Камирен®

General characteristics. Structure:

Active ingredient: 1,215 mg, 2,43 mg or 4,86 mg of a doksazozin of a mezilat that 1,0 mg, 2,0 mg or 4,0 mg of a doksazozin are equivalent.

Excipients: cellulose microcrystallic, lactoses monohydrate, carboxymethylstarch of sodium, magnesium stearate, sodium lauryl sulfate.

The drug rendering hypolipidemic, hypotensive, spasmolytic, vasodilating action. 

Pharmacological properties:

Pharmacodynamics. Doksazozin is the selection competitive blocker of postsynaptic alfa1-adrenoceptors. Reduces the arterial pressure (AP), interfering with reduction of smooth muscles in walls of peripheral vessels and reducing the general peripheric vascular resistance (GPVR). Doksazozin reduces the content of the general cholesterol (GC), cholesterol of lipoproteins of the low density (LPNP), triglycerides (TG) and increases the level of cholesterol of lipoproteins of the high density (LPVP) in a blood plasma; interfering, thus, with development of atherosclerosis and coronary heart disease (CHD).

The therapeutic effect at reception of a single dose of a doksazozin remains for 24 h. The effect concerning the ABP is most expressed during from 2 to 6 h after reception of a doksazozin inside. The maximum therapeutic effect develops in several weeks of regular use of a doksazozin. If the therapeutic effect is insufficient, the patient can use other anti-hypertensive drugs at the same time: beta adrenoblockers, diuretics, blockers of calcium channels and inhibitors of an angiotensin-converting enzyme (APF).

Use of a doksazozin at a high-quality prostatauxe leads to considerable improvement of urodynamic indicators and reduction of symptoms of a disease. The effect is connected with the selection blockade of alfa1-adrenoceptors of the Ia subtype (70% of all subtypes presented in a prostate) which are localized in a muscular stroma, the prostate capsule, in a neck of a bladder and in proximal department of an urethra that reduces a muscle tone of a prostate and facilitates an urination. Renders effect at 66-71% of patients, the beginning of action - in 1-2 weeks of treatment, at most - after 14 weeks, remains for a long time.

Use of a doksazozin for patients with the ABP normal level is not followed by its decrease.

Pharmacokinetics. Absorption and distribution. After intake доксазозин it is well soaked up (absorption of 80-90%) and reaches the maximum concentration in a blood plasma in 1,5 - 3 h. Bioavailability of 60-70%. Almost completely contacts proteins of a blood plasma.

Metabolism. It is metabolized in a liver. The researches in vitro demonstrate that the main way of elimination of drug occurs at the expense of CYP3A4 isoenzyme. In much smaller degree participation of isoenzymes of CYP2D6 and CYP2C19 is possible.

Removal. Doksazozin is brought through intestines, 5% - in not changed look are preferential in the form of metabolites (to 65%); through kidneys about 10% are removed. Elimination half-life of a doksazozin about 16-22 h.

Advanced age. In an equilibrium condition of Cmax and AUC at patients 65 years on average 27% higher and 34%, respectively, in comparison with young people are more senior.

Abnormal liver function. Reception of a doksazozin at patients with a liver failure (a class A on classification of Chayld-Pyyu) increases exposure of a doksazozin in comparison with patients without liver failure by 40%.

Influence of time of a passage on intestines. Much the shortened time of a passage of a doksazozin (e.g., at a syndrome of short intestines) can influence pharmacokinetics of a doksazozin, reducing its concentration in a blood plasma. On the other hand increase in time of a passage on intestines (e.g., at a chronic lock) can increase exposure of a doksazozin that leads to increase in risk of development of undesirable reactions.

Indications to use:

• Benign hyperplasia of a prostate
• Arterial hypertension (including symptomatic) as a part of a combination therapy

Route of administration and doses:

Inside, 1 times a day (in the morning or in the evening) irrespective of meal, without chewing and washing down with enough water. The dose is selected individually depending on reaction of the patient and/or existence of undesirable effects.

If use of the drug Kamiren® is missed, it is necessary to accept the passed dose as soon as possible. If time of use of the following dose approached, the passed pill is not taken, and continue use of the drug Kamiren® according to the established scheme. If the patient does not accept the drug Kamiren® within several days, the course of treatment is begun again with the minimum dose.

