Diazepam 10mg 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 medicine used to stop clusters of seizures quickly. It's given into the rectum and works by calming overactive brain signals. It's not for daily use but for emergencies when seizures won't stop on their own.
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 a second dose is necessary, you may take it 4 to 12 hours after the first dose, but only if your doctor has advised you to do so.
It is essential to use this medication only as directed and not to exceed the recommended frequency. 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. You will know it is ready when you see a green ready band.
If you continue to experience seizures for 15 minutes after taking this medication, contact your doctor immediately, unless they have given you alternative instructions.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry location, avoiding storage in a bathroom.
What to Do If You Miss 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 a second dose is necessary, you may take it 4 to 12 hours after the first dose, but only if your doctor has advised you to do so.
It is essential to use this medication only as directed and not to exceed the recommended frequency. 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. You will know it is ready when you see a green ready band.
If you continue to experience seizures for 15 minutes after taking this medication, contact your doctor immediately, unless they have given you alternative instructions.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry location, avoiding storage in a bathroom.
What to Do If You Miss a Dose
If you miss a dose, seek medical attention right away.
Lifestyle & Tips
- Avoid alcohol and other sedating medications while using this drug, as it 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.
- Follow your doctor's instructions carefully on how and when to administer the rectal gel.
- Always have the rectal gel readily available if prescribed for emergency seizure management.
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:
0.2 mg/kg rectally, maximum 20 mg per dose. A second dose may be given 4-12 hours after the first if needed.
Dose Range:
0.2 - 0.5 mg
Condition-Specific Dosing:
acute_repetitive_seizures:
0.2 mg/kg rectally, maximum 20 mg per dose. A second dose may be given 4-12 hours after the first if needed. Not for chronic daily use.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established for rectal gel formulation for seizures (safety and efficacy not established below 2 years of age).
Child:
2 to 5 years: 0.5 mg/kg; 6 to 11 years: 0.3 mg/kg; 12 years and older: 0.2 mg/kg. Max 20 mg per dose. A second dose may be given 4-12 hours after the first if needed.
Adolescent:
0.2 mg/kg rectally, maximum 20 mg per dose. A second dose may be given 4-12 hours after the first if needed.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended, but use with caution.
Moderate:
No specific dose adjustment recommended, but use with caution.
Severe:
No specific dose adjustment recommended, but use with caution. Monitor for increased sedation.
Dialysis:
Diazepam is not readily dialyzable. Use with caution, monitor for prolonged effects.
Hepatic Impairment:
Mild:
Use with caution, consider lower initial dose.
Moderate:
Use with caution, consider lower initial dose and monitor closely for sedation and respiratory depression.
Severe:
Contraindicated in severe hepatic insufficiency due to risk of encephalopathy. If used, significantly reduce dose and monitor closely.
Pharmacology
Mechanism of Action
Diazepam is a benzodiazepine that binds to specific benzodiazepine receptors on the gamma-aminobutyric acid (GABA)-A receptor complex. This binding enhances the inhibitory effects of GABA by increasing the frequency of chloride channel opening, leading to hyperpolarization of the neuronal membrane and reduced neuronal excitability. This results in anxiolytic, sedative, hypnotic, anticonvulsant, and muscle relaxant properties.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 90% (oral), Rectal gel bioavailability is variable but generally good (around 80-90% compared to IV).
Tmax:
Rectal gel: 1.5 hours (range 0.25-2.5 hours) in children, 1.5 hours (range 0.25-10 hours) in adults.
FoodEffect:
Not applicable for rectal administration.
Distribution:
Vd:
0.8-1.0 L/kg (adults), higher in children and neonates.
ProteinBinding:
98% (primarily to albumin).
CnssPenetration:
Yes, readily crosses the blood-brain barrier.
Elimination:
HalfLife:
Diazepam: 20-100 hours (highly variable, longer in elderly and liver disease). N-desmethyldiazepam: 30-100 hours.
Clearance:
0.2-0.5 mL/min/kg.
ExcretionRoute:
Renal (primarily as conjugated metabolites), small amount in feces.
Unchanged:
<1% (urine)
Pharmacodynamics
OnsetOfAction:
Rectal gel: 5-10 minutes (for anticonvulsant effect).
PeakEffect:
Rectal gel: 1.5 hours (variable).
DurationOfAction:
Rectal gel: 4-12 hours (anticonvulsant effect), longer for sedative effects 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 and death. Assess each patient’s risk prior to prescribing and monitor all patients regularly for the development of these behaviors or conditions.
