What Is Prednisone Tapering?

Prednisone has anti-inflammatory and anti-allergic effects, can inhibit the proliferation of connective tissue, reduce the permeability of capillary walls and cell membranes, reduce inflammatory exudation, and can inhibit the formation and release of histamine and other toxic substances. This product can also promote the breakdown of protein into sugar, reducing the use of glucose. As a result, blood glucose and liver glycogen are increased, diabetes can occur, and gastric juice secretion is increased, which increases appetite. When used in combination with a large number of antibacterial agents, it can have good cooling, anti-toxic, anti-inflammatory, anti-shock, and promote symptomatic relief when used in severe toxic infections. Its water and sodium retention and potassium excretion effects are smaller than those of cortisone, and its anti-inflammatory and anti-allergic effects are relatively strong.

Drug Name: Prednisone
Alias: Prednisone, dehydrocortisone
Foreign name: Prednisone
Whether prescription drugs: Non-prescription drugs
Main indications: Mainly used for allergic and inflammatory diseases

Dosage: Oral, 15 to 40 mg daily for adults, increased to 60 mg if needed
Adverse reactions: Cushing's syndrome
Dosage form: tablet
Athletes use with caution: Use with caution
Whether to include health insurance: Incorporate
Drug type: Adrenal corticosteroids

Prednisone Basic Information

Chinese name: Prednisone

Chinese alias: prednisone acetate; prednisone; dehydrocortisone; dehydrocorticoid; 1-enecortisone

English name: Prednisone

English alias: Deltacortone; Meticorten

Molecular formula: C ₂₁ H ₂₆ O ₅

Molecular weight: 358.43

Properties: Its acetate is commonly used as white or almost white crystalline powder; odorless and bitter. Soluble in chloroform, slightly soluble in acetone, slightly soluble in ethanol or ethyl acetate, insoluble in water.

Prednisone Pharmacopoeia Standard

Prednisone source (name), content (potency)

This product is 17, 21-oxahydroxyprogesterone-1,4-diene-3,11,20-trione. Calculated based on dry products, containing C ₂₁ H ₂₆ O ₅ should be 97.0% to 102.0%.

Prednisone traits

This product is white or off-white crystalline powder; odorless.

This product is slightly soluble in ethanol or chloroform and almost insoluble in water.

Specific rotation

Take this product, weigh it accurately, add dioxane to dissolve and quantitatively dilute it to make a solution containing about 5mg per 1ml, and measure it according to law (Appendix VI E of the second edition of the Pharmacopoeia, 2010 edition). The specific rotation is + 167 ° to + 175 °.

Absorption coefficient

Take this product, weigh it accurately, add ethanol to dissolve and quantitatively dilute it to make a solution containing about 15 g per 1 ml. According to UV-Vis spectrophotometry (Appendix IV A of Pharmacopoeia Part II of 2010 Edition), measure the absorbance at a wavelength of 240 nm The absorption coefficient () is 405 to 435.

Prednisone identification

(1) Take about 5mg of this product, add 2ml of sulfuric acid to dissolve, and stand for 5 minutes to become orange; pour this solution into 10ml of water, and the solution will turn yellow and gradually become blue-green.

(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 light absorption spectrum of this product should be consistent with the control spectrum (Figure 612 of the "Infrared Spectra of Drugs").

