Carlonas Plus

General characteristics. Structure:

Active ingredient: 20 mg of enalapril of a maleate, 12,5 mg of Hydrochlorthiazidum.

Excipients: lactose anhydrous, Natrii hydrocarbonas, starch corn dry, starch prezhelatinizirovanny, magnesium stearate.

Anti-hypertensive drug in a complex with diuretic.

Pharmacological properties:

Pharmacodynamics. CARLONAS PLUS is a maleate enalapril combination – inhibitor the angiotensin-the converting enzyme (ACE) and Hydrochlorthiazidum – diuretic of a class of tiazid. At combined use of enalapril of a maleate and Hydrochlorthiazidum the anti-hypertensive effect increases.

Enalapril is powerful drug of long action which is inhibitor (AKF) and is applied to treatment of arterial hypertension and chronic congestive heart failure. The active metabolite of enalapril – enalaprilat, prevents transformation of inactive angiotensin I into angiotensin II and eliminates its vasoconstrictive action. Decrease in concentration of plasma and fabric angiotensin II results. Owing to inhibition of AKF arterial pressure, at the expense of a vazodilatation of arteries and veins decreases. It has no significant effect on cordial emission and on a stroke output. Reduces the general peripheric resistance of vessels (GPRV), reduces an afterload and preloading, reduces pressure in the right auricle and a small circle of blood circulation. Drug reduces a hypertrophy of a left ventricle. At use of drug the tone of the taking-out arterioles of balls of kidneys decreases, the intraglomerular hemodynamics thereby improves that interferes with development of a diabetic nephropathy.

Hydrochlorthiazidum is diuretic of group of tiazid and is used at treatment of hypertensia and hypostases. The mechanism of action is connected with influence on distal tubules of nephron where the reabsorption of ions of sodium, chlorine and water decreases. Excretion of potassium ions, magnesium and bicarbonate increase, calcium ions are late in an organism.

In too time diuretics of group of tiazid render hypotensive effect by means of decrease in peripheric resistance.

Enalapril reduces the loss of potassium ions caused by use of Hydrochlorthiazidum.

Pharmacokinetics. The combined anti-hypertensive drug. At oral administration about 70% of enalapril are soaked up in digestive tract. Enalapril is metabolized in a liver in an active form - enalaprilat. The peak of concentration of enalaprilat in serum is observed in 3 – 4 hours after reception.

Enalapril is distributed in fabrics and fluid mediums. Gets through a placental barrier, it is allocated with breast milk. For 50–60% enalapril contacts proteins of plasma. Half-life of enalapril makes 11 hours. At a chronic renal failure this period is extended. At a single dose of 10 mg of 60-70% of enalapril of a maleate 30% - with excrements in 24-48 hours in the form of enalapril and enalaprilat are removed with urine.

Hydrochlorthiazidum at oral administration is quickly enough soaked up from digestive tract. Bioavailability makes about 60-80%. Hydrochlorthiazidum is not metabolized. Hydrochlorthiazidum gets through a placental barrier, but does not get through a blood-brain barrier (GEB). The diuretic effect develops in 2 hours after oral administration, reaches a maximum in 6 hours and lasts from 6 to 12 hours. The elimination half-life makes of 6 - 10 o'clock.

At least 61% are removed with urine in not changed look within 24 hours.

Indications to use:

- arterial hypertension (in need of a combination therapy AKF inhibitors and Hydrochlorthiazidum).

Route of administration and doses:

Carlonas Plus is appointed inside, irrespective of meal. At arterial hypertension appoint on 1 tablet of 1 times/days in the morning. In case of need it is possible to increase a dose to 2 tablets of 1 times/days. At the previous therapy by diuretics they are recommended to cancel or reduce a dose, at least, in 2-3 days prior to use to prevent sharp decrease in the ABP.

At clearance of creatinine of 80-30 ml/min. the initial dose usually makes ½ tablets once a day.

At a moderate renal failure it is recommended to carry out monotherapy by enalapril, at the same time the recommended dose makes from 5 mg to 10 mg.

Features of use:

During treatment it is necessary to control disturbances of water and electrolytic balance, such as organism dehydration, hyponatremia, gipokhloremichesky alkalosis, hypomagnesiemia or hypopotassemia which can arise owing to episodes of diarrhea or vomiting. At such patients it is necessary to carry out periodic definition of electrolytic composition of blood through the corresponding periods.

With extra care patients should appoint drug with coronary heart disease or cerebrovascular diseases as the excessive lowering of arterial pressure (ABP) can lead to development of a myocardial infarction or stroke.

At development of arterial hypotension the bed rest and, in case of need, intravenous administration of normal saline solution is shown. Passing arterial hypotension at purpose of Carlonas Plus is not a contraindication to its further use. After normalization of the ABP and volume of the circulating blood therapy can be resumed in slightly reduced doses.

Drug with care is appointed to patients with a renal failure (the clearance of creatinine (CC) <80 ml/min.). Before purpose of drug it is necessary to determine the content of urea and creatinine in blood.

AKF inhibitors have to be appointed with care to patients at whom outflow of blood from a left ventricle of heart is complicated (an aortal stenosis, a hypertrophic cardiomyopathy).

