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11 of the Most Addictive Opioids and Their Side-Effects

11 of the Most Addictive Opioids and Their Side-Effects

Opioids are a class of powerful illicit drugs and prescription pain medications that are increasingly abused in the United States. The use of opioids such as morphine, heroin, and prescription pain medications is becoming a serious global problem affecting an estimated 26.4 to 36 million people. In the United States, an estimated 2.1 million Americans are suffering from substance abuse disorders related to opioids. Of those 2.1 million, 467,000 are addicted to heroin. Why are narcotic pain medications and opioids so addictive? According to the National Institute on Drug Abuse (NIDA), it has everything to do with the brain. “Because prescription opioids are similar to, and act on the same brain systems affected by, heroin and morphine, they present an intrinsic abuse and addiction liability, particularly if they are used for non-medical purposes. They are most dangerous and addictive when taken via methods that increase their euphoric effects (the “high”), such as crushing pills and then snorting or injecting the powder or combining the pills with alcohol or other drugs. Also, some people taking them for their intended purpose risk dangerous adverse reactions by not taking them exactly as prescribed (e.g., taking more pills at once, or taking them more frequently or combining them with medications for which they are not being properly controlled); and it is possible for a small number of people to become addicted even when they take them as prescribed, but the extent to which this happens currently is not known.”

What are Opioids and How Do They Affect a Drug User?

Natural opioids are extracted from the resin of the opium poppy. These are termed “opiates,” although they are now classified more broadly with the other semi- and fully-synthetic opioids. Both opiates and opioids are highly addictive. Due to the difficulty of processing natural opiates, semi- and fully-synthetic opioids are more popular and easier to obtain.

  1. Codeine

It was discovered in 1832 by French chemist Pierre Jean Robiquet. Besides his identification of codeine, he studied amino acids – the building blocks of proteins. Often used as a pain treatment, as cough medicine or as an antidiarrheal, codeine can be used for mild to moderate pain. It is often combined with acetaminophen like Tylenol or nonsteroidal anti-inflammatory drugs such as aspirin or ibuprofen. The duration lasts from four to six hours and peaks around two hours. In the body, codeine is processed and broken down by the liver into morphine. How fast that process happens depends heavily on a person’s genetic predisposition and ability to metabolize medications. Codeine is often used as a recreational drug. It is often available with an anti-nausea medication called promethazine in a syrup form. Street names are “syrup,” “purple drank,” or “lean.” It’s usually available in prescriptions only. Side Effects of Codeine: Drowsiness, constipation, itching, nausea, dry mouth, urinary retention, euphoria, dysphoria, and coughing. Rare adverse side effects of using per physician’s directions, anaphylaxis, respiratory depression, acute pancreatitis, and seizures. Potential dangers with all opioids include those to pregnant women and breastfeeding mothers who can easily pass the drug onto their children.

  1. Morphine

Morphine is a powerful opiate that acts quickly on the central nervous system (CNS) to stop the feeling of pain. It’s sourced from the opium poppy. It is often taken for acute and chronic pain, and it can be ingested by mouth, injected into the muscle, under the skin, intravenously or taken rectally. The duration varies greatly but is usually between three and seven hours. It can also be used to help people with shortness of breath if it’s taken in very small doses. Side Effects of Morphine: Morphine can inhibit gastric emptying and can make a user constipated. It can also cause hormonal imbalances in both men and women. Recreational users can stop getting their period due to suppression of luteinizing hormones. It’s estimated that a majority of opioid addicts have induced hypogonadism. Later, this can cause osteoporosis that can lead to bone fractures. Independence and tolerance are other side effects than can developed over prolonged use of this opiate. Like heroin, morphine is far more likely to produce euphoria over other opioids. Essentially, the drugs are the same seeing as heroin is converted into morphine before binding to opioid receptors in the brain and spinal cord. Semi-synthetic opioids are made from natural opiates or morphine esters. Semi-synthetics include hydrocodone, oxycodone, heroin, etc.

