Although many people use the word opiates to indicate any drug that bind to receptors in the body used by endorphins, opiates actually refers to drugs derived from the opium plant.  Examples of opiates are morphine and codeine.  Heroin is made from the opium plant with the addition of a chemical.

An opioid is a synthetic chemical substance made by the drug companies  that has similar action in the body as the opiates.  Examples of opioids are: methadone, Percodan/Percocet®, Lorcet®, Lortab®, Demerol®, Vicoden®, OxyContin®, Suboxone®, Subustex® and Dilaudid®.

OPIATES AND OPIOIDS IN USE TODAY AND THEIR HISTORY

Opium

The opium poppy is the source of opium.  Referred to by the Sumerians in 3400 BC as “Hul Gil” or joy plant, opium has long been used both to provide feelings of euphoria and for pain relief. The opium poppy is grown in dry, warm climates, mainly in the Middle East and East Asian countries.  The poppy produces a pod that contains a sticky sap that is opium in its raw form. Highly addictive, the smoking of opium was eventually banned but it remained in certain medicines into the early 20th Century in the United States.

Morphine

In the early 1800’s, it was discovered that the source of the pain relieving and euphoria producing effects of opium were morphine (99%) and codeine (1%).  It is believed that Morpheus, the god of dreams in Greek mythology, was the source of the name “morphine”.

Initially given to opium addicts and alcoholics to “cure” them, it was soon discovered that morphine was even more addictive than opium or alcohol.  While used for pain relief, with the development of the hypodermic needle in 1853, the use of morphine for pain relief became a standard medical practice.  As the only really effective pain reliever known at the time, morphine was used extensively in the American Civil War. Unfortunately, but predictably, many of the wounded soldiers became addicted.

Morphine is still carried by soldiers in the field and is still widely used for pain relief in many parts of the world.  The half life of morphine is 4-5 hours. (Half life is the amount of time it takes for ½ of a drug to be removed from the body.)

Codeine

Codeine is not as strong or as addictive as morphine. Many over the counter products contain small amounts of codeine. To be obtained without a prescription in the United States, the product must contain a much larger amount of another non-addictive drug—like acetaminophen (Tylenol®), aspirin and ibuprofen. The assumption is that a person would likely have a toxic response to the other ingredients before they could consume enough codeine to become addicted.

Prescription codeine medications contain a much higher amount of codeine but also contain large amounts of non-addictive drugs like Tylenol, ibuprofen or aspirin.
Codeine is also one of the principal ingredients in hydrocodone which is marketed as Vicodin®, Lorcet®, Lortab® and Norco®. The half life of codeine is between 3-4 hours.

Heroin

Heroin is processed from morphine and usually appears as a white or brown powder. Street names for heroin include “smack,” “H,” “skag,” and “junk.” Other names may refer to types of heroin produced in a specific geographical area, such as “Mexican black tar.”

The first recorded time that heroin was produced from morphine was in a lab in Britain in 1874. Not seeing a way to effectively use the drug, it was largely forgotten until 1898. At that time it was developed by the Bayer pharmaceutical company in Germany and widely promoted as a non-addictive pain killer and cough medicine for children. Bayer also marketed heroin as a cure for morphine addiction.  Apparently, Bayer forgot to tell people that when the liver metabolized the heroin the active ingredient remaining was morphine.

In 1914, the Harrison Narcotics Tax Act was passed to control the sale and distribution of heroin. In an early variation of the methadone treatment policy, heroin was allowed to be used for medical purposes. In a way similar to the approach some “pain management” doctors take today, many doctors prescribed heroin indiscriminately and this allowed many addicts to continue to use heroin. It was not until 1924, that the sale, importation or manufacture of heroin was banned in the United States. It is now a Schedule I substance, and is thus illegal for any medicinal use.

Depending on their metabolism and DNA, generally soon after a person injects heroin they experience a sudden feeling of euphoria.  Because the heroin is depressing the central nervous system, many people then become drowsy and their mental processes are slowed.  Longer term heroin users often have collapsed veins and frequently develop infections affecting the heart and liver.

As with all illegal drugs that are obtained from questionable sources, heroin is normally “cut” or diluted with other substances. Some of these additives can be very toxic and can cause serious complications or even death. Other additives can create clots in the blood vessels which can lead to serious infections or even death.
Because of the competition from oxycodone and hydrocodone products, pharmaceutical grade heroin, the the purity of the heroin purchased on the street has increased from 10%-20% in the 1970’s to 80%-90% today.

The Drug Abuse Warning Network* reports that eight percent of drug-related emergency department (ED) visits in the third and fourth quarters of 2003 involved heroin abuse. Unspecified opiates—which could include heroin—were involved in an additional 4 percent of drug-related visits.

