Сартавель
Сартавель Uses, Dosage, Side Effects, Food Interaction and all others data.
Сартавель is an oral medication that belongs to a class of drugs called angiotensin receptor blockers (ARBs). It is orally active and specific angiotensin II antagonist acting on the AT1 subtype. Angiotensin's attachment to the receptors cause the blood vessels to narrow (vasoconstrict) which leads to an increase in blood pressure (hypertension). Сартавель blocks the angiotensin II receptor. By blocking the action of angiotensin, Сартавель dilates blood vessels and reduces blood pressure without affecting pulse rate. Сартавель has much greater affinity (about 20,000-fold) for the AT1 receptor than for the AT2 receptor. It does not bind or block other hormone receptors or ion channels known to be important in cardiovascular regulation.
Сартавель inhibits the pressor effects of angiotensin II with oral doses of 80 mg inhibiting the pressor effect by about 80% at peak with approximately 30% inhibition persisting for 24 hours. Removal of the negative feedback of angiotensin II causes a 2- to 3-fold rise in plasma renin and consequent rise in angiotensin II plasma concentration in hypertensive patients. Minimal decreases in plasma aldosterone were observed after administration of valsartan.
In multiple-dose studies in hypertensive patients, valsartan had no notable effects on total cholesterol, fasting triglycerides, fasting serum glucose, or uric acid.[F4607]
Hypotension
Trade Name | Сартавель |
Availability | Prescription only |
Generic | Valsartan |
Valsartan Other Names | Valsartan |
Related Drugs | amlodipine, aspirin, lisinopril, metoprolol, losartan, furosemide, carvedilol, hydrochlorothiazide, propranolol, spironolactone |
Type | |
Formula | C24H29N5O3 |
Weight | Average: 435.5188 Monoisotopic: 435.227039819 |
Protein binding | Valsartan is highly bound to serum proteins (95%), mainly serum albumin.[F4607] |
Groups | Approved, Investigational |
Therapeutic Class | Angiotensin-ll receptor blocker |
Manufacturer | |
Available Country | Russia |
Last Updated: | September 19, 2023 at 7:00 am |
![Сартавель Сартавель](https://www.medicinesfaq.com/media/png/sartavel.png)
Uses
Сартавель is used for:
- For hypertension
- To reduce hospitalizations in patients with congestive heart failure
- To reduce death in patients who developed congestive heart failure after myocardial infarction
Сартавель is also used to associated treatment for these conditions: Cardiovascular Mortality, Diabetic Nephropathy, High Blood Pressure (Hypertension), Left Ventricular Dysfunction, Moderate Essential Hypertension, Chronic heart failure with reduced ejection fraction (NYHA Class II), Chronic heart failure with reduced ejection fraction (NYHA Class III), Chronic heart failure with reduced ejection fraction (NYHA Class IV), Hospitalization due to cardiac failure
How Сартавель works
Сартавель belongs to the angiotensin II receptor blocker (ARB) family of drugs, which selectively bind to angiotensin receptor 1 (AT1) and prevent angiotensin II from binding and exerting its hypertensive effects. These include vasoconstriction, stimulation and synthesis of aldosterone and ADH, cardiac stimulation, and renal reabsorption of sodium among others. Overall, valsartan's physiologic effects lead to reduced blood pressure, lower aldosterone levels, reduced cardiac activity, and increased excretion of sodium.
Сартавель also affects the renin-angiotensin aldosterone system (RAAS), which plays an important role in hemostasis and regulation of kidney, vascular, and cardiac functions. Pharmacological blockade of RAAS via AT1 receptor blockade inhibits negative regulatory feedback within RAAS which is a contributing factor to the pathogenesis and progression of cardiovascular disease, heart failure, and renal disease. In particular, heart failure is associated with chronic activation of RAAS, leading to inappropriate fluid retention, vasoconstriction, and ultimately a further decline in left ventricular function. ARBs have been shown to have a protective effect on the heart by improving cardiac function, reducing afterload, increasing cardiac output and prevent ventricular hypertrophy.
