Lecture 16-17 - anaesthetics Flashcards
Definition of anaesthesia
- lack of sensation, total loss of motoric activity
- local: without loss of consciousness
- general: total loss of consciousness
The stages and signs of general anaesthesia?
Stage 1: disordered consciousness - induction
Stage 2: excitement
Stage 3: surgical anesthesia (ie. unconsciousness, amnesia, immobility, unresponsive to surgical stimulation)
Stage 4: overdose
Injectable anaesthetics (+ examples)
- barbiturates (pentobarbitlal, hexobarbital)
- propofol
- imidazole anaesthetics (etomidate, medomidate)
- steroid anaesthetics (alfadolone, alfaxolone)
- NMDAr antagonists
- dissociative anaesthetics (ketamine, tiletamine)
Properties of ideal injectable anaesthetics
- 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
Barbiturates
- pharmacological effets
- kinetics
- classification
- application
- effects: CNS, circulation, respiration
- kinetics: pKa, lipophylicity, lipoid/water partition, redistribution, metabolism
- classification: short acting, ultra-short acting
- application: IV, effective and harmless
Long, middle-long acting barbiturates?
- allobarbital
- amobarbital
- barbital
- phenobarbital
Short, ultra-short acting barbiturates?
- pentobarbital
- methohexital
- hexobarbital
- thiopental
- thiamylal
- venobarbital
Barbiturates (ultra-short acting)
- pharmacological effect
- pharmacokinetics
- indication
- 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
Barbiturates (ultra-short acting)
- side effects
- dose
- 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
Pentobarbital (short)
- IV, 15-60 min duration
- anaesthesia, euthanasia
Thiopental (ultra-short)
- IV, 5-8 min duration
- accumulation, slow/long wake up
- Ø re-administration
- prior to inhalation anaesthesia (rarely), side effects
Propofol
- pharmacological effect GABAa
- pharmacokinetics
- elimination
- 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
Propofol
- indications
- side effects
- dose
- indications: induction and maintain general anaesthesia, TIVA with opioids and sedatohypnotics, convulsions, epileptic seizure (rarely)
- contra indications: cardiac. respiratory,
renal, hepatic impairment
- contra indications: cardiac. respiratory,
- 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
- induction: 5-6 (mammalians), 10 (reptile
Etomidate (imidazole)
- pharmacological effects
- pharmacokinetics
- 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
Etomidate (imidazole)
- indication
- side effets
- dose
- 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
Metomidate (imidazole)
- 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
Steroid anaesthetics
- pharmacological effects
- pharmacokinetics
- side effects
- licenced product
- 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)
Ketamine (NMDA receptor antagonist)
- pharmacological effects
- pharmacokinetics
- 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
Ketamine (NMDA receptor antagonist)
- indications
- side effects
- administration
- indications: anaesthesia (in comb), induction and maintenance
- contra indications: sole use in horses and
dogs, hepatic and/or liver impairment,
late pregnancy
- contra indications: sole use in horses and
- 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
Zoletil
- 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
Combined anaesthesia
- balanced anaesthesia
- TIVA
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
Neuroleptanalgesia
- 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)
Inhalational anaesthetics
- halothane
- isoflurane
- sevoflurane
- dinitrogen mooxide
- desflurane
- methoxyflurane
—-> all organic halogenated (liquid, more stable, increased
efficacy)
Criteria for the efficacy
Inhaled air -> alveolar air -> blood -> brain