Alfuzosin is a medication primarily used to treat benign prostatic hyperplasia (BPH), a condition in which the prostate gland becomes enlarged, leading to difficulties in urination. It belongs to a class of drugs called alpha-1 blockers, which work by relaxing the muscles in the prostate and bladder neck, making it easier to urinate.

Alfuzosin helps to relieve symptoms such as frequent or urgent need to urinate, weak stream, difficulty in starting the flow of urine, and the need to urinate during the middle of the night.

Alfuzosin is an alpha-receptor blocker. It inhibits the activation of alpha receptors present primarily in the smooth muscles of the lower urinary tract. Inhibition of alpha receptors relaxes the smooth muscles relieving symptoms of prostatic hyperplasia and improving urinary flow. It is also used to facilitate the expulsion of small ureteral stones.

Alfuzosin Dose in Adults

Alfuzosin dose in the treatment of Benign prostatic hyperplasia (BPH):

• The typical dose is one 10 mg pill every day.

Alfuzosin dose in the treatment of Ureteral stones, expulsion (off-label use):

• The typical dose is also one 10 mg pill each day.
• After the stone is successfully expelled, which usually takes about 1 to 2 weeks, the medication is stopped.

Use in Children:

Not recommended in children

Pregnancy Risk Factor B

• Alfuzosin has been given a Pregnancy Risk Factor B rating, which means that it's considered relatively safe for pregnant individuals based on animal studies.
• These studies haven't shown any harmful effects on pregnancy.

Use during breastfeeding:

• We're not sure if alfuzosin passes into breast milk.
• So, if you're breastfeeding and considering taking alfuzosin, it's essential to talk with your doctor to weigh the potential risks and benefits for you and your baby.

Alfuzosin dose in kidney disease:

• The manufacturer's instructions don't include specific dose adjustments for alfuzosin.
• However, if you have severe kidney problems with a creatinine clearance (CrCl) less than 30 mL/minute, you should be careful when taking alfuzosin.

Alfuzosin Dose in Liver disease:

• For people with mild liver problems (Child-Pugh class A), the manufacturer's instructions don't specify any changes to the dosage of alfuzosin because it hasn't been studied in this group. It's recommended to use it cautiously.
• But for those with moderate to severe liver problems (Child-Pugh class B or C), alfuzosin should not be used as it's considered unsafe in these cases.

Common side effects of alfuzosin (Uroxatral):

• Respiratory:
  • pharyngitis, and
  • sinusitis
  • Upper respiratory tract infection,
  • bronchitis,
• Central nervous system:
  • headache, and
  • Dizziness,
  • fatigue,
  • pain
• Genitourinary:
  • Impotence
• Gastrointestinal:
  • dyspepsia, and
  • Abdominal pain,
  • constipation,
  • nausea

Rare side effects:

• atrial fibrillation,
• diarrhea,
• edema,
• Angina pectoris (pre-existing CAD),
• angioedema,
• rhinitis,
• hypotension,
• intraoperative floppy iris syndrome (with cataract surgery),
• jaundice,
• chest pain,
• flushing,
• hepatic injury (including cholestatic),
• priapism,
• pruritus,
• skin rash,
• systolic hypotension,
• toxic epidermal necrolysis,
• tachycardia,
• thrombocytopenia,
• urticaria, and
• vomiting

Contraindications to alfuzosin (Uroxatral):

• Alfuzosin should not be used if you have a known allergy to it or any ingredients in the medication, or if you have moderate to severe liver problems (Child-Pugh class B and C).
• Additionally, it's not recommended to take alfuzosin if you're using strong CYP3A4 inhibitors like itraconazole, ketoconazole, or ritonavir, as this could cause harmful effects.
• In Canada, concurrent use with other alpha1-blockers is also listed as a contraindication.

Warnings and Precautions

Angina

• If you're taking alfuzosin and experience symptoms of angina (chest pain or discomfort), it's important to stop taking the medication.

CNS depression

• Alfuzosin can lead to CNS depression, which might affect your ability to think clearly or react quickly.
• This means tasks like operating machinery or driving may become risky.
• Make sure to be cautious and avoid these activities until you know how alfuzosin affects you

Floppy iris syndrome:

• In cataract surgery, some patients who have taken or are taking alpha-blockers like alfuzosin may experience a condition called intraoperative floppy iris syndrome.
• This can affect the surgery process and might require changes to the surgical technique.
• However, stopping alpha-blocker therapy before surgery doesn't seem to provide any extra benefit.
• If you're planning cataract surgery and have been taking alfuzosin, make sure your eye surgeon knows about it so they can plan accordingly.

Orthostatic hypotension and syncope:

• Alfuzosin can lead to orthostatic hypotension, where blood pressure drops suddenly when you stand up, potentially causing dizziness or fainting.
• This effect can occur shortly after taking the medication, or if you stop taking it suddenly for a few days, increase the dosage quickly, or start other medications like certain blood pressure drugs, PDE-5 inhibitors, or nitrates.
• If you already have symptoms of orthostatic hypotension, be cautious when using alfuzosin.