Side Effects
Serious Side Effects: Seek Medical Help Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical attention right away:
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 fainting
Muscle spasms
Twitching
Trouble sleeping
Changes 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 medical help immediately.
Other Side Effects
Most people do not experience serious side effects, and many have no side effects or only minor ones. However, if you experience any of the following side effects, contact your doctor or seek medical attention 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.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical attention right away:
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 fainting
Muscle spasms
Twitching
Trouble sleeping
Changes 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 medical help immediately.
Other Side Effects
Most people do not experience serious side effects, and many have no side effects or only minor ones. However, if you experience any of the following side effects, contact your doctor or seek medical attention 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
- Very slow or shallow breathing
- Bluish lips or skin
- Unusual excitement, agitation, or aggression (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 breastfeeding or plan to breastfeed, 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 whether 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 breastfeeding or plan to breastfeed, 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 whether 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 prescription and over-the-counter medications that can impair your reactions, consult with your doctor.
If you experience a change in the frequency or severity of seizures after initiating this medication, discuss this with your doctor promptly.
This medication can cause drowsiness and reduced alertness, increasing the risk of falls. This risk is particularly elevated in older adults. If you have concerns, consult with your doctor.
If you are 65 years or older, exercise caution when using this medication, as you may be more susceptible to side effects.
When administering this medication to children, use it with caution, as they may have a higher risk of experiencing certain side effects.
There is a potential risk of harm to the unborn baby if this medication is taken during pregnancy. If you become pregnant or are already pregnant, notify your doctor immediately.
Taking this medication in the later stages of pregnancy may increase the risk of respiratory or feeding difficulties, low body temperature, or withdrawal symptoms in the newborn. Discuss this with your doctor to understand 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 prescription and over-the-counter medications that can impair your reactions, consult with your doctor.
If you experience a change in the frequency or severity of seizures after initiating this medication, discuss this with your doctor promptly.
This medication can cause drowsiness and reduced alertness, increasing the risk of falls. This risk is particularly elevated in older adults. If you have concerns, consult with your doctor.
If you are 65 years or older, exercise caution when using this medication, as you may be more susceptible to side effects.
When administering this medication to children, use it with caution, as they may have a higher risk of experiencing certain side effects.
There is a potential risk of harm to the unborn baby if this medication is taken during pregnancy. If you become pregnant or are already pregnant, notify your doctor immediately.
Taking this medication in the later stages of pregnancy may increase the risk of respiratory or feeding difficulties, low body temperature, or withdrawal symptoms in the newborn. Discuss this with your doctor to understand the potential risks and benefits.
Overdose Information
Overdose Symptoms:
- Extreme drowsiness
- Confusion
- Slurred speech
- Slowed reflexes
- Ataxia (loss of coordination)
- Hypotension (low blood pressure)
- Respiratory depression (slow or shallow breathing)
- Coma
What to Do:
Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222. Management includes supportive care, maintaining airway, breathing, and circulation. Flumazenil may be used in severe cases but carries risks, especially in patients with chronic benzodiazepine use or seizure disorders.
Drug Interactions
Major Interactions
- Opioids (e.g., fentanyl, oxycodone, hydrocodone, morphine): Increased risk of profound sedation, respiratory depression, coma, and death.
- Other CNS depressants (e.g., alcohol, barbiturates, other benzodiazepines, tricyclic antidepressants, antipsychotics, general anesthetics): Potentiation of CNS depression.
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir): Increased diazepam levels and effects.
- Strong CYP2C19 inhibitors (e.g., fluoxetine, fluvoxamine, omeprazole): Increased diazepam levels and effects.
Moderate Interactions
- Moderate CYP3A4 inhibitors (e.g., diltiazem, verapamil, grapefruit juice): May increase diazepam levels.
- Moderate CYP2C19 inhibitors (e.g., cimetidine, esomeprazole): May increase diazepam levels.
- Antacids: May delay absorption of oral diazepam (less relevant for rectal gel).
- Digoxin: May increase digoxin serum concentrations.
- Phenytoin: May alter phenytoin levels (increase or decrease).
Minor Interactions
- Theophylline: May antagonize sedative effects of diazepam.
- Levodopa: May reduce therapeutic effects of levodopa.
Monitoring
Baseline Monitoring
Respiratory rate and effort
Rationale: To assess baseline respiratory status, especially important before administering a CNS depressant.
Timing: Prior to administration
Level of consciousness/sedation
Rationale: To establish baseline mental status and monitor for excessive sedation.