Prednisone check

relative substance

Take this product, weigh it accurately, add mobile phase to dissolve and quantitatively dilute to make a solution containing about 0.5mg per 1ml as the test solution; take 1ml precisely, place it in a 100ml volumetric flask, and dilute to the mark with mobile phase , Shake well as the control solution; take another cortisone reference substance, add mobile phase to dissolve and quantitatively dilute to make a solution containing about 5 g per 1 ml, as the reference solution. According to the chromatographic conditions under the content determination item, take 20 l of the control solution and inject it into the liquid chromatograph, and adjust the detection sensitivity so that the peak height of the main component chromatographic peak is about 20% of the full scale. Then accurately measure 20 l of each of the test solution, the control solution and the reference solution, and inject them into the liquid chromatograph respectively, and record the chromatogram to 2.5 times the peak component retention time. If there is a peak in the chromatogram of the test solution that is consistent with the retention time of the cortisone peak in the chromatogram of the reference solution, the peak area calculated according to the external standard method shall not exceed 0.5%; the peak area of other single impurities shall not be greater than the main peak area of the control solution. 0.5 times (0.5%), the sum of the peak areas of each impurity must not be greater than 1.5 times (1.5%) of the main peak area of the control solution. Any peak less than 0.01 times the area of the main peak of the control solution in the chromatogram of the test solution can be ignored.

Loss on drying

Take about 0.5g of this product and dry it at 105 ° C for 3 hours, and the weight loss should not exceed 1.0% (Appendix L of Part Two of the Pharmacopoeia, 2010 Edition).

Determination of prednisone

It was determined by high performance liquid chromatography (Appendix D, Part Two of the Pharmacopoeia, 2010 Edition).

Chromatographic conditions and system suitability tests

Octadecylsilane-bonded silica gel was used as the filler; acetonitrile-water (24:76) was used as the mobile phase; the detection wavelength was 240 nm. Take prednisone and cortisone, dissolve and dilute with mobile phase to make a solution containing about 5 g per 1 ml, and take 20 l into the liquid chromatograph. Record the chromatogram. The resolution of the prednisone peak and the cortisone peak should be Greater than 3.4.

Assay

Take this product, weigh it accurately, add mobile phase to dissolve and quantitatively dilute it to make a solution containing about 50g per 1ml. Precisely measure 20l into the liquid chromatograph and record the chromatogram; take another prednisone reference substance, the same method Determination. Calculate the peak area according to the external standard method to get ^[1] .

Prednisone Categories

Adrenal corticosteroids.

Prednisone storage

Shaded and sealed.

Prednisone version

2010 Pharmacopoeia of the People's Republic of China ^[2] .

Prednisone Drug Analysis

Method name:

Determination of prednisone-high performance liquid chromatography

Application:

This method uses high performance liquid chromatography to determine the content of prednisone.

This method is applicable to prednisone.

Method principle:

Both the test product and the internal standard were made into a methanol solution, and then entered into a high-performance liquid chromatography for chromatographic separation. The ultraviolet absorption detector was used to detect the prednisone (C ₂₁ H ₂₆ O ₅ ) and the internal standard acetanilide at a wavelength of 254 nm. Absorption value and calculate its content.

Reagent:

Methanol

Water

3.Tetrahydrofuran

4. Dilute methanol (1 2)

equipment:

Instrument

1.1 HPLC

1.2 Column

Octadecylsilane-bonded silica gel is used as a filler, and the theoretical plate number should not be less than 3000 based on the prednisone peak calculation.

1.3 UV absorption detector

Chromatographic conditions

2.1 Mobile phase: water tetrahydrofuran + methanol = 688 250 62

2.2 Detection wavelength: 254nm

2.3 Column temperature: room temperature

Sample preparation:

Weigh the test product

Take an appropriate amount of this product and weigh it accurately.

2. Preparation of reference solution

Precisely weigh the appropriate amount of the prednisone reference substance, add methanol to dissolve and dilute it into a solution.

3. Preparation of internal standard solution

Take an appropriate amount of acetanilide, add diluted methanol to make a solution containing about 0.11mg per 1mL, that is, obtained.

4. Preparation of test solution

The above test product was dissolved in dilute methanol and quantitatively diluted to a solution containing about 0.2 mg per 1 mL to obtain a test solution.

Note: "Precision weighing" means that the weighed weight should be accurate to one thousandth of the weight taken. "Precision measurement" means that the accuracy of measuring the volume should meet the accuracy requirements of the volume pipette in national standards.

