Pharmacology Flashcards

1
Q

Define

One-compartment model of pharmacokinetics

A

Assumes the drug is evenly distributed thoughout the body and the rate of elimination (k) is constant

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2
Q

Define

Two-comparment model of pharmacokinetics

A

Assumes a drug is taken up by different tissues and the volume of distribution between tissues is different

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3
Q

In the context of comparment models, a drug is only eliminated through the __ comparment

A

Central

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4
Q

Which compartment model best represents what happens in the body

A

Multi-comparment model

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5
Q

Define

Open model

A

The drug is eliminated from the body through the central compartment

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6
Q

Define

Closed model

A

The drug is recirculated in the body through entero-hepatic circulation

This is rare

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7
Q

Define

Zero order kinetics

A

The rate at which {drug} changes is constant and independent of drug concentration

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8
Q

Define

First order kinetics

A

The rate of drug elimination is proportional to the {drug}

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9
Q

List 4 factors influencing the movement of drugs in the body

A
  1. Physiochemical properties
  2. Location/target tissue
  3. Mechanism of transport
  4. pH & ion trapping

Remember, drugs cross membranes in their non-ionized form

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10
Q

Define

Pharmacokinetics

A

What the body does to the drug

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11
Q

Define

Pharmacodynamics

A

What the drug does to the body

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12
Q

What are the 4 phases of drug pharmacokinetics

Think of the acryonym

A
  1. Absorption
  2. Distribution
  3. Metabolism
  4. Excretion

ADME

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13
Q

List 3 routes of parenteral drug administration

A
  1. Intravenous
  2. Intramuscular
  3. Subcutaneous
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14
Q

Define

Absorption

A

The passage of the drug from the site of administration to the blood stream

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15
Q

Explain

First pass effect

A

Describes how a % of drug is lost as it goes through the liver and portal vein to enter systemic circulation

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16
Q

How can you avoid the % of drug loss associated with the first pass effect

A

By administering the drug rectally or sublingually

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17
Q

Which protein does a drug bind to in the blood?

A

Albumin

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18
Q

Define

Volume of distribution (Vd)

And what is it directly related to?

A

The amount of tissue to which a drug distributes

Plasma concentration

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19
Q

What does a Vd of >2kg/kg indicate?

A

That drug is accumulationg in a specific site or fatty tissue

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20
Q

Where does biotransformation primarily occur?

A

The liver

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21
Q

Where does excretion primarily occur?

A

The kidney

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22
Q

Describe the components of

Phase I reactions

Part of biotransformation

A

Includes hydrolysis, reduction and oxidation

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23
Q

Describe the components of

Phase II reactions

Part of biotransformation

A

Conjugation (includes acetylation, conjugation to amino acids, and glucuronidation)

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24
Q

What is C0?

In the context of volume of distribution

A

The drug plasma concentration after equilibrium but before elimination

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25
Q

Define antimicrobial

A

Agent that kills microbes or inhibits their growth without damaging the host

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26
Q

Define antibiotic

A

Microbial products that kill or inhibit other micro-organisms

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27
Q

Define antibacterial

A

Synthetic agents with activity against bacteria

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28
Q

__ do not cause AMR

A

Antimicrobials

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29
Q

Define inherent resistance

Provide an example

A

Lack of bacterial activity due to inherent phenotype (i.e., lack of appropriate target)

Mycoplasms are resistant to beta-lactams because they do not have a cell

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30
Q

Define chromosomal resistance

What type of transmission is this?

A

Mutations in the organism that confer resistance

Vertical transmission

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31
Q

Define transferable resistance

What type of transmission is this?

A

Resistance genes aquired through mobile genetic elements

Vertical and horizontal transmission

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32
Q

List 3 AMR organisms of concern

A
  1. Methicillin resistant staphylococci
  2. Multidrug resistant cocci
  3. Multidrug resistant enterbacteriacae
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33
Q

Define a nosocomial infection

A

An infection aquired through health care

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34
Q

List 3 risk factors for nosocomial AMR

(aquired through healthcare)

A
  1. Very young or old animals
  2. Immunocomprimised patients
  3. Broad spectrum antibacterial use
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35
Q

What are the 3 most important drivers for antimircobial use in practice?

A
  1. Vet prescribing behaviours
  2. Interactions with clients
  3. Practice norms
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36
Q

List 5 conditions in which system antimicrobials are not needed as a first line treatment

A
  1. Acute vomiting or diarrhoea
  2. Otitis externa
  3. Acute conjunctivitis
  4. Cat bite abscesses
  5. Feline lower urinary tract disease
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37
Q

List the 7 key concepts for responsible antimicrobial use

A
  1. Know there is a bacterial infection
  2. Do you need systemic AM’s?
  3. Is treatment required immediately?
  4. Choose an appropriate AM
  5. Use the correct dose
  6. Choose the correct treatment duration
  7. Improve compliance
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38
Q

List 6 factors affecting PK/PD models

A
  1. Poor bioavailability
  2. Hypovolumic shock
  3. Renal and/or liver disease
  4. Increased MIC
  5. Biofilms
  6. Pus, debris or foregin materials
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39
Q

List 3 factors that may necessitate the need for higher doses of hydrophilic drugs to ensure theraputic concentrations

A
  1. Fluid retention
  2. IV fluids
  3. Increases renal clearance

Means theres an alt fluid balance, drugs may be diluted or excreted fast

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40
Q

__ drugs penetrate tissues more effectively

A

Lipophilic

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41
Q

List one antimicrobial for each category of tissue penetration: excellent, good and poor

A

Excellent: Doxycycline, metronidazole
Good: Tetracyclines, macrolides
Poor: Penicillins, cephalosporins

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42
Q

List a concentration dependent drug

A

Most fluoroquinolones

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43
Q

How is the efficacy of concentration dependent drugs measured?

A

The ratio between the peak concentration and the MIC

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44
Q

How would you dose a concentration dependent drug?

A

Give the maximum dose every 24 hours

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45
Q

List a time dependent drug

A

Penicillin

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46
Q

How do you measure the efficacy of a time dependent drug?

A

Time above MIC

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47
Q

How would you dose a time dependent drug?

A

Give the appropriate dose every 8-12 hours

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48
Q

List one advantage for both bactericidal and bacteriostatic drugs

A

Bactericidal: more effective in immunocomprimised patients
Bacteriostatic: release less toxins

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49
Q

List 3 bacteriostatic drugs

A
  1. Tetracycline
  2. Sulphonamides
  3. Lincosamides
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50
Q

List 3 bactericidal drugs

A
  1. Penicillin
  2. Cephalosporin
  3. Fluoroquinolones
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51
Q

Which dog breed have a specific risk for ADRs to sulphonamides?

A

Dobermans

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52
Q

List 3 drugs that are excreted hepatically

A
  1. Fluoroquinolones
  2. Doxycycline
  3. Rifampicin
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53
Q

List 3 drugs that are excreted both hepatically and renally

A
  1. Tetracyclines
  2. Lincosamides
  3. Fluoroquinolones
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54
Q

List 3 drugs are excreted renally

A
  1. Penicillins
  2. Cephalosporines
  3. Trimethoprim-sulphonamides
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55
Q

List 3 ADRs you can see with tetracyclines

A
  1. Injection site reactions
  2. Hepatic enzyme induction
  3. Oesophageal ulceration
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56
Q

List a pathogen that is most likely causes this infection

Pyoderma

A

Staphylococci

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57
Q

List a pathogen that is most likely causes this infection

Otitis externa

A

Staphylococci or pseudomonas

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58
Q

List a pathogen that is most likely causes this infection

Otitis media

A

Staphylococci or pseudomonas

59
Q

List a pathogen that is most likely causes this infection

Cystitis

A

E. coli

60
Q

List a pathogen that is most likely causes this infection

Prostatitis

A

E. coli

61
Q

List a pathogen that is most likely causes this infection

Gingivites & periodontitis

A

Spirochetes

62
Q

List a pathogen that is most likely causes this infection

Cholangio-hepatitis

A

E. coli

63
Q

List a pathogen that is most likely causes this infection

Anal sacs

A

E. coli or enterococcus

64
Q

List a pathogen that is most likely causes this infection

Conjunctivitis in cats

A

Chlamydophilia felis

65
Q

List a pathogen that is most likely causes this infection

Conjunctivitis in dogs

A

Staphylococci or streptococci

66
Q

List a pathogen that is most likely causes this infection

Upper respiratory tract infection

A

Bordatella

67
Q

List a pathogen that is most likely causes this infection

Pneumonia pyothorax in dogs

A

Gram negative aerobes

68
Q

List a pathogen that is most likely causes this infection

Pneumonia pyothorax in cats

A

Pasturella

69
Q

List a pathogen that is most likely causes this infection

Mastitis

A

E. coli

70
Q

List a pathogen that is most likely causes this infection

Septicaemia

A

Staphylococci or e.coli

71
Q

Define

Catecholamine

Provide 3 examples

A

A monoamine transmitter derived from the amino acid tyrosine

Adrenaline, noradrenaline and dopamine

72
Q

Define

Chronotropic

A

An agent that increases heart rate

73
Q

Define

Dromotropic

A

An agent that affects conduction speed by changing the delay in the AV node

74
Q

Define

Positive dromotrophy

Provide an example of something that does this

A

Something that increases conduction velocity

Adrenaline

75
Q

Define

Negative dromotrophy

Provide an example of something that does this

A

Something that decreases conduction velocity

Vagal stimulation

76
Q

Define

Inotropic

A

An agent that increases the force of contraction

77
Q

Define

Sympathomimetic drugs

A

Drugs with similar actions to the post-ganglionic fibers of the CNS

Also known as adrenergics (they resemble adrenaline)

78
Q

Define

Sympatholytic drugs

A

Drugs that oppose the actions of the post-ganglionic fibers of the SNS

Also known as anti-adrenergics or sympathetic antagonists

79
Q

Define

Parasympathomimetic drugs

A

Drugs that stimulate post-synaptic muscarinic receptors

Also known as cholinergics (they resemble acetlycholine)

80
Q

Define

Parasympatholytic drugs

A

Drugs that oppose the actions of the PNS at the muscarinic receptors

Also known as anti-cholinergics

They do this by blocking the actions of acetylcholine

81
Q

Define

Adrenergic direct acting agonists/agonists

A

Agents that can act at one or more post-synaptic adrenergic receptors

82
Q

Define

Adrenergic indirect acting agonists

A

Agents that increase the release of NE or inhibit its uptake

83
Q

What is the action of mixed acting sympathomimetics

A

They indirectly release noradrenaline and directly activate receptors

84
Q

What are the 2 main neurotransmitters of the ANS

A
  1. Acetylecholine (parasympathetic)
  2. Noradrenaline (sympathetic)
85
Q

All pre-synaptic autonomic fibers and somatic motor fibers are __

A

Cholinergic (stimulated by acteylcholine)

86
Q

What is the function of dopamine as a neurotransmitter in the ANS

A

It is a modulatory transmitter in some ganglia, the enteric NS and renal blood vessels

87
Q

Noradrenaline has a higher affinty for __

A

Alpha receptors

88
Q

Adrenaline has a higher affinity for __

A

Beta receptors

89
Q

What is the final product in most sympathetic post-synpatic neurons

A

Noradrenaline

90
Q

List 5 key features of neurotransmitter function that provide targets for drugs

A
  1. Synthesis
  2. Storage
  3. Release
  4. Binding to receptor
  5. Termination
91
Q

How does adrenaline treat anaphylaxis?

I.e., what receptors does it act on?

A

Alpha-1: increases vasoconstriction and peripheral vascular resistance
Beta-1: increases iontropy and chronotropy
Beta-2: increases bronchodilation and decreases release of inflammatory mediators

92
Q

What is the cellular response following the activation of M1, M3 and M5 muscarinic receptors?

A

Activation of PLC (phospholipase C)

93
Q

What is the cellular response following the activation of M2 and M4 muscarinic receptors?

A

Deactivation of AC (adenylate cyclate)

94
Q

List the class and action of the following PNS drug

Acetylcholine

A

Choline ester (direct muscarinic agonist)
Negative chronotropy, inotropy and dromotropy in the cardiovascular system

95
Q

List the class and action of the following PNS drug

Methacholine

A

Choline ester (direct muscarinic agonist)
Treats bronchial reactivity

96
Q

List the class and action of the following PNS drug

Bethanechol

A

Choline ester (direct muscarinic agonist)
Induces urination (minimal cardiac effects)

97
Q

List the class and action of the following PNS drug

Carbachol

A

Choline ester (significant nicotinic action)
Induces gastric motility, urination and miosis

98
Q

List the class and action of the following PNS drug

Pilocarpine

A

Alkaloids (direct muscarinic agonist)
Induces miosis (used to treat glaucoma)

99
Q

Which class of PNS drugs do anticholinesterases belong to?

A

Indirect muscarinic agonists

100
Q

Describe the action of anticholinesterases

A

They inhibit acetylcholinesterase to increase acetylcholine activity at the post synaptic membrane

101
Q

List the 2 categories of anticholinesterases

A
  1. Reversible
  2. Irreversible
102
Q

List 6 toxic effects of anticholinesterases

SLUDGE

A
  1. Salivation
  2. Lacrimation
  3. Urination
  4. Defecation
  5. GI distress
  6. Emesis

Also muscle tremors, miosis and collapse

103
Q

How can anticholinesterases reverse a neuromuscular block?

A

Anticholinesterases increase the amount of Ach at the NMJ, which can out compete the competitive antagonists for the Ach receptors

104
Q

List the class and action of the following PNS drug

Edrophonium chloride

A

Anticholinesterase
Used in the diagnosis of myasthenia gravis, and reverses non-depolarizing muscle relaxants

105
Q

List the class and action of the following PNS drug

Neostigmine

A

Anticholinesterase
Treatment of myasthenia gravis, and reverses non-depolarizing muscle relaxants

106
Q

List the class and action of the following PNS drug

Pyridostigmine

A

Anticholinesterase
Treatment of myasthenia gravis

107
Q

List the class and action of the following PNS drug

Atropine

A

Anticholingeric (natural muscarinic antagonist)
Increases heart rate, used with anticholinesterases to prevent side effects from reversing neurmuscular blockade, and induces mydriasis

108
Q

List 3 adverse effects of atropine

A
  1. Tachycardia
  2. Urinary retention
  3. Decreases gastric secretion

Can be a problem with CNS stimulation in the horse

109
Q

List the class and action of the following PNS drug

Scopolamine

A

Anticholinergic (natural muscarinic antagonist)
Antispasmadic and antiemetic

110
Q

List the class and action of the following PNS drug

Glycopirrolate

A

Anticholinesterase (synthetic muscarinic antagonist)
Used to prevent and treat bradycarida (has much milder effects than atropine)

111
Q

List the class and action of the following PNS drug

Ipratopium bromide

A

Anticholinergic
Bronchodilation in horses

112
Q

List the class and action of the following PNS drug

Cyclopentolate

A

Anticholinergic
Induces mydriasis (cyclopelgic)

113
Q

List the class and action of the following PNS drug

Tropicamide

A

Anticholinergic
Induces mydriasis (NOT cyclopelgic)

114
Q

How is norepinephrine inactivated at the synaptic junction?

