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Dexamethasone

Dexamethasone

Dexamethasone Wiki

Dexamethasone Covid-19

Peter Horby, Professor of Emerging Infectious Diseases in the Nuffield Department of Medicine, University of Oxford reported on June 16, 2020 preliminary trial results indicating ‘Dexamethasone is the first drug to be shown to improve survival in Covid-19. A total of 2104 patients were randomised to receive dexamethasone 6 mg once per day (either by mouth or by intravenous injection) for ten days and were compared with 4321 patients randomised to usual care alone. Among the patients who received usual care alone, 28-day mortality was highest in those who required ventilation (41%), intermediate in those patients who required oxygen only (25%), and lowest among those who did not require any respiratory intervention (13%). [34]

The Oxford University Recovery study[35] of various drugs that could help against Covid-19 reported that it improved survival of those who had Covid-19 and were receiving oxygen or on a ventilator. For those receiving oxygen it saved one patient’s life of 25 patients treated (cutting deaths by about a fifth). For those on ventilators, it saved a patient’s life of 8 patients treated (cutting deaths by about a third). In particular, it seems to help in staving off the damage caused by a cytokine storm in the most severely affected patients.

It has no effect on whether someone gets the virus, nor on the severity of effects if the virus is caught. Nor does it help those who are only mildly affected by the virus, indicating that it works by treating particular symptoms rather than the virus itself.[36]

The drug itself is quite inexpensive and widely available throughout the globe.[37] This makes it a promising solution for COVID-19 especially in developing countries.

Dexamethasone is a type of corticosteroid medication.[3] It is used in the treatment of many conditions, including rheumatic problems, a number of skin diseases, severe allergies, asthma, chronic obstructive lung disease, croup, brain swelling, eye pain following eye surgery, and along with antibiotics in tuberculosis.[3] In adrenocortical insufficiency, it should be used together with a medication that has greater mineralocorticoid effects such as fludrocortisone.[3] In preterm labor, it may be used to improve outcomes in the baby.[3] It may be taken by mouth, as an injection into a muscle, or intravenously.[3] The effects of dexamethasone are frequently seen within a day and last for about three days.[3]

The long-term use of dexamethasone may result in thrush, bone loss, cataracts, easy bruising, or muscle weakness.[3] It is pregnancy category C in the United States meaning use should be based on benefits being predicted to be greater than risks.[2] In Australia, the oral use is category A, meaning it has been frequently used in pregnancy and not been found to cause problems to the baby.[4] It should not be taken when breastfeeding.[3] Dexamethasone has anti-inflammatory and immunosuppressant effects.[3]

Dexamethasone was first made in 1957 and was approved for medical use in 1961.[5][6] It is on the World Health Organization’s List of Essential Medicines.[7] Dexamethasone is not expensive.[8] In the United States, a month of medication typically costs less than US$25.[3] In India, a course of treatment for preterm labor costs about US$0.5.[8] It is available in most areas of the world.[8] In 2016, it was the 259th most prescribed medication in the United States, with more than a million prescriptions.[9]

The World Health Organization Responded re: Dexamethasone:

The World Health Organization (WHO) welcomes the initial clinical trial results from the United Kingdom (UK) that show dexamethasone, a corticosteroid, can be lifesaving for patients who are critically ill with COVID-19. For patients on ventilators, the treatment was shown to reduce mortality by about one third, and for patients requiring only oxygen, mortality was cut by about one fifth, according to preliminary findings shared with WHO.

The benefit was only seen in patients seriously ill with COVID-19, and was not observed in patients with milder disease. 

“This is the first treatment to be shown to reduce mortality in patients with COVID-19 requiring oxygen or ventilator support,” said Dr Tedros Adhanom Ghebreyesus, WHO Director-General. “This is great news and I congratulate the Government of the UK, the University of Oxford, and the many hospitals and patients in the UK who have contributed to this lifesaving scientific breakthrough.”

Dexamethasone is a steroid that has been used since the 1960s to reduce inflammation in a range of conditions, including inflammatory disorders and certain cancers. It has been listed on the WHO Model List of Essential Medicines since 1977 in multiple formulations, and is currently off-patent and affordably available in most countries.

