Beta Blockers Properties Of Propranolol And Atenolol Biology Essay

Beta Blockers Properties Of Propranolol And Atenolol Biology Essay bring upThis essay reports the properties of propranolol ( oleophilic 1-selective blocker) and atenolol (hydrophilic 1-selective blocker) in the point of view of pharmacology, pharmacokinetics, and physical chemistry. It is observe that their pharmacological and pharmacokinetic properties atomic number 18 different, but its physicochemical properties argon relative close. trigger to -blockersThe -blockers atomic number 18 do drugss which act by blocking the return of mediators and agonists on the relevant receptors. The -blockers suggest an antihypertensive drug exercise, which is ca implementd by reduced cardiac output, decreased leaving of renin, central decrease of sympathetic action. Also, they exhibit an antianginal effect, which is caused by slowing of the ticker rate and thus decreased metabolic demand. The main side set up of general -blockers are cardiac failure, such(prenominal) as cardiac depress ion, hypotension, fistulous withers node dysfunction, atrioventricular block. The side effects depend on the properties of -blockers. For instance, non-selective -blockers show the unwanted effects caused by blocking 2-receptor. These show bronchoconstriction which is potentially austere in asthmatic patients and clinically undesirable in patients with other respiratory problems. Lipophilic -blockers may cause psychological symptoms, such as depression. at that place are or so important factors in the selection of -blockers, which are ISA, MSA, 1-selectivity, lipophilicity, solubility, and the epoch of effects. The 2-selective blockers are non used clinically, because of causing bronchoconstriction. Some -blockers show the effect of non only blocking the receptors, but also stimulating -receptors. It depends on the situation whether ISA positive -blockers stimulate or block -receptors. For example, these act as -blockers under the existence of -agonists. On the other hand, th ese invigorate the receptors under the non-existence of -agonists. such(prenominal) an effect is termed ISA which is intrinsic sympathomimetic action at law. The drugs which corroborate ISA decrease the side effects caused by -blockers. The non-selective blocks of -receptors cause the increase in cardiac afterload and bronchocostriction, because of 2-blocking. The 1-selective drugs slightly realise the effect of 2-blocking, but the risk of causing cardiac afterload and bronchoconstriction is lower than that of non-selective -blockers. The succession of effects depends on the disease. Long acting -blockers are desirable for high blood pressure and heart failure, because of the low frequency of administration. In contrast, short acting -blockers, propranolol, are ideal drugs for angina, because of the fast onset of action. As I stated above, lipophilic -blockers affirm a risk of causing depression. The reason is such drugs are absorbed easily, so can penetrate BBB. MSA, membrane stabilising activity, is an activity which prevents sodium ions from entering inside of cells. Many -blockers, such as propranolol, have the activity, so these are useful for arrhythmia.The properties of propranololPropranolol is a non-selective -blocker, which is clinically used as propranolol hydrochloride. The IUPAC differentiate is (2RS)-1-(1-Methylethyl) amino-3-(naphthalen-1-yloxy) propan-2-ol monohydrochlorid. The molecular weight is 295.80, and the melting point is around one hundred sixty-five degrees. It is colour crystalline powder, and it is easy to dissolve in water and methanol. Also, the methanol solution doesnt exhibit optical activity. Its structural formula is following.Propranolol is absorbed from the gastrointestinal tract, its plasma level reach a peak, 42.9ng/ml, after 1.5 hours of administration. The half brio is nearly 3.9 hours. The metabolism of propranolol is in general conducted by the liver, so it is metabolised to naphthoxylactic acid, glucuro nic acid conjugate, and 4-Hydroxypropranolol. It is mainly metabolised by CYP2D6, CYP1A2, and CYP2C19. As I discussed above, propranolol can penetrate BBB and transition to the brain, because of lipophilic. Its sexually transmitted disease amount is mostly excreted in urine within 48 hours, and the confront is excreted in faeces, which is just less than 4 percentages. Its pharmacological actions include an antihypertensive effect, an antianginal effect, and MSA. Propranolol doesnt show ISA in the experiment with using rats, so it is considered that