Camiren CL - instructions for use, dose, side effects, contraindications

Doxazosin is a selective competitive blocker of postsynaptic alpha 1-adrenergic receptors. By reducing the tone of the muscles of blood vessels doxazosin reduces the overall peripheral vascular resistance, which leads to a decrease in blood pressure (BP). After a single administration of the drug, a maximum of hypotensive action 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 there are no differences in the values of blood pressure in the standing and lying position. Effective in hypertension, including, accompanied by metabolic disorders (obesity, decreased tolerance to glucose).

Reduces the risk of coronary heart disease.

Admission of the drug in individuals with normal arterial pressure (BP) is not accompanied by a decrease in blood pressure. With prolonged use of doxazosin in patients, there is no change in tolerance to the therapeutic antihypertensive effect.

During the treatment with doxazosin, a decrease in the plasma concentration of triglycerides, total cholesterol, is observed. At the same time, there is a certain (by 4-13%) increase in the HDL / total cholesterol ratio.

With prolonged treatment with doxazosin, regression of left ventricular hypertrophy, suppression of platelet aggregation, and an increase in active plasminogen content in tissues are observed.

Due to doxazosin blocks α₁- adrenergic receptors located in the stroma and capsule of the prostate gland and in the neck of the bladder, the resistance and pressure in the urethra decrease, the resistance of the internal sphincter decreases. Therefore, the appointment of doxazosin to patients with symptoms of benign prostatic hyperplasia leads to a significant improvement in urodynamics and a decrease in symptoms of the disease.The 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. Compared with the drug in tablets and the drug in the dosage form of the modified release tablet, the latter improves the relationship between efficacy and safety.

Pharmacokinetics:

After ingestion, Camiren®XL is well absorbed.

Absorption - 80-90% (simultaneous intake of food slows down absorption by 1 hour).

The time to reach the maximum concentration in the blood plasma is 8-9 hours. The level of the maximum concentration in the blood plasma of modified-release tablets is only one-third as compared to conventional tablets, and the level of the minimum plasma concentration is the same in both forms of the preparation. In this regard, the profile of doxazosin in plasma with the use of modified release tablets is more smooth, and the ratio between the maximum and minimum concentration is half that of conventional tablets. Bioavailability - 60-70% (presystemic metabolism). The connection with blood plasma proteins is about 98%.Excretion from the blood plasma occurs in 2 phases, with a finite half-life - 19-22 hours, which allows you to prescribe the drug once a day.

Intensively metabolized in the liver by o-demethylation and hydroxylation. In patients with impaired liver function, as well as when taking drugs that can alter hepatic metabolism, the biotransformation of the drug may be disrupted. The main excretion through the intestine, mainly in the form of metabolites, only 5% is excreted in the urine unchanged. The kidneys show 10%. A study of the pharmacokinetics of doxazosin in elderly patients and patients with kidney disease did not reveal significant pharmacokinetic differences.

Indications:The drug is recommended for the treatment of mild to moderate arterial hypertension (in combination with other antihypertensive agents - thiazide diuretics, beta adrenoblockers, slow calcium channel blockers, angiotensin converting enzyme (ACE) inhibitors) and for symptomatic treatment of benign prostatic hyperplasia .

Contraindications:

Camirin should not be administered to patients with hypersensitivity to doxazosin and other quinazoline derivatives (prazozin, terazosin) or to other components of the drug, under the age of 18 years (efficacy and safety not established).

Due to doxazosin blocks α₁- adrenergic receptors located in the stroma and capsule of the prostate gland and in the neck of the bladder, the resistance and pressure in the urethra decrease, the resistance of the internal sphincter decreases. Therefore, the appointment of doxazosin to patients with symptoms of benign prostatic hyperplasia leads to a significant improvement in urodynamics and a decrease in symptoms of the disease. The 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. Compared with the drug in tablets and the drug in the dosage form of the modified release tablet, the latter improves the relationship between efficacy and safety.

Carefully:Aortic and / or mitral stenosis,right-sided heart failure due to pulmonary embolism or exudative pericarditis, left ventricular heart failure with low filling pressure, simultaneous use of PDE-5 inhibitorssildenafil, vardenafil, tadalafil), intraoperative irrosis of the iris, mild to moderate hepatic insufficiency, (Class A and B according to the Child-Pugh classification), propensity to arterial hypotension (orthostatic disorders of blood circulation regulation), pregnancy.

