CNS Analgesics Flashcards
1
Q
Heroin
A
semi-synthetic extracted from morphine
2
Q
Characteristics of Heroin
A
- Rapid tolerance
- Fastest onset through IV = sever/rapid withdrawal
- Highly lipid soluble (potent: more potent than morphine)
- Euphoria is produced:
1) opioid system are rewarding
2) opioids inhibit GABA (inhibits the inhibitor) = increase dopamine
Effects of use: pain relief, euphoria, drowsiness/sleepiness, pinpoint pupils, constipation, nausea/vomiting, itching.
Euphoria/rush onset 7-8s and lasts 45s; sedation effects for 1-3 hours; use 2-4 x daily to avoid (every 6-12 hours) withdrawal symptoms
Effects of high does: respiratory depression, stop breathing, coma, death
Withdrawal symptoms (rebound effect): runny nose, restlessness, intense cravings, chills, sweat, anxiety, pain/irritability, flu like symptoms, restless, dysphoria, insomnia, diarrhea, pupil dilation
3
Q
Methadone
A
- oral administration of an opioid agonist.
- withdrawal symptoms less severe (but lasts longer)
- used to support the heroin detox process to minimize withdrawal effect (some use it for maintenance)
- Methadone is 24-36 hours and only requires being taken 1 time a day
4
Q
Buprenorphine
A
- oral administration of an opioid partial agonist
- efective because it binds to opioid receptors (high affinity) but produces low effects (low efficacy)
- minimal rewarding effects - withdrawal are less severe
5
Q
Suboxone
A
- oral administration of buprenorphine and naloxone
- noly buprenorphine takes effect
when crushed and attempt injection, naxonlone becomes active and blocks the buprenorphine from taken effect - providing the reinforcing effects - used to help with detox or maintenance
6
Q
Naloxone
A
- injection in response to opioid overdoes
- competitive antagonist
- has binding affinity for opioid receptors and blocks them from producing an effect
- shorter half life than heroin (administered a few times to offset the overdose)
- Higher dose of agonist (heroin) will override antagonist
