Treatment of Premature Ejaculation with Sertraline Hydrochloride

Total Page:16

File Type:pdf, Size:1020Kb

Treatment of Premature Ejaculation with Sertraline Hydrochloride International Journal of Impotence Research (1998) 10, 181±184 ß 1998 Stockton Press All rights reserved 0955-9930/98 $12.00 http://www.stockton-press.co.uk/ijir Treatment of premature ejaculation with sertraline hydrochloride CG McMahon St. Luke's Hospital Complex, Sydney, Australia Purpose: To evaluate the ef®cacy of sertraline hydrochloride in the drug treatment of premature ejaculation (P.E.). Materials and Method: Forty-six normally potent men, aged 22 to 63 years (mean 42 years) with premature ejaculation were treated with oral sertraline in a dose ranging study. All men were either married or in a stable relationship. The mean ejaculatory interval was 1 minute (range 0± 5 min). All men were started on Sertraline 25 mg daily and were increased to 50 mg after 3 weeks and 100 mg after a further 3 weeks. None of the men received any formal psychosexual therapy. Results: With a dose of 25 mg, the mean ejaculatory interval increased to 7.6 min (range 0±20 min). With a dose of 50 mg, the mean ejaculatory interval increased to 13.1 min (range 7 min± anejaculation) with 4 men experiencing anejaculation. With a dose of 100 mg, the mean ejaculatory interval increased to 16.4 min (range 7 min±anejaculation), 10 men experiencing anejaculation. With a dose of 25 mg, 1 man described transient dizziness. With a dose of 50 mg, 1 man described some drowsiness and anorexia and 1 man experienced minor dyspepsia. With a dose of 100 mg, 2 men described erectile dysfunction and reduced libido, 2 men described transient drowsiness and anorexia, 2 men experienced minor dyspepsia and 2 men described feelings of anxiety. Conclusion: Sertraline appears to be a useful agent in the pharmacological treatment of premature ejaculation. Keywords: premature ejaculation; sertraline; selective serotonin re-uptake inhibitors Introduction Although the `cornerstone' of treatment is short term directive sex therapy, premature ejaculation may also be treated pharmacologically with a variety Premature ejaculation (PE) is the most common of different medications. These medications either male sexual disorder, affecting perhaps as many as act centrally or locally to retard the psychoneurolo- 75% of men at some stage in their sexual lives. The gical control of ejaculation and subsequent orgasm. Diagnostic and Statistical Manual of Psychiatry It is well established that major tranquillisers such (DSM-IV) de®nes premature ejaculation as `ejacula- as the phenothiazine, thioridazine, will retard tion that occurs before the individual wishes ejaculation signi®cantly and will, in a signi®cant because of recurrent and persistent lack of reason- percentage of men result in failure to ejaculate.2 able voluntary control of ejaculation and orgasm Although these agents can be used to treat PE their during sexual activity ...'.1 ef®cacy is unfortunately counteracted by the high Premature ejaculation is invariably psychogenic incidence of adverse side effects including drowsi- and can be due to performance anxiety, fear or ness, tardive dyskinesia and other extrapyramidal psychological trauma. Men with premature ejacula- adverse effects. The antidepressant clomipramine is tion progress very rapidly from excitement to often associated with delayed or absent ejaculation orgasm which is often experienced as minimally with an incidence of up to 94%3,4 and has been pleasurable. They appear to have a hypersensitive reported as useful in the treatment of PE.5,6 ejaculatory re¯ex. The fact that anxiety plays a role The selective serotonin re-uptake inhibitors in this process however, is attested by the frequent (SSRIs) are primarily indicated in the treatment of situational nature of the problem and the almost depression and are often associated with a variety of universal experience of good