Pharmacology Flashcards

1
Q

FDA approved proprietary drug

A

safety and efficacy with good laboratory practices
active ingredient, product were manufactured under good lab practices in FDA inspected facilities
therapeutic consistency, product quality, accurate shelf life, scientifically substantiated labeling

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2
Q

brand name vs pharmaceutical ingredient

A

brand name is capitalized
ingredient is lowercase

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3
Q

steps for drug approval

A
  • drug concept is formed
    • investigational new animal drug number assigned
  • dosage regimen determined
  • target animal safety (1x, 2x, 3x, 5x for 90 days)
  • effectiveness (field trial)
  • human food safety (food animal)
  • chemistry, manufacturing, controls
  • environmental impact
  • new animal drug application # (on box)
  • post-marketing surveillance
    • crucial! report adverse effects to FDA
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4
Q

VPCR

A

veterinary client patient relationship

vet has examined the animal, developed a prelim diagnosis, and determined the need for the drug

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5
Q

Schedule 1 drug

A

highest potential for abuse

no medical use

lack of accepted safety

none in vet med (heroin)

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6
Q

schedule II drug

A

high potential for abuse

accepted for medical use with severe restrictions

may lead to severe psychological or physical dependence

morphine

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7
Q

schedule III drug

A

potential for abuse

accepted for medical treatment

abuse may lead to moderate or low physical dependence

ketamine

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8
Q

schedule IV drug

A

potential for abuse

accepted for medical use

may lead to limited dependence

diazepam

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9
Q

schedule V drugs

A

low potential for abuse

accepted for medical use

may lead to limited dependence

gabapentin

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10
Q

generic drugs

A

FDA approved

ANADA abbreviated

bioequivalent

may have brand name

prescription or OTC

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11
Q

generic vs brand name drugs

A

generic= lower cost

different excipients (inactive ingredients)

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12
Q

excipients

A

inactive ingredients

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13
Q

compounded drugs

A

HAVE NOT been tested for bioequivalence, efficacy, safety, strength

may not be manufactured under GMP in federally inspected plants

are NOT approved by FDA

ex: mixing injectables, crushing pills for an oral suspension

changing concentration to fit size of patient

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14
Q

NDC numbers

A

national drug code

approved for a species, not necessarily for your species

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15
Q

dose

A

quantity of a medicine or drug taken at a particular time

total mg or mg/kg

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16
Q

dosage

A

quantity and frequency of a dose of medicine or drug

mg/kg/day, mg/kg every 12 hours

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17
Q

dosage regimen

A

includes the route of administration and duration of dosing

mg/kg IV every 12 hours for 7 days

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18
Q

pharmacodynamics (PD)

A

what the drug does to the body

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19
Q

pharmacokinetics (PK)

A

what the body does to the drug

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20
Q

pharmacogenetics

A

how genes affect responses to drugs

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21
Q

chemotherapy

A

effect of drugs upon microorganisms, parasites, and neoplastic cells living and multiplying in an organism

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22
Q

toxicology/toxic effects

A

study of undesirable effects of chemicals on living systems

result from excessive pharmacological action due to overdose or prolonged usage

may occur in some patients at therapeutic dose

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23
Q

side effects

A

drug action outside the desired site

may be good or bad

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24
Q

adverse drug reaction

A

relates to change in patient

similar to adverse drug effect

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25
Q

adverse drug effect

A

relates to effect of the drug

similar to adverse drug reaction

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26
Q

adverse drug event

A

occurs while a patient is on a drug

causality has not been determined

may or may not be related to drug

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27
Q

dose-response curve for most drugs

A

Magnitude of pharmacologic response is proportionately related to the (log of) drug concentration at the tissue (receptor) site

