What Is Methylprednisolone?

Methylprednisolone is a medium-effect synthetic product. The anti-inflammatory effect of 4mg is about the same as that of 5mg of prednisolone. Sodium retention is weak. The acetate suspension of this product disintegrates slowly and has a long-lasting effect. It can be injected into the muscle and joint cavity. Sodium succinate is water-soluble and can be used for intramuscular injection or intravenous infusion in glucose solution.

Drug Name: Methylprednisolone
Alias: Methylprednisolone
Foreign name: methylprednisolone
Athletes use with caution: Use with caution

Whether to include health insurance: Incorporate
Drug type: Adrenal corticosteroids
Melting point: 228-237
Molecular formula: C22H28O5

Methylprednisolone Basic Information

Chinese name: methylprednisolone

Chinese alias: methylprednisolone; prednisone; 16-methylprednisone; methyl dehydrocortisone; methylprednisolone; methylprednisolone; 6-prednisolone ; Shulu-Metrolol; Yamei Tailong; Methyronon; Methylprednisolone; Methylprednisolone; Sodium succinate-6 Methylprednisolone; Amber methylprednisolone; Methylprednisolone succinic acid Sodium; methylprednisolone needle ^[1]

English name: meprednisone

English alias: 17-Hydroxy-17- (2-hydroxyacetyl) -10,13,16-trimethyl-6,7,8,9,12,14,15,16-octahydrocyclopenta [a] phenanthrene-3,11-dione ; 17,21-dihydroxy-16-methylpregna-1,4-diene-3,11,20-trione; MEDRON; Methylprednisolone Sodium Succinate; Medrol; Solu-Medrol ^[1]

CAS number: 83-43-2

Methylprednisone structure

EINECS number: 214-996-1

Molecular formula: C ₂₂ H ₃₀ O ₅

Molecular weight: 374.5

Melting point: 228-237 ° C

Properties: white or almost white crystalline powder, odorless, tasteless at first and then bitter. Soluble in absolute ethanol and chloroform, almost insoluble in water

Methylprednisolone drug description

Methylprednisolone classification

Endocrine System Drugs> Adrenal Corticosteroids

Methylprednisolone dosage form

1. Powder injection: 40mg;

2. Tablet: 4mg;

3. Injection: 20mg (1ml).

4. Tablet: acetate 2mg, 4mg;

5. Injection: 40mg (1ml) acetate, 80mg (2ml), 40mg sodium succinate;

6. Lotion or cream: 0.25% acetate.

Methylprednisolone pharmacological action

Methylprednisolone has a stronger anti-inflammatory effect and a weaker sodium retention effect. Its anti-inflammatory effect is 7 times that of cortisone; methylprednisolone sodium succinate is a water-soluble prednisolone derivative that is converted in vivo It is methylprednisolone, which can be injected, has a quick-acting effect, and has a medium duration of maintenance. It is the preferred medicine for treating inflammation and allergies. Acetate is a suspension that has a slow onset of action and a long lasting effect after injection. Methylprednisolone is a medium-acting glucocorticoid. The effect is the same as that of prednisolone, its anti-inflammatory effect is three times that of the latter, its sugar metabolism is 10 times stronger than that of hydrocortisone, and its water and sodium retention are weak, without the side effects of potassium excretion. Its acetate suspension is used for intramuscular injection and intra-articular injection, which is slow to decompose and absorb, and maintains for a long time. After 6-8 hours of intramuscular injection, the average peak blood concentration is 14.8 g / L, which can be maintained for 11-17 days . Its sodium succinate is water-soluble and can be injected intramuscularly or intravenously ^[1] .

Methylprednisolone pharmacokinetics

Oral bioavailability is 82%, plasma protein binding rate is 40% to 60%, and half-life is about 2.5h. The plasma half-life of methylprednisolone sodium succinate is about 30 min ^[1] .

Methylprednisolone indications

It is used for emergency treatment of critical illnesses, and can also be used for endocrine disorders, rheumatic diseases, collagenous diseases, skin diseases, allergic reactions, ophthalmic diseases, gastrointestinal diseases, blood diseases, leukemia, shock, cerebral edema, polyneuritis, spinal cord Inflammation and preventing vomiting caused by cancer chemotherapy. Currently it is mainly used in clinical organ transplantation ^[1] .

Methylprednisolone dosage

When oral administration is started, it is usually 16 40mg daily, and it is taken in divided doses. The maintenance dose is 4 to 8 mg daily.

Intravenous infusion or bolus injection (sodium methylprednisolone sodium succinate) General dose (equivalent to methylprednisolone): 10 40mg each time, the maximum dose can be up to 30mg / kg according to body weight. Too fast, generally controlled in about 10-20 minutes, if necessary, medication can be repeated every 4 hours, the dose is 10-40mg each time.

