Week 11: Opioids and Cannabinoids Flashcards
1
Q
Naturally occurring opioids
A
- Morphine (Extract from opium resin)
- Codeine
2
Q
Semisynthetic opioids
A
- Semisynthetic: Synthesized w/ naturally occurring opioid as base
- Bureprenorphine Diacetlymorphine (Heroin)
- Hydrocodone (Vicodin)
- Oxycodone (Oxycontin)
3
Q
Fully synthetic
A
- Fully synthetic: Fully synthesized in lab (no structural similarity w/ naturally occurring/completely independent from morphine/codeine)
- Significant contribution to opioid epidemic
- Fentanyl
- Levacetylmethadyl (LAAM)
- Methadone (Dolophine)
4
Q
Opioids and the BBB
A
- Morphine and heroin easily cross the BBB
- Heroin > morphine
5
Q
Opioid absorption
A
- Differ in lipid solubility
- Primarily metabolized in liver, often producing metabolites that have bio effects
- Active metabolites depend on parent compound
6
Q
Main metabolites
A
- Morphine –> Morphine-6-glucuronide
- Codeine –> Morphine –> Morphine 6 glucuronide
- Heroin –> Monoacetylmorphine –> Morphine –> Morphine-6-glucoronide
- Acetylcodeine –> Codeine –> Morphine –> Morphine-6-glucoronide
7
Q
Opioid elimination
A
- Elimination rate of opioids varies from drug to drug
- Methadone takes up receptor heroin uses, weakening heroine effects
8
Q
Endogenous opioid system
A
- Neuropeptide NTS: System includes opioid NTs and receptors
- Propeptide: Large chain of amino acids; propeptides for eventual neuropeptide
9
Q
Common effect in opioid receptors
A
Analgesia (help respond to pain & inflammation)
10
Q
Opioid receptors
A
- G-protein-coupled metabotropic receptors
- Reduce metabollic activity within neurons
- Inhibitory mechanism = activation of inwardly rectifying K+ channels (support maintenance of cell at baseline)
11
Q
Where are opioid-synthesizing neurons located in the CNS?
A
- Cerebral cortex
- Stratum
- Arcuate nucleus
- Nucleus of solitary tract
- Rosffal ventromedial medulla
- Dorsal hor
12
Q
Where are opioid receptors located in the CNS?
A
- Thalamus
- Nucleus accumbens
- Amygdala
- Hippocampa formation
- Hypothalamus
- Periaqueductal gray
- VTA
- Locus ceruleus
- Nucleus ambiguus
13
Q
Opioid effects in reward circuitry
A
- Decreases/inhibits GABA release in VTA
- Increases Dopamine neuroactivity along dopamine neuron to NA
- Increased dopamine lvls = increased reinforcement effects
- Less GABA activity = more reinforcing effects
14
Q
Pain system
A
Nociceptors —> dorsal horn –> spinothalamic tract –> thalamus –> somatosensory cortex/limbic system
15
Q
Where do input and output pain signals meet?
A
Dorsal horn (come into brain and come out of spinal cord into PNS)