Xatral Medication Information:
Xatral medication comes in several different strengths; click on the strength you need to view prices from pharmacies competing to earn your business.
Xatral 2.500 mg
Xatral 5 mg
Xatral 10 mg
Xatral General Information
Xatral contains alfuzosin hydrochloride and belongs to a group of medications called alpha 1A receptor antagonists and is used to treat the symptoms and signs of benign prostatic hyperplasia (enlargement of the prostate) which causes a decrease of urine flow in men.
How does Xatral work & what does it do?
In men the prostate gland often enlarges with age unfortunately pressing on the urethra and obstructing the flow of urine from the bladder. Xatral relaxes the muscles in the prostate and also the opening of the bladder. This may help to increase the flow of urine and decrease the symptoms of benign prostatic hyperplasia.
When/How is Xatral taken/used/applied?
Xatral should be taken as a 10mg tablet daily preferably after a meal. The pill should be ingested whole and should not be crushed or chewed in any way and should be taken after the same meal around the same time every day.
Side Effects of Xatral
Most medications have side effects and are usually mild enough that it does not deter from the utility of the drug. The most common side effects of Xatral are: runny nose, sore throat, coughing, and dizziness. Less common side effects are: nausea, indigestion, headache, fatigue, constipation, back pain, and decreased sexual drive.
Other Brand Names for Xatral:
Another brand name for Xatral is Alfuzosin which is it's marketing name in the United States.
There are several groups of people who should not take Xatral:
Anyone who has moderate to severe impairment of liver function.
Women and children should not use Xatral.
Anyone who has an allergic reaction to any of the ingredients of the medication.
The dosage is in pill form and is 10mg strength.
The 10 mg pill is a middle white matrix layer between two inactive yellow layers.
What Xatral is used for
Your doctor has prescribed XATRAL because you have a medical condition called benign prostatic hyperplasia (BPH) or acute urinary retention (AUR) related to BPH. This occurs in men.
What Xatral does
XATRAL relaxes muscles in the prostate, bladder neck and base. This results in improved urine flow, and reduced BPH symptoms.
When taken during catheterization for sudden acute urinary retention, XATRAL may help you pass urine after catheter removal. Urinary catheters are flexible tubes placed in the bladder to drain urine.
When Xatral should not be used
If you have ever had an allergic reaction to alfuzosin hydrochloride or to any ingredient in XATRAL (see What the important nonmedicinal ingredients are:).
If you have a moderate to severe decrease in liver function.
If you take other alpha1-blockers for high blood pressure or prostate problems.
If you take ketoconazole, ritonavir (Kaletra; Norvir) or itraconazole (Sporanox).
What the medicinal ingredient is
What the important nonmedicinal ingredients for Xatral are
Colloidal hydrated silica, ethylcellulose, hydrogenated castor oil, hydroxypropyl methylcellulose, magnesium stearate, mannitol, microcrystalline cellulose, povidone, yellow ferric oxide.
What dosage forms Xatral comes in
Prolonged-release tablets. Each tablet contains 10 mg alfuzosin hydrochloride.
Warnings and Precautions
XATRAL is not indicated as a treatment to lower blood pressure.
XATRAL is not indicated nor recommended for use in women and children.
Prostate cancer and BPH cause many of the same symptoms. Prior to starting XATRAL, your doctor will examine you to rule out the presence of prostate cancer.
You (in particular, if you are receiving drugs to lower blood pressure) may experience low blood pressure and feel dizzy at the start of treatment, especially when getting up from a lying or sitting position. In such cases, lie down until the symptoms have completely disappeared.
Tell your doctor or pharmacist, before using the medication, if:
you suffer liver or kidney problems.
you suffer from heart problems.
you have ever had a reaction to the ingredients of this medication.
You have had low blood pressure or signs of low blood pressure [fainting, dizziness] after taking another medicine.
You or any family members have a condition known as congenital prolongation of the QT interval.
You have suffered from QT prolongation following the administration of any drug.
You have a family history of sudden death at an age <50 years.
You have suffered from electrolytes disturbances.
If you will have eye surgery, you must inform your eye surgeon that you are currently using XATRAL.
Interactions with Xatral
XATRAL is metabolized by specific enzymes in the liver. It is not known how combined use of any drugs, herbal products metabolized by the same enzymes or grapefruit juice may influence the efficacy or unwanted side effects of these drugs or herbal medicines.
