#6 Opiate Explanation Summary

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Chapter 13

Opioids

Image sources (injection): Royalty-Free/CORBIS (Image Ch13_21InjectArm)

Image source (morphine bottle, patent medicine label): National Library of Medicine (Images Ch13_11MorphineBottle, Ch13_15SoothingSyrupMorphine)

What Are Narcotics?

The term narcotic (medical term) refers to naturally occurring substances derived from the opium poppy and their synthetic substitutes.
These drugs are referred to as the opioid (or opiate) narcotics because of their association with opium.
The term narcotic (political or legal term) has been used to label many substances, from opium to marijuana to cocaine.

Pharmacology:
Mechanism of Action

Opioids act on selective receptors in the brain
Naturally occurring opioid-like products of the nervous system and endocrine glands activate brain opioid receptors
Enkephalins: morphinelike neurotransmitters found in the brain and adrenals
Endorphins: morphinelike neurotransmitters found in the brain and pituitary gland
Natural and synthetic opioid drugs as well endogenous opioids act on multiple types of opioid receptors in the brain

Cultivation of Opium

Papaver somniferum is an annual flowering plant that grows 3-4 feet high
Most likely origin = the Middle East

Image source (poppy field): Central Intelligence Agency (Ch13_02OpiumField)

Image source (poppy pod): US Drug Enforcement Administration (Ch13_03DryOpiumPoppy)

Cultivation of Opium

Opium is produced and available for collection for only a few days of the plant’s life
Opium harvesters use a sharp, clawed tool to make shallow cuts into the unripe seedpods
The resinous substance that oozes from the cuts is scraped and collected
Raw opium is the substance from which morphine is extracted and then heroin is derived

Image source (scoring opium seedpod): Central Intelligence Agency (Image Ch13_04ScoringPod)

Image source (seed pod): National Institutes of Health (Image Ch13_05OpiumPod)

Image source (raw opium): Drug Enforcement Administration (Image Ch13_06RawOpium)

History of Opium

Egypt
Papyrus (circa 1500 BC) described specific medical uses
Greece and Rome
Mentioned in Homer’s Odyssey
Had an important role in Greek medicines
Arabic world
Opium used as a social drug
Use spread to India and China through trade
Arab physicians wrote widely about use of opium preparations
Europe
Opium used widely beginning in the sixteenth century
Physicians developed a preparation called laudanum, a combination of strained opium and other ingredients

Image source: National Library of Medicine (Image Ch13_07OpiumPlantDrawing)

History: Writers and Opium

Writer Thomas De Quincey drank laudanum and wrote a widely read book (1823) about life as an “opium eater”
Other authors who used laudanum included Elizabeth Barrett Browning and Samuel Taylor Coleridge

Image source: National Library of Medicine (Image Ch13_08DeQuinceyPage)

Image source: National Library of Medicine (Image Ch13_09LaudanumBottle)

History: Opium Wars

1729: Opium smoking outlawed in China, but smuggling was widespread
British East India Company was involved in opium trade, legally in India and illicitly (but indirectly) in China
Pressure grew and eventually war broke out between the British and Chinese

Image source: Library of Congress Prints and Photographs Division (Image Ch13_10OpiumWar)

Morphine

1806: Active ingredient in opium isolated
10 times as potent as opium
Named morphium after Morpheus, the god of dreams

1832: Another alkaloid of opium discovered
Named codeine from the Greek word for “poppy head”

Image source: National Library of Medicine (Image Ch13_11MorphineBottle)

History

In the 1800’s, in America opium could be purchased over-the-counter (OTC) known as laudanum.
Quickly gained popularity in the U.S. due to:

Famous writers Elizabeth Barrett Browning and Samuel Taylor Coleridge drank laudanum.

Stopped diarrhea and was an analgesic.

Diarrhea and pain were two important chronic issues at that time.

Here in America in the 1800’s, we had plenty of opium. Back then, opium could be purchased over-the-counter (OTC) and was known as laudanum. Some famous writers like Elizabeth Barrett Browning and Samuel Taylor Coleridge were known to have partaken in drinking laudanum (“McGraw-Hill,” 2008). The two main therapeutic effects of opium were that it stopped diarrhea and it was an analgesic. Because diarrhea and pain were two important chronic issues of that time, opium quickly gained popularity in the U.S.

