Description overdue on 08/24/2014
- Latin name: Exforge; Co-Exforge
- ATC code: Exforge: C09DB01; Co-Exforge: C09DX01
- Active substance: Exforge: Amlodipine (Amlodipinum), valsartan (Valsartanum); Co-Exforge: Amlodipine (Amlodipinum), valsartan (Valsartanum), hydrochlorothiazide (Hydrochlorothiazide)
- Manufacturer: Novartis (Switzerland)
- Composition
- Product form
- Pharmacological action
- Pharmacodynamics and pharmacokinetics
- Indications
- Contraindications
- Side effects
- Instructions for use Exforge
- Overdose
- Cooperation
- Terms of sale
- Storage conditions
- Shelf life
- Analogs
- Reviews
- Price, where to buy
Composition
Exforge tablets have such active components as Amlodipine and valsartan As well as the following additional ingredients: talc, MCC, magnesium stearate, hypromellose, colloidal silicon dioxide, titanium dioxide, Valium, yellow iron oxide, macrogol 4000.
Ko Exforge, in turn, has the following composition:
- active components - Amlodipine . valsartan . hydrochlorothiazide ;
- additional substances: MCC, colloidal silicon dioxide, Valium, Valium, macrogol, magnesium stearate, titanium dioxide, talc.
Product form
The drugs are available in tablet form.
Pharmacological action
Combined antihypertensive medication.
Pharmacodynamics and pharmacokinetics
The active ingredients of Exforge have complementary, mechanisms of action control Blood Pressure . Amlodipine It belongs to the blockers "slow" calcium channels. The second active ingredient valsartan - refers to angiotensin II receptor antagonists . The combination of these two components has a complement hypotensive effect, which causes a decrease in arterial (blood) pressure.
Amlodipine It acts as a relaxing agent on vascular smooth muscle. It expands the blood vessels, which causes a decrease in PR and decrease blood pressure. Prolonged use is not accompanied by significant changes Heart Rate and content catecholamines And negative inotropic effect .
In people with normal left ventricular function, the drug may cause a slight increase in cardiac index no significant effect on the rate of pressure rise (maximum) in the left ventricle, left ventricular volume and final blood pressure.
The action of amlodipine is effective in those who have chronic stable and vasospastic angina And angiographically confirmed coronary artery disease .
Valsartan selectively affect AT1 receptor Blocking them, which can lead to stimulation AT2 receptors .
With hypertension those who accept valsartan , There is a decrease in blood pressure without changes Heart Rate . The antihypertensive effect in this case is maintained throughout the day. With Heart Failure (chronic) II-IV class reduced the number of hospitalizations. With left ventricular failure or disorders of left ventricle after myocardial infarction fixed reduction in cardiovascular mortality.
The antihypertensive effect after taking the medicine becomes noticeable no later than 2 hours. Lowering blood pressure to the maximum extent after about 5 hours.
The hypotensive effect there is more than one day. Lowering blood pressure to the maximum extent with repeated use can be achieved for 2-4 weeks, it remains at this level during prolonged therapy. If you stop taking valsartan skyrocketing Blood Pressure and other undesirable effects were observed.
At 10/160 mg dose of the drug normalizes Blood Pressure Most patients with inadequate control of blood pressure with amlodipine 10 mg.
When used dosages 10/160 and 5/160 mg after treatment arterial pressure normal in most patients with inadequate control of blood pressure when taking valsartan 160 mg per day.
Action Exforge is not dependent on age, race and gender.
The pharmacokinetics of the drug is characterized by linearity. Following oral administration Exforge maximum concentration of valsartan and amlodipine plasma is about 7, and 3 hours respectively.
Amlodipine actively cleaved in the liver, thereby forming active metabolites . Displayed in two stages, with a half-life of 30-50 hours. Equilibrium concentration in plasma observed in about a week. 10% of the chemical is excreted in unaltered form and about 60% - a metabolites via the kidneys.
About 20% of a pleasant dose of valsartan is defined as metabolites . Active substance derived mainly unchanged via the kidneys and intestines. The half - about 6 hours.
Pharmacodynamics of the drug Co-Exforge, in turn, is characterized by the combined influence of three antihypertensive components that have complementary, mechanisms of action control Blood Pressure . At the same time there is a significant reduction and Sad Dad, when compared with the use of combinations of only two active substances in medicine. Targets Blood Pressure achieved faster.
