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Dr. Arya Mohan
19-MVM-13
NEUROLEPTANALGESIA
VPT 603 CNS PHARMACOLOGY
 Analgesia: - absence of pain
 Tranquilisation: - state of behavioral change where in
anxiety is relieved & patient is relaxed, although
aware of its surroundings
10/28/20202 CNS PHARMACOLOGY
ANALGESICS
NEUROLEPT/
TRANQUILISER
NEUROLEPTANALGESICS
NEUROLEPTANALGESIA
 A state of CNS depression & analgesia
 Characterised by profound sedation, immobilisation,
intense analgesia without loss of consciousness
 Introduced by De Castro & Mundeleer (1959) as
"anesthcsie sans barbituriques"
 Became popular in Europe as "an alternative to
general anesthesia" (Nilsson & Janssen, 1961)
10/28/20203 CNS PHARMACOLOGY
 Body becomes flaccid
 Slowing down of bodily functions such as respiration
 Also has adrenergic blocking, antiemetic,
antifibrillatic & anticonvulsant activities
 Similar to but not equal to a light plane of anesthesia
 1960’s- Phenoperidine & Haloperidol
 Early 1980’s- replaced by Fentanyl & Droperidol
10/28/20204 CNS PHARMACOLOGY
Effects show marked variation, so data on one
animal cannot be transposed on other animals
ADVANTAGES
 Produce more deeper & more reliable sedation
 Produce more reliable analgesia & less marked
respiratory depression
 Neuroleptic component abolishes the emetic effect
and lessens the bradycardia & bradyarrhythmia
produced by opioid analgesics (dogs)
 Produce a stage of immobilisation suitable for
chemical restraint of wild & exotic animals
10/28/20205 CNS PHARMACOLOGY
INDICATIONS
 In minor surgical procedures
 In diagnostic procedures
 Adjunct to local anesthetic
 Used as premedication
 Chemical restraint of wild & ferocious animals
10/28/20206 CNS PHARMACOLOGY
10/28/2020CNS PHARMACOLOGY7
NEUROLEPTANALGESICS
FENTANYL & DROPERIDOL
 Fentanyl- potent opioid agonist
 Droperidol- butyrephenone neuroleptic sedative
 In a ratio 1:50- INNOVAR- VET
 Droperidol potentiates the analgesic effect of Fentanyl
 Droperidol is a potent D₂ receptor antagonist with Histamine
& 5HT antagonist activity
 Possess central antiemetic action, reduce motor tone &
causes tranquilisation & sedation
 Fentanyl acts at μ opioid receptors & produce analgesia
10/28/20208 CNS PHARMACOLOGY
 Combined effect in dogs include a decreased heart
rate secondary to increased vagal tone & decrease in
arterial BP
 In cats heart rate is increased with decrease in BP
PHARMACOKINETICS
 Onset of action within 30-40 min
 Remain sedated for hours
 Metabolised in liver
 Eliminated in urine
10/28/20209 CNS PHARMACOLOGY
SIDE EFFECTS
 Are dose dependent- overdosage
 Bradycardia, respiratory depression, salivation, nystagmus &
defecation
 Wood chest syndrome in dogs & humans after rapid i/v
 Thoracic musculature is rigid & interferes with normal
ventilatory function
 Attributed to Fentanyl & is reversed by Naloxone
 CNS stimulation, ataxia & abnormal behavior in pigs
 Irritation & pain at site of injection
 Overdosage- profound respiratory & CNS depression
10/28/202010 CNS PHARMACOLOGY
CONTRAINDICATIONS
 Not used in food animals
 Perivascular injection avoided- tissue irritation
 Not recommended in cats, horses & ruminants – CNS
stimulation
 Should not be used along with barbiturates in C-section-
hazardous to neonates
 Administration of Atropine prior can prevent bradycardia
& salivation
 Approved for use only in dogs
@0.1-0.15 ml/Kg im & 0.04-0.08ml/Kg iv
10/28/202011 CNS PHARMACOLOGY
0.4mg Fentanyl &
20mg Droperidol in
each ml
ETORPHINE &
ACEPROMAZINE
 Used for immobilisation of various domestic & exotic
species
 Etorphine- Opioid agonist
