Background and overview[1]
Betamethasone sodium phosphate is a glucocorticoid drug. Glucocorticoid drugs have anti-immune and anti-inflammatory effects and have been used clinically for many years. Betamethasone sodium phosphate is a long-acting hormonal drug that is used clinically for anti-inflammatory treatment, immune disease treatment, anti-DSM virus treatment and shock treatment. It has a wide range of effects. Compared with other glucocorticoid drugs, it has the characteristics of small dose, long half-life and obvious effect.
Function and use[2]
This product is a long-acting glucocorticoid and an epimer of dexamethasone. The effect is slightly stronger than dexamethasone. The efficacy of 0.5mg of this product is equivalent to that of dexamethasone 0.75mg, prednisone 5mg or cortisone 25mg. It is easily absorbed when taken orally, with a bioavailability of 72%. The peak plasma concentration is reached within 1 hour after intramuscular injection, and the plasma protein binding rate is low (64%). The ointment can be absorbed through the skin for external use, and is absorbed faster in damaged areas of the skin. The plasma half-life of this product is 190 minutes and the tissue half-life is 3 days. It is mainly used for allergic and autoimmune diseases, and is now mostly used for active rheumatism, rheumatoid arthritis, lupus erythematosus, severe bronchitis, severe dermatitis, acute leukemia, etc. It is also used in the comprehensive treatment of certain critical infections. Topical treatment of allergic dermatitis, eczema, neurodermatitis, seborrheic dermatitis and pruritus.
Usage and dosage[2]
Oral administration: The initial dose is 0.5 to 2 mg per day, divided into 2 to 4 times, and the maintenance dose is 0.5 to 1 mg per day or once in the morning.
Intramuscular injection or intravenous infusion: 2 to 6 mg each time. Sodium phosphate is used for intravenous infusion, often used in critical cases; acetate or sodium phosphate is used for intramuscular injection.
Topical application: ointment 0.1%, liniment 0.025%, apply to the affected area 2 to 3 times a day.
Preparations and Specifications[2]
Tablet: 0.5mg. Injection (sodium phosphate): 1ml: 4mg (equivalent to 5.26mg sodium phosphate). Ointment: 4g: 4mg, 10g: 10mg (0.1%).
Adverse reactions[3]
There are no obvious adverse reactions when glucocorticoids are used in physiological dose replacement therapy. Adverse reactions mostly occur when pharmacological doses are used, and are closely related to the course of treatment, dosage, type of medication, usage and route of administration. Common adverse reactions include the following categories.
(1) Long-term use may cause the following side effects. Iatrogenic Cushing’s syndrome: face and posture, weight gain, edema of the lower limbs, purple lines, easy bleeding tendency, poor wound healing, acne, menstrual disorders, avascular necrosis of the humeral or femoral head, osteoporosis and fractures (including spine Compression fractures, pathological fractures of long bones), muscle weakness, muscle atrophy, hypokalemia syndrome, gastrointestinal irritation (nausea, vomiting), pancreatitis, peptic ulcer or perforation, growth inhibition in children, glaucoma, cataracts, Benign intracranial hypertension syndrome, impaired glucose tolerance, and exacerbation of diabetes mellitus.
(2) Patients may have psychiatric symptoms. Euphoria, agitation, delirium, restlessness, disorientation, and may also manifest as inhibition. Psychiatric symptoms are more likely to occur in people suffering from chronic wasting diseases and those who have had mental disorders in the past.
(3) Concurrent infection is the main adverse reaction of adrenocortical hormones. Mainly fungi, Mycobacterium tuberculosis, Staphylococcus aureus, Proteus, Pseudomonas aeruginosa and various herpes viruses.
(4) Glucocorticoid withdrawal syndrome. Sometimes patients experience dizziness, fainting tendencies, abdominal or back pain, low-grade fever, loss of appetite, nausea, vomiting, muscle or joint pain, headache, fatigue, and weakness after stopping the drug. After careful examination, if adrenal insufficiency and the original disease can be ruled out, If the disease relapses, it may be considered as a syndrome of dependence on glucocorticoids.
Taboo[3]
Contraindicated for those allergic to this product and other steroid hormones. Patients with the following diseases are generally not suitable for use. The pros and cons should be weighed in special cases, but attention should be paid to the possibility of worsening of the condition: severe mental illness (past or present) and epilepsy, active peptic ulcer disease, recent gastrointestinal anastomosis surgery, fractures, trauma repair period , corneal ulcers, hyperadrenocorticism, hypertension, diabetes, pregnant women, infections that cannot be controlled by antibiotics such as chickenpox, measles, fungal infections, severe osteoporosis, etc.
Notes[3]
(1) Inducing infection. Under the influence of hormones, infections that have been controlled can become active. The most common case is the recurrence of tuberculosis infection. The application of hormones in certain infections can reduce tissue damage, reduce exudation, and alleviate the symptoms of infection and poisoning, but it must be treated with effective antibiotics at the same time, and changes in the condition must be closely observed. After short-term use, the dosage should be quickly reduced and the medication should be discontinued.
