Sun Pharma




Full Prescribing Info
Alfuzosin hydrochloride.
Each prolonged release tablet contains Alfuzosin Hydrochloride 10 mg.
FLOTRAL contains alfuzosin hydrochloride as the active ingredient. 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 C19H27N5O4·HCl. The molecular weight of alfuzosin hydrochloride is 425.9.
Pharmacotherapeutic Group: ALPHA-BLOCKER. ATC code: G04CA01 (G: genitourinary system and sex hormones).
Pharmacology: Pharmacodynamics: Alfuzosin is an orally active quinazoline derivative. It is a selective antagonist of post-synaptic alpha-1 adrenoreceptors. Reported pharmacological studies conducted in vitro have confirmed the selectivity of alfuzosin for alpha-1 adrenoreceptors located in the prostate, bladder base and urethra.
Alpha-blockers decrease infravesical obstruction via direct action on prostate smooth muscle. In vivo studies in animals have reported that alfuzosin reduces urethral pressure thereby lowering resistance to urine flow during micturition. A study in awake rats reported a greater effect on urethral pressure than the effect on blood pressure.
Reported placebo-controlled studies in patients with benign prostatic hypertrophy showed that alfuzosin: significantly increases urine flow rate by a mean of 30% in patients with a flow rate of ≤ 15 ml/s. This improvement is observed from the first dose; significantly reduces detrusor pressure and increases volume, producing the desire to void; significantly reduces the residual urine volume.
These effects lead to an improvement in irritative and obstructive urinary symptoms. They have no negative effect on sexual function. Furthermore, maximum urinary flow rate remains significantly increased 24 hours after intake.
Pharmacokinetics: Alfuzosin hydrochloride is reported to be approximately 90% plasma protein binding. Alfuzosin is extensively metabolized in the liver with only 11% of the parent drug excreted in urine. Most of the metabolites (which are inactive) are reported to be excreted in the feces (75 to 90%). The pharmacokinetic profile of alfuzosin is unchanged in patients with chronic heart failure.
Studies have reported that the bioavailability is increased when the drug is administered after a meal (see DOSAGE & ADMINISTRATION). The pharmacokinetic parameters (Cmax and AUC) are not increased in the elderly as compared to middle-aged healthy volunteers.
The mean Cmax and AUC values are reported to be moderately increased in patients with moderately impaired kidney function (creatinine clearance > 30 ml/min), with no change in elimination half-life, as compared to patients with normal kidney function.
Dosage adjustment is, therefore, not necessary in patients with impaired kidney function with a creatinine clearance of > 30 ml/min.
Treatment of the functional symptoms of benign prostatic hypertrophy.
Adjunctive treatment for vesical catheterization in acute urinary retention associated with benign prostatic hypertrophy.
Dosage/Direction for Use
The tablet must be swallowed whole with a glass of water (see PRECAUTIONS).
RECOMMENDED DOSE: The recommended dosage is one 10-mg tablet per day, to be taken immediately after the evening meal.
Adjunctive treatment following insertion of a vesical catheter in acute urinary retention associated with benign prostatic hypertrophy: The recommended dosage is one 10-mg tablet per day, to be taken after a meal, starting on the day of insertion of the urethral catheter.
The treatment is administered for 3 to 4 days, with 2 to 3 days during catheterization and 1 day following its removal.
In the event of overdose, the patient should be hospitalized and kept lying down. Standard treatment for hypotension should be instigated.
Due to its high degree of protein binding, alfuzosin is not easily dialysable.
This medicine must not be administered in the following situations: hypersensitivity to alfuzosin and/or any of the other components, postural hypotension, hepatic insufficiency, combination with other alpha 1-blockers, severe kidney failure (creatinine clearance < 30 ml/min), concomitant administration with potent CYP3A4 inhibitors (see INTERACTIONS).
Special warnings: As with all alpha-1 blockers, some patients, and in particularly those treated with antihypertensives may report postural hypotension within a few hours following administration, possibly with symptoms (dizzy sensations, fatigue, sweating).
If this occurs, patients should remain lying down until the symptoms have completely subsided.
These effects are usually transient, occur at the beginning of treatment and do not generally prevent continued treatment.
Pronounced drop in blood pressure has been reported in post-marketing surveillance in patients with pre-existing risk factors (such as underlying cardiac diseases and/or concomitant treatment with antihypertensive medication). The risk of developing hypotension and related adverse reactions may be greater in elderly patients.
