Opioid FAQs

Frequently Asked Questions about Opioids (Opioid FAQs)

As we promote more awareness of our proposed Med Wreck solution, we hope that more Americans educate themselves on the topic of Opioids.  American’s most frequently asked questions (Opioid FAQs) are below. Please email us any other questions so we can continue to expand our list of Opioid FAQs.

 

What are opioids? – Opioids are a group of substances that act on pain receptors in the brain and spinal cord.  These receptors are known as endorphin receptors. There are multiple classes and subclasses of endorphin receptors.

The first such drug in this class was derived from the opium poppy and known as opium.  In the 19th century, morphine was refined from the opium poppy as a pain medication that one could administer using a hypodermic needle and syringe. Since then, researchers have developed many substances that bind to the opioid receptor to either activate (provide pain relief) them or to block them from action.  The former are known as opioid agonists, and the latter, as opioid antagonists.  Some agents actually serve as both agonist and antagonists.

What are opiates? – An opiate refers to any drug derived from the opium poppy, regardless of its ability to relieve pain in humans.  The poppy produces over 50 alkaloid compounds – 25 of these provide pain relief.  An opiate may be obtained directly from poppies or synthetized in the laboratory.  Most opiates produce both tolerance (a need for higher and higher dosage) and dependence (physical and/or psychological inability to stop the medication)j making them likely to create addiction with prolonged use. The three most active drugs from the poppy are morphine, codeine and thebaine.

What are examples of opioids? – The common opioids and opiates are shown in the table below:

Substance Known as… Derived from… Administration Routes
Morphine MS, Morphine Sulfate

MS-Contin®

Opium Poppy Injection, long acting oral medication. Patch.
Codeine Commonly combined with acetaminophen as Tylenol #3®. Opium Poppy Oral (Better absorbed than morphine)
Opium Opium Opium Poppy Smoked, injected, oral
Heroin “Smack”, “horse”, “brown sugar”, “H”, “junk”, “China white” and others… Opium Poppy or synthesized from Morphine Injection.  This is not approved for any medical use.
Thebaine Not available as a drug Is used as base for several semi-synthetic agents below.
Oripavine Not available as a drug Is a metabolite of Thebaine and only used as base for several semi-synthetic agents below.
Semi-synthetic opiates Typically combined with acetaminophen to potentiate their effects. Synthesized  
Oxymorphone Numorphan®, Opana® From Thebaine Oral (by mouth)
Hydromorphone Dilaudid® From Morphine Injection or Oral (by mouth)
Oxycodone Percocet® From Thebaine Oral (by mouth)
Hydrocodone Vicodin®, Norco®, Lortab® From Codeine Oral (by mouth)
Synthetic opioids   Characteristics  
Buprenorphine Subozone® Used for addiction Agonist – antagonist
Fentanyl Duragesic®, sublimaze® Can be natural or synthesized.  Most potent opioid. Agonist.  Injection or patch.
Meperidine Demerol® Injection, oral
Methadone Very long acting, so used for heroin withdrawal. Oral
Tramadol Ultram® Opioid Agonist.  Addictive with long-term use. Oral
Naloxone Narcan® Short-acting antagonist used for overdose. Not a controlled-substance. Injection

 

Naltrexone Vivitral® Agonist-Antagonist used for opioid addiction.  Not a controlled-substance. Oral

What is the difference between opiates and opioids? -  Opiates refer to any of the 50 alkylated compounds found in the opium poppy.  Opioids refer to compounds that interact with the receptors in our central nervous system, whether they are agonists or antagonists.  Agonists activate the receptor to produce pain relief.  Antagonists block those same receptors so that other opioids cannot bind to the receptor.  Some agents, called agonist-antagonists do both.  They provide some mild pain relief while blocking the effect of the stronger agonists, like morphine and heroin.

What are some of the most common opioids? - See the Table above.

 How do opioids work? - Opioids work by binding with specific receptors in our central nervous system (brain and spinal cord).  These receptors are also known as endorphin receptors (endorphins are substances produces by our bodies as a natural pain killer that is released during moments of extreme stress, such as trauma and intense exercise.).  Activation of these receptors provide us with pain relief and euphoria ("natural high").

