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Pharmacology > 5.1 - Analgesics - Non-Narcotic > Flashcards

5.1 - Analgesics - Non-Narcotic Flashcards

1
Q

Analgesics

A
  • Non-narcotic

* Narcotic

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2
Q

Non-narcotic

A
  • Nociceptive
    • Somatic
    • Visceral
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3
Q

Narcotic

A

Psychogenic/ Affective

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3
Q

Para-amino Phenols

A
  • Phenacitin

* Paracetamol

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3
Q 
– Active form: Paracetamol
– ✖️ used anymore
   - ⬆️ risk of Urinary Tract Cancer
   - ⬆️ risk of acute renal failure
   - methemoglobinemia
A

Phenacitin

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4
Q

– Weak inhibitor of PG synthesis

A

Paracetamol

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5
Q

Paracetamol aka:

A

– Acetaminophen
– APAP
– Acetyl-p-aminophenol

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6
Q

Uses: PARACETAMOL

— Safe to give during pregnancy/ lactation

A

• Analgesic
- Mgt of MILD pain
- 1st line: Mgt if Osteoarthritis
• Antipyretic

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7
Q

S/E: PARACETAMOL

A

• Mild transaminitis
• SJS-TEN
— SJS: 10% TEN: >30%

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8
Q

Toxicity: PARACETAMOL

A

• Hepatic necrosis

- > 150mg/ kg/ day

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9
Q

Maximum Daily Dose: PARACETAMOL

A

Nmt 4 mg

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10
Q

Metabolism: PARACETAMOL

A 
• Glucuronidation (65%)
• Sulfation (30%)
• Oxidation (5%)
 – CYP1A2
  – NAPQI
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11
Q

NSAIDs

— All are WEAK organic acids ✖️ Nabumetone

A

MOA: Inhibition of COX

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12
Q

2 Types of COX

A
  • COX 1

* COX 2

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13
Q

– Constitutive enzyme
– produced by most cells as part of their function
– synthesis of PGs with maintenance functions
- cytoprotection
- vasodilation

A

COX 1

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14
Q

– Inducible Enzyme
– found in immune cells
– Produced in the setting of inflammation

A

COX 2

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15
Q

‼️‼️‼️

In ENDOTHELIAL cells, COX 2 is constitutive

A

– synthesis of PGI2 & PGE 2

- Anti-agreggants

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16
Q

NSAIDs

A

– Nonselective COX inhibitors

– Selective/ Specifix COX2 Inhibitors

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17
Q

Non-narcotic

A
  • Para-amino phenols

* NSAIDs

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18
Q

Nonselective COX Inhibitors

A
  • ASA & Salicylates
  • Pyrazole Derivatives
  • Pyrrole alkanoic acid derivative
  • Indole derivatives
  • Fenamates
  • Oxicam Derivatives
  • Phenyl acetic acid derivatives
  • Propionic Acid derivatives
19
Q

ASA & Salicylates

A
  • Pharmacokinetics
  • Pharmacodynamics
  • S/E
20
Q

Pharmacokinetics

A
  • Absorption

* Excretion

21
Q

Absorption

A

– Stomach

– Upper part of the SI

22
Q

Elimination

A

– < 600 mg/ day (1st order)

– > 600 mg/ day (zero order)

23
Q

Pharmacodynamics

A
  • Analgesic
  • Anti-inflammatory
  • Anti-pyretic
  • Antiplatelet
  • Anticancer
24
Q

Analgesic

— NMT 600 mg/ day

A
  • Peripheral: ✖️PG synthesis

* Central: ✖️ Pain perception in the subcortical sites

25
Q

Anti-inflammatory

— 3.2-4 g/ day

A

– ✖️ PG synthesis

– ✖️Chemotaxis — cell movement

26
Q

Anti-pyretic
— 0.3-2.4 g/ day
— 0.3-1.2 g/ day

A

– ✖️ of response to endogenous pyrogens (interleukin 1) — Central
– induces cutaneous vasodilation — Peripheral

27
Q

Antiplatelet

— NMT 325 mg/ day

A

– Irreversible acetylation (inhibition) of COX in platelets
— TXA2 synthesis
– ⬇️ dose = ⬆️ Antiplatelet effect

28
Q

Anticancer

— Potential

A

Reduction of colonic polyps

29
Q

S/E

A
  • GI S/E
  • Renal
  • Effdct on serum urate level
  • CNS Effects
  • Hypersensitivity reactions
  • Reye’s Syndrome
30
Q

S/E: NON SELECTIVE COX

A
  • GI Intolerance

* Gastritis

31
Q

– Hyperacidity/ dyspepsia
– ✖️ mucosal injury
– Prevention: Intake of NSAIDs after a FULL meal

A

GI Intolerance

32
Q 
– ✔️ mucosal injury
– Prevention:
 - PPIs
 - H2 blockers
 - Misoprostol
A

Gastritis

33
Q

Risk Factors: NSAID-INDUCED GASTRITIS

A
  • Advanced Age
  • ⬆️ dose NSAIDs
  • Multiple NSAID use
  • History of PUD
  • Concomittant use of Corticosteroids
  • Critical illness
34
Q

Renal S/E: ALL NSAIDs

A

⬇️ GFR = reversible

— afferent arteriole - constriction

35
Q

‼️‼️‼️

A
    • NSAIDs nay predisppse pts with pre-existing renal disease to acute rena failure
    • NSAIDs ⬇️⬇️ the effects of Diuretics
36
Q

Effect on serum urate level

— C/I: Gout

A 
• Aspirin
 – < 2 g/ day: Hyperuricemia
• Salicylates
 – > 4 g/ day: Uricosurin
• Tolmetin
37
Q

CNS S/E

A
  • Serum Level

* Clinical Manifestation

38
Q

50-80 mg/ dL

A 
• Salicylism
 - tinnitus
 - ⬇️ hearing
 - vertigo
• Respiratory ALKALOSIS
• Hyperventilation
39
Q

80-110 mg/ dL

A
  • Metabolic ACIDOSIS
  • Hyperthermia
  • Dehydration
40
Q

110-160 mg/ dL

A

Hypoprothrombinemia

Bleeding

41
Q

> 160 mg/ dL

A

Respiratory/ Renal Failure

42
Q

Hypersensitivity Rxn: ALL NSAIDs

A

NSAID-induced bronchial asthma

43
Q

Reye’s Syndrome

A

• ASA + suring/ after a recent viral infection

  • hepatic failure
  • encephalopathy
44
Q

Pyrazolone Derivatives
— Anti inflammatory
— Analgesic

A
  • PhenylbutazONE
  • DipyrONE
  • SulfinoyrazONE
45
Q

– ✖️ NSAID
– Uricosuric
— tx of gout

A

Sulfinpyrazone

46
Q

A/E: PYRAZOLONE DERIVATIVES

A
  • Hematotoxocities

* Nephrotoxicities

47
Q

Hematotoxicities

A
  • Agranulocytosis
  • Aplastic anemia
  • Theombocytopenia

Pharmacology (21 decks)

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