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Methylphenidate 45mg ER (gf:relexi)

Manufacturer TRIGEN LABORATORIES Active Ingredient Methylphenidate Extended- Release Tablets(meth il FEN i date) Pronunciation meth il FEN i date
WARNING: This drug has a high risk of misuse. This can lead to alcohol or drug use disorder. Misuse or abuse of this drug can lead to overdose or death. The risk is higher with higher doses or when used in ways that are not approved like snorting or injecting it. Do not give this drug to anyone else. This drug may be habit-forming if taken for a long time. Do not take for longer than you have been told by your doctor. Use only as you were told. Tell your doctor if you have ever had alcohol or drug use disorder. You will be watched closely while taking this drug.Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets. Throw away unused or expired drugs as you have been told. @ COMMON USES: It is used to treat attention deficit problems with hyperactivity.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Central Nervous System (CNS) Stimulant
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Pharmacologic Class
Norepinephrine-Dopamine Reuptake Inhibitor (NDRI)
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Pregnancy Category
Not available
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FDA Approved
Aug 2000
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DEA Schedule
Schedule II

Overview

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What is this medicine?

Methylphenidate extended-release is a medication used to treat Attention-Deficit/Hyperactivity Disorder (ADHD). It works by helping to balance certain natural chemicals in the brain, which can improve attention, focus, and control over impulsive behaviors. Because it's extended-release, it releases the medicine slowly throughout the day, so you usually only need to take it once in the morning.
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How to Use This Medicine

Taking Your Medication Correctly

To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. It's recommended to take this medication in the morning. However, some medications may need to be taken with food or on an empty stomach, while others may not have specific requirements. Consult your pharmacist to determine the best way to take this medication. When taking your dose, swallow the medication whole - do not chew, break, or crush it.

Storing and Disposing of Your Medication

To maintain the effectiveness and safety of your medication, store it at room temperature, protected from light, and in a dry place. Avoid storing it in a bathroom. Keep your medication in a secure location where children cannot see or reach it, and where others cannot access it. Consider using a locked box or area to store your medication. Remember to keep all medications out of reach of pets.

What to Do If You Miss a Dose

If you miss a dose, skip it and resume your normal dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
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Lifestyle & Tips

  • Take exactly as prescribed, usually once daily in the morning. Do not crush, chew, or divide extended-release tablets.
  • Avoid abrupt discontinuation, especially after prolonged high-dose use, as this can lead to severe depression and fatigue.
  • Inform your doctor about all other medications, supplements, and herbal products you are taking.
  • Avoid alcohol, as it can affect how the medication is released.
  • Store safely to prevent misuse or abuse, especially in households with children or individuals with a history of substance abuse.
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Available Forms & Alternatives

Available Strengths:

Dosing & Administration

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Adult Dosing

Standard Dose: Initial 20 mg extended-release orally once daily in the morning; may increase by 10-20 mg weekly. Usual maintenance dose is 20-80 mg/day. 45 mg is a common maintenance dose.
Dose Range: 20 - 80 mg

Condition-Specific Dosing:

ADHD: Initial 20 mg ER once daily, titrate weekly by 10-20 mg to a maximum of 80 mg/day based on response and tolerability.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: 6-12 years: Initial 10-20 mg extended-release orally once daily in the morning; may increase by 10-20 mg weekly. Max 60 mg/day.
Adolescent: 13-17 years: Initial 20 mg extended-release orally once daily in the morning; may increase by 10-20 mg weekly. Max 72 mg/day.
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Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment recommended, use with caution.
Moderate: No specific dose adjustment recommended, use with caution.
Severe: No specific dose adjustment recommended, use with caution. Monitor for adverse effects.
Dialysis: Not well studied; methylphenidate is not significantly dialyzable. Use with caution.

Hepatic Impairment:

Mild: No specific dose adjustment recommended, use with caution.
Moderate: No specific dose adjustment recommended, use with caution.
Severe: No specific dose adjustment recommended, use with caution. Monitor for adverse effects.

Pharmacology

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Mechanism of Action

Methylphenidate is a central nervous system (CNS) stimulant. Its therapeutic effects in Attention-Deficit/Hyperactivity Disorder (ADHD) are thought to be mediated through the blockade of dopamine and norepinephrine reuptake transporters in the presynaptic neuron, thereby increasing the extracellular concentrations of these monoamines in the striatum and prefrontal cortex.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 20-50% (variable due to first-pass metabolism)
Tmax: Extended-release formulations typically 6-10 hours (for peak plasma concentration)
FoodEffect: Food may delay Tmax but generally does not significantly affect AUC or Cmax for most ER formulations. Some formulations may have specific food instructions (e.g., take with food).

