Pharmacology of Opioids and Analgesics
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Questions and Answers

Which of the following statements about codeine is true?

  • Codeine is used primarily as an antitussive. (correct)
  • Codeine has no risk of respiratory distress.
  • Codeine is a weak opiate antagonist.
  • Codeine is more analgesic than morphine.
  • Opioids only have analgesic properties and do not affect the emotional response to pain.

    False

    Name one opioid antagonist mentioned that can reverse opioid overdose.

    Naloxone

    The opioid receptors targeted by most opioids include mu, delta, and _____ receptors.

    <p>kappa</p> Signup and view all the answers

    What is a significant risk associated with high doses of opioids?

    <p>Respiratory distress</p> Signup and view all the answers

    Match the type of opioid receptor with its effect:

    <p>Mu = Euphoria and analgesia Kappa = Sedation and dysphoria Delta = Antidepressant effects Omega = Pain modulation (not a standard receptor)</p> Signup and view all the answers

    Enkephalins and endorphins are both opioid-like neurotransmitters found in the brain.

    <p>True</p> Signup and view all the answers

    What are two common medical uses for opioids?

    <p>Pain relief, cough suppression</p> Signup and view all the answers

    What is the primary mechanism of action of xanthines?

    <p>They block adenosine receptors in the brain.</p> Signup and view all the answers

    Caffeine always improves cognitive performance in well-rested individuals.

    <p>False</p> Signup and view all the answers

    Name one natural opioid derived from the poppy plant.

    <p>Morphine</p> Signup and view all the answers

    An example of a semisynthetic opioid is __________.

    <p>heroin</p> Signup and view all the answers

    Match the following opioids with their classifications:

    <p>Morphine = Natural opioid Heroin = Semisynthetic opioid Fentanyl = Synthetic opioid Codeine = Natural opioid</p> Signup and view all the answers

    What is the role of opioids as agonists?

    <p>They occupy receptors and activate them.</p> Signup and view all the answers

    What is the main factor considered for the classification of psychedelics?

    <p>Chemical structure</p> Signup and view all the answers

    Antagonists only partially activate receptors.

    <p>False</p> Signup and view all the answers

    Caffeine acts as a __________ by stimulating the central nervous system.

    <p>stimulant</p> Signup and view all the answers

    Withdrawal from opioids is always excruciating.

    <p>False</p> Signup and view all the answers

    Name one example of an indole psychedelic.

    <p>LSD</p> Signup and view all the answers

    The sensation of experiencing sounds as pictures is known as __________.

    <p>synesthesia</p> Signup and view all the answers

    Match the following psychedelics with their chemical structure:

    <p>LSD = Indole MDMA = Catechol Psilocybin = Indole Ketamine = Deliriant</p> Signup and view all the answers

    What is a common misconception about opioid withdrawal?

    <p>You become dependent after one use.</p> Signup and view all the answers

    What is one effect of nicotine on lung health in children?

    <p>Reduced lung functions</p> Signup and view all the answers

    Deliriants cause more mental confusion and clouding of consciousness compared to phantastica.

    <p>True</p> Signup and view all the answers

    What effect do phantastica drugs have on awareness?

    <p>They alter perceptions while allowing communication with the present world.</p> Signup and view all the answers

    The lethal dose of nicotine is approximately 60 mg.

    <p>True</p> Signup and view all the answers

    What is the primary effect of nicotine on the brain?

    <p>Mimics acetylcholine and stimulates receptor sites.</p> Signup and view all the answers

    The active metabolite of nicotine is called _______.

    <p>cotinine</p> Signup and view all the answers

    Which of the following is NOT an effect of nicotine on the circulatory system?

    <p>Decreased blood pressure</p> Signup and view all the answers

    Match the following nicotine effects with their descriptions:

    <p>Stimulant effect = Increases alertness and energy Calming effect = Reduces anxiety Inhibition of hunger = Decreases appetite Increased blood sugar = Provides more energy for the body</p> Signup and view all the answers

    Nicotine replacement therapy eliminates the need for tar and carbon monoxide.

