Exam 2 Questions (Part 2) Flashcards

(33 cards)

1
Q

Procaine (Novocain)

A
  • Rapidly metabolized by blood cholinesterase to an allergen
  • Allergic reactions occur
  • Intermediate onset, short duration
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2
Q

Bupivacaine (Marcaine)

A
  • Slow to intermediate onset, long duration of action
  • Metabolized by CYP450 enzymes in liver
    a. Slower rate than for esters
    b. Good alternative if patients allergic to esters
  • Duration prolonged if liver function impaired
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3
Q

Levobupivacaine (Chirocaine)

A
  • active optical isomer of Bupivacaine (Marcaine)
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4
Q

Exparel

A

Long acting liposomal suspension approved for post surgical pain management

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5
Q

Lidocaine (Xylocaine)

A
  • Rapid onset, intermediate duration of action
  • Same metabolism pathway as bupivacaine
  • Transdermal patch: Lidoderm
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6
Q

Peripheral Nerve Block

A
  • Injection near nerve trunk

- Common for dental procedures, surgery on single extremity, etc

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7
Q

Epidural

A
  • Space between bone and dura mater
  • Large and accessible, route common for obstetrics
  • Type of central neural block
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8
Q

Intrathecal

A
  • Spinal Nerve Blockade: Subarachnoid Space
  • Most effective
  • Most dangerous
  • Patient position and solution density determine area blocked
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9
Q

Central Nerve Blocks (General)

A
  • Two types: Epidural and Intrathecal
  • Postural headaches most common complaint
  • Risk of hematoma if LMWH anticoagulants given concurrently
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10
Q

Sympathetic Block

A
  • Sympathetic activity increases with complex regional pain syndrome
  • Block usually occurs with central neural block, but can specifically inject area surrounding nerve chain ganglia
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11
Q

Diazepam (Valium): Skeletal Muscle Relaxant

A
  • Increased GABA inhibition (via BZ and GABAA receptors) of 1a afferents (presynaptic) thus inhibiting hyperactive reflex arcs; of supra spinal center (sedation)
  • Used for spasticity and muscle spasm
  • Broadest spectrum of BZDs
  • Sedation is a therapeutic benefit and side effect
  • Long term concerns: dependence and withdrawal
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12
Q

Carisoprodol (Soma, Vanadem)

Cyclobenzaprine (Flexeril)

A
  • Polysynaptic inhibitors (other centrally acting compounds)
  • MECHANISM: spinal cord reflex inhibition and sedation
  • USES: Often in combo with acetaminophen and aspirin
  • ADVERSE: Drowsiness, dizziness, dependence, tolerance.
  • Carisoprodol has an active metabolite, Meprobamate (Schedule IV)… avoid abrupt withdrawal
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13
Q

Baclofen (Lioresal)

A
  • Used to treat spasticity
  • Structurally similar to GABA
  • GABA-B receptor agonist… inhibits release of excitatory neurotransmitters. Results in inhibition of alpha motor neuron activity in spinal cord and pain pathways. Relaxation of skeletal muscle and some analgesia
  • Drug of choice for MS
  • ADVERSE: Drowsiness, muscle weakness, withdrawal syndrome
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14
Q

Intrathecal Administration for Baclofen (Lioresal)

A
  • Injection in subarachnoid space surrounding spinal cord
  • Programmable pump system
  • Maximize benefit (including analgesia), minimize side effects
  • Drawbacks
    a. Malfunction of pump system
    b. Tolerance require dose increase over time
    c. Severe withdrawal syndrome possible: merits black box warning
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15
Q

Dantrolene (Dantrium)

A
  • Inhibits Calcium release from sarcoplasmic reticulum in skeletal muscle cells (RyR Antagonist); inhibits muscle contraction
  • Indicated for severe spasticity regardless of cause, CVA, CP, spinal cord lesions, MS, malignant hyperthermia
  • Adverse Effects: Generalized muscle weakness, hepatotoxicity
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16
Q

Gabapentin (Neurontin)

A
  • Mechanism: Enhances GABA activity (antiseizure)

- Uses: Good in combination with others; also indicated fro chronic pain

17
Q

Tizanidine (Zanaflex)

A
  • Mechanism: Alpha 2 receptor agonist
  • Related to clonidine, but less BP effects
  • Inhibitory actions in spinal cord
    a. Presynaptic inhibition of excitatory interneurons
    b. Decreased activity of alpha motor neurons
  • Sedation and dry mouth similar to clonidine
18
Q

Botulinum Toxin

A
  • Mechanism: Binds to presynaptic vesicles and inhibits release of ACh; produces paralysis rather than relaxation
  • Uses: Indicated for dystonias and other specific muscle spasms; local injection paralyzes specific muscles
  • Also approved to treat excess sweating, wrinkles, chronic migraine, and urinary incontinence in patients with spinal injuries
  • Drawbacks: effects wear off in 2-3 months; limited number of muscles may be treated in a given session
  • CAUTION: May spread from injection site
19
Q

Tubocurarine (Curare)