Steps:

5 mL of the test solution and the internal standard solution were accurately pipetted into 50 mL volumetric flasks, diluted with dilute methanol to the mark, and mixed evenly. 10 L was injected into the high performance liquid chromatograph, and measured at a wavelength of 254 nm with an ultraviolet absorption detector The absorption values of norgegestrel and internal standard megestrol acetate are calculated by the peak area based on the internal standard method. Another solution of prednisone reference substance was measured in the same way ^[3] .

Prednisone medication description

Prednisone classification

Respiratory Drugs> Asthma Drugs> Anti-inflammatory Asthma Drugs

Prednisone dosage form

1. Tablet: 5mg;

2. Ointment: 0.5%.

Prednisone pharmacological action

The product has anti-inflammatory and anti-allergic effects, can inhibit the proliferation of connective tissue, and reduce the capillary wall and cell membrane.

Prednisone Permeability, reduce inflammatory exudation, and can inhibit the formation and release of histamine and other toxic substances. This product can also promote the breakdown of protein into sugar, reducing the use of glucose. As a result, blood glucose and liver glycogen are increased, diabetes can occur, and gastric juice secretion is increased, which increases appetite. When used in combination with a large number of antibacterial agents, it can have good cooling, anti-toxic, anti-inflammatory, anti-shock, and promote symptomatic relief when used in severe toxic infections. Its water and sodium retention and potassium excretion effects are smaller than those of cortisone, and its anti-inflammatory and anti-allergic effects are relatively strong. The product must reduce the 11-position keto group to 11-hydroxy group in the liver to show pharmacological effects, and its biological tl /: is 60 minutes. It can be used clinically for various acute severe bacterial infections, severe allergic diseases, collagen diseases (lupus erythematosus, nodular periarteritis, etc.), rheumatism, nephrotic syndrome, severe bronchial asthma, thrombocytopenic purpura, Granulocytopenia, acute lymphoblastic leukemia, various adrenal insufficiency, exfoliative dermatitis, pemphigus, neurodermatitis, eczema, etc.

Prednisone pharmacokinetics

After oral administration, the absorption is rapid and complete, and the biological half-life is about 60 minutes. It can be transported to the whole body in combination with corticosteroid transporters in the body. Prednisone itself has no biological activity and needs to be converted into prednisone in the liver to function. The liver distribution is the highest in the body, followed by the plasma, and there is a certain content in the cerebrospinal fluid, pleural and ascites fluid, and less in the kidney and spleen. Excreted in the urine after metabolism. Prednisone reduces the 11-keto group to the 11-hydroxy group in the liver and has a pharmacological effect ^[1] .

Prednisone indications

1. Such as systemic lupus erythematosus, rheumatoid arthritis, rheumatic fever, nephrotic syndrome, chronic active hepatitis, ulcerative colitis, autoimmune hemolytic anemia, idiopathic thrombocytopenic purpura and other diseases.

2. Shock: For the treatment of cardiogenic shock caused by acute myocardial infarction or cardiac block, prednisone may be used as an adjuvant therapy.

3. Allergic diseases: drug-derived dermatitis and allergic diseases can be taken orally with prednisone.

4. Infectious diseases: Exudative tuberculosis. After antituberculosis treatment, in order to prevent fibrosis and adhesion sequelae, prednisone and other glucocorticoids can be given.

5. Rejection of organ transplantation: Prednisone and other immunosuppressants are commonly used to prevent rejection or delay its occurrence.

6. Leukemia, hematopoietic tumors and solid tumors.

7. Ophthalmic diseases: can be used to treat non-specific ophthalmitis and allergic eye diseases such as conjunctivitis, keratitis, retinitis and optic neuritis.

8. Skin diseases: such as severe drug-derived dermatitis, keloids and hypertrophic scars, local skin lesions, etc.

9. Prednisone is not suitable for the replacement of primary adrenal insufficiency due to its weak mineralocorticoid activity.

