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Methylphenidate 63mg 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
Category C
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FDA Approved
Jan 1970
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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 affecting certain natural chemicals in the brain that are involved in attention and impulse control. The extended-release form releases the medicine slowly over the day, so it's usually taken only 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 regular 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 alcohol, as it can cause the medication to be released too quickly.
  • Inform your doctor about all other medications, supplements, and herbal products you are taking.
  • Regularly monitor blood pressure and heart rate as advised by your doctor.
  • For children, monitor height and weight regularly to check for potential growth effects.
  • Report any new or worsening psychiatric symptoms (e.g., hallucinations, aggression, unusual thoughts) immediately.
  • Store safely to prevent misuse, as it is a controlled substance.
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Available Forms & Alternatives

Available Strengths:

Dosing & Administration

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Adult Dosing

Standard Dose: Initial: 18-36 mg once daily in the morning; titrate by 18 mg increments weekly. Usual maintenance: 18-72 mg once daily.
Dose Range: 18 - 72 mg

Condition-Specific Dosing:

ADHD: Initial: 18-36 mg once daily; Max: 72 mg/day. Some formulations may allow higher doses up to 100 mg/day depending on product.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: 6-12 years: Initial 18 mg once daily; titrate by 18 mg increments weekly. Max: 54 mg/day.
Adolescent: 13-17 years: Initial 18 mg once daily; titrate by 18 mg increments weekly. Max: 72 mg/day.
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Dose Adjustments

Renal Impairment:

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

Hepatic Impairment:

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

Pharmacology

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Mechanism of Action

Methylphenidate is a central nervous system (CNS) stimulant. It is thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space. The therapeutic effect in ADHD is thought to be related to the increased availability of dopamine and norepinephrine in the prefrontal cortex, improving attention, focus, and impulse control.
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Pharmacokinetics

Absorption:

Bioavailability: 22-28% (oral, due to first-pass metabolism)
Tmax: For ER formulations (e.g., Concerta): Biphasic release with initial peak at 1-2 hours and second peak at 6-10 hours. For other ER tablets, Tmax can vary from 4-8 hours.
FoodEffect: Food generally does not affect the extent of absorption but may delay Tmax for some ER formulations.

Distribution:

Vd: 2.65 L/kg (for d-methylphenidate)
ProteinBinding: 10-15%
CnssPenetration: Yes

Elimination:

HalfLife: 3.5 hours (for d-methylphenidate, but ER formulations provide prolonged release)
Clearance: Not readily available for specific ER forms, but generally high due to extensive metabolism.
ExcretionRoute: Primarily renal (90% as ritalinic acid), small amount in feces.
Unchanged: <1% (as parent drug)
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Pharmacodynamics

OnsetOfAction: 1-2 hours (for initial release of ER formulations)
PeakEffect: 6-10 hours (for second peak of ER formulations like Concerta), or 4-8 hours for other ER tablets.
DurationOfAction: 10-12 hours (for Concerta-like ER formulations), 8-10 hours for other ER tablets.

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: 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 liver problems: dark urine, fatigue, decreased appetite, stomach pain or upset, light-colored stools, vomiting, or yellow skin or eyes
Severe headache, dizziness, or fainting
 Joint pain
Purple patches on the skin or mouth
 Changes in vision or eye pain, swelling, or redness
Seizures
 Shakiness
Difficulty controlling body movements
 Difficulty controlling sounds, such as humming, throat clearing, yelling, or making loud noises
Excessive sweating
 Restlessness
Changes in skin color (pale, blue, gray, purple, or red) on hands, feet, or other areas
 Numbness, pain, tingling, or cold sensation in hands or feet
Sores or wounds on fingers or toes
 Muscle pain or weakness, dark urine, or difficulty urinating
Changes in sex drive
 Weakness on one side of the body, difficulty speaking or thinking, balance problems, drooping on one side of the face, or blurred vision
Sudden death has occurred in people with certain heart problems or defects; if you have a heart condition or a family history of abnormal heart rhythms or sudden death, inform your doctor

If you experience any signs of heart problems, such as chest pain, abnormal heartbeat, shortness of breath, or severe dizziness or fainting, seek medical help immediately.

Erectile Dysfunction Warning

If you experience a painful erection (priapism) or an erection lasting longer than 4 hours, seek medical attention right away. This can occur even when not engaging in sexual activity. If left untreated, it may lead to permanent sexual dysfunction.

