Term
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Definition
| The study of drugs and their effects on life processes |
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Term
| Identify and define the subdivision of pharmacology |
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Definition
Pharmacokinetics - What your body does to the drug
Pharmacodynamics - What the drug does to your body |
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Term
| List the different sources of drugs |
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Definition
| Natural (Plant alkaloids, microbes, minerals, Hormones) and synthetics (new compounds and modification of natural products) |
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Term
| Identify different types of pharmaceutical preparations |
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Definition
Crude drugs: obtained from natural sources (coffee, tea, opium)
Pure Drugs: Isolated from natural sources or synthesized in laboratory (morphine, insulin)
Pharmaceutical: Drugs intended for administration to patients |
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Term
| Compare enterel versus parenteral routes of administration |
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Definition
Enteral: involves absorption in GI tract
Parenteral: any route involving a needle
There are other routes as well (transdermal, inhalation, topical) |
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Term
| Differentiate between chemical name, generic name, and trade name |
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Definition
Chemical name is the entire formula name
Generic name is derived from the chemical structure, and is named by some government agency
Trade name is chosen by drug company |
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Term
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Definition
| What the body does to the drug |
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Term
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Definition
Absorption - how the drug gets into circulatory system
Distribution - process of drug leaving bloodstream and into organs and tissues
Metabolism - Transformation of drug into metabolites
Elimination - Removal of drug or its metabolites from the body |
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Term
| List the factors that affect Absorption |
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Definition
Solubility
Drug ionization
Formulation |
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Term
| List the factors that affect Distribution |
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Definition
Blood flow
Plasma protein binding
molecular size
specific tissue barriers |
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Term
| List the factors that can affect metabolism |
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Definition
Blood flow
plasma protein binding
Liver failure |
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Term
| List the factors that can affect elimination |
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Definition
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Term
| Distinguish routes of administration and how the route affects plasma concentrations |
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Definition
Oral administration - Drug usually has to pass liver first (first-pass metabolism), clearing out up to 70% of drug concentration.
Parenteral administration: Drug is administered directly into bloodstream at 100% concentration
(this applies for transdermal as well) |
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Term
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Definition
| Fraction of the administered dose of a drug that reaches systemic circulation |
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Term
| What is the main thing that affects bioavailability |
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Definition
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Term
| Define volume of distribution |
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Definition
The measure of the apparent space in the body available to contain the drug
and/or
a volume that represents the relationship between the dose of a drug and the resulting plasma concentration of the drug |
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Term
| A low volume of distribution means the drug is ____________ |
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Definition
| mostly retained in the vasculature |
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Term
| A high volume of distribution means the drug is ____________ |
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Definition
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Term
| If the drug is mostly retained in the vasculature, you would have a ____________ volume of distribution |
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Definition
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Term
| If the drug is mostly retained in the tissue, you would have a ____________ volume of distribution. |
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Definition
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Term
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Definition
| The volume of body fluid from which a drug is removed per unit of time |
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Term
| With glomerular filtration, your creatinine clearance would be ________________ to renal clearance |
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Definition
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Term
| With tubular secretion, your creatinine clearance would be _________________ to renal clearance |
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Definition
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Term
| With tubular reabsorption, your creatinine clearance would be ___________________ to renal clearance |
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Definition
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Term
| Define rate of elimination |
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Definition
| The amount of the chemical that is removed by metabolism and/or excretion per unit of time |
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Term
| What is the primary different between clearance and elimination? |
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Definition
| Clearance is the volume of drug that is removed, elimination is the amount of drug that is removed |
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Term
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Definition
| Elimination half-life is the time required to reduce the plasma drug concentration by 50% |
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Term
| Define Steady state concentration |
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Definition
| The dosage at which the rate of drug administration equals the rate of drug elimination |
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Term
| Approximately how many half-lives is required to remove the drug from the system |
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Definition
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Term
| The TIME to reach steady state concentration is independent of __________, but dependent on __________ |
