Alfuzosin

Name: Alfuzosin

What other information should I know?

Keep all appointments with your doctor.

Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.

Do I need a prescription for alfuzosin?

Yes

What are the uses for alfuzosin?

Alfuzosin is used in adult men to treat slow urination due to benign prostatic hyperplasia. Most men experience an improvement in urination in 2 to 3 weeks.

Alfuzosin Food Interactions

Grapefruit and grapefruit juice may interact with alfuzosin and lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor.

Alfuzosin Usage

  • Take alfuzosin exactly as your doctor prescribes it.
  • Take one alfuzosin tablet after the same meal each day. Alfuzosin should be taken just after eating food. Do not take it on an empty stomach.
  • Swallow the alfuzosin tablet whole. Do not crush, split, or chew alfuzosin tablets.
  • If you take too much alfuzosin call your local poison control center or emergency room right away.

What happens if I miss a dose?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What other drugs will affect alfuzosin?

Many drugs can interact with alfuzosin, and some drugs should not be used together. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide. Tell your doctor about all medicines you use, and those you start or stop using during your treatment with alfuzosin. Give a list of all your medicines to any healthcare provider who treats you.

Commonly used brand name(s)

In the U.S.

  • Uroxatral

Available Dosage Forms:

  • Tablet, Extended Release

Therapeutic Class: Benign Prostatic Hypertrophy Agent

Pharmacologic Class: Alpha-1 Adrenergic Blocker

Precautions While Using alfuzosin

It is very important that your doctor check your progress at regular visits to make sure that alfuzosin is working properly and for any problems that may be caused by alfuzosin.

Do not use alfuzosin if you are taking certain medicines such as ketoconazole (Nizoral®), itraconazole (Sporanox®), or ritonavir (Norvir®).

Dizziness, lightheadedness, or fainting may occur after you take alfuzosin, especially when you get up from a lying or sitting position. Getting up slowly may help lessen this problem. If you feel dizzy, lie down so you do not faint. Then sit for a few moments before standing to prevent the dizziness from returning.

alfuzosin may cause some people to become dizzy or less alert than they are normally. Make sure you know how you react to alfuzosin before you drive, use machines, or do anything else that could be dangerous if you are dizzy or are not alert.

You should seek medical attention right away if you experience a prolonged erection. This is an extremely rare side effect, but if it goes untreated, can result in permanent erectile dysfunction (impotence).

Stop using alfuzosin and check with your doctor right away if you have arm, back or jaw pain; chest pain or discomfort; chest tightness or heaviness; fast or irregular heartbeat; nausea; shortness of breath; or sweating.

alfuzosin may affect the results of the prostate specific antigen (PSA) test, which may be used to detect prostate cancer. Make sure you tell all of your doctors that you are using alfuzosin.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

alfuzosin Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

Rare
  • Chest pain
  • chills
  • cold sweats
  • confusion
  • dizziness, faintness, or lightheadedness when getting up from a lying or sitting position
  • fainting
  • fast, pounding, or irregular heartbeat or pulse
  • painful or prolonged erection of the penis
Incidence not known
  • Arm, back, or jaw pain
  • chest discomfort
  • chest tightness or heaviness
  • large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
  • nausea
  • shortness of breath
  • sweating
  • swelling

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common
  • Dizziness
Less common
  • Abdominal or stomach pain
  • acid or sour stomach
  • belching
  • body aches or pain
  • congestion
  • cough
  • cough producing mucus
  • decreased interest in sexual intercourse
  • difficulty breathing
  • difficulty having a bowel movement (stool)
  • dryness or soreness of the throat
  • ear congestion
  • fever
  • headache
  • heartburn
  • hoarseness
  • inability to have or keep an erection
  • indigestion
  • loss in sexual ability, desire, drive, or performance
  • loss of voice
  • nasal congestion
  • pain
  • pain or tenderness around the eyes and cheekbones
  • sneezing
  • sore throat
  • stomach discomfort, upset, or pain
  • stuffy or runny nose
  • tender, swollen glands in the neck
  • tightness in the chest
  • trouble with swallowing
  • unusual tiredness or weakness
  • voice changes
  • wheezing
Rare
  • Rash
Incidence not known
  • Diarrhea
  • feeling of warmth
  • hives or welts
  • itching skin
  • redness of the skin
  • redness of the face, neck, arms, and occasionally, upper chest

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

What are some things I need to know or do while I take Alfuzosin?

