Antidepressants fluoxetine

Recently, with the development of more advanced and sensitive analytical methods, studies on the fate of pharmaceuticals in WWTP have taken into account the analysis of pharmaceuticals sorbed into sludge (Table 4, and references therein). The antiseptics triclocarban and triclosan and the antibiotic ofloxacin have been reported in sludge at concentrations up to 441, 133, and 58 mg kgdw-1, respectively. Compounds such as the anti-inflammatory ibuprofen, the antiepileptic carbamazepine and the antidepressant fluoxetine have also frequently been reported though at lower levels (11,6 and 3 mg kgdw 1, respectively), whereas the (3-blockers were found at low... 

The most effective treatment for cataplexy is the tricyclic antidepressants, fluoxetine, or venlafaxine. Imipramine, protriptyline, clomipramine, fluoxetine, and nortriptyline are effective in about 80% of patients. 

Decreased cigarette consumption in smokers, easier to stop smoking Exaggerated response to warfarin and phenytoin Increased efficacy of omeprazole, increased toxicity of mephenytoin Absence of codeine efficacy, no effect of encainide, increased levels of tricyclic antidepressants, fluoxetine, phenothiazines Sustained paralysis to succinylcholine, possible increased toxicity of cocaine Unknown... 

FIGURE 2—22. If an inhibitor of the transport carrier binds to its own binding site, it prevents neurotransmitter molecules from being able to bind to their sites. This figure shows an antidepressant, fluoxetine (Prozac), binding to the serotonin transporter. When this drug binds to the serotonin transporter, it essentially bumps serotonin neurotransmitter molecules out of their seats on the transport carrier. This causes inhibition or blockade of neurotransmitter transport into the neuron. Sodium binding is also decreased, and the tires go flat, so that transport is halted. 

FIGURE 2-24. Shown here is how the antidepressant fluoxetine (Prozac) disrupts neurotransmitter from shuttling into the neuron. In this case, binding of the transport carrier by fluoxetine prevents serotonin neurotransmitter molecules from taking a seat on the shuttle. Thus, there is no ride for the serotonin into the neuron. This means that the neurotransmitter serotonin remains in the synapse until it diffuses away or is destroyed by enzymes. 

FIGURE 6—18. The antidepressants fluoxetine, fluvoxamine, and nefazodone are all inhibitors of CYP450 3A4. More potent inhibitors of this enzyme include the nonpsychotropic drugs ketoconazole, erythromycin, and protease inhibitors. If a 3A4 inhibitor is given with cisapride or astemazole, levels of these substrates can rise to toxic levels. Thus, fluoxetine, fluvoxamine, and nefazodone cannot be given with cisapride or astemazole. 

Anabolic steroids, antidepressants and drugs of abuse affect libido, potency, and ejaculatory function. Anabolic steroids are derivatives of testosterone, and have strong genitotropic effects. There is published evidence indicating that anabolic steroids increases sexual desire however, the frequency of erectile dysfunction is also increased. Treatment with the antidepressant fluoxetine has been associated with sexual side effects including delayed or nonexistent ejaculation and hyposexuality. Mice treated in utero with the anideukemic agent 5-aza-2/-deoxycytidine exhibit abnormal reproductive behavior and low reproductive capacity. 

Orsulak, P. J., Kenney, J. T., Debus, J. R., Crowley, G., Wittman, P. D. Determination of the Antidepressant Fluoxetine and Its Metabolite Norfluoxetine in Serum by Reversed-Phase HPLC, with Ultraviolet Detection. Clin. Chem. 1988, 34, 1875-1878. 

Tricyclic antidepressants + fluoxetine, paroxetine or sertraline —> increased pharmacological and toxicological effects of the tricyclic due to decreased hepatic metabolism. This is a potentially hazardous combination. 

Riad M, Zimmer L, Rbah L, Watkins KC, Hamon M, Descarries L. Acute treatment with the antidepressant fluoxetine internalizes 5-HT1A autoreceptors and reduces the in vivo binding of the PET radioligand [18]MPPF in the nucleus raphe dorsalis of rat. J Neurosci 2004 24 5420-5426. 

Besides the production of (R)-l-phenylethanol as a fragrance,198 various pharmaceutically important chiral compounds have been produced at various lab scales by asymmetric hydrogenation with JST catalysts. These compounds include a P1-receptor antagonist denopamine hydrochloride (149),191 antidepressant fluoxetine hydrochloride (150),191 antipsychotic BMS 181100 (151),191 serotonin and norepinephrine inhibitor duloxetine (129),164 antihistaminic and anticholinergic orphenadrine (152),192 and antihistaminic neobenodine (153).192... 

