Adrenergic Agents Flashcards
Adrenergic agents
Enhance or reduce activity of the sympathetic division of the autonomic nervous system
Act on adrenergic receptors or neurotransmitters
Catecholamines
Adrenergic neurotransmitters
Contain catechol ring and ethylamine moieties
Examples include dopamine, norepinephrine, and epinephrine
Metabolism of norepinephrine and epinephrine
Monoamine oxidase and catechol-O-methyltransferase: important enzymes
Major end product: vanillylmandelic acid
Adrenergic receptors
Alpha and beta receptors (differ in secondary messengers: alpha- phospholipase C, beta- cAMP)
G-protein coupled receptors
Which receptors do what
Constriction: alpha 1 and beta 1
Dilation: alpha 2 and beta 2
Structure-activity relationships for catecholamine-like drugs
Adding -OH to alpha carbon gives greater activity in the peripheral nervous system
Increasing size of R group bound to N: increased beta activity and decreased alpha activity
Adding small alkyl groups to beta carbon: less degradation by MAO
Phenylethanolamines
Mimic epinephrine
Alpha 1 agonists: vasoconstrictors
Clonidine
Alpha 2 agonist: lowers blood pressure
Albuterol
Seclective beta 2 agonist: relaxes bronchial muscles (inhaler active ingredient)
L-Pseudoephedrine
Indirectly-acting sympathomimetic
Fewer CNS effects than ephedrine
Sudafed: nasal decongestant
D-(-)-Ephedrine
Acts on both alpha and beta receptors
CNS stimulant
Propranolol
Beta blocker (beta 1 and beta 2) Treats cardiovascular symptoms, anxiety, and glaucoma (increased pressure in eyes)