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Pharma midterm 1 > Lecture 16-17 - anaesthetics > Flashcards

Lecture 16-17 - anaesthetics Flashcards

1
Q

Definition of anaesthesia

A
  • lack of sensation, total loss of motoric activity
    • local: without loss of consciousness
    • general: total loss of consciousness
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2
Q

The stages and signs of general anaesthesia?

A

Stage 1: disordered consciousness - induction
Stage 2: excitement
Stage 3: surgical anesthesia (ie. unconsciousness, amnesia, immobility, unresponsive to surgical stimulation)
Stage 4: overdose

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3
Q

Injectable anaesthetics (+ examples)

A
  • barbiturates (pentobarbitlal, hexobarbital)
  • propofol
  • imidazole anaesthetics (etomidate, medomidate)
  • steroid anaesthetics (alfadolone, alfaxolone)
  • NMDAr antagonists
  • dissociative anaesthetics (ketamine, tiletamine)
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4
Q

Properties of ideal injectable anaesthetics

A
  • water + lipid soluble
  • sufficiently potent (volume)
  • possess good analgesic activity
  • produce muscle relaxation
  • non-irritant to tissue
  • rapid and safe induction and recovery
  • limited effect on vital functions
  • have high TI
  • not have direct reno- and hepatotoxicity
  • rapid metabolism
  • neither chemical nor pharmacological incompatibility should occur
  • have pharmacological antagonist
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5
Q

Barbiturates

  • pharmacological effets
  • kinetics
  • classification
  • application
A
  • effects: CNS, circulation, respiration
  • kinetics: pKa, lipophylicity, lipoid/water partition, redistribution, metabolism
  • classification: short acting, ultra-short acting
  • application: IV, effective and harmless
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6
Q

Long, middle-long acting barbiturates?

A
  • allobarbital
  • amobarbital
  • barbital
  • phenobarbital
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7
Q

Short, ultra-short acting barbiturates?

A
  • pentobarbital
  • methohexital
  • hexobarbital
  • thiopental
  • thiamylal
  • venobarbital
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8
Q

Barbiturates (ultra-short acting)

  • pharmacological effect
  • pharmacokinetics
  • indication
A
  • effect: unconsciousness, muscle relaxation
  • pharma: duration iv short: 15-60 min, ultra-short: 5-8 min. Fast distribution, able to cross blood-brain barrier. Redistribution in fat and muscle
  • indication: induction, general anaesthesia (combination), convulsive state, epilepsy, euthanasia
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9
Q

Barbiturates (ultra-short acting)

  • side effects
  • dose
A
  • side effects: small TI, respiratory depression (neonates), cardiovascular depression, tissue irritation, prae/postnarcotic excitations
  • dose: mg/kg bw (depends on specie and drug)
    Thiopental, metohexital:
    • large animal: 5-10
    • small pets: 25-30 IV
      Hexobarbital
    • horse: 10-20
    • cat: 30-40 IV
    • lab animals: 100 IP
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10
Q

Pentobarbital (short)

A
  • IV, 15-60 min duration

- anaesthesia, euthanasia

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11
Q

Thiopental (ultra-short)

A
  • IV, 5-8 min duration
  • accumulation, slow/long wake up
  • Ø re-administration
  • prior to inhalation anaesthesia (rarely), side effects
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12
Q

Propofol

  • pharmacological effect GABAa
  • pharmacokinetics
  • elimination
A
  • effects: unconsciousness, muscle relaxation, analgesia in combination with opioids
  • pharma: duration IV 30-45 min (up to 5-15 min). Fast - complete distribution, blood brain barrier, placenta. Quick hepatic + extrahepatic metabolism
  • elimination: in urine in form of metabolites, mainly as glucuronide conjugate or other inactive forms
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13
Q

Propofol

  • indications
  • side effects
  • dose
A
  • indications: induction and maintain general anaesthesia, TIVA with opioids and sedatohypnotics, convulsions, epileptic seizure (rarely)
    • contra indications: cardiac. respiratory,
      renal, hepatic impairment
  • side effects: transient apnoea during induction, cardiovascular depression, vomiting, excitation during recovery, allergy, septicaemias, increased ICP and ocular pressure
  • dose: mg/kg IV
    • induction: 5-6 (mammalians), 10 (reptile
      and bird)
    • maintenance: 2.5-5 (second bolus) or
      continuous infusion 0.1/min
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14
Q

Etomidate (imidazole)

  • pharmacological effects
  • pharmacokinetics
A
  • effects: unconsciousness, muscle relaxation, analgesia in combination with opioids
  • pharma: duration IV up to 10-20 min. Fast - complete distribution, blood brain barrier, placenta. Quick wake up + excitation
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15
Q

Etomidate (imidazole)

