Influence of beta2 agonism and beta1 and beta2 antagonism on adverse effects and plasma lipoproteins: Results of a multicenter comparison of dilevalol and metoprolol

Materson, Barry J.; Vlachakis, Nicolas D.; Glasser, Stephen P.; Lucas, Charles; Ramanathan, Kodangudi B.; Ahmad, Shamim; Morledge, John H.; Saunders, Elijah; Lutz, Lawrence J.; Schnaper, H. William; Maxwell, Morton H.; Poland, Marcia

doi:10.1016/0002-9149(89)90131-8

Cited by 17 publications

(9 citation statements)

References 14 publications

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“…Our results are in line with previous studies, considering also that adverse effects of metoprolol usually occur in the early stages of treatment and are often transient 1 , 2 , 3 , 4 , 5 , 6 . Examination of possible adverse effects of metoprolol on sexual function was 1 major objective of this study, because only a few studies have addressed this issue and the results are conflicting 30 , 31 , 32 , 33 . Of the 89 evaluable patients, about 26% reported sexual dysfunction during this short‐term study.…”

Section: Discussionsupporting

confidence: 88%

“…[1][2][3][4][5][6] Examination of possible adverse effects of metoprolol on sexual function was 1 major objective of this study, because only a few studies have addressed this issue and the results are conflicting. [30][31][32][33] Of the 89 evaluable patients, about 26% reported sexual dysfunction during this short-term study. Curiously enough, sexual dysfunction was significantly more common among the EMs plus UMs than among the PM plus IM group.…”

Section: Discussionmentioning

confidence: 89%

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Impact of genotype on adverse effects during treatment with metoprolol: A prospective clinical study

Fux

Mörike

Pröhmer

et al. 2005

Clinical Pharmacology & Therapeutics

116

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Section: Discussionsupporting

confidence: 88%

Section: Discussionmentioning

confidence: 89%

Impact of genotype on adverse effects during treatment with metoprolol: A prospective clinical study

Fux

Mörike

Pröhmer

et al. 2005

Clinical Pharmacology & Therapeutics

116

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“…Since non-specific drug toxicity is commonly independent of chirality (Materson et al, 1989;Shoenberger et al, 1989;Chrisp & Goa, 1990), it can be expected that each enantiomer contributes equally to labetalol's potential for side effects (such as dizziness, dyspepsia, diarrhoea and nausea, the latter two being dose-related). However, this is not always true and the RR isomer (dilevalol) has recently been withheld from the market due to liver toxicity.…”

Section: Introductionmentioning

confidence: 99%

The α‐ and β‐adrenoceptor blocking activities of labetalol and its RR‐SR (50:50) stereoisomers

Riva¹,

Mennini

Latini

1991

British J Pharmacology

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1 We compared the a,-, a2-and f6l-adrenoceptor blocking potencies of labetalol with those of its two stereoisomers (RR and SR) in pithed rats and in homogenized rat cerebral cortex and heart. 2 In pithed rats, labetalol and the RR-SR combination were given orally either at doses of 25 and 50mg kg-1 body wt. or intravenously at doses of 1 and 5mg kg-' body wt. Prazosin 4 and 20ug kg'-body wt. and propranolol 1 and 5 mg kg-l body wt., were given intravenously for comparison studies of potency at al-and fl1-adrenoceptors, respectively. Effects were studied before and after i.v. administration of either phenylephrine (at doses which increased the mean arterial pressure by approximately 80mmHg) or isoprenaline (at doses that increased heart rate by approximately 100 beats min 1). 3 In pithed rats, labetalol and the RR-SR combination antagonized, in a dose-dependent manner, the pressor effect of phenylephrine (P < 0.05) and the chronotropic effect of isoprenaline (P < 0.05). Following both oral and intravenous dosing, the RR-SR combination was twice potent as labetalol in terms of a,-and 161-adrenoceptor antagonism at equivalent doses. 4 Labetalol and the enantiomers lacked affinity at a2-adrenoceptors while at x1-adrenoceptors the order of potency was prazosin > RR-SR > labetalol. At fl1-adrenoceptors, the affinity of the compound RR-SR was about 3 times that of labetalol. 5 As labetalol is a mixture of active (RR and SR) and inactive (SS and SR) enantiomers (in terms of aand Preceptor actions), the combination of RR and SR may be a valuable substitute for labetalol in the treatment of systemic hypertension. Although the potential for non-specific side effects (common to all four enantiomers) could be expected to be diminished, recent reports by postmarketing surveillance indicate that the RR isomer (dilevalol) can induce liver toxicity. Interestingly, labetalol is devoid of this effect; whether the combination of RR and SR enantiomers could be of clinical importance warrants further investigation.