Treatment of cerebral edema: intramuscular or intravenous injection, once every 4-6h, 40-125mg each time, 4-7 days as a course of treatment.

For organ transplantation: once every 24 to 48 h, 0.5 to 2.0 g each time.

Acute laryngeal bronchitis (asthma): intramuscular injection of 40 mg, administered early in the attack.

Rheumatic diseases, systemic lupus erythematosus, multiple sclerosis: 1g daily, intravenous use for about 3 days.

Pyelonephritis and lupus nephritis: once every 48h, 30mg / kg each time, for 4 days.

Prevent nausea and vomiting caused by chemotherapy of cancer: 1 hour before chemotherapy and at the beginning of chemotherapy, 250 mg intravenously over 5 minutes each.

Other indications: The dose can be from 10 to 500 mg, depending on the condition ^[2] .

Precautions for methylprednisolone

1. (1) acute heart failure or other heart disease; (2) diabetes; (3) diverticulitis; (4) emotional instability and psychotic tendencies; (5) glaucoma; (6) liver damage; (7) Ocular herpes simplex; (8) hyperlipoproteinemia; (9) hypertension; (10) hypothyroidism (at this time the glucocorticoid effect is enhanced); (11) myasthenia gravis; (12) osteoporosis (13) gastric ulcer, gastritis, or esophagitis; (14) impaired renal function or stones; (15) tuberculosis.

2. In some acute treatments, intramuscular injection or intravenous administration is usually used for rapid onset of action.

3. The treatment of acute spinal cord injury should be started within 8 hours after trauma.

4. Methylprednisolone acetate decomposes slowly and has a long-lasting effect. It can be used for intramuscular injection to achieve long-lasting systemic effects, and it can also be used for intra-articular injection. Methylprednisolone sodium succinate is water-soluble and can be used for intramuscular injection or intravenous drip in glucose solution.

5. Methylprednisolone has a short half-life, so when severe shock is treated, it should be repeated after 4 hours.

6. Injectables are easy to decompose and destroy under ultraviolet and fluorescence.

7. Methylprednisolone sodium is generally not used as an alternative treatment for adrenal insufficiency due to its weak effect. If used, it should be combined with mineralocorticoids.

8. Before use, inject drug products should be checked visually for special objects and discoloration. In a sterile environment, add the diluent to a sterile powder vial, and use only specific diluents. Intravenous compatibility and stability of methylprednisolone sodium succinate solution and other drugs in an intravenous infusion mixture are affected by the pH, concentration, time, temperature and the solubility of methylprednisolone in the mixture. To avoid compatibility and stability issues, it is recommended that methylprednisolone be administered separately from other drugs whenever possible.

9. Pregnant women and lactating women should be used with caution.

10. Large doses (greater than 0.5g) and bolus or intravenous drip may cause arrhythmia and even circulatory failure.

11. As with other adrenocortical hormones, the efficacy of septic shock is uncertain and may increase patient mortality.

12. Smallpox vaccine should not be given during treatment to avoid causing neurological complications.

Adverse reactions to methylprednisolone

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.

Syndrome after glucocorticoid discontinuation can have the following different situations. Hypothalamus-pituitary-adrenal insufficiency can be manifested as fatigue, weakness, loss of appetite, nausea, vomiting, low blood pressure, and the recovery of this axial function after long-term treatment generally takes 9 to 12 months. For: i. Hypothalamic adrenocorticotropin (CRF) secretion recovery and increase; ii. ACTH secretion recovered and was higher than normal, at this time the secretion of adrenocortical hormone was still low; iii. The basic secretion of hydrocortin has returned to normal, and the secretion of ACTH from the pituitary has returned to normal. IV. 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, osteoporosis. Withdrawal should be gradually reduced. If anaphylactic shock occurs Withdraw immediately.

There may be sodium retention, adrenal insufficiency, gastrointestinal perforation or bleeding, slow wound healing, negative nitrogen balance caused by protein alienation, increased intracranial pressure, mental disorders, endocrine disorders, increased intraocular pressure, etc. ^[2] .

Contraindications to methylprednisolone

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. China Medical Health Network For premature infants, to avoid respiratory distress syndrome, dexamethasone was given to mothers before delivery to induce the formation of lung surfactant proteins in premature infants. Due to short-term application, the growth and development of young children were not seen. Has adverse effects.

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. Adrenal hyperfunction, hypertension, atherosclerosis, heart failure, diabetes, psychosis, epilepsy, postoperative, stomach, duodenal and corneal ulcers, intestinal diseases, chronic malnutrition should be avoided. Pregnant women are prohibited Viral infections should be used with caution. This product is not suitable for primary adrenal insufficiency. Use with caution in pregnant and lactating women ^[2] .

