metoprolol succinate

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Overview

What is metoprolol succinate?

Metoprolol succinate is a beta-selective (cardioselective) adrenoceptor blocking agent, for oral administration, available as extended-release tablets. Metoprolol succinate extended-release tablets have been formulated to provide a controlled and predictable release of metoprolol for once daily oral administration. The tablets comprise a multiple unit system containing metoprolol succinate in a multitude of controlled-release pellets. Each pellet acts as a separate drug delivery unit and is designed to deliver metoprolol continuously over the dosage interval. The tablets contain 23.75 mg of metoprolol succinate equivalent 25 mg of metoprolol tartrate, USP. Its chemical name is (±) 1-(isopropylamino)-3-[p-(2-methoxyethyl) phenoxy]-2-propanol succinate (2:1) (salt). Its structural formula is:

Metoprolol succinate is a white crystalline powder with a molecular weight of 652.8. It is freely soluble in water; soluble in methanol; sparingly soluble in ethanol; slightly soluble in dichloromethane and 2-propanol; practically insoluble in ethyl-acetate, acetone, diethylether and heptane. Inactive ingredients: calcium stearate, carboxymethylcellulose sodium, carnauba wax, croscarmellose sodium, glyceryl behenate, hydrogenated vegetable oil, hypromellose, maltodextrin, methacrylic acid copolymer, microcrystalline cellulose, polydextrose, polyethylene glycol, povidone, sodium stearyl fumarate, titanium dioxide, triacetin, triethyl citrate, vinyl acetate copolymer.

The USP Drug Release Test is pending.

What does metoprolol succinate look like?

What are the available doses of metoprolol succinate?

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What should I talk to my health care provider before I take metoprolol succinate?

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How should I use metoprolol succinate?

Metoprolol succinate extended-release tablets are indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.

Metoprolol succinate extended-release tablets are intended for once daily administration. For treatment of hypertension and angina, when switching from immediate-release metoprolol to metoprolol succinate extended-release tablets, the same total daily dose of metoprolol succinate extended-release tablets should be used. Dosages of metoprolol succinate extended-release tablets should be individualized and titration may be needed in some patients.

Metoprolol succinate extended-release tablets are scored and can be divided; however, the whole or half tablet should be swallowed whole and not chewed or crushed.

What interacts with metoprolol succinate?

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What are the warnings of metoprolol succinate?

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What are the precautions of metoprolol succinate?

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What are the side effects of metoprolol succinate?

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What should I look out for while using metoprolol succinate?

Metoprolol succinate extended-release tablets are contraindicated in severe bradycardia, heart block greater than first degree, cardiogenic shock, decompensated cardiac failure, sick sinus syndrome (unless a permanent pacemaker is in place), and in patients who are hypersensitive to any component of this product.

What might happen if I take too much metoprolol succinate?

How should I store and handle metoprolol succinate?