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Definition
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Term
| The VALUE of steady state concentration is dependent on _____________ and ______________ |
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Definition
| dose; dosing interval frequency |
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Term
| Define first order elimination |
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Definition
| The amount of drug eliminated per unit time is proportional to concentration |
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Term
| Define Zero order elimination |
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Definition
| steady rate of drug elimination. System can only eliminate a constant amount per unit of time. |
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Term
| What form of elimination removes the drug faster? |
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Definition
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Term
| What are some variations that can alter pharmacokinetics? |
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Definition
| Age, Weight, Sex and percent body fat, genetic variation, and presence of disease |
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Term
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Definition
The study of the detailed mechanism of action by which drugs produce their pharmacologic effects
What the drug does to the body |
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Term
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Definition
| A drug that binds to physiological receptors |
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Term
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Definition
| Drugs that block or reduce the action of an agonist and have no physiological effect alone |
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Term
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Definition
| Partly effective as agonists regardless of drug concentration. Does not reach maximum effect |
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Term
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Definition
| Effectively turns off active receptors to make them stop producing an effect |
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Term
| Define competitive antagonist |
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Definition
| Competitive antagonists bind to receptors at the same binding site (active site) as the endogenous ligand or agonist, but without activating the receptor. |
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Term
| Define irreversible antagonists |
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Definition
| Ligands or other molecules that bind permanently or almost permanently to a receptor (rate of dissociation is effectively zero at relevant time scales) |
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Term
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Definition
Tendency of a drug to combine with its receptor.
Measure of strength of the drug-receptor complex
"strength of the reversible interaction of drug and receptor" |
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Term
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Definition
| The higher the affinity, the higher the selectivity. 1000x greater for one receptor over another. Prefers only type of receptor that can be found anywhere in the body. |
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Term
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Definition
Drugs that interact with a single type of receptor expressed on a limited number of cells have a high specificity
"This drug works on this receptor, on this cell type, in this location of the body" |
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Term
| Explain the difference between selectivity and specificity. |
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Definition
Drug selectivity is talking about what receptor the drug binds to. Drug specificity is talking which organ it acts upon.
A drug is highly selective when it works on only one type of receptor, no matter where it is.
A drug is highly specific when it acts on only one type of receptor in one specific part of the body. |
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Term
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Definition
Characteristic of drug action used for comparing different drug agents
"Amount of a drug that is needed to produce a specific effect." |
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Term
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Definition
The ability of a drug to initiate a cellular effect
"Maximum effect that a drug can produce |
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Term
| What is surmountable antagonism? |
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Definition
| It is a rightward shift in the dose-response curve created when you have a fixed antagonist concentration and an increase in agonist concentration. |
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Term
| Surmountable antagonism is seen in what type of antagonism? |
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Definition
| Competitive or reversible |
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Term
| What is insurmountable antagonism |
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Definition
| When you see a decrease in available receptors for agonist binding, and you increase the concentration of the agonist, you'll get a decrease in maximal efficacy. |
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Term
| Insurmountable antagonism is seen in what type of antagonism? |
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Definition
| noncompetitive or irreversible |
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Term
| Define allosteric antagonism |
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Definition
| Interacts with other sites on the receptor aside from the primary site |
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Term
| Define physiological antagonism |
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Definition
| Two agonists bind different receptors and the subsequent responses oppose each other. |
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Term
| Define chemical antagonism |
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Definition
| when the antagonist interacts directly with the agonist, preventing it from binding to a receptor. |
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Term
| What are the major types of receptors? |
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Definition
| Intracellular receptors, Ligand-regulated transmembrane enzymes, G proteins receptors, cytokine receptors, and ligand-gated ion channels |
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Term
| How do intracellular receptors work and what are some examples? |
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Definition
ligand diffuses through membrane, interacts with receptor inside cell.
Steroids and Thyroid hormone |
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Term
| How do ligand-regulated transmembrane enzymes work? |
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Definition
The enzyme lies embedded in the cell wall. Ligand interacts with extracellular surface, producing an effect on the intracellular side.
