Selective serotonin and norepinephrine reuptake inhibitor

DUAL SELECTIVE SEROTONIN AND NOREPINEPHRINE REUPTAKE INHIBITORS (SSNRIs)... 

Side effects, mainly due to serotonin reuptake inhibition include G1 upset, nervousness, and sexual dysfunction. SSRls are associated with an increased risk of falls. Hyponatraemia due to SIADH is an uncommon, but important side effect in elderly patients. Selective serotonin and norepinephrine reuptake inhibitors (S SNRls) such as venlafaxine and duloxetine are also useful in older patients. Other heterocyclic antidepressants of importance in older patients because of relative safety include bupro-prion and mirtazepine. They are reserved for patients with resistance to or intolerance of SSRls. Currently, trazodone is used mostly for sleep disturbance in depression in doses of 50-100 mg at bedtime. The monoamine oxidase inhibitors phenelzine. 

Post-2000 Renal rhabdomyolysis with the statin, cerivastin cardio-toxicity with the COX-2 inhibitor, rofecoxib and liver damage with the selective serotonin and norepinephrine reuptake inhibitor, atomoxetine. 

Venlafaxine is one of the first selective serotonin and norepinephrine reuptake inhibitors developed for the treatment of depression. It was originally released in the United States in 1994. 

Thiophene seems to be very popular in Li Lilly drugs. Its dual selective serotonin and norepinephrine reuptake inhibitor (SSNRI) for depression, duloxetine (Cymbalta), contains a thiophene. And its atypical antipsychotic drug olanzapine (Zyprexa) has a fused thiophene as its core structure. 

Duloxetine is a selective serotonin and norepinephrine reuptake inhibitor (SNRI). Duloxetine is available as delayed-release capsules for oral route. 

Asymmetric synthesis is also common. Another technique is kinetic resolution. Kinetic resolution relies upon a difference in reactivity between the two enantiomers. For example this technique can be used in the synthesis of duloxetine. Duloxetine is marketed as the hydrochloride salt under the tradename Cymbalta as an antidepressant. It is a selective serotonin and norepinephrine reuptake inhibitor. It is the S enantiomer which is used. 

MAOI, monoamine oxidase inhibitor SARI, serotonin antagonist and reuptake inhibitor SNRI, serotonin and norepinephrine reuptake inhibitor SSRI, selective serotonin reuptake inhibitor TCA, tricyclic antidepressant. 

Two classes of antidepressants act as combined serotonin and norepinephrine reuptake inhibitors selective serotonin-norepinephrine reuptake inhibitors (SNRIs) and tricyclic antidepressants (TCAs). 

The selective serotonin reuptake inhibitors (SSRIs) are the first-line treatment of depression in the elderly. Compared with tricyciic antidepressants (TCAs), they are much safer in overdose and, for the most part, their side-effects are better tolerated. The antidepressants that have been shown, in controlled studies, to be effective in geriatric major depression are the SSRIs fluoxetine, paroxetine, and sertraline, the TCAs clomipramine and nortriptyline, and the serotonin and norepinephrine reuptake inhibitor (SNRi) venlafaxine. Given that most antidepressants are effective in the elderly, the choice of drug is based on its side-effect profile and its potential to interact with other medications. 

One of the main issues related to tramadol is the fact that it blocks serotonin reuptake and may cause serotonin syndrome in susceptible patients. Serotonin syndrome is characterized by neurological and cardiovascular stimulation, and can lead to seizures and death. Risks of developing serotonin syndrome are increased in patients treated with selective serotonin reuptake inhibitors and serotonin and norepinephrine reuptake inhibitors. 

The serotonin and norepinephrine reuptake inhibitors, or SNRIs, have both serotonin and norepinephrine inhibition, and are less selective than the SSRls. They also have nausea as a common adverse event on initiation, and can have dizziness, drowsiness, sweating, and dry mouth, as well as sexual dysfunction, as occur with the SSRI and have been associated with serotonin syndrome. 

Traditionally, benzodiazepines and tricyclic antidepressants (TCAs) have been the most prescribed drug treatments for GAD. However, selective serotonin reuptake inhibitors (SSRIs), as well as selective serotonin and norepinephrine... 

Unit 6 Classical Antidepressants, Serotonin Selective Reuptake Inhibitors and Norepinephrine Reuptake Inhibitors... 

The serotonin reuptake inhibitors have been shown to be uniquely effective for treating these disorders. Recent studies have focused on fluoxetine and other selective serotonin reuptake-inhibiting drugs, although clomipramine, a mixed serotonin and norepinephrine uptake inhibitor, may be more potent. Fluvoxamine is marketed exclusively for this disorder in the United States. 

Serotonin-norepinephrine reuptake inhibitors (SNRIs) (e.g. duloxetine, venlafaxine and desvenlafax-ine) inhibit the reuptake of both serotonin and norepinephrine and are referred to as dual inhibitors or selective serotonin norepinephrine inhibitors . The SNRIs lack of anticholinergic side effects results in a distinct advantage over traditional TCAs [13,77,78]. For example, duloxetine is a potent, balanced inhibitor of serotonin and norepinephrine reuptake [79]. Venlafaxine inhibits serotonin reuptake at lower dosages and inhibits both serotonin and norepinephrine reuptake at higher dosages [70,80]. 

Atomoxetine (Straterra , originally tomoxetine or tomoxetin, 3) was first described and synthesized by chemists at Eli Lilly in the late 1970s and was one of the few compounds that was known to display meaningful selectivity for the norepinephrine reuptake transporter (NET) versus the serotonin reuptake transporter (SERT) and the dopamine reuptake transporter (DAT) (Barnett, 1986 Molloy and Schmiegel, 1997). Atomoxetine was one of several structurally related and commercially successful monoamine reuptake inhibitors that were developed by Lilly for the treatment of various psychiatric disorders (Eig. 17.4). Fluoxetine (43) and duloxetine (44) have both gained approval in the United States as Prozac and Cymbalta , respectively, and nisoxetine (45) is widely used as a tool in biology. 

Disadvantages of the benzodiazepines include the risk of dependence, depression of central nervous system functions, and amnestic effects. In addition, the benzodiazepines exert additive central nervous system depression when administered with other drugs, including ethanol. The patient should be warned of this possibility to avoid impairment of performance of any task requiring mental alertness and motor coordination. In the treatment of generalized anxiety disorders and certain phobias, newer antidepressants, including selective serotonin reuptake inhibitors (SSRIs) and serotonin-norepinephrine reuptake inhibitors (SNRIs), are now considered by many authorities to be drugs of first choice (see Chapter 30). 

SELECTIVE SEROTONIN-NOREPINEPHRINE REUPTAKE INHIBITORS AND TRICYCLIC ANTIDEPRESSANTS... 

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