Diazepam 20mg Rectal Gel
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
Pharmacologic Class
Benzodiazepine; GABA-A Receptor Agonist
Pregnancy Category
Category D
FDA Approved
Jan 1996
DEA Schedule
Schedule IV
Overview
What is this medicine?
Diazepam rectal gel is a medication used to quickly stop clusters of seizures (when a person has several seizures close together). It is given rectally by a trained caregiver. It works by calming overactive brain activity to help stop the seizure.
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.
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 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 instructed you to follow a different course of action.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry location, avoiding bathrooms.
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 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.
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 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 instructed you to follow a different course of action.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry location, avoiding bathrooms.
Missing a Dose
If you miss a dose, seek medical attention right away.
Lifestyle & Tips
- Avoid alcohol and other sedating medications (e.g., opioids, sleeping pills) unless specifically instructed by a doctor, as this can increase the risk of severe drowsiness and breathing problems.
- Do not drive or operate heavy machinery until you know how this medication affects you and the sedative effects have completely worn off.
- Ensure the patient is in a safe, supervised environment after administration.
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 (or 0.15 mg/kg if on concomitant CNS depressants) as a single rectal dose. Max single dose 20 mg. May be repeated once 4-12 hours after the first dose if needed. Max 2 doses in 24 hours.
Condition-Specific Dosing:
acute_repetitive_seizures:
0.2 mg/kg (or 0.15 mg/kg if on concomitant CNS depressants) as a single rectal dose. Max single dose 20 mg. May be repeated once 4-12 hours after the first dose if needed. Max 2 doses in 24 hours.
Pediatric Dosing
Neonatal:
Not established (contraindicated in infants less than 6 months of age)
Infant:
0.5 mg/kg for children 2-5 years of age. Max single dose 20 mg. May be repeated once 4-12 hours after the first dose if needed. Max 2 doses in 24 hours.
Child:
0.3 mg/kg for children 6-11 years of age. Max single dose 20 mg. May be repeated once 4-12 hours after the first dose if needed. Max 2 doses in 24 hours.
Adolescent:
0.2 mg/kg for children 12 years and older. Max single dose 20 mg. May be repeated once 4-12 hours after the first dose if needed. Max 2 doses in 24 hours.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment, use with caution.
Moderate:
No specific adjustment, use with caution.
Severe:
Use with caution, consider lower doses and monitor closely due to potential for prolonged effects.
Dialysis:
Not significantly dialyzable; use with caution and monitor for prolonged effects.
Hepatic Impairment:
Mild:
Use with caution, consider lower doses.
Moderate:
Use with caution, consider lower doses and monitor closely for increased sedation and adverse effects.
Severe:
Contraindicated or use with extreme caution due to impaired metabolism and increased risk of encephalopathy and prolonged sedation.
Pharmacology
Mechanism of Action
Diazepam potentiates the effect of gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter, at the GABA-A receptor. This leads to increased chloride ion influx through the GABA-gated chloride channel, resulting in hyperpolarization of the neuronal membrane and decreased neuronal excitability. This action produces anxiolytic, sedative, hypnotic, anticonvulsant, and muscle relaxant effects.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 90% (rectal)
Tmax:
1.5 hours (rectal)
FoodEffect:
Not applicable for rectal administration.
Distribution:
Vd:
0.8-1.0 L/kg
ProteinBinding:
98%
CnssPenetration:
Yes
Elimination:
HalfLife:
Diazepam: 20-100 hours; Nordiazepam: 30-100 hours
Clearance:
20-30 mL/min
ExcretionRoute:
Renal (primarily as metabolites)
Unchanged:
<1%
Pharmacodynamics
OnsetOfAction:
1-10 minutes (rectal)
PeakEffect:
1.5 hours (rectal)
DurationOfAction:
4-12 hours (anticonvulsant effect, but sedative effects may last longer 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 are serious and can lead to overdose and death. Physical dependence can occur with benzodiazepine use. The risk of dependence and withdrawal increases with longer treatment duration and higher doses. Abrupt discontinuation or rapid dosage reduction of diazepam after continued use may precipitate acute withdrawal reactions, which can be life-threatening.
