Adrenergic pharm-Pechnick Flashcards
(24 cards)
What are the 5 steps in the life cycle of catecholamines (adrenergic transmission)?
- Synthesis
- Storage
- Release
- Receptor interactions
- Termination of action
What is the rate limiting step in the life cycle of catecholamines?
Tyrosine hydroxylation
What do a1 adrenergic receptors do?
- Contraction (smooth muscle)
What do B1 adrenergic receptors do?
- Stimulates renin release
What do B2 adrenergic receptors do?
- Relaxation (smooth muscle)
- Bronchodilation
Epinephrine
- Agonist at B1, B2, a1, a2
- At low doses B predominates (vasodilation)
- At high doses a1 predominates (vasoconstriction)
Norepinephrine
- Agonist at a1, a2, B1
- Causes vasoconstriction
Dopamine
- Agonist at D1, B1, a1, a2
- Low/med dose: increases renal blood flow
- High dose: vasoconstriction
How do indirect acting sympathomimetics work?
Increase synaptic levels of neurotransmitters by inducing neurotransmitter release and/or blocking reuptake
Amphetamine
- Indirect sympathomimetic
- Releases NE and blocks reuptake of NE, dopamine and serotonin
Cocaine
- Indirect sympathomimetic
- Blocks reuptake of NE, dopamine and serotonin
What is the party food effect?
When people who are taking MAOB inhibitors eat a “party food” (cheese, wine, sour cream, etc.) they get fatal hypertension due to tyramine in food being broken down into MAOA
Ephedrine and Pseudoephedrine
- Direct weak agonist at a and B receptors
- Indirectly causes release of NE
Milodrine and Metaraminol
- Direct acting a1 agonists
Phenylephrine
- Selective a1 agonist
Oxymetazoline and Tetrahydrozoline
- Partial a2 agonist with some a1 agonist activity
- Eye drops (constrict eye vessels to decrease redness)
Clonidine
- CENTRALLY ACTING (on the brain)
- Direct a2 agonist
- Inhibits sympathetic outflow
- Decreases HR, cardiac output and peripheral resistance
- Abrupt withdrawal can cause hypertensive crisis, tachycardia and arrhythmias
Phentolamine and Phenoxybenzamine
- Non-selective a receptor antagonists
Prazosin
- Selective a1 receptor antagonist
Isoproterenol and Dobutamine
- B1/B2 receptor agonist
- Cardiac stimulants
Albulterol and Salmeterol
- Selective B2 agonist
- Asthma meds
Mirabegron
- B3 agonist
- Used for treatment of overactive bladder
Propanolol, Nadolol, Carvedilol, Labetalol, Timolol and Carteolol
- Non-selective B antagonists
- Uses: MI, CHF, arrhythmias, migraine, anxiety
Atenolol and Metoprolol
- Selective B1 antagonists