ejaculatory control sexual adverse reactions including delayed ejacula- during solitary masturbation. tion. The side effect pro®le differs between different SSRIs, ¯uoxetine tending to effect ejaculation, orgasm and sexual desire, all of which are restored slowly after withdrawal of the drug, whereas sertra- Received 15 May 1997; revised=accepted 28 December 1997 line and paroxetine tend to affect ejaculation more. Treatment of premature ejaculation CG McMahon 182 This paper reports the results of a prospective Results open label dose ranging study of the ef®cacy of sertraline hydrochloride (Zoloft1, P®zer) in treat- ment of PE. The mean age of the 46 men studied was 42 y (range 22±63 y). The mean pre-treatment ejaculatory la- tency time was 1.0 min with a range of ejaculation occurring from during foreplay or at intromission to 5 min after intromission. The pre-treatment fre- Materials and methods quency of intercourse was 0.6 times=week. Thirty- six men (78%) had primary premature ejaculation, the remaining 10 men (22%) describing secondary Forty-six normally potent men, aged 22±63 y (mean premature ejaculation with previous acceptable 42 y) suffering from PE were enrolled in a prospec- ejaculatory control. Of the 36 men with primary tive dose ranging study to assess the ef®cacy and premature ejaculation, 6 men (17%) had severe tolerance of sertraline hydrochloride (Zoloft1) in the primary premature ejaculation and had never management of PE. All of the study group were achieved intravaginal ejaculation. heterosexual, had no other sexual disorders and In treatment phase 1 (25 mg sertraline=d), the were either married or in a stable relationship. mean ejaculatory latency time of the 46 enrolled Premature ejaculation was regarded as ejaculation men was 7.6 min (range 0±20 min). In treatment that occurred earlier than either the man or his phase 2 (50 mg sertraline=d) the mean ejaculatory partner wished. As no attempt was made to enrol latency time of the 46 enrolled men was 13.1 min men using accepted average ejaculatory latency time (range 7 min anejaculation). Four men were unable intervals, several men had ejaculatory latency inter- to ejaculate after prolonged intercourse with 50 mg vals that would be regarded as acceptable by normal sertraline=d and declined to enrol in treatment standards. Men with erectile dysfunction, reduced phase 3. In treatment phase 3 (100 mg sertraline=d) sexual desire, inhibited male orgasm, chronic the mean ejaculatory latency time of the 42 men psychiatric or physical illness, alcohol or substance enrolled was 16.4 min (range 7 min anejaculation). abuse and the use of psychotropic medication were Ten men were unable to ejaculate after prolonged excluded from the trial. Men were asked not to use intercourse with 100 mg sertraline=d (Table 1). The condoms, topical penile anaesthetic creams or mean pre-treatment ejaculatory latency time of the sprays. None of the men received any formal 14 men who experienced anejaculation was 1.9 min psychosexual counselling. (range 0±5 min). The study comprised three consecutive treatment The mean frequency of intercourse after three phases each separated by a three week washout weeks of treatment was 1.6 times=week in treatment period. In treatment phase I, men received 25 mg phase 1 (25 mg sertraline=d), 2.1 times=week in sertraline daily for three weeks. Following comple- treatment phase 2 (50 mg sertraline=d) and 2.2 tion of phase 1 and the subsequent drug washout times=week in treatment phase 3 (100 mg period, men were enrolled in treatment phase 2 and sertraline=d). The mean frequency of intercourse received 50 mg sertraline daily for a further three after three weeks of treatment was signi®cantly weeks. Following completion of phase 2 and the superior to the pre-treatment mean frequency with subsequent drug washout period, men were enrolled all doses of sertraline (p < 0.001). There was no in treatment phase 3 and received 100 mg