Essence Local Anaesthetic PDF

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Summary

summary on local anaesthetics ...

Description

NSAIDS Drugs

Aspirin (salicylates)

Ibuprofen (Propionic acid)

Classes

Anti-inflammatory Inhibits platelet aggregation

Mild to moderate pain (menstrual pain) Anti-inflammatory

Route of Administration

Orally Rapidly absorb in stomach, more in ileum

Mechanism of Action

Irreversible COX inactivation

Adverse Effect

Pharmacokinetics

CI

Peptic ulcer Diabetics Pregnancy

Mild to moderate pain

Ketoprofen (P.a) Arthritis related inflammatory pain Gout Severe toothaches

Diclofenac (P.a) Musculoskeleton pain Gout Pain management in Kidney stones & gallstones Dysmenorrhea Orall, IM, topical

Safer than aspirin

Hydrolysed by esterases, 25% oxidised, 25% excreted unchanged

Naproxen (Propionic acid)

High protein bound, enters brain, extensively metabolise in liver, rapidly excreted

Nonselective COX inhibitor

Nonselective COX inhibitor Lipoxygenase

Nonselective COX inhibitor, decrease AA bioavailability in some inflammatory cells

Similar to other NSAIDS

GI > Aspirin

GI distress Elevated liver enzyme

Metabolised in the liver

Rapidly absorb Metabolised completely in liver

Rapidly absorb Significant first-pass metabolism Excreted by renal and bile

X used with salicylates, anticoagulants

X used with other NSAIDS, anticoagulants

Drugs

Indomethacin (Indole)

Mefenamic acid (Fenamic acid)

Classes

Gout Antipyretic in Hodgkin’s disease Rheumatoid conditions

Moderate pain Dysmenorrhea Arthritis

Route of Administration

Well absorb orally, ↓in elderly

Mechanism of Action

Nonselective COX inhibitor, inhibits phospholipase A & C ↓T-cell & B-cell proliferation

Adverse Effect

Gastric irritation, nausea, gastric bleeding, diarrhoea, headache

Pharmacokinetics

CI

Metabolised in the liver Excreted in bile and urine

Piroxicam (Oxicam)

Celecoxib

Rheumatoid conditions Dysmenorrhea Postoperative pain

Rheumatoid arthritis, osteoarthritis, acute pain

Nonselective COX inhibitor

Selective COX-2 inhibitor

Similar to other NSAIDS Diarrhoea and abdominal pain

GI toxicity, tinnitus, dizziness, headache, rash, pruritis

↓GI risk, ↑Cardio risk

Enhance effects of oral anticoagulants

Rapidly absorb in stomach Extensively metabolise in liver Excreted as glucuronide conjugation & unchanged

Highly protein bound, metabolised by CYP2C9

Pregnancy & young children

Contains sulfonamid emoiety - may cause allergic reactions...