Distribution:

Vd: Approximately 2.65 L/kg
ProteinBinding: Approximately 10-15%
CnssPenetration: Yes

Elimination:

HalfLife: Extended-release formulations: 3-7 hours (terminal half-life)
Clearance: Approximately 0.53 L/hr/kg
ExcretionRoute: Primarily renal (90% as ritalinic acid), small amount in feces.
Unchanged: Less than 1% (as unchanged drug in urine)
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Pharmacodynamics

OnsetOfAction: Extended-release formulations: 1-2 hours
PeakEffect: Extended-release formulations: 6-10 hours
DurationOfAction: Extended-release formulations: 8-12 hours (varies by specific formulation)

Safety & Warnings

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BLACK BOX WARNING

CNS stimulants, including methylphenidate, have a high potential for abuse and dependence. Assess the risk of abuse prior to prescribing, and monitor for signs of abuse and dependence during therapy.
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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, 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 liver problems, including:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Severe headache, dizziness, or fainting
 Joint pain
Purple patches on the skin or mouth
 Changes in eyesight or eye pain, swelling, or redness
Seizures
 Shakiness
Trouble controlling body movements
 Trouble controlling sounds, such as humming, throat clearing, yelling, or making loud noises
Excessive sweating
 Restlessness
Changes in skin color, such as pale, blue, gray, purple, or red hands, feet, or other areas
 Numbness, pain, tingling, or cold feeling in the hands or feet
Sores or wounds on the fingers or toes
 Muscle pain or weakness, dark urine, or difficulty urinating
Changes in sex interest
 Weakness on one side of the body, trouble speaking or thinking, changes in balance, drooping on one side of the face, or blurred vision

Important Heart-Related Warnings

If you have a heart problem or defect, inform your doctor. Additionally, if a family member has an abnormal heartbeat or died suddenly, notify your doctor. Seek medical help immediately if you experience any signs of heart problems, such as:

Chest pain
 Abnormal heartbeat
Shortness of breath
 Severe dizziness or fainting

Other Serious Side Effects

If you experience a painful erection (hard penis) or an erection that lasts longer than 4 hours, seek medical help right away. This can occur even when you are not having sex, and if left untreated, may lead to lasting sexual problems.
 New or worsening behavior and mood changes, such as changes in thinking, anger, and hallucinations, have been reported with this medication. If you or a family member have a history of mental or mood problems, such as depression or bipolar illness, or if a family member has committed suicide, inform your doctor. Seek medical help immediately if you experience:
+ Hallucinations
+ Changes in behavior
+ Signs of mood changes, such as depression, thoughts of suicide, nervousness, emotional ups and downs, abnormal thinking, anxiety, or lack of interest in life
A severe and potentially life-threatening condition called serotonin syndrome may occur if you take this medication with certain other drugs. Seek medical help immediately if you experience:
+ Agitation
+ Changes in balance
+ Confusion
+ Hallucinations
+ Fever
+ Fast or abnormal heartbeat
+ Flushing
+ Muscle twitching or stiffness
+ Seizures
+ Shivering or shaking
+ Excessive sweating
+ Severe diarrhea, upset stomach, or vomiting
+ Severe headache

Common Side Effects

Not everyone experiences side effects, and many people have only minor side effects. However, if you experience any of the following side effects or if they bother you or do not go away, contact your doctor:

 Dizziness or headache
Feeling sleepy
 Dry mouth
Stomach pain, upset stomach, vomiting, or decreased appetite
 Heartburn
Weight loss
 Feeling nervous and excitable
Trouble sleeping
 Nose or throat irritation

Reporting Side Effects

If you have questions about side effects or want to report a side effect, contact your doctor or the FDA at 1-800-332-1088. You can also report side effects online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Chest pain, shortness of breath, or fainting (seek immediate medical attention).
  • New or worsening mental health problems such as hallucinations, delusions, paranoia, aggression, or mania.
  • Numbness, coolness, or pain in fingers or toes (Raynaud's phenomenon).
  • Unexplained wounds on fingers or toes.
  • Prolonged or painful erections (priapism).
  • Blurred vision or other vision changes.
  • Unexplained weight loss or slowed growth in children.
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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 conditions and situations to ensure safe treatment:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reaction and its symptoms.
 Certain health conditions, including:
+ Glaucoma
+ Agitation
+ Anxiety
+ Overactive thyroid (hyperthyroidism)
A family history of:
+ Blood vessel disease
+ High blood pressure
+ Heart structure problems or other heart conditions
+ Tourette's syndrome or tics
 If you have ever experienced a stroke
Recent use (within the last 14 days) of specific medications for depression or Parkinson's disease, such as:
+ Isocarboxazid
+ Phenelzine
+ Tranylcypromine
+ Selegiline
+ Rasagiline, as this may lead to very high blood pressure
 Difficulty swallowing this product whole
A history of:
+ Cystic fibrosis
+ Narrowing of the gastrointestinal (GI) tract or other GI problems, including:
- Bowel block
- Small bowel disease
- Short gut syndrome
- Slow-moving esophagus or bowel tract
+ Peritonitis
 Concurrent use of certain medications, including:
+ Linezolid
+ Methylene blue

