Estazolam 1mg Tablets

Manufacturer NOVITIUM PHARMA Active Ingredient Estazolam(es TA zoe lam) Pronunciation es TA zoe lam
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.
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Drug Class
Hypnotic
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Pharmacologic Class
Benzodiazepine
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Pregnancy Category
Category D
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FDA Approved
Dec 1989
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DEA Schedule
Schedule IV

Overview

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What is this medicine?

Estazolam is a medication used to treat insomnia, which is trouble falling or staying asleep. It belongs to a class of drugs called benzodiazepines. It works by calming your brain activity to help you fall asleep faster and stay asleep longer.
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How to Use This Medicine

Taking Your Medication

To use this medication correctly, follow your doctor's instructions and read all the information provided. 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 sleep difficulties 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 a bathroom. 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 in your area.

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, do not take it more frequently than directed by your doctor.
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Lifestyle & Tips

  • Take exactly as prescribed, usually just before bedtime. Do not take more than prescribed.
  • Avoid alcohol and other central nervous system depressants (e.g., opioids, cold/allergy medicines, other sedatives) while taking estazolam, as this can lead to dangerous side effects like severe drowsiness, breathing problems, coma, and death.
  • Do not drive or operate heavy machinery until you know how this medication affects you, especially the morning after taking it.
  • Do not stop taking estazolam suddenly, especially if you have been taking it regularly for some time. This can cause withdrawal symptoms, which can be serious. Your doctor will tell you how to slowly reduce your dose.
  • Report any unusual thoughts or behaviors, such as aggression, agitation, hallucinations, or worsening insomnia, to your doctor immediately.
  • This medication is intended for short-term use. Discuss with your doctor if you need to use it for longer periods.
  • Store in a safe place away from children and others who might misuse it.
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Available Forms & Alternatives

Dosing & Administration

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Adult Dosing

Standard Dose: 1 mg orally at bedtime
Dose Range: 0.5 - 2 mg

Condition-Specific Dosing:

elderly_or_debilitated: Initial dose 0.5 mg orally at bedtime, may increase to 1 mg if needed and tolerated.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established
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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, monitor for increased sedation.
Dialysis: Not significantly dialyzable. No specific adjustment recommended, but monitor for effects.

Hepatic Impairment:

Mild: No specific adjustment recommended, use with caution.
Moderate: Consider lower initial dose (0.5 mg) and titrate carefully. Monitor for increased sedation.
Severe: Consider lower initial dose (0.5 mg) and titrate carefully. Avoid if possible due to impaired clearance and increased risk of adverse effects. Monitor closely.

Pharmacology

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Mechanism of Action

Estazolam is a benzodiazepine that binds to stereospecific benzodiazepine receptors on the postsynaptic GABA-A neuron in the central nervous system. This binding enhances the inhibitory effects of gamma-aminobutyric acid (GABA), leading to increased chloride ion influx through the GABA-gated chloride channel, hyperpolarization of the neuron, and decreased neuronal excitability. This results in sedative, hypnotic, anxiolytic, anticonvulsant, and muscle relaxant properties.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 93%
Tmax: 0.5 to 1.6 hours
FoodEffect: Food may delay Tmax but does not significantly affect the extent of absorption (AUC).

Distribution:

Vd: Approximately 1.0 to 2.0 L/kg
ProteinBinding: Approximately 93% (primarily to albumin)
CnssPenetration: Yes

Elimination:

HalfLife: Approximately 10 to 24 hours (average 17 hours)
Clearance: Not available
ExcretionRoute: Primarily renal (as metabolites), small amount in feces
Unchanged: <5% (in urine)
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Pharmacodynamics

OnsetOfAction: 15 to 60 minutes
PeakEffect: 1 to 2 hours
DurationOfAction: 6 to 8 hours (hypnotic effect), residual effects may last longer