A
  • Nondepolarizing blocker (receptor antagonist)
  • Competitive, reversible Nm receptor antagonist.
    a. physically blocks ion channels associated with N receptors
    b. actions can be reversed by ACh
    c. No effect on M receptors
  • Muscle Paralysis Order: Head and neck, limbs, respiratory muscles
  • Adverse effects: Histamine release, hypotension, inhalation anesthetics and certain antibiotics enhance NMJ blockade
20
Q

Antidotes to Curare

A
  • AchE Inhibitors

- Sugammadex (Bridion)

21
Q

Endogenous Opioid Peptides

A
  • Inhibitory transmitters which modify most aspects of pain transmission and perception.
  • Modulate hormonal fluctuations, thermoregulation, stress, anxiety, GI function, pain
  • Three families of peptides have been identified
    a. Pentapeptides (met and leu-enkephalin)
    b. Dynorphins
    c. Endorphins
22
Q

Opioid Mixed Agonists/Antagonists

A

PROTOTYPES

  • Butorphanol (Stadol)
  • Buprenorphine (Buprenex, Butrans)

GENERAL

  • Analgesia due primarily to Kappa receptor activity
  • Only partial agonists or antagonists at mup receptor
    a. may displace stronger agonists from mu receptor sites
    b. may precipitate withdrawal in addicts
  • Mized receptor activity results in “ceiling” (less efficacious) analgesic and respiratory depression with decreased dependence liability

ADVERSE SIDE EFFECTS

  • Dysphoria
  • Anxiety
  • Hallucinations
23
Q

Opioid Antagonist Prototypes

A

PROTOTYPES

  • Naloxone (Narcan) iv
  • Naltrexone (ReVia) po

GENERAL

  • Pure competitive antagonists: highest affinity for mu receptors
  • Used to treat overdoses, accelerate postop recovery, or treat dependence
  • Precipitate withdrawal syndrome in opioid addicts
24
Q

Prototype Opioid Analgesic

A

Prototype: Morphine

PHARMACOLOGICAL ACTIONS: CNS

  • General
    a. With Pain: Analgesia, euphoria, drowsiness, mental clouding
    b. Without Pain: Nausea, apathy, dysphoria prominent
  • Analgesia
  • Pupillary Constriction (good indicator of abuse; no tolerance)
  • Respiratory Depression
  • Suppression of Cough Reflex
  • Nausea and vomiting via stimulation of chemoreceptor trigger zone in brainstem

GI TRACT

  • Decreases glandular secretions
  • Decreases propulsive peristalsis, increases non-propulsive contractions
  • Increase biliary tract pressure

GENITOURINARY TRACT

  • Increase bladder detrusor and sphincter tone: urinary retention and exacerbation of pain due to kidney stones
  • May prolong labor

PHARMOKINETICS

  • Erratic po absorption: extensive first pass metabolism
  • easily crosses placental barrier and fetal BBB
  • Hepatic Metabolism: active metabolite

ADVERSE EFFECTS

  • Tolerance: lack of effectiveness after repeated dosing
  • Dependence: Higher doses required for sufficient pain relief: lacrimation, chills, goosebumps, hyperthermia, mydriasis, anxiety, hostility
  • Overdose: Stupor, coma, respiratory depression, hypotension
25
Naloxone (Narcan, iv)
- Opioid antagonist - Occupy opioid receptor without producing a pharmacological effect - Reverse CNS and GI effects of morphine - Several injections may be required (1 hr half life) - May precipitate sudden and intense withdrawal in opioid addicts
26
Naltrexone (Vivitrol)
- Opioid antagonist - Given po, longer half life (10 hours) - Indications: opioid dependence, apnea in children, alcohol dependence
27
Methadone
- Similar to morphine, with longer duration of action and a longer, but less intense withdrawal syndrome - Used primarily in heroin detoxification and maintenance programs
28
Meperidine (Demerol)
- More consistent oral absorption than morphine - Primary Metabolite: Normeperidine a. May produce CNS excitation and convulsions b. Less respiratory depression than morphine - Fewer GI and GU tract effects - Indicated for labor pain
29
Fentanyl (Sublimaze)
- Anesthesia a. Adjunct: Sedative, anxiolytic and analgesic properties b. Used alone for certain types of CV surgery c. Regional analgesia via direct injection into epidural spaces of the spinal cord (morphine also used) - Transdermal system available for chronic pain (Duragesic) - Iontophoretic system (Ionsys) - Buccal/Transmucosal Admin: Lollipop (Actiq)
30
Partial Mu Agonists with Lower Maximum Efficacy
Codeine - metabolized in part to morphine - genetic variation in the P450 enzyme producing morphine result in decreases or increases in analgesic and respiratory depressant effect
31
Oxycontin
- Oxycodone controlled release form - To be swallowed whole to release drug over 24 hour - Extensive abuse
32
Targiniq ER
- Oxycodone + naloxone | - Designed to prevent abuse via inhalation or injection
33
Tramadol (Rybix, Ryzolt, Ultram)
- Weak mu agonist, strong inhibitor of NE/5HT reuptake - Unique adverse effect: seizures - Caution: May cause respiratory depression in children