The angiotensin-converting enzyme inhibitor (ACEI) class of medications (which includes drugs such as ramipril, lisinopril, and perindopril) inhibits the conversion of angiotensin I to angiotensin II by inhibiting the ACE enzyme but does not prevent the formation of all angiotensin II. ARB activity is unique in that it blocks all angiotensin II activity, regardless of where or how it was synthesized.
Сартавель is commonly used for the management of hypertension, heart failure, and type 2 diabetes-associated nephropathy, particularly in patients who are unable to tolerate ACE inhibitors. ARBs such as valsartan have been shown in a number of large-scale clinical outcomes trials to improve cardiovascular outcomes including reducing risk of myocardial infarction, stroke, the progression of heart failure, and hospitalization. Сартавель also slows the progression of diabetic nephropathy due to its renoprotective effects. Improvements in chronic kidney disease with valsartan include both clinically and statistically significant decreases in urinary albumin and protein excretion in patients diagnosed with type 2 diabetes and in nondiabetic patients diagnosed with chronic kidney disease.
Сартавель also binds to the AT2 receptor, however AT2 is not known to be associated with cardiovascular homeostasis like AT1. Сартавель has about 20,000-fold higher affinity for the AT1 receptor than for the AT2 receptor. The increased plasma levels of angiotensin II following AT1 receptor blockade with valsartan may stimulate the unblocked AT2 receptor.
Dosage
Сартавель dosage
Hypertension: The usual dose of Сартавель is 80 to 160 mg once daily. The maximum dose is 320 mg daily. Maximum blood pressure reduction occurs within 4 weeks.
Heart failure:The usual dose is 40 mg twice daily and may be increased to 80-160 mg twice daily.
Post-Myocardial Infarction:The initial dose after myocardial infarction is 20 mg twice daily. The dose should be increased with a target of 160 mg daily if tolerated without side effects.
Administration of Сартавель with food decreases the absorption of Сартавель by about 40%, so it should be taken on an empty stomach. No initial dosage adjustment is required for elderly patients with mild to moderate renal and hepatic insufficiency.
Side Effects
Сартавель is generally well tolerated and side effects are rare. The most common side effects include headache, dizziness, fatigue, abdominal pain, cough, diarrhea and nausea. Patient may also experience hyperkalemia, impotency, reduced renal function, allergic reactions, dyspnea, constipation, back pain, muscle cramps, rash, anxiety, insomnia and vertigo. Hypotension may also occur if patient have been taking diuretics along with Сартавель.
Toxicity
Approximate LD50 >2000 mg/kg (Gavage, rat) [F3139]
Reproductive Toxicology Studies
No teratogenic effects were seen when valsartan was given to pregnant mice and rats at oral doses up to 600 mg/kg/day and to pregnant rabbits at oral doses reaching up to 10 mg/kg/day. Despite this, marked decreases in fetal weight, pup birth weight, pup survival rate, and delays in developmental milestones were noted in studies in which parental rats were treated with valsartan at oral, maternally toxic doses of 600 mg/kg/day during the organogenesis period or during late gestation and lactation.[F4607]
Pregnancy
When used in pregnancy, drugs that act directly on the renin-angiotensin system (RAAS) can cause injury and death to the developing fetus. When pregnancy is detected, valsartan should be discontinued as soon as possible.[F4607]
Precaution
Impaired Hepatic Function: As the majority of Сартавель is eliminated in the bile, care should be exercised in patients with mild to moderate hepatic impairment including biliary obstructive disorder.
Impaired Renal Function: Dosage reduction or discontinuation may be required with patients having pre-existing renal impairment.
Heart Failure and Myocardial Infarction: Caution should be exercised when initiating therapy in patients with heart failure and post-myocardial infarction patients.
Interaction
No drug interactions of clinical significance have been found. Compounds which have been studied in clinical trials include Cimetidine, Warfarin, Furosemide, Digoxin, Atenolol, Indomethacin, Hydrochlorothiazide, Amlodipine and GlibenclamideAs Сартавель is not metabolized to a significant extent, clinically relevant drug-drug interactions in the form of metabolic induction or inhibition of the cytochrome P450 system are not expected with Сартавель. Although valsartan is highly bound to plasma proteins, in vitrostudies have not shown any interaction at this level with a range of molecules which are also highly protein bound, such as Diclofenac, Furosemide, and Warfarin. Concomitant use of potassium sparing diuretics (e.g., Spironolactone, Triamterene, Amiloride) potassium supplements, or salt substitutes containing potassium may lead to increase in serum potassium. If co medication is considered necessary, caution is advisable
Food Interaction
- Take with or without food. Co-administration with food slightly alters pharmacokinetics, but not to a clinically significant extent.
