Opioids

Question 1

Medical uses of Opioids

Answer 1

coughings, pain, diarrhea (used to prevent in malaria)

Question 2

How Opiates cause analgesia

Answer 2

open K+ channels in dendrites decreasing action potential

Close Ca++ channels in terminal decreasing action potential Presynaptic

Autoreceptors enhance K+ entrance and reduce NT Release

Mediated by MIDBRAIN: PAG & medial thalamus

Spinal cord: inhibit release of substance P between neurons

Brain: Change interpretation of Pain signals in thalamus, brain stem, limbic system

Question 3

Heroin: euphoria

Answer 3

inhibits GABA inhibiting DA in the mesolimbic system (VTA & NAC) allowing for DA release Mostly via mu (if you block mu you block reward & addiction)

Question 4

Heroin effects (3 areas)

Answer 4

Limbic System: whole-body orgasm (IV injection), relieves psychological pain, mental dullness, euphoria

Medulla: respiratory depression, nausea

Peripheral system: pinpoint pupil, constipation

Question 5

Administering/Withdrawal

Answer 5

Low body temp/high body temp low blood pressure/high blood pressure pupil constriction/pupil dilation lowered sex drive/higher sex drive analgesia/pain & irritability calm & euphoria/depression and anxiety muscular relaxation/muscular tension

Question 6

Heroin in body

Answer 6

No major impact on body itself Brain: chronic use leads to altered endorphins & receptor alters pain perception More infections bc HPA (stress) chronically activated decreases immunity

Question 7

Withdrawal symptoms

Answer 7

vomit, diarrhea, erection, cramps, “itchy blood”, muscle spasms “kicking leg syndrome, heavy feeling

Question 8

Lethality of heroin abuse (5 things)

Answer 8

Death by respiratory depression Therapeutic index is low (LD50/ED50) Laced w toxic substances Synergistic combos: alcohol, cocaine, valium Behavioral tolerance

Question 9

Opioid receptors

Answer 9

Mu: analgesia, euphoria, respiratory depression, DA release, physical dependence

Kappa: analgesia, inhibit DA release

Delta: analgesia, dysphoria

Question 10

Stress relief

Answer 10

mu receptors inhibit locus coeruleus -> stress relief

Question 11

Ultra Rapid detox drugs

Answer 11

4-6 hours Anesthesia Naloxone: removes opioid from receptor Clonidine: combats sympathetic symptoms e.g. dry mouth, constipation, anxiety

Question 12

Treatment: Methadone

Answer 12

Partial mu agonist (displaces heroine w less effects) Oral administration (easy to take) Long lasting-> take once a day Less craving Medically safe long term 1-3 years after methadone if they continue in a program 80% remain abstinent, after 6 years 40% still clean BUT Doesn’t block craving for getting high Often alcohol substitutes heroin No one wants methadone clinic -> trucks

Question 13

Blunorphine (Subutex)

Answer 13

3 times/week combined with naloxone less euphoria can be prescribed by physicians No need for health clinics (lower costs) -> Reduced stigma

Question 14

Behavioral and Social Programs

Answer 14

Contingency management therapy Behavioral interventions Therapeutic communities (samaritan village) Multimodality programs: focus on all the needs of the addict (detox, naltroxone, therapy, vocational rehab) Narcotics anonymous

Question 15

Oxycodone

Answer 15

thebaine synthesized 50% stronger than morphine

Question 16

Krokodile

Answer 16

Homemade causes local & systematic damage

Question 17

what is being done

Answer 17

• Pill Mills shut down (late 2000s to now)
• Prescription Drug Monitoring Programs (PDMPs) introduced in many states (late 2000s)
• Reformulated OxyContin introduced (2010)
• •Crush-proof formulation
• •Dissolve-proof formulation

Question 19

Opiates distribution in body

Answer 19

• Concentrated in the spleen, liver, and lungs
• Opioid receptors all over body
• bind to blood proteins
• cross blood brain barrier (If they can)
• Heroin in the brain: Morphine + 6-monoacetyl morphine.
• Eliminated 90% urine (10% unchanged)
• Elimination half-life 2-3 hours
• Can be detected for 24h in urine
• If morphine + codeine found in urine-> patient is suspect of heroin use