ANTI INFLAMMATORY DRUGS

INFLAMMATION Complex biological response of body tissues to injury

It comprises systemic response [involving nervous and hormonal adjustments ,and proliferation of the lympho reticular system ]and local response[ pain,redness, warmth and swelling]

Protective response involving immune cells, blood vessels,and molecular mediators

FUNCTION OF INFLAMMATION;

-To eliminate initial cause of cell injury

- Clear out necrotic cells and tissues

- Initiate cell repair

ANTI INFLAMMATION

Property or treatment that reduces inflammation or swelling

Classification of anti-inflammatory drugs

(1)Non-steroid anti-inflammatory drugs (NSAIDs)

(Antipyretic-Analgesic and Anti-inflammatory Drugs)

EG ; aspirin, acetaminophen, indomethacin, COX inhibitor, ibuprofen

(2) Steroid anti-inflammatory drugs

glucocorticoids: eg. dexamethasone

NON STEROIDAL ANTI INFLAMATORY DRUGS

Prostaglandins are chemicals produced by body cells which promote inflammation necessary for healing but also results in pain and fever support the blood clotting functions and protect the lining of stomach

Prostaglandins are produced within the body cells by the enzyme cyclooxygenase(COX)

There are two COX enzymes-COX-1 and COX-2

COX-1 produces prostaglandins that support platelets and protect the stomach

NSAIDs block the COX enzymes and reduce prostaglandins through out the body which reduces on going inflammation pain and fever

Examples of NSAIDs are:-

Aspirin

Ibuprofen

Naproxen

3. Pharmacodynamic Effects of NSAIDs

Positive

Analgesic (0.3-0.6 g/day) - refers to the relief of pain by a mechanism other than

the reduction of inflammation (for example, headache);

- produce a mild degree of analgesia which is much less than the

analgesia produced by opioid analgesics such as morphine

anti-inflammatory (3-5 g/day) - these drugs are used to treat inflammatory

diseases and injuries, and with larger doses - rheumatoid disorders

antipyretic (0.3-0.6 g/day) - reduce fever; lower elevated body temperature by

their action on the hypothalamus; normal body temperature is not reduced

antiplatelet (30-100 mg/day)- inhibit platelet aggregation, prolong bleeding time;

have anticoagulant effects

HISTORY - SALICYLATES Salicylates were first discovered when the observation was made that chewing willow bark could relieve pain

Hippocrates: Willow bark as a pain killer during childbirth

Stone (1700) Extract of willow bark to reduce fever

• Piria (1838) Isolation of salicin from willow bark

• Kolbe (1853) Synthesis of salicylate from salicin

Von Gerhardt at Beyer Pharmaceutical Co.

synthesized acetyl SA (ASA) in 1850

Hoffman, at Beyer gave ASA to his rheumatoid father

Beyer started sales of Aspirin in1899

Acetylsalicylic acid (aspirin) was introduced as a

pain reliever in 1899, at that time it was used

HISTORY - SALICYLATES

SALICYLATES

Salicylates are esters or salts of salicylic acid

E.g. ; methyl salicylate and sodium salicylate

Also occur as salicylate esters of organic acid such as acetyl salicylic acid [ aspirin ]

Aspirin is the most commonly used salicylate

In smaller doses salicylates exert mainly analgesic action

With larger doses they exert anti inflammatory activity and relieve vascular congestion and oedema

Anti inflammatory and anti rheumatic effect:

salicylates suppress the clinical signs and improve the clinical picture in acute rheumatoid fever and rheumatoid arthritis

Aspirin is used to treat inflammatory conditions such as arthritis and fibromyositis.It can modify or diminish but doesn’t arrest the inflammatory response

Salicylates and other NSAIDs thus reduce the inflammatory compound of the disease by

Inhibiting PG synthesis in the peripheral tissues

Reducing the capillary permeability

Inhibition of neutrophil aggregation and activation

Prostaglandins present in the inflammatory exudate are potent vaso dilators and can cause edema,erythema and pain

Aspirin like drugs by inhibiting the synthesis of PG,preventsensitization of the pain receptors to agents such as histamines, bradykinin etc, the known chemical mediators of pain and inflammation

SIDE EFFECTS OF ASPIRIN Gastrointestinal symptoms

CNS toxicity

Allergic reaction (urticaria), angioneuroticedema, aspirin asthma, occasionally anaphylactic shock)

Salicylate reaction (CNS reaction)

Renal damage

Hematologic effects

Metabolic acidosis stimulates medullaryrespiratory center respiratory alkalosis

PROPIONIC ACID DERIVATIVES

o It includes like ibuprofen,naproxen, fenoprofen,flurbiprofen and ketoprofen.

o These compounds have analgesic-anti pyretic and anti inflammatory properties similar to aspirin

o These are better tolerated orally

o The adverse reactions is lower than that after high doses of aspirin and indomethacin.

o Ibuprofen is a good substitute for aspirin.

o Flurbiprofen is also available as eye drops for eye inflammation

SELECTIVE COX-2 INHIBITORS

These drugs block COX-2 activity more than COX-1 activity

This group includes nimesulide,meloxicam, nabumetone and celecoxib.

