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Phenytoin Sodium 100 mg Rectal Suppository

The Phenytoin Sodium 100 mg Rectal Suppository is a solid dosage form designed for insertion into the rectum. Upon administration, it dissolves or melts, facilitating the release of phenytoin sodium for both local and systemic absorption. This formulation is primarily used in the management of seizures, offering an alternative route of administration for patients unable to take oral medications. It is effective in treating various forms of epilepsy and is also utilized in the prevention and treatment of seizures occurring during or after neurosurgery.

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Phenytoin Sodium
Suppository
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Formula Information

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Phenytoin Sodium 100 mg Rectal Suppository is a solid dosage form designed for rectal administration, where it dissolves or melts to release the active pharmaceutical ingredient, phenytoin sodium, for systemic absorption. This route of administration is particularly useful when oral administration is not feasible, such as in patients with nausea and vomiting, those who are unconscious or unable to swallow, or when medication delivery needs to bypass the gastrointestinal tract to avoid degradation or first-pass metabolism.

Phenytoin is an anticonvulsant medication used primarily in the management of epilepsy. It works by stabilizing the neuronal membrane and reducing the excitability of the central nervous system by inhibiting sodium channels. This action helps to prevent the abnormal electrical activity in the brain that causes seizures. Phenytoin is effective in treating various types of seizures, including tonic-clonic (grand mal) and partial seizures, but it is not effective for absence (petit mal) seizures.

When using phenytoin sodium rectal suppositories, it is important to consider the pharmacokinetics of rectal administration. The absorption of phenytoin from the rectal mucosa can be variable, and factors such as rectal content, pH, and circulation can affect drug delivery. However, this route can provide a relatively steady absorption profile, which is beneficial for maintaining therapeutic drug levels. It is also critical to monitor serum phenytoin levels to ensure they remain within the therapeutic range, as phenytoin has a narrow therapeutic index and is associated with dose-related toxicity.

Patients and prescribers should be aware of potential side effects associated with phenytoin use, which can include central nervous system effects such as nystagmus, ataxia, and dizziness, as well as gastrointestinal disturbances and dermatological reactions. Long-term use of phenytoin may lead to folate deficiency, osteomalacia, and other systemic effects. It is also important to note that phenytoin interacts with a wide range of medications, which can affect its efficacy and safety.

For those interested in using Phenytoin Sodium 100 mg Rectal Suppository, it is essential to consult with a healthcare professional to ensure appropriate dosing, monitoring, and management of any potential adverse effects or drug interactions. Our team at Bayview Pharmacy is available to provide expert advice and support for both patients and prescribers considering this formulation. If you have any questions or require further information, please do not hesitate to reach out to us.

Drug Interactions

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Phenytoin sodium is an anticonvulsant medication used to treat and prevent seizures. When formulated as a 100 mg rectal suppository, it is intended for administration via the rectal route to achieve systemic absorption, particularly when oral administration is not feasible. Phenytoin has a narrow therapeutic index and is known to interact with a wide range of drugs, which can lead to significant clinical implications. It is important for both patients and prescribers to be aware of these potential interactions to ensure safe and effective use of phenytoin.

Phenytoin is a potent inducer of hepatic cytochrome P450 enzymes, which can result in decreased plasma concentrations of drugs metabolized by these enzymes. This includes, but is not limited to, certain antiretrovirals, antineoplastic agents, anticoagulants like warfarin, and other anticonvulsants such as carbamazepine and valproic acid. Monitoring therapeutic drug levels and adjusting doses may be necessary when these medications are co-administered with phenytoin.

Conversely, drugs that inhibit cytochrome P450 enzymes can increase phenytoin levels, potentially leading to toxicity. Examples include some antibiotics like isoniazid and fluconazole, as well as antidepressants such as fluoxetine. It is crucial to monitor for signs of phenytoin toxicity, which can include nystagmus, ataxia, slurred speech, and mental confusion. Regular blood level monitoring of phenytoin is recommended to ensure levels remain within the therapeutic range.

Phenytoin's absorption may also be affected by drugs that alter gastric motility or pH, as well as by enteral feeding formulas, which can bind to the drug and reduce its absorption. Although less relevant for rectal administration, it is still important to consider the timing of administration relative to these factors to ensure consistent absorption and therapeutic effect.

