UNIT 9: DRUG OF ABUSE Flashcards
Drugs that activate G-protein-coupled receptors (GCPRs)
Class 1
Drugs that bind to ionotropic receptors or ion channels
Class 2
Drugs that bind to biogenic amine transporters
Class 3
Enumeration
Class 1 Drugs
Opioids
Cannabinoids
THC
GHB
LSD
Mescaline
Psilocybin
Enumeration
Class 2 Drugs
Benzodiazepines
Nicotine
Ethanol
Alcohol
Ketamine
PCP
Inhalants
Enumeration
Class 3 Drugs
Cocaine
Amphetamine
Ecstacy (MDMA)
Strong analgesics, narcotic
Opioids
Naturally-occuring alkaloids
Opiates
Enumeration
Opiates
Morphine
Codeine
Thebaine
Papaverine
Enumeration
Opioid receptor subtypes
μ (mu)
δ (delta)
κ (kappa)
This opioid receptor subtype causes inhibition of respiration
μ (mu)
Which opioid receptor subtype has a strong affinity to Dynorphins
κ (kappa)
This opioid receptor subtype causes psychotomimetic effects and slowed gastrointestinal transit
κ (kappa)
Natural painkillers in the body with varying affinity to the three types of opioid receptors
Endogenous peptides
The following acts as agonists of the κ (kappa) receptor, except one:
Morphine
Sufentanil
Butorphanol
Nalbuphine
Buprenorphine
Pentazocine
Buprenorphine
Antagonist
Opium is derived from
Scientific name
Papaver somniferum
The principal active ingredient of opium
Morphine
The only antagonist of the μ (mu) receptor
Nalbuphine
Powerful narcotic that causes histamine release
Opium
Smack
H
Ska
Junk
Heroin
Street drug of abuse of opioids
Heroin
An addictive drug as a white or brown powder, IV injected
Heroin
Half-life of Heroin
3-5 hours
Withdrawal time of Heroin
5-10 hours after
Oxycodone is synthesized from ____ and derived from ____
Thebaine, Codeine
Enumeration
Opioids
Opium
Heroin
Oxycodone
Meperidine
Serious interaction with MAOs, can result in MPTP which can cause parkinsonism
Meperidine
Opioid receptors block ____ channels in the dorsal horn
Ca+ channels
Postsynaptically, opioids can inhibit the pain stimulus by enhancing the ____ conductance
K+ conductance
The mechanism of action of opioids involve preventing the release of what neurotransmitters?
Glutamate, Neuropeptides
True or False
The principal effects of opioid analgesics with affinity for mu receptors are on the PNS
False
CNS
Effect of opioids that develops a moderate degree of tolerance
Bradycardia
Slow heart rate
Adverse effects of opioid analgesics can be reversed by
Naloxone
Which drug group results in this interaction with opioids:
Increased CNS depression, particularly respiratory depression
Sedative-hypnotics
Which drug group results in this interaction with opioids:
Increased sedation, Accenuation of cardiovascular effects
Antipsychotic agents
Which drug group results in this interaction with opioids:
High incidence of hyperpyrexic coma and reported hypertension
Monoamine oxidase inhibitors
Which drug group is relatively contraindicated to all opioid analgesics?
Monoamine oxidase inhibitors
Enumeration
Sedative-hypnotics
Alcohol
Barbituates
Benzodiazepines
Gamma-hydroxybutyric acid (GHB)
True or False
Sedative-hypnotics can be short or long-acting
True
Used to be called “Physical Dependence”
Dependence
Used to be called “Psychological Dependence”
Addiction
Hallmark of addiction
Compulsive
Repetitive exposure induces widespread adaptive changes in the brain. What effect of DOA is this?
Altered perception
A combination of signs that defines dependence
Withdrawal Syndrome
Consists of compulsive, relapsing drug use despite negative consequences, at times triggered by cravings that occur in response to contextual cues
Addiction
True or False
Dependence is not always a correlate of drug abuse—it can also occur with many classes of nonpsychoactive drugs
True
Dependence or Addiction
Physical
Dependence
Dependence or Addiction
Tolerance
Dependence
Dependence or Addiction
Psychological
Addiction
Dependence or Addiction
Withdrawal Syndrome
Dependence
Dependence or Addiction
Compulsion
Addiction
Dependence or Addiction
Relapsing
Addiction
Dependence or Addiction
Non-psychoactive drugs
Dependence
Dependence or Addiction
Craving
Addiction
The prime target of addictive drugs
Mesolimbic Dopamine System
True or False
Each addictive drug activates the mesolimbic system via its specific molecular target, engaging distinct cellular mechanisms to increase dopamine levels.
True
Dopamine pathway functions (5)
Reward (motivation)
Pleasure, euphoria
Motor function (fine tuning)
Compulsion
Perseveration
Which class of drugs directly stimulates the dopamine neurons?
Class 2 (Class 1 sa book)
Nicotine
Which class interferes with the reuptake of dopamine or promotes nonvesicular release?
Class 3 (Class 2 sa book)
Cocaine, Amphetamines (respectively)
Which class uses an indirect mechanism, whereby the drugs inhibit γ-aminobutyric acid (GABA) neurons that act as local inhibitory interneurons?
