Doxazosin-Teva, tablets 4 mg 30 pcs

Indications

Active ingredient

Composition

1 tablet contains:

the active ingredient:

doxazosin mesylate (in terms of doxazosin) 4.85 mg (4.00 mg);

excipients:

microcrystalline cellulose 150.11 mg,

lactose (anhydrous) 80.00 mg,

sodium carboxymethyl starch (type A) 2.40 mg,

colloidal silicon dioxide 0.24 mg,

sodium lauryl sulfate 0.24 mg,

magnesium stearate 2.16 mg.

.

How to take, the dosage

Doxazosin is administered orally; it can be taken either in the morning or in the evening.

Benign prostatic hyperplasia

The recommended initial dose of doxazosin is 1 mg once daily in order to

to minimize the possibility of the development of postural hypotension and/or syncopal

state (syncope). Depending on individual urodynamic parameters and the presence of symptoms of BPH, the dose may be increased to 2 mg and then to 4 mg and

to a maximum recommended dose of 8 mg. The recommended interval for increasing the dose

is 1-2 weeks. Generally, the recommended dose is 2 to 4 mg once daily.6

Arterial hypertension

The dosage varies from 1 to 16 mg/day. It is recommended that treatment be started with 1 mg once every

day for 1 or 2 weeks to minimize the possibility of

postural hypotension and/or syncope (syncope) (the “first

dose” phenomenon). After the first dose, the patient should have their blood pressure monitored for 6-8 hours. This is because of the possibility of “first dose” phenomenon, which is particularly pronounced with prior diuretics.

In the next 1 or 2 weeks, the dose may be increased to 2 mg once daily. To achieve the desired BP reduction, if necessary, the daily dose should be increased

gradually, in even intervals up to 4 mg, 8 mg, and up to a maximum of 16 mg, depending on the patient’s response to the medication. The usual dose is 2-4 mg once daily. If a diuretic or other hypotensive drug is added to therapy, the dose of doxazosin must be adjusted depending on the patient’s condition, with further titration under medical supervision.

If therapy with doxazosin has been interrupted for several days, restart with the starting dose.

Use in elderly patients

Dose adjustment is not necessary.

Application in renal failure

The pharmacokinetics of doxazosin in patients with renal failure are not altered, and the

The drug does not worsen the existing renal dysfunction, so in these patients, it

is used in normal doses.

Application in hepatic impairment

Cautious use is necessary.

Application in children

There is no experience with doxazosin in children under 18 years of age.

Interaction

The co-administration of doxazosin with phosphodiesterase type 5 (PDE-5) inhibitors in some patients may lead to symptomatic arterial hypotension.

It has been shown in in vitro studies that doxazosin is a substrate of CYP3A4 isoenzyme. Caution should be exercised when doxazosin and

powerful CYP3A4 isoenzyme inhibitors, such as clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin or voriconazole are used simultaneously.

The majority (98%) of doxazosin in plasma is bound to proteins.

The results of human plasma in vitro studies indicate that doxazosin does not affect the protein binding of digoxin, warfarin, phenytoin or indomethacin. In clinical practice, doxazosin has been used without any evidence of interaction with thiazide diuretics, furosemide, beta-adrenoblockers, antibiotics, oral hypoglycemic agents, uricosuric agents and anticoagulants.

Non-steroidal anti-inflammatory drugs (especially indomethacin), estrogens and sympathomimetic agents may decrease the antihypertensive effect of doxazosin.

Doxazosin, by eliminating the alpha-adrenergic stimulating effects of epinephrine (adrenaline), may lead to tachycardia and arterial hypotension.

The risk of orthostatic hypotension increases when concomitantly taken with sildenafil to treat pulmonary hypertension.

On a single use of doxazosin 1 mg daily for 4 days while concomitant administration of 400 mg cimetidine 2 times daily there was a 10% increase in the mean AUC values and a statistically insignificant increase in the mean Cmax (maximum blood plasma concentration) and mean half-life of doxazosin. A similar 10% increase in mean AUC values of doxazosin with cimetidine is within the range of variability (27%) of mean AUC values for doxazosin compared to placebo.

In concomitant use with other hypotensive agents increases the severity of their effects (dose adjustment is necessary). It is not recommended to take concomitantly with other alpha-adrenoreceptor blockers.

Concomitant use with inducers of microsomal oxidation in the liver may increase the effectiveness of doxazosin, and when used simultaneously with inhibitors – a decrease.

Special Instructions

Ortostatic hypotension/fainting

As with any alpha-adrenoblocker treatment, particularly at the start of therapy, a small percentage of patients have experienced orthostatic (postural) hypotension manifested by dizziness and weakness or loss of consciousness (fainting). Before prescribing any alpha-adrenoblocker, the patient should be warned about how to avoid symptoms of orthostatic hypotension, in particular, it is necessary to refrain from rapid changes of body position. At the start of doxazosin treatment, the patient should be advised to exercise caution if weakness or dizziness occurs.

