Valium

Diazepam is a member of the benzodiazepine family. Benzodiazepines are sedatives that cause dose-related depression of the central nervous system. They are useful in treating anxiety, insomnia, seizures, and muscle spasms.

Diazepam, marketed under brand names Valium, Stesolid, Diazemuls, Seduxen, Bosaurin, Diapam, Antenex, Ducene, Apozepam and Pax (South Africa) is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative, skeletal muscle relaxant and amnestic properties. This makes it a useful drug for treating anxiety, insomnia, seizures, alcohol withdrawal, and muscle spasms. It is also used before certain medical procedures (such as endoscopies) to reduce tension and anxiety, and in some surgical procedures to induce amnesia.

Diazepam is a core medicine in the World Health Organization’s “Essential Drugs List”, which is a list of minimum medical needs for a basic health care system. Diazepam is used to treat a wide range of conditions and has been one of (if not) the most frequently prescribed medications in the world for the past 40 years.

Diazepam was the second benzodiazepine to be invented by Leo Sternbach of Hoffmann-La Roche, and was approved for use in 1963. It is five times more potent than its predecessor, chlordiazepoxide, which it quickly surpassed in terms of sales. After this initial success, other pharmaceutical companies began to introduce other benzodiazepine derivatives.

The benzodiazepines gained popularity among medical professionals as an improvement upon barbiturates, which have a comparatively narrow therapeutic index, and are far more sedating at therapeutic doses. The benzodiazepines are also far less dangerous; death rarely results from diazepam overdose, except in cases where it is consumed with large amounts of other depressants (such as alcohol or other sedatives).

Diazepam was the top-selling pharmaceutical in the United States from 1969 to 1982, with peak sales in 1978 of 2.3 billion pills. While psychiatrists continue to prescribe diazepam for the short-term relief of anxiety, neurology has taken the lead in prescribing diazepam for the palliative treatment of certain types of epilepsy and spastic activity, e.g., forms of paresis. It is also the first line of defense for a rare disorder called stiff-person syndrome.

Diazepam is also found in nature. Several plants, such as potato and wheat, contain trace amounts of naturally occurring diazepam and other benzodiazepines.

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Imovane

Zopiclone is a non-benzodiazepine hypnotic agent, with marked sedative effects. Although unrelated chemically to the benzodiazepines, it produces similar pharmacological effects.

Zopiclone (pronounced IPA: sold as Imovane and Zimovane in Europe, and as the eszopiclone analogue Lunesta in North America, is a novel hypnotic agent used in the treatment of insomnia. Zopiclone is also available world wide under various other trade names. It was first developed by Sepracor and introduced in 1988 by Rho^ne-Poulenc S.A., now part of Sanofi-Aventis, the main worldwide manufacturer of the drug. Zopiclone is a controlled substance in the United States, Canada and some European countries and may be illegal to possess without a prescription.

While it acts on the BZ^(1) receptor and is a short-acting hypnotic agent, it is not a benzodiazepine (with which it shares a number of characteristics and effects), but a cyclopyrrolone derivative, belonging to a novel chemical class which is structurally unrelated to existing hypnotics.

On April 4, 2005, the United States DEA listed zopiclone under Schedule IV, due to some evidence that the drug has addictive properties similar to benzodiazepines.

Zopiclone, as traditionally sold worldwide, is a racemic mixture of two stereoisomers, only one of which is active. In 2005, the pharmaceutical company Sepracor, of Marlborough, Massachusetts, began marketing the active stereoisomer eszopiclone under the name Lunesta in the United States. This had the consequence of placing what is a generic drug in most of the world under patent control in the United States, although in that country, it is expected to be available in generic form by the year 2010. It is already available off-patent in a number of European countries as well as Brazil. The eszopiclone/zopiclone difference is in the dosage—the strongest eszopiclone derivative dosage contains 3mg of the therapeutic stereoisomer, whereas, the highest zopiclone dosage (7.5mg) contains 3.75mg of the active stereoisomer. The two agents have not been studied via head-to-head clinical trials to determine if any clinical differences exist (e.g., efficacy, side-effects, developing dependence on the drug, and safety, etc.).

Zopiclone is known colloquially as a “Z drug”, Other Z drugs include zaleplon (Sonata) and zolpidem (Ambien and AmbienCR) and were thought in initial studies to be less addictive and less habit forming than benzodiazepines. This appraisal has shifted somewhat in the last few years, as cases of addiction and habituation have been presented. It is recommended that zopiclone is taken on a “when required” basis, and daily or continuous use of the drug is not usually advised.

