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Understanding Opioid (Narcotic) Pain Medications

Medically reviewed on Feb 23, 2016 by L. Anderson, PharmD

Narcotics, also called opioids, are a necessary and important part of medical care. Painkillers -- narcotic analgesics -- contain some type of opioid medication to ease the discomfort from a sprained ankle, after wisdom tooth extraction, or after major surgery. Opioids are also used as a cough suppressant, to treat diarrhea, and to help combat narcotic addiction itself. However, the use of prescription opioids for pain is now a highly controversial topic in the U.S. due to a growing epidemic of prescription narcotic addiction, overdose, and death.

You’ve heard of their names: Oxycontin , hydrocodone, Lortab, tramadol , Vicodin, Tylenol with Codeine, Ultram ER. We’ve all been prescribed opioid prescription painkillers from time-to-time, and the choices are many.

But what are opioids and should we be concerned about taking them for a legitimately painful condition? Here’s some detailed history and facts about prescription narcotics to help you better understand painkillers, their prescribing information, and the current concerns about addiction.

A Brief History of Narcotics1

Ancient Times

Narcotics, also known as opioids, date back to 3400 B.C. Narcotics from ancient times all had a common source: the red opium poppy. The earliest records of the opium poppy being cultivated was in Mesopotamia by the Sumerians. The Sumerians referred to opium as the “joy plant” and passed it on to the Egyptians. Around 400 B.C. the first medical references to opium came from Hippocrates, also known as the Father of Medicine.

The Middle Ages

Oddly, opium disappeared from the European records up until around 1500, so documentation is sparse. However, in the early 1500’s Paracelsus, the first toxicologist, created an opium pill also using citrus juice and gold. Paracelsus also made a specific tincture (alcoholic extract) of opium called “laudanum”, from the latin meaning “to praise”. Laudanum contains roughly 10 percent powdered opium by weight, equivalent to 1 percent morphine. Laudanum can still be ordered via prescription in the U.S. today, although it is rare. Most orders are for semi-synthetically derived opium derivatives such as oxycodone, hydrocodone, morphine or codeine.

The 19th and 20th Century

In the 1800’s opium was recognized as a standard painkiller when morphine was isolated from the poppy. German chemist Friedrich Wilhelm Adam Serturner dubbed the isolate “morphine” after the Greek god of dreams, Morpheus. Opiuim, morphine and heroin addiction had become a major problem by the early 1900’s and during the civil war. Congress starting imposing regulations to restrict opium.

  • The Opium Exclusion Act of 1909: Barred importation of opium for purposes of smoking
  • The Harrison Narcotics Tax Act of 1914: Required physician and pharmacist registration for distribution of opiates
  • The Heroin Act of 1924: Heroin importation, manufacture and possession was outlawed in the U.S.

Bayer stopped the production of heroin but in 1916 oxycodone was developed in hopes it would be less addictive. In 1938, the Food, Drug and Cosmetic Act was passed that required all medications to be proven as safe by the FDA; however, older opioid-derived drugs such as morphine, codeine, and oxycodone were “grandfathered” meaning they were automatically allowed without further review. Fast-forward to the 1950’s, 1960’s, and 1970’s and that’s where the more familiar opioids like Percodan (oxycodone/aspirin) start to gain hold in the U.S. market. Since this time, the illegal abuse of semi-synthetic and synthetic narcotics has been a major problem in the U.S..

With the passage of the Controlled Substances Act (CSA) in 1970, greater regulation and scheduling of drugs based on abuse potential occurred. Within the CSA there are five schedules (I-V) that are used to classify drugs based upon their potential for abuse, valid medical applications, and public safety. The schedules range from I to V, with schedule I being the highest for potential abuse and with no current medical use. Heroin and marijuana fall into schedule 1; oxycodone, hydrocodone and morphine are in schedule 2.

The Drug Enforcement Agency was created in 1973, and President Nixon declared ‘The War on Drugs’ noting the high incidence of heroin addiction in the U.S.

