Pharmacology (1-24) Flashcards by Natalie Bubenheim

Q

what does rINN stand for

A

recognised international non-prprietary name

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Q

what does BAN stand for

A

British Approved Name

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Q

what does USAN stand for

A

United States Approved Name

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Q

this determines what the body does to the drug (Absorption, Distrbution, Metabolism, Excretion)

A

pharmacokinetics

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Q

name the 4 parts of pharmacokinetics

A

Absorption
Distribution
Metabolism
Excretion

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Q

this is defined as what the drug does to the body / the relationship to drug concentration at the effect site

A

pharmacodynamics

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Q

name the pharmacokinetic model

helps understanding but is not directly relevant for clinical practice

A

one-compartment model

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Q

name the pharmacokinetic model

describes movement between compartments; drug is only removed from central compartment

A

two-compartment model

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Q

name the pharmacokinetic model

most commonly used to describe clinical scenarios

A

three-compartment model

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Q

name the pharmacokinetic model

drug is eliminated from the body, elimination occurs from central compartment

A

open model

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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

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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

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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

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Q

name 4 pH environments that may lead to ion trapping effect with drugs

A

gastric pH
fetal pH
milk pH
urine pH

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Q

what is the Henderson Hasselbach equation for acids

A

pH - pKa = log(ionized/nonionized)

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Q

what is the Henderson Hasselbach equation for bases

A

pH - pKa = log (nonionized/ionized)

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Q

how to find the pKa of a drug

A

pH at which 50% of the drug is ionized

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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

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Q

name the 3 types of parenteral administration

A

intravenous
intramuscular
subcutaneous

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Q

name the route of administration

most rapid onset of action, rate of administration usually slow

A

intravenous

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Q

name the route of administration

bypasses GIT, achieves sytemic levels more rapidly, advantageous when animal is inappetant or vomiting

A

parenteral

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Q

name the route of administration

often the only option for owners, influenced by speed of gastric emptying and presence of food

A

oral

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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

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Q

what effect does vasoconstriction have on absorption of agent from a site

A

reduces it

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this is an indication of total exposure to the drug, used to define bioavailability, and used to calculate clearance

area under the curve (AUC)

this defines the extent to which an administered does of a drug enters the systemic circulation intact; referred to as F

bioavailability

what is the bioavailability of intravenous drugs

100%

this feature of pharmacokinetics is influenced by movement across membranes, blood flow to different organs, lipid solubility, and plasma protein binding

distribution

this is the main plasma protein drugs bind to

albumin

what is the equation for volume of distribution for a drug

Vd = Dose / C0

this is the peak plasma concentration after equilibrium is achieved and before elemination has begun

C0

this enhances drug access to sites of metabolism

lipid solubility

this enchances possibility of renal excretion of drug

water solubility

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

what are the 3 types of phase 1 biotransformation reactions?

1. hydrolysis 2. reduction 3. oxidation

what are the 3 types of phase 2 biotransformation reactions

1. acetylation 2. glucoronidation 3. conjugation to amino acids

what is the main organ for drug excretion?

kidney

what are the 3 main factors for drug excretion by the kidney

1. water solubility 2. GFR 3. Active Transport

what are the 2 factors for reabsorption of a drug

1. lipid solubility 2. ionisation (ion trapping)

what are the 3 less common routes of drug elimination?

1. biliary 2. skin 3. pulmonary

this is the time taken for the plasma drug concentration to fall by 50%

half-life of elimination

what is the equation for half-life in terms of K (slope of the PDC/time curve)

t 1/2 = 0.693 / K

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

what is the equation for the relationship between half-life and clearance?

t 1/2 = 0.693 x Vd / Cl_B

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

this is where the levels of drug remain stable or consistent from dose to dose

steady state

how many half-lives does it take to reach 95% steady state

5

how many half-lives does it take to reach 99% steady state

7

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

what is the fluctuation within steady state if the dose interval is the same as the half-life

50%

what is the fluctuation within steady state if the dose interval is twice the half-life

75%

name the formula for acids | (pharmacology summary of Formulae)

pH - PKa = log[ionized/non-ionized]

name the formula for bases | (pharmacology summary of Formulae)

pH - PKa = log[non-ionized/ionized]

name the formula for bioavailability | (pharmacology summary of Formulae)

F = AUC oral / AUC IV

name the formula for volume of distribution | (pharmacology summary of Formulae)

Vd = dose/C_0 | (where C_0 = concentration at time 0)

name the formulas for half-life | (pharmacology summary of Formulae)

t 1/2 = 0.693/K t 1/2 = 0.693 x Vd/Cl

name the formula for clearance | (pharmacology summary of Formulae)

Cl = Vd x K

name the formula for dose | (pharmacology summary of Formulae)

Dose = [Cmax] x Vd

this is a macromolecular structure with which the drug reacts; may be a protein, enzyme, nucleic acid, or less specific

drug receptor

this is a drug that binds to a physiological receptor and mimics the effect of the endogenous ligand

agonist

this type of agonist can achieve maximal response even if not all the receptors are occupied

full agonist

this type of agonist is incapable of achieving maximal response even if all the receptors are occupied

partial agonist

this is the tendency of the ligand (drug) to bind to the receptor

affinity

this is a term used to describe how good the drug is at eliciting a response

efficacy

this is a relative term that is often used to compare two drugs - comparing the concentration required to elicit the same response

potency

this is the concentration of the drug required to produce 50% of maximal response

