opioids Flashcards
opium derivatives
morphine 10%
Codeine <1%
Thebaine
Harrison Narcotic Tax Act of 1914
US law that regulated and taxed the production, importation, and distribution of opiates. eventually was extended into modern drug laws.
US Drug Schedule I
No Medical use
LSD, MDMA, heroin
US Drug Schedule II
High abuse potential
amphetamine, morphine
US Drug Schedule III
Moderate abuse potential
ketamine, codeine
US Drug Schedule IV
Mild Abuse Potential
benzodiazepines
US Drug Schedule V
Low abuse potential
buprenorpine
semisynthetic Opioids
- heroin (diacetylmorphine)
- hydromorphone (Dilaudid)
synthetic Opioids
- Methadone (Dolophine)
- Meperidine (Demerol)
- Propoxyphene (Darvon)
- fentanyl (innovar)
Endogenous opioids
enkephalins
endorphins
dynorphins
criteria for opioid agonist classification
Exerts effects similar to morphine
Acts at opioid receptors
Effects blocked by antagonist, Naloxone
Naloxene
Opioid antagonist
other name is narcan
- reverses effects of opioid agonists
- precipitates withdrawal in users
Naltrexone (Trexan)
long acting form of opioid antagonist
opioid administration
weak base
- oral
- parenteral
- inhalation
- intranasal
opioid administration
onset and duration of action
depends on preperation
route of administration
metabolism
opioid receptors
metabotropic, inhibitory
inhibits formation of cyclic amp
post synaptic inhibition - k+ Efflux
Presynaptic inhibition - transmitter release
Autoreceptor activation - less transmitter release`
presynaptic inhibition
kappa receptors - Ca++ channels close - Reduced transmitter release
Autoreceptor activation
Autoreceptors - Ca++ channels close - Reduced Transmitter release
endogenous opioids
endomorphin - Mu receptor
Enkephalin - Proenkephalin precursor - Mu, Delta receptor
Dynorphin - Prodynorphin precursor, Kappa receptor
Endorphin - POMC precursor - Mu, Delta receptor
opioid Acute effects
cortex
sedation
drowsiness
relaxation
opioid Acute effects
(Mesolimbic DA pathway_
Euphoria
opioid Acute effects
Meulla
Pupillary constriction
Nausea, Vomiting
Cough Suppression
Respiratory Suppression
opioid Acute effects
Hypothalamus
Hypothermia
Reduced Sexual Drive
opioid Acute effects
many areas
analgesia
opioid Acute effects
intestine
Constipation
sites of opiod induced analgesia
Spinal -sensation Brain stem -Sensation Limbic, Thalamic and Cortical -Perception
opioid overdose (central nervous system)
sleepiness
loss of consciousness
opioid overdose (Pupils)
Widening
opioid overdose (Skin)
Coldness
Clamminess
Blueness
opioid overdose (Muscular)
Seizures
opioid overdose (Breathing)
Slowed
Shallow
Stopped
occurs in medulla (pontine respiratory centers)
opioid thereapeutic use
analgesia anesthesia substance abuse treatment cough suppression Reduce intestinal
Opioid Tolerance
cellular
Pharmacodynamic
Decrease in opioid receptors
increase in adenylyl cyclase
opioid tolerance
situational
contextual
context in which drug is taken
induces tolerance
opioid physical dependence
withdrawal syndrome
opposite of acute effects
not life threatening
1 - 2 weeks in duration
opioid psychological dependence
powerful reinforcer
intense craving, ‘rush’
increases release of dopamine in accumbens
opioid acute and withdrawal effects
withdrawal effects are literally the exact opposite of acute effects
Opioid pleasurability
they inhibit GABA neurons in the VTA which Disinhibit the dopamine system
Drug therapies for opioid dependence
methadone
buprenorphine
naltrexone
Clonidine
Mixed Preperations
Drug therapies for opioid dependence
methadone
full agonist administered daily, typical opioid effects but milder, reduces effects of heroin and morphine
Drug therapies for opioid dependence
Buprenorphine
Partial agonist at mu receptors, typical opioid effects but milder, reduced risk of overdose, reduced intensity of withdrawal
Drug therapies for opioid dependence
naltrexone
opioid antagonist blocks effects of opioids,precpitates withdrawal in users, blocks life threatening effects
Drug therapies for opioid dependence
Clonidine
Noradrenergic alpha autoreceptor agonist, suppresses physical withdrawal symptoms during week of withdrawal
Drug therapies for opioid dependence
mixed preperations
various combinations of medications are under study
dealin drugs
people love dealin drugs, even when their not on heroine any more
opioid overdose signs
Deep slow snoring or gurgling
Heavy nod, not responsive to stimulation - apply sternal rub (rub breastbone hard with knuckles)
slowed breathing
cyanotic - bluish lips and nail beds
-pinpoint pupils
risks of opioid overdose
loss of tolerance
Mixing drugs
using alone
variation in strength of ‘street’ drugs
Serious illnesses
risks of opioid overdose
loss of tolerance
increased risk after period of abstinence
risks of opioid overdose
mixing drugs
mixing opioids with other drugs, especially depressants such as benzodiazepine or alcohol
risks of opioid overdose
using alone
when using drugs alone there is no one present to see signs of overdose
risks of opioid overdose
variation in strength of ‘street’ drugs
street drugs may vary in strength and effect based on purity of the drug and the amount of other ingredients used to cut the drug
risks of opioid overdose
serious illnesses
AIDS, liver disease, diabetes and heart disease
