Opioid Agonists & Antagonists
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56 terms
Terms | Definitions |
|---|---|
 how does an opioid differ from an opiate | opioid is a generic term referring to all drugs with morphine-like actions opiate is morphine, codeine, other semisynthetic derivatives of morphine from opium |
| what are the 3 main opioid receptor types | mu, delta, kappa |
| what are the pharmacological effects of mu receptors | side effects---euphoria, resp depression, inhibiton of GI motility mu receptors cause most clinically relevant analgesia------mu 1 mediates supraspinal analgesia & mu 2 mediates spinal analgesia |
| what are the pharmacological effects of kappa receptors | mediates both spinal and supraspinal antinociception poss sedation and dysphoria |
| what are the pharmacological effects of delta receptors | mediates mainly at spinal, but also supraspinal antinociception poor analgesia |
| what is a full opioid agonist and what drugs does this include | affinity and activity at all clinically relevant opioid receptors morphine, codiene, meperidine, oxymorphone, hydromorphone, fentanyl, methadone, carfentanil |
| what is a partial opioid agonist and what drugs does this include | affinity but only partial activity for some opioid receptors buprenorphine, nalorphine, tramadol, levallorphan |
| what is a mixed agonist-antagonist and what drugs does this include | affinity for multiple opioid receptors but are agonist at some receptors and are antagonist or weak agonist at other receptors butorphanol & pentazocine |
| what is an opioid antagonist and what drugs does this include | affinity for all opioid receptors but no activity nalaxone, diprenorphine, naltrexone |
| what are the CNS pharmacological effects of opioids incl effect on temp, vomiting center, cough center (in particular morph) | CNS depression--dogs, monkeys, humans CNS stimulation--cats, horses, ruminants, pigs hypothermia--dogs, rabbits, monkeys; hyperthermia--cats, swine, ruminants, horses small dose, puke; large dose, no puke; no puke--swine, chickens, horses, rabbits, rum inhibits cough center, but addictive, so no |
| what are the pharmacological effects of opioids on the eye (morph) | miosis in sp that become sedate (dogs, humans...b/c occulomotor n stimulation) pupil dilation in sp that become excited (cats, sheep, horses, monkeys) |
| what are the pharmacological effects of opioids on the resp syst (morph) | initial stimulation of resp in dogs at sm doses (dissipate heat); decreases after time (and large dose).....mu2 activation depresses brain resp centers |
| what are the pharmacological effects of opioids on the cardio syst (morph) | coronary vasoconstriciton in dogs (poss d.t. activation of alpha receptors); brady and vasodilation d.t. vagal stim.; cerebral vasodilation---increases ICP |
| what are the pharmacological effects of opioids on the GIT, urin syst, imm syst (morph) | GI: vomiting, followed by constipation (segmental m contraction & relaxation of longitudinal m) URIN: mu ag decrease urine d.t. ADH stim; kappa ag inhibit ADH, so increased urine; detrusor inhibition IMM: histamine release if IV; natural endorphans; inhibition of apoptosis during ischemia |
| what drugs have a ceiling effect and why is this important | butorphanol & buprenorphine.............cardio safter, but give less pain relief d.t. their ceiling effect |
| how do opioids cause vomiting | via the CRTZ |
| how do opioids inhibit cough | inhibit the cough center |
| how do opioids cause miosis | oculomotor nerve firing (increased parasympathetic) |
| how do opioids cause mydriasis | catecholamine release prevents miosis |
| why do opioids initially stimulate resp and then sometimes decrease resp after the initial stimulation | at 1st panting b/c trying to dissipate heat; mu2 activation depresses brain |
| how do opioids cause potential cardio depression | ... |
| what causes constipation with opioids | ... |
| how do opioids inhibit urination | ... |
| where are opioids metabolized and excreted | ... |
| what about the pharmacokinetics limits oral availability of opioids | ... |
| what are uses of opioids | ... |
| what are the adverse effects and contraindications of opioids | ... |
| which opioids have short lived analgesia | ... |
| which opioid has the longest lasting analgesia | ... |
| which opioids are weaker analgesics | ... |
| why is buprenorphine difficult to reverse | ... |
| why are full agonists less effective after using butorphanol or buprenorphine | ... |
| which opioids are used as emetics | ... |
| which opioids are used as antitussives | ... |
| which opioids are used as antidiarrheals | ... |
| which opioids cause histamine release and what route of administration is more likely to cause histamine release | ... |
| how are most opioids given | ... |
| which opioids are most commonly given orally (to send home as analgesics or cough suppr) | ... |
| which opioid agonists (full, partial, mixed) are more potent (greater receptor binding affinity) than morphine | ... |
| which opioid has a spasmolytic effect on sm m | ... |
| which opioid has a vagolytic effect rather than an increased vagal effect | ... |
| what opioid is very lipid soluble and therefore is quick-acting and short-lasting | ... |
| which drug is fentanyl combined with and sold as innovar vet (neuroleptoanalgesic) | ... |
| what are the pharmacological effects of innovar vet | ... |
| what are the therapeutic uses effects of innovar vet | ... |
| what are the adverse effects of innovar vet | ... |
| what breed is resistant to innovar vet but more sensitive to side effects | ... |
| how can salivation and bradycardia be controlled when using innovar vet | ... |
| what is a reported reversal agent for innovar vet | ... |
| how long does it take the fentanyl patch to work in cats, dogs, horses | ... |
| how long does the fentanyl patch work | ... |
| what are some precautions with the fentanyl patch | ... |
| which opioid may also inhibit serotonin and NE uptake | ... |
| for which type of analgesia is butorphanol best | ... |
| for which opioid should naloxone not be used | ... |
| if an opioid is more potent, does that mean it provides better analgesia | ... |
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