What Factors Affect a Sufficient Cortisone Dose?

Cortisone is an adrenal corticosteroid. It is mainly used in the replacement of adrenal insufficiency and pituitary insufficiency. It can also be used in allergic and inflammatory diseases. This product can be quickly absorbed by the digestive tract, and converted into active hydrocortisone in liver tissues to exert its effect. It can quickly take effect after oral administration, while intramuscular injection is slower in absorption. Its pharmacological effects are similar to prednisone, but the efficacy is poor. Cortisone can cause changes in myocardial damage and ECG, as well as the risk of increased intracranial pressure.

Drug Name: Cortisone
Alias: Cortin
Foreign name: cortisone

Molecular formula: C21H28O5
Molecular weight: 360.444
Flash point: 311.2

Cortisone compounds

Cortisone Basic Information

Chinese name:

Chinese alias: Cortin

English name: cortisone

English alias: 17-alpha, 21-dihydroxypregn-4-ene-3, 11, 20-trione; 17, 21-dihydroxypregn-4-ene-3, 11, 20-trione; (8xi, 9xi, 14xi) -17 , 21-dihydroxypregn-4-ene-3,11,20-trione

CAS number: 53-06-5

EINECS number: 200-162-4

Molecular formula: C ₂₁ H ₂₈ O ₅

Molecular weight: 360.444

Exact mass: 360.19400

PSA: 91.67000

LogP: 1.98980

InChI: InChI = 1 / C21H28O5 / c1-19-7-5-13 (23) 9-12 (19) 3-4-14-15-6-8-21 (26,17 (25) 11-22) 20 (15,2) 10-16 (24) 18 (14) 19 / h9,14-15,18,22,26H, 3-8,10-11H2,1-2H3 / t14?, 15?, 18? , 19-, 20-, 21- / m0 / s1

Cortisone Information

Density: 1.28g / cm ³

Cortisone structure

Melting point: 220-228 ° C

Boiling point: 567.8 ° C at 760 mmHg

Flash point: 311.2 ° C

Vapor pressure: 2.96E-15mmHg at 25 ° C

Refractive index: 210 ° (C = 1, EtOH)

Storage conditions: -20ºC Freezer

Properties: Acetate is a white or almost white crystalline powder. It is odorless, tasteless at first, and has a lasting bitter taste. Soluble in chloroform, slightly soluble in ethanol or ether, insoluble in water.

Cortisone Safety Information

Customs code: 2937210000

WGK Germany: 3

Safety instructions: S22; S24 / 25

RTECS number: GM9020000 ^[1]

Cortisone production method

1. It can be separated from the adrenal extract, and it can also be made from bile acid and yam saponin.

Cortisone use

1. It is mainly used as an alternative treatment for adrenal insufficiency, but now hydrocortisone has been preferentially used for this disease. Because cortisone itself is inactive, it must be converted into hydrocortisone in the liver first, and certain liver diseases will affect its reliability.

2. Medicinal drugs are easily absorbed by the skin, and are used for the physical treatment of acute and chronic eczema, pruritus and various dermatitis. It is also used in lotions, creams, and hair growth waters to regulate the balance of electrolytes and water in the body, and the metabolism of sugar and proteins. Has anti-inflammatory, anti-allergic and anti-granulation effects ^[1] .

Cortisone drug description

Cortisone pharmacological action

Cortisone

The effect and use of this product are similar to that of hydrocortisone, but the efficacy is poor and the adverse reactions are large. Clinically, it is mainly used as an alternative treatment for adrenal insufficiency. Promote the conversion of protein into sugar, reduce the use of glucose, increase liver glycogen, and increase blood sugar. And has the role of water and sodium retention and potassium excretion.