Side Effects
Serious Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
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. If you have a history of suicidal thoughts or actions, your risk may be higher. Contact your doctor immediately if you experience any new or worsening symptoms, such as:
Depression
Feeling nervous, restless, or irritable
Panic attacks
Other changes in mood or behavior
Suicidal thoughts or actions
Other Possible Side Effects
Most people do not experience significant side effects, but some may occur. If you are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical attention:
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, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
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. If you have a history of suicidal thoughts or actions, your risk may be higher. Contact your doctor immediately if you experience any new or worsening symptoms, such as:
Depression
Feeling nervous, restless, or irritable
Panic attacks
Other changes in mood or behavior
Suicidal thoughts or actions
Other Possible Side Effects
Most people do not experience significant side effects, but some may occur. If you are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical attention:
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:
- Difficulty breathing or very slow, shallow breathing
- Extreme drowsiness or unresponsiveness
- Blue lips or fingernails
- Severe dizziness or loss of balance
- Unusual agitation or aggression (paradoxical reaction)
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 a history of 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
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 consulting your doctor first.
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 a history of 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
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 consulting your doctor first.
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 using this drug, as it may exacerbate its effects.
Prior to using marijuana, other cannabis products, 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, promptly discuss this with your doctor.
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.
If you are pregnant or become pregnant while taking this medication, immediately contact your doctor, as it may harm the unborn baby.
Taking this medication during late pregnancy can increase the risk of respiratory or feeding difficulties, hypothermia, 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 using this drug, as it may exacerbate its effects.
Prior to using marijuana, other cannabis products, 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, promptly discuss this with your doctor.
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.
If you are pregnant or become pregnant while taking this medication, immediately contact your doctor, as it may harm the unborn baby.
Taking this medication during late pregnancy can increase the risk of respiratory or feeding difficulties, hypothermia, or withdrawal symptoms in the newborn. Discuss this with your doctor to understand the potential risks and benefits.
Overdose Information
Overdose Symptoms:
- Severe drowsiness
- Confusion
- Slurred speech
- Slowed reflexes
- Ataxia (loss of coordination)
- Hypotension (low blood pressure)
- Respiratory depression (slowed or stopped breathing)
- Coma
What to Do:
Seek immediate emergency medical attention. Call 911 or your local emergency number. Contact a poison control center at 1-800-222-1222. Flumazenil may be used as an antidote in a hospital setting, but it carries risks, especially in patients with chronic benzodiazepine use or seizure disorders.
Drug Interactions
Contraindicated Interactions
Major Interactions
- Alcohol
- Other benzodiazepines
- Barbiturates
- Tricyclic antidepressants
- Antipsychotics
- Muscle relaxants
- Sedating antihistamines
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, clarithromycin)
- Strong CYP2C19 inhibitors (e.g., fluvoxamine, omeprazole, esomeprazole)
Moderate Interactions
- Moderate CYP3A4/2C19 inhibitors (e.g., fluoxetine, cimetidine, disulfiram, oral contraceptives)
- Certain antihypertensives (additive hypotensive effects)
Minor Interactions
- Antacids (may delay absorption, but not clinically significant for rectal administration)
Monitoring
Baseline Monitoring
Seizure history and characteristics
Rationale: To establish baseline seizure pattern and confirm suitability for acute repetitive seizure treatment.
Timing: Prior to first administration and periodically.
Baseline neurological status
Rationale: To assess pre-treatment level of consciousness and motor function.
Timing: Prior to first administration.
Respiratory function
Rationale: To identify patients at higher risk for respiratory depression.
Timing: Prior to first administration.
Routine Monitoring
Respiratory rate and depth
Frequency: During and for several hours after administration, especially in patients with respiratory compromise or co-administration of CNS depressants.
