Opioids Flashcards
what are narcotics
- ‘opioids’ = any natural or synthetic drug that has morphine-like pharmacological action
- major effects of opioids are on CNS and bowel
what binding sites are called the opiate receptors (for opioids to act as agonists) in the CNS
- mu
- delta
- kappa
what are pure agonists (opioids)
- activate both Mu and Kappa receptors
- strong or moderate in producing an analgesic (relief of pain) effect
- ex. morphine
what are mixed agonists-antagonists (opioids)
- activate Kappa receptors but block Mu receptors
- analgesic (relief of pain) effect with some antagonist activity
- ex. pentazocine (talwin)
- butorphanol (stadol)
what are pure antagonists/blockers (opioids)
- inhibit both Mu and Kappa receptors
- no analgesic effects; used in opioid overdose
- ex. naloxone, naltrexone (revia)
what are some opiate agonists with moderate efficacy
- codeine
- hydrocodone (hycodan)
- oxycodone (oxycontin)
- combined with acetaminophen = Percocet
- combined with ASA = percodan
what are some opioid agonists with high efficacy
- hydromorphone (dilaudid)
- meperidine (demerol)
- morphine
what are some other effects of opioids besides analgesia
- suppress cough reflex
- slow GI motility
- depress CNS
- sedation
- euphoria
what are some adverse effects of opioids on the CNS
- respiratory depression
- cough suppression
- nausea/vomiting
what is an adverse effect of opioids in the GI tract
- constipation
what are some other adverse effects of opioids in general
- tolerance can develop
- physical and psychological dependence
what drugs will interact poorly with opioids
- antihistamines, sedative/hypnotics, alcohol and psychotropics
- increased CNS effects (e.g. sedation)
at what dose will morphine reduce severe pain or eliminate pain
- 5-10 mg
what are the central actions or morphine (and some other opioids)
- analgesia
- drowsiness and sleep
- cough suppression
- vomiting (due to stimulation of chemoreceptor trigger zone in the brain)
- hypotension
- miosis (papillary constriction)
- respiratory depression (high doses): major toxic effect and cause of death because no tolerance is developed to respiratory depression
- euphoria (ecstacy; develop tolerance rapidly to euphoric actions)
- increased release of ADH (antidiuretic hormone), which causes urinary retention
what are some other minor activities (peripheral actions) caused by morphine and some other opioids
- constipation (due to slowing of peristalsis)
- body warmth/flushing/itching (due to histamine release)
when is morphine used
- severe pain due to trauma, cancer, or heart attack
- severe and chronic pain
- pre-anaesthetic medication
what does morphine do (pharmacodynamically)
- binds with mu and kappa receptor sites
- analgesia, euphoria, constriction of pupils, stimulation of cardiac muscle
- relieves SOB with heart failure and pulmonary edema
- for relief of chest pain due to heart attack
what are some side effects of morphine
- dysphoria (restlessness, depression, anxiety)
- hallucinations
- nausea
- constipation
- dizziness
- itching sensation
- in cases of overdose, respiratory depression, cardiac arrest
- do not take with alcohol -> both are CNS depressants
- tolerance and cross tolerance can develop, as well as physical and psychological dependence