Methylphenidate Hydrochloride

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Cat Number

API0232475

CAS Number

298-59-9

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Product Detail Description Scientific Support Customer Q&A

CAS Number

298-59-9

EINECS

206-065-3

Synonyms

Methylphenidate HCl, Ritalin, Ritalin SR

Molecular Formula

C14H19NO2·HCl

Molecular Weight

269.77

Smiles

COC(=O)C(C1CCCCN1)C2=CC=CC=C2.Cl

Appearance

White crystalline powder

Melting Point

224-226ºC

Boiling Point

327.6℃

General Description

Methylphenidate hydrochloride is a central nervous system (CNS) stimulant belonging to the piperidine class, prescribed for attention deficit hyperactivity disorder (ADHD) and narcolepsy.

Mechanism of Action

Methylphenidate 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. It is a racemic mixture comprised of the d- and l-threo enantiomers, with the d-isomer being more pharmacologically active. The drug is metabolized primarily via deesterification to ritalinic acid, which has little or no pharmacologic activity, with approximately 80% of the dose excreted in urine.

Application

Methylphenidate hydrochloride is indicated for the treatment of Attention Deficit Hyperactivity Disorder (ADHD) in pediatric patients 6 years and older and adults, and for narcolepsy. In pediatric patients, therapy is initiated at 5 mg twice daily (before breakfast and lunch) with weekly titration, not exceeding 60 mg/day. Adults typically require 20 to 30 mg daily administered in divided doses 2 or 3 times daily, with a maximum of 60 mg daily.

Mintzer J, et al. conducted a randomized, placebo-controlled trial enrolling 200 patients with Alzheimer disease and clinically significant apathy to receive methylphenidate 10 mg twice daily or placebo for 6 months. Methylphenidate treatment resulted in significantly greater reduction in apathy severity as measured by the Neuropsychiatric Inventory (NPI) apathy subscale (mean difference –1.25; 95% CI –2.03 to –0.47; P = 0.002). The treatment effect was most pronounced within the first 100 days, with a significantly higher proportion of methylphenidate-treated patients achieving resolution of apathy (hazard ratio 2.16).

Fig. 1 Kaplan-Meier estimates of proportion of participants achieving a neuropsychiatric inventory apathy score of 0. (Mintzer J, et al., 2021)

References

Mintzer J, et al. Effect of Methylphenidate on Apathy in Patients With Alzheimer Disease: The ADMET 2 Randomized Clinical Trial. JAMA Neurol. 2021;78(11):1324-1332.

What are the specific storage requirements for Methylphenidate Hydrochloride as a controlled substance?

As a Schedule II CNS stimulant, it must be stored in a securely locked, limited-access area, in compliance with DEA regulations, with complete inventory records maintained.

Is Methylphenidate Hydrochloride sensitive to elevated temperatures during summer shipping?

It is stable at ambient temperatures. However, we monitor shipments during heat waves and use insulated packaging if necessary to prevent any risk of softening or caking.

Does Methylphenidate Hydrochloride require protection from moisture?

It is slightly hygroscopic. We use double polyethylene bags with desiccant inside fiber drums to ensure it remains dry and free-flowing during long-term storage.

What impurities are specifically monitored during stability studies of Methylphenidate Hydrochloride?

We monitor for the erythro isomer (a chiral impurity) and threo enantiomer, as well as degradation products like ritalinic acid, using a validated chiral HPLC method.