Composition, form of production and packaging
Modified-release tablets are round, slightly biconvex, covered with a film coat of white color.
1 tab.
doxazosin mesylate 4.85 mg,
which corresponds to the content of doxazosin 4 mg
Excipients: hypromellose, calcium hydrophosphate anhydrous, lactose monohydrate, magnesium stearate.
The composition of the shell: dye Opaprai white (hypromellose, titanium dioxide / E 171 /), macrogol 400.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
10 pieces. - blisters (9) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Alpha 1- adrenoblocker. Doxazosin is a selective competitive blocker of postsynaptic? 1- adrenoreceptors. By reducing the tone of the muscles of the vessels, doxazosin reduces the OPSS, which leads to a decrease in blood pressure.
After a single dose of the drug, the maximum antihypertensive effect is observed in the period from 2 to 6 hours, and in general the hypotensive effect persists for 24 hours. During the treatment with doxazosin in patients with hypertension, there are no differences in the values ​​of blood pressure in the standing and lying position.
The drug is effective in arterial hypertension, incl. accompanied by metabolic disorders (obesity, decreased tolerance to glucose).
Reduces the risk of IHD.
The use of the drug in individuals with normal blood pressure 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 content of TG, total cholesterol (Xs) in the blood plasma is observed. There is a slight increase in the HDL / Xc ratio by 4-13%.
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.
In connection with the fact that doxazosin blocks? 1- adrenoreceptors located in the stroma and capsule of the prostate 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 onset of action - after 1-2 weeks of treatment, maximum - after 14 weeks, the effect persists for a long time. When compared with doxazosin in the form of conventional tablets, the formulation in the form of modified release tablets improves the relationship between efficacy and safety.
PHARMACOKINETICS
Suction
After ingestion, the drug is well absorbed from the digestive tract. Absorption is 80-90% (simultaneous intake of food slows down absorption by 1 h). The time to reach Cmax in blood plasma is 8-9 h. C max in the blood plasma of doxazosin when used in the form of modified release tablets is only 1/3 as compared to conventional tablets, and the minimum concentration (C min ) of doxazosin in blood plasma is the same for both forms of the drug. In this regard, the profile of doxazosin in blood plasma with the use of modified release tablets is more smooth, and the ratio between C max and C min is 2 times lower than that of conventional tablets. Bioavailability is 60-70% due to presystemic metabolism.
Distribution
Binding to plasma proteins is about 98%.
Metabolism
Intensively metabolized in the liver by? -demethylation and hydroxylation.
Excretion
Derivation of their blood plasma takes place in 2 phases with a finite T 1/2 of 19-22 h, which allows prescribing the drug 1 time / day. It is excreted primarily through the intestine, mainly in the form of metabolites, only 5% is excreted unchanged in urine. The kidneys excreted about 10%.
Pharmacokinetics in special clinical cases
In patients with impaired liver function, as well as when taking drugs that can change hepatic metabolism, there may be a violation of the biotransformation process of doxazosin.
When studying the pharmacokinetics of doxazosin in elderly patients and in patients with kidney disease, no significant pharmacokinetic differences were found.
INDICATIONS
- treatment of mild or moderate arterial hypertension (in combination with other antihypertensive agents - thiazide diuretics, beta-adrenoblockers, slow calcium channel blockers, ACE inhibitors);
- symptomatic treatment of benign prostatic hyperplasia.
DOSING MODE
Assign inside 1 time / day, in the morning or in the evening, regardless of food intake, without chewing and washing down with a sufficient amount of water.
Arterial hypertension
The average dose of Camirin CL is 4 mg (1 tab.) / Day. The effect of the drug may appear on the first day of treatment, the therapeutic effect occurs 4 weeks after the start of treatment. After 4 weeks, in case of good drug tolerance and with insufficient efficiency, a dose increase is possible. The maximum recommended daily dose of Camirin CL is 8 mg (2 tablets) in 1 dose.
If the therapeutic effect is not enough, then you can simultaneously prescribe other antihypertensive drugs: beta-adrenoblockers, diuretics, slow calcium channel blockers, 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 / day).
Benign prostatic hyperplasia in patients with normal blood pressure
Camirin В® CL is prescribed in a dose of 4 mg (1 tab.) / Day. The first dose should be taken in the evening before bedtime. Depending on the effectiveness of treatment, the dose can be gradually increased at intervals of 1-2 weeks to 8 mg 1 time / day. Typically, the daily dose is 2-4 mg. The maximum daily dose is 8 mg.
Benign prostatic hyperplasia in patients with arterial hypertension
Doses of the drug are the same as for arterial hypertension in patients without benign prostatic hyperplasia.
The drug is used for a long time. Duration of treatment the doctor sets individually.
The dose of the drug should be adjusted depending on the effectiveness or possible adverse reactions in specific patients.
Patients with hepatic insufficiency require lower doses due to a slow metabolism of the drug.
If the patient forgot to take Camirin В® CL at the usual time, then the drug should be taken as soon as possible in the appropriate dose. If it is time to take the next dose, then it should be taken without doubling. 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.
SIDE EFFECT
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.
