Opiods Flashcards
Peptide activators of opioid receptors
Endorphins
What are the three families of endorphins?
Endorphins, enkephalins, dynorphins
Located in the CNS and PNS
-activated by endorphins
Opioid receptors
What are the three key subtypes of opioid receptors?
Mu (endorphins), Delta (enkephalins), and Kappa (dynorphins) receptors
Coupled to G-proteins where they close Ca2+ channels on presynaptic neurons
Opioid receptors
What are the affects of opioid receptor binding on the
- ) Presynaptic neuron
- ) Postsynaptic neuron
- ) Closes Ca2+ channels
2. ) Opens K+ channels
Closing of the Ca2+ channels on the presynaptic neuron does what?
Reduces neurotransmitter release
Opening of the K+ channels on the postsynaptic neuron has what affect?
Hyperpolarization and reduced signal transmission
Decreases activity of neurotransmitters such as glutamate, Ach, norepinephrine, serotonin, and substance P
Opioid receptor binding
Activate opioid receptors
Opioid drugs
What are the 5 major opioid drugs?
Morphine, hydromorphone, meperidine, fentanyl, and codeine
We see heavy drug abuse with the opioid drug
Heroin (diamorphine)
The CNS effects of opioids are mediated through the
Mu receptor
Causes pain relief, euphoria, and sedation
Opioids
What are three other major CNS effects of opioid drugs?
Respiratory depression, cough suppression, and Miosis
Which opioid drug does not cause miosis?
Meperidine
What are the two peripheral nervous system effects of opioids?
Constipation and skin warmth/flushing
Which opioid is used for acute pulmonary edema?
IV morphine
Which opioid is used for cough suppression?
Codeine
Which opioid is used for treating diarrhea?
Loperamide
Which opioid is used to treat shivering?
Meperidine/Demerol
Tolerance develops to opioids in which the effects of the drug are lessened over time. What are the only two effects that do not show tolerance to opioids?
Miosis and constipation
Most common cause of drug overdose death
Opioids
What is the clinical triad of acute opioid intoxication?
Decreased respiratory rate, decreased bowel sounds, and miosis
Seizures are commonly seen with acute intoxication from
Tramadol or meperidine
Short acting opioid antagonist used to treat overdose
-May cause withdrawal if dose is too high
Naloxone
Opioid withdrawal in addicted individuals usually starts
6-12 hours after last dose
What are three major symptoms of opioid withdrawal?
Yawning, rhinorrhea/lacrimation, and piloerection
A partial agonist with agonist and antagonist effects that is used to treat opioid withdrawal
Buprenorphine
A sublingual tablet with a long duration of action
Buprenorphine
To prevent abuse, buprenorphine can be combined with
Naloxone
Long-acting oral opiate that reduces cravings in an opiate addict and helps with withdrawal
Methadone
Long acting opioid antagonist that blocks the effects of opioids if taken
Naltrexone
Administered to detoxified patients to prevent relapse
Naltrexone
Naltrexone is also used in
Alcohol abuse
