Chapter 5 Opioids: Opium, Heroin, and Opioid Pain Medications

Morphine

The major active ingredient in opium. - ten times stronger than raw opium

dextromethorphan

a popular non-narcotic ingredient used in over-the-counter cough remedies. The "DM" designation on these preparations refers to dextromethorphan

Buprenorphine

a synthetic opioid used in the treatment of heroin abuse. Brand names are Subtext and (in combination with naloxone) Suboxone

propoxyphene

a synthetic opioid useful in reducing pain. brand names are Darvon, Darvocet

methadone

a synthetic opioid useful in treating heroin abuse

methadone maintenance

a treatment program for heroin abusers in which heroin is replaced by the long-term intake of methadone

antitussive

having an effect that controls coughing

therapeutic communities

living environments for individuals in treatment for heroin and other drug abuse, where they learn social and psychological skills needed to lead a drug-free life

detoxification

the process of drug withdrawal in which the body is allowed to rid itself of the chemical effects of the drug in the bloodstream.

LAAM (levo-alpha-acetylemethadol)

the synthetic narcotic drug used in the treatment of heroin abuse. Brand name is Orlaam

chipping

the taking of heroin on an occasional basis. the heroin abuser is known as a chipper.

multimodality programs

treatment programs in which a combination of detoxification, psychotherapy, and group support is implemented

Opium

An analgesic and euphoriant drug acquired from the dried juice of the opium poppy, known by its botanical name as Papaver somniferum (literally "the poppy that brings sleep").

Codeine

One of the three active ingredients in opium, used primarily to treat coughing - 0.5 % of raw opium

Thebaine

One of three active ingredients in opium - 0.2 % of raw opium

If heroin is injected intravenously..

..there is an almost immediate tingling sensation and sudden feeling of warmth in the lower abdomen, resembling a sexual orgasm, for the first minute or two. There is a feeling of intense euphoria, variously described as a "rush" or a "flash," followed later by a state of tranquil drowsiness that heroin abusers often call being "on the nod." - this period lasts 3-4 hours, decline in sex drive - withdrawals begin in about 4 hours

Fentanyl

A chemical derivative of of thebaine, used as a prescription painkiller. The street name for fentanyl and related compounds is China White

Heroin

A chemically derivative of morphine. It is approximately three times as potent as morphine and a major drug of abuse - used as cough suppressant and as a medication to relieve the chest discomfort associated with pneumonia and tuberculosis -two acetyl groups joined to a basic morphine molecule make heroin more fat-soluble and hence more rapidly absorbed into brain

OxyContin

A controlled-release form of oxycodone, used in the treatment of chronic pain

Narcotics

A general term technically referring to opiate-related or opiate-derived drugs. It is often mistakenly used to include several other illicit drug categories as well.

Naltrexone

A long-lasting form of Naloxone. Brand name prior to 1994 was Trexan; brand name has since been changed to ReVia

Black tar

A potent form of heroin, generally brownish in color, originating in Mexico.

Naloxone

A pure antagonist for morphine and other opioid drugs. Brand name is Narcan.

Opioids can be divided into four broad categories of drugs:

(1) comprises three natural compounds that are directly extracted from opium itself: morphine, codeine, and thebaine. All opioid derivatives have their origin in these compounds. (2) comprises derivative compounds that are created by making specific changes in the chemical composition of morphine. Examples are heroin, hydromorphone (brand name: Dilaudid), oxymorphone (brand names: Numorphan, Opana), and the extended-release form of oxymorphone (brand name: Opana ER). (3) comprises derivative compounds that are created by making specific changes in the chemical composition of codeine or thebaine. Examples are oxycodone (brand names: Percodan, Percocet), the controlled-release form of oxycodone (brand name: OxyCotin), and hydrocodone (brand names: Hycodan, Vicodin). (4) comprises drugs that are not chemically related to any of the natural extracts of opium but rather synthesized entirely in the laboratory. As a result, they are often referred to as [ synthetic opioids ]. Examples include methadone, meperidine (brand name: Demerol), propoxyphene (brand names: Darvon, Darvocet), LAAM (brand name: Orlaam), tramadol (brand names: Ultram, Ultracet), and buprenorphine (brand names: Subutex, Suboxone).

The intensity of a response to heroin changes as a function of

(1) the quantity and purity of the heroin taken, (2) the route through which heroin is administered, (3) the interval since the previous dose of heroin, and (4) the degree of tolerance of the user to heroin itself.

Endogenous opioid peptides

- A class of chemicals produced inside the body that mimic the effects of opioid drugs (1) peptide molecules (amino acids strung together like a necklace), (2) opium-like in function (hence the word opioid), and (3) produced within the central nervous system. - Simply referred to as endorphins

Physiological changes from Heroin use

- a sudden release of histamine in the bloodstream produces an often intense itching over the entire body and a reddening of the eyes. - pupillary constriction, resulting gin the characteristic "pinpoint pupils" that are used as an important diagnostic sign for narcotic abuse - reduces the sensitivity of respiratory centers in the medulla to levels of carbon dioxide, resulting in a depression in breathing. At high doses, this could cause death. - blood pressure is also depressed - suppression of the immune system - slowing down of the gastrointestinal tract, causing labored defecation and intense constipation

The practice of heroin abuse is highly dangerous and potentially lethal for many reasons:

- heroin has a relatively small ration of lethal dose (LD) to effective dose (ED). - heroin abusers risk possible adverse effects from any toxic substance that has been "cut" with the heroin. Lines of cocaine and heroin are alternately inhaled in a single session, which is known as "criss-crossing" - It is also possible that some heroin abusers develop unstable levels of tolerance that are tied to the environmental setting in which the heroin is administered - although the overriding danger of excessive amounts of heroin is the potentially lethal effect of respiratory depression, abusers can die from other physiological reactions. - some forms of synthetic heroin failed to remove an impurity called MPTP that destroys dopamine-sensitive neurons in the substantia nigra of the midbrain. As a result, someone exposed to this type of heroin could acquire full-blown symptoms of Parkinson's disease

Routes of administrating heroin

- the dominant route of administration in heroin abuse is intravenous injection is known as mainlining or shooting - smoking is popular in Middle Eastern countries and in Asia - Snorting through the nose or injecting subcutaneously (sub-Q) (skin-popping) - oral is worthless

Opioids

Drugs with analgesic (pain reducing) properties that act in the brain like opium

Three groups of natural morphine-like molecules have been identified:

Enkephalins, beta-endorphins, and dynorphins. Together, they are known as endogenous opioid peptides.