Courtesy : World Health Organization

Dexamethasone

Dexamethasone

Dexamethasone Medical uses

Dexamethasone phosphate injection vials

Anti-inflammatory

Dexamethasone is used to treat many inflammatory and autoimmune conditions, such as rheumatoid arthritis and bronchospasm.[10] Idiopathic thrombocytopenic purpura, a decrease in numbers of platelets due to an immune problem, responds to 40 mg daily for four days; it may be administered in 14-day cycles. It is unclear whether dexamethasone in this condition is significantly better than other glucocorticoids.[11]

It is also given in small amounts[12] before and/or after some forms of dental surgery, such as the extraction of the wisdom teeth, an operation which often leaves the patient with puffy, swollen cheeks.[medical citation needed]

Dexamethasone is commonly given as a treatment for croup in children, as a single dose can reduce the swelling of the airway to improve breathing and reduce discomfort.[13]

It is injected into the heel when treating plantar fasciitis, sometimes in conjunction with triamcinolone acetonide.[medical citation needed]

It is useful to counteract allergic anaphylactic shock, if given in high doses.[medical citation needed]

It is present in certain eye drops – particularly after eye surgery – and as a nasal spray, and certain ear drops (can be combined with an antibiotic and an antifungal). Dexamethasone intravitreal steroid implants have been approved by the FDA to treat ocular conditions such as diabetic macular edema, central retinal vein occlusion, and uveitis.[14] Dexamethasone has also been used with antibiotics to treat acute endophthalmitis.[15]

Dexamethasone is used in transvenous screw-in cardiac pacing leads to minimize the inflammatory response of the myocardium. The steroid is released into the myocardium as soon as the screw is extended and can play a significant role in minimizing the acute pacing threshold due to the reduction of inflammatory response. The typical quantity present in a lead tip is less than 1.0 mg.[medical citation needed]

Dexamethasone may be administered before antibiotics in cases of bacterial meningitis. It acts to reduce the inflammatory response of the body to the bacteria killed by the antibiotics (bacterial death releases proinflammatory mediators that can cause a response which is harmful), thus reducing hearing loss and neurological damage.[16]

A single vial of dexamethasone phosphate for injection

Cancer

People with cancer undergoing chemotherapy are often given dexamethasone to counteract certain side effects of their antitumor treatments. Dexamethasone can increase the antiemetic effect of 5-HT3 receptor antagonists, such as ondansetron.[17] The exact mechanism of this interaction is not well-defined, but it has been theorized that this effect may be due to, among many other causes, inhibition of prostaglandin synthesis, anti-inflammatory effects, immunosuppressive effects, decreased release of endogenous opioids, or a combination of the aforementioned.[18]

In brain tumors (primary or metastatic), dexamethasone is used to counteract the development of edema, which could eventually compress other brain structures. It is also given in cord compression, where a tumor is compressing the spinal cord.[medical citation needed]

Dexamethasone is also used as a direct chemotherapeutic agent in certain haematological malignancies, especially in the treatment of multiple myeloma, in which dexamethasone is given alone or in combination with other chemotherapeutic drugs, including most commonly with thalidomide (Thal-dex), lenalidomide, bortezomib (Velcade, Vel-dex),[19] or a combination of doxorubicin (Adriamycin) and vincristine or bortezomib/lenalidomide/dexamethasone.[medical citation needed]

Endocrine

Dexamethasone is the treatment for the very rare disorder of glucocorticoid resistance.[20][21]

In adrenal insufficiency and Addison’s disease, dexamethasone is prescribed when the patient does not respond well to prednisone or methylprednisolone.[medical citation needed]

It can be used in congenital adrenal hyperplasia in older adolescents and adults to suppress ACTH production. It is typically given at night.[22]

Pregnancy

Dexamethasone may be given to women at risk of delivering prematurely to promote maturation of the fetus’ lungs. This administration, given from day to one week before delivery, has been associated with low birth weight, although not with increased rates of neonatal death.[23]

Dexamethasone has also been used during pregnancy as an off-label prenatal treatment for the symptoms of congenital adrenal hyperplasia (CAH) in female babies. CAH causes a variety of physical abnormalities, notably ambiguous genitalia. Early prenatal CAH treatment has been shown to reduce some CAH symptoms, but it does not treat the underlying congenital disorder. This use is controversial: it is inadequately studied, only around one in ten of the foetuses of women treated are at risk of the condition, and serious adverse events have been documented.[24] Experimental use of dexamethasone in pregnancy for foetal CAH treatment was discontinued in Sweden when one in five cases suffered adverse events.[25]

A small clinical trial found long-term effects on verbal working memory among the small group of children treated prenatally, but the small number of test subjects means the study cannot be considered definitive.[26][27]

High-altitude illnesses

Dexamethasone is used in the treatment of high-altitude cerebral edema (HACE), as well as high-altitude pulmonary edema (HAPE). It is commonly carried on mountain-climbing expeditions to help climbers deal with complications of altitude sickness.[28][29]

Nausea and vomiting

Intravenous dexamethasone is effective for prevention of nausea and vomiting in people who had surgery and whose post-operative pain was treated with long-acting spinal or epidural spinal opioids.[30]

The combination of dexamethasone and a 5-HT3 receptor antagonist such as ondansetron is more effective than a 5-HT3 receptor antagonist alone in preventing postoperative nausea and vomiting.[31]