Patients should be warned of the possible occurrence of these events. Care should be taken when alfuzosin is administered to patients with symptomatic orthostatic hypotension or in patients on anti-hypertensive medication or nitrates.
Use with caution in patients with acquired or congenital QT prolongation or who are taking medications that prolong the QT interval.
Alfuzosin, like other alpha-1 blockers, has been associated with priapism (persistent painful penile erection unrelated to sexual activity). Because this condition can lead to permanent impotence if not properly treated, patients should be advised about the seriousness of the condition (see ADVERSE REACTIONS).
Special Precautions
Special precautions for use: Care should be taken when alfuzosin is administered to patients who have experienced marked hypotension following administration of another alpha-1 blocker.
In patients with coronary disease, alfuzosin should not be prescribed alone. The specific coronary insufficiency treatment should be continued. If angina pectoris recurs or worsens, alfuzosin treatment should be discontinued.
Intraoperative Floppy Iris Syndrome (IFIS, a variant of small pupil syndrome) has been observed during cataract surgery in some patients on or previously treated with some alpha-1-blockers. Although the risk of this event with alfuzosin hydrochloride prolonged release tablets appears very low, ophthalmic surgeons should be informed in advance of cataract surgery of current or past use of alpha-1-blockers, as IFIS may lead to increased procedural complications. The ophthalmologists should be prepared for possible modifications to their surgical technique.
Patients must be informed that the tablets must be swallowed whole. The tablets must not be crunched, chewed, crushed or ground into a powder. Doing so could lead to inappropriate release and absorption of the medicinal product consequently causing unwanted effects which may be of early onset.
If patient has been told by the doctor of their intolerance to some sugars, contact the doctor before taking FLOTRAL.
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.
Use in Children: Efficacy of alfuzosin hydrochloride prolonged release tablets 10 mg has not been reported in children aged 2 to 16 years. Therefore, alfuzosin hydrochloride prolonged release tablets 10 mg are not indicated for use in pediatric population.
Use in the Elderly: Caution is recommended, particularly in the elderly.
Use In Pregnancy & Lactation
The therapeutic indication does not apply to women.
It is not known whether alfuzosin is safe during pregnancy nor whether it is excreted in breast milk.
Adverse Reactions
The following CIOMS frequency rating is used, when applicable: Very common ≥ 10%; Common ≥ 1 and < 10%; Uncommon ≥ 0.1 and < 1%; Rare ≥ 0.01 and < 0.1%; Very rare < 0.01%. Not known (frequency cannot be estimated from available data).
Blood and lymphatic system disorders: Not known: thrombocytopenia.
CNS and psychiatric disorders: Common: faintness/dizziness, headache.
Uncommon: vertigo, syncope.
Cardiovascular disorders: Uncommon: tachycardia, hypotension (postural), syncope, flushing.
Very rare: angina pectoris in patients with pre-existing coronary artery disease (see PRECAUTIONS).
Not known: atrial fibrillation.
Eye disorders: Not known: intraoperative floppy iris syndrome (see PRECAUTIONS).
Respiratory system disorders: Uncommon: rhinitis.
Gastro-intestinal disorders: Common: nausea, abdominal pain, vomiting.
Uncommon: diarrhea.
Hepato-biliary disorders: Not known: hepatocellular injury, cholestatic liver disease.
Skin and appendages: Uncommon: rash, pruritus.
Very rare: urticaria, angioedema.
Body as a whole: Common: asthenia.
Uncommon: flushes, oedema, chest pain.
Reproductive system and breast disorders: Very rare: priapism.
Drug Interactions
Combinations contra-indicated: Alpha-1-receptor blockers (see CONTRAINDICATIONS) (prazosin, urapidil, minoxidil): Enhance hypotensive effect. Risk of severe postural hypotension.
Potent CYP3A4 inhibitors such as ketoconazole, itraconazole, clarithromycin, erythromycin and ritonavir since alfuzosin blood levels may be increased (see PHARMACOLOGY UNDER ACTIONS).
Combinations to be taken into consideration: Antihypertensives: Enhance antihypertensive effect and increased risk of postural hypotension (cumulative effect) (see WARNINGS).
Do not store above 30°C.
ATC Classification
G04CA01 - alfuzosin ; Belongs to the class of alpha-adrenoreceptor antagonists. Used in the treatment of benign prostatic hypertrophy.
PR tab 10 mg (white to off white, uncoated, round, biconvex, debossed with 'RY 10' on one side) x 3 x 10's.
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