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MTC > Functional groups, ph, acid/base, absorption > Flashcards

Functional groups, ph, acid/base, absorption Flashcards

MTC wk 2

1
Q

For acidic drugs to pass through the membrane, what form must they be in?

A

neutral, unionised pronated form as HA

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2
Q

For basic drugs to pass through the membrane, what form must they be in?

A

neutral, un-ionised deprotonated form as B

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3
Q

If the pH is 1 unit away from pKa….

A

10% left

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4
Q

If the pH is 2 units away from pKa….

A

1% left

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5
Q

For ACIDIC functional groups, if the pH is LESS than pKa.

A

stays protonated as HA

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6
Q

For ACIDIC functional groups, if the pH is GREATER than pKa….

A

gets deprotonated (ionised) to A-

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7
Q

For BASIC functional groups, if the pH is LESS than pKa….

A

gets protonated (ionised) to BH+

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8
Q

For BASIC functional groups, if the pH is GREATER than pKa….

A

stays deprotonated as B

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9
Q

why will some molecules have more than one pKa?

A

If they have more than one charged/acidic/basic functional group

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10
Q

why is pH important in biological systems?

A

Vitally important as biochemical reactions and pathways can only occur/operate in optimal ranges of pH.

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11
Q

what is a buffer?

A

A solution that resits the change in pH

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12
Q

What buffers are used to regulate the pH of blood?

A

Bicarbonate, phospate and protien buffers

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13
Q

what is the equation for a bicarbonate buffer?

A

CO2 + H20 <->H2CO3 + H+

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14
Q

what is the equation for a Phosphate buffer?

A

H2PO4 + OH –> HPO4 + H2O

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15
Q

What happens if the pH of the surrounding medium is lower/higher than pKa

A

the functional group will become protonated or deprotonated

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16
Q

How do protein pump inhibitors manipulate pH of biological systems?

A

shut down stomach acid production and can have an affect on other drugs.

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17
Q

How does acidosis manipulate the pH of biological systems?

A

lowers blood pH via metabolic and respiratory acidosis.

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18
Q

what is Metabolic acidosis?

A

increased production of metabolic acids.

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19
Q

what is Respiratory Acidosis?

A

increase in blood CO2 (hypoventilation)

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20
Q

How does alkalosis manipulate the pH of biological systems?

A

increases blood pH via metabolic and respiratory alkalosis.

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21
Q

what is Respiratory Alkalosis?

A

loss of stomach acid from repeated vomiting.

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22
Q

What is Metabolic Alkalosis?

A

decreased blood CO2 (hyperventilation)

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23
Q

what are examples of drugs that can change the pH of the body and what do they do?

A

Asprin- lowers pH, and Antacids, increase pH of the stomach.

24
Q

what is the pH of a full stomach?

A

2-4

25
Q

What is the pH of an empty stomach?

A

1-1.5

26
Q

What is the pH of the intestine?

A

8-9

27
Q

what can happen if take medications with soft drinks?

A

may have a different effect on body as the pH of the soft drink interacts with the pH of the drug.

28
Q

What is the pH of plasma?

A

7.4

29
Q

Why can the ionisation of functional groups be misleading?

A

1st hydrophobic group compensates for 1st ionised function group, le chatlliers principle and ion channels,

30
Q

what functional group usually has the biggest impact on ionisation?

A

Carboxyl groups.

31
Q

what happens when ions disfavour absorption?

A

ions can’t cross non-polar phospholipd bilayer

32
Q

what happens when ions favour distribution?

A

ions dissolve easily in blood

33
Q

what is the impact of the acidic/basic/neutral nature of functional groups on absorption?

A

Determines where in the body it will be absorbed and how will interact with other drugs (cause potential side effects or make it ineffective)

34
Q

what is pKa (in terms of biochem)

A

strength of an acid/base according to the functional group

35
Q

For ACIDS, a smaller pKa

A

= stronger Acid

36
Q

For bases, larger pKa

A

= stronger base

37
Q

What are Prodrugs?

A

inactive compound that is converted into an active drug

38
Q

what may prodrugs do which is potentially bad?

A

mask problematic functional groups and cause toxic or ineffective drugs.

39
Q

What are the applications of prodrugs?

A

improve absorption, reduce toxicity (if processed correctly), remove bad taste and increase the duration of action.

40
Q

what is an example of a prodrug?

A

Salicylic acid- good painkiller but can cause gastric bleeding

41
Q

what are the two types of competitive inhibitors?

A

Reversible and irreversible

42
Q

what is an irreversible inhibitor and an example?

A

PERMENANT blocking of enzyme forming covalent bonds and changing the lock/key relationship. E.g. treatment for skin cancer that acts as a suicide for uracil and blocks the rapid reproduction of cancer cells.

43
Q

what is a reversible inhibitor?

A

TEMPORARY binding of drug through NON-COVALENT bonding.

44
Q

what is the role of enzyme inhibitors?

A

block enzymes as the drug interacts with target via functional groups.

45
Q

What are the acidic side chains?

A

aspartic acid, glutamic acid, cytesine and trysine

46
Q

what are the basic side chains?

A

arginine, hisidine and lysine

47
Q

if the pH is 3 units away from the pKa what happens?

A

100% of the molecule is changed

48
Q

if the pH is less than the pKa in an acidic solution what stays (when says 10% and 1%)

A

molecule stays protonated as HA

49
Q

if the pH is GREATER than the pKa in an acidic solution what stays (when says 10% and 1%)

A

stays deprotonated to A-

50
Q

if the pH is LESS than the pKa in an BASIC solution what stays (when says 10% and 1%)

A

protoanted to A-

51
Q

if the pH is GREATER than the pKa in an BASIC solution what stays (when says 10% and 1%)

A

stays deprotonated at B

52
Q

are acids proton donors or acceptors?

A

donors

53
Q

what is the impact that of functional groups on drug absorption?

A

Determines the charge state which impacts the absorption.

54
Q

When do acidic solutions become ionoised?

A

When the pH is greater then the pKA so becomes deprotonated

55
Q
A

MTC (14 decks)

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