Nortivan
Northvan: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Nortivan
ATX code: C09CA03
Active ingredient: valsartan (Valsartan)
Manufacturer: Gedeon Richter Poland Co Ltd. (Poland), Gedeon Richter-RUS (Russia)
Description and photo updated: 2018-29-11
Northvan is an antihypertensive drug.
Release form and composition
Dosage form of Nortivan - film-coated tablets:
- dosage 40 mg: round, biconvex, light brown, with a line on one side and engraving "C73" on the other;
- dosage 80 mg: oblong, biconvex, pink, with a line on one side and engraving "C74" on the other;
- dosage 160 mg: oblong, biconvex, pink, with a line on one side and engraving "C75" on the other.
Packing: 10 pcs. in a blister, in a cardboard box 3 blisters and instructions for use of Northvan.
Composition of 1 film-coated tablet:
- active substance: valsartan - 40, 80 or 160 mg;
- auxiliary components: magnesium stearate, colloidal silicon dioxide, crospovidone, microcrystalline cellulose, external phase (microcrystalline cellulose, magnesium stearate);
- film shell: 40 mg tablets - opadry TAN 03B34653 [hypromellose 6 cf, talc, macrogol 400, titanium dioxide (E171), iron dye black oxide (E172), iron dye red oxide (E172), iron dye yellow oxide (E172)]; tablets of 80 mg and 160 mg - opadry PINK 03B34654 [hypromellose 6 cf, talc, macrogol 400, titanium dioxide (E171), iron dye red oxide (E172), iron dye yellow oxide (E172)].
Pharmacological properties
Pharmacodynamics
The active substance of Northvan - valsartan, is an antihypertensive agent, a specific antagonist of angiotensin II receptors. The substance has a selective effect on the AT 1 subtype of receptors responsible for the known effects of angiotensin II - the active hormone of the RAAS (renin-angiotensin-aldosterone system), formed from angiotensin I with the participation of ACE (angiotensin-converting enzyme). Angiotensin II binds to specific receptors that are located in various tissues on cell membranes. It is characterized by a wide range of physiological properties, including direct and indirect participation in the regulation of blood pressure (blood pressure).
Angiotensin II has a potent vasoconstrictor effect, resulting in a direct pressor response. Retains sodium ions in the body and stimulates the secretion of aldosterone.
Valsartan has a significantly higher (approximately 20,000 times) affinity for the AT 1 subtype receptor than for the AT 2 subtype receptor.
The drug does not inhibit ACE (also known as kininase II), which converts angiotensin I to angiotensin II, and destroys bradykinin (prevents it from accumulating). Due to these effects, the likelihood of association of the use of angiotensin II antagonists with cough is low.
In clinical studies in which valsartan was compared with an ACE inhibitor, it was found that in patients treated with valsartan, the incidence of dry cough is significantly lower than in patients taking an ACE inhibitor (this indicator was 2.6% and 7.9%, respectively). In patients who had a history of dry cough while taking ACE inhibitors, the frequency of cough when using valsartan was 19.5%, when taking thiazide diuretics - 19%, when using ACE inhibitors - 68.5%.
Valsartan does not bind or block ion channels and receptors of other hormones that play a significant role in the regulation of cardiovascular activity.
With arterial hypertension, valsartan lowers blood pressure, while not affecting the heart rate (heart rate). After taking a single dose of Nortivan in most patients, the hypotensive effect begins to develop within 2 hours, reaches a peak after 4-6 hours, and lasts for 24 hours.
With repeated doses (regardless of the prescribed dose), the effect of the drug stabilizes, reaches a maximum in 2-4 weeks and is maintained at the achieved level during long-term therapy. If the drug is discontinued, there is no sharp increase in blood pressure or the development of other undesirable clinical consequences. Valsartan does not have any effect on the concentration of fasting glucose, triglycerides, total cholesterol, and uric acid in the blood serum.
In patients with acute myocardial infarction and established heart failure and / or impaired left ventricular systolic function, Nortivan, used as part of combination therapy (includes ACE inhibitors, beta-blockers, thrombolytics, HMG-CoA reductase inhibitors, acetylsalicylic acid), helps to reduce mortality from cardiovascular complications after acute myocardial infarction, increases the time before the development of a cardiovascular event. Treatment also reduces hospitalizations for heart failure and decreases the rate of recurrence of myocardial infarction.
Pharmacokinetics
Valsartan is rapidly absorbed from the gastrointestinal tract, but the degree of absorption is characterized by wide variability. The absolute bioavailability averages 23%. The pharmacokinetic curve of the drug has a descending biexponential character with a half-life (T ½) in the first phase of less than 1 hour, in the second phase - about 9 hours.
In the range of therapeutic doses, the pharmacokinetics of valsartan is linear.
With repeated administration of Nortivan, no changes in the pharmacokinetic parameters of valsartan were noted. When applied once a day, the accumulation in the body is insignificant.
The maximum concentration is reached within 2 hours. Simultaneous food intake by 48% reduces the AUC (area under the concentration-time curve), however, 8 hours after taking Nortivan, the plasma concentrations of the drug taken on an empty stomach and with food are the same. The decrease in AUC is not accompanied by a clinically significant decrease in the therapeutic effect, therefore, tablets can be taken without reference to meals.
In women and men, plasma valsartan concentrations are similar. The drug is characterized by a high bond with blood proteins (mainly albumin) - 94–97%. The volume of distribution at steady state is approximately 17 liters. In comparison with hepatic blood flow (about 30 l / h), the plasma clearance of the drug is low (about 2 l / h).
Valsartan is metabolized to form the main metabolite of valeryl-4-hydroxyvalsartan. The enzymes involved in the biotransformation of the active substance of Northvan have not been determined, they do not belong to isoenzymes of the cytochrome P 450 system.
The drug is excreted through the intestines (83% of the dose taken) and by the kidneys (13%). Valsartan is excreted mainly unchanged, in the form of metabolites - about 20%.
In elderly patients, the systemic effect of valsartan is sometimes more pronounced than in younger patients. In this regard, it is recommended to start treatment with a lower dose of Nortivan - 40 mg.
The renal clearance of valsartan is about 30% of the total clearance. In this regard, with moderate functional impairment of the kidneys [creatinine clearance (CC) 20-50 ml / min] dose adjustment is not required. In severe renal impairment (CC <20 ml / min), treatment begins with a dose of 40 mg. Elimination of the drug from the body during hemodialysis is unlikely, which is explained by its high degree of binding to plasma proteins.
Valsartan does not undergo significant metabolism, therefore its systemic action does not depend on the functional state of the liver. For this reason, patients with hepatic insufficiency of non-biliary origin, provided that there is no obstruction of the biliary tract, dose adjustment is not required. With biliary cirrhosis of the liver and cholestasis, the AUC of valsartan increases by about 2 times (compared with healthy volunteers).
Indications for use
- arterial hypertension;
- acute myocardial infarction in patients with stable hemodynamic parameters, heart failure and / or asymptomatic left ventricular systolic dysfunction (as part of combination therapy to reduce mortality).
Contraindications
Absolute:
- obstruction of the biliary tract (cholestasis);
- cirrhosis of the liver;
- severe liver failure (> 9 points on the Child-Pugh scale);
- age up to 18 years;
- period of pregnancy and lactation;
- hypersensitivity to any component of Northvan.
Relative (special care required):
- conditions accompanied by a decrease in circulating blood volume (including diarrhea, vomiting);
- renal failure (CC <20 ml / min), including hemodialysis;
- bilateral stenosis of the renal arteries or stenosis of an artery of a solitary kidney;
- liver failure (<9 points on the Child - Pugh scale);
- arterial hypotension;
- period after myocardial infarction;
- hyponatremia or following a sodium restricted diet;
- age over 75 years.
Northvan, instructions for use: method and dosage
Nortivan tablets should be taken orally. Meal time does not matter.
Arterial hypertension
In most cases, the optimal dose is 80 mg once a day.
When evaluating the effectiveness of Nortivan, it should be borne in mind that the hypotensive effect develops within 2 weeks; it takes 4 weeks to achieve the maximum effect.
If it is not possible to achieve the required decrease in blood pressure, it is possible to increase the daily dose of Nortivan to 160 mg.
Further enhancement of the antihypertensive effect can be achieved by increasing the dose of Nortivan to a maximum daily dose of 320 mg, or by adding thiazide diuretics or other antihypertensive drugs to therapy.