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28
Q

phase 2 dose response curve

A

linear response with desired effect

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29
Q

phase 1 dose response curve

A

no response observed

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30
Q

dose response curve phase 3

A

no increased response seen, toxic effects possible

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31
Q

ED50

A

Effective dose in 50% of a population

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32
Q

TD50

A

Toxic dose in
50% of a population

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33
Q

LD50

A

Lethal dose in
50% of a population

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34
Q

Therapeutic index

A

Ratio of TD50 to the ED50

Provides some indication of drug safety

The larger (wider) the index, the safer the drug

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35
Q
A

A

wider therapeutic index

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36
Q

most common drug receptor

A

GPCRs

increase/decrease enzyme activity

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37
Q

tachyphylaxis

A

acute tolerance of a drug after only a few doses

need break from the drug for it to work

38
Q

tolerance

A
  • Decreasing response to repeated constant doses of a drug
  • May be pharmacokinetic or dynamic

ex: opioid

39
Q

affinity

A

• Force of attraction between drug
and receptor
• Higher affinity drugs are harder to displace

works for longer, needs higher, more frequent doses of reversal

40
Q

selectivity

A

Specificity of the drug for the target receptor binding

ex: epinephrine (least selective) binds to most sympathetic receptors while dobutamine (more selective) only binds to 2

41
Q

why is selectivity important?

A
  • Stronger effects on the target receptor
  • Fewer effects on unwanted receptors (side effects)
42
Q

potency

A
  • Comparative term
  • Describes the concentration of different drugs necessary to induce the same magnitude of response
43
Q

True or False:
A more potent drug is a better drug.

A

false

44
Q

efficacy

A

MOST IMPORTANT

intrinsic activity

ability of a drug to have a response

complex relationship btwn drug concentration, receptor activation, cellular response

45
Q

agonist

A

receptor interaction results in activation

magnitude of effect is proportional to the # of receptors occupied

46
Q

partial agonist

A

binds and activates a receptor

only results in partial response

maximal response not observed

lower efficacy

47
Q

antagonist

A

drug interacts selectively with receptor but it lacks intrinsic efficacy

blocks or reduces action of an agonist at the receptor

48
Q

competitive vs non competitive antagonists

A
  • Competitive: Looks like the drug– binds at the same site
  • Non-competitive: Binds somewhere else (allosteric site), Changes receptor conformation so the agonist can’t bind

usually to reverse agonist drugs

49
Q

reversible antagonists

A

• Binds to receptor (affinity) but can easily dissociate from the
receptor
• H-bonds, van der waals = all weak/reversible
• Agonist present at sufficiently high concentrations can displace
an antagonist
• Decreases potency because a higher concentration is now necessary to induce the same response

50
Q

irreversible antagonist

A

Binds and stays
• Covalent bonds
• Agonist response can not occur until the receptor is replaced and any remaining unbound antagonist has been removed from the body
• Decreases efficacy preventing the maximal possible response

51
Q

inverse agonists

A

bind and has negative response

confused with antagonist in literature

52
Q

chemical antagonism

A

Direct chemical interaction between two drugs (i.e., a weak acid and weak base)

53
Q

physiologic antagonism

A

Two drugs act in the same physiologic system but act on different receptors or
pathways

54
Q

pharmacokinetic antagonism

A

One drug alters the response to another drug through changes in disposition

55
Q

molecular weight affect on drug transfer

A

smaller = increased

56
Q

lipid solubility affect on drug transfer

A

higher solubility = higher transfer

57
Q

pKa affect on drug transfer

A

unionized= higher transfer

58
Q

protein binding affect on drug transfer

A

lower = higher drug transfer

59
Q

concentration gradient affect on drug transfer

A

higher= higher drug transfer

60
Q

end receptor for parasympathetic NS

A

muscarinic

61
Q

end receptor for sympathetic NS

A

adrenergic

62
Q

neurotransmitters for the PNS

A

acetylcholine

63
Q

SNS neurotransmitters

A

norepinephrine, epinephrine (from adrenal gland)

64
Q

parasympathomimetic

A

aka cholinergic

agonists at muscarinic receptors in PNS

mimic ACh

65
Q

parasympatholytic

A

antagonists at muscarinic receptors

aka anticholinergic

block ACh

66
Q

M1 receptors effect:

A

forebrain,

PNS effector cells,

gastric mucosa,

neurons,

cerebral cortex

67
Q

M2 receptors effects:

A

heart, PNS effector cells, cardiac muscles

68
Q

M3 receptors effect

A

smooth muscle, exocrine

intestinal smooth muscle and glands

69
Q

M4 receptors

A

neostriatum, spinal cord, involved in pain

70
Q

M5 receptors

A

brain, dopamine response

71
Q

classes of Parasympathomimetic drugs

A

Cholinergic agonists
Anticholinesterases

72
Q

Cholinergic agonists

A

Mimic the action of acetylcholine

73
Q

Anticholinesterases

A

Inhibit the destruction of acetylcholine by blocking acetylcholinesterase

74
Q

In general, parasympathomimetic drugs stimulate muscles to contract or relax in target organs? What are the exceptions?