10. Acute lymphocytic leukemia.

11. Malignant lymphoma.

12. Multiple myeloma.

13. Breast cancer, prostate cancer, kidney cancer, etc. ^[1] .

Prednisone dosage usage

Complementary replacement therapy: Oral, 5-10mg once a day, 10-60mg a day, 2/3 after getting up in the morning, 1/3 in the afternoon

Particle diameter Anti-inflammatory: 5 60mg a day orally, the dosage of treatment course varies according to the condition

Autoimmune diseases: Oral, 40-60 mg daily, reduce it when the condition is stable

Allergic diseases: 20 to 40 mg daily, 5 mg every 1 to 2 days after symptoms are alleviated

Prevent organ transplant rejection: Generally, 100 mg orally per day is started 1 to 2 days before surgery, and 60 mg per day is changed one week after surgery. Treatment of acute leukemia, malignant tumors, etc .: Reduce the symptoms after oral symptom relief of 60 to 80 mg.

Prednisone precautions

For patients who have been using this drug for a long time, the dosage should be increased during surgery and within 3 to 4 days after surgery.

Prednisone Inadequate anticortical function. General surgical patients should try not to avoid wound healing.

Both this product and cortisone need to be metabolized and activated by the liver to hydroprednisone or hydrocortisone to be effective, so those with poor liver function should not be used.

This product is not suitable for primary adrenal insufficiency due to its weak mineralocorticoid activity.

Adrenal hyperfunction, hypertension, atherosclerosis, heart failure, diabetes, neuropathy, epilepsy, postoperative patients, and stomach, duodenal and corneal ulcers, intestinal disease or chronic malnutrition, liver function Incomplete patients should not be used; pregnant women should be used with caution or disabled; viral infections should be used with caution.

Prednisone adverse reactions

Glucocorticoids have no obvious adverse reactions when applying physiological dose replacement therapy. Adverse reactions mostly occur when applying pharmacological doses, and are closely related to the course of treatment, dose, type of medication, usage, and route of administration. The common adverse reactions are as follows.

Systemic allergic reactions, including swelling of the face, nasal mucosa, eyelids, urticaria, shortness of breath, chest tightness, and wheezing, may occur with rapid sacral vein administration in large doses.

Long-term medication can cause the following side effects: iatrogenic Cushing syndrome face and body shape, weight gain, lower extremity swelling, purple streaks, tendency to bleed easily, poor wound healing, acne, menstrual disorders, humeral or femoral head ischemic necrosis, Osteoporosis or fractures (including vertebral compression fractures, long bone pathological fractures), muscle weakness, muscle atrophy, hypokalemia syndrome, gastrointestinal irritation (nausea, vomiting), pancreatitis, peptic ulcer or bowel perforation, Growth inhibition, glaucoma, cataracts, benign intracranial pressure syndrome, impaired glucose tolerance and exacerbation of diabetes in children.

(3) Mental symptoms may occur in patients: euphoria, agitation, restlessness, delirium, disorientation, or inhibition. Mental symptoms are particularly likely to occur in people with chronic wasting diseases and in those who have had mental disorders in the past. Prednisone 40mg or more can be used within a few days to two weeks.

Complicated infection is the main adverse reaction of glucocorticoids. Mainly fungi, tuberculosis, staphylococcus, proteus, Pseudomonas aeruginosa and various herpes virus infections. Occurs in the middle or long course of treatment, but can also occur after short-term use of large doses.

Inhibition of the hypothalamic-pituitary-adrenal axis is an important complication of hormonal therapy, and its occurrence is related to factors such as preparation, dose, and course of treatment. When prednisone is used more than 20mg daily for more than 3 weeks, and when iatrogenic Cushing syndrome occurs, adrenal function should be considered to be suppressed.

Symptoms of glucocorticoid withdrawal syndrome can be as follows:

Hypothalamus-pituitary-adrenal insufficiency can be manifested as weakness, weakness, loss of appetite, nausea, vomiting, low blood pressure, and recovery of this axial function after long-term treatment.

