Alfustat
Alfustat Uses, Dosage, Side Effects, Food Interaction and all others data.
Alfustat 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. Alfustat 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, Alfustat 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 | Alfustat |
| Availability | Prescription only |
| Generic | Alfuzosin |
| Alfuzosin Other Names | Alfuzosin, Alfuzosina, Alfuzosine, Alfuzosinum |
| Related Drugs | tamsulosin, finasteride, Flomax, prazosin, tadalafil, Cialis |
| Type | Tablet |
| 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 | Elder Pharmaceuticals Ltd |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Alfustat 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.
Alfustat is also used to associated treatment for these conditions: Benign Prostatic Hyperplasia (BPH)
How Alfustat 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. Alfustat 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
Alfustat dosage
The recommended dosage is one 10 mg Alfustat Hydrochloride tablet daily to be taken immediately after the same meal each day. The tablets should not be chewed or crushed.
Alfustat 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
Alfustat Hydrochloride should not be given to patients with moderate or severe hepatic insufficiency. Caution should be exercised when Alfustat is administered in patients with severe renal insufficiency. If symptoms of angina pectoris should newly appear or worsen, Alfustat Hydrochloride should be discontinued.
Interaction
Alfustat 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.
Alfustat 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.
Alfustat 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
Alfustat 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. Alfustat distributes heavily to the tissues of the prostate.
Elimination Route
Alfustat 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
Alfustat Hydrochloride is not indicated for use in pregnant and lactating mother.
Contraindication
Alfustat Hydrochloride tablet is contraindicated for hypersensitivity to Alfustat Hydrochloride, history of orthostatic hypotension, combination with other alpha-1 receptor blockers, hepatic insufficiency.
Special Warning
Efficacy of Alfustat Hydrochloride has not been demonstrated in children aged 2 to 16 years. Therefore Alfustat Hydrochloride is not indicated for use in the paediatric population.
Acute Overdose
Overdose of Alfustat 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 Alfustat
Alfustat contains Alfuzosin see full prescribing information from innovator Alfustat Monograph, Alfustat MSDS, Alfustat FDA label
FAQ
What is Alfustat used for?
It is used to treat benign prostatic hyperplasia. As an antagonist of the α₁ adrenergic receptor. Alfustat is used to treat the signs and symptoms of benign enlargement of the prostate (benign prostatic hyperplasia or BPH).
How safe is Alfustat?
This study demonstrates the satisfactory long-term safety of this formulation, and its safe use even in at-risk populations. Alfustat 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 Alfustat work?
Alfustat works by relaxing the muscles in the prostate and bladder to allow urine to flow more easily.
What are the common side effects of Alfustat?
Common side effect of Alfustat 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 Alfustat safe during pregnancy?
Alfustat is not for use in women, and the effects of this medicine during pregnancy or in breastfeeding women are unknown. Alfustat is not approved for use by anyone younger than 18 years old.
Is Alfustat safe during breastfeeding?
This Alfustat is not indicated for use in female patients.
Can I drink alcohol with Alfustat?
You are advised not to drink alcohol while you are on Alfustat. Alcohol increases the risk of side-effects from Alfustat, such as feeling faint or dizzy.
Can I drive after taking Alfustat?
You may feel dizzy and weak while taking Alfustat. If this happens do not drive or operate any tools or machines
What is best time to take Alfustat?
To avoid injury from dizziness or fainting, your doctor may tell you to take your first dose of Alfustat 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 Alfustat?
Adults, 10 milligrams (mg) once a day. Children, Use is not recommended.
How long does Alfustat take to work?
Alfustat can start to relieve your BPH symptoms around 4 weeks after starting it. It's important that you continue to take Alfustat even if you don't feel better right away.
How long does Alfustat stay in my system?
Following oral administration of Alfustat 10 mg tablets, the apparent elimination half-life is 10 hours.
How long can I take Alfustat?
Alfustat 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 Alfustat?
You should not take Alfustat if you have moderate to severe liver disease. Alfustat is not approved for use by anyone younger than 18 years old. You should not take Alfustat 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 Alfustat?
Taking too much Alfustat may lead to: low blood pressure, with symptoms including dizziness, lightheadedness, and fainting. other problems with your heart.
What happen If I stop taking Alfustat?
If don't take or stop taking Alfustat, 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 Alfustat affects my heart ?
Alfustat 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 Alfustat affect my liver?
Don't take Alfustat if you have moderate or severe liver problems. If your liver isn't working well, more of the Alfustat may stay in your body.
Can Alfustat affect my kidneys?
For people with kidney problems: Use this Alfustat with caution if you have severe kidney problems.
