dexamethasone

[dì sāi mǐ sōng]
drugs
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Dexamethasone (DXMS for short) was first synthesized in 1957 and listed in the WHO standard list of essential drugs. It is one of the essential drugs in the basic public health system.
On June 16, 2020, WHO said that the preliminary clinical trial results in the UK showed that dexamethasone could save the lives of severe patients with COVID-19, reduce the death rate of patients using respirators by about one third, and reduce the death rate of patients only taking oxygen by about one fifth. [1]
Chinese name
dexamethasone
Foreign name
dexamethasone [4]
chemical formula
C twenty-two H twenty-nine FO five
molecular weight
three hundred and ninety-two point four six one
CAS login number
50-02-2
Melting point
255 to 264 ℃
Boiling point
568.2 ℃
Water solubility
soluble
Density
1.32 g/cm³
Appearance
White crystalline powder
Flash point
297.5 ℃
Security description
S45
Hazard symbol
Xn
Hazard description
R40

A brief history of research

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In 1958, Arth and Oliveto synthesized dexamethasone respectively. In 1960, Merck&Co. produced dexamethasone sodium phosphate, and more than 12 kinds of dexamethasone derivatives were listed.
The chemical structure of dexamethasone is that the fluorine atom is introduced into the B-ring 9 α position of prednisolone, and the methyl atom is introduced into the D-ring 16 α position; 9 α - fluoride and 16 α - methyl significantly enhanced its anti-inflammatory activity, while 16 α - methyl significantly reduced the side effects of dexamethasone on 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 is listed as long-term glucocorticoid.
Like other glucocorticoids, dexamethasone has anti-inflammatory, anti endotoxin, immunosuppressive, anti shock, stress enhancing and other pharmacological effects, so it is widely used in various departments to treat a variety of diseases, such as autoimmune diseases, allergies, inflammation, asthma, dermatological and ophthalmic diseases. Dexamethasone sodium phosphate injection is an indispensable emergency medicine for rescuing critically ill patients. In recent decades, clinicians have used dexamethasone sodium phosphate to treat and prevent drug allergies caused by various Chinese and western medicines, and to treat fever caused by viral colds. As a result, the clinical use of dexamethasone has increased year by year, and China has become the largest market for dexamethasone in the world.

Compound Introduction

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essential information

Chemical formula: C twenty-two H twenty-nine FO five
Molecular weight: 392.461
CAS No.: 50-02-2
MDL No.: MFCD00064136
EINECS No.: 200-003-9
RTECS No.: TU3980000
BRN No.: 2066651

Physical and chemical properties

Density: 1.32g/cm three
Melting point: 255~264 º C
Boiling point: 568.2 ℃
Flash point: 297.5 ℃
Appearance: white crystalline powder
Solubility: soluble in water [2]

Molecular structure data

Molar refractive index: 100.23
Molar volume (cm three /mol):296.2
Isotonic specific volume (90.2K): 812.3
Surface tension (dyne/cm): 56.5
Polarization (10 -24 cm three ):39.73 [2]

Pharmacopoeia information

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essential information

16 for this product α -Methyl-11 β ,17 α , 21-trihydroxy-9 α -Flupregnastero-1,4-diene-3,20-dione, calculated as dry product, containing C twenty-two H twenty-nine FO five It should be 97.0%~102.0%.

character

This product is white or almost white crystalline powder, odorless.
This product is slightly soluble in methanol, ethanol, acetone or dioxane, slightly soluble in chloroform, extremely slightly soluble in ether, and almost insoluble in water.
Specific curl
Take this product, weigh it precisely, add dioxane to dissolve it and dilute it quantitatively to make a solution containing about 10mg per 1mL. Determine according to the law (general rule 0621), and the specific rotation is+72 ° to+80 °.
absorption coefficient
Take this product, weigh it precisely, add ethanol to dissolve it and dilute it quantitatively to make a solution containing about 10 μ g per 1mL, and measure the absorbance and absorption coefficient at a wavelength of 240nm according to the ultraviolet visible spectrophotometry (general rule 0401)( E 1% 1cm )380~410.

