Camyrin

Camyrin is a selective antagonist acting on α1-adrenergic receptors.

Indications of the camyrena

It is used to reduce the increased blood pressure index. In many patients it is the most commonly used drug for monitoring blood pressure. Persons who can not reduce the pressure to the required level with the use of only one hypotensive drug, it is permitted to combine doxazosin with other drugs, for example, calcium antagonists, thiazide type diuretics, ACE inhibitors, and β-blockers.

In addition, the drug is used to remove the delay of urination, as well as manifestations caused by BPH. People with BPH are allowed to use Camiren in the case of high blood pressure, and with normal BP.

Release form

The release takes place in the form of tablets, in the amount of 10 pieces inside the blister plate. In the package - 2 or 3 blisters with tablets.

Pharmacodynamics

Increased blood pressure.

The use of doxazosin in patients with elevated blood pressure causes a significant decrease in this index, reducing peripheral vascular resistance. This effect is due to the selective blockade of α1-adrenergic receptors located inside the vessels. In the case of using drugs once a day, clinically noticeable antihypertensive effect continues for 24 hours. Basically, the maximum decrease in blood pressure values is observed after 2-6 hours after the use of a 1-time dosage.

In comparison with non-selective α1-adrenoblockers, during the prolonged administration of doxazosin, there is no development of tolerance to the drug.

As a result of prolonged use of Camirin, there is sometimes an increase in the activity of the renin substance inside the plasma, as well as the development of tachycardia.

Doxazosin has a positive effect on blood lipids, significantly increasing the ratio of high-density lipids to the general parameters, and also significantly reducing the total number of triglycerides and total cholesterol values. This factor is the advantage of the drug over β-adrenoreceptors and diuretics, because they have a negative effect on these indicators.

Since the association of elevated blood pressure and metabolic disorders of lipids with the emergence of coronary artery disease has been identified, the positive effects of doxazosin on both blood pressure and atherogenic lipid levels help reduce the likelihood of coronary artery disease.

Therapy with doxazosin can reduce left ventricular hypertrophy, slow platelet aggregation, and increase the activity of plasminogen within tissues. Along with this, the drug increases the sensitivity of peripheral tissue to insulin in people who have abnormalities in this area.

Doxazosin has almost no negative metabolic reactions, so it is permitted to use it for people with diabetes and bronchial asthma, and in addition to hyperkeratosis and impaired left ventricular function.

In men with elevated BP indices, there was also an improvement in erectile function when taking the medication. These individuals recorded a reduced incidence of problems with erection (compared with men taking other antihypertensive drugs).

BPH.

The use of doxazosin by people with signs of prostate adenoma causes a significant improvement in urodynamics, a reduction in symptoms and manifestations of pathology. A similar effect of the drug is due to the selective blockade of α1-adrenergic receptors located inside the stroma of the muscles and the capsule of the prostate, and beyond that inside the neck of the ureter.

Doxazosin is a potent blocker acting on α1-adrenergic receptors that are part of the IA subgroup (they account for approximately 70% of all subcategories of receptors located in the prostate). This explains the impact of drugs on men with prostate adenoma.

The medicine demonstrated stable safety, as well as effectiveness with prolonged therapy in persons with BPH (up to 4 years).

[1], [2], [3], [4], [5], [6], [7], [8], [9]

Pharmacokinetics

After oral administration of the dosage, Camyrin is well absorbed to peak levels after approximately 2 hours.

Excretion from the plasma passes in 2 stages, and the final half-life is 22 hours. This allows you to take the pill once a day. The active substance undergoes active biotransformation - only less than 5% of the dosage is excreted unchanged.

Because the drug is exposed to hepatic metabolism, people with liver problems need to use doxazosin cautiously.

Approximately 98% of the substance undergoes protein synthesis in the blood plasma.

The metabolism of doxazosin mainly occurs through hydroxylation processes, as well as O-demethylation.

[10], [11], [12], [13], [14], [15],

Dosing and administration

The medicine can be taken either in the morning or in the evening.

With increased blood pressure.

During the day, it is permitted to take within 1-16 mg of doxazosin. It is recommended at the initial stage of treatment to drink 1 mg once a day. A similar regimen is used for 1-2 weeks to minimize the possibility of developing syncope or postural hypertension. After this time, it is allowed to increase the dosage to 2 mg per day. If necessary, the daily dosage is allowed to be gradually increased at the intervals indicated above to 4, 8 and 16 mg. But at the same time it is required to constantly monitor the patient's therapeutic response in order to achieve the necessary lowering of the blood pressure level. The size of the standard dose per day is 2-4 mg.

With prostate adenoma.

At the initial stage it is recommended to take 1 mg of medicine per day (once). Taking into account the individual characteristics of urodynamics, as well as signs of pathology, further the dose is allowed to be increased to 2 and then 4 mg. The maximum permissible daily dose is 8 mg. Gaps, through which it is allowed to increase the dosage, are 1-2 weeks. Often the dosage for a day is within 2-4 mg.

[24]

Use of the camyrena during pregnancy

Since there are no adequate, well-controlled drug tests during pregnancy or lactation, it is not possible to determine the safety of its intake in these groups of patients. As a result, Camerin is allowed only in situations where the likely benefits of therapy, according to the doctor, exceed the possibility of complications in the baby.

Although the drug did not have a teratogenic effect in animal tests, its use in extremely high doses (approximately 300 times the maximum permissible for humans) caused a decrease in the fetus's life span.

Because there was no study of the drug safety of Camirin, it can not be used during lactation. If doxazosin is still needed, it will be necessary to refuse breastfeeding for the duration of treatment.

Contraindications

The main contraindications:

• the presence of intolerance with respect to the active substance, quinazoline derivatives (such as prazosin or terazosin) or other elements of the drug;
• adenoma of the prostate, against which there is obstruction in the upper part of the urinary system, as well as chronic forms of infections in the urinary system and the presence of concrements inside the urea;
• decreased BP (applies only to men with prostate adenoma);
• a history of orthostatic collapse;
• The drug is prohibited for monotherapy in persons with urea overflow or with anuria, against which there may be a deficiency of kidneys in the progressing stage;
• it is forbidden to use it for children, because as a result of Camirin's tests, this category of patients was not treated.

[16], [17], [18], [19], [20],

Side effects of the camyrena

Taking medication can lead to the appearance of such side effects:

• infectious or invasive lesions - often there are violations in the urinary or respiratory system;
• diseases in the field of systemic blood flow or lymph - there is a single leuco- or thrombocytopenia;
• immune disorders - allergic symptoms sometimes appear;
• alimentary disorders and problems with metabolic processes - sometimes there is an increase or disappearance of appetite, as well as the development of gout;
• problems with the psyche - sometimes there are feelings of nervousness, excitement or anxiety, and in addition to insomnia or a state of depression;
• lesions of the NA function - often headaches, a feeling of drowsiness and dizziness. Sometimes there is a stroke, tremor, syncope or hypoesthesia. Paresthesia or dizziness of the orthostatic type is noted singly;
• disorders of visual function - single visual obscurity is noted. Perhaps the emergence of intraoperative syndrome, developing in the area of atonic iris;
• disorders in the work of auditory organs - often there is a vertigo. Sometimes there are ear noises;
• lesions of cardiac function - tachycardia often develops or heart rhythm increases. Sometimes there is a development of myocardial infarction or angina pectoris. There is an arrhythmia or a bradycardia;
• diseases in the vascular region - often a decrease in blood pressure (also orthostatic). Singly note the appearance of tides;
• reactions of the respiratory system, as well as the sternum with mediastinum - often there is dyspnea, cough or runny nose or develops bronchitis. Sometimes bleeding from the nose is noted. The already existing spasms of the bronchi are strengthened;
• symptoms of gastrointestinal dysfunction - often there are dyspeptic symptoms, abdominal pain, a feeling of nausea and dryness of the oral mucosa. Sometimes swelling, constipation, diarrhea, gastroenteritis or vomiting develops;
• lesions of the hepatobiliary system - sometimes there are deviations in the values of the hepatic function from the norm. There is jaundice, cholestasis, or hepatitis;
• reactions of the subcutaneous layer and skin - often there is an itch. Sometimes a rash is noticed on the surface of the skin. Purple, hives, or alopecia develops single-handedly;
• disturbances in the function of ODA and connective tissue - often there is myalgia or pain in the back. Sometimes arthralgia develops. Occasionally there is weakness in the muscles or their spasms;
• disorders in the urinary system and kidneys - often show incontinence or cystitis. Sometimes there is an increase in urination, dysuria or hematuria. Occasionally, polyuria develops. There are single violations of urination, increased diuresis or nocturia;
• lesions of the mammary glands and reproductive organs - impotence sometimes develops. There is a single priapism or gynecomastia. Ejaculation of retrograde type is possible;
• systemic disorders - often develop pain in the sternum, asthenia, influenza-like symptoms and swelling of the peripheral form. Sometimes there are swelling on the face and pain in the body. Single mark the state of general malaise or increased fatigue;
• laboratory tests - sometimes weight gain is observed.

[21], [22], [23]

Overdose

If, as a result of intoxication, the blood pressure has dropped significantly, it is required to lay the victim on his back and lower his head down. If necessary, other treatment procedures are allowed. Given the high level of protein synthesis of drugs, the dialysis procedure will be ineffective.

If symptomatic maintenance therapy is not enough, to replace the shock, plasma substitutes should be used first. Further, if necessary, vasoconstrictive drugs are used. It is required to monitor the work of the kidneys and to carry out supportive medical measures, if necessary.

Interactions with other drugs

Use together with PDE-5 inhibitors (element of PDE-5).

Taking doxazosin with inhibitors of the PDE-5 element should be done carefully, because in some individuals there may be signs of a decrease in blood pressure.

Doxazosin tests in therapeutic forms with sustained release of the active ingredient have not been performed.

Other medicines.

Almost all doxazosin is subjected to protein synthesis inside the blood plasma (98%). In vitro tests using human plasma have shown that the drug has almost no effect on the protein synthesis of substances such as warfarin with indomethacin, as well as phenytoin with digoxin.

Clinical data demonstrate the absence of negative interactions in the case of combined administration of the drug with diuretics of the thiazide series, β-blockers, furosemide, NSAIDs, antibiotics, oral hypoglycemic drugs, and anticoagulants. However, no research has been carried out on the interaction of the above-mentioned funds.

Doxazosin enhances the antihypertensive properties of other α-adrenoblockers and other antihypertensive drugs.

Information obtained from clinical trials with male volunteers showed that a one-time admission of Kamiren of 1 mg on the first day of a 4-day oral cimetidine treatment (with a 400 mg dose twice a day) caused an increase of 10% AUC of doxazosin, and also did not affect the average figures of the peak concentration and the half-life of this substance. Such an increase in the average AUC of the substance when combined with cimetidine is located within the interindividual fluctuations (27%) of the median AUC values of the drug compared to placebo.

[25]

Storage conditions

Camrien must be kept out of reach of children, which is completely closed from moisture and sunlight. The maximum temperature limits are 30 ° C.

Special instructions

Reviews

Camyrone is commonly used to treat elevated blood pressure. Demonstrates high efficiency in the elimination of this disorder, although there are reviews from those to whom the drug did not help. The disadvantage is that the patients consider a sufficiently high cost of the drug, although for most of them, its effectiveness justifies such a price.

Shelf life

Camyrs are allowed to be used for 5 years from the date of release of the drug.