avanafil
Sources réglementaires consultées
Indications approuvées
- Traitement de la dysfonction érectile chez l’homme adulte ; une stimulation sexuelle est nécessaire.
Contre-indications
Absolues
- Utilisation de dérivés nitrés ou donneurs de monoxyde d’azote ; utilisation de stimulateurs de la guanylate cyclase tels que le riociguat ; hypersensibilité.
- Insuffisance rénale sévère ou dialyse ; insuffisance hépatique sévère.
Mises en garde cliniques
- Mise en garde majeure · Ne pas utiliser si l’activité sexuelle est déconseillée en raison de l’état cardiovasculaire. Une érection durant plus de 4 heures nécessite une prise en charge urgente. — FDA/DailyMed, set_id 1d04e17d-7399-430a-a8bb-fa1912b155e9
- Mise en garde majeure · Arrêter et consulter immédiatement en cas de perte soudaine de la vision ou de diminution/perte soudaine de l’audition. — FDA/DailyMed, set_id 1d04e17d-7399-430a-a8bb-fa1912b155e9
Interactions médicamenteuses
- SévèreDérivés nitrés, donneurs de monoxyde d’azote ou riociguat
Mécanisme: La vasodilatation additive peut provoquer une hypotension sévère.
Recommandation: Association contre-indiquée.
FDA/DailyMed, set_id 1d04e17d-7399-430a-a8bb-fa1912b155e9https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1d04e17d-7399-430a-a8bb-fa1912b155e9
- ModéréeAlpha-bloquants ou antihypertenseurs
Mécanisme: Ils peuvent provoquer une hypotension symptomatique additive.
Recommandation: Stabiliser le traitement, commencer à faible dose et surveiller la pression artérielle et les symptômes.
FDA/DailyMed, set_id 1d04e17d-7399-430a-a8bb-fa1912b155e9https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1d04e17d-7399-430a-a8bb-fa1912b155e9
- SévèreInhibiteurs du CYP3A4
Mécanisme: Ils augmentent l’exposition à l’avanafil.
Recommandation: Ne pas utiliser avec des inhibiteurs puissants ; avec des inhibiteurs modérés, ne pas dépasser 50 mg en 24 heures.
FDA/DailyMed, set_id 1d04e17d-7399-430a-a8bb-fa1912b155e9https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1d04e17d-7399-430a-a8bb-fa1912b155e9
- ModéréeConsommation importante d’alcool
Mécanisme: La vasodilatation additive augmente le risque d’hypotension symptomatique.
Recommandation: Limiter l’alcool et surveiller les vertiges ou la syncope.
FDA/DailyMed, set_id 1d04e17d-7399-430a-a8bb-fa1912b155e9https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1d04e17d-7399-430a-a8bb-fa1912b155e9
Effets indésirables
Communs (≥1%)
Céphalées · Bouffées vasomotrices · Congestion nasale · Rhinopharyngite · Douleur dorsale
Rares mais graves
Priapisme · Neuropathie optique ischémique antérieure non artéritique · Perte auditive soudaine · Événement cardiovasculaire grave
Grossesse et allaitement
Non indiqué chez la femme.
Bibliographie récente (PubMed)
Lodenafil is a class of drugs called an inhibitor of PDE5 which also include a wide range of other erectile medicines, such as sildenafil, tadalafil and vardenafil. It is part of a new generation of PDE5 inhibitors that includes udenafil and avanafil. Lodenafil is a prodrug manufactured in the form of lodenafil carbonate, the carbonate dimer that divides in the body into two active drug lodenafil molecules. The oral bioavailability of this formulation is higher than that of the parent drug. This article discusses, by a critical comprehensive review of the literature on lodenafil in terms of its description, names, formulae, elemental composition, appearance, and therapeutic uses. The article also discusses the methods for preparation of lodenafil, its physical-chemical properties, analytical methods for its determination, pharmacological-toxicological properties, and dosing information.
Avanafil is an oral medication used to treat erectile dysfunction (ED). As a phosphodiesterase type 5 (PDE5) inhibitor, it functions by inhibiting the PDE5 enzyme, which ultimately results in increased levels of cyclic guanosine monophosphate (cGMP) and improved blood flow to the penis. Approved by the FDA in 2012, avanafil is recognised for its rapid onset of action, short half-life, and favourable side-effects profile. While it has been explored for other potential therapeutic applications, its current approved use is limited to ED and should be used as prescribed by a medical professional. This chapter provides a comprehensive review of avanafil, encompassing its nomenclature, physicochemical properties, methods of preparation, and identification. Various techniques for analysing avanafil, such as electrochemical analysis, spectrophotometric, spectrofluorimetric, and chromatographic techniques, are discussed. The pharmacology of avanafil, including its pharmacokinetics and pharmacodynamics, is also examined.
