129938-20-1 Medical Raw Testosterone Powder Hydrochloride
Place of Origin:WuHan
Brand Name: NANJIAN
Model Number:CAS NO.: 62-90-8
Payment & Shipping Terms:
Minimum Order Quantity: 10g
Packaging Details:foil bag or tin.
Delivery Time:With 7 workdays
Payment Terms:Western union,Money gram,t/t
129938-20-1 Medical Raw Testosterone Powder Hydrochloride
Detailed Product Description
Medical Raw Testosterone Powder Hydrochloride CAS 129938-20-1
Synonyms: d- hydrochloride; DL- hydrochloride
Assay: 98% min.
Packing: 1kg net/foil bag or tin.
Delivery: Express courier.
Character: White to Off-White Cyrstalline Solid, odorless, slight sweet taste, Mp 175-177℃, optical rotation +128°
Usage: Selective serotonin reuptake inhibitor (SSRI), pharmaceutical material, hormone.
A contraindication is a situation in which a drug should not be used, because it may be harmful to the patient. should not be used in men with moderate to severe hepatic impairment and in those receiving CYP3A4 inhibitors such as ketoconazole, ritonavir, and telithromycine. can also not be used in patients with heart failure, permanent pacemaker, or other significant ischemic heart disease. Caution is advised in men receiving thioridazine, monoamine oxidase inhibitors, SSRIs, serotonin-norepinephrine reuptake inhibitors, or tricyclic antidepressant. If a patient stops taking one of these drugs, he should wait for 14 days before taking . If a patient stops taking , he should wait for 7 days before receiving these drugs.
The most common effects when taking are nausea, dizziness, dry mouth, headache, diarrhea, and insomnia.Discontinuation due to adverse effects is dose related. According to McMahon in recent study in Asia, the rate of discontinuation is 0.3%, 1.7%, and 5.3% of 1067 studied subjects with placebo, 30 mg, and 60 mg respectively. Unlike other SSRIs used to treat depression, which have been associated with high incidences of sexual dysfunction, is associated with low rates of sexual dysfunction. Taken as needed, has very mild adverse effects on loss of libido (<1%) and ED (<4%).
No case of the drug overdose has been reported during clinical trials.
With phosphodiesterase inhibitors (PDE5 inhibitors)
Many men that have PE also suffer from erectile dysfunction (ED). Treatment for these patients should consider the drug-drug interaction between and PDE5 inhibitors such as tadalafil (Cialis) or sildenafil (Viagra). In Dresser study (2006), plasma concentration of 24 subjects was obtained. Half of the sample pool were treated with 60 mg + tadalafil 20 mg; the other half were treated with 60 mg + sildenafil 100 mg. These plasma samples were then analyzed using liquid chromatography-tandem mass spectrometry. The results showed that does not alter the pharmacokinetic of tadalafil or sildenafil.
Ethanol doesn affect the pharmacokinetics of when taking concurrently with .
Mechanism of actions
The mechanism through which affects premature ejaculation is still unclear. However, it is presumed that works by inhibiting serotonin transporter and subsequently increasing serotonins action at pre and postsynaptic receptors Human ejaculation is regulated by various areas in the central nervous system (CNS). The ejaculatory pathway originates from spinal reflex at the thoracolumbar and lumbosacral level of spinal cord activated by stimuli from male genital. These signals are relayed to the brain stem, which then is influenced by a number of nuclei in the brain such as medial preoptic and paraventricular nulcei. Clements study performed on anaesthetized male rats showed that acute administration of inhibits ejaculatory expulsion reflex at supraspinal level by modulating activity of lateral paragigantocellular nucleus (LPGi) neurons. These effects cause an increase in pudendal motoneuron reflex discharge (PMRD) latency. However, it is unclear whether acts directly on LPGi or on the descending pathway in which LPGi located.
is a white powder substance and water- insoluble. Taken 1-3 hours before sexual activity, it is rapidly absorbed in the body. Its maximum plasma concentration (Cm) is reached 1-2 hours after oral administration. The Cm and AUC (Area Under the plasma vs. time Curve) are dose dependent. The Cm and Tm (time needed to obtain the maximum plasma concentration) after single doses of 30 mg and 60 mg are 297 and 498 ng/mL at 1.01 and 1.27 hours respectively. A high fat meal does reduce the Cm slightly, but it is insignificant. In fact, food doesn’t alter pharmacokinetics. can be taken with or without food.
is absorbed and distributed rapidly in the body. Greater than 99% of is bound to the plasma protein. The mean steady state volume is 162L. Its initial half-life is 1.31hours (30 mg dose) and 1.42 hours (60 mg dose,) and its terminal half life is 18.7 hours (30 mg dose) and 21.9 hours (60 mg dose).
is metabolized extensively in the liver and kidney by multiple enzymes such as CyP2D6, CyP3A4, and flavin monooxygenase 1 (FMO1). The major product at the end of the metabolic pathway is circulating N- oxide, which is a weak SSRI and contributes no clinical effect. The other products presented less than 3% in the plasma are desmethyl and didesmethy, which are equipotent to .
The metabolites of are eliminated rapidly in the urine with a terminal half-life of 18.7 and 21.9 hours for a single dose of 30 mg and 60 mg respectively.
Safety and tolerability
The cardiovascular safety profile of has been studied extensively during the drug development. Phase I trials showed that had neither clinical significant electrocardiographic effects nor delayed repolarization effects, with dosing up to 4-fold greater than the maximum recommended dosage which is 60 mg. Phase III studies in men with PE showed a safety and well tolerate profile of with dosing of 30 and 60 mg. There is no cardiovascular adverse had been found.
Studies of SSRIs in patients with major psychiatric disorders prove that SSRIs are potentially associated with certain neurocognitive adverse effects such as anxiety, akathisia, hypomania, changes in mood, or suicidal thought. However, there is no study on the effects of SSRIs in men with PE. McMahon’s study in 2012 showed that has no effect on mood and is not associated with anxiety or suicidality.
The incidence of antidepressant discontinuation syndrome symptoms in men using to treat premature ejaculation has been described by reviewers as low and/or no different from the incidence of such symptoms in men withdrawn from placebo treatment.The lack of chronic serotonergic stimulation with on-demand minimizes the potentiation action of serotonin at synaptic cleft, thus decreasing the risk of DESS.
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