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Product Name
:
ALFUZOSINE-ELSaad
Chemical Name
:
Alfuzosin HCl
Therapeutic Category
:
Urinary tract drugs
Pharmacologic Category
:
Alpha 1 Blocker
Pharmaceutical Form
:
Tablets
Composition
:
Alfuzosin HCl 2.5mg / 5mg
Lactation
Monitoring Parameters
Dosing
 
Dosing: Adult

Benign prostatic hyperplasia (BPH): Oral: 10 mg once daily

Ureteral stones, expulsion (unlabeled use): Oral: 10 mg once daily, discontinue after successful expulsion (average time to expulsion 1-2 weeks) (Agrawal, 2009; Ahmed, 2010; Gurbuz, 2011). Note: Patients with stones >10 mm were excluded from studies.
Dosing: Geriatric
Refer to adult dosing.
Dosing: Renal Impairment

Bioavailability and maximum serum concentrations are increased by ~50% with mild (Clcr 60-80 mL/minute), moderate (Clcr 30-59 mL/minute), or severe (Clcr <30 mL/minute) renal impairment.

Note: Safety data is limited in patients with severe renal impairment (Clcr <30 mL/minute). Use with caution.
Dosing: Hepatic Impairment

Mild hepatic impairment: Use has not been studied; use caution.

Moderate or severe hepatic impairment (Child-Pugh class B and C): Clearance is decreased 1/3 to 1/4 and serum concentration is increased three- to fourfold; use is contraindicated.
Use
 
Treatment of the functional symptoms of benign prostatic hyperplasia (BPH)
Use - Unlabeled/Investigational
Facilitation of expulsion of ureteral stones
Adverse Reactions
 
1% to 10%:

Central nervous system: Dizziness (6%), fatigue (3%), headache (3%), pain (1% to 2%)

Gastrointestinal: Abdominal pain (1% to 2%), constipation (1% to 2%), dyspepsia (1% to 2%), nausea (1% to 2%)
Genitourinary: Impotence (1% to 2%)

Respiratory: Upper respiratory tract infection (3%), bronchitis (1% to 2%), pharyngitis (1% to 2%), sinusitis (1% to 2%)

<1% (Limited to important or life-threatening): Angina pectoris (pre-existing CAD), angioedema, atrial fibrillation, chest pain, cholestatic liver injury, diarrhea, edema, flushing, hepatocellular injury, intraoperative floppy iris syndrome (with cataract surgery), jaundice, priapism, pruritus, rash, rhinitis, tachycardia, urticaria
Contraindications
 
Hypersensitivity to alfuzosin or any component of the formulation; moderate or severe hepatic insufficiency (Child-Pugh class B and C); concurrent use with potent CYP3A4 inhibitors (eg, itraconazole, ketoconazole, ritonavir) or other alpha1-blocking agents
Warnings / Precautions Drug
 
Concerns related to adverse effects:

Angina: Discontinue if symptoms of angina occur or worsen.

Floppy iris syndrome: Intraoperative floppy iris syndrome has been observed in cataract surgery patients who were on or were previously treated with alpha1-blockers; causality has not been established and there appears to be no benefit in discontinuing alpha-blocker therapy prior to surgery.

Orthostatic hypotension/syncope: May cause significant orthostatic hypotension and syncope, especially with first dose; anticipate a similar effect if therapy is interrupted for a few days, if dosage is rapidly increased, or used with antihypertensives (particularly vasodilators), PDE-5 inhibitors, nitrates or other medications which may result in hypotension. Patients should be cautioned about performing hazardous tasks when starting new therapy or adjusting dosage upward.

Priapism: Priapism has been associated with use (rarely).

Disease-related concerns:

Hepatic impairment: Use with caution in patients with mild hepatic impairment; contraindicated in moderate-to-severe impairment.

Prostate cancer: Rule out prostatic carcinoma before beginning therapy (many symptoms of BPH and prostate cancer are similar).

QT prolongation: Alfuzosin has been shown to prolong the QT interval alone (minimal) and with other drugs with comparable effects on the QT interval (additive). Use with caution in patients with known QT prolongation (congenital or acquired).

Renal impairment: Use with caution in patients with severe renal impairment (Clcr <30 mL/minute).
Concurrent drug therapy issues:

High potential for interactions: Contraindicated in patients receiving strong CYP3A4 inhibitors or other alpha1-blockers.
Other warning/precautions:

Antihypertensive agent: Not intended for use as an antihypertensive drug.
Metabolism/Transport Effects

Substrate of CYP3A4 (major)
Interactions
 
Alpha1-Blockers: May enhance the antihypertensive effect of other Alpha1-Blockers. Risk X: Avoid combination

Antihypertensives: Alfuzosin may enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy

Beta-Blockers: May enhance the orthostatic hypotensive effect of Alpha1-Blockers. The risk associated with ophthalmic products is probably less than systemic products. Exceptions: Levobunolol; Metipranolol. Risk D: Consider therapy modification

Calcium Channel Blockers: Alpha1-Blockers may enhance the hypotensive effect of Calcium Channel Blockers. Risk C: Monitor therapy

CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy

CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Alfuzosin. Risk X: Avoid combination

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy

Herbs (CYP3A4 Inducers): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy

MAO Inhibitors: May enhance the orthostatic hypotensive effect of Orthostatic Hypotension Producing Agents. Risk C: Monitor therapy

Nitroglycerin: Alfuzosin may enhance the hypotensive effect of Nitroglycerin. Risk C: Monitor therapy

Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Alpha1-Blockers. Management: Ensure patient is stable on alpha 1 blocker before starting PDE5 inhibitor; initiate PDE5 inhibitor at lowest possible dose. If patient stable on PDE5 inhibitor, initiate alpha 1 blocker at lowest dose. Risk D: Consider therapy modification

Protease Inhibitors: May increase the serum concentration of Alfuzosin. Risk X: Avoid combination

QTc-Prolonging Agents: Alfuzosin may enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk C: Monitor therapy

Telaprevir: May increase the serum concentration of Alfuzosin. Risk X: Avoid combination

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Pregnancy
 
B
 
Pregnancy Implications
Teratogenic effects were not observed in animal studies.
Mechanism of Action
 

An antagonist of alpha1-adrenoreceptors in the lower urinary tract. Smooth muscle tone is mediated by the sympathetic nervous stimulation of alpha1-adrenoreceptors, which are abundant in the prostate, prostatic capsule, prostatic urethra, and bladder neck. Blockade 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.

Pharmacodynamics / Kinetics
 
Absorption: Decreased 50% under fasting conditions
Distribution: Vd: 3.2 L/kg
Protein binding: 82% to 90%

Metabolism: Hepatic, primarily via CYP3A4; metabolism includes oxidation, O-demethylation, and N-dealkylation; forms metabolites (inactive)

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)
 
   
 
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