The pharmacology of xamoterol: a basis for modulation of the autonomic control of the heart.

Snow, H. M.

doi:10.1111/j.1365-2125.1989.tb03569.x

Cited by 10 publications

(3 citation statements)

References 45 publications

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“…Phosphodiesterase inhibitors (milrinone), oral beta‐1 receptor agonists (pirbuterol 184 and prenalterol 185 ) and drugs with beta‐1 receptor‐agonist activity when sympathetic tone is low and adrenergic‐receptor‐blocking activity when sympathetic tone is high (eg xamoterol 186 – 189 ) have been shown to have some short term beneficial effects in patients with CHF. However, Yusuf (personal communication) performed a meta‐analysis of studies comparing these classes of drugs against placebo in patients with CHF and found a significantly higher death rate in the drug as opposed to placebo groups.…”

Section: Treatmentmentioning

confidence: 99%

Congestive Heart Failure in the Elderly

Luchi¹,

Taffet²,

Teasdale³

1991

J American Geriatrics Society

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Section: Treatmentmentioning

confidence: 99%

Congestive Heart Failure in the Elderly

Luchi¹,

Taffet²,

Teasdale³

1991

J American Geriatrics Society

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“…Lammers et al (45) observed, however, a P2 antagonism of xamoterol in 3 of 11 patients with asthma. This effect was reversed by salbutamol, suggesting occupancy of P,-adrenoceptors by xamoterol (83).…”

Section: Selectivitymentioning

confidence: 91%

Xamoterol, a β₁Adrenoceptor Partial Agonist: Pharmacology and Clinical Use

Vigholt-Sørensen

1991

Cardiovascular Drug Reviews

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The high prevalence of chronic congestive heart failure has encouraged the search for new orally active drugs. In the early stages of heart failure, when symptoms are confined to periods of work stress, the overriding objective of drug therapy is to improve cardiac contractile activity. As heart failure advances and vasoconstriction and increased activity of the neuroendocrine system results in salt and water retention, diuretics can be added. In the terminal stages of disease, the addition of angiotensin converting enzyme (ACE) inhibitors can be expected to benefit the patient (87).In 1948, Ahlquist (1) proposed the existence of two types of receptors in the adrenergic system, a-and P-receptors. Lands et al. (46) presented experimental evidence in 1967 that justified a subdivision of f3-adrenergic receptors into PI-and P,-adrenoceptors. In 1972, Furchgott described (31) the procedure for the characterization of a-and P-adrenoceptors. According to the earlier classification, the responses of the tissues could be classified as being mediated by either P,-or P,-adrenoceptors. Subsequently, PI-and P,-adrenoceptors have been found to coexist in various organs. For example, in the heart of some animals and in the human, we have both receptor types. The functional and pathophysiological roles of these receptors are not fully defined (4,(15)(16)(17)37,38,103).The pharmacological classification of P-adrenoceptors into PI-and &-subtypes has been based on the relative affinity of the receptors for the agonists and on the competition between selective antagonists and nonselective radiolabeled ligands. The P-adrenoceptors have been identified biochemically, and these two mammalian proteins possess identical molecular masses. The structures of PI-and P,-adrenoceptors have been proposed and their genes have been cloned. Recent data establish that the two receptors are products of different genes (30).When an agonist occupies the P-adrenoceptor, adenyl cyclase is activated through its interaction with the guanine nucleotide-binding regulatory proteins, G,. Cyclic AMP is an

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“…, is a partial fll adrenoceptor agonist [5] without direct vasodilatory properties [6,7]. Its intrinsic sympathomimetic activity is about 43 % of that of isoprenaline [8].…”

mentioning

confidence: 99%

Lack of pharmacodynamic interactions between acute dose flosequinan and xamoterol

Walley

Tsao

et al. 1994

Eur J Clin Pharmacol

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The possible cardiovascular pharmacodynamic interactions at rest and during exercise of combining oral flosequinan (100 mg) with xamoterol (200 mg) was investigated in a four-way randomised double-blind placebo-controlled crossover trial in eight healthy male volunteers. Xamoterol was better tolerated than flosequinan. The most common adverse events were mild to moderate headache and facial flushing. One volunteer developed headache and vomiting following flosequinan treatment and was replaced. Compared to placebo, at supine rest, flosequinan significantly increased heart rate (HR) by 5 beats.min-1, but had no effect on cardiac output (CO), stroke volume (SV) and mean blood pressure (MBP). Xamoterol significantly increased CO by 1.5 l.min-1, HR (5 beats.min-1) and MBP (6 mmHg) but not SV. The combined treatment (flosequinan + xamoterol) significantly increased CO (1.7 l.min-1) and HR (10 beats.min-1), but had no effect on SV and MBP. During exercise, flosequinan had no significant effect on any variable compared to placebo. Both xamoterol and combined treatment reduced the increase in CO (-4.6 l.min-1 after xamoterol and -3.4 l.min-1 after combined treatment vs. 0.1 l.min-1 after placebo), but had no effect on other variables. The effect of the combined treatment on each haemodynamic variable were no more than the anticipated additive effects of the two drugs. Thus, no cardiovascular pharmacodynamic interaction was found between flosequinan and xamoterol in healthy volunteers.

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The pharmacology of xamoterol: a basis for modulation of the autonomic control of the heart.

Cited by 10 publications

References 45 publications

Congestive Heart Failure in the Elderly

Congestive Heart Failure in the Elderly

Xamoterol, a β₁Adrenoceptor Partial Agonist: Pharmacology and Clinical Use

Lack of pharmacodynamic interactions between acute dose flosequinan and xamoterol

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The pharmacology of xamoterol: a basis for modulation of the autonomic control of the heart.

Cited by 10 publications

References 45 publications

Congestive Heart Failure in the Elderly

Congestive Heart Failure in the Elderly

Xamoterol, a β1Adrenoceptor Partial Agonist: Pharmacology and Clinical Use

Lack of pharmacodynamic interactions between acute dose flosequinan and xamoterol

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Product

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Xamoterol, a β₁Adrenoceptor Partial Agonist: Pharmacology and Clinical Use