These highlights do not include all the information needed to use Staxyn safely and effectively. See full prescribing information for Staxyn.STAXYN (vardenafil hydrochloride) orally disintegrating tablets Initial U.S. Approval: 2003
Staxyn Information
Product Code 0085-3099 Company Name Schering Plough Corporation Dosage From TABLET, ORALLY DISINTEGRATING Strength 11.85 mg Active Ingredient VARDENAFIL HYDROCHLORIDE
Staxyn (Vardenafil hydrochloride) Indications And Usage
Staxyn (Vardenafil hydrochloride) ™ is indicated for the treatment of erectile dysfunction.
Staxyn (Vardenafil hydrochloride) Dosage And Administration
Staxyn (Vardenafil hydrochloride) is available in 10 mg orally disintegrating tablets. Staxyn (Vardenafil hydrochloride) is not interchangeable with vardenafil 10 mg film-coated tablets (LEVITRA). Staxyn (Vardenafil hydrochloride) provides higher systemic exposure compared to vardenafil 10 mg film-coated tablets (LEVITRA).
Staxyn (Vardenafil hydrochloride) should be taken orally, as needed, approximately 60 minutes before sexual activity. The maximum dosing frequency is one Staxyn (Vardenafil hydrochloride) tablet per day. Sexual stimulation is required for a response to treatment.
Staxyn (Vardenafil hydrochloride) should be placed on the tongue where it will disintegrate. The tablet should be taken without liquid. It should be taken immediately upon removal from the blister.
Those patients who require a lower or higher dose of vardenafil need to be prescribed vardenafil film-coated tablets .
Staxyn (Vardenafil hydrochloride) Dosage Forms And Strengths
Staxyn (Vardenafil hydrochloride) IS AVAILABLE IN 10 MG WHITE, ROUND, ORALLY DISINTEGRATING TABLETS (NOT SCORED), NO DEBOSSING.
Staxyn (Vardenafil hydrochloride) Warnings And Precautions
The evaluation of erectile dysfunction should include a medical assessment, a determination of potential underlying causes and the identification of appropriate treatment.
Before prescribing Staxyn (Vardenafil hydrochloride) , it is important to note the following:
Staxyn (Vardenafil hydrochloride) Adverse Reactions
The following serious adverse reactions with the use of Staxyn (Vardenafil hydrochloride) (vardenafil) are discussed elsewhere in the labeling:
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
Staxyn (Vardenafil hydrochloride)
Adverse drug reactions reported in the Staxyn (Vardenafil hydrochloride) placebo controlled trials were comparable to the adverse drug reactions reported in earlier vardenafil film-coated tablets placebo controlled trials.
All Vardenafil Studies:
In the placebo-controlled clinical trials for vardenafil film-coated tablets and Staxyn (Vardenafil hydrochloride) , the discontinuation rate due to adverse events was 1.9% for vardenafil compared to 0.8% for placebo.
Placebo-controlled trials suggested a dose effect in the incidence of some adverse reactions (for example, dizziness, headache, flushing, dyspepsia, nausea, nasal congestion) over the 5 mg, 10 mg, and 20 mg doses of vardenafil film-coated tablets.
The following section identifies additional, less frequent adverse reactions (
Body as a whole:
Auditory:
Cardiovascular:
Digestive:
Musculoskeletal:
Nervous:
Respiratory:
Skin and appendages:
Ophthalmologic:
Urogenital:
The following adverse reactions have been identified during post approval use of vardenafil in the film-coated tablet formulation. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to estimate their frequency or establish a causal relationship to drug exposure.
Visual disturbances including vision loss (temporary or permanent), such as visual field defect, retinal vein occlusion, and reduced visual acuity, have also been reported rarely in postmarketing experience. It is not possible to determine whether these events are related directly to the use of vardenafil.
Neurologic:
Staxyn (Vardenafil hydrochloride) Drug Interactions
The drug interaction studies described below were conducted using vardenafil film-coated tablets.
Antihypertensives:
Alcohol:
Staxyn (Vardenafil hydrochloride) Use In Specific Populations
Pregnancy Category B: Staxyn (Vardenafil hydrochloride) is not indicated for use in women. There are no studies of Staxyn (Vardenafil hydrochloride) use in pregnant women.
No evidence of specific potential for teratogenicity, embryotoxicity or fetotoxicity was observed in rats and rabbits that received vardenafil at up to 18 mg/kg/day during organogenesis. This dose is approximately 100 fold (rat) and 29 fold (rabbit) greater than the AUC values for unbound vardenafil and its major metabolite in humans given the maximum recommended human dose (MRHD) of 20 mg.
In the rat pre-and postnatal development study, the NOAEL (no observed adverse effect level) for maternal toxicity was 8 mg/kg/day. Retarded physical development of pups in the absence of maternal effects was observed following maternal exposure to 1 and 8 mg/kg possibly due to vasodilatation and/or secretion of the drug into milk. The number of living pups born to rats exposed pre- and postnatally was reduced at 60 mg/kg/day. Based on the results of the pre- and postnatal study, the developmental NOAEL is less than 1 mg/kg/day. Based on plasma exposures in the rat developmental toxicity study, 1 mg/kg/day in the pregnant rat is estimated to produce total AUC values for unbound vardenafil and its major metabolite comparable to the human AUC at the MRHD of 20 mg. There are no adequate and well-controlled trials of vardenafil in pregnant women
Staxyn (Vardenafil hydrochloride) is not indicated for use in women. It is not known if vardenafil is excreted in human breast milk
Vardenafil was secreted into the milk of lactating rats at concentrations approximately 10-fold greater than found in the plasma. Following a single oral dose of 3 mg/kg, 3.3% of the administered dose was excreted into the milk within 24 hours.