What are common side effects of opioids? -  There are multiple side effects of opioids.  We will summarize in simple terms:

  • Addiction - Addiction relates to several factors that perpetuate use of the substance:
    • Tolerance - With repeated exposure to an agent such as an opioid, the body adjusts through a complex process and becomes less sensitive to that substance.  Thereby, the person must experience increasing doses of the agent to get the same effect.
    • Physical (and psychological) dependence - With repeated exposure, the body gets so use to its presence that the person experiences "withdrawal symptoms" as he or she discontinues the agent.  Physical dependence is normal with many medications and in itself does not indicate addiction.  However, it perpetuates the addiction when it occurs.  Examples of withdrawal symptoms include headache, nausea, itching, irritability, sweating, nausea and craving of the agent.
    • Psychological dependence - Irritability, craving and depression are often stated as psychological dependence symptoms, though many include these in the physical dependence category.
  • Constipation - Opioids slow both gastric and intestinal motility. The former may lead to nausea and vomiting while both may lead to constipation, or inability to move one's bowels.  Constipation is a side effect to which tolerance does not occur. Constipation occurs in almost 95% of individuals during chronic use.
  • Nausea & vomiting - This is a common side effect during short term use of opioids. In clinical practice, physicians often combine anti-nausea (known as anti-emetic) medications with opioids to prevent the nausea and vomiting.  Individuals typically become tolerant to this side effect after a week or two of use.
  • Itching - It a rarer side effect from opioids, and more often seen as a withdrawal symptom.
  • Drowsiness - Individuals respond differently and may develop tolerance to sedation.  However, slower reaction times create a public health issue as opioid use may lead to traffic, home or workplace accidents. Thus some sources add disruption of work and increased accident-proneness as additional side effects.
  • Respiratory depression - Respiratory depression occurs when a medication affects the central nervous center function that keeps us breathing, even when we are asleep or unconscious. This is the most serious side effect, more likely to occur with a single dose of opioid rather than with chronic use.
  • Opioid-induced hyperalgesia - This is a rare side effect in which an individual's pain is increased rather than decreased with administration of an opioid.
  • Other rare side effects are numerous and seen with both use and withdrawal.

There are some therapeutic uses of opioids beyond pain relief.  Single doses (e.g. meperidine) may help post-anesthesia rigors (shakes) and intractable hiccups.  Morphine is used acutely to cause vasodilation to assist the treatment of acute pulmonary edema. However, vasodilation causes side effects such as low blood pressure (hypotension and orthostatic [i.e. positional] hypotension), fainting, dizziness, and light-headedness.

Why do they distinguish prescription opioids from synthetic opioids? - In our response to the opioid "crisis", many now draw attention to abuse, overdose and death from prescription vs. synthetic opioids.  Prescription opioids include those taken directly through a physician prescription to that individual and those "diverted" to others.  Diversion occurs through theft of opioids as health care workers (doctors, nurses, or pharmacist) divert medication from actual patients for whom they were intended.  This may be done for personal misuse or for trafficking (selling).

Injectable opioids such as morphine, hydromorphone (Dilaudid®), meperidine (Demoral®) and fentanyl are typical diversion drugs.  However, synthetic fentanyl, is now a growing concern due to its high potency, especially when used to "lace" (i.e. added into) heroin.  Heroin is not available for prescribing in the United States, and is neither synthetic or prescription in nature.  Several oral (taken by mouth) prescription opioids of abuse include hydrocodone, oxycodone and codeine.  These latter drugs are typically prescribed for acute (short-term) pain relief, but can lead to addiction and abuse in longer term use.  Physicians are now encouraged not to prescribe these medications chronically, except for palliative (e.g. Hospice) care.

What are natural (or endogenous) opioids? - Our bodies have a group of naturally occurring substances known as endorphins.  Endorphins activate the same receptors as morphine and other opioids.  Our bodies release endorphins during times of stress, such as trauma injuries and intense exercise.  Activation of these receptors create pain relief and euphoria (a sense of well-being). Therefore what we call the "morphine receptors" or "opioid receptors" are actually our "endorphin receptors."

How long do opioids stay in your system? - Most opioids are fairly short acting, effective for only a few hours.  However, manufacturers have created prescription preparations that create several long-acting opioids. The longest-duration opioids are delivered through patches that deliver the medication through the skin (transdermally) for several days. Long-acting opioids deliver a more consistent dose of opioids to the patient, lessening the effect of "wearing off" of the pain relief between doses.

What are long-acting opioids? - Naturally-occurring opioids are relatively short acting.  This requires the user to take multiple doses a day. It also may mean the patient alternates between periods of good and inadequate pain control while on the short-acting agents. Pharmaceutical manufacturers  have created several forms of opioids to create a more steady release of these agents.  These include "extended-release" oral forms and agents delivered through the skin (transdermally) through patches lasting several days.  These agents are most appropriate for palliative care patients, such as those in the final months of terminal cancer care.

Be sure to search our website for past and ongoing updates on "Med Wreck" and the opioid crisis. Email us any contributions to our Opioid FAQs at MedWreckFreedom@healthITaccelerator.com.

 

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