    <p>True</p> Signup and view all the answers

    What happens to the nicotine level in the blood within 24 hours of quitting smoking?

    <p>It drops to zero.</p> Signup and view all the answers

    What is one of the physical effects of LSD?

    <p>Dilated pupils</p> Signup and view all the answers

    The effects of LSD can last up to 12 hours.

    <p>True</p> Signup and view all the answers

    What is the primary active ingredient in psilocybin mushrooms?

    <p>psilocybin</p> Signup and view all the answers

    LSD acts by stimulating the _______ receptors in the brain.

    <p>serotonin-21</p> Signup and view all the answers

    Match the following substances with their primary effects:

    <p>LSD = Hallucinogenic effects Psilocybin = Euphoria and altered perception Mescaline = Similar effects to LSD MDMA = Increased sociability</p> Signup and view all the answers

    Which of the following substances has a half-life of about 6 hours?

    <p>Mescaline</p> Signup and view all the answers

    MDMA primarily acts through serotonin receptors only.

    <p>False</p> Signup and view all the answers

    What common experience may occur as a psychological effect of LSD?

    <p>Synesthesia</p> Signup and view all the answers

    What is the primary receptor that THC predominantly binds to in the brain?

    <p>CB1 receptors</p> Signup and view all the answers

    Oral THC administration leads to a faster onset of effects compared to smoking.

    <p>False</p> Signup and view all the answers

    What are the two types of cannabinoid receptors mentioned in the content?

    <p>CB1 and CB2</p> Signup and view all the answers

    After ingesting THC, effects typically last about _____ hours.

    <p>8-10</p> Signup and view all the answers

    Match the following effects or uses with their corresponding information:

    <p>Anandamide = Endogenous substance isolated from the brain with marijuana-like effects Dronabinol = Oral THC preparation used as an antiemetic Munchies = Increased appetite after cannabis use Bronchodilation = Improvement of airflow in acute marijuana exposure</p> Signup and view all the answers

    What physiological effect is often observed after smoking cannabis?

    <p>Increased heart rate</p> Signup and view all the answers

    Tolerance to THC generally develops after low levels of usage.

    <p>False</p> Signup and view all the answers

    What withdrawal symptoms can occur after cessation of THC use?

    <p>Anxiety, irritability, disrupted sleep</p> Signup and view all the answers

    Study Notes

    Tobacco

    • Psychoactive chemical: Nicotine; safer cigarettes are discussed.
    • Health hazards and carcinogens: Tobacco and smoke affect nearly every body part (mouth, brain, stomach, reproductive system). Hundreds of harmful chemicals, including acetone, ammonia, and hexamine, are present. Cigarette tar, a sticky brown mass from condensed particles, contains carcinogens. Examples of carcinogens and poisonous substances include Benzo(a)pyrene, Nitrosamines, Urethane, Arsenic, and Hydrogen cyanide. Combined with other substances, carcinogens can cause cancer.
    • Smokeless tobacco and e-cigarettes: Smokeless tobacco has warning labels and increases the risk of oral cancer and dental problems. The product contains carcinogens like nitrosamines, which cause leukoplakia. E-cigarettes and health concerns are also noted.

    E-cigarettes

    • Nicotine delivery system: E-cigarettes deliver nicotine and other chemicals in vapor form.

    Long-Term Effects of Smoking

    • Impact on organs: Smoking harms lungs, heart, blood vessels, and other organs.
    • Leading cause of death: Smoking is the most preventable cause of death, with risk increasing more with earlier and longer exposure.
    • Chronic bronchitis: Inflammation of the airways.
    • Blood vessel damage: Nicotine damages blood vessels, leading to plaque buildup.
    • Diabetic effect: Smoking can worsen diabetes by affecting insulin resistance.

