Opioids What They Do and How to Take Them

Opioids What They Do and How to Take Them
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Opioids What They Do and How to Take Them/Opioids have been regarded for millennia as among the most effective drugs for the treatment of pain. Their use in the management of acute severe pain and chronic pain related to advanced medical illness is considered the standard of care in most of the world. In contrast, the long-term administration of an opioid for the treatment of chronic non-cancer pain continues to be controversial.

Opioids are substances that act on opioid receptors to produce morphine-like effects.[rx] Medically they are primarily used for pain relief, including anesthesia.[rx] Other medical uses include suppression of diarrhea, replacement therapy for opioid use disorder, reversing opioid overdose, suppressing cough, suppressing opioid-induced constipation,[rx] as well as for executions in the United States. Extremely potent opioids such as carfentanil are only approved for veterinary use.[rx][rx][rx] Opioids are also frequently used non-medically for their euphoric effects or to prevent withdrawal.[rx]

Prescription opioids are powerful pain-reducing medications that include oxycodone, hydrocodone, and morphine, among others, and have both benefits as well as potentially serious risks. However, too many Americans have been impacted by the serious harms associated with these medications, and despite ongoing efforts, the scope of the opioid crisis continues to grow.[rx]

Types of Opioids

There are a number of broad classes of opioids

  • Natural opiates – alkaloids contained in the resin of the opium poppy, primarily morphine, codeine, and thebaine, but not papaverine and noscapine which have a different mechanism of action; The following could be considered natural opiates – The leaves from Mitragyna speciosa (also known as kratom) contain a few naturally-occurring opioids, active via Mu- and Delta receptors. Salvinorin A, found naturally in the Salvia divinorum plant, is a kappa-opioid receptor agonist.
  • Esters of morphine opiates – slightly chemically altered but more natural than the semi-synthetics, as most are morphine prodrugs, diacetylmorphine (morphine diacetate; heroin), nicomorphine (morphine nicotinate), dipropanoylmorphine (morphine dipropionate), desomorphine, acetyl propionyl morphine, dibenzoylmorphine, diacetyldihydromorphine;
  • Semi-synthetic opioids – created from either the natural opiates or morphine esters, such as hydromorphone, hydrocodone, oxycodone, oxymorphone, ethylmorphine, and buprenorphine;
  • Fully synthetic opioids – such as fentanyl, pethidine, levorphanol, methadone, tramadol, tapentadol, and dextropropoxyphene;
  • Endogenous opioid peptides – produced naturally in the body, such as endorphins, enkephalins, dynorphins, and endomorphins. Morphine, and some other opioids, which are produced in small amounts in the body, are included in this category.
  • Tapentadol – is likewise challenging to classify. It has a dual mechanism of action in a single molecule (unlike tramadol, which is a racemate) and with respect to analgesia, it has no active metabolites []. It has both an affinity for opioid receptors and contributes to noradrenergic activity in a synergistic way []. With its unique attributes, tapentadol has been classified as an entirely new class of analgesic, although it is often listed as an opioid [].
  • Cebranopadol – is a novel analgesic that acts as both an opioid agonist and also acts on nociception/orphanin FQ-peptide receptors []. This new agent may represent a new classification of the drug. Further study will determine how best to categorize it, but it has marked distinctions from the traditional opioids.
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Tramadol and tapentadol, which act as monoamine uptake inhibitors also act as mild and potent agonists (respectively) of the μ-opioid receptor. Both drugs produce analgesia even when naloxone, an opioid antagonist, is administered.[rx]

Opium alkaloids and derivatives

Opium alkaloids

Phenanthrenes naturally occurring in (opium):

  • Codeine
  • Morphine
  • Thebaine
  • Oripavine

Preparations of mixed opium alkaloids, including papaveretum, are still occasionally used.