Safety & Warnings

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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 concomitant use of benzodiazepines, including estazolam, and opioids may result in profound sedation, respiratory depression, coma, and death. Because of these risks, reserve concomitant prescribing of these drugs for use in patients for whom alternative treatment options are inadequate. Observational studies have demonstrated that concomitant use of opioid analgesics and benzodiazepines increases the risk of drug-related mortality compared to use of opioid analgesics alone. If a decision is made to prescribe estazolam concomitantly with opioids, prescribe the lowest effective dosages and minimum durations of concomitant use, and follow patients closely for signs and symptoms of respiratory depression and sedation. Advise both patients and caregivers about the risks of respiratory depression and sedation when estazolam is used with opioids. Advise patients not to drive or operate heavy machinery until the effects of concomitant use with opioids have been determined. The use of benzodiazepines, including estazolam, exposes patients to the risks of abuse, misuse, and addiction, which can lead to overdose or death. Before prescribing estazolam, assess each patient’s risk for abuse, misuse, and addiction. Educate patients and their families about these risks, signs, and symptoms of abuse, misuse, and addiction, and proper disposal of unused drug. The continued use of benzodiazepines, including estazolam, may lead to clinically significant physical dependence. The risks of withdrawal increase with longer treatment duration or higher doses. Abrupt discontinuation or rapid dosage reduction of estazolam after continued use may precipitate acute withdrawal reactions, which can be life-threatening. To reduce the risk of withdrawal reactions, use a gradual taper to discontinue estazolam or reduce the dosage.
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Side Effects

Urgent 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 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
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. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:

Feeling sleepy the next day
Dry mouth
Upset stomach
Dizziness, tiredness, or weakness
Headache
Feeling nervous and 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.
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Seek Immediate Medical Attention If You Experience:

  • Severe drowsiness or sedation that persists into the next day
  • Difficulty breathing or shallow breathing
  • Unusual changes in behavior or mood (e.g., agitation, aggression, confusion, hallucinations)
  • Memory problems (not remembering events after taking the pill)
  • Worsening of insomnia or new sleep problems
  • Signs of an allergic reaction (e.g., rash, itching, swelling, severe dizziness, trouble breathing)
  • Symptoms of withdrawal if stopped suddenly (e.g., anxiety, tremors, sweating, muscle cramps, seizures)
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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. There are numerous drugs that can have this effect, so consult your doctor or pharmacist if you are unsure.
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 issues 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 adjust the dosage of any medication without first consulting your doctor.
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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.

Prolonged nightly use of sleep medications like this one for more than a few weeks can lead to reduced efficacy in addressing sleep issues, a phenomenon known as 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.

Avoid consuming alcohol while on this medication, and do not take it 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 drugs 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 these events. If you experience such episodes, inform your doctor promptly.

This medication can cause drowsiness and decreased 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 taking this medication, as you may be more susceptible to 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 suspect you are pregnant while on this medication, 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. It is crucial to discuss this with your doctor to understand the potential risks and benefits.
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Overdose Information

Overdose Symptoms:

  • Extreme drowsiness
  • Confusion
  • Slurred speech
  • Slowed reflexes
  • Lack of coordination (ataxia)
  • Hypotension (low blood pressure)
  • Respiratory depression (slow, shallow breathing)
  • Coma

What to Do:

Seek immediate medical attention or call 911. For poison control, call 1-800-222-1222. Overdose treatment may include supportive care, maintaining airway, and administration of flumazenil (a benzodiazepine receptor antagonist) in severe cases, though flumazenil carries risks of withdrawal and seizures.

Drug Interactions

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Contraindicated Interactions

  • Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, nelfinavir) due to significantly increased estazolam exposure and risk of prolonged sedation and respiratory depression.
  • Opioids (due to risk of profound sedation, respiratory depression, coma, and death; Black Box Warning).
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Major Interactions

  • Other CNS depressants (e.g., alcohol, barbiturates, other benzodiazepines, tricyclic antidepressants, antihistamines, antipsychotics, general anesthetics, skeletal muscle relaxants) due to additive CNS depressant effects.
  • Sodium oxybate (concomitant use is contraindicated with other sedative hypnotics).
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Moderate Interactions

  • Moderate CYP3A4 inhibitors (e.g., erythromycin, diltiazem, verapamil, grapefruit juice) may increase estazolam levels and enhance its effects.
  • Drugs that induce CYP3A4 (e.g., carbamazepine, phenytoin, rifampin) may decrease estazolam levels and efficacy.
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Minor Interactions

  • Not available

Monitoring

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Baseline Monitoring

Assessment of sleep disorder

Rationale: To confirm diagnosis of insomnia and rule out underlying medical or psychiatric conditions.

Timing: Prior to initiation of therapy

Medical history (including substance use)

Rationale: To identify risk factors for abuse, dependence, and contraindications.

Timing: Prior to initiation of therapy

Renal and hepatic function tests

Rationale: To assess baseline organ function, especially in elderly or patients with pre-existing conditions, as dose adjustments may be needed.

Timing: Prior to initiation of therapy (if clinically indicated)

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Routine Monitoring

Efficacy (sleep onset, duration, quality)

Frequency: Regularly during therapy, especially during initial weeks and dose adjustments

Target: Improved sleep parameters, reduced insomnia symptoms

Action Threshold: Lack of efficacy or worsening symptoms may indicate need for re-evaluation or alternative therapy.

