UNIT 12: DRUG OF ABUSE AND SUBSTANCE OF ABUSE Flashcards
drugs and substances that are actually
used not of their medical purpose
Drugs of Abuse
“compulsive seeking” of the use
of a drug
Addiction
the term used when the purpose for which drugs are used are not approved by the FDA
“off the label”
the body needs
the drug for it to function
Physical (Dependence)
there would be an increasing concentration for an
individual to achieve the desired effect
Tolerance (Dependence)
negative consequences caused by abrupt termination of the effects of drugs
Withdrawal Syndrome (Dependence)
drugs that do not alter perception
Non-psychoactive drugs
Reduction of concentration
Shorter duration of action
Pharmacokinetic Tolerance
Recruitment of Adaptor Protein (β-arrestin)
Desensitization
Receptor internalization
Pharmacodynamic Tolerance
drugs that alter perception
no reward/euphoria
Nonaddictive drug of abuse
targets of nonaddictive drug of abuse
Cortical and Thalamic System
would be binding to certain G-protein coupled receptors; includes Opioids, Cannabinoids and γ-Hydroxybutyric acid (GHB)
Class 1
would usually bind to ion channels; includes Benzodiazepines, Ethanol, and Nicotine
Class 2
would bind to transporters of Biogenic
Amines; includes Cocaine, Amphetamine, and
Ecstasy
Class 3
Morphine
Papaverine
Codeine
Thebiane
Opiates (naturally occurring alkaloids)
Strong analgesics (painkillers) and narcotics
Opioids
Opioid receptor subtypes
μ (mu), δ (delta), and κ (kappa)
Scientific name of poppy plant
Papaver somniferum
Principal active ingredient of Opium
Morphine
MOA of Opium
SC and IV
Type of Opioid used for cancer pain and post-surgical pain
Opium
Released by Opium
Histamine
Other names for Heroin
Smack, H, ska, junk
Diamorphine drug
Heroin
an addictive drug as a white or brown powder
tends to be used with other drugs
Heroin
MOA of Heroin
IV
t1/2 of Heroin
3-5 hrs
withdrawal effects of heroin can be observed ____ hrs after
5-10
street drug of abuse; non-medical
Heroin
Oxycodone is synthesized from ________
Thebaine
Oxycodone is derived from _______
Codeine
MOA of Oxycodone
Oral (tablet/component of cough syrup)
pethidine; demerol
Meperidine
Strong analgesic for post-surgery
Meperidine
Meperidine can have serious interaction with ________
MAOs
attempts to illicitly produce meperidine has resulted in _______ which can cause _________
MPTP: methyl-phenyl-tetrahydropyridine; parkinsonism
Respiratory depression can be reversed by ________
Naloxone
Adverse effect if chronic opioid use wherein non-painful stimulus may be perceived as pain
Hyperalgesia
Increased central nervous system (CNS) depression, particularly respiratory depression
Sedative-hypnotics
Increased sedation
Variable effects on respiratory depression
Accentuation of cardiovascular effects
(Antimuscarinic alpha-blocking actions)
Antipsychotic agents
Relative contraindication to all opioid analgesics because of the high incidence of hyperpyrexic coma; hypertension has also been reported.
Monoamine oxidase inhibitors
Anxiolytics
Can be short to long- acting sedatives
Sedative-Hypnotics
Examples of Sedative-Hypnotics
Alcohol
Barbiturates
Benzodiazepines
Gamma-hydroxybutyric acid (GHB)
SH used for treatment of epilepsy and seizure states in children
Phenobarbital
Rare occurrence of physiologic dependence
“Therapeutic dose dependence”
Benzodiazepines
Used for date rape
Schedule IV
anterograde amnesia
Flunitrazepam
Target of Barbiturates
GABAa receptors
Barbiturates that are not used anymore due to their unpredictable effect
Secobarbital, pentobarbital Na
Target of Alcohol
GABAa and NMDA
Target of Gamma Hydroxybutyric Acid
GABAb
Naturally found in the body
Can be found in fermented drinks like guava
Gamma Hydroxybutyric Acid
other names for Gamma Hydroxybutyric Acid
Liquid ecstasy, soap, easy lay, vita-G
Georgia homeboy
When used with _______, GHB can produce breathing problems
Alcohol
Treatment for short acting and long acting drugs
Chlordiazepoxide or phenobarbital
Treatment for alcohol
disulfiram and naltrexone
Scientific name for Marijuana
Cannabis sativa
Components of Cannabinoids
Cannabinol, Cannabidiol, and Tetrahydrocannabinol (THC)
Addictive component of Cannabinoid
tetrahydrocannabinol or THC
Target of Cannabinoids
Cannabinoid receptors (CB1)
FDA Approved Cannabinoids
Dronabitol, Nabilone, and Nabiximol
This is used for certain muscle diseases and even ADHD
Cannabinoids
Substances that cause hallucination (auditory, visual and tactile)
Hallucinogens
Types of Hallucinogens
LSD, PCP, Ketamine, and Scopolamine
Part of the brain where pain stimulus is interpreted
Somatosensory Cortex
Meaning of MOR
mu Opioid Receptor
SHs are conjugated to a more _____-soluble state to be excreted via urine
water
Binding site of Benzodiazepines and Flumazenil
Alpha receptors of GABA
Antidote to Benzodiazepines
Flumazenil
SH with a distinct binding site
