Doxazosin-FPO pills 4mg, 30pcs

Composition

1 tablet contains:

Active ingredient:

doxazosin mesylate 1.22 mg / 2.44 mg/ 4.88 mg (in terms of doxazosin

1 mg/2 mg/4 mg);

excipients:

lactose monohydrate 80,18 mg/

90,16 mg/180,32 mg;

calcium phosphate 17,0 mg/35,0 mg/70,0 mg;

povidone K 30 0.4 mg/0.6 mg/1.2 mg;

sodium lauryl sulfate 0.2 mg/0.3 mg/ 0.6 mg;

calcium stearate 0.5 mg/1.0 mg/ 2.0 mg;

talc

0.5 mg/0.5 mg/1.0 mg

drugs, the

Pharmaceutical group:

alpha 1-blocker

Pharmacodynamics :

Doxazosin is a selective competitive blocker of postsynaptic alpha-1-adrenergic receptors (affinity for alpha-1-adrenergic receptors is 600 times higher than for alpha-2-adrenergic receptors), reduces total peripheral vascular resistance (OPSS), prevents vasoconstriction caused by catecholamines, which ultimately leads to a decrease in blood pressure (BP) without the development of reflex tachycardia.

Reduces pre-and post-stress on the heart. After a single dose, a decrease in blood pressure develops gradually, the maximum decrease is observed after 2-6 hours and persists for 24 hours.

After a single dose of the drug, the maximum hypotensive effect is observed in the period from 2 to 6 hours, and in general, the hypotensive effect persists for 24 hours. During treatment with doxazosin in patients with arterial hypertension (AH), there are no differences in blood pressure values in the “standing” and “lying”positions.

It is effective in patients with hypertension, including those accompanied by metabolic disorders (obesity, decreased glucose tolerance).

Reduces the risk of developing coronary heart disease (CHD). Taking the drug in patients with normal blood pressure is not accompanied by a decrease in blood pressure. With prolonged use of doxazosin, patients develop tolerance.

During treatment with doxazosin, there is a decrease in the concentration of triglycerides and total cholesterol in the blood plasma. At the same time, there is a slight (4-13%) increase in the ratio of high-density lipoproteins/total cholesterol.

Long-term treatment with doxazosin results in regression of left ventricular (LV) hypertrophy, inhibition of platelet aggregation, and increased levels of active plasminogen in tissues.

Due to the fact that doxazosin blocks alpha-1-adrenergic receptors located in the stroma and capsule of the prostate gland and in the neck of the bladder, there is a decrease in resistance and pressure in the urethra, a decrease in the resistance of the internal sphincter. Therefore, the use of doxazosin to patients with symptoms of benign prostatic hyperplasia (BPH) leads to a significant improvement in urodynamic parameters and a decrease in the manifestations of symptoms of the disease.

It has an effect in 66-71% of patients, the onset of action – after 1-2 weeks of treatment, maximum-after 14 weeks, the effect persists for a long time.

Pharmacokinetics:  

After oral use in therapeutic doses, doxazosin is well absorbed, absorption is 80-90% (simultaneous food intake slows down absorption by 1 hour), the time to reach the maximum concentration in blood plasma (TMAX) is 3 hours, with evening intake of TMAX is extended to 5 hours.

Bioavailability – 60-70%. The connection with plasma proteins is about 98%. Elimination from blood plasma occurs in 2 phases, with a final half-life (half-life) of 19-22 hours, which allows the drug to be prescribed once a day.

It is extensively metabolized in the liver by o-demethylation and hydroxylation. In patients with impaired liver function, as well as when taking drugs that can change the “hepatic” metabolism, the biotransformation process of the drug may be disrupted. The main excretion is through the intestine (63-65% in the form of metabolites and about 5% in unchanged form).

About 10% is excreted by the kidneys. A study of the pharmacokinetics of doxazosin in elderly patients and patients with kidney disease did not reveal significant pharmacokinetic differences.

Indications

• Benign prostatic hyperplasia: both in the presence of arterial hypertension, and with a normal level of blood pressure.
• Arterial hypertension (as part of combination therapy).

Contraindications

Hypersensitivity to doxazosin and other quinazoline derivatives (prazosin, terazosin) or to other components of the drug;

Tendency to orthostatic hypotension;

hypertension (for patients with benign prostatic hyperplasia);

Patients with BPH and concomitant violation of the outflow of urine from the upper urinary tract, chronic urinary tract infections, bladder stones;

Lactose intolerance, lactase deficiency, or glucose-galactose malabsorption;

Lactation period;

Age up to 18 years (efficacy and safety have not been established);

As monotherapy in patients with either an overflowing bladder or anuria in combination with or without progressive renal failure.

With caution:  Pulmonary edema due to aortic or mitral stenosis;

Right-sided heart failure due to pulmonary embolism or exudative pericarditispravostoronnyaya serdechnaya nedostatochnostʹ vsledstvie legochnoĭ embolii ili ekssudativnyĭ perikardit;

Left ventricular heart failure with low filling pressure;

Concomitant use of phosphodiesterase-5 inhibitors (sildenafil, vardenafil, trandalafil);

Intraoperative iris instability syndrome (narrow pupil syndrome);

Impaired liver function.

Side effects

The frequency of adverse reactions when using the drug Doxazosin is given below in accordance with the generally accepted classification:

very common (≥1/10); common (≥1/100, <1/10); uncommon (≥1/1000, <1/100); rare (≥1/10000, <1/1000); very rare (

From the cardiovascular system:  often-hypertension (including orthostatic), palpitation, tachycardia; infrequently-angina pectoris, myocardial infarction; very rarely-bradycardia, rhythm disorders, ” flushes ” of blood to the skin of the face, peripheral edema.

Central and peripheral nervous system disorders:  often-drowsiness, dizziness, headache; infrequently-stroke, hypesthesia, fainting, tremor, agitation, depression, anxiety, insomnia, nervousness; very rarely-paresthesia, postural vertigo.

From the side of the senses:  often-vertigo; infrequently-tinnitus; very rarely-blurred vision, narrow pupil syndrome.

From the digestive system:  often-abdominal pain, dyspepsia, dryness of the oral mucosa; infrequently-constipation, bloating, vomiting, diarrhea, increased activity of “liver” enzymes, loss of appetite, anorexia; very rarely-hepatitis, cholestasis, jaundice.

Respiratory system disorders:  often – bronchitis, cough, shortness of breath, rhinitis, dryness of the nasal mucosa; infrequently – nosebleeds; very rarely bronchospasm.

From the side of hematopoietic organs:  leukopenia, thrombocytopenia.

Musculoskeletal disorders:  often-back pain, myalgia; not often-arthralgia; rarely-cramps, muscle weakness.

From the side of the skin:  often-pruritus; infrequently-skin rash; very rarely urticaria, allopecia, purpura.

From the genitourinary system:  often cystitis, urinary incontinence; not often-dysuria, increased frequency of urination, hematuria, impotence, gout; rarely-polyuria; very rarely-increased diuresis, urination disorder, nocturia, gynecomastia, priapism, retrograde ejaculation.

General reactions:  often-asthenia, chest pain, malaise; infrequently-pain, swelling of the face, weight loss; very rarely-allergic reactions, fatigue.

Interaction

Doxazosin enhances the antihypertensive effect of antihypertensive agents (when used in combination with them, dose adjustment is required).

No adverse interactions were observed with the simultaneous use of doxazosin and thiazide diuretics, furosemide, beta-blockers, slow calcium channel blockers, angiotensin converting enzyme inhibitors, antibacterial agents, hypoglycemic agents for oral use, indirect anticoagulants and uricosuric agents.

The drug does not affect the degree of binding to plasma proteins of digoxin, phenytoin.

When used concomitantly with inducers of microsomal oxidation enzymes in the liver (ethanol, barbiturates, phenylbutazone, tricyclic antidepressants), it is possible to increase the effectiveness of doxazosin, with inhibitors (cimetidine) – decrease.

Nonsteroidal anti-inflammatory drugs (NSAIDs), especially indomethacin, estrogens (fluid retention), and sympathomimetics may reduce the hypotensive effect of doxazosin.

By eliminating the alpha-adrenostimulating effects of epinephrine, it can lead to tachycardia and hypotension.

Concomitant use with selective phosphodiesterase-5 inhibitors (sildenafil, tadalafil, vardenafil) it can lead to the development of arterial hypotension.

How to take it, course of use and dosage

Inside, once a day (in the morning or in the evening), regardless of food intake, without chewing and drinking enough water.

Patients with hepatic insufficiency require lower doses due to the slow metabolism of the drug.

If the patient has forgotten to take the drug at the usual time, they should take the appropriate dose of the drug as soon as possible. If the time is right for taking the next dose, then only take it (without doubling the dose of the drug). It is important to take the drug regularly.If the patient has not taken the drug for several days, then the new therapeutic course should be started with the lowest dose.

BPH: The initial dose is 1 mg of doxazosin per day. The patient should take the first dose in the evening before going to bed. Depending on the urodynamic parameters and the presence of BPH symptoms, the dose can be gradually increased at intervals of 1-2 weeks to 2 mg,4 mg and 8 mg per day. The recommended maintenance dose is 2-4 mg per day. The maximum daily dose is 8 mg.

After achieving a stable therapeutic effect, the dose is usually reduced (the average therapeutic dose with maintenance therapy is usually 2-4 mg per day).

HYPERTENSION: the initial dose of doxazosin is 1 mg per day before bedtime. After taking the first dose, the patient should stay in bed for 6-8 hours. This is required due to the possibility of developing the phenomenon of the “first dose”, especially pronounced against the background of previous diuretic use. If the therapeutic effect of the drug is insufficient, the daily dose can be increased to 2 mg in 1-2 weeks.

Subsequently, the dose can be increased by 2 mg every 1-2 weeks. In the vast majority of patients, the optimal therapeutic effect is achieved at a dose of 8 mg per day. The maximum daily dose is 16 mg.

Overdose

Symptoms: marked decrease in blood pressure, sometimes accompanied by fainting.

Treatment: gastric lavage, taking activated charcoal.

The patient should be placed on his back and raise his legs. With a pronounced decrease in blood pressure, anti-shock measures are carried out – the volume of circulating blood is replenished, if necessary, vasopressors are prescribed.

Hemodialysis is ineffective.

Special instructions

Special care should be taken when using the drug Doxazosin in patients with impaired liver function, especially in cases where drugs that can change the “hepatic” metabolism are used simultaneously (for example, ethanol, barbiturates, phenylbutazone, tricyclic antidepressants, cimetidine). In cases of deterioration of the functional state of the liver, the drug is immediately discontinued.

In order to prevent orthostatic reactions, patients should avoid sudden and abrupt changes in body position (transition from the “lying” position to the “standing”position).

Caution should be exercised when taking phosphodiesterase-5 inhibitors and doxazosin at the same time, as hypotension may develop. To reduce the risk of hypotension (including orthostatic hypotension), it is necessary to start treatment with phosphodiesterase-5 inhibitors only if the patient has adapted to doxazosin therapy, in addition, a 6-hour time interval from doxazosin should be observed between medications.

During surgical interventions for cataracts while taking the drug, intraoperative instability of the iris (narrow pupil syndrome) may develop, which should be taken into account by the surgeon for preoperative preparation of the patient and during the operation.

Alcohol intake may increase the adverse reactions of doxazosin.

The effect of the “first dose” of the drug is especially pronounced against the background of previous diuretic therapy and a diet with sodium restriction.

Before starting therapy, it is necessary to exclude cancerous degeneration of the prostate gland.

Influence on the ability to drive vehicles and other mechanisms

In the case of taking the drug Doxazosin, care should be taken when driving vehicles or when performing work that requires increased concentration of attention and speed of psychomotor reactions.

Form of production

Tablets are white or white with a creamy tinge of color, round, biconvex in shape.

Storage conditions

In a dark place, at a temperature of 5-25 °C.

Shelf

life is 2 years.

Active ingredient

Doxazosin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For pregnant women as prescribed by a doctor, for Nursing mothers as prescribed by a doctor, For adults as prescribed by a doctor

Indications

Prostatic Hyperplasia, Hypertension