Adverse effects (e.g., daytime drowsiness, dizziness, ataxia, cognitive impairment, paradoxical reactions)

Frequency: Regularly during therapy, especially during initial weeks and dose adjustments

Target: Absence or minimal tolerable side effects

Action Threshold: Significant or intolerable side effects may require dose reduction or discontinuation.

Signs of tolerance, dependence, or withdrawal symptoms

Frequency: Periodically, especially with prolonged use

Target: Absence of signs of dependence or withdrawal

Action Threshold: Development of tolerance or withdrawal symptoms upon dose reduction/discontinuation indicates dependence and requires careful tapering.

Respiratory status (especially with concomitant opioid use or respiratory compromise)

Frequency: As clinically indicated

Target: Normal respiratory rate and effort

Action Threshold: Respiratory depression requires immediate intervention.

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Symptom Monitoring

  • Excessive daytime drowsiness
  • Dizziness
  • Lightheadedness
  • Ataxia (impaired coordination)
  • Confusion
  • Memory impairment (anterograde amnesia)
  • Paradoxical reactions (e.g., agitation, aggression, hallucinations, worsening insomnia)
  • Respiratory depression (especially with opioids)
  • Signs of withdrawal upon discontinuation (e.g., rebound insomnia, anxiety, tremors, seizures)

Special Patient Groups

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Pregnancy

Estazolam is Pregnancy Category D. It should not be used during pregnancy unless the potential benefit justifies the potential risk to the fetus. Benzodiazepines can cause fetal harm when administered to pregnant women.

Trimester-Specific Risks:

First Trimester: Increased risk of congenital malformations (e.g., cleft lip/palate) has been suggested with benzodiazepine use, though data are conflicting and the absolute risk is low.
Second Trimester: Not well-studied, but continued exposure carries risks.
Third Trimester: Use during the third trimester or near delivery may result in 'floppy infant syndrome' (hypotonia, lethargy, feeding difficulties, hypothermia, respiratory depression) and neonatal withdrawal symptoms (e.g., irritability, hypertonia, tremors, feeding difficulties, seizures) after birth.
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Lactation

Estazolam is excreted into breast milk. Due to the potential for sedation, feeding difficulties, and withdrawal symptoms in the breastfed infant, use is generally not recommended. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Infant Risk: L4 (Possibly Hazardous). Potential for sedation, lethargy, poor feeding, and weight gain in the infant. Long-term effects on neurodevelopment are unknown.
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Pediatric Use

Safety and effectiveness in pediatric patients (under 18 years of age) have not been established. Use is not recommended.

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Geriatric Use

Elderly patients are more sensitive to the effects of benzodiazepines and are at increased risk for adverse effects such as excessive sedation, dizziness, ataxia, falls, and cognitive impairment. The initial dose should be reduced to 0.5 mg at bedtime, and the dose should be titrated carefully based on individual response and tolerability. Monitor closely for CNS depression.

Clinical Information

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Clinical Pearls

  • Estazolam is a short-to-intermediate acting benzodiazepine hypnotic, suitable for short-term management of insomnia.
  • Due to its potential for abuse, dependence, and withdrawal, it should be prescribed for the shortest duration possible and at the lowest effective dose.
  • Patients should be warned about the risk of complex sleep behaviors (e.g., sleep-driving, preparing and eating food, making phone calls) while not fully awake, with amnesia for the event.
  • Rebound insomnia and withdrawal symptoms can occur upon abrupt discontinuation, especially after prolonged use. Tapering is crucial.
  • Avoid concomitant use with alcohol and other CNS depressants due to additive effects and increased risk of respiratory depression.
  • The Black Box Warning regarding concomitant opioid use is critical; educate patients thoroughly on this risk.
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Alternative Therapies

  • Other benzodiazepine receptor agonists (BZRAs) for insomnia: zolpidem, zaleplon, eszopiclone (non-benzodiazepine hypnotics)
  • 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 (OTC, generally not recommended for chronic insomnia)
  • Cognitive Behavioral Therapy for Insomnia (CBT-I) - often considered first-line non-pharmacological treatment.
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Cost & Coverage

Average Cost: Varies widely, typically $10-$50 per 30 tablets (generic 1mg)
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 2 (Generic)
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General Drug Facts

If your symptoms or health issues persist or worsen, it is 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, a patient fact sheet that provides crucial information. Please read this guide carefully and review it again whenever you refill your prescription. 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. Be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.