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Pharmacology > Introduction > Flashcards

Introduction Flashcards

1
Q

What is pharmacology

A

The study of the action of drugs on the function of living systems​

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2
Q

What is a drug

A

A chemical substance or natural product that affects the function of cells, organs, systems or the whole body (i.e. is bioactive)​

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3
Q

Where do drugs come from

A

-Natural products
-Serendipity (by accident)
-Changing structures of existing molecules
-Existing drugs on new diseases
-Computer aided design
-Studying disease processes

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4
Q

When was the first antibiotic discovered

A

Penicillium - 1928 (Flemming)
Isolated in 1938

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5
Q

Where does aspirin come from

A

Willow tree

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6
Q

What is Bothrops jararaca

A

Peptide which lowers BP- forerunner of ACE inhibitors
(comes from snake)

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7
Q

What is sildenafil

A

Drug re-purposed to create viagra

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8
Q

What are the types of drug names

A

Chemical
Generic
Proprietary

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9
Q

What is the ‘code-name’

A

Name given to drugs in development to disguise their identity

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10
Q

What is Pharmacokinetics

A

“what the body does to the drug”

Typically used as a generic term to describe the fate of a drug molecule following administration to a living organism or how a drug molecule is affected by exposure to living cells​

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11
Q

What is Pharmacodynamics

A

“what the drug does to the body”​

Typically used as a generic term to describe the mechanism of drug action or what happens to cells, organs, systems, etc., as a result of drug exposure​

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12
Q

What are the different routes of drug penetration into cells

A

Diffusion through lipid membrane
Diffusion through aqueous
channels
Carrier mediated transport
Pinocytosis

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13
Q

How does insulin reach the brain

A

Pinocytosis

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14
Q

What is the major transport route for lipophilic drugs

A

Diffusion through lipid membrane

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15
Q

How do water soluble drugs/hydrophilic drugs enter cells

A

Carrier-mediated transport

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16
Q

Can drugs pass through aqueous channels

A

Most are too large

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17
Q

What is lipinski’s rule of 5

A

A molecular mass less than 500 Daltons​

No more than 5 H-bond donors (total number of N-H and O-H bonds)​

No more than 10 H-bond acceptors (all nitrogen or oxygen atoms)​

An octanol-water partition coefficient log P not greater than 5

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18
Q

What is lipinski’s rule of 5 based on

A

Observation that most orally administered drugs are relatively small and moderately lipophilic molecules

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19
Q

What is AUC

A

Measure of the total exposure to the drug

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20
Q

How do drugs act

A

-Drugs are typically small chemical molecules
-Drug molecules exert a chemical influence on constituents of cells to produce a pharmacological response
-Drug molecules must get close enough to cellular constituents in order that they can interact chemically
-This interaction leads to an alteration in molecular / cellular function

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21
Q

Where must drug molecules bind to on cells

A

Drug Targets

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22
Q

What is Paul Ehrlich famous for

A

Nobel prize for Medicine in 1908

First treatment for syphilis; popularised the concept of the ‘magic bullet’

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23
Q

What does an antagonist drug do

A

Enters the binding site but will not have any effect however it prevents the agonist from entering and producing the normal signal

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24
Q

Why do we have receptors

A

For cell to cell communication

25
Q

What is a receptor

A

A recognition molecule for a chemical mediator through which a response is transduced
Often a protein or complex of two or more proteins and often expressed on the surface of cells (with some exceptions)
Histamine → histamine receptor(s)

Many drugs act to either mimic or block the effects of endogenous molecules at their receptors
Histamine receptor → blocked by anti-histamine drugs

26
Q

What is the basic receptor structure

A
  1. Extracellular domain
    Contains ligand binding sites
    Comprised of hydrophilic amino acids
  2. Transmembrane domain
    Anchors protein in membrane
    Comprised of hydrophobic amino acids

Typically has α-helical structure
3. Intracellular domain
Interacts with effector mechanisms
Comprised of hydrophilic amino acids

