Ch. 9 Narcotics (opioids)

What is the estimated number of heroin addicts in the United States?

-600,000

The principle side effects of opioid narcotics, besides their abuse potential, include:

-Drowsiness -Mental clouding -Respiratory depression -Nausea, vomiting, and constipation -Inability to urinate -Drop in blood pressure -Constricted pupils -Constipation -Physical dependence and withdrawal

What are "shooting galleries"?

-Locations that serve as gathering places for addicts

Factors that relate heroin to crime

-Pharmacological effects encourage antisocial behavior that is crime-related -Heroin diminishes inhibition -Addicts are often self-centered, impulsive, and governed by need -Cost of addiction -Similar personality of criminal and addict

Heroin use by a pregnant woman leads to:

-Physical dependence on heroin in the newborn -Withdrawal symptoms after birth in the newborn (Note: similar withdrawal occurs in newborns of any woman who uses significant amounts of opiate drugs during pregnancy, including prescribed opiate painkillers)

MPTP: A "Designer" Trage

1. Attempts to synthesize illicit designer versions of meperidine by street chemists they have proved tragic 2. A by-product resulting from the sloppy synthesis of the meperidine-like designer narcotic was responsible for irreversible brain damage leading to Parkinson's disease

Tramadol

1. It is a moderately effective analgesic sometimes used as a substitute for opioid painkillers 2. While it does activate opioid receptors, its analgesic properties are related to more than just opioid actions 3. Because it has relatively low risk for dependence, it has not been scheduled by the DEA although some states have classified it as a Schedule IV or V drug. It carries a warning that for some patients dependence can occur

Clonidine

1. It is a nonaddictive drug that stimulates receptors for noradrenaline 2. It is used in relieving the effects of opiate withdrawal; a major advantage of clonidine versus other treatments is that it shortens the time for withdrawal to 14 days

Naloxone/Naltrexone: : Narcotic antagonist; used for narcotic overdoses

1. Pure narcotic antagonists that prevent narcotic drugs from having an effect 2. Sometimes used to treat opioid or alcohol dependence

hydromorphone:

1. Used as an analgesic for moderate to severe pain and as a cough suppressant 2. It is a stronger analgesic than morphine

Pentazocine

1. has analgesic effects slightly greater than those of codeine, but still causes withdrawal symptoms 2. Tends to have less abuse liability

40% of American soldiers during the Vietnam War used heroin and how many continued using after the war?

7% continued using heroin and became the major part of heroin-abusing population in America

Meperidine:

A synthetic drug used for moderate pain

Opioid narcotics relieve pain by activating receptors controlled by endorphins and they...

Block the transmission of pain in the spinal cord and brain stem

Codeine

It is a naturally occurring constituent of opium, and is often prescribed for mild to moderate pain

Opioid narcotics have important therapeutic uses:

Most common clinical use is as analgesics to relieve pain •Visceral and somatic pain •Pain caused by cancer

Oxycodone (OxyCotin)

Oxycodone (OxyContin) 1. A moderate to potent narcotic analgesic that is frequently abused as the proprietary product OxyContin; however, recent modifications to its formulation makes it more difficult to abuse 2. OxyContin is a long-lasting version of this drug and is considered to be an important therapy for the treatment of severe pain 3. Most individuals who have abuse problems with this product already have a history of drug abuse with other drugs

Why has the use of narcotics been declared an epidemic by the Centers for Disease Control (CDC)?

The proportion of persons admitted for substance abuse treatment whose principal problem was non-medical use of prescription pain medication (i.e., narcotic analgesics) has gone from 2.2% to almost 10% in the past decade

Fentanyl:

Very potent narcotic analgesics that are often administered intravenously and sometimes combined with heroin by dealers resulting in lethal overdoses

In 1914 when laws were passed to regulate opium and their derivates, who was the average opiate addict?

a middle-aged, Southern, white woman who legally obtained opium by mail order from Sears or a local store.

What are some guidelines for avoiding unnecessary problems with these drugs?

a. Only use narcotic analgesics when pain severity warrants b. Be as conservative with doses as possible c. Store the medications securely because they are often stolen d. Once the purpose for which the opiate was prescribed is resolved, properly dispose of unused narcotic drug e. It is illegal to share with others, even if you are only trying to be helpful f. A treatment plan should be established between doctor and patient, especially if treatment is going to last more than just a few days g. If significant abuse is suspected, the clinician should frankly discuss the concerns with the patient

Tolerance begins with the first dose of a narcotic, but does not become clinically evident until when?

after 2 to 3 weeks of frequent use.

Morphine is a particularly potent pain reliever and often is used as the __________ ____________ by which other narcotics are compared.

analgesic standard

The greek word narkoticos is described as:

benumbing or deadening

Psychological dependence can also develop with?

continual narcotic use.

Because of its association with popular fashions and entertainment, heroin has been viewed as __________ and ______, especially by many young people, although lately this attitude has been changing.

glamorous and chic

Although opioid narcotics possess abuse potential, they also have what going for them?

important clinical value (e.g., analgesic, antitussive, antidiarrheal).