Methadone

Methadone, an opioid, was first produced in 1939 at the pharmaceutical laboratories of I.G. Farben in Germany. Named Amidon, while there is evidence that some testing was done of the drug, there is no evidence that it was widely used by the Germans in World War II.

After the war, the German patents on Amidon and other drugs were voided and Amidon was tested and released in the United States by Eli Lilly in 1947 as Dolophine. Dolophine was derived from the Latin word dolor (pain) and finis (end).  Later Dolophine came to be known as methadone.  Originally marketed as a pain reliever, it was not until the 1960’s when the number of heroin addicts was accelerating and the negative impact on society became widely known, did the idea of converting the heroin user to a methadone user become accepted as a treatment procedure.

The logic was that even though methadone was in many cases more addictive than heroin, because of its longer half life, between 12 hours and 96 hours, a person could normally be given one dose of methadone and this would last until the next day.  In the case of heroin, the much shorter half life of 4-5 hours, meant that the heroin user would have to shoot up more frequently or go into withdrawal.

Since the ability to dispense methadone is limited to a relatively small group of providers, it has been considered better to allow addicted heroin users to obtain legal methadone because there is less criminality and disease.  In addition, since the user is not forced to seek another dose until the next day, it can allow someone to hold a job and lead a more regular life. (Obviously, this is not a solution that we support because the real solution is to detox these users and get them into an effective rehab program.)

Oxycodone

Oxycodone is made from a compound known as thebaine, which is found in opium. First developed in 1916 in Germany, it was sold as  Eukodal. It was first introduced to the US market in May 1939.  Chemically it is very similar to codeine but is more than 50% more powerful than hydrocodone.  The half life is 4.5 hours for the extended release tablets compared to 3.2 hours for the standard oxycodone tablets.

In the United States, oxycodone is a Schedule II controlled substance both as a single agent and in combination with products containing Tylenol, ibuprofen or aspirin.  Percocet® tablets (oxycodone with Tylenol),  Percodan® tablets (oxycodone and aspirin) and Combunox® (oxycodone and ibuprofen) are routinely prescribed for pain control. OxyContin® (the name is actually short for Oxycodone Continuous release) is commonly marketed for control of pain.

Hydrocodone

Hydrocodone is derived from codeine and thebaine.  Approved for use in the United States in 1951, it is now combined with Tylenol, aspirin and ibuprofen. The concentration of hydrocodone in these medications is normally is not more than one or two percent of the total drug. Vicodin ® and Lortab® (hydrocodone and Tylenol), Lorcet® (hydrocodone and aspirin) and Vicoprofen® (hydrocodone and ibuprofen.)  The half life of these drugs is normally 3-4 hours.
In the body it acts like heroin and is referred to by many doctors as synthetic heroin.

The FDA has received enormous pressure to schedule hydrocodone products as Schedule II drugs and not Schedule III drugs.  The present scheduling allows easy access to this very addictive drug that is often the drug first used that leads to dependence and addiction.

Buprenorphine®, Suboxone®, Subustex®

Suboxone® and Subustex® were approved by the Food and Drug Administration in 2002.  Only doctors approved by the Substance Abuse and Mental Health Services Administration, a department in the United States Department of Health and Human Services, are allowed to dispense Suboxone® and Subustex®.

Suboxone® contains buprenorphine, a partial agonist, and naloxone, an antagonist. The proportion is four parts of buprenorphine and one part naloxone. Suboxone® comes in two dosage forms: 2 mg buprenorphine/0.5 mg naloxone and 8 mg buprenorphine/2 mg naloxone. The Suboxone® drug label is available on the FDA website.

If Buprenorphine is swallowed it has poor oral bioavailability (The ability of a drug to enter the body and be metabolized.).  If taken sublingual, under the tongue, and allowed to dissolve then the bioavailability is much higher.  Normally a person will receive approximately 40-60% of the buprenorphine available when taken sublingual and allowed to dissolve.

If administered sublingual, Naloxone®, the second component of Suboxone®, has low bioavailability and the person will receive only about 10% of the drug. On the other hand, if Suboxone® is crushed and injected into the bloodstream, the effect of the buprenorphine will only be about twice as high as if it were taken sublingual.  However, the effect of the naloxone will be increased by 15 times and will dominate.  The naloxone will bind to the mu receptors and block the buprenorphine from activating the receptors and this will precipitate withdrawal.

Subustex® contains just buprenorphine.  It is taken sublingually like Suboxone®. The half-life of buprenorphine is 24–60 hours.