Film-coated tablet contains:
Alfuzosin Hydrochloride BP...10 mg
Colour: Yellow Iron Oxide NF and Titanium Dioxide BP
CHEMICAL NAME: (RS)-N43-[(4-amino-6,7-dimethoxyquinazolin-2- y1) (methyl)amino]propyl] tetrahydrofuran-2-carboxamide hydrochloride
CATEGORY: Alp hal -adrenoceptor antagonist
DESCRIPTION: Light yellow to yellow coloured round, biconvex film-coated tablet plain on both sides.
MECHANISM OF ACTION:
Alfuzosin is a selective antagonist of post-synaptic alpha1- adrenoreceptors, which are located in the prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra. Alfuzosin exhibits selectivity for alpha adrenergic receptors in the lower urinary tract. Blockade of these adrenoreceptors can cause smooth muscle in the bladder neck and prostate to relax, resulting in an improvement in urine flow and a reduction in symptoms of BPH.
The reported absolute bioavailability of alfuzosin hydrochloride prolonged-release 10 mg tablets under fed conditions is 49%. Following multiple dosing of 10 mg alfuzosin hydrochloride extended-release tablets under fed conditions, the time to maximum concentration is 8 hours. Cmax and AUCO-24 are 13.6 (SD = 5.6) ng/ml and 194 (SD = 75) ng/h/ml, respectively. Alfuzosin hydrochloride extended release tablets exhibit linear kinetics following single and multiple dosing up to 30 mg. Steady- state plasma levels are reached with the second dose of alfuzosinhydrochloride extended-release tablets administration. Steady- state alfuzosin plasma concentrations are 1.2 to 1.6-fold higher than those observed after a single administration.
The volume of distribution following intravenous administration in healthy male middle-aged volunteers was 3.2 Likg. Results of in vitro studies indicate that alfuzosin is moderately bound to human plasma proteins (82% to 90%), with linear binding over a wide concentration range (5 to 5,000 ng/ml).
Alfuzosin undergoes extensive metabolism by the liver, with only 11% of the administered dose excreted unchanged in the urine. Alfuzosin is metabolized by three metabolic pathways: oxidation, 0-demethylation and N-dealkylation. The metabolites are not pharmacologically active. CYP3A4 is the principal hepatic enzyme isoform involved in its metabolism.
Following oral administration of 14C-labeled alfuzosin solution, the recovery of radioactivity after 7 days (expressed as a percentage of the administered dose) was 69% in feces and 24% in urine. Following oral administration of alfuzosin hydrochloride extended release 10 mg tablets, the apparent elimination half-life is 10 hours.
Alfuzosin hydrochloride extended-release tablets are an alpha adrenergic antagonist, indicated for the treatment of signs and symptoms of benign prostatic hyperplasia.
Important Limitations of Use:
Alfuzosin hydrochloride extended-release tablets are not indicated for treatment of hypertension.
Alfuzosin hydrochloride extended-release tablets are not indicated for use in the pediatric population.
DOSAGE AND ADMINISTRATION:
Alfuzosin hydrochloride extended-release tablets 10 mg once daily with food each day. Tablets should not be chewed or crushed.
Moderate or severe hepatic impairment
- Co-administration with potent CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, ritonavir)
- ·Known hypersensitivity (e.g., urticarial or angioedema) to Alfuzosin or any of the ingredients.
WARNING AND PRECAUTIONS:
- Postural hypotension/syncope: Care should be taken in patients with symptomatic hypotension or who have had a hypotensive response to other medications or are concomitantly treated with antihypertensive medication or nitrates.
- Use with caution in patients with severe renal impairment (creatinine clearance <30 mVmin).
- Use with caution in patients with mild hepatic impairment.
- Should not be used in combination with other alpha adrenergic antagonists.
- Prostate carcinoma should be ruled out prior to treatment.
- Intraoperative Floppy Iris Syndrome (IFIS) during cataract surgery may require modifications to the surgical technique. Discontinue Alfuzosin hydrochloride extended-release tablets if symptoms of angina pectoris appear or worsen.
- Use with caution in patients with a history of QT prolongation or who are taking medications which prolong the QT interval.
- Contraindicated for co-administration with potent CYP3A4 inhibitors.
- Should not be used in combination with other alpha-blockers.
PREGNANCY AND LACTATION:
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 teratogenicity, embryo toxic or phototoxic 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.
Use with caution in patients with severe renal impairment (creatinine clearance £ 30 mVmin).
Do not use in patients with moderate or severe hepatic impairment.
USE IN SPECIFIC POPULATIONS
- Pediatric Use: Alfuzosin hydrochloride extended-release tablets are not indicated for use in the pediatric population.
- 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.
Most common adverse reactions in clinical studies (incidence 2% and at a higher incidence than placebo): dizziness, upper respiratory infection and headache.
Should overdose of Alfuzosin hydrochloride extended-release tablets 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.
Packing: Blister of 10 Tablets.
Storage: Store in a cool and dry place below 30°C. Protect from moisture.
Keep out of reach of children.