Store bottles of 1000 SINGULAIR 5-mg chewable tablets and 8000 SINGULAIR 10-mg film-coated tablets at 25°C (77°F), excursions permitted to 15-30°C (59-86°F) [see USP Controlled Room Temperature]. Protect from moisture and light. Store in original container. When product container is subdivided, repackage into a well-closed, light resistant container. Metoprolol succinate extended-release tablets25 mg: NDC 58177-293-04………………….…Bottles of 100 NDC 58177-293-09………………….…Bottles of 1000 NDC 58177-293-12………………….…Bottles of 5000 NDC 58177-293-11………………….…Packages of 100 (10 x 10 cards) Store at 20°-25°C (68°-77°F). [See USP Controlled Room Temperature.] Manufactured byKV Pharmaceutical Co. for St. Louis, MO 63044 P5110-502/09 Metoprolol succinate extended-release tablets25 mg: NDC 58177-293-04………………….…Bottles of 100 NDC 58177-293-09………………….…Bottles of 1000 NDC 58177-293-12………………….…Bottles of 5000 NDC 58177-293-11………………….…Packages of 100 (10 x 10 cards) Store at 20°-25°C (68°-77°F). [See USP Controlled Room Temperature.] Manufactured byKV Pharmaceutical Co. for St. Louis, MO 63044 P5110-502/09 Metoprolol succinate extended-release tablets25 mg: NDC 58177-293-04………………….…Bottles of 100 NDC 58177-293-09………………….…Bottles of 1000 NDC 58177-293-12………………….…Bottles of 5000 NDC 58177-293-11………………….…Packages of 100 (10 x 10 cards) Store at 20°-25°C (68°-77°F). [See USP Controlled Room Temperature.] Manufactured byKV Pharmaceutical Co. for St. Louis, MO 63044 P5110-502/09 Metoprolol succinate extended-release tablets25 mg: NDC 58177-293-04………………….…Bottles of 100 NDC 58177-293-09………………….…Bottles of 1000 NDC 58177-293-12………………….…Bottles of 5000 NDC 58177-293-11………………….…Packages of 100 (10 x 10 cards) Store at 20°-25°C (68°-77°F). [See USP Controlled Room Temperature.] Manufactured byKV Pharmaceutical Co. for St. Louis, MO 63044 P5110-502/09 Metoprolol succinate extended-release tablets25 mg: NDC 58177-293-04………………….…Bottles of 100 NDC 58177-293-09………………….…Bottles of 1000 NDC 58177-293-12………………….…Bottles of 5000 NDC 58177-293-11………………….…Packages of 100 (10 x 10 cards) Store at 20°-25°C (68°-77°F). [See USP Controlled Room Temperature.] Manufactured byKV Pharmaceutical Co. for St. Louis, MO 63044 P5110-502/09 Metoprolol succinate extended-release tablets25 mg: NDC 58177-293-04………………….…Bottles of 100 NDC 58177-293-09………………….…Bottles of 1000 NDC 58177-293-12………………….…Bottles of 5000 NDC 58177-293-11………………….…Packages of 100 (10 x 10 cards) Store at 20°-25°C (68°-77°F). [See USP Controlled Room Temperature.] Manufactured byKV Pharmaceutical Co. for St. Louis, MO 63044 P5110-502/09 Metoprolol succinate extended-release tablets25 mg: NDC 58177-293-04………………….…Bottles of 100 NDC 58177-293-09………………….…Bottles of 1000 NDC 58177-293-12………………….…Bottles of 5000 NDC 58177-293-11………………….…Packages of 100 (10 x 10 cards) Store at 20°-25°C (68°-77°F). [See USP Controlled Room Temperature.] Manufactured byKV Pharmaceutical Co. for St. Louis, MO 63044 P5110-502/09 Metoprolol succinate extended-release tablets25 mg: NDC 58177-293-04………………….…Bottles of 100 NDC 58177-293-09………………….…Bottles of 1000 NDC 58177-293-12………………….…Bottles of 5000 NDC 58177-293-11………………….…Packages of 100 (10 x 10 cards) Store at 20°-25°C (68°-77°F). [See USP Controlled Room Temperature.] Manufactured byKV Pharmaceutical Co. for St. Louis, MO 63044 P5110-502/09 Metoprolol succinate extended-release tablets25 mg: NDC 58177-293-04………………….…Bottles of 100 NDC 58177-293-09………………….…Bottles of 1000 NDC 58177-293-12………………….…Bottles of 5000 NDC 58177-293-11………………….…Packages of 100 (10 x 10 cards) Store at 20°-25°C (68°-77°F). [See USP Controlled Room Temperature.] Manufactured byKV Pharmaceutical Co. for St. Louis, MO 63044 P5110-502/09

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Clinical Information

Chemical Structure

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Clinical Pharmacology

Metoprolol is a beta-selective (cardioselective) adrenergic receptor blocking agent. This preferential effect is not absolute, however, and at higher plasma concentrations, metoprolol also inhibits beta-adrenoreceptors, chiefly located in the bronchial and vascular musculature. Metoprolol has no intrinsic sympathomimetic activity, and membrane-stabilizing activity is detectable only at plasma concentrations much greater than required for beta-blockade. Animal and human experiments indicate that metoprolol slows the sinus rate and decreases AV nodal conduction.

