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Pharmacology II > LEC 8,9 - General + Local Anesthetics > Flashcards

LEC 8,9 - General + Local Anesthetics Flashcards

1
Q

General anesthetic effects (5)

A

Analgesia

Loss of conciousness

Amnesia

Inhibition of snesory + ANS reflexes

Muscle relaxation

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2
Q

Drugs for analgesia (2)

A

N2O

Opiods

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3
Q

Drugs for loss of conciousness (2)

A

IV anesthetics

N2O

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4
Q

Drugs for amensia (3)

A

Midazolam

Droperidol

Ketamine

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5
Q

Drugs for ANS inhibition (3)

A

Atropine

Opiates

Scopolamine

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6
Q

Drugs for muscle relaxation

A

Depolarizing + Nondepolarizing muscle relaxants

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7
Q

What is the purpose of pre-medications?

A

Facilitate anesthesia + surgery

improves rapidity + smoothness of:

Iduction

Anxiety

Analgesia/Amnesia

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8
Q

What are the four major drug groups used for pre-meds?

A

Opiods

tranquilizers

Anticholinergics

Central muscle relaxants

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9
Q

What is the purpose of opioids in pre-meds?

A

Analgesia

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10
Q

What is the purpose of tranquilizers in pre-meds?

A

Pre-operative sedation + amnesia

Prevent/counteract CNS stimulation

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11
Q

What is the purpose of anticholinergics in pre-meds?

A

Prevent salivation + bradycardia

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12
Q

Propofol - Mechanism

A

Activates GABAa receptors

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13
Q

Propofol - admin

A

IV

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14
Q

Propofol - Distribution

A

Rapid redistribution + metaboolism

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15
Q

Propofol - Effects on cerebral pressure

A

Decreases blood flow + oxygen consumption

Safe for animals with head trauma

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16
Q

Propofol - Duration of anesthesia

A

2 to 10 min

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17
Q

Propofol - Distribution/breeds to watch out for

A

Distributes to fat

Sighthounds

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18
Q

Propofol - Metabolism

A

Glucoronidation

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19
Q

Propofol - 1/2 life

A

1 to 2 hours

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20
Q

Propofol - Adverse effects

A

Myoclonic twitching

Myocardial depression

Transient apnea

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21
Q

Etomidate - Mechanism

A

Sedative hypnotic nonbarbiturate

Facilitates GABA transmission

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22
Q

Etomidate - Effects

A

Decrease cerebral blood flow

Metabolic rate

oxygen consumption

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23
Q

Etomidate - Uses

A

Good for patients with:

Cardiac dysfuncton

Head trauma

Critically ill

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24
Q

Etomidate - Metabolism

A

Heptaic hydrolysis

No accumulation

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25
Q

Etomidate - 1/2 life

A

3 hours

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26
Q

Etomidate - Adverse effects

A

Very hypertonic

Pain + Hemolyssi upon IV injection

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27
Q

Alfaxalone - Mechanism

A

Synthetic neuroactive steroid

Interacts with GABA receptors

Anesthesia + Muscle relaxtion

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28
Q

Alfaxalone - 1/2 life

A

< 1 hour

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29
Q

Alfaxalone - Pharmacokinetic curce

A

non-linear aka zero order

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30
Q

Alfaxalone - Use

A

General anesthesia

Bolus or CRI

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31
Q

Alfaxalone - Adverse effects

A

CNS depression

Hypotension

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32
Q

Ketamine - Use

A

FDA approval in cats

Induction

CRI for general anestehsia

Sedation for chemical restraint

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33
Q

Ketamine - Mechanism

A

Inhibits excitaory NT ACh + L-glutamate in spinal cord

Non-competitive antagonist of NNMDA receptor

Dissociative anesthesia

Analgesia

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34
Q

Ketamine - Admin

A

IM/IV - Cats + Dogs + Small Ruminants + Swine

IV - Adult horses

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35
Q

Ketamine - Metabolism

A

CYP450

Congugated with glucuronide

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36
Q

Ketamine - Excretion

A

Kidneys -

Unchanged in cats

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37
Q

Ketamine - 1/2 life

A

Cat

Calf

Horse

= 1 to 1.5 hours

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38
Q

Ketamine - Adverse side effects

A

Seizures (Horses + Dogs )

Profuse salivation (Cats)

SNS stimulation = Inc CO + HR

Rougher induction/recovery

Increase muscle tone

Apneustic breathing pattern

CSF pressure increased

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39
Q

What muscle relaxers are given with ketamine?

