Sedative-Hypnotic Drugs and Opioid Analgesics
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Questions and Answers

Which of the following drugs is most commonly associated with rapid tolerance and dependence when administered intravenously?

  • Fentanyl
  • Morphine
  • Heroin (correct)
  • Codeine
  • Kratom has well-defined opioid effects and is widely prescribed as a treatment option.

    False

    What is the primary treatment for an opioid overdose?

    Naloxone

    The withdrawal effects of opioids are characterized by symptoms such as lacrimation, yawning, and __________.

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

    Match the following opioid analgesics with their common misuse forms:

    <p>Heroin = Injectable or smoked Morphine = Pill form or injectable Oxycodone = Pill form Fentanyl = Patch or injectable</p> Signup and view all the answers

    What is a common effect following the initial 'rush' experienced from IV heroin?

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

    Amphetamines only have stimulant effects that lead to increased appetite and sleepiness during withdrawal.

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

    Which opioid is known for its long half-life and is used for withdrawal symptoms?

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

    Which drug is commonly known as 'angel dust'?

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

    Which of the following drugs is noted for having amnestic properties and is associated with 'date rape'?

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

    MDMA has no effect on serotonin transporters in the central nervous system.

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

    What are the active compounds found in marijuana?

    <p>THC, CBD, and CBN</p> Signup and view all the answers

    Ethanol is classified as a controlled substance with known abuse liability.

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

    ______ and other muscarinic agents may have hallucinogenic effects.

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

    What primary neurotransmitter is facilitated by sedative-hypnotic drugs in the brain?

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

    Match the following hallucinogens with their common names:

    <p>2,5-dimethoxy-4-methylamphetamine = DOM Methylene dioxymethaphetamine = MDMA (Ecstasy) Lysergic acid diethylamide = LSD Mescaline = Psychedelic Cactus</p> Signup and view all the answers

    Sedative-hypnotic drugs reduce inhibitions, suppress anxiety, and produce __________.

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

    Which of the following is NOT a cannabinoid compound?

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

    Match the following drugs with their properties:

    <p>Alprazolam = Short-acting benzodiazepine with high addiction potential Secobarbital = Short-acting barbiturate with high addiction potential Flumazenil = Antidote for benzodiazepine overdose Ethanol = Heavily abused substance not listed as a controlled drug</p> Signup and view all the answers

    Overdose with PCP can lead to horizontal and vertical nystagmus.

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

    What is a significant effect of acute overdoses of sedative-hypnotic drugs?

    <p>Death due to respiratory and cardiovascular depression</p> Signup and view all the answers

    Flumazenil is used as an antidote for both barbiturate and benzodiazepine overdoses.

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

    What is the effect of THC on the central nervous system?

    <p>Feeling of being 'high', euphoria, and changes in perception</p> Signup and view all the answers

    What type of receptors do sedative-hypnotic drugs antagonize to achieve their effects?

    <p>Cholinergic nicotinic receptors</p> Signup and view all the answers

    What is one of the potential therapeutic effects of marijuana?

    <p>Decrease in intraocular pressure</p> Signup and view all the answers

    Chronic use of marijuana does not have implications for cognitive impairment.

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

    What substances are included in Dronabinol?

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

    Inhalation of nitrous oxide without oxygen can lead to ______.

    <p>asphyxia and death</p> Signup and view all the answers

    Match each inhalant with its potential effect:

    <p>Nitrous oxide = Euphoria and disinhibition Chloroform = Loss of consciousness Benzene = Toxic to the liver Amyl nitrate = Dizziness and tachycardia</p> Signup and view all the answers

    Which of the following statements is true regarding anabolic steroids?

    <p>They are controlled substances due to potential for abuse.</p> Signup and view all the answers

    CBD has addictive properties.

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

    What is Sativex composed of?

    <p>THC and CBD</p> Signup and view all the answers

    Which of the following drugs is most commonly associated with respiratory depression when overdosed?

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

    Opioid analgesics are known for causing euphoria followed by sedation when administered intravenously.

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

    What is the primary management for opioid overdose?

    <p>Naloxone or nalmefene</p> Signup and view all the answers

    The sensation of 'cold turkey' is associated with opioid withdrawal and is characterized by ______.

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

    Match the following opioids to their common effects:

    <p>Fentanyl = High efficacy and low cost Methadone = Used for withdrawal treatment Heroin = Euphoria followed by sedation Kratom = Poorly defined opioid effects</p> Signup and view all the answers

    Which symptom is NOT typically associated with opioid withdrawal?

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

    Chronic use of amphetamines can lead to marked tolerance and an increase in appetite during withdrawal.

