Alprazolam XR 3mg Tablets

Manufacturer AUROBINDO PHARMA Active Ingredient Alprazolam Extended-Release Tablets(al PRAY zoe lam) Pronunciation al-PRAY-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 panic attacks.
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Drug Class
Anxiolytic, Sedative-Hypnotic
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Pharmacologic Class
Benzodiazepine, GABA-A Receptor Agonist
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Pregnancy Category
Category D
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FDA Approved
Aug 2003
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DEA Schedule
Schedule IV

Overview

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What is this medicine?

Alprazolam XR is an extended-release tablet used to treat panic disorder. It belongs to a class of medicines called benzodiazepines. It works by calming the brain and nerves, helping to reduce feelings of anxiety and panic. The 'XR' means it releases the medicine slowly over time, so you usually only need to take it once a day.
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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. You can take this medication with or without food. If it causes stomach upset, taking it with food may help. Swallow the medication whole - do 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. Dispose of unused or expired medication by throwing it away. However, do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist. If you have questions about disposing of your medication, consult your pharmacist, who may be aware of drug take-back programs in your area.

Missing a Dose

If you miss a dose, take it as soon as you remember. However, if it is 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 a missed one.
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Lifestyle & Tips

  • Avoid alcohol and other central nervous system depressants (e.g., opioids, sedatives) while taking this medication, as it can increase drowsiness and dangerous breathing problems.
  • Do not drive or operate heavy machinery until you know how this medication affects you, as it can cause dizziness and drowsiness.
  • Do not stop taking this medication suddenly, especially if you have been taking it regularly for a long time, as this can cause withdrawal symptoms (e.g., seizures, severe anxiety). Your doctor will guide you on how to slowly reduce the dose.
  • Take exactly as prescribed; do not take more or less than directed.
  • Swallow the extended-release tablet whole; do not crush, chew, or break it.

Dosing & Administration

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Adult Dosing

Standard Dose: For panic disorder: Initial 0.5 mg to 1 mg once daily. Titrate by no more than 1 mg/day every 3-4 days. Maintenance dose typically 3 mg to 6 mg once daily. The 3mg tablet is a common maintenance dose.
Dose Range: 0.5 - 10 mg

Condition-Specific Dosing:

panic_disorder: Initial 0.5 mg to 1 mg once daily. Titrate as needed and tolerated up to a maximum of 10 mg/day. Average dose is 3 mg to 6 mg/day.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established (Safety and efficacy not established for panic disorder in patients under 18 years of age).
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Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment generally required.
Moderate: No specific dose adjustment generally required, but use with caution.
Severe: Use with caution; consider lower doses. Alprazolam is extensively metabolized, so renal impairment has less impact on clearance of parent drug.
Dialysis: Not significantly removed by dialysis. Use with caution.

Hepatic Impairment:

Mild: Use with caution; consider lower doses.
Moderate: Reduce initial dose by 50% or more. Titrate slowly and monitor closely.
Severe: Contraindicated or use with extreme caution; significant dose reduction (e.g., 50-75% reduction) is necessary. Monitor for increased adverse effects.
Confidence: Medium

Pharmacology

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Mechanism of Action

Alprazolam, a benzodiazepine, binds to specific benzodiazepine receptors on the gamma-aminobutyric acid (GABA)-A receptor complex in the central nervous system. This binding enhances the inhibitory effects of GABA, leading to increased chloride ion influx, hyperpolarization of the neuronal membrane, and decreased neuronal excitability. This results in anxiolytic, sedative, hypnotic, muscle relaxant, and anticonvulsant effects.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 90%
Tmax: 5-11 hours (for XR formulation)
FoodEffect: Food (high-fat meal) delays Tmax by approximately 25% and decreases Cmax by approximately 22%, but does not significantly affect AUC.

