A Venlafaxine

White CM, Gailey RA, Levin GM, Smith T. Seizure resulting from a venlafaxine overdose. Ann Pharmacother 1997 31(2) 178-80. 

Michael A. Venlafaxine-induced painful ejaculation. Br J Psychiatry 2000 177 282. 

This scheme was also used for the synthesis of a venlafaxine analogue containing a four-membered silacycle instead of a six-membered ring but Si-C bond cleavage with silacyclobutane ring opening took place in the amination step (Scheme 4) (04OM4987). 

Pfeffer F, Grube M. An oi nic psychosis due to a venlafaxine-iropafenone interaction. IntJ Psychiatry Med (2001) 31,427-32. 

Kuloglu M, Ekinci O, Caykoylu A. Venlafaxine-associated nocturnal bruxism in a depressive patient successfully treated with buspirone. J Psychopharmacol 2010 24(4) 627-8. 

Venlafaxine (48) is a stmcturaHy novel phenylethylamine derivative that strongly inhibits both noradrenaline and serotonin reuptake. It lacks anticholinergic, antihistaminergic, and antiadrenergic side effects. As compared to placebo, most common adverse events are nausea, somnolence, dizziness, dry mouth, and sweating. Venlafaxine-treated patients also experienced more headaches and nausea, but less dry mouth, dizziness, and tremor than patients treated with comparator antidepressants. 

Antidepressants are used in the treatment of neuropathic pain and headache. They include the classic tricyclic compounds and are divided into nonselective nor-adrenaline/5-HT reuptake inhibitors (e.g., amitriptyline, imipramine, clomipramine, venlafaxine), preferential noradrenaline reuptake inhibitors (e.g., desipramine, nortriptyline) and selective 5-HT reuptake inhibitors (e.g., citalopram, paroxetine, fluoxetine). The reuptake block leads to a stimulation of endogenous monoaminer-gic pain inhibition in the spinal cord and brain. In addition, tricyclics have NMDA receptor antagonist, endogenous opioid enhancing, Na+ channel blocking, and K+ channel opening effects which can suppress peripheral and central sensitization. Block of cardiac ion channels by tricyclics can lead to life-threatening arrhythmias. The selective 5-HT transporter inhibitors have a different side effect profile and are safer in cases of overdose [3]. 

Indeed, 5-HT is also a substrate for the 5-HT transporter, itself an important player in the treatment of depression, and more recently for the whole range of anxiety disorders spectrum (GAD, OCD, social and other phobias, panic and post-traumatic stress disorders). It is the target for SSRIs (selective serotonin reuptake inhibitors) such as fluoxetine, paroxetine, fluvoxamine, and citalopram or the more recent dual reuptake inhibitors (for 5-HT and noradrenaline, also known as SNRIs) such as venlafaxine. Currently, there are efforts to develop triple uptake inhibitors (5-HT, NE, and DA). Further combinations are possible, e.g. SB-649915, a combined 5-HTia, 5-HT1b, 5-HT1d inhibitor/selective serotonin reuptake inhibitor (SSRI), is investigated for the treatment of major depressive disorder. 

The effects of buspirone are decreased when the drug is administered with fluoxetine Increased serum levels of buspirone occur if the drug is taken with erythromycin or itraconazole Should any of these combinations be required, the dosage of buspirone is decreased to 2.5 mg BID, and the patient is monitored closely. Venlafaxine blood levels increase with a risk of toxicity when administered witii MAOIs or cimetidine There is an increased risk of toxicity when trazodone is administered with the phenothiazines and decreased effectiveness of trazodone when it is administered with carbamazepine Increased serum digoxin levels have occurred when digoxin is administered with trazodone There is a risk for increased phenytoin levels when phenytoin is administered witii trazodone... 

MISCELLANEOUS ANTIDEPRESSANTS. An uncommon but potentially serious adverse reaction of trazodone is priapism (a persistent erection of die penis). If not treated within a few hours, priapism can result in impotence The nurse instructs the patient to report any prolonged or inappropriate penile erection. Use of the drug is discontinued immediately and the primary care provider notified. Injection of a-adrenergic stimulants (eg, norepinephrine) may be helpful in treating priapism. In some cases, surgical intervention may be required. Venlafaxine may cause an increase in die blood pressure. A sustained increase in die blood pressure may indicate that die dosage of venlafaxine needs to be decreased. 

C9H(,03 1076-38-6) see Acenocoumarol Ethyl biscoumacetate Tioclomarol Warfarin Zonisamide a-(l-hydroxycyclohexyl)-4-methoxybenzeneacetonitrile (C15H19NO2 93413-76-4) see Venlafaxine (45)-3-[[(lS,2R)-2-hydroxy-3-cyclopenten-l-yl]carbonyl]-... 

Antidepressants Desipramine, imipramine, sertraline, fluoxetine, paroxetine, venlafaxine, bupropion, nefazodone, mirtazapine, gepirone, amineptine Mixed findings suggest that better designed studies may find a niche for some of these drugs. Amineptine was effective for withdrawal symptoms. 

Preskorn A (1997). Pharmacotherapeutic profile of venlafaxine. Eur Psychiatry 2 (suppl. 4),... 

