Alfuzosin (Uroxatral) - Uses, Dose, Side effects, MOA, Brands

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 dosage:

  • Off-label Use in Ureteral stones:

    • 10 mg oral pill, taken one day.
    • After the body has expelled the stone, the medicine should be discontinued.
  • Benign prostatic hyperplasia (BPH):

    • Ten milligrammes orally, one daily.

Use in Children:

Not recommended in children

Pregnancy Risk Factor B

  • The baby has not been adversely affected by Alfuzosin during pregnancy.

Use during breastfeeding:

  • It is unknown whether breastmilk contains any drug excreted. Take care.   

Alfuzosin dose in kidney disease:

  • The manufacturer has not provided any dose adjustment for renal impairment. 
  • Patients who have significant renal impairment should use it with care.

Alfuzosin Dose in Liver disease:

  • Child-Pugh class A patients who have modest hepatic impairment do not require any dosage adjustments, according to the manufacturer.
  • Patients with moderate or severe hepatic impairment should not use alfuzosin (Child-Pugh class B or C).

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):

  • severe allergic response upon use of alfuzosin or any other formulation ingredient
  • hepatic illness that ranges in severity (Child Class C and B)
    simultaneous usage
  • A few examples are alfuzosin and CYP3A4 inhibitors like itraconazole and ketoconazole.
  • Ritonavir and other alpha1-blockers are used together

Warnings and Precautions

  • Angina
    • If the patient experiences symptoms of angina or worsening of angina pre-existing, discontinue treatment.
  • CNS depression
    • Alfuzosin can cause CNS depression, which may lead to impaired mental or physical abilities.
    • Patients who use heavy machinery need to be extra cautious
  • Floppy iris syndrome:
    • In individuals who have undergone cataract surgery, intraoperative Floppy Iris Syndrome may manifest.
    • Alpha-blockers patients may need to be modified in their surgical procedure.
  • Orthostatic hypotension and syncope:
    • Alfuzosin can relax the vascular tone and may cause orthostatic hypotension or syncope.
    • You should increase the dose gradually and avoid the simultaneous use of antihypertensive medications such as nitrates or phosphodiesterase inhibitors, like sildenafil.
  • Priapism:
    • A sustained painful erection or priapism may occur.
    • If the condition persists for more than four hours, it is important to seek medical advice.
  • Cardiovascular disease
    • Patients with heart disease should be cautious as the drug may cause myocardial ischemia and tachyarrhythmias.
  • Prostate cancer:
    • Prostatic carcinoma should not be treated as it can cause similar symptoms.
  • Extension of QT
    • Patients at high risk of developing prolonged QT intervals should not take Alfuzosin.
    • Patients with grave renal impairment you should take the drug with caution.
  • Use restrictions:
    • AlfuzosinShould not be used in conjunction with antihypertensive medication.

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

Risk Factor C (Monitor therapy).

Alpha-/Beta Agonists The vasoconstricting effects of Alpha/BetaAgonists may be lessened by Alpha1-Blockers. Alpha-/Beta Agonists may also lessen the vasodilation caused by Alpha1-Blockers.
Alpha1-Agonists The vasoconstrictive effects of alpha1-1 agonists may be lessened by alpha1-blockers. Alpha1-Agonists may also lessen the vasodilation caused by Alpha1-Blockers.
Aprepitant High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Beta-Blockers Alpha1-Blockers may increase orthostatic hypotensive effects. Ophthalmic products are less likely to pose a risk than systemic drugs. Exceptions: Levobunolol; Metipranolol.
Blood Pressure Lowering Agents Alfuzosin may increase the hypotensive effects of blood pressure lowering medications.
Bosentan Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
Ceritinib High likelihood that inhibitors will raise blood levels of CYP3A4 substrates. Treatment: Ceritinib should not be taken with a limited CYP3A substrate therapeutic index (eg, alfentanil or cyclosporine, dihydroergotamines, ergotamines, fentanyls, pimozide, quinidines, sirolimus, tacrolimus). Exceptions will be covered separately.
Clofazimine High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Moderate CYP3A4 Inducers Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
Moderate CYP3A4 inhibitors Might decrease metabolism of CYP3A4 substrates (High Risk with Inhibitors).
Dapoxetine Alpha1-Blockers may increase the orthostatic hypotensive effects.
Deferasirox Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
Duvelisib High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Fosaprepitant High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Fosnetupitant High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Haloperidol The QTc-prolonging effects of haloperidol may be enhanced by QT-prolonging substances (Indeterminate risk - Caution).
Ivosidenib might decrease serum levels of CYP3A4 substrates (High Risk with Inducers).
Larotrectinib High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Netupitant High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Nitroglycerin The hypotensive effects of Nitroglycerin could be enhanced by Alfuzosin.
Palbociclib High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Phosphodiesterase 5 Inhibitors Phosphodiesterase 5 inhibitors' hypotensive effects may be exacerbated by alpha1-blockers (Uroselective).
Agents that prolong QT (highest risk) The QTc prolonging effect of QT-prolonging medications may be increased by QT-prolonging agents (Indeterminate risk - Caution). Be cautious to keep an eye out for ventricular arrhythmias or a prolonged QTc interval while using these medications together. There may be additional risk factors in patients who are at increased risk for QTc prolongation.
Rilmenidine Rilmenidine may have a hypotensive effect that Alpha1-Blockers might enhance.
Sarilumab Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
Siltuximab Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
Simeprevir High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Tocilizumab might decrease serum levels of CYP3A4 substrates (High Risk with Inducers).

