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Pharmacology > Chapter 8 Nerouvs System (Analgesics, Tranquilizers, Sedatives, and Anesthetics) > Flashcards

Chapter 8 Nerouvs System (Analgesics, Tranquilizers, Sedatives, and Anesthetics) Flashcards

1
Q

Analgesics

A

Drugs used to control pain - reducing the perception of pain without significant loss of other sensations

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2
Q

Pain Pathway

A

Takes place in the nervous system, involves the transmission of information from a stimulus to perception by the brain

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3
Q

Transduction

A

Painful stimulus is transformed into an electrical signal mediated by depolarization of a pain receptor

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4
Q

Nociceptor

A

Pain receptor

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5
Q

Transmission

A

Impulses from the nociceptors are transmitted to the spinal cord

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6
Q

Modulation (modification)

A

Sensory depolarization wave is transmitted from the spinal cord toward the brain. At the level of the spinal cord, this wave can be modified (suppressed or enhanced) This can decrease pain perception at the brain level.

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7
Q

Perception

A

Pain is perceived at the conscious level. GA prevents conscious perception of pain

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8
Q

Hyperalgesia

A

Occurs when pain receptors are more sensitive and responsive to painful stimuli. Increased sensitivity can result from the influence of inflammatory molecules

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9
Q

Wind-Up

A

After initial pain impulse dampening is reduced, the pain is more effectively transmitted up the spinal cord to the brain, increasing pain perception. (Increasing success in transmitting pain up the spinal cord)

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10
Q

Hyperesthesia

A

Increased sensitivity to any stimulus

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11
Q

Opioids

A

Chemically synthesized drugs with opiate characteristics (most potent analgesics in vet med)

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12
Q

Neuroleptanalgesics

A

Opioids combined with tranquilizers or sedatives to lessen opioids undesirable effects

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13
Q

Opiates

A

Extracts from poppy plants

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14
Q

Narcotics

A

Drugs that cause a state of narcosis

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15
Q

Narcosis

A

Unconsciousness or stupor

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16
Q

Known opioid receptors in mammals are:

A

mu (µ), kappa (κ), and delta (δ) receptors

sigma (σ) is sometimes referenced

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17
Q

True or False - Drugs specifically targeting Sigma receptors are often used in vet med

A

False - these drugs are not used in vet med

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18
Q

Mu (µ) receptors

A

Found in pain related nerves in the brain and spinal cord - Agonists to these receptors cause profound analgesic effects

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19
Q

Kappa (κ) receptors

A

Effects of these receptors are milder than Mu (µ) receptors. Some Kappa (κ) agonists are also Mu (µ) receptor agonists, providing a stronger analgesic effect.

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20
Q

Kappa (κ) receptor agonist drugs

A

Butorphanol, Levorphanol, Pentazocine

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21
Q

Full Mu (µ) Agonist drugs

A

Morphine, Hydromorphone, Fentanyl

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22
Q

Partial Mu (µ) agonist drugs

A

Buprenorphine, Butorphanol

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23
Q

Mu (µ)- mediated analgesia occurs when:

A

A decrease in the release of neurotransmitters such as acetylcholine, dopamine and serotonin. This blocks or reduces depolarization waves along the pain pathway

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24
Q

Mu (µ) Antagonist Drug

A

Naloxone - reversal drug for opioid analgesics

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25
Q

List the Schedule II Opioid Analgesics

A 
Morphine
Hydromorphone
Oxymorphone
Fentanyl
Methadone
Meperidine
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26
Q

List the Schedule III Opioid Analgesics

A

Buprenorphine

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27
Q

List the Schedule IV Opioid Analgesics

A

Butorphanol

Tramadol

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28
Q

Visceral Pain

A

Pain involving the internal organs

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29
Q

Somatic Pain

A

Pain involving skin and superficial tissues

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30
Q

Morphine

A
  • Stimulates primarily Mu receptors with some action on Kappa receptors
  • Effective for both Visceral and Somatic pain
  • Low doses IM or SQ cause vomiting and salivation in dogs (Morphine reaches CRTZ before suppressing the mu receptors of the emetic center)
  • Causes histamine induced vasodilation causing a decrease in arterial BP
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31
Q

Hydromorphone/Oxymorphone

A
  • Mu Agonists with a higher potency than Morphine
  • Similar efficacy to Morphine
  • Causes less vomiting and histamine release
  • May cause transient hyperthermia in cats
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32
Q

Fentanyl

A
  • Mu Agonist with greater potency and shorter duration than Morphine
  • Causes less vomiting
  • Given as IV infusion (CRI), patch, or transdermal solution
  • Patch takes several hours to be delivered by patch
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33
Q

Recuvyra

A

Transdermal Fentanyl solution applied 2-4 hours prior to surgery and supplies analgesia for up to 4 days post surgery