identify

1. Take about 2mg of this product, add 2mL of sulfuric acid, shake to dissolve it, and it will appear reddish brown within 5 minutes. Add 10mL of water and mix well, and the color will disappear.
2. In the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
3. The infrared absorption spectrum of this product should be consistent with the control spectrum (spectrum set 741 figure).
4. This product shows the identification reaction of organic fluoride (general rule 0301).

inspect

Related substances
Determine according to the method of high performance liquid chromatography (general rule 0512).
Test solution: Take an appropriate amount of this product, weigh it accurately, add methanol to dissolve it and dilute it quantitatively to make a solution containing about 0.5mg per 1mL.
Control solution: Take an appropriate amount of betamethasone control sample, precisely weigh it, add methanol to dissolve it and quantitatively dilute it to make a solution containing about 0.5mg per 1mL, precisely measure 1mL, place it in a 100mL measuring flask, precisely add 1mL of test solution, dilute it with methanol to the scale, and shake it evenly.
Chromatographic conditions: octadecyl silane bonded silica gel is used as filler, acetonitrile water (28:72) is used as mobile phase, detection wavelength is 240nm, and injection volume is 20 µ L.
System applicability requirements: In the chromatogram of reference solution, the peak sequence is betamethasone peak and dexamethasone peak, and the resolution between the two peaks should meet the requirements.
Determination method: Precisely measure the test solution and the reference solution, respectively inject them into the liquid chromatograph, and record the retention time of the chromatogram to the main component peak 2.5 times.
Limit: In the chromatogram of the test solution, if there is a chromatographic peak with the same retention time as betamethasone, the peak area shall not exceed 0.5% according to the external standard method. The peak area of other single impurities shall not be greater than the peak area of dexamethasone in the reference solution (1.0%), and the sum of the peak areas of other impurities shall not be greater than 1.5 times (1.5%) of the peak area of dexamethasone in the reference solution, The peaks smaller than 0.01 times of the peak area of dexamethasone in the control solution are ignored.
Loss on drying
Take the product and dry it at 105 ℃ for 3 hours. The weight loss shall not exceed 0.5% (general rule 0831).
Ignition residue
It shall not exceed 0.2% (general rule 0841).

Assay

Determine according to the method of high performance liquid chromatography (general rule 0512).
Test solution
Take an appropriate amount of this product, weigh it precisely, add methanol to dissolve it and dilute it quantitatively to prepare a solution containing about 50 µ g per 1mL.
Reference solution
Take an appropriate amount of dexamethasone reference substance, weigh it precisely, add methanol to dissolve it and dilute it quantitatively to prepare a solution containing about 50 µ g per 1mL.
System suitability solution
See reference solution under related substances.
Chromatographic conditions
See related substances.
System suitability requirements
In the chromatogram of system suitability solution, the peak sequence is betamethasone peak and dexamethasone peak, and the resolution between the two peaks should meet the requirements.
Assay
Accurately measure the test solution and the reference solution, respectively inject them into the liquid chromatograph, and record the chromatogram. Calculate by peak area according to external standard method.

category

Adrenocortical hormone drugs.

Storage

Shading, sealed storage.

preparation

Dexamethasone Tablets. [3]

