Glucocorticoids hydrocortisone

Drugs belonging to this class are glucocorticoids (hydrocortisone, 11-dehydrocorti-costerone, corticosterone), mineralocorticoids (aldeosterone, 11-deoxycorticosterone, ll-deoxy-17-oxycorticosterone), and sex hormons (androsterone, androstendion, estrone, progesterone). 

The remaining steroid lipids constitute two main classes of steroid hormones sex hormones and adrenocortical hormones. The sex hormones include androgens (testosterone, androsterone), estrogens (estrone, estradiol), and progestins (progesterone). The adrenocortical hormones include mineralocorticoids (aldosterone) and glucocorticoids (hydrocortisone). 

The adrenocorticotrophic hormone ACTH (corticotropin) stimulates the adrenal cortex to secrete the glucocorticoids hydrocortisone (cortisol) and corticosterone, the mineralocorticoid aldosterone, and a number of weakly androgenic substances, as well as a small amount of testosterone. Aldosterone synthesis is also regulated by renin and angiotensin. 

A synthetic analogue of the major glucocorticoid hydrocortisone (cortisol), prednisolone has proven an effective... 

Hydrocortisone, USP, Hydrocortisone. 11/3,17.21-tri-hydraxyprcgn-4-cnc-3.2().dionc. is the primary natural glu-vocorlieoid in humans. Despite the large number of synthetic glucocorticoids, hydrocortisone, its esters, and its salts rc-in.tin a mainstay of modem adrenocortical steroid therapy iind Ihe standard for comparison of all other glucocorticoids and mineraliKorticoids (sec Table 2.3-8). It is used for all the indications mentioned above. Its esters and. salts illustrate Ihe principles of chemical modification to modify pharmacokinetic use shown in Figure 2.3-6. The commercially available salts and esters (sec Fig. 23-30) include... 

The client diagnosed with multiple sclerosis (MS) is prescribed the intravenous glucocorticoid hydrocortisone (Solu-Cortef). The client has a saline lock. Which procedures should the nurse follow when administering the medication Rank in order of performance. 

When in the late 1940 s the remarkable therapeutic effects of the glucocorticoids cortisone and hydrocortisone were discovered, new raw materials had to be developed to produce these complicated molecules, and new synthetic methods devised to convert either a 20-ketopregnane or 21-acetoxy-20-ketopregnane to the dihydroxyacetone side-chain characteristic of these corticoids. This latter challenge produced some extremely useful new organic chemical reactions, many of which have wider application outside of steroids. 

An endocrine disorder first described by the British Physician Thomas Addison in the mid 1800 s. The adrenal glands fail to produce sufficient amounts of glucocorticoid hormones (cortisol) and sometime mineralocorticoid (aldosterone). If left untreated it is life-threatening, the patient will show muscle weakness, hyperpigmentation and even depression. Typical treatment is hydrocortisone replacement therapy. 

Glucocorticoids are secreted by the cells of the zona fasciculata in the adrenal cortex. Hydrocortisone is the most important, and regulates intermediary metabo-... 

Monitor for adverse reactions from hydrocortisone administration. Glucocorticoid therapy at physiologic replacement doses should not lead to the development of Cushing s syndrome. However, careful monitoring should still be performed. Use the smallest effective dose. 

Non-prescription and herbal products with glucocorticoid activity (e.g., non-prescription anti-itch products with hydrocortisone, herbal products with magnolia bark or those claiming to contain adrenal cortex extracts or other by-products)... 

Stop the glucocorticoid when the equivalent physiologic dose is reached (20 mg/day of hydrocortisone or 5-7.5 mg/day of prednisone or equivalent). 

The cellular mechanism of action of hydrocortisone, a glucocorticoid, is also related to proteins but not by the enhancement of cAMP production. Hydrocortisone is transported by simple diffusion across the membrane of the cell into the cytoplasm and binds to a specific receptor The steroid-receptor complex is activated and enters the nucleus, where it regulates transcription of specific gene sequences into ribonucleic acid (RNA). Eventually, messenger RNA (mRNA) is translated to form specific proteins in the cytoplasm that are involved in the steroid-induced cellular response. 

Hydrocortisone, cortisone, and prednisone are the glucocorticoids of choice, administered twice daily at the lowest effective dose while mimicking the normal diurnal rhythm of cortisol production. 

Because most adrenal crises occur because of glucocorticoid dose reductions or lack of stress-related dose adjustments, patients receiving corticosteroid-replacement therapy should add 5 to 10 mg hydrocortisone (or equivalent) to their normal daily regimen shortly before strenuous activities such as exercise. During times of severe physical stress (e.g., febrile illnesses, after accidents), patients should be instructed to double their daily dose until recovery. 

Hydrocortisone given parenterally is the corticosteroid of choice because of its combined glucocorticoid and mineralocorticoid activity. The starting dose is 100 mg IV by rapid infusion, followed by a continuous infusion or intermittent bolus of 100 to 200 mg every 24 hours. IV administration is continued for 24 to 48 hours. If the patient is stable at that time, oral hydrocortisone can be started at a dose of 50 mg every 8 hours for another 48 hours. A hydrocortisone taper is then initiated until the dosage is 30 to 50 mg/day in divided doses. 

Patients with adrenal insufficiency should carry a card or wear a bracelet or necklace that contains information about their condition. They should also have easy access to injectable hydrocortisone or glucocorticoid suppositories in case of an emergency or during times of physical stress, such as febrile illness or injury. 

Glucocorticoid therapy with IV hydrocortisone 100 mg every 8 hours should be given until coexisting adrenal suppression is ruled out. 

The natural glucocorticoid is hydrocortisone (cortisol). Semi-synthetic 9a-bromohydrocortisone 21-acetate was found to be less active as an anti-inflammatory agent than hydrocortisone 21-acetate by a factor of three, and 9a-iodohydrocortisone 21-acetate was also less active by a factor of 10. However, 9a-fluorohydrocortisone 21-acetate (fludrocortisone acetate) was discovered to be about 11 times more active than hydrocortisone acetate. Although the bromination sequence shown is equally applicable to chlorine and iodine compounds, fluorine must be introduced indirectly by the P-epoxide formed by base treatment of the 9a-bromo-lip-hydroxy analogue. 

I. Replacement therapy. The adrenal cortex (AC) produces the glucocorticoid cortisol (hydrocortisone) and the mine-ralocorticoid aldosterone. Both steroid hormones are vitally important in adaptation responses to stress situations, such as disease, trauma, or surgery. Cortisol secretion is stimulated by hypophyseal ACTH, aldosterone secretion by angiotensin 11 in particular (p. 124). In AC failure (primary AC insuffiency ... 

The primary endogenic glucocorticoids are hydrocortisone and cortisone. Numerous synthetic analogs of natural glucocorticoids have been made and used, and they have turned out to be more effective, and currently they have almost completely replaced cortisone (prednisolon, prednisone, dexamethasone, and others). 

Pharmacokinetics Hydrocortisone and most of its congeners are readily absorbed from the Gl tract altered onsets and durations are usually achieved with injections of suspensions and esters. Hydrocortisone is metabolized by the liver, which is the rate-limiting step in its clearance. The metabolism and excretion of the synthetic glucocorticoids generally parallel hydrocortisone. Induction of hepatic enzymes will increase the metabolic clearance of hydrocortisone and the synthetic... 

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