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

    What type of therapy is buprenorphine used for in opioid addiction?

    <p>Substitution therapy</p> Signup and view all the answers

    Opioid overdose can lead to ______, coma, and death.

    <p>respiratory depression</p> Signup and view all the answers

    Match the following opioid analgesics with their common forms of misuse:

    <p>Heroin = Injection Oxycodone = Pill form abuse Codeine = Cough syrup abuse Fentanyl = Illegal patches</p> Signup and view all the answers

    Which hallucinogen is known as 'angel dust'?

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

    Marijuana primarily acts on dopaminergic pathways in the brain.

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

    What are the psychoactive compounds in marijuana?

    <p>THC, CBD, CBN</p> Signup and view all the answers

    PCP overdose can lead to horizontal and vertical __________.

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

    Match the following drugs with their classifications:

    <p>MDMA = Ecstasy LSD = Hallucinogen MDA = Congener of amphetamines Ketamine = Dissociative anesthetic</p> Signup and view all the answers

    Which of the following compounds is primarily responsible for the psychoactive effects of marijuana?

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

    Cannabinoids have no known therapeutic effects.

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

    What is the proposed effect of MDMA on interpersonal communication?

    <p>Facilitates interpersonal communication</p> Signup and view all the answers

    The endogenous cannabinoids in the CNS include __________ and 2-arachidonyl glycerol.

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

    Which effect is commonly associated with the use of PCP?

    <p>Impaired judgment</p> Signup and view all the answers

    Which sedative-hypnotic drug is known for its high addiction potential when used long-term?

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

    Ethanol is categorized as a controlled substance with known abuse liability.

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

    What is the primary neurotransmitter facilitated by sedative-hypnotic drugs in the brain?

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

    The acute overdoses of sedative-hypnotic drugs can result in __________.

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

    Match the sedative-hypnotic drug with its property:

    <p>Alprazolam = High addiction potential when used long-term Flumazenil = Reverses CNS depressant effects of BDZs Secobarbital = Short-acting barbiturate with abuse potential Ethanol = Heavily abused but not a controlled substance</p> Signup and view all the answers

    Which drug is associated with 'date rape' due to its amnestic properties?

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

    Benzodiazepines are classified as schedule IV drugs with low abuse liability.

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

    What is one method of managing an overdose of benzodiazepines?

    <p>Maintenance of patient airway and ventilatory support</p> Signup and view all the answers

    Sedative-hypnotic drugs are known to reduce inhibitions, suppress anxiety, and produce __________.

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

    Which of the following is not a method to reverse the effects of a barbiturate overdose?

    <p>There is no antidote</p> Signup and view all the answers

    What is one of the therapeutic effects of marijuana?

    <p>Decreases intraocular pressure</p> Signup and view all the answers

    Chronic use of marijuana is associated with cognitive impairment.

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

    What substance is associated with impaired judgment and reflexes when used?

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

    The active ingredient in the controlled-substance formulation of THC is __________.

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

    Match the following inhalants with their potential effects:

    <p>Nitrous oxide = Euphoria and loss of consciousness Benzene = Toxic to the liver and kidneys Amyl nitrate = Dizziness and tachycardia Chloroform = Loss of consciousness and potential asphyxia</p> Signup and view all the answers

    Which of the following is NOT a potential adverse effect of anabolic steroids?

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

    CBD has been approved for specific types of epilepsy and has addictive properties.

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

    What is the name of the botanical drug containing both THC and CBD?

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

    Chronic use of inhalants may lead to toxicity affecting the __________ system.

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

    Which of the following inhalants is recognized for causing asphyxia when inhaled as a pure gas?

    <p>Nitrous oxide</p> Signup and view all the answers

    Study Notes

    Sedative-Hypnotic Drugs

    • Commonly Prescribed: Benzodiazepines (BDZs) for anxiety, categorized as Schedule IV with low abuse liability.
    • High Addiction Potential: Short-acting BDZs like alprazolam and short-acting barbiturates like secobarbital have high addiction potential with long-term use.
    • Ethanol: Ethanol, though not listed on the schedule of controlled substances, has high abuse liability.
    • Actions: Reduce inhibitions, suppress anxiety, and produce relaxation, potentially leading to repetitive use. Facilitate GABA effects, antagonize cholinergic nicotinic receptors, and enhance brain dopaminergic pathways (likely related to addiction).
    • Overdose: Commonly results in death due to depression of the medullary respiratory and cardiovascular centers.
    • Management of Overdose: Maintaining airway and ventilatory support, Flumazenil to reverse BDZ effects, no antidote for barbiturates or ethanol.

