1. modification of ribosome binding site
2. efflux pumps
221
this is an antibiotic closely related to aminoglycosides;
lack most of the systemic toxicity assoc. with aminoglycosides BUT chromosomal resistance can occur rapidly
aminocyclitols
222
what is the mode of action for tetracyclines
| (antibiotics)
block protein synthesis through 30S ribosome subunit
223
name 5 types of tetracyclines
| (antibiotics)
1. tetracycline
2. chlortetracycline
3. oxytetracycline
4. doxycycline
5. minocycline
224
name 3 things resistance to tetracyclines is associated with
| (antibiotics)
1. multiple genes for efflux
2. ribosome binding
3. drug modification
225
what is the mode of action for chloramphenicols
| (antibiotics)
disrupt protein synthesis through 30S and 50S subunits
226
what type of bacteria are chloramphenicols most effective against
anaerobes
227
what is resistance to chloramphenicols associated with
drug inactivating enzymes
228
what is the major adverse effect of chloramphenicols
| (antibiotics)
fatal aplastic anemia in humans
229
what is the mode of action for metronidazole
| (antibiotics)
disrupts DNA strands and inhibits repair enzyme (DNAase-1)
230
what conditions are required for metronidazole to be effective?
what is the only type of bacteria metronidazole is effective against
anaerobic
231
what is an adverse effect of metronidazole
| (antibiotics)
bitter - inappetance and hypersalivation (cats)
232
what is the mode of action for rifampicin
| (antibiotics)
inhibits RNA polymerase and DNA transcription
233
what type of bacteria is rifampicin NOT effective against
| (antibiotics)
gram-negative
234
what is an adverse effect of rifampicin
| (antibiotics)
red-orange discoloration of bodily fluids
235
what is the mode of action for nitrofurans
| (antibiotics)
disrupts mRNA translation (from intracellular bacterial metabolism)
236
what type of bacteria is nitrofurantoin NOT effective against
| (antibiotics)
anaerobes
237
what type of infection is nitrofurantoin (nitrofurans) restricted to and why
UTIs bc of rapid renal excretion
238
what are 3 adverse effects of nitrofurans
| (antibiotics)
1. erythema
2. pruritic
3. oedema
(also toxicity and carcinogenic potential)
239
name 5 antibiotics that are limited to topical use only due to toxicity and PD/PK factors
1. polymixin B
2. bacitacin
3. silver sulphadiazine
4. fusidic acid
5. mupirocin
240
# name the topical antibiotic
cationic agent: disrupts bacterial cell membrane phospholipids;
more effective against gram-neg bacteria;
resistance (decr. permeability) is uncommon;
inactivated by pus and debris
Polymixin B
241
# name the topical antibiotic
acts on gram-pos bacteria by inhibitng cell wall peptoglycan synthesis
bacitracin
242
# name the topical antibiotic
inhibits ribosomal activity and protein synthesis;
mainly active against gram-pos bacteria (staph, strep, corynebacteria);
NOT active against enterococci;
resistance associated with decreased ribosomal binding
fusidic acid
243
# name the topical antibiotic
blocks nucleic acid synthesis;
active against gram-pos bacteria
novobiocin
244
# name the topical antibiotic
inhibits RNA synthesis;
active against gram-pos bacteria (incl MRSP and MRSA) - narrow spectrum ;
resistance associated with mutations in target enzyme
mupirocin
245
what is the initial treatment choice for most fungal infections?
Azoles (imidazoles and triazoles)
246
what is the mode of action for azoles
| (antifungal)
inhibit ergosterol synthesis disrupting fungal cell wall metabolism
247
are azoles fungistatic or fungicidal?
fungistatic
248
which azole's absorption is not affected by food
| (antifungal)
Fluconazole
249
whih azole's absorption is decreased with food
| (antifungal)
voriconazole
250
list the 4 main azoles in order from most well-tolerated to least well-tolerated in terms of adverse effects
| (antifungal)
fluconazole > itraconazole = voriconazole > ketoconazole
| FIVK
251
what is the most common adverse effect of azoles
| (antifungal)
GIT upset
252
what is the mode of action for Allylamines (terbinafine)
| (antifungal)
blocks ergosterol synthesis through inhibition of aqualene epoxidase
253
are allylamines (terbinafine) fungistatic or fungicidal?
fungicidal
254
what type of fungi are allylamines (terbinafine) effective against
dermatophytes
255
is absorption of allylamines (terbinafine) affected by food?
| (antifungal)
no
256
how are allylamines (terbinafine) excreted
| (antifungal)
hepatic metabolism
257
name 2 common polyenes
| (antifungal)
nyastatin and natamycin
258
what is the mode of action for polyenes
| (antifungal)
disrupt fungal cell membranes by occupying ergosterol binding sites
259
are polyenes fungistatic or fungicidal
fungicidal
260
what type of fungi are polyenes used for
superficial fungal infections only (Malassezia and Candida)
261
what is the mode of action for griseofulvin
| (antifungal)
inhibits mitosis, nucleic acid synthesis and cell wall metabolism
262
is griseofulvin fungistatic or fungicidal?
fungistatic
263
what type of fungi is griseofulvin mainly used for
dermatophytosis in horses
264
# name the antifungal
fungicidal;
poorly absorbed by GI tract so must be given parenterally;
dose-related nephrotoxicity
Amphotericin B
265
# name the antifungal
traditional antifungal treatment;
mode of action unclear;
used systemically and topically;
can cause GIT upsets, sialadenitis, and goitre
sodium or potassium iodide
266
# name the antifungal
blocks RNA synthesis;
synergy with amphotericin B for Cryptococcus and Candida;
NOT effective for dermatophytes;
renal excretion;
can cause GIT upsets, bone marrow suppression, hypersensitivity reactions, and neurological problems (cats)
flucytosine
267
what is the mode of action for Acyclovir, Famiciclovir, Ixouridine, and Remdesivir?
