Chinese name:
dexamethasone
English name:
dexamethasone
Definition:
Adrenal corticosteroids. It has anti-inflammatory, anti-allergic, anti-rheumatic and immunosuppressive effects, and is mainly used to treat serious bacterial infections and allergic diseases, various thrombocytopenic purpura, neutropenia, serious skin diseases, organ transplant immune rejection, tumor treatment and glucocorticoid-sensitive eye inflammation.
Applied disciplines:
Immunology (first-class discipline); Applied immunology (two disciplines); Immunotherapy (the third discipline)
The above contents have been approved and published by the National Committee for the Examination and Approval of Scientific and Technical Terminology, and are used to help edit encyclopedia business cards.
Dexamethasone, also known as normethasone and flumethylprednisolone, is an anti-inflammatory and anti-allergic drug. Mainly used as emergency medicine for critical diseases and treatment of various inflammations.
catalogue
Basic information
Brief introduction of drugs
history
pharmacological action
Laboratory determination method
drug interaction
indicate
Dosage and usage
counteraction
Source and prospect
Pay attention to use
Incompatibility (of drugs)
related data
preparation method
Basic information
Brief introduction of drugs
history
pharmacological action
Laboratory determination method
drug interaction
indicate
Dosage and usage
counteraction
Source and prospect
Pay attention to use
Incompatibility (of drugs)
related data
preparation method
launch
Edit this basic information Drug name: Dexamethasone English name: Dexamethasone Synonym: Dexamethasone; Flumethylprednisolone; Fluoromethyl dehydrohydrocortisone; Flumethasone; Medroxyprogesterone acetate, dexamethasone, atopalm, Delongni, dexamethasone, dexamethasone, methylprednisolone, etc. Chemical name: (1 1β, 16α)-9- fluoro-1,17,21-trihydroxy-/kloc-0. 007,923 (1 961to Lab.Franc.Chimiother), German patent1,13,690 (196/kloc-0). Co.), British patent 869,511(to Upjohn). Si Nuo. : 50-02-2 Molecular formula: C22H29FO5 Molecular weight: 392.5 Indications: prednisone. Edit this drug profile.
Dexamethasone (Figure 2)
Dexamethasone, also known as flumethasone, flumethylprednisolone and demisone, is a glucocorticoid. Its derivatives include hydrocortisone and prednisone. Its pharmacological effects are mainly anti-inflammatory, anti-toxic, anti-allergic and anti-rheumatism, and it is widely used in clinic. It is easily absorbed from the digestive tract, and its plasma T 1/2 is 190 minutes, and its tissue T 1/2 is 3 days. After intramuscular injection of dexamethasone sodium phosphate or dexamethasone acetate, the plasma concentration reached its peak at 1 hour and 8 hours respectively. The plasma protein binding rate of this product is lower than other corticosteroids. The anti-inflammatory activity of 0.75 mg of this product is equivalent to 5 mg of prednisolone. Edit this history: 1958, dexamethasone was synthesized by Arth and Oliveto respectively, and 1960 dexamethasone sodium phosphate was produced by Merck. Up to now, the number of dexamethasone derivatives on the market has exceeded 12.
Dexamethasone (Figure 3)
Dexamethasone (Figure 4)
The chemical structure of dexamethasone is that fluorine atom is introduced into the 9α position of prednisolone B ring and methyl group is introduced into the 16α position of D ring; 9α fluoride and 16α methyl significantly enhanced its anti-inflammatory activity, while 16α methyl significantly reduced the side effects of dexamethasone in water and sodium retention. The clinical bioequivalent dose ratio of dexamethasone to prednisolone is 0.75:5, and the biological half-life is 36-54 hours, which belongs to long-acting glucocorticoid. Dexamethasone, like other glucocorticoids, has pharmacological effects such as anti-inflammatory, anti-endotoxin, immunosuppression, anti-shock and stress response, so it is widely used in various departments to treat many diseases, such as autoimmune diseases, allergies, inflammation, asthma, dermatology and ophthalmology. Dexamethasone sodium phosphate injection is an indispensable first-aid medicine to save dying patients. In recent ten years, clinicians have used dexamethasone sodium phosphate to treat and prevent drug allergy caused by various Chinese and western medicines and to treat fever caused by viral cold, so that the clinical dosage of dexamethasone has increased year by year. So far, China has become the largest dexamethasone market in the world. The pharmacological action of this segment is stronger than that of prednisone in anti-inflammatory, anti-allergic and anti-toxic, and it has few side effects of water and sodium retention, so it can be injected by muscle or vein. Edit the laboratory determination method in this paragraph Method Name: Dexamethasone Bulk Drug-Dexamethasone-HPLC Scope of Application: This method uses HPLC to determine the content of Dexamethasone in Dexamethasone Bulk Drug. This method is suitable for dexamethasone bulk drug. Methods: The sample was dissolved in methanol, diluted with mobile phase and separated by HPLC. The peak area of dexamethasone was detected by ultraviolet absorption detector at 240nm wavelength, and its content was calculated. Reagent: 1. Acetonitrile 2. Methanol equipment: 1. Instrument 1. 1 HPLC 1.2 chromatographic column octadecylsilane bonded silica gel is used as filler, and the theoretical plate number should be not less than 3000 calculated by dexamethasone peak.
1.3 ultraviolet absorption detector 2. Chromatographic conditions 2. 1 mobile phase: acetonitrile water = 462.2 detection wavelength: 240nm 2.3 column temperature: room temperature sample preparation: 1. Preparation of control solution Accurately weigh about 15mg of dexamethasone control substance, put it in a 50mL volumetric flask, and add 2mL of methanol to dissolve it. 2. Preparation of test solution Accurately weigh about 15mg of test sample, put it in a 50mL volumetric flask, add 2mL of methanol to dissolve it, dilute it to scale with mobile phase, and shake it evenly to get the test solution. Note: "Accurate weighing" means that the weighing should be accurate to one thousandth of the weighing. "Precise measurement" means that the accuracy of measuring volume should meet the accuracy requirements of volume pipette in national standards. Operating steps: Accurately suck 10mL control solution and test solution respectively, inject them into high performance liquid chromatograph, measure the peak area of dexamethasone (C22H29FO5) at the wavelength of 240nm with ultraviolet absorption detector, and calculate its content. References: China Pharmacopoeia, edited by National Pharmacopoeia Committee, Chemical Industry Press, 2005, Part II, p. 184. Edit this paragraph about drug interaction.
Dexamethasone (Figure 5)
(1) Non-steroidal anti-inflammatory and analgesic drugs can strengthen the ulcer-causing effect of glucocorticoid. It can enhance the hepatotoxicity of acetaminophen. Amlumide can inhibit the function of adrenal cortex, accelerate the metabolism of dexamethasone and shorten its half-life by two times. When combined with amphotericin B or carbonic anhydrase inhibitor, hypokalemia can be aggravated, and the changes of blood potassium and cardiac function should be paid attention to. Long-term use with carbonic anhydrase inhibitors is prone to hypocalcemia and osteoporosis. (2) Combined with anabolic steroids can increase the incidence of edema and aggravate acne. Combined with antacid, it can reduce the absorption of prednisone or dexamethasone. Long-term use of anticholinergic drugs (such as atropine) will increase intraocular pressure. Tricyclic antidepressants can aggravate the mental symptoms caused by glucocorticoid. (3) When combined with hypoglycemic drugs such as insulin, the dosage of hypoglycemic drugs should be adjusted appropriately because it can increase the blood sugar of diabetic patients. Thyroid hormone can increase the metabolic clearance rate of glucocorticoid, so when thyroid hormone or antithyroid drugs are combined with glucocorticoid, the dose of the latter should be adjusted appropriately. Combined with contraceptives or estrogen preparations; It can strengthen the curative effect and adverse reaction of glucocorticoid. Combined with cardiac glycoside, digitalis toxicity and arrhythmia can be increased. Combined with potassium-expelling diuretics, it can cause severe hypokalemia and weaken sodium-expelling diuretic effect due to water and sodium retention.