A

Alpha2 agonists - to horses for muscle relaxation

Diazepam/Midazolam/etx. - to cats/dogs for seizure prevention + skeletal muscle relaxation

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40
Q

Midazolam - Mechanism

A

Benzodiazapine

Increases effects of GABA

Increases frequency of open Cl- channel

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41
Q

Midazolam - Use

A

Induction

Neonatal seizures

Status epilepticus

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42
Q

Midazolam - Neuroleptanalgesic combo

A

+ Opioid

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43
Q

Midazolam - Muscle relaxation combo

A

Ketamine

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44
Q

Midazolam - Protein bidning

A

94 to 97% bound

Unbound crosses BBB to enter CSF

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45
Q

Midazolam - Admin

A

SC + IM + IV

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46
Q

Midazolam - metabolism

A

Glucuronidation in liver

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47
Q

Midazolam - Affinity vs. Potency

A

2x’s affinity for GABA

3x’s potency

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48
Q

Midazolam - Adverse effects

A

Cardiorespiratory depression

Paradoxical excitement

Dysphoria

w/ drugs that have protein binding will increase CSF concentration

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49
Q

Midazolam - reversal

A

Flumazenil

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50
Q

Flumazenil - Mechanism

A

Competitive antagonist for BZD receptors

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51
Q

Tiletamine/Zolazepam - Use

A

Chemical resitrant in fracitous cats

Short term anesthesia in dogs/cats

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52
Q

Tiletamine/Zolazepam - Admin

A

Deep IM

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53
Q

Tiletamine/Zolazepam - Adverse effects

A

Excessive salivation

Erratic recovery

Muscle twitching

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54
Q

How do you treat excessive salivation with Tiletamine/Zolazepam administration?

A

Atropine

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55
Q

Barbiturates - Mechanism

A

Bind to GABA Cl- channels

Increase duration of opening

= hyperpolarization of neurons

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56
Q

Barbiturates - effects

A

Transient hypotension + increased HR

Depress respiratory centers (Cats > Dogs)

General anesthesia

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57
Q

Barbiturates - overdose

A

Apnea

Cardiovascular depression

Death

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58
Q

Barbiturates - Distribution factors

A

Lipid solubility

Protein binding

Ionization

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59
Q

What type of drugs cross the BBB?

A

Non-protein bound

– and –

Non-ionized

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60
Q

Why are thiobarbiturates rapid in onset?

A

High lipid solubiltiy

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61
Q

Characteristics of ultrashort acting barbiturates

A

very lipid soluble

Onset rapid

Duration short (10 to 30min)

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62
Q

Methohexital - use

A

Dogs/Cats

Ultra short procesures

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63
Q

Methohexital - Duration of action

A

5 to 15 minutes

64
Q

Methohexital - Time of onset

A

15 to 60 seconds

65
Q

Methohexital - Distribution

A

No effect on fetus so safer for C-section

Can reduce O2 in pups so move fast

Does not move to fat - good in greyhounds

66
Q

Methohexital - Adverse effects

A

More likely to cause period of excitement during induction

Profound respiratory depression

67
Q

Pentobarbital - Four main uses

A

Sedation

General anesthesia

Seizure control

Euth

68
Q

Pentobarbital - Sedation uses

A

Mechanical ventilation

Ruminants + Horses

69
Q

Pentobarbital - General Anesthetic uses

A

Cats/Dogs

70
Q

Pentobarbital - Seizure uses

A

Refractory to phenobarbital or diazepam

71
Q

Pentobarbital - duration of action

A

30 to 60 min

72
Q

Pentobarbital - 1/2 life

A

Ruminants - 0.9 hours

Dogs - 8 hours

73
Q

Pentobarbital - Adverse effects

A

Low doses - ecitement phase

74
Q

Phenobarbital - mechanism

A

Long-acting

75
Q

Phenobarbital - uses

A

Anticonvulsant in status epilepticus treatment

Excess, chronic drooling in dogs

Chlorinated hydrocarbon detox in cattle

76
Q

Phenobarbital - ADmin

A

PO

IV loading in horses

77
Q

Phenobarbital - Duration of action

A

6 to 12 hours

78
Q

Phenobarbital - Metabolism

A

Liver 75 %

Urine, unchanged 25%

79
Q

Phenobarbital - Adverse effects

A

Ataxia + Lethargy + depression

PU/PD/PP

Coagulopathies + Adrenal insufficency in cats

Increased liver enzymes in dogs

80
Q

Define: MAC

A

1 mac = [] at 1 atm that prevents skeletal muscle movemnet in painful stim in 50% of the population