Esters of morphine

  • Diacetylmorphine (morphine diacetate; heroin)
  • Nicomorphine (morphine dinicotinate)
  • Dipropanoylmorphine (morphine dipropionate)
  • Diacetyldihydromorphine
  • Acetylpropionylmorphine
  • Desomorphine
  • Methyldesorphine
  • Dibenzoylmorphine

Ethers of morphine

  • Dihydrocodeine
  • Ethylmorphine
  • Heterocodeine

Semi-synthetic alkaloid derivatives

  • Buprenorphine
  • Etorphine
  • Hydrocodone
  • Hydromorphone
  • Oxycodone
  • Oxymorphone

Synthetic opioids


  • Fentanyl
  • Alphamethylfentanyl
  • Alfentanil
  • Sufentanil
  • Remifentanil
  • Carfentanyl
  • Ohmefentanyl


  • Pethidine (meperidine)
  • Ketobemidone
  • MPPP
  • Allylprodine
  • Prodine
  • Promedol

Diphenylpropylamine derivatives

  • Propoxyphene
  • Dextropropoxyphene
  • Dextromoramide
  • Bezitramide
  • Piritramide
  • Methadone
  • Dipipanone
  • Levomethadyl Acetate (LAAM)
  • Difenoxin
  • Diphenoxylate
  • Loperamide (does cross the blood-brain barrier but is quickly pumped into the non-central nervous system by P-Glycoprotein. Mild opiate withdrawal in animal models exhibits this action after sustained and prolonged use including rhesus monkeys, mice, and rats.)

Benzomorphan derivatives

  • Dezocine—agonist/antagonist
  • Pentazocine—agonist/antagonist
  • Phenazocine

Oripavine derivatives

  • Buprenorphine—partial agonist
  • Dihydroetorphine
  • Etorphine

Morphinan derivatives

  • Butorphanol—agonist/antagonist
  • Nalbuphine—agonist/antagonist
  • Levorphanol
  • Levomethorphan
  • Racemethorphan


  • Lefetamine
  • Menthol (Kappa-Opioid agonist)
  • Meptazinol
  • Mitragynine
  • Tilidine
  • Tramadol
  • Tapentadol
  • Eluxadoline
  • AP-237
  • 7-Hydroxymitragynine

Allosteric modulators

Plain allosteric modulators do not belong to the opioids, instead, they are classified as opioidergic.

Opioid antagonists

  • Nalmefene
  • Naloxone
  • Naltrexone
  • Methylnaltrexone (Methylnaltrexone is only peripherally active as it does not cross the blood-brain barrier in sufficient quantities to be centrally active. As such, it can be considered the antithesis of loperamide.)
  • Naloxegol (Naloxegol is only peripherally active as it does not cross the blood-brain barrier in sufficient quantities to be centrally active. As such, it can be considered the antitheses of loperamide.)

Indications of Opioids

The indications listed below are based on the results of systematic reviews of randomized controlled trials.

Somatic pain

  • Opioids are useful for chronic musculoskeletal pain that has not responded adequately to acetaminophen or NSAIDs.

Neuropathic pain

  • Randomized trials have demonstrated that opioids are at least as effective as TCAs for neuropathic pain and have fewer side effects., Higher doses of opioids are often needed, however, for neuropathic pain than for somatic pain, and even at high doses, some patients do not respond. A combination of morphine and gabapentin reduces neuropathic pain more effectively and at lower doses than either drug alone does.


  • Two controlled trials using a weak opioid have demonstrated that opioids reduce the pain of fibromyalgia. Functional outcomes did not improve in these trials. A high proportion of fibromyalgia patients have concurrent mood and anxiety disorders,, and antidepressant therapy has had promising results for both mood and pain in fibromyalgia. An exercise program and low doses of amitriptyline are recommended first-line treatments.,
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Other Types of Pain

  • Opioids are sometimes used for recurrent, severe visceral pain, such as that associated with pancreatitis. They are not indicated for irritable bowel syndrome or for tension headaches. Opioids stronger than codeine should be reserved for patients with severe migraine headaches who do not respond to first-line treatments.


