Over the years and with continuously increasing demand, MCCare has been contacted by people experiencing withdrawal due to discontinuing prescribed opioids, and support through the healing process to recovery has been provided.
Like benzodiazepine and antidepressant withdrawal, the people supported are mainly those who took opioids as prescribed by their doctors. Anecdotal evidence suggests that while some are able to discontinue their medication with no significant problems and maybe experience just a mild withdrawal reaction or in some cases, none at all, others experience a severe withdrawal that lasts beyond the reported few weeks.
WHAT IS AN OPIOID?
“Opioid” is a term used for substances (originally derived from the opium poppy) and their semisynthetic and synthetic analogues, that bind to specific opioid receptors. While opioids are synthetic or semisynthetic, opiates are derived naturally from the poppy plant. However, because of similar molecules, the mechanisms are the same and the information here is relevant to both.
Opioids are a class of drugs used to manage severe pain. Apart from pain relief, taking an opioid can result in mental relaxation and euphoric feelings. When taken long-term, the person can become dependent and experience difficulty discontinuing the drug as part of an opioid withdrawal syndrome. UK drug treatment centres reported a 33% rise in patients with prescribed opioid dependency in 2018 and 2019.
TYPES OF OPIOIDS
There are two types of opioids: endogenous and exogenous. Some endogenous opioids that bind to the receptors are enkephalins, endorphins, endomorphins, dynorphins, and nociception/orphanin. Exogenous opioids like morphine, heroin, and fentanyl are substances that are introduced into the body and bind to the same receptors as the endogenous opioids.
There are five types of opioid receptors: mu receptor (MOR), kappa receptor (KOR), delta receptor (DOR), nociception receptor (NOR) and zeta receptor (ZOR). Within these receptors are a subset of subtypes: mu1, mu2, mu3, kappa1, kappa2, kappa3, delta1, and delta2.
OPIOID RECEPTOR BINDING AND ROLES
Mu1,2,3 receptors (MOR) bind to endogenous ligands beta-endorphin, endomorphin 1 and 2. Proopiomelanocortin (POMC) is the precursor.
Mu1 plays a role in analgesia and dependence. The mu-2 receptor in euphoria, dependence, respiratory depression, miosis, decreased digestive tract motility/constipation and the Mu-3 receptor (Prodynorphin as the precursor) causes vasodilation.
Kappa receptors (KOR) bind to dynorphin A and B (Prodynorphin as the precursor). They play a role in analgesia, diuresis, and dysphoria.
Delta receptors (DOR) bind to enkephalins (precursor is Proenkephalin). They play a role in analgesia and reduction in gastric motility.
Nociceptin receptors (NOR) bind to nociceptin/orphanin FQ (Pre-pronociceptin is the precursor) causing analgesia and hyperalgesia.: (This depends on the concentration.)
The role of Zeta receptors (ZOR) is to regulate developmental events in normal and tumorigenic tissues and cells.
TOLERANCE
As the person continues to take the painkiller, drug tolerance develops and more of the drug is needed in order for it to be effective. How long it takes for this happen varies and depends on the individual.
PHYSICAL DEPENDENCE
Like tolerance, how long it takes to become physically dependent varies with each person, and withdrawal reactions can occur any time the drug is missed, stopped, or dosage reduced.
Dependency can be directly tied to the length of time taking a particular drug, dosage amount, which drug was taken, how the drug was taken, and the presence of underlying medical conditions. The experience of withdrawal from an opioid drug can vary from person to person.
TAPERING
It is important to not stop taking your medication abruptly. If you have decided to stop taking the drug, ask your doctor about a withdrawal tapering plan that will safely and gradually reduce the amount of medication you take, until you are completely off it.
The length of taper will vary according to each individual and the medication taken and how long you’ve been taking it. Your doctor will discuss your protocol taking into consideration your medical history, your needs, and the ways to minimise health risks. During your taper, your doctor will monitor your response to discontinuing the drug and ensure your safety and well-being.
It is important to follow your withdrawal plan and your doctor’s instructions. Your body will need to adjust to each stage of your taper, and this is why a gradual and gentle approach is recommended. It will also allow you time to practise coping skills to deal with pain management as well as cope with other symptoms that may emerge.
