ABSTRACT

Adrenergic antagonists are agents capable of antagonizing the adrenergic neurotransmitters like noradrenaline and adrenaline competitively or noncompetitively bound to α, β adrenoceptors. Hence these have a wide range of application clinically. In spite of having a wide range of pharmacological action in areas of CNS, locomotion, ophthalmology, and metabolism, these are of importance in the case of diseases associated with CVS as adrenergic neurotransmitters play a role in vasoconstriction, increased heart rate, and contractility effects of the heart due to interaction with α and β adrenoceptors. Additionally, activity on smooth muscle renders it effective against BPH. Other off-label uses include regulation of anxiety, glaucoma, in improving HDL, an adjuvant in hypothyroidism, and migraine prophylaxis. This chapter highlights this aspect by the discussion of neurotransmission blockade of the sympathetic system by some synthetic agents with antagonistic action. The chapter covers the area of drugs blocking sympathetic system via adrenoceptors α, β either individualized or by combination. In addition to this, few drugs with specific binding to the receptor subtypes are also mentioned.