FLUOROMETHOLONE AND OTHER CORTICOSTEROIDS FOR INFLAMMATION
SUMMARY: Cap like structures that appear on the top of both kidneys are referred as adrenal glands. As they are located above the kidney, they are also referred as ‘suprarenal glands’.1In the transverse section of adrenal gland, two regions can be identified - medulla and cortex.1The medulla region is innervated by sympathetic nervous system which helps in production and release of two important neurotransmitters - Epinephrine and Norepinephrine.1 The cortex is responsible for synthesis and release of three different hormones namely - mineralocorticoids, glucocorticoids and androgens.1 Mineralocorticoids and glucocorticoids are collectively referred as corticosteroids.
…show more content…
During this trial and error procedure of adding and removing different functional groups, structure activity relationship was established which provided us knowledge about the contribution of different functional groups towards efficacy of the drug or towards unwanted effects. Certain molecular modifications helped in achieving targeted drug delivery for different skin disorders and ophthalmic conditions. The data obtained from the preclinical and clinical studies serve as a strong evidence for effectiveness of these synthetic corticosteroids.
STRUCTURE ANALYSIS: Fluorometholone is a synthetic topical corticosteroid consisting of four fused ring systems out of which three rings are of cyclohexane and one of cyclopentane. The three cyclohexane rings are named A, B and C respectively. Figure 1: Structure of Fluorometholone
These three rings form the per-hydro derivative of Phenanthrene to which the fourth cyclopentane ring or D ring is fused. Hence, we can also say it is cyclopenta[a]phenanthrene derivative.3The steroid nucleus can be classified into several classes depending on the chemical constituents. If we analyze the structure of Fluromethalone, it specifically contains the Pregnane4 – Steroid Nucleus consisting of 21 carbons in its skeleton. Moreover, the pregnane nucleus is a planar ring system with two stereo-isomeric forms depending on the spatial arrangement of hydrogen on C-5. Both α – F at C-9 and = at C 1,2
The last glands are the adrenal glands, which are located above the kidneys, and have an inner core and an outer layer. The inner core is called the adrenal medulla, and the outer layer is known as the adrenal cortex.
The adrenal glands are composed of two sections, the medulla and the cortex. The medulla part of the gland is what produces adrenaline-like hormones. The cortex produces a group of hormones called corticosteroids
The adrenal glands are made up of two different sections. The interior (medulla) which produces hormones similar to adrenaline. The (cortex) outer layer has the role of producing a group of hormones that are called corticosteroids; these include mineralocorticoids, glucocorticoids and the male sex hormones known as (androgens).
Aldosterone falls in the class of hormone called mineralocorticoids, produces by the adrenal glands and is found near the kidneys. It sustains blood pressure, water and salt balance within the body. This procedure is assisting the kidneys to preserve sodium and excrete potassium in order to maintain a balance. If Aldosterone production falls, there isn’t enough regulation of salt and water balance (as aldosterone is being lost through urination) triggering blood pressure and blood volume to decline as a result of the kidneys not functioning properly. If body is in need of salt, water is not retained and adrenals release more Aldosterone and salt is reabsorbed from the tubule.
They found out that a tracer amount of Corticosterone put in mice became more abundantly in the hippocampus of adrenalectomized rats and was bounded with high affinity to MR but not GR receptors. Also, MR receptors had high affinity to cortisol than to Corticosterone and showed a greater degree of plasticity in response to neurotrophic peptides. Moreover, corticosterone has maintained through MR receptors, and the corticosterone maintained excitability in the hippocampal neurons and had high excitatory tone over an inhibitory GABAergic network surrounding CRH-producing neurons in the PVN. They said that MR antagonist disinhibits basal and induce stress during the hypothalamus- pituitary-adrenal activation through the receptors interferes with negative feedback and prolonged stress cause hypothalamus -pituitary- adrenal
(D) The structures of the steroid hormones GR, MR, AR, PR and ER are shown with numbering of the rings and the key atoms. (Taken from: 1)
Adrenal glands are endocrine glands that sit atop the kidneys (Shier et al., 2009). The adrenal glands secrete hormones that increase heart rate, the force of cardiac muscle contraction, breathing rate, elevate blood pressure and blood glucose level. This activity prepares the body foe energy expending action, sometimes called fight or flight responses (Shier et al., 2009).
