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Exforge
Last reviewed: 03.07.2025

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Indications Exforge
It is used to reduce elevated blood pressure in people with indications for complex therapy.
Release form
Available in tablets, 14 or 28 pieces per pack.
Exforge N
Exforge N is used to eliminate primary hypertension in people with high blood pressure. It is used with constant monitoring 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 drugs, one of which is complex.
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Pharmacodynamics
Exforge is an antihypertensive drug that contains a combination of two active ingredients.
The first of them is amlodipine, which is a derivative of dihydropyridine. It is included in the category of drugs that block slow Ca channels. By affecting the endings, the substance slows down the transport of calcium into the cell area - into cardiomyocytes and smooth muscle endothelial cells. As a result, the vascular walls relax along with their expansion, as well as a decrease in OPSS. The drug reduces the resistance of the renal vascular endothelium and helps to increase the efficiency of blood circulation inside the kidneys.
Amlodipine helps to lower blood pressure, but does not have a noticeable effect on catecholamine levels and heart rate. The drug in its therapeutic doses, combined with β-blockers, 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 AV conduction indicators.
The second element is valsartan, which is an antagonist of the angiotensin 2 receptor, which selectively affects the AT1 endings.
The active ingredients in such a combination complement each other's medicinal properties. The use of Exforge is considered more effective than taking valsartan and amlodipine separately.
Due to blocking of AT1 receptors, angiotensin II plasma levels increase. A decrease in blood pressure is observed 2 hours after taking a single dose. The maximum decrease in pressure occurs on average after 5 hours. The antihypertensive effect lasts for more than 1 day. No withdrawal syndrome occurs after the end of drug use. A stable decrease in blood pressure is observed after 3 weeks of treatment and is maintained in the case of a longer course.
The use of the drug in people with individual functional phases of CHF, as well as in the period after a heart attack, reduces the number of hospitalizations, as well as deaths.
Pharmacokinetics
Both active components of the drug have linear pharmacokinetics.
Amlodipine.
After taking the substance in a medicinal dosage, the peak value in plasma is observed after 6-12 hours. The calculated level of bioavailability is within 64-80%. Food consumption does not affect the bioavailability values of the component.
The volume of distribution is approximately 21 l/kg. In vitro tests of the substance have shown that its synthesis with plasma protein in people with primary hypertension is approximately 97.5%.
Amlodipine undergoes extensive intrahepatic metabolism (approximately 90% of the substance), during which inactive decay products are formed.
Amlodipine is excreted from plasma in 2 stages, with a half-life of approximately 30-50 hours.
Equilibrium plasma values are observed after regular administration for a period of 7-8 days. Approximately 10% of unchanged amlodipine, as well as 60% of its breakdown products, are excreted in the urine.
Valsartan.
When valsartan is taken orally, it reaches peak plasma levels after 2-4 hours. The average bioavailability is 23%. Food reduces the AUC of valsartan by approximately 40%, and its peak values by 50%. However, after 8 hours of administration, the plasma level of the substance will be the same for both those who took the drug on an empty stomach and those who took it after eating. The decrease in AUC values does not have a noticeable effect on the medicinal efficacy of the drug, as a result of which it is allowed to take valsartan regardless of food intake.
The equilibrium distribution volume of valsartan after intravenous injection is approximately 17 liters, which allows us to conclude that the substance is not intensively distributed within tissues. It has a high level of synthesis with plasma protein - 94-97% (mainly with albumin).
Only a small part of the component undergoes transformation – only 20% of the dosage is converted into decay products. Low values (less than 10% of the AUC level of valsartan) of the hydroxymetabolite substance, which has no medicinal activity, were detected in the plasma.
Valsartan exhibits multiexponential excretion kinetics (the half-life of the α component is <1 hour, and that of the β component is approximately 9 hours). The component is excreted mainly unchanged in the faeces (approximately 83% of the drug) and in the urine (approximately 13%).
After administration of the drug, the plasma clearance rate of the substance is about 2 l/hour, and the renal clearance rate is approximately 0.62 l/hour (about 30% of the total clearance rate). The half-life of valsartan is 6 hours.
Valsartan/amlodipine.
When Exforge is taken orally, the peak plasma level of its active components is reached after 3 (for valsartan) and 6-8 hours (for amlodipine), respectively. The degree and rate of absorption of the drug are similar to the bioavailability of these substances when used separately.
Dosing and administration
The tablets are taken orally with water. You need to drink 1 tablet 1 time per day, without taking into account the time of food consumption.
The tablets contain 5/80 or 5/160, as well as 10/160 or 10/320 mg of active substances (amlodipine/valsartan).
