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Neuropharmacology > Types of Drugs > Flashcards

Types of Drugs Flashcards

1
Q

Local Anesthetics

Prototype

A

Procaine

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2
Q

Local Anesthetics

Mechanism of Action

A
  1. Inhibits sodium channels

2. Channel is open less often

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3
Q

Local Anesthetics

Clinical Uses

A
  1. Local anesthesia

2. Antiarrhythmic

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4
Q

Local Anesthetics

Adverse Effects & Toxicity

A
  1. Lower doses = CNS excitement = seizures
  2. Very high doses = CNS depression
    a. Respiratory collapse
    b. Cardiovascular depression
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5
Q

Local Anesthetics

Contraindications

A
  1. Do NOT use benzocaine or tetracaine in cats
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6
Q

Local Anesthetics

Chemistry

A
  1. Weak bases
  2. Two categories
    a. Esters
    b. Amides
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7
Q

Local Anesthetics

Metabolism

A
  1. Esters = plasma = shorter duration

2. Amides = hepatic = longer duration

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8
Q

Major Tranquilizers

Prototype

A

Acetylpromazine

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9
Q

Major Tranquilizers

Chemistry

A

Two categories

  1. Phenothiazines = Acetylpromazine
  2. Butyrophenone = Droperidol
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10
Q

Major Tranquilizers

Mechanism of Action

A

Antagonist Actions

  1. D, NE & S = monoamines
  2. Muscarinic cholinergic Ach receptors
  3. Alpha-adrenergic receptors = sympathetic NS
  4. Histamine receptors
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11
Q

Major Tranquilizers

Clinical Uses

A
  1. Sedation
  2. Muscle relaxation = less than barbiturates
  3. Hypnosis = catalepsy
  4. Anticholinergic activity = less atropine needed
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12
Q

Major Tranquilizers

Metabolism

A
  1. Highly protein bound

2. Hepatic metabolism

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13
Q

Major Tranquilizers

Adverse Effects & Toxicity

A
  1. Hypotension = use norepinephrine!
  2. Catalepsy
  3. Seizures = accidental IV injection
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14
Q

Major Tranquilizers

Contraindications

A
  1. Patients with epilepsy

2. Strychnine poisoning

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15
Q

Minor Tranquilizers

Prototype

A

Diazepam

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16
Q

Minor Tranquilizers

Chemistry

A

Four groupings

  1. Benzodiazepines = diazepam
  2. Chloral hydrate
  3. Alipathic alcohols
  4. Barbiturates
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17
Q

Minor Tranquilizers

Mechanism of Action

A

A. Interacts with GABA(A) receptor
B. Enhances GABA inhibition
C. Chloride channels = increases opening frequency

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18
Q

Minor Tranquilizers

Clinical Uses

A
  1. Restraint & calming
  2. Anticonvulsant = more than MTs
  3. Pre-anesthetic drug
    a. More skeletal muscle relaxation than MTs
    b. Blocks excitatory effects
  4. Does NOT induce anesthesia
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19
Q

Minor Tranquilizers

Metabolism

A

Metabolites are active!

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20
Q

Minor Tranquilizers

Adverse Effects & Toxicity

A
  1. Ataxia
  2. Excitation in cats
  3. Apnea when given IV
  4. Respiratory depression = more than MTs
  5. Risk for withdrawal = opposite of MTs
  6. Hypothermia
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21
Q

Minor Tranquilizers

Contraindications

A

None discussed

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22
Q

Alcohols

Prototype

A

Ethanol

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23
Q

Alcohols

Chemistry

A

Tertiary alcohols produce the most sedation

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24
Q

Alcohols

Mechanism of Action

A

Ethanol
Potentiates GABA receptor activity
Similar to inhalant anesthetics

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25
Q

Alcohols

Clinical Uses

A
  1. Sedative
  2. Block methanol & ethylene glycol toxicity
  3. Permanent nerve block
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26
Q

Alcohols

Metabolism

A
  1. Rapid absorption

2. Zero-order kinetics = loading dose needed

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27
Q

Alcohols

Adverse Effects & Toxicity

A
  1. Acidosis = acidic metabolites
  2. Hypothermia
  3. CNS & respiratory depression
28
Q

Alcohols

Contraindications

A

None discussed

29
Q

Stimulants

Prototype

A

Variety of compounds

30
Q

Stimulants

Chemistry

A
  1. Methylxanthines = theobromine
  2. Doxapram
  3. Cocaine
  4. Strychnine
31
Q

Stimulants

Mechanism of Action

A

Various

  1. Theophylline & theobromine = inc cortex activity
  2. Doxopram = inc. medulla activity
  3. Strychnine = inhibits Renshaw cells
  4. Cocaine = inhibits reuptake of monoamines
32
Q

Stimulants

Clinical Uses

A
  1. Toxicity

2. Stimulate respiration = doxopram

33
Q

Anticonvulsants

Prototype

A 
Acute = diazepam
Prevention = phenobarbital
34
Q

Anticonvulsants

Mechanism of Action

A

Two actions

  1. Block sodium channels
  2. Increase GABA activity = inhibitory activity
35
Q

Anticonvulsants

Clinical Uses

A

Um… to stop seizures

36
Q

Anticonvulsants

Metabolism

A

Not discussed

37
Q

Anticonvulsants

Adverse Effects & Toxicity

A
  1. Cessation of drug therapy may be lethal to the patient!
38
Q

Anticonvulsants

Contraindications

A

Not all anticonvulsants are good in all situations

39
Q

Barbiturates

Prototype

A
  1. Phenobarbital
  2. Pentobarbital
  3. Thiopental
40
Q

Barbiturates

Chemistry

A
  1. Weak acids
41
Q

Barbiturates

Mechanism of Action

A

Three fold mechanism:

  1. Enhance GABAergic activity
  2. Inhibit NT release
  3. Inhibit calcium uptake
42
Q

Barbiturates

Clinical Uses

A

Injectable anesthesia!