Addison’s Disease is associated with the adrenal glands releasing organs which mean it only has one on each side of the small gland of kidney that will create amount of layers which is cortex and the medulla. What is cortex? Cortex is the outer area that will secrete corticosteroid hormones like cortisol or aldosterone. Medulla is part of the inside area where it controls the sympathetic
Adrenal glands contain cells which produce hormones cortisol, aldosterone (salt retaining hormone) and androgen. Adrenal glands also form small amounts of sex hormones such as testosterone and oestrogen. The amount of cortisol made is controlled by adrenocorticotrophic hormone (ACTH), made by the pituitary gland. Cortisol protects the body from illness or injury by maintaining immunity and anti-inflammatory processes and maintains blood pressure. Cortisol is also responsible for feeding back to inhibit ACTH production. If too much cortisol reaches the pituitary, pituitary inhibits adrenal glands, to return cortisol levels to normal. Cortisol normally starts to be produced in the second month of foetal life however, CAH prevents the formation of
Corticosteroids are normally made by the adrenal glands located on the top of each kidney. It is often prescribed for a major variety of conditions to help reduce inflammation and to let the immune system relax. Specific hormones that the body cannot produce automatically can be replaced by corticosteroids. An example of the body not being able to manufacture hormones itself, would be the Addison’s disease. This disease occurs due to the inability of the adrenal glands to produce the sufficient amount of homones that
Docetaxel chemical name is (2R,3S)-N-carboxy-3-phenylisoserine,N-tert-butyl ester, 13-ester with 5β-20-epoxy-1,2α,4,7β,10β,13α-hexahydroxytax-11-en-9-one 4-acetate 2-benzoate, trihydrate. Docetaxel’s structural formula:
One of the majors the adrenal gland is located above the kidneys. the adrenal insufficient is also known as primary or secondary. Primary adrenal insufficiency and hypocortisolism, is a long-term endocrine disorder and the adrenal gland cannot produce enough steroid hormones that your body needs. Secondary happens when the pituitary gland, a pea sized gland that is located on the base of the brain, it does produce enough adrenocorticotropin “ACTH” this is a hormone that stimulates that adrenal gland and it is the cause of a hormone cortisol, and the production levels will drop. the adrenal gland will eventually shrink due to not producing enough ACTH stimulation cortisol and if ACTH output is to low then the cortisol that is producing will drop. Eventually, the adrenal glands will shrink due to the lack of ACTH stimulation. Cortisol is a steroid that helps
Flutamide and Cyproterone acetate and Spironolactone(a synthetic steroidal derivative of aldosterone) have anti androgenic activity is mostly related to the inhibition of androgen receptors, in particular the ones that bind DHT while estrogens block androgen receptors by inhibit 5-alpha reductase activity and increase hepatic production of sex hormone binding protein lead to reducing blood levels of free testosterone by reducing the fraction available for biological
Hydrocortisone is a topical steroid .It reduces the action of chemicals in the body that cause inflammation, redness, eczema, and swelling. Moreover, Hydrocortisone topical is used to treat inflammation of the skin caused by a number of conditions such as allergic reaction eczema or psoriasis. These topical steroid will not treat a bacterial, fungal or viral skin infection.
Adrenal glands, located near the kidneys, secrete several hormones that are activated by the nervous system. These hormones dictate the body’s reaction to stressful situations. Each person secretes a different amount of hormones, therefore affecting behavior in stressful situations differently (Morris & Maisto, 2005).