Brief Introduction to Drugs

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pharmacological action

Dexamethasone, also known as dexamethasone, fluoromethylprednisolone and dexamethasone, is a glucocorticoid hormone. Its derivatives include hydrocortisone, prednisone, etc. Its pharmacological effects are mainly anti-inflammatory, antitoxic, anti allergic, and anti rheumatic. It is widely used in clinic. It is easily absorbed from the digestive tract, and its plasma t 1/2 For 190 minutes, organize t 1/2 On the 3rd day, the peak plasma concentration of dexamethasone sodium phosphate or dexamethasone acetate was reached at 1 hour and 8 hours respectively after intramuscular injection. The plasma protein binding rate of this product is lower than that of other corticosteroids, and the anti-inflammatory activity of 0.75mg of this product is equivalent to 5mg of prednisolone. Adrenocortical hormone drugs have stronger anti-inflammatory, antiallergic and antitoxic effects than prednisone. The retention of water and sodium and the promotion of potassium excretion are very light. They can be intramuscularly injected or intravenous drip with stronger inhibitory effects on pituitary adrenal gland.
1. Anti inflammatory effect: it can reduce and prevent the reaction of tissues to inflammation, thus reducing the expression of inflammation. Hormones inhibit the aggregation of inflammatory cells, including macrophages and leukocytes, at inflammatory sites, and inhibit phagocytosis, the release of lysosomal enzymes, and the synthesis and release of inflammatory chemical mediators.
2. Immunosuppressive effect: including preventing or inhibiting cell-mediated immune reaction, delayed allergic reaction, reducing the number of T lymphocytes, monocytes, eosinophils, reducing the binding capacity of immunoglobulin and cell surface receptors, and inhibiting the synthesis and release of interleukin, thus reducing the transformation of T lymphocytes to lymphoblasts, And reduce the expansion of primary immune response. It can reduce the immune complex passing through the basement membrane, and reduce the concentration of complement components and immunoglobulin.
This product is easily absorbed from the digestive tract, and its plasma t 1/2 For 190 minutes, organize t 1/2 On the 3rd day, the peak plasma concentration of dexamethasone sodium phosphate or dexamethasone acetate was reached at 1 hour and 8 hours respectively after intramuscular injection. The plasma protein binding rate of this product is lower than that of other corticosteroids. The anti-inflammatory activity of 0.75mg of this product is equivalent to 5mg of prednisolone.

Pharmacokinetics

Dexamethasone is easy to be absorbed from the digestive tract, and can also be absorbed through the skin. After intramuscular injection of dexamethasone sodium phosphate or dexamethasone acetate, the peak blood concentration reached 1h and 8h respectively. The binding rate of plasma protein is lower than that of other corticosteroids, about 77%, which is easy to penetrate the placenta and almost not inactivated. The biological half-life of dexamethasone is about 190 min, and the tissue half-life is about 3 days. More than 65% of the drugs are discharged from the urine within 24 hours, mainly as inactive metabolites.

indication

1. Excitable Adenylate cyclase , suppression phosphodiesterase , increase the level of cAMP, so as to improve the Adrenomime And theophylline sensitivity, indirectly play the role of bronchospasm. It can also play an anti-inflammatory and anti allergic role. To alleviate Bronchospasm Reduce bronchial congestion and edema, and reduce mucus secretion.
2. It is used to treat allergic diseases, such as allergic dermatitis, drug dermatitis (drug eruption), seropathy, rhinitis Drug reaction , urticaria allergic purpura Etc.
3. Shock: it can be used for septic shock Anaphylactic shock and acute myocardial infarction Or myocardial block Cardiogenic shock Adjuvant treatment.
4. Toxic disease: it can alleviate the toxic symptoms caused by bacterial and viral infections, and has a good antipyretic effect.
5、 Ulcerative colitis : It can be used together with Xileisan as retention enema to relieve symptoms.
6. Assist in the diagnosis of hypercortisolism: Dexamethasone inhibition test It is helpful for the diagnosis of this disease.
7. Treatment of intractable hemoptysis: 10~20mg every day, add 1000mL liquid into the intravenous drip, and generally 6~8h. In case of emergency, 10mg intravenous injection can be used. After 2-3 days of intravenous drip, the drug can be stopped or maintained orally depending on the condition to consolidate the curative effect. If the patient does not stop bleeding after 7 days of medication, stop the medication and use other methods to stop bleeding.
8. Treat acute Chemical pulmonary edema : It is advisable to use dexamethasone 10~20mg plus 20mL glucose injection intravenously once or twice a day.
9. Various Inflammatory disease Such as localized enteritis Tuberculous meningitis Uveitis thyroiditis , tuberculosis Trichinosis Allergic otitis externa, infectious otitis externa, etc.
10、 Seborrheic dermatitis lichen planus Neurodermatitis , pemphigus, psoriasis, Stevens Johnson syndrome Cicatricial alopecia , bullous dermatitis, acne and other skin diseases.
11. Eye inflammation caused by various reasons, including keratitis, scleritis, iritis, herpetic ophthalmia Sympathetic ophthalmia Intraocular inflammation after cataract extraction and intraocular lens implantation, glaucoma surgery, corneal transplantation surgery, myopia treatment surgery, etc.
12. Rheumatoid arthritis, gouty arthritis Ankylosing spondylitis , epicondylitis, bursitis, osteoarthritis, tenosynovitis, psoriatic arthritis Systemic lupus erythematosus , lupus nephritis Nephrotic syndrome , adult Still disease, sarcoidosis Hypercalcemia And other diseases.
14. Accompanying Intracranial hypertension Brain edema, etc.
16、 Cushing syndrome The diagnosis and differential diagnosis of etiology.
17、 Aspiration pneumonia LOEFFLER syndrome, beryllium poisoning, steroid 21 hydroxylase deficiency, etc.

