Chapter 05 Drugs Acting on the Central Nervous System: Anti-Depressant Drugs

Chapter 05 Drugs Acting on the Central Nervous System: Anti-Depressant Drugs

• 2.
  Introduction • Antidepressants aredrugs which enhance alertness and may result in an increased output of behavior. • They are used for the relief of symptoms of moderate and severe depressive disorder. • Depression is characterized by feelings of intense sadness or worry, agitation, self- depression, physical changes such as insomnia, anorexia, loss of enthusiasm, and mental slowing. • Major depression is one of the most common psychotic disorders.
• 4.
  • Chemical Formula:C₂₀H₂₃N 3-(10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5-ylidene)-N,N-dimethylpropan-1-amine • Physical Properties: • White to off-white solid, brownish crystals. • Slightly basic in nature. • Freely soluble in water and alcohol. • Insoluble in other organic solvents. • Pharmaceutical Formulation: • Oral preparations: tablets, syrup. • Injectable form: intramuscular. • Stability and Storage: • Store in well-closed airtight containers. • Protect from light. Amitriptyline Hydrochloride
• 5.
  • Brand Names:: •Amitril • Tryptomer • Nactyp • Dose: 50–75 mg daily in divided doses or as a single dose at night. • Medicinal Uses: • Treatment of depression associated with anxiety. • Management of enuresis in children and adolescents.
• 6.
  • Shows high5-HT/NE uptake block ratio. • Useful in endogenous depression, especially manic-depressive and involutional psychosis. • Chemical Formula: C₁₉H₂₄N₂·HCl • Physical Properties: • White to off-white, colourless, odourless powder. • Freely soluble in water. • Less soluble in alcohol. • Sparingly soluble in acetone. • Hydrochloride salt of synthetic tricyclic derivative. • Pharmaceutical Formulation: Tablet, Capsule, Syrup, Intramuscular Injection. Imipramine Hydrochloride 5-[3-(Dimethylamino)propyl]-10,11-dihydro- dibenzazepine hydrochloride
• 7.
  • Stability andStorage: • Store at 20–25°C • Protect from light • Avoid moisture • Brand Names: • Tofromil • Depcure • Microdep • Dose: 50–150 mg daily in divided doses. • Medicinal Uses: • Endogenous depression (manic-depressive, involutional psychosis). • Nocturnal enuresis in children above 6 years.
• 8.
  • Selective serotoninreuptake inhibitor (SSRI). • Used in endogenous depression, OCD, obesity, and alcoholism. • Chemical Formula: C₁₇H₁₈F₃NO • Physical Properties: • White to off-white crystalline solid. • Soluble in methanol and ethanol. • Partially soluble in acetone and acetonitrile. • Sparingly soluble in dichloromethane. • Insoluble in ethyl acetate, toluene, cyclohexane, hexane. • Pharmaceutical Formulation • Oral syrup • Tablets • Veterinary injection also available Fluoxetine N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan- 1-amine
• 9.
  • Stability andStorage: • Store in well-closed airtight containers. • Protect from direct light. • Brand Names: • Fludac • Platin • Flunil • Dose: 20–80 mg/day. • Medicinal Uses: • Depression. • Obsessive-compulsive disorder. • Panic disorder.
• 10.
  • SSRI antidepressant. •Used in major depressive disorder, OCD, and social phobia. • Chemical Formula: C₂₀H₂₁FN₂O • Physical Properties: • Fine white to off-white crystals with faint odour. • Freely soluble in water, ethanol, and chloroform. • On heating emits toxic nitrogen oxides, hydrogen fluoride, and hydrogen bromides. • Pharmaceutical Formulation • Oral solution. • Tablet and capsule. Citalopram 1-[3-(Dimethylamino)propyl]-1-(4-fluorophenyl)-1,3- dihydroisobenzofuran-5-carbonitrile
• 11.
  • Stability andStorage: • Store at 25°C. • Protect from high temperatures. • Brand Names: • Celexa • Citolapram • Citapad • Dose: Maximum dose: 40 mg/day. • Medicinal Uses: • Major depressive disorder. • Off-label use in anxiety and dysthymia.