    Environmental Tobacco Smoke (ETS)

    • Components: ETS contains mainstream smoke (exhaled by smoker), sidestream smoke (from burning end), and thirdhand smoke (residual chemicals on surfaces).
    • Classification: Environmental tobacco smoke is a Class A carcinogen.
    • Exposure effects: Exposure causes health problems in those around smokers and those who live in the environment of secondhand smokers.

    Nicotine Pharmacology

    • Absorption and metabolism: Nicotine is highly absorbed (90%) when inhaled, deactivated in the liver, and excreted by the kidneys.
    • Tolerance: Nicotine use increases liver enzyme activity, contributing to tolerance and making a lethal dose possible.
    • Half-life: Nicotine has a short half-life (24-84 minutes).
    • Mechanism of action: Nicotine mimics acetylcholine, stimulating and then blocking receptors. It triggers a release of dopamine and adrenaline. It has an indirect sympathomimetic effect

    Quitting Smoking

    • Challenges: Quitting smoking is difficult due to physiological and behavioral effects.
    • Treatments: Treatments such as replacement therapy (gum, patches, inhalers) and pharmacological therapy (bupropion) aid quitting attempts.

    Caffeine

    • Class of chemicals: Caffeine belongs to the xanthine class of chemicals.
    • Sources: Caffeine is present in xanthines, including caffeine, theophylline, and theobromine. These chemicals are found in coffee, tea, and chocolate.
    • Plant sources: These are derived from coffee plants, tea plants, and cacao plants.

    Xanthine Content

    • Coffee content: An average cup of coffee has 90-95 mg of caffeine.
    • Tea content: Tea contains 40-60 mg of caffeine per cup, depending on the type and brew strength.
    • Chocolate content: An average cup of cocoa contains 4 mg caffeine.
    • Theophylline and theobromine: Theophylline is mainly found in tea, and used as an asthma medication. Theobromine is present in chocolate and is less potent than caffeine.

    Caffeine Pharmacology

    • CNS and cardiovascular effects: Caffeine is a stimulant. Theophylline and theobromine are the most potent cardiac stimulants; caffeine has less effect.
    • Time course: Fast absorption, peak levels in 30 minutes, half-life about 3 hours (short duration of action)
    • Withdrawal symptoms: Withdrawal symptoms include fatigue and headache.
    • DSM-5: Caffeine is not officially listed as a substance use disorder in DSM-5.
    • Mechanism of action: Xanthines block adenosine receptors in the brain, which also have a calming effect. A decrease in adenosine release results in stimulation
    • Physiological effects: Caffeine and other xanthines stimulate the CNS, skeletal muscles, and can cause sleep disturbances and constrict blood vessels.
    • Cognitive effects: Caffeine can partially counter the effects of fatigue, although it does not improve performance in well-rested individuals.

    Opioids

    • Naturally occurring substance: Derived from the opium poppy plant.
    • Analgesic and anesthetic: Provides pain relief, pleasure, and anxiety relief.
    • Mechanism of action: Bind to opioid receptors in the brain (mu, delta and kappa) affecting pain and emotional centers.
    • Classification: Opioids are categorized as natural (morphine, codeine, thebaine), semi-synthetic (heroin, oxymorphone, hydromorphone) and synthetic (meperidine, methadone, morphinians, benzamorphans).
    • Agonists & antagonists: Agonists activate receptors; antagonists block them.

    Opioid Examples (Morphine, Codeine, Heroin, Fentanyl)

    • Opiate & opioid action: Opiates are generally natural and the first connection to the plant. Opioids are a broad category of drugs with natural and synthetic members.
    • Potency: Morphine is 10 times more potent than opium.
    • Uses: Clinically useful strong analgesic, addictive potential.
    • Codeine: Less analgesic strength than morphine, is an antitussive. High doses can cause respiration problems and death.
    • Misconceptions: Withdrawing is typically described as excruciating-similar to a mild case of the intestinal flu; after one injection, dependence is not necessarily immediate.