Distribution:

Vd: 0.9-1.2 L/kg
ProteinBinding: Approximately 80% (primarily to serum albumin)
CnssPenetration: Yes

Elimination:

HalfLife: 10.6-20.3 hours (for XR formulation)
Clearance: Approximately 0.6-1.0 mL/min/kg
ExcretionRoute: Renal (primarily as metabolites)
Unchanged: Less than 1%
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Pharmacodynamics

OnsetOfAction: Approximately 1-2 hours (for XR formulation)
PeakEffect: 5-11 hours (for XR formulation)
DurationOfAction: Approximately 12-16 hours (for XR formulation)
Confidence: Medium

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 Alprazolam XR, 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. Because of the risks of abuse, misuse, and addiction with benzodiazepines, use Alprazolam XR only in patients for whom alternative treatment options are inadequate. Assess each patient’s risk of abuse, misuse, and addiction prior to prescribing Alprazolam XR and monitor all patients receiving Alprazolam XR for the development of these behaviors or conditions.
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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
Signs of depression, suicidal thoughts, or mood changes, including:
+ Emotional ups and downs
+ Abnormal thinking
+ Anxiety
+ Lack of interest in life
Sudden change in balance
Shortness of breath
Severe dizziness or fainting
Confusion
Memory problems or loss
Difficulty speaking
Trouble urinating
Loss of control over 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 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:

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 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:

  • Extreme drowsiness or sedation
  • Difficulty breathing or shallow breathing
  • Unusual changes in mood or behavior (e.g., agitation, aggression, hallucinations)
  • Yellowing of the skin or eyes (jaundice)
  • Severe skin rash
  • Memory problems or confusion
  • Signs of an allergic reaction (e.g., rash, itching, swelling of face/tongue/throat, severe dizziness, trouble breathing)
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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, 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 advise you on other medications that should not be taken in combination 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 issues. Do not initiate, stop, or modify 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.

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 driving and engaging in activities that require alertness. Additionally, refrain from consuming alcohol while taking this medication.

Before using marijuana, other forms of cannabis, or prescription and over-the-counter (OTC) medications that can 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 can potentially harm an 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 these risks with your doctor.
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Overdose Information

Overdose Symptoms:

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

What to Do:

Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222. Overdose treatment may include supportive care, monitoring vital signs, and in severe cases, administration of flumazenil (a benzodiazepine receptor antagonist), though flumazenil carries risks, including precipitation of acute withdrawal and seizures.

Drug Interactions

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Contraindicated Interactions

  • Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, nefazodone, fluvoxamine, some macrolide antibiotics like clarithromycin, telithromycin, and protease inhibitors like ritonavir, indinavir, nelfinavir)
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Major Interactions

  • Opioids (increased risk of respiratory depression, profound sedation, coma, and death)
  • Other CNS depressants (e.g., alcohol, barbiturates, sedating antihistamines, antipsychotics, tricyclic antidepressants, muscle relaxants) - additive CNS depressant effects
  • Moderate CYP3A4 inhibitors (e.g., fluoxetine, sertraline, diltiazem, verapamil, cimetidine, grapefruit juice) - increased alprazolam concentrations
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Moderate Interactions

  • Digoxin (may increase digoxin levels)
  • Imipramine, desipramine (may increase plasma levels of these antidepressants)
  • Oral contraceptives (may inhibit alprazolam metabolism)
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Minor Interactions

  • Not available

Monitoring

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Baseline Monitoring

Mental status assessment (anxiety, panic symptoms)

Rationale: To establish baseline severity of symptoms and guide treatment.

Timing: Prior to initiation of therapy

Respiratory rate and oxygen saturation

Rationale: To assess baseline respiratory function, especially if co-prescribing with opioids or other CNS depressants.

Timing: Prior to initiation of therapy

Liver function tests (LFTs)

Rationale: Alprazolam is primarily metabolized by the liver; baseline assessment is important, especially in patients with suspected hepatic impairment.

Timing: Prior to initiation of therapy, if clinically indicated

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Routine Monitoring

Efficacy (reduction in panic attacks, anxiety symptoms)

Frequency: Regularly during titration and periodically during maintenance (e.g., monthly initially, then every 3-6 months)

Target: Patient-reported improvement in symptoms, reduction in panic attack frequency/severity

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 during titration and periodically during maintenance

Target: Minimal to tolerable side effects

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

Signs of abuse, misuse, or dependence

Frequency: At every visit

Target: Absence of drug-seeking behavior, escalating doses, or withdrawal symptoms upon dose reduction

Action Threshold: Presence of these signs requires reassessment of treatment plan, potential referral for substance use disorder.

Respiratory status (especially with concomitant opioid use)

Frequency: Regularly, especially during initiation or dose changes of either drug

Target: Normal respiratory rate and effort, no signs of respiratory depression

Action Threshold: Bradypnea, hypoventilation, or decreased oxygen saturation requires immediate medical attention.

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Symptom Monitoring

  • Excessive sedation
  • Dizziness
  • Ataxia (impaired coordination)
  • Confusion
  • Memory impairment
  • Slurred speech
  • Paradoxical reactions (e.g., agitation, aggression, hallucinations)
  • Signs of withdrawal upon discontinuation or dose reduction (e.g., rebound anxiety, insomnia, seizures, tremors, muscle cramps, vomiting, sweating)

Special Patient Groups

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Pregnancy

Alprazolam is classified as Pregnancy Category D. It should not be used during pregnancy unless the potential benefit justifies the potential risk to the fetus. There is evidence of human fetal risk based on adverse reaction data from investigational or marketing experience or studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

Trimester-Specific Risks:

First Trimester: Increased risk of congenital malformations (e.g., cleft lip/palate) has been suggested in some studies, though data are conflicting. Use during the first trimester should be avoided.
Second Trimester: Risk of fetal adverse effects (e.g., respiratory depression, hypotonia, withdrawal symptoms) if used closer to term.
Third Trimester: Use during the third trimester or near term can lead to 'floppy infant syndrome' (hypotonia, lethargy, feeding difficulties, hypothermia, respiratory depression) and neonatal withdrawal symptoms (e.g., irritability, hypertonia, tremors, seizures) after birth.
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Lactation

Alprazolam is excreted into breast milk. Due to the 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: L4 (Possibly Hazardous) - Potential for sedation, poor feeding, weight loss, and withdrawal symptoms in the breastfed infant. Long-term effects on neurodevelopment are unknown.
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Pediatric Use

Safety and efficacy have not been established in pediatric patients (under 18 years of age) for the treatment of panic disorder. Use is generally not recommended.

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Geriatric Use

Elderly patients may be more sensitive to the effects of benzodiazepines, including increased risk of sedation, dizziness, ataxia, and falls. Initial doses should be lower (e.g., 0.5 mg once daily) and titrated slowly. Monitor closely for adverse effects.

Clinical Information

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Clinical Pearls

  • Alprazolam XR is specifically formulated for once-daily dosing, which can improve adherence compared to multiple daily doses of immediate-release alprazolam.
  • Due to the risk of dependence and withdrawal, alprazolam XR should be tapered slowly when discontinuing, typically over several weeks or months, depending on dose and duration of therapy.
  • Patients should be educated on the risks of concomitant use with opioids and alcohol, emphasizing the potential for life-threatening respiratory depression.
  • Paradoxical reactions (e.g., agitation, aggression, hallucinations) can occur, particularly in elderly or pediatric patients, or those with personality disorders. Discontinue if these occur.
  • While effective for panic disorder, long-term use of benzodiazepines is generally discouraged due to risks of dependence, tolerance, and cognitive impairment. Consider alternative long-term treatments like SSRIs/SNRIs or psychotherapy.
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Alternative Therapies

  • Other benzodiazepines (e.g., clonazepam, lorazepam, diazepam) for panic disorder, though often with different pharmacokinetic profiles and dosing frequencies.
  • Selective Serotonin Reuptake Inhibitors (SSRIs) (e.g., sertraline, paroxetine, fluoxetine, escitalopram) - first-line for long-term management of panic disorder.
  • Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) (e.g., venlafaxine) - also effective for panic disorder.
  • Tricyclic Antidepressants (TCAs) (e.g., imipramine, clomipramine) - effective but with more side effects.
  • Cognitive Behavioral Therapy (CBT) and other forms of psychotherapy.
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Cost & Coverage

Average Cost: $50 - $200 per 30 tablets
Generic Available: Yes
Insurance Coverage: Tier 2 or Tier 3 (preferred or non-preferred generic/brand, depending on insurance plan formulary)
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General Drug Facts

If your symptoms or health problems do not improve or worsen over time, it is essential to contact your doctor for further evaluation and guidance. To ensure your safety and the effectiveness of your treatment, never share your medication with others or take someone else's medication.

This medication is accompanied by a Medication Guide, which is a valuable resource that provides important information about its use. It is crucial to read this guide carefully and review it again whenever your prescription is refilled. If you have any questions or concerns about this medication, do not hesitate to discuss them with your doctor, pharmacist, or other healthcare provider.

In the event of a suspected overdose, it is vital to seek immediate medical attention. Call your local poison control center or visit the emergency room right away. When seeking help, be prepared to provide critical information, including the name of the medication taken, the amount consumed, and the time it happened. This information will enable healthcare professionals to provide you with the most appropriate care and treatment.