Afzoline XL 10

Alfuzosin hydrochloride.

Each prolonged release tablet contains alfuzosin hydrochloride 10 mg.

Pharmacodynamics: An antagonist of alpha₁-adrenoreceptor in the lower urinary tract. Blockage 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.
Pharmacokinetics: Absorption: Decrease 50% under fasting conditions.
Distribution: V_d: 3.2 L/kg.
Protein binding: 82% to 90%.
Metabolism: Hepatic, primarily via CYP3A4.
Bioavailability: 49% following a meal.
Half-life elimination: 10 hours.
Time to peak, plasma: 8 hours following a meal.
Excretion: Feces (69%); urine (24%; 11% as unchanged drug).

Treatment of the functional symptoms of benign prostatic hyperplasia (BPH).

Recommended dose: Oral: 10 mg once daily. Tablet should be swallowed whole; do not crush or chew.
Administer immediately following a meal; should be taken at the same time each day.
Safety and effectiveness are not established in children.
Renal impairment: Bioavailability and maximum serum concentrations are increased with mild (CrCl 60-80 mL/minute), moderate (CrCl 30-59 mL/minute), or severe (CrCl <30 mL/minute) renal impairment.
Safety data is limited in patients with severe renal impairment (CrCl <30 mL/minute). Use with caution.
Hepatic impairment: Mild hepatic impairment: Use has not been studied; use with caution.
Moderate or severe hepatic impairment (Child-Pugh class B or C): Use is contraindicated.

Mild to moderate toxicity: Orthostatic hypotension, reflex tachycardia, nausea, vomiting, and dizziness are common; syncope and mild sedation may develop.
Severe toxicity: Hypotension, torsades de pointes, agitation, seizure, and priapism have been reported. Hypotension is generally not life-threatening.
Management of mild to moderate toxicity: Hypotension usually responds to IV fluids.
Management of severe toxicity: Hypotension that does not respond to IV fluids should be treated with adrenergic vasopressors such as phenylephrine or norepinephrine. Intubate patients with significant CNS depression. Treat seizures with benzodiazepines; add propofol or barbiturate if seizure persist or recur.

Hypersensitivity to alfuzosin or any component of the formulation.
Concurrent use with potent CYP3A4 inhibitors (eg. ketoconazole, itraconazole, ritonavir) or other alpha₁-blocking agents.
Moderate or severe hepatic insufficiency (Child-Pugh class B or C).
Severe kidney failure (creatinine clearance <30 ml/min).
Postural hypotension.

Postural hypotension may occur with potential for syncope, especially in patients with a history of symptomatic hypotension, who have had a hypotensive response to other medications, or who are receiving concurrent antihypertensive medications or nitrates.
Risk of new or worsening angina pectoris; discontinue.
Use caution in patients with acquired or congenital QT prolongation or in those taking other medication known to prolong the QT interval.
Use with other alpha-blockers is not recommended.
Use with caution in patients with mild hepatic impairment.
Intraoperative floppy iris syndrome has been reported during cataract surgery; modification to surgical technique may be necessary.
Use with caution in patients with severe renal impairment (CrCl <30 mL/minute).
Rule out carcinoma of the prostate prior to initiating therapy for benign prostatic hypertrophy; both conditions may present with the same symptoms.
Priapism has been reported and may lead to permanent impotence if not treated immediately.
Effects on ability to drive and use machines: There are no data available on the effect on driving vehicles. Particular caution is required when driving vehicles or using machines due to the risks of postural hypotension, vertigo, dizzy sensations, asthenia, visual disturbances, especially at the start of treatment with alfuzosin.

Alfuzosin is not indicated in women.
Pregnancy Risk Factor B.
Animal studies have revealed no evidence of harm to fetus, however, there are no adequate and well-controlled studies in pregnant women.

Central nervous system: Dizziness, fatigue, headache, pain.
Gastrointestinal: Abdominal pain, constipation, dyspepsia, nausea.
Genitourinary: Impotence.
Respiratory: Bronchitis, pharyngitis, sinusitis, upper respiratory tract infection.
Rare but important or life-threatening: Angioedema, atrial fibrillation, chest pain, edema, hepatic injury (including cholestatic), hypotension, intraoperative floppy iris syndrome (with cataract surgery), priapism, pruritus, thrombocytopenia, toxic epidermal necrolysis.