The 21st Century

In the first decade of 2000, a new emphasis on medical control of pain was emphasized by healthcare policy makers, leading to an explosion in opioid prescribing. Brands such as:

were overprescribed, leading to millions of addicted patients and hundreds of thousands of emergency department visits due to painkillers. The pharmaceutical industry began research into development of abuse-deterrent formulations of opioid medications, many of which are now available on the U.S. market.2,3 However, none of these forms prevent oral abuse by taking an excessive number of tablets. The true effect of abuse-deterrent opioids on the reduction of narcotic overdose and death is not yet known. In fact, it will probably take a multi-pronged approach to defeat the epidemic of narcotic abuse in this country.

What Is a Narcotic Medication?

It’s important to define narcotic in a medical sense. The word “narcotic” often denotes a negative connotation associated with illegal drugs and addiction. While this can be true, “narcotic” is also a standard term used in medicine. A narcotic drug, also called a narcotic analgesic or opioid, is a medication prescribed by a doctor to relieve moderate to severe pain, either acute (short-term) or chronic (longer-term or continuous) pain. Narcotic analgesics differ in their ingredients, strengths, dosage forms, and cost. Many are available as oral tablets, capsules, or liquids, while some come as an injection, and others are provided as a patch to provide extended-release control for severe pain.

How Do Narcotics Work?

Overall, narcotic painkillers work by reducing nerve excitability that leads to the sensation of pain. Narcotics bind to special receptors in the brain (central nervous system) and in other areas of the body (peripheral nervous system, like the gastrointestinal tract) called opioid receptors. There are four types of opioid receptors.

  • Mu
  • Delta
  • Kappa
  • Opioid Receptor Like-1 (ORL1)

These receptors either aid with the opening of potassium channels (causing hyperpolarization) or block calcium channel openings, and block the release of excitatory neurotransmitters like substance P that are involved with pain.

Sometimes a painkiller drug may be referred to as a “narcotic-like” medicine, but any true narcotic medication will have action at one of the three opioid receptors. For example, tramadol is often referred to as a “narcotic-like” medication, but this is a misnomer, as it has centrally-acting analgesic action at the opioid mu receptors, blocking pain pathways. Tramadol is also thought to act via weak reuptake inhibition of norepinephrine and serotonin, and this may contribute to its pain effects. In addition, tramadol pain relief is partially blocked by the opiate antagonist naloxone in animal studies.4,5

What Kind of Pain Does a Narcotic Treat?

There are literally hundreds of pain conditions where narcotic analgesics could be used to lessen discomfort. Opioids for acute pain should only be used short-term to help prevent dependence and addiction. Once the severe acute pain subsides other non-narcotic medications such as acetaminophen or ibuprofen may be suitable. Longer-term options, combined with alternative treatments such as exercise, physical therapy, TENS therapy, meditation, and or neuropathic drugs for pain may be helpful. Often, if pain is worse at night and interferes with sleep, an opioid pain medication can be used only at bedtime, using other non-narcotic methods during the daytime. The physician and patient should develop a plan for pain control early in the treatment course.

A pain treatment plan should also be initiated early in the course of chronic (long-term) pain management. Chronic pain can also be treated with narcotics, but the patient should be followed closely by their physician or a pain specialist, and additional and alternative treatments, such as those mentioned above, combined with non-narcotic analgesics should be pursued. Many of the extended-release formulations of opioid pain medications are only to be used in opioid “tolerant” patients (meaning they have already been using other opioids) and for chronic pain that requires 24-hour, around-the-clock pain management.

Opioid medicines such as methadone (Dolophine, Methadose), buprenorphine, buprenorphine combined with naloxone (Suboxone)  and naltrexone (Depade, ReVia) are also used in the treatment of opioid dependence, either from prescription painkillers or illicit narcotics such as heroin.

Is My Drug a Narcotic?

Below is a list of narcotic drugs (opioid analgesics) available on the U.S. market. The generic names are listed first, with brand name products in parentheses. Follow the link for specific prescription information about dosing, side effects, and drug interactions.

List of Prescription Narcotic Drugs (Single Agents)

List of Prescription Narcotic Drugs (Combination Agents)

Narcotic analgesic combinations are products containing a narcotic analgesic with another class of analgesic, such as acetaminophen, ibuprofen or aspirin. They are used to treat moderate to severe pain. Propoxyphene, contained in products such as Darvocet-N 100 (propoxyphene/acetaminophen), was taken off the U.S. market in 2010 due to safety and effectiveness concerns.

Follow the links below for specific information about dosing, side effects, and drug interactions for each drug. The generic drug names are listed first, with brand name products in parentheses.

