BIOMED

INDIAN DENTAL ACADEMY
Leader in continuing dental education
www.indiandentalacademy.com
www.indiandentalacademy.co...
Pain medication
 Paracetamol
 NSAIDs
 Opioids
 Steroids,

radiation, TENS, acupuncture
www.indiandentalacademy.com
Physiology
 Afferent,

peripheral nerves C and A δ

0,5-1,5 µm, <1 m/s,
unmyelinated

 C-fibres

 Aδ-fibrer

1-5 µm, 5-...
www.indiandentalacademy.com
Pain pathways

 Tissue

damage releases bradykinin, serotonin,
histamin, lactate, ATP, ADP, potassium (among
others)

 G...
Pain, pathways
 Nociceptive

neurons in dorsal root ganglion
 Relays via tractus spinothalamicus,
spinomesencephalicus a...
Pain, pathways
 Brain

- upwards probably glutamat main
transmittor

 Downwards

neurons GABA, ACh,
monoamines (serotoni...
Endogenous opioids
 Endorphin,

enkephalin, dynorphin

 Spinal

tract dynorphin interneuron,
enkephalin downward inhibit...
Opioid receptor

 Receptors

in brain and spinal cord
 4 subtypes: µ(my), δ, κ and NOP (ORL-1)
www.indiandentalacademy.c...
Opioid receptor

 G-protein
 Intra/extracellular,

intramembranous
 Pre- and postsynaptic membranes
www.indiandentalaca...
NMDA-receptor
 N-metyl-D-Aspartate
 Learning
 Activation

makes spinal neurons more
sensitive to pain stimulus
 Long-t...
Glutamat
 Presynaptic

ion channel calcium influx 
glutamat release

 Crosses

synapse and binds to NMDAreceptors posts...
Pre- and postsynaptic binding
 G-protein
 Lower

inhibits adenylate cyclase

content intracellular cAMP

 Opens

K+, in...
The opioid receptor

www.indiandentalacademy.com
The opioid receptor
 µ, δ , κ
 identical around 70%
 G-protein binds to 3rd receptor loop

www.indiandentalacademy.com
The opioid receptor µ (mu)
 Mainly

analgesic effects
 Respiratory depression
 Nausea / vomiting
 Constipation
 Cough...
The opioid receptor δ (delta)
 Probably
 Some

effects outside the CNS

analgetic effekts

 Seizures?
 Least

knowledg...
The opioid receptor κ (kappa)
 Analgesia
 Nausea

on mainly spinal cord level

and dysphoria

 Psychotomimetic

effects...
Side effects - mechanisms
 Respiratory

depression
Respiratory centre (medulla oblongata)
Less CO2 stimulation
Decreased ...
Side effects - mechanisms
 Constipation

peripheral and central affection
less GI movement and increased tonus
No toleran...
Side effects - Mechanisms
 Sedation

Overdose
Wrong strategy
Sleep dept

www.indiandentalacademy.com
Drugs
(µ-receptors)
morphine, metadon, fentanyl, heroin

 Agonists

 Partial agonists

buprenorfin, kodein, tramadol
 A...
What is an opioid?
 Alkaloid

(plant) or synthetic

 Morphine

like effekts, inhibited by naloxon

www.indiandentalacade...
Opium

 Narcotic resin from opium poppies:

morphine 10%, noskapin 6%, papaverin 1%, kodein
0,5%

www.indiandentalacademy...
History
 3400

BC
Opium puppies grown in Mesopotamia

 460

BC
Hippocrates medicine (psychiatric disease
and epidemies)
...
History
 330

BC
Alexander the Great introduces opium to Persia
and India

 400

AD
Opium with traders to China

 Parce...
History
 Morphin

1806
 Kodein 1832
 Heroin 1832

www.indiandentalacademy.com
Morphin

 C17H19NO3
 Greek.

