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VPharma 101 > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

Define Pharmacodynamics

A

Studies of action of the drug from its interacrtion with receptors, to the effect on animal populations.

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2
Q

Types of Drug Targets

A
  1. Enzymes
  2. Carriers
  3. Ion Channels
  4. Receptors
  5. DNA and Nucleic Acid
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3
Q

Inhibition of this drug leads to suppression of proinflammatory prostaglandins

A

Cyclooxygenases

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4
Q

An enzyme that metabolizes ACh

A

Acetylcholine esterase

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5
Q

An enzyme that breaks down Trimetoprim and Acetylcholine

A

Dihydrofolate reductase

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6
Q

A type of drug target, also known as membrane transport systems

A

Carriers

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7
Q

Types of Neurotransmitters

A
  1. Endogenous
  2. Exogenous
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8
Q

A molecule or a polymeric structure on the surface / inside the cell that specifically recognizes and binds an endogenous compound.

A

Receptor

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9
Q

Moleculrs without signal transduction pathways, binding will not trigger a physiological response

A

Acceptor

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10
Q

Receptors posses an effector system also called?

A

signal-transduction pathways

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11
Q

A three-dimensional structure, forms pockets/grooves on the surface of protein that allowns specific interactions with compounds known as ligands

A

Binding site

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12
Q

Molecules of compilementary shape to the protein binding site, follows “locka and key” analogy

A

Ligands

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13
Q

A neurotransmitter that acts as molecular messenger, hormones are example of this neurotransmitter

A

Endogenous

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14
Q

A neurotransmitter that may produce a cascade of biochemical events that results in drug interaction, example: drugs

A

Exogenous

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15
Q

Drug Characteristics

A
  1. Intrinsic Activity
  2. Affinity
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16
Q

The property of drug that permits it to initiate post-receptor processes, which lead to a response

A

Intrinsic Activity

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17
Q

Ability of a drug to bind to its receptors

A

Affinity

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18
Q

Drugs that produce measurable pharmacological response and physiological response. Drugs that have both affinity and intrinsic ability.

A

Agonist

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19
Q

Types of Agonist Drugs

A
  1. Primary agonist
  2. Allosteric agonist
  3. Full agonist
  4. Partial agonist
  5. Inverse agonist
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20
Q

A drug that binds to the same site as the endogenous ligands

A

Primary agonist

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21
Q

A drug that binds to a different region of the receptor

A

Allosteric agonist

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22
Q

An agonist that produces a maximal effect under a given set of condition.

A

Full agonist

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23
Q

Drugs that bind to the receptor, suppressing the constitutive signaling activity

A

Inverse agonist

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24
Q

Drugs that are unable to trigger any action on their own but are able to block the action on other agonist, has affinity but no intrinsic activity. Also called “silent drugs”, most drugs are antagonist.

A

Antagonist

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25
Q

An interaction between 2 drugs such that the response of one drug (the agonist) is reduced in the presence of the second drug (the antagonist)

A

Antagonism

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26
Q

Types of Antagonism

A
  1. Receptor antagonism
  2. Physiologic antagonism
  3. Chemical antagonist
27
Q

Forms of Antagonism

A
  1. Competitive
  2. Non-competitive
28
Q

Occurs on same receptor protein such that two drugs compete and bind to the same receptor protein.

A

Receptor antagonism

29
Q

Occurs as a result of activating receptors with opposite phyiologic effect

A

Physiologic antagonism

30
Q

Occurs as a result of drug combining with 2 or more molecules via the formation of chemical bonds

A

Chemical antagonist

31
Q

Antagonist acts on the same receptor as the agonist, usually reversible, can be surmounted by increasing the concentration of the agonist

A

Competitive

32
Q

Occurs when the antagonist is bound covalently / irreversibly to its receptor binding site

A

Irreversible Competitive

33
Q

Refers to the situation where a drug blocks the cascade of events, normally leading to an agonist response at some downstream point

A

Non-competetive

34
Q

Ability of the drug to bind to its receptor

A

Affinity

35
Q

The drug’s ability, once bound, to initiate changes that lead to the production of responses. A property of a ligand/receptor pair.

