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eprosartan mesylate
Overview
What is Eprosartan Mesylate?
Eprosartan mesylate is a non-biphenyl non-tetrazole angiotensin II receptor (AT) antagonist. A selective non-peptide molecule, eprosartan mesylate is chemically described as (E)-[2-Butyl]-1-[(4-carboxyphenyl)-methyl]imidazol-5yl]-2-(2-thienylmethyl)-2-propenoic acid monomethane sulfonate.
Its molecular formula is CHNOS and molecular weight is 520.62. Its structural formula is:
Eprosartan mesylate is a white to off-white crystalline powder that is insoluble in water, freely soluble in ethanol, and melts between 248°C and 250°C.
Eprosartan mesylate tablets are available as film-coated tablets containing eprosartan mesylate equivalent to 600 mg eprosartan zwitterion (white to off-white capsule shaped, unscored tablets).
What does Eprosartan Mesylate look like?
What are the available doses of Eprosartan Mesylate?
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What should I talk to my health care provider before I take Eprosartan Mesylate?
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How should I use Eprosartan Mesylate?
Eprosartan mesylate tablets are indicated for the treatment of hypertension. They may be used alone or in combination with other antihypertensives such as diuretics and calcium channel blockers.
The usual recommended starting dose of eprosartan mesylate tablets is 600 mg once daily when used as monotherapy in patients who are not volume-depleted (see ). Eprosartan mesylate tablets can be administered once or twice daily with total daily doses ranging from 400 mg to 800 mg. There is limited experience with doses beyond 800 mg/day.
If the antihypertensive effect measured at trough using once-daily dosing is inadequate, a twice-a-day regimen at the same total daily dose or an increase in dose may give a more satisfactory response. Achievement of maximum blood pressure reduction in most patients may take 2 to 3 weeks.
Eprosartan mesylate tablets may be used in combination with other antihypertensive agents such as thiazide diuretics or calcium channel blockers if additional blood-pressure-lowering effect is required. Discontinuation of treatment with eprosartan does not lead to a rapid rebound increase in blood pressure.
Elderly, Hepatically Impaired or Renally Impaired Patients:
Eprosartan mesylate tablets may be taken with or without food.
What interacts with Eprosartan Mesylate?
Eprosartan mesylate tablets are contraindicated in patients who are hypersensitive to this product or any of its components.
Do not co-administer aliskiren with eprosartan in patients with diabetes (see ).
What are the warnings of Eprosartan Mesylate?
Fetal Toxicity
Hypotension in Volume- and/or Salt-depleted Patients
In patients with an activated renin-angiotensin system, such as volume- and/or salt-depleted patients (e.g., those being treated with diuretics), symptomatic hypotension may occur. These conditions should be corrected prior to administration of eprosartan, or the treatment should start under close medical supervision. If hypotension occurs, the patient should be placed in the supine position and, if necessary, given an intravenous infusion of normal saline. A transient hypotensive response is not a contraindication to further treatment, which usually can be continued without difficulty once the blood pressure has stabilized.
What are the precautions of Eprosartan Mesylate?
Risk of Renal Impairment
As a consequence of inhibiting the renin-angiotensin-aldosterone system, changes in renal function have been reported in susceptible individuals treated with angiotensin II antagonists; in some patients, these changes in renal function were reversible upon discontinuation of therapy. In patients whose renal function may depend on the activity of the renin-angiotensin-aldosterone system (e.g., patients with severe congestive heart failure), treatment with angiotensin-converting enzyme inhibitors and angiotensin II receptor antagonists has been associated with oliguria and/or progressive azotemia and (rarely) with acute renal failure and/or death. Eprosartan mesylate would be expected to behave similarly.
In studies of ACE inhibitors in patients with unilateral or bilateral renal artery stenosis, increases in serum creatinine or BUN have been reported. Similar effects have been reported with angiotensin II antagonists; in some patients, these effects were reversible upon discontinuation of therapy.
Information for Patients
Female patients of childbearing age should be told about the consequences of exposure to eprosartan mesylate during pregnancy. Discuss treatment options with women planning to become pregnant. Patients should be asked to report pregnancies to their physicians as soon as possible.