This list is not exhaustive, and it is crucial to disclose all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions to your doctor and pharmacist. They will help you determine if it is safe to take this medication with your existing treatments and health status. Never start, stop, or adjust the dose of any medication without 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 are scheduled to have surgery, be sure to discuss this with your doctor beforehand.

To ensure your safety, avoid driving and engaging in activities that require alertness until you understand how this medication affects you. As directed by your doctor, have regular blood tests, blood pressure checks, and heart rate monitoring. You may also need to undergo certain heart tests before starting this medication. If you have any questions or concerns, consult with your doctor.

While taking this medication, it is recommended that you avoid consuming alcohol. Additionally, limit your intake of caffeine (found in tea, coffee, cola, and other products) and chocolate, as combining these with this medication may cause nervousness, shakiness, and a rapid heartbeat.

If you have high blood pressure, it is crucial to discuss with your doctor before using any over-the-counter (OTC) products that may increase blood pressure, such as cough or cold medications, diet pills, stimulants, non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen or naproxen, and certain natural products or aids.

Long-term or high-dose use of this medication may lead to tolerance, where the medication becomes less effective, and higher doses may be required to achieve the same effect. If you notice that the medication is no longer working as well as it should, contact your doctor. Do not take more than the prescribed dose.

This medication may increase the risk of seizures in some individuals, particularly those with a history of seizures. Consult with your doctor to determine if you are at a higher risk of seizures while taking this medication.

For certain brands of this medication, you may notice the tablet shell in your stool. This is a normal occurrence and not a cause for concern. However, if you have any questions, consult with your doctor.

If you are undergoing x-rays near the abdominal area, inform your doctor that you are taking this medication.

In children and teenagers, this medication may affect growth in some cases. Regular growth checks may be necessary. Discuss this with your doctor.

If you are pregnant, planning to become pregnant, or breastfeeding, it is essential to inform your doctor. You will need to discuss the potential benefits and risks of this medication to both you and your baby.
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Overdose Information

Overdose Symptoms:

  • Vomiting, agitation, tremors, hyperreflexia, muscle twitching
  • Convulsions (may be followed by coma)
  • Euphoria, confusion, hallucinations, delirium
  • Sweating, flushing, headache, hyperpyrexia
  • Tachycardia, palpitations, cardiac arrhythmias, hypertension
  • Mydriasis, dry mucous membranes

What to Do:

Seek immediate medical attention. Call 911 or Poison Control at 1-800-222-1222. Management includes supportive care, gastric lavage, activated charcoal, and symptomatic treatment for severe agitation, hypertension, or seizures.

Drug Interactions

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Contraindicated Interactions

  • Monoamine Oxidase Inhibitors (MAOIs): Concomitant use or within 14 days of MAOI administration due to risk of hypertensive crisis.
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Major Interactions

  • Vasopressor agents (e.g., phenylephrine, pseudoephedrine): May potentiate pressor effects.
  • Alcohol: May accelerate the release of methylphenidate from some ER formulations, leading to a rapid increase in plasma levels.
  • Halogenated anesthetics: Risk of sudden blood pressure and heart rate increases during surgery.
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Moderate Interactions

  • Anticoagulants (e.g., warfarin): May inhibit metabolism of coumarin anticoagulants, requiring dose adjustment.
  • Anticonvulsants (e.g., phenobarbital, phenytoin, primidone): May inhibit metabolism of these drugs, requiring dose adjustment.
  • Antidepressants (e.g., tricyclic antidepressants, SSRIs): May inhibit metabolism of these drugs, requiring dose adjustment. Increased risk of serotonin syndrome with SSRIs.
  • Antihypertensive drugs: May reduce the effectiveness of antihypertensive agents.
  • Dopaminergic drugs (e.g., bupropion, levodopa): Increased risk of dopaminergic adverse effects.
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Minor Interactions

  • Caffeine: Additive stimulant effects, increased risk of nervousness, insomnia.

Monitoring

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Baseline Monitoring

Blood Pressure (BP) and Heart Rate (HR)

Rationale: CNS stimulants can cause increases in BP and HR.

