Basic Science Principles Flashcards
(27 cards)
What actions does Ach have on its different receptors?
Nicotinic receptors: on skeletal muscles to produce movement (somatic, voluntary nervous system)
Muscarinic receptors: on the GI tract, bladder, and eyes produce SLUDD (parasympathetic nervous system, autonomic, involuntary)
What does agonism of muscarinic receptors by Ach result?
Agonists: Pilocarpine, bethanechol
1. Salvation
2. Lacrimation
3. Urination
4. Defication
5. Digestion
What does agonism of nicotinic receptors by Ach result in?
- Elevated HR/BP
What does antagonism of muscarinic receptors result in?
Antagonists: atropine, oxybutinin
Decreased SLUDD
What does agonism of alpha-1 receptors (mostly peripheral) by E, NE result in?
Agonists: Phenylephrine, Dopamine (dose-dept)
1. Smooth muscle vasoconstriction
2. Elevated BP
What does antagonism of alpha-1 receptors (mostly peripheral) in?
Antagonists: Alpha-1 blockers (doxazosin, carvedilol, phentolamine)
1. Smooth muscle vasodilation
2. Decreased BP
What does agonism of Alpha-2 rec (mostly CNS) by Epi, NE result in?
Agonist: Clonidine, Brimodine (opth)
1. Decrease Epi/NE release
2. Decrease HR/BP
What does antagonism of alpha-2 rec (mostly CNS) result in?
Antagonists: Ergot alkaloids, yohimbine
1. Increased Epi/NE release
2. Increase HR/BP
What does agonism of beta-1 rec by Epi/NE result in?
Agonism: Dobutamine, Isoproterenol, Dopamine (dose-dept)
1. Increase myocardial contractility (CO)
2. Increased HR
What does antagonism of beta-1 rec result in?
Antagonists: Beta blockers (metorpolol)
1. Decrease CO/HR
What does agonism of beta 2 receptors by Epi result in?
Agonist: Albuterol, terbutiline, Isoproterenol
1. Bronchodilation
What does antagonism of Beta 2 rec result in?
Antagonists: non selective beta blockers
Bronchoconstriction
What does agonism/antagonism of dopamine rec result in?
Agonists: levodopa, pramipexole
Antagonist: Metoclopramine, first gen antipsychotic
1. Renal/Cardiac/CNS effects
What does agonism/antagonism of serotonin result in?
Agonist: Triptans
Antagonist: Ondansetron, second gen antipsycotics
1. Platelet/GI/psychoatric effects
What is the role of the acetylcholinesterase enzyme?
Breaks down Ach
Inhibitors: donepezil, rivastigmine, galantamine
What is the role of the COMT enzyme?
Breaks down levodopa
Inhibitors: Etacapone; prevents breakdown of levodopa by COMT in the periphery increasing duration of levodeopa
What is the role of MAO enzyme?
Breaks down catecholamines (DA, NE, EPI, 5HT)
Inhibitors: phenelzine, isocarboxazid, tranylcypromine, selegiline, rasiligine (treat depression and parkinsons)
What is the role of the COX enzyme?
Converts arachidonic acid to prostaglandins (inflammation) and thromboxane A2 (platelet aggregation)
What is the role of the PDE enzyme?
Breaks down cyclinc GMP (a smooth muscle relaxant)
Inhibitors: sildenafil, tadalifil; prolonging muscle relaxation in the arteries of the penis
What is the role of Vitamin K epoxide reductase enzyme?
converts vit K to the active form required to produce clotting factors
Inhibitors: warfarin inhbitis clotting factors II, VII, Xi,X
What is the role of xanthine oxidase enzyme?
Breaks down hypoxanthine into xanthine and uric acid
What ABX does not contain the beta lactam ring responsible for allergies?
Aztreonam
What reactions can cause drug degradation?
- oxidation/reduction
- Hydrolysis
- Photolysis
What are strategies for preventing drug oxidation?
- Light protection
- Temperature control
- Antioxidants (ascorbic acid, tocophernols vit E)
- Chelating agents
- pH with buffer system