*Buprenorphine/naloxone is a combination medicine used to treat narcotic (opiate) addiction. Buprenorphine/naloxone is not for use as a pain medication.

Common Uses for Narcotic Analgesics

Common Side Effects of Narcotics

Morphine and its derivatives are classified as narcotics analgesics. Narcotics like morphine may cause many different types of side effects, but all cause drowsiness, sedation, and can lead to respiratory depression (difficulty breathing), especially when combined with alcohol or other CNS depressant drugs (which can be fatal).

  • Drowsiness and impaired judgment; do not drink alcohol, drive, or operate heavy machinery
  • Pruritis (itching)
  • Opioid-induced constipation
  • Nausea or vomiting
  • Withdrawal symptoms upon discontinuation; your doctor may suggest to slowly stop your narcotic to lessen withdrawal side effects
  • Tolerance to the pain relief effect can occur over time (meaning you may need a higher dose to get an equal amount of pain control)
  • Dizziness, confusion; may be worse in the elderly

Learn More: Search for a complete list of your opioid side effects

Narcotics for Pain: The Current Controversy

Recent statistics from the National Institute of Drug Abuse show that 1 out of 15 people who take prescription painkillers for recreational use will try heroin within 10 years. And this problem is growing - in 2004, 1.4 million people abused or were dependent on pain medications and 5 percent used heroin. By 2010, 1.9 million people abused or were dependent on pain medications and 14 percent used heroin. Heroin users are 3 times more likely to be addicted than users of prescription painkillers (54% vs. 14%). Relative to the high cost of prescription painkillers on the street, heroin is cheap - and this contributes to its increasing popularity among addicts.

The crackdown on prescription narcotics, and the rescheduling of hydrocodone from CIII to the more restrictive CII, has led many to believe rescheduling may cause a spike in heroin use due to lower availability of prescription painkillers. In 2014, there were more than 914,000 reported users of heroin, an increase of 145 percent since 2007. In addition, there were over 10,500 heroin overdose deaths in 2014.

However, in a 2016 letter in the New England Journal of Medicine6, experts state that the heroin epidemic is not the direct result of the crackdown on prescription painkillers like OxyContin and Vicodin. In fact, the authors state that heroin use among people who use prescription opioids for nonmedical reasons is rare, and the transition to heroin use appears to occur at a low rate. The timing of rescheduling and policy shifts do not coincide with the spikes in heroin use. Instead, increased access to heroin, a reduced price, and higher purity of heroin seem to be the major factors leading to increases in rates of heroin use.7

Learn More: Did the Painkiller Crackdown Cause the Heroin Epidemic?

The FDA Response to Narcotic Addiction

The FDA has developed educational programs for prescribers on the dangers of opioids and overprescribing, and this continues today in 2016.

In September 2013 the FDA instituted safety labeling changes for all extended-release and long-acting prescription opioids. The FDA has also added prescriber education on both management of pain and substance abuse for prescription narcotics through a risk evaluation and mitigation strategy (REMS) plan. In addition, FDA produced a 2015 Guidance for Industry on evaluation and labeling of abuse-deterrent opioids. In February 2016, FDA’s Deputy Commissioner Dr. Robert Califf announced a sweeping review of the agency’s approach to opioid medications to evaluate ways to reverse the epidemic of narcotic abuse while still ensuring access to much-needed pain relief for those who need it.

Learn More: What Are Abuse-Deterrent Opioids?

Rescheduling of Narcotics to Ease Misuse and Diversion

Rescheduling of Tramadol

Tramadol, a common pain medication, has been linked with drug abuse and misuse, dependence, and even fatal overdoses. To address these concerns, in 2014 the DEA placed all forms of tramadol into schedule IV of the Controlled Substances Act (CSA).

Previously, tramadol was thought to be a lower risk drug for abuse and overdose and was a controlled substance in only a few U.S. states. Tramadol prescriptions may now only be refilled up to 5 times in a 6 month period after the date the prescription was first written. After 5 refills or 6 months, whichever occurs first, a new prescription is required from the physician.