Clinical pharmacology studies have confirmed the beta-blocking activity of metoprolol in man, as shown by (1) reduction in heart rate and cardiac output at rest and upon exercise, (2) reduction of systolic blood pressure upon exercise, (3) inhibition of isoproterenol-induced tachycardia, and (4) reduction of reflex orthostatic tachycardia.

The relative beta-selectivity of metoprolol has been confirmed by the following: (1) In normal subjects, metoprolol is unable to reverse the beta-mediated vasodilating effects of epinephrine. This contrasts with the effect of nonselective beta-blockers, which completely reverse the vasodilating effects of epinephrine. (2) In asthmatic patients, metoprolol reduces FEV and FVC significantly less than a nonselective beta-blocker, propranolol, at equivalent beta-receptor blocking doses.

In five controlled studies in normal healthy subjects, the same daily doses of metoprolol succinate extended-release tablets and immediate-release metoprolol were compared in terms of the extent and duration of beta -blockade produced. Both formulations were given in a dose range equivalent to 100 to 400 mg of immediate release metoprolol per day. In these studies, metoprolol succinate extended-release tablets were administered once a day and immediate-release metoprolol was administered once to four times a day. A sixth controlled study compared the beta- blocking effects of a 50 mg daily dose of the two formulations. In each study, beta-blockade was expressed as the percent change from baseline in exercise heart rate following standardized submaximal exercise tolerance tests at steady state. Metoprolol succinate extended-release tablets administered once a day, and immediate-release metoprolol administered once to four times a day, provided comparable total beta-blockade over 24 hours (area under the beta-blockade versus time curve) in the dose range 100 to 400 mg. At a dosage of 50 mg once daily, metoprolol succinate extended-release tablets produced significantly higher total beta-blockade over 24 hours than immediate-release metoprolol. For metoprolol succinate extended-release tablets, the percent reduction in exercise heart rate was relatively stable throughout the entire dosage interval and the level of beta-blockade increased with increasing doses from 50 to 300 mg daily. The effects at peak/trough (i.e., at 24 hours post-dosing) were 14/9, 16/10, 24/14, 27/22 and 27/20% reduction in exercise heart rate for doses of 50, 100, 200, 300 and 400 mg metoprolol succinate extended-release tablets once a day, respectively. In contrast to metoprolol succinate extended-release tablets, immediate-release metoprolol given at a dose of 50 to 100 mg once a day produced a significantly larger peak effect on exercise tachycardia, but the effect was not evident at 24 hours. To match the peak to trough ratio obtained with metoprolol succinate extended-release tablets over the dosing range of 200 to 400 mg, a t.i.d. to q.i.d. divided dosing regimen was required for immediate-release metoprolol. A controlled crossover study in heart failure patients compared the plasma concentrations and beta-blocking effects of 50 mg immediate-release metoprolol administered t.i.d., 100 mg and 200 mg metoprolol succinate extended-release tablets once daily. A 50 mg dose of immediate-release metoprolol t.i.d. produced a peak plasma level of metoprolol similar to the peak level observed with 200 mg of metoprolol succinate extended-release tablets. A 200 mg dose of metoprolol succinate extended-release tablets produced a larger effect on suppression of exercise-induced and Holter-monitored heart rate over 24 hours compared to 50 mg t.i.d. of immediate-release metoprolol.

