Diazepam 2.5mg Rectal Gel (2 Pack)
WARNING: This drug is a benzodiazepine. The use of a benzodiazepine drug along with opioid drugs has led to very bad side effects. Side effects that have happened include slowed or trouble breathing and death. Opioid drugs include drugs like codeine, oxycodone, and morphine. Opioid drugs are used to treat pain and some are used to treat cough. Talk with the doctor.If you are taking this drug with an opioid drug, get medical help right away if you feel very sleepy or dizzy; if you have slow, shallow, or trouble breathing; or if you pass out. Caregivers or others need to get medical help right away if the patient does not respond, does not answer or react like normal, or will not wake up. Benzodiazepines can put you at risk for drug use disorder. Misuse or abuse of this drug can lead to overdose or death, especially when used along with certain other drugs, alcohol, or street drugs. Drug use disorder can happen even if you take this drug as your doctor has told you. Get medical help right away if you have changes in mood or behavior, suicidal thoughts or actions, seizures, or trouble breathing.Benzodiazepines may cause dependence, especially if taken on a regular basis. This drug is not meant for regular daily use.The risk of dependence and withdrawal are raised the longer you take this drug and the higher the dose. Talk to your doctor before you lower the dose or stop this drug. You will need to follow your doctor's instructions. Lowering the dose or stopping this drug all of a sudden may cause withdrawal. This can be life-threatening. Get medical help right away if you have trouble controlling body movements, seizures, new or worse behavior or mood changes like depression or thoughts of suicide, thoughts of harming someone, hallucinations (seeing or hearing things that are not there), losing contact with reality, moving around or talking a lot, or any other bad effects.Sometimes, withdrawal signs can last for several weeks to more than 12 months. Tell your doctor if you have anxiety; trouble with memory, learning, or focusing; trouble sleeping; burning, numbness, or tingling; weakness; shaking; muscle twitching; ringing in the ears; or any other bad effects. @ COMMON USES: It is used to help control certain kinds of seizures.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Anticonvulsant, Anxiolytic, Sedative-Hypnotic
Pharmacologic Class
Benzodiazepine
Pregnancy Category
Category D
FDA Approved
Jan 1997
DEA Schedule
Schedule IV
Overview
What is this medicine?
Diazepam rectal gel is a medication used to stop clusters of seizures (also called acute repetitive seizures) quickly. It's given rectally, which means it's inserted into the rectum. It works by calming overactive brain signals.
How to Use This Medicine
Taking Your Medication Correctly
To use this medication safely and effectively, follow your doctor's instructions carefully. Read all the information provided to you and adhere to the instructions closely. If necessary, your doctor may advise you to take a second dose 4 to 12 hours after the initial dose.
Important Usage Guidelines
Do not use this medication to treat more than 5 episodes in a month or more than 1 episode every 5 days. Before administering the medication, ensure that the correct dose is locked in place, indicated by a visible green ready band.
What to Do in Case of Seizures
If you experience seizures that persist for 15 minutes after taking this medication, contact your doctor immediately, unless they have provided alternative instructions.
Storing and Disposing of Your Medication
Store this medication at room temperature in a dry location, avoiding storage in a bathroom.
Missing a Dose
If you miss a dose, seek medical attention right away.
To use this medication safely and effectively, follow your doctor's instructions carefully. Read all the information provided to you and adhere to the instructions closely. If necessary, your doctor may advise you to take a second dose 4 to 12 hours after the initial dose.
Important Usage Guidelines
Do not use this medication to treat more than 5 episodes in a month or more than 1 episode every 5 days. Before administering the medication, ensure that the correct dose is locked in place, indicated by a visible green ready band.
What to Do in Case of Seizures
If you experience seizures that persist for 15 minutes after taking this medication, contact your doctor immediately, unless they have provided alternative instructions.
Storing and Disposing of Your Medication
Store this medication at room temperature in a dry location, avoiding storage in a bathroom.
Missing a Dose
If you miss a dose, seek medical attention right away.