| (antiviral)
nucleoside analogues that inhibit DNA/RNA synthesis
268
what is Acyclovir most commonly used alongside to increase anti-viral effect
| (antiviral)
recombinent feline IFN-omega OR human IFN-alpha
269
what s Famiciclovir used systemically for?
| (antiviral)
FHV-1 infections
270
what is ixouridine used to treat?
| (antiviral)
topically in FHV-1
271
what is Remdesivir used to treat and how long must it be given?
| (antiviral)
FIP (give SQ or IV for over 12 weeks)
272
what is the mode of action of amantidine?
| (antiviral)
block M2 protein ion channels to prevent endocytosis
273
what type of viruses is amantidine active against
| (antiviral)
enveloped RNA viruses
274
what is teh mode of action for L-lysine
| (antiviral)
peptide, competitive inhibitor of arginine
275
what is L-lysine used for in cats
| (antiviral)
FHV-1
276
# name the interferon
active against many DNA and RNA viruses by direct inhibition of viral replication and stimulating anti-viral immunity;
used for FIV and FeLV in cats;
used for papilloma virus infections in dogs;
topical administration alongside acyclovir for FHV-1 keratitis
| (antiviral)
recombinent human IFN-alpha
277
# name the interferon
used in cats and dogs for acute and chronic viral conditions (FeLV, FIP, FCV and canine parvovirus infection)
| (antiviral)
recombinent feline IFN-omega
278
name 2 mycobacterial derived immunomodulators
| (antiviral)
1. Bacille Calmett-Guerin (BCG)
2. Regressin-V
279
name the 4 nucleoside analogue DNA/RNA synthesis inhitors used in animals
| (antiviral)
1. acyclovir
2. famciclovir
3. idoxuridine
4. remdesivir
| AFIR
280
name a peptide antiviral drug used in animals
L-lysine
281
what does VMR stand for?
veterinary medicines regulations
282
what does VMD stand for?
veterinary medicines directorate
283
this is the executive agency of DEFRA;
they operate the licensing system for animal medicines with aim to safe guard public health, animal health and the environment
veterinary medicines directorate (VMD)
284
this is a national surveillance scheme run by the VMD which aims to record and monitor reports of suspected adverse reactions to veterinary medicines in both animals and humans
SARSS (suspected adverse reaction surveillance scheme)
285
this is designed to provide information on the work of the VMD, plans and results, as well as general developments on the controls on veterinary medicines; publish quarterly reports
MAVIS (Marketing Authorizations Veterinary Information Service)
286
this governing body offers advice to the VMD on behalf of the Secretary of State, in respect of new and renewal marketing authorizations (MA), provisional MAs, variations to MAs and Animal Test Certificates (ATCs)
VPC (veterinary products committee)
287
who should adverse drug reactions be reported to
veterinary medicines directorate (VMD)
| (under SARSS)
288
what 3 things make it ideal to use licensed veterinary products
1. safety
2. quality
3. efficacy
289
name the 6 steps involved in drug development
1. pre-discovery
2. discovery
3. pre-clinical testing
4. clinical trials
5. licensing
6. marketing
290
name the 4 legally classified categories of veterinary medicines
1. prescription only medicine - vet (POM-V)
2. POM-vet, pharmacist, SQP (POM-VPS)
3. non-food animal - vet, pharmacist, SPQ (NFA-VPS)
4. authorized vet medicine-general sales list (AVM-GSL)
291
# name the legally classified category of veterinary medicine
Can be prescribed by a VS after clinical assessment of the animal or herd;
in this category if contains a new active ingredient, has safety issues, a narrow safety margin, due to government policy or because specialised veterinary knowledge required for its use
Prescription Only Medicine – Veterinarian (POM‐V)
292
# name the legally classified category of veterinary medicine
Can be prescribed by VS or SQP, No clinical assessment is required but the prescriber must be sure owner is competent to administer the product;
in this category if: it is used to reduce or prevent endemic disease in herds or flocks or individual animals, there is some risk for user, consumer, animal or environment, but users made aware by verbal or written advice
Prescription Only Medicine – Veterinarian, Pharmacist, SQP (POM‐VPS)
293
# name the legally classified category of veterinary medicine
Similar to POM‐VPS but must be for non‐food animals
Non‐Food Animal – Veterinarian, Pharmacist, SQP (NFA–VPS)
294
# name the legally classified category of veterinary medicine
No restrictions on its supply;
wide safety margin and specialist advice is not required
Authorised Veterinary Medicine – General Sales List (AVM‐GSL)
295
this is an assessment of relevant clinical information, which may include an examination of the animal
"clinical assessment"
296
# which step of 'the cascade' ?
Veterinary medicine with a Marketing Authorisation valid in GB or UK wide for indicated species and
condition
step 1
297
# which step of 'the cascade' ?
Veterinary medicine with a Marketing Authorisation valid in NI for indicated species and condition
step 2
298
# which step of 'the cascade' ?
veterinary medicine with a Marketing Authorization valid in GB, NI or UK wide for a different species or condition
step 3
299
# which step of 'the cascade' ?
human medicine with a Marketing Authorization valid in GB, NI or UK wide OR an authorized vet med from outside the UK
step 4
300
# which step of 'the cascade' ?
extemporaneous preparation prepared by a vet, pharmacist or person holding an appropriate Manufacturer’s Authorization, located in the UK
step 5
301
if the withdrawal period is not specified on a veterinary medicine, what should it be set at for eggs and milk
no less than 7 days
302
if the withdrawal period is not specified on a veterinary medicine, what should it be set at for meat
not less than 28 days
303
if the withdrawal period is not specified on a veterinary medicine, what should it be set at for meat from fish
not less than 500 degree days
304
this is a means of defining the product, its dose and other relevant instructions
prescription
305
what must a written prescription contain?
