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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
Q

when does tolerance to opioids develop?

A
  • when used CHRONICALLY
  • higher doses needed to control pain
  • occurs RAPIDLY
  • more common w/ drugs w/ lower efficacy
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26
Q

when does physical dependence to opioids occur?

A
  • may occur from desensitization of Mu receptors (or uncoupling?)
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27
Q

when does withdrawal occur w/ opioids?

A
  • if stopped abruptly
28
Q

what decreases the development of tolerance to opioids?

A
  • NMDA antagonists
29
Q

to what effects does tolerance develop w/ opioids?

A
  • analgesia, sedation, euphoria, N/V, respiratory depression
30
Q

to what effects does tolerance NOT develop w/ opioids?

A
  • miosis
  • constipation
  • seizures
31
Q

opioids: adverse effects

A
  • N/V
  • constipation
  • urinary retention (worse w/ BPH)
  • respiratory depression (dose dependent)
32
Q

opioids & histamine?

A
  • 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
Q

when does tolerance and dependence to opioids develop?

A
  • 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
Q

symptoms withdrawal?

A
  • dysphoria, anxiety, insomnia
  • anorexia
  • yawning
  • chills, goosebumps
  • vomiting, diarrhea
  • rhinorrhea, lacrimation
  • incr BP, HR, temp
  • muscle aches/twitches
35
Q

how to help symptoms of withdrawal from opioids?

A
  • reduced by use of Clonidine or antagonist (Methadone)
36
Q

What to do in case of overdose?

A
  • support respiration

- use opioid antagonist (Naloxone)

37
Q

symptoms of opioid overdose?

A
  • CNS depression
  • respiratory depression
  • pin point pupils (may dilate if severely hypoxic)
38
Q

opioids: clinical uses, analgesia

A
  • 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
Q

opioids: clinical uses, acute pulmonary edema

A
  • relieves dyspnea
40
Q

opioids: clinical uses, antitussive

A
  • codeine

- dextromethorphan

41
Q

opioids: clinical uses, diarrhea

A
  • loperamide

- dephenoxylate/atropine

42
Q

opioids: clinical uses, anesthesia

A
  • General - adjunct to control pain

- spinal - epidural w/ local anesthetics

43
Q

opioids: drug interactions

A
  • 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
Q

opioids: contraindications

A
  • 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
Q

precautions w/ Meperidine?

A

seizures

46
Q

Morphine: moa

A
  • stimulates ALL opioid receptors
  • strong agonist
  • produces all effects opioids
47
Q

morphine: info

A
  • 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
Q

hydromorphone: info

A
  • 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
Q

Methadone: moa

A
  • stimulates Mu RECEPTORS
50
Q

methadone: info

A
  • 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
Q

meperidine: moa

A
  • Mu AGONIST
52
Q

meperidine: info

A
  • 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
Q

Fentanyl: info

A
  • 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
Q

hydrocodone: info

A
  • 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
Q

oxycodone: info

A
  • 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
Q

codeine: info

A
  • 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
Q

pentazocine: info

A
  • 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
Q

buprenorphine: info

A
  • PARTIAL AGONIST Mu, maybe kappa
  • low abuse potential
  • decreases craving for drug
  • admin = injection, sublingual, intranasal
  • combined w/ nalaxone (sublingual will work)
59
Q

Tramadol: info

A
  • mild to moderate pain
  • Weak Mu agonist, inhibit 5-HT re-uptake
  • side effects mild = dizziness, sedation, constipation, nausea
60
Q

Tramadol + antidepressants = ___

A

seizures

61
Q

Tramadol + MAOIs/TCAs/SSRIs = ___

A

serotonin syndrome

62
Q

dextromethorphan: info

A
  • 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
Q

Naloxone: info

A
  • 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
Q

Naltrexone: info

A
  • 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
Q

difference between Nalmefene & Naloxone?

A
  • Nalmefene = longer duration of action, less liver toxicity

KG - pharmacology 3 (11 decks)

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