EC 50

these drugs habe affinity but have no instrinsic activity & block the effect of the agonist

antagonist

# name the type of antagonist most important, effects are reversible/surmpuntable by increasing amount of agonist

competitive antagonist

# name the type of antagonist cannot be overcome by increasing amount of agonist; ex: Aspirin

non-competitive antagonist

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

this defines the capacity of a drug to preferentially produce one particular effect

selectivity

this is an absolute term; a drug with this tends to only act on one particular receptor type

specificity

this is the ratio of the dose giving an undesirable effect over the dose required to give the desired effect

therapeutic index

name 4 types of drug receptors

1. ion chanell cell surface transmembrane receptor 2. G protin couple receptor 3. protein kinase 4. cytosolic receptor

this type of drug receptor mediates action of a variety of proteins such as insulin

protein kinases

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

this is when receptors become internalized and degraded within the cell

receptor down-regulation

this is a term used to denote the rapid loss of responsiveness to a drug following intial dosing

tachyphylaxis

what are drug dosing regimens based on?

normal healthy individuals

name 4 things that may cause a dosing regimen to need individualization

1. age 2. species 3. health status 4. concurrent treatment

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

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

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

what is the mode of action for systemic macrocytic lactones? | (ectoparasiticide)

bind to glutamate & GABA-activated chloride channels | (leading to paralysis and death)

do systemic macrocytic lactones have repellent or knock-down activity?

no

name the two main groups of systemic macrocytic lactones

1. Avermectins 2. Milbemycins

what are the 2 main parasites that systemic macrocytic lactones act against

1. Mites (Sarcoptiforms & Demodex & other) 2. Fleas (NOT ticks)

what species are systemic macrocytic lactones used clinically for?

range of species

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)

what type of pyrethroid is Permethrin

type 1 (non alpha-cyano)

what type of pyrethroid is Cypermethrin, Deltamethrin, and Flumethrin?

type 2 (alpha-cyano)

what is the mode of action of Pyrethrins & Pyrethroids? | (ectoparasiticides)

affect voltage-gated sodium channels | (causing hyper-exciitability and death)

what species are Pyrethrins & Pyrethroids used clinically on?

dogs, small mammals, horses, farm animals, poultry

do Pyrethrins & Pyrethroids have repellent or knock-down activity?

yes, good

what adverse effects can type 1 Pyrethroids have?

1. excitation 2. tremors 3. hyperthermia

what adverse effects can type 2 Pyrethroids have?

1. salivation 2. extensor tone 3. incoordination 4. seizures 5. apnea

what is the mode of action for oxadiazines?

blocks neuronal sodium channels | (causing paralysis and death)

do oxadiazines have repellent or knowck-down activity?

no

what species are oxadiazines used for clinically?

dogs and cats

what is the mode of action for phenylpyrazoles? | (ectoparasiticide)

bind to GABA & glutamate-activated chloride channels | (leading to hyper-excitability and death)

name two types of phenylpyrazoles | (ectoparasiticide)

1. fipronil 2. pyriprole

what species are phenylpyrazoles used for clinically?

dogs and cats

does phenylpyrazoles have repellent or knowck-down activity?

no

which ectoparasiticide is topical and spreads in sebum?

phenylpyrazoles

what two species are phenylpyrazoles highly toxic to?

rabbits and fish

what is the mode of action for neonicotinoids? | (ectoparasiticide)

bind to nicotinic acetylcholine receptors | (leading to hyper-excitability, paralysis and death)

do neonicotinoids have repellent or knock-down activity?

no (except nitenpyram has knock-down effect)

what species are neonicotinoids used for clinically?

dogs, cats, small mammals

name 3 types of neonicotinoids

1. nitenpyram 2. imidacloprid 3. dinotefuran

what is the mode of action for isoxazolines? | (ectoparasiticide)

bind to GABA and glutamate-activated chloride channels | (causing hyper-excitability and death)

what parasites are isoxazolines efficient on

1. fleas and other insects 2. Sarcoptes, Demodex & other mites 3. ticks

do isoxazolines have repellent or knock-down activity?

NO

what species are isoxazolines used to treat clinically?

dogs, cats, poultry

what percent are isoxazolines passed out unchanged in feces?

80-90%

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)

what parasties are formamidines effictive against?

1. Sarcoptes, Demodex & other mites 2. ticks

do formamidines have repellent or knock-down activity?

yes, good

what species are formamidines used to treat clinically?

small animals, farm animals

what 3 animals are formamidines contraindicated for?

1. cats 2. horses 3. chihuahuas

what is the mode of action for carbamates and organophosphates?

form complexes with acetylcholinesterases

do carbamates and organophosphates have repellent or knock-down activity?

yes, rapid

name 5 adverse effects of muscarinic overstimulation from organophosphate poisoning

1. Salivation 2. Lacrimation 3. Urination 4. Defecation 5. GI cramps 6. Emesis | (SLUDGE)

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)

which ectoparasiticide can cause irreversible chronic neurotoxicity from long term sub-clinical exposure (ataxia, paresis, paralysis)

carbamates and organophosphates

what species are calcium polysulfides and thiosulphates (lime sulphur) used to treat clinically

cats, horses, SA camelids

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

what parasites are calcium polysulfides and thiosulphates (lime sulphur) effective against in horses?

1. Chorioptes 2. lice

what parasites are calcium polysulfides and thiosulphates (lime sulphur) effective against in SA camelids?

1. Chorioptes 2. Sarcoptes

do calcium polysulfides and thiosulphates (lime sulphur) have repellent or knock-down effects?