Doxazosin should be used with caution in elderly patients due to the possibility of orthostatic hypotension. The risk of dizziness, visual disturbances and fainting increases with age.

The patient should be informed about the increased risk of orthostatic hypotension with alcohol consumption, prolonged standing or exercise, and hot weather.

Benign prostatic hyperplasia

In patients with BPD, doxazosin may be prescribed in the presence of arterial hypertension as well as in normal BP. When used in patients with DPH with normal BP, the change in the latter is not significant. At the same time, in patients with a combination of arterial hypertension and BPD, monotherapy is possible. Doxazosin does not affect the plasma concentration of prostate-specific antigen (PSA).

Prostate carcinoma (cancer) causes many of the symptoms that occur with BPH, and the two diseases may coexist in the same patient. Therefore, prostate carcinoma must be ruled out before using doxazosin to treat BPH.

Application in patients with acute cardiovascular disease

As with any other vasodilators and hypotensive agents, caution should be exercised when using doxazosin preparations in patients with

the following acute cardiovascular disease:

– pulmonary edema caused by mitral valve stenosis or aortic stenosis;

– heart failure with increased cardiac output;

– right ventricular heart failure due to pulmonary embolism or exudative pericarditis;

– left ventricular failure with low filling pressure.

Intraoperative atonic iris syndrome

Intraoperative atonic iris syndrome (a variant of “narrow pupil” syndrome) has been observed in some patients undergoing cataract surgery who are or have been treated with alpha1-adrenoblockers. Because intraoperative atony iris syndrome can lead to increased complications during surgery, alpha1-adrenoblockers must be alerted to the surgeon if alpha1-adrenoblockers are currently being taken or were previously taken prior to surgery.

Combined use with FDE-5 inhibitors

When using doxazosin concomitantly with FDE-5 inhibitors (e.g., sildenafil, tadalafil, vardenafil, udenafil), caution should be exercised,

because both drugs have vasodilator effects, which may lead to development of symptomatic arterial hypotension in some patients. In order to decrease the risk of orthostatic hypotension, treatment with FDE-5 inhibitors is recommended to be started only if hemodynamic parameters of the patient have stabilized with the use of alpha-adrenoblockers. In addition, treatment with FDE-5 inhibitors is recommended to start with the lowest possible dose and maintain a 6-hour interval from doxazosin administration. Studies of concomitant use of FDE-5 inhibitors and preparations of doxazosin with prolonged release have not been conducted.

Hepatic impairment

Cautious use of doxazosin as well as other drugs fully biotransformed in the liver should be observed in patients with hepatic impairment and maximum doses should be avoided. Doxazosin-Teva is not recommended in patients with severe hepatic impairment due to insufficient experience of use.

Pryapism

In post-registration studies, cases of prolonged erections and priapism have been reported with therapy with alpha1-adrenoreceptors, including doxazosin. If an erection persists for more than 4 hours, seek medical advice immediately. If priapism therapy is not carried out immediately, it may lead to penile tissue damage and irreversible loss of potency.

Influence on driving, operating machinery

Dizziness and weakness may occur during treatment with Doxazosin-Teva, especially at the beginning of treatment or when increasing the dose. In this regard, caution should be exercised when driving motor vehicles and engaging in other potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

– Hypersensitivity to doxazosin, quinazoline derivatives (e.g.,

prazosin, terazosin) or any of the excipients of the drug;

– orthostatic hypotension and a history of orthostatic dysfunction;

– severe hepatic impairment (no experience with this category of patients);

– urinary tract infections;

– Anuria;

– progressive renal failure;

– concomitant upper urinary tract obstruction;

– bladder stones;

– patients with urinary incontinence due to bladder overflow (paradoxical

isuria);

– Arterial hypotension (only when used for the indication “Benign

Penatic hyperplasia”);

– Breastfeeding (only when used for the indication “Arterial

hypertension”);

– Children under 18 years of age;

– rare hereditary galactose intolerance, lactase deficiency, glucose-

galactose malabsorption syndrome.

With caution

– pulmonary edema caused by mitral valve stenosis or aortic stenosis;

– heart failure with increased cardiac output;

– right ventricular heart failure due to pulmonary embolism or exudative pericarditis;

– left ventricular heart failure with low filling pressure; 5

– cerebral circulation disorders;

– in patients over 65 years of age because of the risk of orthostatic symptoms (syncope,

dizziness);

– concurrent use with phosphodiesterase type 5 (PDE-5) inhibitors (risk

the threat of symptomatic arterial hypotension);

– liver function disorders;

– pregnancy;

– during cataract surgery.

