Proven A+ Notes summarising the common Analgesic and Anti-Inflammatory Drugs including: NSAID's, Corticosteroids, Anti-Gout Drugs, Opiod Analgesics and more.
Secure your A+ in Pharmacology today with these streamlined notes.
Non-Steroidal Anti-Inflammatory Drugs
Drugs Choice of NSAID General Tx Principles of NSAID’s
Aspirin (Disprin) 1)Diff S/E profiles Don’t prescribe 2 at once
Ibuprofen (Brufen) 2) Similar effect on fever & pain but Give lowest effective dose
Indomethican (Indocid) different anti-inflammatory strengths. Take with/post meals: ↓ GI irritation
Diclofenac (Voltaren) Low strength - Less S/E: Better for Avoid high Na food
chronic use. Max therapeutic effect seen > weeks
Mefanamic acid (Ponstan)
Potent- more S/E – better for acute use
COX:Cyclo-Oxygenase
Mechanism of Action LOX: Lipo-Oxygenase
Mechanism: NSAID’s Non-selectively block COX enzyme (COX1 & COX2) preventing the formation of thromboxane
and prostaglandins. Therapeutic uses and s/e’s occur as a result. Blocked COX2 results in the therapeutic analgesic,
anti-inflammatory & antipyretic effects. Blocked COX1 results in adverse effects on GIT (burning, ulcers, pain)
Leukotrienes effect
Adverse Effects of NSAID’s
Bad NSAID (Effects) Blocked COX pathways leads to
Lungs
Bleeding (hemorrhage) domination of LOX pathway.
Nausea, Dyspepsia
Stomach irritation Leukotrienes
Allergy Bronchoconstriction
Impaired Renal Function
Dizzy, drowsy, depression Mimics asthma attack
Stroke/Heart Attack
Unique Effects of Aspirin
Unique ASPIRIN
↑Uric Acid excretion in high doses (Gout)
Anti-inflammatory in high doses
Stroke & MI prevention
Plasma-protein bound: use w caution
Irrev. Inhibits COX in platelets
Copyright F Khan 2021
Reyes Sx Risk in small children
Extra S/E’s in high doses
, Non-Steroidal Anti-Inflammatory Drugs
PG analogues effects on other organs
To induce Labour
Uterus Myzoprostel (PG analogue)
PG inhibit acid & pepsin to protect
GIT mucosa against acid. NSAID’s
causes GIT S/E.
Some PG help control renal flow
Kidney Chronic NSAID’s use can reduce
renal flow leading to chronic kidney
failure.
Prostaglandins E1 Analogues (Mimic PG’s!)
• Dilation of cavernosum arteries
• ImprovesErectile Function
• Protects against Stomach ulcers
• Inhibits Proton-Pumpand
decreases acid secretion.
• Increases bicarbonate & mucus
production
• Neonates w Congenital ♡Defect
• Keeps ductus arteriosum open
(normally closes after birth) in • Labour Induction
babies with heart defects. • By softening the cervix
• It’s kept open until surgery is • Expulsion of UrinaryContents
performed.
• For constipation
• Think of “LUBE”making it easier
forstool to pass through GIT
Copyright F Khan 2021
, COXIB’s
Mechanism: Blocks COX2 pathway preventing the formation of Prostaglandins = analgesic, anti-
inflammatory, antipyretic. Spares COX1 pathways which prevents adverse GIT side effects.
Drugs
Celecoxib
Parecoxib
Principles:
• Spares COX1 = No GIT Side-Effects
• Long-term use = Increased risk of Stroke/ Heart attack due to dominance of thromboxane blood
clotting effects.
Paracetamol
Mechanism: Blocks COX centrally not peripherally, only analgesic & antipyretic effects (Fever & pain).
*Not an NSAID: no anti-inflammatory, antiplatelet or GIT effects.
No mention of inflammation
Organ most affected Liver: paracetamol produces toxic metabolites (NAPQI) when
from paracetamol metabolized in the liver which can cause hepatotoxicity in high doses.
overdose
Antidote: N-acetylcysteine (Parvolex)
How it works: Inactivates NAPQI by conjugation with glutathione.
Administration: Within 8 hours of paracetamol ingestion, IV infusion.
Differences between paracetamol and aspirin. Similarities
Aspirin Paracetamol Aspirin Paracetamol
Anti-inflammatory No significant anti- Analgesic Analgesic
inflammatory effects Antipyretic Anti-pyretic
Anti-platelet No anti-platelet effects
GIT side-effects No GIT adverse effects
Copyright F Khan 2021
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