Azilsartan is an angiotensin receptor blocker that primarily inhibits angiotensin I receptors resulting in vasodilation and inhibiting sodium and water retention.

It is utilised to treat hypertension.

Along with treating individuals with acute coronary syndrome, it is also used off-label for the secondary prevention of cardiovascular events in patients with stable coronary artery disease.

Azilsartan Dose in Adults

Dose in the treatment of Hypertension:

• 40 mg orally once a day.
• The dose may be titrated upwards upto 80 mg once a day.

Azilsartan Dose in Children

Not recommended

Pregnancy Risk Factor D

• [US Boxed Warning]
  • Azilsartan, like other medications that affect the RAAS, has the potential to harm or kill a growing foetus.
  • Once pregnancy has been identified, it needs to end right away.
  • It crosses the placental line and is linked to oligohydramnios, which can result in skeletal abnormalities or foetal lung hypoplasia.
  • Furthermore, oligohydramnios might not show up until severe foetal harm has been done.
  • It can also lead to hypotension, anuria and skull hypoplasia in infants/neonates.
  • ACE-Inhibitors and ARBs should generally be avoided in hypertensive patients of child-bearing ages.
  • Alternative therapies should be considered if necessary.

Use Azilsartan during lactation

• It is unknown if the drug can be absorbed into breastmilk.
• The manufacturer suggests that you stop using the drug and discontinue breastfeeding because of possible adverse effects.

Azilsartan Dose in Renal Disease:

• Adjustment in the dose has not been recommended.
• Renal functions should be monitored.

Azilsartan Dose in Liver Disease:

Adjustment in the dose has not been provided in the manufacturer's labeling, however, it should be used with caution especially in advanced liver disease and those with ascites. 

Common Side Effects of Azilsartan Include:

• Gastrointestinal:
  • Diarrhea

Frequency not defined:

• Cardiovascular:
  • Hypotension
  • Orthostatic Hypotension
• Central Nervous System:
  • Dizziness
  • Fatigue
  • Orthostatic Dizziness
• Gastrointestinal:
  • Nausea
• Neuromuscular & Skeletal:
  • Asthenia
  • Muscle Spasm
• Renal:
  • Increased Serum Creatinine
• Respiratory:
  • Cough

Contraindication to Azilsartan Include:

• Avoid using azilsartan with aliskiren-containing products.
• Allergy 
• Pregnancy
• Breastfeeding

Warnings and Precautions

• Angioedema
  • Zilsartan has been associated with angioedema. This can occur at any stage of treatment.
  • Patients who have a history of idiopathic, hereditary, or angioedema connected to ACE-inhibitors may be at higher risk.
  • If patients experience swelling in the larynx, glottis or face, it is important to monitor them.
  • The drug should be stopped immediately and not be restarted.
  • Aggressive management of the airway and Intramuscular epinephrine should be part of the resuscitation.
• Hyperkalemia:
  • Patients with impaired renal function, Diabetes mellitus, Patients taking potassium-sparing diuretics and patients who take potassium-containing salts or potassium supplements are at increased risk of hyperkalemia.
• Hypotension
  • Hypotension is a risk factor for patients who are salt- and volume-depleted (e.g. patients on high-dose diuretics).
  • The patient must be well hydrated before initiating therapy.
  • Zilsartan therapy is safe for transient hypotension.
• Renal function deterioration:
  • An rise in serum creatinine is a sign that angiotensin receptor blocking medications may worsen renal function.
  • Renal function decline is most likely to occur in patients who are volume-depleted, have heart disease, and have renal artery stenosis.
  • Serum creatinine levels may slightly rise as a result of treatment. Nevertheless, it's crucial to keep up with your medication and keep an eye on your kidney function.
• Mitral and aortic stenosis:
  • Patients suffering from mitral or aortic blockage should be cautious when taking the drug.
• Ascites:
  • Patients suffering from cirrhosis and refractory ascites must be cautious about taking the drug.
  • To avoid rapid decline in renal function, it is important to monitor blood pressure and renal functions.
• Renal artery stenosis
  • This should be avoided in bilateral renal arterial stenosis, and it should only be used in unilateral renal artery narrowing.
• Renal impairment
  • Preexisting renal impairments should be avoided.

Azilsartan: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitoring Parameters:

 Monitor Blood pressure, serum electrolytes, serum creatinine, and BUN.

Target Blood pressure:

• Target blood pressure of less than 130/80 mmHg in patients with hypertension and known cardiovascular disease or the 10-year ASCVD risk is greater than 10%.

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• The target blood pressure of less than 130/80 mmHg may be reasonable in patients with ASCVD risk.

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• Target blood pressure of less than 140/90 mmHg in patients aged 18 – 65 years with Diabetes and hypertension without cardiovascular disease and the 10-year ASCVD risk is less than 15%.

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• Target blood pressure of less than 130/80 mmHg in patients aged 18 – 65 years with Diabetes, hypertension, cardiovascular disease, or the 10-year ASCVD risk is greater than 15%.

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• Target blood pressure of less than 140/90 mmHg in patients aged more than 65 years and without major comorbid conditions.

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• Target blood pressure of less than 150/90 mmHg in patients aged more than 65 years and poor health or comorbid conditions.

How to take Azilsartan?

• It can be taken orally and with or without food.

Mechanism of action of Azilsartan:

• Angiotensin I cannot attach to its receptors when azilsartan is present.
• It is highly attracted to angiotensin I receptors as well as angiotensin I receptors.
• Angiotensin II can cause vasoconstriction and stimulate the synthesis of aldosterone.
• It also stimulates the heart and causes sodium reabsorption.
• Azilsartan inhibits the angiotensin receptors only in the vascular smooth muscle and adrenal glands, with very little effect on the cardiovascular system or bradykinin

More than 99% are covered by the drugprotein-bound. It is then hydrolyzed in your stomach to make it an active metabolite.MetabolizedTo inactive metabolites, use CYP2C9.

It has been abioavailability60% and morehalf-life eliminationA total of 11 hours. The time it takes topeak serum concentrationIt takes 1.5-3 hours. It is excreted primarily via feces (55%) and urine (42%).

International Brands of Azilsartan:

• Azildac
• Azilispire
• Azilsar
• Azilva
• Edarbi
• Ipreziv
• Lan Sha

Azilsartan Brands in Pakistan:

No brands available in Pakistan.