(2) Interference with diagnosis
① Glucocorticoids can increase blood sugar, blood cholesterol, blood fatty acids, and blood sodium levels, and decrease blood calcium and blood potassium; ② The effects on peripheral blood include lymphocytes, eukaryotic cells, and eosinophils and basophils The number of cells decreases, multinucleated white blood cells and platelets increase, and the latter may also decrease; ③ Long-term high-dose glucocorticoid use can cause false negative results in skin tests, such as tuberculin test, histoplasmin test and allergic reaction skin test etc.; ④ It can also reduce the thyroid 131I uptake rate, weaken the response of thyroid stimulating hormone (TSH) to TSH releasing hormone (TRH) stimulation, and make the TRH stimulation test results falsely positive. Interfering with luteinizing hormoneThe results of LHRH stimulation test; ⑤ The isotope brain and bone imaging is weakened or sparse.
(3) The following situations should be used with caution. Heart disease or acute heart failure, diabetes, diverticulitis, emotional instability and psychotic tendencies, systemic fungal infections, glaucoma, liver damage, ocular herpes simplex, hyperlipoproteinemia, hypertension, hypothyroidism (at this time Enhanced effects of glucocorticoids), myasthenia gravis, osteoporosis, gastric ulcer, gastritis or esophagitis, renal impairment or stones, tuberculosis, etc.
(4) Follow-up examination. Those who use glucocorticoids for a long time should check the following items regularly. ① Blood sugar, urine sugar or glucose tolerance test, especially for those with diabetes or diabetes tendency; ② Children’s growth and development should be checked regularly; ③ Eye examination, pay attention to the occurrence of cataracts, glaucoma or eye infection; ④ Serum electrolytes and fecal occult blood; ⑤Examination of high blood pressure and osteoporosis, especially for the elderly.
Drugs for pregnant and lactating women[3]
(1) Medication during pregnancy. The glucocorticoid Cabot silica crosses the placenta. Animal experimental studies have confirmed that administration during pregnancy can increase the incidence of embryonic cleft palate, placental insufficiency, spontaneous abortion and intrauterine growth retardation. The use of pharmacological doses of glucocorticoids in humans increases the incidence of placental insufficiency, neonatal weight loss, or stillbirth.
(2) Medication during lactation. Since glucocorticoids can be excreted in breast milk, they can cause adverse effects on infants, such as growth inhibition and adrenal cortex function suppression.
Pregnant and lactating women should avoid using it as much as possible after weighing the pros and cons.
Pediatric Medication[3]
Be very cautious if children use adrenocortical hormones for a long time.
Drug use in elderly patients[3]
Elderly patients taking glucocorticoids are prone to hypertension and diabetes. The use of glucocorticoids in elderly patients, especially postmenopausal women, can easily aggravate osteoporosis.
Drug interactions[3]
(1) Non-steroidal anti-inflammatory analgesics can enhance their ulcerogenic effects.
(2) Can enhance the hepatotoxicity of acetaminophen.
(3) Combined use with amphotericin B or carbonic anhydrase inhibitors can aggravate hypokalemia. Long-term combined use with carbonic anhydrase inhibitors can easily cause hypocalcemia and osteoporosis.
(4) Combined use with protein anabolic hormones can increase the incidence of edema and aggravate acne.
(5) Long-term combined use with anticholinergic drugs (such as atropine) may increase intraocular pressure.
(6) Tricyclic antidepressants can aggravate the psychiatric symptoms caused by them.
(7) When used in combination with anti-diabetic drugs such as insulin, the dose of anti-diabetic drugs should be appropriately adjusted because it may increase blood sugar in diabetic patients.
(8) Thyroid hormone can increase its metabolic clearance rate. Therefore, when thyroid hormone or antithyroid drugs are used in combination with it, the dosage of the latter should be appropriately adjusted.
(9) Combined use with contraceptives or estrogen preparations can enhance its therapeutic effect and adverse reactions.
(10) Combined use with cardiac glycosides can increase digitalis toxicity and the occurrence of arrhythmia.
(11) Combined use with potassium-excreting diuretics can cause severe hypokalemia and weaken the natriuretic and diuretic effect of diuretics due to water and sodium retention.
(12) Combined with ephedrine, it can enhance its metabolic clearance.
(13) Combined use with immunosuppressants can increase the risk of infection and may induce lymphoma or other lymphocyte proliferative diseases.
(14) It can increase the metabolism and excretion of isoniazid in the liver and reduce the plasma concentration and efficacy of isoniazid.
(15) It can promote the metabolism of mexiletine in the body and reduce the plasma concentration.
(16) Combined use with salicylate can reduce plasma salicylate concentration.
(17) Combined with growth hormone, it can inhibit the growth-promoting effect of the latter.
