Every man should establish good habituation that will really help ensure decades of continuing dynamic good health. Hence, consumption of balanced diet, proper exercise at an early and middle age along with developing an active lifestyle is an essential positive factor from the health point of view. This will reflect in maintaining mental and physical fitness, and to help keep the body in top shape and body weight within sensible limits.
Along with this, keeping one''s mental and emotional health under control is important. Learning to cope with changes and personnel crises of life can have a direct impact on physical well being, as stress and anxiety can result in greater risk for onset of variety of health problems.
Stress-related disorders are cardiovascular diseases, coronary diseases, GIT problems, hypertension, diabetes, and neurological disorders etc, and its imperative to find out the root cause of stress though consulting a physician.
Otherwise a pyramid of disorders will develop and end up with imbalance of biochemical factors in the body. Some of the existing synthetic molecules and new molecules exhibit an excellent role in prevention of some of the abovementioned diseases. Aspirin (acetyl salicylic acid) is the ultimate synthetic drug for cardiac patients in critical situations.
Aspirin: is best choice amongst antiplatelet agents, because it inhibits the two important enzymes Tx-synthetase and Cycloxygenase. The TxAz formation is also suppressed till fresh platelets are formed. Apart from that PG12 synthesis in vessel wall is inhibited. All these mechanisms are possible with low doses of aspirin 75mg and 150 mg respectively. Whereas higher doses (> 900 mg/ day) may decrease both TXA and PG 12 production. One more prominent action of aspirin is it inhibits the release of ADP from platelets and their adhering to each other.
Therapeutic applications:
- Coronary artery diseases
- Cerebrovascular disease
- Coronary bypass implants
- In case of venous thromboembolism
- Prosthetic heart valves and arterio venous shunts
Poly Aspirin: This is a new molecule made from around a hundred individual aspirin molecules in a flexible chain forming a polymer. This has additional benefits as it''s used as carrier molecules to deliver drugs to respective host cells and housed drugs within polymer capsules. Hence, this plastic aspirin provides distinct advantages over traditional forms.
Advantages:
1) Plastic aspirin permits sustained effects
2) Reduction of inflammation by inhibiting of PG-synthesis.
3) Helps to promote healing
4) Used for even treating pericardial diseases.
5) Stimulates bone growth
6) More beneficial with combination therapy.
Disadvantages: Induces gastric ulcers if long term use and bleeding
Clopidogrel: It is similar action of aspirin, action is particularly on platelet aggregation. Usually ADP is responsible for inducing the platelet aggregation. Clopidogrel selectively inhibits the binding of ADP to its receptor and subsequent ADP-mediated activation of the glycoproteins GP 11b/111a complex the result total inhibition of platelet aggregation.
Where as it could not inhibit phosphodiesterase activity, it exhibits excellent property ie, irreversibly modifying the platelet ADP-receptor. Platelets exposed to clopidogrel are affected for the remainder of their life span. Which is extensively metabolized by the liver and its main metabolite is the carboxylic acid derivative. It has no effect on platelet aggregation. Generally bleeding time return to base line values only after treatment is discontinued (5 days). The prolongation of bleeding time is similar to healthy volunteers receiving 75 mg / day which is most potent drug hence can be used in reduction of atherosclerotic events such as myocardial infarction, stroke and death.
Clopidogrel can''t be used in severe hepatic diseases and it should discontinued seven days prior to surgery.
Drug interactions:
1) Clopidogrel + Aspirin : A positive effect is exhibited ie., Clopidogrel potentiated the effect of aspirin collagen induced platelet aggregation.
2) Clopidogrel + NSAIDS : Clopidogrel is usually associated with increased occult GIT blood loss.
Aspirin, which reduces the risk by about 25-50%, prevents vascular diseases in healthy individuals. Nowadays plastic aspirin has significance over acetyl salicylic acid because of additional clinical benefits in molecular design aspects and specifically binds with receptors and enhance the effect on platelets aggregation. To improve the clinical efficacy by combination therapy with polyaspirin + clopidogrel + isosorbid mono or tri nitrate of sustained release, control release or target drug delivery system of formulations are beneficial in clinical point of view.
The onset of action is quick and duration of action is prolonged. Such formulations are badly essential nowadays. The sublingual formulation of aspirin is not possible as today it will hydrolyse in to salicylic acid hence its activity on platelets is not useful, whereas transdermal formulation of these mentioned drugs can be formulated. Hence, the drug directly reaches the circulation and bypasses the liver. The major advantages are there is no burden on the liver and kidney, the enzymatic activity in the liver will not disturbed. Therefore depot formulations or transdermal formulations of these drugs are provided more weightages in improvement of clinical efficacy.
The modern civilization is suffering with some common diseases like hypertension, diabetes and cardiovascular diseases. Connection to cardiovascular problems and healthy individuals need 75 mg of aspirin daily. Therefore, it should be made compulsory for aspirin to be taken by people in the age group 40 years and above to avoid future risks. In these days many new molecules are required to reduce the viscosity of blood and dissolve the clot material in desired part of the coronaries or arteries. While maintaining exact cell biochemical parameters, such drugs have helped increase life spans in people, without being life threatening.
About the authors :
A M Krupanidhi, S G Vasantharaju, D K Ramesh are Lecturers at Bapuji Pharmacy College, Davangere, while Dr Vinutha Krupanidhi is a medical practioner