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282074
Analgesics
Description
Doctorate Anaesthesia Mind Map on Analgesics, created by melian.yates on 16/10/2013.
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anaesthesia
anaesthesia
doctorate
Mind Map by
melian.yates
, updated more than 1 year ago
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Created by
melian.yates
almost 11 years ago
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Resource summary
Analgesics
Opiods
Morphine
Morphine analogue
Naloxon (Antagonist)
Synthetic Derivatives
Phenylpiperdine series
Pethidine
Fentanyl
Methadone series
Methadone
Semisynthetic Thebaine derivatives
Etorphine
Immobilin
Very potent
Buprenorphine
Large animals
Partial Agonist
Metabolism
First pass metabolism w/ PO (???)
Conjugated in Liver
Morphine - 6- glucuronide => Active analgesic
Absorption
Oral (Variable)
IV
NOT Pethidine
IM
S/C
Intrathecal
Distribution
Morphine analogues t 1/2: 3 - 6 hrs
Elimination
Morphine Glucuronides excreted in urine
Glucuronides hydrolysed in gut, but Morphine reabsorbed
Enterohepatic circulation
Side effects
Sedation
Respiratory Depression
Negative Chronotrophy
Except Pethidine
Emesis (Morphine)
Dysphoria
Histamine release
Pethidine
Why given IM vs. IV
Decreased GI motility
Opiod Receptors
GPCRs
INHIBIT Adenylate cyclase
Decrease cAMP
Promote opening of K+ channels
Inhibit opening of voltage gated Ca2+ channels
Blocks/reduces transmission to higher brain centers
Prevents perception of pain
u- receptors (MOP)
CNS (Cerebral cortex, basal ganglia, spinal cord, PAG)
Analgesia (Resp. depression, Decreases gut motility, CVS depression)
k-receptors (KOP)
Spinal Analgesia
Delta - receptors (DOP)
Supraspinal & Spinal Analgesia
Mood regulation ?
NOP receptor
Supraspinal & Spinal
Omega receptors
Not selctive Opiod receptors
Dysphoria
CNS
Analgesia
Acute & Chronic pain
Sedation
Dysphoria
Emesis
Myosis
u & k receptors (Oculomotor nucleus)
Reduced GI motility
Codeine & Loperamide
Resp.
Respiratory Center (Medulla Oblongata): Decreased sensitivity to Pco2
Cough suppression
GI
Histamine release
Bronchoconstriction & Hypotension
NSAIDs
Peri-operative analgesia
Local Anaesthetics
Absorption
Available as solutions for:
Injection
Sprays
Creams
Gels
Formulated as hydrochlroide salt
Usually administered around nerves requiring block
Absorption depends on pKa
Infected tissue has a lower pH than normal, therefore local anaesthetic absorption is impaired
Local infiltration
Splash blocks
Specific nerve blocks
IVRA
Extradural
Topical
EMLA (Eutectic mixture of Local Anaesthetic)
Mixture of Anaesthetics w/ a single chemical composition
Ex. Lidocaine & Prilocaine
Cause Vasodilation, thus Vasoconstrictors added to reduce systemic absorption
Ex. + Adrenalin
Cocaine causes Vasoconstriction
Distribution
Higher PPB, longer duration
Ex. Lidocaine: PPB = 65%
Ex. Bupivicaine: PPB = 95%
Bupivicaine > Ropivicaine>Lidocaine > Prilocaine
Albumin & alpha 1-Acid Glycoprotein
Free drug crosses the placenta & can become trapped if the Foetus is acidotic
Metabolism and Excretion
Esters
Broken down by Plasma Cholinesterases (Inactivates)
Excreted by kidneys
PABA metabolite
Amides
Metabolized by Hepatic Amidases
Excreted by kidneys
Side Effects
CNS
Tremors
Convulsions
Respiratory Depression
CVS
Reduced myocardial contractility
Vasodilation
Low BP
Bupivicaine especially Cardiotoxic
Reduces tissue repair
Inadvertent IV administration
Tissue Irritation
Allergic Rxns
NMDA Antagonists
NMDA (N-methyl-D-aspartate) Receptor
Found in CNS
Receptors for Excitatory Amino Acids (EAA)
Binding of EAA modulates pain transmission => Enhancing pain perception
Glutamate
Aspartate
Block EAA receptors
Reduces pain modulation & CNS activity
Low doses: Analgesia
High doses: Dissociative Anaesthesia
Ketamine
Dogs, Cats, Horses
Cyclohexane derivative
Uses
Peri-operative & Intra-operative Analgesia
Chemical Restraint
Dissociative anaesthesia
Chronic pain
Inhibits central sensitization
Absorption
Bolus
CRI
Alpha 2 Agonists
Intra-operative Analgesics
Medetomidine
Dexmedetomidine
Cats, Dogs, Horses
Reversed
Unlicensed Products
Tramadol
Atypical synthetic Opiod
1/10th potency of Morphine
Binds MOP receptors
But also INHIBITS re-uptake of Seratonin and NA in the CNS
Tx of Chronic pain
No Tissue damage
Gabapentin
Stabilizes electrical nerve activity
Decreases nerve firing
Analgesic (Neuropathic pain)
Nitrous Oxide (N2O)
Colorless, Non-flammable gas
Anaesthetic sparing
Little cardiac effects
Media attachments
Morphine (image/png)
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