ADHD MEDICATION

A guide to switching medications containing methylphenidate

Introduction

Many patients are currently facing difficulties in procuring their prescribed ADHD medication due to ongoing shortages. In such cases, switching to an alternative formulation may be necessary to maintain symptom control. This guide explains how switching works, the differences between medications and how to ensure a smooth transition.

Overview

Long-acting methylphenidate formulations provide extended symptom control for ADHD, reducing the need for multiple daily doses. These formulations differ in their release profiles, duration of action, and effect on symptom control throughout the day. This guide details different long-acting methylphenidate options, their dose equivalence, pharmacokinetics, and switching guidance.

How Methylphenidate Works

Methylphenidate is a central nervous system (CNS) stimulant that works primarily by increasing the levels of dopamine and noradrenaline in the brain. These neurotransmitters play a crucial role in attention, impulse control, and executive function.

How methylphenidate works

Mechanism of Action:

  • Blocks Reuptake: Methylphenidate inhibits the reuptake of dopamine and noradrenaline by blocking their transporters (DAT and NET) at the synapse. This leads to increased concentrations of these neurotransmitters in the prefrontal cortex, which is responsible for attention and impulse control.
  • Enhances Neurotransmission: By increasing the availability of dopamine and noradrenaline, methylphenidate helps improve focus, attention span and executive function, reducing symptoms of ADHD.
  • Immediate vs. Extended Release: Short-acting formulations provide rapid symptom relief, while long-acting formulations (e.g., Concerta XL, Equasym XL, Medikinet XL) use controlled-release mechanisms to sustain effects throughout the day.
  • Effects of Methylphenidate:

    • Improves attention and focus
    • Reduces impulsivity and hyperactivity
    • Enhances executive functioning and task completion

    Types of Long-Acting Methylphenidate Formulations

    Type

    Medications

    IR:MR Ratio

    Duration of Action

    Release profile

    1

    Concerta XL, Xaggitin XL, Matoride XL, Delmosart XL, Affenid XL, Xenidate XL

    22:78

    10-12 hours

    Smooth and prolonged release, peak effect in the afternoon

    2

    Equasym XL

    30:70

    ~8 hours

    Faster initial release, shorter duration

    3

    Medikinet XL, Metyrol XL, Meflynate XL

    50:50

    ~8 hours

    Rapid initial effect, shorter symptom coverage

    Understanding Immediate Release (IR) vs. Extended Release (ER) Components

    Many XL (extended-release) medications combine two types of methylphenidate:

    • Immediate Release (IR): This part of the medication works quickly, usually within 30-60 minutes of taking it. It provides a fast boost of symptom control but wears off quickly.
    • Extended Release (ER): This part of the medication is released slowly over several hours, helping to maintain symptom control throughout the day.

    Think of it like a rollercoaster ride:

    • The IR component is like the first big push up the hill—you feel the effects quickly.
    • The ER component is like a long, steady ride—it keeps you going throughout the day without as many ups and downs.

    Different medications have different IR:ER ratios, meaning some give you more of the fast-acting boost (like Medikinet XL), while others focus more on steady, all-day control (like Concerta XL). Understanding this helps in choosing the right medication based on when you need symptom control the most.

    How to switch

    How Switching Works

    When switching from one formulation to another, consider the following factors:

    • Different release profiles affect symptom control throughout the day.
    • Dosage conversion may be necessary based on immediate-release and extended-release ratios.
    • Side effects may vary, especially if switching to a formulation with a higher immediate-release component.
    • A transition period may be needed, during which symptom control should be closely monitored.
    • Consult your prescribing specialist before making any medication adjustments.

    FINAL ADVICE

    • Always consult a specialist before switching formulations.
    • Monitor for side effects and adjust dosage accordingly.
    • Switching should be done based on symptom control and daily needs.

    SWITCHING

    Actions for Specialists

    Step 1: Prior to Considering a Switch in Modified Release Preparation

    1. Undertake an urgent review/risk assessment of the patient, weighing the pros and cons of switching.
    2. Consider whether a treatment holiday is the best option for the patient.
    3. Discuss with the patient the possible differences in symptom management.
    4. Consider the timing of target symptoms and use this to guide which capsule formulation may be best.
    5. Discuss possible side effects and escalation processes.
    6. Ensure family/carers are aware that any changes in symptoms of co-morbidities should be reported to the prescriber.

    Step 2: Formulation Comparison

  • All long-acting methylphenidate (MPH) preparations include an immediate-release (IR) and modified-release (MR) component.
  • Preparations differ in their IR and ER release profiles, which influences how symptom control is distributed throughout the day.
  • Switching between long-acting preparations should be guided by the different pharmacokinetic profiles in addition to other considerations outlined by the Specialist Pharmacy Services.
  • Step 3: Switching Between Preparations

    1. Switching formulations can result in changes in symptom control at different times of the day.
    2. Example: TYPE 3 medications (e.g., Medikinet XL) target symptoms in the morning more potently, whereas TYPE 1 medications (e.g., Concerta XL) have a stronger clinical effect later in the day (early afternoon).
    3. Patients should be reviewed after the switch, and doses adjusted if required.
    4. Preferred Switching Strategy:Switching between bioequivalent tablets (TYPE 1) is the recommended first option.During shortages, generic prescriptions for TYPE 1 medications should be issued to allow pharmacies to dispense any available equivalent brand.If no supplies are available, consider switching to a suitable long-acting capsule (TYPE 2 or TYPE 3).
    5. Modified Release Capsules MUST be Prescribed by Brand- Different brands have different release profiles, making it essential to prescribe by brand name to ensure consistent symptom control.
    6. Guidance for Adjusting to New Medication: Since clinical equivalence is most closely related to the IR component, IR should be used as a reference when switching between long-acting MPH formulations.Use reference tables for guidance on dose conversions.Patients should be monitored closely post-switch to ensure symptom control remains effective.

    How to switch from Concerta XL to Equasym XL and vice versa

    Switching between Type 1 & Type 2 (Concerta XL 54mg to Equasym XL)

    Use the reference table to identify the IR component of Concerta XL 54mg. Concerta XL 54mg IR Component = 12 mg

    Use the reference table for Type 2 to identify the closest match in IR component. Equasym XL closest IR component = 12mg, contained in Equasym XL 40mg capsules

    Suitable switch would be Equasym XL 40mg Capsules along with monitoring for symptom control.

    Switching between Type 2 & Type 3 (Equasym XL 20mg to Medikinet XL)

    Switching between Type 2 & Type 3 (Equasym XL 20mg to Medikinet XL)

    Use the reference table below to identify the IR component of Equasym XL 20mg. Equasym XL 20mg IR Component = 6mg

    Use the reference table for Type 3 to identify the closest match in IR component. Medikinet closest IR component = 5mg, contained in Medikinet XL 10mg capsules

    Suitable switch would be Medikinet XL 10mg Capsules along with monitoring for symptom control.

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    COMPARISON TABLES

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    Sanctum Healthcare