PHARMACODYNAMICS 3

Question 1

Receptor protein that forms a part of a ligand-gated ion channel

Answer 1

Type 1 Receptor - Ionotropic receptors

Question 2

Characteristics of Ionotropic receptors

Answer 2

Controls movement of ions
Found in cell membranes
Stimulated in milliseconds

Question 3

Type 1 - ionotropic subunit that possess GTPase activity

Answer 3

Alpha subunit (guanosine phosphate - guanosine diphosphate)

Question 4

Receptors that control Chloride ions

Answer 4

GABA receptors

Question 5

GABA receptors are stimulated by drugs such as

Answer 5

Benzodiazepines (Anxiolytic drugs)
Barbiturates

Question 6

(T/F) nicotinic receptor are activated by acetylcholine and controls the entry of sodium

Answer 6

True

Question 7

Receptor type that produces secondary messengers or enzymes

Answer 7

Type II receptors - G-Protein linked receptors or metabotropic receptors

Question 8

Characteristics of type II receptors

Answer 8

Located in cell membrane
Onset is in seconds

Question 9

Examples of G-proteins

Answer 9

Gs -stimulates adenylyl cyclase, increase cAMP
Gi - inhibits adenylyl cyclase decrease cAMP
Gq - increases IP3, DAG, increase intracell calcium

Question 10

(T/F) muscarinic is type II receptor, while nicotinic is type I

Answer 10

True

Question 11

Receptor types with high affinity cell surface receptors, production of kinase

Answer 11

Type II receptors - tyrosine kinase-linked receptors

Question 12

Enzyme produced by insulin binding to a receptor

Answer 12

Glucokinase

Question 13

Examples of type 3 receptors

Answer 13

Imatinib - gastrointestinal stromal tumors
Gefitinib - epidermal growth factor
Erythropoietin receptor - hormone

Question 14

Also known as gene transcription-linked receptors

Answer 14

Type IV receptors

Question 15

Characteristics of Type IV receptors

Answer 15

Located in nucleus/cytosol (cytoplasm)
Onset is in hours
Affects the central dogma (cell division)

Question 16

Replication, Transcription, Translation

Answer 16

Replication - DNA -DNA
Transcription DNA - RNA
Translation - RNA synthesize protein

Question 17

Drugs that bind to type IV receptors

Answer 17

Corticosteroids
Mineralocorticoids
Sex steroids
Vitamin D
Thyroid hormone
Retinoids

Question 18

Refers to drugs able to bind (has affinity) and intrinsic activity

Answer 18

Agonist

Question 19

Drugs with affinity but not intrinsic activity (prevents agonist binding)

Answer 19

Antagonist

Question 20

Type of agonist with full response, and stimulates all different variants of receptors

Answer 20

Full agonist

Question 21

Agonist with less than expected response, and competitively inhibits full agonist response

Answer 21

Partial agonist

Question 22

(T/F) many drugs used as antagonist are partial agonist

Answer 22

True

Question 23

Agonist that bind to the same site as agonist and reverses (opposite effect) constitutive activity of receptors

Answer 23

Inverse agonist

Question 24

Examples of Inverse agonist

Answer 24

Ro 15-4513 (inverse agonist of benzodiazepine)

Question 25

Agonist capable of stabilizing inactive receptor confirmation

Answer 25

Inverse agonist

Question 26

Both active and inactive receptor confirmation

Answer 26

Classical antagonist

Question 27

Classification of Antagonist base on mechanism

Answer 27

Pharmacologic Physiologic Pharmacokinetics Chemical

Question 28

Mechanism antagonist that inhibits agonist by reacting with receptors or other parts of the effector

Answer 28

Pharmacologic Antagonist

Question 29

Pharmacodynamic antagonism effects opposite agonist by binding to same receptors. Examples of this are:

Answer 29

Histamine, Antihistamine, Propranolol (beta blockers) Catecholamines (beta agonist)

Question 30

Pharmacokinetic antagonist reduces the effect of one drug by altering the ADME. examples of this are:

Answer 30

Digoxin + Cholestyramine