Alfuzosin Hcl
FDA Drug Information • Also known as: Uroxatral
- Brand Names
- Uroxatral
- Route
- ORAL
- Dosage Form
- TABLET, EXTENDED RELEASE
- Product Type
- HUMAN PRESCRIPTION DRUG
Description
11 DESCRIPTION Each UROXATRAL extended-release tablet contains 10 mg alfuzosin hydrochloride as the active ingredient. Alfuzosin hydrochloride is a white to off-white crystalline powder that melts at approximately 240°C. It is freely soluble in water, sparingly soluble in alcohol, and practically insoluble in dichloromethane. Alfuzosin hydrochloride is (R,S)-N-[3-[(4-amino-6,7-dimethoxy-2-quinazolinyl) methylamino] propyl] tetrahydro-2-furancarboxamide hydrochloride. The empirical formula of alfuzosin hydrochloride is C 19 H 27 N 5 O 4
What Is Alfuzosin Hcl Used For?
1 INDICATIONS AND USAGE UROXATRAL is indicated for the treatment of signs and symptoms of benign prostatic hyperplasia. UROXATRAL is an alpha adrenergic antagonist, indicated for the treatment of signs and symptoms of benign prostatic hyperplasia. ( 1 ) Important Limitations of Use: UROXATRAL is not indicated for treatment of hypertension. ( 1.1 ) UROXATRAL is not indicated for use in the pediatric population. ( 1.1 , 8.4 , 12.3 ) 1.1 Important Limitations of Use UROXATRAL is not indicated for the treatment of hypertension. UROXATRAL is not indicated for use in the pediatric population.
Dosage and Administration
2 DOSAGE AND ADMINISTRATION The recommended dosage is one 10 mg UROXATRAL (alfuzosin HCl) extended-release tablet once daily. The extent of absorption of alfuzosin is 50% lower under fasting conditions. Therefore, Uroxatral should be taken with food and with the same meal each day. The tablets should not be chewed or crushed. 10 mg once daily with food and with the same meal each day. ( 2 ) Tablets should not be chewed or crushed ( 2 , 12.3 )
Side Effects (Adverse Reactions)
6 ADVERSE REACTIONS Most common adverse reactions in clinical studies (incidence ≥2% and at a higher incidence than placebo): dizziness, upper respiratory tract infection, headache, fatigue. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Advanz Pharma (US) Corp. at 1-877-370-1142 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience 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 clinical practice. The incidence of adverse reactions has been ascertained from 3 placebo-controlled clinical trials involving 1,608 men where daily doses of 10 and 15 mg alfuzosin were evaluated. In these 3 trials, 473 men received UROXATRAL (alfuzosin HCl) 10 mg extended-release tablets. In these trials, 4% of patients taking UROXATRAL (alfuzosin HCl) 10 mg extended-release tablets withdrew from the trial due to adverse reactions, compared with 3% in the placebo group. Table 1 summarizes adverse reactions that occurred in ≥2% of patients receiving UROXATRAL, and at a higher incidence than that of the placebo group. In general, the adverse reactions seen in long-term use were similar in type and frequency to the events described below for the 3-month trials. Table 1 — Adverse Reactions Occurring in ≥2% of UROXATRAL-Treated Patients and More Frequently than with Placebo in 3-Month Placebo-Controlled Clinical Trials Adverse Reaction Placebo (n=678) UROXATRAL (n=473) Dizziness 19 (2.8%) 27 (5.7%) Upper respiratory tract infection 4 (0.6%) 14 (3.0%) Headache 12 (1.8%) 14 (3.0%) Fatigue 12 (1.8%) 13 (2.7%) The following adverse reactions, reported by between 1% and 2% of patients receiving UROXATRAL and occurring more frequently than with placebo, are listed alphabetically by body system and by decreasing frequency within body system: Body as a whole: pain Gastrointestinal system: abdominal pain, dyspepsia, constipation, nausea Reproductive system: impotence Respiratory system: bronchitis, sinusitis, pharyngitis Signs and Symptoms of Orthostasis in Clinical Trials: The adverse reactions related to orthostasis that occurred in the double-blind phase 3 trials with alfuzosin 10 mg are summarized in Table 2. Approximately 20% to 30% of patients in these trials were taking antihypertensive medication. Table 2— Number (%) of Patients with Symptoms Possibly Associated with Orthostasis in 3-Month Placebo-Controlled Clinical Trials Symptoms Placebo (n=678) UROXATRAL (n=473) Dizziness 19 (2.8%) 27 (5.7%) Hypotension or postural hypotension 0 2 (0.4%) Syncope 0 1 (0.2%) Testing for blood pressure changes or orthostatic hypotension was conducted in three controlled studies. Decreased systolic blood pressure (≤90 mm Hg, with a decrease ≥20 mm Hg from baseline) was observed in none of the 674 placebo patients and 1 (0.2%) of the 469 UROXATRAL patients. Decreased diastolic blood pressure (≤50 mm Hg, with a decrease ≥15 mm Hg from baseline) was observed in 3 (0.4%) of the placebo patients and in 4 (0.9%) of the UROXATRAL patients. A positive orthostatic test (decrease in systolic blood pressure of ≥20 mm Hg upon standing from the supine position) was seen in 52 (7.7%) of placebo patients and in 31 (6.6%) of the UROXATRAL patients. 6.2 Post-Marketing Experience The following adverse reactions have been identified during post approval use of UROXATRAL. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. General disorders: edema Cardiac disorders: tachycardia, chest pain, angina pectoris in patients with pre-existing coronary artery disease, atrial fibrillation Gastrointestinal disorders: diarrhea, vomiting Hepatobiliary disorders: hepatocellular and cholestatic liver injury (including...
Drug Interactions
7 DRUG INTERACTIONS Concomitant use of PDE5 inhibitors with alpha adrenergic antagonists, including UROXATRAL, can potentially cause symptomatic hypotension ( 5.4 , 7.4 ) 7.1 CYP3A4 Inhibitors UROXATRAL is contraindicated for use with potent CYP3A4 inhibitors such as ketoconazole, itraconazole, or ritonavir, since alfuzosin blood levels are increased [see Contraindications (4) , Warnings and Precautions (5.4) and Clinical Pharmacology (12.3) ] . 7.2 Alpha Adrenergic Antagonists The pharmacokinetic and pharmacodynamic interactions between UROXATRAL and other alpha adrenergic antagonists have not been determined. However, interactions may be expected, and UROXATRAL should not be used in combination with other alpha adrenergic antagonists [see Warnings and Precautions (5.4) ]. 7.3 Antihypertensive Medication and Nitrates There may be an increased risk of hypotension/postural hypotension and syncope when taking UROXATRAL concomitantly with anti-hypertensive medication and nitrates [see Warnings and Precautions (5.1) ] . 7.4 PDE5 Inhibitors Caution is advised when alpha adrenergic antagonists, including UROXATRAL, are co-administered with PDE5 inhibitors. Alpha adrenergic antagonists and PDE5 inhibitors are both vasodilators that can lower blood pressure. Concomitant use of these two drug classes can potentially cause symptomatic hypotension [see Warnings and Precautions (5.4) ] .
Contraindications
4 CONTRAINDICATIONS UROXATRAL is contraindicated for use: in patients with moderate or severe hepatic impairment (Childs-Pugh categories B and C), since alfuzosin blood levels are increased in these patients [see Use in Specific Populations (8.7) and Clinical Pharmacology (12.3) ]. with potent CYP3A4 inhibitors such as ketoconazole, itraconazole, and ritonavir, since alfuzosin blood levels are increased [see Drug Interactions (7.1) and Clinical Pharmacology (12.3) ] . in patients with known hypersensitivity, such as urticaria and angioedema, to alfuzosin hydrochloride or any component of UROXATRAL tablets [see Adverse Reactions (6.2) ] Moderate or severe hepatic impairment ( 4 , 8.7 , 12.3 ) Co-administration with potent CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, ritonavir) ( 4 , 5.4 , 7.1 , 12.3 ) Known hypersensitivity (e.g., urticaria or angioedema) to alfuzosin or any of the ingredients ( 4 , 6.2 )
Pregnancy and Breastfeeding
8.1 Pregnancy Risk Summary Uroxatral is not indicated for use in women. There are no adequate data on the developmental risk associated with use of UROXATRAL in pregnant women. Based on findings from animal studies, alfuzosin administered during the period of organogenesis was not teratogenic, embryotoxic or fetotoxic at upto 1200 times the MRHD of 10 mg via AUC in rats and 3 times in rabbit, via body surface area. In the U.S. general population, the estimated background risk of major birth defects and miscarriages in clinically recognized pregnancies is 2 to 4% and 15 to 20% respectively. Data Animal data Alfuzosin was not teratogenic, embryotoxic or fetotoxic in rats at plasma exposure levels (based on AUC of unbound drug) up to 1200 times (maternal oral dose of 250 mg/kg/day) the maximum recommended human dose (MRHD) of 10 mg. In rabbits administered up to 3 times the MRHD (based on body surface area) (maternal oral dose of 100 mg/kg/day) no embryofetal toxicity or teratogenicity was observed. Gestation was slightly prolonged in rats at exposure levels (based on AUC of unbound drug) approximately 12 times (greater than 5 mg/kg/day oral maternal dose) the MRHD, but difficulties with parturition were not observed.
Overdosage
10 OVERDOSAGE Should overdose of UROXATRAL 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, vasopressors should then be used, and the renal function should be monitored and supported as needed. Alfuzosin is 82% to 90% protein bound; therefore, dialysis may not be of benefit.
How Supplied
16 HOW SUPPLIED/STORAGE AND HANDLING UROXATRAL is supplied as follows: Package NDC Number Bottles of 100 with child-resistant closure, NDC 59212-200-10 Bottles of 30 with child-resistant closure, NDC 59212-200-30 UROXATRAL (alfuzosin HCl) extended-release tablet 10 mg is available as a round, three-layer tablet: one white layer between two yellow layers, debossed with X10. Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as described in the USP. Protect from light and moisture. Keep UROXATRAL out of reach of children.
About This Information
This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.
What are side effects?
Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.
What are drug interactions?
Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.