Mental Health Warning

New or worsening behavioral and mood changes, such as changes in thinking, anger, or hallucinations, have been reported with this medication. If you or a family member have a history of mental health conditions, such as depression or bipolar disorder, or if a family member has committed suicide, inform your doctor. Seek medical help immediately if you experience hallucinations, changes in behavior, or signs of mood changes, such as depression, suicidal thoughts, nervousness, emotional instability, abnormal thinking, anxiety, or loss of interest in life.

Serotonin Syndrome Warning

A potentially life-threatening condition called serotonin syndrome may occur if you take this medication with certain other medications. Seek medical help immediately if you experience agitation, balance problems, confusion, hallucinations, fever, rapid or abnormal heartbeat, flushing, muscle twitching or stiffness, seizures, shivering or shaking, excessive sweating, severe diarrhea, stomach upset, or vomiting, or severe headache.

Other Possible Side Effects

Most people do not experience severe side effects, but some may occur. If you experience any of the following side effects, contact your doctor or seek medical attention if they bother you or do not go away:

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

This is not an exhaustive list of possible 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:

  • Chest pain, shortness of breath, or fainting (seek immediate medical attention)
  • Numbness, tingling, or coldness in fingers or toes
  • Unexplained wounds on fingers or toes
  • New or worsening aggression or hostility
  • New psychotic symptoms (e.g., hearing voices, believing things that are not true)
  • New manic symptoms (e.g., extreme energy, racing thoughts, unusual behavior)
  • Uncontrolled muscle movements or tics
  • Blurred vision or other vision changes
  • Prolonged or painful erection (priapism)
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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)
Family history of:
+ Blood vessel disease
+ High blood pressure
+ Heart structure problems or other heart conditions
+ Tourette's syndrome or tics
 Previous medical events, such as a stroke
Recent use (within the last 14 days) of specific medications for depression or Parkinson's disease, including:
+ Isocarboxazid
+ Phenelzine
+ Tranylcypromine
+ Selegiline
+ Rasagiline (note: taking these medications with this drug can lead to very high blood pressure)
 Difficulty swallowing this product whole
History of certain gastrointestinal conditions, including:
+ Cystic fibrosis
+ Narrowing of the GI tract or other GI problems (e.g., bowel block, small bowel disease, short gut syndrome)
+ Slow-moving esophagus or bowel tract
+ Peritonitis
 Current use of specific medications, such as:
+ Linezolid
+ Methylene blue

This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist to ensure safe use of this medication. Do not start, stop, or change 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. Before undergoing surgery, discuss this with your doctor.

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

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

If you have high blood pressure and are taking this medication, consult your doctor before using 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 the medication is not working as well as it previously did, contact your doctor. Do not exceed the prescribed dose.

This medication may increase the risk of seizures in some individuals, particularly those with a history of seizures. Discuss your risk of seizures with your doctor.

With 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 your doctor.

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

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

If you are pregnant, plan to become pregnant, or are breastfeeding, 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)
  • Confusion
  • Hallucinations
  • Delirium
  • Sweating
  • Flushing
  • Headache
  • Hyperpyrexia (very high fever)
  • Tachycardia
  • Palpitations
  • Cardiac arrhythmias
  • Hypertension
  • Mydriasis (dilated pupils)
  • Dry mouth and mucous membranes

What to Do:

Call 911 or Poison Control (1-800-222-1222) immediately. Seek emergency medical attention. Management is primarily supportive, including gastric lavage, activated charcoal, and sedation for CNS overstimulation. Monitor vital signs and cardiac rhythm.

Drug Interactions

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Contraindicated Interactions

  • Monoamine Oxidase Inhibitors (MAOIs) - risk of hypertensive crisis (within 14 days of use)
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Major Interactions

  • Vasopressor agents (e.g., phenylephrine, pseudoephedrine) - risk of increased blood pressure
  • Halogenated anesthetics (e.g., halothane, isoflurane) - risk of sudden blood pressure and heart rate increases during surgery
  • Anticoagulants (e.g., warfarin) - may inhibit metabolism, increasing anticoagulant effect
  • Anticonvulsants (e.g., phenobarbital, phenytoin, primidone) - may inhibit metabolism, increasing anticonvulsant levels
  • Antidepressants (tricyclic antidepressants, SSRIs) - may inhibit metabolism, increasing antidepressant levels or risk of serotonin syndrome
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Moderate Interactions

  • Alcohol - may accelerate release of methylphenidate from some ER formulations (dose dumping)
  • Antihypertensive agents - may reduce the hypotensive effect of these drugs
  • Dopaminergic drugs (e.g., levodopa, bromocriptine) - may potentiate dopaminergic effects
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Minor Interactions

  • Caffeine - additive stimulant effects

Monitoring

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Baseline Monitoring

Blood Pressure (BP) and Heart Rate (HR)

Rationale: Risk of cardiovascular adverse events (hypertension, tachycardia).

