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KG - pharmacology 3 > KG - Pharm 3, Exam 1, Opioids & Antagonists > Flashcards

KG - Pharm 3, Exam 1, Opioids & Antagonists Flashcards

1
Q

what do opioid agonists do?

A
  • released in response to pain

- decrease responsiveness to pain

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2
Q

how do Mu receptors work?

A
  • close voltage gated Ca2+ channels on presynaptic nerve terminals (this decreases neuronal activity in these pathways)
  • open K+ channels (causes hyperpolarization, inhibiting nerve transmission)
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3
Q

effects Mu receptors?

A
  • analgesia
  • euphoria
  • sedation
  • side effects
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4
Q

effects Kappa receptors?

A
  • analgesia in some ppl, dysphoria in other ppl
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5
Q

effects delta/sigma receptors?

A
  • dysphoria
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6
Q

effects opioids - pain transmission?

A
  • direct action at inflamed and damaged tissue
  • inhibition of release of excitatory transmitters in dorsal horn - spinal anesthesia
  • thalamic action

GOAL: less signal gets to cortex, decrease suffering associated w/ pain

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7
Q

effect opioids - pain modulation?

A
  • periaqueductal gray, may cause release of endogenous opioids as well
  • rostral ventral medulla
  • NE pathway from locus coeruleus to dorsal horn may also decrease pain
  • inhibition of neurons may increase the activity of pathways that inhibit pain
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8
Q

opioids, effect on GABA?

A
  • GABA usu inhibits descending neuronal pathways that modulate pain
  • opioids decrease release of GABA, allowing pathways to be activated
  • decreases pain transmission in dorsal horn of spinal cord
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9
Q

effects opioids - analgesia?

A
  • decreases sensation of pain
  • decreases reaction to pain
  • tolerance develops to analgesia (titrate dose based on hx)
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10
Q

effects opioids - sedation/mental clouding

A
  • not used as sleep aids, diff kind of sedation

- disrupt REM

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11
Q

morphine overdose causes ___

A

CNS depression

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12
Q

codeine/meperidine overdose causes ___

A

excitement

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13
Q

effects opioids - euphoria/dysphoria?

A
  • sense of floating/pleasure
  • prob depends on receptor distribution in ppl
  • some find experience dysphoric
  • kappa/delta receptors = dysphoric
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14
Q

effects opioids - EMESIS?

A
  • N/V (esp w/ morphine)

- stimulate chemoreceptor trigger zone in brain (CTZ)

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15
Q

effects opioids - antitussive?

A
  • lower dose than for analgesia
  • codeine & dextromethorphan = effective
  • codeine = not good analgesic
  • Meperidine DOESN’T suppress cough
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16
Q

effects opioids - RESPIRATORY DEPRESSION?

A
  • common in overdose, also w/ therapeutic doses
  • decreases response of brain stem to elevated CO2
  • not good in ppl w/ pulmonary dz
  • bronchoconstriction?
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17
Q

effects opioids - elevated intracranial pressure?

A
  • increased CO2 causes vasodilation, increases cerebral blood flow, increases pressure
  • watch out in patients w/ head trauma
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18
Q

effects opioids - MIOSIS?

A
  • except w/ Meperidine (causes dilation instead)
  • no tolerance to this side effect
  • parasympathomimetic - blocked by atropine
  • common in overdose, but may convert to dilation in comatose patients
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19
Q

effects opioids - body temp?

A
  • decreased

- dysregulation in hypothalamus

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20
Q

effects opioids - truncal rigidity?

A
  • supraspinal effect increases tone of large trunk muscles
  • may interfere w/ respiration/ventilation
  • most common w/ FENTANYL
  • use neuromuscular blockers to prevent this effect
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21
Q

effects opioids - cardiovascular?

A
  • BRADYCARDIA
  • decr BP
  • from CNS vasomotor depression/release of histamine?
  • tachycardia w/ Merperidine (anticholinergic)
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22
Q

effects opioids - GI?

