Alprazolam ER 1mg 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 panic attacks.
Drug Class
Anxiolytic; Sedative-Hypnotic
Pharmacologic Class
Benzodiazepine; GABA-A Receptor Agonist
Pregnancy Category
Category D
FDA Approved
Aug 2003
DEA Schedule
Schedule IV
Overview
What is this medicine?
Alprazolam ER is an extended-release medication used to treat panic disorder. It belongs to a class of drugs called benzodiazepines, which work by calming the brain and nerves. Because it's extended-release, you take it once a day, and it releases the medicine slowly over time.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take this medication with or without food. If it causes stomach upset, taking it with food may help. It's essential to swallow the medication whole and not chew, break, or crush it.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding bathrooms. Keep it in a safe location where children and pets cannot access it, and consider using a locked box or area to prevent unauthorized use. 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 or explore local drug take-back programs.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take this medication with or without food. If it causes stomach upset, taking it with food may help. It's essential to swallow the medication whole and not chew, break, or crush it.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding bathrooms. Keep it in a safe location where children and pets cannot access it, and consider using a locked box or area to prevent unauthorized use. 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 or explore local drug take-back programs.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Avoid alcohol and other CNS depressants (e.g., opioids, sedating antihistamines) as they can increase drowsiness and breathing problems.
- Do not drive or operate heavy machinery until you know how this medication affects you.
- Do not stop taking this medication suddenly, especially after prolonged use, as it can cause severe withdrawal symptoms. Your doctor will help you taper off slowly.
- Take exactly as prescribed; do not crush, chew, or break the extended-release tablet.
Available Forms & Alternatives
Available Strengths:
- Alprazolam 0.25mg Tablets
- Alprazolam 0.5mg Tablets
- Alprazolam 1mg Tablets
- Alprazolam 2mg Tablets
- Alprazolam Con 1mg/ml Solution
- Alprazolam 2mg ODT Tablets
- Alprazolam 1mg ODT Tablets
- Alprazolam 0.5mg ODT Tablets
- Alprazolam 0.25mg ODT Tablets
- Alprazolam ER 1mg Tablets
- Alprazolam ER 2mg Tablets
- Alprazolam XR 3mg Tablets
- Alprazolam ER 0.5mg Tablets
Dosing & Administration
Adult Dosing
Standard Dose:
Panic Disorder: Initial 0.5 mg to 1 mg once daily. Titrate every 3-4 days by no more than 1 mg/day. Maintenance 3 mg to 6 mg once daily.
Dose Range:
0.5 - 10 mg
Condition-Specific Dosing:
Panic Disorder:
Initial 0.5 mg to 1 mg once daily. Titrate every 3-4 days by no more than 1 mg/day. Maintenance 3 mg to 6 mg once daily. Max 10 mg/day.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended, use with caution.
Moderate:
No specific adjustment recommended, use with caution.
Severe:
Use with caution; monitor for increased adverse effects.
Dialysis:
Not significantly dialyzable; use with caution.
Hepatic Impairment:
Mild:
Consider lower initial dose (e.g., 0.5 mg once daily).
Moderate:
Consider lower initial dose (e.g., 0.5 mg once daily) and slower titration.
Severe:
Contraindicated in severe hepatic impairment (e.g., cirrhosis) due to increased half-life and risk of encephalopathy.
Pharmacology
Mechanism of Action
Alprazolam, a benzodiazepine, binds to stereospecific benzodiazepine receptors on the postsynaptic GABA-A receptor complex in the central nervous system (CNS). This binding enhances the inhibitory effects of gamma-aminobutyric acid (GABA), leading to increased chloride ion influx, neuronal hyperpolarization, and decreased neuronal excitability. This results in anxiolytic, sedative, hypnotic, muscle relaxant, and anticonvulsant effects.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 80%
Tmax:
5-11 hours (for ER formulation)
FoodEffect:
Food delays absorption (increased Tmax) but does not significantly affect the extent of absorption (AUC).