NO

name 4 adverse effects of calcium polysulfides and thiosulphates (lime sulphur)

1. skin irritatio 2. malodorous 3. yellow stains 4. oral ulcers if ingested

# 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

# 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

# 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

this is an agent that kills microbes or inhibits their growth without damaging the host

antimicrobials

these are microbial products that kill or inhibit other micro-organisms

antibiotic

these are synthetic agents with activity against bacterial

antibacterial

# name the type of resistance lack of acticity due to inherent phenotype (e.g. lack of target, failure to penetrate cell wall, etc.)

inherent

# name the type of resistance mutations that confer resistance

chromosomal

# name the type of resistance resistance genes on mobile genetic elements (e.g. plasmids)

transferable

what are mycoplasmas resistant to?

beta-lactams

what are anaerobes resistant to?

aminoglycosides

what are aerobes resistant to?

metronidazole

this is the biggest driver of antimicrobial resistance

antimicrobial use

name 3 methicillin resistant staphylocci (MRS) organisms of concern

1. S. pseudointermedius (MRSP) 2. S. schleiferi (MRSS) 3. S. aureus (MRSA)

name 2 multidrug resistant (MDR) cocci organisms of concern

1. Streptococcus 2. Enterococcus

name 2 other multidrug resistant (MDR) organisms of concern

1. Pseudomonas 2. Salmonella

what does nosocomial mean?

healthcare-acquired

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

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

this describes the drug-host interaction (bioavailability, penetration and clearance)

pharmacokinetics (PK)

this describes the drug-target interaction (mode of action)

Pharmacodynamics

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

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)

this type of drug penetrates tissues effectively and are less affected by changes in fluid dynamics and clearance

lipophilic (fat-soluble)

# excellent, good, or poor tissue penetration? Chloramphenicols Fluoroquinolones Minocycline Doxycycline Metronidazole Rifampin

excellent

# excellent, good, or poor tissue penetration? Trimethoprim-sulfonamides Lincosamides Macrolides Tetracyclines

good

# excellent, good, or poor tissue penetration? Beta-lactamase inhibitors Penicillins Cephalosporins Aminoglycosides & aminocyclitols

poor

name 3 concentration dependent antimicrobials

1. most fluoroquinolones 2. aminoglycosides 3. metronidazole

name 2 time dependent antimicrobials

1. penicillins 2. cephalosporans

name 3 antimicrobials with mixed effects for mode of action

1. some fluoroquinolones 2. lincosamides 3. tetracyclines

what is the efficacy of concentration dependent antimicrobials

ratio peak concentration (Cmax) to MIC

what is the efficacy of time dependent antimicrobials

time above MIC

what is the efficacy of antimicrobials with mixed effects

total 24h exposure (area under curve)

what is the dosing for concentration dependent antimicrobials

max dose every 24h

what is the dosing for time dependent antimicrobials

appropriate dose every 8-12h

# Bacteristatic or Bactericidal? Lincosamides Macrolides Chloramphenicols Tetracyclines Trimethoprim Sulphonamides

bacteriostatic

# Bacteriostatic or Bactericidal? Penicillins Cephalosporins Fluoroquinolones Trimethoprim-sulphonamides Aminoglycosides & aminocyclitols Metronidazole

bactericidal

# Bacteriostatic or Bactericidal drugs? may be more effective in seriously immunocompromised patients

Bactericidal drugs

# Bacteriostatic or Bactericidal drugs? may result in less toxin release and toxic shock in staphylococcal and streptococcal infections

Bacteriostatic drugs

# Bacteriostatic or Bactericidal drugs? minimum bactericidal concentration (MBC) is much higher than the MIC

bacteriostatic drugs

# Bacteriostatic or Bactericidal drugs? minimum bactericidal concentration (MBC) is close or identical to the MIC

bactericidal drugs

what is the most serious adverse drug reaction (ADR)

hypersensitivity reactions

what breed has a bred-specific risk of adverse drug reactions to sulphonamides

Dobermans

# name the main route of excretion for these drugs Fluoroquinolones Rifampicin Doxycycline Chloramphenicols

hepatic (liver)

# name the main route of excretion for these drugs Tetracyclines Lincosamides Macrolides Fluoroquinolones Metronidazole

mixed hepatic-renal

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

in these tests: the zones of inhibition around each antimicrobial disc are compared to agreed breakpoints

Kirby-Bauer disc diffusion

in Kirby-Bauer disc diffusion tests, what shows that the infection is susceptible

zone of inhibition (ZI) exceeds the breakpoint

in Kirby-Bauer disc diffusion tests, what shows that the infection is resistant

zone of inhibition (ZI) is less than the breakpoint

these methods determine the lowest concentration of antimicrobial that inhibits bacterial growth

MIC methods

if MIC is (lower or higher?) than the breakpoint the infection is considered susceptible

lower

if MIC is (lower or higher?) than the breakpoint the infection is considered resistant

higher

the capital letters ('S' or 'R' or 'I') on a bacterial AST refer to this

the exact MIC

how to determine which antimicrobial is most effective from an AST

compare breakpoint:MIC ratio (want >1)

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

this breakpoint:MIC ratio means that the efficacy is less likely to be affected by factors that alter tissue concentration

