Chapter 2: Basic Science Concepts Flashcards
Substrate
A substance that creates a signal or produces an effect by binding to a receptor, enzyme, or transporter
Endogenous
A substance that is produced by the body
Exogenous
A substance that is produced outside the body (e.g. a drug)
Agonist
A substance that combines with a receptor to initiate a reaction. Can be endogenous or exogenous.
Antagonist
A substance that reduces or blocks a reaction. Can be endogenous or exogenous.
Induction
When a substance increases the activity of an enzyme
Inhibition
When a substance decreases or blocks the activity of an enzyme
Peripheral Nervous System parts
Somatic and autonomic
Somatic Nervous System
Controls voluntary muscle movement
Autonomic Nervous System
Controls involuntary bodily functions (digestion, cardiac output, and blood pressure)
Neurotransmitters
- Acetylcholine (Ach)
- Epinephrine (Epi)
- Norepinephrine (NE)
- Dopamine (DA)
- Serotonin (5-HT)
Acetylcholine
Mostly involved in the somatic nervous system. It’s released in response to neuron signals and binds to nicotinic receptors in skeletal muscles to affect muscle movement.
Autonomic Nervous System parts
Parasympathetic (rest and digest)
Sympathetic (flight or fight)
Parasympathetic Nervous System
“rest and digest”
Works by releasing Acetylcholine (Ach) which binds to muscarinic receptors located throughout the body (gut, bladder, eyes etc..) results in SLUDD (salivation, lacrimation, urination, defecation and digestion)
Sympathetic Nervous System
“fight or flight”
Works by releasing Epi and NE which act on adrenergic receptors (alpha-1, beta-1, and beta-2) in the cardiovascular and respiratory systems. Activation results in increased BP, HR, and bronchodilation. Beta-2 receptors increase glucose production. Digestion and urination are minimized.
Location of muscarinic receptors
bladder and stomach
Location of Alpha-1 receptors
Smooth muscle including blood vessels
Beta-1 Receptor Location
Heart
Beta-2 Receptor Location
Lungs
What is an agonist
A substance that binds to and activates a response
What is an antagonist
Binds to a receptor but does not produce a subsequent reaction; the antagonist blocks the agonist from binding and inhibits the subsequent reaction
Competitive Inhibition
When an antagonist binds to the same active site of a receptor as the endogenous substrate preventing the activity
Non-competitive inhibition
The antagonist binds to the receptor at a site other than the active site which changes the shape of the active site and prevents the endogenous substrate from binding
Muscarinic Receptor
- ACh
- Agonist action increase in SLUDD; pilocarpine, bethanechol
- Antagonist action decrease in SLUDD; atropine, oxybutynin
Nicotinic Receptor
- ACH
- Agonist action increases HR and BP; nicotine
- Antagonist action are neuromuscular blockage; rocuronium
Alpha-1 Receptor (mainly peripheral)
endo substrate, agonist, antagonist
- Epi and NE
- Agonist action is smooth muscle vasoconstriction and increase in BP; phenylephrine, dopamine
- Antagonist action is smooth muscle vasodilation and decrease in BP; doxazosin, carvedilol, phentolamine
Alpha-2 (mainly brain)
endo substrate, agonist, antagonist
- Epi and NE
- Agonist action is decreased release of Epi and NE, decreased BP and HR; clonidine, brimonidine
- Antagonist action is increased BP and HR; ergot alkaloids, yohimbine
Beta-1 (mainly heart)
endo substrate, agonist, antagonist
- Epi and NE
- Agonist action is increase myocardial contractility, CO, and HR; dobutamine, isoproterenol, dopamine
- Antagonist action is decreased CO and HR; metoprolol (b-1 selective), carvedilol, propranolol (non-b selective)
Beta-2 (mainly lungs)
endo substrate, agonist, antagonist
- Epi
- Agonist action is bronchodilation; albuterol, terbutaline, isoproterenol
- Antagonist action is bronchoconstriction; non-selective bb (carvedilol, propranolol)
Dopamine
endo substrate, agonist, antagonist
- Dopamine
- Agonist action are many, includes renal, cardiac, and CNS effects; levodopa, pramipexole
- Antagonist action are many, renal, cardiac, and CNS; 1st gen antipsychotics (haloperidol, metoclopramide)
Serotonin
endo substrate, agonist, antagonist
- Serotonin
- Agonist action many includes platelet, GI, and psychiatric effects; triptans
- Antagonist action many includes platelet, GI, and psychiatric effects; ondansetron, 2nd gen antipsychotics (quetiapine)