81
Q

Oil : Gas ppartition coefficients

A

Measure of potency

82
Q

MAC-awake

A

Inhibits voluntary movements

83
Q

MAC-BAR

A

Blunting autonomic reflexs

84
Q

MIR

A

Eliminates reflexes used to judge depth of anestehisa

85
Q

Blood : Gas Partition Coeffcient

A

Rate of increase of Pa towards Pi

Inversely related to solubility of anesthetic to blood

86
Q

Partition coefficient =

A

Solubility of inhaled anesthetic in different body components

87
Q

Nitrous Oxide - Effects

A

Direct myocradial function depression

SNS stimulation

No sensitization of myocardium to epi

88
Q

Nitrous Oxide - Use

A

Not very potant

Combine with other inhaled anesthetics to make more stable anesthesia

Analgesic

89
Q

Nitrous Oxide - Secondary effects

A

Second gas effect

Diffusional hypozia

90
Q

Describe second gas effect

A

Nitrous + Other inhalant anesthetic

NO highly diffusible, quick to leave alveoli

[] of other compoundss increase in alveoli

[] effect increases theri absorption into the blood

= decrease concentration needed

91
Q

Nitrous Oxide - Distribution

A

Accumulations in gas filled spaces

Rumen of cattle

Cecum of horses

92
Q

Describe diffusion hypoxia

A

NO is turned off

NO quickly diffuses out of blood into alveoli

Intra-alveolar oxygen [] is decreased

93
Q

Treatment for diffusion hypoxia

A

100% oxygen

94
Q

Preventing diffusion hypoxia

A

Wean patients off of NO

95
Q

Isoflurane - Effects

A

Decrease arterial BP

Depresses CV function

Catecholamine sensitization = Cardiac arrhythmias

RR + TV decreased

Increases effect of non-depolarizing muscle relaxers

96
Q

Isoflurane - MAC that effects cerebral blood floow

A

1.2

97
Q

Isoflurane - Use

A

Dog + Cats + Birds + Horses

Anesthetic

Status epilepticus in Dogs (refractory to benzodiazepines)

98
Q

Isoflurane - kinetics

A

Low blood : gas partition coeffiecent

Rapid induction/recovery

Exhaled unmetabolized

99
Q

Isoflurane - Adverse effects

A

Malignant hyperthermia

Higher risk of causing vasodilation

(Responsive to fluid bolus)

100
Q

Sevoflurane - Effects

A

Decrease SV

Depresses myocardial contractility

Decreases arterial BP

101
Q

Sevoflurane - Kinetics

A

Low blood : Gas partition coefficient

Fast induction/recovery

102
Q

Sevoflurane - Elimination

A

Liver - 2 to 5%

The rest is exhaled

103
Q

Sevoflurane - Adverse effects

A

Malignant hyperthermia

104
Q

What is the order in which euthanasia should take place?

A

Rapid loss of conciousness

Loss of motor function

Arrest of respiratory + cardiac functions

Permanent loss of brain function

105
Q

Barbiturates for Euth - mechanism

A

Depress CNS in descending order

Cerebral cortex w/ loss of conciousness to anesthesia

Repsiratory center depression

Cardiac arrest

106
Q

Barbiturates for Euth - Food animals

A

NEVER TO BE USED IN ANIMALS IN THE FOOD CHAIN

107
Q

Dissociative agents + Alpha2 antagonist - use in euth

A

Can be given prior to the admin of euthanasia solutions to minimize animal distress + help with restraint + easier euthanasia for O

108
Q

Acceptable euthanasia methods - Cats

A

IV barbiturates

Anesthetic OD

109
Q

Acceptable euthanasia methods - Cattle

A

IV Barbiturates

110
Q

Acceptable euthanasia methods - Dogs

A

IV barbiturates

Anesthetic OD

111
Q

Acceptable euthanasia methods - Horse

A

IV barbiturates

112
Q

Acceptable euthanasia methods - Poultry

A

Injected barbiturates

Anesthetic OD

113
Q

Acceptable euthanasia methods - Swine

A

Injected barbiturates

114
Q

What are the two types of local anesthetics?

