Fozal

Alfuzosin hydrochloride.

Pharmacologic Classification: α-Adrenergic Blocking Agent.
Pharmacology: Alfuzosin hydrochloride is an α₁-adrenergic blocking agent that exhibits selectivity for α₁-adrenergic receptors in the lower urinary tract (bladder base, bladder neck, prostate, prostatic capsule, prostatic urethra). Relaxation of smooth muscle in the bladder neck and prostate, which improves urine flow and reduces symptoms of benign prostatic hyperplasia (BPH), result from blockade of these adrenoceptors. Alfuzosin hydrochloride relieves moderate to severe irritative and obstructive urinary symptoms of BPH including frequency of urination, urinary urgency, nocturia, hesitancy, interrupted or weak stream, sensation of incomplete bladder emptying, and straining. These effects are generally achieved with alfuzosin hydrochloride doses without clinically important effects on blood pressure or heart rate.
Pharmacokinetics: Bioavailability: Alfuzosin hydrochloride 10 mg modified-release tablet has an absolute bioavailability of about 49% under fed conditions. It exhibits linear kinetics following single and multiple dosing of up to 30 mg.
The pharmacokinetics of a single dose of alfuzosin hydrochloride 10 mg modified-release tablet was evaluated in healthy male adult subjects under fed and fasted conditions. The following are the important pharmacokinetic parameters for the said studies: See table.

Click on icon to see table/diagram/image

The extent of absorption is decreased by about 50% under fasting conditions, thus, it is recommended that alfuzosin hydrochloride modified-release tablet should be taken immediately after a meal. (See DOSAGE & ADMINISTRATION).
Alfuzosin hydrochloride is about 90% bound to plasma proteins and is rapidly and extensively distributed to tissues; its volume of distribution is about 2.5 L/kg.
Alfuzosin hydrochloride is extensively metabolized with only 11% of a dose excreted unchanged in the urine. It undergoes metabolism to form inactive metabolites mainly through the liver via oxidation, O-demethylation, and/or N-dealkylation primarily through cytochrome P-450 (CYP) 3A4. It is not an inhibitor of CYP isoenzymes 1A2, 2A6, 2C9, 2C19, 2D6, or 3A4; it is also not an inducer of CYP isoenzymes 1A, 2A6, or 3A4.
Alfuzosin's apparent half-life following oral administration of a 10 mg modified-release tablet is approximately 10 hours. After 7 days, 69% and 24% of the orally administered dose of ¹⁴C-labeled alfuzosin solution were recovered in the feces and urine, respectively.
Hepatic Insufficiency: The AUC is increased and elimination half-life of alfuzosin hydrochloride is prolonged in patients with moderate to severe hepatic impairment. This results in approximately one-third to one-fourth higher plasma concentrations of alfuzosin in these patients compared to patients with normal liver function. Alfuzosin hydrochloride's pharmacokinetics has not been studied in patients with mild hepatic insufficiency.
Renal Insufficiency: Systemic alfuzosin hydrochloride exposure may increase by about 50% in patients with renal insufficiency (CL_CR <80 mL/minute); safety profile appears to be the same in patients with mild (CL_CR 60-80 mL/minute) or moderate (CL_CR 30-59 mL/minute) renal impairment and in patients with normal renal function. Experience in patients with severe renal insufficiency is limited.

Treatment of signs and symptoms of benign prostatic hyperplasia (BPH).
As an adjunct therapy with urethral catheterization for Acute Urinary Retention related to BPH and management following catheter removal.
Note: Alfuzosin hydrochloride is not indicated for the treatment of hypertension.

