MT6314 DRUGS OF ABUSE Flashcards
T OR F: Drugs of abuse have medical indication
F
“Compulsive” use leads to?
Addiction
Drugs of abuse mainly cause?
Euphoria and altered perception
Dependence or Addiction: Physical
Dependence
Dependence or Addiction: Psychological
Addiction
Dependence or Addiction: Tolerance
Dependence
Dependence or Addiction: Compulsion
Addiction
Dependence or Addiction: Withdrawal syndrome
Dependence
Dependence or Addiction: Relapsing and Craving
Addiction
Dependence or Addiction: No psychoactive drugs
Dependence
What Class: GPCRs
1
What Class: Opioids, THC, GHB
1
What Class: Benzodiazepines, nicotine
2
What Class: ethanol, channels
2
What Class: cocaine, ecstasy, amphetamine
3
What Class: transporters
3
Class 1 and 2 are found in?
Ventral Tegmental Area
Class 3 is found in?
Ventral Tegmental Area and Nucleus Accumbens
Pharmacokinetic or Pharmacodynamic Tolerance: reduction of concentration
KINTETIC
Pharmacokinetic or Pharmacodynamic Tolerance: Shorter duration of action
KINETIC
Pharmacokinetic or Pharmacodynamic Tolerance: Recruitment of Adaptor protein (beta-arrestin)
DYNAMIC
Pharmacokinetic or Pharmacodynamic Tolerance: Desensitization and receptor internalization
DYNAMIC
Example of an adaptor protein?
Beta-arrestin
Common signs of withdrawal?
Elevated BP, body temp
Tachycardia
Sweating
Tremulousness
Dilated pupils
Disorientation
Hyper arousal
Grand mal seizure
Symptoms of withdrawal?
Anxiety
Insomnia
Illusions
Hallucinations
Paranoid ideas
Nausea
Irritability
High motivation to obtain and use
Addiction
Has negative consequences
Addiction
Re-exposure
Stress
Context Call
Relapse
Alter perception, no reward or euphoria
Nonaddictive drugs of abuse
Nonaddictive drugs of abuse target?
Cortical and thalamic systems
Examples of nonaddictive drugs of abuse?
Hallucinogens
Dissociative anesthetics
LSD
PCP/ Ketamine
Dextromethorphan
What kind of drug classifications are in the pharmacology of drug abuse?
Drugs that activate G-protein coupled receptors
Drugs that bind to ionotropic receptors
Drugs that bind to transporters of biogenic amines
WHAT TYPE OF DRUG ACCRDG. TO PHARMACOLOGY:
Opioids
Cannabinoids
Drugs that activate G-protein coupled receptors
WHAT TYPE OF DRUG ACCRDG. TO PHARMACOLOGY:
GHB
LSD, Mescaline and Psilocybin
Drugs that activate G-protein coupled receptors
WHAT TYPE OF DRUG ACCRDG. TO PHARMACOLOGY:
Nicotine
Benzodiazepines
Alcohol
Drugs that bind to ionotropic receptors
WHAT TYPE OF DRUG ACCRDG. TO PHARMACOLOGY:
Ketamine, PCP
Inhalants
Drugs that bind to ionotropic receptors
WHAT TYPE OF DRUG ACCRDG. TO PHARMACOLOGY:
Cocaine
Amphetamines
Ecstacy
Drugs that bind to transporters of biogenic amines
Strong analgesics
Opioids
Examples of opiates?
Morphine
Codeine
Thebaine
Papaverine
“Sleep inducing” opioid
Narcotic
WHAT OPIOID RECEPTOR SUBTYPE: Supraspinal and spinal analgesia; inhibition of respiration, slow GI transit, modulation of hormone and neurotransmitter release
mu
WHAT OPIOID RECEPTOR SUBTYPE: Supraspinal and spinal analgesia, modulation of hormone and neurotransmitter release
delta
WHAT OPIOID RECEPTOR SUBTYPE: Supraspinal and spinal analgesia; psychotomimetic effects, slow GI transit
kappa
Endogenous opioid peptide affinity of mu receptors?
Endorphins > Enkephalins > Dynorphins
Endogenous opioid peptide affinity of delta receptors?
Enkephalins > endorphins and dynorphins
Endogenous opioid peptide affinity of kappa receptors?
Dynorphins»_space; Endorphins and enkephalins
Scientific name of Opium?
