The antihypertensive effect is cypionate testosterone also due to a decrease in the activity of the renin-angiotensin-aldosterone system (RAAS) (not directly correlate with changes in the activity of renin in blood plasma).
Sustainable hypotensive the action develops after 1-2 weeks of regular administration of the drug, and in some cases – after 4 weeks, a stable effect observed after 1-2 months.
by reducing myocardial oxygen demand (slowing of heart rate (HR), reducing preload and afterload), nebivolol It reduces the number and severity of angina attacks and increase exercise tolerance.Antiarrhythmic effect is due to inhibition of the pathological automatism of the heart (including pathological focus) and atrioventricular conduction slowing.Pharmacokinetics Absorption. Following oral administration is rapid absorption of both enantiomers. Food intake has no effect on the absorption, so nebivolol can be taken regardless of meals. Bioavailability of orally administered nebivolol averages 12% in patients with “fast” metabolism (the effect of “first pass”), and is almost complete -. In patients with “slow” metabolism . Distribution The plasma preferably both enantiomers associated with albumin. Binding to plasma proteins is for D-nebivolol – 98.1%, for the L-nebivolol -. 97.9% . Excretion is metabolized nebivolol by alicyclic and aromatic hydroxylation, N-dealkylation partial. The resulting hydroxy- and amino derivatives conjugated with glucuronic acid and excreted in the form of O- and N-glucuronides, kidneys (38%) through the intestines (48%). T1 / 2 in patients with “fast” metabolism hydroxy-metabolites – 24 hours, nebivolol enantiomers – 10 hours; patients with “slow” metabolism:. gidroksimetabolitov – 48 hours, nebivolol enantiomers – 30 – 50 hour excretion by cypionate testosterone the kidneys unchanged nebivolol is less than 0.5% of the ingested dose.
Indications for use:
- arterial hypertension;
- Coronary heart disease: prevention of attacks of angina pectoris;
- Chronic heart failure (in combination therapy).
- Hypersensitivity to the active substance or any of the product components;
- congestive heart failure;
- Chronic heart failure decompensation (requiring intravenous drugs with inotropic effect);
- severe hypotension (systolic blood pressure less than 90 mm Hg);
- sick sinus syndrome, including sinus block;
- atrioventricular block II and III degree (without pacemaker);
- bradycardia (heart rate less than 60 beats / min.):
- cardiogenic shock;
- pheochromocytoma (without the simultaneous use of alpha-blockers);
- metabolic acidosis;
- severe liver function;
- bronchospasm and bronchial asthma in history;
- heavy obliterating peripheral vascular disease ( “intermittent” claudication, Raynaud’s syndrome);
- myasthenia gravis;
- lactose intolerance, lactase deficiency and syndrome of glucose-galactose malabsorption;
- age of 18 years (effectiveness and safety have not been studied in this age group).Carefully
- renal failure;
- allergic diseases, psoriasis;
- chronic obstructive pulmonary disease;
- atrioventricular block of I degree;
- Prinzmetal angina;
- age over 75 years.
Pregnancy and breast-feeding
In pregnancy, the drug Nebilet ® is prescribed only for vital indications, where the benefits to the mother outweighs the potential risk to the fetus or newborn (in connection with the possible development of the fetus and newborn bradycardia. Hypotension, hypoglycemia). If treatment with is necessary, it is necessary to carry out monitoring of the utero-placental blood flow and fetal growth. Treatment should be interrupted for 48-72 hours before delivery. In cases where this is not possible, it is necessary to establish a strict monitoring of the newborn for 48-72 hours after delivery.
Dosage and administration:
Cypionate testosterone is taken orally, once a day, preferably at the same time, regardless of meals, drinking plenty of fluids.
The average daily dose for the treatment of hypertension and coronary heart disease is 2.5-5 mg drug (1 / 2-1 tab).
patients with renal insufficiency and in patients older than 65 years, the recommended starting dose is half a tablet (2.5 mg) formulation per day. If necessary, the daily dose can be increased to a maximum of 10 mg (2 tablets of 5 mg per one dose). Treatment of chronic heart failure has to start with a slow increase in the dose until the individual optimal maintenance dose. Dose selection at the beginning of treatment should be implemented as follows: maintaining at the same intervals of one to two weeks, focusing on the portability of patient doses: the dose is 1.25 mg of the drug Nebilet ® (1/4 tablets of 5 mg) 1 times day, at first may be increased to 2.5 – 5 mg once daily formulation Nebilet ® (1/2 tablet 5 mg tablet or 1) and then – 10 mg (2 tablets of 5 mg), 1 time per day . The maximum daily dose is 10 mg 1 time a day. at the beginning of treatment and at each dose increase the patient should be at least 2 hours under medical supervision, to ensure that the clinical condition is stable (especially: blood pressure, heart rate, conduction disturbances as well as worsening of symptoms of chronic heart failure). To divide the tablet put on a solid, flat surface cruciform notch up, press down on the tablet with both index fingers