Morpheus (God of dreams)
 1806 from opium
 1956 chemical structure

www.indiandentalacade...
Morphine

 Half

life 2-4 hours
 Bioavailability 10-50% (30%)
 Distribution volume 3L/kg
 Bioaactive morphine-6-glucur...
Heroin


C21H23NO5 (morphin
C17H19NO3)

 Higher

fat solubility
 Produced 1874
 Bayer 1899
 Drug Sweden until
1964
 ...
Kodein
 C18H21NO3 (morfin

C17H19NO3)

 Produced

1832
 Low receptor affinity
 10% into morphine  M6G
 7-10% non-res...
Dextropropoxifen
 Half

time 8-18 (90) hours
 Active metabolite norpropoxyfen
 Metabolite half life 30-45 (100) hours
...
Tramadol
 Halflife

4-6 hours
 Active metabolite D-desmetyltramadol
 Halflife metabolite 9-12 hours
 5-10% non-respond...
Fentanyl
 ”Complicated

kinetics”
 Halflife 1 min, 8 min, 8 tim
 Active metabolites unknown
 10mg morfin  0,05 mg fen...
Pethidine
 synthetic
 Most

opioid

histamine release. Seizures.

 100mg

 10mg morphine

 Shivering

www.indiandenta...
Ketogan
 Ketobemidon(hydroklorid)
 NMDA

– receptor antagonist?
 Halflife 2-4 hours
 Unknown metabolite activity
 Abu...
Oxicodon
 Halflife

2-4 timmar
 Probably inaktiva metaboliter
 10mg morfin  5mg oxikodon

www.indiandentalacademy.com
Metadon
 NMDA-receptor

antagonist ?
 Halflife 15-40 hours
 ”Bad reputation”
 Advanced pain treatment

www.indiandenta...
Clinical use
 Cancer

pain
 Postoperative pain
 Long-term pain ?
 Neurogenic pain?
 ”Always” in combination with para...
Intoxication
 Mios

(small pupils)
 Lower conscience
 Breathing

www.indiandentalacademy.com
Antidote – Naloxone (Narcanti)
 opioid

antagonist
 reverses endogenous and exogenous
substanses and acupuncture
 effec...
Abstinence
 sweating,

fever (”cold turkey”), shakings,
muscular cramps, itching, diarrhea,
nausea, vomiting (the flu)

...
Cold Case
 Cancer
 Current

medication:
Tb. Dolcontin (longacting morphine)
60mgx2
Tb. Morphine (shortacting) 20mg as re...
Patientfall
 Patient

insatt på Ketogan tablett 5mgx6
med god effekt. Översatt till Dolcontin
20mgx2. Inkommer efter 1 ve...
Afterlife …..
 Morphina
 Renal
 Treat

is currently Golden Standard

failure

pain!

www.indiandentalacademy.com
www.indiandentalacademy.com
Leader in continuing dental education

www.indiandentalacademy.com
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Biomed /certified fixed orthodontic courses by Indian dental academy

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The Indian Dental Academy is the Leader in continuing dental education , training dentists in all aspects of dentistry and offering a wide range of dental certified courses in different formats.

Indian dental academy provides dental crown & Bridge,rotary endodontics,fixed orthodontics,
Dental implants courses.for details pls visit www.indiandentalacademy.com ,or call
0091-9248678078

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Biomed /certified fixed orthodontic courses by Indian dental academy