>1

these can be effective in surface and superficial infections & some focal deep infections

topical microbials and antibiotics

name some effective antimicrobials

1. chlorohexidine 2. manuka honey 3. hypochlorous acid 4. polihexanide 5. bleach

these antimicrobials have well established breakpoints, efficacy and saftey; appropriate for empirical treatment

first line antimicrobials

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

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

# what line are these antibiotics? Penicillins Ampicillin & amoxicillin 1st & 2nd gen. cephalosporins Clindamycin & lincomycin Tetracyclines Trimethoprim-sulphonamides Spiramycin Metronidazole

first line antimicrobials

# what line are these antimicrobials? 3rd gen. cephalosporins Fluoroquinolones Florfenicol (in cattle)

2nd line antimicobials

# 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

# name the common antimicrobial combination high tissue perfusion; effective against gram- anaerobes, anaerobes, staphylococci and most gram+ aerobes (except streptococci)

Fluoroquinolone & Metronidazole

# name the common antimicrobial combination low tissue penetration; effective against gram- aerobes, most anaerobes and gram+ aerobes

Aminoglycoside & Amoxicillin-clavulanate

# name the common antimicrobial combination mixed tissue penetration; effective against gram- aerobes, most anaerobes & gram+ aerobes

Aminoglycoside & Lincosamides

# name the common antimicrobial combination Mixed tissue penetration; effective against gram- aerobes, most anaerobes and gram+aerobes; high potential for AMR

Fluroquionolone & Amoxicillin-clavulanate

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

this is the treatment of the whole group including infected and non-infected animals; may be considered to prevent the spread of disease

metaphylaxis

what is the mode of action for penicillins

disrupt bacterial cell wall causing lysis (penicillin-binding proteins - PBP)

what bacteria are penicillins most active against

gram-pos bacteria

name 3 categories of penicillins

1. narrow spectrum penicillins 2. aminopenicillins 3. anti-staphylococcal pennicillins

amoxicillin is often combined with this beta-lactamase inhibitor

clavulanic acid

some bacterial PBPs act as beta-lactamases to cleave the beta-lactam ring and inactivate this class of antibiotics

penicillins

name 3 types of beta-lactamase inhibitors

1. clavulanic acid 2. sulbactam 3. tazobactam

# name the antibiotic class inhibit beta-lactamases and enhance activity for penicillins susceptible to these enzymes

beta-lactamase inhibitors

how are cephalosporins classed? | (antibiotic)

generations (1G, 2G, 3G, 4G)

what is the mode of action for cephalosporin antibiotics?

similar to penicillins (disrupt the bacterial cell wall causing lysis)

what bacteria type are Cephalosporins NOT active against

enterococci (limited against anaerobes)

what is the mode of action for lincosamides and macrolides? | (antibiotics)

bind to 50S ribosome subunit to prevent protein synthesis

name 2 types of lincosamides | (antibiotics)

1. clindamycin 2. lincomycin

what type of bacteria are lincosamides and macrolides most effective against?

gram-positive bacteria

what type of bacteria are lincosamides and macrolides NOT effective against?

gram-negative bacteria

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

what is the mode of action for Trimethoprim-sulphonamide ? | (antibiotics)

block folic acid synthesis (required for purine and pyrimidine synthesis)

name an adverse effect of trimethoprim-sulphonamide

very bitter - salivation and foaming (cats)

what type of bacteria are trimethoprim-sulphonamides most effective against (moderate activity)

gram-positive bacteria

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)

what 3 things is resistance to fluoroquinolones associated with | (antibiotics)

1. decreased cell permeability 2. efflux pumps 3. altered topoisomerases

what is the mode of action for aminoglycosides | (antibiotics)

block protein synthesis at 30S ribosome subunit

what type of bacteria are aminoglycosides most effective against

gram-neg bacteria

list the 6 aminoglycosides in order of most to least efficacy | (antibiotics)

amikacin > tobramycin > gentamycin > neomycin = kanamycin > streptomycin | aktgnks

what 2 things is resistance to aminoglycosides associated with | (antibiotics)

1. modification of ribosome binding site 2. efflux pumps

this is an antibiotic closely related to aminoglycosides; lack most of the systemic toxicity assoc. with aminoglycosides BUT chromosomal resistance can occur rapidly

aminocyclitols

what is the mode of action for tetracyclines | (antibiotics)

block protein synthesis through 30S ribosome subunit

name 5 types of tetracyclines | (antibiotics)

1. tetracycline 2. chlortetracycline 3. oxytetracycline 4. doxycycline 5. minocycline

name 3 things resistance to tetracyclines is associated with | (antibiotics)

1. multiple genes for efflux 2. ribosome binding 3. drug modification

what is the mode of action for chloramphenicols | (antibiotics)

disrupt protein synthesis through 30S and 50S subunits

what type of bacteria are chloramphenicols most effective against

anaerobes

what is resistance to chloramphenicols associated with

drug inactivating enzymes

what is the major adverse effect of chloramphenicols | (antibiotics)

fatal aplastic anemia in humans

what is the mode of action for metronidazole | (antibiotics)

disrupts DNA strands and inhibits repair enzyme (DNAase-1)

what conditions are required for metronidazole to be effective? what is the only type of bacteria metronidazole is effective against

anaerobic

what is an adverse effect of metronidazole | (antibiotics)

bitter - inappetance and hypersalivation (cats)

what is the mode of action for rifampicin | (antibiotics)

inhibits RNA polymerase and DNA transcription

what type of bacteria is rifampicin NOT effective against | (antibiotics)

gram-negative

what is an adverse effect of rifampicin | (antibiotics)

red-orange discoloration of bodily fluids

what is the mode of action for nitrofurans | (antibiotics)

disrupts mRNA translation (from intracellular bacterial metabolism)

what type of bacteria is nitrofurantoin NOT effective against | (antibiotics)

anaerobes

what type of infection is nitrofurantoin (nitrofurans) restricted to and why

UTIs bc of rapid renal excretion

what are 3 adverse effects of nitrofurans | (antibiotics)

1. erythema 2. pruritic 3. oedema (also toxicity and carcinogenic potential)

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

# 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

# name the topical antibiotic acts on gram-pos bacteria by inhibitng cell wall peptoglycan synthesis

bacitracin

# 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

# name the topical antibiotic blocks nucleic acid synthesis; active against gram-pos bacteria

novobiocin

# 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

what is the initial treatment choice for most fungal infections?

