Azilsartan

Name: Azilsartan

Adverse Effects

1-10%

Diarrhea (2%)

<1%

Nausea

Asthenia

Fatigue

Muscle spasm

Dizziness

Postural hypotension

Cough

Postmarketing Reports

Nausea

Muscle spasm

Rash, pruritus, angioedema

Azilsartan Overview

Azilsartan is a prescription medication used to treat high blood pressure. Azilsartan belongs to a group of drugs called angiotensin II receptor blockers (ARBs) which block a natural substance that narrows blood vessels, allowing the blood to flow more smoothly and the heart to pump more efficiently.

This medication comes in tablet form and is taken once daily, with or without food.

Diarrhea is the most common azilsartan side effect.

 

Azilsartan Precautions

Contact your doctor right away if you become pregnant while taking azilsartan. See "Pregnancy" and "FDA Warning" sections for more information.

Do not take azilsartan if you are allergic to azilsartan, the active ingredient in azilsartan, or any inactive ingredient in azilsartan. See "Forms of Medication" for a list of inactive ingredients.

Azilsartan can cause very low blood pressure leading to dizziness, lightheadedness, and fainting when you get up too quickly from a lying position. This is more commonly seen at the beginning of therapy in people who take diuretics, or in people on dialysis. Diarrhea, vomiting, not drinking enough fluids, and sweating can cause a decrease in blood pressure and can lead to lightheadedness and fainting. Tell your doctor if you have any of these problems during your treatment. 

  • Avoid getting up too fast from a sitting or lying position.
  • Get up slowly and prevent falls by steadying yourself.
  • Do not drive or operate heavy machinery until you know how azilsartan affects you.
  • Limit alcoholic beverages.

Your doctor may monitor your kidney function if you are elderly, have kidney disease, have severe congestive heart failure (CHF) or if you are taking nonsteroidal anti-inflammatory drugs, as azilsartan may cause a decrease in kidney function.

Do not use potassium supplements or salt substitutes while you are receiving azilsartanazilsartan, unless your doctor instructs you to.

Other Requirements

  • Store azilsartan at room temperature between 59°F to 86°F (15°C to 30°C).
  • Store azilsartan in the original container that you received from your pharmacist or doctor. Do not put azilsartan into a different container.
  • Keep azilsartan in a tightly closed container, and keep azilsartan out of the light.
  • Keep azilsartan and all medicines out of the reach of children.
 

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking azilsartan?

Do not use potassium supplements or salt substitutes while you are taking azilsartan, unless your doctor has told you to.

Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall.

Azilsartan side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

  • painful or difficult urination;

  • little or no urinating;

  • feeling tired or short of breath;

  • a light-headed feeling, like you might pass out; or

  • swelling in your feet or ankles.

Common side effects may include:

  • diarrhea.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Proper Use of azilsartan

In addition to taking azilsartan, treatment for your high blood pressure may include weight control and a change in the foods you eat, especially foods high in sodium (salt). Your doctor will tell you which of these are most important for you. You should check with your doctor before changing your diet.

Many patients who have high blood pressure will not notice any signs of the problem. In fact, many may feel normal. It is very important that you take your medicine exactly as directed and that you keep your appointments with your doctor even if you feel well.

Remember that azilsartan will not cure your high blood pressure, but it does help control it. You must continue to take it as directed if you expect to lower your blood pressure and keep it down. You might have to take high blood pressure medicine for the rest of your life. If high blood pressure is not treated, it can cause serious problems such as heart failure, blood vessel disease, stroke, or kidney disease.

azilsartan may be taken with or without food.

Take all other medicines your doctor has prescribed to treat your condition.

azilsartan comes with a patient information leaflet. It is very important that you read and understand this information. Be sure to ask your doctor about anything you do not understand.

Dosing

The dose of azilsartan will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of azilsartan. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (tablets):
    • For high blood pressure:
      • Adults—80 milligrams (mg) once a day. Certain patients may need to start with 40 mg once daily.
      • Children—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of azilsartan, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Protect the medicine from light and moisture. Keep your medicine in the original container until you are ready to use it.

Uses of Azilsartan

  • It is used to treat high blood pressure.
  • It may be given to you for other reasons. Talk with the doctor.

If OVERDOSE is suspected

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

Pronunciation

(ay zil SAR tan)

Pharmacology

Angiotensin II (which is formed by enzymatic conversion from angiotensin I) is the primary pressor agent of the renin-angiotensin system. Effects of angiotensin II include vasoconstriction, stimulation of aldosterone synthesis/release, cardiac stimulation, and renal sodium reabsorption. Azilsartan inhibits angiotensin II’s vasoconstrictor and aldosterone-secreting effects by selectively blocking the binding of angiotensin II to the AT1 receptor in vascular smooth muscle and adrenal gland tissues (azilsartan has a stronger affinity for the AT1 receptor than the AT2 receptor). The action is independent of the angiotensin II synthesis pathways. Azilsartan does not inhibit ACE (kininase II), therefore it does not affect the response to bradykinin (the clinical relevance of this is unknown) and does not bind to or inhibit other receptors or ion channels of importance in cardiovascular regulation.

Distribution

Vd: ~16 L

Metabolism

Gut: prodrug hydrolyzed to active metabolite; Hepatic: primarily via CYP2C9 to inactive metabolites

Excretion

Feces (~55%); urine (~42%, 15% as unchanged drug)

Clearance: 2.3 mL/minute

Time to Peak

Serum: 1.5-3 hours

Half-Life Elimination

~11 hours

Protein Binding

>99%; primarily to serum albumin

Dosing Adult

Hypertension: Oral: 80 mg once daily; consider initial dose of 40 mg once daily in patients with volume depletion (eg, patients receiving high-dose diuretics); usual dosage (ASH/ISH [Weber 2014]): 80 mg daily

Adverse Reactions

Frequency not always defined.

Cardiovascular: Hypotension, orthostatic hypotension

Central nervous system: Dizziness, fatigue

Gastrointestinal: Diarrhea (2%), nausea

Hematologic & oncologic: Decreased hemoglobin, decreased hematocrit, decreased red blood cells, leukopenia (rare), thrombocytopenia (rare)

Neuromuscular & skeletal: Muscle spasm, weakness

Renal: Increased serum creatinine

Respiratory: Cough

<1% (Limited to important or life-threatening): Angioedema, pruritus, skin rash

Dialysis

Data not available

Azilsartan medoxomil Breastfeeding Warnings

Use is not recommended and a decision should be made to discontinue breastfeeding or discontinue the drug, taking into account the importance of the drug to the mother. Excreted into human milk: Unknown Excreted into animal milk: Yes Comments: The effects in the nursing infant are unknown.

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