Fredrick Serturner and Alexander Wood

1803: Serturner discovered how to extract and purify the active ingredients in opium.
Became a drug 10 times more potent than opium, became known as morphine.
1832: A second compound was purified from opium; it was named codeine
1853: Wood perfected the hypodermic syringe

Intended for preventing morphine addiction

Injecting the drug was theoretically supposed to slow the use of morphine

Instead the potency of morphine increased, increasing likelihood of use, abuse, and dependence.

In 1803, Fredrick Serturner discovered a way to extract and purify the active ingredients in opium, resulting in a drug that was ten times more potent than the opium itself. The new drug was named morphine. This discovery further increased the interest in opium. In 1832, a second compound had been purified from opium; this new drug was named codeine (Hanson, Venturelli, and Fleckenstein, 2012, p. 253, 254). Morphine and codeine remain in medical use today because of their strong analgesic properties. In 1853, Alexander Wood perfected the hypodermic syringe with the intention of preventing morphine addiction made easy by taking the drug orally; injecting the drug would therefore theoretically slow the use of morphine. Unfortunately, just the opposite happened (this is no surprise, because people will always find a way to get high). Because of this new method injection, the potency of morphine increased, thus increasing the likelihood of use, abuse, and dependence (Hanson, Venturelli, and Fleckenstein, 2012, p. 254).

Morphine

Medically useful characteristics
Clinically useful
Pure chemical
Known potency
Use spread due to two developments
1853: Hypodermic syringe allowed delivery of morphine directly into the blood
Widespread use during war provided relief from pain and dysentery
Many veterans were dependent on morphine, and dependence was later called “soldier’s disease” or “army disease”

Image source: TRBfoto/Getty Images (Image Ch13_12Syringe)

Heroin

Two acetyl groups added to morphine in the laboratory, creating diacetylmorphine
Given the brand name Heroin
Placed on the market in 1898
Three times as potent as morphine due to increased lipid solubility of the heroin molecule
Acts like morphine except that it is more potent and acts more quickly
Marketed as a non-habit-forming substitute for codeine
Later linked to tolerance and dependence

Pharmacology: Chemical Characteristics

Narcotic agents isolated or derived from opium

Figure 13.2 from text

History of Opioids:
Patterns of Abuse

Three types of opioid dependence developed in the U.S. in the second half of the 19th century
Oral intake increased as patent medicines spread
Opium smoking increased after 1850, as Chinese laborers arrived in the U.S.
Injection of morphine—the most dangerous form of use
Number and proportion of Americans dependent on opioids peaked at the start of the 20th century
Possibly as high as 1 percent of the population

Image source (opium den): Library of Congress Prints and Photographs Division (Image Ch13_13OpiumDen)

Image source (smoking): World Health Organization/National Library of Medicine (Image Ch13_14OpiumSmoking)

History of Opioids:
Patterns of Abuse

Initially, opioid dependence was not viewed as a major social problem
Opium smoking was limited to certain groups
Patent medicines were socially acceptable
Opioid dependence was viewed as a “vice of middle life”

Typical user was a 30-to-50-year-old middle class white woman, wife and mother
Drugs purchased legally in patent medicines
High drugs levels in patent medicines meant that withdrawal symptoms were severe and relieved only by taking more

Image source: National Library of Medicine (Image Ch13_15SoothingSyrupMorphine)

Government Regulation

Harrison Act of 1914 was the first federal government regulation to be imposed on opiates.

First legitimate effort by the federal government to regulate and control the production, importation, sale, purchase, and free distribution of opium or drugs derived from opium.

The act served as the foundation and reference for subsequent laws directed at facing the issue of opiates.
Harrison Act made opiates difficult to obtain so there were now several changes in the pattern of opioid use due to implementation of the legislation.

Drug users began injecting morphine or heroin

Illegal drug dealers were the only sources of drugs

The cost and risk of drug use increased, resulting in increased intravenous use

Addicts were now looked at as weak and self-indulgent rather than as victims

The first federal government regulation to be imposed on opiate use was the Harrison Act of 1914, which marked the first legitimate effort by the federal government to regulate and control the production, importation, sale, purchase, and free distribution of opium or drugs derived from opium. This act served as the foundation and reference for subsequent laws directed at regulating drug abuse issues (Hanson, Venturelli, and Fleckenstein, 2012, p. 102, 103). The Harrison Act requires prescriptions for products exceeding the allowable limit of narcotics and mandates increased record keeping for physicians and pharmacists who dispense narcotics (“Significant Dates,” 2012). Because the Harrison Act made opiates difficult to obtain, there were now several marked changes in pattern of opioid use directly due to the implementation of this legislation: with oral use restricted by law, drug users began injecting morphine or heroin; illegal drug dealers were now the only sources of drugs; the cost and risk of drug use increased, thus resulting in increased intravenous use; addicts were now looked upon as weak and self-indulgent rather than as victims; oral use among the white middle class declined; between World Wars, drug use was limited to particular social groups; and finally, after World War II, the use of heroin increased in low-income areas of large cities (“McGraw-Hill,” 2008).