propranolol doesnt show humans ISA as well as rats. Some side effects have been reported, such as, bronchoconstriction, slowing of heart rate, and allergic. These days, a new side effect is becoming popular, which is kind symptoms, such as depression, nightmare, and insomnia. There is the drug-drug interaction in propranol. For instance, propranolol cant use with thioridazine which is a psychotropic drug, especially for consolidation dysfunction symptom. The reason is the side effect of thioridazine is likely to happen, because of preventing propranolol from creation metabolised thioridazine by enzymes in the liver. In the same way, propranolol cant use with rizatriptan which is a drug for migraine. Combination use with propranolol and rizatoriptan induce the extension of half life of and the increase of AUC, so increase the side effects. Also, it is essential to evacuate administering rizatoriptan within 24 hours of administration of propranolol for the same reason. Its package tract authorise by US Food and Drug Administration warns.Therefore, its administration should not be stopped suddenly. Above statement is one of the most important warnings in the usage of propranolol.Properties of atenololAtenolol is a 1-selective blocker without covering MSA and ISA, which is used for hypertension, angina, and cardiac dysrhythmias. It is sold as TENORMIN in the market. The IUPAC name is 2-(4-(2RS)-2-Hydroxy-3-(1- methylethyl) amino propyloxy phenyl) acetamide. The molecular weight is 266.34, and the melting point is around 155 degrees. It is white or light yellow crystalline powder, and it is easy to dissolve in water and methanol as well as propranolol. In addition, the methanol solution doesnt exhibit optical activity. Its structural formula is following.Atenolol is around half absorbed from gastrointestinal tract, and the rest enter systemic circulation without acquiring first pass effect on the liver. Its half life is approximately 7 hours. Atenolol is miniature metabolised in the liver, but some are metabolised to glucuronic acid conjugate. The data shows that atenolol is low distribution to brain compared to proranolol, because its drug is hydrophilic. Therefore, it has been reported that atenolol hardly have an influence on mental symptom unlike propranolol. The excretion of oral atenolol is approximately 50% in urine and faeces respectively, but 90% of them are not metabolised. As I stated above, atenolol is a 1-selective blocker, so it is little to affect bronchial tubes which is controlled by 2-receptor. However, the data have been reported atenolol inhibit 2-receptor at high dose. Its side effects are closely the same as propranolol. The main dissimilarity between atenolol and propranolol is the incidence of tracheal symptoms, such as bronchoconstriction and bronchial spasm. Propranolol blocks -receptors non- selectively, so causes different tracheal symptoms. In contrast, atenolol inhibits 1-receptors selectively, so barely makes such symptoms happen. The sudden fulfilment of therapy with atenolol has a possibility of causing cardiac diseases for specific patients. Its leaflet approved by FDA cautions,The properties of -blockers in round patientsThese days, the number of pear-shaped lot is increasing due to high calorie foods and the decrease of exercise. It is common for obese patients to take drug therapy in clinical practice, because obesity is co nnected with some(prenominal) diseases, such as diabetes and cardiovascular disease. Therefore, it is important to identify pharmacological and pharmacokinetic properties in obese patients. Jerzy Wojcickia studied the pharmacological and pharmacodynamic properties between propranolol and atenolol in obese patients. As a result, he concluded following.ConclusionIn summary, in that location are some differences between propranolol and atenolol from the point of view of pharmacology, because of the difference of selectivity of -receptor. In the same way, there are some pharmacokinetic differences as well, such as the duration of half life and the mechanism of metabolism and excretion. In contrast, their physicochemical properties are similar. In clinical use, there are some warnings respectively, and the common cautions are to avoid sudden discontinuation of administration. Its dosage should be progressively decreased over a few weeks in gear up to avoid such side effects. I studied the characters between these -blockers in obese patients. In the study, it was not observed there are the clear differences between obese patients and non-obese patients