Diastat

Primary Uses

Diastat is primarily used as a rescue medication for the short-term treatment of increased seizure activity. It is specifically intended for people with epilepsy who are already taking a stable regimen of daily anti-seizure medications but experience occasional episodes of breakthrough seizures.

These episodes, often referred to as seizure clusters or bouts of increased seizure activity, are typically different from the person's usual seizure pattern. Diastat is used to help stop these clusters and prevent them from progressing into more severe or prolonged seizures.

When It Is Prescribed

Healthcare providers may prescribe Diastat for patients who:

• Have a history of seizure clusters.
• Are at least 2 years of age.
• Need a medication that can be administered quickly by a caregiver during an emergency seizure situation.

It is intended for intermittent use and is not meant to be used as a daily preventive medication.

Mechanism of Action

Diastat contains diazepam, which belongs to a group of medicines known as benzodiazepines. It works by affecting the way certain chemicals in the brain send messages to nerve cells.

The primary way Diastat works is by increasing the activity of gamma-aminobutyric acid (GABA). GABA is a neurotransmitter that acts as a natural braking system for the central nervous system. Its job is to inhibit or slow down excessive electrical activity in the brain.

During a seizure, there is a sudden, uncontrolled burst of electrical activity between brain cells. Diastat helps by:

• Enhancing GABA: It makes the GABA receptors more sensitive, allowing the chemical to work more effectively.
• Calming Nerve Cells: By boosting GABA, the medication helps stabilize nerve cells and prevents them from firing too rapidly.
• Stopping Seizure Activity: This calming effect helps interrupt the abnormal electrical signals, which can stop a seizure that is currently happening or prevent a cluster of seizures from continuing.

Because Diastat is a rectal gel, it is absorbed through the lining of the rectum and enters the bloodstream quickly. This allows the medication to reach the brain faster than an oral tablet, which is necessary for managing acute seizure emergencies.

Common Side Effects

Some people may experience mild side effects while using this medication. These often include:

• Drowsiness or sleepiness
• Dizziness
• Headache
• Diarrhea
• Abdominal or stomach pain
• Nervousness
• Clumsiness or loss of coordination
• Skin rash

Serious Side Effects

Contact a healthcare provider immediately if you notice any of the following serious symptoms:

• Slow, shallow, or difficult breathing
• Extreme drowsiness or inability to wake up
• Confusion or hallucinations
• Unusual changes in mood or behavior, such as aggression or agitation
• Suicidal thoughts or tendencies
• Severe muscle weakness
• Slurred speech
• Difficulty urinating or loss of bladder control

Seek emergency medical help if you experience signs of a severe allergic reaction, such as hives, swelling of the face, lips, tongue, or throat, or difficulty breathing.

Boxed Warning: Risks from Concomitant Use with Opioids

Using Diastat with opioid medicines may result in profound sedation, respiratory depression (slowed breathing), coma, and death. This combination should only be used when alternative treatment options are inadequate.

Boxed Warning: Abuse, Misuse, and Addiction

The use of benzodiazepines, including diazepam, exposes users to risks of abuse, misuse, and addiction, which can lead to overdose or death. These risks are increased when the medication is used more frequently than prescribed or combined with other substances like alcohol.

Boxed Warning: Dependence and Withdrawal

Continued use of Diastat may lead to physical dependence. Abruptly stopping the medication or reducing the dose too quickly can cause life-threatening withdrawal reactions, such as seizures, hallucinations, or psychosis.

Central Nervous System Depression

Diastat causes significant central nervous system depression. Patients may experience extreme drowsiness and decreased mental alertness. Activities requiring coordination or concentration, such as driving or operating machinery, should be avoided until the effects of the medication have completely worn off.

Respiratory Risks

This medication can cause respiratory depression. Caution is necessary for individuals with pre-existing respiratory conditions, such as chronic obstructive pulmonary disease (COPD) or sleep apnea. Caregivers should monitor the patient's breathing closely after administration.

Contraindications

Diastat should not be used in individuals with a known hypersensitivity to diazepam. It is also contraindicated in patients with acute narrow-angle glaucoma, though it may be used in those with open-angle glaucoma who are receiving appropriate treatment.

Suicidal Thoughts and Behavior

Antiepileptic drugs, including benzodiazepines used for seizures, may increase the risk of suicidal thoughts or behaviors. Changes in mood, worsening depression, or unusual behavior should be monitored closely.

Pregnancy

Diastat may cause harm to an unborn baby if used during pregnancy. Some studies suggest an increased risk of birth defects when benzodiazepines are used in the first trimester. If used later in pregnancy, the medication can lead to complications in the newborn, such as muscle weakness (floppy infant syndrome), breathing difficulties, and withdrawal symptoms.

It is important not to start or stop seizure medication without medical advice, as seizures during pregnancy can pose a threat to both the parent and the baby. If you are pregnant or planning to become pregnant, discuss your treatment plan with your doctor.

Breastfeeding

The active ingredient in Diastat passes into breast milk and can affect a nursing infant. Potential side effects for the baby include:

• Excessive drowsiness
• Difficulty feeding
• Weight loss

Because of these risks, breastfeeding while using Diastat is generally discouraged. Consult a healthcare provider to determine the best course of action for your health and the safety of your infant.

Dosage Forms

Diastat is available as a gel intended for rectal administration. It is provided in a specialized delivery system to facilitate administration by a caregiver.

• Rectal Gel: The medication is a non-sterile gel contained within a pre-filled syringe.
• Unit-Dose Delivery System: Each delivery system is designed for use and includes a lubricated tip for rectal insertion.
• Adjustable Delivery System: Certain versions of the device allow a pharmacist to dial and lock the required amount into the delivery system before it is dispensed to the patient.

FDA Approval and Indications

Diastat (diazepam rectal gel) is approved by the U.S. Food and Drug Administration (FDA) for the short-term management of increased seizure activity, often called seizure clusters or breakthrough seizures. It is intended for use in patients who are already taking stable doses of other antiepileptic medications to help control bouts of increased seizure frequency that are different from the patient's usual seizure pattern.

Boxed Warnings

The FDA requires a boxed warning—the most serious type of warning—for Diastat and other benzodiazepines due to several significant safety risks:

• Risks from Concomitant Use with Opioids: Using benzodiazepines with opioid pain or cough medicines can result in profound sedation, respiratory depression (slowed or stopped breathing), coma, and death. Healthcare providers should limit the use of these medications together to the lowest possible dosages and durations.
• Abuse, Misuse, and Addiction: The use of benzodiazepines, even as prescribed, exposes users to the risks of abuse, misuse, and addiction, which can lead to overdose or death.
• Physical Dependence and Withdrawal Reactions: Continued use of Diastat can lead to physical dependence. Stopping the medication suddenly or reducing the dose too quickly can cause life-threatening withdrawal symptoms, such as seizures, hallucinations, or tremors.

Controlled Substance Status

Diazepam, the active ingredient in Diastat, is classified by the Drug Enforcement Administration (DEA) as a Schedule IV controlled substance. This classification indicates that the medication has a potential for abuse and dependence, and its distribution is regulated by federal law.

Risk of Withdrawal

Diastat is a benzodiazepine, a class of medication that can lead to physical dependence. While it is typically used for intermittent treatment of seizure clusters, frequent or prolonged use increases the risk of withdrawal symptoms if the medication is stopped abruptly.

Symptoms of Withdrawal

Withdrawal symptoms may begin shortly after the last dose and can include:

• Tremors or shaking
• Muscle and abdominal cramps
• Vomiting and sweating
• Headache and muscle pain
• Extreme anxiety, tension, and restlessness
• Confusion and irritability

Severe Complications

In severe cases, sudden withdrawal can be life-threatening. Serious symptoms may include:

• Seizures or status epilepticus
• Hallucinations
• Depersonalization (feeling detached from oneself)
• Hypersensitivity to light, noise, and physical contact
• Numbness or tingling in the extremities

To prevent these complications, do not stop using Diastat or change the frequency of use without consulting a healthcare professional. A gradual reduction in dosage, known as a taper, may be required to safely discontinue the drug.