Dexamethasone (Figure 6)
(4) Combined with ephedrine, the metabolic clearance of glucocorticoid can be enhanced. Combined with immunosuppressants, it can increase the risk of infection and may induce lymphoma or other lymphoproliferative diseases. Glucocorticoids, especially prednisolone, can increase the metabolism and excretion of isoniazid in the liver, and reduce the blood concentration and curative effect of isoniazid. (5) Glucocorticoid can promote the metabolism of mexiletine in vivo and reduce the blood drug concentration. Combined with salicylate, the concentration of salicylate in plasma can be reduced. Combined with growth hormone, it can inhibit the growth-promoting effect of the latter. Edit this instruction
A glucocorticoid
Indications are the same as those of prednisolone. This product can also be used to prevent neonatal respiratory distress syndrome, reduce intracranial pressure and diagnose and differentiate Cushing's syndrome. Indications of prednisolone: adrenocortical drugs. Mainly used for allergic and inflammatory diseases. Because the sodium retention effect of this product is weak, it is generally not used as an alternative treatment for adrenal cortical hypofunction. Dexamethasone acetate and dexamethasone sodium phosphate can also be used for intramuscular injection or injection into injured parts such as joint cavity and soft tissue. The product is easily absorbed from digestive tract. The plasma T 1/2 was 190 minutes, and the tissue T 1/2 was 3 days. After intramuscular injection of dexamethasone sodium phosphate or dexamethasone acetate, the plasma concentration reached its peak at 1 hour and 8 hours respectively. The plasma protein binding rate of this product is lower than other corticosteroids. The anti-inflammatory activity of 0.75 mg of this product is equivalent to 5 mg of prednisolone. Edit the dosage and usage of tablets in this paragraph: 0.75mg/ tablet. Start with 0.75~3mg/ time, 2~4 times/day, maintain 0.5 ~ 0.75 mg/d, dexamethasone injection 2.5mg/ 1ml, 5mg/ml. 5~ 10mg/ time, 1~2 times/day. Intramuscular injection or intravenous drip of 500 ml of 5% glucose solution. Ointment: 0.05% orally: 0.75 ~ 6mg 1 day, divided into 2 ~ 4 times. The maintenance dose was 0.5 ~ 0.75 mg for 65438 0 days. Intramuscular injection (dexamethasone acetate injection), 1 time 8 ~ 16 mg, 1 time interval 2-3 weeks. Intravenous drip (dexamethasone sodium phosphate injection), 2 ~ 20 mg each time, or as directed by the doctor. Anti-inflammatory and anti-allergic, 65438+ 0.5 ~ 3 mg per day, once in the morning or twice in the afternoon. Mainly used as emergency medicine for critical diseases, treating various inflammations and allergic reactions. The anti-inflammatory, anti-allergic and anti-toxic effects are stronger than those of prednisone, and the side effects of water and sodium retention are less, which can be intramuscular injection or intravenous drip. Intramuscular injection (dexamethasone acetate injection): 8- 16mg once every 2-3 weeks. Intravenous drip (dexamethasone sodium phosphate injection), 2-20mg each time, or as directed by the doctor. Reference of time pharmacology medication method: Long-term medication should simulate the law of natural hormone secretion. Take 3/4 or the whole dose at 7 am. Dexamethasone tablet 0.75mg, dexamethasone sodium phosphate injection (1)1ml: 2mg (2)1ml: 5mg. Dexamethasone ointment or cream 0.05 ~ 0. 1%. Oral administration, 0.75-6mg per day, divided into 2-4 times, with a maintenance amount of 0.5-0.75mg per day at 1 to make up the whole amount. Do not use medicine after 1 point. Edit this adverse reaction
urticaria
