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N926 Pharmacology > non-opioids > Flashcards

non-opioids Flashcards

1
Q

NSAIDS

Full name of NSAIDS______ are ________nhibitors

  • Prevent binding of _______ to ______enzyme
  • Inhibit the biosynthesis of ________

Common ____, _____ and ______effects

A

NSAIDS

Nonsteroidal anti-inflammatory drugs (NSAIDs) are cyclooxygenase (COX) inhibitors

  • Prevent binding of arachidonic acid to COX enzyme
  • Inhibit the biosynthesis of prostaglandins

Common analgesic, anti-inflammatory and antipyretic effects

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2
Q

COX enzyme exists in two forms:

  • _____
  • _____
A

COX enzyme exists in two forms:

  • COX – 1 isoenzyme
  • COX – 2 isoenzyme
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3
Q

NSAIDs are either:

  • _____
  • _____
A

NSAIDs are either:

  • Non-selective
  • COX – 2 selective (coxibs)
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4
Q

COX – 1 isoenzyme

  • _____ expressed
  • Involved in ____ physiologic functions
  • Maintenance of ____ function
  • ____ protection of the ___ tract

• Production of ______

A

COX – 1 isoenzyme

  • Constitutively expressed
  • Involved in numerous physiologic functions
  • Maintenance of renal function
  • Mucosal protection of the GI tract

• Production of thromboxane A2

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5
Q

COX - 2 isoenzyme

  • Expression induced by ____
  • Role in:
  • ____
  • ____
  • _____
A

COX - 2 isoenzyme

  • Expression induced by inflammatory mediators
  • Role in:
  • Mediation of pain
  • Inflammation
  • Fever
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6
Q

NON-SELECTIVE NSAIDs

Limited use in the perioperative setting

  • ____ toxicity
  • ___ dysfunction

___ healing is delayed with NSAIDs

• Safe in the setting of _____

____ (_____) is most commonly used perioperatively

  • Dosing ___IV or IM Q __h
  • Reduce dosing in patients with ____ function
A

NON-SELECTIVE NSAIDs

Limited use in the perioperative setting

  • Gastrointestinal toxicity
  • Platelet dysfunction

Bone healing is delayed with NSAIDs

• Safe in the setting of primary bone healing

Toradol (ketorolac) is most commonly used perioperatively

  • Dosing 30mg IV or IM Q 6h
  • Reduce dosing in patients with renal function
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7
Q

COX – 2 INHIBITOR

____ (_____) only available COX – 2 for use

  • Have less _____ toxicity
  • Increased _____ risk

Commonly given as part of ____ (_____) protocols

Dosing

  • ____mg PO preoperatively
  • ___mg. __ID x ____ days postoperatively
A

COX – 2 INHIBITOR

Celebrex (celecoxib) only available COX – 2 for use

  • Have less gastrointestinal toxicity
  • Increased cardiovascular risk

Commonly given as part of enhanced recovery after surgery (ERAS) protocols

Dosing

  • 400 mg PO preoperatively
  • 200 mg BID x 5 days postoperatively
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8
Q

NSAIDS PK

All NSAIDs are weak \_\_\_\_
Low Vd (\_\_\_\_)
Plasma half-life is widely \_\_\_

Gastrointestinal absorption occurs ___

____ protein binding

_____ metabolizes most NSAIDs
Eliminated primarily by ___ and ____

A 
All NSAIDs are weak acids
Low Vd (.1-.3 L/kg)
Plasma half-life is widely variable

Gastrointestinal absorption occurs rapidly

Increased protein binding

Liver metabolizes most NSAIDs
Eliminated primarily by renal and biliary excretion

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9
Q

NSAIDS side effects

Platelet function primarily through COX – 1

GI:

____ complications range from _____to ____such as _____ and _____

  • Risk factors include:
  • ____
  • _____
  • _____
  • ______
A

NSAIDS side effects

Platelet function primarily through COX – 1

GI:

Gastrointestinal complications range from mild ulcers to serious incidents such as perforation and bleeding

  • Risk factors include:
  • Elderly
  • Helicobacter pylori infection
  • History of previous ulcer
  • Concomitant use of aspirin, anticoagulants or corticosteroids
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10
Q

NSAIDS side effects

CV

  • Increased risks of ____, _____ and _____
  • In patients with CV risks, _____ is NSAID of choice
A

NSAIDS side effects

CV

  • Increased risks of myocardial infarction, heart failure and hypertension
  • In patients with CV risks, naproxen is NSAID of choice
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11
Q

NSAIDS side effects

Renal

  • Changes in renal function include:
  • ____ excretion, ____ function, interstitial ___ and reversible failure
  • Risk factors
  • Congestive ____, established ____ disease, history of ____, hypertension, _____ and significant ____
  • _____ from any cause increases the potential of renal injury
A

NSAIDS side effects

Renal

  • Changes in renal function include:
  • Sodium excretion, tubular function, interstitial nephritis and reversible failure
  • Risk factors
  • Congestive heart failure, established renal disease, history of diabetes, hypertension, atherosclerosis and significant hypoalbuminemia
  • Hypovolemia from any cause increases the potential of renal injury
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12
Q

