B. 26. Semisynthetic and synthetic opiates Flashcards
list the synthetic opiates
Fentanyl Tramadol Meperidine Loperamide Diphenoxylate Methadone
what is Naloxone?
semi-synthetic opioid antagonist
strong
what is Naltrexone?
synthetic opioid antagonist
strong
list the semisynthetic opiates
oxycodone
dihydrocodeine
Buprenorphine
Nalbuphine
which agent has the highest potency- morphine or fentanyl?
fentanyl is 100x more potent than morphine
what are the strong agonists
Fentanyl
Meperidine
Oxycodone
Methadone
what are the weak agonists
Tramadol Loperamide Diphenoxylate codeine dihydrocodeine
which agent has the highest potency- morphine or Buprenorphine?
Buprenorphine has 25-50x more potent than morphine
which agents have mixed activity?
Buprenorphine
Nalbuphine
ᴋ antagonist
µ agonist (partial)
what are the uses of Fentanyl?
analgesic (post-operative pain, chronic pain syndromes)–> transdermal (chronic pain-25-100µg)/sublingual
anesthesia –>IV
what is the duration of action and max daily dose of Tramadol?
6 hours
max. 400mg
what are the uses of Tramadol?
analgesic (neuropathic pain, dentistry)
what are the SE’s of Tramadol
nausea- vomiting dizziness sweating dry mouth sedation epilepsy respiratory depression
what causes serotonin syndrome when giving Tramadol?
Tramadol inhibits NE and 5-HT reuptake
shouldn’t be combined with MAO inhibitors
can cause epilepsy
what is Meperidine used for?
analgesic use (emergency care, pre-operative)
what might lead to serotonin syndrome when giving Meperidine?
has serotonergic activity
antimuscarinic effect–>antagonizes the smooth muscle effects of opioids –>no constipation or urinary retention
which agent is a potential drug of abuse?
oxycodone
which opiates are anti-diarrheal agents?
Loperamide
Diphenoxylate
when do we use oxycodone?
analgesic use (post-operative pain, chronic pain syndromes)
what are the indications for giving Codeine and Dihydrocodeine?
antitussive (suppress coughing)
analgesic effect in combination with NSAID’s or acetaminophen
what can Codeine and Dihydrocodeine cause?
epileptic seizures
which agent is safer than Morphine?
Nalbuphine
less cardiovascular effects
which agent is used for spinal anesthesia?
Nalbuphine
what are the indications for giving Methadone and Buprenorphine
management of opioid withdrawal syndrome
maintenance programs for addicts (heroin, morphine)
which opiates have a long serum T1/2?
methadone
Buprenorphine
which opiate has good absorption?
buprenorphine
when do we give Naloxone?
management of acute opioid overdose (IV administration)
Naloxone dose
0.4mg
why combine Naloxone with OXYCODONE?
may reduce opioid bowel syndrome –> antagonizes constipation
what is the indications for giving Naltrexone?
management of opioid withdrawal syndrome –>oral 50 mg
management of alcohol withdrawal syndrome
what is the T1/2 of Naltrexone and SE’s
Long T1/2–> up to 48h’
hepatotoxic
what is Methylnaltrexone?
peripheral opioid antagonist
can’t enter the brain
what is Methylnaltrexone usually used for?
avoid constipation from opioid bowel syndrome
without affecting pain relief
