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Diphenhydramine 12.5 mg/Haloperidol 0.5 mg/Lorazepam 0.5 mg Rectal Suppository

The Diphenhydramine 12.5 mg/Haloperidol 0.5 mg/Lorazepam 0.5 mg Rectal Suppository is a solid dosage form designed for insertion into the rectum. Upon administration, the suppository dissolves or melts, facilitating the release of three active pharmaceutical ingredients for both local and systemic absorption. Diphenhydramine is an antihistamine that can help alleviate symptoms of allergies and provide sedation. Haloperidol is an antipsychotic used for managing acute psychosis, including schizophrenia, and can also help control tics and vocal utterances of Tourette's syndrome. Lorazepam, a benzodiazepine, is effective in treating anxiety disorders, providing sedation before surgery, and can be used as part of the therapy for status epilepticus. This combination of medications in a single rectal suppository form is often employed in clinical settings for its sedative, antiemetic, and antipsychotic properties, particularly in managing agitation and restlessness in patients with delirium or severe agitation in end-of-life care.

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Formula Information

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The Diphenhydramine 12.5 mg/Haloperidol 0.5 mg/Lorazepam 0.5 mg Rectal Suppository is a compounded medication designed for rectal administration. This solid dosage form is specifically formulated to be inserted into the rectum, where it dissolves or melts, allowing the active ingredients to be absorbed either locally or systemically. The combination of diphenhydramine, haloperidol, and lorazepam in a single suppository offers a multi-faceted approach to treatment, targeting various symptoms and conditions.

Diphenhydramine is an antihistamine that can help alleviate allergic reactions and also has sedative properties, making it useful in promoting sleep and reducing anxiety. Haloperidol is an antipsychotic medication that can help manage symptoms of acute psychosis, agitation, and can also be used in the treatment of Tourette's syndrome and certain behavioral issues. Lorazepam, a benzodiazepine, is effective in treating anxiety disorders, providing sedation before medical procedures, and can help with seizure control. The combination of these three medications in a rectal suppository form can be particularly beneficial for patients who are unable to take oral medications or in cases where rapid medication absorption is desired.

This compounded medication may be used in various clinical scenarios, such as in palliative care for managing agitation and restlessness, in psychiatric settings for acute control of agitation or psychosis, or in emergency situations where other routes of administration are not feasible. The rectal route provides an alternative for patients with nausea, vomiting, or difficulty swallowing, ensuring that they still receive the necessary medication.

It is important for both patients and prescribers to understand that this formulation should be used under the guidance of a healthcare professional, and it is tailored to meet the specific needs of the patient. The pharmacists at Bayview Pharmacy are equipped to provide detailed information on the proper use, potential side effects, and the mechanism of action of each component in this formulation. If you have any questions or require further clarification on this compounded medication, please do not hesitate to reach out to us for professional advice and support.

Drug Interactions

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The combination of diphenhydramine, haloperidol, and lorazepam in a rectal suppository form is intended for the management of conditions that may benefit from the sedative, antiemetic, antipsychotic, and anxiolytic effects of these medications. However, it is important to consider potential drug interactions when these medications are used in combination.

Diphenhydramine is an antihistamine with sedative properties. It can enhance the sedative effects of other central nervous system (CNS) depressants, such as haloperidol and lorazepam. When used concurrently with other CNS depressants, including alcohol, opioids, or benzodiazepines, there is an increased risk of sedation, respiratory depression, and potentially dangerous impairment of cognitive and motor skills. Caution is advised when patients are taking other medications with sedative properties.

Haloperidol is an antipsychotic medication that can affect the metabolism of other drugs. It is metabolized by the cytochrome P450 (CYP) enzyme system, particularly CYP3A4 and CYP2D6. Drugs that inhibit these enzymes, such as certain antidepressants, antifungals, and protease inhibitors, can increase haloperidol levels and the risk of side effects, including QT prolongation, a potentially serious heart rhythm disturbance. Conversely, medications that induce these enzymes, such as carbamazepine and rifampin, may decrease haloperidol levels and reduce its efficacy.

