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Pharmacology > Pharmacodynamics Long Slide > Flashcards

Pharmacodynamics Long Slide Flashcards

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1
Q

Drugs interfere with the flow of ions through channels that are specific for these ions. What’s are these ion channels?

A

Na
K
Ca
Cl

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2
Q

What are the substances that block sodium channels?

What does the block prevent?

What are they used in?

A

Quinidine
Procainamide

Depolarization leading to nerve conduction block

Cardiac arrhythmias and as local anaesthetics

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3
Q

What drugs block the voltage gated calcium channels?

What are they used in?

A

Nifedipine
Verapamil
Diltiazem

Arrhythmias and hypertension

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4
Q

Blockade of Potassium channels leads to?

A

Prolonged refractory period

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5
Q

Potassium channel drugs include?

Which of them is used in arrhythmias?

A

Sulfonylurea
Amiodarone

Amiodarone

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6
Q

In chloride channels; upon activation, the — receptor selectively conducts Cl- through its pore resulting in — of the neuron which causes — effect on neurotransmission by — the chance of a successful AP occurring e.g —

A

GABA A
Hyperpolarization
Inhibitory
diminishing
Benzodiazepine

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7
Q

Transport of ions across cell membranes generally requires?

A

Carrier proteins

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8
Q

Inhibition of choline carrier is by?

A

Hemicholinium

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9
Q

Inhibition of noradrenaline vesicular uptake is by?

A

Reserpine

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10
Q

Inhibition of neuronal reuptake of Noradrenaline is by?

A

Desipramine

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11
Q

Inhibition of neuronal reuptake of serotonin is by?

A

Fluoxetine

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12
Q

Inhibition of weak acids carrier by drugs— which prevent uric acid tubular —— thus enhancing its ——

A

Probenecid
Reabsorption
Excretion

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13
Q

Drug receptors are regulatory ——

A

Macromolecular proteins

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14
Q

What are target sites for most drugs located on the cell membrane but could also be located intracellularly

A

Receptors

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15
Q

What is the specific chemical constituent of the cell with which drug interacts to produce its pharmacological effects?

A

Receptors

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16
Q

Receptor concept was attributed to the work of who?

A

Langley and Erlich… Late 1800-early 1900

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17
Q

What are ligands?

A

Ligands are substances that interact at the receptor binding site

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18
Q

Ligands are only exogenous

A

F….Could be exogenous or endogenous

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19
Q

Receptors are —— components of a cell with which a drug interacts to produce a response

A

Macromolecular

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20
Q

Drug-receptor interaction is lickened to what model?

A

Lock and key model

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21
Q

What are the characteristics of a receptor?

A

Sensitivity
Specificity
Selectivity
Saturation

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22
Q

What are the molecules serving as receptors?

Study These Flashcards
A

Membrane proteins(lipoproteins, glycoproteins)
Enzymes
Nucleic acid
Complex polysaccharide

23
Q

An agent which activates a receptor to produce an effect similar to that of the physiological signal molecule?

24
Q

Examples of agonists

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A

Adrenaline, noradrenaline, acetylcholine

25
An agent which prevents the action of an agonist on a receptor but has no effect on its own is called?
Antagonist
26
What is a partial agonist?
An agent which activates a receptor to produce submaximal effects but antagonizes the effect of a full agonist
27
Examples of antagonist?
Atropine Scopolamine Phenoxybenzamine
28
An agent which activates a receptor to produce an effect in the opposite direction to that of the agonist is?
Inverse agonist
29
Endogenous substances
Adrenaline Noradrenaline Glutamate Aspartate GABA Ach
30
Examples of inverse agonist?
Beta carbolines
31
The tenacity by which ligands bind to its receptor is called?
Affinity
32
Some drugs possess EFFICACY but not AFFINITY
False. It’s the opposite
33
The capacity to induce functional change in the receptor in a way that produces effect is known as?
Intrinsic activity
34
In terms of Affinity and Intrisic activity classify Agonist, antagonist, PA, IA
Agonist: 1 Antagonist: 0 Partial agonist:IA between 0 and 1 Inverse Agonist:IA between 0 and -1
35
What are the Drug receptor binding forces?
Covalent bond Ionic bond Hydrogen bond Van-der-waals
36
What type of force do most drugs employ?
Ionic bond
37
What force has a bond that is strong and not reversible under biological conditions Examples?
Covalent bond Organophosphate and anticholinesterases
38
Specific conformational perturbation(by agonist) leads to no biological response. T/F
False. Leads to one
39
Non-specific conformational perturbation(antagonist) leads to no biological response
True
40
The idea that a response emanates from a receptor only when it is occupied by an appropriate ligand and the response is proportional to the fraction of occupied receptors is what theory?
Occupancy theory
41
The idea that a response emanates from a receptor in proportion to the kinetic state of onset and offset of a drug binding to the receptor is known as what theory?
Rate theory
42
In what theory is response proportional to the fraction of occupied receptor and intrinsic activity
Stephensons theory
43
In what theory is response a function of affinity and can maximum response be produced without 100% receptor occupation?
Ariens theory
44
In what theory is it said that the binding site is not necessarily complementary with ligand conformation? Nullifying the obsolete key and lock concept
Induced fit theory
45
What theory depends on drug-receptor complex dissociation?
Rate theory
46
What are the two essential functions of receptors?
Recognition of specific ligand Transduction of signal into response
47
What are the two domains on a receptor ?
Ligand binding domain Effectors domain
48
What receptor domain undergoes functional conformational change?
Effectors domain
49
What is not a hypothesis anymore?
Nature of receptors
50
What happens to cell surface receptors?
They remain floated in cell membrane lipids
51
Functions of a receptor are determined by?
Interaction between hydrophilic and lipophilic domains of the peptide chain within the drug molecule
52
About receptors; Non-polar hydrophobic portion of amino acid remain ——in —— while —— hydrophilic remain on cell surface
Buried Membrane Polar
53
What is the classical and oldest approach of receptor classification, based on potencies of selective agonist and antagonists – Muscarinic, nicotinic, alpha and beta adrenergic etc.
Pharmacological criteria
54
What criteria for reception classification has to do with basis for designation of subtype? Give examples
Tissue distribution Cardiac beta adrenergic receptor as beta1 and bronchial as beta 2

Pharmacology (7 decks)

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