sertraline statistical difference between the mean frequency of daily for the ®nal three weeks. intercourse with differing doses of sertraline. Men were supplied with an ejaculation diary and Intravaginal ejaculation was achieved for the ®rst were asked to record their frequency of coitus, time in each of the cohort of six men with severe quality of erection and orgasm, and to measure and primary premature ejaculation who had never record their ejaculatory latency time using a stop- achieved intravaginal ejaculation. Intravaginal ejac- watch. Men were required to attempt coitus on at ulation occurred in four of the six men with 25 mg least two occasions each week. Results were ana- sertraline=d and in all men with 50 mg and 100 mg lysed using standard statistical methods. sertraline=d. The mean age of this group of six men Table 1 Results of dose ranging study of sertraline hydrochloride (25, 50 and 100 mg) in the treatment of premature ejaculation Mean ejaculatory interval Ejaculatory interval range Dose (min) (min) Men with anejaculation Frequency of intercourse Pre-treatment 1.0 0±5 Ð 0.6 25 mg 7.6 0±20 0 1.6 50 mg 13.1 7±anejac. 4 2.1 100 mg 16.4 7±anejac. 10 2.2 Treatment of premature ejaculation CG McMahon 183 was 26.9 years (range 23±32 years). All men in this logical control of ejaculation and subsequent or- cohort were either married or were involved in a gasm. Animal studies have shown that the central long term stable relationship. One man in this cohort neurotransmitter serotonin has an inhibitory effect developed anejaculation with 100 mg sertraline=d. on sexual function, while dopamine is generally Sertraline was, in general, well tolerated. Most stimulatory.7 Sexual effects can occur through any side effects were minor and none prompted with- shift in this serotonin-dopamine balance by an drawal from the study, apart from the anejaculation increase or decrease in either or both neurotrans- experienced by four and 10 men in treatment phase mitter. The serotonin re-uptake inhibitors (SSRI) 2 and 3 respectively.
Recommended publications
  • Impact of CYP2C19 Genotype on Sertraline Exposure in 1200 Scandinavian Patients
    www.nature.com/npp ARTICLE Impact of CYP2C19 genotype on sertraline exposure in 1200 Scandinavian patients Line S. Bråten 1,2, Tore Haslemo1,2, Marin M. Jukic3,4, Magnus Ingelman-Sundberg 3, Espen Molden1,5 and Marianne K. Kringen1,2 Sertraline is an (SSRI-)antidepressant metabolized by the polymorphic CYP2C19 enzyme. The aim of this study was to investigate the impact of CYP2C19 genotype on the serum concentrations of sertraline in a large patient population. Second, the proportions of patients in the various CYP2C19 genotype-defined subgroups obtaining serum concentrations outside the therapeutic range of sertraline were assessed. A total of 2190 sertraline serum concentration measurements from 1202 patients were included retrospectively from the drug monitoring database at Diakonhjemmet Hospital in Oslo. The patients were divided into CYP2C19 genotype-predicted phenotype subgroups, i.e. normal (NMs), ultra rapid (UMs), intermediate (IMs), and poor metabolisers (PMs). The differences in dose-harmonized serum concentrations of sertraline and N-desmethylsertraline-to-sertraline metabolic ratio were compared between the subgroups, with CYP2C19 NMs set as reference. The patient proportions outside the therapeutic concentration range were also compared between the subgroups with NMs defined as reference. Compared with the CYP2C19 NMs, the sertraline serum concentration was increased 1.38-fold (95% CI 1.26–1.50) and 2.68-fold (95% CI 2.16–3.31) in CYP2C19 IMs and PMs, respectively (p < 0.001), while only a marginally lower serum concentration (−10%) was observed in CYP2C19 UMs (p = 0.012). The odds ratio for having a sertraline concentration above the therapeutic reference range was 1.97 (95% CI 1.21–3.21, p = 0.064) and 8.69 (95% CI 3.88–19.19, p < 0.001) higher for IMs and PMs vs.