Lorazepam is a benzodiazepine with anxiolytic and sedative effects. It is metabolized by the liver and can interact with drugs that affect hepatic enzymes. Concurrent use with other CNS depressants can result in additive CNS depression. Additionally, the use of lorazepam with opioids increases the risk of sedation, respiratory depression, coma, and death. Caution is also advised when lorazepam is used with other medications that can increase its sedative effects, such as antihistamines, antipsychotics, and alcohol.

Furthermore, all three components of this suppository can have additive anticholinergic effects when used with other anticholinergic drugs, leading to an increased risk of constipation, urinary retention, dry mouth, and other anticholinergic side effects. Patients with glaucoma, prostatic hypertrophy, or other conditions exacerbated by anticholinergic drugs should be monitored closely.

It is also important to note that the absorption of medications administered rectally can be influenced by various factors, including rectal mucosa health, presence of feces, and rectal motility. These factors can affect the systemic availability of the drugs and potentially alter their interaction profile.

Given the complexity of these interactions, it is crucial for prescribers to review the patient's complete medication profile, including over-the-counter drugs and herbal supplements, to identify and manage potential interactions. Patients should be advised to avoid alcohol and to be cautious when using other medications that can cause drowsiness or CNS depression. Regular monitoring for side effects and therapeutic efficacy is recommended. If you have any questions or require further information regarding this formulation and its interactions, please reach out to us at Bayview Pharmacy.

How Does it Work

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The Diphenhydramine 12.5 mg/Haloperidol 0.5 mg/Lorazepam 0.5 mg Rectal Suppository is a compounded medication designed to deliver a combination of drugs that work synergistically to manage symptoms such as severe agitation, nausea, vomiting, and insomnia, particularly in a palliative care setting. This solid dosage form is specifically designed for rectal administration, where it is inserted into the rectum. Upon insertion, the suppository base, typically made from a substance like cocoa butter or a glycerinated gelatin, begins to melt or dissolve due to the warmth of the body, releasing the active medications for local and systemic absorption through the rectal mucosa.

Diphenhydramine is an antihistamine with sedative properties. It works by blocking histamine H1 receptors, which helps to reduce allergy symptoms. Its sedative effects can also help to induce sleep and reduce agitation. Haloperidol is an antipsychotic medication that works by blocking dopamine receptors in the brain, which can help to control symptoms of psychosis and acute agitation. Lorazepam, a benzodiazepine, enhances the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABA-A receptor, which produces a calming effect on the brain and nerves. This combination can be particularly effective in managing symptoms of delirium, agitation, and restlessness in patients with advanced illness.

The rectal route of administration provides several advantages, including bypassing the gastrointestinal tract, which can be beneficial for patients with nausea, vomiting, or difficulty swallowing. Additionally, it can be a preferred route for patients who are not able to take medications orally. The combination of these three medications in a single suppository allows for the convenience of administering multiple drugs at once, potentially improving patient compliance and comfort.

It is important for both patients and prescribers to understand that this formulation should be used under the guidance of a healthcare professional experienced in managing complex symptoms in seriously ill patients. The dosages of diphenhydramine, haloperidol, and lorazepam in this suppository have been carefully selected to provide symptom relief while minimizing the risk of side effects. However, individual responses to medication can vary, and close monitoring is necessary to ensure safety and efficacy. If you have any questions or require further information about this formulation, please reach out to us at Bayview Pharmacy.

Other Uses

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The combination of diphenhydramine, haloperidol, and lorazepam in a rectal suppository form is primarily utilized for its sedative, antiemetic, and antipsychotic properties. This particular formulation can be beneficial for managing acute agitation or delirium in patients who are unable to take medications orally. Additionally, the rectal route is advantageous in instances where the gastrointestinal tract is compromised, or in patients who are nauseated, vomiting, or at risk of aspiration.

