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Methylphenidate 72mg 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 Stimulant
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Pharmacologic Class
Dopamine and Norepinephrine Reuptake Inhibitor
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Pregnancy Category
Category C
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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 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 (ER) form means the medication is released slowly over 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.

Some medications are best taken with food, while others should be taken on an empty stomach. To determine the best approach for your specific medication, consult with your pharmacist. When taking your medication, swallow the tablet 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 moisture. 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 take in the afternoon or evening as it may cause sleep problems.
  • Swallow the tablet whole with water. Do not chew, crush, or divide the tablet, as this will affect the extended-release mechanism and could lead to a sudden release of the entire dose.
  • Can be taken with or without food.
  • Avoid alcohol, as it may 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.
  • Maintain a healthy diet and regular exercise. For children, monitor growth regularly.
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Available Forms & Alternatives

Available Strengths:

Dosing & Administration

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Adult Dosing

Standard Dose: Initial: 18-36 mg orally once daily in the morning. Titrate weekly by 18 mg increments.
Dose Range: 18 - 72 mg

Condition-Specific Dosing:

ADHD: Max 72 mg/day
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: 6-12 years: Initial 18 mg orally once daily in the morning. Titrate weekly by 18 mg increments to a maximum of 54 mg/day.
Adolescent: 13-17 years: Initial 18 mg orally once daily in the morning. Titrate weekly by 18 mg increments to a maximum of 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: Use with caution; consider lower doses and monitor for adverse effects due to potential for inactive metabolite accumulation.
Dialysis: Not available; methylphenidate is not significantly dialyzable.

Hepatic Impairment:

Mild: No specific dose adjustment recommended, use with caution.
Moderate: No specific dose adjustment recommended, use with caution.
Severe: Use with caution; monitor for adverse effects. No specific guidelines available.

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 into presynaptic neurons, thereby increasing the extracellular levels of these monoamines in the striatum and prefrontal cortex.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 22-28% (due to first-pass metabolism)
Tmax: Bimodal release: First peak ~1-2 hours, second peak ~6-8 hours (for ER formulation)
FoodEffect: Food does not significantly affect the extent of absorption (AUC) but may delay the first peak concentration (Tmax) by approximately 1 hour.

Distribution:

Vd: Approximately 2.65 L/kg
ProteinBinding: Approximately 15% (to plasma proteins)
CnssPenetration: Yes

Elimination:

HalfLife: Approximately 3.5 hours (for ER formulation)
Clearance: Approximately 0.53 L/hr/kg
ExcretionRoute: Primarily renal (90% as PPAA, <1% as unchanged drug)
Unchanged: <1%
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Pharmacodynamics

OnsetOfAction: Approximately 1-2 hours (for ER formulation)
PeakEffect: Approximately 6-8 hours (for ER formulation)
DurationOfAction: Approximately 10-12 hours (for ER formulation)
Confidence: Medium

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 immediate medical attention:

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 vision or eye pain, swelling, or redness
Seizures
 Shakiness
Trouble controlling body movements
 Difficulty controlling sounds, such as humming, throat clearing, yelling, or making loud noises
Excessive sweating
 Restlessness
Changes in skin color, including pale, blue, gray, purple, or red discoloration of 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, trouble 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 defect, inform your doctor. Also, notify your doctor if a family member has an abnormal heartbeat or died suddenly. Seek immediate medical attention if you experience:
+ Chest pain
+ Abnormal heartbeat
+ Shortness of breath
+ Severe dizziness or fainting
 If you experience a painful erection (priapism) or an erection lasting longer than 4 hours, seek medical help right away. This can occur even when not engaging in sexual activity. If left untreated, it may lead to permanent sexual dysfunction.
New or worsening behavioral and mood changes, such as:
+ Changes in thinking
+ Anger
+ Hallucinations
+ Inform your doctor if you or a family member have a history of mental or mood disorders, such as depression or bipolar illness, or if a family member has committed suicide. Seek immediate medical attention if you experience:
- Hallucinations
- Changes in behavior
- Signs of mood changes, including depression, suicidal thoughts, nervousness, emotional instability, abnormal thinking, anxiety, or loss of interest in life
 A potentially life-threatening condition called serotonin syndrome may occur if you take this medication with certain other drugs. Seek immediate medical attention if you experience:
+ Agitation
+ Changes in balance
+ Confusion
+ Hallucinations
+ Fever
+ Rapid or abnormal heartbeat
+ Flushing
+ Muscle twitching or stiffness
+ Seizures
+ Shivering or shaking
+ Excessive sweating
+ Severe diarrhea, upset stomach, or vomiting
+ Severe headache

