azilsartan

Action and Spectrum

Actions and Spectrum: 

azilsartan is an angiotensin receptor blocker (ARB) medication used to lower blood pressure in adults. It works by blocking the actions of a hormone called angiotensin II, which causes blood vessels to narrow and blood pressure to increase. azilsartan is typically used as a second-line treatment for hypertension, after other medications such as diuretics and ACE inhibitors have failed to control blood pressure. It is usually taken once daily, with or without food. Common side effects of azilsartan include headache, dizziness, and back pain. More serious side effects are rare but can include kidney problems and allergic reactions.

Drug Interaction

Adverse Reaction

Frequency Defined  

<1%   

Asthenia  

Muscle spasm  

Fatigue  

Dizziness  

Nausea  

Cough  

Postural hypotension  

1-10%   

Diarrhea (2%)  

Post marketing Reports  

Muscle spasm  

Nausea  

Black Box Warning

Black Box Warning 

azilsartan, a medication used to treat hypertension (high blood pressure), carries a black box warning due to the risk of developing sprue-like enteropathy, a serious condition characterized by chronic diarrhea, weight loss, and malnutrition. 

Contraindication / Caution

Contraindication/Caution: 

azilsartan is contraindicated in individuals who are hypersensitive to the active ingredient or any of the excipients in the medication. It is also contraindicated in individuals with a history of angioedema related to previous treatment with an angiotensin receptor blocker (ARB).  

Caution should be exercised when administering azilsartan to individuals with a history of renal impairment, hepatic impairment, or dehydration as it may exacerbate these conditions. Additionally, caution should be used when administering azilsartan to individuals who are taking other medications that can affect the renin-angiotensin-aldosterone system (RAAS) such as ACE inhibitors, diuretics, or potassium supplements.

Pregnancy / Lactation

Pregnancy warnings:     

US FDA pregnancy category: C for 1st trimester; D for 2nd & 3rd trimesters 

Lactation:   

Excreted into human milk is unknown.  

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   

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 available 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: There is no data available for the drug under this category.

Pharmacology

Pharmacology:  

azilsartan is an angiotensin II receptor blocker (ARB) medication used to treat hypertension (high blood pressure). It works by blocking the action of angiotensin II, a hormone that causes blood vessels to constrict, leading to an increase in blood pressure.  

Pharmacodynamics:  

azilsartan is an angiotensin II receptor blocker (ARB) that is used to treat hypertension (high blood pressure). It works by blocking the actions of angiotensin II, a hormone that causes blood vessels to constrict and raises blood pressure.  

Once in the body, azilsartan binds to the angiotensin II type 1 receptor (AT1R) and blocks the actions of angiotensin II. This leads to the relaxation of blood vessels, which lowers blood pressure. Azilsartan also has a direct vasodilating effect on blood vessels, which further contributes to its blood pressure-lowering effect. 

Pharmacokinetics:  

Absorption  

It is rapidly and extensively absorbed after oral administration, with peak plasma concentrations occurring within 1-3 hours. The bioavailability of azilsartan is approximately 77%.  

Distribution  

azilsartan is highly protein-bound in the bloodstream, primarily to albumin. The volume of distribution is approximately 500 L.  

Metabolism  

It is metabolized primarily by cytochrome P450 (CYP) 3A4 and to a lesser extent by CYP2C9. The primary metabolite is the inactive carboxylic acid derivative.  

Elimination and Excretion  

azilsartan and its metabolites are primarily excreted in the feces, with less than 2% excreted in the urine. The elimination half-life of azilsartan is approximately 12 hours.

Adminstartion

Administration:  

Oral administration: 

azilsartan is typically administered orally, in tablet form. The recommended starting dosage is typically 40 mg once daily, with the option to increase the dosage to 80 mg once daily, if needed. It is important to take azilsartan at the same time each day, with or without food. 

It is important to note that azilsartan should not be used in combination with other medications that contain aliskiren, as this can increase the risk of serious side effects such as kidney problems, high potassium levels, and low blood pressure. 

Patients should also be monitored regularly for blood pressure and kidney function while taking azilsartan, and any changes in symptoms or side effects should be reported to the healthcare provider immediately. 

It is important to take azilsartan as directed by the healthcare provider, and to not stop taking it without consulting with the healthcare provider first, as this can cause the blood pressure to increase again. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: azilsartan 

Why do we use azilsartan? 

azilsartan is an angiotensin receptor blocker (ARB) medication used to lower blood pressure in adults. It works by relaxing the blood vessels, allowing blood to flow more easily and reducing the workload on the heart. It is used to treat hypertension (high blood pressure) and can be used alone or in combination with other blood pressure medications. It can also be used to improve the chance of living longer after a heart attack in people who have high blood pressure and heart failure or left ventricular dysfunction.