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

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Metabolism / Metabolites
Hepatic.

Protein Binding
80%

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Interactions
HYPERGLYCEMIC ACTION OF CORTISONE MAY OFFSET THE HYPOGLYCEMIC EFFECT OF CHLORPROPAMIDE...CONCURRENT ADMIN...MAY INCR LIKELIHOOD OF PPTN GASTRIC ULCER, BUT...NO CLINICAL REPORTS OF THIS...IN HUMANS. ...PARAMETHASONE /SHOULD INTERACT IN SIMILAR MANNER/.
SYSTEMIC EFFECTS OF ADMIN CORTICOSTEROIDS...MAY BE DIMINISHED BY LARGE DOSES OF BARBITURATES SUCH AS PHENOBARBITAL. ...PARAMETHASONE...MAY BE EXPECTED TO INTERACT...
PHENYTOIN...INCR METAB OF HYDROCORTISONE...& METHYLPREDNISOLONE IN HUMANS. ...LIKELY THAT...PARAMETHASONE...WOULD INTERACT SIMILARLY.
The effect of glucocorticoids on oral anticoagulant therapy is variable, and the efficacy of oral anticoagulants has been reported to be enhanced or diminished with concomitant glucocorticoid administration. Patients receiving glucocorticoids and oral anticoagulants concomitantly should be monitored (e.g., using coagulation indices) in order to maintain desired anticoagulant effect. /Corticosteroids/
For more Interactions (Complete) data for PARAMETHASONE (7 total), 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 Agents, Steroidal; Glucocorticoids, Synthetic
PARAMETHASONE, A SYNTHETIC ANALOGUE OF HYDROCORTISONE, IS USEFUL IN TREATING INFLAMMATORY OR ALLERGIC CONDITIONS & OTHER DISEASES THAT RESPOND TO GLUCOCORTICOIDS. IN ANTI-INFLAMMATORY EFFECT, 2 MG PARAMETHASONE IS APPROX EQUIVALENT TO 20 MG HYDROCORTISONE.
IT IS 10 TIMES AS POTENT AS CORTISONE, BUT POTENCY DOES NOT CONFER ANY PARTICULAR ADVANTAGES. /PARAMETHASONE ACETATE/
VET: LIMITED, IN VETERINARY MEDICINE. INTRASYNOVIALLY, 10 MG OF SOL PHOSPHATE ESTER WAS ONLY EFFECTIVE FOR 1 DAY IN STIFLE JOINT OF DOGS.
For more Therapeutic Uses (Complete) data for PARAMETHASONE (6 total), please visit the HSDB record page.

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Drug Warnings
UNDESIREABLE EFFECTS ARE SIMILAR TO THOSE OBSERVED WITH OTHER GLUCOCORTICOIDS. INCR APPETITE WITH WT GAIN OCCURS IN ABOUT 1/3 PT.
...LACKS THE SODIUM-RETAINING PROPERTIES OF HYDROCORTISONE, ALTHOUGH EDEMA & HYPERTENSION ARE OBSERVED INFREQUENTLY. THUS, PARAMETHASONE IS NOT RECOMMENDED FOR REPLACEMENT THERAPY IN ADRENOCORTICAL INSUFFICIENCY.
...ALMOST DEVOID OF MINERALOCORTICOID SIDE EFFECTS... CATABOLIC EFFECTS, SUCH AS PROTEIN DEPLETION & OSTEOPOROSIS, ARE ONLY MODERATE WITH LOW TO MODERATE DOSES OF THE DRUG. /PARAMETHASONE ACETATE/
The immunosuppressive effects of glucocorticoids may result in activation of latent infection or exacerbation of intercurrent infections, including those caused by Candida, Mycobacterium, Toxoplasma, Strongyloides, Pneumocystis, Cryptococcus, Nocardia, or Ameba. Glucocorticoids should be used with great care in patients with known or suspected Strongyloides (threadworm) infection. In such patients, glucocorticoid-induced immunosuppression may lead to Strongyloides hyperinfection and dissemination with widespread larval migration, often accompanied by severe enterocolitis and potentially fatal gram-negative septicemia. /Corticosteroids/
For more Drug Warnings (Complete) data for PARAMETHASONE (29 total), please visit the HSDB record page.

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Pharmacodynamics
Paramethasone is a glucocorticoid with the general properties of corticosteroids. Glucocorticoids are a class of steroid hormones characterised by an ability to bind with the cortisol receptor and trigger a variety of important cardiovascular, metabolic, immunologic and homeostatic effects. Glucocorticoids are distinguished from mineralocorticoids and sex steroids by having different receptors, target cells, and effects. Technically, the term corticosteroid refers to both glucocorticoids and mineralocorticoids, but is often used as a synonym for glucocorticoid. Glucocorticoids suppress cell-mediated immunity. They act by inhibiting genes that code for the cytokines IL-1, IL-2, IL-3, IL-4, IL-5, IL-6, IL-8 and TNF-alpha, the most important of which is the IL-2. Reduced cytokine production limits T cell proliferation. Glucocorticoids also suppress humoral immunity, causing B cells to express lower amounts of IL-2 and IL-2 receptors. This diminishes both B cell clonal expansion and antibody synthesis. The diminished amounts of IL-2 also leads to fewer T lymphocyte cells being activated.

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.)