Drug Interactions
Dual blockade of the RAS with angiotensin receptor blockers, ACE inhibitors, or aliskiren is associated with increased risks of hypotension, hyperkalemia, and changes in renal function (including acute renal failure) compared to monotherapy. Most patients receiving the combination of two RAS inhibitors do not obtain any additional benefit compared to monotherapy. In general, avoid combined use of RAS inhibitors. Closely monitor blood pressure, renal function and electrolytes in patients on eprosartan and other agents that affect the RAS.
Do not co-administer aliskiren with eprosartan in patients with diabetes. Avoid use of aliskiren with eprosartan in patients with renal impairment (GFR < 60 mL/min).
Eprosartan has been shown to have no effect on the pharmacokinetics of digoxin and the pharmacodynamics of warfarin and glyburide. Thus, no dosing adjustments are necessary during concomitant use with these agents. Because eprosartan is not metabolized by the cytochrome P450 system, inhibitors of CYP450 enzyme would not be expected to affect its metabolism, and ketoconazole and fluconazole, potent inhibitors of CYP3A and 2C9, respectively, have been shown to have no effect on eprosartan pharmacokinetics. Ranitidine also has no effect on eprosartan pharmacokinetics.
Eprosartan (up to 400 mg b.i.d. or 800 mg q.d.) doses have been safely used concomitantly with a thiazide diuretic (hydrochlorothiazide). Eprosartan doses of up to 300 mg b.i.d. have been safely used concomitantly with sustained-release calcium channel blockers (sustained-release nifedipine) with no clinically significant adverse interactions.
Non-steroidal Anti-inflammatory Agents Including Selective Cyclooxygenase-2 Inhibitors (COX-2) Inhibitors
In patients who are elderly, volume-depleted (including those on diuretic therapy), or with compromised renal function, co-administration of NSAIDs, including selective COX-2 inhibitors, with angiotensin II receptor antagonists, including eprosartan, may result in deterioration of renal function, including possible acute renal failure. These effects are usually reversible. Monitor renal function periodically in patients receiving eprosartan and NSAID therapy.
The antihypertensive effect of angiotensin II receptor antagonists, including eprosartan may be attenuated by NSAIDs including selective COX-2 inhibitors.
Lithium
Increases in serum lithium concentrations and lithium toxicity have been reported during concomitant administration of lithium with angiotensin II receptor agonists. Monitor serum lithium levels during concomitant use.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Eprosartan mesylate was not carcinogenic in dietary restricted rats or fed mice dosed at 600 mg and 2000 mg eprosartan/kg/day, respectively, for up to 2 years. In male and female rats, the systemic exposure (AUC) to unbound eprosartan at the dose evaluated was only approximately 20% of the exposure achieved in humans given 400 mg b.i.d. In mice, the systemic exposure (AUC) to unbound eprosartan was approximately 25 times the exposure achieved in humans given 400 mg b.i.d.
Eprosartan mesylate was not mutagenic in bacteria or mammalian cells (mouse lymphoma assay). Eprosartan mesylate also did not cause structural chromosomal damage (mouse micronucleus assay). In human peripheral lymphocytes , eprosartan mesylate was equivocal for clastogenicity with metabolic activation, and was negative without metabolic activation. In the same assay, eprosartan mesylate was positive for polyploidy with metabolic activation and equivocal for polyploidy without metabolic activation.
Eprosartan mesylate had no adverse effects on the reproductive performance of male or female rats at oral doses up to 1000 mg eprosartan/kg/day. This dose provided systemic exposure (AUC) to unbound eprosartan approximately 0.6 times the exposure achieved in humans given 400 mg b.i.d.
Nursing Mothers
Eprosartan is excreted in animal milk; it is not known whether eprosartan is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from eprosartan, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric Use
If oliguria or hypotension occurs, direct attention toward support of blood pressure and renal perfusion. Exchange transfusions or dialysis may be required as a means of reversing hypotension and/or substituting for disordered renal function.
Safety and effectiveness in pediatric patients have not been established.
Geriatric Use
Of the total number of patients receiving eprosartan mesylate in clinical studies, 29% (681 of 2,334) were 65 years and over, while 5% (124 of 2,334) were 75 years and over. Based on the pooled data from randomized trials, the decrease in diastolic blood pressure and systolic blood pressure with eprosartan mesylate was slightly less in patients ≥ 65 years of age compared to younger patients. In a study of only patients over the age of 65, eprosartan at 200 mg twice daily (and increased optionally up to 300 mg twice daily) decreased diastolic blood pressure on average by 3 mmHg (placebo corrected). Adverse experiences were similar in younger and older patients.
