Textbook Chpt. 11 Opioids

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Questions and Answers

Which of the following accurately describes the primary difference between naturally occurring opioids and semisynthetic opioids?

  • Semisynthetic opioids have a longer history of use compared to naturally occurring opioids.
  • Semisynthetic opioids are exclusively derived from plants.
  • Naturally occurring opioids are derived from synthetic processes.
  • Naturally occurring opioids are obtained from the opium poppy, while semisynthetic opioids are chemically modified from them. (correct)

In the context of opioid pharmacokinetics, which route of administration typically results in the fastest onset of effect?

  • Transdermal administration
  • Intranasal administration (correct)
  • Oral administration
  • Subcutaneous administration

Which of the following statements about the history of opium is inaccurate?

  • Opium wars significantly impacted trade relations in the 19th century.
  • Opium has been used for both medicinal and recreational purposes for centuries.
  • Historical records indicate that opium consumption dates back to ancient civilizations.
  • The production of opium began in the 19th century with no earlier historical references. (correct)

What is a common misconception regarding the sources of semisynthetic opioids?

<p>They can originate from natural opiates but involve modification processes. (B)</p> Signup and view all the answers

Which of the following factors influences the variance in opioid pharmacokinetics between different administration routes?

<p>The specific chemical structure of the opioid. (A)</p> Signup and view all the answers

What was the primary reason that OxyContin was redesigned into a tamper-resistant formulation in 2010?

<p>To prevent abuse by making it harder to crush or dissolve (C)</p> Signup and view all the answers

In what year were oxymorphone and oxycodone first synthesized?

<p>1914 and 1917, respectively (A)</p> Signup and view all the answers

Which combination of components is marketed as Targin in Germany and Europe?

<p>Oxycodone and naloxone (B)</p> Signup and view all the answers

What major issue arose following the introduction of OxyContin in 1996?

<p>It caused a significant number of accidental overdoses due to misuse (A)</p> Signup and view all the answers

What effect does naloxone have when combined with oxycodone in Targin?

<p>It prevents the euphoric effects typically associated with oxycodone (D)</p> Signup and view all the answers

Which term correctly defines the drugs that bind to opioid receptors, including both natural and synthetic sources?

<p>Opioids (A)</p> Signup and view all the answers

What is the primary natural source of opium that is used to produce opioids?

<p>Papaver somniferum (A)</p> Signup and view all the answers

Which of the following drugs is classified as a non-narcotic analgesic?

<p>Acetaminophen (B)</p> Signup and view all the answers

What phenomenon does the term 'narcotic' originally denote?

<p>Sleep-inducing properties (A)</p> Signup and view all the answers

What is the primary disadvantage of using the term 'narcotic' in modern contexts?

<p>It has legal implications that can misclassify drugs. (B)</p> Signup and view all the answers

How long does the plant Papaver somniferum produce opium in its life cycle?

<p>For just 10 days after the petals fall off (D)</p> Signup and view all the answers

Which act in the United States created a legal designation for narcotics that included opioids?

<p>Harrison Narcotic Act of 1914 (D)</p> Signup and view all the answers

Which of the following statements about analgesics is true?

<p>Narcotic analgesics are a subclass of opioids. (B)</p> Signup and view all the answers

Which active ingredient was serendipitously isolated by Pierre J. Robiquet in 1821?

<p>Codeine (B)</p> Signup and view all the answers

What is the average codeine content in Indian opium?

<p>2.5% (C)</p> Signup and view all the answers

Which country is recognized as the largest producer and licit supplier of opium?

<p>India (D)</p> Signup and view all the answers

Which semisynthetic opioid is derived from codeine and frequently prescribed in the United States?

<p>Hydrocodone (B)</p> Signup and view all the answers

Who first isolated morphine from opium?

<p>Frederick Sertürner (A)</p> Signup and view all the answers

How does hydrocodone compare to codeine in terms of effectiveness for cough suppression?

<p>Equally effective (B)</p> Signup and view all the answers

What is the concentration of morphine in the opium supplied by India?

<p>9.5-12% (C)</p> Signup and view all the answers

Which of the following is NOT a common street name for mixtures of prescription-strength codeine cough syrup?

<p>Opium (C)</p> Signup and view all the answers

What is the primary source of thebaine since 1999?

<p>Poppy straw (A)</p> Signup and view all the answers

What significant event related to morphine occurred in 1831?

<p>Frederick Sertürner was awarded a prize. (B)</p> Signup and view all the answers

Which of the following countries primarily engages in illicit poppy cultivation?

<p>Afghanistan (C)</p> Signup and view all the answers

Which of the following opiates is marketed under the trade name 'Dilaudid'?

<p>Hydromorphone (C)</p> Signup and view all the answers

How does the potency of hydrocodone compare to that of morphine?

<p>Equally potent as morphine (B)</p> Signup and view all the answers

Morphine is commonly sold under which generic name?

<p>Morphine sulfate (C)</p> Signup and view all the answers

Which part of the poppy plant is primarily used for extracting morphine?

<p>Seedpod (A)</p> Signup and view all the answers

Which of the following opiates is derived solely through synthetic processes rather than naturally?

<p>Hydromorphone (A)</p> Signup and view all the answers

What is the primary legal restriction for the possession of heroin in Canada and the United Kingdom?

<p>It's illegal except for therapeutic purposes (B)</p> Signup and view all the answers

What method is primarily used to obtain opium from the poppy seedpod?

<p>Scoring and scraping (C)</p> Signup and view all the answers

Which country exports the highest amount of poppy straw?

<p>Czech Republic (C)</p> Signup and view all the answers

What percentage of India's exported opium was purchased by the United States in 2013?

<p>60% (A)</p> Signup and view all the answers

What is the typical morphine content found in opium cultivated in Afghanistan during the early- to mid-2000s?

<p>14.4% (C)</p> Signup and view all the answers

Which of the following statements about the routes of administration for morphine is accurate?

<p>Morphine can be administered orally, rectally, or parenterally. (D)</p> Signup and view all the answers

What is the primary reason heroin has a greater analgesic effect compared to morphine?

<p>It is more lipid soluble than morphine. (C)</p> Signup and view all the answers

How much dry opium is typically required to produce 1 kg of pure heroin?

<p>10 kg (B)</p> Signup and view all the answers

Which of the following substances is classified as a Schedule I drug in the United States?

<p>Heroin (B)</p> Signup and view all the answers

In comparison to morphine, how does the potency of heroin change due to its chemical structure?

<p>Heroin is significantly more potent due to its increased lipid solubility. (B)</p> Signup and view all the answers

What is a common recreational form of heroin that is known for its sticky texture?

<p>Black tar heroin (A)</p> Signup and view all the answers

Which of the following opioids is not used medically in the United States?

<p>Heroin (A)</p> Signup and view all the answers

What is a key distinction in the administration routes of oxycodone compared to codeine?

<p>Oxycodone can be administered both orally and rectally, while codeine can be administered orally and parenterally. (C)</p> Signup and view all the answers

Flashcards

What is Opium?

Opium is a natural substance derived from the poppy plant, Papaver somniferum, and has been used for medicinal and recreational purposes for thousands of years.

What are Opioids?

Opioids are a class of drugs that bind to opioid receptors in the central nervous system, producing analgesia, euphoria, and other effects. They can be natural, semi-synthetic, or synthetic in origin.

What are Naturally Occurring Opioids?

Naturally occurring opioids, like morphine and codeine, are directly extracted from the poppy plant.

What are Semisynthetic Opioids?

Semisynthetic opioids, such as heroin and oxycodone, are chemically modified versions of natural opioids, resulting in altered pharmacological properties.

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What are Routes of Administration and Pharmacokinetics?

Routes of administration describe how a drug is delivered into the body. Pharmacokinetics describes the drug's movement in the body, including absorption, distribution, metabolism, and elimination.

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What is a Narcotic?

A term used to describe drugs that induce sleep. However, it's often misused and associated with habit-forming substances.

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What is Analgesia?

A loss of sensitivity to pain.

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What is Euphoria?

A state of intense pleasure or euphoria.

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What is Addiction?

A physiological state characterized by tolerance, dependence, and withdrawal symptoms upon discontinuation of the drug.

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What is the history of Opium use?

The opium poppy has been used for medicinal and recreational purposes for thousands of years.

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What is the main active ingredient in Opium?

Opium contains several active constituents, with morphine being the most abundant.

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Who discovered Morphine?

Morphine was first isolated from opium by the German chemist Frederick Sertürner in 1805.

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What is Morphine used for?

Morphine is widely used medically for pain management.

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Who is the main supplier of legal Opium?

India is the largest producer and only licit supplier of opium to the world's market.

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What is Poppy Straw?

Poppy straw, containing active opioid ingredients, is another source of opioids.

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Who produces and exports the most Poppy Straw?

Australia is the leading producer of poppy straw, and the Czech Republic is the main exporter.

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How much Morphine is in Indian Opium?

The opium supplied by India contains morphine in concentrations of about 9.5-12%.

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How are opioids consumed?

Various formulations of morphine and other opioids are used for medical and recreational purposes.

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Morphine Content in Afghan Opium

The percentage of morphine in opium from Afghanistan varied significantly, with an average of 14.4% but some samples containing as low as 5.1% and as high as 24.8%.

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Heroin Synthesis

Heroin is created by adding two acetyl groups to a morphine molecule. This process transforms morphine into a more potent and faster-acting opioid.

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Heroin's Lipid Solubility

Heroin reaches the brain faster than morphine due to its higher lipid solubility, leading to a more intense analgesic effect.

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Heroin's Legal Status in the US

Heroin, unlike morphine, cannot be prescribed medically in the US. It's categorized as a Schedule I drug, meaning it has no accepted medical use and high potential for abuse.

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Opium to Heroin Ratio

About 10 kg of opium is needed to produce just 1 kg of pure heroin. This signifies the significant processing required to extract heroin from its raw source.

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Morphine and Heroin Administration Routes

Morphine is commonly administered orally, rectally, and via injection, while heroin's common routes are injection, snorting, and smoking.

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Codeine vs. Heroin - Medical Usage

Codeine, another opioid, is commonly used in oral medications, while heroin is not prescribed in the United States.

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Heroin Appearance

Common forms of heroin include white or brownish powder and a sticky black substance called 'black tar heroin'.

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Fentanyl Administration Routes

Fentanyl, a highly potent opioid, can be administered orally, intranasally, parenterally, and transdermally.

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Methadone Administration Routes

Methadone, used for opioid addiction treatment, is typically administered orally or by injection.

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What is oxymorphone?

A semisynthetic opioid derived from thebaine, known for its analgesic properties. It is used to treat moderate to severe pain and is available in various formulations, including immediate-release and extended-release tablets.

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What is oxycodone?

A semisynthetic opioid derived from thebaine, widely used to treat moderate to severe pain. It is often combined with non-opioid analgesics like acetaminophen or acetylsalicylic acid.

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What is OxyContin?

A high-dose, controlled-release, long-acting formulation of oxycodone, originally designed for extended pain relief. However, its abuse potential led to reformulations with abuse-deterrent properties.

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What is the new tamper-resistant formulation of OxyContin?

A new formulation of OxyContin designed to prevent abuse by reducing the risk of crushing, snorting, or injecting the drug. It includes features that make it less desirable for non-medical use.

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What is naloxone?

A competitive antagonist of opioid receptors, meaning it blocks the effects of opioids. When combined with oxycodone, it reduces the risk of abuse and decreases gastrointestinal side effects.

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Codeine

A naturally occurring opioid found in opium, used in cough suppressants and painkillers.

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Codeine in OTC meds

Codeine is used in some over-the-counter medications, but is also a target for recreational use.

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Thebaine

Thebaine is a naturally occurring opioid, present in opium but in much smaller quantities than morphine and codeine.

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Poppy Origin

Opioids are derived from poppies, specifically the Papaver somniferum species.

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Morphine Availability

While codeine is used in OTC medications, morphine is only available by prescription.

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Heroin: Illegal Use?

Heroin is a semisynthetic opioid derived from morphine. Its use is illegal in most countries except for restricted medical purposes.

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Heroin's Medical Names

Diacetylmorphine and diamorphine are alternative names for heroin when used in a medical setting.

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Hydrocodone: Most Prescribed

Hydrocodone is a semisynthetic opioid derived from codeine, and is the most commonly prescribed opioid in the United States.

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Codeine Syrup: Recreation

Mixing prescription-strength codeine cough syrup with soda or alcohol creates dangerous and illegal recreational concoctions.

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Codeine Slang

Street names for codeine-based recreational concoctions include "syrup", "sizzurp", "purple drank", and "lean".

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Study Notes

Opioid and Narcotic Drugs

  • Opioids and opiates are often used interchangeably. Opiates refer to naturally occurring opium constituents, while opioids include semisynthetic and fully synthetic substances that bind to opioid receptors.
  • Narcotic analgesics and narcotics are another term for opioids. The term comes from the Medieval Latin "narcoticum," meaning "to make stiff or numb." Technically, a narcotic is a drug that causes sleep, producing analgesia (pain relief) and sleepiness. Acetaminophen and Aspirin are examples of non-narcotic analgesics.
  • The Harrison Narcotic Act of 1914 defined marijuana and cocaine as narcotics, along with opioids. The Narcotic Control Act of 1961 (Canada) regulated habit-forming drugs.
  • The term "narcotic" is avoided. Opioid is used as a more accurate term.

Origins and Sources

  • Papaver somniferum (opium poppy) is the primary natural source of opium. Opium is produced for a short period (10 days) after the petals fall off.
  • Opium is manufactured when opium poppy seedpods are scored to collect the milky fluid (latex).
  • India is the world's largest opium producer. India exports from 300 to 600 tons of opium annually. The largest importing country is the United States, with approximately 60% of India's exports.
  • Bulk of opium is used to extract active ingredients. Other sources include: Poppy straw (all parts except seeds), is another source of active ingredients.
  • Afghanistan, Laos, and Myanmar are major cultivators of illicit opium poppies.

Active Constituents

  • Morphine is the most abundant active constituent of opium and poppy straw. It was first isolated by Frederick Sertürner in 1805.
  • Morphine is used widely in medicine for pain management.
  • The opium from India contains about 9.5 to 12% morphine.
  • Codeine is another opioid, naturally occurring in opium, and manufactured semi-synthetically from morphine. It's an active ingredient in many over-the-counter cough medicines.
  • Other active constituents include: Thebaine, which is used to create other semisynthetic opioids.

Other Opioid Drugs

  • Heroin is a semisynthetic opioid derivative, chemically modifying morphine by adding two acetyl groups.
  • Heroin is more lipid soluble than morphine, reaching the brain more quickly.
  • Other synthetic opioids: Sufentanil, levorphanol, pentazocine, and tramadol.
  • Methadone is a synthetic opioid used as a treatment for opioid addiction. (Methadone is sometimes administered orally, so it's readily available.)
  • OxyContin is a high-dose, controlled-release, orally administered tablet of Oxycodone that is highly susceptible to misuse. (Important to note for potential abuse.)
  • Desmethylprodine (MPPP): A meperidine analog.
  • Carfentanil: An extremely potent fentanyl derivative, used for animal tranquilization, dangerous in high doses to humans.
  • Suboxone: Combines buprenorphine and naloxone and used in opioid maintenance therapy.
  • LAAM: A more recently discontinued opioid maintenance therapy drug.

Routes of Administration

  • Opioid drugs are orally administered as tablets, capsules, and syrups. Other routes include subcutaneous injections, transdermal patches (for prolonged action), intranasal (snorting), smoking, intravenous (IV) injection (for rapid effect).
  • Recreational routes, such as injecting, smoking, or snorting, are common.

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