Prednisone It usually takes 9 to 12 months, and the order of function recovery is as follows:

1. Hypothalamic adrenocorticotropic hormone (CRF) secretion recovered and increased;

2. ACTH secretion recovered and was higher than normal, at this time the secretion of adrenocortical hormone was still low;

3. The basal secretion of hydrocortin has returned to normal, and the secretion of ACTH from the pituitary has returned to normal.

4. The hypothalamic-pituitary-adrenal cortex axis response to stress returned to normal.

After stopping the medicine, the symptoms whose original disease had been controlled reappeared. In order to avoid the occurrence of adrenal insufficiency and the recurrence of the original disease symptoms, the dose should be gradually reduced gradually after long-term hormone treatment and taken from the original several times a day to the daily medication once in the morning or the next morning. once.

glucocorticoid withdrawal syndrome. Sometimes patients have dizziness, fainting tendency, abdominal pain or back pain, low fever, loss of appetite, nausea, vomiting, muscle or joint pain, headache, fatigue, weakness after discontinuation of medication. Careful inspection can rule out adrenal insufficiency and the original disease. The re-ignition can be considered as glucocorticoid dependence syndrome.

Weight gain, hirsutism, acne, blood sugar, elevated blood pressure, and intraocular pressure, water and sodium retention. Can cause hypokalemia, excitement, gastrointestinal ulcers and even bleeding perforations, osteoporosis, and poor wound healing.

This product inhibits antigen-antibody response, inhibits leukocyte migration and phagocytosis, and weakens the body's defense function against external infections.

Prednisone contraindications

medication during pregnancy; glucocorticoids can pass through the placenta. Animal experiments have confirmed that administration during pregnancy can increase the incidence of fissures in the embryo, placental dysfunction, spontaneous abortion and intrauterine growth retardation. Human use of pharmacological doses of glucocorticoids can increase the incidence of placental insufficiency, neonatal weight loss, or stillbirth. Teratogenic effects have not been proven in humans. Those who have received a certain dose of glucocorticoids during pregnancy should pay attention to observe whether there are signs of adrenal insufficiency. For preterm infants, to avoid respiratory distress syndrome, dexamethasone was given to mothers before delivery to induce the formation of lung surfactant proteins in preterm infants. Due to short-term application, there was no adverse effect on the growth and development of young children.

lactation medication: physiological doses or low pharmacological doses (25 mg cortisone or 5 mg prednisone per day, or less) generally have no adverse effects on infants. However, if a nursing mother receives a pharmacologically high dose of glucocorticoids, she should not breastfeed, because glucocorticoids can be excreted from milk and cause adverse effects on infants, such as inhibited growth and inhibited adrenal function.

(3) Pediatric medication: If children use adrenocortical hormones for a long time, they need to be very careful, because hormones can inhibit the growth and development of children. If long-term use is necessary, short-acting (such as cortisone) or intermediate-acting preparations (such Prednisone), avoiding long-acting preparations (such as dexamethasone). Oral medium-effect preparations can reduce the inhibitory effect on growth every other day. Long-term use of glucocorticoids in children or adolescents must be closely monitored. Children are at increased risk for osteoporosis, ischemic necrosis of the femoral head, glaucoma, and cataracts. In addition to the general dose of hormones for children, it should be based on the severity of the disease and the response of the child to treatment. For the treatment of children with adrenal insufficiency, the dosage of hormones should be based on body surface area. If it is based on weight, it is prone to overdose, especially infants and small or obese children.

medication for the elderly: elderly patients with glucocorticoids are prone to hypertension. Elderly patients, especially postmenopausal women, are prone to osteoporosis with glucocorticoids.

