CNS Pharmacology-
Introduction to Drugs of Abuse II/Opoids
Prepared and Presented by:
Marc Imhotep Cray, M.D.
Professor Ba...
2
3
OPIOIDS or NARCOTICS
I. Morphine
II. Codeine
III. Meperidine
IV. Methadone
V. Designer Opioids
4
I.
Morphine, Heroin, Hydromorphone,Oxymorp
hone
A. Pharmacology
- Heroin is very lipid soluble
- Short half-life (t½ = 3...
5
Desirable Effects:
 Euphoria
 Sedation
 Relief of anxiety and
various other forms of
distress
 Analgesia
 Depressio...
6
Undesirable Effects:
Dysphoria Dizziness Nausea
Vomiting Constipation* Biliary tract spasm
Urinary retention
OPIOIDS or ...
7
OPIOIDS
1).Psychological
dependence
 I.V. use preferred by most
users => “rush” or “high”
 Oral abuse => meperidine
 ...
8
 Withdrawal, onset related to time-effect
curve and t½ of narcotic
 6-8hr =>drug seeking behavior, restless, anxious
...
9
 Withdrawal, onset related to time-effect
curve and t½ of narcotic
Not life threatening, no convulsions, no
delirium, n...
10
B. Concurrent or Substitute use:
 Alcohol, sedatives or
cocaine/amphetamines
C. Tolerance
 Yes, develops to all effec...
11
D. Toxicology
1.Tissue and organ toxicity
- “Heroin lung” with acute overdose
- No apparent tissue damage
2. Psychic to...
12
E. Acute Intoxication/Overdose
1. Disruption of central control of
peripheral sympathetic activity
- Respiratory depres...
13
E. Acute Intoxication/Overdose
(con’t)
2. CNS depression
- Euphoria/dysphoria =>drowsiness
=>sedation => coma
Treatment...
14
F. Treatment of
Depenndence
 Narcotic dependence is
one of very few cases
where there are
partially effective
pharmaco...
15
b. LAAM (L-a-acetyl methadol, methadyl
acetate)
 Structurally similar to methadone.
 Longer-acting opiate
 Taken ora...
16
OPIOIDS
c. Buprenorphine
 Partial agonists which substitutes for low
doses of opioids but antagonizes high
doses
 Can...
17
F. Treatment of Dependence
 Major problem in detoxification and
maintenance of abstinence is the
motivational componen...
18
Opiate Antagonists
cause precipitated
abstinence
Naltrexone:
 Used for the long
term maintenance
of abstinence
 Long ...
19
II.Codeine (Methylmorphine); Dihydrocodeine; Hydrocodone
(Dicodid®, Hycodan®); Oxycodone (Percodan®).
A. Pharmacology
...
20
III. Meperidine (Demorol®); Alphaprodine,
(Nisentil®)
A. Pharmacology
- Less potent than morphine
- IM More rapid onset...
21
IV. Methadone
A. Pharmacology
 Pharmacodynamic profile very similar to morphine
 Longer acting (10 hrs) vs Morphine (...
22
IV. Methadone
B. Concurrent or substitute use - Yes Other
narcotics
C. Tolerance: Same as Morphine, Cross-
tolerance wi...
23
V. Designer Opioids
a. MPTP
(1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine).
A meperidine/heroin-like drug, MPTP was syn...
24
G. Mechanism of action
1. Anatomy of m opioid receptors: nucleus
accumbens (N. Acc.), ventral tegmental area
(VTA), cau...
25
Mechanism of action
Opioids act at the Mesolimbic Dopaminergic
System
=> Reward Center of the Brain.
Inhibit the releas...
26
27
Drugs and Neurotransmitters & Mental
Disorders Interactive Tutorials and
Animation Learning Tools
 Psychotropic Medica...
28
Drugs and Neurotransmitters & Mental
Disorders Interactive Tutorials and
Animation Learning Tools
 Schizophrehia UNIVE...
29
eMedicine Articles on Addiction
 Alcohol-Related Psychosis
 Alcoholism
 Amphetamine-Related
Psychiatric Disorders
 ...
Upcoming SlideShare
Loading in …5
×

IVMS-CNS Pharmacology- Intro to Drugs of Abuse II-Opioids

944 views

Published on

Purchase here
http://www.scribd.com/doc/165721160/IVMS-CNS-Pharmacology-Intro-to-Drugs-of-Abuse-II-Opioids