Cortisone pharmacokinetics

Cortisone is a glucocorticoid secreted by the adrenal cortex. It is inactive and needs to be metabolized to hydrocortisone in the body to function. It also has a certain degree of mineralocorticoid effect. Cortisone acetate is easily absorbed orally from the gastrointestinal tract and reaches a peak blood concentration in about 1 hour. It is rapidly metabolized into active hydrocortisone in the liver, and its plasma biological effect t1 / 2 is only 30min. Intramuscular suspension is absorbed much more slowly than oral.

Cortisone indications

It is mainly used as an alternative treatment for adrenal insufficiency, but now hydrocortisone has been preferentially used for this disease. Because cortisone itself is inactive, it must first be converted to hydrocortisone in the liver, and certain liver diseases will affect the reliability of its action.

Cortisone contraindications

1. Those who are allergic to adrenal corticosteroids.

2. Within 2 weeks before and after vaccination.

3. Patients with viral skin diseases.

4. Patients with corneal ulcer.

5. Patients with severe mental illness and epilepsy.

6. Patients with active peptic ulcer.

7. Recent gastrointestinal anastomosis.

8. Wound repair period.

9. Patients with fractures.

10. Hyperadrenal function.

11. Hepatic insufficiency (because cortisone requires liver activation).

12. More severe osteoporosis.

13. Patients with obvious diabetes.

14. Patients with severe hypertension.

15. Viral, bacterial, and fungal infections that cannot be controlled with antibacterials ^[2] .

Cortisone precautions

1. (1) heart disease or acute heart failure; (2) diabetes; (3) diverticulitis; (4) emotional instability and psychotic tendencies; (5) systemic fungal infections; (6) glaucoma; (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 ulcers; (14) gastritis or esophagitis; (15) impaired renal function or stones; (16) tuberculosis; (17) children; (18) pregnant and lactating women.

2. If there is a severe deficiency of aldosterone in the treated adrenal insufficiency, the combination of fludrocortisone and sodium chloride is often required;

3. Due to the strong activity of cortisone sodium, it is generally not the first choice for anti-inflammatory and anti-allergy;

4. Local topical or intra-articular injection of cortisone through skin is invalid.

5. Shake well before using eye drops; 6. For other precautions, refer to the relevant content of hydrocortisone ^[2] .

Cortisone dosage

Alternative treatment: 12.5 25mg each time, 25 100mg per day, divided into doses. Intramuscular injection: 25 to 125 mg each time, 1 to 2 times daily.

Cortisone adverse reactions

Hydrocortisone

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.

(1) Systemic allergic reactions, including swelling of the face, nasal mucosa, eyelids, urticaria, shortness of breath, chest tightness, and wheezing, may occur with rapid intravenous administration of large doses.

(2) Long-term medication can cause the following side effects: face and body shape of iatrogenic Cushing syndrome, weight gain, lower limb edema, purple streaks, tendency to bleeding, poor wound healing, acne, menstrual disorders, humeral or femoral head ischemia Necrosis, osteoporosis or fractures (including vertebral compression fractures, long bone pathological fractures), muscle weakness, muscular atrophy, hypokalemia syndrome, gastrointestinal irritation (nausea, vomiting), pancreatitis, peptic ulcer or bowel Perforation, growth inhibition in children, glaucoma, cataracts, benign intracranial pressure syndrome, impaired glucose tolerance, and exacerbation of diabetes.

(3) Patients may have mental symptoms: 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.

(4) Concurrent 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 hormone therapy, and its occurrence is related to factors such as preparation, dose, course of treatment and so on. 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.

Prednisolone acetate

(5) Syndromes after glucocorticoid withdrawal can have various conditions as follows. 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. The hypothalamic corticotropin releasing hormone (CRF) secretion is restored and increased; 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.

Cortisone Drug Interactions

Hydrocortisone

Cortisone preparation

Tablets: 5 mg / tablet, 10 mg / tablet, 25 mg / tablet. Injection (suspension): 125mg / 5ml.

Cortisone Expert Reviews

It is one of the main alternative medicines for the treatment of adrenal insufficiency, and the effect is definitely ^[2] .

