Estazolam 2mg Tablets
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.You will be watched closely to make sure you do not misuse this drug or develop drug use disorder.Benzodiazepines may cause dependence. Lowering the dose or stopping this drug all of a sudden may cause withdrawal. This can be life- threatening. 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. 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 treat sleep problems.
Drug Class
Hypnotic
Pharmacologic Class
Benzodiazepine
Pregnancy Category
Category X
FDA Approved
Dec 1989
DEA Schedule
Schedule IV
Overview
What is this medicine?
Estazolam is a medication used for the short-term treatment of insomnia (difficulty falling or staying asleep). It belongs to a class of drugs called benzodiazepines. It works by calming your brain to help you fall asleep faster and stay asleep longer.
How to Use This Medicine
Taking Your Medication
To use this medication effectively, follow your doctor's instructions and read all accompanying information carefully. Take this medication either immediately before bedtime or after you've gone to bed and are having trouble falling asleep. It's essential to take it on an empty stomach, avoiding meals and snacks around the time of administration.
Before taking this medication, ensure you have a full night's sleep (at least 7 to 8 hours) available before you need to be active again. If you continue to experience difficulty sleeping after 7 to 10 days, consult your doctor for further guidance.
Storing and Disposing of Your Medication
Store this medication at room temperature, protected from light and moisture. Keep it in a dry place, avoiding storage in bathrooms. To prevent accidental ingestion, store the medication in a secure location where children and pets cannot access it. Consider using a locked box or area to safeguard the medication. Keep all medications out of reach of pets.
When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, consult your pharmacist for guidance on the best disposal method. You may also want to explore local drug take-back programs for safe and responsible disposal.
Missing a Dose
If you take this medication regularly and miss a dose, take it as soon as you remember. However, if taking the missed dose would interfere with getting a full night's sleep (at least 7 hours), skip the missed dose and resume your regular schedule. Avoid taking two doses at the same time or taking extra doses. If you take this medication on an as-needed basis, follow your doctor's instructions and do not take it more frequently than recommended.
To use this medication effectively, follow your doctor's instructions and read all accompanying information carefully. Take this medication either immediately before bedtime or after you've gone to bed and are having trouble falling asleep. It's essential to take it on an empty stomach, avoiding meals and snacks around the time of administration.
Before taking this medication, ensure you have a full night's sleep (at least 7 to 8 hours) available before you need to be active again. If you continue to experience difficulty sleeping after 7 to 10 days, consult your doctor for further guidance.
Storing and Disposing of Your Medication
Store this medication at room temperature, protected from light and moisture. Keep it in a dry place, avoiding storage in bathrooms. To prevent accidental ingestion, store the medication in a secure location where children and pets cannot access it. Consider using a locked box or area to safeguard the medication. Keep all medications out of reach of pets.
When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, consult your pharmacist for guidance on the best disposal method. You may also want to explore local drug take-back programs for safe and responsible disposal.
Missing a Dose
If you take this medication regularly and miss a dose, take it as soon as you remember. However, if taking the missed dose would interfere with getting a full night's sleep (at least 7 hours), skip the missed dose and resume your regular schedule. Avoid taking two doses at the same time or taking extra doses. If you take this medication on an as-needed basis, follow your doctor's instructions and do not take it more frequently than recommended.
Lifestyle & Tips
- Take exactly as prescribed, usually just before bedtime. Do not take more than the prescribed dose.
- Do not take with alcohol or other sedatives, as this can cause dangerous side effects like severe drowsiness or breathing problems.
- Avoid driving or operating heavy machinery until you know how this medication affects you, as it can cause drowsiness and dizziness.
- This medication is for short-term use only (typically 7-10 days). Long-term use can lead to dependence and withdrawal symptoms.
- Do not stop taking this medication suddenly, especially if you have been taking it regularly. Your doctor will tell you how to slowly reduce your dose to avoid withdrawal symptoms.
- Report any unusual thoughts or behaviors, such as aggression, agitation, hallucinations, or worsening depression, to your doctor immediately.
- Inform your doctor about all other medications you are taking, including over-the-counter drugs, herbal supplements, and recreational drugs.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
1 mg orally at bedtime
Dose Range:
0.5 - 2 mg
Condition-Specific Dosing:
insomnia:
0.5 mg to 2 mg orally at bedtime, generally 1 mg is sufficient for most adults. Use the lowest effective dose for the shortest duration possible.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended, but use with caution.
Moderate:
No specific adjustment recommended, but use with caution.
Severe:
No specific adjustment recommended, but use with caution.
Dialysis:
Not significantly dialyzable. Use with caution.
Hepatic Impairment:
Mild:
Consider lower initial dose (e.g., 0.5 mg).
Moderate:
Consider lower initial dose (e.g., 0.5 mg).
