Description
Latin name
Afluprost MP
Release form
sustained release tablets
packaging 30 pcs
Pharmacological action of
Pharmacodynamics of
Alfuzosin is a quinazoline derivative that is active when taken orally. It is a selective antagonist of postsynaptic alpha-1 adrenergic receptors. In vitro pharmacological tests have shown the selectivity of the action of alfuzosin on alpha-1 receptors located in the prostate gland, on the bottom of the bladder and in the prostate urethra. As a result of direct exposure to smooth muscle tissue of the prostate gland, alpha-1-adrenergic blockers reduce resistance to urine outflow.
Alfuzosin improves urination by decreasing urethral tone and resistance to outflow from the bladder, facilitating emptying of the bladder. Reception of alfuzosin in patients with benign prostatic hyperplasia is achieved: a significant increase in the maximum current velocity (Qmax) by an average of 30% in patients with Qmax 15 ml / s. Such an improvement has been observed starting with the first dose of
, a significant decrease in resistance to urine flow and an increase in the volume of excreted urine
a significant decrease in the residual volume of urine.
Pharmacokinetics
absorption: the average relative bioavailability is 104.4% compared to the immediate-release form (2.5 mg twice daily) in healthy middle-aged volunteers, and the maximum plasma concentration is reached 9 hours after taking alfuzosin, compared with 1 hour for immediate release form.
The elimination half-life of alfuzosin is 9.1 hours. Studies have shown that the area under the concentration-time curve when taking alfuzosin after eating is comparable to the results when taking alfuzosin before eating, so eating does not affect the pharmacokinetic profile of the drug. Compared with healthy middle-aged volunteers, elderly patients do not increase pharmacokinetic parameters.
Compared with individuals with normal renal function, the average maximum concentration of the area under the concentration-time curve in patients with renal failure is moderately increased, without changing the half-life. This change in the pharmacokinetic profile of alfuzosin is not considered to have clinical significance, therefore, it does not require dose adjustment.
metabolism: the binding of alfuzosin to plasma proteins is about 90%. Alfuzosin is almost completely metabolized in the liver.
excretion: only 11% of alfuzosin unchanged is found in urine. Most metabolites (which do not have activity) are excreted in 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 surgical intervention, as well as in cases of progressive growth, especially in elderly patients.
Contraindications
Hypersensitivity to alfuzosin and / or other components of the drug Alfuprost MR.
Orthostatic hypotension.
Severe impairment of liver function.
Severe renal failure (creatinine clearance less than 30 ml / min).
Congenital lactase deficiency, lactose intolerance, glucose-galactose malabsorption.
Use during pregnancy and lactation
Alfuprost MR is not intended for use in women.
Composition of
Each sustained-release tablet contains:
active substance: alfuzosin hydrochloride 10 mg.
excipients: lactose anhydrous 77 mg, magnesium stearate 2.5 mg, silicon dioxide colloidal 3 mg, povidone (PVP – K 30) 15 mg, talc 2.5 mg, hypromellose 85 mg, hyprolose 155 mg.
Dosage and administration
Inside – 2.5 mg 3 times / day. For patients over 65 years of age – the initial dose is 2. 5 mg 2 times / day (morning and evening) in the future, the dose can be increased (but not more than 10 mg / day).
Side effects
From the digestive system: epigastric pain, nausea, diarrhea rarely – dry mouth.
From the side of the central nervous system: dizziness, headache rarely – drowsiness.
From the cardiovascular system: rarely – tachycardia, orthostatic hypotension.
Allergic reactions: rarely – skin rash, itching.
Other: malaise rarely – swelling, pain behind the sternum.
Drug Interaction
Not recommended combinations: With alpha-1 receptor blockers (prazosin, urapidil, minoxidil): increased antihypertensive effect, risk of severe postural hypotension.
Combinations to take into account: With antihypertensive drugs: increase in antihypertensive effect and risk of postural hypotension (additive action). With CYP3A4 isoenzyme inhibitors (ketoconazole, itraconazole, ritonavir): increased blood alfuzosin concentration.
Overdose
Symptoms: lowering blood pressure.
In case of overdose, the patient should be hospitalized and be in a lying position. Symptomatic treatment of hypotension (vasoconstrictor agents and plasma substitutes (to increase circulating blood volume)) should be performed. Dialysis is ineffective due to the high degree of binding of alfuzosin to proteins.
Storage conditions
In a dry place, at a temperature not exceeding 25 ° C.
Expiration
3 years.
Deystvuyuschee substances
Alfuzozyn
Dosage form
Dosage form
Tablets
San Pharmaceutical Industries Ltd, India