Papaver somniferum
What is an powerful narcotic, painkiller?
Opioids
Principal active ingredient in opioids?
MORPHINE
Effects of opioids?
insomnia, hallucination,
nightmares
histamine release
Routs of administration of opioids?
SC, IV
Opioids have more pronounced
effects than what drug?
heroin
Other names of heroin?
Smack, H, ska, junk
What kind of chemical is heroin?
diamorphine
What form is heroin usually in?
addictive drug as a white or brown powder
T or F: Heroin is usually used alone
F, tends to be used with other drugs
Route and speed of administration of heroin?
fast-acting; IV
Half life of heroin and how many doses?
3-5 hrs, therefore several doses/ day
How long is withdrawal of heroin?
Withdrawal 5-10 hrs after
Oxycodone is synthesized from?
thebaine
Oxycodone is derived from?
codeine
What form is oxycodone usually in?
tablet or oral form
Other names for Meperidine?
pethidine; Demerol
Meperidine has serious interactions with?
MAOIs
Attempts to illicitly produce meperidine
has resulted in?
MPTP which can cause parkinsonism
What is MPTP?
MPTP: methyl-phenyl-tetrahydropyridine
What carries the pain signals to the dorsal horn of the spinal cord?
Primary afferent neurons
How do pain signals synapse with the secondary neuron?
via glutamate and neuropeptide transmitters
Pain stimuli can be attenuated in the periphery by what?
opioids acting at opioids receptors
Pain stimuli can be blocked in the afferent axon by?
local anesthetics
APs reaching the dorsal horn can be attenuated at the presynaptic ending by?
opioids
calcium blockers (ziconotide)
a2 agonists
drugs that increase synaptic concentrations of norepinephrine (tapentadol)
T or F: Opioids inhibit the post synaptic neuron
T
Inhibition of opioid analgesics happen in what part of the nervous system?
spinal cord
Possible site of action of opioid analgesics can be in the?
amygdala
anterior cingulate gyrus
Dorsal root ganglion
ventral posterolateral nucleus in thalamus
Sites of action of opioid in pain modulating neurons in?
medulla with midbrain periaqueductal gray area
rotral ventral medulla
locus coerculus
What degree of tolerance in opioids: analgesia
high
What degree of tolerance in opioids: bradycardia
moderate
What degree of tolerance in opioids: miosis
minimal or none
What degree of tolerance in opioids: mental clouding and sedation
high
What degree of tolerance in opioids: antidiuresis
high
What degree of tolerance in opioids: respiratory depression and cough suppression
high
What degree of tolerance in opioids: constipation and convulsions
minimal or none
What degree of tolerance in opioids: nausea and vomiting; euphoria, dysphoria
high
What degree of tolerance in opioids: mental clouding, sedation
high
Chronic or Acute use of opioids: urticaria
Acute
Chronic or Acute use of opioids: constipation and urinary retention
Acute
Chronic or Acute use of opioids: respiratory depression; nausea/vomiting
Acute
Chronic or Acute use of opioids: pruritis and delirium
Acute
Chronic or Acute use of opioids: sedation, myoclonus, seizures
acute
Chronic or Acute use of opioids: hypogonadism, immunosuppression
Chronic
Chronic or Acute use of opioids: Increased feeding, increase GH secretion
Chronic
Chronic or Acute use of opioids: Withdrawal effects, tolerance, dependence
Chronic
Chronic or Acute use of opioids: abuse, addiction, hyperalgesia
Chronic
Chronic or Acute use of opioids: Impairment while driving
Chronic
What drug group: Increased CNS depression, particularly respiratory depression
Sedative-hypnotics
What drug group: Increased sedation
Antipsychotic agents
What drug group: Variable effects on respiratory depression
Antipsychotic
What drug group: Accentuation of cardiovascular effects (antimuscarinic and a-blocking actions)
Antipsychotic
What drug group: relative contraindication to all opioid analgesics
Monoamine oxidase inhibitors
MAOIs have a relative contraindication to all opioid analgesics because?
of high incidence of hypercpyrexis coma
What drug group: hypertension has also been reported
Monoamine Oxidase Inhibitors
Examples of sedative hypnotics?
alcohol, barbiturates, benzodiazepines,
gamma-hydroxybutyric acid (GHB)
Length of action of sedative-hypnotics?
can be short- to long- acting
T or F: In sedative hypnotics, the longer the duration, the more chances of withdrawal
F, the longer the duration the less the withdrawal
Effects of sedative hypnotics?
anxiety, tremors, twitches, vomiting
Clinical uses of sedative hypnotics?
relief of anxiety
insomnia
sedation and amnesia
epilepsy and seizures
component of balances anesthesia (IV)
control of ethanol or other sedative-withdrawal states
muscle relaxation
diagnostic aids
What drug: minor active metabolites
Eszopiclone
What drug: rapid oral absorption
Alprazolam
What drug: active metabolites with long t1/2
Flurazepam
What drug: no active metabolites
Lorazepam and Oxazepam; Zolpidem
What drug: slow oral absorption
Temazepam
What drug: rapid onset, short duration of action
Triazolam
What drug: metabolized via aldehyde dehydrogenase
Zaleplon
What drug: Produg; hydrolyzed to active form in stomach
Clorazepate
What drug: active metabolites; erratic bioavailability from IM injection
Chlordiazepoxide
Has rare occurrence of physiologic dependence
Benzodiazepines
Benzodiazepines are also known as?
“Therapeutic Dose Dependence”
Effects of Benzodiazepines?
weight loss, change in perception,
paresthesia, headache
What is used for date rape?
Flunitrazepam
Rohypnol: roofies (1mg tab)
What schedule is Flunitrazepam?
Schedule IV
What does Flunitrazepam cause?
anterograde amnesia
What kind of receptors are barbiturates?
GABAa receptors
Length of action of barbiturates?
usually Short- acting drugs
Examples of barbiturates?
Secobarbital, pentobarbital Na
T or F: Barbiturates are more commonly used than the other drugs
F, not used as much as other drugs
What drug leads to euphoria and Alcoholism?
Alcohol
Alcohol affects?
Affect GABAa and NMDA
Alcohol withdrawal leads to what effects?
motor agitation, anxiety, insomnia,
hallucination, abnormal vital signs,
seizures
Affects GABAb receptors
Gamma Hydroxybutyric Acid
What drug is naturally found in body?
Gamma Hydroxybutyric Acid
Where else can Gamma Hydroxybutyric Acid be found?
can be found in fermented drinks like guava
(Psidium guajava)
Gamma Hydroxybutyric Acid is what kind of drug?
euphoric, sedative, anabolic
What form can Gamma Hydroxybutyric Acid take?
liquid ecstasy, soap, easy lay, vita-G
What drug: Georgia homeboy
Gamma Hydroxybutyric Acid
Gamma Hydroxybutyric Acid use with alcohol can cause?
breathing
problems
Gamma Hydroxybutyric Acid withdrawal effects include?
insomnia, anxiety, tremors, sweating
Treatment for Gamma Hydroxybutyric Acid for short acting and long acting drugs?
chlordiazepoxide or phenobarbital
Treatment for alcohol?
disulfiram, naltrexone
Main treatment for Gamma Hydroxybutyric Acid?
support groups
Kinds of cannabinoids?
Marijuana
Scientific name of marijuana?
Cannabis sativa
Other names of marijuana?
cannabinol, tetrahydrocannabinol, cannabidiol
Marijuana affects what receptors?
cannabinoid receptors (CB1)
Marijuana is usually taken into the body through?
smoking
How does marijuana take effect?
effects in 2-3 inhalations
What are the effects of marijuana?
“high,” euphoria, laughter, relaxation
What schedule is marijuana?
Schedule I
Marijuana effects on the body?
- antiemetic
- tolerance
- uncertain effect on fetus
- Amotivational syndrome
- diseases related to smoking
Examples of medical cannabinoids?
- Dronabinol
- Nabilone - Chemotheraphy Px
- Nabiximol - Multiple sclerosis
Examples of hallucinogens?
- LSD
- PCP
- Ketamine
- Scopolamine
LSD is known as?
Lysergic acid diethylamide Claviceps purpurea
LSD is a synthetic agent related to?
ergot alkaloids
Neurotransmitters affected by LSD?
norepinephrine (NE), dopamine, serotonin
Agonists affected by LSD?
5-HT1a & 5-HT1c agonists
What is known as one of the most potent drugs 1ug/kg?
LSD
Does LSD have any fatalities?
NO
LSD duration is based on?
dose
What kind of effects does LSD have?
waxing and waning effects
* rise in body temp
* Hallucinations
* uterine contractions
* elevated sugar levels
* goosebumps
* Euphoria
* pupil dilation
What drug: Lophophora williamsii
Mescaline
What drug: restricted but allowed
occasionally to North American Indians
Mescaline
Usually dosage of Mescaline?
5-6mg/kg
What drug: Psilocybe mushroom
Psilocybin
Usual Dosage of Psilocybin?
250ug/kg
Effects of Psilocybin on the body?
mydriasis, muscle relaxation, dizziness
Ketamine is also known as?
“special K” “vitamin K”
What drug: anesthetic
Ketamine
Effects of ketamine?
dream-like states,
hallucination, delirium,
amnesia, high BP,
depression,
fatal respiratory
problems
Other names of Phencyclidine?
angel dust, PCP
Phencyclidine is a derivative of?
phenylcyclohexamine
What drug: veterinary anesthetic; animals will self administer it
Phencyclidine
Route of intake of Phencyclidine?
smoked with tobacco, snorted, Oral, IV
Phencyclidine antagonizes?
NMDA
What drug: Olney’s lesions
Phencyclidine
Length of t1/2 of Phencyclidine?
long
What drug: users tend to be violent
and suicidal; “bad-trips”
Phencyclidine
What drug: Hyoscyamus niger
Scopolamine
Scopolamine blocks what?
central muscarinic receptors
What drug is unpleasant to users?
Scopolamine
Scopolamine is also known as?
Devils breath
What drug: Erythroxylon coca
Coccaine
What transmitter is concerned with cocaine?
dopaminergic reuptake
transmitter
Cocaine inhibits the reuptake of?
dopamine and NE
T OR F: Free based cocaine is absorbed slower than IV
F, just as fast
Half life of cocaine?
1hr, repeated 30mins
Symptoms of cocaine include?
- symptoms include a
feeling of bugs
under skin - paranoia and
schizophrenia like state - exhaustion by lack of
sleep and food - appetite, exhaustion,
depression
What drug: alpha-methyl-phenethylamine
Amphetamines
Amphetamines increase?
catecholinergic neurotransmitters
What is more metabolized and is just released in the use of amphetamines?
dopamine
Amphetamines are used to treat?
narcolepsy and ADHD
Amphetamines causes?
- paranoid psychosis
- necrotizing arteritis
T or F: OD in amphetamine use is rarely fatal
T
Amphetamines are managed by?
benzodiazepines
Schedule of amphetamines?
Schedule II
Effects of amphetamines?
-decreased appetite, inc. stamina, energy
sexual drive
-loss of REM sleep, tremor, restlessness,
anxiety
Related drugs to amphetamines?
shabu, ecstasy
Ecstasy is also known as?
Methylene-dioxymethamphetamine (MDMA)
Ecstasy causes?
intimacy and empathy
What drug:
* “raves” designer drug
* SERT
Ecstacy
What drug: Agonist
Opioids
Cannabinoids
What drug: Activate G-protein coupled receptors
Opioids
Cannabinoids
GHB
LSD, mescaline, psilocybin
What drug:
Mol target - m-OR
Opioids
What drug:
Mol target - CB1R
Cannabinoids
What drug:
Mol target - GABABR
GHB
What drug:
Mol target - 5-HT2AR
LSD, mescaline, psilocybin
What drug: Weak agonist
GHB
What drug: Partial agonist
LSD, mescaline, psilocybin
What drug: drugs that bind to ionotropic receptors and ion channels
nicotine
alcohol
benzodiazepines
phencyclidine
ketamine
What drug: drugs that bind to transporters of biogenic amines
cocaine
amphetamine
ecstacy
What drug:
Mol target - nAChR
nicotine
What drug:
Effect on dopamine receptors - disnhibition
opioids
canabinoids
GHB
benzodiazepines
What drug:
Effect on dopamine receptors - blocks DA uptake
cocaine
amphetamine
ecstacy
Effect on dopamine receptors - excitation
nicotine
alcohol
Stimulants are also known as?
uppers
What do stimulants do?
reverse the effects of fatigue on both mental and
physical tasks.
Other names of nicotine?
Nicotiana tobacum
Nicotine is an agonist against?
nicotinic cholinergic receptor
How fatal is nicotine?
