Veralipride ((±)-Veralipride)
(Synonyms: 维拉必利,(±)-Veralipride; LIR166) 目录号 : GC30824
Veralipride ((±)-Veralipride) 是一种 D2 受体拮抗剂。
Cas No.:66644-81-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Veralipride is a D2 receptor antagonist. It is an alternative antidopaminergic treatment for menopausal symptoms.
Veralipride administration (100 mg/day for 30 days) induces a significant reduction in vasomotor symptoms and is more effective than placebo. Treatment is followed by the expected increase in plasma prolactin levels and by a significant decrease in mean plasma LH. A significant reduction is observed in objectively recorded hot flushes after Veralipride treatment[1]. Veralipride is well absorbed when administered orally, achieving maximal concentrations at 2.5 hours. It is poorly metabolized and is eliminated in the urine and feces. After oral administration, the half-life is 4 hours, and 44% is excreted without any changes in urine in the first 120 hours[2]. A total of 57 adverse events are registered during the 386-month treatment. For the 20×10 dosing schedule, the highest incidence is observed for anxiety (2.2%), drowsiness, and weakness (1.5%); for the 5 × 2 dosing schedule, the highest incidence is observed for drowsiness (5.3%) and headache (2.6%)[3]. Veralipride is known to cause extrapiramidal signs such as bucco-facial or limb dyskinesia. Veralipride may cause reversible parkinsonism[4].
[1]. Melis GB, et al. Effects of the dopamine antagonist veralipride on hot flushes and luteinizing hormone secretion in postmenopausal women. Obstet Gynecol. 1988 Nov;72(5):688-92. [2]. Carranza-Lira S, et al. Actual status of veralipride use. Clin Interv Aging. 2010 Sep 7;5:271-6. [3]. Valencia MH, e al. Safety of veralipride for the treatment of vasomotor symptoms of menopause. Menopause. 2014 May;21(5):484-92. [4]. Franchignoni FP, et al. Parkinson syndrome induced by veralipride. Minerva Ginecol. 1995 Jun;47(6):277-9.
| Cas No. | 66644-81-3 | SDF | |
| 别名 | 维拉必利,(±)-Veralipride; LIR166 | ||
| Canonical SMILES | O=C(NCC1N(CC=C)CCC1)C2=CC(S(=O)(N)=O)=CC(OC)=C2OC | ||
| 分子式 | C17H25N3O5S | 分子量 | 383.46 |
| 溶解度 | DMSO : ≥ 100 mg/mL (260.78 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6078 mL | 13.0392 mL | 26.0783 mL |
| 5 mM | 0.5216 mL | 2.6078 mL | 5.2157 mL |
| 10 mM | 0.2608 mL | 1.3039 mL | 2.6078 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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The safety of veralipride
The perimenopausal period, from 1 to 4 years, is characterised by vasomotor symptoms, or hot flushes, and other effects due a deficit of estrogens. Approximately 85% of women have hot flushes for 1 year and 25 - 50% continue for up to 5 years. The cause of hot flushes has been linked to dysfunction of the thermoregulatory centre caused by estrogen withdrawal. One proposal for the aetiology of hot flushes is that the thermoregulatory zone is shifted downward in patients who experience hot flushes. Estrogen withdrawal creates a change of the central opioid system and a thermoregulatory instability. Estrogen and/or progestin replacement is the treatment of choice for this distressing symptom. However, steroid replacement may be associated with risks and complications, and is limited in some subjects by well-known contraindications. Veralipride, a synthetic benzamide derivative with antidopaminergic action, is effective in reducing the frequency and severity of hot flushes associated with menopausal hypoestrogenism, gaining interest as a non-hormonal treatment for climacteric flushing. In recent years, extrapyramidal disorders associated with veralipride therapy have been reported and are often due to drug misuse. Adverse effects include acute dyskinesia or Parkinsonism, which may occur after many months of treatment. An association between adverse effects and mistake of administration has been described. This article discusses available data on the benefits and risks of veralipride therapy for menopausal symptoms.