It is recommended to start treatment with a lower daily dose of 40 mg in the following cases: elderly age over 75 years, impaired renal function with CC <20 ml / min, hemodialysis, a decrease in circulating blood volume (for example, due to taking high doses of diuretics and the impossibility of reducing them).
For patients with mild to moderate hepatic impairment (<9 points on the Child-Pugh scale), the recommended starting daily dose of Nortivan is 40 mg. If necessary, it can be increased to a maximum of 80 mg.
Acute myocardial infarction
You can start taking Nortivan in the first 12 hours after an acute myocardial infarction. The drug can be added to standard therapy for this disease, including beta-blockers, HMG-CoA reductase inhibitors, and acetylsalicylic acid.
The initial recommended dose is 20 mg (½ tablet at a dosage of 40 mg) 2 times a day. If necessary, gradually (over several weeks) increase the dose. The maximum allowable dose is 160 mg 2 times a day.
If arterial hypotension or impaired renal function is detected, a reduction in the dose of Nortivan may be required.
In the presence of concomitant moderate renal failure (CC 20-50 ml / min), there is no need to adjust the dose. There are no data on the safety of using valsartan in severe renal failure (creatinine concentration ≥ 221 μmol / l), therefore, Nortivan should be used with caution, under close monitoring of renal function.
Side effects
Possible side effects of Nortivan (classified as follows: often - from? 1/100 to <1/10; infrequently - from? 1/1000 to <1/100; rarely - from? 1/10 000 to <1/1000; very rarely - <1/10 000, including individual messages):
- on the part of the cardiovascular system: infrequently - a pronounced decrease in blood pressure, orthostatic hypotension, heart failure, peripheral edema;
- from the central nervous system: infrequently - increased fatigue, insomnia, asthenia, fainting, decreased libido; rarely - dizziness; very rarely - mild and transient disturbances in taste sensitivity, headache;
- from the respiratory system: infrequently - nosebleeds, cough;
- from the hematopoietic system: often - neutropenia; rarely - a decrease in hematocrit and hemoglobin; very rarely - thrombocytopenia;
- from the digestive system: infrequently - abdominal pain, diarrhea; rarely - increased activity of hepatic transaminases, hyperbilirubinemia; very rarely - nausea, liver dysfunction;
- from the urinary system: very rarely - decreased renal function, renal failure;
- from the musculoskeletal system: infrequently - back pain; very rarely - myalgia, arthralgia;
- on the part of the organ of hearing: infrequently - vertigo;
- allergic reactions: very rarely - skin rash, itching, angioedema, hypersensitivity reactions (including vasculitis, serum sickness);
- infections: often viral infections; infrequently - sinusitis, pharyngitis, upper respiratory tract infections; very rarely - rhinitis;
- laboratory parameters: infrequently - hyperkalemia; rarely - increased serum urea nitrogen, hypercreatininemia.
In clinical studies of patients with arterial hypertension, adverse events were mostly moderate and transient. The frequency of their development was not associated with the race, sex or age of the patient.
Overdose
There is no sufficient data on valsartan overdose. However, the main expected symptoms are tachycardia and an excessive decrease in blood pressure, up to collapse and / or shock.
There is no specific antidote. If a little time has passed since taking Nortivan, you should induce vomiting, rinse the stomach and take activated charcoal. In the case of a pronounced decrease in blood pressure, intravenous administration of a 0.9% sodium chloride solution is indicated. Hemodialysis is ineffective.
special instructions
It was reported about an increase in the concentration of urea and creatinine in the blood and impaired renal function (in rare cases, the development of acute renal failure). More often, these complications were detected in patients with already existing functional disorders of the kidneys and in patients with severe chronic heart failure.
In the case of the simultaneous use of potassium preparations, their level in the blood serum should be monitored, especially in patients with impaired renal function and the elderly.
The use of Nortivan in patients with myocardial infarction may cause a slight decrease in blood pressure. However, if the recommended dosage regimen is observed, there is usually no need to discontinue the drug due to the development of arterial hypotension. In predisposed patients, renal dysfunction is possible (due to suppression of the RAAS activity). For this reason, treatment should be carried out with caution, under the control of renal function.
A significant additional decrease in blood pressure can be achieved by the combination of Nortivan with hydrochlorothiazide.
Influence on the ability to drive vehicles and complex mechanisms
The effect of the components of the Nortivan tablets on the psychophysical functions of a person has not been studied. However, given the likelihood of increased fatigue and dizziness, during therapy, it is recommended to be careful with vehicle drivers and persons employed in potentially hazardous industries.
Application during pregnancy and lactation
Nortivan is contraindicated during pregnancy. Renal perfusion of the fetus depends on the RAAS. It begins to function in the third trimester of pregnancy, but the risk for the fetus increases when the mother takes valsartan in the second and third trimesters. All drugs acting on the RAAS, if used in the II-III trimesters, can cause damage and even death of the fetus. There are known cases of oligohydramnios, spontaneous miscarriages, impaired renal function in a newborn.
Whether valsartan is excreted in breast milk is unknown. To avoid risk, you should stop feeding if treatment is required during lactation.
Pediatric use
Nortivan is not used in children and adolescents (under 18 years) due to the lack of data on its safety and efficacy in this age group of patients.
With impaired renal function
With mild to moderate renal impairment, there is no need to adjust the dose of Nortivan.
The drug is used with caution to treat patients with severe renal insufficiency (CC <20 ml / min), including patients receiving hemodialysis. Correction of dosage regimen is required.
For violations of liver function
With moderate hepatic impairment (<9 points on the Child-Pugh scale), use Northvan with caution. Correction of dosage regimen is required.
The drug is contraindicated in severe hepatic failure (> 9 points on the Child-Pugh scale), liver cirrhosis, as well as in cholestasis.
Use in the elderly
Northvan is used with caution in elderly patients (over 75 years old). Treatment is recommended to start at lower doses and be carried out under medical supervision.
Drug interactions
Valsartan does not undergo significant metabolism; therefore, its interaction with drugs that are inducers or inhibitors of the cytochrome P 450 system is unlikely.
According to the results of in vitro studies, valsartan is a substrate for the hepatic transporters MRP2 and OATP1B1.
Medicines tested in clinical trials included hydrochlorothiazide, indomethacin, amlodipine, glibenclamide, digoxin, atenolol, warfarin, cimetidine. No significant pharmacokinetic interactions of valsartan have been identified.
It is known about a reversible increase in the concentration of lithium in the blood plasma and an increase in its toxicity in the case of taking lithium preparations simultaneously with ACE inhibitors. In rare cases, these changes were observed when lithium was combined with angiotensin II receptor antagonists. For this reason, Nortivan should be used with caution in combination with lithium preparations.
Acetylsalicylic acid in daily doses of more than 3000 mg and nonsteroidal anti-inflammatory drugs (NSAIDs), including selective COX-2 inhibitors, can reduce the hypotensive effect of valsartan. Concomitant use of NSAIDs and Nortivan increases the risk of developing renal dysfunction, including an increase in plasma potassium levels and acute renal failure, especially in patients with existing functional renal impairment. The use of this combination should be carried out with caution, especially in old age. After the initiation of therapy and periodically during treatment, renal function and circulating blood volume should be monitored.
With the simultaneous use of potassium preparations, potassium-sparing diuretics (for example, spironolactone, amiloride or triamterene), potassium-containing food supplements, an increase in the concentration of potassium in the blood plasma is possible.
Analogs
The analogues of Nortivan are: Aprovel, Atakand, Vazotenz, Valz, Giposart, Diovan, Ibertan, Kanarb, Kozaar, Lozap, Losartan, Lorista, Mikardis, Ordiss, Renicard, Tantordio, Tanidol, Telzap, Firmasta, Edarbi and others.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C out of reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Nortivan
Reviews about Nortivan are mostly positive. This drug is usually prescribed to patients who cannot tolerate ACE inhibitors or who have characteristic side effects - dry cough, angioedema. Also, ACE inhibitors are contraindicated in broncho-obstructive syndrome. In this case, angiotensin II receptor antagonists are better tolerated.
Patients note the effectiveness of Nortivan. After the development of the therapeutic effect, weakness decreased, headaches in the occipital part disappeared, shortness of breath decreased, pain in the heart disappeared. The cost of the drug is generally assessed as acceptable.
No side effects have been reported. Even with long-term use of Nortivan, reactions from the kidneys and liver were not observed, which was confirmed by biochemical studies.
Price for Nortivan in pharmacies
The average price for Northvan for a pack of 30 tablets is: at a dosage of 40 mg - 230 rubles, at a dosage of 80 mg - 290 rubles, at a dosage of 160 mg - 400 rubles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
