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49 Cards in this Set
- Front
- Back
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What is the basic function of opiod analgesics?
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They raise the threshold for pain perception and alter the affective response.
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What are the four main sites of action in the CNS that opiod analgesics have their effect on.
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1. Thalamus- transmission of pain
2. Limbic system- emotion response to pain 3. Brain Stem 4. Spinal cord dorsal horns |
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What type of receptors do opiods work on?
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They work on endogenous opiod receptors found in teh body.
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Endogenous opiod receptors in the body are blocked by which drug?
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Naloxone
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What are the three endogenous opiod precursors?
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Proenkephalin
Pro-opiomelanocortin Prodynorphin |
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Mu, Kappa, and Delta receptors are all what type of receptors in terms of their structure?
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7 transmembrane G-protein receptors.
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What type of receptor is sigma receptor?
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PCP receptor. It can cause hallucinations.
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Opiods cause nasea and vomiting by stimulating what receptor pathway?
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They stimulate the chemoreceptor trigger zone (CTZ).
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What is the effect of opiods on the brain stem respiratory neurons.
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They decrease the response to CO2 and cause respiratory depression.
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How does morphine cause bronchoconstriction?
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It causes the release of histamine which leads to bronchoconstriction
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What is the effect of opiod analgesics on the cough reflex.
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It causes suppression of the cough reflex at sub analgesic doses.
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What is a common clincal exam finding that indicates opiod use?
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Miosis. Pinpoint pupil = Classical sign of opiod use.
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What are the effects of opiods on the endocrine system?
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They cause and increase in ADH release leading to water retention.
They inhibit LH and FSH release. |
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What are the cardiovascular effects of opiods?
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They cause peripheral vasodialtion leading to postural hypotension.
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What are the GI effects of opiod use.
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They cause constipation
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What is the pharmacokinetic difference between morphine and other opiods?
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Morphine is not very orally active and is usually given by IV. Most other opiods have relatively good oral absorption.
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Which opiods cross the blood brian barier well and which do not?
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Morphine is not lipid soluble and does not cross well.
Fentanyl, heroin, and codeine cross much more effectively. |
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What is the major pathway for morphine metabolism?
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Conjugation to glucuronide and excretion in the urine.
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True or False: Opiod tolerance occurs because of metabolic tolerance to the drug.
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False.
It is due to pharmacodynamic tolerance. There is no metabolic tolerance to opiods. |
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How long does it usually take to go through morphine withdrawl?
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36-72 hours. Onset begins 8-12 hours after the last dose.
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What are the symptoms of opiod withdrawl?
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Diarrhea, vomiting, chills, fever, lacrimation, rinorrhea and tremor.
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What drug is used to treat the symptoms of opiod withdrawl?
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Clonidine
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What are the naturally occuring opiods?
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Morphine and Codeine
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Which opiods are partial synthetics?
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Heroin and Naloxone
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What are the synthetic opiods?
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Levorphanol, meperidine, methadone.
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What is the analgesic effect of codeine in comparison with morphine and what is it used for?
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It is 1/10 the potency of morphine and is less efficacious. It is used as an antitussant and an analgesic when combine with aspirin or acetaminophen
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What is the oral and parenteral absorption of heroin?
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Oral absorption is variable but parental absorption is good.
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What is the effect of Hydormorphone in comparison with morphine?
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It has the same effect but is more potent and has a higher oral activity
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Compare oxycodone and morphine.
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Oxycodone has the same effects as morphine but a higher oral activity.
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Apomorphine
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Has little analgesic effect. Causes respiratory depression and is used to induce vomiting by action on teh CTZ.
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Dextromethorphan
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Little analgesic activity ot addictive potential. Used as an antitussant.
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What are the different way that fentanyl can be administered?
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Oral, IV, or through a patch.
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What is the serum half life for fentanyl?
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Very short. 20 min.
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What is teh major means of termination for fentanyl?
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Redistrobution
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What is fentanyl used for.
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It is the only anesthetic used in cardiac surgeries.
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Fentanyl is combined with droperidol to treat what condition?
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Neuroleptic state.
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What is the duration of action for Methadone?
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It has a long duration of action with a half life of 15 hours.
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What is methadoen used for?
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It is used to treat chronic pain and used to control maintenance for heroin withdrawl.
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LAAM
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Used to treat heroin addiction. Longer acting congener of methadone.
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Propoxyphene
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Used to treat mild pain. Similar actions as codeine. Usually combine with aspirin or acetaminophen.
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Diphenoxylate
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Used for the treatment of diarrhea. Combine with atropine to prevent addiction.
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Loperamide
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aka Imodium. Over the counter medication for diarrhea
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What is the classical triad of overdose symptoms?
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Coma
Depressed respiration Pinpoint pupils |
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What is the treatment for overdose?
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Restore respiration
Administer naloxone |
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What are the two competitive antagonists for opiod receptors? Which has a longer duration of action?
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Naloxone and Naltrexone.
Naltrexone has a duration of 24hrs and naloxone is only 1-4 hours. |
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Pentazocine
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Week mu antagonist and kappa and sigma agonist. Blocks morphine analgesia but can act as a spinal analgesic that is as effective as morphine.
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What are some to the side effects of pentazocine?
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Dysphoria and hallucinations due to stimulation of the sigma receptors.
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Nalbuphine and Butorphanol
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Analgesic for moderate pain. Blocks mu receptors but is kappa agonist. Little respiratory depression.
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Buprenorphine
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Analgesic for moderate to severe pain. Partial mu agonist but a kappa antagonist. May cause euphoria.
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