CNS lecture 5
Antidepressants
Classification of drugs
Selective serotonin reuptake
inhibitors ( SSRIs)
Mechanism of action
Therapeutic uses
• 1st line treatment for depression and GAD
• Obsessive compulsive disorder
• Panic disorder
• Generlized anxiety disorder
• Social anxiety disorder
• Posttraumatic stress disorder
• Premenstrual dysphoric disorder
• Bulimia Nervosa
Fluoxetine(prototype of SSRI)
• Differs from other members having longest
half life of 50 hours
• S_ norfluoxetine with half life of 10 days.
• Only drug approved for bulimia
Pharmacokinetics
• Orally used
• Peak levels in 2_8 hours
• Plasma half life of 16_36 hours
• Metabolized by Cytochrome p450 dependent
enzymes
Adverse effects of SSRIs
Serotonin syndrome
Treatment of SSRIS
• Cyproheptadine treats serotonin
syndrome (imp)
Selective norepinephrine reuptake
inhibitors (SNRIs)
Mechanism of action
Therapeutic uses
• Depression in patients in which SSRIS are not
effective
• Chronic joint and muscle pain
• Fibromyalgia
• Urinary stress incontinence ( duloxetine)
• Treat diabetic neuropathy
Mnemonic ( BAD SNRI)
• B _ body wt loss
• A_ anorexia
• D_ Dec blood pressure
• S_suicidal thoughts
• N_Nausea/ vomiting
• R_reproductive / sexual dysfunction
• I_Insomnia
SSRIS SNRIS
• Inhibits reuptake of • Inhibits the reuptake of both
serotonin only. serotonin and nor epinephrine
• 1st line treatment for • Used to treat major depressive
anxiety and disorders for which SSRIs are not
depression effective along with pain
• Less severe side disorders
effects • More side effects than SSRIS
• More tolerant • Less tolerant
• Less cost effective • More cost effective
Tricyclic antidepressants
Mechanism of action
• Inhibition of neurotransmitter reuptake
Nor epinephrine and serotonin
• Blocking of receptors
Antagonist at
1. serotonergic
2. Adrenergic
3. Histaminic
4. Muscuranic receptors
Therapeutic uses
• Moderate to severe depression
• Panic disorders.
• Migraine
• Bipolar affective disorder and phobic disorder.
• Pediatric enuresis (Imipramine). Imp use
Adverse effects
Mnemonic (TCAs)
• T.tachycardia
• C. Cardiac effects inc QT interval
And arrythmias
• A. Anticholinergic
• S. Sexual dysfunction , sedation
Monoamine oxidase Inhibitors
Mechanism of action
Therapeutic uses
• Last line drugs for treatment of depression.
Pharmacokinetics
• Well absorbed orally
• Hepatically metabolized
• Excreted in urine
Adverse effects
Mnemonic (HAHA)
• Hypotension
• Anticholinergic side effects
• Hypertensive crises ( avoid tyramine )
• Anxiety, agitation, anorexia
Important drug
interactions of MAOls
Adverse effects
Important drug interactions of MAOls
• Why MAOls are not used along with tyramine
containing foods?
As tyramine causes release of large amount
of catecholamines from nerve terminals
resulting in hypertensive crises
Hypertensive crises signs
Atypical antidepressants
• Bupropion
• Mirtazapine
• Nefazodone
• Trazodone
• Vilazodone
• Vortioxetine
Bupropion
• Important use :
• Useful for decreasing the cravings and
cessation of smoking.( mcq)
• It does not causes sexual dysfunction as
serotonin is not involved.
• Bupropion is a weak dopamine and
norepinephrine reuptake inhibitor.
Adverse effects
• Seizures
• CNS activating effects.
Contraindications
• In bulimia
• Anorexia Nervosa
Mirtazapine
• Block 5 HT2 and 5HT3 receptor inhibit H1
receptor.
Uses:
• Atypical antidepressant can be used as 1st line
agent to treat depression.
Adverse effects
• Sedation
• Weight gain
• Doesn’t causes sexual dysfunction.
Trazodone
• Antagonist 5 HT receptors and inhibit 5 HT reuptake.
Adverse effects
Due to alpha 1 receptor
• Priapism
• Orthostatic hypotension
Others
• Sedation
• Antihistamine
• Sexual dysfunction
• Can cause serotonin syndrome ( imp)