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Wellbutrin SR

Bupropion is an antidepressant medication that affects chemicals within the brain that nerves use to send messages to each other. These chemical messengers are called neurotransmitters. The neurotransmitters that are released by nerves are taken up…

Bupropion (INN; also amfebutamone, brand names Wellbutrin, Zyban, Budeprion and Buproban) is an atypical antidepressant, which acts as a dopamine reuptake inhibitor, and a nicotinic antagonist. Bupropion belongs to the chemical class of aminoketones and is similar in structure to stimulant cathinone, anorectic diethylpropion and to phenethylamines in general. Bupropion is primarily used as an antidepressant and as a smoking cessation aid. In 2006 it was the fourth most prescribed antidepressant on the U.S. retail market with 21,141,000 prescriptions.

Bupropion was first synthesized by Burroughs Research in 1966, and patented by Burroughs-Wellcome (later Glaxo-Wellcome, and, as of 2000, GlaxoSmithKline) in 1974. It was approved by the Food and Drug Administration (FDA) as an antidepressant in 1984 and marketed under the name Wellbutrin. However, a significant incidence of seizures at the originally recommended dosage (400-600 mg) caused in 1986 the removal of the drug from the market. It was shown that the risk of seizures increases from 0.1% at 100-300 mg/day to 0.3-0.4% at 450 mg/day to 2% at 600 mg/day. Reflecting this experience, bupropion was re-introduced to the market in 1989 with the maximum dose of 450 mg/day.

In 1996 the FDA approved sustained-release (SR) and in 2003 extended release (XL) formulations of Wellbutrin that release bupropion at a slower rate. Wellbutrin SR is taken twice a day and Wellbutrin XL once a day, as compared to three times a day for the immediate release bupropion. Wellbutrin SR and XL are now available in generic form. In 1997, bupropion was approved by the FDA for use as a smoking cessation aid under the name Zyban. In late 2006, Wellbutrin XL was approved for use by the FDA as treatment for seasonal affective disorder.

In the UK, bupropion was approved in 2000 as a smoking cessation aid, and has not been approved for the treatment of depression.

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Xanax

Diazepam is a member of the benzodiazepine family. Benzodiazepines are sedatives that cause dose-related depression of the central nervous system. They are useful in treating anxiety, insomnia, seizures, and muscle spasms.

Alprazolam is a short-acting drug in the benzodiazepine class used to treat anxiety disorders and as an adjunctive treatment for depression. It is also used as a medication to aid the beginning of treatment with SSRI type drugs, since these can cause anxiety in the initial stages of use.

Alprazolam is a triazolobenzodiazepine, that is, a benzodiazepine with a triazolo-ring attached to its structure. Benzodiazepines produce a variety of effects by modulating the GABAA subtype of the GABA receptor, the most prolific inhibitory receptor within the brain. The GABAA receptor is made up from 5 subunits out of a possible 19, and GABAA receptors made up of different combinations of subunits have different properties, different locations within the brain and importantly, different activities in regards to benzodiazepines.

In order for GABAA receptors to be sensitive to the action of benzodiazepines they need to contain an ? and a ? subunit, where the benzodiazepine binds. Once bound, the benzodiazepine locks the GABAA receptor into a conformation where the neurotransmitter GABA has much higher affinity for the GABAA receptor, increasing the frequency of opening of the associated Chloride ion channel and hyperpolarising the membrane. This potentiates the inhibitory effect of the available GABA leading to sedatory and anxiolytic effects. As mentioned, different benzodiazepines can have different affinities for GABAA receptors made up of different collection of subunits. For instance, benzodiazepines with high activity at the ?1 are associated with sedation whereas those with higher affinity for GABAA receptors containing ?2 and/or ?3 subunits have greater anxiolytic activity.

The binding site for benzodiazepines is distinct from the binding site for barbiturates and GABA on the GABA receptor.

There is some evidence for antidepressant treatment of major depression in out patient settings, evidence for inpatients is lacking [2]; other benzodiazepines are not known to have antidepressant activity.

