Ph'macology of Asperin.pptx

Cology

1. Pharmacology of aspirin

2. Introduction Name- Shrinath Bodkhe , Jivan Adsul Roll- 3021, 3003 Class – T. Y. B pharm Batch –A , B Subject- pharmacology-2 Subject teacher- Priyanka Sarda Mam

3. inflammation Inflammation  is part of the complex biological response of body tissues to harmful stimuli, such as  pathogens , damaged cells, or  irritants , and is a protective response involving  immune cells ,  blood vessels , and molecular mediators.

4. Types of inflammation

5. What are NSAIDs ? Full form of NSAIDs is Non-steroidal Anti Inflammatory Drugs. NSAIDs Are members of a therapeutic drug class which reduces pain, decreases inflammation, decreases fever, and prevents blood clots. Side effects depend on the specific drug, its dose and duration of use, but largely include an increased risk of gastrointestinal ulcers and bleeds, heart attack, and kidney disease

6. Nsaids Classification

7. Inflammatory cascade Inflammatory responses arise as an outcome of tissues or organs exposure towards harmful stimuli like injury, toxic chemicals or pathogenic microorganism. It is a complex cascade of immune mechanism to overcome from tissue injury and to initiate the healing process by recruiting various immune cells, chemical mediators such as the vasoactive peptides and amines, pro-inflammatory cytokines, eicosanoids and acute-phase proteins to prevent tissue damage and ultimately complete restoration of the tissue function. The cytokines exhibits a central function in communication between the cells, inflammatory response initiation, amplification and their regulation.

8. This review covers the importance of inflammatory responses; the significance of cytokines in inflammation and numerous inflammatory disorders/ailments due to the abrupt expression of cytokines and the hyper-inflammatory response or cytokine storm associated with poor prognosis in COVID-19 pandemic. Also highlighting the importance of naturally derived anti-inflammatory metabolites to overcome the side-effects of currently prevailing anti-inflammatory drugs.

9. Aspirin Aspirin, also known as acetylsalicylic acid (ASA), is a nonsteroidal anti-inflammatory drug (NSAID) used to reduce pain, fever, and/or inflammation, and as an Antithrombotic. Specific inflammatory conditions which aspirin is used to treat include Kawasaki disease, Pericardium, and Rheumatic fever Aspirin is also used long-term to help prevent further heart attacks, ischaemic strokes, and blood clots in people at high risk. For pain or fever, effects typically begin within 30 minutes. Aspirin works similarly to other NSAIDs but also suppresses the normal functioning of platelets

10. Aspirin belongs to which class ? Aspirin , an acetylated salicylate (acetylsalicylic acid), is classified among the nonsteroidal Anti-inflammatory drugs (NSAIDs). These agents reduce the signs and symptoms of inflammation and exhibit a broad range of pharmacologic activities, including analgesic, antipyretic, and antiplatelet properties.

11. Mode of action- aspirin Aspirin Causes several different effects in the body, mainly the reduction of inflammation, analgesia (relief of pain), the prevention of clotting, and the reduction of fever. Much of this is believed to be due to decreased production of prostaglandins and TXA2. Aspirin’s ability to suppress the production of Prostaglandins and Thromboxane's is due to its irreversible inactivation of the cyclooxygenase (COX) enzyme.

12. Cyclooxygenase is required for prostaglandin and thromboxane synthesis. Aspirin acts as an acetylating agent where an acetyl group is covalently attached to a serine residue in the active site of the COX enzyme. This makes aspirin different from other NSAIDs (such as diclofenac and ibuprofen), which are reversible inhibitors. However, other effects of aspirin, such as uncoupling oxidative phosphorylation in mitochondria, and the modulation of signalling through NF- κB , are also being investigated. Some of its effects are like those of salicylic acid, which is not an acetylating agent.

13. Pharmacological action Antiplatelet action - Aspirin works by irreversibly inhibiting the enzyme Cyclo-oxygenase (COX-1) which is required to make the precursors of thromboxane within platelets. This reduces thromboxane synthesis. Thromboxane is required to facilitate platelet aggregation and to stimulate further platelet activation. Analgesic action - Aspirin causes several different effects in the body, mainly the reduction of inflammation, analgesia (relief of pain), the prevention of clotting, and the reduction of fever. Much of this is believed to be due to decreased production of prostaglandins and TXA2.

14. Antipyretic action - Through the disruption of the production and prevention of release of prostaglandins in inflammation, this drug may stop their action at pain receptors, preventing symptoms of pain. Acetylsalicylic acid is considered an antipyretic agent because of its ability to interfere with the production of brain prostaglandin E1. Effect on kidney - High doses over a long period of time can also lead to chronic kidney disease and even progress to kidney failure. For people without kidney Antipyretic action - Through the disruption of the production and prevention of release of prostaglandins in inflammation, this drug may stop their action at pain receptors, preventing symptoms of pain. Acetylsalicylic acid is considered an antipyretic agent because of its ability to interfere with the production of brain prostaglandin E1. Effect on kidney - High doses over a long period of time can also lead to chronic kidney disease and even progress to kidney failure. For people without kidney

15. Therapeutic uses Used in treatment of – 1) Rheumatoid arthritis 2) Pericarditis 3) Heart attack 4) stroke 5) Colorectal cancer 6) reduce pain and fever

16. Adverse effects of aspirin Abdominal or stomach pain, cramping, or burning.
Black, tarry stools.
Bloody or cloudy urine.
Change in consciousness.
Chest pain or discomfort.
Confusion.
Constipation.
Convulsions, severe or continuing.

17. Contraindications 1) Active peptic ulcer 2) aspirin allergy 3) bleeding disorders – ex- haemophilia 4) Renal failure 5) Severe liver disease 6) gastrointestinal and intracranial bleeding

18. Pharmacokinetics Absorption - rapidly absorbed from the acid environment of the stomach. Enteric coating of aspirin results in its release into the alkaline environment of the small bowel, where it is hydrolysed. As a result, enteric-coated aspirin has lower bioavailability than regular aspirin. Distribution - Salicylate distributes rapidly into the body fluid compartments. It binds to albumin in the plasma. With increasing total plasma salicylate concentrations, the unbound fraction increases. Salicylate may cross the placental barrier and distributes into breast milk.

19. Metabolism - aspirin is rapidly bio-transformed into the active metabolite, salicylate. Therefore, aspirin has a very short half-life. Salicylate, in turn, is mainly metabolized by the liver. Excretion - unchanged salicylate accounts for 10% of the total elimination of salicylate. Excretion of salicylate results of glomerular filtration, active proximal tubular secretion through the organic acid transporters and passive tubular reabsorption.

20. Marketed preparation