  • Tell all of your health care providers that you take alfuzosin. This includes your doctors, nurses, pharmacists, and dentists.
  • Avoid driving and doing other tasks or actions that call for you to be alert until you see how this medicine affects you.
  • To lower the chance of feeling dizzy or passing out, rise slowly if you have been sitting or lying down. Be careful going up and down stairs.
  • If you are having cataract surgery or other eye procedure, talk with your doctor.
  • Have your blood pressure checked often. Talk with your doctor.
  • Have a rectal exam (to check prostate gland) and blood work (PSA test). Talk with your doctor.
  • Talk with your doctor before you drink alcohol.
  • This medicine is not approved for use in children. Talk with the doctor.
  • This medicine is not approved for use in women.
  • Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using alfuzosin while you are pregnant.
  • Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

How is this medicine (Alfuzosin) best taken?

Use this medicine as ordered by your doctor. Read all information given to you. Follow all instructions closely.

  • Take alfuzosin with food with the same meal each day.
  • Swallow whole. Do not chew, break, or crush.
  • Drink lots of noncaffeine liquids unless told to drink less liquid by your doctor.
  • Keep taking this medicine as you have been told by your doctor or other health care provider, even if you feel well.
  • To gain the most benefit, do not miss doses.

What do I do if I miss a dose?

  • Take a missed dose as soon as you think about it.
  • If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
  • Do not take 2 doses at the same time or extra doses.

What are some other side effects of Alfuzosin?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

  • Dizziness.
  • Headache.
  • Feeling tired or weak.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.

Use in specific populations

Pregnancy

Pregnancy Category B. Alfuzosin hydrochloride extended-release tablets are not indicated for use in women, and there are no studies of Alfuzosin in pregnant women.

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.

Pediatric Use

Afluzosin hydrochloride extended-release tablets are not indicated for use in the pediatric population.

Efficacy of Alfuzosin hydrochloride was not demonstrated in a randomized, double-blind, placebo-controlled, efficacy and safety trial conducted in 172 patients ages 2 to 16 years with elevated detrusor leak point pressure (LPP>40 cm H2O) of neurologic origin treated with Alfuzosin hydrochloride using pediatric formulations. The trial included a 12-week efficacy phase followed by a 40-week safety extension period. No statistically significant difference in the proportion of patients achieving a detrusor leak point pressure of <40 cm H2O was observed between the Alfuzosin and placebo groups.

During the placebo-controlled trial, the adverse reactions reported in >2% of patients treated with Alfuzosin and at a higher incidence than in the placebo group were: pyrexia, headache, respiratory tract infection, cough, epistaxis and diarrhea. The adverse reactions reported for the whole 12-month trial period, which included the open-label extension, were similar in type and frequency to the reactions observed during the 12-week period.

Alfuzosin hydrochloride was not studied in patients below the age of 2.

Geriatric Use

Of the total number of subjects in clinical studies of Alfuzosin hydrochloride extended-release tablets, 48% were 65 years of age and over, whereas 11% were 75 and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, but greater sensitivity of some older individuals cannot be ruled out [see Clinical Pharmacology (12.3)]

Renal Impairment

Systemic exposure was increased by approximately 50% in pharmacokinetic studies of patients with mild, moderate, and severe renal impairment [see Clinical Pharmacology (12.3)]. In phase 3 studies, the safety profile of patients with mild (n=172) or moderate (n=56) renal impairment was similar to the patients with normal renal function in those studies. Safety data are available in only a limited number of patients (n=6) with creatinine clearance below 30 mL/min; therefore, caution should be exercised when Alfuzosin hydrochloride extended-release tablets are administered in patients with severe renal impairment [see Warnings and Precautions (5.2)].

Hepatic Impairment

The pharmacokinetics of Alfuzosin hydrochloride extended-release tablets have not been studied in patients with mild hepatic impairment. Alfuzosin hydrochloride extended-release tablets are contraindicated for use in patients with moderate or severe hepatic impairment [see Contraindications (4), Warnings and Precautions (5.3) and Clinical Pharmacology (12.3)].

