| Term | Definition |
| Morphine, Codeine, and Thebaine | Opium contains what three drugs? |
| Endogenous opioid peptides; Short interneurons associated with pain pathways, emotional behavior and motor control | Leucine and Methionine-Enkephalin = ? Found where? |
| endogenous opioid peptide co-released with ACTH | Endorphins = ? |
| Endogenous opioid peptides co-localized with vasopressin | Dynorphins = ? |
| decrease pain perception by binding to opoid receptors | MOA of Endogenous opioid peptides? |
| full; high | Morphine is a ____ agonist; degree of analgesics and dependence is ______. |
| mild | Codeine/Dextropropoxyphene = ______ analgesia and dependence. |
| addicts | Methadone is generally used for treating _____. |
| weaker; respiratory suppression | Tramadol is ______ than Codeine; less ______. |
| Analgesia, Euphoria, Decreased respiration, suppression of the cough reflex, miosis, emesis, GI effects, CV effects, hormone effects | What are the pharmacologic actions of morphine? |
| Activation of mu receptors and kappa receptors (kappa much less than mu) | Morphine MOA? |
| much lower than many other opoids | Rate of Morphine entry to the brain? |
| 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? |
| decreased rate, volume, and tidal exchange | Effects of morphine on respiration? |
| convulsions | Acute morphine overdose causes? |
| vasodilation, decreased BP, release of histamine, suppression of adrenergic tone (and therefore inability to reflex vasoconstrict) | what are the CV effects of morphine? |
| increase in tone and decrease in mobility = constipation; decreased HCl concentration | what are the GI effects of morphine? |
| increased pressure; increased tone of detrusor muscle; bronchoconstriction; contraction | Morphine effects on biliary tract? urinary bladder? bronchial muscle? uterus? |
| Inhibit the release of GnRH and CRF. | Morphine effects on hormones? |
| 10; expensive; less depression of the respiratory center | Oxymorphone = ____ x more potent than morphine; also more _______. Positive compared to morphine? |
| 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? |
| 1/3 the potency | Meperidine: potency compared to morphine? |
| Meperidine; diarrhea; typical opioid effects | Diphenoxylate = _____ congener; treats _____; at high doses causes ______. |
| meperidine; antidiarrheal | Loperamide = ______ congener; anti______. |
| 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? |
| fentanyl; 1000X | Sufentanyl - Congener of _______; ______ more potent than morphine. |
| 20-30; rapid onset | Alfentanil is ______x less potent than fentanyl; onset? |
| equipotent | Remifentanil is _____ with fentanyl. |
| piperidines; short, painful procedures | Afentanil and Remifentanil = _______; used for? |
| Coma, miosis, cyanosis | Acute morphine poisoning - Triad = ? |
| 2g parenterally | Minimum lethal dose of morphine? |
| cancer patients with chronic malignant pain | Transdermal and Intrabuccal fentanyl are used for _____ patients. |
| 8-12 hours | Oxycodone CR duration of action? |
| 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 ________. |
| codeine analog; norepinephrine and seratonin reuptake blockade, also weak mu agonist | Tramadol is a __________. MOA? |
| 6 hours | Tramadol: T1/2? |
| codeine but more potent (comparable to morphine); abused; single highest prescribed drug in USA | Hydrocodone = similar to _____ but ________. Highly ______. Fun fact?? |
| 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? |
| mixed agonist-antagonist. long-acting; mu and kappa; delta | Buprenorphine is a ______. DOA? ___ agonist; ___ antagonist. |
| methadone; moderate opioid agonist; less than 1/2 morphine | D-Propoxyphene is chemically related to _______; it is a ________. Potency? |
| Opioid antagonist; reverse coma and respiratory depression in opioid overdose; Shorter than most opiates | Naloxone is a _______. Use? DOA? |
| Opioid antagonist; longer than naloxone | Naltrexone is a? Duraiton of action? |
| opioid antagonist | Nalmefene = ? |
| 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 |
| Methadone; Buprenorphine | DOC for opiate dependence? Second? |
| full agonist at mu receptor; long acting; methadone clinic | Methadone: MOA? DOA? where? |
| suppresses withdrawal; safety in long-term use; 30 pt limit | Buprenorphine: Does what? Safety? Pt. limit? |
| treatment of opiate dependence | Levomethadyl acetate - use? |
| OTC cough medicine | Dextromethorphan found in? |