Metoprolol and pindolol

Rangno RE, Langlois S. Comparison of withdrawal phenomena after propranolol, metoprolol and pindolol. Br J Clin Pharmacol 1982 13(Suppl 2) S345-51. 

Certain beta-blockers such as propranolol, metoprolol, and pindolol, and alpha-blockers such as prazosin, may cause impotence or a decrease in libido, which is usually dose related and should be... 

Describe the effects of an alpha-blocker on the hemodynamic responses to epinephrine. Describe the effects of an alpha-blocker on the hemodynamic responses to norepinephrine. Compare the effects of propranolol, labetalol, metoprolol, and pindolol. 

P-Adrenoceptor blockers for the treatment of hypertension include (/) the cardioselective P -adrenoceptor blockers without intrinsic sympathomimetic activity (ISA), ie, atenolol (Table 3), bisoprolol (Table 3), and metoprolol (Table 1) (2) the cardioselective with ISA, ie, acebutolol (Table 1) (J) the noncardioselective without ISA, ie, propranolol (Table 1) and timolol [26839-75-8] C23H24N4O2S and (4) the noncardioselective with ISA, ie, oxprenolol [6452-71-7] C 3H23N03, and pindolol. 

Beta Blockers. The beta blockers, which act by interfering with noradrenergic transmission, have been used to manage aggression and other behavioral disturbances in patients who have suffered brain injury due to trauma and stroke for over 25 years. Several beta blockers have been tested including propranolol (Inderal), pindolol (Visken), nadolol (Corgard), and metoprolol (Lopressor). Fat-soluble beta blockers such as propranolol and pindolol more readily cross the blood-brain barrier and are thus better suited to managing psychiatric symptoms such as behavioral lability. 

Fig. 4.5 Central receptor occupancy after oral administration of p-adrenoceptor antagonists A, atenolol B, metoprolol C, pindolol D, propranolol. The high occupancy of pi receptors does not correlate with physicochemical properties (lipophilicity). The occupation of p2 receptors correlates with sleep disturbances and the intrinsic selectivity of the compounds.

Compounds that exhibit roughly the same affinity to and j32 rsceptors independent of dosage such as nadolol, propranolol, pindolol, timolol, and labetalol (combined a- and j3-adrenoblocker) are classified as nonselective blockers. Drugs which in therapeutic doses have higher affinity to -receptors than to j32-receptors such as acebutol, atenolol, metoprolol, and esmolol, are called selective or cardioselective j3-adrenoblockers. 

Propranolol, nadolol, timolol, penbutolol, carteolol, sotalol, and pindolol Bronchial asthma or bronchospasm, including severe chronic obstructive pulmonary disease. Metoprolol Treatment of Ml in patients with a heart rate less than 45 beats/min significant heart block greater than first degree (PR interval 0.24 seconds or more) systolic blood pressure less than 100 mm Hg moderate to severe cardiac failure. Sotalol Congenital or acquired long QT syndromes. 

Drug/Food interactions Food enhances the bioavailability of metoprolol and propranolol this effect is not noted with nadolol, bisoprolol, or pindolol. The rate of carteolol and penbutolol absorption is slowed by the presence of food however, extent of absorption is not appreciably affected. Sotalol absorption is reduced approximately 20% by a standard meal. 

Systemic beta-blockers are used extensively far the treatment of hypertension and other cardiovascular disorders. Of the available oral beta-blockers, atenolol, metoprolol, nadolol, pindolol, propranolol, and timolol have been documented to produce a dose-dependent reduction in lOP. The ocular hypotensive effect associated with systemically administered beta-blockers can be compared with that achieved with topically applied beta-blockers such as timolol. Although specific studies have not been conducted with most of the remaining systemic beta-blockers, these agents might also be expected to reduce lOP at clinically useful doses. 

If Chiralpak AD shows some resolution, the Chiraleel OD column may provide improved. separation. It is particularly effective for fi-blockers, compounds with similar functionality, and for steroids. Examples flavanone, metoprolol, oxprenolol. pindolol, propranolol. 

Pure enantiomer imprinting of L-phenylalanine anilide, (/ )-propranolol, S)-metoprolol and (50-ropivacaine has been undertaken and these MIP capillaries have been used in the CEC mode for enantiomer separations [39-41,60-62,70,71] (Table 16.1). Baseline separations for the enantiomers of phenylalanine (Fig. 16.7) and for propranolol and metoprolol could be carried out in less than 2 min. (Fig. 16.5). A propranolol column was shown to be able to resolve several other j8-blockers, including prenalterol, atenolol, pindolol, etc. (Fig. 16.8) [41] and the ropi-... 