Severe:
Consider lower initial dose (e.g., 0.5 mg) and titrate carefully. Avoid if possible.
Pharmacology
Mechanism of Action
Estazolam is a benzodiazepine that binds to stereospecific benzodiazepine receptors on the postsynaptic GABA-A neuron at various sites in the central nervous system, including the limbic system, reticular formation, and cerebral cortex. It enhances the inhibitory effects of gamma-aminobutyric acid (GABA), leading to increased chloride ion influx, neuronal hyperpolarization, and decreased neuronal excitability, resulting in sedative, hypnotic, anxiolytic, anticonvulsant, and muscle relaxant effects.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 90%
Tmax:
0.5 to 6 hours (mean 2 hours)
FoodEffect:
Food may delay Tmax but does not significantly affect the extent of absorption (AUC).
Distribution:
Vd:
0.8 to 1.5 L/kg
ProteinBinding:
93%
CnssPenetration:
Yes
Elimination:
HalfLife:
10 to 24 hours (mean 17 hours)
Clearance:
Not available
ExcretionRoute:
Renal (urine)
Unchanged:
<5%
Pharmacodynamics
OnsetOfAction:
Within 30-60 minutes
PeakEffect:
1-2 hours
DurationOfAction:
6-8 hours (hypnotic effect), residual effects may last longer due to half-life
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.
Side Effects
Serious Side Effects: Seek Medical Attention Immediately
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 help 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
New or worsening behavioral or mood changes, including:
+ Depression
+ Thoughts of suicide
Hallucinations (seeing or hearing things that are not there)
Memory problems or loss
Changes in balance
Feeling confused or disoriented
Difficulty thinking clearly
Trouble moving around
New or worsening breathing difficulties
Angioedema, a severe reaction that may be life-threatening, characterized by:
+ Swelling of the hands, face, lips, eyes, tongue, or throat
+ Trouble breathing
+ Trouble swallowing
+ Unusual hoarseness
If you experience any of these symptoms, seek medical help immediately.
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. Contact your doctor or seek medical help if you experience any of the following side effects or if they bother you or do not go away:
Feeling sleepy or groggy the next day
Dry mouth
Upset stomach
Dizziness, tiredness, or weakness
Headache
Feeling nervous or excitable
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult 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 help 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
New or worsening behavioral or mood changes, including:
+ Depression
+ Thoughts of suicide
Hallucinations (seeing or hearing things that are not there)
Memory problems or loss
Changes in balance
Feeling confused or disoriented
Difficulty thinking clearly
Trouble moving around
New or worsening breathing difficulties
Angioedema, a severe reaction that may be life-threatening, characterized by:
+ Swelling of the hands, face, lips, eyes, tongue, or throat
+ Trouble breathing
+ Trouble swallowing
+ Unusual hoarseness
If you experience any of these symptoms, seek medical help immediately.
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. Contact your doctor or seek medical help if you experience any of the following side effects or if they bother you or do not go away:
Feeling sleepy or groggy the next day
Dry mouth
Upset stomach
Dizziness, tiredness, or weakness
Headache
Feeling nervous or excitable
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult 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 sedation that persists into the next day
- Difficulty breathing or shallow breathing
- Extreme dizziness or lightheadedness
- Confusion or disorientation
- Memory problems (forgetting events that occurred while on the medication)
- Unusual changes in mood or behavior (e.g., agitation, aggression, hallucinations, depression, suicidal thoughts)
- Allergic reaction symptoms (e.g., rash, itching, swelling of face/tongue/throat, severe dizziness, trouble breathing)
- Signs of withdrawal if stopped suddenly (e.g., anxiety, tremors, sweating, seizures, stomach cramps, muscle pain)
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. Be sure to describe the symptoms you experienced.
If you are currently taking itraconazole or ketoconazole, as these medications may interact with this drug.
If you are taking any other medications that can cause drowsiness, as there are many drugs that can have this effect. If you are unsure, consult your doctor or pharmacist for guidance.
If you are breastfeeding, as you should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions 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 dosage 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. Be sure to describe the symptoms you experienced.
If you are currently taking itraconazole or ketoconazole, as these medications may interact with this drug.
If you are taking any other medications that can cause drowsiness, as there are many drugs that can have this effect. If you are unsure, consult your doctor or pharmacist for guidance.
If you are breastfeeding, as you should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions 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 dosage 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.
After taking this drug, avoid operating a vehicle or engaging in any activities that require alertness, as it may cause drowsiness. This effect can persist into the next day, so refrain from such tasks until you feel fully awake and alert.
When used nightly for an extended period (more than a few weeks), sleep medications like this one may lose their effectiveness in addressing sleep issues due to the development of tolerance. Therefore, it is recommended to use this medication for a short duration only. If your sleep problems persist, consult your doctor for further guidance.