Timing: Prior to initiation of therapy.

Height and Weight

Rationale: Stimulants have been associated with growth suppression in pediatric patients.

Timing: Prior to initiation of therapy.

Psychiatric History (including family history of suicide, bipolar disorder, depression)

Rationale: To assess risk of psychiatric adverse events (e.g., psychosis, mania, aggression).

Timing: Prior to initiation of therapy.

Cardiac History (including family history of sudden death, arrhythmias)

Rationale: To assess risk of serious cardiovascular events.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Blood Pressure (BP) and Heart Rate (HR)

Frequency: At each visit or at least every 3-6 months, and after dose changes.

Target: Within normal limits for age/individual.

Action Threshold: Persistent elevation outside normal range; consider dose reduction or discontinuation.

Height and Weight

Frequency: Every 3-6 months for pediatric patients; annually for adults.

Target: Normal growth trajectory for age; stable weight for adults.

Action Threshold: Significant growth deceleration or weight loss; consider drug holiday or alternative therapy.

Psychiatric Status (e.g., emergence of new or worsening psychotic or manic symptoms, aggression, anxiety)

Frequency: At each visit.

Target: Stable mood and behavior.

Action Threshold: Emergence of new or worsening psychiatric symptoms; consider dose reduction or discontinuation.

ADHD Symptom Control and Functional Improvement

Frequency: At each visit.

Target: Improved attention, reduced hyperactivity/impulsivity, improved academic/occupational/social functioning.

Action Threshold: Lack of efficacy or intolerable side effects; consider dose adjustment or alternative therapy.

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Symptom Monitoring

  • Chest pain, shortness of breath, syncope (cardiovascular)
  • Hallucinations, delusions, mania, aggression, severe anxiety, agitation (psychiatric)
  • Unexplained weight loss, growth deceleration (growth)
  • Peripheral vasculopathy (e.g., Raynaud's phenomenon)
  • Priapism (rare, but serious)

Special Patient Groups

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Pregnancy

Data from observational studies of methylphenidate use in pregnancy have not identified a clear association with major birth defects, miscarriage, or adverse maternal or fetal outcomes. However, some studies suggest a possible small increase in the risk of cardiac malformations. Use during pregnancy should be considered only if the potential benefit justifies the potential risk to the fetus.

Trimester-Specific Risks:

First Trimester: Possible small increased risk of cardiac malformations, though data are conflicting and overall risk appears low.
Second Trimester: Limited data, generally considered lower risk than first trimester for structural anomalies.
Third Trimester: Potential for withdrawal symptoms (e.g., agitation, tremor, poor feeding) in neonates exposed late in pregnancy.
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Lactation

Methylphenidate is excreted into breast milk in small amounts. The relative infant dose is low. Monitor breastfed infants for agitation, insomnia, decreased appetite, or poor weight gain. Use with caution, especially in neonates or preterm infants.

Infant Risk: Low to moderate risk (L3). Monitor infant for adverse effects.
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Pediatric Use

Closely monitor growth (height and weight) and cardiovascular parameters. Assess for emergence or worsening of psychiatric symptoms (e.g., psychosis, mania, aggression). Consider drug holidays to assess continued need and minimize growth suppression.

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Geriatric Use

Use with caution due to increased sensitivity to stimulant effects and higher prevalence of cardiovascular disease. Start with lower doses and titrate slowly. Monitor blood pressure and heart rate closely.

Clinical Information

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Clinical Pearls

  • Extended-release formulations should be swallowed whole; crushing or chewing can lead to rapid release and increased risk of side effects and abuse.
  • Take in the morning to avoid insomnia.
  • Monitor for signs of abuse and diversion, especially given its Schedule II classification.
  • Patients should be screened for pre-existing cardiac conditions and psychiatric disorders before initiation.
  • Consider a trial off medication periodically to assess continued need and minimize long-term side effects, especially in children (e.g., during school breaks).
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Alternative Therapies

  • Other CNS Stimulants (e.g., Amphetamine salts, Lisdexamfetamine, Dexmethylphenidate)
  • Non-stimulants (e.g., Atomoxetine, Guanfacine ER, Clonidine ER)
  • Behavioral therapy
  • Cognitive behavioral therapy (CBT)
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Cost & Coverage

Average Cost: $100 - $400 per 30 tablets (generic ER)
Generic Available: Yes
Insurance Coverage: Tier 2 or Tier 3 (generic often Tier 1 or 2, brand Tier 3)
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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 is a crucial patient fact sheet. Please read it carefully and review it again whenever you receive a refill. If you have any questions or concerns about this medication, consult your doctor, pharmacist, or 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.