tadalafil
Sources réglementaires consultées
Indications approuvées
- Traitement de la dysfonction érectile chez l’homme adulte ; une stimulation sexuelle est nécessaire.
- Traitement des signes et symptômes de l’hyperplasie bénigne de la prostate chez l’homme adulte avec la présentation à 5 mg une fois par jour.
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.
- Activité sexuelle déconseillée en raison d’une cardiopathie ; infarctus récent, angor instable, insuffisance cardiaque récente, arythmie ou hypertension non contrôlée, hypotension, accident vasculaire cérébral récent ou perte visuelle due à une NOIA-NA.
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. — CIMA/AEMPS, ficha técnica 84402
- Mise en garde majeure · Arrêter et consulter immédiatement en cas de perte soudaine de la vision ou de diminution/perte soudaine de l’audition. — CIMA/AEMPS, ficha técnica 84402
- Mise en garde majeure · En cas d’insuffisance rénale sévère, la dose maximale est de 10 mg à la demande et le traitement quotidien n’est pas recommandé. Les données sont limitées en cas d’insuffisance hépatique sévère : utiliser uniquement après une évaluation individuelle attentive du rapport bénéfice-risque. — CIMA/AEMPS, ficha técnica 84402
Interactions médicamenteuses
- SévèreDérivés nitrés, donneurs de monoxyde d’azote ou riociguat
Mécanisme: La vasodilatation additive peut provoquer une hypotension sévère.
Recommandation: Association contre-indiquée.
CIMA/AEMPS, ficha técnica 84402https://cima.aemps.es/cima/dochtml/ft/84402/FT_84402.html
- 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.
CIMA/AEMPS, ficha técnica 84402https://cima.aemps.es/cima/dochtml/ft/84402/FT_84402.html
- ModéréeInhibiteurs ou inducteurs du CYP3A4
Mécanisme: Les inhibiteurs augmentent l’exposition et les inducteurs peuvent réduire l’efficacité.
Recommandation: Réévaluer l’association, la dose et la tolérance.
CIMA/AEMPS, ficha técnica 84402https://cima.aemps.es/cima/dochtml/ft/84402/FT_84402.html
Effets indésirables
Communs (≥1%)
Céphalées · Dyspepsie · Douleur dorsale · Myalgie · Congestion nasale · Bouffées vasomotrices
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)
Cirrhosis affects approximately 2.2 million adults in the US. From 2010 to 2021, the annual age-adjusted mortality of cirrhosis increased from 14.9 per 100 000 to 21.9 per 100 000 people. The most common causes of cirrhosis in the US, which can overlap, include alcohol use disorder (approximately 45% of all cases of cirrhosis), nonalcoholic fatty liver disease (26%), and hepatitis C (41%). Patients with cirrhosis experience symptoms including muscle cramps (approximately 64% prevalence), pruritus (39%), poor-quality sleep (63%), and sexual dysfunction (53%). Cirrhosis can be diagnosed by liver biopsy but may also be diagnosed noninvasively. Elastography, a noninvasive assessment of liver stiffness measured in kilopascals, can typically confirm cirrhosis at levels of 15 kPa or greater. Approximately 40% of people with cirrhosis are diagnosed when they present with complications such as hepatic encephalopathy or ascites. The median survival time following onset of hepatic encephalopathy and ascites is 0.92 and 1.1 years, respectively. Among people with ascites, the annual incidence of spontaneous bacterial peritonitis is 11% and of hepatorenal syndrome is 8%; the latter is associated with a median survival of less than 2 weeks. Approximately 1% to 4% of patients with cirrhosis develop hepatocellular carcinoma each year, which is associated with a 5-year survival of approximately 20%. In a 3-year randomized clinical trial of 201 patients with portal hypertension, nonselective β-blockers (carvedilol or propranolol) reduced the risk of decompensation or death compared with placebo (16% vs 27%). Compared with sequential initiation, combination aldosterone antagonist and loop diuretics were more likely to resolve ascites (76% vs 56%) with lower rates of hyperkalemia (4% vs 18%). In meta-analyses of randomized trials, lactulose was associated with reduced mortality relative to placebo (8.5% vs 14%) in randomized trials involving 705 patients and reduced risk of recurrent ov