Published in: Education, Health & Medicine

IVMS-CNS Pharmacology- Intro to Drugs of Abuse II-Opioids

  1. 1. CNS Pharmacology- Introduction to Drugs of Abuse II/Opoids Prepared and Presented by: Marc Imhotep Cray, M.D. Professor Basic Medical Sciences Clinical: E-Medicine Articles Opioid Abuse
  2. 2. 2
  3. 3. 3 OPIOIDS or NARCOTICS I. Morphine II. Codeine III. Meperidine IV. Methadone V. Designer Opioids
  4. 4. 4 I. Morphine, Heroin, Hydromorphone,Oxymorp hone A. Pharmacology - Heroin is very lipid soluble - Short half-life (t½ = 3 min) - Heroin  6-mono-acetyl morphine  morphine OPIOIDS or NARCOTICS
  5. 5. 5 Desirable Effects:  Euphoria  Sedation  Relief of anxiety and various other forms of distress  Analgesia  Depression of cough reflex* Subjective CNS effects:  Drowsiness  Difficulty concentrating  Apathy  Decreased physical activity  Lethargy  Extremities feel heavy and the body feels warm OPIOIDS or NARCOTICS
  6. 6. 6 Undesirable Effects: Dysphoria Dizziness Nausea Vomiting Constipation* Biliary tract spasm Urinary retention OPIOIDS or NARCOTICS
  7. 7. 7 OPIOIDS 1).Psychological dependence  I.V. use preferred by most users => “rush” or “high”  Oral abuse => meperidine  Emotional or motivational symptoms, “craving”.  Iatrogenic addiction 2).Physical dependence  May develop on repeated use of therapeutic doses  Narcotic Abstinence Syndrome (Withdrawal)
  8. 8. 8  Withdrawal, onset related to time-effect curve and t½ of narcotic  6-8hr =>drug seeking behavior, restless, anxious  8-12hr => Pupils dilated, reactive to light; increased pulse rate, blood pressure, yawning; chills; rhinorrhea; lacrimation; gooseflesh; sweating; restless sleep.  48-72 hrs (peak) => All of the above plus muscular weakness, aches (cramps) and twitches; nausea, vomiting and diarrhea;  temperature and respiration rate elevated; heart rate and blood pressure elevated; dehydration OPIOIDS
  9. 9. 9  Withdrawal, onset related to time-effect curve and t½ of narcotic Not life threatening, no convulsions, no delirium, no disorientation Treatment of withdrawal: symptoms => clonidine OPIOIDS
  10. 10. 10 B. Concurrent or Substitute use:  Alcohol, sedatives or cocaine/amphetamines C. Tolerance  Yes, develops to all effects except constipation and pupillary effects  Cross-tolerance and cross- dependence with other narcotics (Implication in narcotic addict => need to increase dose to experience euphoria)  High level of tolerance is possible; huge amounts of drug can be tolerated after chronic use; potential for overdose if relapse occurs and addict resumes with same high level of drug  Implications for chronic administration for pain OPIOIDS
  11. 11. 11 D. Toxicology 1.Tissue and organ toxicity - “Heroin lung” with acute overdose - No apparent tissue damage 2. Psychic toxicity - Acute and chronic drive reduction 3. Behavioral toxicity - Criminal behavior to obtain drugs 4. Associated diseases/Death - Unsterile syringes: AIDS, hepatitis, SBE, malaria, tetanus, localized infections, pulmonary infiltration of contaminants Neuropathies, Violent deaths OPIOIDS
  12. 12. 12 E. Acute Intoxication/Overdose 1. Disruption of central control of peripheral sympathetic activity - Respiratory depression => apnea=> DEATH - Circulatory depression => BP - Pupils constricted (may be dilated with meperidine) - Convulsions with propoxyphene and meperidine - - Arrhythmias w propoxyphene - Pulmonary edema -  Reflexes OPIOIDS
  13. 13. 13 E. Acute Intoxication/Overdose (con’t) 2. CNS depression - Euphoria/dysphoria =>drowsiness =>sedation => coma Treatment of overdose => Naloxone (Narcan ®) I.V. (0.1-0.4 mg) repeated as necessary Short acting opioid antagonist (1-2 hrs). Give every 30 minutes until patient is controlled Follow by methadone Nalmefene could also be used, has longer half-life Also used to control and reverse effects of therapeutically administered narcotics (anesthesia and labor) OPIOIDS
  14. 14. 14 F. Treatment of Depenndence  Narcotic dependence is one of very few cases where there are partially effective pharmacological therapies 1. Opioid replacement a. Methadone, Dolophin®  Long half-life produces a longer but less stressful withdrawal (although more prolonged).  Onset =>24hrs, peak =>5-7 days  Lessens the “highs” and “lows” of withdrawal  Oral administration OPIOIDS
  15. 15. 15 b. LAAM (L-a-acetyl methadol, methadyl acetate)  Structurally similar to methadone.  Longer-acting opiate  Taken orally in liquid form, lasts 72hrs (visits 3 X a week)  “Take home" medication OPIOIDS
  16. 16. 16 OPIOIDS c. Buprenorphine  Partial agonists which substitutes for low doses of opioids but antagonizes high doses  Can be administered sublingually every 24-48 hours as an alternative to methadone
