DOXAZOSIN PILLS 4MG
DOXAZOSIN PILLS 4MG - 30 tabs
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Dosage Form: pills
Ingredients: 1 tablet:
active ingredient: Doxazosin mesylate 0.00122 g, 0.00244 g and 0.00488 g in terms of doxazosin 0.001 g, 0.002 g and 0.004 g;
excipients: [calcium stearate, Calcium hydrogen phosphate dihydrate, lactose monohydrate, kollidon-30 (povidone), sodium lauryl sulfate, talc].
Description: pills of white or white with a creamy shade of color, round, biconvex shape.
Pharmaceutical group: alpha1-blocker
Pharmacodynamics: Doxazosin is a selective competitive blocker of postsynaptic alpha1-adrenergic receptors (affinity for alpha1-adrenergic receptors is 600 times higher than that for alpha2-adrenergic receptors), reduces total peripheral vascular resistance (OPSS), prevents cf. pressure (BP) without the development of reflex tachycardia.
Reduces the pre-and afterload on the heart. After a single dose, a decrease in blood pressure develops gradually, the maximum decrease is observed after 2-6 hours and lasts for 24 hours.
After a single dose of the drug, the maximum of the hypotensive effect is observed in the period from 2 to 6 hours, and in general, the hypotensive effect lasts for 24 hours. In the period of treatment with doxazosin in patients with arterial hypertension (AH) there are no differences in the values of blood pressure in the "standing" and "lying" positions.
Effective with hypertension, including, accompanied by metabolic disorders (obesity, reduced glucose tolerance).
Reduces the risk of 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, a decrease in plasma concentration of triglycerides, total cholesterol, is observed. At the same time, there is some (by 4–13%) increase in the coefficient of high-density lipoprotein / total cholesterol.
With prolonged treatment with doxazosin, there is regression of left ventricular (LV) hypertrophy, suppression of platelet aggregation and an increase in the content of active plasminogen in the tissues.
Due to the fact that doxazosin blocks alpha1-adrenoreceptors located in the stroma and capsule of the prostate gland and in the bladder neck, there is a decrease in resistance and pressure in the urethra, a decrease in resistance of the internal sphincter. Therefore, the administration of doxazosin to patients with symptoms of benign prostatic hyperplasia (BPH) leads to a significant improvement in urodynamic indicators and a decrease in symptoms of the disease.
It has an effect in 66-71% of patients, the onset of action after 1-2 weeks of treatment, the maximum after 14 weeks, the effect lasts for a long time.
Pharmacokinetics: After ingestion in therapeutic doses, doxazosin is well absorbed, absorption - 80-90% (simultaneous ingestion slows down the absorption for 1 hour), the time to reach the maximum plasma concentration (TCmax) is 3 hours, with evening reception of the vehiclemax lengthened to 5 hours.
Bioavailability - 60-70%. Communication with plasma proteins is about 98%. Removal from blood plasma occurs in 2 phases, with a final half-life (T½) - 19-22 hours, which allows you to prescribe the drug 1 time per day.
Extensively metabolized in the liver by odemethylation and hydroxylation. In patients with impaired liver function, as well as when taking drugs that can change the "liver" metabolism, the process of biotransformation of the drug may be disrupted. The main elimination is through the intestines (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 for use:
· Benign prostatic hyperplasia: both in the presence of arterial hypertension and in the normal level of arterial 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;
AH (for patients with benign prostatic hyperplasia);
Patients with BPH and a concomitant violation of the outflow of urine from the upper urinary tract, chronic urinary tract infections, stones in the bladder;
Lactose intolerance, lactase deficiency or glucose-galactose malabsorption;
Age up to 18 years (efficacy and safety have not been established);
As monotherapy in patients with either an overflowing bladder or anuria, with or without a combination of progressive renal failure.
With caution: Pulmonary edema due to aortic or mitral stenosis;
Right-sided heart failure due to pulmonary embolism or exudative pericarditis pravostoronnyaya serdechnaya nedostatochnostʹ vsledstvie legochnoĭ embolii ili ekssudativnyĭ perikardit;
Left ventricular heart failure with low filling pressure;
The simultaneous use of phosphodiesterase-5 inhibitors (sildenafil, vardenafil, trandalafil);
Syndrome of intraoperative instability of the iris of the eye (narrow pupil syndrome);
Use during pregnancy and during breastfeeding: Pregnant women can take the drug only when the benefit to the mother outweighs the potential risk to the fetus / child. There is no data on the penetration of doxazosin into breast milk, therefore it is recommended that nursing mothers stop feeding during the period of treatment with the drug Doxazosin.
Dosage and administration: Inside, once a day (in the morning or in the evening), regardless of the meal, not chewing and drinking plenty of water.
Patients with hepatic impairment require smaller doses due to slow metabolism of the drug.
If the patient has forgotten to take the drug at the usual time, he should take the appropriate dose of the drug as soon as possible. If the time is right for taking the next dose, then you should only take it (without doubling the dose). 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 bedtime. Depending on urodynamic parameters and the presence of symptoms of BPH, 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 of 2 to 4 mg per day. The maximum daily dose is 8 mg.
After reaching a stable therapeutic effect, the dose is usually reduced (the average therapeutic dose with maintenance therapy is usually 2-4 mg per day).
