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Drugs > EL2, EL3, EL4, EL5, EL 6 > Flashcards

EL2, EL3, EL4, EL5, EL 6 Flashcards

1
Q

What is cis and trans isomerism?

A

cis - same side

trans - opposite

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2
Q

what is an enantiomer?

A

pairs of molecules that are non-superimposable mirror images of each other

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3
Q

what are diastereoisomers?

A

molecules that are not mirror images but which differ in the orientation of one or more chiral centres

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4
Q

what are the types of enantiomers?

A

Enantiomers that rotate light in a clockwise direction are termed d- or (+) e.g. d-nicotine (+)-glutamate

Enantiomers that rotate light in a anticlockwise direction are termed l- or (-) e.g. l-nicotine (-)-glutamate

lower case d,l

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5
Q

how can you measure the rotation of polarized light?

A

The rotation of polarized light can be measured using a polarimeter

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6
Q

What is the D/L system?

A

confusing as fuck yo.

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7
Q

describe the R/S system/ the Cahn-Ingold-Prelog convention.

A

Identify the chiral centre. Usually, it will be a carbon with four different substituents.

Prioritise the substituents according to the atomic NUMBER of the atom connected to the chiral centre.

If two substituent atoms have the same atomic number, work your way out concurrently along the two chains until a point of difference is found. The priorities are then assigned at that point of difference. At the point of difference, priority is assigned on the basis of the highest atomic number. For example:
-CH2-Cl has higher priority than CH2-CH2-CCl3 because at the first point of difference, Cl has a higher atomic number than C.

If a double bond is present, treat it as two single bonds to the same type of atom

Once priorities have been assigned, orient the molecule so that the lowest priority group faces away from you.

If the other groups are arranged in clockwise descending order of priority, the chiral centre is in the R configuration.

If the other groups are arranged in an anticlockwise descending order of priority, the chiral centre is in the S configuration.

If they go from highest to lowest in anticlockwise order, then the molecule is S.

there is no fixed relationship between D/L and R/S.

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8
Q

what are constitutional isomers?

A

structural isomers.

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9
Q

what is the gaddum equation?

A

describes actinos of a comeptitive antagonist.

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10
Q

What is ED50?

A

the dose producing 50% of maximal response.

only used for drug responses measured in animals or man.

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11
Q

what is selectivity?

A

the ability of a drug to bind more tightly or activate more potently one receptor type compared to another.

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12
Q

what is pA2?

A

the concentration of a competitive antagonist such that the concentration of agonist is required to restore the original response.
theoretically it is equal to -log Ki.

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13
Q

what is non competitive antagonism? how does it affect the EC50?

A

binds to a receptor at another site to the agonist binding site.

EC50 for agonist unchanged but maximum response is decreased.
unsurmountable by agonist concentration.

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14
Q

what is IC50?

A

concentration of antagonist that reduces response to a particular concentration of agonist by 50%.

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15
Q

what is the hill langmuir equation?

A

relates binding of a drug to its concentration.

derived from the law of mass action.

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16
Q

what is Ki?

A

can define the affinity of a competitive antagonist
or
define the affinity of a ligand derived from a competition binding assay.

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17
Q

what are these units?

M
mM
uM
nM
pM
A

^3
^6
^9
^12

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18
Q

what is the gaddum equation?

A

describes action of a competitive antagonist. not copying that shit out.

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19
Q

how do you measure potency?

A

agonist - EC50

antagonist - pA2

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20
Q

what is Ki?

A

defines affinity of a ligand derived from a competition binding assay.

21
Q

what is pA2?

A

conc ratio.
conc of competitive antagonist so that twice the conc of agonist is required to get the original response.

theoretically equal to -log Ki.

22
Q

A condition or factor that increased the risk associated with taking a drug would be listed in the British National Formulary under the drug’s

A

cautions

23
Q

In primary (essential or idiopathic) hypertension, the cause is:

A

uknown

24
Q

Losartan is an inhibitor of or antagonist at:

A

angiotensin II receptors.

25
Q

An antagonist selective for β-adrenoceptors as opposed to α-adrenoceptors is:

A

propranolol.

26
Q

Enalapril exterts its therapeutic effects via:

A

inhibition of angiotensin converting enzyme (ACE)

27
Q

how to recognise an ACE antagonist?

A

ACE inhibitors can easily be recognised because they have the suffix -pril. Similarly, ATII antagonists e.g. losartan, all end in -artan.

28
Q

Propranolol causes bradycardia (slowing of the heart rate) via:

A

antagonist actions at β1 adrenoceptors

29
Q

a peptide hormone involved in renal salt and water balance:

A

angiotensin II.

30
Q

What is reteplase and streptokinase?

A

clot busting drug.
activates plasminogen.
can restore blood supply if given soon after a stroke or myocardial infarction.

31
Q

what is dipyridamole?

A

phosphodiesterase inhibitor.

stops breakdown of cAMP to reduce their aggregation.

32
Q

what is prostacyclin?

A

naturally occuring inhibitor of platelet aggregation, regulates coagulation.

33
Q

what is alteplase?

A

clot buster. activates plasminogen (precursor of plasmin).

34
Q

what is simvastatin?

A

statin to treat high cholesterol levels.

targets HMG-CoA reductase.

35
Q

what gene carries the K current needed to repolarise the membrane once an action potential has been fired?

A

ERG.

EAG in drosophilia gogo gene.

36
Q

what is long QT syndrome?

