Dexamethasone Usage And Synthesis |
Introduction |
Dexamethasone is one of the commonly used drugs in clinical practice. It is often used in combination with other drugs in clinical practice.
It has anti-inflammatory, anti-toxic and anti-allergic effects. However, it has no therapeutic effect on the disease and
can only reduce or inhibit the manifestation of inflammation.Therefore, it must be noted when using it clinically. Generally,
it is not used alone and must be used in combination with other drugs to play a better role. |
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This product has more significant anti-inflammatory and skin allergy control effects than prednisone,
but has a milder effect on water and sodium retention and potassium excretion, and a stronger inhibitory effect on the pituitary-adrenal cortex axis.
After intramuscular injection of dexamethasone sodium phosphate or dexamethasone acetate,
the blood concentration reaches its peak in 1 hour or 8 hours, respectively. |
Uses |
Dexamethasone (dexamethasone sodium phosphate EP impurity A) is a glucocorticoid used as an anti-inflammatory agent.
Dexamethasone regulates the survival, growth, and differentiation of T cells. Dexamethasone inhibits the induction of nitric oxide synthase. |
Pharmacological effects |
Dexamethasone (DSMS), also known as flumethasone, flumethasone, and dexamethasone, is a synthetic adrenal cortical hormone.
It is a glucocorticoid anti-inflammatory and anti-allergic drug. Its pharmacological effects are mainly anti-inflammatory, anti-toxic, anti-allergic,
and anti-rheumatic, and it is widely used clinically. In recent years, the European Union believes that eating beef containing hormones such as estrenediol,
progesterone, and medroxyprogesterone can disrupt the normal functions of the human endocrine system, growth and development, immune system, and reproductive system,
and may also cause cancer and teratogenesis, and therefore prohibits the use of such hormones in animals. In addition, dexamethasone is also used as an animal
growth regulator to promote animal protein synthesis and metabolism and increase meat production. It was once widely used as livestock and poultry. However, long-term laboratory
studies have found that dexamethasone can cause cancer and gene mutations in experimental animals. Dexamethasone and its residues have obvious toxic side effects on humans and livestock.
The use of high doses of dexamethasone can lead to side effects such as muscle atrophy and growth inhibition. It can be inferred that long-term use of such drugs by humans or long-term consumption of livestock and poultry to which such growth promoters are added can also lead to cancer and gene mutation. Therefore, such drugs are prohibited from use in treatment and feed. |
Side effects |
Dexamethasone is a synthetic adrenal cortex hormone, which belongs to the long-acting glucocorticoid class. Glucocorticoids can promote the metabolism of three major nutrients and inhibit protein synthesis. Long-term external use can lead to more serious consequences, but the adverse reactions are much smaller than oral medications. Common systemic glucocorticoid side effects include:
Stomach discomfort, increased sensitivity to gastric ulcers.
Increase appetite, leading to significant weight gain.
Potential diabetic patients: Glucose intolerance is aggravated by the patient's original diabetes.
Psychosis, including personality changes, irritability, excitement, and mania.
Long-term treatment of osteoporosis: pathological fractures (such as hip joints). Elevated liver enzymes, fatty liver Wilson's nucleus degeneration (usually reversible).
Long-term high-dose medication for patients with nephrotic syndrome is prone to cause major side effects such as gastrointestinal ulcers and aseptic necrosis of the femoral head.
It is better to use prednisone acetate tablets to treat nephrotic syndrome.
Dexamethasone can be used to treat high-altitude cerebral edema and pulmonary edema.
People use it to relieve altitude sickness during mountaineering expeditions.
Used in combination with marbofloxacin, clotrimazole, etc. to treat ear infections or allergies in dogs or birds, etc. |
Drug interactions |
(1) Oral antacids can reduce the gastrointestinal absorption of dexamethasone.
(2) Aminoglutethimide can inhibit adrenal cortical function, accelerate the metabolism of this drug, and shorten its half-life. Patients using aminoglutethimide can use hydrocortisone if they need to use glucocorticoids in combination.
(3) Dexamethasone can weaken the effects of oral hypoglycemic drugs, anticoagulants, and neuromuscular blockers, and the dose should be adjusted.
(4) Barbiturates, phenytoin, and rifampicin can weaken the metabolic effect of dexamethasone. (5) Dexamethasone can increase the toxicity of salicylic acid.
(6) Dexamethasone antagonizes the effects of vitamin A and should be avoided in combination. |
Uses |
Mainly used for anti-inflammatory and anti-allergic effects, suitable for rheumatoid arthritis and other collagen diseases. |
Production method |
A new production process of dexamethasone 21-hydroxy, using the intermediate 21-acetate as a substrate,
using an appropriate amount of methanol containing 0-10% chloroform as a solvent to semi-dissolve the substrate, using an alkali as a catalyst for hydrolysis reaction,
neutralizing with acetic acid after the reaction is complete, decompressing and concentrating the reaction solution to an appropriate volume, cooling, filtering,
washing the filter cake with water, and drying to obtain 21-hydroxy. This process can shorten the production cycle, improve the quality and yield of 21-hydroxy,
and reduce the content of impurities in 21-hydroxy. |
