sustanon 250

Description

Round biconvex, three-layer tablets: one white layer between two yellow layers with different color intensity. Valid blotches.

Pharmacotherapeutic group

Alpha-1-adrenergic blocker.

pharmacological properties

 

Pharmacodynamics
Sustanon 250 is a quinazoline derivative, active upon oral administration.
It is a selective antagonist of postsynaptic alpha1-adrenergic receptors.
Pharmacological testing in vitro showed selectivity Sustanon 250 for alpha-1 receptors located in the prostate gland at the bottom of the bladder and prostatic urethra.
As a result, direct effects on smooth muscle tissue of the prostate, the alpha 1-blockers reduce the resistance of outflow of urine.
Sustanon 250 improves urinary parameters, reducing the tone of the urethra and resistance to outflow from the bladder, and facilitates emptying of the bladder.
In the placebo-controlled trials of Sustanon 250 in patients with benign prostatic hyperplasia were identified:

  • a significant increase in the maximum flow rate (Qmax) an average of 30% in patients with Qmax ≤ 15 ml / sec. This improvement was observed from the first dose;
  • a significant reduction in current urine resistance and an increase in urine output;
  • significant reduction in residual urine volume.

Pharmacokinetics
The mean relative bioavailability values โ€‹โ€‹of 104.4% as compared to the immediate release form (2.5 mg twice a day) in middle-aged healthy volunteers, and the maximum plasma concentration is reached after 9 hours after dosing, compared with 1 hour for neprolongirovannogo release form.
half-life period is 9.1 hours.
Studies have shown that consistent pharmacokinetic curves are obtained by taking the drug after meals.
compared to healthy middle-aged volunteers in elderly patients the pharmacokinetic parameters do not increase.
compared with those with normal renal function average maximum concentration and area under the curve in patients with renal insufficiency moderately increased without changing the half-life period. This change in the pharmacokinetic profile of the drug is not considered to have clinical value, so it does not require dose adjustments.
Binding Sustanon 250 hydrochloride plasma protein is about 90%. Sustanon 250 undergoes extensive metabolism in the liver, only 11% of the drug in an unmodified form found in urine. Most metabolites (which have no activity) excreted in the feces (75-90%).
The pharmacokinetic profile of Sustanon 250 not change in chronic heart failure.

Indications

Treatment of functional symptoms of benign prostatic hyperplasia.
As an aid in using the catheter for acute urinary retention associated with benign prostatic hyperplasia.

Contraindications

Hypersensitivity to Sustanon 250 and / or other components of the preparation.
Orthostatic hypotension.
Severe hepatic dysfunction.
Severe renal impairment (creatinine clearance <30 mL / min).
Intestinal obstruction (due to the content of the castor oil formulation).

Dosing and Administration

The recommended dose is:. 1 tablet (10 mg) daily, after meal
tablets should be taken in its entirety.

Use as an adjunct to using the catheter for acute urinary retention associated with benign prostatic hyperplasia:
. The recommended dose – 1 tablet of 10 mg per day, after meals, starting from the first day of catheterization
drug used for 3-4 days, then have 2-3 days during use of the catheter and one day after its removal.

Side effect

From the gastrointestinal tract: nausea, epigastric pain, diarrhea, dry mouth. On the part of the central nervous system: headache, dizziness, weakness, drowsiness, asthenic syndrome, fainting, syncope.Since the cardiovascular system: tachycardia , orthostatic hypotension in patients with coronary heart disease – exacerbation of angina symptoms. Allergic reactions: skin rash, itching. Other: edema, flushing of the skin.

Overdose

Symptoms:. Decrease in blood pressure
in the case of an overdose the patient should be hospitalized, remain in a prone position. It is necessary to carry out the traditional treatment of hypotension (introduction vasoconstrictor, macromolecular substances solutions, an increase in the volume of circulating blood). Dialysis is ineffective due to high degree of protein binding Sustanon 250.

Interaction with other drugs

An incorrect combination of
blockers of alpha1-receptors (prazosin, urapidil, minoxidil): increased hypotensive effect, risk of severe postural hypotension.

Combinations to be taken into account
with antihypertensive drugs: antihypertensive effect and increased risk of postural hypotension (additive effect).
With the system CYP3A4 inhibitor (ketoconazole, itraconazole, ritonavir) increase in the blood concentration of Sustanon 250.

Effects on ability to drive vehicles and operate on machines

Side effects such as dizziness, blurred vision and fatigue may occur mainly at the beginning of treatment. This should be taken into consideration when driving a transport and work on the machines.

special instructions

In some individuals, particularly in patients receiving anti-hypertensive treatment for several hours after taking the drug as well as other alpha-1 blockers, adrenergic receptors, postural hypotension can occur with or without symptoms (dizziness, fatigue, sweating). In such cases, the patient must lie until complete disappearance of symptoms. These effects are usually transient, occur at the beginning of treatment and usually does not affect the continued treatment. The patient should be warned of the possibility of such phenomena.
In patients with coronary insufficiency should not be used in monotherapy Sustanon 250. It is necessary to continue the treatment of coronary insufficiency. If the angina worsens or returns, treatment with Sustanon 250 should be discontinued.
Patients should be warned that the tablet should be swallowed whole. Tablets can not crack, chew, crush or rub in powder. These actions can result in inappropriate release and absorption of the active substance and, accordingly, to the side effects that may develop rapidly.

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