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PHARMACOLOGY > CHAPTER 14: OPIOIDS > Flashcards

CHAPTER 14: OPIOIDS Flashcards

1
Q

NARCOTICS: purpose

A

provide treatment for acute or chronic pain
- effect on brain and spinal cord, alter impulses from peripheral nerves

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2
Q

PAIN: 3 types

A
  • PAIN is subjective, ppl respond differently

nociceptive: caused by direct pain receptor stimulus (direct damage to body)

neuropathic pain: caused by nerve injury (ex: diabetes)

psychogenic pain: associated w emotional, psychological, or behavioral stimuli

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3
Q

PAIN: acute v. chronic

A

acute: caused by tissue injury, person aware of injury and leads to seek care

chronic: constant/intermittent pain, keeps occurring past time area would be expected to heal, interfere w daily living

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4
Q

Narcotics: opioids intro
- 3 types
-primary effect

A

Opioids: natural, semisynthetic, or synthetic
- produce morphine like effects

primary effect: relieve pain from surgery, injury, or chronic disease

substance of abuse

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5
Q

endogenous neurotransmitters
- molecules
- found where

A

narcotics have diff type of opioid receptors that respond to naturally occurring molecules/pain reducers:
- enkephalins
- dynorphins
- endorphins

found in CNS, peripheral nerves, gi tract cells

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6
Q

diff types of opioid receptors details

A

Mu: primary pain blocking (analgesia), resp depression
delta: modulate pain transmission, react w enkephalins in periphery
kappa: some analgesia, mydriasis, sedation

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7
Q

Opioid Receptors MOA
- goal?

A

all G PROTEIN COUPLED RECEPTORS
- Gi–> inhib adenylyl cyc, activate K+ channel, deactivate Ca2+ channel (hyperpolarize)

open and close based on AP
GOAL IS LESS TRANSMISSION OF PAIN SIGNAL

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8
Q

Narcotic Agonists: therapeutic use

A
  • agonist to specific opioid rec in CNS to produce analgesia, euphoria, and sedation

-relieve mod/severe acute/chronic pain
-preop meds
-analgesia during anesthesia
-antitussive (anti COUGHING)

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9
Q

Narcotic Agonists: MORPHINE
- receptor
- actions
- routes

A
  • Mu receptor
    ACTIONS: euphoria, resp depression (dose dep), miosis, emesis, constipation, histamine release, dec release hormones
    high dose: hypotens/bradycardia

ROUTES: SC, IV, IM, oral only ER form
some metab still active

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10
Q

Narcotic Agonists: Codeine
- actions
- cautions

A
  • less potent than morphine–> convert into morphine in LIVER
    ACTIONS: analgesia, antitussive

CAUTIONS: life-threatening resp depression, death in children

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11
Q

Narcotic Agonists: Oxycodone and Oxymorphone
- stronger or weaker
- formulations of each

A
  • semisynth analog of morphine
    parenterally STRONGER than morphine
  • formulate w aspirin and acetaminophen sometimes

oxycodone: PO ER form
oxymorphone: PO immediate acting and ER (also avail IM labor, SC, IV)

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12
Q

Narcotic Agonists: Fenatnyl

A
  • synthetic
  • use for anesthesia (IV, epidural, intrathecally)
  • oral transmucosal for treat cancer pain
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13
Q

Narcotic Agonists: Methadone

A
  • synthetic
  • mu rec AGONIST
  • SNRI and NMDA ANTAGONIST
  • for nociceptive and neuropathic pain
  • less euphoria, longer duration compared to morphine
  • used for controlled withdrawal of abusers
  • long half life, accum in fat tissue, can lead to toxicity
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14
Q

narcotic agonists: ADVERSE EFFECTS
- CNS, CV, GI, GU, Others

A

CNS: lightheaded, dizzy, anxiety, fear, psychoses, hallucination, impaired mental process

CV: orthostat hypo

GI: nausea, vomit, constipation (OIC)

GU: ureteral spasm, urine retention, lose libido

OTHER: sweat, physical/psych dependence, withdrawal

narc induced respiratory depression, apnea, cardiac arrest, shock

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15
Q

methylnaltrexone- CONSTIPATION

A
  • opioid antagonist
  • mu receptor blocked–> responsible for constipation
  • SC once a day
  • doesn’t cross BBB

antagonist to treat the effect of agonists

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16
Q

DRUG-DRUG Interactions

A

barbiturates, phenothiazines, MAOIs–> resp depression, hypotension, sedation/coma

SSRI, MAOI, TCA–> inc risk of serotonin syndrome if taken w tapentadol (blocks NE reuptake)

17
Q

MIXED AGONISTS/ANTAGONISTS
- narcotic agonists-antagonists

A
  • act on certain opi rec but block others
  • less abuse potential
  • similar analgesic effect like morphine
18
Q

narcotic agonists-antagonists is/isnt used for which kinds of PTs

A
  • opioid naive PT: never taken opi before, drug is used to treat their pain
  • PT previously exposed to opi, may worsen withdrawal
19
Q

narcotic agonists-antagonists: therapeutic uses

A
  • relief mod/severe pain
  • pre-anesthetic med, supplement surgical anesthesia
  • relieve chronic pain in those susceptible to narcotic dependence
20
Q

Buprenorphine
- type of agonist

A
  • partial ago of mu, antagonist of K rec
  • lipophilic
  • high affinity for receptors/long duration action
  • ceiling effect: less euphoria, lower abuse potential
  • office based treatment
21
Q

Pentazocine

A
  • agonist K, partial agonist mu receptors
  • less euphoria
  • HIGH DOSE= resp depression, inc BP, tachy, hallucination
  • hospital settings
22
Q

DRUG DRUG INTERACTIONS: mixed ago/antagonists

A

tripelennamine: inc hallucinogenic and euphoric effect w pentazocine (Ts and Blues)

trip= antihistamine

23
Q

NARCOTIC ANTAGONISTS

A
  • bind strongly to opi rec but DON’T activate
  • BLOCK receptor, reverse effects of opioids (resp depression and sedation)
24
Q

Narcotic antagonists: Indications

A
  • complete or partial reversal or narcotic depression
  • opi overdose
25
Q

Narcotic Antagonists (2)

A

Naloxone/narcan: reverse AE of narcotics, nasal or autoinjection
- COMPETITIVE antagonists of ALL 3 RECEPTORS

Naltrexone: orally, manage alc/narcotic dependence AFTER PT is detoxified
- tablet or injection
- COMPETITIVE antag of ALL 3 receptors
- LONGER duration of action
hepatotoxicity

26
Q

Narcotic Antagonists: Adverse Effects

A

CNS: excitement, reversal analgesia
CV: tachy, BP changes, dysrhythmias, pulmonary edema

27
Q

Acute Narcotic abstinence syndrome

A

nausea, vomit, tachy, hypertension, anxiety

  • naloxone challenge should be administered before giving naltrexone to avoid acute reactions

naloxone challenge: off drug at least 7-10 days before moving to naltrexone, we use naloxone bc of shorter duration of action so we don’t risk withdrawal symptoms

PHARMACOLOGY (29 decks)

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