Risk Factor D (Consider therapy modifications)

Strong CYP3A4 Inducers May increase metabolism of CYP3A4 substrates (High Risk with Inducers). Management: You may consider a different drug to replace one of the interacting drugs. Some combinations might be contraindicated. Consult appropriate manufacturer labeling.
Dabrafenib High risk of Inducers causing a decrease in serum CYP3A4 substrates. Management: If possible, seek alternatives to the CYP3A4 substrate. Concomitant therapy should be avoided if possible. Monitor the clinical effects of the substrate carefully (especially therapeutic effects).
Enzalutamide High risk of Inducers causing a decrease in serum concentrations of CYP3A4 substrates. Management: Avoid concurrent use of enzalutamide and CYP3A4 substrates with a narrow therapeutic index. You should exercise caution when using enzalutamide or any other CYP3A4 sub-substance.
Lorlatinib High risk of Inducers causing a decrease in serum concentrations of CYP3A4 substrates. Management: Do not use lorlatinib concurrently with any CYP3A4 Substrates. Even a slight decrease in serum concentrations could cause therapeutic failure or serious clinical consequences.
Mitotane High risk of Inducers causing a decrease in serum concentrations of CYP3A4 substrates. Treatment: Patients receiving mitotane may require significant adjustments in the dosage of CYP3A4 Substrates.
Pitolisant High risk of Inducers causing a decrease in serum concentrations of CYP3A4 substrates Management: Avoid combining pitolisant and a CYP3A4 substrat with a low therapeutic index. Pitolisant should not be combined with other CYP3A4 sub-substances.
St John's Wort High risk of Inducers causing a decrease in serum CYP3A4 Substrates. Management: You may consider a different drug to replace one of the interacting drugs. Some combinations might be contraindicated. Consult appropriate manufacturer labeling.
Stiripentol High risk of Inhibitors causing an increase in serum concentrations of CYP3A4 substrates. Management: Avoid stiripentol use with CYP3A4 Substrates that have a narrow therapeutic Index. This is to avoid adverse effects and toxicities. Monitoring of any CYP3A4 substrate that is used with stiripentol should be closely done.

Risk Factor X (Avoid Combination)

Alpha1-Blockers This might enhance how effective Alpha1-Blockers are in lowering blood pressure.
Conivaptan High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Strong CYP3A4 inhibitors May increase the serum concentration of Alfuzosin.
Fusidic Acid (Systemic). High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Idelalisib High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Protease inhibitors May increase the serum concentration of Alfuzosin.

Monitor:

  • Urine flow,
  • blood pressure, and
  • PSA (Prostate-specific antigen) levels periodically

How to take alfuzosin (Uroxatral)?

Take the pill after meals at the same time every day, whole (don't chew or crush).

Alfuzosin mechanism of Action:

  • Alfuzosin, an alpha-adrenergic antagonist receptor blocker, is one example. 
  • It works by blocking the alpha receptors, which are primarily found in the smooth muscle of the lower urinary track.
  • This causes relaxation. This causes a decrease in urine flow symptoms such as hesitancy and urgency, poor stream, post-micturition dizziness, and poor stream.
  • Patients with an enlarged prostate often experience all of these symptoms.

Absorption is reduced by 50% under fasting conditions It is 82% to 90% protein-bound.

Bioavailability is 49% after a meal.

Metabolism is primarily via the liver.

Half-life elimination is about 10 hrs

The time to peak plasma concentration is 8 hours following a meal

Excretion is via faeces (69%) and urine (24% Old patients and patients with impaired hepatic function have a 3 - 4 fold increase in the plasma levels.   

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:

Alfuzosin 5 mg Tablets in Pakistan

EZIFLO SR NABIQASIM INDUSTRIES (PVT) LTD.

 

Alfuzosin 10 mg Tablets in Pakistan

EZIFLO XL NABIQASIM INDUSTRIES (PVT) LTD.
KHLOCK XR WILSONS PHARMACEUTICALS
XATRAL-LP SANOFI AVENTIS (PAKISTAN) LTD.
ZATRAL XR WERRICK PHARMACEUTICALS

 

Alfuzosin 2.5 mg Tablets in Pakistan

KHLOCK WILSONS PHARMACEUTICALS
ZATRAL WERRICK PHARMACEUTICALS

 

Alfuzosin SR 5 mg Tablets in Pakistan

ALFUPROZIN NOVINS INTERNATIONAL
FUZIN PULSE PHARMACEUTICALS
XATRAL SANOFI AVENTIS (PAKISTAN) LTD.

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