Opiates Overview - Chapter 11

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Questions and Answers

Which compound accounts for the highest percentage of raw opium?

Morphine (correct)

Thebaine

Codeine

Psychoactive alkaloids

Which of the following statements about naturally occurring opioids is true?

Opium is derived from a tropical plant species.

Opioids are synthesized entirely in laboratories.

Thebaine is one of the major compounds found in raw opium. (correct)

Codeine is present in higher concentrations than morphine in raw opium.

What is the source of naturally occurring opioids?

Cotton plant

Opium poppy (correct)

Cacti species

Cocoa plant

How is the term 'narcotic' most accurately defined in relation to opioids?

A type of analgesic that includes both opioids and dissimilar drugs. Signup and view all the answers

Which of the following is NOT considered an opioid?

Ibuprofen Signup and view all the answers

What is the primary use of opioids in medical practice?

To provide pain relief through analgesic properties Signup and view all the answers

Which of the following compounds is most abundant in raw opium?

Morphine Signup and view all the answers

What distinguishes naturally occurring opioids from synthetic compounds?

Natural opioids are derived from living plants, while synthetics are chemically manufactured. Signup and view all the answers

Which of the following is NOT a major compound derived from the opium poppy?

Fentanyl Signup and view all the answers

What percentage range of raw opium does codeine typically account for?

0.75% - 2.5% Signup and view all the answers

What are opioids primarily used for?

To relieve pain due to their analgesic properties Signup and view all the answers

Which of the following is a naturally occurring opioid derived from the opium poppy?

Codeine Signup and view all the answers

Which statement differentiates naturally occurring opioids from synthetic ones?

Naturally occurring opioids are derived from the opium poppy. Signup and view all the answers

What is the sap extracted from the opium poppy known as?

Opium Signup and view all the answers

Which opioid compound is most significant in terms of its percentage content in raw opium?

Morphine Signup and view all the answers

Study Notes

Learning Outcomes for Opiates

Opiates are discussed in Chapter 11 of the text
Includes historical use, names of common natural and synthetic opiates
Details potency, metabolism, medical uses, administration methods, pharmacological actions, effects of tolerance, withdrawal, and psychological dependence. Methadone use for treatment is included.

Opioids Overview

Opioids are a class of naturally occurring, derived, and synthetic compounds with analgesic properties.
Often referred to as narcotic analgesics, though this term can be confusing as it includes other dissimilar drugs.

Naturally Occurring Opioids

Sources are derived from the opium poppy (Papaver somniferum).
Opium is the sap extracted from the seedpods.
Major compounds include:
- Morphine (10% of raw opium)
- Codeine (0.75-2.5% of raw opium).
- Thebaine (<1% of raw opium)
Opium extraction:
- Incisions are made in the seedpod after the petals fall
- Milky white juice (raw opium) oozes out.
- The juice oxidizes to reddish-brown tar-like balls.
- The balls have a smell similar to new-mown hay.
- Opium production lasts for 10 days after the petals drop.

Opiate Derivatives/Semi-Synthetics

Heroin: Derived from morphine, 3x more potent, and more lipid-soluble, increasing its ability to cross the blood-brain barrier.
Other derivatives include:
- Hydromorphone (10x more potent than morphine)
- Oxycodone (commonly prescribed for pain)
- Oxymorphone (1.5x more potent than morphine)
- Hydrocodone (slightly more potent than morphine)

Synthetic Opioids

Meperidine (Demerol): A less potent synthetic opioid, often used as a painkiller.
Methadone: Used to treat chronic pain and opioid dependency, with similar analgesic effects to morphine but less euphoria. Methadone is used in opioid maintenance programs for individuals recovering from heroin addiction.
Fentanyl: A potent synthetic opioid available in several forms (e.g., oral transmucosal lozenges, sublingual tablets, nasal sprays, transdermal patches).