Celecoxib is a highly selective COX-2 inhibitor.

Effective as the NSAIDs in the treatment of osteoarthritis and rheumatoid arthritis.

Advantage is that they cause fewer gastric ulcers and do not inhibit platelet aggregation

ACETIC ACID DERIVATIVES

Diclofenac Have greater activity than indomethacin , naproxen and other NSAIDs

probably because of its higher COX-2 inhibiting property

As ant inflammatory agent in rheumatoid arthritis, severe osteoarthritis

INDOMETHACIN

This Indole acetic acid derivative is a potent anti inflammatory agent

In patients with rheumatoid arthritis with swollen joints,it brings about a quick reduction inthe joint swellings

It is particularly useful in the treatment of acute attacks of gout

Given orally,it is absorbed rapidly

Head ache is the most common adverse effect

Negative or adverse effects

Gastric irritant

Decreased renal perfusion

Bleeding

Adverse Effects associated with NSAIDs

Non-selective

ICE TREATMENT

Applying ice, or even cool water, to a tissue injury has an anti inflammatory effect

Often suggested as an injury treatment and pain management technique for athletes

Cool temperatures inhibits local blood circulation which reduces swelling in the injured tissue.

ANTI INFLAMMATORY FOODS

Diets rich in vegetables and low in simple carbohydrates and fats such as saturated fats and trans fats

Anti inflammatory foods include most colourfull fruits and vegetbles , oily fish,nuts,seeds and certain spices such as ginger,garlic etc

EXERCISE

o Contracting muscles release multiple substances known as myokineswhich promote the growth of new tissue, tissue repair and various anti inflammatory functions

SWAYATHUHARA MAHAKASHAYAVARGA

(ANTI INFLAMMATORY)Patalaagnimanthasyonakaabilwakasmaryakandakarikabrhatisaalaparniprsniparnigoksuraka iti dasemaani swayathuharaani bavanti.

cha.su.4/16

1. Patala(Stereospermum suaveolens)

2. Agnimantha(Premna serratifolia)

3. Syonaka(Oroxylum indicum)

4. Bilva(Aegle marmelos)

5. Kasmarya(Gmelina arborea)

6. Kantakarika(Solanum xanthocarpum)

7. Brhati(Solanum indicum)

8. Salaparni( Pseudarthria viscida)

9. Prsniparni(Desmodium gangeticum)

10.Gokshura(Tribulus terrestris)

PATALA

Botanical name:Stereospermumsuaveolens

Family:Bignoniaceae

Malayalam name:Patiri

Useful part:Root bark

AGNIMANTHA

Botanical name:Premnaserratifolia

Family: verbenaceae

Malayalam name:munja

Useful part: Root and leaves

SYONAKA

Botanical name:Oroxylum indicum

Family:Bignonaceae

Malayam name: Palaka payyani

Useful part:Root bark

BILVA

Botanical name:Aegle marmelos

Family:Rutaceae

Malayalam name:Koovalam

Useful part:Root,leaves,unripenedfruit

KASMARYA

Botanical name:Gmelinaarborea

Family:Verbanaceae

Malayalam name:Kumizh

Useful part:Root bark

KANTAKARIKA

Botanical name:Solanumxanthocarpum

Family:Solanaceae

Malayalam name:Puthari chunda

Useful part:Root & whole plant

BRHATI

Botanical name:Solanum indicum

Family:Solanaceae

Malayalam name:Cheruchunda

Useful part:Root,fruit,leaves

PRSNIPARNI

Botanical name:Desmodiumgangeticum

Family:Papilionaceae

Malayalam name:Orila

Useful part:Root

SALAPARNI

Botanical name:Pseudarthria viscida

Family:Pappilionaceae

Malayalam name:Moovila

Useful part:Root

GOKSHURA

Botanical name:Tribulus terrestris

Family:Zygophyllaceae

Malayalam name:Nerungil

Useful part:Roots and fruits

OTHER DRUGS SHOWING ANTI INFLAMMATORY ACTION

1.Guggulu

2.Manjishta

3.Amalaki

4.Bibitaka