Exforge

Exforge - a combined remedy from the category of drugs-inhibitors of angiotensin 2.

[1], [2]

Indications of the exforge

It is used to reduce elevated blood pressure in people with indications for complex therapy.

Release form

Release in tablets, 14 or 28 pieces inside the pack.

Exforge H

Exforge is used to eliminate primary hypertension in people with elevated blood pressure. It is used with a constant control of the drug combination of valsartan with amlodipine, as well as hydrochlorothiazide - they are taken either as 3 separate drugs or in the form of 2 medicines, one of which is complex.

[3]

Pharmacodynamics

Exforge is an antihypertensive drug, which contains a combination of 2 active ingredients.

The first of these is amlodipine, which is a derivative of the dihydropyridine substance. It belongs to the category of means that block the slow channels of Ca. By influencing the endings, the substance slows the transport of calcium into the cell region - inside the cardiomyocytes and smooth muscle endothelial cells. As a result, there is a relaxation of the vascular walls along with their expansion, as well as a decrease in the OPSS. The drug lowers the resistance of the endothelium of the kidney vessels and helps to increase the efficiency of blood circulation inside the kidneys.

Amlodipine helps to lower the level of blood pressure, but it does not have a significant effect on catecholamines and heart rate. The drug in its therapeutic dosages, combined with beta-adrenoblockers, does not cause a negative inotropic effect. Also, with such a combination, there is no effect on the work of the sinus-atrial node and the parameters of AV conductivity.

The second element is valsartan, which is an antagonist of the receptors of the substance angiotensin 2, which selectively affects the terminations of AT1.

The active ingredients in such a combination complement the medicinal properties of each other. Exforge is considered more effective than taking valsartan and amlodipine separately.

Due to the blocking of AT1-receptors, the plasma values of angiotensin II increase. Reduction of blood pressure level is noted after 2 hours after taking a single dose. The maximum decrease in pressure occurs on average after 5 hours. Antihypertensive effect lasts more than 1 day. After the end of drug use, there is no withdrawal syndrome. A stable decrease in blood pressure is noted after 3 weeks of treatment and persists in the case of a longer course.

The use of medication in people with individual functional phases of CHF, as well as in the post-infarction period, reduces the number of hospitalizations, and also deaths.

Pharmacokinetics

Both active drug components have linear pharmacokinetics.

Amlodipine.

After using the substance in the dosage, the peak value inside the plasma is observed after 6-12 hours. The calculated level of bioavailability is in the range of 64-80%. Eating does not affect the bioavailability of the component.

The distribution volume is approximately 21 l / kg. In vitro substance tests showed that its synthesis with a plasma protein in people with primary hypertension is approximately 97.5%.

Amlodipine undergoes intensive intrahepatic metabolism (approximately 90% of the substance), at which inactive decay products are formed.

Excretion of amlodipine from plasma occurs in 2 stages, half-life is about 30-50 hours.

Equilibrium plasma values are observed after a regular intake in the period of 7-8 days. Approximately 10% of unmodified amlodipine, as well as 60% of its decay products are excreted in the urine.

Valsartan.

With oral administration of valsartan, it reaches peak plasma values after 2-4 hours. The average bioavailability is 23%. Food reduces the AUC of valsartan by approximately 40%, and its peak values by 50%. But in this case, after 8 hours after taking the plasma level of the substance will be the same as for those who used drugs on an empty stomach, and those who took it after eating food. A decrease in AUC values does not have a noticeable effect on the drug's drug efficacy, so it is permissible to take valsartan without taking into account the intake of food.

The equilibrium value of valsartan distribution volume after intravenous injection is approximately 17 liters, which allows us to conclude that the substance is not intensively distributed inside the tissues. He has a high level of synthesis with a plasma protein - 94-97% (mainly with albumin).

Only a small part of the component undergoes transformation - only 20% of the dosage is converted to decomposition products. Inside the plasma, low values (less than 10% of the level of AUC of valsartan) of the hydroxymetabolite substance, which has no drug activity, are found.

Valsartan is characterized by a multiexponential kinetics of excretion (the half-life of the element α is <1 hour, and the element β - about 9 hours). The component is mainly excreted unchanged - with feces (about 83% of the drug), and urine (approximately 13%).

After using the drug, the plasma clearance of the substance is about 2 l / h, and the level of the renal clearance is about 0.62 l / h (about 30% of the total clearance). The half-life of valsartan is 6 hours.

Valsartan / amlodipine.

With the internal reception of Exforge, the peak plasma level of its active components is reached after 3, respectively (for valsartan) and 6-8 hours (for amlodipine). The degree and rate of drug absorption are similar to those of bioavailability of these substances when they are used separately.

[4], [5], [6], [7]

Dosing and administration

Tablets are taken orally by washing with water. It is required to drink 1 tablet 1 time per day, without taking into account the time of eating.

Tablets contain 5/80 or 5/160, as well as 10/160 or 10/320 mg of active substances (amlodipine / valsartan).

