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Introduction to Pharmacology > Analgesics > Flashcards

Analgesics Flashcards

1
Q

What is the difference between CNS pharmacology, neuropharmacology, and psychopharmacology?

A

how drugs alter brain activity and offset pathology

how drugs act on neurons at the cellular/molecular level

how drugs modify behavior, perception, and thoughts

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2
Q

Dramatic advances have been made in CNS pharmacology in the last 3 decades. Why are recent developments not as good?

A

large pharmaceutical companies severely restrict neuropsychiatric development efforts citing low chances of successful CNS drug applications

  • 46% of drugs reach Phase III success; 8.2% reach clinical use
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3
Q

What is a CNS drug? What 6 actions of CNS drugs are of therapeutic importance?

A

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

  1. relieve pain and fever
  2. suppress disorders of movement or seizures
  3. induce sleep or arousal
  4. reduce desire to eat
  5. inhibit motion sickness
  6. treat anxiety, mania, depression
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4
Q

What is a prescription drug? Controlled drug?

A

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

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

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5
Q

What do CNS drugs act like? What are the 2 outcomes?

A

act like NT, transferring electrochemical messages between neurons in the brain and spinal cord

  1. speed up transfer —> CNS stimulants
  2. slow down transfer —> CNS depressants
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6
Q

How do CNS drug actions compare to agents like alcohol and anesthetics?

A

CNS DRUGS: act on specific receptors that modulate synaptic transmission

NONSPECIFIC AGENTS: non-receptor-mediated actions that result in alterations in synaptic transmission

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7
Q

Drugs can alter the function of the CNS to provide what 7 responses?

A
  1. analgesia: narcotic (opioids) and non-narcotic (NSAIDs, NMDA receptor agonists)
  2. tranquilization (sedation)
  3. anticonvulsant
  4. antiemetic
  5. anxiolytic, sedative, hypnotic
  6. general anesthesia
  7. behavior changes
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8
Q

What 4 characteristics of CNS drugs affect their action?

A
  1. pharmacokinetics
  2. pharmacodynamics
  3. drug distribution
  4. target tissues and stimulation
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9
Q

What is the difference between agonists and antagonists?

A

AGONIST: bind to and stimulate target tissue (CNS)
ANTAGONIST: bind to target tissue, but don’t stimulate

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10
Q

What are the 8 steps of neurotransmitter release?

A
  1. AP reaches presynaptic fiber
  2. NT is synthesized
  3. NT is stored
  4. NT is metabolized
  5. NT is released
  6. NT undergoes reuptake OR
  7. NT is degraded OR
  8. NT reaches postsynaptic receptor
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11
Q

What are 10 sites of action for CNS drug action?

A
  1. AP potential in presynaptic fiber
  2. NT synthesis
  3. NT storage
  4. NT metabolism
  5. NT release
  6. NT reuptake into presynaptic neuron or glial cell
  7. NT degradation
  8. NT postsynaptic receptor
  9. receptor-induced increase/decrease in ionic conductance
  10. retrograde signaling
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12
Q

What are the 4 main targets for neuroactive drugs? What causes subtle differences in the function and pharmacology of these drugs?

A
  1. ion channels
  2. receptors
  3. enzymes
  4. transport proteins

most of these targets occur in several different molecular isoforms

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13
Q

What can cause the delayed efficacy of antidepressants and tolerance/dependency with opioids?

A

slowly developing secondary response to primary interaction of the drug with its target

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14
Q

What is the blood-brain barrier (BBB)? What is its function?

A

highly selective barrier separating the brain tissue from blood circulation, consisting of a continuous layer of endothelial cells joined by tight junctions and surrounded by astrocytes

CNS protection against toxins, pathogens, and NTs like glutamate

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15
Q

How are necessary drugs able to cross the BBB?

A

non-functional pro-drug (L-Dopa) is able to pass the BBB by itself and is altered into a functional form (Dopa) in the brain

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16
Q

What are the 5 major characteristics of drugs able to cross the BBB?

A
  1. lipid solubility (lipophilicity)
  2. small in molecular size
  3. poorly bound to proteins
  4. non-ionized in at the pH of cerebrospinal fluid
  5. undergo diffusion or carrier-mediated transfer
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17
Q

How does inflammation affect the BBB? How does the neonate BBB compare to a fully formed one?