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34
Q

Methadone

A
  • Mu receptor Agonist
  • Also blocks N-Methyl-D-Asparate (NMDA) receptors
  • Less likely to cause vomiting/histamine release compared to other Mu agonists
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35
Q

Meperidine (Demerol)

A
  • Less potent than morphine
  • Shorter duration
  • Has more cardiovascular depressant effects than other opioids
  • Not widely used in vet med
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36
Q

Buprenorphine

A
  • Partial Mu Agonist and a Kappa antagonist
  • Has a ceiling effect
  • Longer duration of effect than Torb (6-8 hours)
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37
Q

Simbadol

A

SQ brand of Buprenorphine approved for cats

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38
Q

Ceiling Effect

A

Regardless of the dose given, the degree of Buprenorphine analgesia will never reach that of Morphine.
** Increased doses do NOT increase the degree of analgesia/sedation, it only extends/prolongs the duration of the drugs effect **

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39
Q

NMDA (N0methyl-D-aspartate) Receptor

A

Blocking this receptor depresses activity of parts of the brain, thus reducing some of the adverse opioid effects (hypersensitivity, or reactions to other sensory stimuli)

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40
Q

Butorphanol

A
  • Weak partial Mu agonist and a strong Kappa agonist
  • Often mixed with sedatives/other analgesics for a full anesthetic regimen
  • Considered a partial agonist/antagonist because it can be used to reverse some of the respiratory depressant effects of hydromorphone while providing analgesic effects
  • Strong antitussive properties - only FDA approved cough suppressant in small animals
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41
Q

Tramadol

A
  • Must be converted to the active form, O-desmethyltramadol (M1) which is a Mu receptor agonist
  • Inhibits serotonin and norepinephrine re-uptake, blocking muscarinic cholinergic and stimulating alpha2 receptors
  • Cats receive stronger analgesia from Tramadol than dogs (they can produce more M1 metabolite)
  • Should not be administered in animals taking behavioral tricyclic antidepressants (causes serotonin syndrome)
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42
Q

Serotonin Syndrome

A

Clinically significant high serotonin levels

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43
Q

Naloxone (Narcan)

A

Pure Mu and Kappa antagonist used to reverse the effects of opioid overdose
(More difficult to reverse the effects of Buprenorphine given how tightly it binds to the Mu receptors)

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44
Q

Tranquilizers

A

Have anxiety lowering effects/calms the patient

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45
Q

Sedatives

A

Cause drowsiness and sleepiness but does not reduce the patients anxiety or agitation

46
Q

Anxiolytic Agents

A

Literally means “Breaks apart anxiety”

47
Q

Narcosis

A

State of sleep from which the animal is not readily aroused

48
Q

When working with tranquilized animals it is very important to remember:

A

Tranquilized animals in a relaxed state are still capable of feeling pain and responding quickly and viciously to manipulations that elicit pain

49
Q

Acepromazine

A
  • Phenothiazine derivative that works by blocking Dopamine, Alpha-1 Adrenergic, Muscarinic Cholinergic, and histamine receptors in the brain
  • Has antiemetic effects (inhibits receptors on the CRTZ and emetic center)
  • Commonly causes protrusion of the nictitating membrane
  • Can cause temporary or permanent penile prolapse in horses
50
Q

Benzodiazepines

A
  • Gamma-Aminobutyric Acid (GABA) receptor agonists tat provide anxiolytic and muscle-relaxing effects
  • Does not bind to the same site as the endogenous GABA molecule, instead binding to an allosteric site, leading to a tighter binding of GABA to the receptor
  • Schedule IV controlled substances
51
Q

Diazepam (Valium)

A
  • Most common benzodiazepine in vet met
  • Drug of choice to control active seizures, used in anesthetic protocols to reduce muscle rigidity, dysphoria and agitation
52
Q

Tiletamine

A
  • Dissociative anesthetic
  • Drug combined with Zolazepam, known as the commercial drug Telazol
  • Used for minor procedures lasting less than an hour in cats, and less than 30 minutes in dogs
  • Provides stronger analgesia than Ketamine
53
Q

Midazolam

A
  • Most commonly used as a pre-anesthetic tranquilizer

- Has a greater potency than Diazepam

54
Q

Clonazepam

A

Orally administered drug used long-term with Phenobarbital to control seizures in dogs

55
Q

Alpha-2 Agonists

A
  • Cause a decrease in norepinephrine release in the CNS, leading to sedation
  • There is also an analgesic component based on decreased perception of pain
  • These drugs also have a ceiling effect
  • Induce effects on the cardiovascular system
  • Can also have an affect on Alpha-1 receptors (causing vasoconstriction and hypertension)
  • Newer Alpha-2 drugs have a higher selectivity for Alpha-2 receptors
56
Q