Azoles (imidazoles and triazoles)

what is the mode of action for azoles | (antifungal)

inhibit ergosterol synthesis disrupting fungal cell wall metabolism

are azoles fungistatic or fungicidal?

fungistatic

which azole's absorption is not affected by food | (antifungal)

Fluconazole

whih azole's absorption is decreased with food | (antifungal)

voriconazole

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

what is the most common adverse effect of azoles | (antifungal)

GIT upset

what is the mode of action for Allylamines (terbinafine) | (antifungal)

blocks ergosterol synthesis through inhibition of aqualene epoxidase

are allylamines (terbinafine) fungistatic or fungicidal?

fungicidal

what type of fungi are allylamines (terbinafine) effective against

dermatophytes

is absorption of allylamines (terbinafine) affected by food? | (antifungal)

no

how are allylamines (terbinafine) excreted | (antifungal)

hepatic metabolism

name 2 common polyenes | (antifungal)

nyastatin and natamycin

what is the mode of action for polyenes | (antifungal)

disrupt fungal cell membranes by occupying ergosterol binding sites

are polyenes fungistatic or fungicidal

fungicidal

what type of fungi are polyenes used for

superficial fungal infections only (Malassezia and Candida)

what is the mode of action for griseofulvin | (antifungal)

inhibits mitosis, nucleic acid synthesis and cell wall metabolism

is griseofulvin fungistatic or fungicidal?

fungistatic

what type of fungi is griseofulvin mainly used for

dermatophytosis in horses

# name the antifungal fungicidal; poorly absorbed by GI tract so must be given parenterally; dose-related nephrotoxicity

Amphotericin B

# 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

# 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

what is the mode of action for Acyclovir, Famiciclovir, Ixouridine, and Remdesivir? | (antiviral)

nucleoside analogues that inhibit DNA/RNA synthesis

what is Acyclovir most commonly used alongside to increase anti-viral effect | (antiviral)

recombinent feline IFN-omega OR human IFN-alpha

what s Famiciclovir used systemically for? | (antiviral)

FHV-1 infections

what is ixouridine used to treat? | (antiviral)

topically in FHV-1

what is Remdesivir used to treat and how long must it be given? | (antiviral)

FIP (give SQ or IV for over 12 weeks)

what is the mode of action of amantidine? | (antiviral)

block M2 protein ion channels to prevent endocytosis

what type of viruses is amantidine active against | (antiviral)

enveloped RNA viruses

what is teh mode of action for L-lysine | (antiviral)

peptide, competitive inhibitor of arginine

what is L-lysine used for in cats | (antiviral)

FHV-1

# 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

# 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

name 2 mycobacterial derived immunomodulators | (antiviral)

1. Bacille Calmett-Guerin (BCG) 2. Regressin-V

name the 4 nucleoside analogue DNA/RNA synthesis inhitors used in animals | (antiviral)

1. acyclovir 2. famciclovir 3. idoxuridine 4. remdesivir | AFIR

name a peptide antiviral drug used in animals

L-lysine

what does VMR stand for?

veterinary medicines regulations

what does VMD stand for?

veterinary medicines directorate

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)

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)

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)

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)

who should adverse drug reactions be reported to

veterinary medicines directorate (VMD) | (under SARSS)

what 3 things make it ideal to use licensed veterinary products

1. safety 2. quality 3. efficacy

name the 6 steps involved in drug development

1. pre-discovery 2. discovery 3. pre-clinical testing 4. clinical trials 5. licensing 6. marketing

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)

# 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)

# 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)

# 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)

# 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)

this is an assessment of relevant clinical information, which may include an examination of the animal

"clinical assessment"

# which step of 'the cascade' ? Veterinary medicine with a Marketing Authorisation valid in GB or UK wide for indicated species and condition

step 1

# which step of 'the cascade' ? Veterinary medicine with a Marketing Authorisation valid in NI for indicated species and condition

step 2

# 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

# 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

# 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

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

if the withdrawal period is not specified on a veterinary medicine, what should it be set at for meat

not less than 28 days

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

this is a means of defining the product, its dose and other relevant instructions

prescription

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”

what does the abbreviation od mean in prescriptions

once daily (omni die)

what does the abbreviation sid mean in prescriptions

once daily (semel in die)

what does the abbreviation bd mean in prescriptions

twice daily (bis die)

what does the abbreviation tid mean in prescriptions

three times daily (ter in die)

what does the abbreviation qid mean in prescriptions

four times daily (quarter in die)

what does the abbreviation pc mean in prescriptions

after food (post cibum)

what does the abbreviation ac mean in prescriptions

before food (ante cibum)

what does the abbreviation prn mean in prescriptions

when required (pro re nata)

are controlled drugs regulated under the VMR (veterinary medicines regulation)?

no

# 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

# 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

# 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

# name the schedule of controlled drugs Exempt from most of the restrictions of controlled drugs; (ex: benzodiazepines and anabolic substances)

schedule 4

# 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

what 3 things must you record on obtaining a schedule 2 drug

1. date 2. name and address of supplier 3. amount obtained

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

how long are controlled drug prescriptions valid for?