contraindication

1. Yes adrenaline Patients with allergy to corticosteroids.
2. A history of serious mental illness.
3. Active stomach duodenal ulcer
4. After recent gastrointestinal anastomosis.
5. Severe osteoporosis.
6. Obvious diabetes.
7. Severe hypertension.
8. Viral, bacterial and fungal infections that cannot be controlled by antibiotics.
9. Systemic fungal infection.
10. Eye preparations are prohibited Corneal ulcer Herpes simplex keratitis, varicella and other viral diseases of cornea and conjunctiva, fungal infection of eye tissue, mycobacterial infection of eye, glaucoma or family history of glaucoma, and perforation of eardrum.
11. Thrombophlebitis.

matters needing attention

1. (1) Acute heart failure or other heart diseases; (2) Diabetes mellitus; (3) Diverticulitis; (4) Emotional instability and psychotic tendency; (5) Liver function damage; (6) Hyperlipoproteinemia; (7) Hypertension; (8) Hypothyroidism (the effect of glucocorticoid is enhanced at this time); (9) Myasthenia gravis; (10) Osteoporosis; (11) Gastric ulcer, gastritis or esophagitis; (12) Renal function damage or stones; (13) Tuberculosis.
2. Effects of drugs on children: Dexamethasone is a long-acting preparation, generally not used for children who need long-term hormone use.
3. Intravenous administration is often used for the treatment of critical diseases, such as severe shock; Inhalation of dexamethasone is prohibited for asthmatic status and sputum culture with positive candida albicans.
4. Eye infectious inflammation should be used in combination with effective antibiotics. After the condition improves, the number of drug points should be gradually reduced, without sudden stop, to reduce the risk of disease recurrence.
5. The tin foil bag of dexamethasone sustained-release particles contains a rotating drug dispenser, which contains one sustained-release particle. The internal and external packaging can only be opened in the sterile operating room before use.
6. Because the effect of dexamethasone sodium retention is weak, it is generally not used as adrenal cortex Replacement therapy for hypofunction.
7. Dexamethasone sodium phosphate has high permeability, long action time and the same pharmacodynamics as dexamethasone, but it is easily soluble in water and can be made into water-soluble preparations, so it expands the route of administration and scope of application.
8. Prolonged and massive use may lead to increased cortisol, and blood sugar, blood pressure and presence of cortisol must be observed Mental symptoms
9. Taking dexamethasone for a long time can make tuberculosis activity and perforated peptic ulcer Bleeding. Not used after intestinal anastomosis.
10. Effects of drugs on children: Dexamethasone is a long-acting preparation, generally not used for children who need long-term hormone use.
11. Refer to relevant contents of hydrocortisone for other precautions.

