Opiates & Analgesics Flashcards
the point the individual perceives the response as pain
pain threshold
The ability of the individual to experience pain without initiation of pain responses
Pain tolerance
Painful stimuli are sensed by peripheral nociceptive of these types of neurons via ion channels that convert stimuli to membrane potential changes
C or Aδ
Mu receptor that functions in analgesia and euphoria
Mu1
Mu receptor that functions in bradycardia and respiratory depression
Mu2
Component of G protein that modulates ion channels in opioids
Beta and gamma
What effect do opioids have on BP?
Causes hypotension
(at moderate to high doses)
What effect do opioids have on heart rate?
Causes bradycardia
(at moderate to high doses)
What effect do opioids have on repiration?
Depress respiration
Opioids can cause respiratory depression and cerebral vessel dilation, so they are contraindicated in this
Head trauma or severe brain injury
Opioid use is cautioned in patients with asthma or COPD due to the release of this
Histamine
Opioids chronically suppresse hypothalamic-pituitary-gonadal axis to trigger this
Opioid-induce androgen deficiency (OPIAD)
Opioids chronically suppress this to trigger opioid-induced androgen deficiency (OPIAD)
Hypothalamic-pituitary-gonadal axis
No opioid tolerance develops to either of these effects
Miosis and constipation
Peripheral opioid antagonist that is administered orally
Naloxegol
Peripheral opioid antagonist that is a subcutaneous injectable
Methylnaltrexone
Naloxegol and Methylnaltrexone are antagonists to this
Peripheral opioid antagonists
Benzodiazepines should not be used with these drugs due to profound sedation, respiratory depression, coma and risk of death
Opiates
This type of drug should not be used with opiates due to profound sedation, respiratory depression, coma and risk of death
Benzodiazepines
Is dependence likely when morphine is used for pain?
Rare
Does meperidine have a short or long duration of action?
Short
Meperidine is converted to this product that is not conjugated, non-analgesic, proconvulsant, and hallucinogenic
Normeperidine
Normeperidine is a product of biotransformation of this drug
Meperidine
Is Normepederidine (a product of biotransformation of meperidine) analgesic?
No
Normepederidine (a product of biotransformation of meperidine) has these two effects
Proconvulsant
Hallucinogen
Opiate that has anticholinergic activity, and may cause seizures
Meperidine
Opiate that has anticholinergic activity, and has potential for serotonin syndrome if combined with serotonin reuptake inhibitors
Meperidine
Opiate that is contraindicated in epilepsy, cardiac disease, and use with MAOI (due to malignant hyperthermia)
Meperidine
Why is Meperidine contraindicated in patients with epilepsy?
It has anticholinergic activity and cause cause seizures
Meperidine use is contraindication with MAOI’s because concurrent use can cause this
Malignant hyperthermia
Meperidine use is contraindicated with this type of drug due to malignant hyperthermia
MAOIs
What is the main issue with use of Fentanyl, Alfentanil, Sufentanil, Remifentanil?
Potency
Fentanyl, Alfentanil, Sufentanil, Remifentanil are contraindicated in this
Pregnancy
(respiratory depression of mother and newborns; increased sudden infant deaths)
Opiates where potency is an issue
Fentanyl et al.
(Alfentanil, Sufentanil, Remifentanil)
Opiates that may cause respiratory depression of mother and newborns; increased sudden infant deaths
Fentanyl et al.
(Alfentanil, Sufentanil, Remifentanil)
Synthetic opioid that also is an antagonist at (NMDA) receptor and weak inhibitor of norepinephrine and serotonin uptake
Methadone
Methadone is a synthetic opioid that also is an antagonist at this receptor
NMDA
Methadone is a synthetic opioid that also is an antagonist at (NMDA) receptor and weak inhibitor of uptake of these 2 compounds
Norepinephrine and serotonin
Opioid that may be used in nociceptive pain (mu) and neuropathic pain (NMDA and uptake inhibition)
Methadone
Is Methadone short or long lasting?
Long
orally active
Does Methadone cause euphoria?
No
Opioid that is often combined with aspirin or acetaminophen
Codeine
Opioid that has a high degree of histamine release and vasodilation
Codeine
Codeine has a high degree of release of this
Histamine
What effect does Codeine have on vessels?
High degree of vasodilation
2 opioids that are weak inhibitors of norepinephrine and serotonin reuptake
Tramadol and Tapentadol
Tramadol and Tapentadol are weak inhibitors of reuptake of these two compounds
Norepinephrine and Serotonin
With use of Tramadol and Tapentadol, why is respiratory depression less than predicted by analgesic action?
