Notes in 02 PD

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Status	Last Update	Fields
Published	07/30/2024	Four Major Types of Receptors{{c1::Ionotropic receptors}}{{c1::Metabotropotropic receptors}}{{c1::Enzyme-linked receptors}}{{c1::Nuclear receptors}}
Published	07/30/2024	[QC] Time scale1. G-protein-coupled receptors2. Ligand-gated receptors{{c1::A}}
Published	07/30/2024	[QC] Time scale1. G-protein-coupled receptors2. Kinase-linked receptors{{c1::B}}
Published	07/30/2024	[QC] Time scale1. Kinase-linked receptors2. Nuclear receptors{{c1::C}}
Published	07/30/2024	{{c1::Specificity::Role of second messengers}} - Ligands activating the same signaling pathway produce the same effects in the same cell
Published	07/30/2024	{{c1::Diversity::Role of second messengers}} - Same signaling molecule can produce distinct responses in different cells
Published	07/30/2024	{{c1::Amplification::Role of second messengers}} - Each step will produce more effects than the previous ones
Published	07/30/2024	{{c1::Hom::Hom/Heter}}ologous desensitization - act on one receptor with one signal transduction mechanism
Published	07/30/2024	{{c1::Heter::Hom/Heter}}ologous desensitization - different cells with different signal transduction mechanisms that can cross with other cells
Published	07/30/2024	{{c1::Saturation::Characteristic of Drug-Receptor}} - Degree to which receptors are occupied
Published	07/30/2024	{{c1::Competition::Characteristic of Drug-Receptor}} - Ability of different molecules very similar in structure to combine with the same receptor
Published	07/30/2024	{{c1::Efficacy or Intrinsic Activity::Characteristic of Drug-Receptor}} - Degree to which a drug can produce the desired response; quantified by {{c1:…
Published	07/30/2024	{{c1::Potency::Characteristic of Drug-Receptor}} - Amount of drug required to produce 50% of the maximal response the drug is capable of inducing…
Published	07/30/2024	{{c1::Affinity::Characteristic of Drug-Receptor}} - Tendency of a drug to bind to the receptor
Published	07/30/2024	{{c1::Kd or Dissociation/Association constant of a drug}} - Concentration at which 50% of the receptors are occupied; how affinity is quantified
Published	07/30/2024	[VR]1. Kd2. Affinity{{c1::B}}
Published	07/30/2024	EC50 involves a {{c1::single::single/quantal}} dose-response curve and is used when the response {{c1::can::can/cannot}} be graded
Published	07/30/2024	ED50 involves a {{c1::quantal::single/quantal}} dose-response curve and is used when the response {{c1::cannot::can/cannot}} be graded
Published	07/30/2024	{{c1::ED50}} - Concentration of drug which induces a specified clinical effect in 50% of subjects
Published	07/30/2024	{{c1::LD50}} - concentration of the drug which induces death in 50% of subjects; involves a quantal dose-response cruve
Published	07/30/2024	[VR]1. Therapeutic index2. Safety of the drug{{c1::A}}
Published	07/30/2024	[VR]1. Margin/Window of Safety2. Safety of the drug{{c1::A}}
Published	07/30/2024	[VR]1. Product of the concentrations of the reactants2. Rate of chemical reaction{{c1::A}}
Published	07/30/2024	{{c1::Receptor Occupancy}} Theory - Assumes that the magnitude of the response is proportional to the fraction of receptor sites occupied by the …
Published	07/30/2024	[QC] Priority in selecting drugs1. Potency2. Efficacy{{c1::B}}
Published	07/30/2024	[VR]1. Steepness of dose-response curve2. Safety of the drug{{c1::B}}
Published	07/30/2024	[VR] 1. Binding of an antagonist to a receptor2. Production of a response{{c1::C}}
Published	07/30/2024	State receptor model states that receptor can be in 2 forms: {{c1::Active (Ra) and inactive (Ri)}}
Published	07/30/2024	{{c1::Constitutive activity}} - Low activity of receptors even in the absence of the ligand
Published	07/30/2024	{{c1::Full}} Agonist - Agonist with maximal response (high affinity, high intrinsic activity) with full receptor occupancy
Published	07/30/2024	{{c1::Partial}} Agonist - Agonist with submaximal efficacy even with full receptor occupancy (high affinity, low intrinsic activity)
Published	07/30/2024	[QC] Affinity of Partial Agonist 1. Ra state2. Ri state{{c1::A}}
Published	07/30/2024	[QC] Affinity to Ra state1. Full agonist2. Partial agonist{{c1::A}}
Published	07/30/2024	[QC] Affinity of the neutral antagonist1. Ra state2. Ri state{{c1::C}}
Published	07/30/2024	[VR]1. Binding of inverse agonist2. Constitutive activity{{c1::B}}
Published	07/30/2024	[QC] Affinity of inverse agonists1. Ra state2. Ri state{{c1::B}}
Published	07/30/2024	[VR]1. Binding of a competitive antagonist2. Kd{{c1::A}}
Published	07/30/2024	[VR]1. Binding of a competitive antagonist2. EC50{{c1::A}}
Published	07/30/2024	Competitive antagonism reflects antagonism which is {{c1::r::ir/r}}eversible
Published	07/30/2024	[QC] Remedied by an increase in concentration of agonists1. Competitive antagonism2. Noncompetitive antagonism{{c1::A}}
Published	07/30/2024	[VR]1. Binding of a noncompetitive antagonist2. Kd{{c1::C}}
Published	07/30/2024	[VR]1. Binding of a noncompetitive antagonist2. EC50{{c1::C}}
Published	07/30/2024	[QC] Effective Response1. Binding of a full agonist only2. Binding of a full agonist with a partial agonist{{c1::A}}
Published	07/30/2024	Two exemptions to the Receptor-Occupancy Theory:{{c1::Partial agonistsSpare receptors}}
Published	07/30/2024	[QC] Presence of spare receptors1. Kd2. EC50{{c1::A}}
Published	07/30/2024	In the presence of irreversible antagonism with spare receptors:Initially: {{c1::Maximal::Sub/Maximal/Supra}} EffectOnce spared receptors are occupied…
Published	07/30/2024	{{c1::TD50/ Median Toxic Dose 50}} - dose at which 50% of the population manifests a given toxic effect
Published	07/30/2024	{{c1::TD50/ Median Toxic Dose 50}} - dose at which 50% of the population manifests a given toxic effect
Published	07/30/2024	Therapeutic index equation:{{c1::}}
Published	07/30/2024	Steps in Establishing Adverse Drug InteractionsStep 1: {{c1::Classify the type of drugs}}Step 2: {{c1::Classify the type of interactions}}Step 3: {{c1…
Published	07/30/2024	{{c1::Precipant/Interactant::Type of Drug}} - Drug which initiates the adverse drug interaction
Published	07/30/2024	{{c1::Object::Type of Drug}} - Drug whose interaction is affected in an adverse drug interaction
Published	07/30/2024	Three characteristics of Precipitant Drugs: {{c1::highly protein bound}}, {{c1::alter the metabolism of other drugs}}, {{c1::affect renal functio…
Published	07/30/2024	Two characteristics of object drugs: {{c1::steep dose-response curves}}, {{c1::low toxic-therapeutic ratio}}
Published	07/30/2024	{{c1::Pharmaceutical::Type of Drug Interaction}} - Physicochemical interactions either of a drug with an intravenous solution or two drugs in the…
Published	07/30/2024	{{c1::Pharmacodynamic::Type of Drug Interaction}} - Occurs when precipitant drug alters the effect of the object drug at its sites of action
Published	07/30/2024	{{c1::Pharmacokinetic::Type of Drug Interaction}} - Occurs when the absorption, distribution, metabolism, or excretion of the object drug is alte…
Published	07/30/2024	{{c1::Pharmacologic::Type of Direct Pharmacodynamic interaction}} - Interactions at the drug receptor, two drugs at the same receptor
Published	07/30/2024	{{c1::Physiologic::Type of Direct Pharmacodynamic interaction}} - interactions due to different cellular mechanisms acting in concert or in opposition…
Published	07/30/2024	{{c1::Indirect::Type}} pharmacodynamic interaction - Precipitant drug possesses an effect which is not directly related to the effects of the object d…
Published	07/30/2024	Identify the Type of Effect: {{c1::Summation/Addition}}1+1=2
Published	07/30/2024	Identify the Type of Effect: {{c1::Synergism}}1+1>2
Published	07/30/2024	Identify the Type of Effect: {{c1::Potentiation}}0+1 = >1
Published	07/30/2024	Identify the Type of Effect: {{c1::Antagonism}}1+1=<2 or 1+0=0
Status	Last Update	Fields