    [Show full text]
  • ZOLOFT® 50 Mg and 100 Mg Tablets
    NEW ZEALAND DATA SHEET 1. PRODUCT NAME ZOLOFT® 50 mg and 100 mg tablets 2. QUALITATIVE AND QUANTITATIVE COMPOSITION Each 50 mg tablet contains sertraline hydrochloride equivalent to 50 mg sertraline. Each 100 mg tablet contains sertraline hydrochloride equivalent to 100 mg sertraline. For the full list of excipients, see section 6.1. 3. PHARMACEUTICAL FORM ZOLOFT 50 mg tablets: white film-coated tablets marked with the Pfizer logo on one side and “ZLT” scoreline “50” on the other. Approximate tooling dimensions are 1.03 cm x 0.42 cm x 0.36 cm. ZOLOFT 100 mg tablets: white film-coated tablets marked with the Pfizer logo on one side and “ZLT-100” or “ZLT 100” on the other. Approximate tooling dimensions are 1.31 cm x 0.52 cm x 0.44 cm. 4. CLINICAL PARTICULARS 4.1 Therapeutic indications Adults ZOLOFT is indicated for the treatment of symptoms of depression, including depression accompanied by symptoms of anxiety, in patients with or without a history of mania. Following satisfactory response, continuation with ZOLOFT therapy is effective in preventing relapse of the initial episode of depression or recurrence of further depressive episodes. ZOLOFT is indicated for the treatment of obsessive compulsive disorder (OCD). Following initial response, sertraline has been associated with sustained efficacy, safety and tolerability in up 2 years of treatment of OCD. ZOLOFT is indicated for the treatment of panic disorder, with or without agoraphobia. ZOLOFT is indicated for the treatment of post-traumatic stress disorder (PTSD). ZOLOFT is indicated for the treatment of social phobia (social anxiety disorder).
    [Show full text]
  • And N-Demethylation of Venlafaxine in Vitro by Human Liver Microsomes
    O- and N-demethylation of Venlafaxine In Vitro by Human Liver Microsomes and by Microsomes from cDNA-Transfected Cells: Effect of Metabolic Inhibitors and SSRI Antidepressants Steven M. Fogelman, Jürgen Schmider, Karthik Venkatakrishnan, Lisa L. von Moltke, Jerold S. Harmatz, Richard I. Shader, and David J. Greenblatt The biotransformation of venlafaxine (VF) into its two to the formation of NDV for all four livers tested. major metabolites, O-desmethylvenlafaxine (ODV) and Parameters determined by applying a single-enzyme model 5 / / 5 N-desmethylvenlafaxine (NDV) was studied in vitro with were Vmax 2.14 nmol min mg protein, and Km 2504 human liver microsomes and with microsomes containing mM. Ketoconazole was a potent inhibitor of NDV individual human cytochromes from cDNA-transfected production, although its inhibitory activity was not as great human lymphoblastoid cells. VF was coincubated with as observed with pure 3A substrates. NDV formation was selective cytochrome P450 (CYP) inhibitors and several also reduced by 42% by a polyclonal rabbit antibody against selective serotonin reuptake inhibitors (SSRIs) to assess rat liver CYP3A1. Studies using expressed cytochromes their inhibitory effect on VF metabolism. Formation rates showed that NDV was formed by CYP2C9, 22C19, and for ODV incubated with human microsomes were 23A4. The highest intrinsic clearance was attributable to consistent with Michaelis-Menten kinetics for a single- CYP2C19 and the lowest to CYP3A4. However the high in enzyme mediated reaction with substrate inhibition. Mean vivo abundance of 3A isoforms will magnify the 5 parameters determined by non-linear regression were: Vmax importance of this cytochrome. Fluvoxamine (FX), at a / / 5 m m 0.36 nmol min mg protein, Km 41 M, and Ks 22901 concentration of 20 M, decreased NDV production by m M (Ks represents a constant which reflects the degree of 46% consistent with the capacity of FX to inhibit CYP3A, substrate inhibition).