Do not use Staxyn (Vardenafil hydrochloride) in patients with moderate or severe hepatic impairment.
In volunteers with mild hepatic impairment (Child-Pugh A), the Cand AUC following a 10 mg vardenafil (film-coated tablets) dose were increased by 22% and 17%, respectively, compared to healthy control subjects. Staxyn (Vardenafil hydrochloride) can be used in patients with mild hepatic impairment. In volunteers with moderate hepatic impairment (Child-Pugh B), the C and AUC following a 10 mg vardenafil (film-coated tablets) dose were increased by 130% and 160%, respectively, compared to healthy control subjects. Vardenafil has not been evaluated in patients with severe (Child-Pugh C) hepatic impairment. Do not use Staxyn (Vardenafil hydrochloride) in patients with moderate to severe hepatic impairment.
Do not use Staxyn (Vardenafil hydrochloride) in patients on renal dialysis.
In volunteers with mild renal impairment (CLcr = 50–80 mL/min), the pharmacokinetics of vardenafil 20 mg film-coated tablets were similar to those observed in a control group with normal renal function. In the moderate (CLcr = 30–50 mL/min) or severe (CLcr 80 mL/min). Staxyn (Vardenafil hydrochloride) can be used in patients with mild, moderate or severe renal impairment. Do not use Staxyn (Vardenafil hydrochloride) in patients on renal dialysis as vardenafil has not been evaluated in such patients
Staxyn (Vardenafil hydrochloride) Overdosage
The maximum dose of vardenafil for which human data are available is a single 120 mg dose of the film–coated tablets administered to eight healthy male volunteers. The majority of these subjects experienced reversible back pain/myalgia and/or “abnormal vision.”
In cases of overdose, standard supportive measures should be taken as required. Renal dialysis is not expected to accelerate clearance because vardenafil is highly bound to plasma proteins and is not significantly eliminated in the urine.
Staxyn (Vardenafil hydrochloride) Description
Staxyn (Vardenafil hydrochloride) is an oral therapy for the treatment of erectile dysfunction. This monohydrochloride salt of vardenafil is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific PDE5.
Vardenafil HCl is designated chemically as piperazine, 1-[[3-(1,4-dihydro-5-methyl-4-oxo-7-propylimidazo[5,1-f][1,2,4]triazin-2-yl)-4-ethoxyphenyl]sulfonyl]-4-ethyl-, monohydrochloride and has the following structural formula:
Vardenafil HCl is a nearly colorless, solid substance with a molecular weight of 579.1 g/mol and a solubility of 0.11 mg/mL in water.
Staxyn (Vardenafil hydrochloride) is formulated as white round orally disintegrating tablets with no debossing. Each tablet contains 11.85 mg vardenafil hydrochloride, which corresponds to 10 mg vardenafil, and the following inactive ingredients: aspartame, peppermint flavor, magnesium stearate, and Pharmaburst™ B2 (crospovidone, mannitol, silica colloidal hydrated, and sorbitol).
Staxyn (Vardenafil hydrochloride) Clinical Pharmacology
Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMP-specific PDE5; therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP. Because sexual stimulation is required to initiate the local release of nitric oxide, the inhibition of PDE5 has no effect in the absence of sexual stimulation.
In vitro
Staxyn (Vardenafil hydrochloride) Clinical Studies
The efficacy and safety of Staxyn (Vardenafil hydrochloride) were evaluated in two identical multi-national, randomized, double-blind, placebo-controlled trials (studies 1 and 2). Staxyn (Vardenafil hydrochloride) was dosed without regard to meals on an as-needed basis in men with erectile dysfunction (ED), many of whom had multiple other medical conditions. In both pivotal studies, randomization was stratified so that approximately 50% of patients were ≥65 years old. Primary efficacy assessment was by means of the Erectile Function (EF) Domain score of the validated International Index of Erectile Function (IIEF) Questionnaire and two questions from the Sexual Encounter Profile (SEP) dealing with the ability to achieve vaginal penetration (SEP2), and the ability to maintain an erection long enough for successful intercourse (SEP3). The primary endpoints were assessed at 3 months.
Study 1 evaluated 355 mainly European (Belgium, France, Germany, Spain, South Africa, and Netherlands) patients (mean age 61.9; 67% White, 4% Black, 3% Asian, 26% Unknown). The mean baseline EF domain scores were 13 for both placebo and Staxyn (Vardenafil hydrochloride) groups. Study 2 evaluated 331 mainly North American (USA, Canada, Mexico, and Australia) patients (mean age 61.7; 69% White, 5% Black, 4% Asian, 22% Hispanic). The mean baseline EF domain scores were 12 for Staxyn (Vardenafil hydrochloride) and 13 for placebo.
In both studies Staxyn (Vardenafil hydrochloride) demonstrated clinically meaningful and statistically significant improvements over placebo in all 3 primary efficacy variables (see Table 6).
Staxyn (Vardenafil hydrochloride) How Supplied/storage And Handling
Staxyn (Vardenafil hydrochloride) (vardenafil HCl) are white, round orally disintegrating tablets with no debossing. Staxyn (Vardenafil hydrochloride) orally disintegrating tablets are packaged into foil blisterpacks and supplied as a 4 tablet unit or as a 40 tablet bulk pack.
In addition to the active ingredient, vardenafil, each tablet contains aspartame, peppermint flavor, magnesium stearate, and Pharmaburst™ B2 (crospovidone, mannitol, silica colloidal hydrated, and sorbitol).
Store Staxyn (Vardenafil hydrochloride) at 25°C (77°F); excursions permitted to 15–30°C (59–86°F)
Staxyn (Vardenafil hydrochloride) is dispensed in blisterpacks. The patient should be advised to examine the blisterpack before use and not use if blisters are torn, broken, or missing.