• 12.
  • Used inmajor depressive disorder and generalized anxiety disorder. • Chemical Formula: C₂₀H₂₁FN₂O • Physical Properties: • Fine white to slightly yellow powder. • Freely soluble in methanol and DMSO. • Soluble in isotonic saline. • Sparingly soluble in water and ethanol. • Insoluble in heptane. • Pharmaceutical Formulation: • Oral solution. • Tablet and capsule. • Stability and Storage: Store at 25°C and Protect from high temperatures. Escitalopram 1-[3-(Dimethyl amino)propyl]-1-(4-fluorophenyl)-1,3- dihydroisobenzofuran-5-carbonitrile
• 13.
  • Brand Names: •Lexapro • Cipralex • Nexito • Dose: • 10 mg once daily. • Can be increased to 20 mg/day after 3 weeks. • Medicinal Uses: • Major depressive disorder. • Off-label use in anxiety and dysthymia.
• 14.
  Sertraline • Better toleratedthan TCAs. • Effective in GAD and OCD. • Chemical Formula: C₁₇H₁₇Cl₂N • Physical Properties: • White crystalline solid or powder. • Soluble in water. • Slightly soluble in isopropyl alcohol. • Pharmaceutical Formulation: • Oral solution. • Tablet and capsule. • Stability and Storage: • Store at room temperature. • Protect from direct light. 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methylnaphthylamine
• 15.
  • Brand Names: •Zoloft • Serta • Zosert • Dose: 50 mg/day. • Medicinal Uses: • Major depressive disorder. • OCD. • Panic disorder. • PTSD. • Premenstrual dysphoric disorder. • Social anxiety disorder.
• 16.
  Paroxetine • Also usedin premature ejaculation and menopausal hot flashes. • Chemical Formula: C₁₉H₂₀FNO₃ • Physical Properties: • Odourless, bitter, off-white powder. • Melting point: 120–138°C. • Soluble in alcohol and water. • Pharmaceutical Formulation: • Tablet • Suspension • Controlled-release tablet • Capsule 3-[(2H-1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine
• 17.
  • Stability andStorage: • Store at 20–25°C and Protect from light. • Keep container tightly closed. • Brand Names: • Pexep • Paroxtime • Seroxat • Dose: Maximum dose: 62.5 mg/day. • Medicinal Uses: • Depression. • OCD. • Panic attacks. • Anxiety. • PTSD.
• 18.
  Duloxetine • Chemical Formula:C₁₈H₁₉NOS • Physical Properties: • White to beige (slightly brown) crystals • Acid labile • Soluble in water and methanol • Insoluble in neutral organic solvents • Pharmaceutical Formulation: • Tablet • Capsule • Stability and Storage: • Store at 15–30°C and Protect from heat, moisture, and light. • Keep out of reach of children N-methyl-3-naphthalen-1-yloxy-3-thiophen-2-ylpropan-1-amine
• 19.
  • Brand Names: •Effexor • Neulox • Duloxin • Dose: Maximum dose: 120 mg/day. • Medicinal Uses: • Major depressive disorder. • Generalized anxiety disorder. • Fibromyalgia. • Diabetic peripheral neuropathy. • Chronic musculoskeletal pain.
• 20.
  Venlafaxine • Chemical Formula:C₁₇H₂₇NO₂ • Physical Properties: • White to off-white crystalline solid. • Metabolized into active metabolite. • Soluble in water and methanol. • Pharmaceutical Formulation: • Oral tablet (immediate release: 25–100 mg). • Extended release capsules: 37.5–225 mg. • Stability and Storage: • Store in cool, dry place and Protect from light. 1-[2-dimethylamino-1-(4- methoxyphenyl)ethyl]cyclohexanol
• 21.
  • Brand Names: •Effexor • Venlor • Venzee • Dose: • Moderate depression: up to 225 mg/day. • Severe depression (inpatients): up to 375 mg/day. • Medicinal Uses: • Depression. • Generalized anxiety disorder. • Social phobia. • Panic disorder. • Vasomotor syndrome.