An opioid is a psychoactive chemical that works by binding to opioid receptors, which are found principally in the central and peripheral nervous system and the gastrointestinal tract. The receptors in these organ systems mediate both the beneficial effects and the side effects of opioids.
Opioids are among the world's oldest known drugs; the use of the opium poppy for its therapeutic benefits predates recorded history. The analgesic (painkiller) effects of opioids are due to decreased perception of pain, decreased reaction to pain as well as increased pain tolerance. The side effects of opioids include sedation, respiratory depression, constipation, and a strong sense of euphoria. Opioids can cause cough suppression, which can be both an indication for opioid administration and an unintended side effect. Opioid dependence can develop with ongoing administration, leading to withdrawal with abrupt discontinuation. Opioids are well known for their ability to produce a feeling of euphoria, motivating some to recreationally use opioids.
A List of Common Opiates in Increasing Strength
These are some of the common opiates and their generic names. They are listed in order of increasing strength.
These are some of the common opiates and their generic names. They are listed in order of increasing strength.
- Codeine
- Vicodin, Hycodan (hydrocodone)
- MS Contin Kadian (morphine)
- Oxycontin, Percoset (oxycodone)
- Dilaudid (hydromorphone)
- Duragesic (fentanyl)
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| Opiates Addiction and Withdrawal |
Opiates Uses :
Opioids have long been used to treat acute pain (such as post-operative pain). They have also been found to be invaluable in palliative to alleviate the severe, chronic, disabling pain of terminal conditions such as cancer, and degenerative conditions such as rheumatoid arthritis. However, opioids should be used cautiously in chronic non-cancer pain. High doses are not necessarily required to control the pain of advanced or end-stage disease. Tolerance (a physical reaction which makes the body less responsive to analgesic and other effects of opiates) may occur.
Opoids Adverse effects
- Common adverse reactions in patients taking opioids for pain relief include: nausea and vomiting, drowsiness, itching, dry mouth, miosis, and constipation.
- Oxycodone and codeine may double mortality as compared to hydrocodone. In contrast to hydrocodone, oxycodone and codeine are metabolized by cytochrome P-450 CYP2D6which may lead to variable pharmacokinetics due to single-nucleotide polymorphisms and drug interactions.
- Infrequent adverse reactions in patients taking opioids for pain relief include: dose-related respiratory depression (especially with more potent opioids), confusion, hallucinations,delirium, urticaria, hypothermia, bradycardia/tachycardia, orthostatic hypotension, dizziness, headache, urinary retention, ureteric or biliary spasm, muscle rigidity, myoclonus (with high doses), and flushing (due to histamine release, except fentanyl and remifentanil).
- Opioid-induced hyperalgesia has been observed in some patients, whereby individuals using opioids to relieve pain may paradoxically experience more pain as a result of their medication.
- Nausea: tolerance occurs within 7–10 days, during which antiemetics (e.g. low dose haloperidol once at night) are very effective.[citation needed] Due to severe side effects such as tardive dyskinesia, haloperidol is currently rarely used.
- Vomiting.
- Drowsiness: tolerance usually develops over 5–7 days, but if troublesome, switching to an alternative opioid often helps.
Safety Studies over the past 20 years have repeatedly shown opioids to be safe when they are used correctly. In the UK two studies have shown that double doses of bedtime morphine did not increase overnight deaths, and that sedative dose increases were not associated with shortened survival (n=237).
Opiate Tolerance
Tolerance is the process whereby neuroadaptation occurs (through receptor desensitization) resulting in reduced drug effects. Tolerance is more pronounced for some effects than for others; tolerance occurs quickly to the effects on mood, itching, urinary retention, and respiratory depression, but occurs more slowly to the analgesia and other physical side effects. However, tolerance does not develop to constipation or miosis (the constriction of the pupil of the eye to less than or equal to two millimeters).Tolerance to opioids is attenuated by a number of substances, including:
- calcium channel blockers
- intrathecal magnesium and zinc
- NMDA antagonists, such as dextromethorphan, ketamine,and memantine.
- cholecystokinin antagonists, such as proglumide.
Newer agents such as the phosphodiesterase inhibitor ibudilast have also been researched for this application.
Tolerance is a physiologic process where the body adjusts to a medication that is frequently present, usually requiring higher doses of the same medication over time to achieve the same effect. It is a common occurrence in individuals taking high doses of opioids for extended periods, but does not predict any relationship to misuse or addiction.
Dependence is characterized by unpleasant withdrawal symptoms that occur if opioid use is abruptly discontinued. The withdrawal symptoms for opiates include severe dysphoria,sweating, nausea, rhinorrea, depression, severe fatigue, vomiting and pain. Slowly reducing the intake of opioids over days and weeks will reduce or eliminate the withdrawal symptoms. The speed and severity of withdrawal depends on the half-life of the opioid; heroin and morphine withdrawal occur more quickly and are more severe than methadonewithdrawal, but methadone withdrawal takes longer. The acute withdrawal phase is often followed by a protracted phase of depression and insomnia that can last for months. The symptoms of opioid withdrawal can also be treated with other medications, such as clonidine, antidepressants and benzodiazepines, but with a low efficacy. Physical dependence does not predict drug misuse or true addiction, and is closely related to the same mechanism as tolerance.