Side Effects of Opioids

  • Drowsiness and impaired judgment; do not drink alcohol, drive, or operate heavy machinery
  • Pruritis (itching)
  • Opioid-induced constipation
  • Nausea or vomiting
  • Withdrawal symptoms upon discontinuation; your doctor may suggest to slowly stop your narcotic to lessen withdrawal side effects
  • Tolerance to the pain relief effect can occur over time (meaning you may need a higher dose to get an equal amount of pain control)
  • Dizziness, confusion; may be worse in the elderly
  • Shallow breathing, or no breathing at all
  • Blue or grey lips or fingertips
  • Floppy arms or legs
  • Snoring or gurgling
  • Unresponsive, can’t be woken up

Treatments for Opioids Abuse and Addiction

Treatments for opioid abuse and addiction include

  • Medicines
  • Counseling and behavioral therapies
  • Medication-assisted therapy (MAT), which includes medicines, counseling, and behavioral therapies. This offers a “whole patient” approach to treatment, which can increase your chance of a successful recovery.
  • Residential and hospital-based treatment

Which medicines treat opioid abuse and addiction?

The medicines used to treat opioid abuse and addiction are methadone, buprenorphine, and naltrexone.

  • Methadone and buprenorphine can decrease withdrawal symptoms and cravings. They work by acting on the same targets in the brain as other opioids, but they do not make you feel high. Some people worry that if they take methadone or buprenorphine, it means that they are substituting one addiction for another. But it is not; these medicines are a treatment. They restore balance to the parts of the brain affected by addiction. This allows your brain to heal while you work toward recovery. There is also a combination drug that includes buprenorphine and naloxone. Naloxone is a drug to treat an opioid overdose. If you take it along with buprenorphine, you will be less likely to misuse the buprenorphine.

You may safely take these medicines for months, years, or even a lifetime. If you want to stop taking them, do not do it on your own. You should contact your health care provider first, and work out a plan for stopping.

  • Naltrexone works differently than methadone and buprenorphine. It does not help you with withdrawal symptoms or cravings. Instead, it takes away the high that you would normally get when you take opioids. Because of this, you would take naltrexone to prevent a relapse, not to try to get off opioids. You have to be off opioids for at least 7-10 days before you can take naltrexone. Otherwise, you could have bad withdrawal symptoms.
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How does counseling treat opioid abuse and addiction?

Counseling for opioid abuse and addiction can help you

  • Change your attitudes and behaviors related to drug use
  • Build healthy life skills
  • Stick with other forms of treatment, such as medicines

There are different types of counseling to treat opioid abuse and addiction, including

  • Individual counseling – which may include setting goals, talking about setbacks, and celebrating progress. You may also talk about legal concerns and family problems. Counseling often includes specific behavioral therapies, such as
  • Cognitive-behavioral therapy (CBT) – helps you recognize and stop negative patterns of thinking and behavior. It teaches you coping skills, including how to manage stress and change the thoughts that cause you to want to abuse opioids.
  • Motivational enhancement therapy – helps you build up the motivation to stick with your treatment plan
  • Contingency management – focuses on giving you incentives for positive behaviors such as staying off the opioids
  • Group counseling – which can help you feel that you are not alone with your issues. You get a chance to hear about the difficulties and successes of others who have the same challenges. This can help you to learn new strategies for dealing with the situations you may come across.
  • Family counseling – includes partners or spouses and other family members who are close to you. It can help to repair and improve your family relationships.

Counselors can also refer you to other resources that you might need, such as

  • Peer support groups, including 12-step programs like Narcotics Anonymous
  • Spiritual and faith-based groups
  • HIV testing and hepatitis screening
  • Case or care management
  • Employment or educational supports
  • Organizations that help you find housing or transportation

Prescription Opioids

  • Oxycodone
  • Hydrocodone-Acetaminophen
  • Hydrocodone bitartrate
  • Hydrocodone-Homatropine
  • Hydrocodone-Ibuprofen
  • Pseudoephedrine-Hydrocodone
  • Hydrocodone-Chlorpheniramine
  • Hydrocodone-Cpm-Pseudoephed
  • Morphine
  • Morphine-Naltrexone
  • Hydromorphone
  • Fentanyl Citrate
  • Fentanyl
  • Codeine Poli-Chlorphenir Poli
  • Acetaminophen with codeine phosphate/Acetaminophen-Codeine
  • Methadone
  • Methadone Hydrochloride
  • Morphine Sulfate
  • Oxymorphone Hydrochloride
  • Meperidine
  • Tramadol
  • Carfentanil
  • Buprenorphine


Opioids What They Do and How to Take Them

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