A

Efficacy

36
Q

Define Potency

A

Coresponds to the concentration of drugs required to achieve a given effect.

37
Q

The maximum possible effct that can be obtained regardless of how large a dose is administered.

A

High Ceiling Effect

38
Q

Drugs that act only on single target. Linked to the nature of the drug-receptor interaction, considered rare.

A

Specificity

39
Q

Related to the concentration range of drugs. A drug may be specific at low concentration if it activates only one type of target whereas several targets may be involved simultaneously if the drug concentration is increased.

A

Selectivity

40
Q

Reversible Bonds

A
  1. Ioninc Bond
  2. Hydrogwn bond
  3. Van der Waals forces
41
Q

Strongest known non-covalent bond

A

Ionic bond

42
Q

An irreversible bond

A

Covalent bond

43
Q

A very tight bond, unable to dissosiate, rare

A

Covalent bond

44
Q

Activation leads to direct opening or closing an ion channel

A

Ionotropic Receptors

45
Q

Activation leads to some changes in metabolic processes within the cell. When activated, a series of intracellular events is first triggered that may also subsequently result in ion channel opening

A

Metabotropic receptors

46
Q

G-protein coupled receptor is also called?

A

Seven Transmembrane Receptors

47
Q

May act directly on an ionic channel or activate an enzymatic system to release a range of second messengers which ultimately permits certain ions to enter or leave the cell.

A

G-proteins

48
Q

A class of metabotropic cell surface receptors which exerts their regulatory effect by phosphorylating different effector proteins.

A

Tyrosine-Kinase Receptor

49
Q

Primary chemicals that act on RTKs

A

Hormones and growth factors

50
Q

Activates transmembrane ion channels , contains central pore (functions as ligand-gated ion channel)

A

Ionotropic receptors

51
Q

After binding the ligand, the activated receptors translocate to the nucleus and bind to a DNA sequence called the response element and initiate transcription of specific gene(s)

A

Transcription Factor Receptor

52
Q

The effect of the drug diminishes when it is given repeatedly

A

Tolerance and Tachyphylaxis

53
Q

Term used to describe a gradual decrease in responsiveness to chronic drug administration, can take from days to months

A

Tolerance

54
Q

An acute form of tolerance

A

Tachyphylaxis

55
Q

Common reasons for tachyphylaxis/tolerance

A

Pharmacodynamic mechanism: desensitization, loss of receptor, exhaustion of mediator
Pharmacokinetic mechanism: metabolism induction, active extrusion of the drug

56
Q

Tolerance phenomenon known for diuretics. Results from activation of the renin-angiotensin-aldosterone system and the parasympathetic nervous system

A

Braking Phenomenon

57
Q

Results from the chronic stimulation of receptors with drug results in a state of long term desensitization. Often due to a decrease in number of receptors.

A

Down Regulation

58
Q

Under stimulation of receptors (due to an increase in the number of receptors and a functional super sensitivity)

A

Up Regulation

59
Q

Four main levels of pharmacodynamic description

A
  1. Drug action
  2. Drug effect
  3. Clinical response
  4. The final drug effectiveness at the population level.
60
Q

The Four main levels of pharmacodynamic description are influenced by:

A
  1. Physiological factors
  2. Genetic Background of the animal
  3. The disease and its progression
  4. The treatment itself
61
Q

Define therapeutic window

A

A concept coined to describe the range of useful plasma concentrations in which expeced clinical response is obtained with minimal risk of adverse effect.

62
Q

Drugs with this therapeutic index requires drug monitoring to ensure treatment with a reaseonable margin of safety.

A

Narrow therapeutic index

63
Q

Drugs witht his therapeutic index allows more flexibility for the design of a dose regimen

A

Wide therapeutic index

64
Q

Define therapeutic index

A

a ratio that expresses the relationship between useful and toxic drugs.

VPharma 101 (7 decks)

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