Opiates

Physicians around the world prescribe opiates so frequently that it might seem these drugs are completely safe, but anyone who uses opiates faces possible risks including side effects, dependence, addiction and overdose.

An opiate is any drug derived from the opium poppy plant, Papaver somniferum. This plant contains natural opiates, the most useful being morphine, codeine and thebaine. Morphine and codeine are strong analgesics, while the natural form of thebaine is less powerful.

Opiates are among the most commonly prescribed drugs in the world, effective for reducing even the most severe pain for seriously ill patients. Opiates also calms anxiety, cause relaxation and induce a pleasant sense of euphoria. These additional actions make opiates a target for recreational abuse and non-medical use to treat an illness or injury for which it had not been prescribed.

The U.S. Drug Enforcement Agency, or DEA, categorizes drugs according to their medical benefit and potential abuse. The DEA then classifies these drugs according to their relative risk, with a schedule I narcotic posing the most risk and a schedule V representing the least risk.

To reduce the risk for abuse and non-medical use, opiate drugs are available only with a doctor’s prescription.

Recommended Use

Take opiates only as directed by a physician. Do not take stronger doses or use more often than prescribed. The consumer should discontinue opiate treatment when he longer needs the drug to control pain or when a doctor suggests he stop using them. High doses and long-term opiate use increases the risk for side effects, dependence, addiction and overdose.

A consumer who use opiates continuously for more than a few weeks may suffer withdrawal symptoms if he stops using these drugs abruptly. He may also develop an addiction and begin to crave opiates whenever he is not using them.

Using opiates for more than a few days, even at recommended doses, may increase the consumer’s tolerance to this type of drug. Tolerance means the body is less sensitive to the effects of opiates, so the individual must take increasingly stronger doses more frequently to achieve the same analgesic or euphoric effect. Someone with low tolerance is more sensitive to the effects of opiates and, as such, may be at increased risks for side effects or toxic overdose.

Opiate Side Effects

Any medication, including opiate drugs, may cause side effects even when used as directed. The most commonly reported side effects are not serious and disappear after continued use at therapeutic doses. Rarely, adverse reactions are serious and require medical attention.

Opiates relieve pain, reduce anxiety and produce sedation and euphoria by acting directly on the nervous system - opiates change the way the brain perceives pain. As a result, many of the side effects associated with opiates affect the nervous system to cause excessive sleepiness, vision problems like pinpoint pupils and the emotional opposite of euphoria, dysphoria.

Opiates act on the respiratory center in the brain to reduce a nagging cough. Consequently, opiate use may cause serious breathing problems, including respiratory depression where the lungs do not function properly. Symptoms of respiratory depression included slow, shallow or irregular breathing along with a bluish tint around the victim’s eyes, mouth and fingertips.

Opiates also act on smooth muscle groups, like those found in the gastrointestinal tract, to curb diarrhea. As a result, opiates may cause constipation in consumers not suffering from loose stools.

Other side effects can include:

  • Dry mouth
  • Nausea
  • Vomiting
  • Upset stomach
  • Difficult breathing
  • Sedation

The Risk of Dependency, Withdrawal and Addiction

Anyone who uses opiates continuously for a long time may become physically dependent on these drugs; he may even become addicted to opiates. Related by drug use, opiate dependence and addiction are actually separate and independent medical conditions.

The body adapts to the presence of opiates. Over time, some of these adaptations become more permanent as the body learns to rely on a certain level of opiates to feel “normal.” When opiate levels fall drastically, the body struggles to regain chemical stability. Doctors refer to this as detoxification.

The individual feels this battle for detoxification and chemical stability through unpleasant, flu-like withdrawal symptoms. A doctor will diagnose someone as being dependent on opiates if the patient feels withdrawal symptoms when he stops taking opiates.

Symptoms of opiate withdrawal usually occur in two waves, with the first set beginning a few hours after the last dose. Symptoms last five or more days, the worst symptoms appearing on or about the fourth day.

Early symptoms of withdrawal include:

  • Agitation
  • Anxiety
  • Muscle aches
  • Increased tearing
  • Insomnia
  • Runny nose
  • Sweating
  • Yawning

Late symptoms of withdrawal include:

  • Abdominal cramping
  • Diarrhea
  • Dilated pupils
  • Goose bumps
  • Nausea
  • Vomiting

A physician will say someone is addicted to opiates when the patient feels cravings or exhibits drug-seeking behavior when he runs out of opiates. Drug-seeking behavior includes “doctor shopping,” presenting an altered or bogus prescription at a pharmacy, stealing from friends and family or buying opiates from drug dealers.