Because they are weak inhibitors of norepinephrine and serotonin reuptake
Tramadol and Tapentadol may interact with this type of agent
Monoaminergic agents
(especially MAO uptake inhibitors and other reuptake inhibitors)
Opiate that has a convulsant metabolite that restricts use to short term
Meperidine
This opiate and related compounds are very potent so be careful as small doses are powerful (cannot be used during pregnancy or after surgery)
Fentanyl
Opiate that has a long duration of action and allows once daily dosing
Methadone
Opiate that has a very high profile of histamine release
Codeine
2 opiates that enhance norepinephrine and serotonin activity that may reduce opiate-induced respiratory depression
Tramadol and Tapentadol
Yawning is characteristic of this stage of opiate withdrawal syndrome
Stage 1
(also involves anxiety and drug craving)
Piloerection (“cold turkey skin”) is characteristic of this stage of opiate withdrawal syndrome
Stage 3
(also involves tachycardia, nausea and vomiting, hypertension, tremors, spasms, seizures)
Do mixed agonists/antagonists have physical dependence potential?
Low
Is withdrawal a problem with mixed agonists/antagonists?
Potential to induce withdrawal in opioid-dependent
Is milder (like meperidine/Demerol)
Opioid that is both a partial agonist and mixed agonist/antagonist:
Low antagonist action (less risk of triggering withdrawal in dependent patient)
Low abuse potential
Buprenorphine
Does Buprenorphine have abuse potential?
Low
Buprenorphine has low action of this; leading to less risk of triggering withdrawal in dependent patient
Low antagonist action
Opioid that is both a partial agonist and mixed agonist/antagonist:
Respiratory depression that does occur is not easily or fully reversed by naloxone
Buprenorphine
QT prolongation has been noted in this opioid that is both a partial agonist and mixed agonist/antagonist
Buprenorphine
Opioid that is both a partial agonist and mixed agonist/antagonist:
Contraindicated in heart patients or epileptics
(contraindications similar to morphine)
Pentazocine
Pentazocine is contraindicated in patients with either of these 2 conditions
Heart patients
Epileptics
Butorphanol, Buprenorphine, Nalbuphine and Pentazocine are opioids that are both partial agonists and this
Mixed agonists/antagonists
Butorphanol, Buprenorphine, Nalbuphine and Pentazocine are opioids that are both mixed agonists/antagonists and this
Partial agonists
Opioid receptor antagonist that blocks craving and subjective effects of opioids and alcohol
Naltrexone
Combining this opioid receptor antagonist with ketoconazole (CYP 3A4 inhibitor) may trigger withdrawal, as levels may increase nearly 13 fold
Naloxegol
Combining Naloxegol with this drug may trigger withdrawal, as levels may increase nearly 13 fold
Ketoconazole (CYP 3A4 inhibitor)
Are Naloxegol or Methylnaltrexone centrally or peripherally acting for opioid-induced constipation?
Peripherally
Opioid receptor antagonist that may be used for alcohol dependence
Naltrexone
Naloxone and Naltrexone are this type of drug
Opioid receptor antagonists
Naloxegol and Methylnaltrexone are this type of drug
Opioid receptor antagonists
(peripherally acting for opioid-induced constipation)
Only this isomer of opiates causes most of the action
L isomer
Both D or L forms of opiates can have this effect
Antitussive
Pinpoint pupils and depressed respiration are highly suggestive of overdose of this
Opiate
These 2 effects are highly suggestive of opiate overdose
Pinpoint pupils
Decreased respiration
What are opioid receptor antagonists used for?
Opiate overdosage and reversal
(Naltrexone also used for alcohol dependence)
Narcan nasal spray uses this opioid
Naloxone
Use of this opiate is associated with increased risk of QT prolongation (sudden cardiac death)
Methadone
Codeine is converted to this
Morphine
This type of opioid has lower abuse potential and may trigger withdrawal if used in a patient dependent on a different opiate
Mixed agonists/antagonists
Opioid that has very low antagonist activity noted, reported to have low levels of euphoria making it less likely to be abused, may be difficult to reverse using naloxone (requires very large doses at times)
Buprenorphine
Is withdrawal from opioids usually life-threatening or dangerous?
Rarely
Piloerection, mydriasis, diarrhea and yawning are important signs of this
Opioid withdrawal
This drug (NOT an opiate) is a selective allosteric inhibitor of voltage-gated sodium channel NaV1.8 that functions peripherally
Suzetrigine
This opiate may be difficult to reverse using naloxone (requires very large doses at times)
Buprenorphine
Which mixed opioid agonist/antagonist has the lowest risk of abuse?
Buprenorphine
What antagonist can reverse the respiratory depression of opiates?
Naloxone