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Pharmacology - Essay Example

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Lignocaine Author’s Name Institution Section 1. Drug absorption State the oral bioavailability The bioavailability of lignocaine is 35% following an oral administration (Kwan, 2001). Discuss whether the bioavailabilty is influenced by first pass hepatic extraction, gastrointestinal absorption, or both The bioavailability of lignocaine is dependent upon the absorption and hepatic biotransformation of the drug…
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Pharmacology
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Download file to see previous pages In the liver, lignocaine biotransformation involves oxidative N-dealkylation, cleavage of the amide linkage, ring hydroxylation and conjugation (Bennett, 1992). The oxidative N-dealkylation process is the major pathway in biotransformation of the drug in the liver. The oxidative N-dealkylation pathway produces glycinexylidide and monoethylglycinexylidide metabolites that have less potent pharmacologic effects than lignocaine (Kwan, 2001). In addition, these metabolites are less toxic than the primary drug. Section 2. Drug formulation and administration routes List all the formulations and doses available in Australia In Australia, Lignocaine is available as a lignocaine injection, Xylocaine, Xylocaine with adrenaline, Xylocard, Xyloproct suppositories. In addition, it is also sold as Gravocain, Leostesin, Maricaine, Cappicaine, Esracaine, Lidoderm and Anestacon. Many ointments, lotions, creams and gels used topically, contain lignocaine. Lidoderm contains 5% of lignocaine and is used for the treatment of neuropathic pain. Lignocaine injection is approved for administration of 200-300mg for adults and 100mg for children in the treatment of cardiac arrhythmias. Topical ointments and gels contain 5% of lignocaine. Some other formulation have been added to adrenaline and are used for cardiac arrest with arrhythmias. Discuss any administration issues that are followed for safe and efficacious use The loading dose of the drug is usually administered as an infusion dose or a slow infusion so as to avoid the toxic effects of the drugs. When given as rapid bolus, lignocaine causes hypotension due to depression of the myocardial contractility as well as CNS related effects (Grover, 2009). The side effects following rapid bolus infusion are seen more commonly in the elderly. They are also seen in patients with pre-existing heart conditions. In order to achieve the plasma therapeutic dose, the loading dose is followed by a maintenance dose. When the drug is used as a local anaesthetic agent via infiltration method, blood vessels should be avoided (Donald & Henry, 2003). Discuss the reasons why the drug is not available as an oral formulation Lignocaine is well absorbed in the gastrointestinal system. However, due to its extensive hepatic biotransformation, it is administered as parenterally (Bennett, 1992). It is available as topical, mucosal, intravenous, intratracheal and intramuscular formulation so as to avoid the extensive first pass hepatic extraction. The drug is not available as an oral formulation because it provides low concentration of the unchanged drug in plasma. Section 3. Drug distribution State the percent bound to plasma proteins The plasma binding ability of lignocaine is dependent on the concentration of the drug (Kwan, 2001). This implies that the higher the concentration of the drug, the less it is bound to plasma. About 60-80% of the drug is protein bound in a concentration of about 1-4 mcg of free base in every millilitre (Kwan, 2001). In some condition, the binding of the drug is increased or decreased. In case of myocardial infarction and other acute illness, the binding of lignocaine to plasma proteins is increased. This is because of increase the concentration of plasma alpha-1 glycoprotein. Plasma alpha-1 glycoprotein is an acute phase reactant protein. It binds lignocaine thus reducing the concentration ...Download file to see next pagesRead More
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