Lifestyle & Tips
- Avoid alcohol and other sedatives while using this medication, as they can increase drowsiness and breathing problems.
- Do not drive or operate heavy machinery until you know how this medication affects you, as it can cause dizziness and drowsiness.
- Inform your doctor about all other medications you are taking, especially opioids, as serious interactions can occur.
- Keep this medication out of reach of children and pets.
Available Forms & Alternatives
Available Strengths:
- Diazepam 2mg Tablets
- Diazepam 5mg Tablets
- Diazepam 10mg Tablets
- Diazepam 5mg/5ml (1mg/1ml) Oral Sol
- Diazepam 5mg/1ml Oral Concentrate
- Diazepam 5mg/ml Inj, 2ml
- Diazepam 5mg/ml Inj, 10ml
- Diazepam 20mg Rectal Gel
- Diazepam 10mg Rectal Gel( 2 Pack)
- Diazepam 2.5mg Rectal Gel (2 Pack)
- Diazepam 5mg/ml Inj, 2ml
- Diazepam 10mg Rectal Gel (2 Pack)
- Diazepam 20mg Rectal Gel
- Diazepam 10mg/2ml Inj, 2ml
Dosing & Administration
Adult Dosing
Standard Dose:
20 mg once, may repeat in 4-12 hours if needed
Dose Range:
15 - 20 mg
Condition-Specific Dosing:
acute repetitive seizures:
20 mg once, may repeat in 4-12 hours if needed. Max 2 doses per 24 hours.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established for this indication (acute repetitive seizures)
Child:
2-5 years: 0.5 mg/kg; 6-11 years: 0.3 mg/kg; 12 years and older: 0.2 mg/kg. Max single dose 20 mg. May repeat in 4-12 hours if needed. Max 2 doses per 24 hours.
Adolescent:
0.2 mg/kg. Max single dose 20 mg. May repeat in 4-12 hours if needed. Max 2 doses per 24 hours.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended, use with caution.
Moderate:
No specific adjustment recommended, use with caution.
Severe:
No specific adjustment recommended, use with caution.
Dialysis:
Not dialyzable. Use with caution, monitor for prolonged sedation.
Hepatic Impairment:
Mild:
Use with caution, consider lower initial dose.
Moderate:
Use with caution, consider lower initial dose.
Severe:
Contraindicated in severe hepatic insufficiency due to risk of encephalopathy. Use with extreme caution, significant dose reduction may be necessary.
Pharmacology
Mechanism of Action
Diazepam binds to stereospecific benzodiazepine receptors on the postsynaptic GABA-A neuron at several sites within the central nervous system, including the limbic system, reticular formation. This binding enhances the inhibitory effects of gamma-aminobutyric acid (GABA), leading to increased chloride ion influx, hyperpolarization of the neuronal membrane, and decreased neuronal excitability. This results in anxiolytic, sedative, hypnotic, anticonvulsant, and muscle relaxant properties.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 90% (rectal absorption is rapid but variable)
Tmax:
1.5 hours (range 0.25-2.5 hours) after rectal administration
FoodEffect:
Not applicable for rectal administration.
Distribution:
Vd:
0.8-1.0 L/kg
ProteinBinding:
98%
CnssPenetration:
Yes
Elimination:
HalfLife:
20-100 hours (parent drug); 30-100 hours (nordiazepam)
Clearance:
0.2-0.5 mL/min/kg
ExcretionRoute:
Renal (primarily as conjugated metabolites)
Unchanged:
<1%
Pharmacodynamics
OnsetOfAction:
Within minutes (rectal)
PeakEffect:
1.5 hours (rectal)
DurationOfAction:
Several hours (variable, due to active metabolites)
Safety & Warnings
BLACK BOX WARNING
Concomitant use of benzodiazepines and opioids may result in profound sedation, respiratory depression, coma, and death. Reserve concomitant prescribing of these drugs for use in patients for whom alternative treatment options are inadequate. Limit dosages and durations to the minimum required. Follow patients for signs and symptoms of respiratory depression and sedation. The risks of abuse, misuse, and addiction with benzodiazepines can lead to overdose or death. Assess each patient’s risk prior to prescribing and monitor all patients regularly for the development of these behaviors or conditions. Continued use of benzodiazepines may lead to physical dependence. The risks of dependence and withdrawal increase with longer treatment duration and higher doses. Abrupt discontinuation or rapid dosage reduction of benzodiazepines may precipitate acute withdrawal reactions, which can be life-threatening. To reduce the risk of withdrawal reactions, use a gradual taper to discontinue.
