Endogenous Compounds as Drugs – Drug Therapy Example

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"Endogenous Compounds as Drugs"  is a great example of a paper on drug therapy.   Endogenous compounds are substances whose origin is within an organism, tissues, or cells. These compounds include hormones, antibiotics, and steroids among many others. Pharmacological studies carried out on endogenous compounds show that these substances undergo a series of mechanisms in an organism’ s body to preserve and restore its hemostatic equilibrium. These mechanisms include reversible interconversion, active and diffusional transports, saturable enzyme biotransformation, a balance between synthesis and dietary supply, asymmetric distribution; specific body storage, gender differences, and feedback processes. However, when administering the drug to an organism, the presence of endogenous compounds inside the body of the organism or the in the diet should be considered.

The baseline endogenous concentrations in the blood of an organism can be measured and subtracted from the total concentrations in order to prevent the excessive drug from being administered in the body, Below is a table showing the various endogenous compounds, Group Examples  Structures Hormones estrogen Estradiol, estriol or estrone   Antidiuretic hormone Peptides consisting of nine amino acids. Steroids corticosteroids Hydrocortisone, acetonides, betamethasone, esters, halogenated or labile prodrug esters   Anabolic steroids Cyclic steroid rings Antibiotics penicillin Beta-lactam   cephalosporin Beta-lactam   Hormones Hormones relate to the human body chemical messengers produced by the endocrine glands (NLM, 2015, p.

1). The endocrine system entails glands including hypothalamus, thymus, ovaries, testes, thyroid, pituitary gland, pancreas, parathyroid, pineal gland, and adrenal glands. These glands produce specific hormones in the body that on interaction with body cells or tissues produce effects such as reproduction, metabolism, respiration, excretion, lactation, movement, tissue function, sleep, sexual function, mood, growth, and development. The structure of hormones can be protein, steroid, peptide, or amino in nature. Below is an in-depth analysis of the hormones produced in the ovaries that is estrogen in breast cancer therapy. Ovary hormones Estrogen is a hormone produced by the woman’ s ovaries until menopause.

After the onset of menopause, the production of estrogen is shifted to the fat tissues that produce it in small amounts. The estrogen hormone is known to promote the growth of cancers that are estrogen-hormone receptor-positive such as breast cancer. In breast cancer therapy, either the estrogen levels remain lowered or their production stopped. The estrogen production in the pre-menopause stage can remain blocked or minimized by using tamoxifen.

Tamoxifen is thus an anti-estrogen in breast cancer. It binds on the estrogen hormone receptors and thus is similar in structure to the estrogen in order to be a competitor for the active site, according to Medline Plus. However, tamoxifen acts as an estrogen in other tissues such as the uterus and bones. Women who have not undergone menopause mostly use Tamoxifen whereas those who have undergone menopause use aromatase inhibitors. The chemical structure of estrogen is as shown, Steroids Steroids are cyclic organic compounds. The body produces three major types of steroids including Corticosteroids, sex hormones, and androgenic or anabolic steroids.

Anabolic steroids whether synthetic or natural produce affects the human body through interaction with androgen receptors to help increase muscle and bone synthesis. Sex hormones are steroids that produce sex differences, and support reproduction such as estrogens, androgens, and progestagens. Corticosteroids including glucocorticoids regulate metabolism and immune functions. On the contrary, mineralocorticoid maintains the blood volume besides controlling electrolytes renal excretion (Makin, 2010, pp. 45). Corticosteroids are critically discussed below. Corticosteroids Corticosteroids relate to steroid hormones emanating from the adrenal cortex for purposes such as protein catabolism, inflammation regulation, stress response, carbohydrate metabolism, and behavior and blood electrolyte levels.

Drugs with corticosteroids effects and structure can be synthetically produced to treat various disorders such as brain tumors, skin diseases, arthritis, allergic reactions, inflammatory bowel disease, hepatitis, asthma, dermatitis, systemic lupus erythematosus, Addison’ s disease and sarcoidosis, Lednicer (2011, p. 11). However, the use of corticosteroids of both glucose and mineral nature can cause side effects (Wolverton, 2012, p. 781). These side effects include Cushing’ s syndrome, hypertension (high levels of blood pressure), hypernatremia (high levels of sodium in the blood), and immunosuppressive effects that result in impaired healing of the wounds or formation of ulcers.

