Lotensin
Lotensin
Lotensin (Benazepril)Pharmacological action
Lotensin is a promedicine which after hydrolysis turns to an active metabolite, blocking transformation of angiotensin I in angiotensin II. Thus, vasoconstrictive action of angiotensin II and its stimulating influence on production of Aldosteronum, and also raises warm emission. Lotensin reduces peripheric vascular resistance and an afterload on heart. Against Lotensin application is not observed reflex augmentation of a warm rhythm in reply to reduction of the general peripheric resistance.
After unitary Lotensin reception the hypotensive effect becomes perceptible through 1 h, reaches a maximum through 2-4 h and proceeds to 24 h. At regular application proof depression of a BP becomes perceptible in 1 week. Expression of hypotensive effect does not depend on age, a racial accessory and reference values of activity of a renin of plasma. At sudden cancellation of a preparation of sharp lifting of a BP it is not observed.
At patients with a chronic heart failure Lotensin joining to standard therapy led to augmentation of warm emission, rising of shipping of an exercise stress, jamming pressure decrease in pulmonary capillaries, a system BP and to reduction of symptoms of a heart failure. At patients c disturbance of function of kidneys (a clearance of a creatinine of 30-60 ml/mines), with diseases of kidneys of a various genesis, long Lotensin treatment has led to reduction of a proteinuria and depression of risk of the further deterioration of function of kidneys by 53 %.
Indications
- An arterial hypertensia;
- A chronic heart failure (as a part of the combined therapy).
Dosage regimen
At a number of patients to the extremity of this interval the antihypertensive effect can decrease. The total daily dose can be parted further on 2 peer receptions. Maximum daily Lotensin dose at patients with an arterial hypertensia makes 40 mg in 1 or in 2 receptions.
If Lotensin monotherapy does not lead to sufficient depression of a BP, other antihypertensive preparation, for example blocker of calcium channels (originally in a small dose) can be in addition prescribed. In the event that before Lotensin appointment therapy by a diuretic is spent, for 2-3 days prior to the beginning of Lotensin reception it should be stopped, and in the subsequent, if necessary, to renew. For prevention of excessive depression of a BP in case to stop treatment by a diuretic it is not obviously possible, initial Lotensin dose should be reduced (to 5 mg instead of 10 mg).
To patients with a clearance of a creatinine more than 30 ml/mines prescribe Lotensin in an average dose.
For patients with a clearance of a creatinine less than 30 ml/mines the initial dose makes 5 mg.
At a chronic heart failure the recommended initial dose makes 2.5 mg of 1 times/days For prevention of risk of sharp depression of a BP in reply to reception of the first dose of a preparation (effect of the first dose) the patient should is under careful observation. In 2-4 weeks in the event that will not reach the desirable clinical answer and provided that at the patient it does not become perceptible clinically expressed arterial hypotension or other unacceptable by-effects, the preparation dose can be enlarged to 5 mg/sut (in 1 reception). Depending on clinical effect the preparation dose can be enlarged with due intervals to 10 mg and, as a last resort, to 20 mg/sut (in 1 reception).
At the majority of patients reception of a preparation of 1 times/sut is effective. At some patients the best result is reached at reception of a preparation 2 times/days In controllable clinical researches shown, that to patients with a serious heart failure smaller Lotensin doses, than the patient with easy and moderate degree of a heart failure usually are required.
Safety and Lotensin efficiency at children are not established now.
References on a regimen of dosage and a safety measure at patients of advanced age do not differ from those at adults.
Side effect
From cardiovascular system: often - palpitation, an orthostatic hypotension; seldom - clinically expressed arterial hypotension, a pain in a thorax, a stenocardia, arrhythmias; very seldom - a myocardial infarction.
From the party GASTROINTESTINAL TRACT: often - dyspepsia symptoms; seldom - a diarrhoeia, a constipation, a nausea, vomiting, an abdominal pain; very seldom - a pancreatitis.
Dermatological reactions: often - an eruption, inflow to the person, an itch, a photosensitization; very seldom - Stevens-Johnson's syndrome.
From respiratory system: often - unproductive tussis which can lead to a pharynx and larynx boring and hoarseness of a voice.
From party TSNS and peripheric nervous system: often - a headache, giddiness, undue fatigability; seldom - drowsiness, a sleeplessness, the raised nervous excitability; paresthesias.
From hemopoiesis system: very seldom - a hemolitic anaemia, a thrombocytopenia.
From sense organs: very seldom - a sonitus, disturbances of gustatory sensations.
Allergic reactions: seldom - a Quincke's disease, an edema of labiums and-or persons.
From osteomuscular system: seldom - arthralgias, an arthritis.
Rising of these indicators more possibly at patients with a stenosis of the renal arteries also receiving diuretics.
Contraindications
- Pregnancy;
- A lactemia (thoracal feeding);
- A hypersensibility to Benazepril and to other components of a preparation.
Pregnancy and lactemia
Lotensin is contraindicative to application at pregnancy.
Also the oligoamnios presumably caused by disturbance of function of kidneys of a foetus is described; the oligoamnios in such cases was accompanied by development in a foetus of contractures of joints of extremities, deformation of a facial skull and a hypoplasia of lungs.
Special indicatings
In such cases Lotensin should be corresponding treatment is immediately excellent, spent and regular observation before full and stable elimination of complaints and symptoms is provided. When the edema is limited to the person and labiums, this complication usually is authorised after appointment of antihistaminics or even without treatment. The Quincke's disease extending on a larynx, can be fatal. When tongue, a vocal cleft or a larynx are involved, corresponding therapy should be immediately prescribed, including the hypodermic injection of adrenaline in delution 1:1000 (0 ml) is made and-or measures are taken for maintenance of passableness of respiratory tracts.
Use in pediatrics
Safety and efficiency Lotensin at children are not established now.
Influence on ability to driving of motor transport and to management of mechanisms
As well as at use of other antihypertensive agents, it is recommended to be careful at a driving and-or work with mechanisms.
Overdosage
Though data about Lotensin overdosage is not available, a possible basic symptom is the expressed arterial hypotension.
Treatment: in case of recent reception of a preparation it is necessary to wash out a stomach (to cause vomiting). In case of the expressed arterial hypotension spend i.v. introduction of an isotonic solution of sodium of Sodium chloridum.
Medicinal interaction
The probability of development of an arterial hypotension at such patients can be shown to a minimum at cancellation of therapy by diuretics for 2-3 days prior to the beginning of Lotensin treatment.
Conditions and periods of storage
The preparation should be stored in original packing, in a place inaccessible to children at temperature not above 30 C; to protect from moisture influence.
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