Term
| Difference between Trade and Generic drug names |
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Definition
Trade: proprietary name used exclusively by a company
Generic: public nonproprietary name for a drug, approved by FDA |
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Term
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Definition
| The study of reaction of drugs in the body, including interactions between drugs |
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Term
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Definition
-The study of the mechanism of action (MOA) of drugs in the body
-Relationship between drug concentration and effect on the body |
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Term
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Definition
-Study of drug actions as it moves through the body
-How body effects the drug |
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Term
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Definition
| Any substance that brings about a change in biologic function through its chemical action |
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Term
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Definition
-The component of a cell or organism that interacts with a drug
-Initiates the chain of biochemical events leading to the drug’s observed effect |
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Term
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Definition
Molecule that binds to a receptor
Ex= hormone, neurotransmitter, drug, messenger molecule |
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Term
| Difference between a hormone and xenobiotic |
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Definition
-Hormone: Drug that is synthesized within the body
-Xenobiotic: Drug that is made of chemicals outside of the body |
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Term
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Definition
| Drugs that bind to and activate the receptor (directly or indirectly) |
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Term
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Definition
| How well it binds to the receptor |
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Term
| Difference between potency and efficacy |
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Definition
-Potency: Amount of drug necessary to elicit a response
-Efficacy: drugs ability to produce the maximal desired response (more important clinically) |
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Term
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Definition
-Toxin: poisons of biological origin
-Toxicology: study of harmful or poisonous effects of drugs |
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Term
| Difference btw full and partial agonist |
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Definition
-Full:Produces a full response at full receptor occupancy
-Partial Agonist: Binds to the receptor and activates the receptor but with less response than a full agonist
(Response will not equal the max response of a full agonist regardless of concentration) |
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Term
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Definition
| Binds to the receptor and prevents binding by other molecules |
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Term
| Difference between reversible and irreversible antagonists |
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Definition
-Reversible antagonists:
readily dissociate from their receptor
-Irreversible antagonists: form a permanent, irreversible (or nearly irreversible) chemical bond with their receptor |
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Term
| Competitive v. Non-competitive Antagonists |
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Definition
-Competitive Antagonist (reversible)
Concentration of agonists to antagonists determines the effect
Increasing the amount of agonist can reverse the effect of the antagonist and vice versa
-Non-Competitive Antagonist (irreversible) Binds to the receptor with such strong affinity that the receptor is no longer available to bind with an agonist regardless of the concentration
The receptor must be regenerated before an agonist effect can occur |
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Term
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Definition
-Process when normal cell receptor degradation exceeds the synthesis of new receptors
-Total number of cell surface receptors are reduced
-Responsiveness to drug is diminished |
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Term
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Definition
| The measure of the apparent space in the body available to contain the drug |
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Term
| What route of administration has 100% bio availability? |
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Definition
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Term
Advantage v. disadvantage of IV (R.o.A)
Route of Administration |
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Definition
-Advantage – Potentially immediate effects, emergency use
-Disadvantage – increased risk of adverse effect |
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Term
| Advantage v. disadvantage of IM (intramuscular) R.o.A. |
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Definition
-Advantage – appropriate for self administration (insulin)
-Disadvantage – can’t be used with anticoagulation therapy, can cause abnormal creatine kinase labs, not good for immobile pts |
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Term
| What types of R.o.A are painful? |
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Definition
| Intramuscular and subcutaneous |
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Term
| Advantage v. disadvantage of Subcutaneous (Sub Q) R.o.A. |
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Definition
Advantage – good for slow-release implants (birth control implants)
Disadvantage – may cause pain or necrosis |
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Term
| What route of admin avoids 1st pass effect |
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Definition
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Term
| What route of admin avoids 1st pass effect |
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Definition
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Term
| What Route of Admin is most convenience and has significant 1st pass effect |
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Definition
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Term
| What Route of Admin has a lesser 1st pass effect than oral? |
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Definition
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Term
| Which Route of Admin has a rapid onset? |
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Definition
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Term
| Which Route of Admin has a slow onset, bypass 1st pass, and long duration? |
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Definition
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Term
| Advantage v. disadvantage of Sublingual (SL)Route of Admin |
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Definition
-Advantage – oral venous system to SVC, by passes 1st pass effect (in liver)
-Disadvantage – few drugs can be used SL |
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Term
| Advantage v. disadvantage for Oral (PO) Route of Admin? |
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Definition
-Advantage – most common method, safest, & most economical
-Disadvantage – requires pt compliance, pt able to swallow, and GI absorption |
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Term
| Advantage v. disadvantage of Rectal Route of Admin? |
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Definition
-Advantage – good when pt can’t take meds PO
-Disadvantage – irregular and incomplete absorption of some drugs |
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Term
| Advantage v. disadvantage of Inhalation Route of Admin? |
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Definition
Advantage – drug directly to the area drug is needed
Disadvantage – incorrect pt use decreases availability of drug |
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Term
| Advantage v. disadvantage of Transdermal Route of Admin? |
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Definition
| Disadvantage – not all drugs can penetrate the skin, can’t be use on open wounds |
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Term
T/F
Majority of drugs bind to receptors but not all |