Furthermore, they can also cause permanent eye damage. The benefits of corticosteroids outweigh the demerits and thus many pharmaceutical companies utilize these steroids with little modification to produce desired results and minimal side effects. An example of these modifications is the alteration of the 21-carbon skeleton to enable the steroid selectively alters the amount of anti-inflammatory activity, its protein binding affinity, and its metabolic consequences. In addition, a double bond is introduced between C-1 and C-2 to enhance the activity of the steroid.

Fluorination is also introduced at C-9 for better results, according to Lednicer (2011, p. 13). The chemical structure is as shown below (Johansen, 2011, p. 101). Antibiotics Antibiotics also referred to as antibacterial finds use against bacteria by inhibiting their growth or killing them. In addition, some antibiotics are known to be effective against some fungi and protozoans. The working of antibiotics in an organism’ s body as a drug depends on the host defense mechanism, the location of the infection, the pharmacodynamics and pharmacokinetic properties of the antibiotic.

However, the use of antibiotics for therapeutic purposes is under a major challenge of antibiotic resistance. Antibiotics classification relies on chemical structure, mechanism of action, and spectrum of activity. They are classified into penicillins, cephalosporins, glycylcyclines, oxazolidinones, lipiarmycins, macrolides, fluoroquinolones, sulfonamides, tetracycline, and aminoglycosides. Below is a detailed explanation about the penicillin use as endogenous drugs. Penicillin                       Penicillin defines a collection of antibiotics broadly used in the pharmaceutical industry. It is derived from the penicillium fungi. Penicillin is b-lactam antibiotics used over the years for the treatment of bacterial infections which are often due to susceptible gram-positive bacteria such as streptococci, staphylococci, clostridium and Listeria bacteria (Grill and Maganti, 2011, p.

383). However, misuse of penicillin has led to most bacteria developing resistance against the endogenous drug (Hollinger, 2007, p. 112). Despite the use of penicillin  G, V, procaine and benzathine subtypes, more advanced subtypes have also been developed to counter the resistance such as antistaphylococcal penicillins, aminopenicillins, and antipseudomonal penicillins, according to report by WHO, (2014, p. 1).                       Side effects in association with applications of penicillin include nausea, diarrhea, rash, hypersensitivity, superinfection, urticaria, and neurotoxicity.

Modification made in the second-generation penicillin to enable the penicillin to kill a wide range of bacteria is the introduction of Penicillium chrysogenum strain that has a thiazolidine ring connected to a beta-lactam ring with a variable side chain. This combination helps the penicillin resist hydrolysis of their beta-lactam ring by beta-lactamase enzymes present in the bacteria. Thus, the second-generation penicillin is more effective even to the resistant bacterial strains. The chemical structure is as shown below,

References

Grill, M, & Maganti, R 2011, 'Neurotoxic effects associated with antibiotic use: management considerations', British Journal Of Clinical Pharmacology, 72, 3, pp. 381-393, Academic Search Premier, EBSCOhost, viewed 13 March 2015.

Hollinger, Mannfred A. 2007. Introduction to Pharmacology, Third Edition. Boca Raton, Florida..p 112

Johansen, Duus, J. (2011). Contact dermatitis. Berlin, Springer.

Lednicer, D. (2011) Steroid Chemistry At A Glance. Hoboken, N.J. : Wiley

Makin, M. and Gower, D. (2010) Steroid Analysis. Dordrecht. New York. Springer

United States National Library of Medicine (NLM). 2015. Hormones. Medline Plus. US National Library Of Medicine. Web. March 13, 2015. Retrieved from http://www.nlm.nih.gov/medlineplus/hormones.html

Wolverton, S. E. (2012). Comprehensive dermatologic drug therapy. Philadelphia, Pa, Saunders.

World Health Organization (WHO). April 30, 2014. WHO’s First Global Report On Antibiotic Resistance Reveals Serious World Wide Threat To Public Health. The World Health Organization. Web. March 13, 2015. Retrieved from http://www.who.int/mediacentre/news/releases/2014/amr-report/en/

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