Target: Normal for age
Action Threshold: Bradypnea, shallow breathing, or signs of respiratory distress; intervene immediately.
Level of consciousness/sedation
Frequency: During and for several hours after administration.
Target: Awake and responsive, or easily arousable.
Action Threshold: Excessive sedation, unresponsiveness, or coma; intervene immediately.
Seizure activity
Frequency: Continuously after administration.
Target: Cessation of seizure activity.
Action Threshold: Continued or recurrent seizures after appropriate dosing; seek emergency medical attention.
Blood pressure and heart rate
Frequency: Periodically after administration, especially in susceptible patients.
Target: Normal for age
Action Threshold: Significant hypotension or bradycardia.
Symptom Monitoring
- Excessive sedation
- Respiratory depression (slow, shallow breathing)
- Ataxia (loss of coordination)
- Dizziness
- Slurred speech
- Paradoxical reactions (agitation, aggression, hallucinations)
- Hypotension
Special Patient Groups
Pregnancy
Diazepam is classified as Pregnancy Category D. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. There is evidence of human fetal risk.
Trimester-Specific Risks:
First Trimester:
Increased risk of congenital malformations (e.g., cleft lip/palate) if used during the first trimester.
Second Trimester:
Limited data, but continued use may lead to fetal exposure.
Third Trimester:
Risk of neonatal flaccidity, respiratory depression, feeding difficulties, and withdrawal symptoms (e.g., irritability, hypertonia, tremor, diarrhea, vomiting) in the neonate if used late in pregnancy or chronically.
Lactation
Diazepam and its active metabolites are excreted into breast milk. Use during lactation is generally not recommended due to potential for sedation, poor feeding, and weight loss in the infant. If use is necessary, monitor the infant closely.
Infant Risk:
L3 (Moderately safe). Potential for sedation, lethargy, poor feeding, and weight gain in the breastfed infant. Monitor for these effects. Consider pumping and discarding milk for a period after administration, or using an alternative medication.
Pediatric Use
Dosing is weight and age-based. Not recommended for infants younger than 6 months due to potential for respiratory depression and limited safety data. Use with caution and monitor closely for sedation and respiratory depression, especially in younger children.
Geriatric Use
Elderly patients are more sensitive to the CNS depressant effects of diazepam. Lower doses (e.g., 0.15 mg/kg) should be considered, and patients should be monitored closely for excessive sedation, respiratory depression, and increased risk of falls. Impaired hepatic metabolism may prolong elimination half-life.
Clinical Information
Clinical Pearls
- Diazepam rectal gel is a rescue medication for acute repetitive seizures; it is not for daily, chronic seizure prevention.
- Caregivers must be properly trained on the administration technique before an emergency arises.
- Administer the dose immediately upon recognition of a seizure cluster, as early intervention is key to efficacy.
- Do not administer more than two doses within a 24-hour period.
- If seizures do not stop after the second dose, or if respiratory depression or other severe adverse effects occur, seek immediate emergency medical attention.
- Patients should be in a safe, supervised environment after administration due to potential for sedation and ataxia.
- Ensure the prescribed dose matches the available syringe size (e.g., 2.5 mg, 5 mg, 10 mg, 20 mg).
Alternative Therapies
- Midazolam nasal spray (Nayzilam, Valtoco)
- Midazolam buccal solution (Buccolam - outside US)
- Lorazepam intravenous (IV) or intramuscular (IM)
- Other benzodiazepines (e.g., clonazepam, clobazam) for chronic management, but not typically for acute rescue in this formulation.
Cost & Coverage
Average Cost:
Varies widely (e.g., $200-$1000+) per single-use rectal syringe
Generic Available:
Yes
Insurance Coverage:
Often Tier 2 or Tier 3, may require prior authorization.
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 provides crucial information for patients. Please read this guide carefully and review it again whenever you receive a refill of this medication. 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 seeking help, be prepared to provide details about the overdose, including the medication taken, the amount, and the time it occurred.