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Pharmacology of  Opiates
Dr. Dawn-Elise Snipes PhD, LPC-MHSP, LMHC
Executive Director: AllCEUs.com Counseling Continuing Education
Podcast Host: Counselor Toolbox, Happiness Isn’t Brain Surgery

Counseling and social work CEUs are available on Demand for this podcast at https://allceus.com/member/cart/index/search?q=opiates

Objectives
~    Examine the following for opiates
~    Types of drugs
~    The short and long term effect on the person
~    Symptoms of intoxication and withdrawal
~    Detoxification issues
~    Current state of abuse
~    Recommended treatments

Side Note
~    Method of administration greatly effects the intensity and duration of onset for various drugs
~    Oral (slowest)
~    Inhalation/Snorting
~    Inhalation/Smoking
~    Injection
~    Rectal suppository
~    Skin patches
Opiates
~    Types of Drugs: Analgesic (pain killer); CNS Depressant

How they Work
~    Body naturally produces opiate-like substance Endogenous opioids
~    Regulate pain perception
~    Hunger
~    Mood
~    “Runners High”

How they Work
~    Opiates bind to the same receptors but are 50-1000 times stronger and…
~    Reduce GABA (which regulates dopamine and anxiety)  increase in Dopamine   pleasure and possible energy & focus (norepinephrine (increased arousal from decreased GABA))
~    Increase available serotonin levels (reduced anxiety/depression, improved pain tolerance)

Neurotransmitter Review
~    Dopamine
~    Pleasure
~    Energy, focus, motivation (norepinepherine)
~    Reduced GABA
~    Increased anxiety  HPA Axis activation  energy
~    Increased anxiety during detox (warming a cold bath)
Opiates
~    Tolerance starts to develop in 5-7 days
~    Tolerance reversal also  starts in only a few days
~    Short term impact (up to 5 hours)
~    Depends heavily on:
~    The dose
~    The route of administration
~    Previous exposure

Opiates
~    Short term impact (up to 5 hours)
~    Psychological: Euphoria, feeling of well-being, relaxation, drowsiness, sedation, disconnectedness, delirium.
~    Physiological: Analgesia, depressed heart rate and respiration depression, constipation, flushing of the skin, sweating, pupils fixed and constricted, diminished reflexes

Opiates
~    Complications and Side Effects
~    Medical complications among abusers arise primarily from adulterants and in non-sterile injecting practices
~    Include skin, lung and brain abscesses, collapsed veins, endocarditis, hepatitis, HIV/AIDS, death
Opiates
~    Complications and Side Effects
~    Alcohol or depressants such as benzodiazepines, hypnotics, and antihistamines increase the CNS effects of opiates
~    Sedation/drowsiness
~    Decreased motor skills.
~    Respiratory depression, hypotension
Opiates
~    Potentiation: Combining 2 drugs because one intensifies the other:  Antihistamine + narcotic intensifies its effect, there by cutting down on the amount of the narcotic needed.
~    Synergism: Two drugs taken together that are similar in action  effect out of proportion to that of each drug taken separately, 1+1= 5
Opiates
~    Long term impact
~    Vein collapse
~    Depression
~    Brain changes/damage
~    Reduction of the production of natural pain killers

Opiates
~    Symptoms of intoxication
~    Constricted pupils
~    Sleepiness or extreme relaxation
~    Agitation
~    Scratching and picking
~    20-25% of people get opiate itch. (remember that antihistamines potentiate opiates)

Opiates
~    Symptoms of withdrawal
~    Begin within 6-12 hours; last 5-10 days; peak between 48-72 hours
~    Yawning
~    Drug Craving
~    Irritability/dysphoria/depression
~    Flu like Symptoms: Runny nose, sweating. vomiting, chills, abdominal cramps, body aches, muscle and bone pain, muscle spasms, insomnia.
Opiates
~    Detoxification Issues
~    Tolerance decreases rapidly, so overdosing during relapse is easy
~    Biggest focus during opiate withdrawal is to provide palliative care
~    In general, opiate withdrawal is not life threatening, but opiate relapse is!

Opiates
~    Current state of Use/Abuse
~    Fentanyl is 30-50x stronger than heroin.  Overdose rates are extremely high.
~    Difficulty getting prescription opioids has led to increases in demand for heroin and fentanyl
~    Nearly 6% of 12th graders report using narcotics other than heroin for recreational purposes

Opiates
~    Recommended Treatment/Interventions
~    Methadone—long acting synthetic opiate agonist
~    Buprenorphine—Partial agonist/ceiling effect
~    Suboxone– Burprenorphine+Naloxone to prevent injection
~    Naloxone—Antagonist
~    Therapy

Summary
~    As we learn more about the different types of opiate receptors we are learning more about why some people are more at risk for development of addiction via self-medication.
References
~    http://thebrain.mcgill.ca/flash/i/i_03/i_03_m/i_03_m_par/i_03_m_par_heroine.html
~    Intravenous opioids stimulate norepinephrine and acetylcholine release  https://www.ncbi.nlm.nih.gov/pubmed/8572328
~    http://www.indiana.edu/~engs/rbook/drug.html
~    Case Scenario: Opioid Association with Serotonin Syndrome http://anesthesiology.pubs.asahq.org/article.aspx?articleid=1934431
~    Drug Interactions of Clinical Importance among the Opioids, Methadone and Buprenorphine, and other Frequently Prescribed Medications: A Review  https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3334287/#R71
~    Opioid Receptors: Distinct roles in mood disorders https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3594542/