Maximum antihypertensive effect when receiving Co-Exforge It can be seen after 2 weeks from the start of the course. The therapeutic effect is not dependent on age, race and gender.
The maximum concentration amlodipine . valsartan and hydrochlorothiazide after receiving Ko Exforge appears through 7, 3 and 2 hours, respectively.
Hydrochlorothiazide bioavailability when administered orally - 70%. The half-life - 6-15 hours. The substance of their body appears unchanged in the urine.
Indications
Both drugs are used for hypertension . Exforge take those patients receiving combination therapy. A Co-Exforge prescribed for grade II and III hypertension .
Contraindications
Exforge contraindicated if you are hypersensitive to the components of the drug, and pregnancy . With care, the tool should be taken to treat liver diseases, mitral or aortic stenosis . hyperkalemia , Hypertrophic obstructive cardiomyopathy , Severe renal impairment, deficiency of sodium and / or reduction BCC .
Co-Exforge is contraindicated in:
- significant violations of the liver;
- hypersensitivity to the drug;
- refractory to adequate therapy hypokalemia . hypercalcemia . hyponatremia and hyperuricemia ;
- pregnancy ;
- Lactation ;
- significant violations of the kidneys;
- childhood.
Be wary when taking medication:
- renal artery stenosis And artery only kidneys, mitral or aortic stenosis ;
- decreasing BCC ;
- systemic lupus erythematosus ;
- mild and moderate disorders of the liver;
- violations of water-electrolyte balance;
- hypertrophic obstructive cardiomyopathy ;
- diabetes .
Side effects
At reception Exforge you experience the following side effects:
- by Respiratory : nasopharyngitis . flu , Cough, sore throat or throat;
- by CNS : paresthesia . headache . drowsiness . dizziness ;
- by CCC : tachycardia . orthostatic hypotension , Palpitations;
- skin reactions : Rash, erythema ;
- by digestive organs : diarrhea / constipation , Abdominal pain, dry mouth, nausea;
- by Musculoskeletal System : Swelling of the joints, arthralgia , Back pain;
- Other: pastoznost , Peripheral edema, asthenia , Flushing, hot flashes, facial edema, fatigue.
In rare cases, observed: Hypersensitivity, blurred vision, marked reduction in blood pressure, tinnitus, anxiety , Syncope, hyperhidrosis Itching, feeling of heaviness, rash , Muscle cramps, thamuria . erectile dysfunction . polyuria .
In addition, the side effects of each of the components may manifest itself in the use of Exforge, even if it has not been observed in clinical studies.
The preparation Co-Exforge It has the following side effects:
- by Metabolism : hypokalemia . anorexia . hyperlipidemia . hyponatremia . hypercalcemia ;
- by Nervous System : paresthesia . fainting , Lethargy, dizziness , Taste disturbances, headache , Impaired coordination, neuropathy ;
- by Hearing : vertigo ;
- by Respiratory Cough, throat irritation, breathlessness ;
- by skin : Itching, increased perspiration ;
- by kidney and urinary tract : thamuria Increase in plasma creatinine, renal failure ;
- general disorders : abasia , Peripheral edema, fatigue, asthenia , Pain in the chest, abnormal gait, weakness;
- by psyche : drowsiness Sleep disorders;
- by organs of vision : visual impairment ;
- by CCC : phlebitis , A significant decrease in blood pressure, orthostatic hypotension . tachycardia . thrombophlebitis ;
- by Digestive System : dyspepsia , Unpleasant odor in the mouth, abdominal discomfort, diarrhea , Dry mouth, nausea, vomiting;
- by musculoskeletal : Pain in the extremities and back pain, joint swelling, muscle spasms, muscle weakness, myalgia ;
- by reproductive system : erectile dysfunction ;
- Other: weight gain, hyperuricemia .
Instructions for use Exforge
Instructions for use Exforge (Exforge) it provides preoral use. The drug is taken once a day, drinking some water, regardless of mealtime. Dosages Exforge 10/160, 10/320, 5/80, 5/160, 5/320 mg. The maximum daily dose - 10/320 mg.
For those who are appointed Co-Exforge , Instructions for use advise to use it once daily tablet, depending on the doctor's prescription, containing:
- 5 mg of amlodipine in combination with 160 mg of valsartan and 12 mg of hydrochlorothiazide 5;
- 10 mg of amlodipine in combination with 160 mg of valsartan and 12 mg of hydrochlorothiazide 5;
- 10 mg of amlodipine in combination with 320 mg of valsartan and hydrochlorothiazide 25 mg (2 tablets).