Even though tramadol may have other pain mechanisms in addition to a narcotic effect, people with a history of drug abuse may be at a greater risk of addiction. Tramadol is related to other opioids like codeine and morphine and can lead to psychological and physical dependence, drug-seeking behavior, addiction, and withdrawal symptoms. Withdrawal symptoms may occur if tramadol is abruptly stopped. Dose reduction of long-term tramadol use should be directed by a doctor.

Rescheduling of Hydrocodone

In a 2013 survey, it was reported that schedule III hydrocodone and schedule II oxycodone were the most popular drugs among Americans who abuse prescription painkillers. These drugs, used as pain relievers or cough suppressants, contain either hydrocodone or oxycodone and some other substance, like acetaminophen, ibuprofen, or a cough/cold product. Well-known brand names include Vicodin, Lortab or Tussionex.

In October 2014, hydrocodone was rescheduled from schedule III to schedule II of the Controlled Substances Act. Patients now need a new prescription each time they renew their prescription for any hydrocodone product; refills are no longer allowed. The DEA put this rule into place to help curb abuse, diversion, and encourage patients and healthcare providers to consider other, more safe ways to combat pain.

Can I Become Addicted to a Prescription Narcotic Painkiller?

If and how quickly you become addicted depends on many factors. Addiction is a multi-faceted condition that involves:

  • Personality and behaviors
  • Brain chemistry
  • Age
  • Environmental and family surroundings
  • Types of drug abuse
  • Past personal and family history of drug abuse

While one individual may use a drug once or many times and not become addicted, another person may overdose with the first use, or become addicted quickly. Each person varies in their susceptibility to drug addiction.

Any opioid-based painkiller can lead to addiction. Narcotics often involved in prescription painkiller addiction and overdose include:

  • Morphine
  • Oxymorphone (Opana ER)
  • Oxycodone (Oxycontin, Oxecta)
  • Hydrocodone (Zohydro ER)
  • Codeine
  • Methadone
  • Fentanyl

Also concerning is that many of these medications (such as Lorcet, Tylenol with Codeine, Vicodin) may also contain acetaminophen (Tylenol) which in itself can be toxic to the liver at excessive doses. Codeine is also found in headache combinations such as Fioricet with Codeine.

  • Always store prescription narcotics safely in your home away from children, pets and teenagers. If needed, lock them up securely.
  • Most adults should not exceed 4,000 milligrams (4 grams) of acetaminophen  over a 24-hour period.
  • Do not exceed the recommended 24 hour dose of acetaminophen (4 grams) from all products (prescription and over-the-counter).

What Is Naloxone (Narcan)?

A narcotic reversal agent called naloxone (Narcan, Evzio) can be a life-saving drug for patients who overdose on narcotics.

All narcotic painkillers will produce various levels of central nervous system (CNS) depression like drowsiness and sedation. One of the most serious concerns with excessive opioid use is slowed breathing (respiratory depression). When narcotics are combined with other CNS depressants, like alcohol or benzodiazepines, severe, possibly fatal respiratory depression can occur. If you believe someone has overdosed on narcotics, call 911 immediately. If okayed by your doctor, Evzio or Narcan Nasal can be kept by family members or caregivers for administration in emergencies. Discuss this with your healthcare provider, if needed.

Learn More: FDA Approves Nasal Spray to Reverse Narcotic Painkiller Overdose

Popular Culture and Drug Use

The use of illicit and prescription drugs is pervasive throughout pop culture. From music stars, to TV personalities, college and professional sports, to prime time television and blockbuster cinema -- drug and alcohol use is frequently highlighted in the news. The youth of America, and indeed, the world, are the recipients of these disturbing forms of media.

Television shows such as Jersey Shore, Breaking Bad, House, Narcos, and Weeds promote, highlight or glamorize the use of illicit or prescription drugs, marijuana and alcohol as the main topic. Sports figures, such as cyclist Lance Armstrong have been the center of controversial substance abuse investigations. Sean Penn conducted an interview with notorious Mexican drug lord El Chapo leading to a publication in Rolling Stone magazine. Musical pop stars are frequently involved in drug abuse scandals.

According to the Substance Abuse and Mental Health Services Administration (SAMHSA) an estimated 1.3 million U.S. adolescents ages 12 to 17 had a substance use disorder in 2014 (5 percent of all adolescents). Impressionable teens may find these messages about drug use and misuse confusing or alluring. Presenting drug use in popular culture and mainstream media may result in substance abuse imitation instead of rejection by today’s youth.8,9

Drug Testing for Narcotics

Prescription and illicit opioids are a regular component of workplace drug testing in the U.S. Urine drug screening may also take place in the clinic during management of pain therapy.