| (10)
1. Name, address and phone number of prescriber
2. Credentials of the prescriber
3. Name and address of the person receiving the prescription
4. A description of animal
5. Drug, dose and instructions (incl. withdrawal period)
6. Note if prescribing under the cascade
7. Date
8. Written in indelible format
9. Signed
10. “For animals under my care”
306
what does the abbreviation od mean in prescriptions
once daily (omni die)
307
what does the abbreviation sid mean in prescriptions
once daily (semel in die)
308
what does the abbreviation bd mean in prescriptions
twice daily (bis die)
309
what does the abbreviation tid mean in prescriptions
three times daily (ter in die)
310
what does the abbreviation qid mean in prescriptions
four times daily (quarter in die)
311
what does the abbreviation pc mean in prescriptions
after food (post cibum)
312
what does the abbreviation ac mean in prescriptions
before food (ante cibum)
313
what does the abbreviation prn mean in prescriptions
when required (pro re nata)
314
are controlled drugs regulated under the VMR (veterinary medicines regulation)?
no
315
# name the schedule of controlled drugs
Vets have no authority to possess or prescribe these except with special license from Home Office
(ex: cannabis and LSD)
schedule 1
316
# name the schedule of controlled drugs
Special requirements for requisition, prescribing, record keeping, storage and disposal;
Requisition in writing to the supplier signed by the VS;
Stored in a home office approved, locked receptacle;
Destroyed in presence of a person authorised by the Secretary of State
(Ex: morphine, ketamine, fentanyl, secobarbital)
schedule 2
317
# name the schedule of controlled drugs
Subject to the same prescription and requisition requirements as schedule 2, BUT do not need to keep a record in a register;
Most should be kept in a locked receptacle;
(ex: pentobarbital, phenobarbital, buprenorphine and midazolam)
schedule 3
318
# name the schedule of controlled drugs
Exempt from most of the restrictions of controlled drugs;
(ex: benzodiazepines and anabolic substances)
schedule 4
319
# name the schedule of controlled drugs
Certain preparations containing codeine, cocaine and morphine in less than specified amounts;
Exempt from most of the requirements except that invoices need to be kept for two years
schedule 5
320
what 3 things must you record on obtaining a schedule 2 drug
1. date
2. name and address of supplier
3. amount obtained
321
what 4 things must you record on supplying a schedule 2 drug
1. date
2. name and address of person supplied
3. vet's name
4. amount supplied
322
how long are controlled drug prescriptions valid for?
28 days
323
how long should incoming and outgoing transaction records of POM-V and POM-VPS drugs be kept for
5 years
324
# name the scheme
Some veterinary products can be marketed without a marketing authorisation and therefore are not required to prove safety, quality or efficacy (but must be manufactured to certain standards)
exemption scheme for small pet animals
325
products including these 3 agents are not included in the exemption scheme for small pet animals
1. antibiotics
2. narcotics
3. psychotropics
326
how long is a prescription for medicated feedstuffs valid for
3 months
327
name 5 categories of feed additives
1. technological additives
2. sensory additives
3. nutritional additives
4. zootechnical additives
5. coccidostats and histomonostats
328
these can be defined as a substance used to maintain animals in good health or favorably affect their performance
feed additives
329
name 2 things the person supplied sheep dip must have one of
1. Certificate of Competence in the Safe Use of Sheep Dips
2. NPTC Level 2 Award in the Safe Use of Sheep Dip (QCF)
330
name the 2 things that must be given to the purchaser if the sheep dip is an organophosphorous compound
1. two pairs of heavy duty gauntlet style gloves
2. A4 laminated safety notice
331
name 4 features the permanent building for storing medicines must have
1. secure
2. clean
3. vermin proof
4. refridgerated space with temp monitoring
332
these are monoamines derived from the amino acid tyrosine;
they are water soluble and 50% bound to plasma proteins in circulation;
include adrenaline, noradrenaline and dopamine
catecholamine transmitters
333
these are drugs with similar actions to the postganlionic fibers of the SNS;
they resemble adrenaline in their actions and are also referred to as adrenergics
sympathomimetics
334
these are drugs that oppose the actions of the postganglionic fibers of the SNS;
they are also referred to as antiadrenergics or sympathetic (adrenergic) antagonists
sympatholytic
335
these are drugs that stimulate postsynaptic muscarinic receptors;
their actions resemble acetylcholine and they are also referred to as cholinergics or parasympathetic agonists
parasympathomimetics
336
these are drugs that oppose the actions of the PNS at the muscarinic receptors by blocking the actions of acetylcholine;
also referred to as anticholinergics, parasympathetic antagonists or occasionally vagolytics
parasympatholytics
337
# adrenergic or cholinergic?
all presynaptic efferent autonomic fibers and the somatic motor fibers
cholinergic
338
what do most postsynaptic sympathetic fibers release
noradrenaline
339
what is the effect of the sympathetic nervous system on the heart?
increased activity (beta1)
| (rate, strength, conduction)
340
what is the effect of the sympathetic nervous system on blood vessels
vasoconstriction (alpha1 and alpha2)
341
what is the effect of the sympathetic nervous system on the iris
dilation of pupil (mydriasis) (alpha1)
342
what is the effect of the sympathetic nervous system on the bronchi?
relaxation (beta2)
343
what is the effect of the sympathetic nervous system on the GIT
decreased activity (alpha1&2, beta1&2)
344
what is the effect of the sympathetic nervous system on the adrenal medulla
secretion (adrenaline)
345
name the 5 key features of neurotransmitter function that provide potential targets for pharmacologic therapy
1. synthesis
2. storage
3. release
4. binding to receptor
5. termination of action of the transmitter and receptor effects
346
what is the synthesis step of adrenergic neurotransmission?
