Pharm Foundations: Basic Science Concepts Flashcards
Endogenous Muscarinic Substrate/Action
Acetylcholine
-Action: Increased SLUDD
SLUDD
- Salivation
- Lacrimation
- Urination
- Defecation/Diarrhea
- Digestion
Muscarinic Drug Agonist/Action
Pilocarpine or Bethanechol
-Action: Increased SLUDD
Muscarinic Drug Antagonist/Action
Atropine or Oxybutynin
-Action: Decreased SLUDD
Endogenous Alpha-1 Substrate/Location/Action
- Epinephrine or norepinephrine
- Mainly peripheral
- Action: Smooth muscle vasoconstriction, increased BP
Alpha-1 Drug Agonist/Action
- Phenylephrine or dopamine (dose dependent)
- Action: Smooth muscle contraction, increased BP
Alpha-1 Drug Antagonist/Action
- Alpha-1 blockers like doxazosin, carvedilol, phentolamine
- Action: Smooth muscle dilation, decreased BP
Endogenous Nicotinic Substrate/Action
Acetylcholine
-Action: Increased HR and BP
Nicotinic Drug Agonist/Action
Nicotine
-Action: Increased HR/BP
Nicotinic Drug Antagonist/Action
Neuromuscular blockers like rocuronium
-Action: Neuromuscular blockade
Alpha-2 Endogenous Substrate/Location/Action
- Epinephrine and NE
- Mainly brain and central NS
- Action: decreased release of epi/NE, decreased BP/HR
Alpha-2 Drug Agonist/Action
- Clonidine, brimonidine (ophthalmic for glaucoma)
- Action: decreased release of epi/NE, decreased BP/HR
Alpha-2 Drug Antagonist/Action
Ergot alkaloid or yohimbine
-Action: increased BP and HR
Beta-1 Endogenous Substrate/Location/Action
- Epi and NE
- Mainly heart
- Action: increased myocardial contractility, CO, HR
Beta-1 Drug Agonist/Action
- Dobutamine, isoproterenol, dopamine (dose-dependent)
- Action: Increased myocardial contractility, CO, and HR
Beta-1 Drug Antagonist/Action
- Beta-blockers metoprolol (selective), propranolol, and carvedilol (non-selective)
- Action: Decreased CO and HR
Beta-2 Endogenous Substrate/Location/Action
- Epi
- Mainly lungs
- Action: Bronchodilation
Beta-2 Drug Agonist/Action
Albuterol, terbutaline, isoproterenol
-Action: Bronchodilation
Beta-2 Drug Antagonist/Action
Nonselective b-blockers (propranolol and carvedilol)
-Action: bronchoconstriction
Dopamine Receptor Endogenous Substrate/Action
Dopamine
-Action: Many, including renal/cardiac/CNS effects
Dopamine Drug Agonist/Action
Levodopa or pramipexole
-Action: Many, including renal/cardiac/CNS effects
Dopamine Drug Antagonist/Effects
First generation antipsychotics (haloperidol) and metoclopramide
-Action: Many, including renal/cardiac/CNS effects
Serotonin Receptor Endogenous Substrate/Action
- Serotonin
- Action: Many, including platelet/GI/psychiatric effects
Serotonin Drug Agonist/Action
Triptans for migraines
-Action: Many, including platelet/GI/psychiatric effects
Serotonin Drug Antagonist/Action
Ondansetron and second generation antipsychotics (quetiapine)
-Action: Many, including platelet/GI/psychiatric effects
Acetylcholinesterase
- Enzyme that breaks down ACh
- Inhibitors: donepezil, rivastigmine, galantamine
- Drug Action: by blocking this enzyme, ACh levels increase and can treat conditions like Alzheimers
ACE
- Converts angiotensin I to angiotensin II (potent vasoconstrictor)
- Inhibitor: ACE-I (lisinopril, ramipril, etc.)
- Action: By inhibiting angiotensin II production, there is less vasoconstriction/aldosterone secretion which can treat HTN, heart failure, and kidney disease
COMT
- Catechol-O-methyltransferase
- Breaks down levodopa
- Inhibitors: COMT-I (entacapone)
- Action: increases duration of action of levodopa to treat conditions like Parkinson’s
COX
- Cyclooxygenase
- Converts arachidonic acid to prostaglandins and thromboxane A2 (inflammation and platelet aggregation respectively)
- Inhibitors: NSAIDs (aspirin, ibuprofen)
- Action: Decrease end products to treat pain/inflammation and decrease platelet activation/aggregation
MAO
- Monoamine oxidase
- Breaks down catecholamines (5HT, NE, Epi, DA)
- Inhibitors: MAO-I (selegiline, rasagiline, methylene blue, linezolid)
- Action: Increasing catecholamine levels to treat depression (tyramine: too high can lead to hypertensive crisis and 5HT syndrome)
PDE
- Phosphodiesterase
- Breaks down cGMP, smooth muscle relaxant
- Inhibitors: PDE-5i (sildenafil, tadalafil)
- Action: competitively binds to prevent cGMP breakdown to increase smooth relaxation to treat erectile dysfunction
Vitamin K epoxide reductase
- Converts vitamin K to active form needed to clotting
- Inhibitor: Warfarin
- Action: Blocks vitamin K metabolism and decreases clotting factors II, VII, IX, and X to treat/prevent blood clots
Xanthine Oxidase
- Breaks down hypoxanthine and xanthine to uric acid
- Inhibitor: Allopurinol
- Action: Decreases uric acid production to prevent gout attacks
