Sympathomimetic drugs Part II
Selectivity for alpha versus β receptors (SAR):
- Sympathomimetic drugs (Part II)
- N-alkyl substitution… increases potency at β and decreases potency at alpha receptors.
- Phenol group…important for β more than alpha agonists.
- alpha-substitution…increases alpha2 selectivity.
- N-alkyl extension… good for β selectivity.
Examples of Sympathomimetic drugs (Part II) alpha and beta agonists
- Selective alpha1-agonists.
- Act as vasoconstrictors.
- Used topically for nasal congestion.
- Selective alpha2 agonist (centrally) leads to inhibition of sympathetic outflow from the CNS.
- Used in hypertension
- Central nervous (CNS) system stimulant
- Increasing levels of dopamine and noradrenaline in the synaptic cleft.
- Long-acting beta-2 agonist
- For Asthma and COPD
- Adrenergic agonist
- Neurotransmitter
- Adrenergic agonist
- Neurotransmitter
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