Oleh

Dimas P.Nugraha
Bagian farmakologi FK UR

Inflammation:
it is a biological response of
vascular tissues to harmful
stimuli, such as pathogens,
damaged cells, or irritants.
Inflammation may ends with
either
:
Permanent destruction
Complete healing
of tissues

of tissues

 Inflammatory mediators:
histamine
5-HT (serotonin)
Bradykinin
Prostaglandins (eg PGE2 )
Interleukines
Substance P
Nitrous oxide

Main
inflammatory
mediator

Mediators of inflammation

Oedema with histamine

Eicosanoids and
inflammation

Anti-inflammatory
Drugs

Steroidal
- Cortisone
- Hydrocortisone

Non-steroidal
- Acetaminophen
- Aspirin

Steroids (SAIDs)
- Containing steroid moiety in their sturcure
Glucocorticoids (GC)

Cortisone

Mechanism of Action for

Anti-Inflammatory Steroids

Mechanism of Action for AntiInflammatory Steroids

1. Suppress T-cell activation and cytokine production.
2. Suppress mast cell degranulation.
3. Decrease capillary permeability indirectly by
inhibiting mast cells and basophils.
4. Reduce the expression of cyclooxygenase II and
prostaglandin synthesis.
5. Reduce prostaglandin, leukotriene and platelet
activating factor levels by altering phospholipase
A2 activity.

Routes of Administration for GC

Local (Preferred)

Intra-articular, IA
Intrabursal, IB
Intralesional, IL
Intrasynovial, IS
Soft tissue, ST
Intrarectal, IR
Topical
Nasal
Inhaled

Systemic
Oral, PO
Intramuscular, IM
Intravenous, IV
Subcutaneous, SC

Short- to medium-acting glucocorticoids

Hydrocortisone (cortisol)
Cortisone
Prednisone
Prednisolone
Methylprednisolone
Meprednisone

Intermediate-acting glucocorticoids
Triamcinolone
Paramethasone
Fluprednisolone
Long-acting glucocorticoids
Betamethasone
Dexamethasone
Mineralocorticoids
Fludrocortisone
Desoxycorticosterone acetate

Some commonly observed effects of long-term corticosteroid

Drug Interactions

Drugs that Enhance Corticosteroid Effects

Estrogens
Oral contraceptives
Antifungal agents
Antibiotics
*all of these agents inhibit cytochrome P450 enyzymes

Drugs that Reduce Corticisteroid Effects

Antacids
Cholestyramine

*these drugs decrease the absorption of corticosteroids

Phenytoin: inhibits cytochrome P450 enyzymes

NSAIDs

General characteristics
Drugs that inhibit one or more steps in the
metabolism of arachidonic acid (AA)
Aspirin-like drugs or COX inhibitors
Major action:
inhibit Cyclooxygenase (COX)
Pharmacological effects
Suppress inflammation
Relieve pain
Reduce fever

Categories of NSAIDs

There are two major categories for non-stero

NSAIDs and COX-1 and COX2

Salicylates

NSAIDs

13

NSAIDs

14

Summary of Nonsteroidal antiinflammatory agents (NSAIDs)

Disease-Modifying Antirheumatic
Agents
Disease-modifying antirheumatic drugs
(DMARDs) are used in the treatment of RA and
have been shown to slow the course of the
disease, induce remission, and prevent further
destruction of the joints and involved tissues
When a patient is diagnosed with RA, the American
College of Rheumatology recommends initiation of
therapy with DMARDs within 3 months of diagnosis
(in addition to NSAIDs, low-dose corticosteroids,
physical therapy, and occupational therapy)
Therapy with DMARDs is initiated rapidly to help
stop the progression of the disease at the earlier
stages

Most experts begin DMARD therapy with one of the traditional drugs, su

ALHAMDULILLAH.