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21 Cards in this Set

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Enkephalins
– 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
Dynorphins
– 8-17 AA from prodynorphin
– distributed through CNS
- like proenkephalin
Endorphins
– 17-31 AAs from proopiomelanocortin (POMC)
– also has ACTH, melanocyte-stimulating hormone, β-endorphin, etc
– POMC limited to the arcuate nucleus and pituitary
μ receptor
- 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
δ receptor
– supraspinal/spinal Analgesia
– plus or minus resp depression
– causes euphoria and dysphoria
– no (+) reinforcement
– leu-enkephalins
– no GI tone increase
– dynorphin prototypical agonist
κ receptor
– spinal Analgesia
– some resp depression
– causes dysphoria (out of body)
– (+) reinforcement
– Dynorphins
– no GI tone increase
– leu-enkephalin is the prototypical agonist
Fentanyl
- synthetic potent opiod agonist
– 15 – 30 minutes
– 100 times more potent than morphine
– Induction of general anesthesia
– Transdermal & sublingual for chronic pain
Heroin
- alkaloid potent opiod agonist
– Acetylmorphine (semi-synthetic)
– Fast acting
Morphine
- alkaloid potent opiod agonist
– 4 to 6 hrs
– Prototypical
– Reduces coughing
meperidine
- 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)
potent opioid agonists
- Tx of severe pain
– High affinity for μ-R
– Ultra-short acting
weaker opioid agonist
Relieve moderate pain or post-operative analgesia
Codeine
- alkaloid, weaker opioid agonist
– Lower abuse liability
– Moderate pain control
– Oxycodone similar structure and the more potent
mixed opioid agonists
Useful for dependent patients & for post-op analgesia
pentazocine
- mixed opioid agonists, synthetic Talwin
– κ-receptor agonist (dysphoria) w/ weak μ-receptor antagonist properties
– Moderate to severe pain
naloxone
- 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
naltrexone
- opiod antagonist
- 10 – 48 hours [t1/2 ~3 hr]
– Maintenance tx of opioid abuse
– Precipitates withdrawal à also used in detox
– Oral availability ~40%
dextromethorphan
a synthetic Antitussive opioid
Methadone
- synthetic opioid
– t1/2 ~14 hr
- Oral Availability ~92%
opioids + TCAs and & antipsychotics
decrease seizure threshold and increase sedation + resp depression
opioid plus MAOIs
cause serotonin syndrome, HTN, hyperthermia, seizures, death (esp. meperidine)