 Acepromazine- phenothiazine tranquiliser
 Acepromazine is a potent dopamine receptor antagonist
with some histamine, serotonin, muscarinic & α
adrenergic receptor blocking actions
 Etorphine is an opioid agonist widely used to
immobilize large domestic & wild animals such as
elephants 10/28/202012
 Recommended in domestic animals such as horses,
pigs, cattle & sheep
 Combination causes marked & persistent
tachycardia, transient rise in BP, increased muscle
tone & mydriasis
 Highly toxic to humans- should wear gloves
 Immobilisation should not be used without
availability of an opioid antagonist Naloxone
10/28/202013 CNS PHARMACOLOGY
Highly potent neuroleptanalgesic supplied
along with antagonist Diprenorphine
10/28/202014 CNS PHARMACOLOGY
Contain 2.45mg/ml Etorphine with
Acepromazine 10mg/ml in IMMOBILON
& 3mg/ml Diprenorphine in REVIVON
FENTANYL & FLUANISONE
 Recommended in dogs, primates & rabbits
 Fluanisone- butyrephenone derivative
 Fentanyl @ 0.325mg/ml & Fluanisone @ 10mg/ml
10/28/202015 CNS PHARMACOLOGY
Other Combinations
COMBINATION SPECIES
ETORPHINE &
METHOTRIMEPRAZINE
Dogs
BUTORPHANOL & MEDETOMIDINE Dogs & Cats
BUTORPHANOL & XYLAZINE Horses
BUTORPHANOL & DETOMIDINE Horses
BUTORPHANOL & ACEPROMAZINE Horses
METHADONE & ACEPROMAZINE Horses
METHADONE & XYLAZINE Horses
MORPHINE & XYLAZINE Horses
PETHIDINE & ACEPROMAZINE Dogs & Horses
BUPRENORPHINE &
ACEPROMAZINE
Dogs & Cats
OXYMORPHONE & ACEPROMAZINE Dogs & Cats 10/28/2020
16
CNS PHARMACOLOGY
NEUROLEPTANESTHESIA
 Concurrent administration of 65-70% N₂O to
neuroleptanalgesics
 State of amnesia is produced
 Patient completely detached from environment
 Loss of consciousness
 Loss of ability to obey commands & communicate
 Inability to move or change position
 Fentanyl + Droperidol + N₂O
10/28/202017 CNS PHARMACOLOGY
10/28/202018 CNS PHARMACOLOGY

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Neuroleptanalgesia

  • 2.  Analgesia: - absence of pain  Tranquilisation: - state of behavioral change where in anxiety is relieved & patient is relaxed, although aware of its surroundings 10/28/20202 CNS PHARMACOLOGY ANALGESICS NEUROLEPT/ TRANQUILISER NEUROLEPTANALGESICS
  • 3. NEUROLEPTANALGESIA  A state of CNS depression & analgesia  Characterised by profound sedation, immobilisation, intense analgesia without loss of consciousness  Introduced by De Castro & Mundeleer (1959) as "anesthcsie sans barbituriques"  Became popular in Europe as "an alternative to general anesthesia" (Nilsson & Janssen, 1961) 10/28/20203 CNS PHARMACOLOGY
  • 4.  Body becomes flaccid  Slowing down of bodily functions such as respiration  Also has adrenergic blocking, antiemetic, antifibrillatic & anticonvulsant activities  Similar to but not equal to a light plane of anesthesia  1960’s- Phenoperidine & Haloperidol  Early 1980’s- replaced by Fentanyl & Droperidol 10/28/20204 CNS PHARMACOLOGY Effects show marked variation, so data on one animal cannot be transposed on other animals
  • 5. ADVANTAGES  Produce more deeper & more reliable sedation  Produce more reliable analgesia & less marked respiratory depression  Neuroleptic component abolishes the emetic effect and lessens the bradycardia & bradyarrhythmia produced by opioid analgesics (dogs)  Produce a stage of immobilisation suitable for chemical restraint of wild & exotic animals 10/28/20205 CNS PHARMACOLOGY
  • 6. INDICATIONS  In minor surgical procedures  In diagnostic procedures  Adjunct to local anesthetic  Used as premedication  Chemical restraint of wild & ferocious animals 10/28/20206 CNS PHARMACOLOGY
  • 8. FENTANYL & DROPERIDOL  Fentanyl- potent opioid agonist  Droperidol- butyrephenone neuroleptic sedative  In a ratio 1:50- INNOVAR- VET  Droperidol potentiates the analgesic effect of Fentanyl  Droperidol is a potent D₂ receptor antagonist with Histamine & 5HT antagonist activity  Possess central antiemetic action, reduce motor tone & causes tranquilisation & sedation  Fentanyl acts at μ opioid receptors & produce analgesia 10/28/20208 CNS PHARMACOLOGY
  • 9.  Combined effect in dogs include a decreased heart rate secondary to increased vagal tone & decrease in arterial BP  In cats heart rate is increased with decrease in BP PHARMACOKINETICS  Onset of action within 30-40 min  Remain sedated for hours  Metabolised in liver  Eliminated in urine 10/28/20209 CNS PHARMACOLOGY
  • 10. SIDE EFFECTS  Are dose dependent- overdosage  Bradycardia, respiratory depression, salivation, nystagmus & defecation  Wood chest syndrome in dogs & humans after rapid i/v  Thoracic musculature is rigid & interferes with normal ventilatory function  Attributed to Fentanyl & is reversed by Naloxone  CNS stimulation, ataxia & abnormal behavior in pigs  Irritation & pain at site of injection  Overdosage- profound respiratory & CNS depression 10/28/202010 CNS PHARMACOLOGY
  • 11. CONTRAINDICATIONS  Not used in food animals  Perivascular injection avoided- tissue irritation  Not recommended in cats, horses & ruminants – CNS stimulation  Should not be used along with barbiturates in C-section- hazardous to neonates  Administration of Atropine prior can prevent bradycardia & salivation  Approved for use only in dogs @0.1-0.15 ml/Kg im & 0.04-0.08ml/Kg iv 10/28/202011 CNS PHARMACOLOGY 0.4mg Fentanyl & 20mg Droperidol in each ml
  • 12. ETORPHINE & ACEPROMAZINE  Used for immobilisation of various domestic & exotic species  Etorphine- Opioid agonist  Acepromazine- phenothiazine tranquiliser  Acepromazine is a potent dopamine receptor antagonist with some histamine, serotonin, muscarinic & α adrenergic receptor blocking actions  Etorphine is an opioid agonist widely used to immobilize large domestic & wild animals such as elephants 10/28/202012
  • 13.  Recommended in domestic animals such as horses, pigs, cattle & sheep  Combination causes marked & persistent tachycardia, transient rise in BP, increased muscle tone & mydriasis  Highly toxic to humans- should wear gloves  Immobilisation should not be used without availability of an opioid antagonist Naloxone 10/28/202013 CNS PHARMACOLOGY
  • 14. Highly potent neuroleptanalgesic supplied along with antagonist Diprenorphine 10/28/202014 CNS PHARMACOLOGY Contain 2.45mg/ml Etorphine with Acepromazine 10mg/ml in IMMOBILON & 3mg/ml Diprenorphine in REVIVON
  • 15. FENTANYL & FLUANISONE  Recommended in dogs, primates & rabbits  Fluanisone- butyrephenone derivative  Fentanyl @ 0.325mg/ml & Fluanisone @ 10mg/ml 10/28/202015 CNS PHARMACOLOGY
  • 16. Other Combinations COMBINATION SPECIES ETORPHINE & METHOTRIMEPRAZINE Dogs BUTORPHANOL & MEDETOMIDINE Dogs & Cats BUTORPHANOL & XYLAZINE Horses BUTORPHANOL & DETOMIDINE Horses BUTORPHANOL & ACEPROMAZINE Horses METHADONE & ACEPROMAZINE Horses METHADONE & XYLAZINE Horses MORPHINE & XYLAZINE Horses PETHIDINE & ACEPROMAZINE Dogs & Horses BUPRENORPHINE & ACEPROMAZINE Dogs & Cats OXYMORPHONE & ACEPROMAZINE Dogs & Cats 10/28/2020 16 CNS PHARMACOLOGY
  • 17. NEUROLEPTANESTHESIA  Concurrent administration of 65-70% N₂O to neuroleptanalgesics  State of amnesia is produced  Patient completely detached from environment  Loss of consciousness  Loss of ability to obey commands & communicate  Inability to move or change position  Fentanyl + Droperidol + N₂O 10/28/202017 CNS PHARMACOLOGY