27
Q

What are the steps of signal transduction

A

Signal
Reception
Transduction
Response

28
Q

What is a very fast signalling receptor

A

Nicotinic acetylcholine

29
Q

What receptor may take days for signal transduction

A

Oestrogen

30
Q

What is a fast receptor

A

Muscarinic acetylcholine

31
Q

What receptor may be classified as slow due to the rate of signal transuction

A

Cytokine

32
Q

What is an agonist

A

a drug that binds to a specific site on a receptor, mimics the effect of the endogenous ligand for that site

33
Q

What is a ligand

A

Any chemical that binds to a receptor

34
Q

What is an antagonist

A

a drug that binds to a specific site on a receptor, blocks the effect of the endogenous ligand (same or different binding site as ligand)

35
Q

What is the difference between an agonist and antagonist drug

A

An agonist drug fits into the lock; mimics the action of the key; can be used to pick the lock and activate the receptor

An antagonist drug also fits into the lock; gets stuck and prevents opening of the lock (i.e. activation of the receptor) by either endogenous ligand or agonist

36
Q

What does an antagonist drug lack

A

Efficacy

37
Q

What would a low affinity drug mean

A

Binds briefly or is displaced by one with a higher affinity

38
Q

What does a low efficacy, high affinity drug result in

A

binds very strongly but ability to switch receptor on is very poor

39
Q

What is affinity

A

A measure of the strength of association between ligand and receptor

40
Q

What is efficacy

A

A measure of the ability of an agonist to evoke a (cellular) response

41
Q

What are the main causes of pharmacological variability

A

Age

Genetics

Disease state

Drug interactions

Environment

42
Q

What is pharmacological variability

A

Drug response is not always the same

Responses vary between people (i.e. inter-individual variability)

Responses vary within the same person (i.e. intra-individual variability)

43
Q

What is the difference between general and local anaesthetics

A

GENERAL
-Sedates entire body
-Loss of conciousness

LOCAL
-Sedates localised area
-No loss of conciousness

44
Q

What are the three main states of Na+ channels

A

Resting
Open
Inactivated

45
Q

How do local anaesthetics work

A

-Bind to target site on the intracellular side of the Na+ channel
-Prevents Na+ influx - prevents depolarisation - prevents action potential propagation-prevents perception of pain
-Prevents Na+ influx by blocking channel and stabilising it in inactivated conformation
-Causes REVERSIBLE BLOCK of nerve conduction

46
Q

What do LAs need to do to be effective

A

Diffuse from the site of administration, across the nerve cell membrane to the intracellular side

Bind to the LA target site

47
Q

What is the difference between ester and amide linked anaesthetics

A

ESTER
-rapidly metabolised by the tissue and plasme cholinesterases
-t1/2< 3 mins

AMIDE
-primarily metabolised slowly in the liver by P450 enzymes
-t1/2 1-3 hours

48
Q

What occurs when the pKa of the LA =pH of the solution

A

50% will be in its ionised form and 50% in its un-ionised form

49
Q

What is the range of LA pKa’s

A

7.6-9

50
Q

When do both ionised and neutral forms of the LA exist

A

pH 7.4

51
Q

Which anaesthetics are weak bases

A

Local anaesthetics

52
Q

What causes side effects of LAs

A

The escapeinto the systemic circulation from localised point

53
Q

What is usually administered along with a LA

A

Vasoconstrictor (adrenaline)

54
Q

Examples of LA

A

Cocaine
Procaine
Lidocaine
Tetracaine
Prilocaine

55
Q

What are the uses of different LAs

A

Epidural - Lidocaine, bupivacaine

Nerve block - Most LAs

Spinal anaesthia - Lidocaine

Topical - (mucous membranes only not skin) Lidocain, tetracaine, benzocaine

56
Q

What are the three things we should knowabout a drug

A

What it does - the response to the drug
Its potency
Its selectivity

57
Q

What is potency

A

A measure of the dose (or concentration) of a drug at which it is effective
A potent drug is one that is effective in low doses (concentrations)

58
Q

When is a drug selective

A

A DRUG IS SELECTIVE IF IT WORKS ON ONE RECEPTOR BUT NOT ON OTHERS

Pharmacology (3 decks)

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