NO no no analgesia!

43
Q

Barbiturates

Metabolism

A
  1. Lipid solubility determines duration of action
  2. High protein binding
  3. Redistribution is important
44
Q

Barbiturates

Adverse Effects & Toxicity

A
  1. Inc GI motility
  2. Dec uterine contractions
  3. Inc secretions
  4. Laryngeal spasms
  5. Cardiac depression = dec. BP and CO
  6. Inhibits respiratory drives
    a. Chemogenic drive = CO2
    b. Hypoxic drive = O2
  7. Tissue irritation = IV ok
45
Q

Barbiturates

Contraindications

A
  1. High plasma protein binding

= can displace other drugs

46
Q

Dissociatives

Prototype

A

Ketamine

47
Q

Dissociatives

Chemistry

A

Very lipid soluble

48
Q

Dissociatives

Mechanism of Action

A
  1. Inhibition of the NMDA receptors

2. Binds sigma-type opioid receptors

49
Q

Dissociatives

Clinical Uses

A
  1. Sedative
    a. Can be used alone in cats
    b. Dogs & horses require a pre-medicatio sn
  2. Anesthesia = but maintain muscle tone
  3. Catalepsy = dissociation from enviroment
50
Q

Dissociatives

Metabolism

A

Hepatic

51
Q

Dissociatives

Adverse Effects & Toxicity

A 
1. Do NOT use in trauma situations 
= increase in intracranial pressure
= Increase in BP = bleeding risk
2. 50% of dogs will have seizures w/o pre-med
3. Risk for emesis during emergence
52
Q

Dissociatives

Contraindications

A
  1. Epilepsy

2. Head trauma or any trauma

53
Q

Inhalant Anesthetics

Prototype

A

Methoxyflurane

54
Q

Inhalant Anesthetics

Chemistry

A

A. Dose = partial pressure or volume precent
B. Lower MAC value = MORE potent
C. More lipid soluble = more potent

55
Q

Inhalant Anesthetics

Mechanism of Action

A

Affects the function of 3 channels:

  1. GABA channels
  2. Glycine ion channels
  3. Inhibition of nicotinic cholinergic receptors
56
Q

Inhalant Anesthetics

Clinical Uses

A
  1. CNS depression

2. Surgical anesthesia

57
Q

Inhalant Anesthetics

Metabolism

A
  1. Tissue uptake
    a. Highest blood flow = brain, GI, liver, kidneys
    b. Greatest mass = skin, muscle
    c. Body fat = high solubility but low blood flow
  2. Metabolism
    a. Risk in fluorinated anesthetics
    b. More metabolism = more toxicity
    c. May not be much metabolism
  3. Elimination
    a. Lungs
    b. Skin & mucus membranes
    c. Urine & milk
58
Q

Inhalant Anesthetics

Adverse Effects & Toxicity

A
  1. CNS depression
  2. Increase in intracranial pressure
  3. Respiratory depression = acidosis
    a. Blunts response to CO2
  4. Relaxation of cardiac & vascular muscle
    a. Decreased CO & BP
  5. Changes in blood flow
    a. Increased cerebral
    b. Decreased renal & hepatic
59
Q

Opioid Analgesics

Prototype

A

Morphine

60
Q

Opioid Analgesics

Chemistry

A
  1. Types
    a. Agonist
    b. Partial agonist
    c. Competitive antagonist
  2. Isomers
    a. L-isomer = best anaLgesic
    b. D-isomer = best antitussive
61
Q

Opioid Analgesics

Mechanism of Action

A
  1. Opens potassium channels = hyperpolarization
  2. Closes calcium channels = less NT release
  3. Decreases cAMP = inhibitory
62
Q

Opioid Analgesics

Clinical Uses

A
  1. Analgesia
  2. Antidiarrheal
  3. Antitussive = NOT through opioid receptors
  4. Sedation = dogs, rats, rabbits, primates
63
Q

Opioid Analgesics

Metabolism

A

Bioavailability

  1. Codeine = 60%
    a. Codeine can be metabolized to morphine!
  2. Morphine = 25%
64
Q

Opioid Analgesics

Adverse Effects & Toxicity

A
  1. Respiratory depression = Delta & Mu only
  2. Emesis
  3. Constipation
  4. Histamine release = esp. dogs
  5. Little to no cardiovascular effects!!!
65
Q

Opioid Analgesics

Contraindications

A

Immune compromised animals

Neuropharmacology (2 decks)

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