Increase in levels of cholesterol and triglycerides can be also connected with therapy by diuretics of a tiazidovy row, however at the dose of Hydrochlorthiazidum of 12,5 mg which is contained in 1 tablet of Carlonas Plus, similar effects either were not observed, or were insignificant.

Therapy of a tiazidama can lead to a hyperuricemia and/or gout at some patients. However, enalapril can increase the content in urine of uric acid and, thereby, weaken giperurikemichesky effect of Hydrochlorthiazidum.

At treatment AKF inhibitors described exceptional cases of a Quincke's disease of the person, extremities, lips, language, a glottis and/or throat. In such cases the immediate termination of treatment by drug and establishment of careful observation of a condition of the patient for the purpose of control of clinical symptoms is necessary. When hypostasis extends to area of the person and lips, specific treatment usually is not required, in these cases therapy by antihistaminic drugs is effective. When hypostasis is localized in the field of language, a glottis or a throat that can lead to obstruction of respiratory tracts, it is necessary to enter immediately subcutaneously adrenaline 1:1000 solution (0.3-0.5 ml) and to hold other relevant medical activities.

In rare instances at the patients receiving AKF inhibitors heavy anaphylactoid reactions developed during desensitization allergen from poison of Hymenoptera. Similar reactions can be avoided if prior to carrying out desensitization it is temporary to stop AKF inhibitor reception.

Against the background of therapy of AKF cough cases are noted. As a rule, cough has unproductive persistent character and disappears after the end of therapy. The cough connected using AKF inhibitors should be considered at differential diagnosis of cough.

The increased content of salt in food weakens effect of Carlonas Plus.

Features of influence of medicine on ability to manage the vehicle or potentially dangerous mechanisms. With care appoint drug to the patients who are engaged in potentially dangerous types of activity requiring special attention.

Side effects:

- cough, short wind;

- dizziness, headache, increased fatigue, adynamy;

- nausea, vomiting, dryness of a mucous oral cavity, dyspepsia, lock, diarrhea, abdominal pains, pancreatitis.

Seldom:

- orthostatic hypotension, heartbeat, tachycardia;

- increase in level of enzymes of a liver and bilirubin in plasma;

- sleeplessness, irritability, paresthesias, drowsiness;

- passing increase in level of an urea nitrogen and creatinine, infection of urinary tract;

- itch, rash, Quincke's disease, Stephens-Johnson's syndrome, hyperhidrosis;

- retrosternal pains, a short-term loss of consciousness, an asthma, the increased sweating, a ring in ears;

- dorsodynias, arthralgias, mialgiya, vasculitis, muscular spasms;

- impotence, decrease in a libido;

- decrease in level of hemoglobin and gematokritny indicator.

Interaction with other medicines:

At simultaneous use of CARLONAS PLUS with:

- other anti-hypertensive means, tricyclic antidepressants, fenotiazina and alcohol anti-hypertensive effect of Carlonas Plus amplifies;

- analgetics, non-steroidal anti-inflammatory drugs, holestiraminy or holestipoly weaken effect of Carlonas Plus;

- by drugs of lithium it is slowed down removal of lithium and its action amplifies;

- kaliysberegayushchy diuretics and drugs of potassium, can lead to a hyperpotassemia;

- Allopyrinolum, cytostatics, immunodepressants or system glucocorticosteroids can cause a leukopenia, anemia or a pancytopenia;

- cyclosporine, leads to development of a renal failure;

- sulfonamides or hypoglycemic means from group of sulfanylurea for intake can cause allergic reactions (skin allergic reactions, a photosensitization);

- glucocorticosteroids the risk of development of a hypopotassemia increases;

- alcohol, barbiturates and narcotic analgetics can cause orthostatic hypotension;

- peroral hypoglycemic means and insulin weaken hypoglycemic effect;

- at the general anesthesia the risk of developing of arterial hypotension increases.

Contraindications:

- hypersensitivity to maleate enalapril, Hydrochlorthiazidum;

- hypersensitivity to other derivatives of sulfonamide;

- a Quincke's disease in the anamnesis after use of inhibitors of an angiotensin-converting enzyme;

- anury;

- a hemodialysis at patients with a renal failure;

- the expressed abnormal liver functions;

- primary hyper aldosteronism;

- porphyria;

- Addison's disease;

- pregnancy and period of a lactation;

- children's and teenage age up to 18 years.

Overdose:

Symptoms: the expressed arterial hypotension beginning approximately in 6 h after administration of drug, a stupor, a hypopotassemia, a hypochloraemia, a hyponatremia and dehydration as a result of an excess urination. If earlier therapy was carried out by digitalis drugs, strengthening of arrhythmia owing to a hypopotassemia is possible.

Treatment: calling of vomiting and/or gastric lavage. Carrying out a symptomatic and maintenance therapy for the purpose of correction of disturbances of water and electrolytic balance and arterial hypotension. Enalapril the maleate can be removed from system blood circulation by means of a hemodialysis.

Storage conditions:

To store at a temperature not above 25 °C in the dry, protected from light place. To store in the place, unavailable to children! Period of storage 2 years. Not to apply after a period of storage.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging from a film of polyvinyl chloride and printing aluminum foil.

On the 2nd blister strip packagings together with the instruction on a medical use in the state and Russian languages place in a pack from a cardboard with the hologram of manufacturing firm.