Distribution:
Vd:
0.9-1.2 L/kg
ProteinBinding:
Approximately 80% (primarily to albumin)
CnssPenetration:
Yes
Elimination:
HalfLife:
10.6-20.3 hours (for ER formulation)
Clearance:
Not available
ExcretionRoute:
Renal (primarily as metabolites)
Unchanged:
<1% (in urine)
Pharmacodynamics
OnsetOfAction:
1-2 hours (for ER formulation)
PeakEffect:
5-11 hours (for ER formulation)
DurationOfAction:
Approximately 24 hours (for ER formulation)
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 Help Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. 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
Signs of depression, suicidal thoughts, or mood changes, including:
+ Emotional ups and downs
+ Abnormal thinking
+ Anxiety
+ Lack of interest in life
Change in balance
Shortness of breath
Severe dizziness or fainting
Confusion
Memory problems or loss
Difficulty speaking
Trouble urinating
Difficulty controlling body movements
Muscle twitching
Rapid heartbeat
Blurred vision
Changes in menstrual period (in women)
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 contact your doctor or seek medical help if you experience any of the following:
Dizziness, drowsiness, fatigue, or weakness
Dry mouth
Changes in appetite
Constipation, diarrhea, vomiting, or stomach upset
Changes in sex drive
Sexual problems
Weight gain or loss
Sleep disturbances
Headache
Excessive sweating
This is not an exhaustive list of possible side effects. If you have concerns or questions 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 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
Signs of depression, suicidal thoughts, or mood changes, including:
+ Emotional ups and downs
+ Abnormal thinking
+ Anxiety
+ Lack of interest in life
Change in balance
Shortness of breath
Severe dizziness or fainting
Confusion
Memory problems or loss
Difficulty speaking
Trouble urinating
Difficulty controlling body movements
Muscle twitching
Rapid heartbeat
Blurred vision
Changes in menstrual period (in women)
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 contact your doctor or seek medical help if you experience any of the following:
Dizziness, drowsiness, fatigue, or weakness
Dry mouth
Changes in appetite
Constipation, diarrhea, vomiting, or stomach upset
Changes in sex drive
Sexual problems
Weight gain or loss
Sleep disturbances
Headache
Excessive sweating
This is not an exhaustive list of possible side effects. If you have concerns or questions 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 sedation
- Difficulty breathing or shallow breathing
- Extreme confusion or disorientation
- Unusual changes in mood or behavior (e.g., agitation, aggression, hallucinations)
- Yellowing of skin or eyes (jaundice)
- Signs of an allergic reaction (e.g., rash, itching, swelling, severe dizziness, trouble 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 symptoms you experienced.
If you have been diagnosed with glaucoma.
* If you are currently taking any of the following medications: Clarithromycin, itraconazole, or ketoconazole. Your doctor or pharmacist can provide guidance on other medications that should not be taken in conjunction with this drug.
Additionally, if you are breast-feeding, please note that you should not breast-feed 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. Do not initiate, discontinue, or modify 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, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have been diagnosed with glaucoma.
* If you are currently taking any of the following medications: Clarithromycin, itraconazole, or ketoconazole. Your doctor or pharmacist can provide guidance on other medications that should not be taken in conjunction with this drug.
Additionally, if you are breast-feeding, please note that you should not breast-feed 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. Do not initiate, discontinue, or modify 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.
If you have been using this medication for an extended period or at high doses, you may develop tolerance, which means it may not be as effective, and you may require higher doses to achieve the same effect. If you notice this medication is no longer working as well as it should, contact your doctor. Do not exceed the prescribed dose.
Until you understand how this medication affects you, avoid operating a vehicle or engaging in activities that require your full attention. Additionally, refrain from consuming alcohol while taking this medication.
