8.1: Drug of Abuse Flashcards
- No medical indication
- Abuse vs Misuse
- Euphoria
- Altered perception
- “Compulsive” 🡪 Addiction
Drug of Abuse
Identify if Dependence or Addiction:
- Physical
- Tolerance
- Withdrawal Syndrome
Dependence
Identify if Dependence or Addiction:
- Psychological
- Compulsion
- Relapsing
- Craving
Addiction
Identify what Regulation Schedule:
High potential for abuse, no known medical use and lacks accepted safety for use.
Schedule I
What are the examples of Schedule I?
- Heroin
- Lysergic acid diethylamide
Identify what 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
What are the examples of Schedule II?
- Morphine
- Cocaine
- Methadone
- Methampetamine
- Phencyclidine
MoCoMeMeP
Identify what Regulation Schedule:
- Less potential for abuse than schedule I or II; with accepted medical use
- Abuse may cause moderate or low physical dependence or high psychological dependence
Schedule III
Regulation Schedule:
What are the examples of Schedule III?
- Anabolic steroids
- Codeine with hydrocodone
- Aspirin or Tylenol
Identify what Regulation Schedule:
- The drug or other substance has a low potential for abuse relative to the drugs or other substances in Schedule III
- Abuse of the drug or other substance may lead to limited physical dependence or psychological dependence relative to the drugs or other substances in Schedule III
Schedule IV
What are the examples of Schedule IV?
- Valium
- Xanax
Identify what 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:
What are the examples of Schedule V?
- Cough syrups
- Codeine
What are the pharmacokinetic tolerance?
- Reduction of concentration
- Shorter duration of action
What are the pharmacodynamic tolerance?
- Recruitment of Adaptor protein (β-arrestin)
- Desensitization
- Receptor internalization
Enumerate the withdrawal symptoms:
- Restlessness
- Eating more than usual
- Excessive hunger
- Anxiety/tension
- Impatience
- Depression
- Disorientation
- Loss of energy/fatigue
- Tremors
- Craving for cigarettes
This is a high motivation to obtain and use and has a negative consequences.
Addiction
They revert back because of the environment and drug availability. It has re-exposure, stress, and context recall.
Relapse
This alter perception and has no reward/euphoria. It targets cortical and thalamic system.
Nonaddictive Drug of Abuse
Examples of nonaddictive drug of abuse:
- Hallucinogens
- Dissociative anesthetics
- LSD
- PCP/Ketamine
- Dextromethorphan
What are the Class I drugs that Activate G-protein coupled receptors?
- GHB
- LSD, Mescaline & Psilocybin
- Opioids
- Cannabinoids
GLOC :3
What are the Class II drugs that Bind to Ionotropic receptors?
- Nicotine
- Benzodiazepines
- Alcohol
- Ketamine & PCP
- Inhalants
NiBAKIn
What are the Class III Drugs that Bind to Transporters of Biogenic Amines?
- Cocaine
- Amphetamines
- Ecstasy (MDMA)
Identify this nonaddictive drug abuse:
- Strong analgesics
- Opiates – morphine, codeine, thebaine, papaverine
- Narcotic – “sleep inducing”
- Leads to respiratory arrest
Opioids
Identify the opioid receptor subtypes:
- Supraspinal and spinal analgesia
- Sedation
- Inhibition of respiration
- Slowed gastrointestinal transit
- Modulation of hormone and neurotransmitter release
µ (mu)
Identify the opioid receptor subtypes:
- Supraspinal and spinal analgesia
- Modulation of hormone and neurotransmitter release
δ (delta)
Identify the opioid receptor:
- Supraspinal and spinal analgesia
- Psychotomimetic effects
- Slowed gastrointestinal transit
κ (kappa)
What are the common opioid analgesics that are strong agonist (+++,++, ++)?
- Morphine
- Oxycodone
- Hydromorphone
- Oxymorphone
- Methadone
- Meperidine
- Fentanyl
- Sufentanil
- Alfentanil
- Remifentanil
- Levorphanol
MOHOMMFeSARL :D
What are the common opioid analgesics that are partial or weak agonist (±)?
- Buprenorphine
- Butorphanol
- Codeine
- Hydrocodone
- Pentazocine
BuBuCoHyP :P
What are the common opioid analgesics that are antagonist (-)?
Nalbuphine
Plant source of opioids:
Papaver somniferum
True or False:
Opioids is a powerful narcotic painkiller where the principal active ingredient is morphine.
True
Mode of administration of opioids:
Subcutaneous, Intravenous
Effects of opioids:
Insomnia, hallucination, nightmares
True or False:
Opioids is a histamine release and have more pronounced effects than heroin.
