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Oxycodone

What is the chemistry of Oxycodone?

Oxycodone is a semisynthetic opioid (1.5 times as powerful as morphine) derived from the alkaloid thebaine. As with other opioids, its original source is the poppy plant, and it has relaxing and pain-relieving effects because it binds to nerve receptors in the brain resulting in the blocking of pain signals, and a general calming and anti-depressing effect.

Oxycodone is best known as the active ingredient in OxyContin, a prescription pain reliever manufactured and marketed by Purdue Pharma.

What is the history of Oxycodone? 

Although opium products have been used both recreationally (to “feel good”) and as medications since the time of Hippocrates, oxycodone was first developed in Germany in 1917. It was intended as a safer alternative to heroin and morphine, whose addictive risks were already well known. Few anticipated that oxycodone (now a Schedule II narcotic in the United States) would eventually become one of the most widely abused prescription drugs.

The publicity and controversy surrounding oxycodone hit its heights after Purdue Pharma released OxyContin in 1995, highly marketing and falsely promoting their new medication as a long-lasting pain reliever with very little potential for abuse or addiction. By 2004, OxyContin was called a “leading drug of abuse” And in 2007 Purdue Pharma paid a $634 million fine for claiming OxyContin was less addictive than other, similar pain medications. From 1999 to 2015, more than 183,000 people have died in the U.S. from overdoses related to prescription opioids. Still, by 2017, over thirty-five billion dollar’s worth of OxyContin had been sold—and “opioid epidemic” was an everyday phrase in the English language.

In 2010, the FDA approved a new OxyContin formulation designed to reduce incidents of people breaking open or crushing the slow-release tablets to get bigger oxycodone doses faster, however, they do nothing to prevent the use of additional doses by those wanting to get high on their medication.

What are the side effects of oxycodone use?

Development of tolerance, dependence and addiction are just one set of side effect of abusing Oxycontin.  Some people are allergic to oxycodone and may suffer hives, breathing difficulties, and swelling of face and throat. More common, if less dangerous, side effects include nausea, loss of appetite, dry mouth, unusual perspiration, itchiness, dry mouth, dizziness, headaches, and fatigue.

In higher doses, oxycodone may noticeably slow heart rate, cause severe dizziness, or make the pupils of the eyes constrict and the skin turn cold and clammy. Life-threatening effects are caused by the continual slowing of respirations until the user is no longer breathing.

How was oxycodone intended to be used?

Oxycodone is one of many opioid medications developed as a prescription to relieve acute pain.  It’s potential for addiction is a serious side effect. The National Institute on Drug Abuse estimates that over two million Americans are have misused or are dependent on opioid pain relievers

Addiction most frequently develops when someone takes pills over a period of time and takes and increasing number of pills.  If you need prescriptions opioids like oxycodone or others, remember to take them as prescribed.

How is oxycodone used illicitly?

People who are prescribed oxycodone or other prescription opioids develop an addiction when take continually increasing amounts because they believe the prescribed dosage is ineffective, or they want to achieve the euphoric effect that comes with initial use or they are trying to ward off the discomfort of withdrawal.  Often, they then rely on their own judgment to decide if they need more pills. The only safe response to an oxycodone prescription’s failing to meet expectations is to consult with the prescribing doctor—especially if it’s a case of reduced effect, which could mean you’re building up tolerance, a frequent first step on the path to addiction. Fortunately, doctors have become more aware of the risks in prescribing oxycodone and other opioids.

People who are drawn to the euphoric effects of opioids may crush their medication and snort or inject it, releasing the active ingredients more quickly. Nearly any drug takes effect faster when introduced into the body via the respiratory system or bloodstream in comparison to the stomach.

What are the signs of illicit use of oxycodone?

Symptoms of abuse or addiction include: constant drowsiness, unexplained bursts of euphoria,  “pinpoint pupils” in the eyes, chronic constipation or nausea, “drunken” behavior in the absence of alcohol consumption, tolerance or dependence on the drug, requesting prescription refills with unusual frequency, becoming negligent of everyday responsibilities, “losing” money or personal property for unexplained reasons (which may indicate money is being spent for drugs), and giving up priorities such as work or family responsibilities.

Symptoms of withdrawal include: unusual anxiety or irritability, rapid breathing, runny nose, aches and pains, severe abdominal cramps, diarrhea, heavy perspiration, enlarged pupils, body tremors, and loss of appetite.

Symptoms of overdose include: pinpoint pupils, labored breathing, unconsciousness, skin turning pale and clammy, and bluish tinge to lips and fingernails. Call for emergency medical help if you experience withdrawal or overdose symptoms in conjunction with taking oxycodone or another opioid—and, after the emergency is over, look immediately into addiction detox and treatment options.

How Does Recovery Centers of America Treat Oxycodone Addiction?

For patients desiring detoxification and treatment for oxycodone:

Detoxification from Oxycodone (or other similar opioid) dependence or addiction is profoundly uncomfortable if done without medical supervision and intervention, it can be life-threatening if the individual is also abusing other drugs such as alcohol or a class of medications known as Benzodiazepines (Xanax, Klonopin, Alprazolam, etc).

Withdrawal symptoms generally start as soon as 8-12 hours after the last dose, but they are typically not severe in the first 24 hours.  The time of onset, severity and duration of withdrawal symptoms will vary based on the oxycodone formulation used (immediate-release or extended-release), amount of drug used, over what period of time, and but what route of administration (swallowing pills, smoking, injecting).