For the day you can take a dosage, not exceeding the size of 10/320 mg.

[8], [9]

Use of the exforge during pregnancy

It is forbidden to prescribe Exforge during pregnancy, as well as during her planning. Taking the medication is associated with a risk to the fetus due to the effect of the drug on the function of the RAAS. In case of pregnancy, it is necessary to immediately abolish the use of drugs.

Contraindications

Among the contraindications of drugs:

• increased sensitivity to valsartan with amlodipine, as well as additional elements of the drug;
• lactation period;
• narrowing of the arteries inside the kidneys;
• recently transferred kidney transplant;
• the presence of testimony in children, as well as adolescents.

Caution is required when appointing in such cases:

• disorders in the work of the liver;
• presence of HCM;
• Obstruction in the area of GWP;
• kidney disease with a QC level <10 ml / minute;
• hyponatremia or hyperkalemia;
• stenosis of the aortic or mitral valve mouth;
• reduced BCC.

Side effects of the exforge

Use of the drug can cause the development of such side effects:

• cough, rhinopharyngitis, runny nose, flu-like conditions, sinusitis, pain in the larynx or pharynx;
• constipation, epigastric pain, diarrhea, nausea, and in addition pancreatitis, gastritis and hepatitis;
• exanthema, erythema (also polyforma), anaphylaxis, skin rashes and itching, as well as urticaria and edema of Quincke;
• headaches, dizziness (also orthostatic type), a feeling of drowsiness, anxiety, insomnia and emotional lability;
• paresthesia, arthralgia, muscle spasms, vasculitis, swelling in the joints, back pain, swollen peripheral type, and excessive sweating;
• facial pastosity, visual disorders, and in addition to polyuria and polukuriya;
• tachycardia, orthostatic collapse, increased angina pectoris, heart rhythm disorder;
• hyperglycemia, leuko-, thrombocyto-, neutropenia;
• tides, syncope, ear noise, a sense of heaviness, dyspnea, and in addition pulmonary edema and asthenic conditions;
• dryness of the oral mucosa, hyperplasia of the mucosa in the gum area;
• baldness, an increase in creatinine;
• impotence or gynecomastia;
• peripheral form of neuropathy.

Overdose

There is no official information about Exforge intoxication. In theory, dizziness, shock and tachycardia of the reflex type can develop, and pressure may decrease.

When taking a large number of tablets, it is necessary to induce vomiting, rinse the stomach and give the patient sorbents. In case of an overdose and a decrease in pressure, the victim must lie with his legs raised. Calcium gluconate and vasoconstrictive medication may also be prescribed. The procedure of hemodialysis does not have the desired effect.

[10], [11], [12]

Interactions with other drugs

Combination with drugs that block β-adrenoreceptors, increases the antianginal and antihypertensive properties of drugs. There is also an elimination of reflex type tachycardia associated with the use of amlodipine. With simultaneous admission, you need to monitor blood pressure.

The compound with organic nitrates leads to a summation of the antianginal effect. In addition, there is a potentiation of reflex type tachycardia and an increase in the probability of a pronounced decrease in blood pressure.

CYP3A4 isoenzyme inhibitors drugs increase the level of amlodipine inside the plasma.

Substances that induce isoenzyme CYP3A4 (such as carbamazepine, phenobarbital, primidone with phenytoin and phosphenytoin with rifampicin, as well as St. John's wort medicines) contribute to a decrease in the indices of amlodipine inside the plasma.

Drugs containing potassium (this includes also potassium-sparing diuretics), when combined with Exforge, can lead to the development of hyperkalemia.

When combining the drug with NSAIDs, its antihypertensive properties decrease.

The combination with diuretics can lead to the development of hypoglycemia, and also worsen the work of the kidneys.

Simultaneous reception with antidiabetics can potentiate hypoglycemia.

Preparations blocking α-adrenoreceptors, potentiate the antihypertensive effect of Exforge.

When combined with lithium drugs, there is a decrease in renal lithium excretion, as well as an increase in the toxic effect of lithium-containing drugs.

Preparations for general anesthesia in combination with Exforge cause a marked decrease in pressure.

[13]

Storage conditions

Store Exforge required under standard conditions for Pharmaceuticals, at a temperature of not more than 30 ^of C.

[14], [15], [16], [17]

Special instructions

Reviews

Exforge is a very effective medicine that works well for prolonged hypertension, which is difficult to treat. According to many reviews, the drug has a long-lasting effect and fully controls the blood pressure. In this case, the development of adverse reactions is rare (in rare cases, there is a slight dizziness, as well as nausea - with prolonged use of drugs, these reactions disappear on their own).

The disadvantage of this drug is its high cost, so not everyone can afford this drug, as treatment with Exforge should be long.

[18], [19]

Shelf life

Exforge can be used during the 3 years since the release of the medicine. The expiration date of Exforge H is 2 years.

[20], [21]