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Shortness of breath
Change in balance
Feeling confused
Hallucinations (seeing or hearing things that are not there)
Memory problems or loss
Severe dizziness or passing out
Muscle spasm
Twitching
Trouble sleeping
Change in eyesight
Slurred speech
Severe upset stomach, vomiting, or loss of appetite that does not go away
Like other medications used to treat seizures, this drug may rarely increase the risk of suicidal thoughts or actions, especially in people who have had suicidal thoughts or actions in the past. If you experience any new or worsening symptoms, such as:
Depression
Feeling nervous, restless, or irritable
Panic attacks
Other changes in mood or behavior
contact your doctor right away. If you have suicidal thoughts or actions, seek immediate medical attention.
Other Possible Side Effects
Most people do not experience significant side effects, but some may occur. If you notice any of the following side effects, contact your doctor if they bother you or do not go away:
Feeling sleepy
Feeling tired or weak
Muscle weakness
* Headache
This is not a comprehensive list of all possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Shortness of breath
Change in balance
Feeling confused
Hallucinations (seeing or hearing things that are not there)
Memory problems or loss
Severe dizziness or passing out
Muscle spasm
Twitching
Trouble sleeping
Change in eyesight
Slurred speech
Severe upset stomach, vomiting, or loss of appetite that does not go away
Like other medications used to treat seizures, this drug may rarely increase the risk of suicidal thoughts or actions, especially in people who have had suicidal thoughts or actions in the past. If you experience any new or worsening symptoms, such as:
Depression
Feeling nervous, restless, or irritable
Panic attacks
Other changes in mood or behavior
contact your doctor right away. If you have suicidal thoughts or actions, seek immediate medical attention.
Other Possible Side Effects
Most people do not experience significant side effects, but some may occur. If you notice any of the following side effects, contact your doctor if they bother you or do not go away:
Feeling sleepy
Feeling tired or weak
Muscle weakness
* Headache
This is not a comprehensive list of all possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe drowsiness or difficulty waking up
- Slow, shallow, or difficult breathing
- Blue lips or fingernails
- Unusual agitation, aggression, or hallucinations (paradoxical reactions)
- Signs of an allergic reaction (rash, hives, swelling of face/lips/tongue, difficulty breathing)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Breathing problems
+ Glaucoma
+ Liver disease
+ Myasthenia gravis
+ Sleep apnea
If you have been diagnosed with psychosis
Recent consumption of large amounts of alcohol or use of medications that may cause drowsiness, such as phenobarbital or certain pain medications like oxycodone
If you are breast-feeding or plan to breast-feed, as you may need to avoid doing so while taking this medication
If the patient is a child, as this medication may not be suitable for all ages of children
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Breathing problems
+ Glaucoma
+ Liver disease
+ Myasthenia gravis
+ Sleep apnea
If you have been diagnosed with psychosis
Recent consumption of large amounts of alcohol or use of medications that may cause drowsiness, such as phenobarbital or certain pain medications like oxycodone
If you are breast-feeding or plan to breast-feed, as you may need to avoid doing so while taking this medication
If the patient is a child, as this medication may not be suitable for all ages of children
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Before operating a vehicle or engaging in any activity that requires alertness and clear vision, wait until you understand how this medication affects you.
Refrain from consuming alcohol while taking this drug, as it may exacerbate its effects.
Prior to using marijuana, other forms of cannabis, or any prescription or over-the-counter medications that may cause drowsiness, consult with your doctor to discuss potential interactions.
If you experience a change in the frequency or severity of seizures after initiating this medication, notify your doctor promptly.