From the cardiovascular system: swelling, fainting.
From the central nervous system and peripheral nervous system: dizziness, headache, drowsiness.
On the part of the digestive system: nausea, vomiting, diarrhea, gastritis.
From the respiratory system: rhinitis.
Common reactions: asthenia, fatigue, malaise.
Benign prostatic hyperplasia
In patients with benign prostatic hyperplasia, the same side effects as in patients with hypertension, as well as:
From the cardiovascular system: a decrease in blood pressure, orthostatic hypertension.
From the side of the central nervous system and peripheral nervous system: dry mouth, priapism, hypoesthesia, paresthesia, tremor, impotence, insomnia, increased excitability.
On the part of the endocrine system: gynecomastia.
On the part of the digestive system: abdominal pain, constipation, diarrhea, dyspepsia, flatulence, loss of appetite, nausea, increased activity of hepatic transaminases, cholestasis, jaundice, hepatitis.
On the part of the organs of hematopoiesis: leukopenia, purpura, thrombocytopenia.
From the musculoskeletal system: arthralgia, muscle cramps, weakness in the muscles, myalgia.
On the part of the respiratory system: bronchospasm, cough, shortness of breath, nosebleed.
Dermatological reactions: alopecia.
From the senses: blurred vision, tinnitus.
From the urinary system: dysuria, hematuria, urination disorder, nocturia, polyuria, urinary incontinence.
Allergic reactions: skin rash, hives.
Other: back pain, sensation of heat (hot flushes in the skin of the face).
The following side effects were also observed in patients with arterial hypertension (cause-and-effect relationship with taking the drug is not established): bradycardia, tachycardia, palpitations, chest pain, angina pectoris, myocardial infarction, cerebral circulation disorder, arrhythmia.
CONTRAINDICATIONS
- age under 18 years (efficiency and safety not established);
- hypersensitivity to doxazosin and other components of the drug;
- hypersensitivity to other quinazoline derivatives (prazosin, terazosin).
With caution should be used in aortic and mitral stenosis, in patients with impaired liver and / or kidney function, with orthostatic arterial hypotension.
PREGNANCY AND LACTATION
The use of Camirin CL in pregnancy is possible only for life indications in the event that the prospective benefit to the mother exceeds the potential risk to the fetus.
Safety of application of Camiren CL for infants is not established, therefore, if it is necessary to prescribe the drug during lactation, the question of stopping breastfeeding should be solved.
APPLICATION FOR FUNCTIONS OF THE LIVER
Caution should be used in patients with impaired renal function.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Particular care should be taken when administering Camirin CL to patients with impaired liver function, especially when using drugs that may adversely affect liver function. In case of deterioration of the functional state of the liver, the drug should be immediately withdrawn.
Patients with hepatic insufficiency require lower doses due to a slow metabolism of the drug.
APPLICATION FOR CHILDREN
Contraindication: age under 18 years (efficacy and safety not established).
SPECIAL INSTRUCTIONS
Particular care should be taken when administering Camirin CL to patients with impaired liver function, especially when using drugs that may adversely affect liver function. In case of deterioration of the functional state of the liver, the drug should be immediately withdrawn.
In order to prevent orthostatic reactions, patients should avoid sudden and abrupt changes in body position (transition from lying to standing position).
The effect of the first dose is especially pronounced against the background of previous therapy with diuretics and a diet with sodium restriction.
Before the start of therapy, it is necessary to exclude malignant degeneration of the prostate gland.
When taking alcohol, the undesirable effects of doxazosin may be increased.
Use in Pediatrics
Safety and efficacy of doxazosin in children is not established, therefore, use in pediatrics is contraindicated.
Impact on the ability to drive vehicles and manage mechanisms
Due to the fact that doxazosin is able to cause orthostatic reactions at the beginning of treatment and during the period of increasing the dose, it is advisable for patients to refrain from potentially dangerous activities, in particular from driving vehicles and working with mechanisms.
OVERDOSE
Symptoms: marked decrease in blood pressure, sometimes accompanied by fainting.
Treatment: the patient must be immediately moved to a horizontal position on the back with a low headboard. Conduction of symptomatic therapy. Dialysis is ineffective.
DRUG INTERACTION
Doxazosin enhances the antihypertensive effect of antihypertensive agents.
There was no adverse interaction with simultaneous use of doxazosin and thiazide diuretics, furosemide, beta-adrenoblockers, slow calcium channel blockers, ACE inhibitors, antibiotics, oral hypoglycemic agents, indirect anticoagulants and urocozuric agents.
With simultaneous use with induction of microsomal oxidation in the liver, it is possible to increase the effectiveness of doxazosin, with inhibitors - a decrease in efficacy.
NSAIDs (especially indomethacin), sympathomimetic drugs can reduce the hypotensive effect of doxazosin. Since estrogens can cause fluid retention in the body, with simultaneous application it is also possible to reduce the hypotensive effect of doxazosin.
Eliminating the alpha-adrenostimulating effects of epinephrine, doxazosin can cause tachycardia and arterial hypotension.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of the reach of children, at a temperature of no higher than 25 В° C. Shelf life - 5 years.