True
It is a diamorphine addictive drug as a white or brown powder that tends to be used with other drugs.
Heroin
Mode of administration of Heroin:
Fast-acting; Intravenous
What is the half-life of heroin?
3-5 hours, several doses per day
Hours of withdrawal of heroin:
5-10 hours after
It is derived from codeine and synthesized from thebaine. This type of drug is in tablet or oral form.
Oxycodone
This type of drug has a serious interaction with MAO’s, and has resulted in MPTP which can cause parkinsonism.
Meperidine (pethidine; Demerol)
Degrees of tolerance:
What are the effects of high degree of opioid efficacy?
- Analgesia
- Euphoria, dysphoria
- Mental clouding
- Sedation
- Respiratory depression
- Antidiuresis
- Nausea and vomiting
- Cough suppression
Degree of tolerance:
What are the effects of moderate degree of opioid efficacy?
Bradycardia
Degrees of tolerance:
What are the effects of minimal or none degree of opioid efficacy?
- Miosis
- Constipation
- Convulsions
What are the adverse effects of opioid analgesics in acute use?
- Respiratory depression
- Nausea/vomiting
- Pruritus
- Urticaria
- Constipation
- Urinary retention
- Delirium
- Sedation
- Myoclonus
- Seizures
What are the adverse effects of opioid analgesics in chronic use?
- Hypogonadism
- Immunosuppression
- Increased feeding
- Increased growth hormone secretion
- Withdrawal effects
- Tolerance, dependence
- Hyperalgesia
- Impairment while driving
Identify what drug group based on the interaction with opioids
Increased CNS depression, particularly respiratory depression.
Sedative-hypnotics
Identify what drug group based on the interaction with opioids:
Increased sedation, variable effects on respiratory depression. Accentuation of cardiovascular effects (antimuscarinic and α-blocking actions).
Antipsychotic agents
Identify what drug group based on the interaction with opioids:
Relative contraindication to all opioid analgesics because of the high incidence of hyperpyrexic coma; hypertension is also reported.
Monoamine oxidase inhibitors
Identify the opioid drug interaction
- alcohol, barbiturates, benzodiazepines, gamma-hydroxybutyric acid (GHB)
- can be short- to long-acting
- the longer the duration the less the withdrawal
- anxiety, tremors, twitches, vomiting
Sedative-hypnotics
Clinical uses of sedative-hypnotics:
- Relief of anxiety
- Insomnia
- Sedation and amnesia before and during medical and surgical procedures
- Treatment of epilepsy and seizure states
- Component of balanced anesthesia (IV administration)
- Control of ethanol or other sedative-hypnotic withdrawal states
- Muscle relaxation in specific neuromuscular disorders
- Diagnostic aids or for treatment in psychiatry
Identifythis nonaddictive drug use:
- rare occurrence of physiologic dependence
- “Therapeutic Dose Dependence”
- weight loss, change in perception, paresthesia, headache
Benzodiazepines
What type of benzodiazepine drug is used for date rape and has a Schedule IV and anterograde amnesia?
Flunitrazepam (Rohypnol)
- GABAa receptors
- usually short-acting drugs
- not used as much as other drugs
Barbiturates
Example of drugs of barbiturates:
Secobarbital, pentobarbital Na
Identify this non-addictive drug of abuse:
- euphoria
- Alcoholism
- Affect GABAa and NMDA
- withdrawal (motor agitation, anxiety, insomnia, hallucination, abnormal vital signs, seizures)
Alcohol
Identify this nonaddictive drug abuse:
- GABAb
- naturally found in body
- can be found in fermented drinks like guava (Psidium guajava)
- euphoric, sedative, anabolic
- widely sold until 1992
- liquid ecstasy, soap, easy lay, vita-G
- Georgia homeboy
- use with alcohol can produce breathing problems
Gamma Hydroxybutyric Acid
What are the withdrawal effects of Gamma Hydroxybutyric Acid?
Insomnia, anxiety, tremors, sweating
What is the treatment for short and long acting drugs?
Chlordiazepoxide or Phenobarbital
What is the treatment for alcohol?
Disulfiram, naltrexone
Plant source of Cannabinoids:
Cannabis sativa
Identify this nonaddictive of abuse:
- CB1 receptors
- Can be smoked or joined with ingredients in making brownies or fermented products (beer)
- Effects in 2-3 inhalations (“high,” euphoria, laughter, relaxation)
- Schedule I
Cannabinoids
Identify this drug:
- Antiemetic
- tolerance
- uncertain effect on fetus
- Amotivational syndrome
- diseases related to smoking
Marijuana
Examples of Cannabinoids:
- Dronabinol
- Nabilone (chemotherapy)
- Nabiximol (MS)
What are the four hallucinogens that cause hallucinations?
