Topiramate ER 50mg Sprinkle Caps

Manufacturer UPSHER-SMITH Active Ingredient Topiramate Extended-Release Sprinkle Capsules(toe PYRE a mate) Pronunciation toe PYRE a mate
It is used to treat seizures.It is used to prevent migraine headaches.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Anticonvulsant; Migraine Prophylaxis
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Pharmacologic Class
Sulfamate-substituted monosaccharide; Voltage-gated sodium channel blocker; GABA-A receptor modulator; AMPA/kainate glutamate receptor antagonist; Carbonic anhydrase inhibitor
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Pregnancy Category
D
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FDA Approved
Mar 2014
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Topiramate extended-release sprinkle capsules are a medication used to help prevent seizures in people with epilepsy and to prevent migraine headaches. It works by affecting certain chemicals in the brain.
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How to Use This Medicine

Taking Your Medication

To take this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication with or without food, as directed. Continue taking it even if you feel well, unless your doctor or healthcare provider advises you to stop.

It's essential to stay hydrated, so drink plenty of non-caffeinated liquids, unless your doctor recommends limiting your fluid intake. You can swallow the medication whole or mix it with a spoonful of soft food, such as applesauce. However, do not crush or chew the medication before swallowing. If you mix it with food, take the mixture immediately and do not store it for later use. After taking the medication with food, drink some fluid to ensure the medication is swallowed properly.

Storing and Disposing of Your Medication

Store your medication at room temperature in a dry place, away from the bathroom. Keep the lid tightly closed and store all medications in a safe location, out of reach of children and pets. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so. If you're unsure about the best way to dispose of your medication, consult your pharmacist. You may also want to check if there are 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's close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not take two doses at the same time or take extra doses. If you miss two doses, contact your doctor for guidance.
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Lifestyle & Tips

  • Stay well-hydrated by drinking plenty of fluids throughout the day to help prevent kidney stones.
  • Avoid or limit alcohol consumption, as it can increase side effects like dizziness and drowsiness.
  • Use caution when driving or operating machinery until you know how this medication affects you, as it can cause dizziness, drowsiness, and vision problems.
  • Do not stop taking this medication suddenly without consulting your doctor, as it can lead to increased seizures.
  • If using sprinkle capsules, they can be swallowed whole or opened and sprinkled on a small amount of soft food (e.g., applesauce, yogurt) and swallowed immediately without chewing.

Dosing & Administration

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Adult Dosing

Standard Dose: Epilepsy (adjunctive): Initial 50 mg once daily, titrate weekly by 50 mg/day to target 200-400 mg/day. Migraine prophylaxis: Initial 50 mg once daily, titrate weekly by 50 mg/day to target 100 mg/day.
Dose Range: 50 - 400 mg

Condition-Specific Dosing:

epilepsy_adjunctive: Initial 50 mg once daily, titrate weekly by 50 mg/day to target 200-400 mg/day (max 600 mg/day).
epilepsy_monotherapy: Initial 50 mg once daily, titrate weekly by 50 mg/day to target 400 mg/day.
migraine_prophylaxis: Initial 50 mg once daily, titrate weekly by 50 mg/day to target 100 mg/day.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Epilepsy (adjunctive, β‰₯10 years): Initial 50 mg once daily, titrate weekly by 50 mg/day to target 200-400 mg/day. Migraine prophylaxis (β‰₯12 years): Initial 50 mg once daily, titrate weekly by 50 mg/day to target 100 mg/day.
Adolescent: Epilepsy (adjunctive, β‰₯10 years): Initial 50 mg once daily, titrate weekly by 50 mg/day to target 200-400 mg/day. Migraine prophylaxis (β‰₯12 years): Initial 50 mg once daily, titrate weekly by 50 mg/day to target 100 mg/day.
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Dose Adjustments

Renal Impairment:

Mild: CrCl 50-79 mL/min: No specific adjustment, but monitor for side effects.
Moderate: CrCl 30-49 mL/min: Reduce dose by 50% (e.g., administer half the usual dose or extend dosing interval).
Severe: CrCl < 30 mL/min: Reduce dose by 50% (e.g., administer half the usual dose or extend dosing interval).
Dialysis: Topiramate is dialyzable. Supplemental dose may be needed after hemodialysis. Administer half the usual daily dose on dialysis days, in 2 divided doses (one at start, one at end of dialysis).

Hepatic Impairment:

Mild: Use with caution, slower titration may be needed.
Moderate: Use with caution, slower titration may be needed.
Severe: Use with caution, slower titration may be needed.

