Pharmacodynamics of antihypertensive drugs, is a specific antagonist of the angiotensin II receptor (ATI subtype). He suppresses the kinase II – the enzyme that destroys bradykinin.Reduces the total peripheral vascular resistance (SVR), the blood concentration of adrenaline and aldosterone blood pressure (BP), the pressure in the pulmonary circulation; reduces afterload, it has a diuretic effect. It prevents the development of myocardial hypertrophy, increases exercise tolerance in heart failure patients.After a single dose of the hypotensive effect (reduced systolic and diastolic blood pressure) reaches a maximum after 6 hours, then for 24 hours, gradually decreasing.
The maximum antihypertensive effect is achieved within 3-6 weeks after starting the drug.
Pharmacological data indicate that testosterone enanthate 250 plasma concentration in patients with cirrhosis is significantly increased, so patients with liver disease drug should be used in history at a lower dose.
The pharmacokinetics of
testosterone enanthate 250 is rapidly absorbed from the gastrointestinal tract. Bioavailability – about 33%. It has the effect of “first pass” through the liver, metabolized by carboxylation with the participation of isoenzyme of cytochrome P450 2C9 to the active metabolite. Contact with blood plasma proteins – 99%. The time to reach maximum concentration of testosterone enanthate 250 1 hour active metabolite 3-4 hours after ingestion. The half-life of 1.5 – 2 hours, and its main metabolite 6-9 hours, respectively. About 35% of the dose is excreted in the urine, about 60% – through the intestines.
Indications for use
- Arterial hypertension;
- Chronic heart failure (in a combination therapy, in case of intolerance or failure of therapy with ACE inhibitors).
- Hypersensitivity to the drug;
- Pregnancy and lactation;
- Age 18 years (effectiveness and safety have not been established in patients under 18 years).
Precautions liver and / or kidney failure.
Dosing and Administration
The drug Bloktran ® is taken orally, regardless of food intake, the multiplicity of reception – 1 times per day.
When hypertension the average daily dose is 50 mg. In some cases, for greater effect dose increased to 100 mg in one or two doses per day.
The starting dose for patients with heart failure is 12.5 mg 1 time per day. Typically, the dose is titrated at weekly intervals (i.e., 12.5 mg / day, 25 mg / day and 50 mg / day) to an average maintenance dose of 50 mg 1 time per day, depending on patient tolerability of the drug.
When administering the drug to patients receiving high doses of diuretics, the initial dose should be reduced to 1 to 25 mg once a day.
No need to adjust the dose in patients of advanced age or patients with impaired renal function, including patients on hemodialysis.
Patients with impaired hepatic function should be prescribed lower doses of the drug.
Safety and efficacy have not been established in children.
* Marked side effects, the incidence of which is comparable with placebo.
Communication of side effects occurring with a frequency of less than 1% of cases, with the use of testosterone enanthate 250 is not proven.
In most cases, Bloktran® well tolerated, side effects are transient in nature and do not require discontinuation of the drug .
From the nervous system and sensory organs: 1% or more – dizziness, asthenia, headache, fatigue, insomnia; less than 1% – anxiety, sleep disturbance, drowsiness, memory disorders, peripheral neuropathy, paresthesia, gipostezii, migraine, tremor, ataxia, depression, syncope, tinnitus, taste disturbance, changes in vision, conjunctivitis.
The respiratory system: 1% or more – nasal congestion, cough *, upper respiratory tract infection (fever, sore throat, sinusopatiya *, sinusitis, pharyngitis), less than 1% – dyspnea, bronchitis, rhinitis.
On the part of the gastrointestinal tract: 1% or more – nausea, diarrhea *, dyspepsia *, abdominal pain; less than 1% – anorexia, dry mouth, toothache, vomiting, flatulence, gastritis, constipation.
From the musculoskeletal system: 1% or more – cramps, myalgia *, back pain, chest, legs; less than 1% -artralgiya, shoulder pain, knee arthritis, fibromyalgia.
Since the cardiovascular system: orthostatic hypotension (dose-dependent), palpitations, tachy or bradycardia, arrhythmia, angina, anemia.
With the genitourinary system: less than 1% – urgent need to urinate, urinary tract infection, renal failure, weakening of libido, impotence.
For the skin: less than 1% – dry skin, erythema, flushing, photosensitivity, increased sweating, alopecia.
Allergic reaction: less than 1% – urticaria, rash, pruritus, angioedema, including face, lips, pharynx and / or language.
Other: hyperkalemia (serum potassium greater than 5.5 mmol / l).
Symptoms: marked reduction of blood pressure, tachycardia, due to parasympathetic (vagal) stimulation may occur bradycardia. Treatment: forced diuresis, symptomatic therapy; Hemodialysis is ineffective.
Interactions with other drugs
may be administered with other antihypertensive agents.
There was no clinically significant interaction with hydrochlorothiazide, digoxin, indirect anticoagulants, cimetidine, phenobarbital.
In patients with dehydration (previous treatment with high doses of diuretics) may occur marked reduction in blood pressure.
(Mutually) the effect of other antihypertensive agents (diuretics, beta-blockers, simpatolitikov).
It increases the risk of hyperkalemia when combined with potassium-sparing diuretics and potassium preparations.
should be carried out to correct dehydration Bloktrana® destination or starting treatment with the drug at a lower dose. Drugs that affect the renin-angiotensin system may increase the concentration of urea in the blood and serum creatinine in patients with bilateral renal artery stenosis or stenosis of a solitary kidney.
During treatment should regularly monitor the concentration of potassium in the blood, especially in elderly patients with renal impairment.
Pregnancy and lactation
Data on the use of testosterone enanthate 250 during pregnancy does not. However, it is known that drugs acting directly on the renin-angiotensin system, when used in the II and III trimester of pregnancy can cause defects or even death of the developing fetus. Therefore, in the event of pregnancy Bloktrana® reception should be stopped immediately.
In the appointment during lactation should decide to discontinue breast-feeding or discontinue therapy Bloktranom®.