Glucocorticoids and infections: Patients with adrenal insufficiency are prone to infection and are more serious. As an important cause of death, giving physiological doses of adrenal corticosteroids can improve patients' resistance to infection. Non-adrenal insufficiency patients are prone to infection after receiving pharmacological doses of glucocorticoids. This is because patients 'original diseases often have weakened cellular and / or humoral immune functions. Long-term superphysiological doses of corticosteroids make patients' inflammation The sexual response, cellular immunity, and humoral immune function are weakened, and the pathogens invading from the skin and mucous membranes cannot be controlled. Under the action of hormones, infections that have been controlled can become active. The most common is recurrence of tuberculosis infection. Patients receiving glucocorticoids are susceptible to missed diagnosis due to mild inflammatory reactions and insignificant clinical symptoms after infection. The above shows that non-physiological glucocorticoids are not good for fighting infections. On the other hand, the application of hormones in certain infections can reduce tissue damage, reduce exudation, and reduce symptoms of infection poisoning. However, it must be treated with effective antibiotics at the same time, and changes in the condition must be closely observed. After short-term medication, it should be quickly reduced. Volume, discontinuation.

The following cases should be used with caution; heart disease or acute heart failure, diabetes, diverticulitis, emotional instability and psychotic tendencies, systemic fungal infections, glaucoma, liver damage, herpes simplex, hyperlipoproteinemia, high Blood pressure, hypothyroidism (increased glucocorticoid effect), myasthenia gravis, osteoporosis, gastric ulcer, gastritis or esophagitis, impaired renal function or stones, tuberculosis, etc.

Corticosteroids should not be used in the following cases: severe history of mental illness, active gastric and duodenal ulcers, recent postoperative gastrointestinal anastomosis, heavier osteoporosis, significant diabetes, severe hypertension, failed to use Antibacterial drugs control viral, bacterial, and fungal infections. Hyperadrenal function, hypertension, atherosclerosis, heart failure, diabetes, psychosis, epilepsy, postoperative, stomach, duodenal and corneal ulcers, intestinal diseases, chronic chronic malnutrition should be avoided. Disable pregnant women. Viral infections should be used with caution.

Prednisone drug interactions

1. Improving the sensitivity of blood vessels to booster drugs;

2. Suppress the immune response, can not be used at the same time as the vaccine;

3. Combined with thiazide diuretics is more prone to hypokalemia;

4. Combined with immunosuppressive drugs, the incidence of ulcers and bleeding increases;

5. Reduce the effect of hypoglycemic drugs and antagonize insulin;

6.Protein assimilation hormone can correct the effect of prednisone to break down proteins to a certain extent, and correct the negative nitrogen balance;

7. With the use of digitalis, because of low potassium, digitalis poisoning is more likely to occur, should pay attention to potassium supplementation;

8. Phenobarbital and phenytoin sodium can accelerate the prednisone metabolism and reduce the efficacy;

9. Combination with indomethacin is more prone to ulcers. When combined with cyclosporine, the metabolism of prednisone is inhibited. When used in combination with anticancer drugs, immune system suppression becomes worse ^[1] .

Prednisone expert review

It is a commonly used oral glucocorticoid in clinical practice. It is the most important drug in the treatment of autoimmune diseases such as systemic lupus erythematosus, rheumatism and nephrotic syndrome. Has a good therapeutic effect. Prednisone has strong anti-inflammatory and anti-allergic effects, less adverse reactions, and is convenient for oral administration. It is suitable for long-term users and those who take maintenance doses. Its dose conversion, reduction and increase are more convenient. The rate of complete remission for children with acute lymphoblastic leukemia alone is 60%, and the effect on adult acute lymphoblastic leukemia is worse than that on children, and the effect on non-acute lymphocytic leukemia is lower than acute. Multiple myeloma has a single effective rate of 40%, and ovarian cancer has a single effective rate of 25%. It also has a certain effect on prostate cancer. The complete response rate of Hodgkin's disease using MOPP combined with chemotherapy is 81%, and the 5-year generation rate is 64%. The complete response rate of non-Hodgkin's lymphoma with CHOP is 50% to 80%. The application must strictly control the indications to prevent the abuse of prednisone.