Opioid analgesics and antagonists
Terms
undefined, object
copy deck
- codeine analog; norepinephrine and seratonin reuptake blockade, also weak mu agonist
- Tramadol is a __________. MOA?
- Analgesia, Euphoria, Decreased respiration, suppression of the cough reflex, miosis, emesis, GI effects, CV effects, hormone effects
- What are the pharmacologic actions of morphine?
- Methadone; Buprenorphine
- DOC for opiate dependence? Second?
- suppresses withdrawal; safety in long-term use; 30 pt limit
- Buprenorphine: Does what? Safety? Pt. limit?
- increased pressure; increased tone of detrusor muscle; bronchoconstriction; contraction
- Morphine effects on biliary tract? urinary bladder? bronchial muscle? uterus?
- mixed agonist-antagonist. 1/3 that of morphine; kappa; mu and delta; both shorter than morphine
- Pentazocine is a ________. Potency? ___ agonist, ___ antagonist. DOA and onset?
- Endogenous opioid peptides co-localized with vasopressin
- Dynorphins = ?
- 1/3 the potency
- Meperidine: potency compared to morphine?
- 2g parenterally
- Minimum lethal dose of morphine?
- methadone; moderate opioid agonist; less than 1/2 morphine
- D-Propoxyphene is chemically related to _______; it is a ________. Potency?
- piperidines; short, painful procedures
- Afentanil and Remifentanil = _______; used for?
- Inhibit the release of GnRH and CRF.
- Morphine effects on hormones?
- addicts
- Methadone is generally used for treating _____.
- equipotent
- Remifentanil is _____ with fentanyl.
- less sedation; direct myocardial depression; GI stimulation; post-surgical pain because only lasts 1-2 hours
- Meperidine: positive over morphine? Only opioid to cause _________; very little ____ stimulation; Not for _____ because?
- full; high
- Morphine is a ____ agonist; degree of analgesics and dependence is ______.
- codeine but more potent (comparable to morphine); abused; single highest prescribed drug in USA
- Hydrocodone = similar to _____ but ________. Highly ______. Fun fact??
- 20-30; rapid onset
- Alfentanil is ______x less potent than fentanyl; onset?
- much lower than many other opoids
- Rate of Morphine entry to the brain?
- full agonist at mu receptor; long acting; methadone clinic
- Methadone: MOA? DOA? where?
- Endogenous opioid peptides; Short interneurons associated with pain pathways, emotional behavior and motor control
- Leucine and Methionine-Enkephalin = ? Found where?
- 10; expensive; less depression of the respiratory center
- Oxymorphone = ____ x more potent than morphine; also more _______. Positive compared to morphine?
- cancer patients with chronic malignant pain
- Transdermal and Intrabuccal fentanyl are used for _____ patients.
- Morphine, Codeine, and Thebaine
- Opium contains what three drugs?
- partial agonist of opioid receptor; less dependence (blocks withdrawal in mildly dependent people; precipitates withdrawal; 20-50x morphine
- Buprenorphine = _______; physical dependence? Use? Moderate to severely dependent people? Potency
- mixed agonist-antagonist. long-acting; mu and kappa; delta
- Buprenorphine is a ______. DOA? ___ agonist; ___ antagonist.
- Coma, miosis, cyanosis
- Acute morphine poisoning - Triad = ?
- treatment of opiate dependence
- Levomethadyl acetate - use?
- opioid antagonist
- Nalmefene = ?
- OTC cough medicine
- Dextromethorphan found in?
- 6 hours
- Tramadol: T1/2?
- weaker; respiratory suppression
- Tramadol is ______ than Codeine; less ______.
- increase in tone and decrease in mobility = constipation; decreased HCl concentration
- what are the GI effects of morphine?
- morphine; moderate pain; antitussive; morphine; CNS stimulation
- 10% of codeine is converted to ________. Used for ____ and as a _____; higher oral efficiency than _________; High doses cause ________.
- 75-125; short; minimal CV except bradyarrhythmias; respiratory more severe than morphine
- Fentanyl = _______ to ______ times more potent than morphine; duration of action? CV and respiratory side effects?
- Opioid antagonist; longer than naloxone
- Naltrexone is a? Duraiton of action?
- Opioid antagonist; reverse coma and respiratory depression in opioid overdose; Shorter than most opiates
- Naloxone is a _______. Use? DOA?
- chronic non-malignant pain; acute pain, dyspnea, pre-anesthesia, open heart surgery, decrease fear in dying
- DO NOT use morphine in _________; use in other ____ pain; also use for what?
- decrease pain perception by binding to opoid receptors
- MOA of Endogenous opioid peptides?
- mild
- Codeine/Dextropropoxyphene = ______ analgesia and dependence.
- decreased rate, volume, and tidal exchange
- Effects of morphine on respiration?
- meperidine; antidiarrheal
- Loperamide = ______ congener; anti______.
- Activation of mu receptors and kappa receptors (kappa much less than mu)
- Morphine MOA?
- fentanyl; 1000X
- Sufentanyl - Congener of _______; ______ more potent than morphine.
- vasodilation, decreased BP, release of histamine, suppression of adrenergic tone (and therefore inability to reflex vasoconstrict)
- what are the CV effects of morphine?
- 8-12 hours
- Oxycodone CR duration of action?
- endogenous opioid peptide co-released with ACTH
- Endorphins = ?
- convulsions
- Acute morphine overdose causes?
- Meperidine; diarrhea; typical opioid effects
- Diphenoxylate = _____ congener; treats _____; at high doses causes ______.