Cortisone Discovery

Hydrocortisone acetate Today, people with a little medical knowledge know that rheumatoid arthritis is an autoimmune disease. The patient's immune system mistakes his joint tissue as an enemy and attacks it. As a result, the joint is inflamed, red, swollen, stiff, and severe. The patient was unable to walk at all, lost mobility, and was very distressed. But at the beginning of the last century, rheumatoid arthritis was also thought to be caused by some kind of bacterial infection. Fortunately, antibiotics had not been found at the time, otherwise doctors would definitely give every patient with arthritis a penicillin.

arthritis

In 1928, the director of the Department of Pharmacy, Mayo School of Medicine, University of Minnesota, Philip. PhilipHench received a strange patient. The 65-year-old patient was actually a doctor at the hospital, and he told him a strange thing: Since he had jaundice, his rheumatoid arthritis symptoms Disappeared. After 4 weeks, his jaundice was cured, but his arthritis did not recur until 7 months later.

Although Hengqi felt that this was a little strange, he believed in his colleagues because the doctor's description of his illness was definitely more reliable than that of ordinary patients. Since then he has kept an eye on and started paying close attention to the relationship between jaundice and arthritis. Soon he found several similar patients, and he also observed a more bizarre phenomenon: once a woman with arthritis becomes pregnant, her symptoms will be relieved immediately.

Various indications indicate that for these patients, the cure for arthritis is not likely to be anti-infective drugs, but some kind of endocrine-related substance, which Hengqi calls "substance X". He speculated that the bile of jaundice patients might contain this mysterious substance X, which is like a certain hormone and will increase with pregnancy. His idea violated the consensus of the medical community at that time. No one believed him. He had to silently embark on the journey of searching for substance X. It was 20 years away.

Hengqi couldn't think of any other good method. He had to give arthritis patients all kinds of substances that may contain substance X, including bile, bile crystal salt and liver extract. He even transfused blood from jaundice patients directly to arthritis patients, but No effect at all.

Coincidentally, a colleague of Hengqi was studying hormones at the time. This person's name is Edward. Edward Kendall, a chemist, was the first to purify thyroxine. When he met Hengqi, he was studying the adrenal glands, and purified four kinds of substances secreted by the adrenal glands, named compounds A, B, E, and F, respectively. He suggested that Hengqi try these compounds. Unfortunately, the purification process at that time was very poor, and it was difficult to get enough compounds for clinical experiments.

At this time World War II broke out, the U.S. military was informed that the Luftwaffe was purchasing a large amount of bovine adrenal glands in Argentina and was preparing to give their pilots an injection to improve their tolerance to hypoxia. Adrenaline-injected pilots are said to be able to fly the plane to an altitude of 13,000 meters without being choked by hypoxia. Therefore, the US military immediately allocated a large sum of money and began to study how to purify adrenaline on a large scale. The experiment was carried out for a long time, and it was not until 1948 that scientists at Merck Pharmaceuticals overcome the difficulties, got a few grams of Compound E, and passed it to Hengqi.

On July 26, 1948, Hengqi injected 100 mg of Compound E into a female patient with severe rheumatoid arthritis. The patient's symptoms improved significantly after 2 days, and she was able to walk on her own. Previously, she could only use a wheelchair. Later, it was pointed out that Hengqi violated the convention and used an excessive dose of Compound E, otherwise the effect would not be so significant. Hengqi filmed the patient's appearance before and after treatment, and played it at a scientific conference the following year. After the show, the audience stood and applauded. Everyone was stunned by the discovery. This is the first time that humans have cured an incurable disease with an endogenous chemical, which indicates that modern medicine can not only use foreign fungicides (antibiotics) to treat diseases, but also find ways to mobilize the human body itself Disease resistance. This compound E was later named cortisone. Hinch and Kendall were awarded the Nobel Prize for Medicine in 1950 for discovering the efficacy of cortisone, setting the fastest record for the Nobel Prize.