Usage and dosage

Overview: room temperature storage. Avoid eye and other objects contacting the bottle mouth to contaminate the liquid medicine. If the medicine solution contains the preservative benzalkonium chloride, the wearer of soft corneal contact lens shall take off the contact lens before medication, and wear the contact lens 15 minutes after medication. As for other eye drops, the interval between two drops shall be more than 5 minutes. It is not allowed to prolong the medication time and change the medication frequency without authorization, so as to avoid irreversible eye complications. [7 ]
1. Adult
(1) Oral administration
0.75~3mg each time, 2~4 times a day; The maintenance amount is about 0.75mg, depending on the condition.
(2) Intravenous injection
① Treatment of critical state of disease, such as severe shock: Dexamethasone sodium phosphate, 2~20mg each time, repeated administration for 2~6h until the condition is stable, but continuous administration of large doses generally does not exceed 72h.
② Alleviation of brain edema caused by malignant tumor: 10mg of the first dose was injected intravenously, and then 4mg was injected intramuscularly every 6 hours. Generally, patients can get better after 12 to 24 hours. The dose gradually decreased after 2 to 4 days, and the drug was stopped after 5 to 7 days.
③ Brain tumor unsuitable for surgery: 50mg of the first dose is given intravenously, 8mg is given repeatedly every 2h, and then gradually reduced to 2mg every day after several days, which is given intravenously for 2-3 times.
(3) Intramuscular injection
① General usage and dosage: use dexamethasone acetate injection, 5~15mg each time according to the condition, and inject once every 2~3 weeks.
② It is used to alleviate brain edema caused by malignant tumor: see intravenous injection.
③ Intensive treatment or for allergic disease and shock: 2~6mg each time; For severe cases, the drug can be given repeatedly every 2-6 hours.
④ Brain coma caused by brain edema caused by falciparum malaria: 3-10mg each time, once every 8 hours.
(4) Intraarticular injection
0.8-4mg each time, depending on the size of the joint cavity. Intrathecal injection: 5-10mg each time, once every 1-3 weeks.
(5) Inhalation
For allergic rhinitis, spray and inhale 1.7%~2.3% aerosol 2~4 times a day.
(6) Transocular administration
① Eye drops: 0.001% concentration can be used for external eye inflammation, 4-5 times a day; After internal eye inflammation and surgery, the drug concentration can be increased to 0.1%, 4-5 times a day.
② Implantation of particles: after ophthalmic surgery and removal of viscoelastic substances, use precision toothless tweezers to remove one dexamethasone sustained-release particle from the package and place it in the anterior chamber or the posterior chamber. If it is placed in the anterior chamber, the drug particle should be placed at 12 o'clock on the iris base; If it is placed in the posterior chamber, it should be placed at 6 points between the iris and the anterior surface of the intraocular lens, and then the incision should be closed in a conventional manner.
③ Intravitreous injection: 0.4 mg each time.
(7) Local administration: Rub the affected part with 0.05%~0.1% cream 2-3 times a day.
2. Children
(1) Oral administration
General usage and dosage: 0.03-0.15mg/kg or 1-5mg/kg every day, once every 6-12 hours. Steroid 21 hydroxylase deficiency: the initial dose is 0.25~0.28mg/mg, which should be taken in the morning. After effective treatment, the maintenance dose should be adjusted according to the situation.
(2) Intramuscular injection
① Treatment of brain edema: the load dose is 1.5 mg/kg, followed by 1.5 mg/kg per day, once every 4-6 hours, a total of 5 days. The dosage shall be reduced and stopped on the second 5 days;
② Acute asthma attack: children aged 6-12 months: 16mg, once; Children aged 13-35 months: 24mg, once; Children older than 36 months: use 36 mg once.
(3) Intravenous injection: Treatment of brain edema: see intramuscular injection.