Actual status of veralipride use
During the climacteric period, several symptoms exist that motivate women to seek medical advice; one of the most common is the hot flush, which presents in 75%-85% of these during a variable time span. For the treatment of hot flush, several non-hormonal treatments exist; among them, veralipride has shown to be a useful treatment of vasomotor symptoms during the climacteric period. In recent times, several medical societies have discredited its use. The purpose of this review, therefore, is to define a measured position in relation to the use of this drug. On completion of this review, it was possible to conclude that this drug has an antidopaminergic mechanism of action. The recommended schedule is: 100 mg/day for 20 days, with 10 days drug free. Since the risk of undesirable secondary effects such as galactorrhea, mastodynia, and extrapyramidal can increase with use, no more than 3 treatment cycles are recommended. This drug has a residual effect that can allow drug-free intervals, which permit a longer time between schedules.
[Veralipride and menopause]
Twenty post-menopausal women (10 natural and 10 surgical menopauses) with climateric manifestations consisting mainly in hot flushes were given veralipride. Overall satisfactory results obtained in two-thirds of cases evidence the value of tis non-hormonal therapy, especially in cases of natural menopause which responded consistently. Clinical tolerance of veralipride proved satisfactory. Biological investigations (total and differential blood cell counts, glucid and lipid metabolism, BUN, transaminases) before and after three twenty-day courses of veralipride showed no modifications. Hormonal assays done in four patients showed no action of veralipride on FSH and LH.
Veralipride for hot flushes induced by a gonadotropin-releasing hormone agonist: a controlled study
Objectives: To evaluate the efficacy of veralipride, a benzamide derivative, in the treatment of hot flushes induced by GnRH agonists (GnRH-a) and to study peripheral blood mononuclear cell beta-endorphin concentrations during drug administration.
Design: Randomized, placebo-controlled, double-blind trial.
Setting: Academic department of obstetrics and gynecology.
Patients: Forty women of mean age 43 +/- 5 years who experienced disturbing hot flushes during a 4-month course of tryptorelin depot for myoma-associated menorrhagia.
Interventions: Treatment with oral veralipride 100 mg/d (20 subjects) or matching placebo (20 subjects) during the third month of GnRH-a administration.
Main outcome measures: Modifications of frequency and severity of hot flushes as shown by a 0 to 6-point vasomotor scoring system and variations of beta-endorphin levels in peripheral blood mononuclear cells.
Results: Two subjects in each group dropped out of the study. The median (range) vasomotor score at the end of the second month of treatment was 4 (3 to 6) in both the veralipride and placebo group. At the end of the third and fourth months the median (range) scores were, respectively, 2 (0 to 6) versus 4 (1 to 6) and 2 (0 to 5) versus 4 (1 to 6). No significant variations in mononuclear cell beta-endorphin concentrations were recorded. Serum PRL levels rose from 11.7 +/- 5.7 to 132.3 +/- 65.0 ng/mL (conversion factor to SI unit, 1.0) during veralipride administration and returned to 10.6 +/- 3.7 ng/mL after drug withdrawal.
Conclusion: Veralipride reduced vasomotor symptoms induced by a GnRH-a. Transient hyperprolactinemia was the main side effect observed. The mode of action of the drug in GnRH-a-treated patients and possible interactions with endogenous opioid peptides need further elucidation.
[Consensus conference of the Mexican Association for the Study of Climateric on veralipride prescription for patients with vasomotor symptoms]
Vasomotor symptoms are one of the main reasons for climateric women to consult a physician. Hormone therapy is the first treatment choice, but it is not indicated to all patients. Veralipride is an option for those who cannot or will not try hormone treatment. The Mexican Association for the Study of Climateric (AMEC) assembled an interdisciplinary group of medical experts so that they revised the medical literature on the subject and reached a consensus on veralipride indication, doses, counterindications and safety. The recommendations of the consensus conference on veralipride are: (1) Physicians must be familiar with its indication, side effects, pharmacokinetics and dosage. (2) Patients must be informed on other therapeutical options. (3) Patients' mental and neurological state must be evaluated, in particular to identify movement disorders, extrapyramidal symptoms (tremor or dystonia), anxiety and depression that can be mistaken for climateric symptoms. (4) Any adverse effect associated with the drug must be reported. (5) A random multicenter trial must be carried out in order to identify the frequency and severity of side effects, and (6) Written information on possible health risks when using the drug must be provided.