PHARMACODYNAMICS 3 Flashcards

1
Q

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

A

Type 1 Receptor - Ionotropic receptors

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2
Q

Characteristics of Ionotropic receptors

A

Controls movement of ions
Found in cell membranes
Stimulated in milliseconds

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3
Q

Type 1 - ionotropic subunit that possess GTPase activity

A

Alpha subunit (guanosine phosphate - guanosine diphosphate)

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4
Q

Receptors that control Chloride ions

A

GABA receptors

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5
Q

GABA receptors are stimulated by drugs such as

A

Benzodiazepines (Anxiolytic drugs)
Barbiturates

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6
Q

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

A

True

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7
Q

Receptor type that produces secondary messengers or enzymes

A

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

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8
Q

Characteristics of type II receptors

A

Located in cell membrane
Onset is in seconds

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9
Q

Examples of G-proteins

A

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

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10
Q

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

A

True

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11
Q

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

A

Type II receptors - tyrosine kinase-linked receptors

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12
Q

Enzyme produced by insulin binding to a receptor

A

Glucokinase

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13
Q

Examples of type 3 receptors

A

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

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14
Q

Also known as gene transcription-linked receptors

A

Type IV receptors

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15
Q

Characteristics of Type IV receptors

A

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

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16
Q

Replication, Transcription, Translation

A

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

17
Q

Drugs that bind to type IV receptors

A

Corticosteroids
Mineralocorticoids
Sex steroids
Vitamin D
Thyroid hormone
Retinoids

18
Q

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

A

Agonist

19
Q

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

A

Antagonist

20
Q

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

A

Full agonist

21
Q

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

A

Partial agonist

22
Q

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

A

True

23
Q

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

A

Inverse agonist

24
Q

Examples of Inverse agonist

A

Ro 15-4513 (inverse agonist of benzodiazepine)

25
Q

Agonist capable of stabilizing inactive receptor confirmation

A

Inverse agonist

26
Q

Both active and inactive receptor confirmation

A

Classical antagonist

27
Q

Classification of Antagonist base on mechanism

A

Pharmacologic
Physiologic
Pharmacokinetics
Chemical

28
Q

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

A

Pharmacologic Antagonist

29
Q

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

A

Histamine, Antihistamine, Propranolol (beta blockers)

Catecholamines (beta agonist)

30
Q

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

A

Digoxin + Cholestyramine