Active material: Doksazozin
When ATH: C02CA04
CCF: Alpha1-adrenoblokator. Antihypertensive drugs. Preparation, used in violation of urination in benign prostate hyperplasia glands
ICD-10 codes (testimony): I10, N40
When CSF: 01.01.02.02
Manufacturer: KRKA d.d. (Slovenia)
The modified-release tablet round, slightly biconcave, Film-coated in white.
| 1 tab. | |
| doxazosin mesylate | 4.85 mg, |
| that corresponds to the content of doxazosin | 4 mg |
Excipients: gipromelloza, calcium hydrogen phosphate, anhydrous, lactose monohydrate, magnesium stearate.
The composition of the shell: colorant Opadry white (gipromelloza, titanium dioxide / E 171/), macrogol 400.
10 PC. – блистеры (1) – пачки картонные.
10 PC. – блистеры (3) – пачки картонные.
10 PC. – блистеры (9) – пачки картонные.
Alpha1-adrenoblokator. Doxazosin is a selective competitive blocker of postsynaptic α1-adrenoreceptorov. By reducing the muscle tone of blood vessels doxazosin reduces round, 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 no, and in general hypotensive effect is maintained for a 24 no. During treatment with doxazosin in hypertensive patients with no difference between the values of blood pressure when standing, and lying down.
The drug is effective in hypertension, incl. accompanied by metabolic disorders (obesity, reduced glucose tolerance).
It reduces the risk of coronary heart disease.
Use of the drug in people with normal blood pressure are not accompanied by a decrease in blood pressure. With prolonged use of doxazosin in patients no change in tolerance to the therapeutic effect of antihypertensive.
During treatment with doxazosin is observed reduction of plasma TG, total cholesterol (Hs). Отмечается некоторый рост коэффициента ЛПВП/Хс – на 4-13%.
Long-term treatment with doxazosin observed regression of left ventricular hypertrophy, inhibition of platelet aggregation and increase of tissue plasminogen active.
Because, that doxazosin blocks α1-adrenoreceptory, located in the stroma and the capsule of the prostate and bladder neck, a decrease in resistance and pressure in the urethra, reduced resistance to the internal sphincter. Therefore, the appointment of doxazosin to patients with symptomatic BPH results in a significant improvement in urodynamics and reduce the appearance of disease symptoms.
Начало действия – через 1-2 week of treatment, максимум – после 14 weeks, effect persists for a long time. When compared with doxazosin in the form of conventional tablets of medication in the form of tablets with modified release improves the ratio between efficacy and safety.
Absorption
After oral administration, the drug is well absorbed from the gastrointestinal tract. Absorption sostavlyaet 80-90% (simultaneous intake of food slows the absorption on 1 no). The time to reach Cmax in plasma is 8-9 no. Cmax plasma doxazosin when used in the form of tablets with modified release of only 1/3 compared with conventional tablets, and the level of the minimum concentration (Cmin) doxazosin blood plasma is the same for both forms of the drug. In connection with this profile doxazosin plasma when using modified release tablet smoother, and a ratio between Cmax and Cmin in 2 times lower, than conventional tablets. Bioavailability is 60-70% as a result of first-pass metabolism.
Distribution
Plasma protein binding is about 98%.
Metabolism
Intensively metabolized in the liver by α-demethylation and hydroxylation.
Deduction
Withdrawal of blood plasma takes place in 2 with the final phase T1/2 19-22 no, that allows you to assign the drug 1 time / day. Write mainly through the intestine, primarily as metabolites, only 5% excreted in the urine as unchanged. The kidneys remove about 10%.
Pharmacokinetics in special clinical situations
In patients with impaired liver function, and upon receipt of drugs, capable of altering the hepatic metabolism, possible violation of the biotransformation process of doxazosin.
In the study of the pharmacokinetics of doxazosin in the elderly and in patients with kidney disease not revealed significant differences in the pharmacokinetic.
- The treatment of mild to moderate hypertension (в сочетании с другими антигипертензивными средствами – тиазидными диуретиками, beta-blockers, blockers of slow calcium channels, ACE inhibitors);
- Symptomatic treatment of benign prostatic hyperplasia.
Assign inside 1 time / day, in the morning or evening, regardless of the meal, not chewing and drinking plenty of water.
Arterial hypertension
The average dose of Camiri® HL sostavlâet 4 mg (1 tab.)/d. Effect of the drug can be shown on the first day of treatment, a therapeutic effect occurs within 4 weeks after initiation of treatment. Through 4 of the week, in the case of good tolerability and lack of efficacy, may increase the dose. The maximum recommended daily dose of Camiri® HL sostavlâet 8 mg (2 tab.) in 1 reception.
If the therapeutic effect is not enough, it is possible to simultaneously assign other antihypertensives: beta-blockers, Diuretic, blockers slow calcium channels, ACE inhibitors.
After reaching a stable dose of a therapeutic effect is usually somewhat lower (average therapeutic dose for maintenance therapy is usually 2-4 mg / day): You can go to the reception Camiri® in the form of tablets 2 mg or 4 mg.
Benign prostatic hyperplasia in patients with normal blood pressure
Camiri® CL prescribe a dose 4 mg (1 tab.)/d. The first dose should be taken in the evening before going to bed. Depending on the effectiveness of treatment dose can be gradually increased at intervals 1-2 weeks before 8 mg 1 time / day. Usually, daily dose is 2-4 mg. You can go to the reception Camiri® CL in the form of tablets 2 mg or 4 mg. The maximum daily dose is 8 mg.
