Phenytoin: Medication Information and Guidelines

The recommended dose of phenytoin varies depending on the indication being treated, the patient’s age, weight, and response to treatment. For the management of epilepsy, the typical starting dose for adults is 100 mg orally three times daily, with titration to a maintenance dose of 300 to 400 mg daily based on individual patient response and tolerability. For pediatric patients, the starting dose is 5 mg/kg/day orally in divided doses, with titration to a maintenance dose of 4 to 8 mg/kg/day. Phenytoin should be administered with or without food, as directed by a healthcare provider. Dosage adjustments may be necessary in elderly patients or those with hepatic impairment. Consult with a healthcare provider for personalized dosing recommendations.

Frequency of Administration

Phenytoin is typically administered orally in divided doses two to three times daily, depending on the indication being treated and individual patient factors. The dosing frequency may be adjusted based on the patient’s response to treatment, tolerability, and seizure control. Patients should take phenytoin exactly as prescribed by their healthcare provider and follow the recommended dosing schedule to achieve optimal therapeutic outcomes. Do not exceed the prescribed dose or duration of treatment without medical supervision.

Route of Administration

Phenytoin is administered orally in the form of capsules, chewable tablets, or oral suspension, which should be swallowed whole with a full glass of water to facilitate drug absorption and ensure proper dosing. Phenytoin capsules and tablets should not be chewed, crushed, or opened, as this may alter the drug’s pharmacokinetics and decrease efficacy. Phenytoin may be taken with or without food, as directed by a healthcare provider. The oral suspension should be measured with an appropriate dosing device to ensure accurate dosing. Consult with a healthcare provider for guidance on proper administration techniques and dosing instructions.

Mechanism of Action (MOA)

Phenytoin exerts its pharmacological effects primarily by blocking voltage-gated sodium channels in neuronal membranes, thereby stabilizing the neuronal membrane potential and reducing the generation and spread of action potentials. By inhibiting excessive neuronal firing, phenytoin suppresses abnormal electrical activity in the brain associated with seizure disorders, such as epilepsy. Phenytoin also modulates the release of neurotransmitters, such as glutamate and gamma-aminobutyric acid (GABA), and may exert antiepileptic effects through additional mechanisms, including enhancement of GABA-mediated inhibition and reduction of glutamatergic excitotoxicity.

Pharmacokinetics (PK)

The pharmacokinetics of phenytoin are complex and variable, with nonlinear, saturable absorption and dose-dependent metabolism. Phenytoin is well absorbed after oral administration, with peak plasma concentrations achieved within 1 to 4 hours. The bioavailability of phenytoin is approximately 90% and is not significantly affected by food intake. Phenytoin is extensively bound to plasma proteins and undergoes hepatic metabolism via the cytochrome P450 enzyme system, primarily CYP2C9, to form inactive metabolites. The elimination half-life of phenytoin is dose-dependent and ranges from 7 to 42 hours, with longer half-lives observed at higher doses due to saturation of metabolic pathways. Dosage adjustments are necessary in patients with hepatic impairment or those taking concomitant medications that may interact with phenytoin.

Pharmacodynamics (PD)

Phenytoin exerts its pharmacological effects primarily by blocking voltage-gated sodium channels in neuronal membranes, thereby stabilizing the neuronal membrane potential and reducing the generation and spread of action potentials. By inhibiting excessive neuronal firing, phenytoin suppresses abnormal electrical activity in the brain associated with seizure disorders, such as epilepsy. Phenytoin also modulates the release of neurotransmitters, such as glutamate and gamma-aminobutyric acid (GABA), and may exert antiepileptic effects through additional mechanisms, including enhancement of GABA-mediated inhibition and reduction of glutamatergic excitotoxicity.

Pathophysiology

Epilepsy is a chronic neurological disorder characterized by recurrent, unprovoked seizures due to abnormal electrical activity in the brain. Phenytoin is a first-line antiepileptic drug used for the management of partial seizures, generalized tonic-clonic seizures, and status epilepticus. Phenytoin stabilizes neuronal membranes by blocking voltage-gated sodium channels, thereby reducing the generation and spread of abnormal electrical discharges that underlie seizure activity. Phenytoin therapy should be individualized based on the specific seizure type, patient factors, and treatment goals. The goal of phenytoin therapy is to achieve seizure control while minimizing adverse effects and drug interactions.

Primary Indications

Phenytoin is indicated for the management of various seizure disorders, including partial seizures, generalized tonic-clonic seizures, and status epilepticus, in adults and pediatric patients. Phenytoin therapy may be used as monotherapy or adjunctive therapy in combination with other antiepileptic drugs, depending on the patient’s seizure type, response to treatment, and tolerability. Phenytoin should be initiated and titrated to the lowest effective dose based on individual patient response and seizure control. The goal of phenytoin therapy is to achieve seizure freedom or significant reduction in seizure frequency while minimizing adverse effects and drug interactions.