1. Tyrosine converted to Dopa by tyrosine hydroxylase
2. Dopa converted to dopamine
347
what is the storage step of adrenergic neurotransmission?
1. dopamine transported into synaptic vessel by VMAT
2. dopamine converted to NE in the vesicle
348
what is the release step of adrenergic neurotransmission?
1. action potential opens calcium channels
2. fusion of vesicles with surface membrane using SNARE receptors and VAMP proteins
3. release of NE
349
what can block the release of noradrealine in adrenergic neurotransmission
botulinum toxin
| (cleaves SNARE proteins in neurons)
350
what can be used to block the reuptake of noradrenaline by the norepinephrne transporter (NET)
tricyclic antidepressants
351
# name the adrenergic receptor
contracts smooth muscles:
1. vasoconstriction
2. pyloric sphincter contraction (stomach)
3. urinary sphincter contraction
4. pupillary dilation (mydriasis)
5. positive ionotropic effect (myocardium)
| (Gq)
Alpha1 receptors
352
# name the adrenergic receptor
Presynaptic nerve terminals:
1. inhibits norepinephrine release
2. inhibits ACh release
3. inhibits insulin release
| (Gi)
Alpha2 receptors
353
# name the adrenergic receptor
Heart and Kidneys:
1. incr. heart rate
2. incr. cardiac contractility and stroke
3. incr. renin release
| (Gs)
Beta1 receptors
354
# name the adrenergic receptor
Relaxes Smooth Muscles, liver, pancreas, eye:
1. bronchodilation
2. decr. gastric contraction
3. decr. intestinal peristalsis
4. urinary retention
5. liver: glycogen to glucose
6. vasodilation
| (Gs)
Beta2
355
# name the adrenergic receptor
Adipose Tissue:
1. sdipose tissue lipolysis
2. decr. urination
| (Gs)
Beta3 receptors
356
what is the effect of the parasympathetic nervous system on the heart
decr. activity
| (M2 > M3)
357
what is the effect of the parasympathetic nervous system on the blood vessels
vasodilation
| (M2)
358
what is the effect of the parasympathetic nervous system on the iris
contraction of pupil (myosis)
| (M2, M3)
359
what is the effect of the parasympathetic nervous system on the bronchi
constriction
| (M2 = M3)
360
what is the effect of the parasympathetic nervous system on the GIT
incr. activity
| (M2=M3)
361
what is the effect of the parasympathetic nervous system on the adrenal medulla
no effect
362
what is the synthesis step of cholinergic neurotransmission
1. choline transported into presynaptic nerve terminal
2. ACh synthesized from choline and acetyl CoA by choline acetyltransferase (ChAT)
363
what is the storage step of cholinergic neurotransmission
1. ACh transported into large, clear vesicles by VAT along with neuropeptides and ATP
364
what is the release step of cholinergic neurotransmission
1. voltage sensitive Ca2+ channels open
2. influx of Ca2+
3. fusion of vesicles with surface membrane (involves SNAPs and VAMPs)
4. expulsion of ACh and co-transmitters into synaptic cleft
365
what can the release of ACh from the nerve terminal be blocked by
botulinum toxin
366
how many muscarinic receptors are there
5 (M1-M5)
367
what do muscarinic receptors M1, M4, and M5 act on
CNS
368
what does muscarinic receptor 2 act on
heart (reduces HR)
369
what does muscarinic receptor 3 act on
smooth muscle (contract)
370
# which cholinergic receptor?
blocked by curare;
linked to ion channels;
response is fast and brief;
located at neuromuscular junctions and autonomic ganglia;
mediate excitation in target cells;
post-synaptic
nicotinic
371
# which cholinergic receptor?
blocked by atropine;
linked to G-couple proteins;
found in smooth muscle;
mediate excitation and inhibition in target cells;
both pre- and postsynaptic
muscarinic
372
name 3 possible mechanisms of drugs acting on the autonomic nervous system
1. act on neurotransmitter receptor
2. interfere with NT biosynthesis
3. interfere with degradation of NT
373
what do direct acting agonists or antagonists act on
| (adrenergic drugs)
one or more postsynaptic adrenergic receptors (alpha1&2, beta1&2)
374
# name the type of adrenergic drug
increase release of NE or inhibit reuptake or block metabolising enzyme
indirect acting agonists
375
name 2 ways a drug acting on the ANS can interfere with degradation of neurotransmitter
1. inhibit degradation enzyme
2. inhibit neurotransmitter reuptake
376
name 2 ways a drug acting on the ANS can interfere with neurotransmitter biosynthesis
1. inhibit precursor uptake
2. inhibit enzyme for biosynthesis
377
what are the ACh receptors
nicotinic and muscarinic
378
what are teh 3 main types of nicotinic receptors
1. muscle (NMJ)
2. ganglionic (ANS)
3. CNS (brain)
379
name the 4 main classes of drugs affecting PNS
1. Muscarinic agonists (parasympathomimetics)
2. muscarinic antagonists (anticholinergics)
3. nicotinic agonists
4. nicotinic antagonists (ganglion blockers)
380
name 4 choline ester drugs (direct muscarinic agonists)
| (parasympathomimetics)
1. ACh
2. Methacholine
3. Bethanecol
4. Carbachol
381
what receptor do choline esters have a direct action on?