Dexamethasone, when used as an anti emetic during surgery, does not appear to increase rates of wound infection and it is unclear if it has an effect on wound healing.[32]

Sore throat

A single dose of dexamethasone or another steroid speeds improvement of a sore throat.[33]

Covid-19

Peter Horby, Professor of Emerging Infectious Diseases in the Nuffield Department of Medicine, University of Oxford reported on June 16, 2020 preliminary trial results indicating ‘Dexamethasone is the first drug to be shown to improve survival in Covid-19. A total of 2104 patients were randomised to receive dexamethasone 6 mg once per day (either by mouth or by intravenous injection) for ten days and were compared with 4321 patients randomised to usual care alone. Among the patients who received usual care alone, 28-day mortality was highest in those who required ventilation (41%), intermediate in those patients who required oxygen only (25%), and lowest among those who did not require any respiratory intervention (13%). [34]

The Oxford University Recovery study[35] of various drugs that could help against Covid-19 reported that it improved survival of those who had Covid-19 and were receiving oxygen or on a ventilator. For those receiving oxygen it saved one patient’s life of 25 patients treated (cutting deaths by about a fifth). For those on ventilators, it saved a patient’s life of 8 patients treated (cutting deaths by about a third). In particular, it seems to help in staving off the damage caused by a cytokine storm in the most severely affected patients.

It has no effect on whether someone gets the virus, nor on the severity of effects if the virus is caught. Nor does it help those who are only mildly affected by the virus, indicating that it works by treating particular symptoms rather than the virus itself.[36]

The drug itself is quite inexpensive and widely available throughout the globe.[37] This makes it a promising solution for COVID-19 especially in developing countries.

Contraindications

Contraindications of dexamethasone include,[38][39] but are not limited to:

Adverse effects

The exact incidence of the adverse effects of dexamethasone are not available, hence estimates have been made as to the incidence of the adverse effects below based on the adverse effects of related corticosteroids and on available documentation on dexamethasone.[39][40][41][42][43]

Common

  • Acne
  • Insomnia
  • Vertigo
  • Increased appetite
  • Weight gain
  • Impaired skin healing
  • Depression
  • Euphoria
  • Hypertension
  • Increased risk of infection
  • Raised intraocular pressure
  • Vomiting
  • Dyspepsia
  • Confusion
  • Amnesia
  • Irritability
  • Nausea
  • Malaise
  • Headaches
  • Cataract (in cases of long-term treatment it occurs in about 10% of patients)

Unknown frequency

Withdrawal

Sudden withdrawal after long-term treatment with corticosteroids can lead to:[39]

Interactions

Known drug interactions include:[39]

Pharmacology

As a glucocorticoid, dexamethasone is an agonist of the glucocorticoid receptor (GR). It has no mineralocorticoid activity.[44][45]

Chemistry

Dexamethasone is a synthetic pregnane corticosteroid and derivative of cortisol (hydrocortisone) and is also known as 1-dehydro-9α-fluoro-16α-methylhydrocortisone or as 9α-fluoro-11β,17α,21-trihydroxy-16α-methylpregna-1,4-diene-3,20-dione.[46][47]

Synthesis

To synthesize dexamethasone, 16β-methylprednisolone acetate is dehydrated to the 9,11-dehydro derivative.[48][49] This is then reacted with a source of hypobromite, such as basic N-bromosuccinimide, to form the 9α-bromo-11β-hydrin derivative, which is then ring-closed to an epoxide. A ring-opening reaction with hydrogen fluoride in tetrahydrofuran gives dexamethasone.[medical citation needed]

Dexamethasone

Dexamethasone synthesis

History

Dexamethasone was first synthesized in 1957.[5] It was introduced for medical use in 1958.[45]

Society and culture

Price

Dexamethasone is inexpensive.[8] In the United States a month of medication is typically priced less than US$25.[3] In India, a course of treatment for preterm labor is about US$0.50.[8] The drug is available in most areas of the world.[8]

Route

It may be taken by mouth, as a tablet or elixir, as an injection into a muscle, intravenously, or via an eye drop.[3]

Nonmedical use

Dexamethasone is given in legal Bangladesh brothels to prostitutes not yet of legal age, causing weight gain aimed at making them appear older and healthier to customers and police.[50]

Dexamethasone and most glucocorticoids are banned by sporting bodies including the World Anti-Doping Agency.[51]

Veterinary use

Combined with marbofloxacin and clotrimazole, dexamethasone is available under the name Aurizon, CAS number 115550-35-1, and used to treat difficult ear infections, especially in dogs. It can also be combined with trichlormethiazide to treat horses with swelling of distal limbs and general bruising.[52]

Courtesy : WikiPedia


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