Detox can begin prior to the onset of withdrawal symptoms based on history, drug testing and constant symptom monitoring. RCA will monitor the patient round the clock, continually evaluating physiological and psychological symptoms and will use medications to control many of these symptoms.  Medications that may be used include those to wean off the oxycodone and palliative or “comfort” medications such as Clonodine, Robaxin, Trazadone, Phenobarbital, Ativan (in case of seizure), Bentyl, Librium, Tigan, and others.

Physical/medical aspects of detox may last up to 10 days but is more typically 6-7 days before patients are medically stable.  This doesn’t mean they don’t still have symptoms, just that those symptoms may not require round the clock, constant medical attention.

Psychiatric symptoms and craving can continue for many months.

At assessment, RCA staff administer the assessment in a calm environment, providing something to eat and beverages to keep the individual comfortable.  If, due to an inability to concentrate or onset of withdrawal symptoms, the individual finds it difficult to participate, the assessment can be divided into smaller sections.   Comfort medications can be provided as soon as the nursing assessment and some tests are done.

RCA staff provide a clear orientation to the treatment choices, the process, program rules, and expectations for participation to ensure each patient knows their options and to assist in decreasing any externally related anxiety about the process.

A controlled tapering of the drug, alleviating most withdrawal symptoms with medications (as noted previously) and wellness services is the safest, most tolerable method, resulting in the least discomfort.

As with any disorder, it’s also very important to involve significant others.  During the initial assess­ment and intake processes, RCA identifies family members or significant others who will support the patient and their treatment goals and get them involved immediately.

After medical detoxification, treatment will include small group therapy sessions, individual sessions, educational seminars, and workshops.  For our patients struggling with oxycodone or other opioids, additional services to assist with calming the body and the mind such as mindful meditation, yoga, progressive relaxation, and other therapeutic techniques are provided.

Through wellness seminars, life skills workshops, and various therapies, RCA focuses patients on developing a balanced lifestyle that includes restoring healthy eating and sleeping habits, participation in physical exercise and recreational activities, as well as building healthy relationships and a healthy support group to get them started on the road to long-term recovery.

Medication-Assisted Options

For patients who plan to detox fully from opioids, injectable Naltrexone sold under the trade name Vivitrol, a form of long-term blocker, can be especially helpful. naltrexone/Vivitrol are opioid “antagonists,” meaning they blocks the effects of opioid medications.  Vivitrol binds to the receptor that opioids use to provide pleasurable feelings and does not allow the opioid to have its effect. In fact, it’s strength in binding to the receptor is so much greater than the opioids ability, it will knock the opioid off the receptions even if they were there first.  Therefore, you should have 1-2 weeks without any opioid use to start vivitrol as using it will put an active opioid user into complete withdrawal.  It has also been shown to decrease cravings for both alcohol and opioids.

For patients who start with detoxification/treatment and find that complete abstinence is not tolerable for them due to cravings or difficulty functioning without medication, opioid replacement therapy is another method of ensuring that the opioid receptors remain at least partially engaged in a measured way while reducing these symptoms. This includes the medications suboxone and methadone.

The main/active ingredient in Suboxone is buprenorphine.  Buprenorphine is a partial agonist.  An agonist is a medication that binds to the receptor site – oxycodone, heroin and other opioids are “full agonists,” they bind to the receptors and activate them fully producing the euphoria users seek.  Suboxone is a partial agonist, it binds to and activates the same receptors as other opioids, but has only part of the effect that a full agonist such as oxycodone will have on the user. Suboxone remains active in the bloodstream for longer and does not produce quite the same euphoric effects as full agonists like oxycodone. The “high” is not as intense if these partial agonists are taken in higher doses, and buprenorphine even has a ceiling so that after a certain amount is taken, it no longer increases in effect.

Interestingly, Suboxone also contains the medication naloxone (that’s where the “oxone” portion of its name comes from). Naloxone, when given alone, is an opioid antagonist (completely blocks the effects of an opioid). If the Suboxone is taken as prescribed, the Naloxone will be inert (cause no effect).  If, in an effort to get all the medication into the bloodstream at one time the user crushes and injects the sublingual tablet, the naloxone effect dominates, and the medication blocks the receptors causing opioid withdrawal.  This decreases the likelihood that the Suboxone will be abused.

Methadone is another form of medication-assisted treatment.  a synthetic opioid, methadone is a longer-acting opioid replacement medication, it binds with the opiate receptors but without quite the euphoria as heroin and other opioids. Methadone is typically taken as a liquid medication and people taking it generally report to a clinic specializing in medication-assisted treatment at least 5 days per week.

Among other benefits, methadone maintenance gives users a daily, stable dose of opioids, decreases the likelihood that users will be injecting drugs, therefore getting Hepatitis or HIV, eliminates the need to find ways to pay for their opioids and helps people take the first steps toward getting back to normal life.  Although it is not entirely without its own health concerns, and dependence that is similar in strength to heroin, methadone is considered effective and safe and is included in the World Health Organization’s (WHO) list of Essential Medications.  One thing all treatment providers agree on – medications alone are not the complete answer for achieving long-term abstinence. Addiction is a brain disease that affects many aspects of a person’s physical and mental well-being as well as their personal, family and social relationships. RCA also includes behavioral therapies, pragmatic workshops, counseling sessions, and long-term support groups when helping those with opioid abuse and dependency issues.

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