Class 1 (Class 3 sa book)
Opioids, Cannabis
Drugs That Activate G Protein–Coupled Receptors
Opioids
Cannabinoids
γ-Hydroxybutyric acid (GHB)
LSD, mescaline, psilocybin
Drugs That Activate G Protein–Coupled Receptors
Main molecular target of Opioids
μ-OR (Gio)
Drugs That Activate G Protein–Coupled Receptors
Main molecular target of Cannabinoids
CB1R (Gio)
Drugs That Activate G Protein–Coupled Receptors
Main molecular target of γ-Hydroxybutyric acid (GHB)
GABABR (Gio)
Drugs That Activate G Protein–Coupled Receptors
Main molecular target of LSD, mescaline, psilocybin
5-HT2AR (Gq)
Drugs That Bind to Ionotropic Receptors and Ion Channels
Main molecular target of Nicotine
nAChR (α4β2)
Drugs That Bind to Ionotropic Receptors and Ion Channels
Main molecular target of Alcohol
GABAAR, 5-HT3R, nAChR, NMDAR, Kir3 channels
Drugs That Bind to Ionotropic Receptors and Ion Channels
Main molecular target of Benzodiazepines
GABAAR
Drugs That Bind to Ionotropic Receptors and Ion Channels
Main molecular target of Phencyclidine, Ketamine
NMDAR
Drugs That Bind to Transporters of Biogenic Amines
Main molecular target of Cocaine
DAT, SERT, NET
Drugs That Bind to Transporters of Biogenic Amines
Main molecular target of Amphetamine
DAT, NET, SERT, VMAT
Drugs That Bind to Transporters of Biogenic Amines
Main molecular target of Ecstasy
SERT > DAT, NET
Drugs That Activate G Protein–Coupled Receptors
Opioids
Pharmacology
Agonist
Drugs That Activate G Protein–Coupled Receptors
Cannabinoids
Pharmacology
Agonist
Drugs That Activate G Protein–Coupled Receptors
γ-Hydroxybutyric acid (GHB)
Pharmacology
Weak Agonist
Drugs That Activate G Protein–Coupled Receptors
LSD, mescaline, psilocybin
Pharmacology
Partial Agonist
Drugs That Bind to Ionotropic Receptors and Ion Channels
Nicotine
Pharmacology
Agonist
Drugs That Bind to Ionotropic Receptors and Ion Channels
Benzodiazepines
Pharmacology
Positive Modulator
Drugs That Bind to Ionotropic Receptors and Ion Channels
Phencyclidine
Pharmacology
Antagonist
Drugs That Bind to Ionotropic Receptors and Ion Channels
Ketamine
Pharmacology
Antagonist
Drugs That Bind to Transporters of Biogenic Amines
Cocaine
Pharmacology
Inhibitor
Drugs That Bind to Transporters of Biogenic Amines
Ecstasy
Pharmacology
Reverses transport
Drugs That Bind to Transporters of Biogenic Amines
Amphetamine
Pharmacology
Reverses transport
Drugs That Activate G Protein–Coupled Receptors
Disinhibition
Effect on Dopamine (DA) Neurons
Opioids
Cannabinoids
γ-Hydroxybutyric acid (GHB)
Drugs That Bind to Ionotropic Receptors and Ion Channels
Nicotine
Effect on Dopamine (DA) Neurons
Excitation
Drugs That Bind to Ionotropic Receptors and Ion Channels
Alcohol
Effect on Dopamine (DA) Neurons
Excitation, Disinhibition
Drugs That Bind to Ionotropic Receptors and Ion Channels
Benzodiazepines
Effect on Dopamine (DA) Neurons
Disinhibition
Drugs That Bind to Transporters of Biogenic Amines
Cocaine
Effect on Dopamine (DA) Neurons
Blocks DA uptake
Drugs That Bind to Transporters of Biogenic Amines
Amphetamine
Effect on Dopamine (DA) Neurons
Blocks DA uptake
Synaptic depletion
Drugs That Bind to Transporters of Biogenic Amines
Ecstasy
Effect on Dopamine (DA) Neurons
Blocks DA uptake
Synaptic depletion
Serious side effect of Tolerance
Respiratory Depression
True or False
Tolerance to opioids may be due to an increase of the concentration of a drug or a longer duration of action in a target system (pharmacokinetic tolerance)
False
Reduction of concentration, not increase; shorter duration of action
Regulation Schedules
High potential for abuse
No known medical use
Lacks accepted safety for use
Eg, Heroin, Lysergic acid diethylamide
Schedule I
Regulation Schedules
Potential for abuse
Proven and accepted medical use with severe restrictions
Abuse may cause severe psycho/physio dependence
Eg, Morphine, Cocaine, Methadone, Methampetamine, Phencyclidine
Schedule II
Regulation Schedules
Less potential for abuse
With accepted medical use
Abuse may cause moderate or low physical dependence or high psychological dependence
Eg, Anabolic steroids, Codeine and hydrocodone with aspirin or Tylenol
Schedule III
Regulation Schedules
Low potential for abuse
Abuse may lead to limited physical or psychological dependence
Eg, Valium and Xanax
Schedule IV
Regulation Schedules
Low potential for abuse relative to drugs in Schedule IV
Eg, Cough syrups and Codeine
Schedule V
Pharmacokinetic or Pharmacodynamic Tolerance
Reduction of Concentration
Pharmacokinetic Tolerance
Pharmacokinetic or Pharmacodynamic Tolerance
Shorter duration of action
Pharmacokinetic Tolerance