Alfuzosine
Alfuzosine Uses, Dosage, Side Effects, Food Interaction and all others data.
Alfuzosine Hydrochloride is a selective antagonist of post-synaptic a1 adrenoreceptors, which are located in the prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra. Alfuzosine Hydrochloride relaxes the tone of the prostate smooth muscle, prostate capsule, bladder neck and proximal urethra. It competitively and selectively binds to the post synaptic a1-adrenergic receptors in the lower urinary tract. It also relaxes sympathetic nervous stimulation, reduces resting urethral pressure and inhibits urethral hypertonia-induced sympathetic nervous stimulation. As an uroselective agent, Alfuzosine Hydrochloride preferentially binds to prostatic a1 receptors, blockage of these receptors result in reduction of BPH symptoms, improvement of urine flow and decreased potential for hypertensive events.
By selectively inhibiting alpha adrenergic receptors in the lower urinary tract, alfuzosin causes smooth muscle relaxation in the bladder neck and prostate, improving urine flow, thereby reducing BPH symptoms. Additionally, alfuzosin reduces the vasoconstrictor effect of catecholamines (epinephrine and norepinephrine), leading to peripheral vasodilation. This leads to a risk of postural hypotension/syncope, and prescribing information warns that caution should be exercised in patients who take nitrates, antihypertensives, or have experienced decreased blood pressure after using other medications.
| Trade Name | Alfuzosine |
| Availability | Prescription only |
| Generic | Alfuzosin |
| Alfuzosin Other Names | Alfuzosin, Alfuzosina, Alfuzosine, Alfuzosinum |
| Related Drugs | tamsulosin, finasteride, Flomax, prazosin, tadalafil, Cialis |
| Type | |
| Formula | C19H27N5O4 |
| Weight | Average: 389.4488 Monoisotopic: 389.206304377 |
| Protein binding | The protein biding of alfuzosin is moderate and ranges from 82% to 90%. Alfuzosin is 68.2% bound to human serum albumin and 52.5% bound to human serum alpha-glycoprotein. |
| Groups | Approved, Investigational |
| Therapeutic Class | Alpha adrenoceptor blocking drugs |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Alfuzosine Hydrochloride is used for the treatment of the signs and symptoms of benign prostatic hyperplasia(BPH), lower urinary tract symptoms (LUTS) including urinary frequency, nocturia, incomplete emptying and urinary hesitancy associated with BPH.
Alfuzosine is also used to associated treatment for these conditions: Benign Prostatic Hyperplasia (BPH)
How Alfuzosine works
Alpha(1)-adrenoreceptors are found in the prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra; their activation may lead to contraction of smooth muscle and urinary symptoms in patients with BPH. Alfuzosine selectively binds to and inhibits alpha(1)-adrenergic receptors in the lower urinary tract. This leads to the relaxation of smooth muscle in both the prostate and bladder neck, resulting in the improvement in urine flow and a reduction of urinary symptoms.
Dosage
Alfuzosine dosage
The recommended dosage is one 10 mg Alfuzosine Hydrochloride tablet daily to be taken immediately after the same meal each day. The tablets should not be chewed or crushed.
Alfuzosine Hydrochloride tablet should be swallowed whole.
Side Effects
This formulation is generally well tolerated. However the following adverse events have been reported include abdominal pain, dyspepsia, constipation, nausea, impotence, bronchitis, sinusitis and pharyngitis.
Toxicity
The oral LD50 of alfuzosin is 2300 mg/kg in male mice and 1950 mg/kg in female mice. An overdose of alfuzosin can cause hypotension. Cardiovascular support should be initiated immediately. The patient should be kept in the supine position to aid in restoring pressure and managing heart rate. Fluid resuscitation should also be considered in severe cases; sometimes, vasopressors are required. Renal function should be monitored frequently. Dialysis may not be of benefit to alfuzosin protein binding of up to 90%.