A

increases permeability

poorly developed —> chemicals can easily gain access to the neonatal brain

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18
Q

What are analgesics? What is the goal of this therapy?

A

drugs that act on the CNS to inhibit pain processing

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

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19
Q

What is pain?

A

unpleasant sensory and emotional experience associated with actual or potential tissue damage —> recognized for its contribution to morbidity and mortality

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20
Q

How is pain classified based on duration?

A

ACUTE: sudden in onset, resolves in 1-3 days, initiated from traumatic insult, and is well controlled with an analgesic

CHRONIC: slow in onset, persists for weeks/months, alters homeostasis, long-term distress, needs a combination of potent analgesics

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21
Q

How is pain classified based on location?

A

VISCERAL: abdominal or thoracic cavity

SOMATIC: musculoskeletal damage

NEUROPATHIC: damage affecting somatosensory nervous system

22
Q

What are the 4 steps of the pain processing system?

A
  1. TRANSDUCTION: noxious stimuli are transformed into electrical signals at the periphery
  2. TRANSMISSION: conduction of impulses from peripheral pain receptors to the spinal cord
  3. MODULATION: amplification or suppression of pain impulses by neurons in the spinal cord
  4. PERCEPTION: processing and recognition of pain in the brain
23
Q

What are opioids derived from?

A

opium - an extract from the white, milky sap of unripe bulbs of the poppy plant

24
Q

What are the active chemical compounds in opium? How are each used?

A

MORPHINE - analgesic, anesthetic, sedative

CODEINE - hypnotic, analgesic, suppressant

25
Q

What is the difference between opiates and opioids?

A

OPIATES: narcotic drugs derived from poppy opium or semi-synthetic derivatives with narcotic properties —> natural or not natural; opium, morphine, heroine

OPIOIDS: fully synthetic or semi-synthetic narcotic drugs that mimic the natural opiate —> not found in nature; hydrocodone, oxycodone, fentanyl, tramadol

26
Q

What are endogenous opioid neuropeptides?

A

endorphins, enkephalins, and dynorphins released by neuroendocrine cells to activate receptors

27
Q

Opioids are controlled substances. What are 2 exceptions?

A
  1. antagonists
  2. nalbuphine (partial agonist)
28
Q

How do cats compare to other animals in opioid metabolism?

A

cats are deficient in the metabolic pathway, making the halflife of most opioids prolonged

29
Q

What are the 2 major uses of opioids?

A
  1. ANALGESIA: prevent and treat postoperative pain (+ tranquilizers for neuroleptanalgesia)
  2. PRE-ANESTHETIC: agonists, partial agonists, mixed agonist-antagonists (alone or in combination with tranquilizers and anticholinergics)
30
Q

What pharmacological effects do opioids have? How do adverse affects compare in dogs and cats/horses/ruminants?

A

mimic endogenous opioid peptides (endorphins, dynorphins, encephalins), naturally made in the body to cause analgesia and sedation

DOGS: narcosis
C/H/R: CNS stimulation, bizarre behavior, dysphoria

31
Q

What is the mechanism of action of opioids affecting the CNS?

A

bind to receptors in the brain and spinal cord, which mediates the inhibition of neurotransmission and endocrine secretion

32
Q

What are the possible opioid receptors? How does action at each receptor compare?

A

μ, κ, δ

each opioid has a different effect at each receptor

33
Q

What are the major opioid receptor agonists, partial agonists, mixed agonist-antagonists, and antagonists?

A

AGONISTS: morphine, fentanyl (75-125x potent), hydromorphone, oxymorphone, tramadol

PARTIAL AGONISTS: buprenorphine, butorphanol (μ)

MIXED: butorphanol (μ agonist, κ agonist), nalbuphine (κ agonist, μ antagonist), buprenorphine (μ partial agonist, κ antagonist)

ANTAGONISTS: naloxone, naltrexone (reversals)

34
Q

What kind of receptors are opioid receptors? Where are they located?

A

G-coupled protein receptors

  • brain
  • spinal cord
  • GI tract
  • urinary tract
  • vas deferens
35
Q

What do the 3 receptor subtypes of opioid receptors do?