    Opioid Analgesics

    • Pharmacologic Action: Primarily act on opioid receptors, also disinhibit dopaminergic pathways in the CNS.
    • Most Commonly Abused: Heroin, morphine, codeine, oxycodone, hydrocodone, hydromorphone, meperidine, fentanyl.
    • Effects: IV heroin results in a "rush" followed by euphoria and sedation. IV administration leads to rapid tolerance, dependence, and addiction. Oral administration/smoking provides milder effects and slower onset of tolerance and dependence.
    • Fentanyl Crisis: High efficacy, abundance, and low cost contribute to a current fentanyl crisis.
    • Overdose: Respiratory depression, coma, and death. Managed with naloxone or nalmefene and ventilatory support.
    • Kratom: Crude plant extract with poorly defined opioid effects, misused due to OTC availability.
    • Withdrawal Effects: Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh (cold turkey), nausea, vomiting, tremor, muscle jerks.
    • Treatment: Replacement with a pharmacologically active equivalent, e.g., methadone, followed by slow dose reduction. Buprenorphine (partial agonist at µ-receptors) is also used for withdrawal symptoms and substitution therapy.

    Stimulants - Amphetamines

    • CNS Alteration: Alter amine transporter activity in the CNS, increasing dopamine, norepinephrine, and serotonin release, leading to feelings of euphoria and self-confidence and rapid addiction.
    • Drugs Included: Dextroamphetamine, methamphetamine ("speed"), crystal form (“ice”) that can be smoked.
    • Chronic Abuse: Leads to a psychotic state with delusions and paranoia.
    • Overdose Symptoms: Agitation, restlessness, tachycardia, hyperthermia, hyperreflexia, and possible seizures. No antidote; supportive care focuses on temperature control, arrhythmia prevention, and seizure management.
    • Tolerance: Marked, withdrawal symptoms include increased appetite, sleepiness, exhaustion, and mental depression.
    • Congeners: 2,5-dimethoxy-4-methylamphetamine (DOM[STP]), dioxymethaphetamines (MDA), methylene dioxymethaphetamines (MDMA, ecstasy).
    • MDMA: Selective serotonin transporter in the CNS, purportedly facilitating interpersonal communication and acting as a sexual enhancer.

    Hallucinogens

    • PCP and Ketamine: Antagonists at the glutamate NMDA receptor with no action on dopaminergic neurons.
    • Common Psychotic Reactions: Impaired judgment often leading to reckless behavior.
    • Overdose: Horizontal and vertical nystagmus, marked HTN, and fatal seizures. Diazepam or lorazepam used to curb excitation and prevent seizures.
    • Other Hallucinogenic Drugs: LSD, mescaline, psilocybin.
    • Scopolamine and Muscarinic Agents: Act on serotonin receptors, indirectly increase glutamate receptor release, no dependence, and do not act on dopaminergic pathways.
    • Descriptive Terms: Psychedelic and mind revealing.

    Marijuana

    • Active Principles: Cannabinoid compounds - tetrahydrocannabinol (THC), cannabidiol (CBD), cannabinol (CBN).
    • Subspecies: Hemp plant (low THC, high CBD), medical marijuana plants (higher THC vs CBD levels).
    • Hashish: Partially purified THC-containing material with higher potency.
    • Endogenous Cannabinoids: Anandamide and 2-arachidonyl glycerol act as retrograde messengers to inhibit presynaptic release of dopamine.
    • Exogenous Cannabinoid Targets: Receptors for endogenous cannabinoids are thought to be the targets for exogenous cannabinoids in marijuana.
    • CNS Effects: Euphoria, disinhibition, uncontrollable laughter, perceptual changes, dream-like state due to THC at the CB1 receptor.
    • Mental Concentration: Difficult.
    • Vasodilation: Increases pulse rate.
    • Habitual Users: Reddened conjunctiva.
    • Withdrawal States: Experienced by heavy users.
    • Dangers: Impaired judgment and reflexes, effects potentiated by sedative-hypnotics, including ethanol.
    • Chronic Use: Cognitive impairment, cannabis use disorder, hyperemesis.
    • Therapeutic Effects: Lower intraocular pressure, analgesic effects, antiemetic action.
    • Preparations: Dronabinol (THC), Nabilone (synthetic THC) for nausea and pain management. Nabiximols (Sativex) (THC and CBD) for specific types of epilepsy.
    • CBD: No addictive properties.
    • Rimonabant: Inverse agonist at CB1 receptors for obesity treatment in Europe but withdrawn.

