Neuro Pharm 6

Front 1

Enkephalins

Back 1

– pentapeptides from proenkephalin, large polypeptide w/ multiple sequences of enkephalins
– Proenkephalin widely distributed in CNS, esp in areas associated w/ perception of pain
- YGGFM=Tyr-Gly-Gly-Phe-Met
- YGGFL= Tyr-Gly-Gly-Phe-Leu

Front 2

Dynorphins

Back 2

– 8-17 AA from prodynorphin
– distributed through CNS
- like proenkephalin

Front 3

Endorphins

Back 3

– 17-31 AAs from proopiomelanocortin (POMC)
– also has ACTH, melanocyte-stimulating hormone, β-endorphin, etc
– POMC limited to the arcuate nucleus and pituitary

Front 4

μ receptor

Back 4

- supraspinal/spinal analgesia
– big resp depression
– causes euphoria and sedation
– big (+) reinforcement
– met-enkephalins and endorphins
– big GI tone
– morphine prototypical agonist
- only one that inhibits postsynaptic excitability

Front 5

δ receptor

Back 5

– supraspinal/spinal Analgesia
– plus or minus resp depression
– causes euphoria and dysphoria
– no (+) reinforcement
– leu-enkephalins
– no GI tone increase
– dynorphin prototypical agonist

Front 6

κ receptor

Back 6

– spinal Analgesia
– some resp depression
– causes dysphoria (out of body)
– (+) reinforcement
– Dynorphins
– no GI tone increase
– leu-enkephalin is the prototypical agonist

Front 7

Fentanyl

Back 7

- synthetic potent opiod agonist
– 15 – 30 minutes
– 100 times more potent than morphine
– Induction of general anesthesia
– Transdermal & sublingual for chronic pain

Front 8

Heroin

Back 8

- alkaloid potent opiod agonist
– Acetylmorphine (semi-synthetic)
– Fast acting

Front 9

Morphine

Back 9

- alkaloid potent opiod agonist
– 4 to 6 hrs
– Prototypical
– Reduces coughing

Front 10

meperidine

Back 10

- synthetic potent opiod agonist Demerol
– 2-4 hrs, Reduces post-op shivering
– Does not reduce coughing
– Regional blocks (I.V. or I.M., epidural or intrathecal)

Front 11

potent opioid agonists

Back 11

- Tx of severe pain
– High affinity for μ-R
– Ultra-short acting

Front 12

weaker opioid agonist

Back 12

Relieve moderate pain or post-operative analgesia

Front 13

Codeine

Back 13

- alkaloid, weaker opioid agonist
– Lower abuse liability
– Moderate pain control
– Oxycodone similar structure and the more potent

Front 14

mixed opioid agonists

Back 14

Useful for dependent patients & for post-op analgesia

Front 15

pentazocine

Back 15

- mixed opioid agonists, synthetic Talwin
– κ-receptor agonist (dysphoria) w/ weak μ-receptor antagonist properties
– Moderate to severe pain

Front 16

naloxone

Back 16

- opiod antagonist
- 1-2 hrs (iv only) [t½ ~ 1 hr]
– Oral Availability 2%
– Non selective w/ μ>δ>κ – Acute tx of opioid intoxication (detox)
– Reverses overdose
– Precipitates withdrawal

Front 17

naltrexone

Back 17

- opiod antagonist
- 10 – 48 hours [t1/2 ~3 hr]
– Maintenance tx of opioid abuse
– Precipitates withdrawal à also used in detox
– Oral availability ~40%

Front 18

dextromethorphan

Back 18

a synthetic Antitussive opioid

Front 19

Methadone

Back 19

- synthetic opioid
– t1/2 ~14 hr
- Oral Availability ~92%

Front 20

opioids + TCAs and & antipsychotics

Back 20

decrease seizure threshold and increase sedation + resp depression

Front 21

opioid plus MAOIs

Back 21

cause serotonin syndrome, HTN, hyperthermia, seizures, death (esp. meperidine)