What is Methylprednisolone?
Methylprednisolone is a glucocorticoid that is used for treating conditions like arthritis, renal diseases, certain allergic reactions, and immune system diseases and disorders. It works by minimizing the immune system’s response to various threats like the aforementioned diseases.
First synthesized in 1957, methylprednisolone is the 4th most prescribed drug in the United States. It has been used extensively during the COVID-19 pandemic.
Definition
Methylprednisolone is a synthetic glucocorticoid that is prescribed for inflammatory conditions. Apart from that, it has immunosuppressive effects as well.
Chemical & Physical Features
IUPAC name: (6S,8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-17-(2-hydroxyacetyl)-6,10,13-trimethyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
CAS: 83-43-2
Molecular formula: C22H30O5
Molecular weight: 374.5
Form: Solid crystals
Solubility: 120 mg/L (at 25 °C)
Brand Names
Medrol, Medrol Dosepak, Medrone, Medrate
Methylprednisolone Forms and Specifications
From a pharmaceutical point of view, there are two key forms of methylprednisolone. These are methylprednisolone sodium succinate powder and methylprednisolone acetate powder.
Methylprednisolone Sodium Succinate Powder
The chemical name for the succinate variant of methylprednisolone is pregna-1, 4-diene-3, 20 Dione, 21-(3-carboxy-1-oxopropoxy)-11, 17-dihydroxy-6-methyl-monosodium salt. It is available commercially by the name of SOLU-MEDROL. Representative of esterification of sodium succinate with methylprednisolone, this API of SOLU-MEDROL exists as an amorphous solid. White and odorless, it is highly soluble in water and alcohol. This property makes it an ideal candidate for intravenous administration in scenarios that demand a rapid injection of methylprednisolone into the bloodstream.
Methylprednisolone Acetate Powder
The chemical name for methylprednisolone acetate is pregna-1, 4-diene-3, 20-dione, 21-(acetyloxy) - 11, 17-dihydroxy-6-methyl-, (6α, 11ß). It is available commercially by the name of DEPO-MEDROL. Insoluble in water but sparingly soluble in liquids like alcohol, acetone, and ether, methylprednisolone acetate exists as a white crystalline powder. Its indications include intramuscular administration, intra-articular administration, and intralesional administration.
Methylprednisolone Acetate vs Succinate
DEPO MEDROL is often used for managing allergic reactions, dermatological diseases, endocrinal disorders, gastrointestinal disorders, hematologic disorders, and certain neoplastic diseases like leukaemia. SOLU-MEDROL is used when the oral therapy option is not feasible for the aforementioned conditions. Hence, an intravenous injection of the succinate API is used for managing such disorders and diseases.
Methylprednisolone vs Prednisone
While both of these drugs hail from the same tribe i.e. corticosteroids, several differences must be kept in mind. Despite the similarity that exists between the two drugs, a major difference lies in the relative effective strength. Methylprednisolone is a little more potent than prednisone, its 8mg equal 10 mg of prednisolone. Also, methylprednisolone is available as an injectable solution while prednisone is available as an oral solution. And of course, the difference in branding is also an important one. Methylprednisolone is sold as Medrol/Depo-Medrol/Solu-Medrol while prednisolone is sold under the brand name of Rayos.
Mechanism of Action of Methylprednisolone
Corticosteroids work by either decreasing vasodilation, increasing capillary permeability, or by decreasing leukocytic migration to the inflammation site. Research shows that a lower dose of corticosteroids leads to an anti-inflammatory effect while the immunosuppressive effects are predominant at higher doses. Corticosteroids bind to the glucocorticoid receptors, a binding that leads to several signalling pathways. Key cellular events that stem from this binding include inhibition of neutrophil apoptosis, inhibition of phospholipase A2 and promotion of anti-inflammatory genes like interleukin-10.
Methylprednisolone Manufacturing Process
A crystallization method is used for the industrial production of methylprednisolone. Methylprednisolone succinate is crystallized, which helps increase the purity of the compound while reducing the impurity content percentage. This method produces lyophilized powder of premium quality which is used in methylprednisolone injections available in the market. The method for the production of methylprednisolone with acetate API differs slightly, but the main technology remains the same.
What is Methylprednisolone Used For?
There are several conditions for which methylprednisolone is used. We talk about a few uses of methylprednisolone briefly in the following lines of this article.
Methylprednisolone for poison ivy
Poison ivy is an allergic Asian/ North American plant that often leads to rashes on the skin. Corticosteroids like methylprednisolone can help during the poison ivy season since they can help with the swelling that follows the reaction.
Methylprednisolone for Back Pain
While medications like methylprednisolone or prednisone can be used for relieving pain that is associated with inflammation, these drugs are not commonly prescribed for managing or alleviating back pain.
Other uses
Methylprednisolone is used for treating conditions like arthritis, renal diseases, certain allergic reactions, and immune system diseases and disorders.
Methylprednisolone Dosage
The drug is available in dosages of varying potency in various forms. For example, the tablets are available in 2, 4,8,16, and 32 mg, while the injectable suspensions are available in the 20, 40, and 80 mg/mL suspension. As for the powder form used in injection, 40, 125, 500 mg are the most popular picks. The exact dosage varies from patient to patient, depending on various factors such as patient age, condition, and corticosteroid tolerance.
Methylprednisolone Side Effects
Some of the side effects associated with this drug include nausea, heartburn, and headache, and increased sweating.
Methylprednisolone API price
Although the exact price depends upon several trade variables, the average price of methylprednisolone API is estimated at around 1850 USD/ KG.
Methylprednisolone API Manufacturers in China
Below are some trustworthy active pharma ingredients manufacturers in China.
Guangzhou Bairui Medicine Co., Ltd
Been in the business of pharmaceutical-grade API manufacturing for many years, this company is a trustworthy manufacturer of methylprednisolone.
Zhejiang Shenzhou Pharmaceutical Co., Ltd
This is a company that specializes in the production of steroid API and intermediates. It supplies the aforementioned products at a global level and has been in business since 1989.
Zhejiang Xianju Pharmaceutical Co., Ltd.
Producing more than 100 premium quality API since the last five decades, this company is yet another reputable name in the field of methylprednisolone API production.
Pharmasources
Are you looking for more manufacturers of methylprednisolone API? At pharmasources, you can search for hundreds of suppliers and manufacturers of methylprednisolone API in China, all of which are producing premium quality drug API. Learn more about their modus operandi at pharmasources.
FAQs
Why take methylprednisolone before breakfast?
Because doing this will mimic the body’s production of cortisone.
How long does methylprednisolone stay in your system?
It leaves the system completely after 13-20 hours.
Is methylprednisolone a strong steroid?
Yes. It is five times stronger than cortisol and four times stronger than prednisone.
References
https://www.webmd.com/drugs/2/drug-6470/methylprednisolone-oral/details
https://pubchem.ncbi.nlm.nih.gov/compound/Methylprednisolone#section=MeSH-Entry-Terms
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/011856s103s104lbl.pdf
https://www.rxlist.com/depo-medrol-drug.htm#dosage
https://www.healthline.com/health/rheumatoid-arthritis/methylprednisolone-vs-prednisone
https://patents.google.com/patent/CN103159817A/en
https://reference.medscape.com/drug/medrol-medrol-dosepak-methylprednisolone-342746
https://www.pharmacompass.com/price/methylprednisolone
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