TEVETEN- eprosartan mesylate tablet
Abbott Laboratories
Rx Only
PRESCRIBING INFORMATION
WARNING: FETAL TOXICITY
See full prescribing information for complete boxed warning.
When pregnancy is detected, discontinue TEVETEN as soon as possible.
Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus. See WARNINGS: Fetal Toxicity
DESCRIPTION
TEVETEN� (eprosartan mesylate) is a non-biphenyl non-tetrazole angiotensin II receptor (AT1 ) antagonist. A selective non-peptide molecule, TEVETEN� is chemically described as the monomethanesulfonate of (E )-2-butyl-1-(p -carboxybenzyl)-?-2-thienylmethylimid-azole-5-acrylic acid.
Its empirical formula is C23 H24 N2 O4 S�CH4 O3 S and molecular weight is 520.625.
Eprosartan mesylate is a white to off-white free-flowing crystalline powder that is insoluble in water, freely soluble in ethanol, and melts between 248�C and 250�C.
TEVETEN� is available as aqueous film-coated tablets containing eprosartan mesylate equivalent to 400 mg or 600 mg eprosartan zwitterion (pink, oval, non-scored tablets or white, non-scored, capsule-shaped tablets, respectively).
Inactive Ingredients
The 400 mg tablet contains the following: croscarmellose sodium, hypromellose, iron oxide red, iron oxide yellow, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, pregelatinized starch, and titanium dioxide. The 600 mg tablet contains crospovidone, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, pregelatinized starch, and titanium dioxide.
CLINICAL PHARMACOLOGY
Mechanism of Action
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 AT1 receptor found in many tissues (e.g., vascular smooth muscle, adrenal gland). There is also an AT2 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 AT1 receptor. Its affinity for the AT1 receptor is 1,000 times greater than for the AT2 receptor. In vitro binding studies indicate that eprosartan is a reversible, competitive inhibitor of the AT1 receptor.
INDICATIONS AND USAGE
TEVETEN� is indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensives such as diuretics and calcium channel blockers.
CONTRAINDICATIONS
TEVETEN� is contraindicated in patients who are hypersensitive to this product or any of its components.
Do not co-administer aliskiren with TEVETEN in patients with diabetes.
DOSAGE AND ADMINISTRATION
The usual recommended starting dose of TEVETEN� is 600 mg once daily when used as monotherapy in patients who are not volume-depleted (see WARNINGS, Hypotension in Volume- and/or Salt-Depleted Patients). TEVETEN� 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.
TEVETEN� 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
No initial dosing adjustment is generally necessary for elderly or hepatically impaired patients or those with renal impairment. No initial dosing adjustment is generally necessary in patients with moderate and severe renal impairment, with maximum dose not exceeding 600 mg daily.
TEVETEN� may be taken with or without food.