A

Esters

– and –

Amides

115
Q

Characteristics of esters

A

Shorter duration

Increased toxicity

116
Q

How does sterochemistry effect local anesthetics?

A

Potency

Clinical properties

117
Q

What is the purpose of salts in local anesthetics?

A

Increase stability + solubility

118
Q

pKa of local anesthetics

A

7.5 to 9

119
Q

Predominant form of Local anesthetic in body

A

Ionized form LAH+

120
Q

Where is the binding site for the local anesthetics?

A

Inner membrane

121
Q

What is steps in which local anesthetics enter the cell?

A

Non-ionized cross membrane

Become ionized within the cell and become stuck

Ionized form binds within the cell

aka Hydrophobic pathway

122
Q

Target of local anesthetics

A

Block Na+ channel = inhibit neuronal firing

123
Q

effect of local anesthetics on the neuron

A

Increased t-hold for excitation

Slowed impulse conduction

124
Q

What is the amount by which the local anesthetic blocks the area dependent on?

A

Voltage

Firing time

125
Q

What channel type are local anesthetics have the highest affinity for?

A

Acitvated + inactivated

126
Q

What neuronal activity level do local anesthetics have the highest affinity for?

A

Rapidly firing

127
Q

Where are the adverse effects targeted with local anesthetics?

A

CNS + Cardiac

128
Q

Duration of action dependent on =

A

Time at site

129
Q

Toxic effects dependent on =

A

1/2 life

130
Q

What effect does epi have on local anesthetics?

A

Decreased diffusion of the drug

Prolongs duration of action

Decreases systemic absorption

Decreases risk of systemic toxicity

131
Q

Amides - Elimination

A

Metabolized by liver CYP450s

132
Q

Amides - Toxicity

A

seen with -

Hepatic disease

Reduced hepatic blood flow

133
Q

Local anesthetics - Secretion

A

Renal

134
Q

Esters - Metabolism

A

Rapid metabolism by butyrylcholinesterase in plasma

135
Q

What are the four major adverse effects with local anesthetics?

A

CNS

CV system

Methemoglobinemia

Tissue damage

136
Q

Local Anesthetics - CNS adverse effects

A

Skeletal muscle twitching first sign

Tonic-clonic seizures normally first clinical sign

137
Q

Local Anesthetics - MetHg adverse effect

A

Use of prilocaine + benzocaine in cats and rabbits

138
Q

Local Anesthetics - Tissue damage

A

Neurotoxicity

Myotoxicity

139
Q

Local Anesthetics - CV system adverse effects

A

Prolonged PR + QRS interval due to slowed impulse conduction

Hypotension

Decreased myocardial strength

140
Q

Tetracaine - Use

A

Opthalmological

141
Q

Tetracaine - Mechanism

A

Ester

142
Q

Tetracaine - Onset of action

A

> 10 mintues

143
Q

Tetracaine - Duration of action

A

2 to 3 hours

144
Q

Tetracaine - Adverse effects

A

Burning + Chemosis

Allergic reaction

Chornic use = keratitis

Supressed blink reflex

145
Q

Lidocaine - use

A

Correct Vtach + SVT + PVT in dogs

Analgesia (Dogs +Horses)

Prokinetic effects (Horses)

146
Q

Lidocaine - Mechanism

A

Amide

147
Q

Lidocaine - Duration

A

Rapid absorption

Intermediate duration of action

148
Q

Bupivacaine - Mechanism

A

Amide

149
Q

Bupivacaine - use

A

Post-op pain control

150
Q

Bupivacaine - Adverse affect

A

Greater cardiotoxicity

Binds more Na channels

Dissociates slower from the channels

151
Q

Proparacaine - Mechanism

A

Amide

152
Q

Proparacaine - Action

A

Fast onset

Short duration

Cats = 15 min

Dogs = 45 min

153
Q

Mepivacaine - Mechanism

A

Amide

154
Q

Mepivacaine - Use

A

Equine limb block

Diffuses through surrounding tissue

Les postinjection edema

155
Q

Benzocaine - Mechanism

A

Ester

156
Q

Benzocaine - Use

A

Topically absobed -

Lozenges

Fish anesthesia

Pharmacology II (20 decks)

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