Concurrent use of mesoridazine, thioridazine, piperaquine, dronedarone, cisapride, pimozide, ziprasidone, bepridil, amifampridine, terfenadine, sparfloxacin, hydroxychloroquine, zuclopenthixol, fluoxetine, metronidazole, anagrelide, selected gonadotropin releasing hormone agonists, clozapine, escitalopram, moxifloxacin, dabrafenib, tizanidine, pasireotide, ivabradine, panobinostat, pitolisant, vinflunine, amiodarone, pimavanserin, tacrolimus, crizotinib, levofloxacin, quetiapine, aripiprazole, sevoflurane, delamanid, or bedaquiline and QT interval prolonging drugs may result in increased risk of QT interval prolongation.
Concurrent use of alfuzosin and ketoconazole, atazanavir, fosamprenavir, saquinavir, itraconazole, ritonavir, nelfinavir, idelalisib, boceprevir, telaprevir, tipranavir, indinavir, cobicistat, diltiazem, cyclosporine, delavirdine, erythromycin, nefazodone, voriconazole, imatinib, amprenavir, quinupristin/dalfopristin, or cimetidine may result in an increased alfuzosin plasma concentrations.
Concurrent use of alfuzosin and lopinavir/ritonavir, fluconazole, protriptyline, amoxapine, or toremifene may result in an increase in alfuzosin exposure and result in an increased risk of torsades de pointes.
Concurrent use of alfuzosin and posaconazole, telithromycin, clarithromycin, salmeterol, granisetron, azithromycin, trimipramine, astemizole, perflutren lipid microsphere, chlorpromazine, dasatinib, clomipramine, gatifloxacin, trifluoperazine, flecainide, propafenone, vandetanib, ranolazine, mefloquine, telavancin, trazodone, domperidone, ciprofloxacin, sodium phosphate, ondansetron, pazopanib, haloperidol, dofetilide, ofloxacin, lapatinib, asenapine, ibutilide, fingolimod, apomorphine, chloroquine, sorafenib, paliperidone, gemifloxacin, artemether/lumefantrine, tetrabenazine, nortriptyline, disopyramide, prochlorperazine, citalopram, procainamide, amitriptyline, desipramine, norfloxacin, quinine, quinidine, vemurafenib, imipramine, sunitinib, dolasetron, arsenic trioxide, promethazine, droperidol, solifenacin, iloperidone, or halofantrine may result in increased alfuzosin plasma concentrations and an increased risk of QT interval prolongation.
Concurrent use of alfuzosin and darunavir may result in an increase in alfuzosin levels, thereby increasing the risk for serious and/or life-threatening reactions.
Concurrent use of amisulpride, or sulpiride and QT prolonging agents are contraindicated and may result in increased risk of torsade de pointes.
Concurrent use of alfuzosin and tadalafil may result in potentiation of hypotensive effects.
Concurrent use of donepezil and QT prolonging agents may result in increased risk of QT interval prolongation and torsade de pointes.
Concurrent use of nilotinib and selected CYP3A4 substrates that prolong the QT interval may result in increased exposure of CYP3A4 substrate and increased risk of QT interval prolongation.
Concurrent use of vardenafil or sildenafil and alpha₁-adrenergic blockers may result in potentiation of hypotensive effects.
Concurrent use of alpha₁-adrenergic blockers and beta-adrenergic blockers may result in an exaggerated hypotension response to first dose of the alpha-blocker.
Concurrent use of alfuzosin and avanafil may result in increased risk of hypotension.
Concurrent use of yohimbine, or ma huang and alpha₁-adrenergic blockers may result in reduced effectiveness of alpha₁-adrenergic blockers.

Store below 30°C.

Drugs for Bladder & Prostate Disorders

G04CA01 - alfuzosin ; Belongs to the class of alpha-adrenoreceptor antagonists. Used in the treatment of benign prostatic hypertrophy.

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