Before using marijuana, other forms of cannabis, or any prescription or over-the-counter medications that may cause drowsiness, consult with your doctor.
If you are taking this medication long-term, your doctor may recommend regular blood tests to monitor your condition.
If you regularly consume grapefruit juice or eat grapefruit, discuss this with your doctor, as it may interact with your medication. Similarly, if you start or stop smoking, inform your doctor, as your dosage may need to be adjusted.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
This medication may pose a risk to the unborn baby if taken during pregnancy. If you become pregnant or are already pregnant while taking 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. Discuss the potential risks with your doctor.
If you have been using this medication for an extended period or at high doses, you may develop tolerance, which means it may not be as effective, and you may require higher doses to achieve the same effect. If you notice this medication is no longer working as well as it should, contact your doctor. Do not exceed the prescribed dose.
Until you understand how this medication affects you, avoid operating a vehicle or engaging in activities that require your full attention. Additionally, refrain from consuming alcohol while taking this medication.
Before using marijuana, other forms of cannabis, or any prescription or over-the-counter medications that may cause drowsiness, consult with your doctor.
If you are taking this medication long-term, your doctor may recommend regular blood tests to monitor your condition.
If you regularly consume grapefruit juice or eat grapefruit, discuss this with your doctor, as it may interact with your medication. Similarly, if you start or stop smoking, inform your doctor, as your dosage may need to be adjusted.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
This medication may pose a risk to the unborn baby if taken during pregnancy. If you become pregnant or are already pregnant while taking 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. Discuss the potential risks with your doctor.
Overdose Information
Overdose Symptoms:
- Somnolence (extreme drowsiness)
- Confusion
- Impaired coordination (ataxia)
- Diminished reflexes
- Slurred speech
- Hypotension (low blood pressure)
- Respiratory depression
- Coma
- Death
What to Do:
Seek immediate medical attention. Call 911 or Poison Control at 1-800-222-1222. Flumazenil may be used as an antidote but carries risks, especially in patients with long-term benzodiazepine use or co-ingestion of tricyclic antidepressants.
Drug Interactions
Contraindicated Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, nefazodone)
Major Interactions
- Opioids (increased risk of respiratory depression, profound sedation, coma, and death)
- Other CNS depressants (e.g., alcohol, barbiturates, other benzodiazepines, sedating antihistamines, tricyclic antidepressants, antipsychotics, general anesthetics)
- Moderate CYP3A4 inhibitors (e.g., fluconazole, erythromycin, clarithromycin, diltiazem, verapamil, grapefruit juice)
- Cimetidine
- Fluvoxamine
Moderate Interactions
- Oral contraceptives (may decrease alprazolam clearance)
- Digoxin (may increase digoxin levels)
- Imipramine, desipramine (may increase plasma levels of these antidepressants)
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Mental status and psychiatric symptoms
Rationale: To establish baseline for efficacy and adverse effects.
Timing: Prior to initiation
Liver function tests (LFTs)
Rationale: Alprazolam is metabolized by the liver; assess for baseline hepatic impairment.
Timing: Prior to initiation, especially in patients with suspected hepatic dysfunction
Renal function (BUN, creatinine)
Rationale: To assess baseline renal function, though dose adjustment is not typically needed for mild-moderate impairment.
Timing: Prior to initiation, especially in patients with suspected renal dysfunction
Routine Monitoring
Efficacy (reduction in panic attacks/anxiety)
Frequency: Regularly during titration and maintenance
Target: Individualized
Action Threshold: Lack of efficacy or worsening symptoms may require dose adjustment or alternative therapy.
Adverse effects (e.g., sedation, dizziness, ataxia, cognitive impairment)
Frequency: Regularly, especially during titration
Target: Minimal to tolerable
Action Threshold: Intolerable side effects may require dose reduction or discontinuation.
Signs of dependence or withdrawal symptoms (upon discontinuation or dose reduction)
Frequency: Throughout therapy and during tapering
Target: Absence of severe symptoms
Action Threshold: Presence of withdrawal symptoms indicates dependence and requires careful, slow tapering.
Respiratory status (especially with concomitant opioid use)
Frequency: Regularly, particularly at initiation or dose increase of either drug
Target: Normal respiratory rate and effort
Action Threshold: Bradypnea, hypoventilation, or respiratory distress requires immediate intervention.
Symptom Monitoring
- Excessive sedation
- Drowsiness
- Dizziness
- Ataxia (impaired coordination)
- Confusion
- Memory impairment
- Slurred speech
- Paradoxical reactions (e.g., agitation, aggression, hallucinations)
- Respiratory depression
- Signs of withdrawal (e.g., seizures, tremors, anxiety, insomnia, palpitations, sweating, muscle cramps)
Special Patient Groups
Pregnancy
Alprazolam is classified as Pregnancy Category D. It should not be used during pregnancy, especially during the first trimester, due to increased risk of congenital malformations (e.g., cleft lip/palate). Use in the third trimester or near delivery can lead to neonatal flaccidity, respiratory depression, feeding difficulties, and withdrawal symptoms in the newborn.
Trimester-Specific Risks:
First Trimester:
Increased risk of congenital malformations (e.g., cleft lip/palate).
Second Trimester:
Potential for fetal growth restriction; less data on specific malformations.
Third Trimester:
Risk of neonatal withdrawal syndrome (irritability, hypertonia, tremors, feeding difficulties, respiratory distress) and 'floppy infant syndrome' (hypotonia, lethargy, hypothermia) if used near term.
Lactation
Alprazolam and its active metabolites are excreted into breast milk. Due to potential for sedation, feeding difficulties, and withdrawal symptoms in the infant, use is generally not recommended during breastfeeding. If use is necessary, monitor the infant closely for adverse effects.
Infant Risk:
Moderate risk (L3). Potential for sedation, lethargy, poor feeding, and withdrawal symptoms upon discontinuation in the infant. Long-term effects on neurodevelopment are unknown.
Pediatric Use
Safety and effectiveness in pediatric patients (<18 years of age) have not been established. Use is generally not recommended due to lack of data and potential for adverse effects.
Geriatric Use
Elderly patients may be more sensitive to the effects of benzodiazepines, including increased risk of sedation, dizziness, falls, and cognitive impairment. Lower initial doses (e.g., 0.5 mg once daily) and slower titration are recommended. Monitor closely for adverse effects.
Clinical Information
Clinical Pearls
- Alprazolam ER is designed for once-daily dosing and should not be crushed, chewed, or broken, as this will destroy the extended-release properties and lead to rapid absorption and potential toxicity.
- Due to the risk of dependence and withdrawal, alprazolam ER should be tapered slowly when discontinuing, typically by no more than 0.5 mg every 3 days, or even slower in some patients.
- Patients should be warned about the additive CNS depressant effects of alcohol and other sedatives.
- Paradoxical reactions (e.g., excitement, agitation, rage) can occur, especially in pediatric, geriatric, or psychiatric patients.
- Consider alternative treatments for anxiety or panic disorder, such as SSRIs or SNRIs, especially for long-term management, due to the risks associated with benzodiazepine use.
Alternative Therapies
- Other benzodiazepines (e.g., clonazepam, lorazepam, diazepam)
- Selective Serotonin Reuptake Inhibitors (SSRIs) (e.g., sertraline, paroxetine, fluoxetine)
- Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) (e.g., venlafaxine, duloxetine)
- Buspirone
- Beta-blockers (e.g., propranolol for situational anxiety)
- Cognitive Behavioral Therapy (CBT)
Cost & Coverage
Average Cost:
$30 - $100 per 30 tablets (1mg ER)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (generic)
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, which is a crucial patient fact sheet. Please read it 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 other 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 substance taken, the amount, and the time it occurred.