Atenolol, Mtaprolol and Propranolol have affects on both the beta 1 and beta 2 adrenergic receptors which makes them favorable in the treatment of uncomplicated hypertension but a patient with asthma and renal impairment should not be given these drugs as they have beta-2 blocking affects too. Te beta-2 blocking affects of these drugs could trigger an attack of asthma in an asthmatic patient due to the absence of beta-2 mediated bronchodilatation. Aso, i renal impairment these drugs could lead to worsening of the disease (Katzung 2009, p175-177).
of paracetamol occurs mainly in the liver after it is absorbed from the gastric system, te rate at which paracetamol is absorbed from the GIT depends mainly on the fact that how fast is the rate of emptyming of stomach. Ater the drug reaches the liver it undergoes the process of metabolism which include the process of conjugation and activation of the drug. Te amount of drug that raches the systemic circulation after being absorbed and metabolised is 75% of the total. Min process of metabolism occurs in the however, sme minor metabolism and brakdown process occurs in the renal system too.
I these two systems, te drug undergoes three main processes of metabolism namely 1) Glucoronidation, 2 oxidaion and 3) Sulfation. Oidation is the process which yields the useful and activated product. The activated product N-acetyl-p-benzoquinonemimime is mainly toxic for the body but this product is then conjugated with glutathione to form a conjugated and non toxic product which is then excreted mainly in the urine. Te other two metaolic pathways that include glucoronidation and Sulfation usually not that much importance as they mainly yield inactivated products.
Gucoronidation involves an enzyme UDP-Glucoronyltransferase which is the main enzyme catalysing this reaction. Wile in Sulfation, oly small quantities of paracetamol is usually converted to a product called N-acetyl-p-benzoquinonemimie by two major enzymes groups of the P450 family namely CYP3A4 and CYP2E1. Te activated product is then conjugated and converted to a less/non toxic mteabolite. Te matebolism of paracetamol as described earlier occurs in the liver where it is first activated and then conjugated by the processes sulfation and Te first process which involves its metabolism is the process of oxidation which results in the formation of NAPQI, te activated toxic. ..
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