A
  1. μ receptors: spinal and supraspinal analgesia, euphoria, mild sedation, miosis, respiratory depression*, chemical dependence, inhibition of Ach and dopamine release, decrease in GI motility (brain, spinal cord)
  2. κ receptors: spinal and supraspinal analgesia, sedation, dysphoria, diuresis, miosis (cerebral cortex, spinal cord, other brain regions)
  3. δ receptors: spinal and supraspinal analgesia, inhibition of dopamine release, cardiovascular depression (LIMBIC SYSTEM, cerebral cortex, spinal cord)
36
Q

Opioids drug-receptor relationship:

A
37
Q

What adverse effects can opioids have on the CNS and cardiovascular system?

A

CNS:
- anxiety
- disorientation
- excitement
- dysphoria

CARDIOVASCULAR SYSTEM:
- bradycardia

38
Q

What adverse effects can opioids have on the respiratory system and GI?

A

RESPIRATORY SYSTEM
- decreased respiration and tidal volume (μ-receptor agonist)
- decreased PaO2 and PaCO2
- ceiling effect where increased dosage will have no effect

GI
- salivation and vomiting in small animals
- diarrhea
- constipation following initial GI stimulation
- colic in horses

39
Q

How can opioids affect the eyes?

A

DOGS: miosis (μ- and κ-receptors)

CATS, HORSES, RUMINANTS: mydriasis

  • increases intraocular and intracranial pressure
40
Q

How can opioids affect internal temperature?

A

DOGS: hypothermia

CATS: malignant hyperthermia

41
Q

What are some additional adverse effects of opioids?

A
  • increased responsiveness to noise
  • sweating in horses
  • decreased urine production with urine retention
  • facial swelling and hypotension
  • addiction
  • drug interactions
42
Q

What is done in emergencies when opioid-treated animals start exhibiting adverse effects? In what 4 circumstances is this done?

A

reversal (wake up animal after sedation)

  1. CNS and respiratory depression
  2. overdose
  3. reverse neuroleptanalgesia
    .4 reviving neonates delivered by C-section
43
Q

What 2 drugs are used to reverse opioids?

A
  1. NALOXONE HYDROCHLORIDE: IM or slow IV administration to dogs, horses, cats, and exotics
  2. NALTREXONE: IV or IM to wild animals; PO to dogs for behavioral problems
    - longer lasting

(antagonists)

44
Q

What is the common adverse effect of naloxone hydrochloride? How can they be prevented?

A

sudden analgesia loss can cause excitement, anxiety, and sympathetic nervous system stimulation

using mixed agonist-antagonists

45
Q

Action and selectivity of opioid drugs:

A
46
Q

What are NMDA receptors? What are their ligands?

A

N-methyl-D-aspartate receptors —> glutamate receptor and ion channel

  • glutamate (activating)
  • glycine (inactivating)
47
Q

What drugs acting on the NMDA receptors can act as analgesics? What are 5 examples?

A

NMDA receptor antagonists

  1. Amantadine - dogs, cats for acute and chronic pain
  2. Ketamine
  3. Gabapentin - neuropathic pain, cancer-related pain
  4. Amitriptyline - antidepressant
  5. Lidocaine patch - pain management
48
Q

What is the mechanism of action of NSAIDs? What effects do they have?

A

non-opioid analgesic
inhibition of the pro-inflammatory enzyme cyclooxygenase (nonselective for COX1 and 2; selective for COX2)

reduce swelling, stiffness, and joint pain caused by inflammation

49
Q

What NSAIDs are not typically used in veterinary medicine? Why?

A
  • acetaminophen (Tylenol)
  • ibuprofen
  • aspirin (limited amount of time)

dogs are unable to metabolize these drugs, causing liver damage and ulcers

50
Q

What 4 NSAIDs are used in veterinary medicine and what are some possible side effects for each?

A
  1. Carprofen (dogs, cats, reptiles, birds) - kidney damage
  2. Deracoxib (dogs post-surgery) - liver damage
  3. Firocoxib (dogs, horses osteoarthritis and surgery) - GI problems
  4. Meloxicam (dogs, cats osteoarthritis) - drug-drug interactions

Introduction to Pharmacology (39 decks)

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