A
  • decr gastric activity, local & CNS
  • CONSTIPATION!!! (be proactive w/ laxative!)
  • decr gastric motility
  • biliary colic, constriction of sphincter of Oddi
  • decreased secretions
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23
Q

effects opioids - GU?

A
  • ADH effect - decr urine output
  • decr renal blood flow
  • increases sphincter tone - harder to urinate
  • increases urethral tone - harder to pass stones
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24
Q

effects opioids - uterus?

A
  • may prolong labor
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25
when does tolerance to opioids develop?
- when used CHRONICALLY - higher doses needed to control pain - occurs RAPIDLY - more common w/ drugs w/ lower efficacy
26
when does physical dependence to opioids occur?
- may occur from desensitization of Mu receptors (or uncoupling?)
27
when does withdrawal occur w/ opioids?
- if stopped abruptly
28
what decreases the development of tolerance to opioids?
- NMDA antagonists
29
to what effects does tolerance develop w/ opioids?
- analgesia, sedation, euphoria, N/V, respiratory depression
30
to what effects does tolerance NOT develop w/ opioids?
- miosis - constipation - seizures
31
opioids: adverse effects
- N/V - constipation - urinary retention (worse w/ BPH) - respiratory depression (dose dependent)
32
opioids & histamine?
- opioids can produce histamine release - can cause flushing, itching, sweating - could be due to central effects opioids - more common w/ injections - pretreat w/ Benadryl
33
when does tolerance and dependence to opioids develop?
- in ppl who use opioids chronically - for euphoric effect - more likely if UNDERPRESCRIBED (reward pathway activated - if given before pain too bad, reward pathway not stimulated)
34
symptoms withdrawal?
- dysphoria, anxiety, insomnia - anorexia - yawning - chills, goosebumps - vomiting, diarrhea - rhinorrhea, lacrimation - incr BP, HR, temp - muscle aches/twitches
35
how to help symptoms of withdrawal from opioids?
- reduced by use of Clonidine or antagonist (Methadone)
36
What to do in case of overdose?
- support respiration | - use opioid antagonist (Naloxone)
37
symptoms of opioid overdose?
- CNS depression - respiratory depression - pin point pupils (may dilate if severely hypoxic)
38
opioids: clinical uses, analgesia
- for acute pain, trauma, cancer, terminal pain - for chronic non-terminal pain - sedation common - stay ahead of dosing - combine w/ non-opioids when possible - titrate to degree of pain - PATIENT CONTROLLED ANALGESIA used POST-SURGERY
39
opioids: clinical uses, acute pulmonary edema
- relieves dyspnea
40
opioids: clinical uses, antitussive
- codeine | - dextromethorphan
41
opioids: clinical uses, diarrhea
- loperamide | - dephenoxylate/atropine
42
opioids: clinical uses, anesthesia
- General - adjunct to control pain | - spinal - epidural w/ local anesthetics
43
opioids: drug interactions
- sedative hypnotics = incr CNS & respiratory depression - antipsychotics = sedation - MAOIs = MEPERIDINE & DEXTROMETHORPHAN serotonin syndrome, may inhibit serotonin re-uptake, AVOID OPIOIDS w/ MAOIs - CYP2D6 inhibitors = codeine, oxycodone, hydrocodone not metabolized to active compounds - FLUOXETINE & PAROXETINE worst for inhibition
44
opioids: contraindications
- use of partial agonist w/ full agonist (impairs analgesia, cause withdrawal) - pts w/ head injuries (incr cranial pressure) - pregnancy (esp delivery) - impaired pulm function - impaired hepatic/renal function - some endocrine diseases
45
precautions w/ Meperidine?
seizures
46
Morphine: moa
- stimulates ALL opioid receptors - strong agonist - produces all effects opioids
47
morphine: info