Some examples include insulin, EGF, and PDGF |
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Term
| Ligand-gated ion channels |
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Definition
| Ligand attaches to receptor, opening a channel in the enzyme that regulates the flow of ions across the membrane. Results in depolarization or hyperpolarization of cell. |
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Term
| How do G proteins and second messengers work? |
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Definition
| Ligand binds to GPCR, which causes it to undergo conformation change. alpha subunit exchanges GPP for GTP, dissociates from complex, and regulates target proteins. Beta-gamma subunits also move to regulate other proteins. |
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Term
| List the receptors that Gs acts for and what it's effector/signaling pathway is. |
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Definition
| Gs acts as a stimulant and is found in receptors for B-adrenergic amines, histamine, serotonin, and many hormones. It increases adynylyl cyclase and CAMP. |
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Term
| List the receptors that Gi1, Gi2, and Gi3 G proteins work for and what its effector/signaling pathway is. |
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Definition
| Gi1, Gi2, and Gi3 G proteins are inhibitors, and work for a2-adrenergic amines, ACh, opioids, and serotonin. It acts by decreasing adenylyl cyclase and cAMP. It also opens cardiac K+ channels and decreases heart rate. |
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Term
| What receptors does the G protein Gg work for and list the effector/signaling pathway for it. |
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Definition
| Gg works on ACh, serotonin, and many others by increase PLC, IP3, DAG, and cytosolic Ca2+. |
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Term
| Define signal transduction |
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Definition
Signal transduction is the overall process of a transmission of molecular signals from the cell's exterior to its interior.
If receptor is a g-protein carrier receptor, this will also amplify the signal. |
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Term
| Define secondary messengers |
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Definition
Secondary messengers are molecules inside cells that act to transmit signals from a receptor to a target protein.
Adenylyl cyclase and cAMP are secondary messengers |
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Term
| Define receptor desensitization |
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Definition
| Reduced effect after prolonged exposure to the same drug concentration by reducing the number of receptors on a molecule, reducing its sensitivity. |
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Term
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Definition
Usually follows withdrawal from a long-term receptor stimulation, its a massive increase in the number of receptors making the cell super sensitive to an agonist.
Can lead to withdrawal in the patient. |
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Term
| What are the assumptions of the dose-response relationship |
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Definition
- Intensity of a response is proportionate to number of occupied receptors
- one drug molecule per one receptor
- Amount of drug binding to receptor is very small compared to the amount of the drug in system
- Binding is usually reversible and of short duration
- Binding of one receptor won't affect other receptors
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Term
| Describe the overall anatomy of the ANS |
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Definition
| The ANS is divided into two subcategories, the sympathetic nervous system and parasympathetic nervous system. This is also known as the thoracolumbar division and craniosacral division. |
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Term
| What is another name of the sympathetic division of the ANS |
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Definition
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Term
| What is another name of the parasympathetic division of the ANS |
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Definition
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Term
| What nerves compose the thoracolumbar division? |
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Definition
Thoracic nerves T1-T12
Lumber nerves L1 and L2 |
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Term
| What nerves compose the craniosacral division? |
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Definition
Cranial nerves 3, 7, 9, 10.
Sacral nerves 2-4 |
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Term
| How does the length of the pre and postganglionic processes differ between the two divisions of the ANS |
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Definition
Sympathetic: pre/postgang neurons are somewhat equal in length.
Parasympathetic: pregang neurons travel to just short of target organ, postgang neuron travels into organ.
"You go 90, she goes 10" - Hitch |
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Term
| Where is epinephrine produced and released |
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Definition
| Epinephrine is only made in the adrenal medulla |
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Term
| Where is norepinephrine produced and released |
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Definition
| Norepinephrine is produced in both the adrenal medulla as well as the terminal of neurons. |
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Term
| What is the ratio of EPI and NE produced by the adrenal medulla |
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Definition
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Term
| Where is acetylcholine produced and released |
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Definition
| ACh is synthesized and released in the terminal of neurons. ; |
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Term
| True or false: All preganglionic fibers are cholinergic |
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Definition
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Term
| True or False: All postganglionic fibers in the parasympathetic division are adrenergic |
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Definition
False.
All or almost all postganglionic fibers in the parasympathetic division are cholinergic. |
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Term
| In the sympathetic division, most postganglionic fibers are adrenergic. Name the exception. |
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Definition
| Postganglionic fibers to the sweat glands are cholinergic. |
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Term
| True or false: Most postganglionic fibers in the sympathetic division are cholinergic. |
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Definition
False
Most postgang fibers are adrenergic. |
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Term
| What are some fight or flight responses you would see? |
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Definition
Pupil dilation
Salivary (thick mucus), sweat, and apocrine secretion
Decrease in digestion/increase in sphincter tone
HR and contractility increase
Vasoconstriction |
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Term
| What are some rest and digest responses you would see? |
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Definition
Pupil constriction/accommodation (focusing)
Salivary (watery) secretion, baseline sweat/apocrine secretions
Increase in digestion
HR and contractility decreases
Blood vessels remain at baseline. |
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Term
| What is the enzyme that synthesizes acetylcholine |
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Definition
choline acetyltransferase (ChAT)
synthesized from choline and acetyl Co-A |
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Term
| What is the enzyme that synthesizes NE/EPI |
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Definition
Dopamine B-hydroxylase converts dopamine into NE.
Phenylethanolamine-N-methyltransferase converts NE to EPI |
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Term
| What molecule does NE and EPI both originate from |
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Definition
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Term
| What is the termination mechanism for acetylcholine? |
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Definition
| ACh is terminated by Acetylcholinesterase (AChE) to produce Acetate and Choline, the later of which is reabsorbed into synapse. |
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Term
| What is the termination mechanism of NE/EPI? |
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Definition
| NE/EPI will bind to recepters, and then either be recycled into synapse by transporter or is broken down by MAO or COMT |
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Term
| What are the major subtypes of muscarinic receptors? |
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Definition
M1-M5
G-protein coupled receptors |
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Term
| What are the major effects of muscarinic receptors? |
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Definition
M1, M3, M5 receptors are simulators
M2 and M4 are inhibitors
These receptors stimulate and inhibit certain things depending on receptors. |
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Term
| What are the major subtypes of nicotinic receptors? |
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Definition
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Term
| What are the major effects of nicotinic receptors |
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Definition
| Mainly responsible for depolarizing cells. Both open NA+ and K+ channels. |
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Term
| What are the major subtypes of adrenergic receptors? |
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Definition
A1, A2, B1, B2, B3
G-protein coupled receptors |
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Term
| What are the major effects of alpha receptors |
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Definition
Alpha receptors are responsible for: vasoconstriction,
iris dilation,
intestinal sphincter contraction,
pilomotor contraction,
bladder sphincter contraction,
and inhibits neurotransmitter release. |
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Term
| What are the major effects of beta receptors |
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Definition
Beta receptors are responsible for:
Vasodilation
Increased HR/contractility
Intestinal/utero relaxation
Bronchodilation
Calorigenesis
Glycogenolysis, lipolysis, bladder wall relaxation, thermogenesis |
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Term
| True or false: NE has a higher affinity for alpha receptors compared to beta receptors? |
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Definition
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Term
| True or False: EPI has a higher affinity for beta receptors than for alpha receptors? |
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Definition
False
EPI has equal affinity for alpha and beta receptors. |
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Term
| True or False: EPI is more effective than NE at Beta receptors |
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Definition
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Term
| Define sympathetic and parasympathetic tone |
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Definition
| Sympathetic and parasympathetic systems are constantly activated. Their basal rates are considered the tone. |
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Term
| What is the value of sympathetic and parasympathetic tone? |
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Definition
| The value of tone is simply the ability of the systems to both increase and decrease activity |
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Term
| Give an example of sympathetic and parasympathetic tones |
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Definition
Sympathetic tone maintains arteriole constriction to 1/2 max diameter and adjusts when needed.
Parasympathetic tone maintains movement in the GI tract, and adjusts when needed. |
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