A

hERG mutation, changes in cardiac rhythm.
time between Q wave and end of T wave is lengthened.

can precipitate TdP - tachycardia.

usually comes from drugs interfering with hERG, not usually due to mutation.

37
Q

digoxin:

a. causes increased force of contraction of the heart
b. is a class III (Vaughan Williams) antidysrhythmic drug
c. is a cardiac glycoside
d. yields therapeutic effects across a narrow range of plasma concentrations

A

b

38
Q

class of digoxin?

A

unclassifed.

39
Q

Select a phosphodiesterase inhibitor that is used as a second-line treatment for heart failure:

a. dipyrimadole
b. dobutamine
c. metoprolol
d. milrinone

A

d.

Dipyridamole is also a phosphodiesterase inhibitor, but it is used as an antithrombosis drug. Dobutamine is a beta1 adrenoceptor agonist with weak beta2 activity. Metoprolol (as its olol suffix should tell you), is a beta blocker (beta1 selective).

40
Q

he component of the cardiac cycle during which blood flow to cardiac muscle occurs is:

A

diastole.

41
Q

Digoxin is used to treat cardiac failure. This drug:

a. competes for binding with Na+ ions on the Na+/K+-ATPase
b. is a positive inotropic agent
c. is obtained from deadly nightshade
d. prolongs the cardiac action potential

A

b

Good job! Positive inotropic agents increase the heart’s force of contraction. Digoxin binds to the sodium pump, but to the potassium site, not the sodium site. Digoxin is obtained from foxgloves. Atropine is obtained from deadly nightshade.

42
Q

Statement X: Organic nitrates decrease cardiac preload
Statement Y: Organic nitrates reduce cardiac oxygen demand

a. Statement X is false; statement Y is false
b. Statement X is false; statement Y is true
c. Statement X is true; statement Y is false
d. Statement X is true; statement Y is true AND X is NOT the reason for Y
e. Statement X is true; statement Y is true AND X IS the reason for Y

A

e

43
Q

Statement X: Digoxin binds to the same site as sodium on the sodium pump
Statement Y: The toxicity of digoxin is increased when plasma sodium levels are low

a. Statement X is false; statement Y is false
b. Statement X is false; statement Y is true
c. Statement X is true; statement Y is false
d. Statement X is true; statement Y is true AND X is NOT the reason for Y
e. Statement X is true; statement Y is true AND X IS the reason for Y

A

a

It is actually low POTASSIUM levels that increase the toxicity of digoxin - because digoxin competes with potassium for sites on the sodium pump.

44
Q

Statement X: Cardiac ischaemia results in the release of soluble pain signals such as K+, bradykinin and adenosine.
Statement Y: The pain from angina can frequently spread to the left shoulder or arm.

a. Statement X is false; statement Y is false
b. Statement X is false; statement Y is true
c. Statement X is true; statement Y is false
d. Statement X is true; statement Y is true AND X is NOT the reason for Y
e. Statement X is true; statement Y is true AND X IS the reason for Y

A

d

Both statements are true but the reason why pain is felt in the arm and shoulder is not due to soluble mediators from cardiac tissue entering the blood stream and travelling to other tissues. This type of pain is known as referred pain. There are several theories about how it arises but most suggest that there is some kind of convergence between sensory neurones from the heart and from the left side of the body that means that the CNS can’t tell exactly where the pain is coming from.

45
Q

Statement X: Loop diuretics reduce the body’s salt and water load
Statement Y: Loop diuretics are useful treatments for cardiac failure

a. Statement X is false; statement Y is false
b. Statement X is false; statement Y is true
c. Statement X is true; statement Y is false
d. Statement X is true; statement Y is true AND X is NOT the reason for Y
e. Statement X is true; statement Y is true AND X IS the reason for Y

A

e

Tissue and pulmonary oedema are common symptoms of heart failure (they are caused by a failure to return blood properly to the heart). These accumulations of fluid can be treated with diuretics, which increase loss of water and salt from the body.

46
Q

Statement X: Propranolol increases cardiac output
Statement Y: High dose propranolol is a useful emergency treatment for heart failure

a. Statement X is false; statement Y is false
b. Statement X is false; statement Y is true
c. Statement X is true; statement Y is false
d. Statement X is true; statement Y is true AND X is NOT the reason for Y
e. Statement X is true; statement Y is true AND X IS the reason for Y

A

a

Both are untrue. Propranolol decreases cardiac output by blocking sympathetic activity. This makes it a dangerous drug for patients with heart failure unless it is started very at low dose (when it can help).

47
Q

First-line treatments for angina of effort include:

A

beta blockers
organic nitrates
calcium channel blockers.

48
Q

incorrect answer:

Glyceryl trinitrate (GTN):

a. activates soluble adenylyl cyclase
b. is an example of a prodrug
c. is frequently prescribed in a sublingual formulation
d. is valuable in the treatment of angina pectoris

A

a

GTN activates soluble guanylate cyclase rather than adenylate. It is a prodrug (NO is the active principle), is prescribed as sublingual tablets to avoid liver metabolism, and is used to treat angina.

49
Q

Therapeutic strategies for cardiac failure include:

a. ACE inhibitors
b. angiotensin II agonists
c. diuretic drugs
d. organic nitrates

A

a, c, d.

Angiotensin II agonists would make things worse - they would cause vasoconstriction which would mean that the failing heart would have to work harder to pump blood.

Drugs (10 decks)

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