Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0012833 (dizziness)
 9,689 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Dapoxetine is a serotonin transporter inhibitor currently in development for the treatment of premature ejaculation. This randomized, 2-sequence, 2-treatment crossover study assessed the single- and multiple-dose pharmacokinetics of dapoxetine following once-daily administration of dapoxetine 30 mg and 60 mg to healthy male volunteers. Dapoxetine was rapidly absorbed following oral administration, with peak plasma concentrations reached approximately 1 hour after dosing; plasma concentrations after single doses of dapoxetine decreased rapidly to approximately 5% of peak concentrations by 24 hours. Elimination was biphasic, with an initial half-life of approximately 1.4 hours and a terminal half-life of approximately 20 hours. Dapoxetine showed time-invariant pharmacokinetics and dose proportionality between doses, and its pharmacokinetics was unaffected by multiple dosing. The pharmacokinetics of dapoxetine metabolites, desmethyldapoxetine and dapoxetine-N-oxide, was similarly unaffected by multiple dosing. There were no serious adverse events; the most commonly reported adverse events were diarrhea, dizziness, and nausea.
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PMID:Single- and multiple-dose pharmacokinetics of dapoxetine hydrochloride, a novel agent for the treatment of premature ejaculation. 1649 Aug 6

The tolerability of dapoxetine, a short-acting selective serotonin reuptake inhibitor being developed for premature ejaculation, was evaluated when coadministered with tamsulosin. Adult men on a stable dose of tamsulosin were randomized to also receive dapoxetine 30 or 60 mg, or placebo, in a crossover design. Supine and standing vital signs were measured on days 1 and 7. Plasma samples were collected for measurement of tamsulosin, dapoxetine, and dapoxetine metabolites. Coadministration of dapoxetine with tamsulosin did not alter orthostatic profiles or affect the incidence of orthostatic hypotension. Tamsulosin and dapoxetine pharmacokinetics were not altered. Adverse events were reported by 5.4%, 10.9%, and 23.2% of participants receiving tamsulosin with placebo, dapoxetine 30 mg, and dapoxetine 60 mg, respectively. The most common adverse events were diarrhea, dizziness, headache, and nausea. Therefore, dapoxetine had no clinically important effects on the pharmacokinetics or orthostatic profile of tamsulosin in men on a stable tamsulosin regimen.
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PMID:Effect of dapoxetine on the pharmacokinetics and hemodynamic effects of tamsulosin in men on a stable dose of tamsulosin. 1883 88

Premature ejaculation (PE) is a common problem in men worldwide. It has a significant impact on affected men and their partners in terms of self-esteem, dissatisfaction with their sexual relationships, personal distress, and interpersonal difficulty. Psychological therapies may achieve short-term improvements, but there are limited data on the long-term success of these methods. Oral therapy with long-acting selective serotonin reuptake inhibitors (SSRIs) improves intravaginal ejaculatory latency time (IELT), but these agents are designed to be administered daily and may be associated with unwanted sexual side effects and withdrawal symptoms upon abrupt discontinuation. Dapoxetine is a short-acting SSRI that can be taken as needed (prn) by men with PE. It has been studied in five separate multicenter, randomized, double-blind, placebo-controlled trials involving more than 6000 men with PE. In four studies that evaluated IELT as an endpoint (N = 4843), dapoxetine 30 and 60 mg prn achieved statistically significant increases in IELT versus placebo. Dapoxetine also showed statistically significant improvements in perceived control over ejaculation, PE-related personal distress, and other patient-reported outcomes in all five trials. Dapoxetine treatment is generally well-tolerated, with low incidences of discontinuation syndrome, sexual dysfunction, and treatment-emergent mood symptoms. The most common adverse events with dapoxetine included nausea, diarrhea, headache, dizziness, and somnolence.
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PMID:Emerging treatments for premature ejaculation: focus on dapoxetine. 1955 98