The modified-release tablet should be swallowed whole. Do not chew or crush or divide the modified-release tablet since this may cause inappropriate release and absorption of the drug that may lead to early adverse reactions.
Usual Dose for BPH: Orally, 10 mg (1 tablet) once daily immediately after the same meal every day.
Acute Urinary Retention: Orally, 10 mg (1 tablet) once daily immediately after a meal to be taken on the first day of catheterization and continued beyond catheter removal unless there is a relapse of acute urinary retention or disease progression.
Or, as prescribed by a physician

Postural Hypotension: Postural hypotension with or without symptoms such as dizziness, fatigue and sweating may occur within a few hours after alfuzosin hydrochloride administration. There is also a potential for syncope. Advise patients to avoid situations where injury could result should syncope occur. There may be an increased risk of hypotension/postural hypotension and syncope when taking alfuzosin hydrochloride concomitantly with anti-hypertensive medication or nitrates. Administer alfuzosin hydrochloride with caution in patients with symptomatic hypotension or patients who have had a hypotensive response to other medications.
Coronary Insufficiency: Discontinue alfuzosin hydrochloride treatment if symptoms of angina pectoris should appear or worsen.
Patients with Congenital or Acquired QT Prolongation: Alfuzosin hydrochloride may cause prolongation of QT interval which should be considered in clinical decisions when prescribing alfuzosin hydrochloride in patients with known history of QT prolongation or patients who are taking medications which prolong QT interval. No signs of torsades de pointes have been seen in post-marketing experience with alfuzosin hydrochloride.
Prostatic Carcinoma: Carcinoma of the prostate and BPH have similar symptoms and these two diseases frequently co-exist. Evaluate patients prior to starting alfuzosin hydrochloride treatment to rule out the presence of carcinoma of the prostate.
Intraoperative Floppy Iris Syndrome (IFIS): IFIS has been reported during cataract surgery in some patients on or previously treated with alpha-1 blockers. IFIS, a variant of small pupil syndrome, manifests as a combination of a flaccid iris that billows in response to intraoperative irrigation currents, progressive intraoperative miosis even with preoperative dilation with standard mydriatic drugs and potential prolapse of the iris toward the phacoemulsification incisions. Modifications of surgical technique such as utilization of iris hooks, iris dilator rings, or viscoelastic substance may be used by the patient's ophthalmologist. There appears to be no benefit when α₁- blocker therapy is stopped before cataract surgery.
Hepatic Insufficiency: Do not use alfuzosin hydrochloride in patients with moderate or severe hepatic insufficiency since alfuzosin blood levels are increased in these patients (see PHARMACOLOGY: PHARMACOKINETICS under ACTIONS and CONTRAINDICATIONS).
Renal Insufficiency: Exercise caution when alfuzosin hydrochloride is administered to patients with renal insufficiency. (See PHARMACOLOGY: PHARMACOKINETICS under ACTIONS).
Effects on Ability to Drive or Use Machines: Advise patients to avoid hazardous tasks including driving and operating machinery since alfuzosin hydrochloride may potentially cause vertigo, dizziness and asthenia.

CNS: Dizziness/faintness, headache, vertigo, malaise, drowsiness.
Respiratory: Upper respiratory tract infection, bronchitis, sinusitis, rhinitis, and laryngitis, pharyngitis, influenza-like symptoms.
Gastrointestinal: Abdominal pain, dyspepsia, constipation, nausea, vomiting, diarrhea, and dry mouth.
Musculoskeletal: Pain, asthenia, back pain, neuralgia, neuropathy, and lumbar disc lesion, joint disorders including arthritis, arthrosis, arthropathy, arthralgia, and bursitis.
Hepatobiliary disorders: Hepatocellular and cholestatic liver injury (including cases with jaundice leading to drug discontinuation).
Reproductive system disorders: Impotence, priapism, ejaculation disorders.
Skin and subcutaneous tissue disorders: Rash, urticaria, angioedema, pruritus.
Cardiovascular: Tachycardia, palpitations, chest pain, angina pectoris in patients with pre-existing coronary artery disease, and other symptoms associated with orthostasis such as hypotension or postural hypotension and syncope. Isolated spontaneous cases of QT interval prolongation, ventricular arrhythmias, including torsades de pointes, ventricular tachycardia, and fibrillation.
Eye Disorders: IFIS during cataract surgery in some patients on or previously treated with α₁-blockers. (see PRECAUTIONS), abnormal vision.
Others: Fatigue, edema, flushing, bite, inflicted injury, pain.

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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