Cardura pills 2mg, 30pcs

Composition

1 tablet contains:

Active ingredient:

doxazosin (in the form of mesylate) 2 mg.

Auxiliary substances:

Sodium starch glycolate,

Microcrystalline cellulose,

Lactose,

Magnesium stearate,

Sodium Lauryl

Sulfate Pharmacological action

Cardura is a vasodilator.

Pharmacodynamics

of BPH

The use of doxazosin to patients with BPH symptoms leads to a significant improvement in urodynamic parameters and a decrease in the manifestations of symptoms of the disease. This effect of the drug is associated with selective blockade of alpha_-1-adrenergic receptors located in the stroma and capsule of the prostate gland, the neck of the bladder.

Doxazosin has been shown to be an effective blocker of the alpha_-1-adrenergic receptor subtype 1A, which accounts for approximately 70% of all alpha_-1-adrenergic receptor subtypes found in the prostate gland. This explains its effect in patients with BPH.

The maintenance effect of doxazosin treatment and its safety have been proven with prolonged use of the drug (for example, up to 48 months).

Arterial hypertension

The use of doxazosin in patients with arterial hypertension leads to a significant decrease in blood pressure as a result of a decrease in OPSS. The appearance of this effect is associated with selective blockade of alpha_-1-adrenergic receptors located in the vascular network. When taking the drug once a day, a clinically significant antihypertensive effect persists for 24 hours, blood pressure decreases gradually; the maximum effect is usually observed 2-6 hours after taking the drug orally. In patients with arterial hypertension ADP during doxazosin treatment was the same in the supine and standing positions.

It was noted that, in contrast to non-selective alpha_-1blockers, long-term treatment with doxazosin did not develop tolerance to the drug. During maintenance therapy, increased plasma renin activity and tachycardia are uncommon.

Doxazosin has a beneficial effect on the blood lipid profile, significantly increasing the ratio of HDL to total cholesterol and significantly reducing the content of total triglycerides and total cholesterol. In this regard, it has an advantage over diuretics and beta-blockers, which do not favorably affect these parameters. Taking into account the established connection of arterial hypertension and blood lipid profile with coronary heart disease, normalization of blood pressure in patients with coronary heart disease is recommended. Blood pressure and lipid concentrations during doxazosin use lead to a reduced risk of CHD.

It was observed that treatment with doxazosin resulted in regression of left ventricular hypertrophy, inhibition of platelet aggregation, and increased activity of the tissue plasminogen activator. In addition, doxazosin has been shown to increase insulin sensitivity in patients with impaired glucose tolerance.

Doxazosin has no adverse metabolic effects and can be used in patients with bronchial asthma, diabetes mellitus, left ventricular insufficiency and gout.

In vitro studies have shown the antioxidant properties of 6′- and 7′- hydroxymetabolites of doxazosin at a concentration of 5 mmol.

In controlled clinical trials conducted in patients with arterial hypertension, treatment with doxazosin was accompanied by an improvement in erectile function. In addition, patients treated with doxazosin experienced less recurrent erectile dysfunction than those treated with antihypertensive drugs.

Pharmacokinetics

After oral use in therapeutic doses, doxazosin is well absorbed; T_max in the blood is reached in about 2 hours.

Doxazosin is approximately 98% bound to plasma proteins.

The primary pathways of doxazosin metabolism are O-demethylation and hydroxylation.

Elimination from blood plasma is biphasic, with a final T_1/2 of 22 hours, which allows the drug to be prescribed once a day. Doxazosin undergoes active biotransformation; only less than 5% of the dose is excreted unchanged.

Use in special patient groups

According to pharmacokinetic studies, in elderly patients and patients with renal insufficiency, the pharmacokinetics of the drug does not significantly differ from those in younger patients with normal renal function.