A

contract

S alivation

L acrimation

U rination

D efecation

D igestion

except HR- slows HR, slow breathing

75
Q

clinical uses of parasympathomimetic drugs

A
  • Stimulate GI motility and gastric emptying
  • Stimulate bladder emptying
  • Constrict the pupil (some forms of glaucoma)
76
Q

In general, parasympatholytic drugs relax or contract muscles in target organs?

A

Relax

A nhidrosis (lack of sweating)

B lurry vision (mydriasis/dry eye)

D ry mouth (decreased salivation)

U rine retention

C onstipation (ileus)

T achycardia

77
Q

parasympatholytic drugs clinical uses

A
  • Cause bronchodilation
  • Stop diarrhea
  • Antiemetics (stop vomiting)
  • Cause mydriasis (pupil dilation)
  • Treat bradycardia (low heart rate)
78
Q

major subtypes of sympathetic drugs

A

alpha adrenergic (a1 and a2)

beta adrenergic (b1 and b2)

79
Q

sympathomimetics

A

agonists at these receptors

adrenergic agonists

80
Q

sympatholytics

A

adrenergic antagonists/blockers

Drugs that act as antagonists

Block the actions of the sympathetic nervous system

Most drugs in this class will be specific for either alpha or beta receptors

81
Q

3 classes of sympathomimetic drugs

A

direct acting

indirect acting

dual acting

82
Q

direct acting sympathomimetic drugs

A

Directly stimulate adrenergic receptors

83
Q

indirect acting sympathomimetic drugs

A

Stimulate the release of NE from nerve endings in the synapse

84
Q

dual acting sympathomimetic drugs

A

Directly stimulate adrenergic receptors and Stimulate the release of NE from nerve endings in the synapse

85
Q

alpha 1 adrenergic receptor

A

main location: blood vessels, eye

main agonist actions: vasoconstriction, pupil dilation

main clinical uses: hypotension, antiarrhythmic, mydriasis

main adverse effects: Hypertension, Arrhythmias, CNS stimulation

86
Q

alpha 2 agonist drugs

A

main location: CNS, pancreas

main agonist actions: Decreased sympathetic outflow, Decreased NE release, Decreased insulin secretion

main clinical uses: sedative, analgesic, muscle relaxation, anxiolysis

main adverse effects: Initial hypertension which results in baroreceptor-mediated reflex bradycardia (As the peripheral effects diminish, central alpha-2 actions predominate, leading to decreased blood pressure and cardiac output)
• Arrhythmias
• Vomiting (particularly in cats!)
• Increased urine output
• Transient hyperglycemia
• Increased myometrial tone and intrauterine pressure 25

***stim of alpha 2 cause sympathetic inhibition!!

87
Q

beta 1 adrenergic agonist drugs

A

main location: heart, kidney

main agonist actions: increased HR, increased heart contractility, increased renin release

main clinical uses: hypotension, anesthesia/shock, bradycardia

main adverse effects: hypertension, tachycardia, arrhythmias

88
Q

beta 2 adrenergic agonist drugs

A

main location: lungs (we have 2 lungs), uterus, blood vessels (but not brain/skin

main agonist actions: bronchodilation, uterine relaxation, vasodilation

main clinical uses: Respiratory disease/asthma, Delaying parturition

main adverse effects: Tachycardia/myocardial necrosis, CNS excitement, Muscle tremors

89
Q

alpha 1 antagonists

A

• Treat congestive heart failure/hypertension; urine retention

90
Q

alpha 2 antagonists

A

Reverse the sedation and bradycardic effects of alpha-2 agonists

91
Q

beta 1 antagonists

A

treat congestive heart failure

92
Q

beta 2 antagonists

A
  • No specific uses
  • Most beta-1 antagonists have beta-2 antagonist ability

• Use with caution in asthmatic patients (cause bronchoconstriction)