muscarinic receptors
382
# name the choline ester drug (muscarinic agonist - parasympathomimetic)
mainly muscarinic;
used inhaled for bronchial reactivity diagnosis
methacholine
383
# name the choline ester drug (muscarinic agonist - parasympathomimetic)
long acting;
highly specific for muscarinic receptors;
minimal cardiac negative chronotropic and ionotropic effects;
used to induce urination
bethanechol
384
# name the choline ester drug (muscarinic agonist - parasympathomimetic)
long acting;
significant nicotinic action;
used to induce gastric motility and urination and tpically to induce miosis
carbachol
385
name 3 types of alkaloid drugs (direct muscarinic agonists)
| (parasympathomimetics)
1. pilocarpine
2. muscarine
3. arecoline
386
# name the alkaloid drug (muscarinic agonist - parasympathomimetic)
dominant muscarinic activity;
tertiary amine alkaloid, so increased lipid solubility;
added topically to the eye to induce miosis;
used for treatment of glaucoma;
contraindicated in uveitis and anterior lens luxation
pilocarpine
387
these are indirectly acting parasympathomimetics;
they inhibit AChE to incr. ACh activity;
have a cholinergic effect initially but prolonged depolarization may have desensitization
anticholinesterases
388
name 3 factors that contribute to the effects/toxicity of anticholinesterases
| (indirect parasympathomimetics)
1. reversible or irreversible
2. affinity for receptor
3. how readily they can access receptor (volatility and lipid solubility)
389
name the 6 cholinergic effects of anticholinesterases that may lead to toxicity if in excess
| (indirect parasympathomimetics)
1. Salivation
2. Lacrimation
3. Urination
4. Defecation
5. Gastrointestinal distress
6. Emesis
| (SLUDGE)
390
what are the 3 main uses of anticholinesterases?
| (indirect parasympathomimetics)
1. diagnosis of myasthenia gravis
2. in anaesthesia to reverse neuromuscular blockade
3. in connection with eye and GIT
391
# name the anticholinesterase (indirect parasympathomimetic)
very short acting quaternary ammonium compound;
reversal of non-depolarizing muscle relaxants;
diagnosis of myasthenia gravis
Edrophonium chloride 'tensilon'
392
# name the anticholinesterase (indirect parasympathomimetic)
moderate duration of action;
reversal of non-depolarizing muscle relaxants;
treatment of myasthenia gravis (orally: TID, dose reduced as required)
Neostigmine
393
# name the anticholinesterase (indirect parasympathomimetic)
moderat duration;
more lipid soluble;
treatment of myasthenia gravis (orally: BID)
Pyridostigmine
394
# name the anticholinergic drug (muscarinic antagonist)
lipid soluble (crosses BBB);
used to increase HR and with anticholinesterases to prevent side effects from muscarinic stimulation;
not recommended in horses and rabbits are resistant;
atropine
395
# name the anticholinergic drug (muscarinic antagonist)
naturally ocurring agent;
crosses BBB - sedation;
used for drying secretions;
has antemetic properties;
contained in antispasmodic Buscopan with dipyrone metamizole
scopolamine (aka hyoscine)
396
# name the anticholinergic drug (muscarinic antagonist)
synthetic agent;
does not cross placenta or BBB;
less tachycardia;
slower onset and longer duration;
used to prevent and treat bradycadia (anaesthesia, vagal stimulation);
less CNS effects
Glycopirrolate
397
# name the anticholinergic drug (muscarinic antagonist)
bronchodilation in horses (R.A.O.);
inhalation - poor absorption therefore minimal side effects
Ipratopium bromide
398
# name the anticholinergic drug (muscarinic antagonist)
mydriatic and cycloplegic;
long duration of action
cyclopentolate
399
# name the anticholinergic drug (muscarinic antagonist)
used as a mydriatic (NOT cycloplegic);
drug of choice for intra-occular exam;
rapid acting, shorter duration of several hours
tropicamide
400
name 3 naturally occuring catecholamines
| (sympathomimetics)
1. adrenaline
2. noradrenaline
3. dopamine
401
# name the sympathomimetic drug
non-selective: acts at both alpha- and beta-adrenoceptors;
effects: incr. HR, incr. force of contraction, vasocontriction;
used for cardiac arrest and anaphylaxis;
can induce tachycardias and arrhythmias
adrenaline
402
# name the sympathomimetic drug
alpha effects > beta1 effects > beta2 effects;
primarily a vasopressor via alpha stimulation;
used to treat hypotension
noradrenaline
403
# name the sympathomimetic drug
acts at dopamine receptors alpha- and beta-adrenoceptors;
dose dependent effect;
mixed effects in practice;
used to treat hypotension
dopamine
404
what is the effect of dopamine at low doses
dopa effects:
1. vasodilation
2. incr. renal perfusion and filtration
405
what is the effect of dopamine at medium doses
beta effects:
positive inotropy and chronotropy
406
what is the effect of dopamine at high doses
alpha effects:
vasoconstriction
407
# name the sympathomimetic drug category
induces vasoconstriction and can increase the force of myocardial contraction;
includes phenylephrine and methoxamine
alpha1 agonists
408
# name the sympathomimetic drug
alpha1 agonist;
used in ocular preparations to induce mydriasis;
used in anaesthesia to increase arterial pressure;
used following anaesthesia in horses as nasal spray to cause vasoconstriction and reduce nasal congestion
phenylephrine
409
# name the sympathomimetic drug category
extensively used in vet med for their sedative nd analgesic properties;
CV effects: incr. SVR leading to reflex bradycardia;
includes: dexmedetomidine, medetomidine, xylazine, detomidine, romifidine
alpha2 agonists
410
# name the sympathomimetic drug
Beta1:
in equine anaesthesia to maintain mean arterial pressure;
used in SA for inotropic support in acute cardiac crisis;
short half life and rapid metabolism;
beta1 > beta2 > alpha1
Dobutamine
411
# name the sympathomimetic drug
beta2 agonist;
used in treatment of R.A.O. in horses;
can induce vasodilation;
growth promoting effect: hypertrophy of muscle fibers, protein deposition and lipolysis in adipose cells
Clenbuterol
412
what are the 2 main effects of beta2 agonists?
