Term
|
Definition
OPIOID AGONIST
mu opioid agonist
potent
short acting synthetic analgesic
used for anesthesia during surgery (administered by injection for fast onset effects and precise control of dosage)
Produces strong respiratory depression |
|
|
Term
| Codeine (3-methylmorphine) |
|
Definition
OPIOID AGONIST
weak mu opioid agonist
natural compound found in poppy plant
antitussive, analgesic for mild pain
prodrug: metabolized in vivo to the primary active compounds morphine and codeine-6-glucuronide
also combined with NSAIDs |
|
|
Term
|
Definition
|
|
Term
| Heroin (diacetylmorphine, diamorphine) |
|
Definition
OPIOID AGONIST
mu opioid agonist
nonpolar, so rapidly enters the brain where it is metabolized to morphine (prodrug)
intense euphoria
not used clinicaly in US |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
OPIOID AGONIST
weak mu opioid agonist, widely used for analgesia during delivery
does not delay birth process, and does not antagonize oxytocin
CAUTION: meperidine + MAOIs = severe rxns, resp depression, excitation, delerium, and convulsions |
|
|
Term
|
Definition
OPIOID AGONIST
orally active, long acting mu opioid receptor agonist
Cross tolerance with morphine or heroin and therefore useful as treatment for heroin addicts |
|
|
Term
|
Definition
|
|
Term
|
Definition
OPIOID AGONIST
weak opioid agonist
used in combination with NSAIDs for analgesia
(oxycodone + aspirin = Percodan)
(oxycodone + acetaminophen = Percocet) |
|
|
Term
|
Definition
OPIOID AGONIST
mu opioid agonist used for mild to moderate pain, commonly given with aspirin or acetaminophen
FDA warning "Propoxyphene in high doses, taken by itself or in combination with other drugs, has been associated with drug-related deaths. Do not take in combination with other drugs that cause drowsiness: alcohol, tranquilizers, sleep aids, antidepressants, or antihistamines |
|
|
Term
|
Definition
OPIOID AGONIST
potent, ultra short acting synthetic opioid analgesic given to patients during surgery to relieve pain as well as an adjunct to an anesthetic
used for sedation, with other drugs in G/A
It's use has made possible the use of high dose opioid and low dose hypnotic anesthesia, due to synergism between remifentanil and various hypnotic drugs and volatile anesthetics |
|
|
Term
|
Definition
OPIOID AGONIST
orally acting analgesic weakly binds to opioid receptors and inhibits the uptake of NE and serotonin
Used for mild to moderate pain |
|
|
Term
|
Definition
OPIOID AGONIST
powerful synthetic opioid analgesic
about 5 to 10x more potent than its analog, Fentanyl
Potent, ultra-short acting synthetic opioid analgesic given to patients during surgery to relieve pain and as an adjunct to anesthesia
Causes significant respiratory depression, may cause respiratory arrest if given too rapidly |
|
|
Term
|
Definition
MIXED AGONIST/ANTAGONIST
partial agonist at mu opioid receptors but a kappa opioid receptor antagonist
IV buprenorphine before induction of anesthesia is more effective and has fewer side effects than morphine in post op pain management
Buprenorphine available in Europe as a transdermal formulation for treatment of chronic pain
extremely high binding affinity at the mu and k-opioid receptors. Partial agonist activity at mu-opioid receptor, partial or full agonist activity at the delta-opioid receptor, and competitive antagonist activity at the kappa-opioid receptor.
Although it is a good analgesic, it is now mainly used in long-term replacement therapy in opioid dependency
(Suboxone = buprenorphine HCl + naloxone HCl) |
|
|
Term
|
Definition
MIXED AGONIST/ANTAGONIST
low intrinsic activity at mu opioid receptors but an agonist at k-opioid receptors |
|
|
Term
|
Definition
MIXED AGONIST/ANTAGONIST
kappa receptor agonist
mu receptor antagonist
at low dosages, found to be much more effective analgesic by women than by men
Produces lower incidence of post op nausea and vomiting compared to morphine and is used to supplement anesthesia during surgery.
Also indicated for use during labor |
|
|
Term
|
Definition
MIXED AGONIST/ANTAGONIST
kappa opioid receptor agonist and a mu receptor antagonist
More likely to cause hallucinations and other psychomimetic effects
Cardiovascular effects make it unsuitable for use in myocardial infarction
Unlike morphine, its respiratory action is subject to a "ceiling" effect
Can be used as an analgesic for dental extractions except in heroin addict patients |
|
|
Term
|
Definition
ANTAGONIST
short acting
Naloxone and Naltrexone are pure opioid antagonists
Most potent at mu receptors but will antagonize the actions of delta and kappa agonists
Used to reverse the effects of opioid overdose (eg. respiratory depression and coma)
CAUTION: will cause abrubt withdrawl syndrome in opioid treated patient or heroin addict |
|
|
Term
|
Definition
ANTAGONIST
longer acting
Naloxone and Naltrexone are pure opioid antagonists
Most potent at mu receptors but will antagonize the actions of delta and kappa agonists
Used to reverse the effects of opioid overdose (eg. respiratory depression and coma)
CAUTION: will cause abrubt withdrawl syndrome in opioid treated patient or heroin addict |
|
|
Term
|
Definition
OPIOID AGONIST
short acting, powerful opioid analgesic w/ potency about x100 of morphine
used for breakthrough pain
also available as transdermal patch (Durogesic/Duragesic) for continuous delivery |
|
|
Term
|
Definition
OPIOID AGONIST
mu opioid agonist
poorly absorbed after oral admin
retained in GI tract, low abuse potential, used as antidiarrheal
Does not cross BBB in significant amounts thus has no analgesic properties (any that does cross is rapidly exported from brain as P-glycoprotein)
Tolerance in response to long term use has not been reported |
|
|