Benign hyperplasia of a prostate. An initial dose - 1 mg a day. It is desirable to accept the first dose of the drug Kamiren® in the evening, before going to bed. Depending on therapeutic effect, it is possible to increase a dose of the drug Kamiren® gradually bucketed in 1 - 2 weeks, at first to 2 mg, then to 4 mg and 8 mg of 1 times a day. There is usually enough from 2 mg to 4 mg a day. The maximum daily dose - 8 mg.

Arterial hypertension. An initial dose - 1 mg a day. It is desirable to accept the first dose of the drug Kamiren® in the evening, before going to bed. Depending on the ABP level, it is possible to increase a dose of the drug Kamiren® gradually at an interval of 1 - 2 week, at first to 2 mg, then to 4 mg and 8 mg of a doksazozin of 1 times a day. There is usually enough from 2 mg to 8 mg a day. The maximum daily dose - 16 mg.

Elderly patients. Dose adjustment is not required.

Abnormal liver function. At patients with an abnormal liver function, enough minimum doses (1-2 mg) as доксазозин it is metabolized very slowly.

Renal failure. Dose adjustment is not required.

Features of use:

With care: an aortal and/or mitral stenosis, heart failure owing to a pulmonary embolism or an exudative pericardis, heart failure with low filling pressure, simultaneous use of inhibitors of phosphodiesterase-5 (sildenafit, vardenafit, tadalafit), a syndrome of intraoperative instability of an iris of the eye of an eye, a liver failure (a class A and B on classification of Chayld-Pyyu), pregnancy.

During drug Kamiren® use, patients have to be warned about a possibility of development of orthostatic hypotension.

Postural effects, up to a faint, are especially probable after use of the first dose of the drug Kamiren®. Therefore, the first dose of drug (1 mg) is accepted in the evening, before going to bed. The dose of drug needs to be increased gradually, bucketed in 1 or 2 weeks.

Against the background of drug Kamiren® use, in order to avoid development of orthostatic hypotension, it is necessary to abstain from bystry postural changes of a body.

The drug Kamiren® is not recommended to be accepted to persons with the lowered ABP.

It is necessary to be careful at simultaneous use of inhibitors of phosphodiesterase-5 and the drug Kamiren® since decrease in the ABP is possible. It is necessary to observe a 6-hour interval between use of inhibitors of phosphodiesterase-5 and use the drug Kamiren® (for reduction of risk of decrease in the ABP treatment is begun with use of inhibitors of phosphodiesterase-5).

At surgical interventions concerning a cataract against the background of use of the drug Kamiren® development of a syndrome of intraoperative instability of an iris of the eye of an eye is possible that needs to be considered when carrying out preoperative training of the patient and carrying out surgical intervention.

At an abnormal liver function (especially at simultaneous use of HP with a hepatotoxic action) it is necessary to apply the minimum dose of drug. In case of deterioration in indicators of a functional condition of a liver the drug Kamiren® needs to be cancelled.

Before symptomatic therapy of a hyperplasia of a prostate it is necessary to undergo inspection at the oncologist.

Special inforation about some components of drug. The drug Kamiren® contains lactose in this connection, use of drug is not recommended to patients with a hereditary lactose intolerance, deficit of lactase or a syndrome of glyukozo-galaktozny malabsorption.

There are no data on use of a doksazozin for pregnant women. The drug Kamiren® should not be used during pregnancy except cases when the potential advantage for mother surpasses possible risk for a fruit.
In need of use of the drug Kamiren® in the period of a lactation breastfeeding should be stopped.

 At the beginning of therapy or at increase in a dose of the drug Kamiren® perhaps sharp decrease in the ABP owing to what dizziness can develop. In this regard it is necessary to be careful at control of vehicles and work with the difficult technical devices demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Classification of frequency of development of side effects (WHO):
very often  > 1/10
often             from> 1/100 to <1/10
infrequently         from> 1/1000 to <1/100
seldom             from> 1/10000 to <1/1000
very seldom  from <1/10000, including separate messages.

From cardiovascular system: - it is frequent: arterial hypotension (including orthostatic), heart consciousness, tachycardia; - infrequently: stenocardia, myocardial infarction; - it is very rare: bradycardia, disturbances of a cordial rhythm, "inflows" of blood to face skin, peripheral hypostases.

From a nervous system: - it is frequent: drowsiness, dizziness, headache; - infrequently: stroke, hypesthesias, faint, tremor, agitation, depression, alarm, sleeplessness, nervousness; - it is very rare: paresthesias, postural dizziness.

