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Pharmacology > Pharmacodynamics Long Slide > Flashcards

Pharmacodynamics Long Slide Flashcards

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?

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?

A

Agonist

24
Q

Examples of agonists

A

Adrenaline, noradrenaline, acetylcholine

25
Q

An agent which prevents the action of an agonist on a receptor but has no effect on its own is called?

A

Antagonist

26
Q

What is a partial agonist?

A

An agent which activates a receptor to produce submaximal effects but antagonizes the effect of a full agonist

27
Q

Examples of antagonist?

A

Atropine
Scopolamine
Phenoxybenzamine

28
Q

An agent which activates a receptor to produce an effect in the opposite direction to that of the agonist is?

A

Inverse agonist

29
Q

Endogenous substances

A

Adrenaline
Noradrenaline
Glutamate
Aspartate
GABA
Ach

30
Q

Examples of inverse agonist?

A

Beta carbolines

31
Q

The tenacity by which ligands bind to its receptor is called?

A

Affinity

32
Q

Some drugs possess EFFICACY but not AFFINITY

A

False. It’s the opposite

33
Q

The capacity to induce functional change in the receptor in a way that produces effect is known as?

A

Intrinsic activity

34
Q

In terms of Affinity and Intrisic activity classify Agonist, antagonist, PA, IA

A

Agonist: 1
Antagonist: 0
Partial agonist:IA between 0 and 1
Inverse Agonist:IA between 0 and -1

35
Q

What are the Drug receptor binding forces?

A

Covalent bond
Ionic bond
Hydrogen bond
Van-der-waals

36
Q

What type of force do most drugs employ?

A

Ionic bond

37
Q

What force has a bond that is strong and not reversible under biological conditions

Examples?

A

Covalent bond

Organophosphate and anticholinesterases

38
Q

Specific conformational perturbation(by agonist) leads to no biological response. T/F

A

False. Leads to one

39
Q

Non-specific conformational perturbation(antagonist) leads to no biological response

A

True

40
Q

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?

A

Occupancy theory

41
Q

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?

A

Rate theory

42
Q

In what theory is response proportional to the fraction of occupied receptor and intrinsic activity

A

Stephensons theory

43
Q

In what theory is response a function of affinity and can maximum response be produced without 100% receptor occupation?

A

Ariens theory

44
Q

In what theory is it said that the binding site is not necessarily complementary with ligand conformation? Nullifying the obsolete key and lock concept

A

Induced fit theory

45
Q

What theory depends on drug-receptor complex dissociation?

A

Rate theory

46
Q

What are the two essential functions of receptors?

A

Recognition of specific ligand
Transduction of signal into response

47
Q

What are the two domains on a receptor ?

A

Ligand binding domain
Effectors domain

48
Q

What receptor domain undergoes functional conformational change?

A

Effectors domain

49
Q

What is not a hypothesis anymore?

A

Nature of receptors

50
Q

What happens to cell surface receptors?

A

They remain floated in cell membrane lipids

51
Q

Functions of a receptor are determined by?

A

Interaction between hydrophilic and lipophilic domains of the peptide chain within the drug molecule

52
Q

About receptors;
Non-polar hydrophobic portion of amino acid remain ——in —— while —— hydrophilic remain on cell surface

A

Buried
Membrane
Polar

53
Q

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.

A

Pharmacological criteria

54
Q

What criteria for reception classification has to do with basis for designation of subtype?

Give examples

A

Tissue distribution

Cardiac beta adrenergic receptor as beta1 and bronchial as beta 2

Pharmacology (7 decks)

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