If you are taking this medication long-term, your doctor may recommend regular blood tests to monitor your condition. Be sure to discuss this with your doctor.
It is crucial to avoid consuming alcohol while taking this drug, and do not take the medication if you have had alcohol that evening or before bedtime. Additionally, consult your doctor before using marijuana, cannabis, or any prescription or over-the-counter medications that may cause drowsiness or impair your reactions.
Some individuals taking sleep medications have reported engaging in activities such as driving, cooking, eating, or having sex while not fully awake, often without any memory of doing so. If you experience such episodes, inform your doctor promptly.
This medication can cause drowsiness and reduced alertness, increasing the risk of falls, particularly in older adults. If you have concerns, discuss them 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.
There is a risk of harm to the unborn baby if this medication is taken during pregnancy. If you become pregnant or suspect you are pregnant while taking this drug, contact your doctor immediately. Taking this medication late in pregnancy may increase the risk of respiratory or feeding problems, low body temperature, or withdrawal symptoms in the newborn, so it is essential to discuss this with your doctor.
After taking this drug, avoid operating a vehicle or engaging in any activities that require alertness, as it may cause drowsiness. This effect can persist into the next day, so refrain from such tasks until you feel fully awake and alert.
When used nightly for an extended period (more than a few weeks), sleep medications like this one may lose their effectiveness in addressing sleep issues due to the development of tolerance. Therefore, it is recommended to use this medication for a short duration only. If your sleep problems persist, consult your doctor for further guidance.
If you are taking this medication long-term, your doctor may recommend regular blood tests to monitor your condition. Be sure to discuss this with your doctor.
It is crucial to avoid consuming alcohol while taking this drug, and do not take the medication if you have had alcohol that evening or before bedtime. Additionally, consult your doctor before using marijuana, cannabis, or any prescription or over-the-counter medications that may cause drowsiness or impair your reactions.
Some individuals taking sleep medications have reported engaging in activities such as driving, cooking, eating, or having sex while not fully awake, often without any memory of doing so. If you experience such episodes, inform your doctor promptly.
This medication can cause drowsiness and reduced alertness, increasing the risk of falls, particularly in older adults. If you have concerns, discuss them 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.
There is a risk of harm to the unborn baby if this medication is taken during pregnancy. If you become pregnant or suspect you are pregnant while taking this drug, contact your doctor immediately. Taking this medication late in pregnancy may increase the risk of respiratory or feeding problems, low body temperature, or withdrawal symptoms in the newborn, so it is essential to discuss this with your doctor.
Overdose Information
Overdose Symptoms:
- Extreme drowsiness
- Confusion
- Slurred speech
- Ataxia (loss of coordination)
- Hypotension (low blood pressure)
- Bradycardia (slow heart rate)
- Hypoventilation (shallow breathing)
- Coma
What to Do:
Seek immediate medical attention or call 911. For poison control, call 1-800-222-1222. Management is primarily supportive, including maintaining a patent airway, monitoring vital signs, and administering intravenous fluids. Flumazenil, a benzodiazepine receptor antagonist, may be considered in severe cases but carries risks (e.g., seizures).
Drug Interactions
Contraindicated Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, nelfinavir, clarithromycin, nefazodone) due to increased estazolam levels and risk of excessive sedation/respiratory depression.
- Opioids (concomitant use significantly increases risk of profound sedation, respiratory depression, coma, and death).
Major Interactions
- Alcohol (increased CNS depression)
- Other CNS depressants (e.g., other benzodiazepines, barbiturates, tricyclic antidepressants, antihistamines, antipsychotics, general anesthetics, skeletal muscle relaxants) - increased risk of sedation, respiratory depression.
- Moderate CYP3A4 inhibitors (e.g., erythromycin, diltiazem, verapamil, fluconazole) - may increase estazolam levels.
Moderate Interactions
- Grapefruit juice (may inhibit CYP3A4, increasing estazolam levels)
- Cimetidine (may inhibit estazolam metabolism)
- Digoxin (benzodiazepines may increase digoxin levels in some cases, monitor)
Minor Interactions
- Theophylline (may antagonize benzodiazepine effects)
Monitoring
Baseline Monitoring
Medical history (including substance abuse)
Rationale: To assess risk of dependence, abuse, and contraindications.
Timing: Prior to initiation
Mental status examination
Rationale: To establish baseline cognitive function and assess for underlying psychiatric conditions.
Timing: Prior to initiation
Liver function tests (LFTs)
Rationale: To assess hepatic impairment, which may require dose adjustment.
Timing: Prior to initiation, especially in patients with suspected hepatic dysfunction
Routine Monitoring
Efficacy (sleep onset, duration, quality)
Frequency: Regularly during treatment, especially during initial weeks
Target: Improved sleep parameters
Action Threshold: Lack of efficacy after appropriate trial, consider alternative or re-evaluate diagnosis.