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Definition
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Term
| Characteristics of receptors |
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Definition
| -Specific or selective, binding results in an alteration ob biologic system, intracellular or on cell surface, usually interacts with macromolecules to produce a response, magnitude of response if proportional to # drug-receptor complexes |
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Term
| General rule of receptors: As the dose of a drug goes up its selectivity.... |
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Definition
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Term
| Function of Ion Channel receptors |
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Definition
| Facilitate rapid movement of ions across cell membrane down their electrochemical gradient |
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Term
| Types of Ion Channel receptors |
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Definition
-Ligand-gated ion channels: Transition between states in response to binding to ligands
-Voltage-gated ion channels: Transition between states in response to changes in membrane potential |
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Term
| Types of Ligand-gated ion channel receptors |
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Definition
ACh (Muscarinic & Nicotinic)
Serotonin
GABA
Glutamate |
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Term
| Muscarinic M1 receptor location and function |
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Definition
Located in: CNS, Autonomic ganglia gastric and salivary glands, and enteric nerves
Function:
CNS - increase cognitive fxn (learning & memory) and increase seizure activity
Gastric, salivary and enteric: increases secretions |
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Term
| Muscarinic M2 ACh receptor location and function |
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Definition
Located in: CNS, heart, & smooth muscle
Function:
Heart – SA node to decrease HR; AV node to decrease conduction; atrium & ventricle to decrease contraction
Smooth muscle – increase contraction
CNS – increase tremors |
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Term
| Muscarinic M3 ACh receptor location and function |
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Definition
M3
Located in: smooth muscle and glands
Function:
Smooth muscle – increase contraction (bladder & lung)
Glands – increase secretions in salivary gland |
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Term
| Serotonin (5-HT) receptor |
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Definition
All are G-protein coupled receptors, except 5-HT3
Some are inhibitory
Activation of receptor may result in:
CNS-anxiety, Neuronal excitation, Emesis |
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Term
| What serotonin receptor is different from all others? |
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Definition
| 5-HT3 bc ligand-gated and excitatory |
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Term
| GABA (gamma-aminobutyric) receptors |
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Definition
-Widely distributed in CNS
-Inhibitory neurotransmitter in CNS
-purpose: control fear or anxiety experienced when neurons are overexcited
-Two classes of GABA receptors
GABA A - Ligand-gated ion channel receptor
GABA B - G-protein coupled receptor |
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Term
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Definition
2 categories responsible for fast sensory information processing in brain
Ionotropic receptors-ligand-gated ion channels
Metabotropic receptors-G protein coupled receptors |
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Term
| G-protein coupled receptors |
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Definition
Most abundant class of receptors
-Major role is to activate productiof of secondary messengers
(alpha, beta, gamma) |
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Term
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Definition
| Binding of ligand to the extracellular receptor domain activates or inhibits enzyme inside cell (ex. Tyrosine Kinase) |
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Term
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Definition
| Most common enzyme-linked receptor. Plays important role in DNA synthesis, insulin receptors, blood vessel formation |
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Term
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Definition
| Located intra cellular for drugs that can penetrate the membrane – steroids and thyroid |
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Term
| Types of receptors with unknown ligands |
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Definition
| Orphan receptors (alpha & beta -adrenergic) |
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Term
| Alpha 1A location and effects |
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Definition
Location: heart, liver, smooth muscle, blood vessels, lung, vas deferens, prostate, cerebellum, cortex, and hippocampus
Effects:
Contraction of vascular smooth muscle
Promotes cardiac growth
Vasoconstriction of large resistant arterioles in skeletal muscle |
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Term
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Definition
Location: kidney, spleen, lung, blood vessels, cortex, brainstem
Effects: promotes cardiac growth |
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Term
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Definition
Location: platelets, prostate, aorta, coronary artery, cortex, hippocampus
Effects: vasoconstriction in aorta and coronary artery |
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Term
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Definition
Location: platelets, sympathetic neurons, pancreas, coronary/CNS vessels, brainstem, spinal cord
Effects: inhibitory on sympathetic neuron and vasoconstriction of small vessels in skeletal muscle |
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Term
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Definition
Location: liver, kidney, blood vessels, coronary/CNS vessels, diencephalon, pancreas, and platelets
Effects: mediates a2 vasoconstriction |
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Term
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Definition
Location: basal ganglia, cortex, cerebellum, and hippocampus
Effects: inhibit hormone release from the adrenal medulla |
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Term
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Definition
Location: heart, kidney, skeletal m., olfactory m., cortex, cerebellar nuclei, brain stem, and spinal cord
Effects: heart - produces a positive inotropic and chronotropic effects (increase HR/contraction) |
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Term
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Definition
Location: heart, lung, blood vessels, bronchial & GI smooth muscle, kidney, skeletal m., olfactory bulb, cortex, and hippocampus
Effects: smooth muscle relaxation and skeletal muscle hypertrophy |
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Term
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Definition
Location: GI tract and heart
Effects: produces metabolic effects
(Austen said of no great significance) |
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Term
| Stages of testing with drug development |
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Definition
Preclinical - animal and In vitro studies
Clinic
Marketing |
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Term
| Phases with Human drug testing |
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Definition
All 3 clinical phases require patient consent
Phase 1 – Tested in 25-50 health volunteers (usually) to determine dose
Phase 2 – Tested in 10-200 patients with the disease to determine efficacy
Phase 3 – Tested in 1000’s to further establish safety and efficacy
All 3 clinical phases require patient consent
Phase 1 – Tested in 25-50 health volunteers (usually) to determine dose
Phase 2 – Tested in 10-200 patients with the disease to determine efficacy
Phase 3 – Tested in 1000’s to further establish safety and efficacy
All 3 clinical phases require patient consent
Phase 1 – Tested in 25-50 health volunteers (usually) to determine dose
Phase 2 – Tested in 10-200 patients with the disease to determine efficacy
Phase 3 – Tested in 1000’s to further establish safety and efficacy
Phase 4 – Postmarketing surveillance – monitors safety - no fixed duration |
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