Before using any prescription, over-the-counter medicines or herbal products, check with your doctor or your pharmacist.
Drugs that interact with XATRAL include:
Alpha1-blockers for high blood pressure or prostate problems.
Anti-infection drugs: ketoconazole, itraconazole (Sporanox) and ritonavir (Kaletra; Norvir ).
Drugs for high blood pressure.
Drugs for heart problems (nitrates).
Sildenafil (Viagra, Revatio).
Proper Use of Xatral
Follow your doctor's instructions very carefully about how to take XATRAL.
The recommended dosage is one tablet (10 mg) daily to be taken right after the same meal each day or from the first day of catheterization. The tablet should be swallowed whole.
DO NOT CHEW, CRUSH, POUND, GRIND OR CRUNCH THE TABLET AS HIGH BLOOD LEVELS OF XATRAL MAY OCCUR.
If you interrupt your treatment for several days or more, resume treatment after consulting with your doctor.
If you have taken too much XATRAL, immediately see your doctor or go to your nearest hospital emergency department or contact poison control centre. Show the doctor your bottle of tablets. Do this even if there are no signs of discomfort or poisoning. Overdose of alfuzosin may lead to low blood pressure.
Side Effects for Xatral and What to Do About Them
Like all prescription drugs, XATRAL may cause side effects. Most side effects are mild.
Side effects due to XATRAL may include dizziness and headache. In some cases, side effects may decrease or disappear while the patient continues to take XATRAL.
You may experience dizziness or fainting caused by a decrease in blood pressure after taking XATRAL. However, these effects are usually transient, occur at the beginning of treatment and do not usually prevent the continuation of treatment. In such cases, lie down until the symptoms have completely disappeared. Although these symptoms are unlikely, do not drive, operate machinery or perform hazardous tasks for 12 hours after the initial dose.
Cases of liver disorder have been observed in patients taking XATRAL. You should inform your doctor if you experience symptoms such as nausea, fatigue, jaundice (yellow colour to the skin and/or eyes), dark urine, light-coloured stools, generalised itching or abdominal pain.
Cases of priapism (painful erection greater than 6 hours) have been rarely reported with the use of XATRAL. If you experience painful erection lasting more than 4 hours, you should contact your doctor immediately. If priapism is not immediately treated, penile tissue damage and erectile dysfunction could result.
|Serious Side Effects, How Often They Happen and What to Do About Them|
|Symptom/Effect||Talk with your doctor or pharmacist||Stop taking drug and call your doctor or pharmacist|
|Only if severe||In all cases|
|Priapism/erection lasting longer than 4 hours||•|
This is not a complete list of side effects. For any unexpected effects while taking XATRAL, contact your doctor or pharmacist.
The active ingredient in Xatral was approved by the FDA for treatment of benign prostatic hyperplasia (BPH) in June 2003.
Xatral is marketed in the United States using the trade name Uroxatral.
Xatral is a trade name for a medication containing the active ingredient alfuzosin.
Xatral belongs to a group of medications known as alpha 1A receptor antagonists.
The potential drug interactions of XATRAL with atenolol was studied in clinical trials. The results showed that XATRAL may be used with atenolol taking into account the hypotensive effects specific to drugs in this group.
The potential drug interactions of XATRAL with hydrochlorothiazide was studied in clinical trials. The results showed that XATRAL can be prescribed without risk of interactions in combination with hydrochlorothiazide.
The potential drug interaction of XATRAL with tadalafil was studied in a clinical trial. The results showed that there is no clinically significant hemodynamic interaction between XATRAL 10 mg once daily and tadalafil 20 mg. XATRAL can be prescribed in combination with tadalafil.
The potential drug interaction of XATRAL with vardenafil was not studied in a clinical trial.
XATRAL should not be used in combination with other alpha1-blockers (see Contraindications).
The potential drug interactions of XATRAL with warfarin was studied in clinical trials. The results showed that XATRAL can be prescribed without risk of interactions in combination with warfarin.
Repeated coadministration of XATRAL and digoxin for 7 days did not influence the steady-state pharmacokinetics of either drug.
XATRAL is not an inducer or an inhibitor of any of the principal hepatic enzymes involved in the metabolism of other drugs.