Xylazine

A
  • 1st alpha-2 agonist used in vet med
  • Horses require a much smaller dose than the dog, cattle even less than the horse, and goats less than the cattle
  • Swine are considered highly resistant to the dose (requiring a higher dose than the dog)
  • Should not be used in dogs with a history or susceptibility for gastric dilation
  • Cattle are susceptible to rumen stasis
57
Q

Detomidine

A
  • Alpha-2 Agonist
  • Labeled for use only in horses
    (Extra label uses in cattle and small ruminants)
58
Q

Medetomidine

A
  • Alpha-2 Agonist
  • Labeled for use in dogs as a sedative when minor surgery doesn’t require muscle relaxation
    (extra label uses in cats and horses)
59
Q

Dexmedetomidine (Dexdomitor)

A
  • Alpha- 2 Agonist
  • Labeled for use in dogs and cats
  • This is the dextrorotatory only form of medetomidine (has 1:1 “dextro” and “levo” forms)
  • More potent than medetomidine but has the same ceiling effect
60
Q

Romifidine

A
  • Alpha-2 Agonist

- Labeled for use in horses to ease handling for examinations and minor procedures

61
Q

Alpha-2 Antagonists

A

Drugs that reverse the effects of Alpha-2 Agonists

62
Q

Yohimbine

A
  • Alpha-2 Antagonist

- Still used to reverse the effects of Xylazine

63
Q

Tolazoline

A
  • Alpha-2 Antagonist
64
Q

Atipamezole (Antisedan)

A
  • Alpha-2 Antagonist
  • Used the most in vet med because of its better selectivity for alpha-2 receptors
  • Caution should be used when giving this drug IV
65
Q

Anesthesia

A

Refers to a state of no sensation

66
Q

Local Anesthesia

A

Reversible loss of local sensation of the region of the body without loss of consciousness

67
Q

General Anesthetics

A

The reversible loss of sensation associated with unconsciousness

68
Q

Barbiturates

A

Used for anesthetic induction and euthanasia. Drugs in this class work directly at the GABA site of GABA receptors

69
Q

Pentobarbital

A
  • Short acting barbiturate
  • Used more for long term control of convulsions in dogs with epilepsy
  • Used in vet med as an anesthetic agent for short procedures when gas anesthetics were unavailable
70
Q

Propofol

A
  • Injectable anesthetic agent unrelated chemically to barbiturates and other injectable anesthetics
  • Used to induce anesthesia and for short-duration diagnostic procedures
  • Effects also mediated via the GABA receptors, but also inhibit NMDA receptors
  • Net effect = suppression of neuronal activity in the brain, resulting in sedation or anesthesia
  • Causes apnea, especially after rapid administration
71
Q

Apnea

A

Cessation of breathing

72
Q

Ketamine

A
  • Dissociative anesthetic - short acting
  • NMDA antagonists, and can stimulate Mu and Kappa opioid receptors
  • Effect caused is that of being disconnected from the body (cataleptic state)
  • Not suited for use alone fr internal procedures (limited efficacy at blocking visceral pain)
73
Q

Methohexital

A
  • Ultrashort-acting Barbiturate

- Still available but has largely fallen out of use

74
Q

Phenobarbital

A
  • Long acting barbiturate

-

75
Q

Phenobarbital

A
  • Long acting barbiturate
  • Previously used successfully for anesthesia
  • Anticonvulsant drug of choice for long-term control of epilepsy in small animals
76
Q

Cataleptic State

A

Characterized by an appearance of being awake but being unable to respond to external stimuli

77
Q

Etomidate

A
  • Short acting anesthetic agent
  • Enhances GABA effects on GABA receptors
  • Used primarily for induction of anesthesia, especially in patients with cardiovascular problems (has minimal negative effect on the heart)
  • Has no significant analgesic effects
78
Q

Alfaxalone (Alfaxan)

A
  • Neurosteroid / Neuroactive steroid - meaning it is similar to endogenous hormone-like steroids synthesized in the brain that alter the neuronal activity within the brain
  • Causes inhibition of the brain and CNS depression
  • Still causes apnea like propofol
  • Can cause cardiovascular
79
Q

Dysphoria

A

Bad hallucination

80
Q

Idiosyncratic Reaction

A

Unpredictable reactions that is not dose related and cannot be predicted by an identifiable risk factor

81
Q

Inhalant Anesthetics

A

Anesthetic agents delivered as a gas via the lungs that is absorbed from the alveoli into the blood and distributes to the brain to produce unconsciousness - used for anesthetic maintenance

82
Q

MAC (Minimum Alveolar Concentration)

A

The lowest concentration of gas anesthetic that must be achieved in the alveoli of the lungs to produce safe anesthesia.
Each type of gas anesthetic has a specific MAC
(The lower the MAC the more potent the drug and the less drug that is required to achieve proper anesthesia)