Physicians who manage pain may engage some patients in a treatment plan that includes urine drug screening to monitor their opiate management. These laboratory results can provide the doctor with objective data on which to make therapeutic and diagnostic decisions, identify misuse or diversion, and assess compliance. Doctors should describe the screening and frequency at the initial evaluation. Patients must be willing to participate in the screening to help manage their pain.

Which drug test is used for workplace drug screening is dependent upon the private employer, federal requirements, or other workplace guidelines that may be in place. Patients should inform the lab of the prescription and OTC medications they currently take.

Employers may use a standard five-panel test of commonly abused drugs such as marijuana (THC), cocaine, PCP, opiates (e.g., codeine, morphine, methadone) and amphetamines like methamphetamine. Employers may also elect a multi-drug panel test that also includes other prescription drugs, such as hydrocodone, oxycodone, hydromorphone, benzodiazepines, or barbiturates. They may also choose to screen for alcohol in the sample. Other more recent drugs of abuse or designer drugs, such as MDMA (Ecstasy) may be included.

Drug Detection Time in Urine10

Drug Approximate Retention Time
Amphetamines 48 hours
Barbiturates Short acting, such as secobarbital: 24 hours
Long acting, such as phenobarbital: up to 3 weeks
Benzodiazepines Roughly 3 days if short-term dose
Up to 6 weeks after 12 months or longer dosage
Cocaine

Metabolite
2 to 4 days
Ethanol (alcohol) 2 to 4 hours
Methadone Up to 3 days
Opiates Up to 3 days
Cannabinoids Moderate smoker (3-4 times/week): 5 to 6 days
Heavy smoker (smoking daily): 10 days
Retention time for chronic smokers may be 20 to 28 days
Phencyclidine Roughly 8 days
Chronic use: up to 30 days

Note: All times are approximate and may vary based on patient-specific drug metabolism, drug half-life, patient’s medical conditions, other drug treatments, and frequency of drug ingestion.

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See Also:

Recommended for you

Sources

  1. The Atlantic. A Brief History of Opioids: Pain, Opioids, and Medicinal Use. Accessed February 10, 2016 at http://www.theatlantic.com/sponsored/purdue-health/a-brief-history-of-opioids/184/
  2. Fudin J. Abuse-deterrent Opioid Formulations. Purpose, Practicality, and Paradigms. Pharmacy Times. January 27, 2016. Accessed February 12, 2015 at http://www.pharmacytimes.com/contributor/jeffrey-fudin/2015/01/abuse-deterrent-opioid-formulations-purpose-practicality-and-paradigms
  3. Moorman-Li R, Motycka CA, Inge LD, Congdon JM, Hobson S, Pokropski B. A Review of Abuse-Deterrent Opioids For Chronic Nonmalignant Pain. Pharmacy and Therapeutics. 2012;37(7):412-418. Accessed February 12, 2016 at http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3411218/
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  6. Compton WM, Jones CM, Baldwin GT. Relationship between Nonmedical Prescription-Opioid Use and Heroin Use. N Engl J Med 2016; 374:154-163. Accessed February 15, 2016 at http://www.nejm.org/doi/full/10.1056/NEJMra1508490
  7. Did the Painkilller Crackdown Cause Heroin Epidemic? January 13, 2016. Drugs.com. Accessed February 12, 2016 at https://www.drugs.com/news/did-painkiller-crackdown-cause-heroin-epidemic-59725.html
  8. Stoddart T. Sobernation. Drugs in Pop Culture. March 8, 2013. Accessed February 16, 2016 at https://www.sobernation.com/drugs-in-pop-culture/
  9. Substance Abuse and Mental Health Services Administration (SAMHSA). Age and Gender-based Population. Last updated 10/30/2015. Accessed February 18, 2016 at  http://www.samhsa.gov/specific-populations/age-gender-based
  10. Helt H, Gourlay D. Philosophy of Urine Drug Testing in Pain Management. Prescribe Responsibly. Updated July 2015. Accessed February 12, 2016 at http://www.prescriberesponsibly.com/articles/urine-drug-testing#tableThree
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