tasosartan

Action and Spectrum

Actions and Spectrum  

Tasosartan acts through the blockade of the angiotensin II type 1 (AT1) receptor since this receptor accounts for most or all the major actions of angiotensin II. Angiotensin-converting enzyme inhibitors are a first-line antihypertensive treatment for most patients with essential hypertension. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Headache  

Fatigue  

Nausea  

Abdominal pain  

Decreased WBC count  

Dizziness  

Diarrhea  

Vomiting  

Increased liver enzymes  

Black Box Warning

Black Box Warning 

There was no specific black box warning associated with tasosartan  

Contraindication / Caution

Contraindication /Caution  

Contraindication 

Hypersensitivity  

Severe Hepatic Impairment  

Hypotension  

Caution 

Renal Impairment  

Electrolyte Imbalance  

Hyperkalemia  

Pregnancy / Lactation

Pregnancy/Lactation  

Pregnancy consideration: pregnancy category: not assigned  

Lactation: Excreted into human milk: unknown  

Pregnancy category:  

• Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester.  
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.  
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.     
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.     
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.     
• Category N: No data is available for the drug under this category.  

Pharmacology

Pharmacology 

It is an Angiotensin II type 1 (AT1) receptor antagonist which is long-acting, selective, potent and orally active non-peptide compound. It acts as an antagonist to the AT1 receptor, preventing the interaction of the hormone Angiotensin II which is a strong vasoconstrictor. This leads to vasodilation, decreased peripheral resistance, and therefore low blood pressure. It has relatively short time of onset of action, in the range between 1 and 2 hours, and relatively long time of action, in the range between 12 and 24 hours. 

Pharmacodynamics 

Tasosartan acts as an angiotensin II type 1 receptor antagonist and thus inhibits the rise in blood pressure resulting from the constriction of blood vessels and secretion of aldosterone. This led to relaxation of blood vessels, thereby decreasing peripheral vascular resistance and hence blood pressure. It also suppresses the secretion of aldosterone leading to reduced blood volume and pressure. Tasosartan may also exhibit cardiodepressant effects which help in lessening the cardiac after load and enhancing cardiac performance, such as in heart failure. 

Pharmacokinetics  

Absorption 

Bioavailability is approximately 50%.  

Distribution 

It is highly protein-bound (approximately 99%) to albumin.  

Metabolism 

It is extensively metabolized by the cytochrome P450 system, primarily CYP3A4 and CYP2C9.  

Elimination/Excretion 

Small portion is eliminated through the feces  

Adminstartion

Administration 

It is administered orally  

Patient Information Leaflet

Patient information leaflet  

Generic Name: tasosartan  

Pronounced: (tah-so-SAR-tan)  

Why do we use tasosartan?  

In clinical trials the antihypertensive drug tasosartan is mainly used as the target for essential Hypertension patients. It is used to reduce diastolic and systolic blood pressure in patients with essential hypertension.