  1. Hydrocodone

Hydrocodone is synthesized using codeine. It was first synthesized in Germany in 1920 and was approved by the FDA in 1943. Ninety-nine percent of hydrocodone consumed is by the United States. It is prescribed for moderate to severe pain and is used for cough treatment. This popular opioid is often combined with acetaminophen, ibuprofen, and aspirin. Due to its abuse, the U.S. government made tougher rules for prescribing hydrocodone in 2014. Side Effects of Hydrocodone: Side effects include nausea, constipation, drowsiness, lightheadedness, anxiety, dry throat, itching, rash, narrowing of pupils, tight chest and irregular breathing. In the U.S., the FDA considers hydrocodone a pregnancy category C drug and it should not be taken while pregnant. The child will be born dependent on the drug, and it could cause the child to be in respiratory distress at birth. The risk of becoming addicted to hydrocodone is like that of morphine.

  1. Oxycodone

This opioid is used to manage moderate to severe acute or chronic pain. Derived from the opioid alkaloid thebaine, it’s been used clinically since 1917. It’s available combined with other medications for immediate and controlled release such as acetaminophen and nonsteroidal anti-inflammatory drugs. Due to its common abuse, it’s often combined with naloxone to prevent opioid withdrawal symptoms as well as stopping the euphoric effects. In the U.S., oxycodone is only approved for oral use. Side Effects of Oxycodone: Like many opioids, euphoria, pain relief, and relaxation are reported. Adverse side effects include constipation, nausea, vomiting, itching, dry mouth, and sweating. By people who have not developed a tolerance to oxycodone, high doses can lead to slowed heart rate, shallow breathing, low blood pressure, respiratory arrest, and death. Withdrawal symptoms can be extreme. They can include anxiety, muscle pain, nausea, panic attacks, fever, and other flu-like symptoms.

  1. Heroin

In 1895, the drug company Bayer marketed diacetylmorphine as Heroin, an over-the-counter cough suppressant. At the time, morphine was being abused as a recreational drug, and Bayer was hoping to create a drug that didn’t have any adverse side effects but treated the same symptoms. However, the drug is just as addictive as morphine. Unlike other opioids, heroin is for recreational use only and is not available via prescription. It is usually injected, though it can be inhaled, snorted or smoked. The effects of the drug can last a few hours. It’s a popular recreational drug to do its euphoric side effects. Tolerance develops quickly, however, and an increased dosage is needed to feel the same euphoric effects. This rapid tolerance build-up is extremely like morphine, and it is why both drugs are commonly abused and create addiction. As reported by NIDA, “According to the National Survey on Drug Use and Health (NSDUH), in 2012 about 669,000 Americans reported using heroin in the past year, a number that has been on the rise since 2007. This trend appears to be driven largely by young adults aged 18–25 among whom there have been the greatest increases. The number of people using heroin for the first time is unacceptably high, with 156,000 people starting heroin use in 2012, nearly double the number of people in 2006 (90,000).” NIDA goes on to state, “The emergence of chemical tolerance toward prescribed opioids, perhaps combined in a smaller number of cases with an increasing difficulty in obtaining these medications illegally, may in some instances explain the transition to abuse of heroin, which is cheaper and in some communities easier to obtain than prescription opioids.” Side Effects of Heroin: In the long term, pure heroin can cause dependence and constipation. The purity of heroin sold on the street, however, can vary. This can lead to overdoses since no one knows precisely what’s in the drug. Intravenous use of heroin can cause a person to contract a bloodborne disease such as HIV or hepatitis, develop bacterial or fungal venous infections, develop abscesses, be poisoned due to chemical contaminants, and suffer from decreased kidney function. Heroin overdose is often treated with the opioid antagonist naloxone or naltrexone. This immediately reverses the effects of heroin. Immediate relief of these side effects can lead to withdrawal symptoms. Withdrawal symptoms naturally occur between six and 24 hours after use. That time can fluctuate depending on the user’s tolerance to the drug. Symptoms of withdrawal include sweating, anxiety, depression, nausea, vomiting, diarrhea, cramps, and spasms in the limbs.