Government Regulation Cont..

The additional government regulations imposed to control opiate use over the past 100 years include:
The Heroin Act of 1924- makes it illegal to manufacture heroin
The Narcotics Control Act of 1956- intended to impose very severe penalties for those convicted of narcotics
The Comprehensive Drug Abuse Prevention and Control Act- replaced previous laws and categorized drugs based on abuse and addiction potential as well as therapeutic value
The Methadone Control Act of 1973- places controls on methadone licensing
The U.S. Drug Enforcement Administration (DEA) Act of 1973- remodeled the Bureau of Narcotics and Dangerous Drugs to become the DEA
The Analogue (Designer Drug) Act of 1986- makes illegal the use of substances similar in effects and structure to substances already scheduled
The Drug Addiction Treatment Act of 2000- Allows qualified physicians to dispense or prescribe specially approved schedule III IV and V narcotics for the treatment of opioid addiction.
The Secure and Responsible Drug Disposal Act of 2010- Allows customers to give controlled to specially designated individuals for disposal

Additional government regulations imposed to control opiate use over the past 100 years include: the Heroin Act of 1924, which makes illegal to manufacture heroin; The Narcotics Control Act of 1956, which was intended to impose very severe penalties for those convicted of narcotics; The Comprehensive Drug Abuse Prevention and Control Act, which replaced previous laws and categorized drugs based on abuse and potential as well as therapeutic value; The Methadone Control Act of 1973, which places controls on methadone licensing; The U.S. Drug Enforcement Administration (DEA) Act of 1973, which remodeled the Bureau of Narcotics and Dangerous Drugs to become the DEA; The Analogue (Designer Drug) Act of 1986, which makes illegal the use of substances similar in effects and structure to substances already scheduled; The Drug Addiction Treatment Act of 2000, which allows qualified physicians to dispense or prescribe specially approved Schedule III, IV, and V narcotics for the treatment of opioid addiction in medical treatment settings; and finally, The Secure and Responsible Drug Disposal Act of 2010, which allows customers to give controlled substances to specially designated individuals for disposal (Hanson, Venturelli, and Fleckenstein, 2012, p. 103). All of this legislation clearly shows how the federal government has attempted to step in and contol opiate use, abuse and addiction during the past 100 years.

History of Opioids:
Patterns of Abuse

After the 1914 Harrison Act
Oral use among the white middle class declined
Use between World War I and World War II was limited to particular social groups

After World War II, use of heroin increased in low-income areas of large cities
The 1960s
Regular and irregular heroin use increased in large cities
Heroin use was associated with crime and considered socially unacceptable

Image source: Don Farrall/Getty Image (Image Ch13_16InjectArm2)

Heroin and Mexico

By 1975, most of America’s heroin came from Mexico
Pure heroin was made by opium being processed into morphine in a new way.

The new heroin had a black or brown color

Became known as Mexican brown heroin or black tar heroin

By 1975, most of America’s heroin came from Mexico. Opium was processed into morphine by a new and different process which resulted in pure heroin. This new heroin had a brown or black color; it became known as Mexican brown heroin or black tar heroin (“McGraw-Hill,” 2008). Heroin smoking became popular in the mid 1980’s, but this was in response to the AIDS scare. Because there was increased risk of HIV infection by using needles to shoot heroin intravenously, users resorted to smoking instead. The effect of inhaling heroin is the same as the intense effect caused by injection, but in order to accomplish this, the heroin has to be pure. To this day, because of the increased purity of heroin, smoking and snorting the drug continues to be a popular method of administration (Hanson, Venturelli, and Fleckenstein, 2012, p. 255) & (“McGraw-Hill,” 2008).

Patterns

Smoking heroin became popular in the mid 1980’s, but in response to the AIDS scare.
The effect of inhaling heroin is the same as the effect as injecting but the heroin has to be pure to accomplish it.
The increased purity of street heroin went from 5% to 95% pure

Sources of Illicit Heroin
for the U.S.

