Opioid Analgesics Flashcards
Opioid
Biological effects through interactions with mu, kappa, and delta receptor
Reversed by naloxone
Opiate
An opioid similar to morphine
Opioid mechanism of action
At nerve endings impedes the release of neurotransmitters
Preventing pain recognition
Inhibiting negative emotion with pain
Mu receptors
Clinically useful drugs Central depression (euphoria, bradycardia, physical tolerance and dependence)
Kappa receptors
Natural addiction control mechanism
Sedation, mild respiratory depression, low addiction liability
Delta receptors
Delusions, hallucinations
Full agonists
Examples
Affinity toward certain receptor type
Treatment of moderate to severe acute or chronic pain
(Morphine, codeine, fentanyl)
Mixed agonists-antagonists
Agonist effect at one receptor, antagonist effect at another
Less likely to cause dependence
Full antagonist
Rescued analgesic effect, treatment of opioid intoxication
Naloxone
Pharmacological effects
Analgesia
Sedation and euphoria
Cough suppression
GI effects
Analgesia
Moderate to severe pain
Chronic pain with cancer and terminal illness
Sedation and euphoria
Kappa receptor stimulation
Additive sedation when combined with other cns depressants
Pain removed euphoria results
GI effects
Increase smooth muscle tone
Decreases guts contractions and motility
Antidiarrheal
Adverse effects
Respiratory depression (cause of death from overdose)
Cns effects
Cardiovascular effects
Dermatologic
Chronic administration
Tolerance
Cross tolerance
Dependence