Glucocorticoids, such as dexamethasone, have no obvious adverse reactions in the application of physiological dose replacement therapy, and most of the adverse reactions occur in the application of pharmacological dose, which is closely related to the course of treatment, dose, drug type, usage and route of administration. The common adverse reactions are as follows: 1. Long-term use can cause the following side effects: face and posture, weight gain, edema of lower limbs, purple stripes, bleeding tendency, poor wound healing, acne, menstrual disorder, ischemic failure of humerus or femoral head, osteoporosis and fractures (including vertebral compression fractures and pathological fractures of long bones), muscle weakness, muscular atrophy and hypokalemia. 2. Patients may have mental symptoms: euphoria, excitement, delirium, anxiety, disorientation or inhibition. Mental symptoms include people who are prone to chronic wasting diseases and people who have mental disorders in the past. 3. Infection is the main adverse reaction of adrenocortical hormone. Mainly fungi, tuberculosis, staphylococcus, Proteus, Pseudomonas aeruginosa and various herpes viruses. 4. Glucocorticoid withdrawal syndrome. Sometimes patients have dizziness, fainting tendency, abdominal pain or backache, low fever, loss of appetite, nausea, vomiting, muscle or joint pain, headache, fatigue and weakness after stopping taking the drug. If careful examination can rule out adrenal hypofunction and recurrence of primary disease, it can be considered as glucocorticoid dependence syndrome. Disorder of substance metabolism and water and salt metabolism Long-term and large-scale application of glucocorticoids can cause disorder of substance metabolism and water and salt metabolism, resulting in adrenocortical syndrome, such as edema, hypokalemia, hypertension, diabetes, skin thinning, full moon face, buffalo back, centripetal obesity, hirsutism, acne, myasthenia gravis, muscular atrophy, etc., which generally do not need special treatment and can subside automatically after stopping taking drugs. But the recovery of myasthenia is slow and incomplete. Measures such as low salt, low sugar and high protein diet and adding potassium chloride can alleviate these symptoms. In addition, glucocorticoid can delay the wound healing of trauma patients by inhibiting the synthesis of protein. In children, it can lead to negative nitrogen balance by inhibiting the secretion of growth hormone, thus affecting growth and development. Glucocorticoid can inhibit the immune function of the body and has no antibacterial effect, so long-term application can often induce or aggravate the infection, which can spread the potential infection focus in the body or rekindle the static infection focus, especially for patients with decreased original resistance, such as nephrotic syndrome, tuberculosis, aplastic anemia and so on. Because patients often feel good about themselves when taking glucocorticoids, it masks the symptoms of infection development. Therefore, before deciding to take long-term treatment, they should check their bodies to eliminate potential infection, be vigilant in the application process, use effective antibacterial drugs when necessary, and pay special attention to the prevention and treatment of potential tuberculosis lesions. Glucocorticoid is a complication of digestive system, which can stimulate the secretion of gastric acid and pepsin, inhibit the secretion of gastric mucus and reduce the resistance of gastric mucosa, so it can induce or aggravate peptic ulcer. Glucocorticoid can also cover up the initial symptoms of ulcer, leading to serious complications such as sudden bleeding and perforation, which should be paid attention to. Long-term use will aggravate gastric or duodenal ulcer. This side effect is more likely to occur when combined with other drugs with gastric irritation (such as aspirin, indomethacin and butazolamide). A few patients can induce pancreatitis or fatty liver. Long-term use of glucocorticoids to treat cardiovascular complications can lead to sodium and water retention and elevated blood lipids, which can induce hypertension and atherosclerosis. Osteoporosis and vertebral compression fracture Osteoporosis and vertebral compression fracture are serious complications of glucocorticoid treatment for patients of all ages. Ribs and vertebrae have high beam-column structures and are