Figure 13.1 from text

History of Opioids:
Patterns of Abuse

Heroin use by American troops in Vietnam
Rate of use = about 5% (officially)
30-50% unofficially
Heroin in SE Asia was
Inexpensive
About 95 pure (compared to 5 percent in the U.S.)
Easy to obtain
Most users smoked or sniffed the drug
Most users (93%) stopped when they returned to the U.S.
Vietnam experience showed
Under certain conditions, a relatively high percent of individuals will use opioids recreationally
Opioid dependence and compulsive use are not inevitable among users

Opioids: Current
Patterns of Abuse

Heroin: 0.1 percent of Americans report past-year use
Prescription pain relievers (nonmedical use): 5 percent of Americans report past-year use
Most are taken orally
Dependence and toxicity can occur from misuse of prescription opioids
Special problem of Oxycontin (Schedule II drug); Illicit users crush the time-release capsules to obtain a high dose

Image source: US Drug Enforcement Agency (Image Ch13_18Oxycontin)

Prescription Narcotic Analgesics

Natural products
Morphine
Codeine
Semisynthetics
Heroin

Synthetics
Methadone
Meperidine
Oxycodone
Oxymorphone
Hydrocodone
Hydromorphone
Dihydrocodeine
Propoxyphene
Pentazocine
Fentanyl

Image source: US Drug Enforcement Agency (Image Ch13_19HeroinPowder)

2011 PDMP

Prescription drug monitoring program (PDMP) is a statewide electronic database which collects designated data on substances dispensed in the state.
The PDMP is a tool used by the states to address prescription drug abuse, addiction, and diversion.
Oregon PDMP

The DEA is not involved with the administration of any state PDMP.

A prescription drug monitoring program (PDMP) is a statewide electronic database which collects designated data on substances dispensed in the state. The PDMP is housed by a specified statewide regulatory, administrative, or law enforcement agency. The housing agency distributes data from the database to individuals who are authorized under state law to receive the information for purposes of their profession. The DEA is not involved with the administation of any state PDMP. The PDMP is therefore a tool used by the states to address prescription drug abuse, addiction, and diversion.

PDMP Activities and Purposes

Activities and purposes served by the PDMP include to:

Support access to legitimate medical use of controlled substances

Identify, deter, or prevent drug abuse and diversion

Facilitate and encourage the identification and intervention with persons addicted to prescription drugs

Inform public health initiatives through outlining treatment use, abuse, and trends

Educate individuals about the use for PDMP’s

Lastly, to educate individuals about the use, abuse, and diversion of prescription drugs as well as the addiction to the drugs

As of October 16, 2011, 37 states gave operational PDMP’s that have the capability to receive and distribute controlled substance prescription information to authorized users.

Activities and purposes served by the PDMP include: to support access to legitimate medical use of controlled substances; to identify, deter, or prevent drug abuse and diversion; to facilitate and encourage the identification and intervention with persons addicted to prescription drugs; to inform public health initiatives through outlining of use, abuse, and trends; to educate individuals about the use of PDMP’s ; and finally to educate individuals about the use, abuse, and diversion of prescription drugs as well as the addiction to the drugs. As of October 16, 2011, 37 states gave operational PDMP’s that have the capability to receive and distribute controlled substance prescription information to authorized users (“State Prescription Drug Monitoring Programs,” 2011).

Facts About Heroin Abuse

What is the estimated number of heroin addicts in the United States?
600,000
What is the estimated number of Rx opiate addicts in the United States?
2,000,000

Current Opiate numbers

2014 NIDA Report to Congress

ASAM 2016 Facts and Figures

CDC Info-graphic

InfoFacts - High School and Youth Trends

National Institute on Drug Abuse - The Science of Drug Abuse and Addiction
See recent report from director, treatment advances opiate addiction

Medical Uses

Pain relief
Reduces the emotional response to pain and diminishes the patient’s awareness of, and response to, the aversive stimulus
Typically causes drowsiness but does not induce sleep
Treatment of intestinal disorders
Reduces colic and counteracts diarrhea and the resulting dehydration
Acts by decreasing the number of peristaltic contractions
An opium solution known as a paregoric is still available for relief of diarrhea

Image source: US Food and Drug Administration (Image Ch13_20Paregoric)

Medical Uses

Cough suppressant
Codeine has long been used to reduce coughing
It remains available in prescription cough medications

