Pharmacokinetic and Pharmacodynamic Properties of Drug Delivery Systems Essay
Discussion initial Post Topic
- Explain why nitroglycerine is usually not given orally and give an example of another drug that is effected by the route of administration.
- Why different routes of administration are utilized.
- What effect do the different routes of administration have on the bioavailability of the drug?
Be sure to address all three items Pharmacokinetic and Pharmacodynamic Properties of Drug Delivery Systems Essay
Nitroglycerine
Nitroglycerin is a vasodilator nitrate drug whose primary goal is to relieve angina chest pain. The FDA has approved it for acute prevention of angina pectoris resulting from coronary artery disease or for acute relief of an attack (Kim et al., 2023). The Nitrate prodrug gets split to nitric oxide, the active medium, resulting in activation of the guanylyl cyclase enzyme, which in turn leads to increased levels of intracellular guanosine 3′, 5′ – cyclic monophosphate (cGMP) (Pirahanchi & Dimri, 2020). cGMP then modifies the actions of cyclic nucleotide phosphodiesterases and activates the cGMP-dependent protein kinase (PKG). This, in turn, induces the dephosphorylating of the myosin light chain and decreases the calcium ion concentration in the cytoplasm. This relaxes smooth muscle within blood vessels, producing the desired vasodilation effect. This discussion will examine the nitroglycerin’s administration routes, rationale, and impact on bioavailability.
PLACE YOUR ORDER HERE NOW
Why is nitroglycerin not given orally?
Nitroglycerin is not commonly administered orally for various reasons. When taken orally, nitroglycerin is extensively metabolized in the liver during first-pass metabolism, which greatly breaks it down before it enters systemic circulation. This process reduces its therapeutic efficacy, rendering oral ingestion ineffective for accomplishing the intended results. Furthermore, nitroglycerin’s oral absorption can be erratic and variable, which adds to the medication’s inconsistent effects. While the oral route is not the most favored method of administration due to its slower onset of action compared to alternatives like the sublingual route, it may not be ideal for conditions such as angina that demand immediate medication.
Warfarin, a common blood thinner, is another example of a medication whose administration method has a significant impact. While the most prevalent method of administering warfarin is orally, the use of intravenous (IV) administration is uncommon due to the increased risk of bleeding complications. The difference is due to the slower onset and longer duration of action seen with oral administration compared to intravenous administration, allowing for more precise control over blood clotting. Thus, the route of administration plays a major role in determining the safety and therapeutic effectiveness of drugs such as nitroglycerin and warfarin. Pharmacokinetic and Pharmacodynamic Properties of Drug Delivery Systems Essay
Why different routes of administration are utilized?
Choosing how to administer a drug is a vital aspect of pharmacotherapy, influenced by the drug’s characteristics, therapeutic goals, patient attributes, and clinical considerations. Regarding the drug’s absorption, distribution, metabolism, and elimination (ADME), each route has a unique pharmacokinetic profile that impacts the drug’s bioavailability and therapeutic effectiveness (Glassman & Muzykantov, 2019). Healthcare providers consider different factors when selecting the most appropriate route of administration. Recommended for situations requiring immediate action, like acute angina attacks, sublingual administration is selected to ensure rapid relief (Kubica et al., 2022). Stielow et al. (2023) emphasize the importance of bioavailability in ensuring that the right amount of medication reaches the intended location for effective treatment. Safety and tolerability vary depending on the route of administration, each presenting its risks and potential side effects. Healthcare providers consider these factors the anticipated advantages when selecting the most suitable treatment method for a specific patient.
What effect do the different administration routes have on the drug’s bioavailability?
Bioavailability, the amount of a drug that reaches its intended site and causes the intended effect, differs greatly depending on the method of administration (Stielow et al., 2023). Sublingual administration places the drug under the tongue for direct absorption into the bloodstream through the sublingual tissues. This avoids the first-pass metabolism, resulting in greater bioavailability (Kim & De Jesus, 2023). Nitroglycerin, for instance, is frequently administered sublingually to alleviate angina promptly and effectively. Though convenient, oral administration may result in varying levels of bioavailability because of unpredictable absorption in the gastrointestinal tract that is unpredictable and first-pass metabolism (Kim & De Jesus, 2023). Administering a substance intravenously bypasses absorption processes, resulting in the most reliable and highest bioavailability (Kim & De Jesus, 2023). Nevertheless, there are risks associated with IV administration due to the direct injection into the bloodstream, such as the possibility of infection and adverse reactions.
Transdermal administration, often using patches, delivers the drug gradually through the skin, providing prolonged effects. Transdermal administration may lead to reduced peak bioavailability compared to certain other routes. Therefore, choosing the route of administration is a crucial decision in pharmacotherapy as it affects the drug’s bioavailability, therapeutic effectiveness, and safety characteristics. Healthcare providers can tailor treatment regimens to meet individual patient needs and clinical goals by comprehending the pharmacokinetic properties of various administration routes.
References
Glassman, P. M., & Muzykantov, V. R. (2019). Pharmacokinetic and pharmacodynamic properties of drug delivery systems. Journal of Pharmacology and Experimental Therapeutics, 370(3), 570–580. https://doi.org/10.1124/jpet.119.257113
Kim, J., & De Jesus, O. (2023, August 23). Medication routes of administration. PubMed; StatPearls Publishing. https://www.ncbi.nlm.nih.gov/books/NBK568677/
Kim, K. H., Kerndt, C. C., & Schaller, D. J. (2023, July 31). Nitroglycerin. PubMed; StatPearls Publishing. https://www.ncbi.nlm.nih.gov/books/NBK482382/#:~:text=Nitroglycerin%20is%20a%20vasodilatory%20drug
Kubica, J., Adamski, P., Ładny, J. R., Kaźmierczak, J., Fabiszak, T., Filipiak, K. J., Gajda, R., Gąsior, M., Gąsior, Z., Gil, R., Gorący, J., Grajek, S., Gromadziński, L., Gruchała, M., Grześk, G., Hoffman, P., Jaguszewski, M. J., Janion, M., Jankowski, P., Kalarus, Z., … Zielińska, M. (2022). Pre-hospital treatment of patients with acute coronary syndrome: Recommendations for medical emergency teams. Expert position update 2022. Cardiology Journal, 29(4), 540–552. https://doi.org/10.5603/CJ.a2022.0026
Pirahanchi, Y., & Dimri, M. (2020). Biochemistry, guanylate cyclase. PubMed; StatPearls Publishing. https://www.ncbi.nlm.nih.gov/books/NBK537151/
Stielow, M., Witczyńska, A., Kubryń, N., Łukasz Fijałkowski, Nowaczyk, J., & Nowaczyk, A. (2023). The bioavailability of drugs—the current state of knowledge. Molecules, 28(24), 8038–8038. https://doi.org/10.3390/molecules28248038