| (sympathomimetics)
bronchodilation and uterine relaxation
413
# name the sympathomimetic drug
beta2 agonist;
used in equine anaesthesia to treat hypoxemia due to V/Q mismatch;
can produce tachycardia
Salbutamol
414
# name the sympathomimetic drug
beta2 agonists;
used as a bronchodilator;
more cardiac side effects;
can be used to treat hyperkalemia
Terbutaline
415
# name the sympathomimetic drug
beta2 agonists;
used in the treatment of navicular disease;
induces vasodilation;
used as a tocolytic drug (decr. uterine contraction and delay parturition)
isoxuprine
416
# name the sympathomimetic drug
mixed effects on alpha and beta;
direct and indirect actions;
prone to tachyphylaxis;
used as a bolus to treat hypotension under GA
ephedrine
417
# name the sympathomimetic drug
alpha1-agonist properties (direct) and triggers noradrenaline release (indirect);
used for treatment of urinary incontinence in dogs;
has been used as a nasal decongestant
Phenylpropanolamine
418
# name the adrenoceptor antagonist drug
alpha1 antagonist:
highly selective;
produces vasodilation;
used in treatment of certain urinary tract conditions
Prazosin
419
# name the adrenoceptor antagonist drug
non-selective alpha antagonist:
irreversible, long-acting alpha-antagonist;
predominant alpha1-adrenoceptor blocking effect;
uses: pheochromocytoma stabilization, laminitis
Phenoxybenzamine
420
# name the adrenoceptor antagonist drug
non-selective alpha antagonists:
competitive, short acting;
predominant, alpha1-adrenoceptor blocking effect;
used to treat hypertensive crises;
can cause insulin secretion, leading to hypoglycemia
Phentolamine
421
name the 4 cardinal signs of inflammation
1. redness
2. heat
3. swelling
4. pain (loss of function)
422
name 4 benefits of inflammation
1. incr. blood flow to injured tissue
2. oedema formation (dilution effect)
3. attraction of leukocytes and macrophages
4. antibody production at site of infection
423
name the 4 main uses of anti-inflammatory drugs (control of adverse effects of inflammatory response)
1. analgesia (acute and chronic)
2. anti-pyretic
3. anti-endotoxic effect
4. anti-thrombotic effect
424
# name the inflammatory mediator
released from mast cells, basophils, eosinophils;
causes vasodilation, incr. vascular permeability
histamine
425
# name the inflammatory mediator
originates from plasma, formed from kininogen by factor XII;
causes vasodilation, pain mediator
bradykinin
426
# name the inflammatory mediator
produced by many cell types;
causes gastroprotection, renoprotection, inflammation, reduction of pain threshold
prostaglandins (PGF2alpha, PGD2, PGE2)
427
# name the inflammatory mediator
produced by platelets;
causes platelet aggregation, vasoconstriction
thromboxanes (TXA2)
428
# name the inflammatory mediator
produced by platelets, mast cells;
cause incr. vascular permeability
Leukotrienes (LTB4)
429
# name the inflammatory mediator
produced by WBC, mast cells;
causes platelet aggregation, adherence of leukocytes to endothelium, lysosomal enzyme release
platelet aggregating factor
430
# name the inflammatory mediator
produced by plasma proteins;
cuase chemotaxis, opsonization
complement
431
# name the inflammatory mediator
produced by macrophages and mast cells;
cause initiation of inflammation and chemotaxis, pain mediator
cytokines
432
# name the inflammatory mediator
produced by mast cells and platelets;
cause vasoconstriction
5-HT
433
name the 2 broad groups of NSAIDs
1. enolic acids
2. carboxylic acids
434
what is the mechanism of action for NSAIDs?
inhibit cyclo-oxygenase (COX) enzyme 1 and/or 2
435
# which COX?
contitutive, constant production;
produce PGs involved in normal physiological processes
COX1
436
# which COX?
inducible, produced by inflammatory cells;
produce PGs invlved in inflammation
COX2
437
name 2 NSAIDs which lead to an increased bleeding time
aspirin and ketoprofen
438
name 2 NSAIDs which do NOT lead to increased bleeding time
meloxicam and carprofen
439
where are NSAIDs absorbed well
stomach
440
is metabolism and excretion of NSAIDs in young animals faster or slower?
slower
441
what order of kinetics do most NSAIDs display?
(incr. concentration, faster clearance)
first order kinetics
442
name 5 adverse side effects of NSAIDs (related mainly to inhibition of COX1)
1. GI ulceration
2. nephrotoxicity
3. hepatotoxicity
4. coagulation effects
5. wound healing
443
what species is paracetamol contraindicated in?