Opiate Addiction
Do You Have an Opiate Addiction?
- Has your use of opiates increased over time?
- Do you experience withdrawal symptoms when you stop using?
- Do you use more than you would like, or more than is prescribed?
- Have you experienced negative consequences to your using?
- Have you put off doing things because of your drug use?
- Do you find yourself thinking obsessively about getting or using your drug?
- Have you made unsuccessful attempts at cutting down your drug use?
If you answered yes to at least three of those questions, then you are addicted to opiates.
Addiction is the process whereby physical and/or psychological dependence develops to a drug - including opioids. The withdrawal symptoms can reinforce the addiction, driving the user to continue taking the drug. Psychological addiction is more common in people insufflating or injecting opioids recreationally rather than taking them orally for medical reasons.
Opiates produce a sense of wellbeing or euphoria that can be addictive to some people. Opiates are legitimately used for treating pain. When used for pain relief, many people develop tolerance, meaning they need more and more to get the same effect. Some people go on to develop an addiction to opiates. They begin to obsessively think about getting more opiates and in some cases engage in illegal activities such as double doctoring.
A high dose of opiates can cause death from cardiac or respiratory arrest. Tolerance to the euphoric effect of opiates develops faster than tolerance to the dangerous effects. Therefore people often overdose by mistake because they are trying to get a higher high and take too much.
A high dose of opiates can cause death from cardiac or respiratory arrest. Tolerance to the euphoric effect of opiates develops faster than tolerance to the dangerous effects. Therefore people often overdose by mistake because they are trying to get a higher high and take too much.
Opiate overdose can be reversed in hospital with intravenous naltrexone. Please contact emergency services if you feel you are in danger of an overdose.
Opioids Pharmacology
Opioids bind to specific opioid receptors in the nervous system and other tissues. There are three principal classes of opioid receptors, μ, κ, δ (mu, kappa, and delta), although up to seventeen have been reported, and include the ε, ι, λ, and ζ (Epsilon, Iota, Lambda and Zeta) receptors. Conversely, σ (Sigma) receptors are no longer considered to be opioidsreceptors because: their activation is not reversed by the opioid inverse-agonist naloxone, they do not exhibit high-affinity binding for classical opioids, and they are stereo selective for dextro-rotatory isomers while the other opioid receptors are stereo-selective for laevo-rotatory isomers.
Opiates Classification
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.
Esters of morphine opiates: slightly chemically altered but more natural in nature than the semi-synthetics as most are morphine-prodrugs,
- diacetylmorphine (morphine diacetate-heroin),
- nicomorphine (morphine dinicotinate),
- dipropanoylmorphine (morphine dipropionate),
- desomorphine,
- acetylpropionylmorphine,
- dibenzoylmorphine,
- diacetyldihydromorphine.
Semi-synthetic opioids: created from either the natural opiates or morphine esters as
- hydromorphone,
- hydrocodone,
- oxycodone,
- oxymorphone,
- ethylmorphine
- and buprenorphine .
Fully synthetic opioids: as
- fentanyl,
- pethidine,
- levorphanol,
- methadone,
- tramadol
- 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.
Endogenous opioids Opioid-peptides that are produced in the body include:
- Endorphins
- Enkephalins
- Dynorphins
- Endomorphins
Opiate Withdrawal
Opiate withdrawal can be extremely uncomfortable. The important thing to remember is that opiate withdrawal is not life threatening if you are withdrawing only from opiates and not a combination of drugs. (Withdrawal from alcohol and some drugs such as benzodiazepines is potentially dangerous)
Opiate withdrawal symptoms include:
Opiate withdrawal symptoms include:
- Low energy, Irritability, Anxiety, Agitation, Insomnia
- Runny nose, Teary eyes
- Hot and cold sweats, Goose bumps
- Yawning
- Muscle aches and pains
- Abdominal cramping, Nausea, Vomiting, Diarrhea
Opiate withdrawal symptoms can last anywhere from one week to one month. Especially the emotional symptoms such as low energy, anxiety and insomnia can last for a few months after stopping high doses of opiates.
Once the early stage withdrawal symptoms are over, you will still experience post-acute withdrawal symptoms. These are less severe but last longer.
Once the early stage withdrawal symptoms are over, you will still experience post-acute withdrawal symptoms. These are less severe but last longer.
Opiates Recovery Plan
- Break the cycle of guilt and shame. Do your recovery with other people who are going through the same thing. This is the benefit of going to 12-step meetings such as Narcotics Anonymous NA or Alcoholics Anonymous AA. (More resources.)
- Ask for help. Have a strong support system.
- Be honest, and practice sharing how you feel.
- Avoid high risk situations.
- Learn relapse prevention strategies.
- Do your recovery one day at a time.