  1. Hydromorphone

As a derivative of morphine, hydromorphone is to morphine what hydrocodone is to codeine. It’s a semi-synthetic, centrally-acting pain medication. Due to its solubility, it can be added to water for injection much more easily. Those who mistake it for heroin have been known to overdose more easily. It was discovered in 1924 in Germany. In the U.S., it can be used as a pain medication and has increased in prescriptions 287% between 1998 and 2006. It is a Schedule II controlled substance. Side Effects of Hydromorphone: Common side effects include dizziness, sedation, constipation, itching, nausea, vomiting, headache, hallucinations, and sweating. These are most common in patients using the drug recreationally. If too much is taken, respiratory and circulatory depression can occur. This may lead to death. Naloxone can be used to treat overdose, as well as oxygen supplementation. If hydromorphone is taken with alcohol, the risk is even greater. Prolonged use can lead to toxic levels that can affect cognitive function, induce a tremor and agitation.

  1. Oxymorphone

Oxymorphone is a treatment for severe to moderate pain and is often used as an obstetric analgesic during births. It does not seem to have the cough suppressive effects of some opioids. It is often taken as an extended-release tablet for pain management. It’s often only used for patients who have been using opioids as a pain reliever over an extended period. This drug is extremely addictive. It’s known by street names: Blue Heaven, Blues, Mrs. O, New Blues, Octagons, Oranges, Orgasna IR, OM, Pink, Pink Heaven, Pink Lady, Pink O, Stop Signs, and The O Bomb Side Effects of Oxymorphone: According to the Drug Enforcement Administration (DEA), “Acute overdose of oxymorphone, like other pure opioid agonists, can produce severe respiratory depression, somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, and reduction in blood pressure and heart rate. In some cases, an acute overdose may result in apnea, circulatory collapse, cardiac arrest, and death. Opioid receptor antagonist such as naloxone is a specific antidote against respiratory depression resulting from overdose or unusual sensitivity to oxymorphone. Oxymorphone related deaths have been reported in various states. Medical Examiners Commission Reports released by the Florida Department of Law Enforcement (FDLE) indicate that there were 185 oxymorphone related deaths in Florida for January through June 2012. Of these 185 deaths, 55 of them were caused by oxymorphone.”

  1. Buprenorphine

According to NIDA, “The arrival of buprenorphine represented a significant health services delivery innovation. FDA approved Subutex® (buprenorphine) and Suboxone® tablets (buprenorphine/naloxone formulation) in October 2002, making them the first medications to be eligible for prescribing under the Drug Addiction Treatment Act of 2000. Subutex contains only buprenorphine hydrochloride. This formulation was developed as the initial product. The second medication, Suboxone, contains naloxone to guard against misuse (by initiating withdrawal if the formulation is injected). Subutex and Suboxone are less tightly controlled than methadone because they have a lower potential for abuse and are less dangerous in an overdose. As patients progress in their therapy, their doctor may write a prescription for a take-home supply of the medication. To date, of the nearly 872,615 potential providers registered with the Drug Enforcement Administration (DEA), 25,021 registered physicians are authorized to prescribe these two medications. The development of buprenorphine and its authorized use in physicians’ offices gives opioid-addicted patients more medical options and extends the reach of addiction medication to remote populations.” Buprenorphine was first synthesized in 1969 after 10 years of attempting to create a drug that could treat pain without the adverse side effects. Now, research is trying to prove if this semi-synthetic opioid could be useful in the treatment of depression and cocaine dependence. It is also currently under investigation to treat neonatal abstinence syndrome. These are children who were exposed to opioids during pregnancy. Side Effects of Buprenorphine: Like other opioids, side effects can include nausea, vomiting, dizziness, memory loss, male ejaculatory difficulty, and decreased libido. Unlike morphine, there are fewer issues with central nervous system damage and constipation. Unfortunately, buprenorphine does carry the risk of dependence. It does have a slow onset and a half-life of 24 to 60 hours. In the case of fatal overdose, respiratory distress is often the cause. When mixed with other central nervous system depressants such as alcohol or benzos, fatal respiratory distress is possible. They should not be taken together.