Adverse effects (e.g., daytime sedation, dizziness, ataxia, cognitive impairment, paradoxical reactions)
Frequency: Regularly, especially during initial weeks and with dose changes
Target: Absence or minimal tolerable side effects
Action Threshold: Significant or intolerable side effects, consider dose reduction or discontinuation.
Signs of tolerance, dependence, or withdrawal symptoms upon discontinuation
Frequency: Throughout treatment, particularly with prolonged use
Target: Absence of these signs
Action Threshold: Development of tolerance/dependence, consider tapering or alternative strategies. Withdrawal symptoms upon discontinuation require slow tapering.
Respiratory status (especially with concomitant opioid use or respiratory compromise)
Frequency: As clinically indicated, particularly at initiation or dose changes
Target: Normal respiratory rate and effort
Action Threshold: Bradypnea, hypoventilation, or respiratory distress, requires immediate intervention.
Symptom Monitoring
- Excessive daytime sleepiness
- Dizziness
- Lightheadedness
- Ataxia (impaired coordination)
- Confusion
- Memory impairment (anterograde amnesia)
- Paradoxical reactions (e.g., agitation, aggression, hallucinations, worsening insomnia)
- Signs of depression or suicidal ideation (especially in patients with pre-existing psychiatric conditions)
- Respiratory depression (shallow breathing, difficulty breathing)
Special Patient Groups
Pregnancy
Estazolam is classified as Pregnancy Category X. It is contraindicated in pregnant women due to evidence of fetal risk and potential for congenital malformations (e.g., cleft lip/palate) and neonatal flaccidity, respiratory depression, and withdrawal symptoms if used during pregnancy, especially in the first trimester or near term.
Trimester-Specific Risks:
First Trimester:
Increased risk of congenital malformations (e.g., cleft lip/palate).
Second Trimester:
Potential for fetal CNS depression and growth restriction.
Third Trimester:
Risk of neonatal flaccidity, respiratory depression, hypothermia, and withdrawal symptoms (e.g., irritability, hypertonia, tremors, feeding difficulties) in the newborn.
Lactation
Estazolam is excreted into breast milk. Due to the potential for serious adverse reactions in breastfed infants (e.g., sedation, poor feeding, weight loss, respiratory depression), breastfeeding is generally not recommended during estazolam therapy. The decision should weigh the importance of the drug to the mother versus the risk to the infant.
Infant Risk:
L3 (Moderate risk) - Potential for sedation, lethargy, poor feeding, and respiratory depression in the infant. Long half-life may lead to accumulation.
Pediatric Use
Safety and effectiveness in pediatric patients (under 18 years of age) have not been established. Use is generally not recommended.
Geriatric Use
Elderly patients are more sensitive to the effects of benzodiazepines and may be at increased risk for adverse effects such as sedation, dizziness, ataxia, and falls. A lower initial dose (e.g., 0.5 mg) is recommended, and dosage should be carefully titrated based on individual response and tolerability.
Clinical Information
Clinical Pearls
- Estazolam is a short-term hypnotic; prolonged use (beyond 7-10 days) is generally discouraged due to risk of dependence and withdrawal.
- Patients should be advised to take estazolam immediately before going to bed, as it has a relatively rapid onset of action.
- Warn patients about the potential for next-day residual sedation, especially with higher doses or in sensitive individuals.
- Emphasize the critical importance of avoiding alcohol and other CNS depressants due to the risk of severe respiratory depression and sedation.
- Educate patients on the risks of dependence, tolerance, and withdrawal symptoms, and the need for gradual tapering if discontinuing after prolonged use.
- Consider non-pharmacological interventions for insomnia (e.g., CBT-I, sleep hygiene) as first-line or adjunctive therapy.
Alternative Therapies
- Other benzodiazepine receptor agonists (BZRAs) for insomnia: zolpidem, zaleplon, eszopiclone (Z-drugs)
- Other benzodiazepines for insomnia: temazepam, triazolam, flurazepam
- Melatonin receptor agonists: ramelteon
- Orexin receptor antagonists: suvorexant, lemborexant, daridorexant
- Antidepressants with sedative properties: trazodone, doxepin (low dose)
- Antihistamines: diphenhydramine, doxylamine
- Non-pharmacological: Cognitive Behavioral Therapy for Insomnia (CBT-I), sleep hygiene education, relaxation techniques.
Cost & Coverage
Average Cost:
$10 - $50 per 30 tablets (generic 1mg or 2mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor promptly. To ensure safe use, never share your medication with others or take someone else's medication. This medication is accompanied by a Medication Guide, which provides crucial information. Please read this guide carefully and review it again whenever you receive a refill. If you have any questions or concerns about this medication, consult your doctor, pharmacist, or 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 details about the medication taken, the quantity, and the time it occurred.