Timing: Prior to administration
Seizure activity/duration
Rationale: To document the nature and severity of the acute seizure episode.
Timing: During seizure episode
Routine Monitoring
Respiratory rate and depth
Frequency: Every 5-15 minutes initially, then as clinically indicated until stable.
Target: Normal for age, no signs of distress.
Action Threshold: Bradypnea, shallow breathing, cyanosis, or signs of respiratory distress; intervene immediately.
Level of consciousness/sedation
Frequency: Every 5-15 minutes initially, then as clinically indicated until stable.
Target: Awake and alert or easily arousable.
Action Threshold: Excessive sedation, unresponsiveness, or difficulty arousing; consider supportive measures.
Seizure cessation/recurrence
Frequency: Continuously during acute event, then periodically for 4-12 hours.
Target: Cessation of seizure activity.
Action Threshold: Continued seizure activity or recurrence; consider second dose or alternative treatment.
Blood pressure and heart rate
Frequency: As clinically indicated, especially if signs of cardiovascular depression.
Target: Within normal limits for age.
Action Threshold: Significant hypotension or bradycardia.
Symptom Monitoring
- Respiratory depression (slow, shallow breathing)
- Excessive sedation or drowsiness
- Dizziness
- Ataxia (loss of coordination)
- Slurred speech
- Confusion
- Paradoxical reactions (e.g., excitement, aggression, hallucinations)
- 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 in certain serious conditions (e.g., life-threatening seizures).
Trimester-Specific Risks:
First Trimester:
Increased risk of congenital malformations (e.g., cleft lip/palate) if used during the first trimester, though data are conflicting.
Second Trimester:
Risk of fetal CNS depression and withdrawal symptoms in the neonate if used chronically.
Third Trimester:
Risk of 'floppy infant syndrome' (hypotonia, lethargy, feeding difficulties, hypothermia, respiratory depression) and neonatal withdrawal symptoms (irritability, hypertonia, tremors, diarrhea, vomiting) if used near term or during labor.
Lactation
Diazepam and its active metabolites are excreted into breast milk. The American Academy of Pediatrics considers it a drug for which the effect on the nursing infant is unknown but may be of concern. Use with caution, monitor infant for sedation, poor feeding, and weight gain.
Infant Risk:
L3 (Moderate risk). Potential for sedation, lethargy, poor feeding, and weight loss in the infant. Long half-life of active metabolites can lead to accumulation. Consider alternative agents or monitor infant closely.
Pediatric Use
Safety and efficacy of diazepam rectal gel for acute repetitive seizures have not been established in pediatric patients under 2 years of age. Dosing is weight-based and age-dependent for children 2 years and older. Children may be more sensitive to CNS depressant effects. Paradoxical reactions (e.g., hyperactivity, agitation) may occur.
Geriatric Use
Elderly patients are more sensitive to the effects of benzodiazepines due to decreased metabolism, increased volume of distribution, and increased brain sensitivity. They are at increased risk of sedation, dizziness, falls, and respiratory depression. Lower doses are generally recommended, and careful monitoring is essential. Avoid if possible, or use the lowest effective dose for the shortest duration.
Clinical Information
Clinical Pearls
- Diazepam rectal gel is a rescue medication for acute repetitive seizures, not for daily maintenance therapy.
- Ensure caregivers are properly trained on administration technique, including priming the syringe and proper insertion.
- Monitor for respiratory depression and excessive sedation, especially in patients also receiving opioids or other CNS depressants.
- A second dose may be given if seizures recur, but not more than two doses per 24-hour period.
- Patients should be lying on their side or stomach for administration.
- The rectal gel formulation provides a rapid onset of action, making it suitable for emergency seizure management outside of a hospital setting.
- Counsel patients and caregivers on the importance of seeking emergency medical attention if seizures do not stop or if respiratory depression occurs.
Alternative Therapies
- Lorazepam (IV, IM, intranasal, buccal for acute seizures)
- Midazolam (intranasal, buccal, IM, IV for acute seizures)
- Clonazepam (oral, for chronic seizure management)
- Other antiepileptic drugs (e.g., phenytoin, fosphenytoin, levetiracetam, valproate for status epilepticus)
Cost & Coverage
Average Cost:
Not available per 2-pack
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (varies by plan)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. 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 patient fact sheet. Please read it carefully and review it again whenever you receive a refill. If you have any questions or concerns about this medication, we encourage you to discuss them with your doctor, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide detailed information, including the substance taken, the quantity, and the time it occurred.