they have reduced levels of glutathione, so a much lower toxic dose
cats
444
# name the NSAID
alternatice mechanism of action (COX1, COX2, myeloperoxidase inhibitor);
good anitpyretic and analgesic, poor anti-inflammatory;
metabolism: glucoronidation, conjugaton, N-hydroxylation;
glutathione binds toxic metabolites which would otherwise cause hepatic necrosis
paracetamol
445
# name the NSAID
COX2 selective;
licensed in dogs, cats, horses, cattle, pigs, guinea pigs;
uses: acute and chronic musculoskeletal disorders, postoperative surgical pain, perioperative use;
do NOT use in prgnant or lactating animals OR animals < 6 weeks of age OR cats < 2kg
meloxicam
446
# name the NSAID
COX2 selective;
licensed in dogs, cats, cattle, horses;
uses: postoperative soft tissue/orthopedic pain, OA, perioperative use;
animals < 6 weeks have additional risk
carprofen
447
# name the NSAID
COX2 selective;
dogs and cats;
uses: peri and postoperative use, ST and orthopedic pain, OA;
safety NOT established in pregnancy/lactation, cats <4mo, dogs <2mo, or animals <2.5kg
Robenacoxib
448
# name the NSAID
COX2 selective;
dogs, horses;
uses: postoperative analgesia, OA;
cotraindications: pregnancy and lactation
firocoxib
449
# name the NSAID
COX2 selective;
dogs;
long term analgesia for OA in dogs;
contraindications: <12mo, < 5 kg
Mavacoxib
450
# name the NSAID
COX2 selective;
dogs;
uses: peri and postoperative pain due to orthopedic and soft tissue surgery, OA;
contraindications: <10 weeks, pregnancy and lactation
Cimicoxib
451
# name the equine NSAID
anti-inflammatory > analgesic;
COX1 and COX2;
concentrates in inflammatory exudate;
toxicity: PLE;
not for use in food-producing horses
Phenylbutazone aka "Bute"
452
# name the equine NSAID
prodrug, metabolized to phenylbutazone in liver;
more palatable, reduced GI ulceration;
expensive
Suxibuzone "Danilon"
453
# name the equine NSAID
analgesic dose and "anto-endotoxic" dose;
injectable, use in colic/ST or orthopedic pain
Flunixin
454
# name the equine NSAID
oral paste licensed for ST or orthopedic pain, preoperative use;
COX2 > COX1 ;
licensed in pregnancy;
has food withdrawal
Vedaprofen
455
# name the farm animal NSAID
name 3 farm animal NSAIDs
1. flunixin
2. meloxicam
3. ketoprofen
456
# name the novel drug
non-COX inhibiting, specific prostaglandin receptor antagonist;
specifically targets EP4 receptor therefore minimal side effects;
long-term pain control for OA;
expensive
Grapiprant
457
name 3 NSAIDs licensed for perioperative use
1. meloxicam
2. carprofen
3. robenacoxib
458
what are endogenous corticosteroids produced by
adrenal cortex
459
what are the 2 categories of endogenous corticosteroids
1. mineralocorticoids
2. glucocorticoids
460
what a re endogenous corticosteroids synthesized from
cholesterol
461
where are corticosteroids metabolized
liver
462
what is the active form of cortisone
cortisol
463
what is the active form of prednisone
prednisolone
464
what 4 types of effects do corticosteroids have
1. metabolic effects
2. systemic effects
3. anti-inflammatory effects
4. immune suppressive effects
465
what type of effect do low doeses of corticosteroids have
physiological
466
what type of effect do medium doeses of corticosteroids have
anti-inflammatory
467
what type of effect do high doeses of corticosteroids have
immune suppressive
468
name 5 systemic effects of corticosteroids
1. elevated liver enzymes (dogs)
2. alteration of CNS function
3. PU/PD
4. incr. appetite
5. muscle wastage
469
what do corticosteroids inhibit for effective anti-inflammatory action
inhibit PLA2 (entire AA pathway)
470
name 7 adverse effects of corticosteroids
1. gastric ulceration
2. PU/PD
3. hyperglycemia
4. muscle atrophy
5. osteoporotic effect
6. Cushing's disease
7. suppression of HPA axis
471
name 3 short acting (<24h) glucocorticoids
1. predisolone
2. Prednisone
3. Methylprednisolone
472
name 3 long acting (>24h) glucocorticoids
1. dexamethasone
2. betamethasone
3. triamcinolone
473
# name the corticosteroid
parenteral formulation;
water soluble salts, ideal for IV administration
Dexamethasone
474
# name the corticosteroid
parenteral formulation;
insoluble esters, long acting, IM administration
1. methylprednisolone acetate
2. dexamethasone phenylproprionate / isonicotinate
475
name 5 clinical uses of corticosteroids
1. anti-inflammatory
2. immune-mediated disease
3. neoplasia
4. treatment for hypoadrenocorticism
5n. septic shock
476
name 3 clinical uses of corticosteroids in farm animals
1. termination of pregnancy / induce parturition
2. acute trauma, neuropathies
3. chronic resp. disease
477
what are the two most commonly used classes of anthelmintic drugs in small animal practice
1. Benzimidazoles
2. Macrocylic lactones
478
what do all Benzimidazole drugs licensed for dogs and cats contain (or its prodrug)
| (anthelmintics)
fenbedazole (febental)
479
# name the small animal anthelmintic class
given orally, poorly absorbed from GIT (enhanced with food);
inhibit nematode tubulin polymerization and prevent microtubule formation affecting cellular transpot and energy metabolism;
metabolized in liver and mostly excreted in feces (small amount in urine and milk);
broad spectrum of action agaist nematodes in GIT and resp. tract (both adult and immature);
will treat Giardia;
limited action against cestodes
Benzimidazoles
480
what are the two classes of Macrocyclic lactones
| (anthelmintics)
1. Avermectins
2. Milbemycins
481
# name the small animal anthelmintic class
topical or oral admin;
accumulate in fat so long duration of action;
act on glutamate-gated chloride channels in nerve cells (paralysis);
narrower safety margin in cats;
largely excreted in feces and urine (small amount in milk);
topical products removed by bathing or swimming (harmful to aquatic life);
effective against wide range of nematodes in larval, immature and adult stages;
no activity against cestodes;
some can be used against Diofilaria
Macocytic lactones
482
# name the small animal anthelmintic
available as a spot on preparation for cats only in combination with ectoparasiticides and praziquantel;
slow absorption;
will treat GI nematodes, hookworm and capillaria;
