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Opioids

All information on this page pertaining to treatment options are provided as a reference only, and are not intended as treatment advice.

 

Opioids, also known as Narcotics, are a class of drugs related to morphine, the active ingredient derived from the Opium Poppy plant. These drugs are used medically to treat pain but are also abused illicitly because of their ability to induce states of euphoria at higher doses.

Heroin is perhaps the most renown of the opioids to be used illicitly. Other common opioids that are used medically include codeine, hydromorphone, oxycodone, methadone, mepedridine, and fentanyl. There are over 20 different opioid drugs currently available (see here for further information).

American statistics show that about 1.8% of people will try heroin, and of these about 25% go on to develop heroin abuse or dependence [ref].

How Opioids Work

Opioids can be ingested orally, snorted, and injected intravenously or subcutaneously. When taken orally, the effect is usually felt within 30 minutes, and when snorted and injected the effect occurs immediately. Heroin's effects last for a few hours, while the effects of long-acting opioids like methadone tend to last a full day. Most opioids are detectible in the urine up to 4 days after use, and in hair samples up to 3 months after use.

Opioids bind to opioid receptors in the brain, thus mimicking the effects of the body's own naturally occurring opioid-like hormones, called endorphins. Endorphins are released following an acute injury and serve to reduce the pain. They are also released during strenuous exercise, states of arousal, and orgasm, and produce feelings of well-being and relaxation. Opioid drugs tend to produce effects that are much more intense than what is experienced from endorphins, especially when used in higher doses.

The feelings of well-being caused by opioids seem to be due at least in part to their stimulation of the brain's dopaminergic reward pathway. This strongly reinforces the continued use of these substances.

Regular Opioid Use

Opioids are commonly used medically for treating pain, cough and diarrhea.

Opioid Intoxication

Especially when used illicitly and in high doses, opioids will produce a euphoric high accompanied by a feeling of warmth. Drowsiness and sedation tend to set in as the high wanes. Slurred speech and impaired memory and concentration occur at higher doses.

The physical symptoms include dry mouth, itchiness and flushing in the face, a feeling of heaviness in the arms and legs, slowed breathing, pupillary constriction, and constipation. First time users often experience nausea and vomiting.

Overdose of opioids can cause coma, respiratory depression, hypothermia, lowered blood pressure and a slowed heart rate, and can be fatal.

Effects of Long-Term Regular Opioid Use

Especially when used illicitly, opioids lead to tolerance - where increasingly large doses are required to give similar effects - and dependence. The greatest dangers of repeated opioid use come from the hazardous lifestyle associated with illicit use. This includes the risk of contracting HIV or viral hepatitis from needle sharing, but also includes the medical and social consequences of neglecting one's health, nutrition and social obligations due to the all-consuming nature of opioid dependence.

Opioid Withdrawal

Following regular opioid use, withdrawal symptoms can develop as soon as 6-8 hours after the last dose of a short-acting opioid like heroin or morphine, and within a day or two after the last dose of a long-acting opioid like methadone. These symptoms usually peak after a couple of days and can linger for a couple of weeks.

These symptoms include dysphoric and irritable moods, restlessness, severe muscle cramps and bone aches, nausea and vomiting, profuse diarrhea, insomnia, fever and sweats, tearing and runny nose, yawning, pupillary dilation, elevated blood pressure and heart rate, and piloerection or gooseflesh (thus giving the term "Cold Turkey" to the withdrawal syndrome). These symptoms are usually not life-threatening, though it is important to be drinking adequate amounts of fluids with electrolytes in order to prevent dehydration and electrolyte imbalance from excessive vomiting and diarrhea.

Treating opioid withdrawal can be accomplished on an outpatient basis with individuals who can be trusted to follow the procedures and not continue to misuse opioids. Otherwise, the withdrawal can be managed on an inpatient unit.

For people who abuse heroin, an effective method is to replace it with Buprenorphine (a partial opioid agonist) 4 to 16mg daily, or Methadone 20 to 35 mg daily, and then to taper the dose progressively until discontinued over a period of a couple of weeks. Once this has been accomplished, clonidine 0.1mg every four hours as needed can be used for up to five days in a tapering fashion to minimize withdrawal symptoms. Alternatively, lofexidine 0.2mg twice a day for five days can be used.

In situations where Buprenorphine or Methadone cannot be used, one could instead give Clonidine 0.1 to 0.2mg every four hours and tapered progressively over 10 days, or Lofexidine titrated up to 1.2mg twice daily, and then progressively tapered over 10 days. Diffuse pains could be managed with acetaminophen or NSAIDs, nausea could be managed with antiemetics, diarrhea could be treated with Loperamide, antispasmodics could be used for abdominal cramps, and anxiety and irritability managed with Diazepam.

Rapid detoxification is a procedure where an individual is withdrawn from opioids over a period of three to five days using a combination of Clonidine, Naltrexone, and in some cases Buprenorphine. This procedure requires medical monitoring by an experienced team and is not necessarily more effective than the longer detoxification processes described above.

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Treating Opioid Abuse and Dependence

Treating opioid use disorders follows the general principles described here, and specialized treatment programs offering a combination of psychotherapy/ counseling and medications is often required. Regarding medication use, choice depends on whether the individual is able to remain completely abstinent from all opioids, or whether replacement therapy is required.

Replacement therapy involves prescribing the individual a long-acting opioid medication in a controlled and regulated fashion. The two main forms currently in use are Methadone and Buprenorphine [ref]. Using these medications prevents withdrawal symptoms or drug cravings while keeping individuals invested in a treatment program where they can receive psychotherapy/ counseling and curb their high-risk life-style patterns associated with opioid abuse and dependence. The goal is eventually to taper and discontinue these medications, but some individuals remain on them for years. Methadone seems to be more effective than Buprenorphine at keeping individuals in treatment and preventing illicit opioid use [ref]. However, Buprenorphine has less abuse potential, especially when prescribed in the combination Buprenorphine-Naloxone tablet, and produces less withdrawal symptoms when it is being tapered.

For individuals who have managed to withdraw fully from opioids and are now abstinent, Naltrexone can be used to prevent relapse as it blocks the actions of other opioids. Because this treatment only works when it is being taken regularly, it tends to be more effective for highly motivated individuals living in stable social situations [ref]. More generally, there is insufficient evidence to conclude that it is effective for most individuals, at least in the oral form that needs to be taken daily [ref]. It is possible that the long-acting injectible format, which can be given once a month, will produce more consistent results.

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Nicotine

Phencyclidine