Fosphenytoin Sodium Pharmacology

Fosphenytoin Sodium

About Fosphenytoin Sodium
Fosphenytoin sodium is a prodrug intended for parenteral administration; phenytoin is its active metabolite. The anti convulsant effects of fosphenytoin are attributable to phenytoin.
Mechanism of Action of Fosphenytoin Sodium
Fosphenytoin is the prodrug of Phenytoin. Fosphenytoin undergoes hydrolysis and yields Phenytoin, phosphate and formaldehyde. The pharmacological and toxicological effect of Fosphenytoin includes those of Phenytoin.
Phenytoin acts on the motor cortex where it stabilizes neuronal membrane and inhibits the spread of seizure discharge. It prolongs the inactivated state of voltage sensitive neuronal sodium ion channel either by increasing the efflux or decreasing the influx of sodium ion across the cell membrane and inhibits the high frequency discharge.
At high concentrations Phenytoin
1. Enhances calcium binding to phospholipids in neuronal membrane and results in a more stable neuronal membrane.
2. It enhances the concentration of inhibitory neurotransmitter GABA
3. It inhibits the excitatory glutamate receptors.
All these indicate that Phenytoin limits the development of maximal seizure activity and reduce the spread of the seizure process from the active focus.
Antiarrhythmic action: Phenytoin exerts its action by normalizing sodium entry to Purkinje`s fibers in patient with cardiac glycoside induced arrhythmias.
Pharmacokinets of Fosphenytoin Sodium
Absorption: It is administered as parenteral route (IV infusion or IM injection). Distribution: It is very widely distributed in the body in highly protein bound form. Metabolism: Phenytoin derived from Fosphenytoin is metabolised in the liver to5- (p-Hydroxyphenyl)-5-phenylhydantoin. Excretion: Fosphenytoin is not excreted in urine
Onset of Action for Fosphenytoin Sodium
Duration of Action for Fosphenytoin Sodium
Half Life of Fosphenytoin Sodium
15 minutes (conversion half life of Fosphenytoin to Phenytoin)
Side Effects of Fosphenytoin Sodium
11.Heart failure
13.Dry mouth
16.Abdominal discomfort
Contra-indications of Fosphenytoin Sodium
1.Hypersensitivity to the Fosphenytoin and other Hydantoins
2.Atrioventricular block
3.Sinus Bradycardia
4.Sino Atrial block
5.Adams-Stokes syndrome
Special Precautions while taking Fosphenytoin Sodium
1.Hepatic impairment
2.Myocardial infarction
4.Renal impairment
5.Diabetic mellitus
Pregnancy Related Information
Old Age Related Information
Use with caution
Breast Feeding Related Information
Children Related Information
NEONATES: contraindicated
Indications for Fosphenytoin Sodium
1.Status epilepticus
2.Prevention and treatment of seizure during neurosurgery
3.Short term substitution for oral Phenytoin therapy
Interactions for Fosphenytoin Sodium
Typical Dosage for Fosphenytoin Sodium
Adults: IV/IM
Status epilepticus:
Loading dose: (IV) 15 - 20 mg Phenytoin sodium equivalent (PE)/kg
Infusion rate: 100 - 150 mg / minute
Maintenance dose: 4 - 6 mg PE /kg/day
Prevention and treatment of seizure during neurosurgery:
Loading dose: (IV/IM) 10 - 20 mg Phenytoin sodium equivalent (PE)/kg
Infusion rate below 150 mg / minute
Maintenance dose: 4 - 6 mg PE /kg/day
Short term substitution for oral Phenytoin therapy:
Total oral Phenytoin sodium daily dose (200 - 400 mg / day) is given as single IM or IV at an infusion rate below 150 mg / minute
Schedule of Fosphenytoin Sodium
Storage Requirements for Fosphenytoin Sodium
Store under refrigeration at 2- 8 degree C.
Effects of Missed Dosage of Fosphenytoin Sodium
Do not apply since injections are given by Health care professionals..
Effects of Overdose of Fosphenytoin Sodium
Give supportive measures and symptomatic treatment. Drug can be removed from the body by gastric lavage or inducing emesis. Maintain fluid and electrolyte balance. Haemodialysis or peritoneal dialysis can be done if necessary.

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