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Pharmacology I > 14. General anaesthetics: Injectable anaesthetics > Flashcards

14. General anaesthetics: Injectable anaesthetics Flashcards

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1
Q

Analgesia

A

Lack of pain sensation

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2
Q

Anaesthesia

A

Lack of sensation, total loss of motoric activity (+pain?)

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3
Q

Give the stages of general anaesthesia

A

Stage:

  1. Disordered consciousness - Induction
  2. Excitement
  3. Surgical anaesthesia
  4. Overdose
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4
Q

Induction is by…

A

Injectable anaesthetics

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5
Q

Maintenance is by…

A

Inhalational anaesthetics

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6
Q

List the injectable anaesthetics

A
  • Barbiturates
  • Propofol
  • Imidazole anaesthetics
  • Steroid anaesthetics
  • NMDAr antagonists (dissociative anaesthetics)
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7
Q

List the barbiturate anaesthetics

A
  • Pentobarbital
  • Methohexital
  • Hexobarbital
  • Thiopental
  • Thiamylal
  • Phenobarbital
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8
Q

List the steroid anaesthetics

A
  • Alfadolone
  • Alfaxolone (in fix combination)
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9
Q

Imidazole anaesthetics

A
  • Etomidate
  • Medomidate
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10
Q

NMDAr/Dissociative anaesthetics

A
  • Ketamine
  • Tiletamine
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11
Q

Other injectable anaesthetics

A
  • Propofol
  • Propanidid
  • MgSO4
  • Chloral hydrate
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12
Q

Properties of ideal injectable anaesthetics

A
  • Water + Lipid soluble
  • Sufficiently potent (volume)
  • Good analgesic activity
  • Should produce muscle relaxation
  • Non-irritant to tissue
  • Rapid + safe induction
  • High TI
  • It should have a pharmacological antagonist
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13
Q

Barbiturates: Mechanism of effects combined

A
  • GABA-BDZ-Barbiturate-receptor complex (GABAA) allosteric action.
  • Further supposed effects: Decrease in Ca2+ accumulation → inhibition in the release of transmitters
  • Stabilisation of membranes
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14
Q

Barbiturates: paradox phenomenon

A

General inhibition

  • But the sensitivity of certain structures differs
  • Some are suitable for general anaesthesia
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15
Q

Barbiturates: Pharmacological effects

A
  • CNS
  • Circulation
  • Respiration
  • Unconsciousness
  • Muscle relaxation
  • Analgesia (but not appropriate)
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16
Q

Barbiturates: Kinetics

A
  • pKa
  • Lipophilicity
  • Lipoid/water partition
  • Redistribution
  • Metabolism
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17
Q

Barbiturates are classified according to…

A

The duration of action:

  • Short-acting
  • Ultra-short acting
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18
Q

Administration of barbiturates

A

Only IV

  • Effective & harmless
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19
Q

Barbiturates: Pharmacokinetics

A
  • Duration (IV) :
    • = 15-60min (short)
    • = 5-8min (ultra-short)
  • Distribution: Fast - Complete, BBB
  • Placenta → Foetus (pronounced side effect)
  • Redistribution → Fat, muscle → Leave CNS → Wake up
  • Accumulation (fat) → Readministration Ø
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20
Q

Barbiturates: Indication

A
  • Induction, general anaesthesia (combination)
  • Convulsive state, epilepsy (pentobarbital I.v)
  • Euthanasia
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21
Q

Barbiturates: Contra-indications

A
  • Younger age (under 2 months)
  • Diminished cardia output
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22
Q

Barbiturates: Side effect

A

Small therapeutic index (Life-threatening)

  • Respiratory depression
  • Cardiovascular depression
  • Tissue irritation
  • Prenarcotic excitation (Cats)
    • Postnarcotic excitation (Horse, dog)
  • Greyhounds are oversensitive
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23
Q

List the ultra-short acting barbiturates

A
  • Thiopental
  • Methohexital
  • Hexobarbital
  • Pentobarbital
  • Thiamylal
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24
Q

Dosage: Methohexital

A

BRIETAL®

IV:

  • Large animal = 5-10mg/kg
  • Small animal = 25-30 mg/kg
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25
Dosage: Thiopental
INTRAVAL® IV: * Large animal = 5-10mg/kg * Small animal = 25-30 mg/kg
26
Dosage: Hexobarbital
NOVOPAN® IV * Horse = 10-20mg/kg * Cat = 30-40mg/kg * Lab. animals = 100mg/kg (IP)
27
Dosage: Pentobarbital
NEMBUTAL® IV * Cat & Dog = 25-35mg/kg * Lab animals = 50-80mg/kg (IP)
28
Dosage: Thiamylal
SURITAL® IV * Horse = 4-6mg/kg * Cattle = 8-12mg/kg * Dog & Cat = 10-20mg/kg
29
Pentobarbital (short-acting) effect
* IV: 15-60min duration * Anaesthesia * Euthanasia
30
Thiopental (ultra-short) effect
* IV 5-8min duration * Accumulation, slow/long wake-up * Ø Readministration * Prior to inhalational anaesthesia (rare) (side-effect)
31
Propofol: Pharmacological effect
GABAA * Unconsciousness * Muscle relaxation (good) * Analgesia (not pronounced) → Combination (opioids)
32
Propofol: Pharmacokinetics
* Duration * IV = 30-45sec → 5-15min * Quick recovery (minutes) * Distribution: fast - Complete, BBB, placenta * Quick hepatic + extrahepatic metabolism * Can be administered during liver failure * Elimination in the form of metabolites * Glucuronide conjugate
33
Propofol: Indications
* Induction and maintain general anaesthesia * TIVA (Total IV anaesthesia) with opioids and sedatohypnotics * Convulsions, epileptic seizure (rare)
34
Propofol: Contraindications
* Cardiac impairment * Respiratory impairment * Renal impairment * Hepatic impairment
35
Propofol: Side effects
* Transient apnoea during induction * Cardiovascular depression * Vomiting, excitation during recovery (rare) * Allergy, septicaemias * Increased ICP & occular pressure
36
Propofol: Proprietary products
* Narcofol inj. * Vetofol 1.0% * Fresofol® 1.0% * Diprican inj./inf. (human)
37
Propofol: Dosage
IV * Induction * Mammals = 5-6mg/kg * Reptiles & birds = 10mg/kg * Maintenance * 2.5-5mg/kg (double-bolus) * or continuous infusion = 0.1/mg/kg/min
38
List the Imidazole anaesthetics
* Etomidate * Metomidate
39
Etomidate: Pharmacological effect
GABAA receptor * Unconsciousness * Muscle Relaxation - Good * Analgesia (not pronounced) → Combination (opioids)
40
Etomidate: Pharmacokinetics
* Duration: IV = up to 10-20min * Distribution: Fast - Complete, BBB, placenta * Quick wake-up & excitation
41
Etomidate: Indications
* Induction, before inhalational anaesthesia * Combination (opioids) * Short procedures
42
Etomidate: Side effects
Broad therapeutic index * Severe tissue irritation - only IV * Respiratory depression (mild) * Cardiovascular depression Ø * Adrenocortical suppression (2-3 hours) * Pre-/postnarcortic excitation
43
Etomidate: Dosage
Mouse = 23-33mg/kg (IP)
44
Metomidate
Methyl analogue of etomidate used mainly in pigs * Moderate analgesic effect * Highly acidic * Cardio-respiratory depression is moderate * Resps. ↓ but volume ↑ * Horses: Tremors, convulsions
45
Metomidate: Dosage
* Dog = 10-15mg/kg IV * Cat = 3-5mg/kg IV * Pig 4-10mg/kg IV *(with Azaperone)* * Reptiles = 10mg/kg IM * Fish = 1-20mg/L water
46
Give a steroid anaesthetic
Alfaxalone/Alfadolone = Althesin®
47
Alphaxalone/alfadolone: Pharmacological effect
* Unconsciousness * Muscle relaxation - Good * Analgesia (not pronounced) → Combination (opioids)
48
Alphaxalone/alfadolone: Pharmacokinetics
* Onset: * IV 30sec; * IM 5-10min * Duration = up to 10-30min * Quick metabolism; Ø Accumulation * Readministration * Quick recovery
49
Alphaxalone/alfadolone: Side effect
Broad therapeutic index * Cardiovascular depression * Hypotension, negative ionotropic * Histamine release → Allergy → Necrosis (rare) * Postnarcotic excitation (rare) * Stimulation during recovery (vocalisation)
50
Alphaxalone/alfadolone: Licensed product
* Cremofor → Cat
51
NMDA-r antagonists
* Ketamine * Tiletamine
52
Ketamine: Proprietary names
* Bioketan® inj. * CP-Ketamin® inj * Narketan® inj. * Calypsol® inj. (human)
53
Tiletamine: Proprietary name
Zoletil® inj. 50/100
54
Ketamine: Pharmacological effect
An antagonist of the NMDA receptors in the CNS * Unconsciousness (species-dependent) → Catalepsy * Analgesia - Pronounced (modulation of opioid receptors) * Ø Muscle relaxation → Muscle rigidity
55
Ketamine: Pharmacokinetics
* Onset: * IV: 1min * IM: 5-10min * A relatively long duration of action - Delayed recovery (hours) * Distribution: Crosses placenta barrier * Metabolised in the liver (80%) into norketamine * Norketamine → Hydroxylised → Urine and bile
56
Ketamine: Indications
* Anaesthesia * Induction * Maintenance
57
Ketamine: Contra-indications
* Sole use in horses & dogs * Hepatic & liver impairment * Late-pregnancy
58
Ketamine: Side effects
* Catalepsy-like condition * ↑ Sympathetic tone * ↑ CO, HR, BP, arrhythmias * Mild respiratory depression, ↑ tidal volume * Salivation * Pre-/postaesthetic excitations, convulsion * ↑ ICP/eye pressure
59
Ketamine: Dosage
IM (SC, IV) 10% injection * Dogs & horses → Used in combination **ONLY** * α2-agonists
60
Ketamine: TI
Broad TI
61
Ketmaine: Metabolisation in cats and dogs
* Dog: Primary metabolized in liver * Cat: Primarily excreted by kidneys
62
Neuroleptanalgesia
A state of sedation combined with analgesia (neuroleptic + analgesic)
63
Give an example of a combination used for neuroleptanalgesia
Etorphine & Acepromazine

Pharmacology I (19 decks)

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