However, Hengqi was not elated because he knew that cortisone could only slow down the symptoms of arthritis and not completely cure it. The patient came back as soon as the drug was stopped. Not only that, but cortisone also has strong side effects, which often outweigh the benefits. As a result, Cortisone was discontinued before it was used on a large scale in the clinic.

After 20 years of hard work, Hengqi got only a hormone that could not be used for medicine? Absolutely not. A series of subsequent clinical trials have shown that cortisone has significant effects on diseases such as drug allergy, chronic asthma, systemic lupus erythematosus, nodular polyarteritis and irisitis. The treatment of these diseases does not require a large dose of cortisone, but only requires topical application or short-term medication to work, thus greatly reducing the side effects of cortisone.

Nowadays, cortisone and its derivatives are called "hormones" and are widely used in the medical field. Those who have benefited from this must thank Hengqi. It was precisely because he was not superstitious about dogma, believed the facts, and persisted for 20 years that he brought a magical "universal medicine" to human beings.

Cortisone Development

Cortisone was of great interest to scientists during the Second World War. Both sides of the war believe that cortisone can help ease the emotional depression known as "war fatigue." But no pharmaceutical company can produce cortisone in large quantities. Later in 1944, an American chemist named Lewis Salet managed to extract cortisone from the bile of cattle.

Cortisone appeared too late to play a role in World War II. However, Hengqi and Kader decided to try it for rheumatoid arthritis patients. The effect was surprising. For this reason, they won the Nobel Prize. Cortisone can reduce inflammation and allergic reactions, so it was quickly used in many diseases treatment.

However, it was soon discovered that although cortisone reduced the pain of rheumatoid arthritis, it could not stop the development of the disease, and if patients took cortisone for too long, it could cause diabetes or hypertension. Therefore, the dose of cortisone is strictly controlled.

In the 1950s, when surgeons began transplanting allogeneic kidneys, hearts, or skin, they discovered new uses for cortisone. Under normal circumstances, the body's immune system rejects anything it thinks is a foreign object. This rejection rejects the transplanted organ. Cortisone helps alleviate this rejection.

Cortisone Cortisone Eye Drops

Indications: For allergic conjunctivitis.

Dosage: eye drops. Drop this product into the conjunctival sac, 1-2 drops at a time, 3-4 times a day. Shake well before use.

Dosage form: eye drops

Adverse reactions:

1. Long-term or heavy use can cause increased intraocular pressure or glaucoma, optic nerve damage, visual field defects, and cataracts; excessive use can cause systemic adverse reactions.

2. Long-term use can cause secondary eye infections.

Contraindications: Disabled in patients with simple or ulcerative keratitis.

Precautions:

1. Do not touch the nozzle with your hands and eyes during eye drops.

2. Pregnant and lactating women should not use it frequently and for a long time.

3. Glaucoma patients should be used under the guidance of a physician.

4. This product should not be used for a long time, and the continuous use should not exceed 2 weeks. If the symptoms are not relieved, the drug should be discontinued.

5. When the eye is infected, this product should not be used alone. It should be combined with antibacterial drugs under the guidance of a doctor or pharmacist.

6. For those who are allergic to this product, it is forbidden, and those with allergies should be used with caution.

7. It is forbidden to use this product when its properties are changed.

8. Keep this product out of the reach of children.

9. Children must use under adult supervision.

10. If you are using other medicines, please consult your physician or pharmacist before using this product.

Properties: This product is a suspension of fine particles. After standing, the fine particles sink and shake to form a uniform milky white suspension.

Drug interactions: 1. When using this product, do not use other eye drops at the same time.

2. Drug interaction may occur if used with other drugs at the same time, please consult your doctor or pharmacist for details.

Storage: shading, sealed (10 ~ 30 ) storage.

Drug validity: 24 months

Implementation Standards: Ministry of Standards, Volume II, Volume 5

Manual revision date: 2007-05-28 ^[3]