4. HISTORY
-Methylphenidate was first
synthesized in 1944, and
was identified as a stimulant
in 1954.
-Methylphenidate was
synthesized by Ciba (now
Novartis) chemist Leandro
Panizzon.
-Beginning in the 1960s, it
was used to treat children
with ADHD or ADD
5. Methylphenidate (Ritalin, MPH, MPD) is a
psychostimulant drug approved for treatment of -ADHD
-Narcolepsy
-Treatment-resistant depression
7. BRANDS & AVAILABLE FORMS
• The dosage forms of methylphenidate are tablets, capsules, patches,
and liquid.
• A formulation by the Novartis trademark name Ritalin, is an
immediate-release racemic mixture, although a variety of
formulations and generic brand names exist.
• Generic brand names include Ritalina, Rilatine, Attenta, Metadate,
Methylin, and Rubifen.
• sustained release tablets or capsules Concerta, Metadate CD,
Methylin ER, Ritalin LA, and Ritalin-SR
• Focalin is a preparation containing only dextro-methylphenidate
• Transdermal patch (under the brand name Daytrana)
9. • ENHANCEMENT OF
DOPAMINE
1) Dorsolateral pre frontal
cortex
2) Basal ganglia
3) Medial prefrontal cortex
& Hypothalamus
10. SIDE EFFECTS
• COMMONLY SEEN:
-Insomnia
-Headache
-Dizziness
-Tremor
-Anorexia
-Abdominal pain
-Weight loss
11. • LIFE THREATENING SIDE
EFFECTS:
- Psychotic episodes
- Seizures
- CVS adverse effects
• PHARMACOKINETICS:
Half life
Adults- 3.5 hrs
Children- 2.5 hrs
12. DOSAGE
• ADHD
- Upto 2mg/kg/day
in children > 6yrs age
max dose 60mg/day
- Adults : 20-30mg/day
max dose 40-60mg/day
• NARCOLEPSY
- 20 to 60 mg/day
in 2-3 divided doses
13. • IMMEDIATE RELEASE TABLET
2 to 4 hrs duration of action
• EXTENDED RELEASE TABLET
(RITALIN SR, METADATE ER)
4 to 6 hrs duration of action
• NEWER SUSTAINED RELEASE TABLET
-CONCERTA
12 hrs duration of action
-RITALIN LA & METADATE CD
8 hrs duration of action
16. ABUSE POTENTIAL
- Schedule II drug
- Methylphenidate has high potential for abuse due to
its pharmacological similarity to cocaine and
amphetamines
- Methylphenidate, like other stimulants, increases
dopamine levels in the brain, but at therapeutic doses
this increase is slow, and thus euphoria does not
typically occur except in rare instances.
- The abuse potential is increased when
methylphenidate is crushed and insufflated (snorted),
or when it is injected, producing effects somewhat
similar to cocaine.
17. DRUG INTERACTIONS
1) Methylphenidate use within 14 days of MAO
inhibitors is not advised
2) It could inhibit antipsychotic drugs actions
3) No dose adjustments in hepatic & renal
impairment, used with caution in cardiac
impairment
18.
19. ATOMOXETINE
It is a selective norepinephrine
reuptake inhibitor approved for the
treatment of attention-deficit
hyperactivity disorder (ADHD).
Atomoxetine was originally known as
"tomoxetine". However, the U.S. Food
and Drug Administration (FDA)
requested the name be changed
because of the similarity of
"tomoxetine" to "tamoxifen" could lead
to dispensing errors at pharmacies.
20. • Atomoxetine is designated chemically as
N-methyl-3-phenyl-3-propylamine
hydrochloride
BRANDS:
- Strattera
- Attentrol
- Axepta
21. MECHANISM OF ACTION
• Despite its
name selective
norepinephrine
reuptake
inhibitor , it
enhances both
Dopamine &
Norepinephrine
in frontal cortex
22. • Atomoxetine may be preferred over
amphetamine-based stimulants in patients
with :
• psychiatric disorders,
• those who cannot tolerate stimulants,
• and those with a substance misuse recurring
history.
24. •
-
DANGEROUS SIDE EFFECTS:
Increase HR & BP
Liver damage
Induction of mania
Suicidal ideation
• PHARMACOKINETICS:
Hepatic Metabolism by CYP450 2D6
Half life 5 hrs
Excretion : mainly urine
Time to peak , plasma: 1-2 hrs
25. DOSAGE
• 0.5 to 1.2
mg/kg/day
In children upto
70kg
Max dose
1.4mg/kg/day or
100mg/day
whichever less
-40 to 100 mg/day in
adults
26. ABUSE POTENTIAL
• Lack of enhancing
dopamine activity
in limbic area
theoretically
explains
atomoxetine’s lack
of abuse potential.
27. DRUG INTERACTIONS
• Drugs inhibiting CYP 450 2D6 increases plasma
concentration of atomoxetine
• Atomoxetine not to be used with or within 14
days of MAOIs use.
• No dose adjustment in renal impairment
• Dose adjustment required in hepatic
impairment
• Caution in cardiac impairment.
