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Intro to Pharmacology > Week 5 - Analgesics > Flashcards

Week 5 - Analgesics Flashcards

1
Q

CNS Pharmacology:

A

how drugs alter brain activity and offset pathology

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2
Q

NeuroPharmacology:

A

how drugs act on neurons at cellular/molecular level

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3
Q

PsychoPharmacology:

A

how drugs modify behavior, perception, affect a thought

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4
Q

In the last three decades, dramatic advances have been made in ?

A

CNS pharmacology

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5
Q

Regrettably, recent developments are not that good. Why?

A

Large pharm companies severely restricting
neuropsychiatric drug development efforts citing

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6
Q
A
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7
Q

Drug is defined as

A

A substance used to prevent or treat conditions associated with stimulation or depression
of the brain associated with both mental and physical processes

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8
Q

Describe the therapeutic Importance of drugs.

A
  • Relieve pain and fever
  • Suppress disorders of movement or seizures
  • Induce sleep or arousal
  • Reduce desire to eat
  • Inhibit motion sickness
  • Treat anxiety, mania, depression
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9
Q

Prescription Drug is defined as

A

A drug that is limited to use under the supervision of a veterinarian
because of potential danger, difficulty of administration, or other indications

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10
Q

Controlled Drug is defined as

A

Drugs that have a potential for abuse or dependence;
classified into schedules according to their level of abuse potential

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11
Q

Drugs act like ________, transferring _____-______ messages
between ______ in the brain and spinal cord.

A

neurotransmitters, electro-chemical, neurons

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12
Q

Drugs can _____-___ the transfer of these signals and are called ?

A

speed - up, CNS stimulants

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13
Q

Drugs can slow - down the transfer and are called ?

A

CNS depressants

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14
Q

CNS drugs act on ______ receptors that modulate
_______ ______.

A

specific, synaptic transmission

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15
Q

Some nonspecific agents (such as ______, ________) have
____-______-mediated actions that result in
alterations in synaptic transmission

A

alcohol, anesthetics, non-receptor

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16
Q

DRUGS can alter the function of CNS to provide:

A

Analgesia: narcotic (opioids) and non-narcotic (NSAIDs & NMDA receptor antagonists)
* Tranquilization (sedation) effects
* Anticonvulsant effects
* Antiemetic effects
* Anxiolytic, sedative, and hypnotic
* General anesthetic effects
* Behavior changes: CNS stimulants
CNS Depressants (antidepressants, anxiolytic drugs)

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17
Q

CNS Drugs
Actions

A
  • Pharmacokinetics
  • Pharmacodynamics
  • Drug distribution
  • Target tissues and stimulation (CNS: depression or stimulation
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18
Q

Agonists:
* Bind to and ______ target tissue (CNS)

A

stimulate

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19
Q

Antagonists:
* Bind to target tissue but

A

don’t stimulate

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20
Q

Different things can happen to result in drug action.
5. Release of NT into synapse cleave?
After communciation with receptor on post-synaptic neuron

A
  1. The action potential in the presynaptic fiber
  2. Synthesis of the NT
  3. Storage
  4. Metabolism
  5. Release
  6. Reuptake
  7. Degradation
  8. Post-synaptic receptor
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21
Q

Drugs can act on synthesis, storage, metabolism, uptake, release. Retrograde signalling we won’t be discussing.

Glial cells can also participate in some functions of the synapse communication.

Cocaine blocks uptake of catecholamine which are dopamine, serotonin, and norepinephrine. Adrengeric synapses?
ACh is ?
Post-synaptic region provides primary site of drug action and things can happen here to interfere with real signaling.

A
  1. Action potential in presynaptic fiber
  2. Synthesis of neurotransmitter (NT)
  3. Storage
  4. Metabolism
  5. Release
  6. Reuptake into the presynaptic neuron or glial cell
  7. Degradation
  8. Receptor for the NT
  9. Receptor-induced increase/decrease in ionic conductance
  10. Retrograde signaling
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22
Q

Main targets for neuro-active drugs:

A

 Ion channels
 Receptors
 Enzymes
 Transport proteins

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23
Q

Most of the targets occur in several different _______ _____,
giving rise to subtle differences in function and pharmacology

A

molecular isoforms

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24
Q

Slowly developing secondary responses to the primary interaction of the drug
with its target are often important (delayed efficacy of antidepressants,
tolerance and dependency with opioids).

A
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25
Q

The term BBB denotes the highly-selective barrier separating the brain tissue from the blood circulation.

A

A lot of drugs are unable to pass the BBB.

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26
Q

The main function of the BBB is the ?

A

protection of CNS against toxins, pathogens and even NTs (glutamate)

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27
Q

The BBB consists of a _______ layer of _______ cells joined by _____ ______
and surrounded by _______l.

