Exforge 10 / 160mg No. 14 tablets
Author Ольга Кияница
|Amount in a package||-|
|Manufacturer||Novartis Pharma (Switzerland)|
|The main medicament||-|
Controlling blood pressure using Exforge application will help in the treatment of patients with essential hypertension.The effectiveness of the drug, according to Exforge instruction, is based on its complex effect, due to the presence of several active substances in the composition, which increases the speed of action of the therapeutic agent.
EXFORGE instruction manual
One tablet contains
active substances : amlodipine besylate (equivalent to amlodipine) valsartan
5 mg / 80 mg 5 mg 80 mg
5 mg / 160 mg 5 mg 160 mg
10mg / 160mg 10mg 160mg
auxiliary substances : silicon dioxide colloidal anhydrous, crospovidone, magnesium stearate, microcrystalline cellulose,
composition of the shell : hydromellose, polyethylene glycol, talc, titanium dioxide
(E 171), iron oxide red (E 172) (for a dosage of 10 mg / 160 mg), iron oxide is yellow (E 172).
Tablets 5mg / 80mg: dark yellow, rounded, film-coated, with bevelled edges, the inscription "NVR" on one side of the tablet and the inscription "NV" on the other side of the tablet.
Tablets 5mg / 160mg: dark yellow, oval, film-coated, with bevelled edges, the inscription "NVR" on one side of the tablet and the inscription "ЕСЕ" on the other side of the tablet.
Tablets 10mg / 160mg: pale yellow, oval, film-coated, with bevelled edges, the inscription "NVR" on one side of the tablet and the inscription "UIC" on the other side of the tablet.
Angiotensin II antagonists and calcium channel blockers
ATS code C09D B01
The pharmacokinetics of Exforge are characterized by linearity. Since there is no pharmacokinetic interaction between valsartan and amlodipine, the pharmacokinetics for each drug are given below.
After ingestion of amlodipine in therapeutic doses, the maximum concentration of amlodipine in the blood plasma is reached in 6-12 hours. The absolute bioavailability values are calculated to be between 64% and 80%. Eating food does not affect the bioavailability of amlodipine. The distribution volume is approximately 21 l / kg. 97.5% of the circulating drug binds to plasma proteins. Amlodipine is intensively (90%) metabolized in the liver with the formation of active metabolites. Excretion of amlodipine from plasma is biphasic with a terminal half-life of 30 to 50 hours. Equilibrium plasma concentrations are achieved after prolonged use for 7-8 days. Ten percent of unchanged amlodipine and 60% of amlodipine in the form of metabolites is excreted in the urine.
After ingestion of one valsartan, the maximum concentration of valsartan is reached after 2-3 hours. The average absolute bioavailability is 23%. Valsartan has a multiexponential character of the excretion parameters (t 1 / 2α <1 h and t 1/2 ß about 9 h). Food reduces the bioavailability (by AUC value) of valsartan by 40% and the maximum concentration in the blood plasma (Cmax) by almost 50%, although almost 8 hours after taking the concentration of valsartan in the blood plasma are the same in both eating and fasting. This decrease in AUC, however, is not accompanied by a clinically significant decrease in the therapeutic effect; Valsartan, therefore, can be administered with either a meal or an empty stomach. In the equilibrium state, the volume of valsartan distribution after intravenous administration is 17 liters, indicating that there is no extensive distribution of valsartan in the tissue. Valsartan binds to a high degree with serum proteins (94-97%), mainly with serum albumins. Valsartan does not undergo a pronounced metabolism; only about 20% of the dose is determined in the form of metabolites. The hydroxyl metabolite is identified in plasma at low concentrations (less than 10% of the valsartan AUC). This metabolite is pharmacologically active. Vasartan is excreted mainly unchanged with feces (about 83% of the dose) and mostly unchanged in urine (about 13% of the dose). After intravenous administration, the plasma clearance of valsartan is about 2 l / h and its renal clearance is 0.62 l / h (about 30% of the total clearance). The half-life of valsartan is 6 hours.
After ingestion of Exforge, maximum concentrations of valsartan and amlodipine are reached after 3 and 6-8 hours, respectively. The speed and degree of absorption of Exforge are equivalent to the bioavailability of valsartan and amlodipine when taken in each of them in the form of tablets.
Exforge is a combination of two antihypertensive substances with a complementary mechanism for controlling blood pressure in patients with essential hypertension: amlodipine belongs to the class of calcium antagonists and valsartan to the class of preparations of angiotensin II antagonists. The combination of these ingredients has an additive antihypertensive effect, reducing arterial pressure more than each component alone.
When taking Exforge in a single dose, the antihypertensive effect persists for 24 hours. With prolonged use, the Exforge effect persists for 1 year. The sudden withdrawal of Exforge is not accompanied by a rapid increase in blood pressure. In patients who had arterial pressure adequately controlled by amlodipine, but who had very pronounced edema, with the same therapy, the same control of blood pressure was achieved with less pronounced swelling. Age, sex and race do not affect the effectiveness of Ekfor.
Indications for use
- treatment of essential hypertension with ineffectiveness of monotherapy
Dosing and Administration
Patients whose blood pressure can not be adequately controlled with only one amlodipine (or another calcium channel blocker of the dihydropyridine derivative) or only one valsartan (or another angiotensin II receptor blocker) can be switched to combination therapy with Exforge. The recommended dose is 1 tablet per day (5 mg of amlodipine and 80 mg of valsartan or 5 mg of amlodipine and 160 mg of valsartan, or 10 mg of amlodipine and 160 mg of valsartan). In clinical compliance, a direct transition from monotherapy to a fixed dose combination can be considered.