Premature ejaculation (PE) is a common male sexual disorder which is associated with substantial personal and interpersonal negative psychological consequences. Pharmacotherapy of PE with off-label antidepressant selective serotonin reuptake inhibitors (SSRIs) is common, effective and safe. Development and regulatory approval of drugs specifically for the treatment of PE will reduce reliance on off-label treatments and serve to fill an unmet treatment need. The objective of this article is to review evidence supporting the efficacy and safety of dapoxetine in the treatment of PE. MEDLINE, Web of Science, PICA, EMBASE and the proceedings of major international and regional scientific meetings were searched for publications or abstracts published during the period 1993-2012 that used the word 'dapoxetine' in the title, abstract or keywords. This search was then manually cross referenced for all papers. This review encompasses studies of dapoxetine pharmacokinetics, animal studies, human phase I, II and III studies, independent postmarketing and pharmacovigilance efficacy and safety studies and drug-interaction studies. Dapoxetine is a potent SSRI which is administered on demand 1-3 h prior to planned sexual contact. It is rapidly absorbed and eliminated, resulting in minimal accumulation, and has dose-proportional pharmacokinetics which are unaffected by multiple dosing. Dapoxetine 30 mg and 60 mg has been evaluated in five industry-sponsored randomized, double-blind, placebo-controlled studies in 6081 men aged at least 18 years. Outcome measures included stopwatch-measured intravaginal ejaculatory latency time (IELT), Premature Ejaculation Profile (PEP) inventory items, Clinical Global Impression of Change (CGIC) in PE, and adverse events. Mean IELT, all PEP items and CGIC improved significantly with both doses of dapoxetine versus placebo (all p <0.001). The most common treatment-related adverse effects included nausea (11.0% for 30 mg, 22.2% for 60 mg), dizziness (5.9% for 30 mg, 10.9% for 60 mg), and headache (5.6% for 30 mg, 8.8% for 60 mg), and evaluation of validated rated scales demonstrated no SSRI class-related effects with dapoxetine use. Dapoxetine, as the first drug developed for PE, is an effective and safe treatment for PE and represents a major advance in sexual medicine.
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PMID:Dapoxetine: a new option in the medical management of premature ejaculation. 2302 5

Premature ejaculation (PE) is a most common sexual dysfunction, for which dapoxetine, a novel selective serotonin (5-HT) re-uptake inhibitor (SSRI), is the only licensed oral medicine at present. With the advantages of fast absorption, rapid action, on-demand medication, and short half-life time, dapoxetine has been proved by clinical trials to be effective in prolonging the intravaginal ejaculation latency time (IELT) and improving the overall condition of PE patients in various areas and populations. Compared with the traditional SSRIs, dapoxetine has a better safety and tolerability. The most frequently reported dapoxetine-related adverse events include nausea, diarrhea, headache and dizziness, but with very few severe or serious cases.
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PMID:[Dapoxetine for premature ejaculation: Advances in clinical studies]. 2666 85

Male erectile dysfunction is common and frustrating after the age of forty years. Erectile dysfunction is a cause of misery, relationship difficulties, and significantly reduced quality of life. Sildenafil citrate (Viagra) has shown promising results in recently published clinical trials. Sildenafil is a potent and competitive inhibitor of cGMp specific phosphodiesterase-5, predominant isoenzyme in the human corpus cavernosum. It is effective in erectile dysfunction of diverse origin, however it requires a patent vascular system to be effective. It is not effective in patients with endocrinal impotence, loss of libido, premature ejaculation or infertility. Its main adverse effects are headache, flushing, dyspepsia, diarrhoea, nasal congestion, indigestion, visual disturbances, dizziness and rash. Ventricular tachycardia and acute myocardial infraction have been reported in patients of ischaemic heart disease after consumption of sildenafil. Six deaths have been reported in patients taking nitrates. In India it is likely to be prescribed by a primary care physician without complete evaluation of patient on complaint of impotence. Hence the ethical question of who should prescribe this drug should be addressed by medical fraternity and proper guidelines formulated to avoid misuse of sildenafil. Phosphodiesterase is distributed in nerve, central nervous system, and systemic vasculature, hence long-term effects of drug on these tissues has to be ascertained. It should be made mandatory to report all adverse drug reactions to ADR monitoring centres. It is a wonder for those who require it, but has potentially dangerous adverse effects and drug interactions and hence is and not a wonder pill for all kinds of impotence.
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PMID:VIAGRA : IS IT A WONDER DRUG ? 2736 78

The purpose of this analysis is to assess the efficacy and safety of phosphodiesterase-5 inhibitors (PDE5Is) for the treatment of premature ejaculation (PE). A comprehensive search was performed to ascertain from trials about PDE5Is for the treatment of PE and compare the results, including intravaginal ejaculatory latency time (IVELT), score of sexual satisfaction scale, and side effects, between the group treated with PDE5Is and that treated with placebo. Seven studies involving a total of 471 patients were included in this meta-analysis. This analysis showed that patients who were treated with PDE5Is had significantly increased IVELT (mean difference [MD] 2.60; 95% CI [1.85, 3.36]; p < .00001) and score of sexual satisfaction scale (MD 2.04; 95% CI [0.78, 3.30]; p = .002) compared with the group on placebo. More patients had side effects while taking PDE5Is, such as headache, dizziness, flushing, and nasal congestion. PDE5Is were significantly more effective than placebo in the treatment of PE. Side effects were more common among patients who were treated with PDE5Is.
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PMID:Phosphodiesterase-5 Inhibitors for Premature Ejaculation: Systematic Review and Meta-Analysis of Placebo-Controlled Trials. 3237 42