Adverse reactions

There is no obvious adverse reaction of dexamethasone and other glucocorticoids in the application of physiological dose replacement therapy. The adverse reactions mostly occur in the application of pharmacological dose, and are closely related to the course of treatment, dose, drug type, usage and route of administration. Common adverse reactions are as follows:
1. Long term use can cause the following side effects: iatrogenic Cushing's syndrome, facial appearance and posture, weight gain, edema of lower limbs, purple lines, bleeding tendency, poor wound healing, acne, menstrual disorder, ischemic necrosis of the humerus or femoral head, osteoporosis and fractures (including vertebral compression fractures, pathological fractures of long bones), muscle weakness, muscular atrophy, hypokalemia syndrome Gastrointestinal tract irritation (nausea and vomiting), pancreatitis, peptic ulcer or perforation, growth inhibition of children, glaucoma, cataract, benign intracranial hypertension syndrome, impaired glucose tolerance and increased diabetes.
2. Patients may have mental symptoms: euphoria, excitement, delirium, restlessness, disorientation, or depression. Mental symptoms include those who are prone to chronic consumptive diseases and those who have had mental disorders in the past.
3. Complicated infection is the main adverse reaction of adrenocortical hormone. Fungus, tubercle bacillus, staphylococcus, proteus, pseudomonas aeruginosa and various herpesviruses are the main pathogens.
4. Glucocorticoid withdrawal syndrome. Sometimes the patient has dizziness, fainting tendency, abdominal or back pain, low fever, anorexia, nausea, vomiting, muscle or joint pain, headache, fatigue, weakness after stopping the drug. If careful examination can exclude adrenal cortex dysfunction and the recurrence of the original disease, it can be considered as glucocorticoid dependence syndrome.
Substance metabolism and water and salt metabolism disorder Long term and massive use of glucocorticoids can cause substance metabolism and water and salt metabolism disorder, and produce adrenocortical hyperfunction syndrome, such as edema, hypokalemia, hypertension, diabetes, skin thinning, full moon face, buffalo back, centripetal obesity, hirsutism, acne, muscle weakness, muscle atrophy and other symptoms, which generally do not need special treatment, It can subside by itself after drug withdrawal. But the recovery of myasthenia is slow and incomplete. Low salt, low sugar, high protein diet and potassium chloride can alleviate these symptoms. In addition, glucocorticoid can delay the wound healing of trauma patients due to its inhibition of protein synthesis. In children, negative nitrogen balance can be caused by inhibiting the secretion of growth hormone, which affects the growth and development.
Inducing or aggravating the infection of glucocorticoid can inhibit the immune function of the body, and has no antibacterial effect. Therefore, long-term use can often induce or aggravate the infection, which can make the potential infection focus in the body diffuse or static infection focus rekindle, especially for those with decreased original resistance, such as nephrotic syndrome, pulmonary tuberculosis, aplastic anemia patients, etc. Because patients often feel good about themselves when using glucocorticoid to cover up the symptoms of infection development, they should check their bodies before deciding to use long-term treatment to eliminate potential infection. They should also be vigilant during the application process. If necessary, they should use it together with effective antibiotics, with special attention to the prevention and treatment of potential tuberculosis lesions.
The digestive system complications (Gucocorticoid) 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 exacerbate peptic ulcer. Glucocorticoids can also cover the initial symptoms of ulcer, resulting in serious complications such as sudden bleeding and perforation, which should be noted. Long term use can aggravate gastric or duodenal ulcer. This side effect is more likely to occur when other drugs with gastric irritation (such as aspirin, indomethacin, butazolidin) are used together. It can induce pancreatitis or fatty liver in a few patients.
Long term use of glucocorticoids for cardiovascular system complications can cause hypertension and atherosclerosis due to sodium, water retention and elevated blood lipids.
Osteoporosis and vertebral compression fractures Osteoporosis and vertebral compression fractures are serious complications of glucocorticoid therapy in patients of all ages. Ribs and vertebrae have a high beam column structure, which is 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 osteocytes to parathyroid hormone. If osteoporosis occurs, the drug must be stopped. In order to prevent and cure osteoporosis, vitamin D, calcium salt and protein assimilation hormone should be supplemented.
If taken in large quantities, it is easy to cause diabetes and Cushing like syndrome. If taken for a long time, it is easy to cause mental symptoms and psychosis. People with a history of conjecture and psychosis should not use it. Patients with ulceration, thrombophlebitis, active pulmonary tuberculosis, and intestinal anastomosis should not use or use with caution.
Glucocorticoid dexamethasone, commonly known as "skin opium", is a prohibited ingredient in cosmetics. Consumers who use cosmetics added with dexamethasone will initially feel that their skin is significantly better, but long-term use will not only cause dependence, but also lead to dermatitis and even various diseases.
Adverse reaction table of dexamethasone
classification
Clinical report (unknown incidence)
Disposal of adverse reactions
immune system
Anaphylactic shock
When stopping the drug, inject adrenaline intramuscularly, and consider anti allergic treatment when adverse skin reactions occur
digestive system
hiccup
The drug should be stopped immediately or the dosage should be adjusted, and gastric mucosal protective agent can be considered
nervous system
Euphoria, excitement, anxiety, disorientation, inhibition, dizziness, insomnia
Use sedatives when dizziness and insomnia occur
cardiovascular system
Hypertension, hyperlipidemia, arrhythmia
endocrine system
Diabetes, hypokalemia
In case of hypokalemia, adequate potassium supplementation is required
Eye system
Obstruction or spasm of glaucoma and retinal artery
When glaucoma occurs, it is necessary to immediately apply intraocular pressure lowering drugs; In case of retinal artery occlusion or spasm, vasodilators can be used
other
Complicated with infection, glucocorticoid withdrawal syndrome, obesity, limb weakness
[5 ]

