Alfuzosin

Oral
Benign prostatic hyperplasia

Oral
Acute urinary retention associated with benign prostatic hyperplasia

Benign prostatic hyperplasia:
As conventional tab: Initially, 2.5 mg bid, adjust according to response. As extended-release tab: Mild to moderate: 5 mg once daily, adjust according to response. Severe (CrCl <30 mL/min): Contraindicated.

Acute urinary retention associated with benign prostatic hyperplasia:
Elderly: Severe (CrCl <30 mL/min): Contraindicated.

Benign prostatic hyperplasia:
As conventional tab: Mild to moderate: Initially, 2.5 mg once daily, may increase to bid according to response. As extended-release tab: Severe (Child-Pugh class C): Contraindicated.

Acute urinary retention associated with benign prostatic hyperplasia:
Elderly: Severe (Child-Pugh class C): Contraindicated.

Should be taken with food.
extended-release: Should be taken with food. Take immediately after the same meal each day. Swallow whole, do not chew/crush.

History of orthostatic hypotension. Severe hepatic and renal impairment. Concomitant use with other α₁-receptor blockers and potent CYP3A4 inhibitors.

Patient with acute cardiac failure, history of tachyarrhythmia or certain CV disease (e.g. myocardial ischaemia), QT prolongation (congenital or acquired), or taking medications that prolong QT interval. Patient undergoing cataract surgery. Mild to moderate renal and hepatic impairment. Not intended for the treatment of hypertension. Not intended for use in women and children. Elderly.

Significant: Angina, CNS depression, intraoperative floppy iris syndrome (cataract surgery patients), orthostatic hypotension, syncope, risk of cerebral ischaemic disorders. Rarely, priapism.
Cardiac disorders: Tachycardia.
Eye disorders: Visual disturbances.
Gastrointestinal disorders: Nausea, diarrhoea, dry mouth, abdominal pain, dyspepsia.
General disorders and admin site conditions: Asthenia, malaise, oedema, chest pain.
Nervous system disorders: Dizziness, vertigo, headache.
Respiratory, thoracic and mediastinal disorders: Rhinitis.
Skin and subcutaneous tissue disorders: Rash, pruritus.
Vascular disorders: Flushing.

PO: B

This drug may cause dizziness or weakness, if affected, do not drive or operate machinery.

Rule out prostatic carcinoma before initiation of therapy (many symptoms of BPH and prostate cancer are similar). Monitor blood pressure (regularly, especially at the beginning of therapy), urine flow, and prostate-specific antigen (PSA).

Symptom: Hypotension. Management: Maintain the patient in a supine position to restore blood pressure and normalise the heart rate. IV fluids and/or vasopressors may also be needed.

May enhance the hypotensive effect of antihypertensive agents, nitrates (e.g nitroglycerin, isosorbide dinitrate,) and phosphodiesterase-5 inhibitors (e.g. sildenafil, tadalafil). Administration with general anaesthesia may result in blood pressure instability.
Potentially Fatal: Enhanced hypotensive effect with other α₁-blockers (e.g. tamsulosin). Increased serum concentration with potent CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, ritonavir, clarithromycin, telithromycin, nefazodone, nelfinavir).

Food increases the extent of absorption.

Description:
Mechanism of Action: Alfuzosin, a quinazoline derivative that selectively blocks α₁-receptors in the lower urinary tract which causes smooth muscle relaxation in the prostate and bladder neck, resulting in the improvement of urine flow and reduction of symptoms in benign prostatic hyperplasia (BPH).
Pharmacokinetics:
Absorption: Readily absorbed from the gastrointestinal tract. Food increases absorption. Bioavailability: 49% following a meal. Time to peak plasma concentration: 8 hours following a meal.
Distribution: Volume of distribution: 3.2 L/kg. Plasma protein binding: 82-90%.
Metabolism: Extensively metabolised in the liver by CYP3A4 isoenzymes via oxidation, O-demethylation, and N-dealkylation into inactive metabolites.
Excretion: Mainly via faeces (69%); urine (24%; 11% as unchanged drug). Elimination half-life: 10 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 2092, Alfuzosin. https://pubchem.ncbi.nlm.nih.gov/compound/Alfuzosin. Accessed Mar. 29, 2022.

Store below 30°C. Protect from light and moisture.

Thuốc trị các rối loạn ở bàng quang & tuyến tiền liệt

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

Anon. Alfuzosin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 10/02/2022.

Buckingham R (ed). Alfuzosin Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/02/2022.

Joint Formulary Committee. Alfuzosin Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/02/2022.

Preston CL (ed). Alfuzosin Drug Interactions. Stockley’s Drug Interactions [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/02/2022.

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Xatral 2.5 mg Film Coated Tablet (Aventis Pharma Limited). MHRA. https://products.mhra.gov.uk. Accessed 10/02/2022.

Xatral XL 10 mg (Sanofi Winthrop Industrie). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 10/02/2022.

Zochek 10 mg Prolonged-Release Tablets (Milpharm Limited). MHRA. https://products.mhra.gov.uk. Accessed 10/02/2022.