Relapse and Overdose

Opiate dependence and addiction are chronic medical conditions and, as such, are marked with cycles of relapse and remission. Without professional treatment to reduce withdrawal symptoms or rehabilitation that changes the behaviors associated with drug abuse, overcoming opiate dependence or addiction is a difficult road. Severely uncomfortable and prolonged withdrawal symptoms force even the most determined individuals back to opiate abuse, especially if the individual has not learned healthy lifestyle habits that reduce the risk for drug abuse.

Any amount of detoxification reduces the body’s tolerance to opiates, increasing the risk for toxic overdose. It is possible for someone to overdose on a smaller amount of opiates than he used to take before experiencing even moderate withdrawal symptoms.

Opiate dependence and addiction require the individual to consume large amounts of opiates, increasing his risk for side effects and overdose. Despite strict controls on its use, prescription drug overdose kills nearly 15,000 people in the United States every year.

Professional assistance can make a big difference in the lives of opiate-dependent individuals, addicts and their families. Many hospitals now offer detoxification services that include medicines to ease withdrawal symptoms and trained staff to monitor the patient’s condition. Programs such as rapid opiate detox are able to minimize, and in many cases, eliminate opiate withdrawal symptoms.

Opiates are an important part of therapy for patients struggling with painful and serious medical conditions. Consumers who have struggled with opiate dependence or addiction in the past should avoid using opiates to reduce pain, or ask for special assistance when it comes time to stop using these effective and useful drugs.

Opiate History

People throughout history have enjoyed the benefits of opiates for both medicinal and recreational purposes. These drugs have long been prized for their ability to control pain. Historically, these narcotic medications have also been used for the euphoria and sedation they can produce.

Opiates are derived from the opium poppy plant. No one is entirely sure when the first poppy plant was cultivated, but some say it occurred in Mesopotamia in 3400 BC. The problems and risks associated with the use of opiates go back nearly as long. There is some evidence in 16th Century manuscripts that people were well aware of problems including tolerance, the potential for abuse and addiction.

Opiate Timeline

  • Opium was used to make morphine in the early 1800s.
  • Codeine was synthesized a few years later. These are naturally occurring opiate alkaloids that are used to make many of today's prescription medications.
  • The Bayer Company of Germany first produced heroin from morphine in the late 1800s.
  • A few years later, heroin was introduced commercially because it was thought to have less abuse potential when compared to morphine. It didn't take long to realize that many people were becoming addicted.
  • Heroin was still legally available after 1914, but to a lesser extent because of The Harrison Narcotics Tax Act, a measure designed to control the sale and distribution of heroin and other opioids.
  • Heroin was legally available in the U.S. until 1924 when Congress made it illegal to sell, import or manufacture it.
  • The U.S. Controlled Substances Act was established in 1970. This established a schedule that classifies opiates based on medical use and abuse potential. For example, heroin is a Schedule I controlled substance, as it has no legal medical use. Oxycodone and Hydrocodone are Schedule II substances because they have medical use but a very high potential for abuse.

Current Trends In Opiate Use

Today, opiates are one of the most prescribed medications in the world. They are unmatched in both their ability to control pain and risks that may develop. Most doctors will weigh the benefits and risks of prescribing opiates and decide if another treatment protocol is necessary. Opiates are supposed to be prescribed in the lowest possible dosage. This can always be adjusted if need be.

Opiates are among the most abused drugs – legal or illegal – in the U.S. The key to safe opiate use is taking them as directed. Patients should not take it upon themselves to take more medication than what's prescribed. This could lead to problems that include dependence, addiction and overdose.

Many people benefit a great deal from opiate therapy and this can be accomplished safely. Any misuse or abuse is dangerous. People who become dependent upon this medication often need professional assistance to detox. This is because opiates create withdrawal symptoms that can be both painful and dangerous. The right detox or rehab program will safely and successfully address these issues.

Opiate Origin

No one is sure exactly when the opium poppy was first cultivated, but experts agree opium was used in ancient times for pain relief and to experience euphoria. Some say it was first cultivated in lower Mesopotamia in 3400 B.C. There is also evidence that people used it around 1500 BC as a remedy for excessive crying in children. Hard to believe, but true.

Manuscripts dating back to the 16th Century allude to issues such as opium drug abuse and tolerance in countries including Turkey, Egypt, England and Germany. Morphine was isolated from opium in the early 1800s and codeine a few years later. These naturally occurring opiate alkaloids can be potent and many of today's prescription medications are synthesized from them.