Side effects

The incidence of side effects is classified according to the recommendations

of the World Health Organization: Very common, at least 10%; common, at least 1%,

but less than 10%; infrequent, at least 0.1%, but less than 1%; rare, at least 0.01%, but less than 0.1%;

very rare, including isolated reports, less than 0.01%.

Benign prostatic hyperplasia7

According to controlled clinical studies, patients with BPH have had the same adverse reactions as patients with arterial hypertension.

The following

adverse reactions have been reported in postmarketing use of doxazosin preparations:

Blood and lymphatic system disorders

very rare: leukopenia, thrombocytopenia.

Disorders of the immune system

very rare: anaphylactic reactions.

Disorders of the metabolism and nutrition

infrequent: anorexia;

rarely: podagra, increased appetite.

Mental disorders

often: excitement, anxiety, insomnia;

infrequent: depression.

Nervous system disorders

very often: dizziness, headache;

often: paresthesia;

not infrequently: hypoesthesia, syncope, tremor.

Visual disturbances

often: impairment of color perception;

infrequent: atonic iris syndrome.

Hearing organ and labyrinth disorders

infrequent: ear noise.

Cardiac disorders

often: tachycardia;

frequently: stenocardia, myocardial infarction, impaired heart rhythm;

very rarely: bradycardia.

vascular disorders

infrequent: “flushes” of blood to the skin of the face, marked decrease in BP, orthostatic

Hypotension.

Disorders of the respiratory system, chest and mediastinal organs

frequently: dyspnea, rhinitis;

infrequent: cough, nasal bleeding; 8

very rare: exacerbation of existing bronchospasm.

Gastrointestinal tract disorders

frequently: abdominal pain, diarrhea, dyspepsia, dry oral mucosa;

not infrequently: meteorism, constipation, gastroenteritis, vomiting;

unknown: disorder of taste.

Liver and biliary tract disorders

very rare: cholestasis, hepatitis, jaundice.

Skin and subcutaneous tissue disorders

infrequent: alopecia, skin itching, skin rash, purpura;

very rarely: hives.

Musculoskeletal and connective tissue disorders

infrequent: arthralgia, back pain, muscle spasms, muscle weakness, myalgia.

Renal and urinary tract disorders

frequently: cystitis, urinary incontinence;

infrequent: increased frequency of urination, polyuria;

very rarely: dysuria, hematuria, nicturia.

Disorders of the genitals and mammary glands

infrequent: impotence;

very rarely: gynecomastia, priapism, retrograde ejaculation.

General disorders and disorders at the site of administration

infrequent: pain of various localization.

Influence on the results of laboratory and instrumental examinations

infrequent: increased body weight;

very rarely: increased liver transaminase activity.

Arterial hypertension

In controlled clinical trials of doxazosin, the most common

adverse reactions that can be categorized as postural (occasionally associated with

fainting) or nonspecific, which included:

Infectious and parasitic diseases

often: respiratory tract infections, urinary tract infections.

Nervous system disorders

very often: dizziness, headache;9

often: postural dizziness (after the first dose may develop

a pronounced decrease in BP, which may lead to orthostatic vertigo, in

/p>

in severe cases, especially with rapid transition from lying to standing

or sitting to fainting

), somnolence.

Hearing and labyrinth disorders

often: vertigo.

Disorders of the respiratory system, thorax and mediastinum

frequently: rinitis.

Gastrointestinal tract disorders

often: nausea.

General disorders and disorders at the site of administration

frequently: asthenia, swelling of the lower extremities, fatigue, weakness.

The following adverse reactions have been noted during the marketing use of

doxazosin in patients with arterial hypertension, although in general these symptoms could

be observed in the absence of treatment with this drug:

frequently: tachycardia, palpitations, chest pain;

not infrequently: stenocardia, myocardial infarction and arrhythmias;

very rarely: bradycardia, cerebral circulatory disorders.

Overdose

Pregnancy use

Pregnancy

While doxazosin did not have teratogenic effects in animal experiments, reduced fetal survival was observed when it was used at exceptionally high doses. These doses were about 300 times higher than the maximum recommended doses in humans.

In the absence of adequate well-controlled studies in pregnant or breastfeeding women, the safety of doxazosin use during pregnancy or during breastfeeding has not yet been established. Therefore, during pregnancy, Doxazosin-Teva may be prescribed only when, in the opinion of the physician, the potential benefit to the mother exceeds the potential risk to the fetus or child.

Breastfeeding period

A case of doxazosin penetration into women’s breast milk has been reported. Studies on laboratory animals have shown that doxazosin accumulates in milk. If it is necessary to use the drug Doxazosin-Teva during lactation, breastfeeding should be stopped.

Similarities