Opioid analgesic Flashcards
Opioid analgesic
https://youtu.be/t2tKyjj7u5Y
Drug that shows Full agonist, binds tightly to the opioid receptor on Mu and undergo significant conformational change to produce maximal effect
Morphine
Drug that Cannot be glucuronidase at 6-position
Hydrocodone
Codeine derivative, used for pain cough suppression, More addiction than codeine
Hydrocodone
THat can be used in renal failure
Hydrocodone
Drug that must be avoided in <12 years
Codeine
Drug that Used for cough suppression and mild to moderate pain.
Codeine
Drug that shows Analgesia does not increase with dose (ceiling effect)
Codeine
Codeine derivative used for pain and cough suppression
Oxycodone
Half life of Methadone
36-48 HRS
Methadone acts on
Acts on mu receptor agonist and NMDA antagonist.
Drug that shows slows withdrawal symptoms
Methadone
Used for treatment of opioid withdrawal symptoms and reduction opioid craving
Methadone
Drug that shows Less emetic effect
Methadone
Meperidine acts on
Mu receptor as an agonist
Drug that Used during labor for labor pain because this has least respiratory depression
Meperidine, Nalbuphine
Opioid agonist that has Anticholinergic effect
Meperidine
Opioid agonist that doesnot shows miosis, tachycardia (IV), and toxic doses may cause CNS stimulation.
Meperidine
Which is the Most allergic opioid
Meperidine
Opioid that exhibit The least respiratory depression and less constipation
Meperidine
Which drug in its metabolite form causes hallucinations and convulsions in renal disease patients.
Meperidine [Normeperidine (metabolite)]
Which drug has Constipation and urinary retention less than for morphine
Meperidine
Which drug exhibit Weak antagonist at mu receptors and agonist at kappa receptors
Pentazocine
Strong agonist at kappa
Butorphanol
Which drug is not effective in treating severe pain.
Butorphanol (The kappa agonist has lower ceiling analgesic)
Which drug is used intranasal for refract headache
Butorphanol
Which drug exhibit Antagonist at mu receptors and agonist at kappa
Nalbuphine
Nalbuphine is a ________opioid
synthetic
Naloxone
Antidote of mu agonist opioids. Full antagonist at mu receptors
Naloxone dosage form
IV administered by healthcare professionals and IM and nasal spray can be administered by bystander.
Why naloxone is not available oral?
first pass effect is 98%.
treatment of cocaine abuse
Naltrexone and buprenorphine
Partial antagonist at mu receptors
Naltrexone
Brief Tramadol isomers
The (+)/R isomer weak mu agonist (30%) and (-)/S isomer neurotransmitter 5HT and NE reuptake inhibitor (70%).
Drugs that can cause serotonin syndrome
Meperidine, methodone, fentanyl, tapentadol, tramadol
Avoid using with MAOi
D-isomer of morphine
Dextromethorphan
Duration of action of Fentanyl patch compared to other route
patch 72 hr(Onset of action:12 hr)
other 1-2 hr
Drugs that does not cause histamine release up on iv injection
fentanyl, sufentanyl, Tramadol
Partial mu agonist and kappa antagonist ( opposite action of pentazocin and Nalbuphine)
Buprenorphine
Very long half-life once daily or alternate day dosing
Buprenorphine
Opioid that Can be used for persons in remote areas
Buprenorphine
Sublingual opioid tablets combination.
Naloxone+ Buprenorphine .
Naloxone has poor oral bioavailability(98% first pass effect) therefore oral naloxone can block GI effects of opioids without blocking central analgesia.
D-isomer of morphine, has NO analgesic effect. Has NMDA antagonist.
Dextromethorphan-Cough suppressant
Patient using codeine plus acetaminophen for pain after abdominal surgery. What drugs are commended to prevent constipation?
Sennakot
What opioid is highly fat soluble and used for anesthesia?
Fentanyl, Sufentanil remifentanil
Morphine active metabolite →
morphine-6-glucoronide
Codeine is metabolized by →
CYP2D6
Patient taking Tylenol # 3 + hydromorphone →
can cause constipation
Methadone is used for →
opioid withdrawal management, suboxone is also used
Which opioids have highest addiction potential →
morphine, hydromorphone, heroin, fentanyl,
In angina pain what opioids is used →
morphine
Opioids least used in→
head trauma (Avoid opioids in head trauma patients)
Pinpoint pupil is opioids →
over dose symptoms
Enkephalins, endrophins, dynorphins are peptide type opioid neurotransmitters all have common group?
Tyr (tyrosine)-Gly (glycine)-Gly-Phe (phenylalanine)
Where to apply fentanyl transdermal patch →
shoulders, abdomen, thighs and less hairy area.
Where to apply scopolamine patch
Behind ear ( vestibulocochlear)
Allergic to morphine (due to histamine release) can use →
fentanyl
Sequence of addiction/abuse liability:
Fentanyl > Morphine = Meperidine = Methadone > codeine > Propoxyphene
Methadone is regulated as?
Straight narcotic
Available as an oral liquid and administered by diluting in juice.
Methadone
Which opioid analgesic is available in nursing ward of hospital?
Morphine
Treatment of alcohol withdrawal syndrome:
Naltrexone is contraindicated in patients on opioid therapy due to precipitation of opioid withdrawal; a patient must be opioid-free for ≥7 days prior to Naltrexone initiation.
Use with caution in those with hepatic dysfunction due to the risk of hepatotoxicity
Opioid contraindicated in seizure
tramadol