One of these compounds, venlafaxine (licensed in the UK in 1996), is regarded as an inhibitor of both 5-HT and noradrenaline reuptake but this is based on its actions in vitro. At low doses in vivo, it is a more potent inhibitor of 5-HT (Ki 39 nM) than noradrenaline reuptake (K 210 nM). Moreover, its active metabolite, O-demethylven-lafaxine, is a weaker inhibitor of NA reuptake, and has a longer half-life, than its parent compound. However, at high doses, venlafaxine inhibits reuptake of both these monoamines but has negligible activity at muscarinic, Hi-receptors or ai-adrenoceptors and... 

Venlafaxine, a serotonin-norepinephrine reuptake inhibitor (SNRI), alleviates anxiety in GAD patients with and without... 

Venlafaxine extended release, in doses of 75 to 225 mg/day, improves social anxiety, performance, and avoidance behavior with a reduction in disability.61 Treatment with venlafaxine results in response rates similar to those seen with paroxetine.60 Venlafaxine may be effective in SSRI non-responders.62 As with SSRIs, doses should be tapered slowly when discontinuing therapy. Tolerability is similar to that observed in depression trials with venlafaxine extended release. Common side effects are anorexia, dry mouth, nausea, insomnia, and sexual dysfunction. 

Peripheral neuropathy is the most common complication reported in type 2 DM. This complication generally presents as pain, tingling, or numbness in the extremities. The feet are affected more often than the hands and fingers. A number of treatment options have been tried with mixed success. Current options include pregabalin, gabapentin, low-dose tricyclic antidepressants, duloxetine, venlafaxine, topiramate, non-steroidal anti-inflammatory drugs, and topical capsaicin. 

A number of non-hormonal therapies have been studied for symptomatic management of vasomotor symptoms, including antidepressants [e.g., selective serotonin reuptake inhibitors (SSRIs) and venlafaxine], herbal products (e.g., soy, black cohosh, and dong quai), and a group of miscellaneous agents (e.g., gabapentin, clonidine, and megestrol). The choice of therapy depends on the patient s concomitant disease states, such as depression and hypertension, and the risk for potential adverse effects. 

SSRIs are theorized to reduce the frequency of hot flashes by increasing serotonin in the central nervous system and by decreasing LH. Of the SSRIs, citalopram, paroxetine, and sertraline all have been studied and have demonstrated a reduction in hot flashes while treating other symptomatic complaints such as depression and anxiety.33 Venlafaxine, which blocks the reuptake of serotonin and norepinephrine, has demonstrated a reduction in hot flashes primarily in the oncology population.34 Overall, these antidepressant medications offer a reasonable option for women who are unwilling or cannot take hormonal therapies, particularly those who suffer from depression or anxiety. These agents should be prescribed at the lowest effective dose to treat symptoms and may be titrated based on individual response. 

Fukuda, T. et al. (2000). The impact of the CYP2D6 and CYP2C19 genotypes on venlafaxine pharmacokinetics in a Japanese population. Eur. J. Clin. Pharmacol, 56, 175-80. 

Stewart, Andrew A. Nierenberg, Michael E. Thase, Louise Ritz, Melanie M. Biggs, Diane Warden, James F. Luther, Kathy Shores-Wilson, George Niederehe and Maurizio Fava, Bupropion-Sr, Sertraline, or Venlafaxine-Xr after Failure of SSRIs for Depression , New England Journal of Medicine 354 (2006b) 1231-42... 

In a recent open clinical trial, patients receiving venlafaxine XR or fluoxetine for six weeks without sleep improvement were randomly assigned to either mirtazapine (7.5 mg) or zolpidem (10 mg). Although both groups improved in terms of their sleep, the patients with either fluoxetine or venlafaxine had a more rapid... 

These types of antidepressant were introduced around 10 years after the SSRIs. They include the serotonin noradrenaline reuptake inhibitor venlafaxine and the selective noradrenaline reuptake inhibitor reboxetine. Although there are fewer data about these drugs, clinical experience has shown they are well tolerated and, unlike the SSRIs, they are only weak inhibitors of drug metabolism (Kent, 2000). Depression is a common psychiatric disorder seen in the elderly and often remains untreated or inadequately treated (Forsell and Fastbom, 2000). Venlafaxine was shown to improve the mood in a group of 36 older patients without any effect on cognitive function, an important consideration where there is the possibility of the coexistence of mild or undiagnosed dementia (Tsolaki et al., 2000). 

Tsolaki M, Fountoulakis KN, Nakopoulou E and Kazis A (2000). The effect of antidepressant pharmacotherapy with venlafaxine in geriatric depression. International Journal of Geriatric Psychopharmacology, 2, 83-85. 

Alternatives to estrogen for hot flushes are shown in Table 31-6. Progesterone alone may be an option in women with a history of breast cancer or venous thrombosis, but side effects limit their use. For women with contraindications to hormone therapy, selective serotonin reuptake inhibitors and venlafaxine are considered by some to be first-line therapy, but efficacy of venlafaxine beyond 12 weeks has not been shown. 

Selective serotonin reuptake inhibitors are considered to be less effective than TCAs for migraine prophylaxis and should not be considered first- or second-line therapy. However, they may be beneficial when depression is a significant contributor to headache. Preliminary data suggest a possible benefit with venlafaxine. 

A metaanalysis showed that SSRIs, TCAs, and CBT are similarly effective. Alprazolam, clonazepam, sertraline, paroxetine, and venlafaxine are... 

The serotonin-norepinephrine reuptake inhibitors include venlafaxine and duloxetine. Venlafaxine is an inhibitor of 5-HT and NE reuptake and a weak inhibitor of DA reuptake. Desvenlafaxine (Pristiq) was recently approved by the FDA. The dose is 50 mg once daily. 

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