Medical use
Main article: PDE5 inhibitor vardenafil brand name
It is indications and contraindications are the same as with other PDE5 inhibitors; it is closely related in function to sildenafil citrate (Viagra) and tadalafil (Cialis). The difference between the vardenafil molecule and sildenafil citrate is a nitrogen atom’s position and the change of sildenafil’s piperazine ring methyl group to an ethyl group. Tadalafil is structurally different from both sildenafil and vardenafil. It is relatively short effective time is comparable to but somewhat longer than sildenafil’s. It also does not have an effect on PDE6, which means that it does not have vision adverse effects.
Beyond its indications for erectile dysfunction, vardenafil powder may be effective in the treatment of premature ejaculation, where it may significantly increase the time from penetration to ejaculation.
Description
Vardenafil is a new PDE5 inhibitor launched for oral treatment of male erectile dysfunction and it has significant structural similarity with sildenafil (Viagra?), which was the first PDE5 inhibitor introduced in 1998 for this indication. It is synthesized in three steps starting with a cyclization reaction of 2-ethyoxybenzamidine with 2-butyramidopropionic acid and ethoxyallyl chloride to construct the imidazotriazine ring system, followed by sulfonation to the corresponding sulfonyl chloride and subsequent condensation with 1-ethylpiperazine. The potency of PDE5 inhibition by vard (IC50=0.7 nM) is ～10 times greater than that of sildenafil (IC50=6.6 nM).
Vardenafil is typically administered in single doses of 10 and 20 mg. The time to reach maximum plasma concentration is 0.75 h, which is slightly shorter than those of sildenafil (tmax=1.16 h) and tadalafil (tmax=2h), and the half-life is 4–5 h. Although it is almost completely absorbed following oral administration, the mean absolute bioavailability of a 10 mg dose is ～15%, resulting from extensive first pass metabolism. Vardenafil is metabolized in the liver primarily by CYP3A4 and is eliminated mainly in feces. In clinical studies, 10–20 mg doses of It was well tolerated and efficacious in patients with ED of various severities, including subjects with comorbidities such as diabetes mellitus or hypertension or hyperlipidemia.
Vardenafil side effect
The side-effect profile of It is similar to that of sildenafil, with headache, flushing, dyspepsia and nasal congestion being the most common adverse events. Vardenafil has systemic vasodilatory properties, which can cause transient decrease in supine blood pressure; however, it does not appear to translate into clinical effects. The mean maximum decreases in supine systolic blood pressure following 20 and 40 mg vardenafil were 6.9 and 4.3 mmHg, respectively, when compared to placebo. However, single and multiple oral doses of vardenafil up to 40 mg produced no clinically relevant changes in the ECGs of normal male volunteers.
Uses erectil dysfunction;PDE5 inhibitor
Uses Vardenafil Hydrochloride Trihydrate (cas# 330808-88-3) has therapeutic applications and used in cosmetics and personal care products.
Definition ChEBI: The sulfonamide resulting from formal condensation of the sulfo group of 4-ethoxy-3-(5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one-2-yl)benzenesulfonic acid and the secondary amino group of 4-ethylpiperazine.
Brand name Levitra
Flammability and Explosibility Non flammable
Clinical Use Treatment of erectile dysfunction
Drug interactions Potentially hazardous interactions with other drugs
Alpha-blockers: enhanced hypotensive effect – avoid for 6 hours after alpha-blockers (max dose 5 mg).
Antifungals: concentration increased by ketoconazole, and itraconazole – avoid concomitant use.
Antivirals: concentration increased by fosamprenavir, indinavir and ritonavir- avoid with indinavir and ritonavir; increased risk of ventricular arrhythmias with saquinavir – avoid; avoid with telaprevir, use tipranavir with caution.
Cobicistat: concentration of It possibly increased – reduce dose of vardenafil.
Grapefruit juice: concentration possibly increased – avoid concomitant use.
Nicorandil: possibly enhanced hypotensive effect – avoid concomitant use.
Nitrates: possibly enhanced hypotensive effect – avoid concomitant use.
Riociguat: enhanced hypotensive effect – avoid concomitant use.
Metabolism Vardenafil is metabolised in the liver primarily by cytochrome P450 isoenzymes CYP3A4 (the major route) as well as CYP3A5 and CYP2C isoforms. The major metabolite produced by desethylation of vard also has some activity.
Vard is excreted as metabolites mainly in the faeces (91 to 95
%), and to a lesser extent in the urine.
buy Vardenafil Chemical Properties
Melting point 230-235°C
density 1.37
vapor pressure 0.001Pa at 71.34℃
Fp 9℃
storage temp. Sealed in dry,Store in freezer, under -20°C
solubility >22.5mg/mL in DMSO
form Powder
pka 9.86±0.20(Predicted)
Water Solubility 7mg/L at 20℃
BCS Class 2
InChIKey NOIHTGOGFDFCBN-UHFFFAOYSA-N
SMILES N12C(CCC)=NC(C)=C1C(=O)N=C(C1=CC(S(N3CCN(CC)CC3)(=O)=O)=CC=C1OCC)N2
LogP 2.5 at 23℃
More Introduction:https://en.wikipedia.org/wiki/Vardenafil
