atomoxetine & methylphenidilate

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atomoxetine & methylphenidilate

  1. 1. - DR DEEPIKA SINGH, RESIDENT, DEPT OF PSYCHIATRY, GSMC & KEMH
  2. 2. DRUG TREATMENT: • STIMULANT DRUGS - METHYLPHENIDATE - DEXTROAMPHETAMINES • - NONSTIMULANT DRUGS ATOMOXETINE HCL BUPROPION VENLAFAXINE CLONIDINE, GUANAFACINE
  3. 3. 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
  4. 4. Methylphenidate (Ritalin, MPH, MPD) is a psychostimulant drug approved for treatment of -ADHD -Narcolepsy -Treatment-resistant depression
  5. 5. Molecular formula: C14-H19-N-O2 Other systematic names: 2-Piperidine acetic acid, alpha-phenyl, methyl ester
  6. 6. 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)
  7. 7. MECHANISM OF ACTION
  8. 8. • ENHANCEMENT OF DOPAMINE 1) Dorsolateral pre frontal cortex 2) Basal ganglia 3) Medial prefrontal cortex & Hypothalamus
  9. 9. SIDE EFFECTS • COMMONLY SEEN: -Insomnia -Headache -Dizziness -Tremor -Anorexia -Abdominal pain -Weight loss
  10. 10. • LIFE THREATENING SIDE EFFECTS: - Psychotic episodes - Seizures - CVS adverse effects • PHARMACOKINETICS: Half life Adults- 3.5 hrs Children- 2.5 hrs
  11. 11. 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
  12. 12. • 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
  13. 13. CONCERTA
  14. 14. 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.
  15. 15. 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
  16. 16. 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.
  17. 17. • Atomoxetine is designated chemically as N-methyl-3-phenyl-3-propylamine hydrochloride BRANDS: - Strattera - Attentrol - Axepta
  18. 18. MECHANISM OF ACTION • Despite its name selective norepinephrine reuptake inhibitor , it enhances both Dopamine & Norepinephrine in frontal cortex
  19. 19. • 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.
  20. 20. SIDE EFFECTS • Commonly seen: -decreased appetite -increase HR & BP -Insomnia, dizziness, anxiety, agitation , aggression, irritability, sweating -Dry mouth , nausea , vomiting, dyspepsia, abdominal pain, -Urinary hesitency & retention -Sexual dysfunctions
  21. 21. • - 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
  22. 22. 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
  23. 23. ABUSE POTENTIAL • Lack of enhancing dopamine activity in limbic area theoretically explains atomoxetine’s lack of abuse potential.
  24. 24. 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.
  25. 25. THANKYOU…
  26. 26. REFERENCES 1] Kaplan & Sadock’s Comprehensive Textbook Of Psychiatry 2] Stephen Stahl's Essential Psychopharmacology 3] Stephen Stahl’s Prescribers guide 4] The Maudsley’s Prescribing Guidelines
  27. 27. QUESTIONS

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