- for SEVERE PAIN - admin = oral, parenteral, rectal, intrathecal, epidural - more effective when INJECTED (high first pass metabolism) - short half life - for chronic/terminal its use extended release
48
hydromorphone: info
- STRONG analgesic, more potent than morphine - MOD to SEVERE pain - good for renal dysfunction bc no metabolites - less likely to cause histamine release/itching - admin = oral, sc, IV, IM, rectal
49
Methadone: moa
- stimulates Mu RECEPTORS
50
methadone: info
- long half life/duration of action - used for maintenance tx of addicts - LOW DOSES USED TO PREVENT WITHDRAWAL SYMPTOMS - WITHDRAWAL MORE MILD, but MORE PROLONGED - used for LONG TERM CONTROL OF PAIN - for hard to treat pain - lower incidence tolerance to analgesia
51
meperidine: moa
- Mu AGONIST
52
meperidine: info
- cause EUPHORIA - only use for 48 hrs (can cause renal failure from metabolite - normeperidine, seizures) - anticholinergic, TACHYCARDIA, PUPIL DILATION - NO COUGH SUPPRESSION - obstetrics, less resp dep in baby - less constipation/urinary retention than morphine - SEROTONIN SYNDROME WITH MAOIs!!!
53
Fentanyl: info
- highly potent, lipid soluble - short half life - HIGH ABUSE POTENTIAL (anesthesiologists) - for SHORT surgical procedures - cause truncal rigidity if given rapidly via IV - available in patches/lollipops - metal by CYP3A4
54
hydrocodone: info
- moderate to severe pain - often combined w/ acetaminophen (Vicodin) - usu oral - conversion by CYP2D6 needed for analgesic effect (doesn't work as well in pts on SSRIs - esp fluoxetine, paroxetine) - schedule II (or III if combo) - often abused
55
oxycodone: info
- moderate to severe pain - for Tourette's, restless leg - admin = oral - often combined w/ acetaminophen or aspirin - metab by CYP2D6 - incr analgesic effectiveness (FLUOXETINE inhibits and decreases effectiveness) - schedule II
56
codeine: info
- COUGH SUPPRESSANT (dose lower than for analgesia) - mild to moderate pain - must be metab by CYP2D6 to be active (inhibited by FLUOXETINE) - converted to morphine - usu admin = oral (combined w/ acetaminophen or aspirin) - some abuse potential - not for small kids - schedule II alone, III when combined, IV if cough
57
pentazocine: info
- Kappa RECEPTOR AGONIST, Mu PARTIAL AGONIST - moderate pain - admin = oral, injected - less sedating - less resp depression, GI effects (all mediated by Mu) - may cause DYSPHORIA (kappa?) - low abuse potential, schedule IV
58
buprenorphine: info
- PARTIAL AGONIST Mu, maybe kappa - low abuse potential - decreases craving for drug - admin = injection, sublingual, intranasal - combined w/ nalaxone (sublingual will work)
59
Tramadol: info
- mild to moderate pain - Weak Mu agonist, inhibit 5-HT re-uptake - side effects mild = dizziness, sedation, constipation, nausea
60
Tramadol + antidepressants = ___
seizures
61
Tramadol + MAOIs/TCAs/SSRIs = ___
serotonin syndrome
62
dextromethorphan: info
- COUGH SUPPRESSANT - not likely to cause constipation - BLOCKS NMDA RECEPTORS - abuse potential - decreases 5-HT re-uptake (SEROTONIN SYNDROME w/ MAOIs) - drug of abuse in teens (deaths)
63
Naloxone: info
- DOC opioid overdose - can reverse resp depression, consciousness, awareness of pain, miosis, constipation - INJECTION - GIVE UNTIL PUPILS DILATE! - short duration of action (2 hrs) - may need repeat dosing - now being combined w/ agonists to prevent abuse
64
Naltrexone: info
- admin = ORAL - long acting (24 hrs) - for tx opioid addicts - WILL PRECIPITATE WITHDRAWAL - decreases craving in recovering alcoholics - MAY CAUSE LIVER TOXICITY when used chronically
65
difference between Nalmefene & Naloxone?
- Nalmefene = longer duration of action, less liver toxicity

KG - pharmacology 3 (11 decks)

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