Hard to Believe But Heroin Was Once Legally Prescribed for Pain, Cough

Heroin, an opioid synthesized from morphine, was first produced in the late 1800s by The Bayer Company of Germany. It was thought to have less abuse potential than its predecessors. The drug was introduced commercially three years later as a morphine substitute and cough suppressant. It was soon discovered that heroin was a quicker acting form of morphine and people were becoming addicted to it.

The Harrison Narcotics Tax Act passed in 1914 to control the sale and distribution of heroin and other opioids. Heroin was allowed to be sold for medical purposes, but in 1924, the U.S. Congress stepped in and made it illegal to sell, import or manufacture heroin.

Opiate Politics

Opiates have been used historically for treatment of pain and other ailments. At one time, heroin was legally dispensed in this country. The controversy surrounding opiates has been around nearly as long. In fact, two wars were fought because of issues surrounding opium.

Opiates can be highly addicting and can lead to many social problems including crime and accidental deaths. Communities across the country are trying to deal with an escalation in addiction, abuse and diversion. The more that government and health officials try to contain these problems, the worse they seem to get.

Opiates Are Ranked Based On Their Medical Use And Potential For Abuse

Because of their potency and risks, opiates need to be controlled in some way. In the United States, opiates are considered a controlled substance based on their medical use and potential for abuse. Though tight controls have been put in place, the demand has continued to grow. And where there is demand, there is supply. Availability, both legally and on the black market, doesn’t seem to be slowing.

Opiates are derived from the opium poppy. They activate opiate receptors in the brain and body, blocking pain signals and stimulating the brain’s pleasure and reward center. Pharmaceutical opiates such as OxyContin have flooded the market in the last several years and are sometimes over prescribed when less potent opiates would work.

Opiate Dangers Addressed At Every Level Of Government, With Little Success

Federal, state and local officials have long tried to address the social, legal and health problems associated with opiates, both legal and illicit. Presidents have declared “wars” on the dangers of drugs and there have been public education campaigns designed to lessen opiate abuse and addiction. The world was taught to “Just Say No,” but that has proven more difficult as the profile of dangerous drugs has changed.

It used to be that people were taught to fear the kind of drugs that could only be found on the street - cocaine, marijuana and heroin. Prescription drugs are dispensed legally, so people tend to think they are generally safe. While most of these prescription medications can be taken safely, there are drawbacks.

Opiates can be highly addicting if misused or abused in any way. Doctors have been urged to always prescribe the lowest possible dose. And it’s incumbent upon patients to learn all they can about the medication they are taking and safe use.

Congress Intends to Tightly Control Opiates Through 1970 Legislation

The U.S. Controlled Substances Act was established in 1970, setting a schedule to which opiates were classified based on medical use and abuse potential. There are five classifications. For example, heroin is a Schedule I drug because it has no legal medical use and a very high abuse potential.

Schedule II drugs, including oxycodone, have a very high potential to be abused but are approved for medical use. Drugs under schedules III, IV and V are approved for medical use and have less potential for abuse. Schedule III drugs include some stimulants and depressants. Schedule IV drugs include some sedatives and non-narcotic analgesics. Schedule V drugs include some cough medicines or anti-diarrhea preparations.

Problems Can Arise For Some People Who Take Opiates and Opioids

Opiates and opioids have their place in the treatment of medical conditions and they can be taken safely by most people. Misuse or abuse of any kind can lead to serious problems and people may require professional opiate detox.

These highly potent drugs have wreaked havoc in many communities, which struggle to stem the cases of addiction and related crimes. Safe use of opiates and opioids is critical and risks can be minimized by following guidelines closely and arming yourself with information.

Opiate Controlled Substance

Opiate abuse and addiction rates have climbed to alarming rates in the United States despite the fact that these drugs are supposed to be tightly controlled. Opiates and their derivatives, opioids, are usually prescribed for treatment of pain. However, over the last several years, drugs including OxyContin have exploded on the black market, paving the way for abuse, crime, addiction and accidental death due to overdose. In addition, many communities are dealing with the resurgence of heroin, which is often cheaper and easier to obtain than other opiates.

The U.S. Controlled Substances Act was adopted in 1970 with the purpose of allowing the U.S. Drug Enforcement Administration to regulate pharmaceutical controlled substances. This allows the agency to try and "prevent, detect and investigate the diversion of legally manufactured controlled substances while, at the same time, ensuring that there are adequate supplies to meet the legitimate medical needs in the United States."

