Buy Alfuprost MR pills 10 mg, 30 pcs
  • Buy Alfuprost MR pills 10 mg, 30 pcs

Alfuzosin

Sun Pharmaceutical Industries Ltd
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2019-09-19
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Clinical Pharmacology

Pharmacodynamics
Alfuzosin is a quinazoline derivative that is active when taken orally. This is a selective antagonist of postsynaptic alpha1-adrenoreceptors. Pharmacological tests in vitro showed the selectivity of alfuzosin on alpha1receptors located in the prostate gland, at the bottom of the bladder and in the prostate part of the urethra. As a result of direct effects on the smooth muscles of the tissues of the prostate gland, alpha1-blockers reduce resistance to urine outflow.

Alfuzosin improves urination parameters, reducing urethra tone and resistance to outflow from the bladder, facilitating the emptying of the bladder. Alfuzosin in patients with benign prostatic hyperplasia achieves:

  • significant increase in maximum current velocity (Qmax) an average of 30% in patients with Qmax ≤ 15 ml / s. This improvement was observed starting from the first dose;
  • a significant decrease in resistance to urine flow and an increase in the volume of urine excreted;
  • significant decrease in residual urine volume.

Pharmacokinetics

suction: the average relative bioavailability is 104.4% compared with an immediate release form (2.5 mg twice a day) in healthy middle-aged volunteers, and the maximum plasma concentration is reached 9 hours after taking alfuzosin, compared to 1 hour for the form immediate release.
The half-life of alfuzosin is 9.1 hours. Studies have shown that the area under the concentration-time curve when taking alfuzosin after a meal is comparable to the results of taking alfuzosin before a meal, therefore the meal does not affect the pharmacokinetic profile of the drug. Compared with healthy middle-aged volunteers, elderly patients do not increase pharmacokinetic parameters.

Compared with persons with normal renal function, the average values ​​of the maximum concentration of the area under the "concentration-time" curve in patients with renal insufficiency are moderately increased, without changing the half-life. This change in the pharmacokinetic profile of alfuzosin is not considered to have clinical significance, and therefore it does not require dose adjustment.

metabolism: Alfuzosin binding to plasma proteins is about 90%. Alfuzosin is almost completely metabolized in the liver.

elimination: only 11% of alfuzosin unchanged is found in the urine. Most of the metabolites (which are not active) are excreted in the feces (75-90%).
The pharmacokinetic profile of alfuzosin does not change in chronic heart failure.

Indications

Treatment of functional manifestations of benign prostatic hyperplasia in the absence of the possibility of surgical intervention, as well as in cases of progressive growth, especially in elderly patients.

Composition

Each tablet of prolonged action contains:
active substance: alfuzosin hydrochloride 10 mg.
Excipients:anhydrous lactose 77 mg, magnesium stearate 2.5 mg, colloidal silicon dioxide 3 mg, povidone (PVP - K 30) 15 mg, talc 2.5 mg, hypromellose 85 mg, hyprolosis 155 mg.

Alfuzosin is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Alfuprost MR Sun Pharmaceutical Industries Ltd India pills
Dalfaz CP Sanofi-aventis France pills
Dalfaz retard Sanofi-aventis France pills

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Alfuzosin

Dosage and Administration

Inside - 2.5 mg 3 times / day. For patients older than 65 years old - the initial dose is 2.5 mg 2 times / day (morning and evening); further, the dose may be increased (but not more than 10 mg / day).

Adverse reactions

From the digestive system: epigastric pain, nausea, diarrhea; rarely, dry mouth.

From the side of the central nervous system: dizziness, headache; rarely - drowsiness.

Since the cardiovascular system: rarely - tachycardia, orthostatic hypotension.

Allergic reactions: rarely - skin rash, itching.

Other: malaise; rarely - swelling, pain behind the sternum.

Contraindications

  • Hypersensitivity to alfuzosin and / or other components of the drug Alfuprost MR.
  • Orthostatic hypotension.
  • Severe abnormal liver function.
  • Severe renal failure (creatinine clearance less than 30 ml / min).
  • Congenital lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Drug interactions

Not recommended combinations:
With alpha blockers1-receptors (prazosin, urapidil, minoxidil): increased hypotensive effect, the risk of severe postural hypotension.
Combinations to be taken into account:
With antihypertensive drugs: increased hypotensive effect and the risk of postural hypotension (additive effect). With CYP3A4 isoenzyme inhibitors (ketoconazole, itraconazole, ritonavir): an increase in the concentration of alfuzosin in the blood.

Pregnancy and Lactation

The drug Alfuprost MR is not intended for use in women.