Contraindications

Contraindications to phenytoin use include hypersensitivity to phenytoin or any component of the formulation. Phenytoin should not be used in patients with a history of hypersensitivity reactions, such as Stevens-Johnson syndrome or toxic epidermal necrolysis, to phenytoin or other antiepileptic drugs. Use caution when prescribing phenytoin to patients with a history of cardiac arrhythmias, as phenytoin may exacerbate conduction abnormalities or induce arrhythmias. Phenytoin is contraindicated in patients with a history of porphyria or hepatic impairment, as phenytoin metabolism may be impaired, leading to drug accumulation and potential toxicity. Consult with a healthcare provider for guidance on appropriate patient selection and monitoring.

Purpose of Taking Medication

The purpose of phenytoin therapy is to achieve seizure control and prevent the recurrence of epileptic seizures in patients with epilepsy or seizure disorders. Phenytoin exerts its pharmacological effects primarily by blocking voltage-gated sodium channels in neuronal membranes, thereby stabilizing the neuronal membrane potential and reducing the generation and spread of abnormal electrical discharges that underlie seizure activity. The overall goal of phenytoin therapy is to improve quality of life, enhance functional status, and minimize the impact of epilepsy on daily activities and social functioning.

Usage Instructions

Phenytoin should be taken exactly as prescribed by your healthcare provider, typically in divided doses two to three times daily, with or without food. Phenytoin capsules or tablets should be swallowed whole with a full glass of water to facilitate drug absorption and ensure proper dosing. Do not chew, crush, or open phenytoin capsules or tablets, as this may alter the drug’s pharmacokinetics and decrease efficacy. Follow the specific dosing regimen prescribed by your healthcare provider and do not exceed the recommended dose or duration of treatment without medical supervision. Complete the full course of phenytoin therapy as prescribed, even if symptoms improve before the medication is finished, to achieve optimal seizure control and prevent recurrence of epileptic seizures. Follow-up with your healthcare provider regularly to monitor seizure activity and adjust therapy as needed.

Precautions and Care

Patients taking phenytoin should be monitored regularly for signs of adverse reactions or complications, such as dizziness, drowsiness, ataxia, or diplopia. Phenytoin therapy may be associated with an increased risk of gingival hyperplasia, osteoporosis, or vitamin D deficiency, particularly with long-term use or high doses. Use caution when prescribing phenytoin to elderly patients or those with renal impairment, as dosage adjustments may be necessary to avoid drug accumulation and potential toxicity. Educate patients about the signs and symptoms of potential adverse effects and instruct them to promptly report any new or worsening symptoms to their healthcare provider. Consult with a healthcare provider for guidance on appropriate monitoring and management of adverse reactions associated with phenytoin therapy.

Dietary Considerations

There are no specific dietary restrictions associated with phenytoin therapy, but patients should maintain a balanced diet and adequate hydration to support overall health and well-being during treatment. Encourage patients to maintain good oral hygiene and schedule regular dental check-ups to monitor for signs of gingival hyperplasia, a common side effect of phenytoin therapy. Patients should also be advised to avoid excessive alcohol consumption, as alcohol may potentiate the central nervous system depressant effects of phenytoin and increase the risk of drowsiness or dizziness. Consult with a registered dietitian or nutritionist for personalized dietary recommendations and lifestyle modifications to complement phenytoin therapy.

Missed Dose

If a dose of phenytoin is missed, it should be taken as soon as remembered unless it is almost time for the next scheduled dose. Patients should not double the dose to make up for a missed one. Complete the full course of phenytoin therapy as prescribed by your healthcare provider, even if symptoms improve before the medication is finished, to achieve optimal seizure control and prevent recurrence of epileptic seizures. Follow-up with your healthcare provider regularly to monitor seizure activity and adjust therapy as needed.

Possible Side Effects

Common side effects of phenytoin may include dizziness, drowsiness, ataxia, diplopia, and gastrointestinal disturbances. Less common but more serious side effects may include gingival hyperplasia, osteoporosis, vitamin D deficiency, or hypersensitivity reactions. Phenytoin therapy may be associated with an increased risk of Stevens-Johnson syndrome or toxic epidermal necrolysis, particularly in patients with a history of hypersensitivity reactions to phenytoin or other antiepileptic drugs. Contact your healthcare provider if you experience severe or persistent side effects while taking phenytoin, as they may require medical evaluation or adjustment of therapy. Consult with a healthcare provider for guidance on appropriate monitoring and management of adverse reactions associated with phenytoin therapy.

Storage and Disposal

Phenytoin capsules or tablets should be stored at room temperature away from moisture, heat, and light, in their original packaging. Keep phenytoin out of reach of children and pets to prevent accidental ingestion or misuse. Unused or expired medication should be disposed of properly according to local guidelines, such as through a medication take-back program or by mixing with an undesirable substance (such as coffee grounds or cat litter) and disposing of in the household trash. Do not flush phenytoin capsules or tablets down the toilet or pour them down the drain, as this may contaminate water sources and harm the environment.

Overdose or Emergency

In case of overdose or emergency, contact your local poison control center or emergency medical services immediately. Symptoms of phenytoin overdose may include severe central nervous system depression, respiratory depression, cardiovascular collapse, or status epilepticus. Emergency medical treatment may be necessary to manage symptoms of overdose, such as airway management, administration of activated charcoal or gastric lavage, and supportive care. Do not attempt to induce vomiting or administer other medications without medical supervision.

Always consult with a healthcare professional for personalized medical advice and guidance regarding the use of phenytoin, especially regarding dosing, administration, and potential side effects.