  1. 1. BIOMED INDIAN DENTAL ACADEMY Leader in continuing dental education www.indiandentalacademy.com www.indiandentalacademy.com
  2. 2. Pain medication  Paracetamol  NSAIDs  Opioids  Steroids, radiation, TENS, acupuncture www.indiandentalacademy.com
  3. 3. Physiology  Afferent, peripheral nerves C and A δ 0,5-1,5 µm, <1 m/s, unmyelinated  C-fibres  Aδ-fibrer 1-5 µm, 5-35 m/s, myelinated (larger Aβ touch, vibration, proprioception) www.indiandentalacademy.com
  4. 4. www.indiandentalacademy.com
  5. 5. Pain pathways  Tissue damage releases bradykinin, serotonin, histamin, lactate, ATP, ADP, potassium (among others)  Glutamate (excitatory) transmittor in dorsal horn synapse  GABA (inhibitory) transmittor interneuron www.indiandentalacademy.com
  6. 6. Pain, pathways  Nociceptive neurons in dorsal root ganglion  Relays via tractus spinothalamicus, spinomesencephalicus and spinoreticularis  Reaches thalamus and pons  Connects to cortex  Inhibitory neurons  Inhibitory mechanoreceptors www.indiandentalacademy.com
  7. 7. Pain, pathways  Brain - upwards probably glutamat main transmittor  Downwards neurons GABA, ACh, monoamines (serotonin, NA, DA). www.indiandentalacademy.com
  8. 8. Endogenous opioids  Endorphin, enkephalin, dynorphin  Spinal tract dynorphin interneuron, enkephalin downward inhibitory neurons.  In brain around ”pain centre” but also in areas not involved in nociception and nonneuronal tissues www.indiandentalacademy.com
  9. 9. Opioid receptor  Receptors in brain and spinal cord  4 subtypes: µ(my), δ, κ and NOP (ORL-1) www.indiandentalacademy.com
  10. 10. Opioid receptor  G-protein  Intra/extracellular, intramembranous  Pre- and postsynaptic membranes www.indiandentalacademy.com
  11. 11. NMDA-receptor  N-metyl-D-Aspartate  Learning  Activation makes spinal neurons more sensitive to pain stimulus  Long-term C-fiberstimulation activates NMDA  central sensitisation  NMDA-antagonists www.indiandentalacademy.com
  12. 12. Glutamat  Presynaptic ion channel calcium influx  glutamat release  Crosses synapse and binds to NMDAreceptors postsynapticly  depolarisation  hyperexcitability in nociceptive neurons www.indiandentalacademy.com
  13. 13. Pre- and postsynaptic binding  G-protein  Lower inhibits adenylate cyclase content intracellular cAMP  Opens K+, inhibits Ca2+  Inhibits pre-synaptic release of glutamat www.indiandentalacademy.com
  14. 14. The opioid receptor www.indiandentalacademy.com
  15. 15. The opioid receptor  µ, δ , κ  identical around 70%  G-protein binds to 3rd receptor loop www.indiandentalacademy.com
  16. 16. The opioid receptor µ (mu)  Mainly analgesic effects  Respiratory depression  Nausea / vomiting  Constipation  Cough reflex  Euphoria  Addiction  Sedation  Most analgesic opioids are µ-agonists www.indiandentalacademy.com
  17. 17. The opioid receptor δ (delta)  Probably  Some effects outside the CNS analgetic effekts  Seizures?  Least knowledge www.indiandentalacademy.com
  18. 18. The opioid receptor κ (kappa)  Analgesia  Nausea on mainly spinal cord level and dysphoria  Psychotomimetic effects – limits abuse potential www.indiandentalacademy.com
  19. 19. Side effects - mechanisms  Respiratory depression Respiratory centre (medulla oblongata) Less CO2 stimulation Decreased respiratory rate  Nausea / vomiting Area postrema (medulla oblongata) (triggerzone vomiting reflex) Stimulation of DA-receptors Stimulation mechano/chemoreceptors GI tract www.indiandentalacademy.com
  20. 20. Side effects - mechanisms  Constipation peripheral and central affection less GI movement and increased tonus No tolerans Laxatives necessary Peroral naloxone possible  Itching Histamine release or centrally mediated www.indiandentalacademy.com
  21. 21. Side effects - Mechanisms  Sedation Overdose Wrong strategy Sleep dept www.indiandentalacademy.com
  22. 22. Drugs (µ-receptors) morphine, metadon, fentanyl, heroin  Agonists  Partial agonists buprenorfin, kodein, tramadol  Antagonist naloxone www.indiandentalacademy.com
  23. 23. What is an opioid?  Alkaloid (plant) or synthetic  Morphine like effekts, inhibited by naloxon www.indiandentalacademy.com