How The Controlled Substances Act Works

Opiates are narcotic medications that can be habit forming and should be used medically when the benefits outweigh the risks. Drugs such as codeine, oxycodone and hydrocodone are placed within a schedule that lists them according to established medical use and abuse potential.

Drugs that fall under the Schedule I category of the Controlled Substances Act are deemed to have no established medical use and a very high potential for abuse. Heroin, which is illegal, falls under this category. Schedule II drugs, including oxycodone, have a very high potential to be abused but are approved for medical use. Drugs under schedules III, IV and V are approved for medical use and have less potential for abuse.

Schedule III drugs include some stimulants and depressants. Schedule IV drugs include some sedatives and non-narcotic analgesics. Schedule V drugs include some cough medicines or anti-diarrhea preparations.

Opiate Diversion and Theft Affect Nearly Every Community

Opiates and opioids are often used recreationally or abused by people who want to experience the other effects that include sedation and euphoria. Misuse of any kind can be dangerous, but as more people fall prey to addiction, problems continue to escalate.

These drugs are susceptible to diversion and theft. Opiate-related crime has affected nearly every community and law enforcement officials are trying to figure out how to deal with it. Pharmacy and personal thefts are on the rise, and teens and other young people are increasingly stealing these medications from cabinets of friends and family members.

Opiate addiction can be treated. Options include opiate detox, opiate rehab, opiate replacement therapy and rapid opiate detox.

Opiate Receptors

It's important to understand how opiates work in the body to produce effects that include analgesia, sedation and euphoria. These receptors can be found in the brain, gastrointestinal tract and spinal cord. The receptors are activated once opiates reach the brain, producing effects and stimulating pleasure centers that signal reward.

Areas of the brain that are activated include the ventral tegmental area (VTA), cerebral cortex and nucleus accumbens. Heroin, morphine, codeine and other opiates and opioids stimulate receptors, resulting in feelings of reward. Naturally occurring opiates include codeine and morphine. Opioids are synthesized from naturally occurring opiates and include oxycodone and hydrocodone.

How Specific Opiate Receptors Work Within The Body

These drugs activate pleasure circuits through the release of dopamine, a neurotransmitter involved in the body's reward and pleasure centers. This is what causes some users to experience a "rush" or intense feelings of euphoria. These feelings are usually short lived and are replaced by feelings of calm and relaxation. Continued activation of the reward system and excessive release of dopamine can lead to opiate addiction.

Opiate receptor subgroups include delta, kappa, mu and Nociceptin. Each controls different functions of the brain. For example, opiates and endorphins block pain signals by binding to the mu receptor site. The delta receptor in the brain is involved in pain relief, antidepressant effects and physical dependence. Kappa receptors in the brain and spinal cord are involved with sedation, spinal analgesia and pupil constriction.

Opiate Use Can Become Problematic, Resulting In The Need For Detox

Opiates can be a beneficial part of a pain management program. People who use them may find unparalleled relief, especially if they suffer with chronic pain. There are certain drawbacks, however. First, these drugs can become habit forming. It's essential for patients to use opiates as directed. Any misuse or abuse can result in problems that include tolerance, inadequate pain relief, heightened sensitivity to pain, dependence, addiction and overdose.

Opiates are powerful and people who become dependent may need professional opiate detox or opiate rehab. This can help them through the opiate withdrawal period. Detoxing from opiates can be dangerous so patients are advised not to try and stop taking these drugs cold turkey. Gradual weaning with the supervision of a doctor may be possible, but it depends on factors specific to the individual.

Endorphins

Endorphins are a brain chemical known as neurotransmitters. Once they are released, they help to combat stress and pain. These endorphins can be found in the brain, throughout the nervous system and the pituitary gland.

Endorphins interact with opiate receptors to reduce the perception of pain. They act in a similar way to opiates such as morphine and codeine. In addition to working to fight pain, the secretion of endorphins can produce feelings of euphoria and are thought to enhance the immune system.

Endorphins, or endogenous opioid polypeptide compounds, are often released in response to trauma, pain, stress and danger. Vigorous exercise can also bring about the release of endorphins.

Many Chronic and Serious Pain Sufferers Are Treated With Opiates

Pain is a very real part of life for millions of people. Chronic pain sufferers live in near constant misery if they are unable to find relief. Endorphins that are released may be inadequate in treating serious pain or chronic pain. Opiates are narcotics that are among the most prized pain relievers out there. They are often prescribed to treat illnesses such as cancer and degenerative, painful conditions.