Cannot be reversed by Flumazenil
Barbiturates
Synthetic agent related to ergot alkaloids
Lysergic Acid Diethylamide
Neurotransmitters affected by LSD
NE, Dopamine, and Serotonin
LSDs are agonists of ____ and ____
5-HT1a and 5HT1c (serotonin receptors)
One of the most potent drugs (1µg/kg) with no known fatalities
Lysergic Acid Diethylamide
Effects of LSD
Waxing and Waning
Scientific name for Mescaline
Lophophora williamsii
Dose of Mescaline
5-6 mg/kg
Restricted but allowed occasionally to North American Indians as herbal medicine
Mescaline
Scientific name of Psilocybin
Psilocybe mushroom
Dose of psilocybin
250 µg/kg
Effects of Psilocybin
Mydriasis, muscle relaxation, dizziness
Anesthetic used before for race horses
Ketamine
Other names for Ketamine
Special K
Vitamin K
Hallucinogen that causes fatal respiratory problems
Ketamine
Other names for Phencyclidine
Angel dust
PCP
PCP is a __________ derivative
Phenylcyclohexylamine
Veterinary anesthetic
PCP
MOA of PCP
Smoked with tobacco, snorted, Oral, IV
Lesions caused by PCP
Olney’s lesions (in nasal mucosa)
Users tend to be violent and suicidal; “Bad-trips”
PCP
Scopolamine is derived from the plant ___________
Hyoscyamus niger
PCP antagonizes _____
NMDA
Blocked by Scopolamine
Central Muscarinic Receptors
Other name for Scopolamine
Devil’s breath
produces anterograde anemia similar to benzodiazepine rohypnol
Scopolamine
Cocaine is derived from the plant ________
Erythroxylon coca
Cocaine affects the transport of ________
Amines
Also known as “crack” because of the crackling sound when it is melted
Cocaine
Dopaminergic reuptake transmitter
Cocaine
Inhibit reuptake of dopamine and NE
Cocaine
Half life of Cocaine
1 hr
Symptoms include a feeling of bugs under skin
Cocaine
Symptoms of Cocaine withdrawal
Paranoia and schizophrenia like state
Exhaustion by lack of sleep and food
Appetite, exhaustion, depression
Chemical name for Amphetamines
alpha-methyl-phenethylamine
Amphetamines increase __________ neurotransmitters
catecholaminergic
Amphetamine inhibits _______ metabolism
dopamine
Previously used as an anti-obesity drug
Amphetamines
Treat narcolepsy and ADHD
Amphetamines
Amphetamines can cause
Paranoid psychosis
Necrotizing arteritis
Designer drug managed by benzodiazepines
Amphetamines
Chemical name for Ecstasy
Methylene-dioxymethamphetamine (MDMA)
Fosters false intimacy and empathy
Ecstasy
“Raves” designer drug
Ecstasy
Serotonin reuptake transporter (SERT)
Ecstasy
Drugs That Activate G Protein-Coupled Receptors
Oh Crap Good Luck
- Opioids
- Cannabinoids
- GHB
- LSD, mescaline, psilocybin
Drugs That Bind to Ionotropic Receptors and Ion Channels
Poor Nico Buys Alcohol
- PCP, ketamine
- Nicotine
- Benzadiazepines
- Alcohol
Drugs that Bind to Transporters of Biogenic Amines
ACE
- Amphetamine
- Cocaine
- Ecstasy
Uppers
Reverse the effects of fatigue on both mental and physical
tasks
Stimulants
Scientific name of tobacco plant
Nicotiana tobacum
Nicotine antagonizes ______ ______ receptor
Nicotinic cholinergic
the endogenous ligand of the cholinergic receptor
Acetylcholine
Stronger psychological and physiological dependence than heroin and cocaine
Nicotine
Chemical name for Caffeine
1,3,7-trimethylxanthine
Xanthine alkaloid
Caffeine
Caffeine is derived from the plant ________
Coffea arabica
Caffeine antagonizes _______ receptors
adenosine
Low chance of abuse and addiction
Caffeine
Inhalants involve the use of
Anesthetic gasses
Industrial solvents
Aerosol propellants
Organic nitrites
Affect white matter of the brain
Inhalants
Cause difficulty in concentrating
Hypnosis or dreaminess
Euphoria
Numbness
Tingling sensation
Anesthetics
Examples of Anesthetics in the laboratory
Ether and Chloroform
Nitric Oxide (N2O) is used in ___%
35
Examples of Industrial Solvents
Got To Be True
- Gasoline
- Toluene
- Benzene
- Trichloro-ethylene
Exposure with industrial solvents within ____ minutes can cause euphoria, drunk feeling, and disorientation
5-15
Examples of Organic Nitrites
Amyl nitrite and Isobutyl nitrite
Can cause speeding and flushing of skin
Organic Nitrites
used to enhance and prolong erection (same mechanism with Viagra)
Organic Nitrites
Basic structure of anabolic steroids
Cyclopentanoperhydrophenanthrene ring
Bodybuilders use it for muscle growth and athletes use it
for performance boost
Anabolic steroids
Acne and oily skin are effects of steroids due to activated ____________ glands
sebaceous
Effects of Anabolic steroids
Change in libido
Irritability
Violence
Mood swings
Forgetfulness
Confusion
Schedule __: Anabolic Steroids
Schedule III
Schedule __: Flunitrazepam
Schedule IV
Schedule __: Cannabinoids
Schedule I
Schedule __: Amphetamines
Schedule II
“physical dependence”
dependence
“psychological dependence”
addiction
Non-addictive drugs that cause a feeling of separation of mind and body (dissociative anesthetics)
PCP and Ketamine