Therapeutic uses The primary indication for fluoxetine is depression, where it is as effective as the tricyclic antidepressants. Fluoxetine is effective in treating bulimia nervosa and obsessive-compulsive disorder. The drug has been used for a variety of other indications, including anorexia nervosa, panic disorder, pain associated with diabetic neuropathy, and for premenstrual syndrome. 

In an in vitro study of midazolam biotransformation using human liver microsomes, midazolam metabolism was competitively inhibited by the antifungal azoles keto-conazole, itraconazole, and fluconazole, and the antidepressant fluoxetine and its metabolite norfluoxetine (55). The degree of inhibition was consistent with the inhibition reported in pharmacokinetic studies, and suggests that in vitro assay is useful for predicting significant interactions. 

ZOLPIDEM ANTIDEPRESSANTS-FLUOXETINE, PAROXETINE, SERTRALINE, VENLAFAXINE Cases of agitation hallucinations Uncertain Avoid co-administration... 

BUPROPION 1. ANTICANCER DRUGS - thiotepa 2. ANTIDEPRESSANTS-fluoxetine, fluvoxamine, paroxetine, sertraline 3. ANTIVIRALS - efavirenz, protease inhibitors t plasma concentrations of bupropion and risk of adverse effects Inhibition of CYP2B6 Warn patients about adverse effects and use alternatives when possible. Avoid co-administration of bupropion with protease inhibitors. Co-adminis-ter efavirenz and bupropion with caution. A retrospective study showed that two patients received a combination without reported adverse effects. Potential T risk of seizures... 

IMATINIB 1. ANTIARRHYTHMICS -flecainide, mexiletine, propafenone 2. ANTIDEPRESSANTS - fluoxetine, paroxetine, TCAs, trazodone, venlafaxine 3. ANTIPSYCHOTICS -clozapine, haloperidol, perphenazine, risperidone, thioridazine 4. BETA-BLOCKERS - metoprolol, propanolol, timolol 5. DONEPEZIL 6. METHAMPHETAMINE Imatinib may cause t plasma concentrations of these drugs, with a risk of toxic effects Inhibition of CYP2D6-mediated metabolism of these drugs Watch for early features of toxicity of these drugs... 

Examples of simple organic compounds—methane, a component in natural gas ethanol, the alcohol in beer and wine and trichloroflouromethane, a refrigerant and aerosol propellant implicated in ozone destruction Some complex organic compounds that are useful dmgs—the antibiotic amoxicillin, the antidepressant fluoxetine (Prozac), and AZT, a drug used to treat HTV... 

How differences in the three-dimensional structure of starch and cellulose affect their shape and function (Section 5.1) The three-dimensional structure of thalidomide, the anti-nausea dmg that caused catastrophic birth defects (Section 5.5) How mirror image isomers can have drastically different properties— the analgesic ibuprofen, the antidepressant fluoxetine, and the anti-inflammatory agent naproxen (Section 5.13)... 

Childs et al. formulated crystalline complexes with a salt form of an API with carboxylic acids. The antidepressant, fluoxetine hydrochloride, was cocrystallized with benzoic acid, succinic acid, and fumaric acid where the chloride ion acts as a hydrogen bond acceptor for the carboxylic acid groups of the three ligands. Intrinsic dissolution studies were carried out at 10°C because at 25°C, the rates were so rapid that the dissolution rates of the cocrystals could not be distinguished from one another. The fumaric acid 2 1 complex had a similar dissolution rate to that of the crystalline fluoxetine hydrochloride, but the dissolution rate for the benzoic acid 1 1 complex was half that of fluoxetine hydrochloride. Fluoxetine hydrochloride succinic acid 2 1 complex had approximately three times higher dissolution rate, but the dissolution was so fast that an accurate value was difficult to measure. ... 

Because this group as a whole engages in frequent suicidal acting out, it is advisable to treat borderline patients with medications that have been found to have a low degree of toxicity when taken in overdose. These include antipsychotics and the following antidepressants fluoxetine, paroxetine, bupropion (note above caution), trazodone, and sertraline. Most other antidepressants are quite toxic when taken in overdose. 

High suicide risk Less toxic antidepressants (fluoxetine, trazodone, paroxetine, sertraline, bupropion, venlafaxine, nefazodone)... 

The Antidepressants Fluoxetine, Idazoxan and Phenelzine Alter Corticotropin-Releasing Hormone and Tyrosine Hydroxylase mRNA levels in Rat Brain Therapeutic Implications. Brain Res 1992 527 117-125. 

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