    [Show full text]
  • Determination of Sertraline and Its Metabolite by High-Pressure Liquid Chromatography in Plasma
    ACADEMIA ROMÂNĂ Rev. Roum. Chim., Revue Roumaine de Chimie 2015, 60(5-6), 543-548 http://web.icf.ro/rrch/ DETERMINATION OF SERTRALINE AND ITS METABOLITE BY HIGH-PRESSURE LIQUID CHROMATOGRAPHY IN PLASMA Nazan YUCE-ARTUN,a Erguvan Tuğba ÖZEL KIZIL,b Bora BASKAK,b Halise Devrimci ÖZGÜVEN,b Yalçın DUYDUc and Halit Sinan SUZENc,* aBiotechnology Institute, Ankara University, Golbasi, Ankara, Turkey bDepartment of Psychiatry, School of Medicine, Ankara University, Dikimevi, Ankara, Turkey cDepartment of Toxicology, Faculty of Pharmacy, Ankara University, Tandogan, Ankara, Turkey Received November 10, 2014 A fast, simple and sensitive high-pressure liquid chromatography (HPLC) method with UV detection was developed for frequently prescribed antidepressant, sertraline (SERT) and its main B metabolite N-desmethylsertraline (DSERT), in human plasma. SERT and DSERT were extracted by an optimized solid phase chromatographic (SPE) method using C-18 cartridges and DSE SER Clomipramine was used as external standard (ES). The analytes ES were separated on C18, 4.6 mm × 150 mm, 5 µm column at 50 °C with a mobile phase of 45% acetonitrile + 55% NaH2PO4 at a flow rate of 0.4 mL/min. Detector responses monitored at 4 different wave-lengths; 200-205-210-215 nm. The method proved to be rapid and effective for the plasma sample analyses of therapeutic drug monitoring for sertraline treated patients. INTRODUCTION* depression, panic disorder, generalised anxiety disorder, and social phobia.2 Like other SSRIs, it High rates of poor compliance, considerable has a wide therapeutic index and seems to be better genetic variability in metabolism, and the clinical tolerated than tricyclic antidepressants.3 The drug heterogeneity of depression are the main problems is slowly absorbed with a time to peak plasma for the practical application of selective serotonin concentration of approximately 4–8 h and an reuptake inhibitors (SSRI).1 Therapeutic drug elimination half life of 22–35 h.
    [Show full text]
  • LEGISLATIVE ASSEMBLY Question on Notice
    LEGISLATIVE ASSEMBLY Question On Notice Thursday, 15 February 2018 2560. Ms M. M Quirk to the Minister for Police; I refer to the commencement of operation of the Road Traffic Amendment Act 2016 in March 2017 which introduced compulsory blood or urine samples to be taken from drivers involved in serious crashes, and I ask: (a) since March 2017 how many such samples have been taken; (b) for what specific substances are those blood or urine samples tested; (c) what are the results of those tests to date; and (d) what percentage of drivers have been found to have ingested more than one substance capable of impairing driving skills? Answer (a) The compulsory taking of blood from all drivers involved in serious crashes commenced on 10 March 2017. Between 10 March 2017 and 22 February 2018 (inclusive) a total of 398 blood test samples have been collected under the provision of the Road Traffic Amendment Act 2016. There have been no urine tests collected. (b) Please see attached table for a list of substances in blood sample that are identifiable in ChemCentre toxicology analysis (Paper Number). (c) Of the 398 blood samples collected, 48 are pending results of ChemCentre analysis. Of the 350 analysed, 259 samples had a specific substance(s) detected and 91 samples had no specific substance detected. d) Of the 259 samples with specific substance(s) detected, 92% were found to have multiple substances (more than one). Detectable Substances in Blood Samples capable of identification by the ChemCentre WA. ACETALDEHYDE AMITRIPTYLINE/NORTRIPTYLINE
    [Show full text]
  • Sertraline in Children and Adolescents with Obsessive-Compulsive Disorder a Multicenter Randomized Controlled Trial
    Sertraline in Children and Adolescents With Obsessive-Compulsive Disorder A Multicenter Randomized Controlled Trial John S. March, MD, MPH; Joseph Biederman, MD; Robert Wolkow, MD; Allan Safferman, MD; Jack Mardekian, PhD; Edwin H. Cook, MD; Neal R. Cutler, MD; Roberto Dominguez, MD; James Ferguson, MD; Betty Muller, MD; Robert Riesenberg, MD; Murray Rosenthal, DO; Floyd R. Sallee, MD, PhD; Hans Steiner, MD; Karen D. Wagner, MD, PhD Context.—The serotonin reuptake inhibitors are the treatment of choice for pa- APPROXIMATELY 1 in 200 young per- tients with obsessive-compulsive disorder; however, empirical support for this as- sons has obsessive-compulsive disorder sertion has been weaker for children and adolescents than for adults. (OCD),1 which many believe to be the 2 Objective.