Opioids Flashcards
What are the pharmacological effects of opioids?
- analgesia
- sedation
- bradycardia
- excitation
- respiratory depression
- nausea and vomiting
- decreased GI motility
- various urinary effects
- antitussive?
- minimal effect on inotrophy
- effects on the pupil, miosis (dogs), mydriasis (cats)
What opioid receptors are found in the brain and spinal cord?
- mu
- kappa
- delta
- NOP (nociception opioid peptide) receptor
Whatare the three families involved in the endogenous opioid system that has naturally occuring peptides?
- beta endorphin
- leucine (leu)- and methionine (met) - enkephalins
- dynorphins
What are neurotransmitters?
naturally occuring peptides
What is the endogenous ligand for the nociception opioid peptide?
nociceptin
What location is the delta receptir found?
brain and peropheral sensory neurones
What is the function of the delta receptor?
- analgesia
- antidepressant effects
-convulsive effects - physical dependence
- may modulate mu-opioid receptor-mediated respiratory depression
What is the location of the kappa receptor?
brain, spinal cord, peripheral sensory neurones
What are the functions of the kappa receptor?
- analgesia
- anticonvulsant effects
- depression
- dissociative/hallucinogenic effects
- diuresis
- miosis
- dysphoria
- neuroprotection
- sedation
- stress
What is the location of the mu receptor?
brain, spinal cord, periperal sensory neurones
What is the function of mu1 receptor?
analgesia and physical dependence
What is the function of the mu2 receptor?
respiratory depression, miosis, euphoria, reduced GI mortility, physical dependence
What is the function of the mu3 receptor?
possible vasodilation
What do full mu agonists do?
bind to and activate a receptor with the maximum response that an agonist can elicit at that receptor
What do partial agonists do?
bind to and activate a receptor but only have partial efficacy, even if they bind to all receptors
How will we know how the opioid will act?
- what receptors/receptor subtypes they have
- mechanism of action at these receptors (full or partialagonists, antagonitst)
- pharmacokinetics
- species differences
What are examples of a full mu agonist?
methadone and fentanyl
What are examples of partial agonists?
buprenorphine
What are examples of a mixed agonist-antagonist?
butorphanol
What are examples of antagonist?
naloxone
What is potency
how much you need to get an effect
What does efficacy meam?
how much effect you get
What can happen if you give pethidine IV?
allergic reaction
How can opioids be administered?
intramuscular, intravenous, subcutaneous, oral transmucosal/buccal, transdernal and epidural/spinal