usually the most seriously affected. This may be related to glucocorticoid inhibiting osteoblast activity, increasing calcium and phosphorus excretion, inhibiting intestinal calcium absorption and increasing the sensitivity of bone cells to parathyroid hormone. If osteoporosis occurs, the drug must be stopped. D (To prevent and treat osteoporosis, vitamin D, calcium salt and anabolic steroids from protein should be supplemented. Edit the source and prospect of this paragraph. The chemical structure of dexamethasone is that fluorine atom is introduced into the 9α position of prednisolone B ring and methyl group is introduced into the 16α position of D ring; 9α fluoride and 16α methyl significantly enhanced its anti-inflammatory activity, while 16α methyl significantly reduced the side effects of dexamethasone in water and sodium retention. The clinical bioequivalent dose ratio of dexamethasone to prednisolone is 0.75:5, and the biological half-life is 36-54 hours, which belongs to long-acting glucocorticoid. Dexamethasone, like other glucocorticoids, has pharmacological effects such as anti-inflammatory, anti-endotoxin, immunosuppression, anti-shock and stress response, so it is widely used in various departments to treat many diseases, such as autoimmune diseases, allergies, inflammation, asthma, dermatology and ophthalmology. Dexamethasone sodium phosphate injection is an indispensable first-aid medicine to save dying patients. In recent ten years, clinicians have used dexamethasone sodium phosphate to treat and prevent drug allergy caused by various Chinese and western medicines and to treat fever caused by viral cold, so that the clinical dosage of dexamethasone has increased year by year. So far, China has become the largest dexamethasone market in the world. When editing this paragraph, pay attention to taking it in large quantities, which may easily lead to diabetes and Cushing's syndrome. Long-term use is more likely to cause mental symptoms and psychosis. If you have a memory and a history of mental illness, it is best not to use it. Patients with ulcer, thrombophlebitis, active pulmonary tuberculosis and intestinal anastomosis should not use it or use it with caution. For other precautions, please refer to the "Application Precautions" of this kind of drugs. Specification: 1. Demisone acetate tablets: 0.75 mg per tablet. Dexamethasone sodium phosphate injection: 1mg( 1ml), 2mg( 1ml) and 5mg( 1ml) respectively. Glucocorticoid dexamethasone, commonly known as "skin opium", is a banned ingredient in cosmetics. When consumers use cosmetics containing dexamethasone, their skin will feel obviously better at first, but long-term use will not only lead to dependence, but also lead to dermatitis and even various diseases. Compatibility contraindications of dexamethasone with calcium chloride, sulfadiazine sodium, tetracycline hydrochloride, oxytetracycline hydrochloride, diphenhydramine, chlorpromazine, promethazine, phenylethylamine, procaine hydrochloride and scopolamine hydrobromide. It is easy to cause turbidity or precipitation, making the drug ineffective; Combined with furosemide and sodium salicylate can increase its toxicity. Edit the relevant data of MDLNo in this paragraph. :MFCD00064 136 EINECSNo。 : 200-003-9 rtec number: TU3980000 BRNNo:206665 1 publication number: 24893536 molar refractive index: 100.23 molar volume (m3/ Mol): 296.2 isotonic specific volume (90.2k): 8. A new production process of dexamethasone 2 1- hydroxy compound was adopted. Semi-soluble substrate with appropriate amount of methanol containing 0 ~ 10% chloroform as solvent, hydrolysis reaction with alkali as catalyst, neutralization with acetic acid after the reaction, decompression concentration of reaction solution to appropriate volume, cooling, filtering, washing filter cake with water and drying to obtain 2 1- hydroxy compound. This process can shorten the production cycle, improve the quality and yield of 2 1- hydroxy compound, and reduce the impurity content in 2 1- hydroxy compound.