Pharm 25 Strong Analgesic Drugs

Front 1

Opiate

Back 1

any of several analgesic alkaloids found in opium

Front 2

Opioid

Back 2

all agonists and antagonists which have morphine like effects, or act predominantly at opioid receptors.

Front 3

Mechanism of action of opioid receptors

Back 3

Act typically at presynaptic cleft. G-protein coupled --> adenylate cyclase inhibited --> cAMP decreased --> potassium conductance increased --> calcium conductance decreased to decreased NT release. this pathway is typically suppressed in absence of pain by increased GABA

Front 4

Enkephalin
1) Drug class
2) affinity for what receptors
3) derived from what to what
4) where do they act?

Back 4

1) endogenous opioids
2) m and d
3) proenkephalin --> leu and met
4) PAG and inhibitory interneurons of dorsal horn of spinal cord

Front 5

b-endorphin
1) Drug class
2) derived from what?
3) affinity for what receptors?
4) sites of action

Back 5

1) endogenous opioid
2) POMC
3) m and d
4) Arcuate nucleus of hypothalamus which projects to PAG, + limbic system

Front 6

Dynorphins
1) Drug class
2) Derived from what?
3) Receptor affinity
4) Sites of action

Back 6

1) endogenous opioid
2) prodynorphin to A and B and alpha
3) k, and A binds to m
4) Spinal cord and PAG

Front 7

Morphine
1) Drug class
2) Receptor affinity
3) Adverse effects

Back 7

1) Opiod R agonist
2) m
3) CNS -nausea, drowsiness, lethargy, inability to concentrate, euphoria, depressed respiration
Eyes- pinpoint pupils
GI - increased resting tone but reduced propulsive waves --> constipation, reduced biliary and pancreatic secretions
Skin - flushed, warm, via dilation of cutaneous blood vessels from histamine release
Bronchospasms can also occer

Front 8

Morphine
4) Absorption
5) Distribution
6) Metabolism
7) Excretion

Back 8

4) Well absorbed in all ways
5) Can't get through BBB
6) Considerable first pass, some metabolites active others not. Mainly via hepatic glucoronidation.
7) conjugates excreted by kidney

Front 9

Morphine
8) Tolerance
9) NK -1 antagonists?

Back 9

8) With repeated use tolerance and dependence can develop but not usually precursors to abuse. Withdrawal sxs can be diminished with weaning off.
9) NK-1 r may be repsonsible for reward effects of drug so targeting it with therapy could hinder dependence.

Front 10

Codeine
1) Structure
2) Affinity
3) Use
4) Combos

Back 10

1) Methylmorphine
2) Less affinity for m receptor
3) First pass --> morphine so allows morphine to exist at higher concentrations after oral dose
4) often used with non-opioid analgesic to increase effect with out increasing side effects.

Front 11

Codeine:
5) Anti tussive effects

Back 11

5) Binds both m and non opioid receptors in CNS.

Front 12

Dextromethorphan
1) Structure
2) Activity

Back 12

1) Like codeine
2) No analgesic effects but antipertussive effects by binding non opioid receptors

Front 13

Oxycodone
1) Derived from what
2) Administration
3) Combos

Back 13

1) Thebaine, inactive constituent of opium
2) orally effective
3) Percodan = w/ aspirin
Percocet = with acetominophen

Front 14

Methadone
1) Drug class
2) Receptor affinity
3) Uses
4) Administration
5) Length of action

Back 14

1) opioid agonist
2) m receptor
3) severe chronic pain and opioid addiction
4) effective orally
5) long duration, slow onset --> little high and less intense withdrawal

Front 15

Meperidine
1) Drug class
2) Action
3) Duration
4) Indications for use
5) Benefits
6) Counterindicator

Back 15

Demerol
1) Opioid agonist, m receptor
2) Like morphine in analgesic and other effects
3) Short onset, shorter duration
4) Labor b/c causes less respiratory depression in fetus than morphine
5) Less constipation than morphine
6) not to use with MAO inhibitors, and not for long term use due to possible toxicity

Front 16

Fentanyl
1) Drug class
2) Action
3) Duration
4) Uses
5) Benefits

Back 16

1) m agonist
2) similar to morphine
3) rapid and brief
4) General anesthesia and postoperative pain
5) Less constipation, does not cause histamine release

Front 17

Pentazocine
1) Drug class
2) Receptor affinity
3) Advantages
4) Drawbacks

Back 17

1) opioid agonist
2) kappa receptor, and partial agonist at m
3) since partial agonist --> less respiratory effects at high doses than morphine
4) Dysphoria and psychomimesis possible at high doses

Front 18

Nalbuphine
1) Drug class
2) Receptor affinity
3) Use
4) Advantages
5) Drawback

Back 18

1) Opioid mixed agonist/antagonist
2) k agonist, m antagonist
3) analgesic
4) Less potential for psychotomimesis than pentazocine
5) Can produce abstinence syndrome in morphine dependent pts due to m block

Front 19

Buprenorphine
1) Drug class
2) Receptor affinity
3) Use, why?

Back 19

1) Mixed agonist/antagonist of opioid R
2) k antagonist, partial m agonist but with much higher affinity for m than morphine
3) more effective than methadone for treatment of opioid addiction b/c cannot produce high not matter what dose, so can be given to patien in multi dose form (also has minimal side effects)

Front 20

Naloxone
1) Drug class
2) Receptor affinity
3) Uses
4) Administration

Back 20

1) Opioid antagonist
2) m and k receptors
3) Opioid overdose, has rapid effect
4) parenterally

Front 21

Naltrexone
1) Drug class
2) Receptor affinity
3) Uses
4) Advantages over naloxone

Back 21

1) Opioid antagonist
2) m and k
3) to treat addiction
4) higher oral efficacy and longer lasting