U8.1.1 DRUG OF ABUSE Flashcards
Dependence / Addiction
Physical, Tolerance
Dependence
T/F Drugs of Abuse has no no medical indication
T
Dependence / Addiction
Withdrawal Syndrome, Non-psychoactive drugs
Dependence
Dependence / Addiction
Psychological, Compulsion
Addiction
Dependence / Addiction
Relapsing, Craving
Addiction
Mesolimbic Dopamine System
reward neurotransmitter
Dopamine
Mesolimbic Dopamine System
for reward, pleasure, euphoria, motor function, compulsion & perseveration
Dopamine
Mesolimbic Dopamine System (Class Type)
Target GPCRs - G protein coupled receptors
Class 1
Mesolimbic Dopamine System (Class Type)
Opioids, THC, GHB, Cannabinoids, LSD, Mescaline, Psilocybi
Class 1
Mesolimbic Dopamine System (Class Type)
Target ion channels
Class 2
Mesolimbic Dopamine System (Class Type)
Drugs that bind to Ionotropic receptors
Class 2
Mesolimbic Dopamine System (Class Type)
Benzodiazepines, Nicotine, Ethanol, Alcohol, Ketamine & PCP, Inhalants
Class 2
Mesolimbic Dopamine System (Class Type)
Drugs that Bind to Transporters of Biogenic Amines
Class 3
Mesolimbic Dopamine System (Class Type)
Targets transporters which are post-protein receptors that transports for recycling or for storage of our neurotransmitters
Class 3
Mesolimbic Dopamine System (Class Type)
Cocaine, Amphetamine, Ecstasy (MDMA)
Class 3
T/F Drugs have different schedules on how they can be regulated legally for each drug
F
Regulation Schedule
High potential for abuse, no known medical use and lacks accepted safety for use
Schedule I
Regulation Schedule
Heroin, Lyserg ic acid diethylamide
Schedule I
Regulation Schedule
Potential for abuse with proven and accepted medical use but WITH SEVERE RESTRICTIONS, because abuse may cause severe psycho/physio dependence
Schedule II
Regulation Schedule
morphine, cocaine, methadone, methampetamine, phencyclidine
Schedule II
Regulation Schedule
Less potential for abuse than schedule I or II; with accepted medical use
Schedule III
Regulation Schedule
Abuse may cause moderate or low physical dependence or high psychological dependence
Schedule III
Regulation Schedule
Anabolic steroids, codeine and hydrocodone, with aspirin or Tylenol
Schedule III
Regulation Schedule
The drug or other substance has a low potential for abuse relative to the drugs or other substances in Schedule III
Schedule IV
Regulation Schedule
Abuse of the drug or other substance may lead to limited physical dependence or psycholog ical dependence relative to the drugs or other substances in Schedule III
Schedule IV
Regulation Schedule
Valium and Xanax
Schedule IV
Regulation Schedule
The drug or other substance has a low potential for abuse relative to the drugs or other substances in Schedule IV
Schedule V
Regulation Schedule
Cough syrups and codeine
Schedule V
Tolerance
Reduction of concentration
Pharmacokinetic Tolerance
Tolerance
Shorter duration of action
Pharmacokinetic Tolerance
Tolerance
Recruitment of Adaptor protein (β-arrestin)
Pharmacodynamic Tolerance
Tolerance
Desensitization
Pharmacodynamic Tolerance
Tolerance
Receptor internalization
Pharmacodynamic Tolerance
Counter-regulatory system in our body
Withdrawal Symptoms
- High motivation to obtain and use
- Negative consequences
Addiction
Addiction
Re-exposure, Stress, Context recall
Relapse
- Alter perception; no reward/euphoria
- Targets cortical and thalamic system
Non addictive Drug Abuse
Type of Non-addictive Drug
Opioids, Cannabinoids, GHB, LSD, Mescaline, & Psilocybin
Drugs that Activate G-protein coupled receptors
Type of Non-addictive Drug
Nicotine, Benzodiazepines, Alcohol, Ketamine & PCP, Inhalants
Drugs that Bind to Ionotropic receptors
Type of Non-addictive Drug
Coccaine, Amphetamines, Ecstasy (MDMA)
Drugs that Bind to Transporters of Biogenic Amines
Type of Drug
- Strong analgesics
- Narcotic – “sleep inducing”
Opioids
Type of Drug
Opiates – morphine, codeine, thebaine, papaverine
Opioids
Opioid receptor subtype
Supraspinal and spinal analgesia; sedation; inhibition of respiration; slowed gastrointestinal transit; modulation of hormone and neurotransmitter release
μ (mu)
Opioid receptor subtype
Endorphins > enkephalins > dynorphins
μ (mu)
Opioid receptor subtype
Supraspinal and spinal analgesia; modulation of hormone and neurotransmitter release