Opiates and the drugs derived from them, opioids, can be a very effective part of a pain management program. There are some serious drawbacks, however. Taking these medications long term can lead to habitual use, dependence, addiction and a heightened sensitivity to pain.

The Brain Can Become Used To Opiates, Leading to Possible Addiction

The other problem is that long-term opiate use can lead to a depletion of the body's natural endorphins in the nerve cells. People who abuse these drugs over a prolonged period of time may cause a change in the way nerve cells work in the brain. The cells can become accustomed to having the drugs present, and they begin to require the drugs in order to work normally. This leads to issues that include opiate tolerance and opiate addiction.

People who become addicted to opiates may feel like they are part of a never-ending cycle. It is possible to break this cycle, but it may be difficult to do without the appropriate help. Opiate withdrawal is difficult in terms of pain, strong cravings and other bothersome symptoms. It can be very dangerous to stop taking opiates cold turkey after prolonged use. Many people require treatment with professional opiate detox or opiate rehab.

Opiate Agonist

Methadone is an example of an opiate agonist, a drug that mimics effects of endorphins that naturally occur in the body. They produce an opiate-like effect by working on the opioid receptor sites.

Opiate agonists are synthetic, designed to stave off cravings and opiate withdrawal. They are not supposed to cause feelings of euphoria or a "high," though these drugs can become habit forming. Opiate agonists can be used in opiate replacement therapy to treat addiction to opiates including heroin and OxyContin.

Opiate Antagonists and Partial Opiate Agonists

To contrast, an opiate antagonist (naloxone, naltrexone) is a drug that replaces opiate agonists at the receptor sites. This drug prevents people from experiencing opiate effects of the agonist drug.

An example of a partial opiate agonist is buprenorphine. This drug is included in medications such as Suboxone and Subutex and helps to manage opiate withdrawal. The withdrawal associated with opiates can be grueling physically, mentally and emotionally. People may find it nearly impossible to go through withdrawal without professional assistance. Symptoms can include serious cravings, harsh flu-like symptoms, severe agitation, sleep problems and possible seizures. Death during opiate withdrawal has also been reported.

Opiate Replacement Therapy May Not Be The Answer For Everyone

People who try to withdrawal from opiates on their own may be fighting an uphill battle. Withdrawal can be overwhelming and the fear of this causes some to relapse over and over. Opiate replacement therapy with opiate agonists, or withdrawal management with partial opiate agonists may work for some people. These treatments tend to be more long term. Using opiates to treat opiate addiction is also risky because they can also lead to dependence.

Others may find that in-patient opiate treatment works better if detox is offered in a professional setting. This way, patients don't have to be on opiate replacement therapy long term. They may also find the support they need in a program that offers detox, counseling and other services.

Opiate Half Life

The term "opiate half life" refers to the amount of time it takes a person's body to break down and eliminate half of the initial dose. This is important information to know because some drugs stay in the system longer than others. This presents a risk because people may not still feel the effects of a certain medication but they may take something that interacts with it.

Let's take heroin as an example. It has a relatively short half life – just a few hours. Compare this to Suboxone, a semi-synthetic opiate used to treat opiate addiction. The half life of this drug can be measured in days – about 5 to 7.

Opiates Should Not Be Used With Some Other Substances

Opiates depress the central nervous system and tend to slow respiration. Taken in too high of a dose, drugs such as codeine, morphine and OxyContin can cause an opiate overdose.

These drugs can also be deadly if mixed with certain other substances that affect the central nervous system. These include other opiates, tranquilizers, alcohol, sedatives and some sleeping medications.

How To Find Out a Particular Opiate's Half Life

Information about a particular drug's half life should be included in the pamphlet that accompanies a prescription. It's important to know this information. If you have questions, speak to the doctor or pharmacist about it.

The number of hours it takes for the body to eliminate a dose of opiates can depend on other factors, including how often the medication is used and in what dosage. For this reason, the number of hours is usually given in a range.

What You Need to Know About Opiate Half Life

Many people think that drugs that have a shorter half life may be safer in some instances, but effects usually wear off rather quickly. This can cause a person to take more of the drug than what's recommended. Drugs that have a longer half life can also be dangerous. They may stay in the blood for a longer period of time without diminishing in strength.

The half life of an opiate usually coincides with the onset of withdrawal. This can be a very painful time for people because opiate withdrawal can bring symptoms including:

  • Vomiting
  • Strong cravings
  • Extreme agitation
  • Tremors
  • Nausea
  • Depression