The daily dosage that can be taken is no more than 10/320 mg.
Use Exforge during pregnancy
It is prohibited to prescribe Exforge during pregnancy, as well as during the period of its planning. Taking the drug is associated with a risk to the fetus due to the effect of the drug on the function of the RAAS. If pregnancy is established, it is necessary to immediately stop using the drug.
Contraindications
Among the contraindications of the drug:
- hypersensitivity to valsartan with amlodipine, as well as additional components of the drug;
- lactation period;
- narrowing of the arteries inside the kidneys;
- recent kidney transplant;
- presence of indications in children and adolescents.
Caution is required when prescribing in the following cases:
- liver dysfunction;
- presence of HCM;
- obstruction in the area of the gallbladder;
- renal diseases with CC level <10 ml/minute;
- hyponatremia or hyperkalemia;
- stenosis of the aortic or mitral valve;
- decreased BCC index.
Side effects Exforge
The use of the drug may cause the development of the following side effects:
- cough, nasopharyngitis, runny nose, flu-like conditions, sinusitis, pain in the larynx or pharynx;
- constipation, epigastric pain, diarrhea, nausea, as well as pancreatitis, gastritis and hepatitis;
- exanthema, erythema (also multiform), anaphylaxis, skin rashes and itching, as well as urticaria and Quincke's edema;
- headaches, dizziness (also orthostatic type), feeling of drowsiness, anxiety, insomnia and emotional lability;
- paresthesia, arthralgia, muscle spasms, vasculitis, swelling in the joints, back pain, peripheral swelling, and increased sweating;
- facial puffiness, visual disturbances, and in addition polyuria and pollakuria;
- tachycardia, orthostatic collapse, increased angina, heart rhythm disorders;
- hyperglycemia, leuko-, thrombocyto-, neutropenia;
- hot flashes, syncope, tinnitus, feeling of heaviness, dyspnea, as well as pulmonary edema and asthenic conditions;
- dryness of the oral mucosa, hyperplasia of the mucous membrane in the gum area;
- baldness, increased creatinine levels;
- impotence or gynecomastia;
- peripheral form of neuropathy.
Overdose
There is no official information about Exforge intoxication. In theory, dizziness, shock, and reflex tachycardia may develop, as well as a decrease in blood pressure.
If a large number of tablets are taken, vomiting should be induced, the stomach should be washed out, and the patient should be given sorbents. In case of overdose and decreased pressure, the victim should lie down with his legs raised. Calcium gluconate and a vasoconstrictor may also be prescribed. The hemodialysis procedure does not have the desired effect.
Interactions with other drugs
Combination with drugs that block β-adrenoreceptors enhances the antianginal and antihypertensive properties of the drug. Also, the elimination of amlodipine-related reflex tachycardia occurs. When taken simultaneously, blood pressure readings should be monitored.
Combination with organic nitrates leads to summation of the antianginal effect. In addition, potentiation of reflex tachycardia and an increase in the likelihood of a significant decrease in blood pressure are observed.
Drugs that inhibit the CYP3A4 isoenzyme increase the plasma level of amlodipine.
Substances that induce the CYP3A4 isoenzyme (such as carbamazepine, phenobarbital, primidone with phenytoin and fosphenytoin with rifampicin, as well as St. John's wort preparations) contribute to a decrease in plasma amlodipine levels.
Medicines containing potassium (this also includes potassium-sparing diuretics), when combined with Exforge, can lead to the development of hyperkalemia.
When the drug is combined with NSAIDs, its antihypertensive properties are reduced.
Combination with diuretic drugs can lead to the development of hypoglycemia and also worsen kidney function.
Concomitant use with antidiabetic agents may potentiate hypoglycemia.
Drugs that block α-adrenergic receptors potentiate the antihypertensive effect of Exforge.
When combined with lithium drugs, there is a decrease in renal excretion of lithium, as well as an increase in the toxic effects of lithium-containing drugs.
General anesthetic drugs in combination with Exforge cause a significant decrease in blood pressure.
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Special instructions
Reviews
Exforge is a very effective drug that works well for long-term hypertension, which is difficult to treat. According to many reviews, the drug has a long-term effect and completely controls blood pressure. At the same time, the development of side effects is observed quite rarely (in rare cases, mild dizziness and nausea appear - with prolonged use of the drug, these reactions disappear on their own).
The disadvantage of this drug is its high cost, so not everyone can afford this drug, since treatment with Exforge must be long-term.
Attention!
To simplify the perception of information, this instruction for use of the drug "Exforge" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.