Medications Used to Treat Opiate Addiction
- Suboxone, Subutex (buprenorphine)
- Revia (naltrexone)
- Methadone
The Stages of Relapse
Relapse is a process, it's not an event. In order to understand relapse prevention you have to understand the stages of relapse. Relapse starts weeks or even months before the event of physical relapse. In this page you will learn how to use specific relapse prevention techniques for each stage of relapse. There are three stages of relapse.- Emotional relapse
- Mental relapse
- Physical relapse
Emotional Relapse
In emotional relapse, you're not thinking about using. But your emotions and behaviors are setting you up for a possible relapse in the future.The signs of emotional relapse are:
- Anxiety
- Intolerance
- Anger
- Defensiveness
- Mood swings
- Isolation
- Not asking for help
- Not going to meetings
- Poor eating habits
- Poor sleep habits
The signs of emotional relapse are also the symptoms of post-acute withdrawal. If you understand post-acute withdrawal it's easier to avoid relapse, because the early stage of relapse is easiest to pull back from. In the later stages the pull of relapse gets stronger and the sequence of events moves faster.
Early Relapse Prevention
Relapse prevention at this stage means recognizing that you're in emotional relapse and changing your behavior. Recognize that you're isolating and remind yourself to ask for help. Recognize that you're anxious and practice relaxation techniques. Recognize that your sleep and eating habits are slipping and practice self-care.
If you don't change your behavior at this stage and you live too long in the stage of emotional relapse you'll become exhausted, and when you're exhausted you will want to escape, which will move you into mental relapse.
Practice self-care. The most important thing you can do to prevent relapse at this stage is take better care of yourself. Think about why you use. You use drugs or alcohol to escape, relax, or reward yourself. Therefore you relapse when you don't take care of yourself and create situations that are mentally and emotionally draining that make you want to escape.
For example, if you don't take care of yourself and eat poorly or have poor sleep habits, you'll feel exhausted and want to escape. If you don't let go of your resentments and fears through some form of relaxation, they will build to the point where you'll feel uncomfortable in your own skin. If you don't ask for help, you'll feel isolated. If any of those situations continues for too long, you will begin to think about using. But if you practice self-care, you can avoid those feelings from growing and avoid relapse.
Mental Relapse
In mental relapse there's a war going on in your mind. Part of you wants to use, but part of you doesn't. In the early phase of mental relapse you're just idly thinking about using. But in the later phase you're definitely thinking about using.
The signs of mental relapse are:
- Thinking about people, places, and things you used with
- Glamorizing your past use
- Lying
- Hanging out with old using friends
- Fantasizing about using
- Thinking about relapsing
- Planning your relapse around other people's schedules
It gets harder to make the right choices as the pull of addiction gets stronger.
Techniques for Dealing with Mental Urges
Play the tape through. When you think about using, the fantasy is that you'll be able to control your use this time. You'll just have one drink. But play the tape through. One drink usually leads to more drinks. You'll wake up the next day feeling disappointed in yourself. You may not be able to stop the next day, and you'll get caught in the same vicious cycle. When you play that tape through to its logical conclusion, using doesn't seem so appealing.
A common mental urge is that you can get away with using, because no one will know if you relapse. Perhaps your spouse is away for the weekend, or you're away on a trip. That's when your addiction will try to convince you that you don't have a big problem, and that you're really doing your recovery to please your spouse or your work. Play the tape through. Remind yourself of the negative consequences you've already suffered, and the potential consequences that lie around the corner if you relapse again. If you could control your use, you would have done it by now.
Tell someone that you're having urges to use. Call a friend, a support, or someone in recovery. Share with them what you're going through. The magic of sharing is that the minute you start to talk about what you're thinking and feeling, your urges begin to disappear. They don't seem quite as big and you don't feel as alone.
Distract yourself. When you think about using, do something to occupy yourself. Call a friend. Go to a meeting. Get up and go for a walk. If you just sit there with your urge and don't do anything, you're giving your mental relapse room to grow.
Wait for 30 minutes. Most urges usually last for less than 15 to 30 minutes. When you're in an urge, it feels like an eternity. But if you can keep yourself busy and do the things you're supposed to do, it'll quickly be gone.
Do your recovery one day at a time. Don't think about whether you can stay abstinent forever. That's a paralyzing thought. It's overwhelming even for people who've been in recovery for a long time.
One day at a time, means you should match your goals to your emotional strength. When you feel strong and you're motivated to not use, then tell yourself that you won't use for the next week or the next month. But when you're struggling and having lots of urges, and those times will happen often, tell yourself that you won't use for today or for the next 30 minutes. Do your recovery in bite-sized chunks and don't sabotage yourself by thinking too far ahead.
Make relaxation part of your recovery. Relaxation is an important part of relapse prevention, because when you're tense you tend to do what’s familiar and wrong, instead of what's new and right. When you're tense you tend to repeat the same mistakes you made before. When you're relaxed you are more open to change.
Physical Relapse
Once you start thinking about relapse, if you don't use some of the techniques mentioned above, it doesn't take long to go from there to physical relapse. Driving to the liquor store. Driving to your dealer.It's hard to stop the process of relapse at that point. That's not where you should focus your efforts in recovery. That's achieving abstinence through brute force. But it is not recovery. If you recognize the early warning signs of relapse, and understand the symptoms of post-acute withdrawal, you'll be able to catch yourself before it's too late.
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