Timing: Prior to initiation of therapy.

Height and Weight

Rationale: Risk of growth suppression in pediatric patients.

Timing: Prior to initiation of therapy.

Psychiatric History and Mental Status Exam

Rationale: Assess for pre-existing psychiatric conditions (e.g., bipolar disorder, psychosis) that may be exacerbated.

Timing: Prior to initiation of therapy.

ECG (Electrocardiogram)

Rationale: Consider for patients with pre-existing cardiac conditions or family history of sudden cardiac death/arrhythmias.

Timing: Prior to initiation, if indicated.

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Routine Monitoring

Blood Pressure (BP) and Heart Rate (HR)

Frequency: At each visit (e.g., every 3-6 months or more frequently during titration).

Target: Within normal limits for age.

Action Threshold: Persistent elevation (e.g., >95th percentile for age/sex/height or clinically significant increase); consider dose reduction or discontinuation.

Height and Weight

Frequency: Every 3-6 months in pediatric patients.

Target: Normal growth trajectory.

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

Psychiatric Symptoms

Frequency: At each visit.

Target: Absence of new or worsening psychosis, mania, aggression, or severe anxiety.

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

ADHD Symptom Control

Frequency: At each visit.

Target: Improved attention, reduced hyperactivity/impulsivity.

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
  • Palpitations
  • New or worsening aggression
  • Hallucinations
  • Delusions
  • Mania
  • Severe anxiety
  • Depression
  • Tics or abnormal movements
  • Numbness, tingling, or coldness in fingers/toes (Raynaud's phenomenon)
  • Unexplained wounds on fingers/toes

Special Patient Groups

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Pregnancy

Use during pregnancy should be considered only if the potential benefit justifies the potential risk to the fetus. Studies in animals have shown some evidence of developmental toxicity at high doses. Human data are limited but do not suggest a major teratogenic risk.

Trimester-Specific Risks:

First Trimester: Limited human data; animal studies show some risk at high doses. Consider risks vs. benefits.
Second Trimester: Limited human data; continued monitoring of fetal growth and development is advised.
Third Trimester: Limited human data; potential for premature birth and low birth weight. Neonatal withdrawal symptoms (e.g., agitation, tremors) have been reported with stimulant exposure late in pregnancy.
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Lactation

Methylphenidate is excreted into breast milk in small amounts. The American Academy of Pediatrics considers methylphenidate to be compatible with breastfeeding. Monitor the infant for adverse effects such as agitation, insomnia, or poor weight gain.

Infant Risk: Low risk (L3). Monitor for irritability, poor feeding, or sleep disturbances.
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Pediatric Use

Approved for ADHD in children 6 years and older. Monitor growth (height and weight) regularly due to potential for growth suppression. Monitor for emergence or worsening of psychiatric symptoms (e.g., psychosis, mania, aggression).

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Geriatric Use

Use with caution in elderly patients, as they may be more sensitive to the effects of stimulants, particularly cardiovascular and psychiatric adverse effects. Start with lower doses and titrate slowly. Not typically indicated for ADHD in this population unless diagnosed in childhood and continued into old age.

Clinical Information

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Clinical Pearls

  • Extended-release formulations are designed for once-daily dosing, typically in the morning, to provide symptom control throughout the school or work day.
  • Do not crush, chew, or divide extended-release tablets, as this can lead to rapid release of the entire dose and increased side effects.
  • Patients should be screened for cardiac abnormalities and psychiatric conditions (e.g., bipolar disorder, psychosis) before initiating therapy.
  • Regular monitoring of blood pressure, heart rate, and growth (in children) is crucial.
  • Educate patients and caregivers about the potential for abuse and dependence, and the importance of secure storage.
  • Some ER formulations (e.g., Concerta) may appear in the stool as an intact tablet shell; this is normal and does not mean the medication was not absorbed.
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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 (for generics); Tier 3 or higher (for brands), often requiring prior authorization.
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General Drug Facts

If your symptoms or health problems 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 you receive a refill of this medication. 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 amount, and the time it occurred.