- LSP
- PCP
- Ketamine
- Scopolamine
Plant source of LSD:
Claviceps purpurea
Identify what hallucinogens:
- synthetic agent related to ergot alkaloids
- NE, dopamine, serotonin
- 5-HT1a & 5-HT1c agonists
- one of the most potent drugs 1ug/kg
- absence of known fatalities
- duration based on dose
- waxing and waning effects
LSD (Lysergic acid diethylamide)
Identify what Hallucinogen based on its effects:
- rise in body temp
- Hallucinations
- uterine contractions
- elevated sugar levels
- goosebumps
- Euphoria
- pupil dilation
Lysergic acid diethylamide (LSD)
Plant source of Mescaline:
Lophophora williamsii
Identify what hallucinogens:
- restricted but allowed occasionally to North American Indians
- 5-6mg/kg
Mescaline
Identify what hallucinogen:
- 250ug/kg
- mydriasis, muscle relaxation, dizziness
Psilocybin
Plant source of Psilocybin:
Psilocybe mushroom
Identify what hallucinogen:
- anesthetic
- “special K” “vitamin K”
- dream-like states, hallucination, delirium, amnesia, high BP, depression,
- fatal respiratory problems
Ketamine
Identify what hallucinogen:
- veterinary anesthetic
- smoked with tobacco, snorted
- MOA: Oral, IV
- antagonize NMDA
- animals will self administer it
- Olney’s lesions
- long t1/2
- users tend to be violent and suicidal
- “bad-trips”
Phencyclidine (angel dust, PCP)
Plant source of Scopolamine:
Hyoscyamus niger
Identify what hallucinogen:
- block central muscarinic receptors
- unpleasant to users
- same effects as other hallucinogen
- “Devil’s breath”
Scopolamine
Plant source of Cocaine:
Erythroxylon coca
Identify what hallucinogen:
- dopaminergic reuptake transmitter
- inhibit reuptake of dopamine and NE
- free base is absorbed as fast as IV
- t1/2= 1hr, repeated 30min
Cocaine
Identify what hallucinogen based on its effects:
- symptoms include a feeling of bugs under skin
- paranoia and schizophrenia like state
- exhaustion by lack of sleep and food appetite, exhaustion, depression
Cocaine
Identify what hallucinogen:
- increase catecholinergic neurotransmitters
- dopamine not be metabolized thus released
- treat narcolepsy and ADHD
- paranoid psychosis
- necrotizing arteritis
- OD is rarely fatal
- managed by benzodiazepines
Amphetamines
alpha-methyl-phenethylamine
Identify what hallucinogen:
- Schedule II
- decreased appetite, increase stamina, energy sexual drive
- loss of REM sleep, tremor, restlessness, anxiety,
- related drugs (shabu, ecstasy)
Amphetamines
What are the drugs that targets the NMDA receptor antagonist?
Phencyclidine, ketamine
What is the drug that targets acetylcholine receptor agonist (nAChr)?
Nicotine
What are the drugs that reverses transport of serotonin receptor (SERT) > dopamine receptor (DAT) and norepinephrine receptor (NET)?
Ecstasy
What is the drug that inhibits dopamine receptor (DAT), serotonin receptor (SERT), and norepinephrine receptor (NET)?
Cocaine
What is the drugs that reverses transport of dopamine receptor (DAT), norepinephrine receptor (NET), serotonin receptor (SERT), and vesicular monoamine transporter (VMAT)?
Amphetamine
What is the drug that targets the GABAa receptor positive modulator?
Benzodiazepines
What is the drug that targets the GABAa receptor positive modulator, 5-HT3 receptor, nAChR, NMDAR, Kir3 channels?
Alcohol
What is the drug that targets 5-HT(2A)R partial agonist?
LSD, mescaline, psilocybin
What is the drug that targets μ (Mu) receptor agonist?
Opioids
What is the drug that targets CB1 receptor agonist?
Cannabinoids
What is the drug that targets GABAb receptor weak agonist?
γ-Hydroxybutyric acid (GHB)
Identify this substance of abuse:
- “uppers”
- reverse the effects of fatigue on both mental and physical tasks.