The relationship between plasma metoprolol levels and reduction in exercise heart rate is independent of the pharmaceutical formulation. Using an E model, the maximum effect is a 30% reduction in exercise heart rate, which is attributed to beta-blockade. Beta-blocking effects in the range of 30 to 80% of the maximal effect (approximately 8 to 23% reduction in exercise heart rate) corresponds to metoprolol plasma concentrations from 30 to 540 nmol/L. The relative beta-selectivity of metoprolol diminishes and blockade of beta-adrenoceptors increases at plasma concentrations above 300 nmol/L.

Although beta-adrenergic receptor blockade is useful in the treatment of angina, hypertension, and heart failure there are situations in which sympathetic stimulation is vital. In patients with severely damaged hearts, adequate ventricular function may depend on sympathetic drive. In the presence of AV block, beta-blockade may prevent the necessary facilitating effect of sympathetic activity on conduction. Beta-adrenergic blockade results in passive bronchial constriction by interfering with endogenous adrenergic bronchodilator activity in patients subject to bronchospasm and may also interfere with exogenous bronchodilators in such patients.

In other studies, treatment with metoprolol succinate extended-release tablets produced an improvement in left ventricular ejection fraction. Metoprolol succinate extended-release tablets were also shown to delay the increase in left ventricular end-systolic and end-diastolic volumes after 6 months of treatment.

Non-Clinical Toxicology

Metoprolol succinate extended-release tablets are contraindicated in severe bradycardia, heart block greater than first degree, cardiogenic shock, decompensated cardiac failure, sick sinus syndrome (unless a permanent pacemaker is in place), and in patients who are hypersensitive to any component of this product.

Catecholamine-depleting drugs (e.g., reserpine, monoamine oxidase (MAO) inhibitors) may have an additive effect when given with beta-blocking agents. Patients treated with metoprolol succinate extended-release tablets plus a catecholamine depletor should therefore be closely observed for evidence of hypotension or marked bradycardia, which may produce vertigo, syncope, or postural hypotension.

Drugs that inhibit CYP2D6 such as quinidine, fluoxetine, paroxetine, and propafenone are likely to increase metoprolol concentration. In healthy subjects with CYP2D6 extensive metabolizer phenotype, coadministration of quinidine 100 mg and immediate release metoprolol 200 mg tripled the concentration of S-metoprolol and doubled the metoprolol elimination half-life. In four patients with cardiovascular disease, coadministration of propafenone 150 mg t.i.d. with immediate-release metoprolol 50 mg t.i.d. resulted in two- to five-fold increases in the steady-state concentration of metoprolol. These increases in plasma concentration would decrease the cardioselectivity of metoprolol.

Both digitalis glycosides and beta-blockers slow atrioventricular conduction and decrease heart rate. Concomitant use can increase the risk of bradycardia.

Beta-blockers may exacerbate the rebound hypertension which can follow the withdrawal of clonidine. If the two drugs are coadministered, the beta blocker should be withdrawn several days before the gradual withdrawal of clonidine. If replacing clonidine by beta-blocker therapy, the introduction of beta-blockers should be delayed for several days after clonidine administration has stopped.

Metoprolol succinate extended-release tablets should be used with caution in patients with impaired hepatic function. In patients with pheochromocytoma, an alpha-blocking agent should be initiated prior to the use of any beta-blocking agent (see ).

Worsening cardiac failure may occur during up-titration of metoprolol succinate extended-release tablets. If such symptoms occur, diuretics should be increased and the dose of metoprolol succinate extended-release tablets should not be advanced until clinical stability is restored (see ). It may be necessary to lower the dose of metoprolol succinate extended-release tablets or temporarily discontinue it. Such episodes do not preclude subsequent successful titration of metoprolol succinate extended-release tablets.

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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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Professional

Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72

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Interactions

A total of 440 drugs (1549 brand and generic names) are known to interact with Imbruvica (ibrutinib). 228 major drug interactions (854 brand and generic names) 210 moderate drug interactions (691 brand and generic names) 2 minor drug interactions (4 brand and generic names) Show all medications in the database that may interact with Imbruvica (ibrutinib).

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