CYP3A4 is the principal hepatic enzyme isoform involved in the metabolism of XATRAL.
Potent CYP3A4 inhibitors, such as ketoconazole, itraconazole and ritonavir, increased XATRAL blood levels and exposure (AUC). Therefore, XATRAL should not be co-administered with potent inhibitors of CYP3A4 (see Contraindications). See Drug-Drug Interactions for details of increased XATRAL blood levels. As this is only a partial list, the physician is advised to consult current scientific literature regarding other CYP 3A4 competitive inhibitors prior to prescribing XATRAL if other concomitant medications are used as high blood levels of XATRAL can result.
It is not known how combined exposure of any medications metabolized by the CYP3A4 hepatic enzyme isoform (such as modern alpha1-blockers), herbal remedies (particularly St. John's Wort, Milk thistle) and grapefruit juice may influence the overall efficacy and unwanted side effects of these medications, therefore, caution should be exercised.
XATRAL should be prescribed carefully in combination with antihypertensive drugs. (see Warnings and Precautions, Cardiovascular and Drug-Drug Interactions, Cardiovascular Drugs).
The effect on QT/QTc interval of the combination of XATRAL 10 mg and sildenafil 100 mg has been studied in an electrophysiology trial (see Action and Clinical Pharmacology, Pharmacodynamics, Electrocardiography).
XATRAL should be taken after a meal.
It is not known how combined exposure of grapefruit juice may influence the overall efficacy and unwanted side effects of these type of medications, therefore, caution should be exercised.
Because of the vasodilatory effects of alpha-blockers and PDE5-inhibitors, patients treated with alpha-blocker therapy should be hemodynamically stable before treatment with PDE5-inhibitors is initiated.
Treatment with XATRAL for up to 12 months produced no clinically significant changes in urinalysis, the routine biochemical and hematologic tests as well as in prostate specific antigen (PSA).
Repeated coadministration of 240 mg/day of diltiazem, a moderate-potency inhibitor of CYP3A4, with 7.5 mg/day alfuzosin (equivalent to the exposure with XATRAL) increased the Cmax and AUC0-24 of alfuzosin 1.5- and 1.3-fold, respectively. Alfuzosin increased the Cmax and AUC0-12 of diltiazem 1.4-fold. No changes in blood pressure were observed.
Interactions with herbal products have not been established. It is not known how combined exposure of herbal remedies (particularly St. John's Wort, Milk thistle) may influence the overall efficacy and unwanted side effects of these medications, therefore, caution should be exercised when taking herbal remedies with these types of medications.
CYP3A4 is the principal hepatic enzyme involved in the metabolism of XATRAL. Ketoconazole is a strong-potency inhibitor of CYP3A4. Repeated 200 mg daily dosing of ketoconazole, for seven days increased XATRAL Cmax 2.11-fold and AUClast 2.46-fold following a single 10 mg dose of XATRAL under fed condition. Other parameters such as tmax and t1/2 were not modified. The 8-day repeated administration of ketoconazole 400 mg daily increased Cmax of XATRAL by 2.3-fold, AUClast and AUC by 3.2 and 3.0 respectively.
XATRAL should be prescribed carefully in combination with nitrates.
The potential drug interactions of XATRAL with cimetidine was studied in clinical trials. The results showed that XATRAL can be prescribed without risk of interactions in combination with cimetidine.
Information for the Patient
Special Handling Instructions
There are no special handling instructions.
Dosage and Administration
The recommended dosage is one 10 mg XATRAL tablet daily to be taken after the same meal each day.
The recommended dosage is one 10 mg XATRAL tablet daily after a meal to be taken from the first day of catheterization and continued beyond catheter removal unless there is a relapse of acute urinary retention or disease progression.
The tablet should be swallowed whole. Any other mode of administration, such as crunching, crushing, chewing, grinding or pounding to powder should be prohibited. These actions may lead to an inappropriate release and absorption of the drug and therefore possible early adverse reactions.
Cases of intraoperative floppy iris syndrome have been reported (see Warnings and Precautions, Ophthalmologic).
Cases of priapism have been reported.
The following adverse events have also been reported in postmarketing experience: The following frequency rating is used; very common (≥10%), Common (≥1% and <10%), Uncommon (≥0.1% and <1%), Rare (≥0.01% and <0.1%), Very rare (<0.01%).