For convenience, patients receiving valsartan and amlodipine in individual tablets can be transferred to Exforge containing these components in the same doses. Exforge can be taken with food or regardless of food intake with a small amount of water.
Side effects are given according to their frequency, using the following concepts: very often (≥ 1/10); often (> 1/100, ≤ 1/10), infrequently (> 1/1000, ≤ 1/100), rarely (> 1/10000, ≤ 1/1000), very rarely (<1/10000), including individual message.
- flu-like symptoms, nasopharyngitis
- dizziness, drowsiness
- change of mood
- peripheral neuropathy
- tachycardia, dyspnea
- Orthostatic hypotension
- cough, sore throat and larynx
- rhinitis, sinusitis
- abdominal pain
- constipation, stool, diarrhea, indigestion
- gastritis, pancreatitis, hepatitis
- dry mouth
- gingival hyperplasia
- swelling of the joints
- leukopenia, thrombocytopenia
- increase of creatinine
- blurred vision
- noise in ears
- increased sweating
- muscle cramps
- a feeling of heaviness in the legs
- frequent urination, polyuria
swelling of the face, lower limbs
- pulmonary edema
- the feeling of tides
- asthenia, fatigue
- erectile dysfunction
- significant changes in the indicators of laboratory tests, namely the increase of urea nitrogen in the blood
- Hypersensitivity to the active substance or to any of the excipients
- severe violations of liver function, biliary cirrhosis and cholestasis
- anuria, severe renal dysfunction (creatinine clearance <30 ml / min)
- severe arterial hypotension
- pregnancy and lactation
- children's and adolescents under 18 years of age
With Exforge, combination with thiazide diuretics, beta-blockers, angiotesin-converting enzyme inhibitors, long acting nitrates, sublingual nitroglycerin, digoxin, warfarin, atorvastatin, sildenafil, maalox, cimetidine, nonsteroidal anti-inflammatory drugs, antibiotics and oral hypoglycemic agents is safe.
And as there is no clinically significant interaction with the following drugs: cimetidine, warfarin, furosemide, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine, glibenclamide.
When used simultaneously with dietary supplements containing potassium, potassium-sparing diuretics, potassium-containing salt substitutes or with other drugs that can cause an increase in the potassium concentration in the blood (for example, with heparin), caution and frequent determination of the potassium concentration in the blood is required.
Patients with sodium deficiency and / or decrease (circulating blood volume) BCC
In patients with uncomplicated hypertension, excessive hypotension was observed. In patients with activated renin-angiotensin-aldosterone system (in such cases as deficiency of bcc and / or salts in patients receiving diuretics in high doses) who receive angiotensin receptor blockers, symptomatic arterial hypotension may develop. It is recommended that this condition be corrected prior to Exforge's appointment or careful medical supervision at the beginning of therapy.If hypotension is observed when taking Exforge, the patient should be placed in a horizontal position, if necessary, an intravenous infusion of physiological saline. Treatment should continue until the stabilization of blood pressure.
When used simultaneously with dietary supplements containing potassium, potassium-sparing diuretics, potassium-containing salt substitutes, or with other drugs that can cause an increase in the potassium concentration in the blood (for example, with heparin), caution and frequent determination of the potassium concentration in the blood are required.
Dysfunction of the liver
Particular care should be taken when prescribing Exforge to patients with liver disease and obstructive biliary tract disease.
Patients with impaired renal function from mild to moderate degree of Exforge dose correction are not required.
Stenosis of aortic and mitral valves, obstructive hypertrophic cardiomyopathy
Particular caution is indicated for patients suffering from aortic or mitral stenosis, or obstructive hypertrophic cardiomyopathy.
Pregnancy and lactemia
Exforge should not be given to women who are planning a pregnancy. The doctor should warn the woman about the potential risk when prescribing Exforge during pregnancy. If pregnancy is established during the therapy, the drug should be stopped immediately.
Features of the influence of the drug on the ability to drive vehicles or other potentially dangerous mechanisms
It is advisable to use caution when driving and controlling machinery.
Pronounced hypotension with dizziness, as well as increasing peripheral vasodilation and reflex tachycardia.
A significant and potentially prolonged systemic hypotension has been reported, including shock and fatal outcome.
If the drug is taken recently, vomiting or gastric lavage should be performed. Absorption of Exforge is significantly reduced when using activated charcoal immediately or for 2 hours after ingestion.
Clinically significant arterial hypotension caused by Exforge overdose requires active support of the cardiovascular system, including constant monitoring of cardiac and respiratory function, lifting limbs and attention to the volume of circulating fluid and urination. To restore vascular tone and blood pressure, a vasoconstrictor may be helpful, given the absence of contraindications for its use. To remove the blockade of calcium channels, it may be advisable to use intravenous calcium gluconate.
Form of production and packaging
Tablets, film-coated, 5 mg / 80 mg in a planar cell pack of 14 pcs., 1 or 2 packs together with instructions for medical use of the drug in a cardboard box.
Tablets, film-coated, 5 mg / 160 mg in a contiguous cell pack of 14 pcs., 1 or 2 packs, along with instructions for medical use of the drug in a cardboard box.
Tablets, film-coated, 10 mg / 160 mg in a contiguous cell pack of 14 pcs., 1 or 2 packs, along with instructions for medical use of the drug in a cardboard box.
Store at a temperature not higher than +30 ° C.
Keep out of the reach of children!
The drug should not be used after the period indicated on the package.
Conditions of leave from pharmacies