Availability

Alprazolam is generally sold in generic form in Italy and the United States. It is also sold under many other brand names, depending on the country:

* Aceprax® - Uruguay
* Afobam® - Poland
* Alplax® - Argentina
* Alpralid® - Israel
* Alpravecs® - Italy
* Alprax® - India
* Alprazig® - Italy
* Alprox® - Finland
* Altrox® - Philippines
* Alviz® - Indonesia
* Alzolam® - India, Malaysia
* Apo-Alpraz® - Canada (also made by other companies under different names)
* Apraz® - Brazil
* Azor® - South Africa
* Calmax® - Ireland
* Constan® - Japan
* Dormonoct® - Portugal
* Farmapram® - Mexico
* Frontal® - Brazil, Italy
* Frontal XR® - (an extended release formulation) Brazil
* Frontin® - Hungary, Slovak Republic, Czech Republic
* Helex® - Croatia, Slovenia
* Jialeding® (???)- China
* Kalma® - Australia
* Kinax® (???) - Taiwan
* Ksalol® - Serbia
* Manorest® - Sri Lanka
* Mialin® - Italy
* Misar® - Croatia
* Neurol® - Czech Republic, Slovak Republic
* Niravam® - (formulation that dissolves on the tongue) United States
* Paxal® - Iceland
* Ralozam® - Australia
* Restyl® - Bahrain, Cyprus, Egypt, India, Iran, Iraq, Jordan, Kuwait, Lebanon, Libya, Oman, Qatar, Republic of Yemen, Saudi Arabia, Syria, United Arab Emirates
* Sedipral® - Paraguay
* Solanax® - Japan
* Tafil® - Austria, Costa Rica, Germany, Mexico, Portugal, Switzerland, Venezuela
* Trankimazin® - Spain
* Xanax XR® - (an extended release formulation) Israel [3], United States, Portugal
* Xanax® - Australia, Belgium, Bulgaria, Croatia, France, Germany, Greece, Hungary, Ireland, Italy, Netherlands, New Zealand, Pakistan, Poland, Portugal, Romania, Serbia, Singapore, Slovak Republic, Switzerland, Turkey, United Kingdom, United States
* Xanor® - Austria, Finland, Norway, Philippines, South Africa, Sweden
* Xanor SR® - (slow release) South Africa
* Zamhexal® - Australia
* Zolarem® - Bahrain, Benin, Burkina-Faso, Cyprus, Egypt, Ethiopia, Gambia, Ghana, Guinea, Iran, Iraq, Israel, Ivory Coast, Jordan, Kenya, Kuwait, Lebanon, Liberia, Libya, Malawi, Mali, Mauritania, Mauritius, Morocco, Niger, Nigeria, Oman, Qatar, Republic of Yemen, Saudi Arabia, Senegal, Seychelles, Sierra-Leone, South Africa, Sudan, Syria, Tanzania, Tunisia, Uganda, United Arab Emirates, Zambia, Zimbabwe
* Zoldac® - Benin, Burkina-Faso, Ethiopia, Gambia, Ghana, Guinea, India, Ivory Coast, Kenya, Liberia, Malawi, Mali, Mauritania, Mauritius, Morocco, Niger, Nigeria, Senegal, Seychelles, Sierra-Leone, South Africa, Sudan, Tanzania, Tunia, Uganda, Zambia, Zimbabwe
* Zomiren® - Poland

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Geodon

Geodon is used to treat severe mental disorders.

Ziprasidone (marketed as Geodon, Zeldox) was the fifth atypical antipsychotic to gain FDA approval (February 2001). Ziprasidone is Food and Drug Administration (FDA) approved for the treatment of schizophrenia, and the intramuscular injection form of ziprasidone is approved for acute agitation in schizophrenic patients. Ziprasidone has also received approval for acute treatment of mania associated with bipolar disorder. The brand name Geodon has been suggested to bring to mind the phrase ‘down (don) to earth (geo)’ referring to the goals of the medication.

The oral form of ziprasidone is the hydrochloride salt, ziprasidone hydrochloride. The intramuscular form, on the other hand, is the mesylate salt, ziprasidone mesylate trihydrate, and is provided as a lyophilized powder.

Ziprasidone has a high affinity for dopamine, serotonin, and alpha-adrenergic receptors and a medium affinity for histaminic receptors. Ziprasidone is somewhat unique among the “atypicals” in that it also displays some inhibition of synaptic reuptake of serotonin and norepinephrine, although the clinical significance of this is unknown. The mechanism of action of ziprasidone is unknown. However it is theorized that its antipsychotic activity is mediated primarily by antagonism at dopamine receptors, specifically D2. Serotonin antagonism may also play a role in the effectiveness of ziprasidone, but the significance of 5-HT2A antagonism is debated among researchers. Antagonism at histaminic and alpha adrenergic receptors likely explains some of the side effects of ziprasidone, such as sedation and orthostasis.