Dextromethorphan: OTC antitussive

is a synthetic used in cough remedies that in high doses can have effects like those of PCP and is sometimes abused by adolescents

Propoxyphene

is structurally related to methadone, with much weaker analgesic and its removal has been requested by the FDA

Because of the dramatic impact and addictive properties of the opium poppy, the Chinese eventually banned the drug in 1729, which led to what?

it Led to hostilities with Great Britain and eventually the Opium Wars 1839-42, and the loss of Hong Kong to the British

Heroin facts and combinations:

• Pure heroin is a white powder. • More than 90% of world's heroin is from Afghanistan. • Heroin is usually "cut" (diluted) with lactose. • When heroin first enters the United States, it may be 95% pure; by the time it is sold, it may be 3% to 70% pure. • If users are unaware of the variance in purity and do not adjust doses accordingly, results can be fatal. •Heroin has a bitter taste and is often cut with quinine, which can be a deadly adulterant. •Heroin plus the artificial narcotic fentanyl can be dangerous due to its unexpected potency. •Heroin is most frequently used with alcohol. •Heroin combined with cocaine is called "speedballing."

Morphine is used to:

relieve moderate to intense pain, morphine is about half as potent as heroin

Heroin addicts often share locations to stash supplies called?

shooting galleries

Tolerance occurs most rapidly with high doses given in long, mildly long or short intervals?

short intervals

Because of AIDS what became popular in the 1980's?

smoking Heroin became popular in the 1980s •Smoking effects are as intense as injection.

Initially, China grew their own poppies for medical use but in the late 1690's what did the people start to use the drug for?

the people began using it for fun/diversion

All Opioid narcotics activate opioid receptors and have what kind of potential?

they have abuse potential.

With continual use...

tolerance develops to the analgesic effects of morphine and other narcotics.

Physicians frequently ________________ narcotics, for fear of causing narcotic addiction.

under prescribe

Because heroin users generally have a low level of employment, they exist in what kind of living conditions?

unstable living conditions, and socialize with other illicit drug users; heroin useencourages criminal activity

opiate drugs are closely linked with what?

war

what are examples of other narcotics?

• Morphine • Methadone • Fentanyl • Hydromorphone • Oxycodone (OxyContin) • Meperidine • Buprenorphine • MPTP • Codeine • Pentazocine • Tramadol

Methadone

•1. lasts longer, and if properly used, it is a safe drug to use in treatment of opioid addicts •2. However, it still has the same side effects as heroin and morphine •3. In the past decade, methadone-related deaths have increased 5-fold

What is some of the history of narcotics?

•A 6000-year-old Sumerian tablet depict the poppy as joy plus plant • The Egyptians listed opium with other medicinal compounds • The Greeks portrayed gods carrying and wearing crown of opium pods. • Arab traders introduced opium to China and India

Withdrawal symptoms of Heroine

•After the effects of the heroin wear off, the addicts have only a few hours in which to find the next dose before severe withdrawal symptoms begin. •A single "shot" of heroin lasts 4 to 6 hours. •Withdrawal symptoms: runny nose, tears, minor stomach cramps, loss of appetite, vomiting, diarrhea, abdominal cramps, chills, fever, aching bones, and muscle spasms. •Severe withdrawal symptoms called dope sickness can last up to 4 or 5 days, after which users still continue to crave the drug

Facts about Heroine Abuse

•Heroin is a Schedule I drug and is one of the most widely abused illegal drugs in the world; accounts for >$120 billion sales/year • Illicitly used more than any other drug of abuse in the United States (except for marijuana) until 20 years ago, when it was replaced by cocaine •Heroin abuse is sometimes an indirect consequence of increased abuse of prescription opioid painkillers

What does the term narcotic mean?

-in general it means a central nervous system (CNS) depressant that produces insensibility or stupor. -The term narcotic currently 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.

Heroin abuse facts:

-in recent years, heroin has become purer, (60% to 70% purity) and cheaper (~$10/bag) -Greater purity leads users to administer heroin in less efficient ways

Buprenorphine

1. A mild to moderate narcotic analgesic that has been available as a pain reliever for years 2. Approved for use in treatment of narcotic addiction in a primary care physician's office 3. There are thousands of physicians who have been trained to use this drug to treat addiction

Narcotics are frequently prescribed for what 3 things?

pain relief (analgesics) reduce coughing (antitussive) and to reduce diarrhea.

Opioid receptors are the site of action of what naturally occurring transmitters found throughout the nervous system such as the endorphins that are important for pain relief and modulation of stress?

peptidetransmitters

Describe American Opium use:

•In 1803, morphine was discovered, which aggravated the opium problem in the United States. •In 1832 codeine was created •In 1853 the hypodermic needle was introduced •Civil War morphine was used to treat pain, dysentery, and fatigue which caused wide spread addiction known as "soldier's disease" •In 1898 there was a modification of morphine created in order to create better medicines -diacetylmorphine was created as a cold suppressant by Bayer. •It was to be heroic drug, without the addictive potential of morphine- thus it received its name heroin. •Quickly discovered that it was more addictive than other narcotics •1900 about 300,000 Americans were dependent on opiates •Chinese laborers brought opium over as it was legal to smoke opium during that time •Easy availability of morphine and hypodermic needles •No control over medicines that contained opium derivatives

What are the stages of dependence for heroin?

•Initially, the effects of heroin are often unpleasant. •Euphoria gradually overcomes the aversive effects. •The positive feelings increase with narcotic use, leading to psychological dependence. •In addition to psychological dependence, physical dependence occurs with daily use over a 2-week period. •If the user abruptly stops taking the drug after physical dependence has developed, severe withdrawal symptoms result

What are some ways of treating heroine abuse and withdrawal?

•Methadone or buprenorphine are frequently used to help narcotic addicts. •These drugs block withdrawal symptoms. •Treatment should also include regular counseling and other supplemental services such as job training.

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.

What are methods of administering Heroin?

•Sniffing the powder •Injecting it into a muscle (intramuscular) •Smoking •Mainlining (intravenous injection)

Heroin is deliberately combined with other drugs such as CNS stimulants like cocaine

•This combination is called speedballing