Alfuprost MP - instructions for use, dose, side effects, contraindications

lactose anhydrous 77 mg, magnesium stearate 2.5 mg, silicon dioxide colloid 3 mg, povidone (PVP - To 30) 15 mg, talc 2.5 mg, hypromellose 85 mg, giprolose 155 mg.

Description:From white to almost white, round, biconvex tablets without shell with engraving "RY 10 "on one side.

Pharmacotherapeutic group:Alpha-1-blocker

ATX: & nbsp

G.04.C Drugs for the treatment of benign prostatic hyperplasia

Pharmacodynamics:

Alfuzosin is a derivative of quinazoline, active when ingested. It is the selective antagonist of postsynaptic alpha-1-adrenergic receptors.

Pharmacological tests in vitro showed the selectivity of the action of alfuzosin on alpha-1 receptors located in the prostate gland, at the bottom of the bladder and in the prostate part of the urethra.As a result of direct influence on the smooth muscles of the prostate tissue, alpha-1-adrenoblockers reduce resistance to urine outflow.

Alfuzosin improves the parameters of urination, reducing the tone of the urethra and resistance to outflow from the bladder, facilitating the emptying of the bladder. The use of alfuzosin in patients with benign prostatic hyperplasia is achieved by:

- a significant increase in the maximum current speed (Qmax) on average by 30% in patients with Qmax <15 ml / s. This improvement was observed starting with the first dose;

- 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:

Suction:the mean 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 to 1 hour for forms of 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 with the results when taking alfuzosin before meals, hence eating does not affect the pharmacokinetic profile of the drug. Compared with healthy volunteers of middle age in elderly patients, pharmacokinetic parameters do not increase.

In comparison with individuals with normal renal function, the mean values of the maximum area concentration under the concentration-time curve in patients with renal insufficiency are moderately increased, without changing the half-life. it the change in the pharmacokinetic profile of alfuzosin is not considered to be clinically relevant, and therefore it does not require a dose adjustment.

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

Excretion: Only 11% of alfuzosin is unchanged in urine. Most metabolites (which do not have activity) are excreted with feces (75-90%).

The pharmacokinetic profile of alfuzosin does not change with chronic heart failure.

Indications:

Treatment of functional disorders of urination with benign prostatic hyperplasia.

Contraindications:

Hypersensitivity to alfuzosin and / or other components of the drug. Orthostatic hypotension. Severe liver dysfunction. Severe renal insufficiency (creatinine clearance <30 mL / min).

Congenital lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Dosing and Administration:

Inside.

The recommended dose is: 1 tablet of prolonged action of 10 mg daily after meals. Tablets should be taken whole.

Side effects:

The undesirable effects listed below are given in accordance with the following gradations in the frequency of their occurrence:

Very often: (> 10%);

Often: (> 1% - <10%);
Not often: (> 0.1% - <1%);
Rarely: (0.01% - 0.1%);
Very rarely: (<0.01%) (including individual cases).

From the side of the central nervous system and the psyche: often - weakness, a feeling of general discomfort, headache; infrequently - drowsiness, dizziness, ischemia of the brain in patients with ischemic brain disease.

From the cardiovascular system: infrequently - tachycardia, palpitation, fainting, orthostatic hypotension; very rarely - angina in patients with ischemic heart disease, atrial fibrillation.

On the part of the respiratory system: infrequently - rhinitis.

From the digestive system: often - nausea, abdominal pain, dry mouth; infrequently, diarrhea; very rarely - damage to hepatocytes, liver disease with cholestasis.

Skin and allergic reactions: infrequently - rash, itching; very rarely - hives, angioedema.

Other: often - asthenia; infrequently - skin hyperemia, swelling, chest pain; very rarely - priapism.

Overdose:

Symptoms: lowering of blood pressure.

In case of an overdose, the patient should be hospitalized, in the "lying" position. It should be symptomatic treatment of hypotension (the introduction of vasoconstrictors and plasma substitutes (to increase the volume of circulating blood)). Dialysis is ineffective due to the high degree of binding of alfuzosin to proteins.

Interaction:

Unsupported combinations:

With blockers of alpha-1 receptors (prazozin, urapidil, minoxidil): increased hypotensive effect, risk of severe postural hypotension.

Combinations that should be considered:

FROM hypotensive drugs: increased hypotensive effect and risk of postural hypotension (additive effect).

With inhibitors of isoenzyme CYP3A4 (ketoconazole, itraconazole, ritonavir): increased concentration of alfuzosin in the blood.

Special instructions:

Some patients, especially those who receive antihypertensive treatment, may develop postural hypotension within a few hours after taking alfuzosin, as well as with other alpha-1-adrenoblockers, with or without symptoms (dizziness, fatigue, sweating). In such cases, the patient must lie until the symptoms disappear completely. 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 appointed alfuzosin in monotherapy.

It is necessary to continue treatment of coronary insufficiency. If angina pectoris returns or worsens, alfuzosin treatment should be discontinued. Patients should be warned that the tablet should be swallowed whole. Tablets can not be biting, chewing, grinding or triturating. These actions can lead to inappropriate release and absorption of the active substance and, accordingly, to side effects that can quickly develop.Particular risks associated with the initiation of treatment, when there may be phenomena such as dizziness, visual disturbances and asthenia. This should be taken into account when carrying out potentially hazardous activities requiring special attention and quick reactions (driving and other vehicles, working with moving mechanisms, dispatcher and operator work, etc.).

Effect on the ability to drive transp. cf. and fur:See "Special instructions".

Form release / dosage:Long-acting tablets 10 mg.

Packaging:

10 tablets in a blister of aluminum foil, PVC and acrylic. For 1, 2, 3 and 6 blisters together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-001176

Date of registration:11.11.2011

The owner of the registration certificate:Ranbaxy Laboratories LimitedRanbaxy Laboratories Limited India

Manufacturer: & nbsp

RANBAXY LABORATORIES, Ltd. India

Representation: & nbspRABBAYS LABORATORY LIMITEDRABBAYS LABORATORY LIMITED

Information update date: & nbsp22.08.2015

Illustrated instructions

Instructions

Alfuprost® MR (Afluprost® MP)