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