Opiates

Question 1

Opiates

Answer 1

Narcotic - pain relief

Analgesics - make you sleepy

Question 2

Active Ingredient of Opiates

Answer 2

10% morphine, 0.5% codeine

Question 3

Heroin - Form

Answer 3

Black tar - IV injections can cause venous sclerosis

Question 4

Routes of administration (opiates)

Answer 4

Snort
Inject
Orally
Inhalation

Question 5

Elimination (opiates)

Answer 5

Kidneys

Question 6

Exposure during pregnancy (opiates)

Answer 6

pass through placental barrier

Newborns enter withdrawals w/in a few hours of birth

Question 7

Pharmacological Effects - CNS

Answer 7

drowsiness
decreased sensitivity to stimuli
loss of anxiety/inhibitions
muscle relaxant
pain reliever (analgesic)
decreased ability to concentrate

Question 8

Pharmacological Effects - ANS

Answer 8

CV and respiratory depression
constriction of pupils (pin-point pupils”
Nausea (area postrema)

Question 9

Pharmacological Effects - Increasing dose/Overdose

Answer 9

Increasing dose, more euphoria/elation “rush” and nausea worsens (“good sick” based on learning/conditioning)

Overdose - drowsiness deepens to loss of consciousness, and respiratory depression (loose CO2 trigger response)

Question 10

Pharmacological Effects - GI Tract

Answer 10

decreases tonus and motility of muscles of stomach and intestines
slower passage of contents through tract
increased absorption of water
increased solidity of feces
constipation

Question 11

Mu receptors

Answer 11

Most widely distributed - found in all GRCReceptors

Analgesia (medial thalamus,Peri Aqueductal Gray (PAG), median raphe nucleus, spinal cord)

Reinforcement (NAc, limbic system)

Autonomic functions (brain stem, medulla, area postrema)

Mu and delta exist in overlapping neuronal populations

Question 12

Delta Receptors

Answer 12

More restricted distribution

Olfaction

Motor Integration (neocortex, striatum, substantia nigra)

Reinforcement (NAc)

Analgesica (brain stem, spinal cord)

Mu and delta exist in overlapping neuronal populations

Question 13

Kappa Receptors

Answer 13

Most restricted distribution

Analgesia - PAG, Raphe Nuclei, Spinal Cord, Locus Coeruleus

Hormonal Control - temperature, H2O balance, food intake (hypothalamus, pituitary)

Dysphoria - amygdala, NAc

Question 14

Heroin - Form

Answer 14

Black tar - IV injections can cause venous sclerosis

Question 15

Routes of administration (opiates)

Answer 15

Snort
Inject
Orally
Inhalation

Question 16

Elimination (opiates)

Answer 16

Kidneys

Question 17

Exposure during pregnancy (opiates)

Answer 17

pass through placental barrier

Newborns enter withdrawals w/in a few hours of birth

Question 18

Pharmacological Effects - CNS

Answer 18

drowsiness
decreased sensitivity to stimuli
loss of anxiety/inhibitions
muscle relaxant
pain reliever (analgesic)
decreased ability to concentrate

Question 19

Endogenous Opiates: Prodynorphin

Answer 19

Kappa receptors

Alpha-neoendorphin, beta-neoendorphin, DYNORPHIN

Question 20

Pharmacological Effects - Increasing dose/Overdose

Answer 20

Increasing dose, more euphoria/elation “rush” and nausea worsens (“good sick” based on learning/conditioning)

Overdose - drowsiness deepens to loss of consciousness, and respiratory depression (loose CO2 trigger response)

Question 21

Pharmacological Effects - GI Tract

Answer 21

decreases tonus and motility of muscles of stomach and intestines
slower passage of contents through tract
increased absorption of water
increased solidity of feces
constipation

Question 22

Mu receptors

Answer 22

Most widely distributed - found in all GRCReceptors

Analgesia (medial thalamus,Peri Aqueductal Gray (PAG), median raphe nucleus, spinal cord)

Reinforcement (NAc, limbic system)

Autonomic functions (brain stem, medulla, area postrema)

Mu and delta exist in overlapping neuronal populations

Question 23

Delta Receptors

Answer 23

More restricted distribution

Olfaction

Motor Integration (neocortex, striatum, substantia nigra)

Reinforcement (NAc)

Analgesica (brain stem, spinal cord)

Mu and delta exist in overlapping neuronal populations

Question 24

Kappa Receptors

Answer 24

Most restricted distribution

Analgesia - PAG, Raphe Nuclei, Spinal Cord, Locus Coeruleus

Hormonal Control - temperature, H2O balance, food intake (hypothalamus, pituitary)

Dysphoria - amygdala, NAc

Question 25

Cellular Mechanisms: Postsynaptic Inhibition

Answer 25

Open K+ channels to hyperpolarize | Found in Mu and delta receptors

Question 26

Cellular Mechanisms: Axoaxonic inhibition

Answer 26

Close Ca++ channels - decreases Ca conductance --> decreased NT release Found in mu, delta, and kappa receptors

Question 27

Cellular Mechanisms: Autoreceptors

Answer 27

Inhibits NT release seen in mu and delta receptors **Disinhibition - when you inhibit an inhibitory neuron --> excitatory

Question 28

Endogenous Opiates: Pro-opiomelanocortin

Answer 28

Mu and delta | Beta-endorophin

Question 29

Endogenous Opiates: Proenkephalin

Answer 29

Mu and delta | Met-ENK AND Leu-ENK

Question 30

Endogenous Opiates: Prodynorphin

Answer 30

Kappa receptors Alpha-neoendorphin, beta-neoendorphin, DYNORPHIN

Question 31

Tolerance

Answer 31

- After several months of heavy use, some addicts administer 40-50 times the normal lethal dose for a naive individual - euphoria and analgesia show rapid tolerance - constipation and pupil constriction show little tolerance - cross tolerance appears to be receptor dependent - predominant mechanism is pharmacodynamic

Question 32

Physical Dependence/Withdrawal Symptoms

Answer 32

- Opposite of acute symptoms - unpleasant, flu-like (strong motivator for continued use) - onset: 3-4 hrs - peaks: 36-48 hrs - lasts 7-10 days - cross dependence - intensity of symptoms varies with intensity of drug use and health of individual

Question 33

Mechanisms of Tolerance and Dependence

Answer 33

1) downregulation of opioid synthesis (KO CREB --> decreased enkephalin) 2) downregulation of opioid receptors (less R's) --> not a lot of evidence 3) Receptor desensitization by G-P uncoupling --> Less FUNCTIONAL receptors --> lots of evidence

Question 34

Treatment

Answer 34

No current treatment is curative Basic goals are to reduce withdrawal symptoms, cravings, block effects of drug, improve functional living Agonist maintenance approach - treat with long-acting agoinst like Methadone (mu receptor agonist 1/2 life~20 hrs) or buprenorphone (mu agonist/K antagonist 1/2 life~37 hrs)