Drug interaction

Dexamethasone and calcium chloride Sulfadiazine sodium Tetracycline hydrochloride Oxytetracycline hydrochloride diphenhydramine chlorpromazine Promethazine Ethamsylate Procaine hydrochloride Hyoscyamine hydrobromide and other compatible drugs are prone to turbidity or precipitation, which will make the drug ineffective; And Furosemide Sodium salicylate Combined use of class A drugs can increase their toxicity.
1. When taken together with barbiturates, phenytoin and rifampicin, the metabolic promotion effect of this product is weakened.
2. And Salicylates Combined use of drugs can increase its toxicity.
3. It can weaken the effect of anticoagulants and oral hypoglycemic drugs, and the dosage should be adjusted.
4. When used with diuretics (except potassium preserving diuretics), hypokalemia can be caused, and attention should be paid to the dosage.
5. Non steroidal anti-inflammatory and analgesic drugs can enhance the ulcerative effect of glucocorticoid. Can be enhanced Acetaminophen Hepatotoxicity. AMRUMITE It can inhibit the function of adrenal cortex, accelerate the metabolism of dexamethasone, and shorten its half-life by 2 times. With amphotericin B or Carbonic anhydrase inhibitor When used together, it can aggravate hypokalemia. Attention should be paid to changes in blood potassium and cardiac function. Long term use with carbonic anhydrase inhibitors is prone to hypocalcemia and osteoporosis.
6. Combined with protein assimilation hormone, it can increase the incidence of edema and aggravate acne. When used together with antacids, it can reduce the absorption of prednisone or dexamethasone. And Anticholinergic drug (such as atropine) can increase intraocular pressure if used together for a long time. Tricyclic antidepressants can aggravate the mental symptoms caused by glucocorticoids.
7. When used in combination with hypoglycemic drugs such as insulin, the dosage of hypoglycemic drugs should be appropriately adjusted because it can increase the blood sugar of diabetic patients. Thyroid hormone can increase the metabolic clearance rate of glucocorticoid, so thyroid hormone or Antithyroid drug When combined with glucocorticoid, the dosage of the latter should be properly adjusted. Used together with contraceptives or estrogen preparations; It can strengthen the therapeutic effect and adverse reaction of glucocorticoid. Combined with cardiac glycosides, digitalis toxicity and arrhythmia can be increased. Combined with potassium excretion diuretics, it can cause severe hypokalemia, and weaken the sodium excretion diuretic effect of diuretics due to water and sodium retention.
8. Combined with ephedrine, it can enhance the metabolic clearance of glucocorticoid. And Immunosuppressant Combined use can increase the risk of infection and may induce lymphoma or other diseases lymphocyte Hyperplasia. Glucocorticoids, especially prednisolone, can increase the metabolism and excretion of isoniazid in the liver, and reduce the blood concentration and efficacy of isoniazid.
9. Glucocorticoid can promote the metabolism of mexiletine in vivo and reduce the blood concentration. And salicylate When used together, it can reduce the concentration of plasma salicylate. Combined with growth hormone, it can inhibit the growth promoting effect of the latter.
Table of incompatibilities of dexamethasone
Drug category
Taboo principle
Contraindications
Effective measures
Salicylic acid drugs
salicylic acid
Increased toxicity
Avoid syndication
NSAIDs
aspirin
Strengthen the ulcerative effect of glucocorticoid
Anticholinergic drug
atropine
May cause increased intraocular pressure
Avoid long-term joint use
Hypoglycemic drugs
insulin
Increase blood sugar in diabetic patients
Properly adjust the dosage of hypoglycemic drugs [6 ]

security information

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Safety terminology

S45:In case of accident or if you feel unwell, seek medical advice immediately (show the lable where possible).
In case of an accident or feeling unwell, seek medical advice immediately (show the label if possible).

Risk terminology

R40:Possible risks of irreversible effects.
There may be risk of irreversible effects.