AH: The initial dose of doxazosin is 1 mg per day before bedtime. After taking the first dose, the patient should be in bed for 6-8 hours. This is required in connection with the possibility of the development of the “first dose” phenomenon, especially pronounced against the background of previous diuretic intake. With a lack of therapeutic effect of the drug, the daily dose can be increased to 2 mg in 1-2 weeks.In the next every 1-2 weeks, the dose can be increased by 2 mg. 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.
Side effect: The frequency of adverse reactions with the use of the drug Doxazosin is given below in accordance with the generally accepted classification:
very often (≥1 / 10); often (≥1 / 100, <1/10); infrequently (≥1 / 1000, <1/100); rarely (≥1 / 10000, <1/1000); very rarely (<1/10000).
From the side of the cardiovascular system: often - hypertension (including orthostatic), palpitations, tachycardia; infrequently - angina, myocardial infarction; very rarely - bradycardia, rhythm disturbances, "flushes" of blood to the skin of the face, peripheral edema.
From the central and peripheral nervous system: often - drowsiness, dizziness, headache; infrequently - stroke, hypesthesia, syncope, tremor, agitation, depression, anxiety, insomnia, nervousness; very rarely - paresthesia, postural dizziness.
From the senses: often vertigo; infrequently - ringing in the ears; very rarely - blurred vision, narrow pupil syndrome.
From the digestive system: often - abdominal pain, dyspepsia , dryness of the oral mucosa; infrequently - constipation, abdominal distension, vomiting, diarrhea, increased activity of “liver” enzymes, loss of appetite, anorexia; very rarely - hepatitis, cholestasis , jaundice.
On the part of the respiratory system: often - bronchitis, cough, shortness of breath, rhinitis, dryness of the nasal mucosa; infrequently - nosebleeds; very rarely bronchospasm.
From the side of blood-forming organs: leukopenia, thrombocytopenia.
From the musculoskeletal system: often - back pain, myalgia; not often - arthralgia; rarely - cramps, weakness in the muscles.
From the skin: often itching; infrequently - skin rash; very rarely urticaria, alopecia, purpura.
From the genitourinary system: often cystitis, urinary incontinence; not often - dysuria, increased frequency of urination, hematuria, impotence, gout; rarely polyuria; very rarely - an increase in diuresis, urinary 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.
Overdose: Symptoms: marked decrease in blood pressure, sometimes accompanied by fainting.
Treatment: gastric lavage, taking activated charcoal. The patient must be laid on his back and lift his legs. In case of a pronounced decrease in blood pressure, anti-shock measures are taken - they fill the circulating blood volume, and, if necessary, prescribe vasopressors.
Hemodialysis is ineffective.
Interaction with other drugs: Doxazosin enhances the antihypertensive effect of antihypertensive drugs (when used in combination with them, dose adjustment is required).
Adverse interactions with simultaneous use of doxazosin and thiazide diuretics, Furosemide , beta adrenoblockers, blockers of “slow” calcium channels, angiotensin-converting enzyme inhibitors, antibacterial agents, hypoglycemic agents for oral administration, indirect anticoagulants and urico-curricular agents have not been observed.
The drug does not affect the degree of binding to plasma proteins of Digoxin , phenytoin.
With simultaneous use of enzymes of microsomal oxidation in the liver (ethanol, barbiturates, phenylbutazone, tricyclic antidepressants) with inducers, the effectiveness of doxazosin may be increased, with inhibitors (cimetidine) - reduction. Nonsteroidal anti-inflammatory drugs (NSAIDs), especially Indomethacin , estrogens (fluid retention) and sympathomimetic drugs can reduce the hypotensive effect of doxazosin.
Eliminating the alpha-adrenostimulating effects of epinephrine can lead to tachycardia and arterial hypotension.
Concomitant use with selective phosphodiesterase-5 inhibitors (sildenafil, tadalafil, vardenafil) can lead to the development of arterial hypotension.
Special instructions: Particular caution should be exercised when using the drug Doxazosin in patients with impaired liver function, especially in cases where drugs are used at the same time that can change the “liver” metabolism (for example, ethanol, barbiturates, phenylbutazone,tricyclic antidepressants, cimetidine). In cases of deterioration of the functional status of the liver, the drug is immediately canceled.
In order to prevent orthostatic reactions, patients should avoid unexpected and abrupt changes in body position (moving from the "lying" to the "standing" position).
Care should be taken when taking phosphodiesterase-5 and doxazosin inhibitors at the same time. possible development of arterial hypotension. To reduce the risk of arterial hypotension (including orthostatic), it is necessary to begin treatment with phosphodiesterase-5 inhibitors only if the patient has adapted to doxazosin therapy, and besides, between the administration of drugs, the 6-hour interval from doxazosin administration should be observed.
In case of surgery for cataract on the background of the drug intake, the syndrome of intraoperative instability of the iris of the eye (narrow pupil syndrome) may develop, which must be taken into account by the surgeon for the preoperative preparation of the patient and during the operation.
Taking alcohol can increase the undesirable reactions of doxazosin.
The effect of the “first dose” of the drug is especially pronounced against the background of previous diuretic therapy and a sodium-restricted diet.
Before starting therapy, it is necessary to exclude a cancerous degeneration of the prostate gland.
Influence on ability to drive vehicles and other mechanisms
In the case of taking the drug Doxazosin, caution should be exercised when driving or when performing work that requires high concentration of attention and speed of psychomotor reactions.
Storage conditions: In a dry dark place at a temperature of no higher than 25 aboutC. Keep out of the reach of children.