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ANTI INFLAMMATORY DRUGS
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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
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FUNCTION OF INFLAMMATION;
-To eliminate initial cause of cell injury
- Clear out necrotic cells and tissues
- Initiate cell repair
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ANTI INFLAMMATION
Property or treatment that reduces inflammation or swelling
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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
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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
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Examples of NSAIDs are:-
Aspirin
Ibuprofen
Naproxen
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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
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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
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HISTORY - SALICYLATES
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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
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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
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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
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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
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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
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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
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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
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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
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Negative or adverse effects
Gastric irritant
Decreased renal perfusion
Bleeding
Adverse Effects associated with NSAIDs
Non-selective
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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.
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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
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EXERCISE
o Contracting muscles release multiple substances known as myokineswhich promote the growth of new tissue, tissue repair and various anti inflammatory functions
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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)
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PATALA
Botanical name:Stereospermumsuaveolens
Family:Bignoniaceae
Malayalam name:Patiri
Useful part:Root bark
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AGNIMANTHA
Botanical name:Premnaserratifolia
Family: verbenaceae
Malayalam name:munja
Useful part: Root and leaves
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SYONAKA
Botanical name:Oroxylum indicum
Family:Bignonaceae
Malayam name: Palaka payyani
Useful part:Root bark
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BILVA
Botanical name:Aegle marmelos
Family:Rutaceae
Malayalam name:Koovalam
Useful part:Root,leaves,unripenedfruit
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KASMARYA
Botanical name:Gmelinaarborea
Family:Verbanaceae
Malayalam name:Kumizh
Useful part:Root bark
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KANTAKARIKA
Botanical name:Solanumxanthocarpum
Family:Solanaceae
Malayalam name:Puthari chunda
Useful part:Root & whole plant
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BRHATI
Botanical name:Solanum indicum
Family:Solanaceae
Malayalam name:Cheruchunda
Useful part:Root,fruit,leaves
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PRSNIPARNI
Botanical name:Desmodiumgangeticum
Family:Papilionaceae
Malayalam name:Orila
Useful part:Root
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SALAPARNI
Botanical name:Pseudarthria viscida
Family:Pappilionaceae
Malayalam name:Moovila
Useful part:Root
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GOKSHURA
Botanical name:Tribulus terrestris
Family:Zygophyllaceae
Malayalam name:Nerungil
Useful part:Roots and fruits
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OTHER DRUGS SHOWING ANTI INFLAMMATORY ACTION
1.Guggulu
2.Manjishta
3.Amalaki
4.Bibitaka
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