Acetylcholinesterases
endo effects, drugs, drug action
- break down ACh
- Acetylcholinesterase inhibitors: donepezil, rivastigmine, galantamine
- Blocks acetylcholinesterase resulting in increased Ach levels. Used to treat Alzheimer’s disease
Angiotensin-converting enzyme (ACE)
endo effects, drugs, drug action
- Converts angiotensin 1 to angiotensin 2 (a potent vasoconstrictor)
- ACE inhibitors: lisinopril, ramipril, enalapril
- Inhibits prod of angiotensin 2 resulting in decreased vasoconstriction and aldosterone production. Used to treat HTN, HF, and kidney disease
Catechol-O-methyltransferase (COMT)
endo effects, drugs, drug action
- Breaks down levodopa
- COMT inhibitor: entacapone
- Blocks COMT enzyme to prevent peripheral breakdown of levodopa, resulting in increased duration of action of levodopa. Used to treak Parkinson disease
Cyclooxygenase (COX)
endo effects, drugs, drug action
- Converts arachidonic acid to prostaglandins (cause inflammation) and thromboxane A2 (causes platelet aggregation)
- NSAIDs (ibu, asa)
- Block COX enzyme to decrease prostaglandins and thromboxane A2; used to treat pain/inflammation and decrease platelet activation/aggregation (asa)
Monoamine oxidase (MAO) (endo effects, drugs, drug action)
- Breaks down catecholamines (DA, NE, Epi, 5-HT)
- MAO inhibitors: phenelzine, tranylcypromine, isocarboxazid, selegiline, rasagiline, methylene blue, linezolid
- Block MAO which increases catecholamine levels; used to treat depression
Phosphodiesterase (PDE)
endo effects, drugs, drug action
- Breaks down cyclic guanosine monophosphate (cGMP) a smooth muscle relaxant
- PDE-5 inhibitors: sildenafil, tadalafil
- Competitively binds to the same active site as cGMPon the PDE-5 enzyme, prevents breakdown of cGMP and prolonging the smooth muscle relaxation (e.g arteries of penis) used to treat erectile dysfunction
Vitamin K epoxide reductase
endo effects, drugs, drug action
- Converts vit k to the active form required for production of select clotting factors
- Warfarin
- Blocks vit k epoxide reductase enzyme which decreases production of clotting factors II, VII, IX, and X; used to prevent and treat blood clots
Xanthine Oxidase (endo effects, drugs, drug action)
- Breaks down hypoxanthine and xanthine into uric acid
- Allopurinol
- Blocks xanthine oxidase enzyme which decreases uric acid production; use to prevent gout attacks
Amide-type anesthetic
I before -caine
lidocaine, bupivicaine, ropivicaine
Ester-type anesthetic
benzocaine, procaine
Hydroxyl or alcohol
Neutral functional group
Ketone
Neutral functional group
Aldehyde
Neutral functional group
Amide
Neutral functional group
Nitrate
Neutral functional group
Nitro
Neutral functional group
Aromatic benzene ring
Neutral functional group
Urea
Neutral functional group
Carbonate
Neutral functional group
Carbamate
Neutral functional group
Ether
Neutral functional group
Thioether
Neutral functional group
Carboxyl
Acidic functional group
Phenol
Acidic functional group
Imide
Acidic functional group
Sulfonamide
Acidic functional group
Amine (primary)
Basic functional group
Amine (tertiary)
Basic functional group
Imine
Basic functional group
Amidine
Basic functional group
Amoxicillin
Bets-lactam, penicillin abx
Hypersensitivity: cross-reactive to other drugs with beta lactam ring (ceftriaxone and ertapenem)
Ceftriaxone
Beta-lactam, cephalosporin abx
Contains beta-lactam ring fused to 6 sided ring
Hypersensitivity: drugs with beta-lactam ring (amox and ertapenem)
Ertapenem
Beta-lactam, carbapenem abx
Contains beta-lactam ring fused to a 5 sided ring
Hypersensitivity: drugs with beta lactam ring
Aztreonam
Monobactam abx
Contains beta-lactam ring not fused to another ring
Hypersensitivity: not cross reactive to beta-lactam abx
Gentamicin
Aminoglycoside abx
Contains an amine group and sugar group
Sulfamethoxazole
Sulfonamide abx
Contains sulfonamide group
Hypersensitivity: cross reactive to other drugs containing sulfonamide group (celecoxib)
Aspirin
Salicylate nsaid
Contains acidic carboxyl group
Ibuprofen
NSAID
Contains a carboxyl group
Amphetamine
Stimulant
Contains a primary amine
Levothyroxine
Thyroid hormone (t4) Contains 4 iodine molecules
Amiodarone
Class III antiarrhythmic
Contains 2 iodine molecules
Fenofibrate
Fibrate, high cholesterol
Contains ketone groups
Amitriptyline
Tricyclic antidepressant
Contains 3 rings
Chlorpromazine
Phenothiazine antipsychotic
Contains thioether group