  • indication
  • side effets
  • dose
A
  • indication: induction (before inhalational anaesthesia), combination (opioids)
  • side effects: broad TI, respiratory depression (mild), cardiovascular insufficiency, tissue irritation (acidic pH, only IV), prae/postnarcotic excitations, adrenocortical suppression
  • dose: mouse 23-33 mg/kg bw IP
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16
Q

Metomidate (imidazole)

A
  • commonly used in pigs
  • moderate analgesic effect
  • highly acidic, IV only into large veins
  • frequent prae/post anaesthetic excitation
  • moderate cardio-respiratory depression
  • dose: mg/kg
    • pig: 4-10 IV (with azaperone)
    • dog: 10-15 IV
    • cat: 20-25 IV
17
Q

Steroid anaesthetics

  • pharmacological effects
  • pharmacokinetics
  • side effects
  • licenced product
A
  • effects: unconsciousness, muscle relaxation, analgesia in combination with opioids
  • pharma: IV 30 min, IM 5-10, duration up to 10-30 min. Quick metabolism, quick recovery
  • side effects: broad TI, cardiovascular depression, histamine release, postnarcotic excitation
  • product: cremofor (cat), cyclodextrine (dog, cat)
18
Q

Ketamine (NMDA receptor antagonist)

  • pharmacological effects
  • pharmacokinetics
A
  • effects: unconsciousness (specie dependent), analgesia, muscle rigidity
  • pharma: onset IV 1 min, IM 5-10 min, relative long duration of action, distribution- crosses placenta barrier, metabolised in liver (80%) into norketamine which is excreted in urine and bile
19
Q

Ketamine (NMDA receptor antagonist)

  • indications
  • side effects
  • administration
A
  • indications: anaesthesia (in comb), induction and maintenance
    • contra indications: sole use in horses and
      dogs, hepatic and/or liver impairment,
      late pregnancy
  • catalepsy, increased symp. nervous system tone, increased cardiac output, heart rate and blood pressure, mild respiratory depression, salivation, prae/post anaesthetic excitation, hallucinations
  • admin: IM (SC, IV) (5) - 10 % injection
    • dogs, horses only in combinations
20
Q

Zoletil

A
  • very fast onset unconsciousness (2-5 min)
  • side effects: increased sympathetic tone, dose dependent respiratory depression, pain response when the drug is given by the IM or SC
  • dose: cats 10-15 mg/kg, dogs 5-10 mg/kg
21
Q

Combined anaesthesia

  • balanced anaesthesia
  • TIVA
A

Balanced anaesthesia

  • combination of antimuscarinics, sedatives, opioids, anaesthetics and muscle relaxants
  • goal: “good sleep”, safe and deep anaesthesia, pain control, less side effects, relaxed body, smooth recovery

TIVA (total intravenous anaesthesia)

  • combination of agents given exclusively by the intravenous route without the use of inhalation agents
  • eg: propofol + fentanyl + lidocaine + ketamine
22
Q

Neuroleptanalgesia

A
  • a sate sedation combines with analgesia
  • similar, but not equal to a light plane anaesthesia
  • animal does not respond to pain or surroundings, but is not totally unconscious
  • advantages: less amount of sedatives (safer), prior anaesthesia (safer induction, analgesia more pronounced)
23
Q

Inhalational anaesthetics

A
  • halothane
  • isoflurane
  • sevoflurane
  • dinitrogen mooxide
  • desflurane
  • methoxyflurane
    —-> all organic halogenated (liquid, more stable, increased
    efficacy)
24
Q

Criteria for the efficacy

A

Inhaled air -> alveolar air -> blood -> brain

25
Q

Halothane

A
  • most efficacious
  • induction/arousal phases are long
  • excitements are frequent
  • obese animal –> delayed awake
  • dose: induction 4 - 5%, maintenance 1.5 - 2.5%
26
Q

Isoflurane

A
  • indications: induction and maintain general anaesthesia
    • contra indications: younger age, pregnant,
      lactating animals, susceptibility to malignant
      hyperthermia
  • side effects: cardiovascular and respiratory depression, cardiac arrhytmias, malignant hyperthermia
  • dose: induction 2-5 %, maintenance 0.25-3 %
27
Q

Sevoflurane

A
  • indications: induction and maintain general anaesthesia
    • contra indications: younger age, pregnant,
      lactating animals, susceptibility to malignant
      hyperthermia
  • side effects: cardiovascular and respiratory depression, cardiac arrhytmias
  • dose: induction 5 - 7 %, maintenance 3.3 - 3.8 %
28
Q

Desflurane

A
  • side effects are more common that of formerly mentioned drugs: respiratory tract irritation, tachycardia
29
Q

Methoxyflurane

A
  • because of low gas-tension and excitements more preferred to use for maintenance
  • respiratory inhibition is more pronounced
  • contraindicated in reptiles, strong nephrotoxicity

Pharma midterm 1 (14 decks)

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