Priapism:

• While rare, alfuzosin use has been linked to priapism, a painful and prolonged erection lasting longer than four hours.
• If you experience this condition, it's crucial to seek immediate medical attention to prevent potential complications.
• Prompt treatment is necessary to avoid permanent damage to the penis.

Cardiovascular disease

• Alfuzosin should be used cautiously in individuals with a history of certain heart rhythm abnormalities (tachyarrhythmia) or specific cardiovascular conditions like myocardial ischemia, which is reduced blood flow to the heart muscle.
• These conditions can potentially be aggravated by the effects of alfuzosin.

Hepatic impairment:

• In individuals with mild liver problems, alfuzosin should be used cautiously.
• However, if you have moderate to severe liver impairment, it's best to avoid using alfuzosin altogether.

Prostate cancer:

• Before starting alfuzosin therapy, it's essential to rule out prostate cancer.
• This is because many symptoms of benign prostatic hyperplasia (BPH) and prostate cancer can be similar.

Extension of QT

• Alfuzosin has been found to slightly prolong the QT interval on its own, and when combined with other medications that have similar effects on the QT interval, the effect can be additive.
• Therefore, it's important to use alfuzosin cautiously in patients with known QT prolongation, whether it's congenital (present from birth) or acquired (developed later in life).

Renal impairment:

• For individuals with severe renal impairment, characterized by a creatinine clearance (CrCl) less than 30 mL/minute, alfuzosin should be used cautiously.

Alfuzosin: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitor:

Urine Flow:

• Keep track of how easily and frequently you can urinate. Alfuzosin is meant to improve urine flow, so any changes should be noted.

Blood Pressure:

• Monitor your blood pressure regularly, especially when starting alfuzosin or changing the dose. It can cause a sudden drop in blood pressure, especially when standing up, which may lead to dizziness or fainting.

PSA (Prostate-Specific Antigen):

• PSA levels should be monitored periodically, especially in older men, to screen for prostate cancer. Alfuzosin may affect PSA levels, so it's essential to keep an eye on them. However, remember that PSA levels can be affected by other factors besides cancer.

How to take alfuzosin (Uroxatral)?

• Timing: Take alfuzosin right after a meal, at the same time each day. This helps the medication work effectively and reduces the chance of stomach upset.
• Swallow Whole: Take the tablet whole with water. Do not crush or chew it, as this can affect how the medication is released in your body.

By following these instructions, you can ensure that alfuzosin is absorbed properly and works as intended to manage your condition.

mechanism of Action:

• Alfuzosin works by blocking alpha-adrenoreceptors in the lower urinary tract.
• These receptors are sensitive to signals from the sympathetic nervous system, which can cause the smooth muscles in the prostate, prostatic capsule, prostatic urethra, and bladder neck to contract.
• By blocking these receptors, alfuzosin helps these muscles relax, leading to improved urine flow rate and reduced symptoms of benign prostatic hyperplasia (BPH).
• This relaxation makes it easier for urine to pass through the urinary tract, relieving symptoms like frequent urination, weak stream, and difficulty starting urination.

Absorption:

• Absorption of alfuzosin decreases by 50% under fasting conditions. Taking it with food improves absorption, with a bioavailability of 49% following a meal.

Distribution:

• The volume of distribution (V) is 3.2 liters per kilogram (L/kg), indicating its distribution throughout the body.

Protein Binding:

• Alfuzosin binds to proteins in the blood, with a binding rate of 82% to 90%.

Metabolism:

• Hepatic metabolism, primarily via the enzyme CYP3A4, is the main route of metabolization for alfuzosin. It undergoes oxidation, O-demethylation, and N-dealkylation, forming inactive metabolites.

Half-life Elimination:

• The half-life of elimination for alfuzosin is approximately 10 hours.

Time to Peak, Plasma:

• Following a meal, alfuzosin reaches its peak plasma concentration around 8 hours after administration.

Excretion:

• Alfuzosin is primarily excreted through feces (69%) and urine (24%), with only 11% of the drug being excreted unchanged in urine.

International Brand Names of alfuzosin:

• Alfu-Kal XL
• Alfumax
• Alfurix XL
• Nuo Shu An
• Profuzosin
• Alfron XL
• Alfsin XL
• Uroxatral
• Uroxatral OD
• Uroxatral uno
• Alfasin XR
• Alfirum
• Alfu
• Alfusin
• Alfutor ER
• Azosin SR
• Benestan
• Benestan OD
• Benprostex
• Bundisarin
• Dalfaz
• Danafusin
• Alfuzo XL
• Alfuzon XL
• Alsiful S.R.
• Flotral
• Fozal
• Fuzocim
• Lafunomyl
• Lafuzo
• Lura XL
• Mittoval
• Prosterol
• Ranfuzosin
• Tevax
• Unibenestan
• Urion
• Uritab XL
• Uriten
• WeiPing
• Xatger
• Xatosin XL
• Xatral
• Xatral LP
• Xatral OD
• Xatral Retard
• Xatral SR
• Xatral XL
• Xatral XL PR
• Xatral XR 10
• Zapros XL
• Apo-Alfuzosin
• Sandoz-Alfuzosin
• Teva-Alfuzosin PR

Alfuzosin brand names in Pakistan: