Metoprolol, release

Hydroserpine 2 Tablets—hydrochbrothiazide, reserpine Hyzaar—hydrochlorothiazide, losartan potassium Inderide—hydrochlorotliiazide, propranolol HC1 Inderide LA—hydrochlorotliiazide, propranolol HC1 Lexxel Extended-Release—enalapril maleate, felodipine Lopressor—hydrochlorothiazide, metoprolol Lotensin HCT—hydrochlorothiazide, benazepril Lotrel—amlodopine, benazepril... 

Metoprolol P,-Selective No 50-1 00 mg twice daily (once daily for extended-release)... 

GS Rekhi, ND Eddington, MJ Fossler, P Schwartz, LJ Lesko, LL Augsburger. Evaluation of in vitro release rate and in vivo absorption characteristics of four metoprolol tartrate immediate release tablet formulations. Pharm Devel Tech 2(1) 11-24, 1997. 

The jejunal perfusion approach generates data which may be used to predict absorption/bioavailability and to establish in vivo-in vitro correlation (IVIVC) even for extended release (ER) products. If a dmg is transported mainly by passive diffusion and has a jejunal Peff higher than metoprolol (1.5 x 10-4 cm s 1 = high-permeability compound), it can be expected to be completely absorbed throughout the small and large intestine [5, 46]. 

Metoprolol CR/XL, carvedilol, and bisoprolol are the only /J-blockers shown to reduce mortality in large HF trials. It cannot be assumed that immediate-release metoprolol will provide benefits equivalent to metoprolol CR/XL. Because bisoprolol is not available in the necessary starting dose of 1.25 mg, the choice is typically limited to either carvedilol or metoprolol CR/XL. On the basis of regimens proven in large clinical trials to reduce mortality, initial and target oral doses are as follows ... 

Both products have metoprolol as active ingredient. ZOC is a slow release formulation. 

For highly potent APIs, profound effects can occur at low ng levels, the adverse effect of ethynylestradiol on fish populations is one example [107]. Another example is the development of resistant bacterial strains induced by the release of antibiotics into the environment [112, 113]. Dome et al. [114] concluded that fluoxetine, ibuprofen, diclofenac, propranolol and metoprolol exhibit relatively high acute toxicity to aquatic species. In addition, due to the inherent properties of these chemicals, pharmacodynamic effects were observed in the heart rate of Daphnia magna for the (3-blockers propranolol and metoprolol. 

Tablets, extended release - The extended-release tablets are for once daily administration. When switching from immediate-release metoprolol tablets to extended-release, use the same daily dose.

Teksin, Z.S., Horn, K., Balakrishnan, A. and Polli, J.E. (2006) Ion pair-mediated transport of metoprolol across a three lipid-component PAM PA system. Journal of Controlled Release, 116, 50-57. 

Hjalmarson A, Goldstein S, Fagerberg B, Wedel H, Waag-stein F, Kjekshus J et al. Effects of controlled-release metoprolol on total mortality, hospitalizations, and well-being in patients with heart failure the Metoprolol CR/XL Randomized Intervention Trial in congestive heart failure (MERIT-HF). MERIT-HF Study Group. JAMA 2000 283(10) 1295-302. 

Most of the drugs in this class are well absorbed after oral administration peak concentrations occur 1-3 hours after ingestion. Sustained-release preparations of propranolol and metoprolol are available. 

Adverse effects The adverse events associated with (3 blockers may be avoided by starting treatment at very low doses. However, treatment can be associated with complaints of fatigue and weakness, which usually resolve in a few weeks, Sometimes it is necessary to decrease the dose of the (3 blocker or diuretic. Symptomatic bradycardia is another serious adverse effect of (3 blockers, and requires a decrease in the dose or sometimes cardiac pacing to allow the use of this vital medication, Hypotension is another potential side effect however, it is rarely seen as the therapy is started with a very low dose (3,25 mg twice a day for carvedilol, I mg for bisoprolol and 12,5 mg for extended release metoprolol). The administration of ACE inhibitor and diuretic at a different time of day than the (3 blocker can... 

Abbreviations-. BEST, beta-blocker evaluation survival trial CAPRICORN, caiveclilol postinfarct suivival control in left ventricular dysfunction C1B1S II, Cardiac Insufficiency Bisoprolol Study II COMET, Carvedilol or Metoprolol European Trial COPERNICUS, carvedilol prospective randomized cumulative survival HF, heart failure LVEF, left ventricular ejection fraction MDC, metoprolol in dilated cardiomyopathy MERIT-HF, metoprolol controlled-release randomized intervention trial in congestive heart failure fJYHA, New York Heart Association. 

Goldstein S, Fagerberg B, Hjalmarson A, et al. Metoprolol controlled release/extended release in patients with severe heart failure analysis of the experience in the MERIT-HF study, J Am Coll Cardiol 2001 38 932-938. 

A comparison of Equations (6)-(8) shows important similarities they depend on the solubility of the drug, the area of the device, and the thickness of the membrane. This means that an increased solubility, larger area of the membrane, and thinner membranes will facilitate the drug release rate. This can be exemplified by a study by Ragnarsson and Johansson [11], who showed that, for different salt forms of metoprolol, an increased solubility also increased the drug release rate, which was predicted from the equations. Furthermore, Equations (6)-(8) show constant and time-independent release rates. This constant amount of released drug will be a biopharmaceutical benefit since it theoretically makes it possible to achieve a constant concentration of the drug in the blood plasma. 

Nellore, R. V., Rekhi, G. S., Hussain, A. S., Tillman, L. G., and Augsburger, L. L. (1998), Development of metoprolol tartrate extended-release matrix tablet formulations for regulatory policy consideration, J. Controlled Release, 50,247-256. 

Very limited drug absorption due to the lack of microvilli and the more viscous and semisolid nature of the lumen contents. A few drugs such as theophylline and metoprolol are absorbed in this region. Drugs that are absorbed well in this region are good candidates for an oral sustained-release dosage form... 

Eddington, N.D. Marroum, P. Uppoor, R. Hussain, A. Augsburger, L. Development and internal validation of an in vitro-in vivo correlation for a hydrophilic metoprolol tartrate extended release tablet formulation. Pharm. Res. 1998, 5, 466-473. 

A modified-release formulation of metoprolol has been associated with more skin reactions, probably due to the succinate component, instead of the tartrate component used in the old fast-acting formulation (SEDA-16, 195). 

Felton LA, McGinity JW. Influence of plasticisers on the adhesive properties of an acrylic resin copolymer to hydrophilic and hydrophobic tablet compacts. Int J Pharm 1997 154(2) 167—178. Okarter TU, Singla K. The effects of plasticisers on the release of metoprolol tartrate from granules coated with a polymethacrylate film. Drug Dev Ind Pharm 2000 26(3) 323—329. 

The use of a fast hydrating grade of HPMC (HPMC 2208) has been reported to have successfully provided 12-hour extended release to metoprolol tartrate tablets when used as a hydrophilic matrix. The three processes of direct compression, high-shear granulation, and fluid bed granulation were compared and in the latter two processes another grade of HPMC, Methocel E5, was also selected as the binder of choice. It was found that... 

Rekhi G, Nellore RV, Hussain AS, Tillman LG, Malinowski HI, Augsburger LL. Identification of critical formulation and processing variables for metoprolol tartrate extended release (ER) matrix tablets. J Control Release 1999 59 327-42. 

Arterial hypertension P-Antagonists Reduce cardiac output and renin release Atenolol, Bisprolol, Metoprolol... 

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