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96 Cards in this Set
- Front
- Back
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What is morphine?
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strong opiate agonist
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What is heroine?
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strong opiate agonist - diacetyl derivative of morphine
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What is meperidine?
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strong opiate agonist
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What is methadone?
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strong opiate agonist
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What is fentanyl?
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strong opiate agonist
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What is tramadol?
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intermediate opiate agonist
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What is codeine?
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moderate opiate agonists and antitussive
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What is oxycodone?
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moderate opiate agonists
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What is hydrocodone?
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moderate opiate agonists
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What is propoxyphene?
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weak opiate agonist
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What is pentazocine?
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mixed opiate agonist/antagonist
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What is buprenorphine?
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mixed opiate agonist/antagonist
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What is butorphanol?
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mixed opiate agonist/antagonist
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What is nalbuphine?
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mixed opiate agonist/antagonist
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What is naloxone?
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opiate antagonist
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What is naltrexone?
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opiate antagonist
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What is nalmefene?
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opiate antagonist
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What is diphenoxylate?
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antidiarrheal
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What is loperamide?
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antidiarrheal
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What is dextromethorphan?
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antitussive (cough suppressant)
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What other effects does meperidine have?
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anticholinergic effects
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What would not occur in meperdine overdose
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miosis
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What should not be taken with meperdine?
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MAO inhibitors
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Why is heroin so addictive?
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it has enhanced capacity to enter the CNS
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What is the duration of methadone?
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Long, it does not produce peaks and valleys of response
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What is methadone used for?
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given orally for replacement therapy in patients addicted to heroin or other shorter acting agents
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What is the effect of methadone?
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analgesic profile and potency similar to morphine
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Where does fentanyl distribute in the body?
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It is redistributed from the CNS to the fat and muscle
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How is remifentanil, a derivative of fentanyl inactivated?
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It is rapidly inactivated by esterases in the blood
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What is fentanyl used for?
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IV anesthesia in patients who can't tolerate cardiovascular effects of general anesthesia
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What is the mechanism of tramadol?
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modest mu receptor stimulator, some inhibition of serotonin and NE uptake into CNS neurons
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What is effect naloxone on the action of tramadol?
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tramadol is only partially antagonized by naloxone
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What is tramadol used for?
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pain relief
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What is the adverse effect of tramadol?
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can cause seizure activity in some patients
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What is codeine derived from?
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it naturally occurs in poppy seeds
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What is codeine used for?
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mild to moderate pain relief
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Other than pain relief what other effect does codeine have?
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antitussive (cough suppressant)
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Why is codeine commonly given with NSAIDs?
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Giving them together allows for a lower dose of codeine to be given
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What are oxycodone and hydrocodone used for?
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analgesia
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What are oxycodone and hydrocodone usually formuated with?
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aspirin or acetaminophen
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What is the major problem with oxycodone and hydrocodone?
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addiction is rampant
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What is propoxyphene used for?
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pain relief - same potency as aspirin
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What is the major problem with propoxyphene?
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death due to overdose - increasing incidence especially in combo with alcohol or other sedative/hypnotics
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What is pentazocine used for?
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moderate pain relief
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How is pentazocine administered?
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orally
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What is a side effect of pentazocine?
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highly sedative
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How must naloxone be administered to antagonize pentazocine?
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by IV if given orally no antagonist effects will occur
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Which action of pentazocine is antagonized by naloxone?
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opioid receptor action
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How are buprenorphine, butorphanol and nalbuphine administered?
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by IV - not orally efficacious
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Is there a large abuse liability with buprenorphine, butorphanol or nalbuphine?
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No
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Which receptor is the primary site of action for buprenorphine, butorphanol and nalbuphine?
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kappa receptors
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What is the side effect of buprednorphine, butorphanol and nalbuphine?
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considerable sedation
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What can occur to a patient taking pure opiod agonists if given bupredonorphine, butorphanol or nalbuphine?
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precipitation of withdrawal can occur
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Which receptors are affected by opioid antagonists?
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all 3 with slight preference for mu receptors
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What is the structural substitution of opioid antagonists?
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large substituions on the N-17 position
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How is naloxone administered?
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must be by IV - not orally efficacious
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How long is the duration of naloxone action?
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short
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What is naloxone used for?
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repeated injections to reverse opioid overdose
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How is naltrexone administered?