Other Possible Side Effects

Most people do not experience significant side effects, but some may occur. If you are concerned about any of the following side effects or if they persist, contact your doctor:

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

This is not an exhaustive list of possible side effects. If you have questions or concerns, 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:

  • Chest pain, shortness of breath, or fainting (seek immediate medical attention).
  • New or worsening psychiatric symptoms such as hallucinations, delusions, mania, aggression, or severe anxiety.
  • Unexplained numbness, pain, skin color change, or sensitivity to temperature in fingers or toes.
  • New or worsening tics (uncontrolled movements or sounds).
  • Blurred vision or other vision changes.
  • Severe headache.
  • Signs of allergic reaction (rash, itching, swelling, 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 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
A 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, or rasagiline, as this may lead to very high blood pressure
 Difficulty swallowing this product whole
Presence of certain gastrointestinal conditions, such as:
+ Cystic fibrosis
+ Narrowing of the gastrointestinal tract or other GI problems (e.g., bowel block, small bowel disease, short gut syndrome, or slow-moving esophagus or bowel tract)
+ Peritonitis
 Concurrent use of linezolid or 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 problems with your doctor and pharmacist. They will help determine the safety of taking this medication with your other treatments and health conditions. 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. Regularly monitor your blood work, blood pressure, and heart rate as directed by your doctor. You may 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 and limit your intake of caffeine (found in tea, coffee, cola) and chocolate, as combining these substances 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 the potential risks of 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 experience a decrease in the medication's effectiveness, contact your doctor. Do not exceed the prescribed dose.

This medication may increase the risk of seizures in certain individuals, including 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 some formulations of this medication, you may notice the tablet shell in your stool, which is a normal occurrence and not a cause for concern. However, if you have any questions or concerns, discuss them 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 adolescents, this medication may affect growth in some cases, and regular growth checks may be necessary. Consult with your doctor to discuss the potential risks and benefits.

If you are pregnant, planning to become pregnant, or breastfeeding, it is essential to discuss the benefits and risks of this medication with your doctor to ensure the best possible outcome for 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 (very high fever)
  • Tachycardia (fast heart rate)
  • Palpitations
  • Cardiac arrhythmias
  • Hypertension (high blood pressure)
  • Mydriasis (dilated pupils)
  • Dry mouth

What to Do:

Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222.

Drug Interactions

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Contraindicated Interactions

  • Monoamine Oxidase Inhibitors (MAOIs) - concurrent use or within 14 days of MAOI discontinuation due to risk of hypertensive crisis.
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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 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; additive serotonergic effects with SSRIs.
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Moderate Interactions

  • Alcohol - may accelerate the release of methylphenidate from extended-release formulations, leading to dose dumping.
  • Antihypertensive agents - methylphenidate may reduce the effectiveness of drugs used to treat hypertension.
  • Dopaminergic drugs (e.g., levodopa, bromocriptine) - potential for additive 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: Methylphenidate can cause dose-related increases in BP and HR.

Timing: Prior to initiation of therapy.

Height and Weight

Rationale: Monitor for potential growth suppression in pediatric patients.

Timing: Prior to initiation of therapy.

Psychiatric History (e.g., bipolar disorder, psychosis, tics)

Rationale: To assess risk of psychiatric adverse events or exacerbation of pre-existing conditions.

Timing: Prior to initiation of therapy.

Cardiac History (e.g., structural cardiac abnormalities, family history of sudden death)

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.

Target: Maintain within normal limits for age/baseline.

Action Threshold: Significant or sustained increases (e.g., >10-20 mmHg systolic/diastolic, >10-20 bpm HR) warrant investigation and potential dose adjustment or discontinuation.

Height and Weight

Frequency: Every 3-6 months in pediatric patients.

Target: Maintain normal growth trajectory.

Action Threshold: Significant deviation from expected growth curve warrants investigation and potential dose adjustment or drug holiday.

ADHD Symptom Control

Frequency: Regularly, at each follow-up visit.

Target: Improved attention, reduced hyperactivity/impulsivity.

Action Threshold: Lack of efficacy or worsening symptoms may indicate need for dose adjustment or alternative therapy.

Emergence/Exacerbation of Psychiatric Symptoms (e.g., psychosis, mania, aggression, anxiety, depression, tics)

Frequency: Regularly, at each follow-up visit.

Target: Absence of new or worsening symptoms.

Action Threshold: Any new or worsening psychiatric symptoms warrant immediate evaluation and potential discontinuation.

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Symptom Monitoring

  • Chest pain
  • Shortness of breath
  • Syncope
  • Palpitations
  • New or worsening tics
  • Hallucinations
  • Delusional thinking
  • Mania
  • Aggression
  • Severe anxiety
  • Depressed mood
  • Unexplained weight loss
  • Sleep disturbances

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 doses higher than human therapeutic doses. There are limited human data, but some studies suggest a possible increased risk of cardiac malformations with first-trimester exposure, though findings are inconsistent.

Trimester-Specific Risks:

First Trimester: Possible increased risk of cardiac malformations (inconsistent data).
Second Trimester: Not well-studied, but generally lower risk of major malformations.
Third Trimester: Potential for premature birth, low birth weight, and withdrawal symptoms in the neonate (e.g., agitation, tremors, poor feeding) if used close to delivery.
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Lactation

Methylphenidate is excreted into human milk. Monitor breastfed infants for agitation, insomnia, decreased appetite, or poor weight gain. Consider the developmental and health benefits of breastfeeding along with the mother's clinical need for methylphenidate and any potential adverse effects on the breastfed infant.

Infant Risk: L3 (Moderately Safe) - Monitor infant for irritability, sleep disturbances, and feeding issues.
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Pediatric Use

Approved for ADHD in children 6 years and older. Monitor growth (height and weight) carefully due to potential for growth suppression. Monitor for emergence or exacerbation of psychiatric symptoms.

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Geriatric Use

Safety and efficacy have not been established in geriatric patients. Use with caution due to increased sensitivity to stimulant effects and potential for underlying cardiovascular conditions. Start with lower doses and titrate slowly.

Clinical Information

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Clinical Pearls

  • Extended-release methylphenidate formulations are designed for once-daily dosing, typically in the morning, to provide symptom control throughout the school or workday.
  • Patients should be instructed to swallow the tablet whole; crushing or chewing can lead to dose dumping and increased side effects.
  • Monitor cardiovascular parameters (BP, HR) regularly, especially at baseline and after dose adjustments.
  • Be vigilant for psychiatric adverse events, including new-onset psychosis, mania, or severe anxiety, particularly in patients with a history of psychiatric illness.
  • Growth suppression is a concern in pediatric patients; regular height and weight monitoring is crucial, and drug holidays may be considered if growth is significantly affected.
  • Educate patients and caregivers about the potential for abuse and dependence, and the importance of secure storage.
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Alternative Therapies

  • Other CNS stimulants (e.g., amphetamine salts, lisdexamfetamine)
  • Non-stimulants (e.g., atomoxetine, guanfacine ER, clonidine ER)
  • Behavioral therapy
  • Cognitive behavioral therapy (CBT)
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Cost & Coverage

Average Cost: $200 - $600+ per 30 tablets
Generic Available: Yes
Insurance Coverage: Tier 2 or Tier 3 (for brand-name ER formulations); Tier 1 (for generic immediate-release)
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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 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 for guidance. 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.