Methylphenidate (Brand Names in India: Concerta, Addwize, Inspiral, Equasym, Medikinet)

1. Generic Name

Methylphenidate Hydrochloride

2. Brand Names

• Concerta (Janssen-Cilag)
• Addwize (Lupin)
• Inspiral (Sun Pharmaceuticals)
• Equasym (Shire India)
• Medikinet (Dr. Reddy’s Laboratories)

3. Pharmaceutical Formulation

• Tablets: 5 mg, 10 mg, 20 mg
• Extended-Release Tablets: 18 mg, 27 mg, 36 mg, 54 mg
• Extended-Release Capsules: 10 mg, 20 mg, 30 mg, 40 mg

4. Therapeutic Classification

Central Nervous System (CNS) Stimulant

5. Indications

Methylphenidate is indicated for:

• Attention Deficit Hyperactivity Disorder (ADHD): Children ≥6 years, adolescents, and adults.
• Narcolepsy: Symptomatic management.

6. Mechanism of Action

Methylphenidate inhibits the reuptake of dopamine and norepinephrine in the prefrontal cortex by blocking their transporters. This increases their availability in synaptic clefts, enhancing focus, attention, and impulse control.

7. Dosage and Administration

Children and Adolescents (≥6 years):

• Immediate-Release Tablets: Start with 5 mg twice daily (morning and noon); increase weekly in increments of 5-10 mg/day. Maximum dose: 60 mg/day.
• Extended-Release Formulations: Start with 18 mg once daily in the morning; adjust weekly in 18 mg increments. Maximum dose: 72 mg/day.

Adults:

• Immediate-Release Tablets: Start with 10 mg twice daily; titrate as needed. Maximum dose: 60 mg/day.
• Extended-Release Formulations: Start with 18-36 mg once daily; adjust as necessary.

Administration:

• Immediate-release formulations can be given 2-3 times per day.
• Extended-release formulations should be taken once daily, preferably in the morning.

8. Onset of Action

Immediate-Release Tablets: Onset within 30-60 minutes; duration 3-4 hours.
Extended-Release Formulations: Onset within 1-2 hours; duration 8-12 hours.

9. Contraindications

• Known hypersensitivity to methylphenidate or its excipients.
• Severe anxiety, agitation, or tension.
• Glaucoma.
• Tics or a family history of Tourette syndrome.
• Concurrent use with monoamine oxidase inhibitors (MAOIs) or within 14 days of discontinuation.

10. Warnings and Precautions

• Cardiovascular Events: Risk of sudden death, stroke, or myocardial infarction in patients with structural cardiac abnormalities or serious heart conditions.
• Growth Suppression: Monitor height and weight in pediatric patients.
• Psychiatric Symptoms: May exacerbate anxiety, aggression, or psychosis.
• Abuse Potential: High risk of misuse and dependency.
• Seizures: Use cautiously in patients with a history of seizures.

11. Side Effects

Common:

• Insomnia, headache, loss of appetite
• Nervousness, abdominal pain, weight loss

Serious:

• Cardiovascular events (e.g., palpitations, hypertension, arrhythmias)
• Psychiatric effects (e.g., psychosis, mania, suicidal ideation)
• Growth suppression in children

12. Drug Interactions

• MAOIs: Risk of hypertensive crisis; contraindicated.
• Antihypertensives: Reduced efficacy.
• Serotonergic Drugs: Increased risk of serotonin syndrome.
• CYP2D6 Inhibitors: May increase methylphenidate levels.

13. Overdose Management

Symptoms: Vomiting, agitation, tremors, hyperreflexia, convulsions, confusion, hallucinations, tachycardia, arrhythmias.
Treatment: Symptomatic and supportive care. Activated charcoal may help if administered early. Monitor cardiovascular and respiratory status.

14. Pharmacokinetics

• Absorption: Rapid; extended-release forms provide controlled drug delivery over time.
• Distribution: Low plasma protein binding (~10-33%).
• Metabolism: Primarily hepatic via de-esterification to inactive metabolites.
• Elimination: Excreted primarily in urine; half-life ~2-3 hours (immediate-release).

15. Storage and Handling

Store at a temperature below 30°C, protected from light and moisture. Keep out of reach of children.

16. Packaging

Available in blister packs or bottles containing 10, 20, or 30 tablets/capsules.

17. Manufacturer Information

• Concerta: Janssen-Cilag
• Addwize: Lupin
• Inspiral: Sun Pharmaceuticals
• Equasym: Shire India
• Medikinet: Dr. Reddy’s Laboratories