There are only limited data obtained in patients with impaired liver function on the effects of drugs that can alter hepatic metabolism (for example, cimetidine). In a clinical study in 12 patients with moderate hepatic impairment, a single dose of doxazosin was associated with a 43% increase in AUC and a 40% decrease in true oral clearance. Caution should be exercised when prescribing doxazosin, as well as other drugs that are completely biotransformed in the liver, to patients with impaired liver function (see “Special Instructions”).

Indications

• hypersensitivity to chinazoline, doxazosin or any of the auxiliary components of the drug;
• lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
• the age of 18;
• severe liver failure in the absence of experience in this category of patients;
• urinary tract infection;
• anuria;
• progressive renal failure;
• hypotension and a tendency to orthostatic disorders (including in the anamnesis);
• concomitant obstruction of the upper urinary tract
• stones in the bladder.

With caution:  mitral and aortic stenosis, heart failure with increased minute output, right ventricular failure due to pulmonary embolism or exudative pericarditis, left ventricular failure with low filling pressure, cerebral circulation disorders, elderly age, concomitant use with phosphodiesterase type 5 (PDE-5) inhibitors, as symptomatic hypotension and liver failure may occur.

Contraindications

Hypersensitivity (including to other quinazolines).

Side effects

of BPH

According to controlled clinical trials, patients with BPH experienced the same adverse reactions as those with arterial hypertension.

The following adverse reactions have been reported with post-marketing use of the drug.

From the hematopoietic and lymphatic system:  very rarely — leukopenia, thrombocytopenia.

From the side of the organ of hearing and vestibular apparatus:  infrequently-tinnitus.

From the side of the visual organ:  often-violation of color perception; infrequently-atonic iris syndrome.

From the gastrointestinal tract:  often — abdominal pain, diarrhea, dyspepsia, dryness of the oral mucosa; infrequently-flatulence, constipation, vomiting.

From the liver:  very rarely — cholestasis, hepatitis, jaundice.

From the immune system:  very rarely — anaphylactic reactions.

Laboratory parameters:  infrequently-an increase in body weight; very rarely-an increase in the activity of hepatic transaminases.

From the side of metabolism:  infrequently — anorexia.

From the musculoskeletal system:  infrequently — arthralgia, back pain, muscle spasms, muscle weakness, myalgia.

From the central nervous system and peripheral nervous system:  often-paresthesia; infrequently-hypesthesia, tremor.

From the side of the psyche:  often — agitation, anxiety, insomnia; infrequently-depression.

Urinary tract disorders:  infrequently-frequent urination, polyuria, urinary incontinence; very rarely-dysuria, hematuria, nocturia.

From the side of the reproductive system:  very rarely — gynecomastia, impotence, priapism; very rarely-retrograde ejaculation.

Respiratory system disorders:  often — shortness of breath, rhinitis; infrequently — cough, nosebleeds; very rarely-exacerbation of existing bronchospasm.

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

From the CCC side:  infrequently — flushes of blood to the skin of the face, a pronounced decrease in Blood pressure, postural hypotension.

Other services:  infrequently-pain of various localization.

Arterial hypertension

In controlled clinical trials of the drug Cardura, the most common adverse reactions were those that can be attributed to the type of postural (occasionally associated with syncope) or non-specific, which included the reactions listed below.

From the side of the organ of hearing and vestibular apparatus:  often — vertigo.

From the gastrointestinal tract:  often — nausea.

From the central nervous system and peripheral nervous system:  very often — dizziness, headache; often-postural dizziness (after taking the first dose, a pronounced decrease may develop). Blood pressure, which can lead to orthostatic dizziness, in severe cases, especially with a rapid transition from a lying position to a standing position or to a sitting position – to fainting), drowsiness.

Respiratory system disorders:  often — rhinitis.

Other services:  often-asthenia, swelling of the lower extremities, fatigue, weakness.

Interaction

Concomitant use of Cardura with PDE5 inhibitors may lead to symptomatic hypotension in some patients.