Precaution
Alfuzosine Hydrochloride should not be given to patients with moderate or severe hepatic insufficiency. Caution should be exercised when Alfuzosine is administered in patients with severe renal insufficiency. If symptoms of angina pectoris should newly appear or worsen, Alfuzosine Hydrochloride should be discontinued.
Interaction
Alfuzosine may interact with other alpha-blockers, Atenolol, Cimetidine, Diltiazem, Ketoconazole and Ritonavir.
Food Interaction
- Take after a meal. Take alfuzosin after the same meal everyday. Do not take on an empty stomach.
[Moderate] ADJUST DOSING INTERVAL: Administration of alfuzosin with food enhances oral bioavailability.
According to the manufacturer, extent of absorption is 50% higher when administered under fed conditions compared to fasting conditions.br>
MANAGEMENT: To ensure maximal oral absorption, alfuzosin should be administered with or immediately after a meal.
Alfuzosine Alcohol interaction
[Moderate] GENERALLY AVOID:
The concurrent use of ethanol and alpha-1 adrenergic blockers may cause increased hypotensive effects.
Patients with aldehyde dehydrogenase deficiencies (primarily Asians) may be at a higher risk of this interaction.
The mechanism has not been determined.
Data exist for prazosin and other alpha adrenergic blockers are expected to interact also.
In addition, any patients taking alpha adrenergic blockers may experience excessive orthostatic hypotension with ethanol ingestion, due to ethanol's unopposed vasodilatory effects in the presence of alpha adrenergic blockade.
Patients who develop
a flushing reaction after ethanol ingestion (indicates a possible aldehyde dehydrogenase deficiency) should be advised to avoid ethanol or limit their intake.
All patients should be warned about the possibility of orthostatic hypotension with concurrent ethanol use.
Alfuzosine Drug Interaction
Moderate: tadalafil, tadalafil, metoprolol, metoprololUnknown: aspirin, aspirin, aspirin, aspirin, rosuvastatin, rosuvastatin, apixaban, apixaban, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol
Alfuzosine Disease Interaction
Major: hepatic impairmentModerate: QT prolongation, renal impairment, hypotension, cataracts
Volume of Distribution
The volume of distribution of alfuzosin after intravenous administration in healthy volunteers is about 3.2 L/kg. Alfuzosine distributes heavily to the tissues of the prostate.
Elimination Route
Alfuzosine is readily absorbed in the gastrointestinal tract and the absolute bioavailability under fed conditions is 49%. In patients over 75 years of age, alfuzosin is absorbed more rapidly and peak plasma levels are higher. One source mentions a bioavailability of 64%. After multiple doses under fed conditions, Cmax is achieved in 8 hours. Cmax and AUC0-24 values are about 13.6 ng/mL and 194 ng·h/mL, respectively. Steady-state plasma concentrations are achieved after the second dose and are 1.2 to 1.6 times higher than after a single dose. With the extended-release formulation, alfuzosin release is sustained over 20 hours with a rate of dissolution ranging between 2 and 12 hours.
Half Life
The apparent elimination half-life of alfuzosin after oral administration is about 10 hours. The terminal half-life is 3-5 hours.
Clearance
Exercise caution if renal clearance is < 30 mL/min. The clearance of alfuzosin is increased in renal insufficiency (with or without dialysis), due to an increase in the free fraction.
Elimination Route
It is partially metabolised and excreted mainly in the bile and faeces. Following oral administration of a radiolabeled alfuzosin solution, the detection of radioactivity after one week was 69% in the feces and 24% in the urine.
Pregnancy & Breastfeeding use
Alfuzosine Hydrochloride is not indicated for use in pregnant and lactating mother.
Contraindication
Alfuzosine Hydrochloride tablet is contraindicated for hypersensitivity to Alfuzosine Hydrochloride, history of orthostatic hypotension, combination with other alpha-1 receptor blockers, hepatic insufficiency.
Special Warning
Efficacy of Alfuzosine Hydrochloride has not been demonstrated in children aged 2 to 16 years. Therefore Alfuzosine Hydrochloride is not indicated for use in the paediatric population.
Acute Overdose
Overdose of Alfuzosine Hydrochloride should 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.