From sense bodys: - infrequently: a ring in ears; - it is very rare: illegibility of visual perception, syndrome of a "narrow" pupil.

From the alimentary system: - it is frequent: abdominal pain, dyspepsia, dryness of a mucous membrane of an oral cavity; - infrequently: lock, abdominal distention, vomiting, diarrhea, increase in activity of "hepatic" enzymes, appetite loss, anorexia; - it is very rare: hepatitis, cholestasia, jaundice.

From respiratory system: - it is frequent: bronchitis, cough, short wind, rhinitis, xeromycteria; - infrequently: nasal bleeding; - it is very rare: bronchospasm.

From bodies of a hemopoiesis: leukopenia, thrombocytopenia.

From a musculoskeletal system: - it is frequent: dorsodynia, mialgiya;
- not often: arthralgia; - it is rare: spasms, weakness in muscles.

From integuments: - it is frequent: itch; - infrequently: skin rash; - it is very rare: small tortoiseshell, alopecia, purpura.

From urinogenital system: - it is frequent: cystitis, urine incontience; - it is not frequent: dysuria, increase in frequency of an urination, hamaturia, impotence, exacerbation of gout; - it is rare: polyuria; - it is very rare: increase in a diuresis, nocturia, gynecomastia, priapism, retrograde ejaculation.

General reactions: - it is frequent: adynamy, thorax pain, indisposition; - infrequently: face edema, decrease in body weight; - it is very rare: allergic reactions, feeling of fatigue.

Interaction with other medicines:

Doksazozin increases expressiveness of action of antihypertensives (when using a combination with them dose adjustment is required). 

Adverse interaction at simultaneous use of a doksazozin and thiazide diuretics, furosemide, a beta - adrenoblockers, blockers of "slow" calcium channels, APF inhibitors, antibacterial agents, hypoglycemic means for intake, indirect anticoagulants and uricosuric means is noted.

Does not influence extent of linkng with proteins of a blood plasma of digoxin, Phenytoinum, indometacin.

At simultaneous use with inductors of a microsomal oxidation increase in efficiency of a doksazozin, with inhibitors - decrease is possible.
Cimetidinum raises AUC of a doksazozin.

Non-steroidal anti-inflammatory drugs (NPVP), especially indometacin, estrogen (liquid delay) and sympathomimetic means can reduce hypotensive action of a doksazozin.

Eliminating alpha адреностимулирующие effects of Epinephrinum, use of a doksazozin can lead to development of tachycardia and decrease in the ABP.

Simultaneous use of a doksazozin with phosphodiesterase-5 inhibitors (sildenafit, tadalafit, vardenafit) can lead to development of arterial hypotension.

Contraindications:

Hypersensitivity to a doksazozin, to one of components of drug or to other derivatives of quinazoline;
Tendency to orthostatic hypotension;
Benign hyperplasia of a prostate with the accompanying disturbance of outflow of urine from upper parts of urinary tract, persistent infections of uric ways, stones in a bladder;
Lactose intolerance, deficit of lactase, syndrome of glyukozo-galaktozny malabsorption;
The expressed liver failure (a class C on classification of Chayld-Pyyu);
Breastfeeding period;
Age up to 18 years (efficiency and safety are not established);
The crowded bladder, anury in a combination or without the progressing renal failure (as monotherapy).

Overdose:

Symptoms: the expressed decrease in the ABP, a headache, a loss of consciousness, an asthma, a heart consciousness, tachycardia, disturbances of a heart rhythm, nausea, vomiting; the hypoglycemia and a hypopotassemia are possible.

Treatment: gastric lavage, reception of absorbent carbon; the patient needs to be transferred to situation "lying" on spin and to raise legs. At the expressed decrease in the ABP to hold events for completion of the volume of the circulating blood (VCB), if necessary to accept vazopressor. The hemodialysis is inefficient since it доксазозин almost completely contacts proteins of a blood plasma.

Storage conditions:

To store at a temperature not above 30 °C in the places not available to children.

Issue conditions:

According to the recipe

Packaging:

Tablets of 1 mg, 2 mg and 4 mg. On 10 tablets in the blister from the combined material (PVH/PVDH) and aluminum foil. On 2 or 3 blisters together with the application instruction place in a pack cardboard.