Opioids are a set of substances derived from opium.

These substances are then artificially made and are used in a medical context as medications.

Opioid medications act on the Nervous System to help with pain relief.

A prescription is required in all cases of opioid medication use.

Common examples include:

  • Morphine
  • Oxycodone (Oxycontin, Roxycodone, Percocoet, Roxicet)
  • Hydrocodone  (Lortab, Norco, Vicodin)
  • Hydromorphone  (Dilaudid
  • Codeine
  • Meperidine (Demerol)
  • Methadone

Despite pain treatment, a large concern with opioid medications is that they can lead to opioid dependence.

Withdrawal syndrome can be seen with abrupt discontinuation.

Opioids can be used recreationally – which means above the prescription written by a provider and even without a prescription.

It is believed some 30+ million people, between the ages of 15 and 65, used opiods recreationally in 2013.

 

Types

Fentayl – Fentanyl Extended Released Transdermal System

Methadone – Methadone hydrochloride tablets or oral solution

Morphine Sulfate – Morphine Sulfate Extended Release Capsules or Tablets

Butrans – Buprenorphine Transdermal system

Dolophine – Methadone Hydrochloride Tablets

Duragesic – Fentanyl Transdermal System

Exalgo – Hydromorphone Hydrochloride Extended Release Tablets

Avinza – Morphine Sulfate Extended Release Capsules

Kadian – Morphine Sulfate Extended Release Tablets

MS Contin –  Morphine Sulfate Controlled Release Tablets

Nucynta ER – Tapentadol Extended Release Oral Tablets

Opana ER – Oxymorphone Hydrochloride Extended Released Tablets

OxyContin – Oxymorphone Hydrochloride Controlled Release Tablets

Embeda – Morphine Sulfate and Naltrexone Extended Release Capsules – (No longer being marketed – but still approved)

Palladone – Hydromorphone Hydrochloride Extended Released Tablets – (Voluntary recall – not available or marketed – but still approved)

 

 

Method of Action

  • Opioids work by binding to opioid receptors found primarily in the central and peripheral nervous system.
  • They come from the opium poppy.
  • Some are created synthetically – these result in an opium like effect.
  • Therefore – all opiates are opioids but not opioids are opiates.

 

Medical Uses

1.) Acute Pain

  • Effective for pain following surgery
  • Important in Pallative Care (Complicated medical approach to serious medical issues)
  • Chronic Cancer Pain
  • Degenerative Conditions
  • Rheumatoid Arthritis

2.) Chronic Non-Cancer Pain

  • This is high risk category – risks often greater than benefits in the category.
  • Typically other medications – Tylenol, NSAIDs, and other options prior to opioid categories.
  • The effectiveness of opioids in less complicated neuropathic pains is unclear.
  • Not first line treatment in Headaches
  • Used occasionally in Back Pain
  • Used rarely in Fibromyalgia
  • Non-malignant chronic pain

3.) Shortness of Breath

4.) Diarrhea

  • Used in some cases of diarrhea-predominate Irritable Bowel Syndrome.

Side Effects

  • Drowsiness
  • Euphoria
  • Increased Sleep
  • Mental Confusion
  • Respiration Problems
  • Nausea
  • Vomiting
  • Constipation
  • Dry Mouth
  • Itching
  • Decreased/Impaired Sex Drive/Function
  • Depression
  • Changes in Menstrual Period
  • Increased Risk for Falls

 

Tolerance

  • This is a process of Adaptation that results in reduced effectiveness of a drug.
  • Receptor downregulation can occur.
  • Tolerance is not seen in everyone and can vary in severity.
  • Can require a higher dosing to achieve the same benefit.
  • Often seen when use of opioids continues for extended periods.
  • Does not predict future risk for misuse or addiction.

 

Physical Dependence

  • The Physiological Adaptation to the presence of opioid medication in the system.
  • Can occur with Medications other than Opioids.
  • Withdrawal symptoms occur when substance is discontinued.
  • Can also be seen when the dose is reduced.
  • This is a normal occurrence and doesn’t necessarily mean that addiction is present, but is seen in patients that are addicted.
  • Less likely to have symptoms occur if you slowly reduce opioids over days and weeks if applicable.
  • Treatment of withdrawal can be done with Clonidine

Withdrawal Symptoms

  • Sweating
  • Irritability
  • Nausea
  • Tremor
  • Rhinorrea
  • Myalgia
  • Vomiting

 

 

Addiction

  • This is a complex area that includes manipulative actions or words that are associated with the misuse of certain drugs.
  • This is a psychological compulsion that causes the individual to continue actions that can lead to dangerous and unhealthy outcomes.

Misuse of a medication may include but are not limited to the following:

  • Amount of medications used
  • Obtaining a prescription falsely
  • Purchasing pills on the streets
  • Stealing prescription medications
  • Injecting medications (unless medically advised)
  • Crushing medications (unless medically advised)
  • Using opioids for purposes other than pain
  • Self Harm in order to get medications
  • Many more.

 

Interactions

  • Adding Opioids to other medications can come at a risk.
  • Adjustments of medications may be required in some cases.
  • Use of Opioids and Benzodiazepines and/or Alcohol greatly increases the risk and rates of adverse effects, overdoses, and deaths.
  • Use if Sedatives greatly increases risks for breathing problems

 

Opioid Antagonist

  • These are medications that can reverse side effects or overdose of opiods

Naloxone or Naltrexone

  • Can competitively bind to opioid receptors with a higher affinity but they don’t activate them.
  • It can also displace the Opioid from the receptor.
  • The Half life is shorter so repeat dosing or prolonged infusion may be required

Nalmefene

  • A longer Acting Antagoinist that acts similarly.
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