The systemic bioavailability of ziprasidone administered intramuscularly is 100%, or 60%, administered orally with food. After a single dose intramuscular administration, the peak serum concentration typically occurs at about 60 minutes after the dose is administered, or earlier. Steady state plasma concentrations are achieved within one to three days. The mean half-life ranges from two to five hours. Exposure increases in a dose-related manner and following three days of intramuscular dosing, little accumulation is observed.

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Effexor

Trazodone is an oral antidepressant drug that affects the chemical messengers (neurotransmitters) within the brain that nerves use to communicate with (stimulate) each other. The major neurotransmitters are acetylcholine, norepinephrine, dopamine…

Venlafaxine hydrochloride (Effexor) is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class. It is prescribed for the treatment of clinical depression and anxiety disorders. Due to the side effects and suspicions that venlafaxine may cause suicide it is not recommended as a first line treatment. However, it is often effective for depression not responding to SSRI. Venlafaxine was first introduced by Wyeth in 1993. It is the sixth antidepressant based on the amount of retail prescriptions in the US (17.1 million).

Venlafaxine was shown to be effective for depression in multiple double blind studies. Venlafaxine is similar in efficacy to trazodone and tricyclic antidepressants amitriptiline (Elavil) and imipramine and it was better tolerated than amitriptiline. Venlafaxine appears to have efficacy similar or somewhat better than sertraline (Zoloft) and fluoxetine (Prozac) depending on the criteria and rating scales used. In particular, higher doses of venlafaxine are more effective, and more patients achieved remission or were “very much improved”. At the same time the efficacy was similar if the number of patients who achieved “response” or were “improved” was considered. A meta-analysis comparing venlafaxine and combined groups of SSRI or tricyclic antidepressants indicated superiority of venlafaxine. Based on the same set of criteria, venlafaxine was similar in efficacy to an atypical antidepressant bupropion (Wellbutrin); however, the remission rate was significantly lower for venlafaxine. Venlafaxine was also marginally inferior in efficacy to a newer SSRI escitalopram (Lexapro) and had twice higher frequency of the side effects, in particular, nausea, ejaculation disorder, somnolence and sweating.

Interestingly, a popular magazine Consumer Reports, which originally rated venlafaxine as the most effective among six commonly prescribed antidepressants, no longer recommends it. Fluoxetine, citalopram and bupropion have been chosen as Consumer Reports Best Buy drugs in the updated version of their guide.

As with most antidepressants, lack of sexual desire is a common side effect. Venlafaxine can raise blood pressure at high doses, so it is usually not the drug of choice for persons with hypertension.

It has a higher rate of treatment emergent mania than many modern antidepressants, and many people find it to be a more activating medication (one that increases energy or wakefulness) than other antidepressants.[citation needed] Paradoxically, some users find it highly sedating and find that it must be taken in the evening.

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Desyrel

Trazodone is an oral antidepressant drug that affects the chemical messengers (neurotransmitters) within the brain that nerves use to communicate with (stimulate) each other. The major neurotransmitters are acetylcholine, norepinephrine, dopamine…

Trazodone (trade names Desyrel, Molipaxin, Trittico, Thombran, Trialodine) is a psychoactive compound with sedative, anxiolytic, and antidepressant properties. The various manufacturers claim that the antidepressant activity becomes active in the first week of therapy. Trazodone has less prominent anticholinergic (dry mouth, constipation, tachycardia) and adrenolytic (hypotension, male sexual problems) side effects than most tricyclic antidepressants.

Although trazodone is often conceived to be a tricyclic antidepressant it belongs to the family of tetracyclic antidepressants.

Trazodone was originally discovered and developed in Italy in the 1960s by Angelini research laboratories as a second-generation antidepressant. This agent was developed according to the mental pain hypothesis, which was postulated from studying patients and which proposes that depression is associated with a decreased pain threshold. Trazodone was patented and marketed in many countries all over the world. It was approved by the FDA at the end of 1981.

Trazodone is a serotonin reuptake inhibitor and is also a 5-HT2 receptor antagonist. However, in contrast to the selective serotonin reuptake inhibitors such as fluoxetine (trade name Prozac), trazodone’s antidepressant effects may be due to its antagonistic effect at the 5-HT2 receptor site.