To evaluate if therapy with a nutraceutical combination of alpha lipoic acid, Vitis vinifera L. and Ginkgo biloba (Blunorm forte®) can be helpful and be synergic with Avanafil. The trial included 123 males with type 2 diabetic mellitus and with erectile dysfunction (ED), aged ≥18 years. Patients were divided in four different arms: 1st arm: placebo during the three months of treatment and before sexual act; 2nd arm: placebo for three months and Avanafil: 1 tablet, 200 mg, 15-30 minutes before sexual act; 3rd arm: Blunorm forte: 1 tablet, 40 minutes before the meal (breakfast) during the three months and Avanafil: 1 tablet, 200 mg, 15-30 minutes before sexual act; 4th arm: Blunorm forte: 1 tablet, 40 minutes before the meal (breakfast and dinner) during the three months and placebo 15-30 minutes before sexual act. A significant reduction of fasting plasma glucose, and homeostasis model assessment-insulin resistance index were recorded both in Avanafil + Blunorm forte and with Blunorm forte. Metalloproteinases-2, and -9 were reduced in the Avanafil + Blunorm forte group. High sensitivity-C-reactive protein was decreased by both Avanafil, and Avanafil + Blunorm forte group. No variations were recorded with the other treatments. The group treated with Blunorm forte and Avanafil reached a higher International Index of Erectile Function (IIEF) score after 3 months of therapy compared to baseline and placebo and compared to Avanafil and Blunorm forte taken alone. Blunorm forte® can be helpful and synergic with Avanafil in increasing sexual performance compared to placebo.
Phosphodiesterase type 5 inhibitors (PDE5Is), due to their efficacy and tolerable profile for more than 2 decades,are considered a good addition to the available treatments in patients with erectile dysfunction (ED). We sought to assess the possible influence of oral PDE5Is on male human reproduction. A literature review was performed in several databases, including the PubMed/Medline database, Scopus, Cochrane Library, EMBASE, Academic Search Complete, and Egyptian Knowledge Bank databases. The keywords/search terms were "PDE5Is," "sildenafil," "vardenafil," "tadalafil," or "avanafil," combining and crossing them with "male infertility," "semen," "reproductive hormones," or "sperm." Overall, 101 articles were selected. After removal of duplicates and animal studies, 75 articles were finally subjected to review covering the different items related to male human reproduction, including effects of PDE5Is on different parameters of semen or reproductive hormones, as uses of PDE5Is in cases related to distinctive male factor infertility, such as ED, temporary ED, or ejaculatory failure alongside assisted reproduction (AR) procedures, and ejaculatory dysfunction in spinal cord lesions. We found 26 articles that addressed the direct effects of PDE5Is on semen and reproductive hormonal profiles, 16 in vivo studies and 10 in vitro studies. Oral PDE5Is have in general a stimulatory effect on sperm motility, while other semen parameters and reproductive hormonal profiles showed varied outcomes. Such effects are more pronounced with a long-term daily regimen than with an on-demand regimen. However, it seems that the best-controlled studies suggested no change in the sperm quality of male reproductive potential. Oral PDE5Is have in general stimulatory effects on sperm motility, while other semen parameters and hormone profiles showed varied results. In addition, oral PDE5Is have played a useful role in conditions related to distinctive male factor infertility, such as ED, tempo
Erectile Dysfunction (ED) is a prevalent sexual health condition affecting a significant portion of the male population worldwide. The conventional therapeutic approaches for ED often involve the use of pharmaceutical agents targeting the phosphodiesterase-5 (PDE5) enzyme. Currently, treatment with PDE-5 inhibitors is the standard approach for ED, and four PDE-5 inhibitors, namely sildenafil, vardenafil, tadalafil, and avanafil, are in use. However, these pharmaceutical interventions may be associated with adverse effects and limitations. As a result, there has been a growing interest in exploring alternative and complementary treatment options for ED, such as nutraceuticals, which are bioactive compounds derived from natural sources. Nutraceuticals, which include vitamins, minerals, herbs, and other dietary supplements, have gained popularity for their potential health benefits. Certain nutraceuticals have demonstrated the ability to modulate various physiological pathways, including those involved in erectile function. A notable mechanism of action is the inhibition of the PDE5 enzyme, which plays a pivotal role in the regulation of cGMP levels. By inhibiting PDE5, nutraceuticals can promote the accumulation of cGMP, leading to enhanced penile blood flow and improved erectile function. A comprehensive analysis of the literature showcases various nutraceutical agents, including plant-derived compounds like flavonoids, polyphenols, and amino acids which have exhibited PDE5 inhibitory effects. Mechanistic insights into their action involve modulation of NO release, cGMP elevation, and relaxation of penile smooth muscles, all critical factors for achieving and sustaining erections. This review focuses on elucidating the role of nutraceuticals in treating erectile dysfunction through the inhibition of the PDE5 enzyme.