WITHDRAWAL SYNDROME
Not tapering safely off an opioid or rapid discontinuation can result in uncontrolled pain and other withdrawal symptoms. Like other prescribed drug withdrawal syndromes, even in cases where a taper has been used, symptoms can be experienced.
The withdrawal syndrome associated with opioids or opiates is generally described as a flu-like illness, but withdrawal symptoms may range from mild to severe, depending on how dependent the individual is on an opioid drug.
Early Withdrawal Symptoms
These usually start within 6-12 hours for short-acting opiates, and they start within 30 hours for longer-acting ones:
Tearing up
Muscle aches
Agitation
Trouble falling and staying asleep
Excessive yawning
Anxiety
Nose running
Sweats
Racing heart
Hypertension
Fever
Late Withdrawal Symptoms
These peak within 72 hours and usually last a week or so:
Nausea and vomiting
Diarrhea
Goosebumps
Stomach cramps
Depression
Drug cravings
Some of the psychological withdrawal symptoms and cravings for opioid drugs may continue longer than a few weeks or months in some cases.
Withdrawal effects must be monitored and medically treated. Persistent vomiting and diarrhoea if left untreated can result in dehydration, and other complications.
Apart from medical monitoring and treatment, therapy and psychological support can help with coping with the symptoms and side effects of withdrawal. Stopping opioids can be difficult, but it can be done. Having adequate and appropriate medical care, planning and sticking with your taper, finding good coping resources and using them, and learning alternative ways of coping with pain, will all be beneficial as you make your way to recovery.
COPING
Coping with opioid withdrawal requires the same approach as one takes with tranquilliser and antidepressant withdrawal. Self-kindness, acceptance, patience, perseverance and the use of coping tools will help tremendously with coping. All the resources on this website are applicable as they have also been used by people supported through opioid withdrawal and with good results. Everything on this website is shared with consideration for anyone who is discontinuing an opioid, benzodiazepine or antidepressant drug.
Caution: Never stop taking your painkiller abruptly or rush your taper. Always taper off slowly using a method recommended by your doctor, under the supervision of your doctor.
References
American Psychiatric Association. (2013). Diagnostic and statistical manual of mental disorders (5th). Arlington, VA: American Psychiatric Publishing.
Center for Substance Abuse Treatment. (2006). Detoxification and substance abuse treatment. Treatment Improvement Protocol (TIP) Series 45, DHHS Publication No. (SMA) 06-4131. Rockville, MD: Substance Abuse and Mental Health Services Administration.
Cowan D, Wilson-Barnett J, Griffiths P, Allan L. (2003). A Survey of Chronic Non-Cancer Pain Patients Prescribed Strong Opioid Analgesics. Pain Medicine. 4. 340-351.
FDA Drug Safety. https://www.fda.gov/drugs/drug-safety-and-availability/fda-identifies-harm-reported-sudden-discontinuation-opioid-pain-medicines-and-requires-label-changes. Accessed Oct. 1, 2022
Kampman K, Jarvis M. American Society of Addiction Medicine (ASAM) National Practice Guideline for the use of medications in the treatment of addiction involving opioid use. J Addict Med. 2015;9(5):358-367. PMID: 26406300
Merck. Opioid toxicity and withdrawal. Merck Manual Professional Version. https://www.merckmanuals.com/professional/special-subjects/recreational-drugs-and-intoxicants/opioid-toxicity-and-withdrawal. Accessed Dec. 13, 2019.
Moore A, Journal of Nursing Opioid Misuse: Breaking the Prescription Addiction Cycle, Nursing
Standard, Alison Moore volume 34 number 7 / July 2019 / 59.
Nikolaides JK, Thompson TM. Opioids. In: Walls RM, Hockberger RS, Gausche-Hill M, eds. Rosen’s Emergency Medicine: Concepts and Clinical Practice. 9th ed. Philadelphia, PA: Elsevier; 2018:chap 156.
Ritter JM, Flower R, Henderson G, Loke YK, MacEwan D, Rang HP. Drug abuse and dependence. In: Ritter JM, Flower R, Henderson G, Loke YK, MacEwan D, Rang HP, eds. Rang and Dale’s Pharmacology. Philadelphia, PA: Elsevier; 2020:chap 50.
Toubia T, Khalife T. The Endogenous Opioid System: Role and Dysfunction Caused by Opioid Therapy. Clin Obstet Gynecol. 2019 Mar;62(1):3-10.