Trazodone is well absorbed after oral administration with mean peak blood levels obtained at approximately 1 hour after ingestion. Absorption is somewhat delayed and enhanced by food. The mean blood elimination half-life is biphasic: the first phase’s half-life is 3–6 hours, and the following phase’s half-life is 5–9 hours. The drug is extensively metabolized with 3 or 4 major metabolites having been identified in man, some of which such as mCPP may contribute to the side effect profile of trazodone. Approximately 70–75% of C14-labelled trazodone was found to be excreted in the urine within 72 hours (PMID 1037253). Trazodone is highly protein-bound.

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Ambien

Zolpidem belongs to a class of medicines that effects the central nervous system, called sedative hypnotics. Zolpidem is closely related to a family of drugs called benzodiazepines. These drugs cause sedation, muscle relaxation, act as anti-convulsan.

Zolpidem is a prescription short-acting nonbenzodiazepine hypnotic that potentiates gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter, by binding to gamma-aminobutyric acid receptors. Zolpidem is used for the short-term treatment of insomnia. It works quickly (usually within 15 minutes) and has a short half-life (2-3 hours). Some trade names of zolpidem are Ambien, Stilnox, Stilnoct, Hypnogen, Zolfresh,Nimadorm, Sanval, and Myslee. Its hypnotic effects are similar to those of the benzodiazepine class of drugs, but it is actually classified as an imidazopyridine. Flumazenil, which is used for benzodiazepine overdose, can also reverse zolpidem’s sedative/hypnotic effects. As an anticonvulsant and muscle relaxant, the beneficial effects start to emerge at 10 and 20 times the dose required for sedation, respectively. For that reason, it has never been approved for either muscle relaxation or seizure prevention. Such drastically increased doses are more inclined to induce one or more negative side effects, including hallucinations and/or amnesia.

The patent 4382938 in the United States on zolpidem was held by the German-French pharmaceutical corporation Sanofi-Aventis. On April 23, 2007 the US FDA approved 13 generic versions of zolpidem tartrate. Zolpidem is available from several generic manufacturers in the UK, as generic from Sandoz in South Africa, as well as from other manufacturers such as Ratiopharm.

Recently, zolpidem has been cited in various medical reports mainly in the United Kingdom as waking persistent vegetative state (PVS) patients, and dramatically improving the conditions of people with brain injuries.

Zolpidem is approved for the short-term (usually two to six weeks) treatment of insomnia, and it has been studied for nightly use up to six months in a single-blind trial published in 1991, an open-label study lasting 180 days published in 1992 (with continued efficacy in patients who had kept taking it as of 180 days after the end of the trial), and in an open-label trial lasting 179 days published in 1993.

The United States Air Force uses zolpidem, under trade name Ambien, as “no-go pills” to help pilots sleep after a mission; another drug used for the same purpose is temazepam (Restoril). (Cf. the “go-pills” amphetamine, served under the name Dexedrine, or its recent modafinil (Provigil) replacement, act as a stimulant for the same pilots, the effects of which are reversed by the aforementioned “no-go pills”)

Zolpidem is also used off-label to treat restless leg syndrome and, as is the case with many prescription sedative/hypnotic drugs, it is sometimes used by stimulant users to “come down” after the use of stimulants such as methamphetamine, cocaine, MDMA (ecstasy), or amphetamine.

Recently, the drug has been reported anecdotally to have positive effects for patients in persistent vegetative state. Results from phase IIa trials are expected in June 2007. The trials are being conducted by Regen Therapeutics of the UK, who have a patent pending on this new use for Zolpidem.

A clinical trial on a single patient performed at the Toulouse University Hospital using PET shows that zolpidem repeatably improves brain function and mobility of a patient immobilized by akinetic mutism caused by hypoxia

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Zoloft

Sertraline belongs to a class of drugs called selective serotonin reuptake inhibitors (SSRI). Other drugs in this class are Prozac (fluoxetine), Paxil (paroxetine), Celexa (citalopram) and Luvox (fluvoxamine). Serotonin is a neurotransmitter.

Sertraline hydrochloride (also labeled under numerous brand names: Zoloft, Sertralin, Lustral, Apo-Sertral, Asentra, Gladem, Serlift, Stimuloton, Xydep, Serlain, Concorz) is a popular orally administered antidepressant of the selective serotonin reuptake inhibitor (SSRI) type. It was first approved by the Food and Drug Administration (FDA) for use in the USA in 1991. It is approved for use in the UK by the National Institute for Health and Clinical Excellence.

Sertraline is manufactured by Pfizer and sold as Zoloft in the United States as small green 25 mg tablets, blue 50 mg tablets, and yellow 100 mg tablets (Generic 100 mg sertraline tablets are also yellow), each of which is scored to allow easy halving.