Uncommon: edema, chest pain.
Uncommon: tachycardia. Very Rare: angina pectoris in patients with pre-existing coronary artery disease (see also Warnings and Precautions, Cardiovascular). Isolated spontaneous cases of QT interval prolongation, ventricular arrhythmias, including Torsade de Pointes, ventricular tachycardia and fibrillation have been reported particularly in patients with preexisting cardiovascular diseases; however, a relationship between these adverse events and the XATRAL treatment was not clearly established due to concomitant cardiac disorders, concomitant medications or absence of pre-treatment ECG measurement.
Cases of hepatocellular injury and cholestatic liver disease have been reported.
Dizziness and headache are the most frequent adverse drug reactions with XATRAL.
XATRAL was associated with a low incidence of postural symptoms. As with all alpha1-blockers, there is also a potential for syncope.
XATRAL was not associated with deleterious effects on sexual function.
A subset of patients from Study 1 had blood pressure measurements 12 to 16 hours after the first dose to assess the potential to produce orthostatic hypotension. None of the 35 XATRAL treated patients showed a positive test for systolic, diastolic, or orthostatic blood pressure change.
No age effect on the overall incidence of patients reporting adverse events was observed in the XATRAL group; elderly patients (≥65 years) did not experience more vasodilatory adverse events than the younger patients.
Uncommon: rash, pruritus. Very rare: urticaria, angioedema.
Indications and Clinical Use
XATRAL has been found to be safe and effective when administered at the therapeutic dose (10 mg once-daily) to patients over the age of 65 years.
XATRAL is not indicated for use in children.
XATRAL is not indicated nor recommended for use in women.
For management of a suspected drug overdose, CPhA recommends that you contact your regional Poison Control Centre. See the eCPS Directories section for a list of Poison Control Centres.
Should overdose of XATRAL lead to hypotension, support of the cardiovascular system is of first importance. Restoration of blood pressure and normalization of heart rate may be accomplished by keeping the patient in the supine position. If this measure is inadequate, then the administration of intravenous fluids should be considered. If necessary, vasopressor should then be used and the renal function should be monitored and supported as needed. XATRAL is 87% (82-90%) protein-bound, therefore, dialysis may not be of benefit.
Dosage Forms, Composition and Packaging
Each once-daily, prolonged-release, three-layer, round and biconvex tablet, contains: alfuzosin HCl 10 mg in a white matrix layer between two inactive yellow layers. Nonmedicinal ingredients: colloidal hydrated silica, ethylcellulose, hydrogenated castor oil, hydroxypropyl methylcellulose (hypromellose), magnesium stearate, mannitol, microcrystalline cellulose, povidone and yellow ferric oxide. High Density Polyethylene (HDPE) bottles of 100.
Warnings and Precautions
The pharmacokinetic parameters (Cmax and AUC) are not increased in elderly patients when compared to healthy male volunteers. XATRAL has been found to be a safe and effective alpha1-blockers when administered at the therapeutic dose (10 mg once-daily) to patients over the age of 65 years.
Prostatic carcinoma: Carcinoma of the prostate and BPH cause many of the same symptoms. These two diseases frequently coexist. Therefore, patients thought to have BPH should be examined prior to starting therapy with XATRAL to rule out the presence of carcinoma of the prostate.
Patients with known hypersensitivity to alpha1-blockers should be closely monitored while on XATRAL.
There are no data available on the effect on driving vehicles. Adverse reactions such as vertigo, dizziness and asthenia may occur essentially at the beginning of treatment. This has to be taken into consideration when driving vehicles and operating machines.
Patient should be warned that the tablet should be swallowed whole. Any other mode of administration, such as crunching, crushing, chewing, grinding or pounding to powder should be prohibited. These actions may lead to inappropriate release and absorption of the drug and therefore possible early adverse reactions (see Dosage and Administration, Administration).
XATRAL is not indicated for use in children.
Intraoperative Floppy Iris Syndrome (IFIS, a variant of small pupil syndrome) has been observed during cataract surgery in some patients on or previously treated with some alpha-1-blockers. Cases of IFIS have been observed with XATRAL use. Ophthalmic surgeons should be informed in advance of cataract surgery of current or past use of alpha-1-blockers, as IFIS may lead to increased procedural complications. The ophthalmologists should be prepared for possible modifications to their surgical technique.