Pulmonary arterial hypertension (PAH) is a subtype of pulmonary hypertension (PH), characterized by pulmonary arterial remodeling. The prevalence of PAH is approximately 10.6 cases per 1 million adults in the US. Untreated, PAH progresses to right heart failure and death. Pulmonary hypertension is defined by a mean pulmonary artery pressure greater than 20 mm Hg and is classified into 5 clinical groups based on etiology, pathophysiology, and treatment. Pulmonary arterial hypertension is 1 of the 5 groups of PH and is hemodynamically defined by right heart catheterization demonstrating a mean pulmonary artery pressure greater than 20 mm Hg, a pulmonary artery wedge pressure of 15 mm Hg or lower, and a pulmonary vascular resistance of 3 Wood units or greater. Pulmonary arterial hypertension is further divided into subgroups based on underlying etiology, consisting of idiopathic PAH, heritable PAH, drug- and toxin-associated PAH, pulmonary veno-occlusive disease, PAH in long-term responders to calcium channel blockers, and persistent PH of the newborn, as well as PAH associated with other medical conditions including connective tissue disease, HIV, and congenital heart disease. Early presenting symptoms are nonspecific and typically consist of dyspnea on exertion and fatigue. Currently approved therapy for PAH consists of drugs that enhance the nitric oxide-cyclic guanosine monophosphate biological pathway (sildenafil, tadalafil, or riociguat), prostacyclin pathway agonists (epoprostenol or treprostinil), and endothelin pathway antagonists (bosentan and ambrisentan). With these PAH-specific therapies, 5-year survival has improved from 34% in 1991 to more than 60% in 2015. Current treatment consists of combination drug therapy that targets more than 1 biological pathway, such as the nitric oxide-cyclic guanosine monophosphate and endothelin pathways (eg, ambrisentan and tadalafil), and has shown demonstrable improvement in morbidity and mortality compared with the previ
Up to 40% of men older than 50 years have lower urinary tract symptoms, including urinary urgency, nocturia, and weak urinary stream, due to disorders of the bladder and prostate. These symptoms negatively affect quality of life and may be associated with urinary retention, which can cause kidney insufficiency, bladder calculi, hematuria, and urinary tract infections. In men, lower urinary tract symptoms can be caused by bladder outlet obstruction secondary to benign prostatic hyperplasia (BPH), an overactive bladder detrusor (a syndrome of urinary urgency and frequency), or both. Behavioral therapy, including pelvic floor physical therapy, timed voiding (voiding at specific intervals), and fluid restriction, can improve symptoms. Medications including α-blockers (such as tamsulosin), 5α-reductase inhibitors (such as finasteride), and phosphodiesterase 5 inhibitors (such as tadalafil) improve lower urinary tract symptoms (mean improvement, 3-10 points on the International Prostate Symptom Score [IPSS], which ranges from 0-35, with higher scores indicating greater severity) and can prevent symptom worsening measured by increased IPSS greater than or equal to 4 points or development of secondary sequelae, such as urinary retention. Combination therapies are more effective than monotherapy. For example, α-blockade (eg, tamsulosin) combined with 5α-reductase inhibition (eg, finasteride) lowers progression risk to less than 10% compared with 10% to 15% with monotherapy. Treatment for overactive bladder detrusor muscle, including anticholinergics (eg, trospium) and β3 agonists (eg, mirabegron), reduces voiding frequency by 2 to 4 times per day and reduces episodes of urinary incontinence by 10 to 20 times per week. Surgery (eg, transurethral resection of the prostate, holmium laser enucleation of the prostate) and minimally invasive surgery are highly effective for refractory or complicated cases of BPH, defined as persistent symptoms despite behavioral and pharmacologic
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.