Vardenafil Hydrochloride

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Cat Number

API0232245

CAS Number

224785-91-5

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Product Detail Description Scientific Support Customer Q&A

CAS Number

224785-91-5

EINECS

664-451-0

Storage

Store at room temperature

Synonyms

Vardenafil HCL; Nuviva; VARDENAFIL MONOHYDROCHLORIDE; IF61NL91H3; vardenafil hydrochloride anhydrous; BAY 38-9456

Molecular Formula

C23H33ClN6O4S

Molecular Weight

525.1

Smiles

CCCC1=NC(=C2N1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)CC)OCC)C.Cl

Appearance

White to off-white solid powder

Boiling Point

692.2°C at 760 mmHg

General Description

Vardenafil hydrochloride is a synthetic imidazotriazinone derivative, a phosphodiesterase type 5 (PDE5) inhibitor, with a piperazine ring and a sulfonamide group. Its chemical structure is 2-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one hydrochloride.

Mechanism of Action

Vardenafil selectively inhibits the PDE5 enzyme, which is responsible for the degradation of cyclic guanosine monophosphate (cGMP) in the corpus cavernosum. By blocking PDE5, the drug increases the concentration of cGMP, prolonging the vasodilatory effect of nitric oxide and enhancing penile blood flow, leading to an erection. The drug has a higher selectivity for PDE5 than for other PDE isoenzymes.

Application

Vardenafil is indicated for the treatment of erectile dysfunction (ED), improving the ability to achieve and maintain an erection. It is also used for the treatment of pulmonary arterial hypertension (PAH) in some countries, where it acts as a pulmonary vasodilator. The drug is effective in patients with ED of various etiologies, including diabetes and spinal cord injury.

RT234 (vardenafil inhalation powder) was safe and well tolerated in healthy adults after single (0.2–2.4 mg) and repeated doses (up to 2.4 mg q4h for 9 days). Vardenafil was rapidly absorbed with dose‑proportional exposure, no clinically relevant accumulation, and systemic exposure lower than oral vardenafil 20 mg. Mild‑to‑moderate headache was the most common adverse event. These findings support further evaluation of RT234 for as‑needed treatment of pulmonary arterial hypertension.

Fig. 1 Observed and model-predicted plasma vardenafil concentrations versus time from all subjects receiving repeated doses. (Eldon MA, et al., 2021)

References

Eldon MA, et al. Safety, Tolerability, and Pharmacokinetics of RT234 (Vardenafil Inhalation Powder): A First-in-Human, Ascending Single- and Multiple-Dose Study in Healthy Subjects. J Aerosol Med Pulm Drug Deliv. 2021;34(4):251-261.

Does Vardenafil Hydrochloride require protection from light during long-term storage?

Yes, it is photosensitive. Light exposure can cause photodegradation of the imidazotriazinone ring. Store in light-resistant containers, preferably amber glass or original packaging.

What is the recommended storage temperature for Vardenafil Hydrochloride?

Store at controlled room temperature (15-25°C). Avoid excessive heat above 30°C, which can soften the powder and accelerate oxidative degradation.

Is Vardenafil Hydrochloride hygroscopic, and how is this managed?

It is slightly hygroscopic. Under high humidity (>70% RH), it may absorb moisture and clump. Storage in tightly sealed containers with desiccant is recommended.

How is the impurity vardenafil N-oxide (an oxidative degradation product) monitored?

This degradation product is quantified using a stability-indicating HPLC method, ensuring it remains within pharmacopoeial limits.