NSAIDS other side effects

Liver

• Elevations in ______ levels and liver failure have been reported

Pulmonary

• Use of _____ in patients with history of ________

Hypersensitivity with NSAIDs rarely occurs. However:

• _____ + ____+ _____ = Risk of ___

Drug-Drug Interactions

  • Increased bleeding with _____ agents
  • Decreased _____ and _____ clearance secondary to _____ inhibition and altered ____ flow
A

NSAIDS other side effects

Liver

• Elevations in transaminase levels and liver failure have been reported

Pulmonary

• Use of COX - 2 in patients with history of aspirin-exacerbated disease

Hypersensitivity with NSAIDs rarely occurs. However:

• allergic rhinitis + nasal polyps + asthma = Risk of Anaphylaxis

Drug-Drug Interactions

  • Increased bleeding with antiplatelet agents
  • Decreased digoxin and lithium clearance secondary to prostaglandin inhibition and altered renal flow
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13
Q

ASPIRIN

____ and most _____ medicinal compound in the world

Derivative of ______

Rapidly metabolized by

• ____, ____ and ____

Two main uses

  • _____
  • _____
A

ASPIRIN

Oldest and most widely used medicinal compound in the world

Derivative of salicylic acid

Rapidly metabolized

• Plasma esterases, erythrocytes and liver

Two main uses

  • General analgesic
  • ”Irreversible” platelet inhibitor
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14
Q

ASPIRIN

OVERDOSE

Toxicity related to drug ____ and ____

Symptoms include:

  • ___, ____, ____ pain, ____ impairment, ___ depression,
  • Higher doses can result in ____acidosis, ___ failure, CNS ___ (____, ____, ____), and ____ with respiratory ____

_____ increases salicylate elimination

A

ASPIRIN

OVERDOSE

Toxicity related to drug acidity and prostaglandin inhibition

Symptoms include:

  • Nausea, vomiting, abdominal pain, hearing impairment, CNS depression,
  • Higher doses can result in metabolic acidosis, renal failure, CNS changes (agitation, confusion, coma), and hyperventilation with respiratory alkalosis

Urine alkalinization increases salicylate elimination

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15
Q

ACETAMINOPHEN

Has ___ and ____ properties

• Central analgesic effect through:

  • Activation of _____ pathways
  • Antagonism of ___, ___ and _____ pathways

• No _____ actions

Excellent oral bioavailability

  • Dosing ____-____mg Q _-_h
  • Total not to exceed ____mg/____h (____mg for chronic alcoholics)

An intravenous preparation (____) is available for clinical use

  • ____mg IV Q __h
  • Total not to exceed _____mg/___h
A

ACETAMINOPHEN

Has analgesic and antipyretic properties

• Central analgesic effect through:

  • Activation of serotonergic pathways
  • Antagonism of NMDA, substance P and nitric oxide pathways

• No anti-inflammatory actions

Excellent oral bioavailability

  • Dosing 325-650mg Q 4-6h
  • Total not to exceed 4,000mg/24h (2,000mg for chronic alcoholics)

An intravenous preparation (Ofirmev) is available for clinical use

  • 1,000mg IV Q 6h
  • Total not to exceed 4,000mg/24h
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16
Q

Acetaminophen PK

Metabolized in the _____
Leading cause of acute ____ failure in US

• Chronic usage of < ____g not associated with liver damage

Damage to the liver result from a metabolite:

  • ______ leads to liver failure by depleting ____, a natural ___
  • Treatment aimed at ____ acetaminophen (____) and replacing ____ (_____ administration)
A

Acetaminophen PK

Metabolized in the liver
Leading cause of acute liver failure in US

• Chronic usage of < 2g not associated with liver damage

Damage to the liver result from a metabolite:

  • N-acetyl-p-benzoquinoneimine leads to liver failure by depleting glutathione, a natural antioxidant
  • Treatment aimed at removing acetaminophen (charcoal) and replacing glutathione (acetylcysteine administration)
17
Q

GABAPENTIN

Gabapentin is a structural analogue of ____

• Acts on ___-dependent ____ channels inhibiting ____

Approved as an _____ medication

• Has demonstrated some efficacy in ____ pain

Used as part of multimodal pain management in ______ protocols

• Generally accepted to be effective in reducing ____ ____ pain and _____ consumption

A

GABAPENTIN

Gabapentin is a structural analogue of gamma-aminobutyric- acid (GABA)

• Acts on voltage-dependent calcium channels inhibiting glutamate

Approved as an anticonvulsant medication

• Has demonstrated some efficacy in neuropathic pain

Used as part of multimodal pain management in enhanced recovery after surgery (ERAS) protocols

• Generally accepted to be effective in reducing immediate postoperative pain and opioid consumption

18
Q

Gabapentin PK

Absorption is _____ to a relatively small part of the ____

• Absorption can be impaired by _____

Exhibit ____ protein binding and excreted _____ significant metabolism

A

Gabapentin PK

Absorption is limited to a relatively small part of the duodenum

• Absorption can be impaired by antacids

Exhibit minimal protein binding and excreted without significant metabolism

19
Q

GABAPENTIN

Dosing

  • Preoperatively _____mg ____ h before surgery
  • _____mg Q__h x ____days

Side-Effects include:

• ___, _____ or _____ and ______ disturbances

A

GABAPENTIN

Dosing

  • Preoperatively 1,200mg 1-2 h before surgery
  • 600mg Q8h x 14days

Side-Effects include:

• Sedation, dizziness or headache and visual disturbances

20
Q

LIDOCAINE

Lidocaine is an _____ local anesthetic

  • Weak ____
  • pKa slightly _____ physiologic pH

Infusions are routinely used as part of a ______plan to supplement _____

Mechanism of action ______

  • May involve ____ channels
  • Block priming of ____ _____
A

LIDOCAINE

Lidocaine is an amide local anesthetic

  • Weak base
  • pKa slightly above physiologic pH

Infusions are routinely used as part of a multimodal pain management plan to supplement general anesthesia

Mechanism of action not certain

  • May involve sodium channels
  • Block priming of polymorphonuclear granulocytes
21
Q

LIDOCAINE

Pharmacokinetics

  • Undergoes first-pass extraction in the _____
  • Metabolized in the ____
  • Metabolism prolonged in patients under ____

Dosing

  • ____ bolus dose
  • _____ infusion
A

LIDOCAINE

Pharmacokinetics

  • Undergoes first-pass extraction in the lungs
  • Metabolized in the liver
  • Metabolism prolonged in patients under general anesthesia

Dosing

  • 1.5 mg/kg bolus dose
  • 1-2 mg/kg/hour infusion
22
Q

LIDOCAINE

_____ for all surgical procedures

  • Reduces ___ and speeds up _____in ____ cases
  • Decreases ___, improves functional outcomes in ____, ____ and major ____ cases

_____ is a concern; however, at doses given during _____ protocols serum levels are well below ____

_____ at risk patients is advised

A

LIDOCAINE

Not beneficial for all surgical procedures

  • Reduces pain and speeds up return of bowel function in laparoscopic cases
  • Decreases pain, improves functional outcomes in prostatectomy, thoracic and major spine cases

Accumulation is a concern; however, at doses given during ERAS protocols serum levels are well below toxicity

Monitoring at risk patients is advised

23
Q

MAGNESIUM SULFATE

Analgesic properties related to:

  • Regulation of _____ influx into cells
  • Antagonism of ____ receptors in CNS

Dosing

  • ____ bolus
  • _____ infusion

Studies show a decrease in ____ consumption and pain

Side-effects included ____ and _____

A

MAGNESIUM SULFATE

Analgesic properties related to:

  • Regulation of calcium influx into cells
  • Antagonism of NMDA receptors in CNS

Dosing

  • 30-50 mg/kg bolus
  • 10 mg/kg/h infusion

Studies show a decrease in opioid consumption and pain

Side-effects included bradycardia and hypotension

24
Q

CAPSAICIN

______channel agonist

• Activation releases high-intensity ___ and release ____

The major pungent ingredient of ____ and ____

Applied _____ for ____ and ____

Available over the counter in:

• ____, _____ and _____ creams and/or _____

A

CAPSAICIN

Transient receptor potential vanilloid (TRPV1) channel agonist

• Activation releases high-intensity impulses and release substance P

The major pungent ingredient of chili peppers and botanicals

Applied topically for neuralgia and neuropathies

Available over the counter in:

• 0.025%, 0.075% and 0.25% creams and/or transdermal patches

25
Q

KETAMINE

____ antagonist modulates ____

  • Induced by ____ and ____
  • Role in preventing opioid-induced ____

Dosing

•_____ prior to surgical incision

Side-effects

  • ______
  • ____, _____, _____
A

KETAMINE

NMDA antagonist modulates central sensitization

  • Induced by incision and tissue damage
  • Role in preventing opioid-induced hyperalgesia

Dosing

• 0.5-1 mg/kg prior to surgical incision

Side-effects

  • Psychomimetic
  • Dizziness, blurred vision, nausea and vomiting
26
Q

DEXMEDETOMINDINE

_____agonist

• Blunts _____

Dosing

• _____

Side-effects include:

  • _____
  • _____
A

DEXMEDETOMINDINE

Selective alpha – 2 agonist

• Blunts central sympathetic response

Dosing

• 0.5 – 2 ug/kg

Side-effects include:

  • Hypotension
  • Bradycardia
27
Q

PERIPHERAL OPIOIDS

Analgesic effects are mediated by ______receptors

Peripherally acting opioids can reduce:

• Plasma _____, ____, ____ neuropeptides, immune ____ and tissue _____

Role in ____ and _____disease

A

PERIPHERAL OPIOIDS

Analgesic effects are mediated by peripheral opioid receptors

Peripherally acting opioids can reduce:

• Plasma extravasation, vasodilation, proinflammatory neuropeptides, immune mediators and tissue destruction

Role in arthroplasty and inflammatory bowel disease

N926 Pharmacology (16 decks)

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