A

continuous, endothelial, tight junctions, astrocytes

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28
Q

Circulating drugs must cross BBB in order to gain access to the neurons of the brain

A
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29
Q

DRUGS that can cross the BBB:
 ____ in molecular size (Examples?)
 Lipid ____ (________)
 _____ bound to protein
 Non- ______ at the ___ of cerebrospinal fluid (CSF)
 _____ or ____-mediated transfer (L-DOPA)

A

Small, CO2, caffeine, nicotine, heroin, soluble, lipophilicity, Poorly, ionized, pH, Diffusion, carrier

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30
Q

The BBB tends to increase in ________ in the presence of ________ or at the site of ____

A

permeability, inflammation, tumor

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31
Q

The BBB is poorly developed in ______; hence, chemicals can easily gain access
to the ________ _____.

A

neonates, neonatal brain

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32
Q

Analgesic drugs are used to inhibit ______ processing at different levels

A

pain

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33
Q

Goal of therapy: ?

A

reduction of transduction, transmission, modulation, and perception of pain

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34
Q

Pain: is an unpleasant ____ and _____ experience associated with ____ or ____ tissue damage. Pain has been recognized for its contribution to ____ and _____

A

sensory, emotional, actual, potential, morbidity, mortality

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35
Q

Classes of Pain
Duration

A
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36
Q

Classes of Pain
Location

A
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37
Q

Pain processing System

A
  1. Transduction
  2. Transmission
  3. Modulation
  4. Perception
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38
Q

Pharmacological Intervention of Pain Processing

A
39
Q

Opioids are?

A

Derivatives of opium (poppy plant)

40
Q

Opium: extract from the ______ ______ ____ of unripe bulbs
of the _____ plant contains morphine and codeine.

A

white milky sap, poppy

41
Q

The active chemical compounds in opium are _____ and _____

A

Morphine,Codeine

42
Q
A

Difference between morphine and codeine are their chemical structure. Pay attention to this.

43
Q

Opiates: _____ drugs derived from opium ____ or semi- ______ derivatives
with narcotic properties. Opiates can be ____ or ____.
Representatives: ?

A

narcotic, poppy, synthetic, Natural, unnatural

opium, morphine, heroin (3x > potent)

44
Q

Opioids: ___-synthetic or ___-synthetic ____ drugs that mimic the natural ____.
Not found in ____.
Representatives: ?

A

fully, semi, narcotic, opiate, nature
hydrocodone, oxycodone, fentanyl, tramadol

45
Q

Endogenous opioid neuropeptides: ?

A

endorphins, enkephalins, dynorphins are
release by the neuroendocrine cells to activate receptors

46
Q
A

CH2 methyl group allows it to be lipophyllic and can cross BBB.

47
Q

Opioids are _______ substances
except for _____ and ______ (partial agonist)

A

Controlled, antagonists, nalbuphine

48
Q

Administering Opiods:
Routes of Administration: ?

A

IV, IM, SC, oral, rectal, transdermal, subarachnoid, and epidural

49
Q

PK: Metabolized in the liver and excreted in the urine
* Wide margin of safety (dogs don’t ask for prescription or go to black market)
 Cats are deficient in the metabolic pathway, the t1/2 of most opioids in cats may be prolonged
 The elimination t1/2 is 1 hr in dogs, 3 hr in cats, and 1.5 hr in horses

A
50
Q

Opiods
* Produce _____ and _____
* _____ induction when combined with other drugs
* Classified as ____ agonists, _____ agonists, mixed ?

A

analgesia, sedation, Anesthetic, full, partial, agonist-antagonists

51
Q

Opiod Uses:
Analgesia

A

Analgesia
* Prevent and treat postoperative pain
* Used with tranquilizers to produce neuroleptanalgesia

52
Q

Opiods Pre-anesthetic

A

agonists, partial agonists, or mix agonist-antagonists (agonistic effect on one receptor, antagonistic on another receptor)
* May be used alone or in combination with
- Tranquilizers
- Anticholinergics

She said this was VERY important.

53
Q

Opiods mimic ?
* May be used ____ or in combination with?

A

agonists, partial agonists, or mix agonist-antagonists
alone
- Tranquilizers
- Anticholinergics

54
Q

Opioids
Pharmacological effects: _____ and ____ but depend on many factors

A

Analgesia, sedation

55
Q

Opioids in dogs —> ?

A

Dogs: sedation
narcosis

56
Q

Opioids in cats, horses, and ruminants —> ?

A

Cats, horses, and ruminants:
may cause CNS stimulation
bizarre behavior patterns or dysphoria

57
Q

Opioids MOA
* Bind to the receptors in the ____ and ____ _____ and mediate the ____
of _______ and ______ secretion
* Stimulate ____ receptors [?]
* Each opioid has a different ____ at each receptor
* Receptors are present in ?