δ (delta)
Opioid receptor subtype
Enkephalins > endorphins and dynorphins
δ (delta)
Opioid receptor subtype
Supraspinal and spinal analgesia; psychotomimetic effects; slowed gastrointestinal transit
κ (kappa)
Opioid receptor subtype
Dynorphins > > endorphins and enkephalins
κ (kappa)
Opioid receptor subtype
Among the 3, the very important is the ____ receptor subtype that can cause inhibition of respiration
μ (mu)
Type of Drug
- Papaver somniferum
- powerful narcotic,
painkiller principal active ingredient is MORPHINE
Opioids
Type of Drug
Insomnia, hallucination, nightmares
Opioids
Type of Drug
More pronounced e ects than heroin
Opioids
Type of Drug
Smack, H, ska, junk
Heroin
Type of Drug
- An addictive drug as a white or brown powder
- Tends to be used with other drugs
Heroin
Type of Drug
- T1/2= 3-5 hrs, therefore several doses/ day
- Withdrawal symptoms 5-10 hrs after
Heroin
Type of Drug
- One of the componenrts of some cough syrups
- synthesized from thebaine
Oxycodone
Type of Drug
- derived from codeine
- tablet or oral form
- increasingly popular
Oxycodone
Type of Drug
pethidine; Demerol
Meperidine
Type of Drug
serious interaction with MAO’s
Meperidine
Type of Drug
attempts to illicitly produce meperidine has resulted
in MPTP which can cause parkinsonism
Meperidine
Opioid drug interactions (Drug Group)
Increased central nervous system depression, particularly respiratory depression.
Sedative- hypnotics
Opioid drug interactions (Drug Group)
Relative contraindication to all opioid analgesics because of the high incidence of hyperpyrexic coma; hypertension has also been reported.
Monoamine oxidase inhibitors
Opioid drug interactions (Drug Group)
Increased sedation. Variable effects on respiratory depression. Accentuation of cardiovascular effects (antimuscarinic and α-blocking actions).
Antipsychotic agents
Type of Drugs
Alcohol, barbiturates, benzodiazepines, gamma-hydroxybutyric acid (GHB)
Sedative - hypnotics
Type of Drug
- Can be short- to long- acting
- The longer the duration the less the withdrawal
Sedative - hypnotics
Type of Drug
Anxiety, tremors, twitches, vomiting
Sedative - hypnotics
Type of Drug
Rare occurrence of physiologic dependence
Benzodiazepines
Type of Drug
- “Therapeutic Dose Dependence”
- weight loss, change in perception, paresthesia, headache
Benzodiazepines
Type of Drug
- used for date rape
- causes Anterograde amnesia
Flunitrazepam
Type of Drug
- GABAa receptors
- usually Short- acting drugs
Barbiturates
Type of Drug
Secobarbital, pentobarbital Na
Barbiturates
Type of Drug
Euphoria, Alcoholism, A ffect GABAa and NMDA
Alcohol
Type of Drug
Withdrawal : motor agitation, anxiety, insomnia, hallucination, abnormal vital signs, Seizures
Alcohol
Type of Drug
- GABAb
- Naturally found in body
Gamma Hydroxybutyric Acid
Type of Drug
- Can be found in fermented drinks like guava
(Psidium guajava) - Euphoric, sedative, anabolic
Gamma Hydroxybutyric Acid
Type of Drug
Component of liquid ecstasy, soap, easy lay, vita-G
Gamma Hydroxybutyric Acid
Type of Drug
Use with alcohol can produce breathing problems
Gamma Hydroxybutyric Acid
Type of Drug
Withdrawal eff ects include insomnia, anxiety, tremors, sweating
Gamma Hydroxybutyric Acid
Treatment
For Short acting and Long acting drugs
chlordiazepoxide or phenobarbital
Treatment
For alcohol
disulfiram, naltrexone
Type of Drug
Marijuana Cannabis sativa
Cannabinoids
Type of Drug (Cannabinoids)
Tetrahydrocannabinol (is the one that is addictive), cannabinol and cannabidiol (already approved for ADHD, cerebral palsy etc.)
Marijuana
Type of Drug (Cannabinoids)
- Cannabinoid receptors (CB1), separate receptor
- Can be Smoked or joined with ingredients in making brownies or fermented products (beer)
Marijuana
Type of Drug (Cannabinoids)
- Eff ects in 2-3 inhalations
Marijuana
Type of Drug (Cannabinoids)
Antiemetic, Tolerance, uncertain e ect on fetus, Amotivational syndrome, diseases related to smoking
Marijuana
Type of Drug (Cannabinoids)
for chemotherapy patients
Nabilone
Type of Drug (Cannabinoids)
used for MS (Multiple Sclerosis)
Nabiximol
Type of Drug Group
Marijuana, Dronabinol, Nabilone, Nabiximol
Cannabinoids
Antidote/Medication to GABAb
Phenobarbital
Benzodiazepine toxicity/overdose
can be reversed by
Flumazenil
