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D&T II Exam 2 > Treatment of Pain > Flashcards

Treatment of Pain Flashcards

1
Q

Pharmacologic Approaches

A

Non-opioid analgesics, opioids, alpha2 adrenergic, antidepressants, anti epileptic, topical/local analgesics, NMDA receptor antagonists, Muscle relaxants

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2
Q

Non opioid analgesics

A

Mechanism: inhibition of COX
Use: mild to moderate pain, soft tissue injury, strains, sprains, HA, and arthritis
Other: Synergistic when combined with opioid
Side Effects: Acetaminophen is hepatotoxic, NSAIDs and Aspirin cause gastric ulcers and inhibit platelet aggregation
Cautions: Acetaminophen in liver disease and alcoholics, Avoid NSAIDs in patients on aspirin for CV protection

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3
Q

Opioid Receptors

A

mu, delta, and kappa
all three cause the activation of inwardly rectifying K+ channels, inhibition of Ca2+ channels, and inhibition of adenylyl cyclase

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4
Q

Mu receptor

A

found in CNS (neocortex, thalamus, nucleus accumbens, hippocampus, and amygdala) and myenteric neurons in gut and vas deferens
mediates supra spinal analgesia, respiratory depression, euphoria, dependence, and mitosis gastric transit

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5
Q

Mu receptor agonists and antagonists

A

Endogenous agonists: endomorphin 1&2, enkephalins, and beta endorphin
Drug agonists: morphine, fentanyl, methadone, meperidine, buprenorphine
Antagonists: naloxone, naltrexone

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6
Q

Delta Receptor

A

found in olfactory bulb, nucleus accumbent, caudate, putamen, neocortex
Involved in affective behaviors

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7
Q

Delta Receptor Agonists and antagonists

A

Endogenous agonists: enkephalins
Drug Agonists: None
Antagonists: Naltrindole

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8
Q

Kappa Receptor

A

Found in cerebral cortex, nucleus accumbent, claustrum, hypothalamus, spinal cord
Mediates spinal cord analgesia, mitosis, and sedation

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9
Q

Kappa Receptor Agonists and Antagonists

A

Endogenous agonists: dynorphins

Drug agonists: Butorphanol, Pentazocine, nalbuphine

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10
Q

Strong Opioid Agonists

A

Morphine, Hydromorphone, Methadone, Heroin, Oxycodone, Meperidine, Fentanyl, Alfentanil, Remifentanil, Sufentanil

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11
Q

Moderate to Low Agonists

A

Codeine, Propoxyphene

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12
Q

Mixed Agonists/ antagonists

Partial agonists

A

Buprenorphine, Pentazocine, Butorphanol, Nalbuphine

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13
Q

Antagonists

A

Naloxone, Naltrexone, Nalmefene

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14
Q

Morphine

A

Gold Standard, acts at mu receptor impacting respiration, pain perception, mood, and emotion, acts at kappa receptor in spinal cord, prevents substance P release
Use: relief of moderate to severe acute and chronic pain, pulmonary edema, preanesthetic
Interactions: phenothiazines, MAO-Is, TCAs
Contraindication: Hepatic insufficiency, respiratory insufficiency, or head injury
Administered: SC/IM/PO/suppository/pump
Metabolism: glucoronide conjugation with urinary excretion

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15
Q

Morphine effects

A

analgesia without loss of consciousness, drowsiness, itchy nose, euphoria, dysphoria, nausea and vomiting, miosis, depressed respiration, peripheral vasodilation, constipation, decrease levels of LH and testosterone

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16
Q

Morphine Withdrawal

A

rebound phenomenon, hyperalgesia, hyperventilation, dilation of pupils, diarrhea, and dysphoria

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17
Q

Cough Suppression

A

codeine/hydrocodone
decrease sensitivity of CNS cough centers, decrease mucosal secretion
CYP2D6 converts codeine to morphine

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18
Q

Hydromorphone

A

hydrogenated ketone of morphine, used for severe pain, PO/IV/IM/extended release

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19
Q

Methadone

A

analgesic, no kappa activity, constipation and biliary spasms common, long half life
used in Tx of opiate withdrawal, tolerance develops slower

20
Q

Heroin

A

Diacetylmorphine –> 6-monoacetylmorphine –> morphine

Diacetyl and 6mono have higher BBB penetration

Urine tests look for 6mono

21
Q

Hydrocodone + Acetaminophen

A

orally equipotent to morphine, moderate to severe pain, cough

22
Q

Oxycodone

A

management of moderate to severe pain, in combo with nonopijoid analgesics, orally active

Oxycontin - delayed release formulation has large potential for abuse
can be combined with ibuprofen, aspirin, or acetaminophen

23
Q

Synthetic Derivatives

A

Meperidine, Fentanyl, Sufenanyl, Alfentanil, Remifantanil

24
Q

Meperidine

A

mu agonists, less potent, CNS stimulant at toxic doses, not blocked by naloxone, respiratory depression, postural hypotension, doesn’t suppress cough, better bioavailability, tolerance develops slower

MAO-I + Meperidine = excitation, delirium, hyperpyrexia, convulsions, respiratory depression

25
Q

Fentanyl

A

mu agonist, analog of meperidine, 80x as potent, available as a patch or lozenge, IV pre/post surgery, rapid onset, short duration, produce less nausea