A

brain, spinal cord, inhibition, neurotransmission, endocrine, opioid, mu (μ), kappa (κ), and delta (Δ), action, numerous cells/ tissues

58
Q

Name the analgesics that are agonists

A

Morphine, hydromorphone, oxymorphone (10 times >), fentanyl (75-125 times > potent), tramadol (<)

59
Q

Name the analgesics that are Partial Agonists

A

Buprenorphine, Butorphanol (μ-receptor)

60
Q

Name the analgesics that are Mixed Agonist-Antagonists

A

Butorphanol (partial μ-receptor agonist and agonist for k-receptor)
Nalbuphine (agonist for k-receptor and antagonist for the μ-receptor)
Buprenorphine (μ-partial, k-antagonist)

61
Q

Name the analgesics that are antagonists

A

Naloxone and Naltrexone

62
Q

All opioid receptors are __-____ receptors that mediate the inhibition of _______
and ______ secretion.

A

G-coupled, neurotransmission, endocrine

63
Q

μ-receptors are present in the brain, spinal cord and, when bound, lead to?

A

Spinal and supraspinal analgesia
euphoria
mild sedation
miosis
respiratory depression
chemical dependence
inhibition of Ach and dopamine release decrease in GI motility

64
Q

κ-receptors are present in the cerebral cortex, spinal cord and other brain regions and, when bound, lead to?

A

Spinal and supraspinal analgesia
sedation
dysphoria
diuresis
miosis

65
Q

Δ-receptors are present in the limbic system, cerebral cortex, and spinal cord and, when bound, lead to ?

A

Spinal and supraspinal analgesia
inhibition of dopamine release
cardiovascular depression

66
Q

_____ agonist binds to receptors.

A

Full

67
Q

Red = ____ effect
Green = allows ____ events to occur

A

blocks, normal

68
Q
A
69
Q

Adverse Effects of Opioids on CNS

A
70
Q

Adverse Effects of Opioids on Cardiovascular system

A
71
Q

Adverse Effects of Opioids on Respiratory system

A
72
Q

Adverse Effects of Opioids on GI

A
73
Q

Adverse Effects of Opioids (cont)

A
74
Q

Emergencies: Reverse undesirable effects
 CNS and respiratory depression
 Overdose
 Reverse neuroleptanalgesia
 Reviving neonates delivered by C-section
Wake up patient following sedation

A
75
Q

Naloxone hydrochloride
* ____ or ______ ___ administration
* Used in what species?

A

IM, slow IV, Dogs, horses, cats, exotic mammals

76
Q

Naltrexone
* Used in ___ animals (___, ___ against ______ effects)
* Orally in ____ for behavioral problems (?)
* ______ lasting

A

wild, IV, IM, carfentanil, dogs, constant licking, tail chasing, Longer

77
Q

What is the MOA of Naloxone hydrochloride?

A

Unknown

78
Q

Describe the PK of Naloxone hydrochloride

A
79
Q

Describe the adverse effects of Naloxone hydrochloride

A
80
Q

??

A
81
Q

N-methyl-D-aspartate (NMDA) receptor is a _____ receptor
and ___ channel
* Ligands: _____ and ____
* Mediating ______ and _____ functions

A

Glutamate, ion, Glutamate, Glycine, learning, memory

82
Q

Amantadine is an antagonist that can be used on ____ and ____ for ____ and ____ pain.

A

dogs, cats, acute, chronic

83
Q

Ketamin is used in?

A

hospital settings

84
Q

Gabapentin is used to treat what type of pain?

A

neuropathic pain, cancer-related pain

85
Q

Amitriptyline is an ?

A

antidepressant

86
Q

Lidocaine patch is a form of veterinary ______ _____________

A

pain management

87
Q
A
88
Q

Non-Opiod Analgesic Drugs

A

Tylenol can damage liver
Ibuprofen can cause GI ulcers in certain dogs, even at very low doses and at high doses can lead to severe liver damage.
NSAIDs are used as pain killers.
Make cards for rest of info on this

89
Q

What is the MOA of NSAIDs?

A
90
Q

Carprofen is an ______ and can be used on what species?

A

NSAID, dogs, cats, reptiles, and birds

91
Q

Deracoxib is an ______ and can be used on which species? For what reasons?

A

NSAID, dogs, after surgery

92
Q

Firocoxib is an ______ and can be used on which species? For what reasons?

A

NSAID, dogs, horses, osteoarthritis and surgery

93
Q

Meloxicam is an ______ and can be used on which species? For what reasons?

A

Dogs, cats, osteoarthritis

94
Q

What are the side effects of NSAIDs

A

Usually safe but some common side effects are: kidney, liver, and GI problems, drug to drug interaction

Intro to Pharmacology (31 decks)

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