Methylprednisolone drug interactions

Non-steroidal anti-inflammatory analgesics can enhance the ulcer-causing effect of glucocorticoids. China Medical Health Network can enhance the liver toxicity of acetaminophen.

(3) Aminoglutethimide can inhibit the function of the adrenal cortex, accelerate the metabolism of dexamethasone, and shorten its half-life by 2 times.

When combined with amphotericin B or carbonic anhydrase inhibitors, hypokalemia can be aggravated. Attention should be paid to changes in potassium and cardiac function. Long-term combination with carbonic anhydrase inhibitors is prone to hypocalcemia and osteoporosis.

Combination with protein assimilation hormone can increase the incidence of edema and make acne worse.

Combined with antacids, it can reduce the absorption of prednisone or dexamethasone.

Long-term combination with anticholinergic drugs (such as atropine) can cause increased intraocular pressure.

Tricyclic antidepressants can worsen the psychiatric symptoms caused by glucocorticoids.

When combined with hypoglycemic agents such as insulin, the dose of hypoglycemic agents should be adjusted appropriately because it can increase blood sugar in patients with diabetes.

Thyroid hormone can increase the metabolic clearance rate of glucocorticoids, so when thyroid hormones or antithyroid drugs are combined with glucocorticoids, the dosage of the latter should be adjusted appropriately.

Combined with contraceptives or estrogen preparations; can strengthen the therapeutic effect and adverse reactions of glucocorticoids.

The combination of tincture with cardiac glycoside can increase the toxicity of digitalis and heart rhythm disturbance.

Combined with potassium-releasing diuretics, it can cause severe hypokalemia, and attenuate the sodium-releasing and diuretic effects of diuretics due to water and sodium retention.

The combination of tincture with ephedrine can enhance the metabolic clearance of glucocorticoids.

Combined with immunosuppressants can increase the risk of infection and may induce lymphoma or other lymphoplastic diseases.

Glucocorticoids, especially prednisolone, can increase isoniazid metabolism and excretion in the liver, reduce isoniazid blood concentration and efficacy.

Glucocorticoids can promote the metabolism of mexiletine in the body and reduce blood concentration.

Cooperating with salicylate can reduce the concentration of salicylate in plasma.

combined with growth hormone can inhibit the growth-promoting effect of the latter ^[1] .

Methylprednisolone clinical cases

The selected patients were randomly divided into the methylprednisolone treatment group and the control group. Fifty-five patients in the methylprednisolone group, aged 35 to 60 years, with an average of 4,315 years, were randomly divided into two groups, A and B. There were 54 cases in the control group, aged 33 to 61 years, with an average of 4215 years. There was no significant difference in gender, age, previous history, contusion site and area between the methylprednisolone group and the control group and between the methylprednisolone group A and B groups. . There were also no significant differences in neurological deficit scores (light, moderate, and severe) at admission, with no secondary hernias, and no medication outside the valve for 5 days.

After treatment, the difference in neurological deficit scores between the methylprednisolone group and the control group gradually decreased, but the advanced neurological functions such as consciousness and speech in the methylprednisolone group were significantly improved, and the average improvement points and severe disability mortality differences between the two groups were different. Significance (P <0105). Methylprednisolone group A and group B neurological deficit degree scores gradually decreased, but methylprednisolone group A improved significantly compared with group B, the average improvement points and severe disability mortality between the two groups were significantly different (P <0105) .

Methylprednisolone formulation specifications

Methylprednisolone Methylprednisolone tablets 2mg 4mg

Methylprednisolone acetate suspension injection (local injection) 1m1: 20mg 1m1: 40mg

Methylprednisolone sodium succinate for injection 53mg (equivalent to methyldehydrocortisone 40mg)

Intra-articular and intramuscular injection, 10-80 mg each time; orally, starting with 16-24 mg a day, divided into two times. The maintenance amount is 4-8 mg daily.

Methylprednisolone Expert Reviews

According to domestic reports, 38 cases of pediatric nephrotic syndrome were treated with methylprednisolone perfusion, 13-30 mg / kg once, and 250 ml of 5% glucose injection was added intravenously, once a day for 3 consecutive times as a course of treatment for 1 5 courses. After shock treatment, 20 cases of urinary protein turned negative, 16 cases of urinary protein decreased, and the total effective rate was 93.7% in the near future, which had better effect on primary nephropathy. Mainly used for the treatment of shock, nephrotic syndrome, lupus nephritis, etc., injection of joint cavity to treat arthritis, can get better results ^[1] .