This medication may cause drowsiness and impaired alertness, increasing the risk of falls. This risk is particularly elevated in older adults. If you have concerns, discuss them with your doctor.
If you are 65 years or older, exercise caution when taking this medication, as you may be more susceptible to side effects.
When administering this medication to children, use it with caution, as they may be at a higher risk for certain side effects.
If you are pregnant or become pregnant while taking this medication, immediately contact your doctor, as it may pose a risk to the unborn baby.
Taking this medication during late pregnancy may increase the likelihood of respiratory or feeding difficulties, hypothermia, or withdrawal symptoms in the newborn. Consult with your doctor to discuss the potential risks and benefits.
Before operating a vehicle or engaging in any activity that requires alertness and clear vision, wait until you understand how this medication affects you.
Refrain from consuming alcohol while taking this drug, as it may exacerbate its effects.
Prior to using marijuana, other forms of cannabis, or any prescription or over-the-counter medications that may cause drowsiness, consult with your doctor to discuss potential interactions.
If you experience a change in the frequency or severity of seizures after initiating this medication, notify your doctor promptly.
This medication may cause drowsiness and impaired alertness, increasing the risk of falls. This risk is particularly elevated in older adults. If you have concerns, discuss them with your doctor.
If you are 65 years or older, exercise caution when taking this medication, as you may be more susceptible to side effects.
When administering this medication to children, use it with caution, as they may be at a higher risk for certain side effects.
If you are pregnant or become pregnant while taking this medication, immediately contact your doctor, as it may pose a risk to the unborn baby.
Taking this medication during late pregnancy may increase the likelihood of respiratory or feeding difficulties, hypothermia, or withdrawal symptoms in the newborn. Consult with your doctor to discuss the potential risks and benefits.
Overdose Information
Overdose Symptoms:
- Extreme drowsiness
- Confusion
- Slurred speech
- Slowed reflexes
- Lack of coordination
- Hypotension (low blood pressure)
- Respiratory depression (slowed or stopped breathing)
- Coma
What to Do:
Seek immediate medical attention. Call 911 or Poison Control at 1-800-222-1222. Flumazenil may be used as an antidote in severe cases, but it carries risks, especially in patients with epilepsy.
Drug Interactions
Contraindicated Interactions
- Opioid analgesics (concomitant use with benzodiazepines can result in profound sedation, respiratory depression, coma, and death)
- Other CNS depressants (e.g., alcohol, barbiturates, other benzodiazepines, tricyclic antidepressants, antipsychotics, general anesthetics) - risk of additive CNS depression
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir) - risk of increased diazepam exposure and toxicity
- Strong CYP2C19 inhibitors (e.g., fluvoxamine, omeprazole) - risk of increased diazepam exposure and toxicity
Major Interactions
- Anticonvulsants (e.g., phenytoin, carbamazepine, phenobarbital) - altered diazepam metabolism or additive CNS depression
- Muscle relaxants (e.g., baclofen, tizanidine) - increased risk of respiratory depression and sedation
- Cimetidine, fluoxetine, propoxyphene - increased diazepam levels
- Digoxin - may increase digoxin levels
Moderate Interactions
- Antacids - may delay absorption (less relevant for rectal gel)
- Oral contraceptives - may alter diazepam metabolism
- Theophylline - may antagonize sedative effects of diazepam
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Respiratory rate and effort
Rationale: To assess baseline respiratory function before administration, especially in patients with respiratory compromise.
Timing: Prior to administration
Level of consciousness
Rationale: To establish baseline neurological status.
Timing: Prior to administration
Routine Monitoring
Respiratory rate and depth
Frequency: Frequently after administration (e.g., every 5-15 minutes for the first hour, then as clinically indicated)
Target: Normal for age
Action Threshold: Bradypnea, shallow breathing, or signs of respiratory distress; intervene immediately.
Level of consciousness/Sedation
Frequency: Frequently after administration, then as clinically indicated
Target: Awake and alert, or easily arousable
Action Threshold: Excessive sedation, unarousable state; consider supportive measures.