XATRAL is not indicated nor recommended for use in women. No embryotoxic and/or teratogenic effects in the rat and rabbit were observed with XATRAL. Parameters of male and female fertility, parturition, lactation and pup development were not modified by XATRAL.
XATRAL is not indicated nor recommended for use in women. It is unknown if the drug is excreted in human milk.
XATRAL is not indicated for the treatment of hypertension.
As with all alpha1-blockers in some patients, in particular, patients receiving antihypertensive medications, postural hypotension with or without dizziness or other symptoms may develop within a few hours following administration of XATRAL. However, these effects are usually transient, occur at the beginning of treatment and do not usually prevent the continuation of treatment. In such cases, the patients should lie down until the symptoms have completely disappeared. As with other alpha1-blockers (alpha1-adrenergic blocking agents), there is a potential for syncope. Patients beginning treatment should be warned of the possible occurrence of such events.
Care should be taken when XATRAL is administered to patients with symptomatic orthostatic hypotension or patients who have had a pronounced hypotensive response to another alpha1-blocker.
As with all alpha1-blockers, alfuzosin has been observed to increase heart rate. Caution should be taken in patients with histories of tachyarrhythmia or with certain cardiovascular conditions, such as myocardial ischemia. The heart rate increasing effects of alfuzosin are additive to those of other heart rate increasing drugs (see Drug Interactions).
Coronary insufficiency: Specific treatment for coronary insufficiency should be continued; however, if angina pectoris reappears or becomes worse, XATRAL should be discontinued.
Patients with congenital QTc prolongation, with a known history of acquired QTc prolongation or who are taking drugs known to increase the QTc interval should be evaluated before and during the administration of alfuzosin.
Co-administration of alfuzosin with a drug known to be a QTc prolonging drug should be evaluated by the physician based on individual patient’s condition (see Action and Clinical Pharmacology, Pharmacodynamics, Electrocardiography).
Storage and Stability
Store at room temperature (15-30°C). Keep in a safe place out of the reach of children.
Action and Clinical Pharmacology
The volume of distribution calculated following intravenous administration is 2.5 L/kg which indicates a distribution into extracellular fluids of the body. XATRAL is moderately bound to plasma proteins with the free fraction accounting for 13.3% in healthy volunteers. Fractions bound to serum albumin and α1-glycoproteins are 68.2 and 52.5%, respectively. Salicylic acid, hydrochlorothiazide, diltiazem, digoxin and indomethacin does not affect the binding of XATRAL to human plasma proteins. Based on in vivo data, it is not likely that XATRAL will affect the extent of binding of these drugs to human plasma proteins. There is an increase in free fraction in renal insufficiency patients (16.8%) and in patients with hepatic disease (20.8%).
The XATRAL tablet is based on the GEOMATRIX System, a patented prolonged-release technology designed to provide a sustained and continuous delivery of the active ingredient consistent with a once-daily administration. The pharmacokinetic properties of this system have been evaluated in healthy adult volunteers after single and/or multiple administrations with daily doses ranging from 7.5 mg to 30 mg, and in patients with BPH at doses from 7.5 mg to 15 mg.
Bioavailability is reduced when XATRAL is administered under fasting conditions. A consistent pharmacokinetic profile is obtained when XATRAL is administered following a meal. A mean peak plasma concentration of 12.3±6.6 ng/mL is reached in 6 to 14 hours after a single dose.
Under fed conditions and after repeated doses, mean Cmax and Cthrough values are 13.6 (SD=5.6) and 3.1 (SD=1.6) ng/mL respectively. Mean AUC0-24 is 194 (SD=75) mg.h/mL. A plateau of concentration is observed from 3 to 14 hours with concentrations above 8.1 ng/mL (Cav) for 11 hours.
Following intravenous or oral administration, the elimination of XATRAL is characterized, in healthy young subjects and in the target population, by a terminal half-life of about 4.8 hours and a total clearance of 0.3 L/h/kg.
The apparent half-life of XATRAL is increased to 9.1 hours in healthy middle-aged volunteers and to 10.1 hours in elderly volunteers.
The pharmacokinetic profile of XATRAL administered intravenously is not affected by chronic cardiac insufficiency.
