Edarbyclor (azilsartan medoxomil/chlorthalidone)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Azilsartan medoxomil is an angiotensin II type 1 (AT1) receptor antagonist (also referred to as an angiotensin II receptor blocker (ARB)). The drug is commercially available as the potassium salt, azilsartan kamedoxomil.
Chlorthalidone, which is structurally and pharmacologically similar to the thiazides, is a diuretic and antihypertensive agent.
Azilsartan medoxomil is an angiotensin II type 1 (AT1) receptor antagonist. Through selective blockade of angiotensin II binding at the AT1 receptor in many tissues such as vascular smooth muscle and the adrenal gland, azilsartan blocks the physiologic actions of angiotensin II, including vasoconstrictor and aldosterone-secreting effects. Azilsartan has more than a 10,000-fold greater affinity for the AT1 receptor than for the AT2 receptor.
Azilsartan does not inhibit angiotensin-converting enzyme (ACE), the enzyme involved in the conversion of angiotensin I to angiotensin II and degradation of bradykinin. Azilsartan does not bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation. Increased plasma renin activity and angiotensin II circulating levels due to angiotensin receptor blockade do not overcome the effect of azilsartan on blood pressure.
Azilsartan medoxomil is a prodrug that is hydrolyzed to azilsartan in the GI tract during absorption. The absolute bioavailability of azilsartan is approximately 60%. Increases in azilsartan exposure are dose proportional following single or multiple doses of azilsartan medoxomil in the range of 20-320 mg.
Peak plasma azilsartan concentrations are reached in 1.5-3 hours after oral administration. Steady-state plasma concentrations are achieved within 5 days, and most of the antihypertensive effect of azilsartan is observed within 2 weeks. Food does not affect the bioavailability of azilsartan.
Azilsartan is highly bound (>99%) to human plasma proteins, primarily albumin. Azilsartan crossed the placental barrier in animal studies. Azilsartan is metabolized principally by cytochrome P-450 (CYP) 2C9 to 2 primary metabolites, which are pharmacologically inactive; metabolite M-II (the major metabolite) is formed by O-dealkylation, and metabolite M-I (the minor metabolite) is formed by decarboxylation.
Systemic exposures to M-II and M-I are approximately 50% and <1%, respectively, that of azilsartan.
Approximately 55% of an administered dose of azilsartan medoxomil is recovered in feces, and 42% is recovered in urine (15% as azilsartan). The elimination half-life of azilsartan is approximately 11 hours.
USES: This medication is used to treat high blood pressure. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. This product contains 2 medications, azilsartan and chlorthalidone.
Azilsartan belongs to a class of drugs known as angiotensin receptor blockers (ARBs). It works by relaxing blood vessels so blood can flow more easily. Chlorthalidone is a "water pill" (diuretic) that causes you to make more urine.
This helps your body get rid of extra water and salt.
Generic name: azilsartan medoxomil/chlorthalidone
Pronunciation: (AY-zil-SAR-tan/klor-THAL-i-done)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Edarbyclor
Indications
The following indications are listed for Edarbyclor:
- Hypertension
Also known as: Elevated Blood Pressure, Essential Hypertension, Hyperpiesia, Hyperpiesis, Hypertensive Disorder, Systemic Arterial Hypertension.
Dosing
Azilsartan medoxomil is commercially available as azilsartan kamedoxomil (the potassium salt of azilsartan medoxomil); dosage is expressed in terms of azilsartan medoxomil.
Dosage of chlorthalidone should be individualized according to the patient's requirements and response. If chlorthalidone is added to the regimen of a patient stabilized on a potent hypotensive agent, the dosage of the hypotensive agent should initially be reduced to avoid the possibility of severe hypotension.
Azilsartan kamedoxomil is administered orally without regard to meals. It is available as 40 mg or 80 mg oral tablets.
Azilsartan is also commercially available in fixed-combination tablets containing azilsartan kamedoxomil and chlorthalidone; see the full prescribing information for administration of this combination product.
Azilsartan tablets must be dispensed and stored in the original manufacturer's container. Do not repackage. Tablets should be stored at 25degreesC (excursions permitted between 15-30degreesC) and protected from light and moisture.
Chlorthalidone is administered orally.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Azilsartan is primarily metabolized by cytochrome P-450 (CYP) 2C9.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Concomitant use of azilsartan and aliskiren-containing products in patients with diabetes mellitus.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse reaction in adults was diarrhea (2%).
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and effectiveness of azilsartan in pediatric patients have not been established. Use of azilsartan is not recommended in children younger than 2 years of age; it is not known whether azilsartan use in such patients, before kidney function has fully matured, causes long-term harm to the kidneys.
Azilsartan can cause fetal harm when administered to a pregnant woman. Use of drugs that act on the RAS during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death. Oligohydramnios caused by drugs that act on the RAS can result in reduced fetal renal function leading to anuria and renal failure, fetal lung hypoplasia, skeletal deformations including skull hypoplasia, hypotension, and death. Discontinue azilsartan as soon as possible when pregnancy is detected.
Perform serial ultrasound examinations to assess the intra-amniotic environment. Fetal testing may be appropriate, based on the week of pregnancy. Patients and physicians should be aware that oligohydramnios may not appear until after the fetus has sustained irreversible injury.
Hypertension in pregnancy increases maternal risk for pre-eclampsia, gestational diabetes, premature delivery, and delivery complications (e.g., need for cesarean section, and post-partum hemorrhage). Hypertension increases the fetal risk for intrauterine growth restriction and death. Pregnant women with hypertension should be carefully monitored and managed accordingly.
Closely observe infants with a history of in utero exposure to azilsartan for hypotension, oliguria, and hyperkalemia. Support blood pressure and renal perfusion if oliguria or hypotension occurs. Exchange transfusions or dialysis may be required to reverse hypotension and/or substitute for disordered renal function.
Azilsartan is distributed into milk in rats; it is not known whether azilsartan is distributed into human milk, its effects on the breast-fed infant, or the effects on milk production. Because of the potential for adverse reactions to azilsartan in nursing infants, breast-feeding is not recommended during treatment with azilsartan.
No dosage adjustment is necessary in geriatric patients.
In clinical studies of azilsartan, 26% of patients were 65 years of age and older, and 5% were 75 years of age and older. Abnormally high serum creatinine values were more likely among patients 75 years of age or older. There were no other differences in safety or effectiveness between elderly and younger patients; however, greater sensitivity of some geriatric patients cannot be ruled out.
ICD codes
No ICD codes are available for this drug.
Formulary status
Search health-plan coverage for this drug by ZIP code.
Choose the first character of a health plan name.
Last reviewed · Source: First Databank (FDB) drug data
On this page
Actions
Sign in to save favorites
Saving this drug requires a free Physicians Office Resource account.