    Inhalants

    • Euphoric and Disinhibitory Effects: Gases or volatile liquids.
    • Anesthetics: Nitrous oxide, chloroform, diethyl ether - affect judgment and induce loss of consciousness.
    • Nitrous Oxide Asphyxia: Asphyxia and death without oxygen.
    • Industrial Solvents: Gasoline, paint thinners, aerosol propellants, glues, rubber cement, shoe polish.
    • Active Ingredients: Benzene, hexane, methylethylketone, toluene, trichloroethylene.
    • Toxicity: Liver, kidneys, lungs, bone marrow, and peripheral nerves.

    Organic Nitrates

    • Nitrites: Amyl nitrate, isobutyl nitrite ("poppers") - used as sexual enhancers.
    • Inhalation Effects: Dizziness, tachycardia, hypertension, flushing.

    Steroids

    • Controlled Substances: Anabolic steroids due to abuse potential in many countries.
    • Effects: Increased muscle mass and strength, rather than euphoria.
    • Excessive Use: Adverse behavioral, cardiovascular (MI), and musculoskeletal effects.
    • Androgenic Side Effects: Acne and masculinization in females.

    Sedative-Hypnotic Drugs

    • Includes benzodiazepines (BDZs), barbiturates, and ethanol
    • BDZs are commonly prescribed for anxiety and are classified as Schedule IV, indicating a low potential for abuse
    • Short-acting BDZs like alprazolam have a high potential for addiction when used long-term
    • Short-acting barbiturates, like secobarbital, have a similar high potential for addiction
    • Ethanol is not listed on the schedule of controlled substances with abuse liability, but is heavily abused
    • These drugs reduce inhibitions, suppress anxiety, and produce relaxation, encouraging repetitive use
    • Primary actions: facilitates GABA effects, antagonizes cholinergic nicotinic receptors
    • Enhances brain dopaminergic pathways, a factor potentially linked to addiction
    • CNS depressants, effects are enhanced by concomitant use of ethanol, opioids, analgesics, antipsychotic agents, marijuana, and other drugs with sedative properties
    • Acute overdoses can lead to death due to the depression of the medullary respiratory and cardiovascular centers
    • Treatment of overdose: maintain patient airway and ventilatory support
    • Flumazenil is used to reverse the CNS depressant effects of BDZs
    • No antidote for barbiturates or ethanol
    • Flunitrazepam (Rohypnol) is a potent, fast-acting BDZ with amnestic properties, used in "date rape"
    • Rohypnol is often added to alcoholic beverages, chloral hydrate or GHB in sufficient doses, rendering the victim incapable of resisting rape

    Opioid Analgesics

    • Opioids act mainly on opioid receptors
    • Other actions include disinhibition of dopaminergic pathways in the CNS
    • Most commonly abused drugs: Heroin, Morphine, Codeine, Oxycodone, hydrocodone, hydromorphone, Meperidine, Fentanyl
    • IV heroin effects are described as a "rush" or organic feeling followed by euphoria and sedation
    • IV administration of opioids results in rapidly developing tolerance, dependence, and addiction
    • Oral administration/smoking produce milder effects with slower onset of tolerance and dependence
    • Fentanyl's high efficacy, abundance, and low cost resulted in a fentanyl crisis
    • Overdose of opioids leads to respiratory depression, coma, and death
    • Overdose is managed with parenteral naloxone or nalmefene and ventilatory support
    • Kratom, a crude plant extract with poorly defined opioid effects, has been misused because it is available as an OTC botanical
    • Opioid withdrawal effects (abstinence syndrome): lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh ('cold turkey'), nausea, vomiting, tremor, muscle jerks
    • Treatment includes replacing illicit drugs with pharmacologically active equivalent agents like methadone, followed by slow dose reduction
    • Buprenorphine, a partial agonist at µ-receptors and a longer-acting opioid (t1/2 >40hrs) is also used for withdrawal symptoms and substitution therapy for opioid addicts

    Stimulants - Amphetamines

    • Alter amine transporter activity in the CNS (dopamine, norepinephrine, and serotonin) increasing their release
    • Feelings of euphoria and self-confidence contribute to the rapid development of addiction
    • Drugs include: Dextroamphetamine, Methamphetamine ('speed'), and a crystal form ("ice") that can be smoked
    • Chronic high-dose abuse leads to a psychotic state with delusions and paranoia
    • Overdose symptoms: agitation, restlessness, tachycardia, hyperthermia, hyperreflexia and possible seizures
    • No antidote, supportive care involves controlling body temperature, protecting against cardiac arrhythmias and seizures
    • Tolerance can be marked, withdrawal symptoms include increased appetite, sleepiness, exhaustion, and mental depression
    • Amphetamine congeners: 2,5-dimethoxy-4-methylamphetamine (DOM[STP]), dioxymethaphetamines (MDA), methylene dioxymethaphetamines (MDMA, ecstasy)
    • MDMA selectively acts on serotonin transporters in the CNS, purportedly facilitating interpersonal communication and acting as a sexual enhancer