Pharmacology

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Mechanism of Action

Topiramate's precise mechanism is not fully understood but involves multiple actions: it blocks voltage-dependent sodium channels, enhances the activity of the neurotransmitter gamma-aminobutyrate (GABA) at GABA-A receptors, antagonizes the AMPA/kainate subtype of the glutamate receptor, and inhibits carbonic anhydrase, particularly isozymes II and IV.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 81%
Tmax: Approximately 6-8 hours (for ER formulation)
FoodEffect: Minimal effect on absorption or Cmax.

Distribution:

Vd: 0.6-0.8 L/kg
ProteinBinding: 13-17%
CnssPenetration: Yes

Elimination:

HalfLife: Approximately 21 hours
Clearance: Approximately 20-30 mL/min (in healthy adults)
ExcretionRoute: Primarily renal
Unchanged: Approximately 70% (in urine)
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Pharmacodynamics

OnsetOfAction: Gradual, due to slow titration schedule (weeks to months for full effect)
PeakEffect: Achieved after several weeks of titration to target dose
DurationOfAction: Once daily dosing due to extended-release formulation and half-life

Safety & Warnings

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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 medical attention immediately:

Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of acidosis (too much acid in the blood): confusion, rapid breathing, rapid heartbeat, irregular heartbeat, severe stomach pain, nausea, vomiting, excessive sleepiness, shortness of breath, or feeling extremely tired or weak.
Signs of infection: fever, chills, severe sore throat, ear or sinus pain, cough, increased sputum production or change in sputum color, painful urination, mouth sores, or a wound that won't heal.
Signs of high ammonia levels: irregular heartbeat, abnormal breathing, confusion, pale skin, slow heartbeat, seizures, sweating, vomiting, or twitching.
Unexplained bruising or bleeding.
Confusion, difficulty focusing, or changes in behavior.
Memory problems or loss.
Speech difficulties.
Sleep disturbances.
Balance problems.
Severe dizziness or fainting.
Inability to eat.
Back pain, abdominal pain, or blood in the urine (may indicate a kidney stone).
Abnormal burning, numbness, or tingling sensations.
Bone pain.
Chest pain.
Muscle pain or weakness.
Shakiness.
Difficulty walking.
Inability to control eye movements.

Like other seizure medications, this drug may increase the risk of suicidal thoughts or behaviors, particularly in individuals with a history of such thoughts or actions. If you experience any new or worsening symptoms, such as depression, anxiety, restlessness, irritability, panic attacks, or mood changes, contact your doctor immediately. If you have suicidal thoughts or behaviors, seek help right away.

This medication may cause severe eye problems, potentially leading to permanent vision loss if left untreated. If you notice any new eye symptoms, such as blurred vision, changes in vision, eye pain, or eye redness, contact your doctor immediately.

Rarely, this medication has caused liver problems, which can be fatal. If you experience any signs of liver problems, such as dark urine, fatigue, decreased appetite, nausea, stomach pain, pale stools, vomiting, or yellow skin or eyes, contact your doctor immediately.

Sweating less and high body temperatures have been reported with this medication, sometimes requiring hospitalization. Be cautious in hot weather and during physical activity. If you experience a fever or decreased sweating, contact your doctor immediately.

A severe skin reaction (Stevens-Johnson syndrome/toxic epidermal necrolysis) may occur, potentially causing long-term health problems or death. If you experience any signs, such as red, swollen, blistered, or peeling skin (with or without fever), red or irritated eyes, or sores in your mouth, throat, nose, or eyes, seek medical help immediately.

Other Possible Side Effects

Most people do not experience significant side effects, but some may occur. If you experience any of the following side effects or any other symptoms that concern you or do not resolve, contact your doctor:

Constipation, diarrhea, stomach pain, nausea, vomiting, or decreased appetite.
Changes in taste.
Weight loss.
Feeling anxious or excitable.
Dizziness, drowsiness, fatigue, or weakness.
Headache.
Flushing.
Common cold symptoms.
* Joint pain.

This is not an exhaustive list of potential side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Sudden vision changes, eye pain, or redness (could be acute angle-closure glaucoma, seek immediate medical attention)
  • Severe abdominal or back pain, blood in urine (signs of kidney stones)
  • Unexplained fatigue, loss of appetite, rapid breathing, irregular heartbeat (signs of metabolic acidosis)
  • Confusion, memory problems, difficulty finding words, slowed thinking ('topiramate fog')
  • Decreased sweating, fever, or hot flashes (especially in hot weather or during exercise)
  • New or worsening depression, anxiety, or thoughts of self-harm
  • Unusual bleeding or bruising
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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 as a result of the allergy.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial because this medication may interact with other drugs or exacerbate existing health problems.
* Any health issues you are experiencing, as they may affect the safety and efficacy of this medication.