    Mechanism of Action on the Brain, Opioid Receptors, and Antagonists

    • Brain mechanisms: Opioids and related compounds function by binding to receptors in the brain and glands (enkephalins & endorphins).
    • Specific receptors & Neurotransmitters: Targeting mu, delta, and kappa opioid receptors. Interfering with GABA & norepinephrine receptors is a common target..

    Acute and Chronic Opioid Toxicity and Misuse

    • Acute toxicity: Opioids cause respiratory depression, and sometimes nausea and vomiting.
    • Chronic toxicity: Injection and use leads to spread of blood-borne diseases.
    • Tolerance: Higher doses needed to maintain effects.
    • Physical dependence: withdrawal is unpleasant, but not life-threatening. Can be prevented with opioid agonists.
    • Psychological dependence: Positive and negative reinforcement related to drug use. Psychological issues are often associated with overuse.
    • Misconceptions: Withdrawal issues can range from mild to intense, requiring professional guidance. Dependence can occur quickly.

    Psychedelics

    • Alter perceptions and moods: Oldest known drugs that change how the brain perceives and acts.
    • Medical uses: Used to treat mental health illnesses (LSD, psilocybin, MDMA).
    • Chemical groups: Belong to indole chemical groups, with examples including LSD, psilocybin, and MDMA.
    • Brain activity effects: Altered levels of serotonin play a significant role in how the brain works, creating synesthesia (sound perceived as colors etc) or confusion.
    • Factors for classification Include chemical structure and pharmacological properties, comparing relative dangers, and how severe hallucinations or other effects are.

    Phantastica and Deliriants

    • Phantastica: Allow user to communicate with the present world while altering perceptions. LSD, psilocybin, mescaline, and MDMA are in this category.
    • Deliriants: Lead to mental confusion and reality distortion. PCP and ketamine are examples of deliriants.

    Mechanism of action(LSD, Psilocybin, Mescaline, MDMA)

    • Physical Effects: Dilated pupils, increased body temperature, increased heart rate, and blood pressure.
    • Psychological effects: Feelings of spiritual connection, terrifying thoughts and sensations (synesthesia, or crossing over of senses).
    • Mechanism of action: Stimulates serotonin-21 receptors in the brain, impacting dopamine and norepinephrine receptors and other neurotransmitters, like glutamate.

    Cannabis

    • Derived from cannabis plants: Chemicals in cannabis plants can be used for medicinal substances. Marijuana is a type of processed preparation from leafy material of the plant.
    • THC: A dominant chemical component in marijuana, causing psychoactive effects and is one of the reasons marijuana is considered a schedule 1 drug.
    • Cannabinoids: A group of psychoactive ingredients.
    • CBD: Does not create feelings of "high" but has various medicinal uses like relieving pain, being neuroprotective, and other applications.
    • THC Pharmacology & time-course: Oral and smoked THC differ in absorption speed and duration of effects. THC is metabolized in the liver.
    • Mechanism of action: THC binds to CB1 and CB2 receptors in the brain triggering anandamine production in the brain.

    Medical Uses of Marijuana and Physiological Effects

    • Effective medicine: Safe and effective medicine for various conditions including nausea and appetite stimulation..
    • Physiological effects: Increased heart rate, reddened eyes, dryness, munchies (increased appetite), and elevated mood (euphoria). Duration of effects may vary with methods of consumption.

    Abuse Potential and Dependence

    • Different time course: Different methods of using THC have differing impact duration and effects.
    • Tolerance: Repeated exposure can increase tolerance, leading to needing higher doses to experience a similar effect.
    • Withdrawals: Withdrawals are typically not life-threatening but may be unpleasant and include anxiety and irritability. The duration can last from a day to 12 days.
    • Acute/chronic effects: Increased heart rate , lung damage (impaired air flow), lower sperm counts in men and lower birth rates in women. Some associated risks for those with existing conditions like cardiovascular disease.

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    Test your knowledge on the pharmacology of opioids and their effects. This quiz covers the classification, mechanisms, and risks associated with opioid use, as well as related substances like xanthines. Perfect for students in pharmacology or healthcare fields!

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