—To evaluate the safety and efficacy of the selective serotonin reup- paradigmatic neuropsychiatric illness. take inhibitor sertraline hydrochloride in children and adolescents with obsessive- Individuals with OCD experience obses- sions, which are recurrent and persis- compulsive disorder. tent thoughts, images, or impulses that Design.—Randomized, double-blind, placebo-controlled trial. are egodystonic, intrusive, and, for the Patients.—One hundred eighty-seven patients: 107 children aged 6 to 12 years most part, acknowledged as senseless.3 and 80 adolescents aged 13 to 17 years randomized to receive either sertraline (53 children, 39 adolescents) or placebo (54 children, 41 adolescents). See also p 1784 and Patient Page. Setting.—Twelve US academic and community clinics with experience con- ducting randomized controlled trials. Intervention.—Sertraline hydrochloride was titrated to a maximum of 200 mg/d Common obsessions are generally ac- during the first 4 weeks of double-blind therapy, after which patients continued to companied by distressing negative af- fects, such as fear, disgust, doubt, or a receive this dosage of medication for 8 more weeks.
    [Show full text]
  • 21-436/S-018
    CENTER FOR DRUG EVALUATION AND RESEARCH APPLICATION NUMBER: 21-436/S-018 CLINICAL PHARMACOLOGY AND BIOPHARMACEUTICS REVIEW(S) Clinical Pharmacology and Biopharmaceutics Review ______________________________________________________________________________ NDA: 21-436 S018, 21-713 S013, 21-729 S005, 21-866 S005 Generic Name: Aripiprazole Trade Name: Abilify™ Dosage Forms: Tablets, Oral Solution, ODT, IM Indication: Adjunctive treatment of Major Depressive Disorder Sponsor: Otsuka/Bristol Myer Squibb Submission Type: Efficacy Supplement Submission Date: 5/16/07 OCP Division: DCP1 (HFD-860) OND Division: DPP (HFD-130) Reviewer: Kofi A. Kumi, Ph.D. Secondary Reviewer: Andre Jackson, Ph.D. Team Leader: Raman Baweja, Ph.D. ______________________________________________________________________________ Table of Contents 1. EXECUTIVE SUMMARY .............................................................................................. 2 1.1. Recommendations ............................................................................................... 2 1.2. Phase IV Commitments ....................................................................................... 2 1.3. Comments to Medical Division............................................................................. 2 1.4. Comments to Sponsor ......................................................................................... 3 1.5. Summary of Clinical Pharmacology Findings....................................................... 3 1.5.1. Background.......................................................................................................................3
    [Show full text]
  • ZOLOFT ® (Sertraline Hydrochloride)
    ZOLOFT® (sertraline hydrochloride) Tablets and Oral Concentrate Suicidality and Antidepressant Drugs Antidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults in short-term studies of major depressive disorder (MDD) and other psychiatric disorders. Anyone considering the use of ZOLOFT or any other antidepressant in a child, adolescent, or young adult must balance this risk with the clinical need. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction in risk with antidepressants compared to placebo in adults aged 65 and older. Depression and certain other psychiatric disorders are themselves associated with increases in the risk of suicide. Patients of all ages who are started on antidepressant therapy should be monitored appropriately and observed closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. ZOLOFT is not approved for use in pediatric patients except for patients with obsessive compulsive disorder (OCD). (See Warnings: Clinical Worsening and Suicide Risk, Precautions: Information for Patients, and Precautions: Pediatric Use) DESCRIPTION ZOLOFT® (sertraline hydrochloride) is a selective serotonin reuptake inhibitor (SSRI) for oral administration. It has a molecular weight of 342.7. Sertraline hydrochloride has the following chemical name: (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine hydrochloride. The empirical formula C17H17NCl2HCl is represented by the following structural formula: 1 Reference ID: 3536868 NHCH3 HCl Cl Cl Sertraline hydrochloride is a white crystalline powder that is slightly soluble in water and isopropyl alcohol, and sparingly soluble in ethanol.