Pregnancy and lactation:Pregnant women can prescribe the drug only for vital signs, when the benefit to the mother exceeds the potential risk for the fetus / child. Safety of the drug in infants is not established, therefore, it is recommended that nursing mothers stop feeding during doxazosin treatment.

Dosing and Administration:

Inside, 1 time per day (morning or evening), regardless of food intake, without chewing and drinking with sufficient water.

The dose of the drug should be adjusted depending on the effectiveness of the drug or possible side effects in specific patients.Patients with hepatic insufficiency require lower doses due to a slow metabolism of the drug.

If the patient forgot 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, you should only take it (without doubling the dose of the drug). It is important to take the drug regularly. If the patient did not take the drug for several days, the new therapeutic course should begin with the lowest dose.

Arterial hypertension: The usual dose of Camirena® CL is 1 tablet (4 mg) per day. Its effect can be observed as early as the first day, the therapeutic effect occurs 4 weeks after the start of treatment. After 4 weeks, in case of good tolerability of the drug and if the doctor finds the effect insufficient, higher doses may be prescribed. The maximum recommended daily dose of Camirena® CL is 2 tablets (8 mg) in one session.

If the therapeutic effect is not enough, patients can simultaneously receive other antihypertensive agents: beta-blockers, diuretics, slow calcium channel blockers, and ACE inhibitors.

After achieving a stable therapeutic effect, the dose is usually somewhat reduced (the average therapeutic dose with maintenance therapy is usually 2-4 mg per day), you can go on taking Camiren® CL, tablets of 2 or 4 mg.

Benign hyperplasia prostate gland in patients with normal blood pressure: the usual dose is 1 tablet (4 mg) Camirena® CL per day. The patient should take the first dose in the evening before bedtime. Depending on the effect of the drug, the dose can be gradually increased at intervals of 1-2 weeks to 8 mg once a day. Typically, the average daily doses range from 2 mg to 4 mg, you can switch to taking Camiren® CL, tablets of 2 or 4 mg Maximum daily dose is 8 mg.

Benign hyperplasia of the prostate gland of patients with arterial hypertension: the dose of the drug is the same as in the case of hypertension without benign prostatic hyperplasia (see doses for hypertension).

The drug is used for a long time. The duration of treatment is determined by the attending physician.

Side effects:

Arterial hypertension.

In clinical trials, orthostatic hypotension was most often observed, especially at the beginning of treatment, which in rare cases can lead to fainting.

Common reactions: asthenia, fatigue, malaise.

From the cardiovascular system: swelling, fainting.

From the central and peripheral nervous system: dizziness, headache, drowsiness.

From the gastrointestinal tract:

nausea, vomiting, diarrhea, gastritis.

From the respiratory system:

rhinitis.

Benign prostatic hyperplasia (BPH)

Patients with BPH have the same side effects as patients with hypertension, as well as:

Common reactions:

allergic reactions, skin rashes, urticaria, back pain, a feeling of heat ("hot flashes" of blood to the skin of the face).

From the cardiovascular system:

reduction of blood pressure, orthostatic hypotension.

From the central and peripheral nervous system:

dry mouth, priapism, hyposthenia, parasthesia, tremor, impotence, insomnia, increased excitability.

From the endocrine system:

gynecomastia.

From the gastrointestinal tract:

abdominal pain, constipation, diarrhea, dyspepsia, flatulence, nausea, loss of appetite.

From the hematopoiesis:

leukopenia, purpura, thrombocytopenia.

From the hepatobiliary system:

increased activity of "hepatic"

enzymes, cholestasis, hepatitis, jaundice.

From the musculoskeletal system:

arthralgia, muscle cramps, weakness in the muscles, myalgia.

From the respiratory system:

bronchospasm, cough, shortness of breath, nosebleed. From the skin: alopecia.

From the sense organs:

blurred vision, tinnitus.

From the urinary system:

dysuria, hematuria, disorder

urination, nocturia, polyuria, urinary incontinence.

