PHARMACODYNAMICS 3 Flashcards
Receptor protein that forms a part of a ligand-gated ion channel
Type 1 Receptor - Ionotropic receptors
Characteristics of Ionotropic receptors
Controls movement of ions
Found in cell membranes
Stimulated in milliseconds
Type 1 - ionotropic subunit that possess GTPase activity
Alpha subunit (guanosine phosphate - guanosine diphosphate)
Receptors that control Chloride ions
GABA receptors
GABA receptors are stimulated by drugs such as
Benzodiazepines (Anxiolytic drugs)
Barbiturates
(T/F) nicotinic receptor are activated by acetylcholine and controls the entry of sodium
True
Receptor type that produces secondary messengers or enzymes
Type II receptors - G-Protein linked receptors or metabotropic receptors
Characteristics of type II receptors
Located in cell membrane
Onset is in seconds
Examples of G-proteins
Gs -stimulates adenylyl cyclase, increase cAMP
Gi - inhibits adenylyl cyclase decrease cAMP
Gq - increases IP3, DAG, increase intracell calcium
(T/F) muscarinic is type II receptor, while nicotinic is type I
True
Receptor types with high affinity cell surface receptors, production of kinase
Type II receptors - tyrosine kinase-linked receptors
Enzyme produced by insulin binding to a receptor
Glucokinase
Examples of type 3 receptors
Imatinib - gastrointestinal stromal tumors
Gefitinib - epidermal growth factor
Erythropoietin receptor - hormone
Also known as gene transcription-linked receptors
Type IV receptors
Characteristics of Type IV receptors
Located in nucleus/cytosol (cytoplasm)
Onset is in hours
Affects the central dogma (cell division)
Replication, Transcription, Translation
Replication - DNA -DNA
Transcription DNA - RNA
Translation - RNA synthesize protein
Drugs that bind to type IV receptors
Corticosteroids
Mineralocorticoids
Sex steroids
Vitamin D
Thyroid hormone
Retinoids
Refers to drugs able to bind (has affinity) and intrinsic activity
Agonist
Drugs with affinity but not intrinsic activity (prevents agonist binding)
Antagonist
Type of agonist with full response, and stimulates all different variants of receptors
Full agonist
Agonist with less than expected response, and competitively inhibits full agonist response
Partial agonist
(T/F) many drugs used as antagonist are partial agonist
True
Agonist that bind to the same site as agonist and reverses (opposite effect) constitutive activity of receptors
Inverse agonist
Examples of Inverse agonist
Ro 15-4513 (inverse agonist of benzodiazepine)
Agonist capable of stabilizing inactive receptor confirmation
Inverse agonist
Both active and inactive receptor confirmation
Classical antagonist
Classification of Antagonist base on mechanism
Pharmacologic
Physiologic
Pharmacokinetics
Chemical
Mechanism antagonist that inhibits agonist by reacting with receptors or other parts of the effector
Pharmacologic Antagonist
Pharmacodynamic antagonism effects opposite agonist by binding to same receptors. Examples of this are:
Histamine, Antihistamine, Propranolol (beta blockers)
Catecholamines (beta agonist)
Pharmacokinetic antagonist reduces the effect of one drug by altering the ADME. examples of this are:
Digoxin + Cholestyramine
