Dexamethasone properties

The natural compounds cortisol [50-23-7], cortisone [53-06-5], and corticosterone [50-22-6] vary only slightly in stmctures and pharmacologic properties (see Steroids). The synthetic analogues inmore modem practice, prednisolone [52438-85-4], dexamethasone [50-02-2], triamcinolone [124-94-7], and betamethasone have greater antiinflammatory potency, and their effects on sodium retention tend to be less severe. 

Metoclopramide is used for its antiemetic properties in patients with diabetic gastroparesis and with dexamethasone for prophylaxis of delayed nausea and vomiting associated with chemotherapy administration. 

The thalidomide analogs CPS49 (30) and CPS11 (31) have been reported to inhibit PI3/AKT signaling in multiple myeloma cells via an anti-angiogenic effect. These compounds are devoid of the teratogenic properties seen with thalidomide and are currently in preclinical development [66]. Compound 30, and to a lesser extent 31, induced a dose-dependent inhibition of proliferation in several multiple myeloma cell lines and reduced phospho-AKT levels [66]. These compounds also inhibited DNA synthesis in cell lines resistant to conventionally used anti-multiple myeloma drugs (e.g. dexamethasone, anthracyclines and melphalan) in a dose-dependent manner. 

Other agents such as actinomycin D, C-Myc antisense, dexamethasone, and matrix metalloproteinase inhibitors, aimed at altering inflammatory and smooth muscle actions in the biological repair response to vascular injury, are being evaluated. The success of these devices depends upon multiple issues, including stent platform, carrier, drug properties, and pharmacokinetic profile (18-26). Large randomized, controlled trials, demonstrate a restenosis rate of 5% to 10% with DES (27). 

Melgert et al. [103] used this in vitro system to determine whether the drug targeting preparation containing the anti-inflammatory drug dexamethasone coupled to HS A, was still able to manifest its anti-inflammatory properties in hver slices. Dexamethasoncio-HSA and uncoupled dexamethasone showed effective inhibition of LPS-induced NO and TNFa pro-... 

Glucocorticoids have potent anti-inflammatory and immunosuppressive properties. This is particularly evident when they are administered at pharmacological doses. A variety of synthetic glucocorticoids, some far more potent than cortisol, have been created for therapeutic use, such as hydrocortisone, prednisone, prednisolone, dexamethasone and betamethasone. 

The adrenal cortex produces steroidal hormones that are associated with carbohydrate, fat, and protein metabolism, electrolyte balance, and gonadal functions. One of these, cortisone. C2iH2805 (11), demonstrated a remarkable ability to relieve the symptoms of inflammatory conditions. Other glucocorticoid steroids, such as dexamethasone, Cj2H2gFO< (12, R = F, R = CIlj), and prednisolone, U21II28O5 (12, R — R — 11), also have antiinflammatory properties. 

Corticosteroids such as prednisone or dexamethasone have lympholytic properties. They reduce the lymphoid contents of the lymph nodes and the spleen without influencing the myeloid or erythroid stem cells. Corticosteroids have the following pharmacological effects on immunosuppression ... 

Corticosteroids (dexamethasone, methylprednisolone) have antiemetic properties, but the basis for these effects is unknown. These agents are commonly used in combination with other agents in the... 

Sustained release intravitreal dexamethasone implants have a potential use in reducing ocular inflammation and treating PVR. The device consists of a 5 mg pellet of dexamethasone coated with 10% PVA and EVA giving a mean release rate of 1.2 0.1 pg/hr over a period of 5 months. A slow release daunomycin implant was fabricated by loading the polysulfone capillary fibre with 1% w/w of daunomycin in tristearin. The controlled release is attributed to the diffusion-retardant properties of the fat. An experimental evaluation of the kinetics and efficacy of this device in a rabbit model at 15 fig and 30 fig/ device resulted in a therapeutically sustained level of daunomycin for up to 21 days after device implantation. Exhausted devices have to be removed surgically, which is an important limitation. 

Dexamethasone has been used either in the form of the free alcohol, or in one of the esterified forms in the treatment of conditions for which corticosteroid therapy is indicated. Its return to mineralocorticoid properties makes dexamethasone particularly suitable for treating conditions where water retention would be a disadvantage. 

Dexamethasone and betamethasone are isomeric fluorinated derivatives of methyl-prednisolone, but their solubilities are not identical, which might be a crystal property or a solution property. A simpler example of differences in isomeric solubility is that of the 0-, m-, and p-dihydroxybenzenes referred to above. A steric argument may be applied to the case of dexamethasone, water molecules being less able to move close to the 17-OH group than in the case of betamethasone. 

Dexacort dexamethasone. dexamethasone [ban, inn] (dexamethasone acetate, [usan] dexamethasone acefurate [inn] dexamethasone sodium phosphate [usan] dexamethasone pivalate dexamethasone phosphate dexamethasone metasulphobenzoate [ban] Dexacort Decadron Hexadrol Stiedex and many other names) is a potent CORTICOSTEROID, a GLUCOCORTICOID with ANTIINFLAMMATORY and ANTIALLERGIC properties. It is used topically to treat severe, non-infective inflammation of the skin caused by conditions such as eczema and psoriasis. It can be used systemically or orally for adrenocortical insufficiency, dexamethasone acefurate dexamethasone. dexamethasone acetate dexamethasone. dexamethasone phosphate dexamethasone. dexamethasone pivalate dexamethasone. dexamethasone metasulphobenzoate dexamethasone. 

The dominant path of distribution and elimination in the vitreous depends on a molecule s physicochemical properties and its substrate affinity. Lipophilic compounds, such as fluorescein (250) or dexamethasone (251), and compounds subject to active transport mechanisms, tend to be eliminated via the retina (Fig. 16). On the other hand, hydrophilic substances, such as fluorescein glucuronide, and compounds with poor retinal permeability, such as fluorescein dextran, tend to exit the vitreous anteriorly through the hyaloid membrane into the posterior chamber and subsequently into the anterior chamber, where they are subject to elimination pathways for aqueous humor (250). In general, shorter vitreal half-lives are associated with elimination through the retina, with its high surface area, whereas longer half-lives are indicative of elimination through the hyaloid membrane. 

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