effective against D. immitis larvae but not adults
Eprinomectin (Avermectin)
| (Macrocyclic lactone)
483
# name the small animal anthelmintic
available for both cats and dogs;
applied topically, bathing will not affect efficacy after 2h drying time;
will treat roundworms, hookworms and prevent D. immitis;
some reports of salivation or vomiting in cats after licking site & of alopecia at site
Selamectin (Avermectin)
| (Macrocyclic lactone)
484
# name the small animal anthelmintic
administered orally and largely excreted unchanged in feces;
any that is absorbed will be excreted in bile;
absorbed quickly but eliminated rapidly;
treats GI roundworms, hookworm and whipworm;
can be used as lungworm treatment or prevention
Milbemycin
| (Macrocyclic lactone)
485
what is the available drug for small animals in the Tetrahydropyrimidines class of anthelmintics
Pyrantel
486
# name the small animal anthelmintic
act on nicotinic acetylcholine receptors to initially cause muscle contraction and then paralysis;
giving with food will delay absorption;
max concentration achieved is more important than duration of exposure for effectiveness;
effective against adult and larval stages of GI nematodes;
can be used in puppies and kittens and during pregnancy
Pyrantel
| (Tetrahydropyrimidines)
487
# name the small animal anthelmintic
acts at neuromuscular junction to stimulate presynaptic secretin receptors which causes paralysis of the parasite;
available as a spot on preparation for cats;
effective against GI nematodes, hookworm and A. abstrusus;
absorbed slowly over 2-3 days and thought to be stored in fat;
eliminated slowly in bile and feces
Emodepside
| (Cyclodepsipeptides)
488
# name the small animal anthelmintic
effective against roundworm (adult only);
blocks neuromuscular transmission via GABA-gated chloride channels and causes paralysis of parasite;
rapidly absorbed and metabolized;
wide safety margin, can be used in puppies, kittens and pregnant animals but NOT in animals with liver or renal disease;
should not be used with Pyrantel (agonists)
Piperazine
489
# name the small animal anthelmintic
diphenylether;
may act by uncoupling oxidative phosphorylation and depleting energy;
given orally to dogs only;
causes neurological signs in cats;
broad spectrum of acticity against GI nematodes and some tapeworms;
irritant and can cause vomiting so give whole tablets to dogs
Nitroscante
490
name 4 clinical uses of GnRH
1. induction of follicular growth
2. induction of ovulation
3. improvement of conception rates (cattle)
4. Tx of follicular cysts (dairy cattle)
491
when would you give GnRH in cattle to improve conception rates
11-12 days post-service
492
name the 2 categories of gonadotropins
1. pituitary (FSH, LH)
2. chorionic (CGs)
493
which has a longer half life, FSH/LH or CGs, and why?
CGs because more heavily sialylated (more sialic acid residues)
494
name 5 clinical uses of gonadotropins
1. Induction of ovulation
2. Induction of follicular growth during anestrus
3. Detection of cryptorchidism (horses)
4. Induction of spermatogenesis or enhance libido
5. Induction of superovulation (cattle)
495
what gonadotropin is used to induce ovulation
hCG
496
whih gonadotropins are used to induce follicular growth during anestrus
eCG / rFSH
497
what gonadotropin stimulation test is used for detection of cryptorchidism in horses
hCG
498
which gonadotropins are used to induce spermatogenesis or enhance libido
eCG / rFSH
499
when to start rFSH injections for induction of superovulation in cattle
mid estrus cycle (day 9-14)
500
name 6 indications for use of oxytocin
1. dystocia due to uterine inertia
2. promote uterine involution
3. expulsion of retained fetal membranes (horses)
4. uterine prolapse
5. facilitate clearance of uterine discharge (mares)
6. milk let down
501
name 3 cases where oxytocin is contra-indicated and could lead to uterine rupture if used
1. abnormal fetal position
2. insufficient cervical dilation
3. previous uterine surgery
502
name the two blood proteins that bind reproductive steroids
1. sex hormone binding globulin (SHBG)
2. corticosteroid binding globulin (CBG)
503
what 2 reproductive steroids are bound by sex hormone binding globulin (SHBG)
1. testosterone
2. estradiol
504
what 2 reproductive steroids are bound by Corticosteroid binding globulin (CBG)
1. cortisol
2. progesterone
505
what 2 ways do binding proteins regulate reproductive steroid activity
1. regulating steroid metabolism
2. regulating steroid access to target cells
506
name 2 clinical uses of Progestagens
1. synchroniztion of estrus (cattle)
2. induction of estrus in anestrus animals
507
name 3 adverse effects of progestagens in small animals
1. uterine disorders (endometrial hyperplasia, pyometra)
2. adrenal corticol suppression
3. mammary tumors, pseudopregnancy, exacerbate diabetes
508
what is the main clinical use of PGF2⍺
induction of luteolysis
509
name 3 indications of PGF2⍺ as a luteolytic agent in mares
1. persistent CL
2. termination of pregnancy
3. synchronization of estrus
510
name 6 indications of PGF2⍺ as a luteolytic agent in cattle
1. luteal cysts
2. persistent CL
3. endometritis
4. pyometra
5. termination of pregnancy
6. synchronization of estrus
511
in order to terminate pregnancy, PGF2⍺ must be given before this day of pregnancy in cattle
day 150
512
in order to terminate pregnancy, PGF2⍺ must be given before this day of pregnancy in sheep
day 50
513
in order to terminate pregnancy, PGF2⍺ must be given before this day of pregnancy in horses
day 35
514
what must be present in order for PGF2⍺ to work
responsive CL
515
how far apart should 2 injections of PGF2⍺ be given in order to synchronize estrus in cattle
11 days
516
name 5 adverse effects of PGF2⍺
1. transient sweating
2. mild colic
3. incr. HR
4. incr. resp. rate
5. muscle weakness
517
# name the hormone
induces Lh/FSH release from the pituitary;
stimulates follicular maturation/ovulation
GnRH
518
# name the hormone
FSH/LH agonist which stimulates maturation of follicles
eCG / PMSG
519
these provide exogenous progesterone source to prevent ovulation ("a CL on a stick")
progesterone implants
520
# name the hormone
induces luteolysis
PGF2⍺
