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Pharm Y1 > The Medicine Semester 1 > Flashcards

The Medicine Semester 1 Flashcards

1
Q

What is the formula for molarity?

A
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2
Q

What is the formula for molality?

A
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3
Q

What is the formula for equivalents?

A

Eq= ionic valency x number of ions in solution

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4
Q

What shape and bond angle does an sp3 hybridised molecule have?

A

Tetrahedral shape with a 109 degree bond angle

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5
Q

What shape and bond angle does an sp2 hybridised molecule have?

A

Planar (trigonal) shape with a 120 degree bond angle

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6
Q

What shape and bond angle does an sp hybridised molecule have?

A

Linear shape with 180 degree bond angle

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7
Q

Which is more stable and why?

A

Staggered conformation is more stable

Less energy and reduced rotation as H atoms are as far away from eachother as possible

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8
Q

What is the dihedral/torsion angle?

A

The angle formed between two intersecting planes

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9
Q

In chair conformation which is preferred? Axial or equatorial?

A

Equatorial as it provides less steric strain

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10
Q

What causes E/Z isomerism and how are the isomers distinguished?

A

Lack of rotation around a double bond causes E/Z isomerism

If the two groups with the highest priority (largest molecular weight) are on the same side of the double bond, the Z isomer has formed.

If they are on opposite sides, it is the E isomer.

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11
Q

In optical isomerism how are the R/S isomers distinguished?

A

Group with the lowest priority (usually H should be drawn facing backwards

The three other groups should be numbered in order of priority, if the numbers read in a clockwise direction (1,2,3) it is the right handed (R) isomer

If they read in an anticlockwise direction, it is the left handed (S) isomer

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12
Q

What quantities are given for the differing solubilities?

(Think parts of solvent:1 part of solute)

A
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13
Q

Define solubility

A

The maximum amount of solid that can be dissolved

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14
Q

Define dissolution

A

The transfer of molecules from solid to liquid state

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15
Q

What is the common pharmaceutical name for the solvent within a drug?

A

The vehicle

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16
Q

What causes solubility to decrease?

A

Increased molecule size

With smaller surface area

With presence of hydrophobic regions

Presence and position of substituents

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17
Q

What other factors affect solubility?

A

Solid state (crystalline/amorphous)

Polymorph type

Salts and counter ions

Composition of aqueous media (buffer)

Ionic strength

Temperature

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18
Q

Define miscibility

A

Mutual solubilities within a liquid-liquid system

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19
Q

What is the dielectric constant?

A

It measures the ability of a substance to be able to store electrical energy within an electric field

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20
Q

What is the equation for Ka?

A
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21
Q

What is the equation for pH?

A
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22
Q

What is the equation for pKa?

A
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23
Q

What are the equations for % ionisation of weak acids and weak bases?

A
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24
Q

What is the relationship between pH and pKa at 99%, 50% and 1% ionised?

A
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25
Q

How is the pI calculated?

A

The average of pKa 1 and pKa 2 is taken

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26
Q

What is Ksp?

A

The solubility product= [+ions][-ions]

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27
Q

How do the solubilities of charged and uncharged compounds compare?

A

Charged compounds are more soluble in water

Uncharged compounds are typically soluble in organic solvents and cell membranes

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28
Q

Define an acid

A

An acid donates a proton

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29
Q

Define a base

A

A base is a proton acceptor

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30
Q

Pharmaceutically define a strong base

A

Protonated at physiological pH

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31
Q

What is a heteroatom?

A

An atom other than a carbon

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32
Q

What is a heterocycle?

A

A cyclic compound where one or more of the atoms in the ring are heteroatoms

33
Q

What is an alkaloid?

A

A natural product containing one or more nitrogen heteroatoms

34
Q

What property in particular do N-heterocycles show?

A

They are strong bases

35
Q

What is the role of a buffer?

A

To minimise change in pH upon the addition of a small amount of acid or base to the solution

36
Q

What is the most common combination for a buffer?

A

A weak acid and its conjugate base

37
Q

Define an isotonic cell

A

Concentration of solute is equal inside and out

38
Q

Define a hypertonic cell

A

The concentration of solute is higher outside the cell

39
Q

Define a hypotonic cell

A

The solute concentration is higher inside the cell

40
Q

Define osmolarity

A

Concentration of a solution i.e osmoles per litre

41
Q

Define an osmole

A

A particle dissolved in solution, regardless of charge, weight or size

42
Q

What is tonicity?

A

A measure of osmotic pressure exerted on a membrane- specific to membrane types

43
Q

What are the three known methods for adjusting tonicity?