Seizure activity
Frequency: Continuous observation
Target: Cessation of seizure activity
Action Threshold: Continued or recurrent seizures; consider repeat dose or alternative therapy.
Symptom Monitoring
- Signs of respiratory depression (slow, shallow breathing, cyanosis)
- Excessive sedation or unresponsiveness
- Paradoxical reactions (e.g., agitation, hallucinations, aggression)
- Signs of allergic reaction (rash, itching, swelling)
Special Patient Groups
Pregnancy
Diazepam is classified as Pregnancy Category D. It can cause fetal harm when administered to a pregnant woman. There is evidence of human fetal risk, but potential benefits may warrant use of the drug in pregnant women despite potential risks (e.g., life-threatening situation). Neonatal flaccidity, respiratory and feeding difficulties, and hypothermia have been reported in infants born to mothers who have received benzodiazepines late in pregnancy.
Trimester-Specific Risks:
First Trimester:
Increased risk of congenital malformations (e.g., cleft lip/palate) based on some studies, though data are conflicting.
Second Trimester:
Risk of withdrawal symptoms in the neonate if used chronically.
Third Trimester:
Risk of neonatal flaccidity, respiratory depression, feeding difficulties, and hypothermia (floppy infant syndrome) if used near term or during labor. Risk of neonatal withdrawal syndrome with chronic use.
Lactation
Diazepam and its active metabolites are excreted into breast milk. Due to the long half-life of diazepam and its active metabolites, accumulation in the infant can occur, leading to sedation, poor feeding, and weight loss. Use is generally not recommended during breastfeeding. If essential, monitor the infant closely for sedation and feeding difficulties.
Infant Risk:
L3 (Moderate risk) - Potential for infant sedation, poor feeding, and accumulation due to long half-life.
Pediatric Use
Diazepam rectal gel is approved for acute repetitive seizures in children 2 years of age and older. Dosing is weight-based. Close monitoring for respiratory depression and sedation is crucial, especially in younger children and those with underlying respiratory compromise.
Geriatric Use
Elderly patients may be more sensitive to the effects of benzodiazepines, including increased risk of sedation, respiratory depression, and falls. Lower doses are generally recommended. Monitor closely for adverse effects.
Clinical Information
Clinical Pearls
- Diazepam rectal gel is a rescue medication for acute repetitive seizures and is not for daily, chronic use.
- Caregivers should be thoroughly trained on proper administration technique and recognition of adverse effects.
- A second dose may be given if seizures recur, but not sooner than 4-12 hours after the first dose, and no more than two doses within a 24-hour period.
- Patients should be transported to an emergency facility for evaluation after administration of the second dose or if seizures do not stop after the first dose.
- The pre-filled syringe is designed for single use and should be discarded after use, even if not fully emptied.
Alternative Therapies
- Midazolam (intranasal, buccal, or intramuscular for acute seizures)
- Lorazepam (intravenous for status epilepticus)
- Levetiracetam (intravenous for status epilepticus)
- Fosphenytoin/Phenytoin (intravenous for status epilepticus)
Cost & Coverage
Average Cost:
Check current pricing per 2-pack
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (often requires prior authorization for brand, generic may be preferred)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication.
This medication is accompanied by a Medication Guide, which is a valuable resource that provides important information about your treatment. Please read this guide carefully and review it again whenever you receive a refill of your medication. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, pharmacist, or other healthcare provider for clarification.
In the event of a suspected overdose, it's crucial to seek immediate medical attention or contact your local poison control center. When reporting the incident, be prepared to provide detailed information, including the name of the medication taken, the amount consumed, and the time it occurred.
This medication is accompanied by a Medication Guide, which is a valuable resource that provides important information about your treatment. Please read this guide carefully and review it again whenever you receive a refill of your medication. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, pharmacist, or other healthcare provider for clarification.
In the event of a suspected overdose, it's crucial to seek immediate medical attention or contact your local poison control center. When reporting the incident, be prepared to provide detailed information, including the name of the medication taken, the amount consumed, and the time it occurred.