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The Development of Beta Receptor Agonist Drugs
Published in Richard Beasley, Neil E. Pearce, The Role of Beta Receptor Agonist Therapy in Asthma Mortality, 2020
Independently, chemists at Draco (now part of the Astra group) in Sweden had synthesized a series of resorcinolamines with bulkier N-substituent groups. Replacement of the N-isopropyl group of orciprenaline with a N-t-butyl group also resulted in a potent beta agonist bronchodilator with less cardiac effects. The drug had the required oral activity and longer duration of action. This was the compound terbutaline (Figure 2).49-51 The good bronchodilator effects of these drugs in asthma with lesser, although not absent, cardiac stimulant side effects were supported by many clinical studies.52-55
Sympathomimetic Amines: Actions and Uses
Published in Kenneth J. Broadley, Autonomic Pharmacology, 2017
Dopamine (IntropinR) exerts positive inotropic and chronotropic effects through mixed indirect and direct sympathomimetic activity. Its cardiac stimulant activity is mainly via β1-adrenoceptors. Additionally, the haemodynamic properties of dopamine owe much to the stimulation of peripheral dopamine receptors in the vasculature and kidney; these properties will be described later (Chapter 12). Dopamine is administered by intravenous infusion to provide brief inotropic support in severe heart failure. Total peripheral resistance is usually unchanged with low to moderate doses, since a dopaminergic vasodilatation in the kidney and mesentery predominates over an α1-adrenoceptor-mediated vasoconstriction elsewhere. However, at higher doses, the latter effect comes into play and may be significant in the shock patient where substantial reflex vasoconstriction may already exist. This will place further load on the already weakened heart. Tachycardia and the consequent risk of precipitating arrhythmias are a further potential disadvantage. Vasoconstriction may cause gangrene of fingers or toes during prolonged infusions. Dopamine is rapidly metabolized via COMT and MAO (it should be avoided in patients receiving MAO inhibitors) and any adverse effects soon disappear if the infusion is stopped.
Abies Spectabilis (D. Don) G. Don (Syn. A. Webbiana Lindl.) Family: Coniferae
Published in L.D. Kapoor, Handbook of Ayurvedic Medicinal Plants, 2017
Medicinal properties and uses — Arjuna is popularly used as a cardiac tonic.866 In doses of 14 to 28 ml in the form of decoction it is very useful in hemorrhages and other fluxes; also in diarrhea, dysentery, and sprue. It is also useful in bilious affections and as an antidote to poisons. The decoction of thick bark of arjuna (3 g), cane sugar (24 g), and boiled cow’s milk (200 ml) is highly recommended in heart disease complicated with endocarditis, pericarditis, and angina. Ayurvedic physicians recommend the use of arjuna bark in derangement of all the three humors,kapha, pitta, and vayu, and all sorts of conditions of cardiac failure and dropsy. Powdered bark relieves hypertension, and has a diuretic and a general tonic effect in case of cirrhosis of the liver. It is considered a cardiac stimulant.178 Bark is prescribed for bilious affections, for sores, and as an antidote to poisons. The ash of bark is prescibed in scorpion sting. Fruit is tonic and deobstruent.1,3
Insight into the cardiovascular mechanisms of blood pressure lowering effect of gitogenin: a steroidal saponin
Published in Clinical and Experimental Hypertension, 2021
Imran Ul Haq, Taous Khan, Taseer Ahmad, Abdul Jabbar Shah
In conclusion, our data on the cardiovascular activities of gitogenin have shown that it possesses blood pressure-lowering effect in SD rats. Gitogenin induces vasodilatory effect through endothelium-dependent muscarinic receptors linked NO and possible antagonistic effect on angiotensin II receptors in the vascular smooth muscles. However, the negative chronotropic and inotropic effects of gitogenin are the outcomes of cardiac M2 receptors stimulant effect with a potential cardiac stimulant effect, which might be of clinical significances in cases of hypertension-associated complications.