28 days

how long should incoming and outgoing transaction records of POM-V and POM-VPS drugs be kept for

5 years

# 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

products including these 3 agents are not included in the exemption scheme for small pet animals

1. antibiotics 2. narcotics 3. psychotropics

how long is a prescription for medicated feedstuffs valid for

3 months

name 5 categories of feed additives

1. technological additives 2. sensory additives 3. nutritional additives 4. zootechnical additives 5. coccidostats and histomonostats

these can be defined as a substance used to maintain animals in good health or favorably affect their performance

feed additives

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)

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

name 4 features the permanent building for storing medicines must have

1. secure 2. clean 3. vermin proof 4. refridgerated space with temp monitoring

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

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

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

these are drugs that stimulate postsynaptic muscarinic receptors; their actions resemble acetylcholine and they are also referred to as cholinergics or parasympathetic agonists

parasympathomimetics

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

# adrenergic or cholinergic? all presynaptic efferent autonomic fibers and the somatic motor fibers

cholinergic

what do most postsynaptic sympathetic fibers release

noradrenaline

what is the effect of the sympathetic nervous system on the heart?

increased activity (beta1) | (rate, strength, conduction)

what is the effect of the sympathetic nervous system on blood vessels

vasoconstriction (alpha1 and alpha2)

what is the effect of the sympathetic nervous system on the iris

dilation of pupil (mydriasis) (alpha1)

what is the effect of the sympathetic nervous system on the bronchi?

relaxation (beta2)

what is the effect of the sympathetic nervous system on the GIT

decreased activity (alpha1&2, beta1&2)

what is the effect of the sympathetic nervous system on the adrenal medulla

secretion (adrenaline)

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

what is the synthesis step of adrenergic neurotransmission?

1. Tyrosine converted to Dopa by tyrosine hydroxylase 2. Dopa converted to dopamine

what is the storage step of adrenergic neurotransmission?

1. dopamine transported into synaptic vessel by VMAT 2. dopamine converted to NE in the vesicle

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

what can block the release of noradrealine in adrenergic neurotransmission

botulinum toxin | (cleaves SNARE proteins in neurons)

what can be used to block the reuptake of noradrenaline by the norepinephrne transporter (NET)

tricyclic antidepressants

# 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

# name the adrenergic receptor Presynaptic nerve terminals: 1. inhibits norepinephrine release 2. inhibits ACh release 3. inhibits insulin release | (Gi)

Alpha2 receptors

# name the adrenergic receptor Heart and Kidneys: 1. incr. heart rate 2. incr. cardiac contractility and stroke 3. incr. renin release | (Gs)

Beta1 receptors

# 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

# name the adrenergic receptor Adipose Tissue: 1. sdipose tissue lipolysis 2. decr. urination | (Gs)

Beta3 receptors

what is the effect of the parasympathetic nervous system on the heart

decr. activity | (M2 > M3)

what is the effect of the parasympathetic nervous system on the blood vessels

vasodilation | (M2)

what is the effect of the parasympathetic nervous system on the iris

contraction of pupil (myosis) | (M2, M3)

what is the effect of the parasympathetic nervous system on the bronchi

constriction | (M2 = M3)

what is the effect of the parasympathetic nervous system on the GIT

incr. activity | (M2=M3)

what is the effect of the parasympathetic nervous system on the adrenal medulla

no effect

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)

what is the storage step of cholinergic neurotransmission

1. ACh transported into large, clear vesicles by VAT along with neuropeptides and ATP

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

what can the release of ACh from the nerve terminal be blocked by

botulinum toxin

how many muscarinic receptors are there

5 (M1-M5)

what do muscarinic receptors M1, M4, and M5 act on

CNS

what does muscarinic receptor 2 act on

heart (reduces HR)

what does muscarinic receptor 3 act on

smooth muscle (contract)

# 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

# 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

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

what do direct acting agonists or antagonists act on | (adrenergic drugs)

one or more postsynaptic adrenergic receptors (alpha1&2, beta1&2)

# name the type of adrenergic drug increase release of NE or inhibit reuptake or block metabolising enzyme

indirect acting agonists

name 2 ways a drug acting on the ANS can interfere with degradation of neurotransmitter

1. inhibit degradation enzyme 2. inhibit neurotransmitter reuptake

name 2 ways a drug acting on the ANS can interfere with neurotransmitter biosynthesis

1. inhibit precursor uptake 2. inhibit enzyme for biosynthesis

what are the ACh receptors

nicotinic and muscarinic

what are teh 3 main types of nicotinic receptors

1. muscle (NMJ) 2. ganglionic (ANS) 3. CNS (brain)

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)

name 4 choline ester drugs (direct muscarinic agonists) | (parasympathomimetics)

1. ACh 2. Methacholine 3. Bethanecol 4. Carbachol

what receptor do choline esters have a direct action on?

muscarinic receptors

# name the choline ester drug (muscarinic agonist - parasympathomimetic) mainly muscarinic; used inhaled for bronchial reactivity diagnosis

methacholine

# 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

# 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

name 3 types of alkaloid drugs (direct muscarinic agonists) | (parasympathomimetics)