While the primary indication for this formulation is to provide sedation and to manage symptoms of agitation and delirium, these medications combined may also be useful in addressing severe cases of insomnia, especially when the cause of sleeplessness is due to an underlying temporary psychotic episode or extreme agitation that does not respond to typical hypnotics. Furthermore, this formulation can be considered in end-of-life care settings, where managing symptoms like restlessness, anxiety, and psychosis is critical for patient comfort. It must be noted, however, that the use of haloperidol, even in a palliative care setting, requires careful consideration of the potential for extrapyramidal symptoms and other side effects.

Due to the anticholinergic effects of diphenhydramine, the combination suppository may show efficacy in the management of dystonic reactions that are medication-induced. However, healthcare providers should be attentive to the cumulative anticholinergic load in patients, particularly the elderly, to avoid cognitive impairment or delirium. Moreover, while the antipsychotic action of haloperidol might offer benefits in managing certain psychiatric presentations, prescribers should weigh the risks associated with long-term use of antipsychotics, such as the development of tardive dyskinesia.

As pharmacists specializing in compounding, we are aware of the complexity and the need for individualized medication regimens. We encourage prescribers and patients to reach out to us with any questions or concerns regarding the use of this rectal suppository formulation or to discuss alternative therapeutic options. Our goal is to support and educate our clients to ensure that each customized medication meets the unique needs of the patient.

Frequently Asked Questions

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What is the purpose of the Diphenhydramine/Haloperidol/Lorazepam rectal suppository?

This medication is a compounded preparation designed to deliver a combination of Diphenhydramine, Haloperidol, and Lorazepam via the rectal route. It is typically used for its antihistamine, antiemetic, antipsychotic, and anxiolytic effects, especially in situations where oral administration is not practical.

How should this rectal suppository be stored?

The suppository should be stored in a cool place, preferably in a refrigerator, in order to maintain its solidity. It should be kept out of the reach of children and pets, and stored in its original packaging to prevent exposure to moisture and light which might degrade the medication.

How is the Diphenhydramine/Haloperidol/Lorazepam rectal suppository administered?

For rectal administration, the suppository should be inserted point first into the rectum, ensuring that it passes the anal sphincter to prevent expulsion. Proper hygiene should be maintained during administration, and hands should be washed before and after insertion.

What are the potential side effects of this medication?

The potential side effects may include drowsiness, dry mouth, constipation, urinary retention, blurred vision, and confusion. It is important to contact your healthcare provider if you experience any severe or persistent side effects.

Can this medication be used in children?

The use in children should be strictly under the guidance of a healthcare provider. Special precautions must be taken due to the dosages of the active ingredients and the sensitivity of pediatric patients to these medications.

What should I do if I miss a dose?

If you miss a dose, administer the suppository as soon as you remember. However, if it's near the time for your next dose, skip the missed dose and resume your regular dosing schedule. Do not double up on doses to make up for a missed one.

Can I use this suppository while pregnant or breastfeeding?

Consult your healthcare provider before using this medication if you are pregnant or breastfeeding. The active ingredients may have risks associated with them during pregnancy and while nursing that need to be weighed against the benefits of treatment.

How quickly does the suppository work?

The onset of action can vary depending on individual absorption rates, but typically, rectal suppositories begin to work within 15 to 60 minutes after administration. It may take longer to notice the effects due to systemic absorption.

Are there any interactions with other medications?

Yes, this compound could potentially interact with other medications. Inform your healthcare provider of all the medications you are taking, including over-the-counter drugs, vitamins, and herbal supplements, to avoid any potential interactions.

What should I avoid while using this medication?

While using this suppository, you should avoid activities that require alertness, such as driving or operating heavy machinery, until you know how the medication affects you. Additionally, avoid consuming alcohol as it can increase the sedative effects of the medication.

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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.
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