t-opiods

Question 1

absorption

Answer 1

less effective orally than parenterally
not lipid soluble and not rapidly absorbed in intestine
easier to control levels
codeine more bioavailble orally
inhaling increases bioavailbiility with less risk than needle

Question 2

distribution

Answer 2

concentrate in lungs heart kidney liver and brain
PG- associated with pain
opiod antagonists enter the brain much faster

Question 3

elimination

Answer 3

metabolized in liver and DT and excreted by kidneys
1. cytochrome p430 links drug to hydrophilic substance
2. enzymes break down
morphine heroin and oxymorphone are not broken down by p450

Question 4

endogenous opiod ligands

Answer 4

endorphins, morphins, enkephalins, nociceptin

bind to opiods receptors: 4 types (u,k,o,ORL)

Question 5

neuropharmacology of opiod receptors

Answer 5

g protein coupled receptor opens inward K channels- closing Ca and hyperpolarizing the cell
adenylyl cyclase is inhibited and cAMP can not be produced
reduced excitability of post synaptic cell

Question 6

opiod drug affect on receptors

Answer 6

agonsit- target and stimulate u receptor at varying affinities (potency) ex. morphine
mixed agonist/antagonist- ex. nalorphine

Question 7

principal effects of opiods

Answer 7

analgesia- reduce excitability of nociceptors
reward- VTA-NA dopaminergic
binding disinhibits the VTA and increases DA release
life functions- respiratory depression (in medulla oblongota) vomitting, coughing

Question 8

effects on body

Answer 8

nausea and vomitting- CTZ (vomitting center)
narrows pupils
lower bp due to dilation
constipation- impede muscles from pushing along GT

Question 9

effects on sleep

Answer 9

doesnt cause restful sleep- but instead lethargy and drowsiness
can cause insomnia and sleep deprivation

Question 10

cognitive performance & subjective effects

Answer 10

inattention, difficulty concentrating and memory deficits
sleep-like nod, visual or auditory dreams
effects vary between first time users and experience and users experiencing pain

Question 11

which drug has the most potential for abuse

Answer 11

oxycodone

Question 12

lethal effects

Answer 12

• depression of breathing
• lower seizure threshold and cause convulsions
  mostly in experienced users - loss of tolerance
  may not be a larger dose than the usual
  combining with alcohol or benzos potentiates

Question 13

chronic effects

Answer 13

lifestyle- expensive and illegal

years of potential life lost- calculate number of years of potential life that are lost in a population

Question 14

tolerance & sensitization

Answer 14

rapod and extensive tolerance to most effects
pain sensitivity shows tolerance and may even be enhanced
- changes in metabolizing enzymes
- changes in density of opiods receptors

Question 15

withdrawal

Answer 15

not as severea as portrayed- not as bad as barbituates and alcohol (not fatal)
- person not able to stay awake, chills, short breaths, goosebumps
YEN SLEEP
primarily u receptor

Question 16

detoxification

Answer 16

• long lasting changes in the brain exist for longer than the physical changes (ex. detox doesnt cure addiction)

Question 17

maintence therapy

Answer 17

give addict a cheap reliable source of drug
- methadone
full agonist of u receptor- blocks action of heroin and alleviates withdrawal
- buprenorphine
doesnt need to be administered every single day
partial agonist - less sedation/dysphoria
heroin- second line treatment provides safe source of drug

Question 18

antagonist therapy

Answer 18

patients are detoxified from opiod drug and kept abstinent
given doses of antagonist taken orally (no abuse potential)
high dropout rates