[Moderate] GENERALLY AVOID: Moderate-to-high dietary intake of potassium, especially salt substitutes, may increase the risk of hyperkalemia in some patients who are using angiotensin II receptor blockers (ARBs).
ARBs can promote hyperkalemia through inhibition of angiotensin II-induced aldosterone secretion.
Patients with diabetes, heart failure, dehydration, or renal insufficiency have a greater risk of developing hyperkalemia.
MANAGEMENT: Patients should receive dietary counseling and be advised to not use potassium-containing salt substitutes or over-the-counter potassium supplements without consulting their physician.
If salt substitutes are used concurrently, regular monitoring of serum potassium levels is recommended.
Patients should also be advised to seek medical attention if they experience symptoms of hyperkalemia such as weakness, irregular heartbeat, confusion, tingling of the extremities, or feelings of heaviness in the legs.
Сартавель Drug Interaction
Moderate: aspirin, aspirin, pregabalin, metoprolol, metoprololUnknown: ubiquinone, rosuvastatin, duloxetine, apixaban, omega-3 polyunsaturated fatty acids, atorvastatin, esomeprazole, clopidogrel, levothyroxine, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, rivaroxaban, cetirizine
Сартавель Disease Interaction
Major: diabetes, angioedema, hypotensionModerate: CHF, hyperkalemia, renal artery stenosis, renal impairment, renal/liver disease
Volume of Distribution
The steady state volume of distribution of valsartan after intravenous administration is small (17 L), indicating that valsartan does not distribute into tissues extensively.[F3139,F3607]
Elimination Route
After one oral dose, the antihypertensive activity of valsartan begins within approximately 2 hours and peaks within 4-6 hours in most patients.[F3139] Food decreases the exposure to orally administered valsartan by approximately 40% and peak plasma concentration by approximately 50%. AUC and Cmax values of valsartan genereally increase linearly with increasing dose over the therapeutic dose range. Сартавель does not accumulate appreciably in plasma following repetitive administration.[F4607]
Half Life
After intravenous (IV) administration, valsartan demonstrates bi-exponential decay kinetics, with an average elimination half-life of about 6 hours.[F4607]
Clearance
Following intravenous administration, plasma clearance of valsartan is approximately 2 L/hour and its renal clearance is 0.62 L/hour (about 30% of total clearance).[F4607]
Elimination Route
Сартавель, when administered as an oral solution, is primarily recovered in feces (about 83% of dose) and urine (about 13% of dose). The recovery is mainly as unchanged drug, with only about 20% of dose recovered as metabolites.[F4607]
Pregnancy & Breastfeeding use
Pregnancy: Сартавель should not be used in pregnancy, as in 2nd and 3rd trimester it can cause injury and even death to fetus. When pregnancy is detected, Сартавель should be stopped as soon as possible.
Nursing mothers: It is not known whether Сартавель is excreted in human milk. Because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Contraindication
Сартавель is contraindicated in patients who are hypersensitive to any component of this product.
Special Warning
Pediatric use: Safety and effectiveness in paediatric patients have not been established.Geriatric use: No overall difference in the efficacy or safety of Сартавель was observed in this patient population, but greater sensitivity of some elderly persons cannot be ruled out.Hepatic Impairment:
- Mild to moderate: Max: 80 mg once daily.
- Severe: Contraindicated.
Acute Overdose
Limited data are available related to overdosage in humans. The most likely manifestations of overdosage would be hypotension and tachycardia, bradycardia could occur from parasympathetic (vagal) stimulation. If excessive hypotension occurs, the patient should be placed in the supine position and if necessary, has to be given an intravenous infusion of normal saline.
Storage Condition
Store between 15-30° C. Protect from moisture and heat.
Innovators Monograph
You find simplified version here Сартавель
Сартавель contains Valsartan see full prescribing information from innovator Сартавель Monograph, Сартавель MSDS, Сартавель FDA label
FAQ
What is Сартавель used for?
Сартавель is used to treat high blood pressure and heart failure. It is also used to improve the chance of living longer after a heart attack. It works by relaxing blood vessels so that blood can flow more easily. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems.
What are the common side effects of Сартавель?
Check with your doctor immediately if any of the following side effects occur:
- Less common
- Bloody urine
- cold sweats
- confusion
- decreased frequency or amount of urine
- difficult breathing
- dizziness, faintness, or lightheadedness when getting up from a lying position
- fainting
- increased thirst
- irregular heartbeat
- loss of appetite
- lower back or side pain
- nausea
- nervousness
- numbness or tingling in the hands, feet, or lips
- swelling of the face, fingers, or lower legs
- unusual tiredness or weakness
- vomiting
- weakness of heaviness of the legs
- weight gain
Why is Сартавель bad for you?
You may have a higher risk if you're dehydrated or take high doses of diuretics (water pills). High blood potassium warning: This Сартавель can increase your potassium levels.
How safe is Сартавель?
Сартавель is not toxic, but the drug should always be taken as directed may safe.Сартавель lowers blood pressure, so taking too much valsartan could result in dangerously low blood pressure.
Is Сартавель safe during pregnancy?
Do not take Сартавель if you are pregnant. If you become pregnant while you are taking Сартавель, stop taking Сартавель and call your doctor immediately.Сартавель may cause death or serious injury to the fetus when taken in the last 6 months of pregnancy.
Is Сартавель safe for breastfeeding?
Small amounts of Сартавель may get into breast milk. This can cause low blood pressure in the baby. Talk to your doctor, as other medicines might be better while you are breastfeeding.
Is Сартавель a safe blood pressure medicine?
Сартавель is a high blood pressure drug that is considered generally safe and tolerated better by patients than alternative treatments.
Is Сартавель bad for kidneys?
If Сартавель continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failur.
When should I take Сартавель?
Our results indicate that doses of 160 mg/d Сартавель are equally effective for BP control when taken once daily either on awakening or at bedtime.
Is Сартавель kidney protective?
Bedtime administration of Сартавель is considered to normalize circadian rhythm and protect the kidneys and heart in CKD patients.
Can I drink alcohol while taking Сартавель?
It is best to stop drinking alcohol until you see how the medicine affects you.Drinking alcohol can increase the blood pressure-lowering effect of Сартавель, which can make you feel dizzy or lightheaded.
Does Сартавель make me tired?
Сартавель oral tablet doesn't cause drowsiness or tired. but it can cause other side effects.
How long does Сартавель last?
Сартавель can last up to 24 hours.Dosing strength varies depending on the condition being treated.
Can I stop Сартавель suddenly?
Stopping it suddenly may cause your blood pressure to spike. This may increase your chance for a heart attack or stroke.Don't stop taking this drug without talking to your doctor.
Does Сартавель help anxiety?
Сартавель reverses anxiety ,like behavior and induces hippocampal neurogenesis and expression of BDNF protein in unpredictable chronic mild stress mice.
Does Сартавель increase heart rate?
Сартавель does not directly cause a drop in heart rate, but it might have that effect indirectly in a small percentage of people who take it.
Does make make me lose weight?
In this population of overweight or obese patients with mild to moderate hypertension,Сартавель was well tolerated, and could be effective in controlling blood pressure and achieving weight loss in such patients.
Does Сартавель make I pee?
Сартавель is a combination of Сартавель and hydroclorothiazide, a diuretic, and it has been reported to cause nocturia, or frequent night urination.Сартавель has caused little or no increase in urination by itself.
Does Сартавель lower diastolic blood pressure?
Сартавель and enalapril induced a significant and comparable reduction of systolic and diastolic blood pressure.
Is Сартавель a diuretic?
Сартавель is a combination of an angiotensin receptor blocker and a diuretic used for treating hypertension (high blood pressure).
Does Сартавель cause liver damage?
The FDA has received reports that Сартавель has been linked with acute liver injury and elevations in some liver enzymes.
Can I take Сартавель for a long time?
Сартавель is generally safe to take for a long time.it works best when you take it for a long time. taking Сартавель for a long time can sometimes cause your kidneys not to work as well as they should.