Nonprescription cough remedies contain the opioid analogue dextromethorphan
It produces hallucinogenic effects at high doses

Dependence Potential

Tolerance
Tolerance develops to most effects from both medical and recreational usage
Higher doses needed to maintain effects
Cross-tolerance exists among all the opioids
Psychological processes play a key role in tolerance
Dependent individuals develop a conditioned reflex response to the stimuli associated with taking the drugs

Dependence Potential

Physical dependence
Symptoms of withdrawal appear in sequence following the timing of the most recent dose and the individual’s history of use
Opioid withdrawal is unpleasant but rarely life-threatening
Methadone (long-lasting synthetic opioid) produces withdrawal symptoms that appear later and are less severe than those from heroin

Dependence Potential

Psychological dependence
Positive reinforcement
Positive effects reliably follow use of the drug
Negative reinforcement
Use of the drug removes withdrawal symptoms
Fast-acting injectable opioids are most likely to lead to dependence

Image source: Royalty-Free/CORBIS (Image Ch13_21InjectArm1)

Dependence Potential

Psychological dependence
The needle habit
Each heroin administration is following by a decrease in discomfort and/or an increase in pleasure
Users become conditioned so that the process of using heroin becomes rewarding in and of itself

Image source: Doug Menuez / Getty Images (Images Ch13_23LightingHeroin, Ch13_24AfterShootingHeroin)

Withdrawal Syndrome Symptoms

Approximate hours after previous dose

Signs	Heroin or Morphine	Methadone
Craving for drugs, anxiety	6	24
Yawning, perspiration, running nose, teary eyes	14	34-48
Increase in above signs plus pupil dilation, goose bumps, tremors, hot and cold flashes, aching bones and muscles, loss of appetite	16	48-72
Increased intensity of above, plus insomnia; raised blood pressure; increased temperature, pulse rate, respiratory rate and depth; restlessness; nausea	24-36
Increased intensity of above, plus curled-up position, vomiting, diarrhea, weight loss, spontaneous ejaculation or orgasm, hemoconcentration, increased blood sugar	36-48

Toxicity Potential

Acute toxicity
Opioids depress respiratory centers in the brain
Breathing becomes slower and shallower
Effects with alcohol are additive
Opioid overdose triad
Coma
Depressed respiration
Pinpoint pupils
Clouding of consciousness
Chronic toxicity is associated with injection method of use
Infections and the spread of blood-borne diseases

Pharmacology: Chemical Characteristics

Opioid antagonists = drugs that block the action of opioids
Examples: Naloxone and nalorphine
Effects:
Reverse depressed respiration from opioid overdose
Precipitate withdrawal syndrome
Prevent dependent individuals from experiencing a high from subsequent opioid use

Treatment

Misconceptions and Preconceptions

Not all users experience euphoria from initial dose
Tolerance to negative effects may develop more rapidly than tolerance to positive effects
Withdrawal is often similar to a mild case of the intestinal flu
People usually don’t become dependent after one dose
Current users:
Probably about 500,000 opioid-dependent Americans and two to three times that many heroin chippers (occasional users)

Heroin Addicts and AIDS

More than 250,000 patients in United States contracted AIDS by drug injection, of which most were heroin users.
Fear of contracting HIV from IV heroin use has contributed to the increase in smoking or snorting heroin.
Many who start by smoking or snorting progress to IV administration due to its more intense effects.

Life of a Heroin User

Three to four injections needed daily to prevent withdrawal
Expensive habit (cost of drugs and paraphernalia)
Risk of overdose due to variable potency of different batches
Health problems associated with injection habit
Skin infections
Blood-borne infections
Masking of early symptoms of illness
Some users “mature out”

Image source: Creatas/PunchStock (Image Ch13_25DiscardedNeedles)

Pharmacology: Chemical Characteristics

Raw opium is about 10 percent morphine by weight
With the added acetyl groups, heroin can pass through the blood-brain barrier faster, making heroin more potent than morphine
Researchers searching (unsuccessfully) for ways to separate the analgesic and dependence-producing effects of opioids have developed a variety of prescription pain killers

Chapter 13

Opioids

Image sources (injection): Royalty-Free/CORBIS (Image Ch13_21InjectArm)

Image source (morphine bottle, patent medicine label): National Library of Medicine (Images Ch13_11MorphineBottle, Ch13_15SoothingSyrupMorphine)