Synthetic opioids:

Opiates vs opioids? The difference lies in synthesis. Opiates are naturally occurring chemicals while semi- and fully-synthetic opioids are extracted for opiates or fully manmade. Synthetic opioids were invented through the discovery of biological mechanisms during the 20th century. They were created to find better, safer ways to relieve pain. Although all offer pain relief, all are addiction risks.

  1. Meperidine

Also known as pethidine and Demerol, meperidine is another opioid pain medication. It was created in 1939 in Germany and was the first fully synthetic opioid developed. It was the most commonly prescribed opioid for much of the 20th century. It was thought that meperidine was safer to use than morphine and that it carried a lower risk of addiction. It is still the most widely used pain reliever during labor and delivery. Side Effects of Meperidine: Like other opioids, the list of adverse side effects is long and includes: agitation, cardiac arrest, coma, constipation, dizziness, dry mouth, dysphoria, euphoria, nausea, physical dependence, psychological dependence, respiratory arrest, sedation, seizures, sweating and weakness. This medication can also interact with some common drugs like antidepressants. According to the Patient Safety Authority of Pennsylvania, “Clinically, the predominant side effect that differentiates meperidine from the other opioids is its neurotoxicity. Meperidine has been implicated in “Serotonin Syndrome.” Serotonin Syndrome (SS) is thought to be caused by elevated levels of serotonin (5-HT) in the CNS. Most cases of SS reported in the literature were associated with patients taking two or more medications that increase CNS serotonin levels by different mechanisms such as monoamine oxidase inhibitors (MAOI) used in conjunction with meperidine, tricyclic antidepressants, or Selective Serotonin Reuptake Inhibitor (SSRI) antidepressants. Examples of commonly used SSRI antidepressants, also known as 5-HT-selective reuptake inhibitors, include fluoxetine (PROZAC), paroxetine (PAXIL), sertraline (ZOLOFT), and citalopram (CELEXA)”

  1. Fentanyl

This potent synthetic opioid is 50 to 100 times stronger than morphine. It was created in the 1960s following the creation of meperidine. In the mid 90’s, it was used in many forms: patch, lollipop, dissolving tablets and an oral spray.  It is also widely used recreationally and is responsible for many overdose deaths. Side Effects of Fentanyl: The most common side effects of fentanyl include nausea, diarrhea, constipation, dry mouth, weakness, sweating, fatigue, weight loss, anorexia, anxiety, depression, flu-like symptoms, and apnea. Accidental overdose of this drug is common, including children’s accidental exposure to skin patches. This drug is often used to cut heroin, and due to its potency, is a high risk for accidental overdose.

  1. Methadone

Methadone is used as a maintenance therapy to assist in detoxification of people struggling with opioid dependence. The effects last about six hours, and it is often taken by mouth. It was developed in Germany during the 1930s. According to NARCONON, “Because of this lack of euphoria, a person new to abusing methadone may take more and more of it in an attempt to achieve the rush. They may manage to overdose by doing so, which can result in death.” Side Effects of Methadone: NARCONON states, “The other manifestation of a person using methadone is that when withdrawal symptoms begin to kick in, they will generally become obsessed with getting more of the drug. A person starting withdrawal may manifest yawning, muscle aches, restlessness and dilated pupils. They may sweat and their eyes may tear. They probably will be unable to sleep. If withdrawal proceeds, they may have vomiting, diarrhea and stomach cramps. If a person with these symptoms is insistent on getting some money and leaving the house or office, you may be looking at abuse of methadone or another opiate.” Needless to say, both opiates and opioids are extremely risky to use recreationally. Even under the supervision of a doctor, these narcotic painkillers have the potential to create lifelong addictions. There are opioid recovery treatment and detox options for opioid addicts. The first step in sobriety is realizing there is a problem.