The tablets are taken orally with or without food. They need to drink water.
Overdose
Valsartan in high doses can lead to a marked decrease in blood pressure and dizziness , a Amlodipine - To have a reflex tachycardia . hypotension , Excessive peripheral vasodilatation .
Overdose hydrochlorothiazide fraught with symptoms that are associated with loss of electrolytes and dehydration . The most likely symptoms: nausea, muscle spasms, heart arrhythmia and drowsiness .
As treatment cause vomiting or gastric lavage is performed. May help reception Activated Carbon .
With hypotension the patient must take the position of "lying" with raised legs, in addition, provides for measures to maintain the normal operation of the CCC. To normalize Blood Pressure You can assign vasoconstrictor .
Cooperation
Clinically significant interactions were observed when combined amlodipine with thiazide diuretics, Nitroglycerin sublingual application, ACE inhibitors, Warfarin . Sildenafil . Cimetidine . antibiotics , Beta-blockers, nitrates, calculated on a long-term effect, Digoxin . Atorvastatin . Maalox , NSAIDs, oral hypoglycemic medications.
The combination amlodipine from Diltiazem patients in the elderly retards the cleavage of amlodipine, which causes an increase of its content in the plasma by about half. Together with the more powerful CYP3A4 inhibitors systemic exposure of amlodipine is increased.
The combination amlodipine from inducers of CYP3A4 On the contrary, it leads to a reduction of its concentration. Therefore, you should maintain control of its content in the plasma.
No clinically significant interaction with the combination valsartan from Cimetidine, Furosemide . Atenolol . Hydrochlorothiazide . Glibenclamide . Warfarin . Digoxin . Indomethacin and Amlodipine .
It is necessary to constantly monitor the concentration of potassium, while the use of Exforge in conjunction with biologically active additives Which contain kalisberegate diuretics , Potassium and kalisodergaszczye salt substitutes, as well as with other means, causes an increase in blood potassium levels.
At reception Co-Exforge It should also take into account the interaction hydrochlorothiazide with other agents. So you need to carry out the control of application of this drug in combination with lithium, hypoglycemic drugs For oral administration, and insulin . It may be necessary to correct dosage.
Furthermore, hydrochlorothiazide potentiates the effect of peripheral muscle relaxants, may intensify the effect of hyperglycemia Diazoxide , Increased sensitivity to Allopurinol Increase the risk of adverse events Amantadine , Reduction of excretion through the kidneys cytotoxic agents And their potentiation myelosuppressive action . In turn, the combination with NSAIDs reduces diuretic and antihypertensive the effect of hydrochlorothiazide. In cooperation with the drugs that reduce the concentration of potassium increases the risk hypokalemia . Heart glycosides also increase the risk of its occurrence, as well as hypomagnesemia and Arrhythmia .
Together with Mr. holinoblokatorami the bioavailability of hydrochlorothiazide increases. When combined with Methyldopa reported cases hemolytic anemia , from Cyclosporine - The risk of development hyperuricemia and development of symptoms gout , from Kabamazepinom - hyponatremia And with Vitamin D and calcium salts likely to increase the level of calcium in the blood serum. Kolestiramin reduces the absorption of hydrochlorothiazide.
Terms of sale
Exforge and Exforge Ko dispensed strictly on prescription.
Storage conditions
Keep the medication you need in reach of small children, dry place. The optimum temperature is not higher than 25 ° C.
Shelf life
Exforge Shelf life - 2 years, Koh Exforge - 1, 5 years.
Analogs of Exforge
Pharmacies can be found the following analogues Exforge and Exforge Ko:
- Difors 160;
- Difors 80;
- Difors XL;
- Sardip.
Reviews of Exforge
Reviews Exforge there are both positive and negative. Many patients say its effectiveness. Some, however, say that they have any side effects, because of which had to stop the drug.
In fact, any expert in advance can not eliminate the occurrence of undesirable effects. The tool is much more effective than the use of amlodipine or valsartan alone, but its reception should be well controlled. Many, in addition, more profitable to buy analogues Exforge.
Reviews Co-Exforge Usually positive. Patients say the obvious effectiveness of this tool, and recommend it to others.
Price Exforge where to buy
Cost Exforge It is considered to be quite high. Buy in Moscow and other Russian cities this tool can be, on average, for 1400-1800 rubles.
Cost Co-Exforge The average is about 2,000 rubles.