  24. 24. Opium  Narcotic resin from opium poppies: morphine 10%, noskapin 6%, papaverin 1%, kodein 0,5% www.indiandentalacademy.com
  25. 25. History  3400 BC Opium puppies grown in Mesopotamia  460 BC Hippocrates medicine (psychiatric disease and epidemies) www.indiandentalacademy.com
  26. 26. History  330 BC Alexander the Great introduces opium to Persia and India  400 AD Opium with traders to China  Parcelsus (1490-1541) opium as medicine  Laudanum (opium, sherry, cinnamon, clove bud oil, saffron) 17th century www.indiandentalacademy.com
  27. 27. History  Morphin 1806  Kodein 1832  Heroin 1832 www.indiandentalacademy.com
  28. 28. Morphin  C17H19NO3  Greek. Morpheus (God of dreams)  1806 from opium  1956 chemical structure www.indiandentalacademy.com
  29. 29. Morphine  Half life 2-4 hours  Bioavailability 10-50% (30%)  Distribution volume 3L/kg  Bioaactive morphine-6-glucuronid (kidneys)  M6G half life 4-15 hours www.indiandentalacademy.com
  30. 30. Heroin  C21H23NO5 (morphin C17H19NO3)  Higher fat solubility  Produced 1874  Bayer 1899  Drug Sweden until 1964  Half life 30 minutes  Morphine www.indiandentalacademy.com
  31. 31. Kodein  C18H21NO3 (morfin C17H19NO3)  Produced 1832  Low receptor affinity  10% into morphine  M6G  7-10% non-responders  Half life 2-4 hours.  10 mg morfin  Kodein 60mg www.indiandentalacademy.com
  32. 32. Dextropropoxifen  Half time 8-18 (90) hours  Active metabolite norpropoxyfen  Metabolite half life 30-45 (100) hours  Alcohol enhances respiratory inhibition  10mg morfin  100mg Dextropropoxifen www.indiandentalacademy.com
  33. 33. Tramadol  Halflife 4-6 hours  Active metabolite D-desmetyltramadol  Halflife metabolite 9-12 hours  5-10% non-responders  Inhibits reuptake NA / 5-HT www.indiandentalacademy.com
  34. 34. Fentanyl  ”Complicated kinetics”  Halflife 1 min, 8 min, 8 tim  Active metabolites unknown  10mg morfin  0,05 mg fentanyl (iv) www.indiandentalacademy.com
  35. 35. Pethidine  synthetic  Most opioid histamine release. Seizures.  100mg  10mg morphine  Shivering www.indiandentalacademy.com
  36. 36. Ketogan  Ketobemidon(hydroklorid)  NMDA – receptor antagonist?  Halflife 2-4 hours  Unknown metabolite activity  Abuse risk  ”Less documented morphine alternative”  ”only” indication  renal failure (+NMDA?)  10mg morphine  10mg ketobemidon www.indiandentalacademy.com
  37. 37. Oxicodon  Halflife 2-4 timmar  Probably inaktiva metaboliter  10mg morfin  5mg oxikodon www.indiandentalacademy.com
  38. 38. Metadon  NMDA-receptor antagonist ?  Halflife 15-40 hours  ”Bad reputation”  Advanced pain treatment www.indiandentalacademy.com
  39. 39. Clinical use  Cancer pain  Postoperative pain  Long-term pain ?  Neurogenic pain?  ”Always” in combination with paracetamol and NSAID  Elderly ?  Try not to mix different opioids www.indiandentalacademy.com
  40. 40. Intoxication  Mios (small pupils)  Lower conscience  Breathing www.indiandentalacademy.com
  41. 41. Antidote – Naloxone (Narcanti)  opioid antagonist  reverses endogenous and exogenous substanses and acupuncture  effect within 2 minutes  Iterated  iv + im when abuse overdose www.indiandentalacademy.com
  42. 42. Abstinence  sweating, fever (”cold turkey”), shakings, muscular cramps, itching, diarrhea, nausea, vomiting (the flu)  At pain treatment because of to quick withdrawal  re-medicate! www.indiandentalacademy.com
  43. 43. Cold Case  Cancer  Current medication: Tb. Dolcontin (longacting morphine) 60mgx2 Tb. Morphine (shortacting) 20mg as req. inj. Ketogan 5mgvb Tb. Tramadol 100mgx2  Pain. What to do? www.indiandentalacademy.com
  44. 44. Patientfall  Patient insatt på Ketogan tablett 5mgx6 med god effekt. Översatt till Dolcontin 20mgx2. Inkommer efter 1 vecka till akuten: illamående, kräkning  Diffdiagnos (opioidrelaterat) ?  Ytterligare status etc?  Vad göra? www.indiandentalacademy.com
  45. 45. Afterlife …..  Morphina  Renal  Treat is currently Golden Standard failure pain! www.indiandentalacademy.com
  46. 46. www.indiandentalacademy.com Leader in continuing dental education www.indiandentalacademy.com

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