XATRAL undergoes metabolism by the liver, with only 11% of the parent compound being excreted as unchanged in the urine. The metabolites which are all inactive are eliminated in the urine (15-30%) and feces (75-91%). XATRAL is metabolized by three metabolic pathways (oxidation, O-demethylation, N-dealkylation) which are qualitatively identical to those observed in the animal (rat and dog).
CYP3A4 is the principal hepatic enzyme isoform involved in its metabolism.
In placebo-controlled clinical studies in patients with BPH, XATRAL was shown to:
significantly increase urine peak flow rate (Qmax) by 30% which is observed after the first dose.
significantly reduce detrusor pressure and increase bladder capacity.
significantly reduce residual urine volume.
These favourable urodynamic effects lead to an improvement of lower tract irritative and obstructive symptoms without any deleterious effect on sexual function. The Quality of Life Index was also significantly improved by 33% in the XATRAL-treated patients.
In addition, the efficacy of alfuzosin 10 mg OD on peak flow rate and the limited effect on blood pressure have been demonstrated to be related to its pharmacokinetic profile. Moreover, the efficacy on peak flow rate is maintained up to 24 hours after intake.
A lower frequency of acute urinary retention was observed in the alfuzosin treated patient than in the untreated patient.
QT interval prolongation has not been studied in patients with BPH, therefore similar data is not available. This population may suffer from other conditions and have a higher risk to develop QT interval prolongation due to concomitant risk factors or pre-existing cardiovascular disorders. Based on individual patient’s condition, monitoring for ECG abnormalities should be considered by the physician during treatment.
The clinical manifestations of benign prostatic hyperplasia are due to bladder outlet obstruction caused by anatomical (static) and functional (dynamic) factors. The static component is related to an increase in prostate size which may not cause symptoms. The dynamic component is related primarily to an increase in smooth muscle tone in the prostate, prostatic capsule, bladder base, bladder neck, and prostatic urethra. This increased tone is mediated by the activation of α1-adrenoceptors and leads to an increased resistance to urinary voiding and the symptoms of BPH such as a hesitant, interrupted, weak stream; urgency and leaking or dribbling; and/or more frequent urination, especially at night. XATRAL blocks α1-adrenoceptors leading to a relaxation of the smooth muscle in the bladder neck and prostate.
In animal studies, alfuzosin was shown to be functionally uroselective by preferentially decreasing urethral blood pressure over arterial blood pressure. In human tissue, in vitro, alfuzosin has induced preferential α1-adrenoceptor antagonist activity on prostatic cells relative to renal artery cells. This is illustrated in Figure 1.
Compared to healthy middle-aged volunteers, the pharmacokinetic parameters of XATRAL (Cmax and AUC) are not increased in elderly patients.
After a single oral administration of XATRAL in patients with severe hepatic insufficiency, the elimination half-life is prolonged. A two-fold increase in Cmax values and a three-fold increase in the AUC is observed. Bioavailability is increased in comparison with that in healthy volunteers (see Contraindications).
XATRAL, indicated for the treatment of benign prostatic hyperplasia (BPH) and as adjunctive therapy with urethral catheterization for acute urinary retention related to BPH and management following catheter removal, is a uroselective antagonist of post-synaptic α1-adrenoceptors located in the prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra.
Compared to subjects with normal renal function, the mean Cmax and AUC values of XATRAL are moderately increased (1.5- to 1.6-fold) in patients with various stages of renal impairment, with no change in the apparent elimination half-life. This change in the pharmacokinetic profile is not considered clinically relevant; and therefore, does not necessitate a dosing adjustment. XATRAL has not been evaluated in patients with end-stage renal disease.
XATRAL is contraindicated in:
Patients with a known hypersensitivity to XATRAL or to any ingredient in the formulation. For a complete listing, see Dosage Forms, Composition and Packaging.
Patients with moderate to severe hepatic insufficiency, since alfuzosin blood levels are increased in these patients (see Action and Clinical Pharmacology, Pharmacokinetics, Special Populations and Conditions, Hepatic Insufficiency).
Combination with other alpha1-blockers.
Combination with potent CYP3A4 inhibitors such as ketoconazole, ritonavir and itroconazole, because alfuzosin blood levels and exposure (AUC) are increased (see Drug Interactions, Overview).