What are the side effects of Eprosartan Mesylate?
Sorry No records found
What should I look out for while using Eprosartan Mesylate?
Eprosartan mesylate tablets are contraindicated in patients who are hypersensitive to this product or any of its components.
Do not co-administer aliskiren with eprosartan in patients with diabetes (see ).
What might happen if I take too much Eprosartan Mesylate?
Limited data are available regarding overdosage. Appropriate symptomatic and supportive therapy should be given if overdosage should occur. There was no mortality in rats and mice receiving oral doses of up to 3000 mg eprosartan/kg and in dogs receiving oral doses of up to 1000 mg eprosartan/kg.
How should I store and handle Eprosartan Mesylate?
Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature]. Keep tightly closed (protect from moisture). Protect from light.Eprosartan Mesylate Tablets are available containing eprosartan mesylate equivalent to 600 mg of eprosartan.The 600 mg tablets are white to off-white film-coated, capsule shaped, unscored tablets imprinted with in black ink on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-6629-93bottles of 30 tabletsStore at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Manufactured for: Morgantown, WV 26505 U.S.A.Manufactured in India by: Hyderabad — 500 034, IndiaCode No.: MH/DRUGS/25/NKD/8975055504REVISED NOVEMBER 2014MX:EPRS:R4Eprosartan Mesylate Tablets are available containing eprosartan mesylate equivalent to 600 mg of eprosartan.The 600 mg tablets are white to off-white film-coated, capsule shaped, unscored tablets imprinted with in black ink on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-6629-93bottles of 30 tabletsStore at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Manufactured for: Morgantown, WV 26505 U.S.A.Manufactured in India by: Hyderabad — 500 034, IndiaCode No.: MH/DRUGS/25/NKD/8975055504REVISED NOVEMBER 2014MX:EPRS:R4Eprosartan Mesylate Tablets are available containing eprosartan mesylate equivalent to 600 mg of eprosartan.The 600 mg tablets are white to off-white film-coated, capsule shaped, unscored tablets imprinted with in black ink on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-6629-93bottles of 30 tabletsStore at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Manufactured for: Morgantown, WV 26505 U.S.A.Manufactured in India by: Hyderabad — 500 034, IndiaCode No.: MH/DRUGS/25/NKD/8975055504REVISED NOVEMBER 2014MX:EPRS:R4Eprosartan Mesylate Tablets are available containing eprosartan mesylate equivalent to 600 mg of eprosartan.The 600 mg tablets are white to off-white film-coated, capsule shaped, unscored tablets imprinted with in black ink on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-6629-93bottles of 30 tabletsStore at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Manufactured for: Morgantown, WV 26505 U.S.A.Manufactured in India by: Hyderabad — 500 034, IndiaCode No.: MH/DRUGS/25/NKD/8975055504REVISED NOVEMBER 2014MX:EPRS:R4Eprosartan Mesylate Tablets are available containing eprosartan mesylate equivalent to 600 mg of eprosartan.The 600 mg tablets are white to off-white film-coated, capsule shaped, unscored tablets imprinted with in black ink on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-6629-93bottles of 30 tabletsStore at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Manufactured for: Morgantown, WV 26505 U.S.A.Manufactured in India by: Hyderabad — 500 034, IndiaCode No.: MH/DRUGS/25/NKD/8975055504REVISED NOVEMBER 2014MX:EPRS:R4Eprosartan Mesylate Tablets are available containing eprosartan mesylate equivalent to 600 mg of eprosartan.The 600 mg tablets are white to off-white film-coated, capsule shaped, unscored tablets imprinted with in black ink on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-6629-93bottles of 30 tabletsStore at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Manufactured for: Morgantown, WV 26505 U.S.A.Manufactured in India by: Hyderabad — 500 034, IndiaCode No.: MH/DRUGS/25/NKD/8975055504REVISED NOVEMBER 2014MX:EPRS:R4Eprosartan Mesylate Tablets are available containing eprosartan mesylate equivalent to 600 mg of eprosartan.The 600 mg tablets are white to off-white film-coated, capsule shaped, unscored tablets imprinted with in black ink on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-6629-93bottles of 30 tabletsStore at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Manufactured for: Morgantown, WV 26505 U.S.A.Manufactured in India by: Hyderabad — 500 034, IndiaCode No.: MH/DRUGS/25/NKD/8975055504REVISED NOVEMBER 2014MX:EPRS:R4Eprosartan Mesylate Tablets are available containing eprosartan mesylate equivalent to 