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Fosphenytoin (disodium)

Cat. No. M20961
Fosphenytoin (disodium) Structure
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Biological Activity

Fosphenytoin (disodium) is the sodium salt form of fosphenytoin, a prodrug that is hydrolyzed to the anticonvulsant phenytoin upon parental administration.

Chemical Information
Molecular Weight 406.24
Formula C16H13N2Na2O6P
CAS Number 92134-98-0
Solubility (25°C) DMSO 81 mg/mL
Water 81 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] L B Cohen. Aliment Pharmacol Ther. Clinical trial: a dose-response study of fospropofol disodium for moderate sedation during colonoscopy

[2] S A Chan, et al. Acta Neurochir (Wien). Fosphenytoin reduces hippocampal neuronal damage in rat following transient global ischemia

[3] R E Ramsay, et al. Neurology. Intravenous administration of fosphenytoin: options for the management of seizures

[4] C M Lai, et al. Res Commun Mol Pathol Pharmacol. Binding of fosphenytoin, phosphate ester pro drug of phenytoin, to human serum proteins and competitive binding with carbamazepine, diazepam, phenobarbital, phenylbutazone, phenytoin, valproic acid or warfarin

[5] B D Jamerson, et al. Epilepsia. Absolute bioavailability of phenytoin after 3-phosphoryloxymethyl phenytoin disodium (ACC-9653) administration to humans

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