A

Freezing point depression

Sodium chloride equivalent method

White-Vincent method

44
Q

What is the aim when adjusting tonicity?

A

The freezing point of the final solution must equate the freezing point of the physiological fluid in question

45
Q

What are the roles of intermolecular forces in receptors?

A

Stabilise receptor shape in water

Determine how receptor and small molecule react

Determine how small molecule and protein react

Insight into improvement of molecule and formulation

46
Q

Which residues within a peptide chain (alpha helix) form hydrogen bonds?

A

The -C terminus of i and the -N terminus of i+4

47
Q

What is the approximate strength of a hydrogen bond?

A

-5kcal/mol

48
Q

What is the approximate strength of the interactions within the protein backbone?

A

-8kcal/mol but is dependent on partner charge

49
Q

What is Wallace’s Rule and what does it mean?

A

Adding a G-C pair to a peptide chain will increase the melting point by 2 degrees

Adding an A-T pair to a peptide chain will increase its melting point by 4 degrees

Applies to segments up to 20 base pairs in length

50
Q

What is the strength of a salt bridge interaction at short range?

A

Approximately 10-100kcal/mol

51
Q

What particular interactions seek to minimise empty space?

A

Van der Waals

52
Q

What is the typical strength of vdW packing between two CH2?

A

Approximately 0.5kcal/mol

53
Q

What is pi-pi stacking?

A

Aromatic rings packing together

The larger the ring, the greater the interaction

54
Q

What happens if covalent bonds form between drug and receptor?

A

Pharmacological action is prolonged or possibly even irreversible

55
Q

How is a crystal formed?

A

Atoms or molecules closely pack together with non-covalent interactions in order to minimise potential energy, with this order repeating indefinitely

56
Q

What is the unit cell of a crystal?

A

The smallest division of the crystal that can be made without altering any properties or its chemical composition

57
Q

What are the three steps of crystal formation?

A
  1. Supersaturation- cooling or evapourating to form precipitant
  2. Nucelation- collision of molecules, seeding
  3. Crystal growth- continuous deposition of molecules on faces at a rate proportional to the difference in concentrations between bulk and crystal surface
58
Q

What is the relationship between the melting point and the crystal lattice?

A

A relatively weak crystal lattice will have a lower melting point

59
Q

What is the habit of a crystal?

A

The overall shape of the crystal

e.g. acicular, prismatic, lamellar

60
Q

What is the form of a crystal?

A

The number of faces it has

61
Q

What can alter the habit of a crystal?

A

Precipitation

pH

Impurities and excipients

Modifying the habit may affect its ability to flow as a solid

62
Q

What is polymorphism?

A

The ability of a substance to exist in different forms

63
Q

How many polymorphs will be stable?

A

Only one, the rest will be metastable

However, over time, they will all transform into the stable form

64
Q

Define a solvate

A

Solvent entrapped during crystallisation

65
Q

Define a hydrate

A

Entrapped water within a crystal when there is water in the solvent

66
Q

Define an anhydrate

A

Crystals containing no water or solvent

67
Q

What is a polymorphic solvate?

A

Solvent molecules that have bonded within the lattice which, when heated, recrystallise in new form

68
Q

What is a pseudopolymorphic solvate?

A

Solvent molecules that barely occupy voids and upon heating evapourate, without changing the shape of the lattice

69
Q

What is the aim of solid dispersion?

A

To reduce crystallinity and allow poorly aqueous soluble drugs to be held within an inert hydrophillic carrier

70
Q

What does the physical state of solid dispersion depend on?

A

Physiochemical properties of drug and carrier

Drug-carrier interactions

Preparation method

71
Q

What is the melting fusion preparation method for solid dispersion?

A

All components are heated above their melting point

Followed by mixing and cooling

72
Q

What is the solvent method of solid dispersion?

A

A common solvent must be found

A solution is then made

The solvent is then evapourated

73
Q

What are the benefits and disadvantages of amorphous solids?

A

No long range interactions between atoms or molecules

Higher molecular mobility

More readily solubilised, increasing bioavailability

Most materials can be prepared amorphously

Faster than crystallisation

Less stable, shorter half life

74
Q

What is a lead candidate in drug development?

A

A compound demonstrating a property likely to be therapeutically useful

75
Q

What is an active principle in drug development?

A

A compound isolated from a natural extract that is principally responsible for the pharmacological activity

76
Q

Define affinity

A

Strength with which compounds bind to a receptor

77
Q

Define efficacy

A

Measure of maximum biological effect resulting from binding of a compound to a receptor

78
Q

Define potency

A

Concentration of an agonist required to produce 50% of the maximum possible effect

Pharm Y1 (11 decks)

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