1. pilocarpine 2. muscarine 3. arecoline

# 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

these are indirectly acting parasympathomimetics; they inhibit AChE to incr. ACh activity; have a cholinergic effect initially but prolonged depolarization may have desensitization

anticholinesterases

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)

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)

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

# name the anticholinesterase (indirect parasympathomimetic) very short acting quaternary ammonium compound; reversal of non-depolarizing muscle relaxants; diagnosis of myasthenia gravis

Edrophonium chloride 'tensilon'

# 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

# name the anticholinesterase (indirect parasympathomimetic) moderat duration; more lipid soluble; treatment of myasthenia gravis (orally: BID)

Pyridostigmine

# 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

# 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)

# 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

# name the anticholinergic drug (muscarinic antagonist) bronchodilation in horses (R.A.O.); inhalation - poor absorption therefore minimal side effects

Ipratopium bromide

# name the anticholinergic drug (muscarinic antagonist) mydriatic and cycloplegic; long duration of action

cyclopentolate

# 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

name 3 naturally occuring catecholamines | (sympathomimetics)

1. adrenaline 2. noradrenaline 3. dopamine

# 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

# name the sympathomimetic drug alpha effects > beta1 effects > beta2 effects; primarily a vasopressor via alpha stimulation; used to treat hypotension

noradrenaline

# name the sympathomimetic drug acts at dopamine receptors alpha- and beta-adrenoceptors; dose dependent effect; mixed effects in practice; used to treat hypotension

dopamine

what is the effect of dopamine at low doses

dopa effects: 1. vasodilation 2. incr. renal perfusion and filtration

what is the effect of dopamine at medium doses

beta effects: positive inotropy and chronotropy

what is the effect of dopamine at high doses

alpha effects: vasoconstriction

# name the sympathomimetic drug category induces vasoconstriction and can increase the force of myocardial contraction; includes phenylephrine and methoxamine

alpha1 agonists

# 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

# 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

# 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

# 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

what are the 2 main effects of beta2 agonists? | (sympathomimetics)

bronchodilation and uterine relaxation

# name the sympathomimetic drug beta2 agonist; used in equine anaesthesia to treat hypoxemia due to V/Q mismatch; can produce tachycardia

Salbutamol

# name the sympathomimetic drug beta2 agonists; used as a bronchodilator; more cardiac side effects; can be used to treat hyperkalemia

Terbutaline

# 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

# 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

# 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

# name the adrenoceptor antagonist drug alpha1 antagonist: highly selective; produces vasodilation; used in treatment of certain urinary tract conditions

Prazosin

# name the adrenoceptor antagonist drug non-selective alpha antagonist: irreversible, long-acting alpha-antagonist; predominant alpha1-adrenoceptor blocking effect; uses: pheochromocytoma stabilization, laminitis

Phenoxybenzamine

# 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

name the 4 cardinal signs of inflammation

1. redness 2. heat 3. swelling 4. pain (loss of function)

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

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

# name the inflammatory mediator released from mast cells, basophils, eosinophils; causes vasodilation, incr. vascular permeability

histamine

# name the inflammatory mediator originates from plasma, formed from kininogen by factor XII; causes vasodilation, pain mediator

bradykinin

# name the inflammatory mediator produced by many cell types; causes gastroprotection, renoprotection, inflammation, reduction of pain threshold

prostaglandins (PGF2alpha, PGD2, PGE2)

# name the inflammatory mediator produced by platelets; causes platelet aggregation, vasoconstriction

thromboxanes (TXA2)

# name the inflammatory mediator produced by platelets, mast cells; cause incr. vascular permeability

Leukotrienes (LTB4)

# name the inflammatory mediator produced by WBC, mast cells; causes platelet aggregation, adherence of leukocytes to endothelium, lysosomal enzyme release

platelet aggregating factor

# name the inflammatory mediator produced by plasma proteins; cuase chemotaxis, opsonization

complement

# name the inflammatory mediator produced by macrophages and mast cells; cause initiation of inflammation and chemotaxis, pain mediator

cytokines

# name the inflammatory mediator produced by mast cells and platelets; cause vasoconstriction

5-HT

name the 2 broad groups of NSAIDs

1. enolic acids 2. carboxylic acids

what is the mechanism of action for NSAIDs?

inhibit cyclo-oxygenase (COX) enzyme 1 and/or 2

# which COX? contitutive, constant production; produce PGs involved in normal physiological processes

COX1

# which COX? inducible, produced by inflammatory cells; produce PGs invlved in inflammation

COX2

name 2 NSAIDs which lead to an increased bleeding time

aspirin and ketoprofen

name 2 NSAIDs which do NOT lead to increased bleeding time

meloxicam and carprofen

where are NSAIDs absorbed well

stomach

is metabolism and excretion of NSAIDs in young animals faster or slower?

slower

what order of kinetics do most NSAIDs display? (incr. concentration, faster clearance)

first order kinetics

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

what species is paracetamol contraindicated in? they have reduced levels of glutathione, so a much lower toxic dose

cats

# 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

# 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

# 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

# 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

# name the NSAID COX2 selective; dogs, horses; uses: postoperative analgesia, OA; cotraindications: pregnancy and lactation

firocoxib

# name the NSAID COX2 selective; dogs; long term analgesia for OA in dogs; contraindications: <12mo, < 5 kg

Mavacoxib

# 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

# 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"

# name the equine NSAID prodrug, metabolized to phenylbutazone in liver; more palatable, reduced GI ulceration; expensive

