The paper discusses fluoxetine critically: history, chemical structure, mode of action, use, possible adverse effects, and in general, how it has impacted the treatment of mental illness.
History and Evolution of Fluoxetine
It wasn’t until several decades after its discovery and invention that it was permitted its first FDA approval in 1987 for the disorder referred to as major depressive disorder, the most common disorder it was approved for. It was later sold commercially under other brand names, among them Prozac and Serafim.
It is the first drug within this class, now commonly termed selective serotonin reuptake inhibitors, or SSRIs.
These were landmark major histories in the world of antidepressive drugs. Such drugs only worked on serotonin; hence most side effects that had been attributed to the first-generation drugs such as TCAs and MAOIs became irrelevant. Due to that, it gained popularity so fast because it was less dangerous and well-tolerated compared to the older drugs.
Chemical Structure and Pharmacology of Fluoxetine
Fluoxetine is also a set of enantiomers consisting of two substances, R-fluoxetine and S-fluoxetine. Thus, the chemical properties that exist in fluoxetine are going to lead to selective activity upon serotonin transporters in the brain.
Nearly 100 % oral bio availability when administered orally, it gets mainly metabolised in the liver and then further formation of its active metabolite is better known as nor fluoxetine. Fluoxetine and nor fluoxetine have relatively long half-lives; half-life of fluoxetine lasts 2-4 days, while that of nor fluoxetine was approximately 7-15 days.
This would only allow slow onset of action and also increase retention in the system following discontinuation, thus may reduce withdrawal symptoms but poses dosing issues.It is a medicine like Ibuprofen.
Pharmacodynamics
Since it was presupposed to strengthen the effects of serotonin, it was intuitively considered that it would lift mood and help with symptoms of depression and anxiety.While the mechanism through which these drugs act to produce clinically
observed antidepressive effect is unknown, it has been considered that they act through serotonin activity for mood stabilization and other psychologic processes.
Indeed, it is selective for the transporter and augmentees serotonergic activity in the CNS; it is this which explains most of its activity as an antidepressant and anxiolytic; the serum level of serotonin has been correlated with good mood, low levels of anxiety, and overall well-being. The effects it exerts on pathways both of norepinephrine and dopamine are rather soft. These are much weaker and thus not clinically relevant. Such selectivity will minimize risks of side effects, which have hitherto accompanied the old drugs that worked on a few neurotransmitter systems.
Indications and Uses of Fluoxetine
Fluoxetine has been approved for many medicinal uses, and beside those, it has been used off-label for many more too.
Approved Uses
1. MDD: Therapy given that diminish symptoms of depression most notably by uninteresting in doing anything, feeling tired, the most commonly used drugs are fluoxetine, among others for similar reasons, such would have an excellent tolerated safety profile as well as efficacy rank them amongst the first line of treatments for the patients.
2. Bulimia Nervous: Bulimia nervous has been treated with only one FDA-approved antidepressant, that is Fluoxetine, and here, frequency of singeing and purging can be reduced in these patients.
3. Premenstrual Dysphoric Disorder (PM DD): Fluoxetine is also used as a medication for treatment of PM DD-the severe form of premenstrual syndrome. The drug reverses symptoms including mood swing, irritability, and aching in various parts of the body. Off-label use Besides the applications above that are approved by the FDA, fluoxetine also has application in managing other classes of disorders. Such as: It is used in a treatment of some symptoms of the posttraumatic stress disorder but still has no approval from the FDA for treating the disorder. It is sometimes used with social anxiety, though probably less effective than a few of the other SSRIs in that disorder.
4.Generalised Anxiety Disorder (GAD): Fluoxetine is sometimes used for GAD but an SSRI or SNRIs is prescribed much more often. This product is available in capsule, tablet, and oral solution. For instance, an administration in a case where the treatment of depression or OCD is in an adult-maintenance dosing would be 20 mg/day. Titration over weeks, possibly weeks-80mg is a common daily dose but in some patients, the physician may add more doses. Fluoxetine is one such medication given or prescribed to some women on specific days of their monthly cycles to assist in handling some of these conditions such as PMDD.
5. Side effects and risks of Fluoxetine: Every drug, fluoxetine included, has side effects. But again, as in most cases tolerance for many, many patients will suffer through slight and moderate up to very severe reactions with this drug.
Common General Adverse Events
The common general side effects are:
Vomiting: It tends to be common among patients in the initial stages of treatment.
Insomnia: Fluoxetine can cause the insomnia of the patient and later develop to one form of sleeping disorder in some patients. Dryness of mouth: Some patients experience dryness of mouth and they may have to increase the water intake.
Weight loss: Among the side effects is a change in weight, and for fluoxetine, it is changing in weight.
Sexual Dysfunction: Libido, retarded ejaculation and failure to ejaculate, among others are some of the sexual side effects most commonly associated with SSRIs.
Severe Adverse Reactions
The worse fluoxetine adverse effects are mild, and among the most serious ones include
Here’s Serotonin Syndrome: One of the most severely potentially dangerous side effects of elevated synaptic levels of serotonin in the brain, it is characterised by confusion, fever, and tachycardia.
Other conditions for which patients treated with fluoxetine and other SSRIs have been reported to have attempted or have committed suicide, even at the initiation of treatment.
This leads to hypothermia and subsequently grave sodium depletion especially among the elderly.
With this high half-life, however, the window for withdrawal is much smaller; but abrupt withdrawal may precipitate withdrawal symptoms in some patients who, if the drug is withdrawn abruptly, manifest in the form of mood changes, irritability, and dizziness.
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It may ultimately result in hyponatremia, which is also anticipated to be a side effect. Therefore, the fluoxetine dose of this medication should be titrated with utmost care and caution in the monitoring of the patient. Patients with Hepatic Impairment. Since it has been established already that fluoxetine is metabolized in the liver, those whose problems lie in the liver should be given low doses.
Fluoxetine Effects on Mental Health Treatment
Fluoxetine really opened the face of mental health treatment with a practicable alternative and with a less adverse effect profile compared to its elder peers. It’s coming was paired by the replacement of the long enacted medicinal approaches to depression and other mental health issues by change in view about drugs that relate to antidepressants. Prozac played an extremely highly influential role in such a reduction to the extent that more people began coming seeking treatment. This emergence made the present SSRI market from just an existence to the emergence of subsequent SSRIs that further fine-tuned the treatment option to various mental conditions.
Conclusion
With a heritage that has fundamentally altered the treatment of depression, and many other mental health conditions as well, Fluoxetine could perhaps be considered the Archstone of modern psychiatry. All of this has placed mill of patients around the world, with relative security and the availability and effectiveness use their product as a darling among themselves. Drugs that too are not free from danger and side effect but without these treatments cannot be deprived the chance of contributing significantly in treatments of mental and brain cases; it also defeated several obstacles between striving for help at time.
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