Special instructions

In some individuals, especially in patients receiving antihypertensive treatment, within a few hours after taking alfuzosin, as with other alpha1-adrenergic blockers, postural hypotension may develop, with or without symptoms (dizziness, fatigue, sweating). In such cases, the patient must lie until the symptoms disappear. These phenomena are usually temporary, occur at the beginning of treatment and usually do not affect the continuation of treatment. The patient should be warned about the possibility of such phenomena.

Patients with coronary insufficiency should not be prescribed alfuzosin in monotherapy. It is necessary to continue the treatment of coronary insufficiency. If angina returns or worsens, treatment with alfuzosin should be discontinued. Patients should be warned that pills should be swallowed whole. pills should not be cracked, chewed, crushed or powdered. These actions can lead to inappropriate release and absorption of the active ingredient and, accordingly, to side effects that can quickly develop. A particular risk is associated with the start of treatment, when phenomena such as dizziness, visual disturbances and asthenia can be observed. This should be taken into account when performing potentially hazardous activities that require special attention and quick reactions (driving and other vehicles, working with moving machinery, the work of the dispatcher and operator, etc.).

Overdosage

Symptoms: lowering blood pressure.
In case of overdose, the patient should be hospitalized, be in the "lying" position. Symptomatic treatment of hypotension (administration of vasoconstrictor agents and plasma substitutes (to increase circulating blood volume)) should be carried out. Dialysis is ineffective due to the high degree of binding of alfuzosin to proteins.

  • Brand name: Alfuzosin
  • Active ingredient: Alfuzosin
  • Dosage form: Injection.
  • Manufacturer: Biotechnos SA
  • Country of Origin: Romania

Studies and clinical trials of Alfuzosin (Click to expand)
  1. Voltammetric Analysis of Alfuzosin HCl in Pharmaceuticals, Human Serum and Simulated Gastric Juice
  2. Improved performance of the second generation α1-AGP columns: Applications to the routine assay of plasma levels of alfuzosin hydrochloride
  3. Validated HPLC and HPTLC stability-indicating methods for determination of alfuzosin hydrochloride in bulk powder and pharmaceutical formulations
  4. Effect of intravenous alfuzosin on urethral pressure in patients with neurogenic bladder dysfunction
  5. Zero-order delivery of a highly soluble, low dose drug alfuzosin hydrochloride via gastro-retentive system
  6. Selective and automated sample pretreatment by molecularly imprinted polymer for the analysis of the basic drug alfuzosin from plasma
  7. Safety and pharmacokinetics of alfuzosin 10 mg once daily formulation comparatively to standard formulation (2.5 mg tid) in elderly subjects
  8. High-performance liquid chromatographic determination of alfuzosin in biological fluids with fluorimetric detection and large-volume injection
  9. Direct high-performance liquid chromatographic determination of the enantiomers of alfuzosin in plasma on a second-generation α1-acid glycoprotein chiral stationary phase
  10. Alfuzosin-induced hepatotoxicity
  11. Clinical uroselectivity: evidence from patients treated with slow-release alfuzosin for symptomatic benign prostatic obstruction
  12. Comparison of tamsulosin with alfuzosin in the treatment of patients with lower urinary tract symptoms suggestive of bladder outlet obstruction (symptomatic benign prostatic hyperplasia)
  13. Sustained-release alfuzosin and trial without catheter after acute urinary retention: a prospective, placebo-controlled
  14. The clinical uroselectivity of alfuzosin is not significantly affected by the age of patients with lower urinary tract symptoms suggestive of benign prostatic hyperplasia
  15. Alfuzosin in the treatment of high leak-point pressure in children with neurogenic bladder
  16. Comparison of the relaxant effects of alfuzosin, phentolamine and sildenafil on rabbit isolated corpus cavernosum
  17. Safety and efficacy of alfuzosin 10 mg once-daily in the treatment of lower urinary tract symptoms and clinical benign prostatic hyperplasia: a pooled analysis of three double-blind, placebo-controlled studies
  18. Dose-titration study of alfuzosin, a new alpha1-adrenoceptor blocker, in essential hypertension
  19. Haemodynamic and pharmacokinetic evaluation of alfuzosin in man. A dose ranging study and comparison with prazosin
  20. Wirksamkeit und Sicherheit von Alfuzosin SR bei der BPH
  21. Wirksamkeit und Sicherheit von Alfuzosin SR bei der BPH. Erfahrungen einer Anwendungsbeobachtung mit 11562 Patienten
  22. Effect of alfuzosin on female primary bladder neck obstruction
  23. Alfuzosin: a clinically uroselective α1-blocker
  24. Long Term Follow Up of Men with Alfuzosin who Voided Successfully Following Acute Urinary Retention*

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