To ensure your safety, it is vital to verify that it is safe to take this medication with all your current medications and health conditions. Always consult your doctor before starting, stopping, or changing the dose of any medication.
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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. Before engaging in activities that require alertness, such as driving, wait until you understand how this drug affects you.

To minimize the risk of seizures, do not abruptly stop taking this medication without consulting your doctor. If you need to discontinue use, your doctor will guide you on how to gradually stop taking it. Adhere to your doctor's recommendations for regular blood work and other laboratory tests.

While taking this medication, it is recommended that you avoid consuming alcohol. Additionally, consult your doctor before using marijuana, cannabis, or prescription and over-the-counter drugs that may cause drowsiness.

This medication may increase the risk of developing metabolic acidosis, a condition characterized by an acid imbalance in the blood. This risk is higher in children, individuals with kidney problems, respiratory issues, or diarrhea. The risk may also be elevated if you are taking certain medications, undergoing surgery, or following a ketogenic diet. If left untreated, metabolic acidosis can lead to complications such as kidney stones, bone problems, or growth issues in children.

There is a potential increased risk of bleeding associated with this medication, which can be life-threatening in some cases. Discuss this risk with your doctor.

Concomitant use of this medication with valproic acid may cause hypothermia, leading to symptoms such as fatigue, confusion, or coma. Consult your doctor if you are taking valproic acid.

When administering this medication to children, exercise caution, as the risk of certain side effects may be higher in this population. This medication may affect growth in children and adolescents, and regular growth checks may be necessary. Consult your doctor to discuss the potential risks and benefits.

The effectiveness of birth control pills and other hormone-based contraceptives may be reduced when taking this medication. Consider using an additional form of birth control, such as condoms, to prevent pregnancy. If you experience any changes in your menstrual bleeding pattern while taking hormone-based birth control, inform your doctor.

This medication may harm the unborn baby if taken during pregnancy. If you become pregnant or suspect you are pregnant while taking this medication, contact your doctor immediately. If you are of childbearing age and do not wish to become pregnant, use a reliable form of birth control to prevent pregnancy while taking this medication.

If you are breastfeeding, consult your doctor to discuss the potential risks to your baby.
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Overdose Information

Overdose Symptoms:

  • Severe drowsiness or dizziness
  • Blurred or double vision
  • Difficulty thinking or concentrating
  • Loss of coordination
  • Fainting
  • Seizures
  • Coma
  • Severe metabolic acidosis (rapid breathing, fatigue)
  • Hypotension (low blood pressure)
  • Hypokalemia (low potassium)

What to Do:

Seek immediate medical attention. Call 911 or Poison Control (1-800-222-1222). Treatment is supportive, including gastric lavage or activated charcoal if ingestion was recent. Hemodialysis can effectively remove topiramate from the body.

Drug Interactions

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Major Interactions

  • Oral contraceptives (decreased efficacy of estrogen component)
  • Valproic acid (increased risk of hyperammonemia with or without encephalopathy)
  • Other carbonic anhydrase inhibitors (e.g., zonisamide, acetazolamide; increased risk of metabolic acidosis and kidney stones)
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Moderate Interactions

  • CNS depressants (e.g., alcohol, benzodiazepines, opioids; additive CNS depression)
  • Digoxin (decreased digoxin levels)
  • Metformin (decreased metformin levels)
  • Lithium (altered lithium levels, monitor)
  • Phenytoin, Carbamazepine (may alter topiramate levels, monitor)

Monitoring

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Baseline Monitoring

Renal function (CrCl, BUN, creatinine)

Rationale: Topiramate is primarily renally excreted; dose adjustment needed in renal impairment.

Timing: Prior to initiation

Serum bicarbonate levels

Rationale: Risk of metabolic acidosis due to carbonic anhydrase inhibition.

Timing: Prior to initiation

Weight

Rationale: Topiramate can cause weight loss.

Timing: Prior to initiation

Intraocular pressure (IOP) / Eye exam

Rationale: Risk of acute angle-closure glaucoma.

Timing: Prior to initiation (if history of glaucoma or risk factors)

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Routine Monitoring

Serum bicarbonate levels

Frequency: Periodically (e.g., every 6-12 months or as clinically indicated)

Target: 22-29 mEq/L

Action Threshold: If persistently low or symptomatic, consider dose reduction or discontinuation, or bicarbonate supplementation.

Renal function (CrCl, BUN, creatinine)

Frequency: Periodically (e.g., annually or as clinically indicated)

Target: Normal for age

Action Threshold: If significant decline, adjust dose.

Weight

Frequency: Periodically (e.g., every 3-6 months)

Target: Stable

Action Threshold: Significant or rapid weight loss may require intervention.

Electrolytes (Potassium, Chloride)

Frequency: Periodically (especially if bicarbonate is low)

Target: Normal

Action Threshold: Abnormalities may indicate metabolic derangement.

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Symptom Monitoring

  • Vision changes (e.g., acute myopia, secondary angle-closure glaucoma symptoms like eye pain, redness, blurred vision)
  • Cognitive changes (e.g., difficulty concentrating, memory problems, word-finding difficulties, 'topiramate fog')
  • Mood or behavioral changes (e.g., depression, anxiety, suicidal ideation)
  • Symptoms of kidney stones (e.g., flank pain, hematuria)
  • Symptoms of metabolic acidosis (e.g., fatigue, anorexia, rapid breathing, cardiac arrhythmias)
  • Decreased sweating or fever (especially in hot weather or during exertion)
  • Symptoms of hyperammonemia (e.g., lethargy, vomiting, confusion, hypothermia, especially with valproic acid co-administration)

Special Patient Groups

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Pregnancy

Topiramate is associated with an increased risk of oral clefts (e.g., cleft lip/palate) when used during the first trimester of pregnancy. It may also increase the risk of low birth weight and preterm delivery. Use during pregnancy should only be considered if the potential benefit outweighs the potential risk to the fetus. Patients should be counseled on the risks and enrolled in a pregnancy registry.

Trimester-Specific Risks:

First Trimester: Increased risk of oral clefts (cleft lip/palate).
Second Trimester: Potential for fetal growth restriction, low birth weight.
Third Trimester: Potential for fetal growth restriction, low birth weight, and withdrawal symptoms in neonates.
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Lactation

Topiramate is excreted into breast milk. The amount transferred to the infant is variable but can be significant. Monitor breastfed infants for drowsiness, diarrhea, irritability, and poor weight gain. The decision to breastfeed should consider the developmental and health benefits of breastfeeding, the mother’s clinical need for topiramate, and any potential adverse effects on the breastfed infant.

Infant Risk: L3 (Moderately Safe) - Monitor infant for drowsiness, diarrhea, poor feeding, and developmental milestones. Consider alternative if infant experiences adverse effects.
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Pediatric Use

Topiramate ER is approved for adjunctive therapy in patients β‰₯10 years with partial-onset or primary generalized tonic-clonic seizures, and for monotherapy in patients β‰₯10 years with partial-onset seizures. It is also approved for migraine prophylaxis in adolescents β‰₯12 years. Younger children may experience more cognitive side effects, decreased sweating, and hyperthermia. Careful monitoring and slow titration are crucial.

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Geriatric Use

Use with caution, starting with lower doses and slower titration due to potential age-related decreases in renal function and increased susceptibility to side effects (e.g., cognitive impairment, dizziness, falls). Monitor renal function and electrolytes closely.

Clinical Information

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Clinical Pearls

  • Always titrate topiramate slowly to minimize cognitive side effects ('topiramate fog') and other adverse reactions.
  • Emphasize adequate hydration to patients to reduce the risk of kidney stone formation.
  • Counsel patients on the risk of acute angle-closure glaucoma; any sudden vision changes or eye pain require immediate medical attention.
  • Monitor serum bicarbonate levels periodically due to the risk of metabolic acidosis, especially in patients with renal impairment or those on other carbonic anhydrase inhibitors.
  • Topiramate can cause weight loss, which may be beneficial for some patients but should be monitored.
  • For sprinkle capsules, ensure patients understand they can be opened and sprinkled on soft food, but the mixture must be swallowed immediately without chewing.
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Alternative Therapies

  • For Epilepsy: Levetiracetam, Lamotrigine, Valproic acid, Carbamazepine, Oxcarbazepine, Zonisamide, Lacosamide, Phenytoin.
  • For Migraine Prophylaxis: Beta-blockers (e.g., Propranolol), Tricyclic antidepressants (e.g., Amitriptyline), CGRP inhibitors (e.g., Erenumab, Fremanezumab), OnabotulinumtoxinA (Botox).
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Cost & Coverage

Average Cost: $300 - $600+ per 30 capsules (50mg ER)
Generic Available: Yes
Insurance Coverage: Tier 2 or Tier 3 (for brand name; generic may be Tier 1)
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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, which provides crucial information for patients. Please read this guide carefully and review it again whenever your prescription is refilled. 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. When reporting the incident, be prepared to provide details about the medication taken, the quantity, and the time it occurred.