Anti inflammatory drugs
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Anti-inflammatory drugs. By Dr Soha AlSayed Lecture of Pharmacology Faculty of Medicine Suez Canal University. Classifications of anti-inflammatory drugs. Steroids: Drugs which contain steroid nucleus They are glucocorticoids or mineralocorticoids

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Anti-inflammatory drugs

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Anti inflammatory drugs

Anti-inflammatory drugs

By

Dr Soha AlSayed

Lecture of Pharmacology

Faculty of Medicine

Suez Canal University


Classifications of anti inflammatory drugs

Classifications of anti-inflammatory drugs

  • Steroids:

    • Drugs which contain steroid nucleus

    • They are glucocorticoids or mineralocorticoids

    • Glucocorticoids have significant anti-inflammatory effect

      2. Non-steroids anti-inflammatory drugs (NSAIDs) characterized by:

      • Lower high body temperature (Antipyretic)

      • Relieve pain (Analgesic)

      • Some have anti-inflammatory effect


Anti inflammatory drugs

Non steroidal anti-inflammatory drugs

Types of COX enzyme:

1. COX-1 (constitutive) especially in stomach  decrease HCl (prevent PU) & Kidney vasodilatation

2. COX-2 (inducible) by infection

  • Infection ►toxins ► IL-1&TNF ► COX-II ►▲ PG ► Inflammation ►

    A. CNS:

    a. hypothalamus ► elevates Heat regulatory centre► Fever

    b. Thalamus► pain

    2. Periphery:

    a. Sensitize Nociceptors to histamine, Bradykinin & 5-HT ► pain

    b. Potentiates effect of histamine & bradykinin

    • VD Redness, Hotness, capillary permeability


Anti inflammatory drugs

Non steroidal anti-inflammatory drugs

Types of NSAIDS:

1. Non-selective COX inhibitors (COX 1,2,3)

2. Selective COX-2 inhibitors (Celecoxib, Rofecoxib)

3. COX-3 inhibitors : paracetamol (not anti-inflammatory). Why?

Mechanism of action of NSAIDS

They inhibit cyclo-oxygenase enzyme ►▼Prostaglandins ► ▼Fever, pain, Inflammation.

1. Antipyretic action: decrease set point of heat regulatory centre in hypothalamus, increase sweating


Anti inflammatory drugs

The anti-inflammatory actions of NSAIDS

  • Due to reduction of PGE2 and PGI2 that participate in the inflammatory process

  • Stabilize lysosomes

  • Inhibit granulocyte adherence to damaged vasculature

  • Inhibit migration of macrophages to the inflammatory sites

  • Inhibit Kinin-Kallikrein system


Anti inflammatory drugs

Shared Adverse effects of NSAIDS

  • GIT side effects: Dyspepsia, Gastric ulceration

  • Disturbances of renal function: (Analgesic abuse nephropathy) due to decreased vasodilatory PGs

  • Hypersensitivity: e.g. aspirin induced asthma

  • Bleeding tendency

  • Displacing other drugs from plasma proteins

  • Salt and water retention and hyperkalemia

  • May prolong pregnancy and spontaneous labor


Anti inflammatory drugs

Aspirin=Acetyl salicylic acid

Pharmacokinetics:

  • Administration: Effective orally & pareneterally

  • Absorption: Absorbed from stomach & Upper intestine. Why?

  • Distribution: Bound to PP (50-80%).

  • Metabolism: mainly by conjugation to glycine & glucoronic acid.

  • Excretion: unchanged and conjugated form by kidney. How can you increase excretion?

  • In low concentration first order kinetics?

  • In high concentration zero order kinetics?


Anti inflammatory drugs

Pharmacological actions of Aspirin

1. CNS:

A. Analgesic action: central and peripheral

B. Antipyretic Action: ▼PGE

2. Anti-inflammatory actions:

3. Respiration and Acid/Base balance:

  • Ordinary doses; little effect

  • large dose ►▲RR►R alkalosis.

  • V. high L doses► Resp. depression ► Resp. acidosis.

    4. Renal effects:▲ Na, water retention


Anti inflammatory drugs

Pharmacological actions of aspirin

5. Uric acid:

A. Small dose: Retention of UA

B. Large dose: Excretion of UA 

6. Blood:

A. Small dose (75-150 mg/day): ▼platelet aggregation and▲ bleeding time

B. In patients with G-6-PD defiiency ►hemolytic anemia (idiosncrasy).

7. GIT:

Epigastric distress, nausea, vomiting, ulceration, bleeding.


Anti inflammatory drugs

Indications of Aspirin

  • Fever: (Not preferred in children. Why?)

  • Analgesic: Mild to moderate pain. headache, arthritis, myalgia, common cold ( 0.5-2 gm/day)

  • Acute Rheumatic fever: Symptomatic treatment only, 10 gm /day

  • Rheumatoid arthritis: 8 gm/day

  • Antithrombotic: 75-150 mg/day

  • Gout?: > 5gm /day


Anti inflammatory drugs

Side effects & contraindicationsof Aspirin

  • GIT: What?

  • Idiosyncrasy:

  • Hypoprothrombinemia, bleeding tendency

  • Chronic use: Salicylism: Headache, mental confusion, drowsiness, vertigo, ringing in ears (Tinnitus), sweating, thirst, nausea, vomiting

    5. Hepatic: Severe hepatic injury and encephalopathy in Reye’s syndrome (in children with viral infection especially influenza, Chicken pox)

    6. Bronchospasm 7. Allergy


Anti inflammatory drugs

Acute Salicylate poisoning

Acute salicylate poisoning:

Hallucination, restlessness, tremors, convulsions, vomiting, dehydration, hypotension, hyperglycemia, hyperpyrexia

  • Treament of acute salicylate poisoning;

    • Gastric lavage with sod. Bicarbonates. Why?

    • Correction of hyperpyrexia (cold fomentation, ethyl alcohol evaporation

    • Correction of dehydration , acid/base balance

    • Alkalinization of urine with NaHCO3. Why?

    • Hemodialysis: Symptomatic treatment


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