    [Show full text]
  • Treatment of Erythromelalgia with a Serotonin/Noradrenaline Reuptake Inhibitor
    Treatment of erythromelalgia with a serotonin/noradrenaline reuptake inhibitor. by Drs. A.Moiin, S.S. Yashar, J.E. Sanchez, B. Yashar 2002 British Association of Dermatologists, British Journal of Dermatology, 146, 331- 344 (Letter to the Editor) SIR, Erythromelalgia is an unusual disorder characterized by the triad of red, hot and painful extremities. The symptoms are exacerbated by heat and improved by cold. Its aetiology is not fully understood. Numerous different medications including aspirin, gabapentin, amitriptyline, benzodiazepines and opiates have been used in attempts to treat the symptoms of erythromelalgia, with varying success.[1] We report our experience with the use of venlafaxine (Efexor®; Wyeth Ayerst Pharmaceuticals, St Davids, PA, USA), a serotonin and noradrenaline reuptake inhibitor, in the treatment of primary erythromelalgia. Venlafaxine has previously been reported to improve the symptoms in one case of Raynaud's phenomenon [2] and two cases of erythromelalgia.[3] Ten patients with primary erythromelalgia were studied. Appropriate investigations were performed to exclude associated causes. Patients were subsequently treated with oral venlafaxine 37.5 mg twice daily. The patients were examined weekly for evaluation of symptoms, as well as for severity and extent of skin warmth and erythema. All patients were able to tolerate the treatment without major side-effects. Following 1 week of therapy, a marked improvement in pain and burning was reported by all patients. There was also an appreciable decrease in the warmth and erythema in all patients. The most common side effect was nausea, reported in two patients. The patients continued the treatment for up to 6-18 months with continued benefit, and no adverse reactions.
    [Show full text]
  • Antidepressant Screening Demonstrated Non-Monotonic Responses to Amitriptyline, Amoxapine and Sertraline in Locomotor Activity Assay in Larval Zebrafish
    cells Article Antidepressant Screening Demonstrated Non-Monotonic Responses to Amitriptyline, Amoxapine and Sertraline in Locomotor Activity Assay in Larval Zebrafish Michael Edbert Suryanto 1,† , Gilbert Audira 1,2,†, Boontida Uapipatanakul 3 , Akhlaq Hussain 1, Ferry Saputra 1 , Petrus Siregar 1, Kelvin H.-C. Chen 4,* and Chung-Der Hsiao 1,2,5,* 1 Department of Bioscience Technology, Chung Yuan Christian University, Chung-Li 320314, Taiwan; [email protected] (M.E.S.); [email protected] (G.A.); [email protected] (A.H.); [email protected] (F.S.); [email protected] (P.S.) 2 Department of Chemistry, Chung Yuan Christian University, Chung-Li 320314, Taiwan 3 Department of Chemistry, Faculty of Science and Technology, Rajamangala University of Technology Thanyaburi, Thanyaburi 12110, Thailand; [email protected] 4 Department of Applied Chemistry, National Pingtung University, Pingtung 900391, Taiwan 5 Center for Nanotechnology, Chung Yuan Christian University, Chung-Li 320314, Taiwan * Correspondence: [email protected] (K.H.-C.C.); [email protected] (C.-D.H.) † These authors contributed equally to this work. Abstract: Antidepressants are well-known drugs to treat depression and major depressive disorder for humans. However, the misuse and abuse of antidepressants keep increasing with several side Citation: Suryanto, M.E.; Audira, G.; effects reported. The aim of this study was to assess the potential adverse effects of 18 antidepressants Uapipatanakul, B.; Hussain, A.; by monitoring zebrafish larval locomotor activity performance based on the total distance traveled, Saputra, F.; Siregar, P.; Chen, K.H.-C.; burst movement count, and total rotation count at four dark-light intercalated phases.