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

There was no evidence of a drug-related increase in the incidence of tumors in mice following dietary administration of 100 mg/kg/day Alfuzosin for 98 weeks (13 and 15 times the maximum recommended human dose [MRHD] of 10 mg based on AUC of unbound drug), in females and males, respectively. The highest dose tested in female mice may not have constituted a maximally tolerated dose. Likewise, there was no evidence of a drug-related increase in the incidence of tumors in rats following dietary administration of 100 mg/kg/day Alfuzosin for 104 weeks (53 and 37 times the MRHD in females and males, respectively).

Alfuzosin showed no evidence of mutagenic effect in the Ames and mouse lymphoma assays, and was free of any clastogenic effects in the Chinese hamster ovary cell and in vivo mouse micronucleus assays. Alfuzosin treatment did not induce DNA repair in a human cell line.

There was no evidence of reproductive organ toxicity when male rats were administered oral doses of several hundred times (250 mg/kg/day for 26 weeks) the MRHD of Alfuzosin. No impairment of fertility was observed following oral (gavage) administration to male rats at doses of up to 125 mg/kg/day for 70 days. Estrous cycling was inhibited in rats and dogs at approximately 12 and 18 times the MRHD respectively (doses of 25 mg/kg and 20 mg/kg, respectively), but did not result in impaired fertility in female rats.

How Supplied/Storage and Handling

Afluzosin Hydrochloride Extended-Release Tablets, USP 10 mg

White, round, beveled edged tablets with '155' debossed on one side and 'U' debossed on other side.

Bottles of 30   : NDC 29300-155-13

Bottles of 90   : NDC 29300-155-19

Bottles of 100 : NDC 29300-155-01

Store at 200 to 250C (680 to 770F) [see USP Controlled Room Temperature].

Protect from light and moisture.

Keep this and all drugs out of reach of children.

Brand Names U.S.

  • Uroxatral

Pharmacology

An antagonist of alpha1-adrenoreceptors in the lower urinary tract. Smooth muscle tone is mediated by the sympathetic nervous stimulation of alpha1-adrenoreceptors, which are abundant in the prostate, prostatic capsule, prostatic urethra, and bladder neck. Blockade of these adrenoreceptors can cause smooth muscles in the bladder neck and prostate to relax, resulting in an improvement in urine flow rate and a reduction in BPH symptoms.

Absorption

Decreased 50% under fasting conditions

Distribution

Vd: 3.2 L/kg

Metabolism

Hepatic, primarily via CYP3A4; metabolism includes oxidation, O-demethylation, and N-dealkylation; forms metabolites (inactive)

Excretion

Feces (69%); urine (24%; 11% as unchanged drug)

Time to Peak

Plasma: 8 hours following a meal

Half-Life Elimination

10 hours

Protein Binding

82% to 90%

Dosing Adult

Benign prostatic hyperplasia (BPH): Oral: 10 mg once daily

Ureteral stones, expulsion (off-label use): Oral: 10 mg once daily, discontinue after successful expulsion (average time to expulsion 1-2 weeks) (Agrawal, 2009; Ahmed, 2010; Gurbuz, 2011). Note: Patients with stones >10 mm were excluded from studies.

Liver Dose Adjustments

Severe hepatic insufficiency: Contraindicated

Precautions

This drug is not recommended for use in children.

Consult WARNINGS section for additional precautions.

Other Comments

Patient advice:
-Patients (especially those receiving antihypertensive medications), should be counseled on the possibility of orthostatic hypotension with or without symptoms occurring within a few hours following administration. The patient should be advised to lie down until the symptoms have disappeared. These effects are usually transient, occur at the beginning of treatment, and do not generally affect continuation of treatment.
-Patients should be advised that side effects including vertigo, dizziness, and asthenia may occur primarily at the beginning of treatment and may affect their ability to drive vehicles or operate machinery. They should not undertake such activities until they know how alfuzosin affects them.
-Tablets should not be chewed or crushed.
-Patients with hereditary problems of galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption should not take this medicine.
-Alfuzosin should be administered after the same meal each day.

Alfuzosin Breastfeeding Warnings

This drug is not indicated for use in female patients. Excreted into human milk: Unknown Excreted into animal milk: Unknown

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