Opiate Antagonists

Naloxone (Brand Name: Narcan): Can reverse opioid effects, especially respiratory depression, within minutes. Administered intravenously (IV) or intramuscularly (IM).
Naltrexone: Has mild agonist effects resembling morphine-like activity, but can last longer than Naloxone. Primarily used in opioid addiction treatment.

Medical Uses of Opioids

Pain relief (morphine is a key agent)
Diarrhea treatment (loperamide)
Cough suppression (codeine)

Opioids: Historical Medical Uses

Opium was documented in Egyptian medical scrolls (Ebers Papyrus) in 1550 BC.
Used for various conditions, including excessive crying in children.
Galen (Greek physician) prescribed opium for multiple conditions.

Opioids: Historical Recreational Uses

Opium use dates back to the Bronze Age.
Widespread availability of opium cakes and candy was evident by the 2nd Century AD.
Opium smoking became widespread in the 18th century (China) resulting in the rise of opium dens.
Opium dens emerged globally offering specialized pipes, lamps, and paraphernalia for smoking. Opium dens catered to all social classes, with more luxurious dens for wealthier patrons.

Opium was widely accepted for medical and recreational use in the early to mid-1800s.
Addiction issues were not viewed as a predominant medical or social problem.
Increased regulation began in the U.S and Britain in the mid to late 1800s due to concerns about chronic use and anti-Chinese prejudice linked to opium dens. Regulation was driven by a combination of public health concerns, social perception shifts, and political considerations.

Opioids: History and Canada's Opium Act (1908 & 1911)

The Opium Acts focused on prohibiting the importation, manufacture, and sale of opium for non-medical purposes. Medical use was restricted.
Stricter controls (e.g., limiting sales to pharmacies) were a feature of the 1911 Act.
The Acts restricted use to medical purposes, and manufacturing, selling, and possession of opium for smoking was prohibited.
The 1911 Act also expanded the scope of regulation, adding substances like cocaine, morphine, and eucaine to the list of controlled substances. Legislative details are provided in the text.

Methods of Administration

Oral: Examples (pills, capsules, liquid forms). Slower onset due to first-pass metabolism.
Parenteral: Examples (IM, SC, IV). Injected directly into the body, bypassing the GI tract.
Inhalation: Smoking opium, or vaporized fentanyl. Rapid absorption into the bloodstream.
Transdermal: Examples (Fentanyl patches for chronic pain) Absorbed through the skin.

Opioids: Metabolism

Many opioids are inactive until metabolized into their active forms in the liver.
Metabolization is generally rapid, except for some synthetic opioids.
Specific enzymes and half-lives are referenced for various key opioids including Heroin, Codeine, Methadone, LAAM, and Fentanyl.

Opioids: CNS Effects

Analgesic effects (act on Mu, Delta, and Kappa receptors in the spinal cord to block pain signals).
Euphoria, dysphoria (unpleasant feelings).
Decreased concentration (sedative effects).
Emotional pain dulling (acting on receptors within the limbic system and frontal lobe).

Opioids: Tolerance & Dependence

Tolerance develops to certain effects with continued use (e.g., respiratory depression, analgesia).
Tolerance to some effects, such as constipation or pupil constriction, does not develop. Conditions leading to different tolerances are described.

Dependence: Characteristics of Withdrawal

Initial symptoms (restlessness, agitation, yawning, fever, chills).
Peak symptoms (intensify and reached peak 36-72 hours after last use)
Physical symptoms (cramps, limb twitching, profuse sweating, nausea, muscle pain, loss of body fluids, and possible hallucinations). Variations in severity are described. Life-threatening aspects of withdrawals are detailed.
Psychological dependence is more challenging to treat than physical addiction; treatment options are mentioned.

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Explore the crucial aspects of opiates as discussed in Chapter 11. This quiz delves into the history, types, potency, medical uses, and effects of opiates, including their administration methods and treatment for withdrawal. Gain a deeper understanding of both naturally occurring and synthetic opiates.