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/