FLUOXETINE
FLUOXETINE
- First Selective Serotonin Reuptake Inhibitors (SSRI) drug introduced.
- Non-sedating antidepressant.
- Mode of action:
- Potent serotonin blocker.
- Inhibition of axonal uptake of 5HT by interacting with serotonin transporter (SERT).
PHARMACOKINETICS:
| Bioavailability | 60–80% |
|---|---|
| Protein binding | 94–95% |
| Metabolism | Liver (mostly CYP2D6-mediated) |
| Biological half-life | 1–3 days (acute) 4–6 days (chronic) |
| Excretion | Urine (80%), faeces (15%) |
USES:
- Major depressive disorder
- Obsessive-compulsive disorder (OCD).
- Used in only children older than 7 years.
- Post-traumatic stress disorder (PTSD)
- Bulimia nervosa,
- Panic disorder
- Premenstrual dysphoric disorder
- Trichotillomania.
- Cataplexy
- Obesity
- Alcohol dependence.
- Binge eating disorder.
- Autism spectrum disorders (moderate success in adults).
ADVERSE EFFECTS:
- Abnormal ejaculation,
- Anorexia
- Anxiety
- Asthenia
- Diarrhoea
- Dry mouth
- Dyspepsia
- Flu syndrome
- Impotence
- Decreased libido
- Nausea
- Nervousness
- Pharyngitis.
- Sinusitis.
- Somnolence.
- Sweating.
- Tremor.
- Vasodilatation.
- Fluoxetine is considered most stimulating SSRIs.
- Most prone to cause insomnia & agitation.
- Also most prone among SSRI’s, producing dermatologic reactions.
- E.g. Urticaria – hives, rash, itchiness, etc.
OVERDOSE:
Most frequent adverse effects during overdose include
Nervous system effects
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Gastrointestinal effects
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Other effects
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Exam Important
- Drug of choice for OCD is Fluoxetine
- Fluoxetine is a potent reuptake blocker of Serotonin
- In a patient with palpitations, breathlessness, sweating and a fear of impending death. Has one episode of such attacks every week. There are no identifiable triggers for the episodes. Fluoxetine is the Drug of choice.
- Loose stools – Common side effect of Fluoxetine therapy
- Non-sedating antidepressant is Fluoxetine
- Mode of action of fluoxetine Inhibition of axonal uptake of 5HT.
- Side effect of Fluoxetine is Weight gain, Anxiety, Sweating & Diarrhoea
- Drug of choice in depression in old person is Fluoxetine.
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