83
Q

Isoflurane

A
  • Inhalant anesthetic
  • Smoother induction and recovery than Halothane
  • Has cardiac stabilizing effects
  • Can cause a decrease in arterial BP
  • Known for its distinct odor
  • Minimally metabolized by the liver
84
Q

Sevoflurane

A
  • Inhalant anesthetic
  • Faster induction and recovery than Isoflurane
  • Has good cardiac stabilizing effects
  • Newer than Isoflurane
  • Minimally metabolized by the liver
  • Does react with the CO2 scavenger compounds (soda lime) and cause production of a chemical called Compound A
85
Q

Desflurane

A
  • Inhalant anesthetic
  • least used of the 3 common anesthetic gases
  • Low potency (requires a higher MAC)
  • Odor similar to Isoflurane
  • High cost
  • Requires a special heated and pressurized vaporizer to turn the liquid into a vapor that can be inhaled
86
Q

Compound A

A

Sevoflurane reacts with the CO2 scavenger compounds commonly used in anesthetic machines and causes production of this chemical compound. It is has been found to cause nephrotoxicity in rats - controlled studies in dogs did not have the same conclusions

87
Q

Nitrous Oxide

A
  • Inhalant anesthetic (cannot be used alone)
  • Added to inhalant anesthetic regimens to reduce the amount of other anesthetics needed
  • Contraindicated in animals with distended rumen, twisted necrotic intestinal tissue, gastric dilatation, and pneumothorax
  • Once Nitrous Oxide has been d/c’d 100% O2 must be administered for several minutes to prevent diffusion hypoxia
88
Q

Diffusion Hypoxia

A

“Second gas effect” When Nitrous Oxide is ceased, it rapidly diffuses out of tissues into the blood and then into the alveoli, where it dilutes the O2 concentration. If 100% O2 is no longer being delivered and the animal is receiving room air (containing 15-17% O2) the O2 concentration in the lungs can be diluted enough by the nitrous oxide to produce hypoxia

89
Q

CNS Stimulants

A

Occasionally used to stimulate respiration in anesthetized animals or to reverse CNS depression cause by anesthetic or sedative agents

90
Q

Caffeine and Theobromine belong to a broad group of drugs known as …

A

Methylxanthine compounds- which include respiratory bronchodilating drugs like Theophylline and Aminophylline

91
Q

The active ingredient in chocolate is…

A

Theobromine

92
Q

Doxapram (Dopram)

A
  • CNS Stimulant
  • Works primarily in the medulla of the brainstem to increase respiration in animals with apnea, bradypnea, or other conditions in which the respiratory rate and depth of ventilation need to be increased
  • Use with caution in animals that are predisposed to seizures
93
Q

Halothane

A
  • Inhalant anesthetic

- Discontinued in US in 1995

94
Q

Bradypnea

A

Slow breathing

95
Q

True or False - Gas anesthetics provide analgesia

A

False. Gas anesthetics do not provide analgesia and the rapid recovery from gas anesthesia can produce delirium because of the transition from unconscious state to a sudden awareness, especially if the animal is in pain

96
Q

Apneustic Breathing Pattern

A

Respiratory rhythm is often altered so that the animal takes a long, deep inspiration, holds the breath momentarily, and then quickly exhales, producing a respiratory pattern

97
Q

γ-aminobutyric acid (GABA) receptor

A

One of the more important inhibitory neurotransmitters found in the CNS of mammals

98
Q

GABAA receptor

A

Located on the excitatory neuron and causes the GABA inhibitory neurotransmitter to bind more tightly with its receptor, opening chloride channels that flood the neuron cell with chloride and decrease the neurons ability to depolarize when stimulated

99
Q

Flumazenil

A
  • Benzodiazepine antagonist
  • In the unlikely overdose of a benzodiazepine, or if there is a need to shorten a prolonged recovery (especially in cats) this drug can be used to reverse them
100
Q

Hyperthermia

A

Increased body temperature

101
Q

Potency

A

The relationship between the therapeutic effect of a drug and the dose necessary to achieve that effect (higher potency = smaller dose)

102
Q

Efficacy

A

Expressed as effect

103
Q

Mydriasis

A

Pupil dilation

104
Q

Myosis

A

Pupil constriction

105
Q

Euphoria

A

Pleasant hallucinatory effect

106
Q

Agonist

A

Drug exerts a notable effect on the receptor

107
Q

Partial Agonist

A

Partial effect on the receptor - some intrinsic activity

108
Q

Antagonist

A

No effect on the receptor

109
Q

Mixed agonist/Antagonist Drugs

A

The drug combines with multiple types of opioid receptors

110
Q

Redistribution

A

Represents relocating the drug to an area of the body that is less likely to produce adverse reactions (moves the drug from the brain to other tissues)

Pharmacology (13 decks)

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