  17. 17. 17 F. Treatment of Dependence  Major problem in detoxification and maintenance of abstinence is the motivational component of the CNS effect, which is responsible for the “drug craving” sensations,  Also conditional dependence and social factors play an important role. OPIOIDS
  18. 18. 18 Opiate Antagonists cause precipitated abstinence Naltrexone:  Used for the long term maintenance of abstinence  Long half-life, oral, 3 times a week Naloxone:  Use in life- threatening situations for overdose  Short half life (1-2-hrs) control and reverse effects of therapeutically administered narcotics (anesthesia and labor). OPIOIDS
  19. 19. 19 II.Codeine (Methylmorphine); Dihydrocodeine; Hydrocodone (Dicodid®, Hycodan®); Oxycodone (Percodan®). A. Pharmacology  << Potent than morphine IM, but almost never administered parentally  "Weak" opioids.  Used as a cough suppressants (antitussive) and combined with aspirin and acetaminophen as painkillers.  Dependence liability < < than morphine OPIOIDS
  20. 20. 20 III. Meperidine (Demorol®); Alphaprodine, (Nisentil®) A. Pharmacology - Less potent than morphine - IM More rapid onset, shorter duration Similar to heroin - Used in anesthesiology - Dependence liability - Same as Morphine OPIOIDS
  21. 21. 21 IV. Methadone A. Pharmacology  Pharmacodynamic profile very similar to morphine  Longer acting (10 hrs) vs Morphine (4-5 hrs)  Equipotent and equieffective to morphine  Tolerance and dependence develop more slowly than with morphine  Withdrawal signs and symptoms are milder but more prolonged  Use for detoxification or maintenance of a heroin addict OPIOIDS
  22. 22. 22 IV. Methadone B. Concurrent or substitute use - Yes Other narcotics C. Tolerance: Same as Morphine, Cross- tolerance with other narcotics D. Acute intoxication/Overdose: Similar to other narcotics E. Withdrawal: Same as Morphine F. Treatment: None G. Mechanism of action: m opioid receptors OPIOIDS
  23. 23. 23 V. Designer Opioids a. MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine). A meperidine/heroin-like drug, MPTP was synthesized in the 1980’s. It contained MPP+ impurities that cause Parkinson's like-symptoms in the young adults who used it by destroying DA neurons. b. Fentanyl (Sublimaze) China White: alpha-methyl fentanyl => deaths by overdose 6000 times more potent than morphine OPIOIDS
  24. 24. 24 G. Mechanism of action 1. Anatomy of m opioid receptors: nucleus accumbens (N. Acc.), ventral tegmental area (VTA), caudate, thalamus, cortex, spinal cord2. Actions in thalamus => Sensory modalities. 3. Actions in spinal cord => Analgesia 4. Actions at Mesolimbic dopaminergic system => Reward. Inhibit the release of GABA at the VTA Desinhibition of DA =>DA activity OPIOIDS
  25. 25. 25 Mechanism of action Opioids act at the Mesolimbic Dopaminergic System => Reward Center of the Brain. Inhibit the release of GABA at the VTA  Desinhibition of Dopamine neurons  DA activity OPIOIDS
  26. 26. 26
  27. 27. 27 Drugs and Neurotransmitters & Mental Disorders Interactive Tutorials and Animation Learning Tools  Psychotropic Medications and Neurotransmitters Wisconsin Online  Alcohol and the brain from PBS  The Effect of Drugs and Disease on Snaptic Transmission Harvard Education  Nicotine Patch by Nucleus Communications  GABA Inhibition of Glutamate Bay Area Pain Medical Associates  Acute Pain Bay Area Pain Medical Associates  How Drugs Affect Neurotransmitters INMHA
  28. 28. 28 Drugs and Neurotransmitters & Mental Disorders Interactive Tutorials and Animation Learning Tools  Schizophrehia UNIVERSITY OF CENTRAL LANCASHIRE  Epilepsy UNIVERSITY OF CENTRAL LANCASHIRE  Pharmacologic Action of Meth RnCeus.com  How is Pain Produced University of Edinburgh  How Much Alcohol can YOU TAke BBC  The Brain: Understanding Neurobiology Through the Study of Addiction National Institutes of Health  The Science of Addiction University of Utah, Genetic Science Learning Center  Stimulants and Antidepressants Dr. Ian Winship of the University of Alberta  Tranquilizers and CNS Depressants Dr.Ian Winship of the University of Alberta  Genetics of Addiction Genetics Science Learning Center
  29. 29. 29 eMedicine Articles on Addiction  Alcohol-Related Psychosis  Alcoholism  Amphetamine-Related Psychiatric Disorders  Caffeine-Related Psychiatric Disorders  Cannabis Compound Abuse  Cocaine-Related Psychiatric Disorders  Hallucinogens  Inhalant-Related Psychiatric Disorders  Injecting Drug Use  Nicotine Addiction  Opioid Abuse  Phencyclidine (PCP)-Related Psychiatric Disorders  Sedative, Hypnotic, Anxiolytic Use Disorders  Stimulants  Substance-Induced Mood Disorders: Depression and Mania

×