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orally - can precipitate withdrawal reactions by this route
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What is naltrexone used for?
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to reduce cravings for alcohol and opioid drugs
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What is the adverse effect of natrexone?
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liver damage at high doses
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What is the duration of nalmefene?
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long acting
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How is nalmefene administered?
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by injection
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When is nalmefene used?
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to reverse opioid overdose (similar indications as naloxone)
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Does dextromethorphan have morphine effects?
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No, it has no CNS activity so it has less potential for abuse - thus available OTC as antitussive
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What drug is used in addiction therapy?
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methadone
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What drug is used as an anesthetic/sedative-induction?
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fentanyl or fentanyl + dorperidol
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What is used to treat pulmonary edema?
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morphine
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What drug is used to reverse opioid overdose?
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naloxone or nalmefene
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What drug is used to reduce alcohol or opioid cravings?
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naltrexone
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What are two actions of opioids that do not develop tolerance?
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miosis or constipation
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What are the CNS actions of strong opioid agonists (morphine)?
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analgesia, euphoria, sediation, cough suppression, respiratory suppression, miosis, emetic action, truncal rigidity, hormonal changes, increased intracranial pressure, physical dependence or tolerance
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Strong agonists (morphine) are most effective at relieving what kind of pain?
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pain of visceral origin
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How do strong agonists (morphine) relieve pain?
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suppress both the perception of and reaction to pain
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How do strong agonists (morphine) act as an antitussive?
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suppress the cough reflex center in the medulla
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What is the mechanism of the respiratory depression of strong agonists (morphine)?
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depression of the brainstem respiratory mechanism and a decreased responsiveness to carbon dioxide
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What type of patients should be watched closedly on strong agonists due to the respiratory depression effects?
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emphysema patients
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What is the mechanism of the emetic action of strong agonists?
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initial doses can stimulate the chemoreceptor trigger zone (CTZ) in the medulla producing nausea and vomiting; larger or subsequent doses suppress the CTZ
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What is the effect of strong agonists on hormones?
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decreases LH and FSH and lowers testosterone and cortisol; prolactinand growth hormone are incrased due to dimished inhibition by dopamine
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What is the mechanism of increased intracranial pressure due to strong agonists?
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cerebral vasodilation caused by respiratory depression and carbon dioxide retention
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What action of strong agonists is problematic in abdominal surgeries?
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truncal rigidity
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What action of strong agonists is problematic in neuro surgeries?
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increased intracranial pressure
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What drugs interact with strong opioid agonists to enhanced the depressant actions?
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neuroleptic and antidepressants
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What drugs interact with strong opioid agonists to enhance the sedative effects?
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anti-histamines and tricyclic antidepressants
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What drug can interact with strong opioid agonists to cause hyperpyrexic coma?
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MAO inhibitors
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What are the cardiovascular effects of strong opioid agonists?
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minimal effects - parental opioids cause local histamine release and itching, vasodilation and bronchospasm in susceptible individuals
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What is the GI action of strong opioid agonists?
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constipation = increase resting tone, decrease sections and propulsive activity; minimal to no tolerance will develop for this effect
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How do strong opioid agonists affect sphincters?
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increases tone of urinary and anal sphincters, causes biliary colic and postoperative urinary retention
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In which patients is there significant urinary retention when given strong opioid agonists?
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patients with prostatic hyperplasia
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What is the effect of strong agonists on the uterus?
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reduces uterine tone - may prolong labor; readily crosses the placenta
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How are opioid agonists absorbed?
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readily absorbed from subcutaneous, intramuscular sites and mucosa of the nose and GI tract; significant first pass effect
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What is the distribution of opioids in the body?
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skeletal muscles and fatty tissues act as reserviors; can cross blood brain barrier and the placenta
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How are opioids metabolized?
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conjugation - with free hydroxyl groups to glucurnoic acid and hydrolysis: esters are rapidly hydrolyzed by tissue esterases
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Why is codeine not metabolized by conjugation?
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it has methoxy groups which prevent conjugation = orally efficacious
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What is the property of opioid agonists conjugated with glucurnoic acid?
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analgesic properties even stronger than morphine
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How are opioid agonists excreted?
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they are convereted to polar metabolites and excreted in the urine; glucoronide conjugates are excreted in the bile
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