1 drop is fatal
Effects of nicotine?
strong psychological and physiological
dependence (more addictive than heroin
and cocaine)
T or F: Nicotine is carcinogenic and causes sudden infant death syndrome
T
Other names of caffeine?
1,3,7-trimethylxanthine
Caffeine is from?
xanthine alkaloid from Coffea arabica
What kind of receptors is caffeine?
adenosine receptors
T or F: Low chances of abuse and addiction are seen in caffeine
T
Types of inhalants?
- anesthetic gases
- industrial solvents
- aerosol propellants
- organic nitrites
Effects of inhalants on the body?
- psychoactive effects
- alcohol-like intoxications,
hallucinations, - hypoxia, pneumonia,
cardiac fauilure - headache, nausea,
vomiting, slurred
speech, loss of motor
coordination,
wheezing
What has difficulty in concentrating, dreaminess,
euphoria, numbness, tingling?
Anesthetics
When are Anesthetics fatal?
N2O= 35% used; 100% death
Examples of anesthetics?
ether & chloroform
Examples of industrial solvents?
gasoline, toluene,
benzene, trichloro-ethylene
Glue, correction fluid,
gas
How many minutes do industrial solvents last?
5-15min
Effects of industrial solvents?
euphoria, “drunk” feeling,
disorientation
What substance: amyl nitrite, isobutyl nitrite
Organic nitrites
Effects of Organic nitrites?
- dizziness, rapid heart rate, lowered BP,
“speeding,” flushing of skin - enhance, prolong erection
Toxicities of Organic nitrites?
- Liver, kidney, peripheral nerve, and brain
damage - bone marrow suppression,
- pulmonary disease
- death
cyclopentanoperhydrophenanthrene ring
Anabolic Steroids
bone growth, appetite, puberty, muscle
growth
Anabolic Steroids
Schedule of Anabolic Steroids?
3
Effects of Anabolic Steroids?
- change in libido, irritability, violence, mood
swings, forgetfulness, confusion - fatigue, depressed mood, craving for steroids
- hypertrophied muscles,
acne, oily skin,
hirsutism in females,
gynecomastia in
males, needle punctures - high LDL; low HDL
- elevated liver function
The most commonly abused drug in the world
Alcohol
Continue consumption of alcohol despite
suffering consequences
Alcohol abuse
Inability to control drinking,
devoting much time to getting and using alcohol, or
recovering from its effects
Alcohol dependence
use disorders are complex; has genetic and
environmental factors
Alcohol
Main molecular target of opioids?
mu-OR
Main molecular target of cannabinoids?
CB1 receptors
Main molecular target of GHB?
GABAb
Main molecular target of LSD, mescaline, psilocybin?
5-HT1 receptors
Main molecular target of nicotine?
nACh receptors
Main molecular target of alcohol?
NMDAs and GABAa
Main molecular target of ketamine and PCP?
NMDAR
Main molecular target of benzodiazepines?
GABAa
Main molecular target of Cocaine, Amphetamine and Ecstasy?
Cocaine - DAT, SERT, NET
Amphetamine - DAT, SERT, NET, VMAT
Ecstasy - SERT > DAT, NET
Pharmacology of benzodiazepines?
Positive modulator
Pharmacology of PCP and ketamine?
Antagonist
“uppers”
Stimulants
What do stimulants do?
Reverse fatigue
Examples of stimulants?
Nicotine and Caffeine
Nicotine is an antagonist of?
nicotinic cholinergic receptors
Nicotine causes increase in what hormone?
Dopamine
Nicotine causes?
SIDS, and cancer (carcinogen)
Caffeine is involved with what receptors?
Adenosine receptors
How much percent of N2O is used to ensure 100% death?
35%
Anabolic steroids are what schedule?
3
Mu opioid receptor partial / weka agonists
Petazocine
Buprenorphine
Butorphanol
Codeine
Hydrocodone
Mu opioid receptor antagonist
Nalbuphine
Delta opioid receptor antagonist
Buprenorphine
Delta opioid receptor agonist (+)
Sufentanil
Kappa opioid receptor agonist (+)
Morphine
Sufentanil
Pentazocine
Kappa opioid receptor agonist (++,+++)
Nalbuphine (++)
Butorphanol (+++)
Kappa opioid antagonist
Buprenorphine