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Pharm B3

Opioids

QuestionAnswer
alpha and delta fibers small, myelinated, rapid conduction, activated by mechanical and thermal stimuliproduces sharp localized pain
C fibers large, unmyelinatedactivated by mechanical, thermal and chemical stimuliproduce dull, diffuse, aching or burning pain
mu, kappa, and delta opioid receptors G- protein coupled receptors; coupled to adenyl cyclase through Gi 2nd messengers; DECREASE cAMP, INCREASE K conductance, DECREASE Ca conductance; inhibiting neuronal activity
CNS effects analgesia, euphoria, sleep; INCREASE ICP- not used in head trauma treatment
Hypothalamic effects of opioids acute use- decreases body temperature; chronic use- increases body temperature
Neuroendocrine effects of opioids decreased pituitary trophic hormones= decreased testosterone and cortisol
Miosis effects of opioids mu and kappa agonists; cause miosis or 'pin-point' pupils (except- meperidene that causes mydriases or dilated pupils)
Other side effects of opioids Respiratory depression; Depressed cough reflex; convulsion in children at high doses; nausea and vomiting; orthostatic hypotension (morphine); decreased secretions constipation; biliary spasms; decreased urination; prolongs labor; face flushing; cross tol
Morphine Full agonist; Given IV or IM; mu receptor agonist
Diacetylmorphine full agonist;mu receptor agonist; 3-5 times more potent than morphine; legal in UK
Hydromorphone full agonist; 7 times more potent than morphine
Methadone full agonist; equal potency to morphine; orally active; use: controlled withdrawl of opioid addicts
Meperidine full agonist; mu receptor agonist; 1/10th less potent than morphine; orally active; DILATES pupils; with MAOI's can cause hyperpyrexic coma
Fentanyl full agonist; mu receptor agonist; 80 times more potent than morphine; IV during anesthesia or transdermal patch; rapid onset (highly lipid soluble); in combo with droperidol (neuroleptic anesthesia)
Codeine low affinity for mu receptors; prodrug (to morphine); anti-cough use
Oxycodone mu receptors; 2/3rds as potent as morphine; orally active; oxycontin- timed release
Hydrocodone mu receptor agonist; orally active
Tramadol weak mu agonist; inhibits NE and serotonin uptake; less resp. depression and constipation; induces analgesia (not entirely reversible); may cause seizures; CONTRAINDICATED- MAOI's and SSRI's
Propoxyphene 'worthless' drug; 1/24th potency of morphine; resp and CNS depression, cardiotoxicanalgesic
Buprenorphine agonist/ antagonist; much more potent than morphine; less resp. depression; longer duration; maintenance for opioid-dependent pts
Pentazocine agonist/ antagonist; strong kappa agonist; 1/15th potency of morphine; orally active; precipitate withdrawal symptoms; formulated with naloxone to prevent IV use
Nalbuphine agonist/ antagonist; equal potency to morphine; depresses respiration
Butorphanol agonist/ antagonist; strong kappa agonist; 5 times more potent than morphine; nasal spray; for acute pain; increases work load of heart
Naloxone opioid antagonist; IV for opioid overdose; also, diagnose dependance; duration of action 1-4 hours
Naltrexone opioid antagonist; not orally active; duration of action 24 hours; Treats alcohol abuse
Nalmefene pure opioid antagonist; IV combo with naloxone or naltrexone for increased efficacy
Dextromethorphan miscellaneous analog; opioid antagonists; codeine derivative; no analgesic or addictive properties(doesn't act on opioid receptors); low toxicity CNS depression in large doses
Diphenoxylate (with atropine) miscellaneous analog; opioid antagonist; meperidine analogused for diarrhea
Created by: talktovalhere
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