Absorption, Distribution and Excretion
Corticosteroids are primarily metabolized in the liver and then excreted via the kidneys. Some topical corticosteroids and their metabolites are also excreted via bile.

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Metabolism/Metabolites

Hepatitis.

Protein Binding
80% Interaction: The hyperglycemic effect of cortisone may counteract the hypoglycemic effect of chlorpromazine…Concomitant use…may increase the risk of PPTN-induced gastric ulcers, but…there are no human clinical reports. …The interaction with acetaminophen may be similar. High-dose barbiturates (such as phenobarbital) can reduce the systemic effects of corticosteroids. …Pamethasone…may interact with… Phenytoin sodium…accelerates the metabolism of hydrocortisone…and methylprednisolone in the body. …Pamethasone…may also produce similar interactions. The effect of glucocorticoids on oral anticoagulant therapy varies from person to person; concomitant use of glucocorticoids has been reported to enhance or diminish the efficacy of oral anticoagulants. Patients taking both glucocorticoids and oral anticoagulants should be monitored (e.g., using coagulation indicators) to maintain the desired anticoagulant effect. /Corticosteroids/
For more complete data on interactions of the seven types of pamithas, please visit the HSDB record page.

[1]. Effects of corticosteroid treatment and inflammation on the cellular content of blood and exudate in mice. J Pathol. 1975 Jan;115(1):17-26.

Therapeutic Uses
Anti-inflammatory drug, steroid; synthetic glucocorticoid. Acetaminophen (barmethotrexate) is a synthetic analogue of hydrocortisone and is used to treat inflammatory or allergic diseases and other conditions that respond to glucocorticoids. In terms of anti-inflammatory effects, 2 mg of acetaminophen is approximately equivalent to 20 mg of hydrocortisone. It is 10 times more potent than cortisone, but this higher potency does not represent any particular advantage. /Acetaminophen acetate/ Veterinary use: For veterinary use only. Intrasynovial injection of 10 mg phosphate solution was effective only for the knee joint in dogs for one day. For more complete data on the therapeutic uses of acetaminophen (6 types), please visit the HSDB record page. Drug Warnings Adverse reactions are similar to other glucocorticoids. Increased appetite and weight gain occur in approximately one-third of patients. …lacking the sodium retention properties of hydrocortisone, although edema and hypertension are occasionally observed. Therefore, acetaminophen is not recommended for replacement therapy in adrenocortical insufficiency. ...Side effects of mineralocorticoids are rare...Low to moderate doses of the drug may only cause mild catabolic effects, such as protein loss and osteoporosis. /Acetaminophen Acetate/
The immunosuppressive effects of glucocorticoids may lead to the activation of latent infections or the exacerbation of secondary infections, including those caused by Candida, Mycobacteria, Toxoplasma gondii, Strongyloides stercoralis, Pneumocystis, Cryptococcus, Nocardia, or Entamoeba histolytica. Glucocorticoids should be used with caution in patients with known or suspected Strongyloides stercoralis (nematode) infection. In these patients, glucocorticoid-induced immunosuppression may lead to overinfection and dissemination of Strongyloides stercoralis with extensive larval migration, often accompanied by severe enteritis and potentially fatal Gram-negative bacterial sepsis. /Corticosteroids/
For more complete data on drug warnings for peramisone (of 29), please visit the HSDB record page.

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Pharmacodynamics
Peramisone is a glucocorticoid with the general characteristics of corticosteroids. Glucocorticoids are a class of steroid hormones characterized by their ability to bind to cortisol receptors and trigger a variety of important cardiovascular, metabolic, immune, and homeostatic effects. Glucocorticoids differ from mineralocorticoids and sex steroids in that they have different receptors, target cells, and functions. Strictly speaking, the term "corticosteroid" refers to both glucocorticoids and mineralocorticoids, but it is often used as a synonym for glucocorticoids. Glucocorticoids suppress cell-mediated immune responses. They act by inhibiting genes encoding cytokines IL-1, IL-2, IL-3, IL-4, IL-5, IL-6, IL-8, and TNF-α, with IL-2 being the most important. Reduced cytokine production limits T cell proliferation. Glucocorticoids also suppress humoral immunity, leading to a decrease in IL-2 expression and its receptor on B cells. This reduces B cell clonal expansion and antibody synthesis. Decreased IL-2 levels also result in a decrease in the number of activated T lymphocytes.

C22H29FO5

392.4674

392.2

53-33-8

5875

Typically exists as solid at room temperature

1.32 g/cm3

573.5ºC at 760 mmHg

228-241ºC

300.6ºC

1.589

1.751

3

6

2

28

790

9

OCC([C@]1([C@H](C)C[C@]2([C@@]3(C[C@]([H])(F)C4=CC(C=C[C@]4(C)[C@@]3([H])[C@H](C[C@]12C)O)=O)[H])[H])O)=O

MKPDWECBUAZOHP-AFYJWTTESA-N

InChI=1S/C22H29FO5/c1-11-6-14-13-8-16(23)15-7-12(25)4-5-20(15,2)19(13)17(26)9-21(14,3)22(11,28)18(27)10-24/h4-5,7,11,13-14,16-17,19,24,26,28H,6,8-10H2,1-3H3/t11-,13+,14+,16+,17+,19-,20+,21+,22+/m1/s1

(6S,8S,9S,10R,11S,13S,14S,16R,17R)-6-fluoro-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one

CS 1483; Paramethasone

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)