And also the following adverse reactions in patients with arterial hypertension (cause-and-effect relationship not established): bradycardia, tachycardia, palpitation, chest pain, angina pectoris, myocardial infarction, cerebral circulation disorder and arrhythmia.

Overdose:

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

Treatment: the patient must immediately put in a horizontal position, with his head down, raise his legs.Symptomatic therapy is performed.

Dialysis is ineffective.

Interaction:

Doxazosin enhances the antihypertensive effect of antihypertensive agents.

There was no adverse interaction with simultaneous use of doxazosin and thiazide diuretics, furosemide, βadrenoblockers, blockers of "slow" calcium channels, ACE inhibitors, antibiotics, oral hypoglycemic agents, indirect anticoagulants and uricosuric agents.

With simultaneous use with induction of microsomal oxidation in the liver, it is possible to increase the effectiveness of doxazosin, with inhibitors - decrease. Non-steroidal anti-inflammatory drugs (especially indomethacin), estrogens (fluid retention) and sympathomimetic agents can reduce the hypotensive effect of doxazosin.

Special instructions:

Postural hypotension / syncope.

As with any α-blockers, especially at the beginning of therapy, a small percentage of patients have a postural hypotension, manifested by dizziness and weakness or loss of consciousness (fainting).In this regard, it is recommended to monitor blood pressure, especially at the beginning of therapy with the drug Camiren® CL. Against the background of taking the drug Camiren® CL, in order to avoid the development of postural hypotension, one should refrain from rapid changes in body position. Patients should be advised to take special care in situations that can lead to injuries in the event of dizziness or weakness. Simultaneous application with inhibitors of phosphodiesterase-5 (PDE-5)

Care should be taken when application of

preparation Camirin® HL with PDE-5 inhibitors, since in some patients this can lead to symptomatic hypotension. Studies of simultaneous the use of PDE-5 inhibitors and Camirin® CL was not performed.

Intraoperative syndrome of atonic iris (variant of the syndrome "narrow pupil ") was observed in some patients for cataract surgery who received or received treatment with beta-blockers.Since the intraoperative syndrome of atonic iris can lead to more complications during surgical interventions,

It is necessary to warn the surgeon that α₁-adrenoconvertors are taken at this time or were taken earlier before the operation. Priapism

There are reports of cases of development of prolonged erection and priapism in the background of therapy α₁adrenoblockers, including doxazosin. If the erection persists for more than 4 hours, you should immediately seek medical help. If the therapy of priapism has not been carried out immediately, the ego can lead to damage to the tissues of the penis and an irreversible loss of potency.

Impaired liver function

Care should be taken when using the drug Camiren® CL, as well as other drugs completely exposed to biotransformation in the liver, to patients with impaired liver function. The use of the drug Camiren® CL in patients with severe impairment of liver function has not been studied, and therefore, the use of the drug in this category of patients is not recommended.

Use in patients with impaired function of the gastrointestinal tract Significant increase in the passage speed of the drug Camiren® CL in the gastrointestinal (for example, after surgical resection) may affect the pharmacokinetics of the drug and its clinical effectiveness.

In patients with severe gastrointestinal stenosis tract

(pathological or iatrogenic), the drug Camiren® CL, like any other non-deformable tablets, should be used with caution. There have been reports of rare cases of obstruction symptoms in patients with strictures receiving other drugs in the form of non-deforming dosage forms with sustained release of the active substance.

Before the onset of symptomatic therapy of prostatic hyperplasia, it is necessary to exclude her cancerous degeneration.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased

concentration of attention and speed of psychomotor reactions (risk of dizziness, weakness).

Form release / dosage:Modified-release tablets 4 mg.

Packaging:10 tablets in a blister pack. 1, 3 or 9 blisters in a cardboard box together with instructions for use.

Storage conditions:10 tablets in a blister pack. 1, 3 or 9 blisters in a cardboard box together with instructions for use.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001917

Date of registration:23.02.2011 / 11.11.2015

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

KRKA, dd, Novo mesto, AO Slovenia

Representation: & nbspKRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Information update date: & nbsp25.01.2016

Illustrated instructions

Instructions

Camirin® HL (Kamiren® XL)