Prexxartan Uses, Dosage, Side Effects, Food Interaction and all others data.

Prexxartan 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). Prexxartan blocks the angiotensin II receptor. By blocking the action of angiotensin, Prexxartan dilates blood vessels and reduces blood pressure without affecting pulse rate. Prexxartan 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.

Prexxartan 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]


Trade Name Prexxartan
Availability Prescription only
Generic Valsartan
Valsartan Other Names Valsartan
Related Drugs amlodipine, aspirin, lisinopril, metoprolol, losartan, furosemide, carvedilol, hydrochlorothiazide, propranolol, spironolactone
Type Oral
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
Available Country United States
Last Updated: September 19, 2023 at 7:00 am


Prexxartan 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

Prexxartan 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 Prexxartan works

Prexxartan 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.

Prexxartan 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.

Prexxartan 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. Prexxartan 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.

Prexxartan also binds to the AT2 receptor, however AT2 is not known to be associated with cardiovascular homeostasis like AT1. Prexxartan 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.


Prexxartan dosage

Hypertension: The usual dose of Prexxartan 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 Prexxartan with food decreases the absorption of Prexxartan 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

Prexxartan 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 Prexxartan.


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]


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]


Impaired Hepatic Function: As the majority of Prexxartan 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.


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 Prexxartan 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 Prexxartan. 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.

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. Prexxartan 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]


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

Prexxartan, 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: Prexxartan 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, Prexxartan should be stopped as soon as possible.

Nursing mothers: It is not known whether Prexxartan 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.


Prexxartan 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 Prexxartan 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 Prexxartan

Prexxartan contains Valsartan see full prescribing information from innovator Prexxartan Monograph, Prexxartan MSDS, Prexxartan FDA label


What is Prexxartan used for?

Prexxartan 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 Prexxartan?

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 Prexxartan 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 Prexxartan can increase your potassium levels.

How safe is Prexxartan?

Prexxartan is not toxic, but the drug should always be taken as directed may safe.Prexxartan lowers blood pressure, so taking too much valsartan could result in dangerously low blood pressure.

Is Prexxartan safe during pregnancy?

Do not take Prexxartan if you are pregnant. If you become pregnant while you are taking Prexxartan, stop taking Prexxartan and call your doctor immediately.Prexxartan may cause death or serious injury to the fetus when taken in the last 6 months of pregnancy.

Is Prexxartan safe for breastfeeding?

Small amounts of Prexxartan 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 Prexxartan a safe blood pressure medicine?

Prexxartan is a high blood pressure drug that is considered generally safe and tolerated better by patients than alternative treatments.

Is Prexxartan bad for kidneys?

If Prexxartan 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 Prexxartan?

Our results indicate that doses of 160 mg/d Prexxartan are equally effective for BP control when taken once daily either on awakening or at bedtime.

Is Prexxartan kidney protective?

Bedtime administration of  Prexxartan is considered to normalize circadian rhythm and protect the kidneys and heart in CKD patients.

Can I drink alcohol while taking Prexxartan?

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 Prexxartan, which can make you feel dizzy or lightheaded. 

Does Prexxartan make me tired?

Prexxartan oral tablet doesn't cause drowsiness or tired. but it can cause other side effects.

How long does Prexxartan last?

Prexxartan can last up to 24 hours.Dosing strength varies depending on the condition being treated.

Can I stop Prexxartan 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 Prexxartan help anxiety?

Prexxartan reverses anxiety ,like behavior and induces hippocampal neurogenesis and expression of BDNF protein in unpredictable chronic mild stress mice.

Does Prexxartan increase heart rate?

Prexxartan 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,Prexxartan was well tolerated, and could be effective in controlling blood pressure and achieving weight loss in such patients.

Does Prexxartan make I pee?

Prexxartan is a combination of Prexxartan and hydroclorothiazide, a diuretic, and it has been reported to cause nocturia, or frequent night urination.Prexxartan has caused little or no increase in urination by itself.

Does Prexxartan lower diastolic blood pressure?

Prexxartan and enalapril induced a significant and comparable reduction of systolic and diastolic blood pressure.

Is Prexxartan a diuretic?

Prexxartan is a combination of an angiotensin receptor blocker and a diuretic used for treating hypertension (high blood pressure).

Does Prexxartan cause liver damage?

The FDA has received reports that Prexxartan has been linked with acute liver injury and elevations in some liver enzymes.

Can I take Prexxartan for a long time?

Prexxartan is generally safe to take for a long works best when you take it for a long time. taking Prexxartan for a long time can sometimes cause your kidneys not to work as well as they should.

*** Taking medicines without doctor's advice can cause long-term problems.