Lipid solubility (13) determines the extent to which a drug partitions between an organic solvent and water. Propranolol, oxprenolol, metoprolol, and timolol are the most lipid-soluble beta-adrenoceptor antagonists, and atenolol, nadolol, and sotalol are the most water-soluble acebutolol and pindolol are intermediate (14). 

Diuretics have been combined with 8-blockers in fixed combinations as exemplified by clopamlde and pindolol (Viskaldix ) and by metoprolol... 

If a patient with bronchial hyperreactivity requires /3-blocker therapy, one of the selective /3i-blockers (e.g., acehutolol, atenolol, metoprolol, or pindolol) should be used at the lowest possible dose. Celiprolol and betaxolol appear to possess greater cardioselectiv-ity than currently marketed drugs. " Fatal status asthmaticus has occurred with the topical administration of the nonselective timolol maleate ophthalmic solution for the treatment of open-angle glaucoma. Early investigations with ophthalmic hetaxolol suggest that it is well tolerated even in timolol-sensitive asthmatics. - ... 

Answer D. The effectiveness of labetalol in the management of hypertension and in severe hypertensive states appears to be due to a combination of antagonistic actions at both alpha and beta adrenoceptors. Labetalol is not a P selective blocking agent (unlike atenolol and metoprolol), and (unlike pindolol and acebutolol) it lacks intrinsic sympathomimetic activity. Labetalol is available for both peroral and parenteral use unfortunately, it blocks p2 receptors in bronchiolar smooth muscle. 

In the treatment of hypertension, a major use of beta-blockers is in combination with hydralazine. The direct vasodilators bring about reflex cardiac stimulation, and beta-blockers prevent these adverse effects (see also Figure 67). Beta-blockers also reduce blood pressure by exerting a central effect or a peripheral action, or both, which decreases renin activity. Metoprolol and atenolol are beta selective, and they are safer agents in patients with asthma, diabetes mellitus, or low-renin hypertension. Some beta-blocking agents such as pindolol have intrinsic sympathomimetic activity and may be used in the treatment of pronounced bradycardia (sick sinus syndrome). Unlike propranolol, metoprolol is not a very lipid-soluble... 

Xie, H.G. Zhou, H.H. Assay of metoprolol and alpha-hydroxymetoprolol in human urine hy reversed-phase liquid chromatography with direct-injection. Chung Kuo Yao Li Hsueh Poo, 1995, 16, 32—35 Bailey, C.J. Ruane, R.J. Wilson, I.D. Packed-column supercritical fluid chromatography of fl-blockers. J.Chromatogr.Sci., 1994, 23, 426—429 [SFC simultaneous alprenolol, atenolol, lahetalol, metoprolol, oxprenolol, pindolol, practolol, propranolol, toliprolol, xamoterol]... 

The plasma levels of lidocaine after intravenous, and possibly oral, use can be increased by propranolol. Isolated cases of toxicity attributed to this interaction have been reported. Nadolol and penbutolol possibly interact similarly, but there is uncertainty about metoprolol. Atenolol and pindolol appear not to interact. 

There is evidence that most NSAIDs can increase blood pressure in patients taking antihypertensives, although some studies have not found the increase to be clinically relevant In various small studies, indometacin reduced the antihypertensive effects of the beta biockers. There is some evidence that piroxicam usually interacts similarly. Ibuprofen and naproxen have reduced the effect of beta blockers in some small studies but not others. Two isolated cases of hypertension have been reported with naproxen and ibuprofen in patients treated with propranolol and pindolol, respectively. Celecoxib, but not rofecoxib, inhibits the metabolism of metoprolol. Limited information su ests that normally di-... 

The enandoselecdve nltro-aldol reacdon catalyzed by C/fi-LLB is effecdvely applied to the synthesis of three kmds of opdcally acdve fi-receptor blocking dnigs fS -metoprolol, " fS -propanolol, " and fS -pindolol " " fScheme 3.17i. 

Similar to dihydropyridine calcium blockers, many 0-adrenoreceptor antagonists exhibit antioxidant activity. Mak and Weglinski [290] showed that the pretreatment of canine myocytic sarcolemmal membranes with 0-adrenoreceptor antagonists (propranolol, pindolol, metoprolol, atenolol, or sotalol) (Figure 29.15) inhibited superoxide-induced sarcolemmal... 

Similarly, this reaction has also been applied in the synthesis of other fi-rcccptor blocking drugs such as (Vj-metoprolol,117 (Vj-pindolol,118 and the HIV protease inhibitors KNI-227 and KNI-272.119... 

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