26
Q

Fentanyl derivatives

A

Sufentanil - mu agonist, 6000 x as potent, IV, expensive, less hemodynamic instability, respiratory depression and chest wall rigidity
Alfentanil - mu agonist
Remifentanil - mu agonist, short acting, 20x more potent than alfentanil

27
Q

Codeine

A

less potent analgesic than morphine, used with non-opioids, in cough syrups
Uses: pain control, relief of acute and chronic pain, terminal illness, cough, to produce constipation, opium tincture/paregoric
Metabolized to morphine by CYP2D6, slow metabolizers (codeine is ineffective) fast metabolizers (leads to overdose)

28
Q

Propoxyphene

A

weak mu agonist

used in combo with acetaminophen or aspirin, less potential for dependence

29
Q

Pentazocine

A

PO, weak mu antagonist, kappa agonist
analgesia, sedation, respiratory depression
may block morphine analgesia, may cause withdrawal
used for acute pain
now combined with Naloxone to prevent drug abuse
has psychotomimetic effects
if given tripelennamine with pentazocine creates high degree of euphoria

30
Q

Buprenorphine

A

partial mu agonist, kappa antagonist
less effective analgesia than morphine
IM/IV/sublingual
Used for Tx of opioid dependence

31
Q

Tramadol

A

chemically unrelated, binds opiate receptors, inhibits NE and 5-HT reuptake, partial inhibition by naloxone
Side effects: constipation, nausea, vomiting, dizziness, drowsiness
PO for moderate pain

32
Q

Opiate antagonists

A

binds to mu receptor, no analgesia, used to treat opioid poisoning and prevention of dependence/addiction

Naloxone: used in opioid OD, IM/IV half life = 1 hour
Nalmefene: IV, half life = 10 hours, more potent
Naltrexone: PO, half life = 24 hours, use for alcoholism

Antagonists can induce withdrawal

33
Q

Dextromethorphan

A

synthetic derivative of morphine, suppresses response of cough center, elevates threshold, no analgesia, less constipation, not antagonized by naloxone, Robotripping

34
Q

Clonidine

A

alpha 2 adrenergic agonist, NE inhibits pain by activation of pre and post alpha 2 receptors stimulation in projection neurons of dorsal horn and primary afferents
Uses: neuropathic pain, cancer pain

35
Q

Antidepressants

A 
TCA - amitriptyline
SNRI - Venlafaxine, Duloxetine
NE and 5HT reuptake inhibitors promote NE activation of pre and post receptors in projection neurons of dorsal horn and primary afferents
Use: neuropathic pain
SSRIs are ineffective in pain
36
Q

Antiepileptics

A 
alpha2delta ligands (gabapentin, pregabalin): reduce activation of N and P/Q Ca2+ channels
Carbamazepine: stabilize inactive state of voltage gated sodium channels
Uses: neuropathic pain, post herpetic neuralgia, diabetic neuropathy, fibromyalgia, trigeminal neuralgia
37
Q

Capsaicin

A

chili pepper alkaloid adjunctive, TRPV1 antagonist

38
Q

Ketamine

A

blocks NMDA and thus glutamate signaling

39
Q

Centrally Active Muscle Relaxants

A

used as antispasmodics or in relief of lower back pain

can interact with CNS depressants

40
Q

Baclofen

A

Gaba receptor activator
Uses: spasticity and hiccups
Takes 3-4 days to work, PO, 85% excreted intact
Side effects: drowsy, vertigo, dizzy, insomnia, slurred speech, ataxia, hypotonia, weakness, chest pain, syncope

Avoid abrupt withdrawal - leads to organ failure and fatalities, hyperpyrexia, obtundation, spasticity, rigidity, and rhabdomyolysis

41
Q

Diazepam

A

Use: IV/IM for muscle spasms

PO for muscle relaxant

42
Q

Carisoprodol

A

unknown mechanism
use: acute musculoskeletal
PO- rapid onset, last 4-6 hours, CYP2C19, active metabolite- meprobamate
Side effects: anticholingeric activity, drowsy, dizzy, headache, agitation
Don’t use if you are old or under 16, do not use for more than 2-3 weeks because tolerance and dependence, be careful in patients with history of drug abuse

43
Q

Chlorzoxazone

A

unknown mechanism
Use: acute muscle spasm and pain
PO- onset in 1 hour, last 6-12 hours, hepatic glucuronidation, metabolized by CYPs
Side effects: Drowsy, Dizzy, Light headed, malaise, liver dysfunction
Don’t use in elderly
Get periodic liver tests

44
Q

Cyclobenzaprine

A

Use: acute muscle spasms and pain, TMJ
Large half life
CYP3A4,1A2,2D6
Side effects: related to TCAs, drowsy, dizzy, fatigue, headache, irritability, xerostemia
Be careful with elderly, do not use if liver impaired

45
Q

Tizanadine

A

alpha 2 adrenergic agonist, related to clonidine, acts at spinal cord
Use: Tx of muscle spasticity, tension headaches, lower back pain
PO onset 1-2 hours, Hepatic CYP1A2
Side Effects: Hypotension, Bradycardia, Somnolence, Dizzy, visual hallucinations, anxiety, depression, Xerostemia, Weakness, increased liver enzymes
Use care in elderly

D&T II Exam 2 (7 decks)

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