A

By reuptake into the pre-synaptic cell

115
Q

What is the precursor of norepinephrine?

List the 3

A

Tyrosine -> dopa -> dopamine

116
Q

Adrenoreceptors and muscarinic receptors are __ receptors

A

G-protein coupled

117
Q

Where is this receptor located

Alpha-1

A

Vascular smooth muscle

118
Q

Where is this receptor located

Alpha-2

A

CNS

119
Q

Where is this receptor located

Beta-1

A

Heart

120
Q

Where is this receptor located

Beta-2

A

Smooth muscle

121
Q

Where is this receptor located

Beta-3

A

Adipose tissue

122
Q

Where is this receptor located

M1

A

CNS and stomach

123
Q

Where is this receptor located

M2

A

Heart

124
Q

Where is this receptor located

M3

A

Glands and smooth muscle

125
Q

Where is this receptor located

M4

A

CNS and heart

126
Q

Where is this receptor located

M5

A

CNS

127
Q

List 3 naturally occuring sympathomimetics

Aka SNS agonists

A
  1. Adrenaline
  2. Noradrenaline
  3. Dopamine
128
Q

List the class and action of the following SNS drug

Adrenaline

A

SNS agonist
Acts on alpha and beta receptors to increase HR, force of contraction and vasoconstriction (used for cardiac arrest and anaphylaxis)

129
Q

List the class and action of the following SNS drug

Noradrenaline

A

SNS agonist
Primarily acts on alpha receptors to induce vasoconstriction, also beta receptors to increase contractility

130
Q

List the class and action of the following SNS drug

Dopamine

A

SNS agonist
At low doses, acts on dopa receptors to cause vasodilation
At medium doses, acts on beta receptors to increase strength and rate of heart
At high doses, acts on alpha receptors to cause vasoconstriction

131
Q

List the class and action of the following SNS drug

Phenylephrine

A

Alpha-1 agonist
Induces mydriasis and increases arterial pressure

132
Q

What are the general effects of alpha-1 agonists

A

They induce vasoconstriction and increase the force of contraction

133
Q

What are the general effects of alpha-2 agonists

A

They increase systemic vascular resistance and cause vasoconstriction

Also used for sedative and analgesic properties

134
Q

What are the general effects of beta-1 agonists

A

They increase heart rate and the force of contraction

135
Q

List the class and action of the following SNS drug

Dobutamine

A

Beta-1 agonist
Used in equine anaesthesia to maintain arterial pressure, and small animal surgery to increase heart strength

136
Q

List the class and action of the following SNS drug

Clenbuterol

A

Beta-2 agonist
Used for the treatment of recurrent airway obstruction in horses (bronchodilation and vasodilation)

137
Q

List the class and action of the following SNS drug

Terbutaline

A

Beta-2 agonist
Used for bronchodilation and to treat hyperkalemia

138
Q

List the class and action of the following SNS drug

Salbutamol

A

Beta-2 agonist
Used in equine anaesthesia to treat hypoxaemia

139
Q

List the class and action of the following SNS drug

Isoxuprine

A

Beta-2 agonist
Induces vasodilation and decreases uterine contraction to delay parturition

140
Q

What are the general effects of beta-2 agonists

A

Bronchodilation and uterine relaxation

141
Q

List the class and action of the following SNS drug

Prazosin

A

Alpha-1 antagonist
Induces vasodilation and promotes urine output

142
Q

What is the general effect of alpha-2 antagonists

A

They reverse sedation induced by alpha-2 agonists

143
Q

List the class and action of the following SNS drug

Phenoxybenzamine

A

Non-selective alpha antagonist
Long-acting alpha-1 adrenoreceptor blocker

144
Q

List the class and action of the following SNS drug

Phentolamine

A

Non-selective alpha antagonist
Short-acting alpha-1 adrenoreceptor blocker