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“…73,84 In placebo controlled studies of atenolol, metoprolol CR, and pindolol, the edema rates for the ␤-blockers varied from 1.7% to 6% compared with 1.9% to 20% in the placebo groups. 23,24,59,111 A number of non-placebo-controlled studies of ␤-blockers have reported variable rates of edema: 1% to 6% for atenolol 25,43,60,72 ; 0% to 5% for metoprolol 35,36,59,112,113 ; 0% for carvedilol 45 ; 0% for pindolol 45 ; and 1% for dilevalol. 112 Two trials that lacked a placebo group documented lower extremity edema frequently in subjects treated with ␤-blockers.…”

Section: ␤-Blockersmentioning

confidence: 99%

“…23,24,59,111 A number of non-placebo-controlled studies of ␤-blockers have reported variable rates of edema: 1% to 6% for atenolol 25,43,60,72 ; 0% to 5% for metoprolol 35,36,59,112,113 ; 0% for carvedilol 45 ; 0% for pindolol 45 ; and 1% for dilevalol. 112 Two trials that lacked a placebo group documented lower extremity edema frequently in subjects treated with ␤-blockers. The LIFE trial found that 14% of subjects in the atenolol arm of the trial had edema, 105 and the STOP-Hypertension-2 study found an edema rate of 8.5% in the group treated with atenolol, metoprolol, pindolol, or HCTZ plus amiloride.…”

Section: ␤-Blockersmentioning

confidence: 99%

Fluid Matters in Choosing Antihypertensive Therapy: A Hypothesis That the Data Speak Volumes

Blankfield

2005

The Journal of the American Board of Family Medicine

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Assuming that blood pressure is lowered equivalently, diuretics are more effective than angiotensinconverting enzyme inhibitors (ACEIs), calcium channel blockers (CCBs), and ␣-adrenergic receptor blockers (␣-blockers) at preventing heart failure, and they are more effective than ACEIs and ␣-blockers at preventing strokes. Compared with ␤-adrenergic receptor blockers (␤-blockers) and ACEIs, CCBs are less effective at reducing myocardial infarcts and heart failure. There is currently no conceptual framework by which to organize data indicating that some antihypertensive medications are better than others at preventing cardiovascular diseases. The thesis of this article is that the fluid reduction or fluid retention attributable to antihypertensive medications, either alone or in combination, provides a basis for ranking these medications. Diuretics have a theoretical advantage compared with other antihypertensive medications because they reduce total body fluid more than other agents. Therefore, they are the preferred drugs for treating hypertension. Provided that blood pressure is lowered comparably, diuretics have been demonstrated to be more effective than angiotensin-converting enzyme inhibitors (ACEIs), calcium channel blockers (CCBs), and ␣-adrenergic receptor blockers (␣-blockers) at preventing heart failure, and diuretics have been found to be more effective than ACEIs and ␣-blockers at preventing stokes.

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Influence of beta2 agonism and beta1 and beta2 antagonism on adverse effects and plasma lipoproteins: Results of a multicenter comparison of dilevalol and metoprolol

Cited by 17 publications

References 14 publications

Impact of genotype on adverse effects during treatment with metoprolol: A prospective clinical study

Impact of genotype on adverse effects during treatment with metoprolol: A prospective clinical study

The α‐ and β‐adrenoceptor blocking activities of labetalol and its RR‐SR (50:50) stereoisomers

Fluid Matters in Choosing Antihypertensive Therapy: A Hypothesis That the Data Speak Volumes

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