Additionally, phenytoin can affect the metabolism of certain drugs leading to either an increase in their clearance, which can reduce their efficacy, or a decrease in their clearance, which can increase the risk of side effects. For example, it can decrease the effectiveness of oral contraceptives, necessitating the use of alternative or additional non-hormonal birth control methods.

It is also important to note that abrupt withdrawal of phenytoin can precipitate seizures. If the decision is made to discontinue phenytoin, it should be done gradually to minimize the risk of seizure exacerbation. Patients should be counseled on the importance of adherence to prescribed dosing schedules and not to discontinue therapy without consulting their healthcare provider.

Due to the complexity of phenytoin pharmacokinetics and its wide array of drug interactions, prescribers should conduct a thorough medication review for each patient prior to initiating therapy with phenytoin rectal suppositories. Pharmacists can provide valuable assistance in identifying potential drug interactions and recommending appropriate monitoring strategies. If you have any questions or require further information regarding the use of phenytoin rectal suppositories, please reach out to us at Bayview Pharmacy for assistance.

How Does it Work

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Phenytoin Sodium is an anticonvulsant medication that is commonly used to manage and prevent seizures in various forms of epilepsy. The active ingredient, phenytoin sodium, works by stabilizing the threshold against hyperexcitability caused by excessive stimulation or environmental changes capable of reducing the membrane sodium gradient. This action helps to limit the spread of seizure activity and reduces the risk of seizure propagation.

In the form of a 100 mg rectal suppository, phenytoin sodium is designed for rectal administration, which can be particularly useful in patients who are unable to take medications orally due to vomiting, unconsciousness, or other conditions that affect oral intake. The suppository is inserted into the rectum, where it dissolves or melts at body temperature. As the suppository base dissolves, it releases the phenytoin sodium for local absorption through the rectal mucosa. From there, the drug enters the systemic circulation and is distributed throughout the body to exert its anticonvulsant effects.

Rectal administration of phenytoin can provide a more consistent absorption profile compared to oral administration, especially in patients with gastrointestinal issues. This route bypasses the first-pass metabolism in the liver, which can be advantageous in maintaining therapeutic drug levels. Additionally, rectal suppositories can be a valuable alternative when intravenous access is not available or practical.

Phenytoin suppositories are used to treat various disease states associated with seizures, including tonic-clonic (grand mal) seizures, complex partial seizures, and seizures occurring during or after neurosurgery. The medication can also be used for status epilepticus, a condition where seizures follow one another without recovery of consciousness between them. In this emergency situation, rapid administration and absorption of anticonvulsant medication are critical, and rectal suppositories can be an effective route of administration.

It is important for both patients and prescribers to understand that while phenytoin rectal suppositories can provide benefits in certain situations, they must be used with caution. Monitoring of phenytoin serum levels is necessary to ensure therapeutic levels are achieved without reaching toxic concentrations. Adverse effects, such as ataxia, slurred speech, and mental confusion, may occur if the drug levels are too high. Additionally, patients with a history of hypersensitivity to phenytoin or other hydantoins should not use this medication.

If you have any questions or require further information about the use of Phenytoin Sodium 100 mg Rectal Suppository, please reach out to us at Bayview Pharmacy. Our team of compounding pharmacists is here to provide guidance and support to ensure the safe and effective use of this medication.

Other Uses

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Phenytoin sodium is predominantly known for its anticonvulsant properties, but the usage of phenytoin in a rectal suppository form can encompass a variety of off-label indications aside from its primary application in seizure control. The choice of a rectal suppository delivery system can be advantageous in patients who are unable to take medications orally due to nausea, surgery, or gastrointestinal disturbances. Given its mechanism of action, phenytoin might be explored for its potential neuroprotective effects in conditions where cognitive protection is desired, though such uses would be considered experimental and are not widely supported by clinical data.

In cases of status epilepticus where intravenous administration is not feasible, rectal suppositories such as this formulation provide an alternative route for drug administration to achieve systemic levels necessary for seizure control. Furthermore, phenytoin has been demonstrated to have antiarrhythmic properties similar to lidocaine, and thus, this formulation could hypothetically be used in the management of certain cardiac dysrhythmias, although this is an unconventional approach and typically not a primary indication.