    [Show full text]
  • Pharmacologically Active Metabolites of Currently Marketed Drugs: Potential Resources for New Drug Discovery and Development
    hon p.1 [100%] YAKUGAKU ZASSHI 130(10) 1325―1337 (2010) 2010 The Pharmaceutical Society of Japan 1325 ―Review― Pharmacologically Active Metabolites of Currently Marketed Drugs: Potential Resources for New Drug Discovery and Development Myung Joo KANG, Woo Heon SONG, Byung Ho SHIM, Seung Youn OH, Hyun Young LEE, Eun Young CHUNG, Yesung SOHN,andJaehwiLEE Division of Pharmaceutical Sciences, College of Pharmacy, Chung-Ang University, 221 Heuksuk-dong, Dongjak-gu, Seoul 156756, South Korea (Received April 14, 2010; Accepted July 14, 2010) Biotransformation is the major clearance mechanism of therapeutic agents from the body. Biotransformation is known not only to facilitate the elimination of drugs by changing the molecular structure to more hydrophilic, but also lead to pharmacological inactivation of therapeutic compounds. However, in some cases, the biotransformation of drugs can lead to the generation of pharmacologically active metabolites, responsible for the pharmacological actions. This review provides an update of the kinds of pharmacologically active metabolites and some of their individual phar- macological and pharmacokinetic aspects, and describes their importance as resources for drug discovery and develop- ment. Key words―pharmacologically active metabolite; biotransformation; metabolism; drug discovery gents exhibited by biotransformation can sometimes INTRODUCTION lead to the generation of pharmacologically active Xenobiotics are chemical substances found in living metabolites, which can responsible for the pharmaco- being but not normally produced or present in body, logical responses.1,46) It has been reported that about including pollutants, dietary components and drugs. 22% of the top 50 drugs prescribed in the USA in To defense the body against xenobiotic substances, an 2003 undergo biotransformation into metabolites array of biotransformation reactions (or metabolic that play signiˆcant roles in the pharmacological ac- reactions) is undergone.
    [Show full text]
  • Pdf (Accessed December 2015)
    The author(s) shown below used Federal funds provided by the U.S. Department of Justice and prepared the following final report: Document Title: Identification and Prevalence Determination of Novel Recreational Drugs and Discovery of Their Metabolites in Blood, Urine and Oral Fluid Author(s): Amanda L.A. Mohr, Melissa Friscia, Barry K. Logan Document No.: 250338 Date Received: October 2016 Award Number: 2013-DN-BX-K018 This report has not been published by the U.S. Department of Justice. To provide better customer service, NCJRS has made this federally funded grant report available electronically. Opinions or points of view expressed are those of the author(s) and do not necessarily reflect the official position or policies of the U.S. Department of Justice. Identification and Prevalence Determination of Novel Recreational Drugs and Discovery of Their Metabolites in Blood, Urine, and Oral Fluid Award Number: 2013-DN-BX-K018 Amanda L.A. Mohr, Melissa Friscia, Barry K. Logan This document is a research report submitted to the U.S. Department of Justice. This report has not been published by the Department. Opinions or points of view expressed are those of the author(s) and do not necessarily reflect the official position or policies of the U.S. Department of Justice. Abstract Designer drug products which contain a variety of unregulated psychoactive constituents have become mainstream on the illicit drug market. These compounds, collectively known as novel psychoactive substances (NPS) are generally abused for their stimulatory and euphoric effects. Because of their physical and mind-altering effects, NPS are commonly used at electronic dance music (EDM) festivals to enhance attendees’ experience of the music and the event.
    [Show full text]