Storage Condition
Store in a cool and dry place, protected from light
Innovators Monograph
You find simplified version here Alfuzosine
Alfuzosine contains Alfuzosin see full prescribing information from innovator Alfuzosine Monograph, Alfuzosine MSDS, Alfuzosine FDA label
FAQ
What is Alfuzosine used for?
It is used to treat benign prostatic hyperplasia. As an antagonist of the α₁ adrenergic receptor. Alfuzosine is used to treat the signs and symptoms of benign enlargement of the prostate (benign prostatic hyperplasia or BPH).
How safe is Alfuzosine?
This study demonstrates the satisfactory long-term safety of this formulation, and its safe use even in at-risk populations. Alfuzosine may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.
How does Alfuzosine work?
Alfuzosine works by relaxing the muscles in the prostate and bladder to allow urine to flow more easily.
What are the common side effects of Alfuzosine?
Common side effect of Alfuzosine are include:
- tiredness
- headache
- runny or stuffy nose
- pain
- stomach pain
- heartburn
- constipation
- nausea
- decrease in sexual ability
- sore throat, fever, chills, cough and other signs of infection
Is Alfuzosine safe during pregnancy?
Alfuzosine is not for use in women, and the effects of this medicine during pregnancy or in breastfeeding women are unknown. Alfuzosine is not approved for use by anyone younger than 18 years old.
Is Alfuzosine safe during breastfeeding?
This Alfuzosine is not indicated for use in female patients.
Can I drink alcohol with Alfuzosine?
You are advised not to drink alcohol while you are on Alfuzosine. Alcohol increases the risk of side-effects from Alfuzosine, such as feeling faint or dizzy.
Can I drive after taking Alfuzosine?
You may feel dizzy and weak while taking Alfuzosine. If this happens do not drive or operate any tools or machines
What is best time to take Alfuzosine?
To avoid injury from dizziness or fainting, your doctor may tell you to take your first dose of Alfuzosine with food at bedtime so that your body can get used to its effects. Take this medication regularly to get the most benefit from it. To help you remember, take it after the same meal each day.
How often can I take Alfuzosine?
Adults, 10 milligrams (mg) once a day. Children, Use is not recommended.
How long does Alfuzosine take to work?
Alfuzosine can start to relieve your BPH symptoms around 4 weeks after starting it. It's important that you continue to take Alfuzosine even if you don't feel better right away.
How long does Alfuzosine stay in my system?
Following oral administration of Alfuzosine 10 mg tablets, the apparent elimination half-life is 10 hours.
How long can I take Alfuzosine?
Alfuzosine 10 mg administered for 2 years in real practice is effective in improving LUTS and quality of life, and is well tolerated from a cardiovascular perspective, including in elderly men and those receiving antihypertensive co-medication.
Who should not take Alfuzosine?
You should not take Alfuzosine if you have moderate to severe liver disease. Alfuzosine is not approved for use by anyone younger than 18 years old. You should not take Alfuzosine if you are allergic to it, or if you have: moderate to severe liver disease.
What happens if I miss a dose?
Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.
What happen if I take too much Alfuzosine?
Taking too much Alfuzosine may lead to: low blood pressure, with symptoms including dizziness, lightheadedness, and fainting. other problems with your heart.
What happen If I stop taking Alfuzosine?
If don't take or stop taking Alfuzosine, you may have increased symptoms of BPH, such as difficulty starting to urinate, straining while trying to urinate, frequent urges to urinate, pain during urination, and dribbling after urination.
Can Alfuzosine affects my heart ?
Alfuzosine may cause increased heart rate or decreased blood pressure, which may affect control of angina symptoms. People with angina (chest pain) should stop using this medication if their symptoms reappear or become worse.
Can Alfuzosine affect my liver?
Don't take Alfuzosine if you have moderate or severe liver problems. If your liver isn't working well, more of the Alfuzosine may stay in your body.
Can Alfuzosine affect my kidneys?
For people with kidney problems: Use this Alfuzosine with caution if you have severe kidney problems.