While the potential neuronal benefits of phenytoin may suggest its utility in conditions like neuropathic pain, the evidence to support such use is limited and thus would not be routinely recommended. It is critical to remember that phenytoin, like all drugs, has a spectrum of possible side effects from mild to severe, and its use should be judiciously considered, particularly in off-label contexts. This application would require thorough investigation and should only be pursued under the guidance and supervision of a healthcare professional, acknowledging the potential risks and monitoring for adverse effects.

We advise healthcare providers and patients considering the use of phenytoin sodium 100 mg rectal suppositories for any off-label purposes to carefully weigh the potential benefits against the risks. Close monitoring for efficacy, as well as for any sign of toxicity or adverse reactions, is imperative. If you have any questions or require additional information about the formulation or its potential other uses, please reach out to us at Bayview Pharmacy. Our team of compounding pharmacists is always ready to assist and provide professional advice to ensure the safe and effective use of medications.

Frequently Asked Questions

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What is a Phenytoin Sodium 100 mg Rectal Suppository?

A Phenytoin Sodium 100 mg Rectal Suppository is a solid dosage form containing 100 milligrams of the active ingredient Phenytoin Sodium. It is designed to be inserted into the rectum, where it dissolves or melts to release the medication for absorption.

How does a rectal suppository work?

A rectal suppository works by melting or dissolving once inserted into the rectum. The body's warmth facilitates this process, allowing the active drug, Phenytoin Sodium, to be absorbed into the bloodstream through the rectal mucosa for local or systemic effects.

Who may be prescribed a Phenytoin Sodium Rectal Suppository?

Phenytoin Sodium Rectal Suppositories may be prescribed to patients who require seizure control and cannot take medications orally. This can include individuals with gastrointestinal issues, vomiting, or restricted from oral intake.

How should the Phenytoin Sodium Rectal Suppository be stored?

The suppositories should be stored in a cool, dry place, away from direct sunlight and heat. They should be kept in their original packaging until they are ready to be used to maintain stability and prevent melting.

What is the proper way to insert a rectal suppository?

Wash your hands thoroughly. Lie on your side with the lower leg straightened out and the upper leg bent forward toward your stomach. Lift upper buttock to expose the rectal area. Then, gently insert the suppository pointed end first into the rectum. Hold it in place for a few moments to ensure it does not come out.

Is the Phenytoin Sodium Rectal Suppository painful to use?

Most people do not experience pain when using rectal suppositories correctly. There may be initial discomfort, but it should not be painful. If pain is experienced, contact your healthcare provider as it may indicate incorrect insertion or another problem.

Can I use the Phenytoin Sodium Rectal Suppository if I have hemorrhoids or anal fissures?

Patients with hemorrhoids or anal fissures should consult their healthcare provider before using rectal suppositories as insertion may exacerbate these conditions.

How quickly does the suppository take effect?

The onset of action for a Phenytoin Sodium Rectal Suppository can vary but generally begins within 30 minutes to an hour after insertion. However, absorption rates can vary from person to person.

What should I do if the suppository comes out after insertion?

If the suppository comes out after insertion, you should wash your hands and gently re-insert it to ensure proper absorption. If it continues to come out, consult with your healthcare provider for further advice.

Can Phenytoin Sodium Rectal Suppositories cause side effects?

Yes, like any medication, Phenytoin Sodium Rectal Suppositories can cause side effects, though not everyone experiences them. Possible side effects include local irritation, dizziness, confusion, and ataxia. If you experience any concerning symptoms, contact your healthcare provider.

Can I discontinue the use of Phenytoin Sodium Rectal Suppositories abruptly?

No, you should not stop using Phenytoin Sodium Rectal Suppositories abruptly as it may increase the risk of seizures or withdrawal symptoms. Always consult with your healthcare provider before making any changes to your medication regimen.

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Formulas and/or material listed are not to be interpreted as a promise, guarantee or claim of therapeutic efficacy or safety. The information contained herein is not intended to replace or substitute for conventional medical care, or encourage its abandonment. Every patient is unique, and formulas should be adjusted to meet their individual needs.

No compounded medications are reviewed by the FDA for safety or efficacy.