Tadalafil CAS 171596-29-5

Indication - Order Tadalafil

Tadanafil is used to treat erectile dysfunction (ED) and pulmonary hypertension in men.

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Tadalafil, with the formula C22H19N3O4 and molecular weight 389.4, has been widely used to treat erectile dysfunction in men since 2003 under the trade name Cialis. In 2008, Eli Lilly and Company sold the commercial development rights for PAH treatment to United Therapeutics. In June 2009, the FDA approved Tadanafil for the treatment of patients with pulmonary arterial hypertension (PAH) in the United States under the trade name Adcirca. Tadanafil was introduced as a treatment for ED in  in 2003, and the effect was effective 30 minutes after administration, but the optimal effect was 2 hours after onset, and the effect lasted for 36h, and its efficacy was not affected by food. Tadanafil is administered in doses of 10 or 20mg, and the recommended initial dose is 10mg, depending on the patient's reaction and adverse reactions. Pre-market studies showed that after 12 weeks of oral administration of 10 or 20mg of tadanafil, response rates were 67% and 81%, respectively. Many studies have shown that tadanafil has better efficacy in treating ED.

Tadalafil

CAS 171596-29-5

Molecular formula C22H19N3O4

Molecular weight 389.4

EINECS number 687-782-2

Melting point 298 to 300°C

Specific rotation D20+71.0°

Predicted boiling point 679.1±55.0°C

Predicted density 1.51±0.1g/cm3

Flash point 2 ° C

Storage conditions Sealedindry,2-8°C

: solubility DMSO soluble20mg/mL, the clear powder form

Predicted acidity coefficient (pKa)16.68±0.40

Color whitetobeige

opticalactivity [α]/D+68to+78°,c=1inchloroform-d

Mechanism of action

Erectile dysfunction: Tadanafil and sildenafil belong to the same selective type 5 phosphodiesterase (PDE5), but its structure is different from that of the latter, and high fat diet does not interfere with its absorption. Under sexual stimulation, nitric oxide synthase (NOS) in penile nerve endings and vascular endothelial cells catalyzes the synthesis of nitric oxide (NO) from the substrate L-arginine. NO activates guanylate cyclase, which converts guanyl triphosphate into cyclic guanosine phosphate (cGMP), which activates cyclic guanosine phospho-dependent protein kinase, resulting in decreased calcium concentration in smooth  muscle cells, resulting in relaxation of the smooth muscle of the cavernous penis and erection. Phosphodiesterase type 5 (PDE5) degrades cGMP into an inactive product, causing the penis to enter a weak state. Tadanafil causes cGMP buildup by inhibiting PDE5 degradation, which relaxes the smooth muscle of the cavernous body of the penis and leads to penile erection. Since nitrates are NO donors, their combination with tadanafil can significantly increase the level of cGMP and lead to severe hypotension. Therefore, their combination is contraindicated clinically.

Drug interaction

Tadanafil affects this by inhibiting PDES. GMP degradation, so when used in combination with nitric acetogens may cause an extreme drop in blood pressure and increase the risk of syncope. CY3PA4 inducer can reduce the abiotic availability of tadana, and the combination with  rifampicin, cimetidine, erythromycin, clarithromycin, itraconwa, ketoconwa and HVI protease inhibitors may increase the blood concentration of this product. Attention should be paid to the dose adjustment. So far, there has been no report that the pharmacokinetic parameters of this product are affected by diet and alcohol.

Erectile dysfunction drugs for men

Cialis is Tadalafil, an oral drug developed by Eli Lilly Pharmaceutical Company for the treatment of erectile dysfunction in men. It is a second-generation phosphodiesterase 5 inhibitor. Research reports show that compared with sildenafil, Cialis takes effect very quickly, about 15 to 20 minutes, and the effect lasts for up to 36 hours. T1/2 is 17.5 hours. In a study of 348 men with mild to severe erectile dysfunction randomized to tadalafil 20mg or placebo, sexual success improved both 24 and 36 hours after taking compared to placebo, with most men successfully having sex twice at 36 hours. There was no difference in the incidence and severity of adverse drug reactions compared with placebo. Headache and indigestion occurred in more than 5% of men in the Tadalafil group. [Adverse reactions] No serious adverse reactions were observed, such as flushing and abnormal vision. Occasionally headache, dyspepsia. [Precautions] Patients who are taking nitrates, angina pectoris, heart disease, uncontrolled hypertension or hypotension, and patients who have had stroke in the last 6 months should not be allowed.

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