Adrenergic Agonists Flashcards
Sympathomimetics Actions
Increase BP + HR (Vasoconstriction + Vasodilation of skeletal muscles bv),
Bronchodilation ,
Mydriasis, alertness , glycogenolysis
Norepinephrine Synthesis Steps
Synthesis of NE (tyr - Dopamine)
Storage
Release ( Ca influx = exocytosis)
Receptor binding
Removal of NE ( recycle via NET COMT in liver + MAO in mitochondria)
Adrenergic Receptor Types
A 1 , 2 + B 1 , 2
A1 sites + effects
{Gq}
BV (VC + increase peripheral resistance = high BP)
Pupil dilator muscles (mydriasis)
Bladder\ Prostate/VD (contraction , urinary retention , ejaculation)
Liver (Glycogenolysis )
A2 sites + effects
{Gi}
presynaptic nerve terminals ( inhibit NE & Ach release = DECREASE BP)
Pancreas (decreases insulin)
B1 sites + effects
{Gs}
Heart ( tachycardia , contractility )
Kidney JGCs (renin release) = inc. BP
Lipolysis
B2 sites + effects
{Gs}
bronchodilation , vasodilation , smooth muscle relaxation (uterus) , decreases peripheral resistance , glycogenolysis , glucagon release
D1 effects
low doses (inc. RBF , diuresis , natriuresis)
Int. Doses (activates B1-R)
High Doses (activates A1-R)
Desensitization of receptors
Sequestration of the receptors
Downregulation by decreased synthesis
Inability to couple to G-protein
Adrenergic Agonists absorption
absorbed slowly : subcutaneous tissues = local vasoconstriction (α-effect).
rapidly absorbed :intramuscular sites = (β2-mediated vasodilatation)
Poor CNS penetration (hydrophilic)
NE , Phenylephrine, Oxymetazoline
Alpha 1 agonists (Ophthalmic,
Intranasal, IV)
NE , Phenylephrine, Oxymetazoline (NOxyPhen)
Acute hypotension , hemorrhage, accidents (VC) , congestion , need mydriasis
Methyldopa , Clonidine (MC2)
Alpha 2 agonists (central antihypertensive drugs)
Dobutamine
B1 agonist IV ( Acute heart failure :Increase myocardial contractility)
Albuterol/ Terbutaline
B2 agonists inhalers (Bronchial asthma, preterm labor : VD + SM relax)
Ephedrine
Pseudoephedrine
A & B : decongestants
Dopamine Uses
cardiogenic + septic shock
enhances kidney perfusion + diuresis
Treatment of hypotension, heart failure and bradycardia unresponsive to other treatments.
Methylphenidate
ADHD
Epinephrine MOA
low doses (B effects : VD)
high doses (A effects: VC)
Epinephrine Uses
Bronchospasm (B2 VD)
Anaphylactic shock (A1 VC)
Cardiac arrest (A1 VC)
Local anaesthesia (A1 VC)
Intraocular surgery (A1 mydriasis)
NE MOA
Affects alpha receptors = VC = inc peripheral resistance =
vagus n. stimulation = PNS stimulation = Acetylcholine release = binds to M2 receptors = decrease in HR ( reflex bradycardia )
NE uses
Septic shock (inc vascular resistance)
Dopamine MOA
stimulates B1-R + at high conc. A1-R
Amphetamine, Methamphetamine and Methylphenidate
Indirect Sympathomimetic drugs (displace stored catecholamines)
Amphetamine, Methamphetamine and Methylphenidate
CNS stimulants “mood and alertness”, and appetite suppressants
Cocaine
inhibit NE transporters (inhibits reuptake)