600 mg of eprosartan.The 600 mg tablets are white to off-white film-coated, capsule shaped, unscored tablets imprinted with in black ink on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-6629-93bottles of 30 tabletsStore at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Manufactured for: Morgantown, WV 26505 U.S.A.Manufactured in India by: Hyderabad — 500 034, IndiaCode No.: MH/DRUGS/25/NKD/8975055504REVISED NOVEMBER 2014MX:EPRS:R4Eprosartan Mesylate Tablets are available containing eprosartan mesylate equivalent to 600 mg of eprosartan.The 600 mg tablets are white to off-white film-coated, capsule shaped, unscored tablets imprinted with in black ink on one side of the tablet and blank on the other side. They are available as follows:NDC 0378-6629-93bottles of 30 tabletsStore at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.Manufactured for: Morgantown, WV 26505 U.S.A.Manufactured in India by: Hyderabad — 500 034, IndiaCode No.: MH/DRUGS/25/NKD/8975055504REVISED NOVEMBER 2014MX:EPRS:R4
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Angiotensin II (formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme [kininase II]), a potent vasoconstrictor, is the principal pressor agent of the renin-angiotensin system. Angiotensin II also stimulates aldosterone synthesis and secretion by the adrenal cortex, cardiac contraction, renal resorption of sodium, activity of the sympathetic nervous system, and smooth muscle cell growth. Eprosartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT receptor found in many tissues (e.g., vascular smooth muscle, adrenal gland). There is also an AT receptor found in many tissues but it is not known to be associated with cardiovascular homeostasis. Eprosartan does not exhibit any partial agonist activity at the AT receptor. Its affinity for the AT receptor is 1,000 times greater than for the AT receptor. binding studies indicate that eprosartan is a reversible, competitive inhibitor of the AT1 receptor.
Blockade of the AT receptor removes the negative feedback of angiotensin II on renin secretion, but the resulting increased plasma renin activity and circulating angiotensin II do not overcome the effect of eprosartan on blood pressure.
Eprosartan does not inhibit kininase II, the enzyme that converts angiotensin I to angiotensin II and degrades bradykinin; whether this has clinical relevance is not known. It does not bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.
Non-Clinical Toxicology
Eprosartan mesylate tablets are contraindicated in patients who are hypersensitive to this product or any of its components.Do not co-administer aliskiren with eprosartan in patients with diabetes (see ).
As a consequence of inhibiting the renin-angiotensin-aldosterone system, changes in renal function have been reported in susceptible individuals treated with angiotensin II antagonists; in some patients, these changes in renal function were reversible upon discontinuation of therapy. In patients whose renal function may depend on the activity of the renin-angiotensin-aldosterone system (e.g., patients with severe congestive heart failure), treatment with angiotensin-converting enzyme inhibitors and angiotensin II receptor antagonists has been associated with oliguria and/or progressive azotemia and (rarely) with acute renal failure and/or death. Eprosartan mesylate would be expected to behave similarly.
In studies of ACE inhibitors in patients with unilateral or bilateral renal artery stenosis, increases in serum creatinine or BUN have been reported. Similar effects have been reported with angiotensin II antagonists; in some patients, these effects were reversible upon discontinuation of therapy.
Eprosartan mesylate has been evaluated for safety in more than 3,300 healthy volunteers and patients worldwide, including more than 1,460 patients treated for more than 6 months, and more than 980 patients treated for one year or longer. Eprosartan was well tolerated at doses up to 1200 mg daily. Most adverse events were of mild or moderate severity and did not require discontinuation of therapy. The overall incidence of adverse experiences and the incidences of specific adverse events reported with eprosartan were similar to placebo.
Adverse experiences were similar in patients regardless of age, gender, or race. Adverse experiences were not dose-related.
In placebo-controlled clinical trials, about 4% of 1,202 patients treated with eprosartan mesylate discontinued therapy due to clinical adverse experiences, compared to 6.5% of 352 patients given placebo.
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
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