Opioids

Question 1

Where does opium come from?

Answer 1

• sap derived from the poppy

Question 2

What is the difference between an analgesic and a narcotic?

Answer 2

• analgesic: pain relieving

- narcotic: opium based analgesic (subcategory)

Question 3

What are the categories of opioids?

Answer 3

• endogenous (occuring within): endirphin
• alkaloids (directly extracted): morphine and codeine
• semisynthetic (derivative): oxycodone, heroin
• synthetic (structurally different): methadone, fentanyl

Question 4

What general effects does opium exhibit?

Answer 4

• euphoric (stimulant) and anxiolytic (depressant) effects

- used as a medicine (anti-psychotic)

Question 5

How is opium (heroin and morphine) administered? What effects are seen?

Answer 5

• oral: mood alleviation, cough suppression
• inhalation: euphoria
• intravenous: euphoria, pain relief
• injection: three stages

Question 6

What are the three stages of injecting opium?

Answer 6

• stage 1: rush/flash: intense euphoria (sexual orgasm)
• stage 2: on the nod: tranquil drowsiness (lowering testosterone)
• stage 3: withdrawal

Question 7

What is fentanyl?

Answer 7

• china white, china girl, TNT, apache percopop, duragesic sublimaze
• designed for palliative care (lollipop)
• 100x more potent than morphine

Question 8

What is the method of intake for fentanyl?

Answer 8

• oral, transdermal, insufflation
• problem: respiratory depression increases with faster absorption
• less nausea and itching

Question 9

How do the analogues of fentanyl compare?

Answer 9

• 10 000x more potent

- resistant to metabolism

Question 10

What is desomorphine?

Answer 10

• sedation and analgesia
• 8x more potent than morphine
• increase in respiratory depression, septicemia and cardiac arrest
• synthesized from codeine

Question 11

How is desomorphine synthesized from codeine?

Answer 11

• paint-thinner, HCL
• reduction by gasoline/kerosine, iodine, phosphorus
• high toxicity
• inflammation liver, kidney, thyroid damage, “phossy jaw”, gangrene

Question 12

What is the general mechanism of opium?

Answer 12

• agonism

- endogenous neuropeptides

Question 13

What is the agonist action of opium?

Answer 13

• cleavage: separating molecule into separate chains (internal enzymatic action and active metabolite)
• G-protein metabotropic receptors (allows K influx to return to resting)

Question 14

What is the action of pure agonist opium?

Answer 14

• pain relief

- fentanyl and morphine

Question 15

What is the action of partial agonist opium?

Answer 15

• pain relief with no respiratory effect

- buprenorphine

Question 16

What is the action of mixed agonist-antagonists?

Answer 16

• treating opioid addiction

- naloxone and methadone

Question 17

What is the agonist mechanism of opium?

Answer 17

• GABA receptor antagonist
• ventral tegmental area: suppression of inhibitory response on dopamine receptors
• nucleus accumbens: activation of mu opioid receptors that inhibit GABA neurons

Question 18

What is the inhibitory mechanism of opium?

Answer 18

• nociception: sensory pathway related to pain perception
• Adelta and C fibers: sensory pain signal ( inhibited)
• glutamate and substance P: sensory pain signal (activation of medulla inhibits)

Question 19

Does opium produce tolerance?

Answer 19

• dose dependent
• accrued and relational
• selective to analgesia, euphoria and respiratory depression

Question 20

Does opium produce withdrawal?

Answer 20

• lasts 5-10 days
• craving
• flu-like symptoms
• pupil dilation, anorexia, piloerection, spastic arm/leg movements

Question 21

What is evidence for conditioning?

Answer 21

• 90% relapse after withdrawal associated with environment

Question 22

What assists with long term and short term detoxification?

Answer 22

• methadone and buprenorphine
• agonist or partial agonist
• prevent withdrawal, long-lasting effects, weak/no euphoria

Question 23

What assists with rapid or ultra rapid detoxification?

Answer 23

• naloxone
• inverse agonist
• binds as an agonist and induces opposite pharmacological response
• increase withdrawal symptoms, decrease duration
• ultra rapid: in conjunction with sedation/anesthetized for first few hours