- Nicotine - tobacco products
- Caffeine - coffee, tea, some soft drinks, and many non-prescription medicines
Stimulants
Plant source of Nicotine:
Nicotiana tobacum
Identify this substance of abuse:
- nicotinic cholinergic receptor agonist
- 1 drop is fatal
- strong psychological and physiological dependence (more addictive than heroin and cocaine)
- dopamine
- SIDS, carcinogenic
Nicotine
Identify this substance of abuse:
- adenosine receptors
- low chance of abuse and addiction
- 5 cups/ day
Caffeine (1, 3, 7-trimethylxanthine)
Identify this substance of abuse:
- anesthetic gases
- industrial solvents
- aerosol propellants
- organic nitrites
Inhalants
Identify this substance of abuse:
- psychoactive effects
- alcohol-like intoxications, hallucinations,
- hypoxia, pneumonia, cardiac failure
- headache, nausea, vomiting, slurred speech, loss of motor coordination, wheezing
Inhalants
Identify this substance of abuse:
- difficulty in concentrating, dreaminess, euphoria, numbness, tingling
- N2O = 35% used; 100% death
- ether & chloroform
Anesthetics
Identify this substance of abuse:
- gasoline, toluene, benzene, trichloro-ethylene
- 5-15min
- euphoria, “drunk” feeling, disorientation (slow passage of time)
- Eg. Glue, correction fluid, gas
Industrial solvents
Identify this substance of abuse:
- amyl nitrite, isobutyl nitrite
- dizziness, rapid heart rate, lowered BP, “speeding,” flushing of skin
- enhance, prolong erection
Organic nitrites
Identify this substance of abuse:
- Liver, kidney, peripheral nerve, and brain damage
- bone marrow suppression
- pulmonary disease
- death
Toxicities
Identify this substance of abuse:
- cyclopentanoperhydrophenanthrene ring
- bone growth, appetite, puberty, muscle growth
- Schedule III
- change in libido, irritability, violence, mood swings, forgetfulness, confusion
- fatigue, depressed mood, craving for steroids
Anabolic Steroids
Identify this substance of abuse:
- hypertrophied muscles, acne, oily skin, hirsutism in females, gynecomastia in males, needle punctures
- high LDL; low HDL
- elevated liver function
Anabolic Steroids
A nonselective antagonist drug that is used for opioid overdose.
Naloxone
An antagonist drug that is used for treatment for alcoholism, opioid addiction.
Naltrexone
A slow-acting agonist of μ-opioid receptor that is used for substitution therapy for opioid addicts.
Methadone
An “enantiopure” methadone containing only the left-enantiomer of the molecule that is used for substitution therapy.
Levomethadone
A salt containing morphine sulfate pentahydrate that is used for substitution therapy.
Morphine sulphate
A partial agonist at μ-opioid receptors that is used for oral substitution therapy for opioid addicts.
Buprenorphine
A partial agonist of nicotinic acetylcholine receptor that is used for smoking cessation.
Varenicline
A positive modulator of the GABAa receptors that increases frequency of channel opening and is used for delirium tremens.
Oxazepam
An antagonist of NMDA glutamate receptors that is used for treatment of alcoholism.
Acamprosate
A CB1 receptor inverse antagonist drug that is used to treat obesity but withdrawn, smoking cessation but not approved, but remains an off-label indication.
Rimonabant
An agonist melatonin receptor hypnotic drugs that is used for patients who have difficulty in falling asleep, and is located in the suprachiasmatic nuclei of the brain.
Ramelteon
A 5-HT receptor partial agonist drug that has a slow-onset of anxiolytic effects and has a minimal psychomotor impairment.
Buspirone
An orexin antagonist that blocks the binding of orexins, neuropeptides that promote wakefulness.
Suvorexant
Newer hypnotics that bind selectively to GABAa subgroup receotors, acting like Benzodiazepines to enhance membrane hyperpolarization.
- Eszopiclone
- Zaleplon
- Zolpidem
Barbiturate drugs that is a dose-dependent depressant effects on the CNS and has a steeper dose-response relationship than Benzodiazepines.
- Amorbital
- Butabarbital
- Mephobarbital
- Pentobarbital
- Phenobarbital
- Secobarbital
An antagonist drug at benzodiazepine-binding sites on the GABAa receptor.
Flumazenil
Benzodiazepine drugs that is a dose-dependent depressant effects on the CNS.
- Alprazolam
- Chlordiazepoxide
- Clonazepam
- Clorazepate
- Diazepam
- Estazolam
- Fluazepam
- Lorazepam
- Midazolam
- Oxazepam
- Quazepam
- Temazepam
- Triazolam
bwct basta puro am last
A barbiturate drug that is lipid-soluble, intravenous administration, and use for the induction of anesthesia.
Thiopental and methohexital