    Hallucinogens

    • Phencyclidine (PCP) ('angel dust') and ketamine ('special K'): antagonists at the glutamate NMDA receptor
    • No action on dopaminergic neurons in the brain
    • Psychotic reactions are common with PCP, impaired judgment often leads to reckless behavior
    • PCP Overdose: horizontal and vertical nystagmus, marked HTN, and seizures, potentially fatal
    • Parenteral BDZs (diazepam, lorazepam) are used to curb excitation and protect against seizures
    • Other hallucinogenic drugs with abuse potential: lysergic acid diethylamide (LSD), mescaline, psilocybin
    • Scopolamine and other muscarinic agents may have hallucinogenic properties
    • Act on serotonin receptors and indirectly increase glutamate receptor release in the CNS, not known to cause dependence or act on dopaminergic pathways
    • Terms used to describe these drugs: psychedelic and mind-revealing

    Marijuana

    • Marijuana ('grass' or 'pot'): a collective term for the psychoactive constituents in crude extracts of the plant Cannabis sativa and Cannabis indica
    • Active principles include cannabinoid compounds: tetrahydrocannabinol (THC), cannabidiol (CBD), and cannabinol (CBN)
    • Cannabis sativa has subspecies: hemp plant (low THC and high CBD) and medical marijuana flowering/bud plants (generally higher THC vs CBD levels)
    • Hashish is partially purified THC-containing material that is more potent
    • Endogenous cannabinoids in the CNS (anandamide and 2-arachidonyl glycerol) are released postsynaptically and act as retrograde messengers to inhibit presynaptic release of conventional transmitters like dopamine
    • The receptors for these endogenous compounds are believed to be the targets for exogenous cannabinoids present in marijuana

    Effects of Marijuana

    • CNS effects: feeling of being "high" with euphoria, disinhibition, uncontrollable laughter, changes in perception, and a dream-like state
    • These effects are attributed to THC on the cannabinoid type-1 (CB1) receptor
    • Mental concentration is difficult
    • Vasodilation and increased pulse rate
    • Habitual users often have reddened conjunctiva
    • Withdrawal states are noted in heavy users
    • Dangers: impairment of judgment and reflexes
    • Effects are potentiated by concomitant use of sedative-hypnotics, including ethanol
    • Chronic use is associated with cognitive impairment, cannabis use disorder, and hyperemesis
    • Perceived risk of automobile accidents, roadside tests for "driving while high"
    • Potential therapeutic effects: decrease intraocular pressure, analgesic effects, antiemetic action

    Preparations

    • Dronabinol: a controlled-substance formulation of THC, used to combat severe nausea and as an adjunct for chronic pain
    • Nabilone: a synthetic analogue of THC, used to combat severe nausea and as an adjunct for chronic pain
    • Nabiximols (Sativex): a botanical drug composed of THC and CBD
    • CBD has recently been approved for specific types of epilepsy but lacks any addictive properties
    • Rimonabant: an inverse agonist at CB1 receptors, approved for use in treating obesity in Europe, but has been withdrawn

    Inhalants

    • Certain gases or volatile liquids are abused for their euphoric and disinhibitory effects
    • Anesthetics: nitrous oxide, chloroform, diethyl ether
    • Affect judgment and induce loss of consciousness
    • Inhalation of nitrous oxide as a pure gas (without oxygen) has caused asphyxia and death

    Industrial Solvents

    • Solvents and a wide range of volatile compounds found in commercial products like gasoline, paint thinners, aerosol propellants, glues, rubber cement, and shoe polish
    • Active ingredients: benzene, hexane, methylethylketone, toluene, and trichloroethylene
    • Many of these compounds are toxic to the liver, kidneys, lungs, bone marrow, and peripheral nerves

    Organic Nitrates

    • Amyl nitrate, isobutyl nitrite, and other organic nitrites referred to as "poppers" are used as sexual intercourse enhancers
    • Inhalation of nitrites causes dizziness, tachycardia, hypertension, and flushing

    Steroids

    • Anabolic steroids are controlled substances in many countries due to their potential for abuse
    • Effects sought by abusers: increased muscle mass and strength rather than euphoria
    • Excessive use: adverse behavioral, CV (MI), and musculoskeletal effects
    • Acne (sometimes severe) and masculinization in females are anticipated androgenic adverse effects

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