Suxibuzone "Danilon"

# name the equine NSAID analgesic dose and "anto-endotoxic" dose; injectable, use in colic/ST or orthopedic pain

Flunixin

# name the equine NSAID oral paste licensed for ST or orthopedic pain, preoperative use; COX2 > COX1 ; licensed in pregnancy; has food withdrawal

Vedaprofen

# name the farm animal NSAID name 3 farm animal NSAIDs

1. flunixin 2. meloxicam 3. ketoprofen

# 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

name 3 NSAIDs licensed for perioperative use

1. meloxicam 2. carprofen 3. robenacoxib

what are endogenous corticosteroids produced by

adrenal cortex

what are the 2 categories of endogenous corticosteroids

1. mineralocorticoids 2. glucocorticoids

what a re endogenous corticosteroids synthesized from

cholesterol

where are corticosteroids metabolized

liver

what is the active form of cortisone

cortisol

what is the active form of prednisone

prednisolone

what 4 types of effects do corticosteroids have

1. metabolic effects 2. systemic effects 3. anti-inflammatory effects 4. immune suppressive effects

what type of effect do low doeses of corticosteroids have

physiological

what type of effect do medium doeses of corticosteroids have

anti-inflammatory

what type of effect do high doeses of corticosteroids have

immune suppressive

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

what do corticosteroids inhibit for effective anti-inflammatory action

inhibit PLA2 (entire AA pathway)

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

name 3 short acting (<24h) glucocorticoids

1. predisolone 2. Prednisone 3. Methylprednisolone

name 3 long acting (>24h) glucocorticoids

1. dexamethasone 2. betamethasone 3. triamcinolone

# name the corticosteroid parenteral formulation; water soluble salts, ideal for IV administration

Dexamethasone

# name the corticosteroid parenteral formulation; insoluble esters, long acting, IM administration

1. methylprednisolone acetate 2. dexamethasone phenylproprionate / isonicotinate

name 5 clinical uses of corticosteroids

1. anti-inflammatory 2. immune-mediated disease 3. neoplasia 4. treatment for hypoadrenocorticism 5n. septic shock

name 3 clinical uses of corticosteroids in farm animals

1. termination of pregnancy / induce parturition 2. acute trauma, neuropathies 3. chronic resp. disease

what are the two most commonly used classes of anthelmintic drugs in small animal practice

1. Benzimidazoles 2. Macrocylic lactones

what do all Benzimidazole drugs licensed for dogs and cats contain (or its prodrug) | (anthelmintics)

fenbedazole (febental)

# 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

what are the two classes of Macrocyclic lactones | (anthelmintics)

1. Avermectins 2. Milbemycins

# 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

# 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)

# 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)

# 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)

what is the available drug for small animals in the Tetrahydropyrimidines class of anthelmintics

Pyrantel

# 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)

# 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)

# 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

# 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

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)

when would you give GnRH in cattle to improve conception rates

11-12 days post-service

name the 2 categories of gonadotropins

1. pituitary (FSH, LH) 2. chorionic (CGs)

which has a longer half life, FSH/LH or CGs, and why?

CGs because more heavily sialylated (more sialic acid residues)

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)

what gonadotropin is used to induce ovulation

hCG

whih gonadotropins are used to induce follicular growth during anestrus

eCG / rFSH

what gonadotropin stimulation test is used for detection of cryptorchidism in horses

hCG

which gonadotropins are used to induce spermatogenesis or enhance libido

eCG / rFSH

when to start rFSH injections for induction of superovulation in cattle

mid estrus cycle (day 9-14)

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

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

name the two blood proteins that bind reproductive steroids

1. sex hormone binding globulin (SHBG) 2. corticosteroid binding globulin (CBG)

what 2 reproductive steroids are bound by sex hormone binding globulin (SHBG)

1. testosterone 2. estradiol

what 2 reproductive steroids are bound by Corticosteroid binding globulin (CBG)

1. cortisol 2. progesterone

what 2 ways do binding proteins regulate reproductive steroid activity

1. regulating steroid metabolism 2. regulating steroid access to target cells

name 2 clinical uses of Progestagens

1. synchroniztion of estrus (cattle) 2. induction of estrus in anestrus animals

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

what is the main clinical use of PGF2⍺

induction of luteolysis

name 3 indications of PGF2⍺ as a luteolytic agent in mares

1. persistent CL 2. termination of pregnancy 3. synchronization of estrus

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

in order to terminate pregnancy, PGF2⍺ must be given before this day of pregnancy in cattle

day 150

in order to terminate pregnancy, PGF2⍺ must be given before this day of pregnancy in sheep

day 50

in order to terminate pregnancy, PGF2⍺ must be given before this day of pregnancy in horses

day 35

what must be present in order for PGF2⍺ to work

responsive CL

how far apart should 2 injections of PGF2⍺ be given in order to synchronize estrus in cattle

11 days

name 5 adverse effects of PGF2⍺

1. transient sweating 2. mild colic 3. incr. HR 4. incr. resp. rate 5. muscle weakness

# name the hormone induces Lh/FSH release from the pituitary; stimulates follicular maturation/ovulation

GnRH

# name the hormone FSH/LH agonist which stimulates maturation of follicles

eCG / PMSG

these provide exogenous progesterone source to prevent ovulation ("a CL on a stick")

progesterone implants

# name the hormone induces luteolysis

PGF2⍺