In the UK, the brand name is Lustral and is available in white 50 mg or 100 mg scored tablets, according to the British National Formulary (BNF). Elsewhere in the EU the brand name is Zoloft, available in white 50 mg or 100 mg scored tablets. In Australia, only the 50 mg and 100 mg strengths are available, both as white tablets.

Sertraline is an odorless, white, sparingly soluble crystalline solid. The minimum effective dose is usually 50 mg per day (it can be still effective at 25 mg or 37.5 mg), but lower doses may be used in the initial weeks of treatment to acclimatize the patient’s body, especially the liver, to the drug and to minimize the severity of any side effects. Patients who do not experience relief of symptoms at 50 mg a day may have their dose increased, up to 200 mg a day.

The patent for this brand-name drug expired in June 2006. The drug is now available in generic form in the United States. The generic version of the drug is being produced by Greenstone Ltd. (a Pfizer Inc. subsidiary) and Israeli drug maker Teva. In Scandinavia a generic drug called Sertralin, manufactured by HEXAL, is available. The price differences between Zoloft and Sertraline are as much as 1.50 U.S. dollars per pill.[citation needed] In India, this drug is sold under the name Zosert.

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Prozac

Fluoxetine is in a new class of antidepressant medications that affects chemical messengers within the brain. These chemical messengers are called neurotransmitters. Many experts believe that an imbalance in these neurotransmitters is the cause of de…

Prozac is a brand name for the antidepressant drug fluoxetine. Fluoxetine is approved for the treatment of depression (including pediatric depression), obsessive-compulsive disorder (in both adult and pediatric populations), bulimia nervosa, panic disorder and premenstrual dysphoric disorder. Other indications include hypochondriasis and body dysmorphic disorder.

Despite the availability of newer agents, it remains extremely popular. Over 21.7 million prescriptions for generic formulations of fluoxetine were filled in the United States in 2006 making it the third most prescribed antidepressant.

According to David Wong the work which eventually led to the discovery of fluoxetine began at Eli Lilly in 1970 as a collaboration between Bryan Molloy and Robert Rathburn.

It was known at that time that antihistamine diphenhydramine shows some antidepressant-like properties. 3-Phenoxy-3-phenylpropylamine, a compound structurally similar to diphenhydramine, was taken as a starting point, and Molloy synthesized dozens of its derivatives. Testing the physiological effects of these compounds in mice resulted in nizoxetine, a selective norepinephrine reuptake inhibitor currently widely used in biochemical experiments.

Later, hoping to find a derivative inhibiting only serotonin reuptake, Wong proposed to re-test the series for the in-vitro reuptake of serotonin, norepinephrine and dopamine. This test, carried out by Jong-Sir Horng in May 1972, showed the compound later named fluoxetine to be the most potent and selective inhibitor of serotonin reuptake of the series.

A controversy ensued after Lilly researchers published a paper entitled “Prozac (fluoxetine, Lilly 110140), the first selective serotonin uptake inhibitor and an antidepressant drug” implicitly claiming fluoxetine to be the first selective serotonin reuptake inhibitor (SSRI). Two years later they had to issue a correction, admitting that the first SSRI was zimelidine developed by Arvid Carlsson and colleagues. (However, unlike its successful cousin, zimelidine was banned worldwide because of serious side effects.) Fluoxetine was the third SSRI on the market. Fluvoxamine (Luvox) had been marketed in Europe since 1983. Fluoxetine made its appearance on the Belgium market in 1986 and was approved for use by the Food and Drug Administration (FDA) in the United States in December 1987.

The bioavailability of fluoxetine is relatively high (72%), and peak plasma concentrations are reached in 6 to 8 hours. It is highly bound to plasma proteins, mostly albumin.

Fluoxetine is metabolized in the liver by isoenzymes of the cytochrome P450 system, including CYP2D6. The role of CYP2D6 in the metabolism of fluoxetine may be clinically important, as there is great genetic variability in the function of this enzyme among people. Only one metabolite of fluoxetine, norfluoxetine (demethylated fluoxetine), is biologically active.

Fluoxetine is cleared slowly from the body; its elimination half-life ranges from 1 to 3 days—after a single dose—to 4 to 6 days (after long-term use) in healthy adults, and is prolonged in those with liver disease. The half-life of norfluoxetine is longer (16 days after long-term use). Complete excretion of the drug may take several weeks.

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