Benign prostatic hyperplasia in patients with hypertensive blood pressure
Doses same, as in hypertension patients without benign prostatic hyperplasia.
The drug is used for a long time. The duration of treatment the doctor sets individually.
Dose should be adjusted depending on the effectiveness or adverse reactions in certain patients.
Patients with hepatic insufficiency require smaller doses due to slow drug metabolism.
If the patient has forgotten to take Camiri® CL at the usual time, the drug should be taken as soon as possible in the appropriate dose. If it is time for the next dose, then it should take no doubling. It is important to take the drug regularly. If the patient is taking the drug for several days, the new therapeutic course should start with the lowest dose.
Arterial hypertension
In clinical studies, the most frequently observed, especially at the beginning of treatment, orthostatic hypotension, which in rare cases can cause fainting.
Cardio-vascular system: swelling, fainting.
From the central and peripheral nervous system:
dizziness, headache, drowsiness.From the digestive system: nausea, vomiting, diarrhea, gastritis.
The respiratory system: rhinitis.
Common reactions: asthenia, fatiguability, malaise.
Benign prostatic hyperplasia
Patients with benign prostatic hyperplasia same side effects, that in patients with hypertension, and:
Cardio-vascular system: decrease in blood pressure, orthostatic hypertension.
From the central and peripheral nervous system: dry mouth, priapism, gipesteziya, paresthesia, tremor, impotence, insomnia, hypererethism.
On the part of the endocrine system: gynecomastia.
From the digestive system: stomach ache, constipation, diarrhea, dyspepsia, flatulence, loss of appetite, nausea, increase in liver transaminases, cholestasis, jaundice, hepatitis.
From the side of hematopoiesis: leukopenia, purpura, thrombocytopenia.
On the part of the musculoskeletal system: arthralgia, muscle cramps, muscle weakness, myalgia.
The respiratory system: bronchospasm, cough, breathlessness, nose bleed.
Dermatological reactions: alopecia.
From the senses: blurred vision, noise in ears.
From the urinary system: dizurija, hematuria, violation of urination, nocturia, polyuria, urinary incontinence.
Allergic reactions: skin rash, hives.
Other: backache, feeling the heat (rush of blood to the skin of the face).
Also note the following side effects in patients with hypertension (a causal relationship to drug intake is not installed): bradycardia, tachycardia, palpitations, chest pain, angina, myocardial infarction, cerebrovascular accident, arrhythmia.
- Up to 18 years (efficacy and safety have not been established);
- Hypersensitivity to doxazosin and other ingredients;
- Increased sensitivity to other quinazoline derivatives (prazosin, terazosin).
FROM caution use in patients with aortic and mitral stenosis, in patients with impaired liver and / or kidney, in orthostatic hypotension.
Application of Camiri® CL during pregnancy is possible only for health reasons in the event, when the intended benefits to the mother outweighs the potential risk to the fetus.
Safety of Camiri® CL for infants is not installed, so if necessary, the appointment during lactation should decide the issue of termination of breastfeeding.
Particular caution should be exercised when administering Camiri® CL patients with impaired liver function, especially with concomitant use of drugs, which may adversely affect the function of the liver. In case of deterioration of the functional state of the liver medication should be lifted immediately.
In order to prevent orthostatic reactions, patients should avoid sudden and drastic changes in body position (the transition from a lying position to a standing position).
The effect of the first dose is especially pronounced on the background of previous therapy with diuretics and diet with restriction of sodium.
Before therapy is necessary to eliminate the malignant transformation of prostate cancer.
Upon receipt of alcohol may increase the undesirable effects of doxazosin.
Use in Pediatrics
Safety and efficacy of doxazosin in children has not been established, therefore use is contraindicated in pediatric patients.
Effects on ability to drive vehicles and management mechanisms
Because, doxazosin, which is capable of inducing orthostatic reaction, early treatment and during dose escalation, patients it is advisable to refrain from potentially hazardous activities, in particular from driving and working mechanisms.
Symptoms: marked reduction in blood pressure, sometimes accompanied by fainting.
Treatment: the patient should be immediately transferred to a horizontal position on the back with a low headboard. Symptomatic therapy. Dialysis nyeeffyektivyen.
Doxazosin increases the hypotensive effect of antihypertensive drugs.
There were no adverse interaction with the simultaneous application of thiazide diuretics and doxazosin, furosemida, beta-blockers, blockers slow calcium channels, ACE inhibitors, antibiotics, oral hypoglycemic agents, indirect anticoagulants and urokozuricheskih funds.
In an application with inducers of microsomal oxidation in the liver may increase the effectiveness of doxazosin, с ингибиторами – снижение эффективности.
NSAIDs (especially indomethacin), sympathomimetic agents may reduce the antihypertensive effect of doxazosin. Since estrogen can cause fluid retention, while the application is also possible to decrease the hypotensive effect of doxazosin.
Eliminating alpha adrenostimuliruyuschee effects of epinephrine, doxazosin can cause tachycardia and hypotension.
The drug is released under the prescription.
The drug should be stored out of reach of children, at a temperature no higher than 25 ° C. Shelf life - 2 year.
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