The majority (98%) of doxazosin in blood plasma is bound to proteins.The results of an in vitro study of human plasma indicate that doxazosin does not affect protein binding to digoxin, warfarin, phenytoin, or Indometacin. In clinical practice, Cardura was used without any signs of interaction with thiazide diuretics, furosemide, beta-blockers, NSAIDs, antibiotics, oral hypoglycemic drugs, uricosuric agents and anticoagulants.

With a single application of Cardura at a dose of 1 mg / day for 4 days and with simultaneous use of cimetidine at a dose of 400 mg 2 times / day, there was a 10% increase in the average AUC values and a statistically insignificant increase in the average plasma Cmax and average T 1/2 of doxazosin. A similar 10% increase in mean doxazosin AUC values during cimetidine use is within the range of fluctuations in the variability (27%) of mean doxazosin AUC values compared to placebo.

How to take, course of use and dosage

The drug can be prescribed for taking both in the morning and in the evening.

In benign prostatic hyperplasia, the initial dose of Cardura is 1 mg 1 time / day in order to minimize the possibility of developing postural hypotension and / or syncopal state (syncope). Depending on the individual characteristics of urodynamics and the presence of BPH symptoms, the dose can be increased to 2 mg, and then to 4 mg and to the maximum recommended dose of 8 mg. The recommended interval for increasing the dose is 1-2 weeks. The average recommended dose is 2-4 mg once a day.

In patients with arterial hypertension, the dose of the drug varies from 1 to 16 mg / day. Treatment is recommended to start with 1 mg 1 time / day for 1 or 2 weeks in order to minimize the possibility of developing postural hypotension and / or syncopal state (syncope). Over the next 1 or 2 weeks, the dose can be increased to 2 mg 1 time / day. To achieve the desired reduction in blood pressure, if necessary, the daily dose should be increased gradually, at regular intervals, up to 4 mg,8 mg and up to a maximum of 16 mg, depending on the severity of the patient’s reaction. The average dose is 2-4 mg 1 time / day.

The pharmacokinetics of doxazosin in patients with renal insufficiency does not change, and the drug itself does not aggravate the existing renal dysfunction, so in patients of this group, Cardura is used in normal doses.

When prescribing the drug to elderly patients, no dosage adjustment is required.

There is no experience of using the drug Cardura in children.

Overdose

Symptoms: marked decrease AD, sometimes accompanied by fainting spells.

Treatment: it is necessary to immediately lay the patient on his back and raise his legs, if necessary, conduct symptomatic therapy. The binding of doxazosin to plasma proteins is high, so dialysis is ineffective.

Special instructions

As with treatment with any alpha-blockers (especially at the beginning of therapy), a very small percentage of patients experienced postural hypotension, manifested by dizziness and weakness, or loss of consciousness ( fainting ). Before starting the appointment of any alpha-blocker, the patient should be warned about how to avoid symptoms of postural hypotension. At the beginning of treatment with Cardura, the patient should be advised about the need to exercise caution in case of weakness or dizziness.

Caution should be exercised when Cardura is co-administered with phosphodiesterase type 5 inhibitors, as this may lead to symptomatic hypotension in some patients.

Caution should be exercised when prescribing Cardura, as well as other drugs that are completely biotransformed in the liver, to patients with impaired liver function, avoiding the appointment of maximum doses.

The pharmacokinetics of doxazosin in patients with renal insufficiency does not change, and the drug itself does not aggravate the existing renal dysfunction, so in patients of this group, Cardura is used in normal doses.

When prescribing the drug Cardura, it should be taken into account that the ability to drive a car and mechanisms may deteriorate, especially at the beginning of treatment. Possible development of dizziness.

Form of production

Tablets

Storage conditions

The drug should be stored in a dry place protected from light at a temperature not exceeding 30°C.

Shelf

life is 5 years.

Active ingredient

Doxazosin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets