 Methylphenidate
Systematic (IUPAC) name
methyl phenyl(piperidin-2-yl)acetate
Identifiers
CAS number : 113-45-1
ATC code : N06BA04
PubChem : 4158
DrugBank : APRD00657
ChemSpider : 4015
Chemical data
Formula : C14H19NO2
Mol. mass : 233.31 g/mol
SMILES : eMolecules & PubChem
Pharmacokinetic data
Bioavailability 11–52%
Protein binding 30%
Metabolism Liver
Half life 2–4 hours
Excretion Urine
Therapeutic considerations
Pregnancy cat. C
Routes Oral, Transdermal, IV, Nasal
Methylphenidateis the most commonly prescribed psychostimulant and is
indicated in the treatment of attention-deficit hyperactivity disorder,
Postural Orthostatic Tachycardia Syndrome and narcolepsy, although
off-label uses include treating lethargy, depression, neural insult, and
obesity. In North America it is most commonly known as the brand name
Ritalin, which is an instant-release racemic mixture, although a variety
of brand names and formulations exist.Methylphenidate is a potent
central nervous system stimulant derived from amphetamine, and is
thought to exert its effect by increasing dopaminergic stimulation in
the brain.
History
Methylphenidate was patented in 1954 by the CIBA pharmaceutical company
(now Novartis) as a potential cure for Mohr's disease
Beginning in the 1960s, it was used to treat children with ADHD or ADD,
known at the time as hyperactivity or minimal brain dysfunction (MBD).
Today methylphenidate is the most commonly prescribed medication to
treat ADHD around the world.Production and prescription of
methylphenidate rose significantly in the 1990s, especially in the
United States, as the ADHD diagnosis came to be better understood and
more generally accepted within the medical and mental health
communities.
Attention deficit hyperactivity disorder Methylphenidate is approved by
the FDA for the treatment of attention-deficit hyperactivity disorderThe
addition of behavioural modification therapy (e.g. CBT) has additional
benefits on treatment outcomeThere is a lack of evidence of the
effectiveness in the long term of beneficial effects of methylphenidate
with regard to learning and academic performance.A meta analysis of the
literature concluded that methylphenidate quickly and effectively
reduces the signs and symptoms of ADHD in children under the age of 18
in the short term but found that this conclusion may be biased due to
the high number of low quality clinical trials in the literature. There
have been no placebo controlled trials investigating the long term
effectiveness of methylphenidate beyond 4 weeks thus the long term
effectiveness of methylphenidate has not been scientifically
demonstrated. Serious concerns of publication bias regarding the use of
methylphenidate for ADHD has also been noted.A diagnosis of ADHD must be
confirmed and the benefits and risks and proper use of stimulants as
well as alternative treatments should be discussed with the parent
before stimulants are prescribed.The dosage used can vary quite
significantly from individual child to individual child with some
children responding to quite low doses whereas other children require
the higher dose range. The dose therefore should be titrated to an
optimal level which achieves therapeutic benefit and minimal side
effectsTherapy with methylphenidate should not be indefinite. Weaning
off periods to assess symptoms are recommended.
Pregnancy Implications
There are no well-controlled studies establishing safety in pregnant
women. Animal studies have shown teratogenic effects to the fetus. Do
not use in women of childbearing age unless the potential benefit
outweighs the possible risk.
Lactation
Excretion in breast milk unknown/use caution
 Contraindications
Hypersensitivity to methylphenidate, any component of the formulation,
or idiosyncrasy to sympathomimetic amines; marked anxiety, tension, and
agitation; glaucoma; use during or within 14 days following MAO
inhibitor therapy; Tourette's syndrome or tics
Warnings/Precautions:
Has demonstrated value as part of a comprehensive treatment program for
ADHD. Safety and efficacy in children <6 years of age not established.
Use with caution in patients with bipolar disorder, diabetes mellitus,
cardiovascular disease, hyperthyroidism, seizure disorders, insomnia,
porphyria, or hypertension. Use caution in patients with history of
ethanol or drug abuse. May exacerbate symptoms of behavior and thought
disorder in psychotic patients. Do not use to treat severe depression or
fatigue states. Potential for drug dependency exists - avoid abrupt
discontinuation in patients who have received for prolonged periods.
Visual disturbances have been reported (rare). Stimulant use has been
associated with growth suppression. Growth should be monitored during
treatment. Stimulants may unmask tics in individuals with coexisting
Tourette's syndrome. should not be used in patients with esophageal
motility disorders or pre-existing severe gastrointestinal narrowing
(small bowel disease, short gut syndrome, history of peritonitis, cystic
fibrosis, chronic intestinal pseudo-obstruction, Meckel's diverticulum).
Stability
Immediate release tablet: Do not store above 30°C (86°F); protect from
light Extended release capsule: Store in dose pack provided at 25°C
(77°F) Sustained release tablet: Do not store above 30°C (86°F); protect
from moisture Osmotic controlled release tablet Store at 25°C (77°F);
protect from humidity
Mechanism of Action
Mild CNS stimulant; blocks the reuptake mechanism of dopaminergic
neurons; appears to stimulate the cerebral cortex and subcortical
structures similar to amphetamines
Methylphenidate is a medication prescribed for individuals (usually
children)
who have attention-deficit hyperactivity disorder (ADHD), which consists
of a
persistent pattern of abnormally high levels of activity, impulsivity,
and/or
inattention that is more frequently displayed and more severe than is
typically
observed in individuals with comparable levels of development. The
pattern of
behavior usually arises between the ages of 3 and 5, and is diagnosed
during
the elementary school years due to the child’s excessive locomotor
activity, poor attention, and/or impulsive behavior.
Most symptoms improve during adolescence or adulthood, but the disorder
can
persist or present in adults. It has been estimated that 3–7 percent of
school-age children have ADHD. Methylphenidate also is occasionally
prescribed for
treating narcolepsy.
Health Effects
Methylphenidate is a central nervous system (CNS) stimulant. It has
effects
similar to, but more potent than, caffeine and less potent than
amphetamines. It has a notably calming and “focusing” effect on those
with ADHD, particularly
children.
 Note:
These API/ chemicals are designated as
those that are used in the manufacture of the controlled substances and
are important to the manufacture of the substances. For any (Control
Substance) products Import and Export *** subjected to your country
government laws /control substance ACT.
Note /Government Notification:
These chemicals are designated as those that are used in the manufacture
of the controlled substances and are important to the manufacture of the
substances. For any (Control Substance) products Import and Export ***
subjected to your country government laws /control substance ACT.
Information: The information on this web page is provided to help you
to work safely, but it is intended to be an overview of hazards, not a
replacement for a full Material Safety Data Sheet (MSDS). MSDS forms can
be downloaded from the web sites of many chemical suppliers. ,also that
the information on the PTCL Safety web site, where this page was hosted,
has been copied onto many other sites, often without permission. If you
have any doubts about the veracity of the information that you are
viewing, or have any queries, please check the URL that your web browser
displays for this page. If the URL begins "www.tajapi.com/www/Denatonium
Benzoate.htm/" the page is maintained by the Safety Officer in Physical
Chemistry at Oxford University. If not, this page is a copy made by some
other person and we have no responsibility for it.
The Controlled Substances Act (CSA) was enacted into law by the Congress
of the United States as Title II of the Comprehensive Drug Abuse
Prevention and Control Act of 1970.[1] The CSA is the federal U.S. drug
policy under which the manufacture, importation, possession, use and
distribution of certain substances is regulated. The Act also served as
the national implementing legislation for the Single Convention on
Narcotic Drugs.
|
|
India
