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week 17 > the medicine > Flashcards

the medicine Flashcards

1
Q

What is the effect of temperature on stability?

A

temperature affect the rate of drug degradation by enhancing all chemical processes involved

Roughly a 10°C increase in temperature will produce a 2 to 3 fold increase in the rate of reaction

Can cause the Arrhenius equation to predict the effect of temperature on reaction rate

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2
Q

what is -Ea/R

A

gradient

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3
Q

what is InA

A

y intercept

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4
Q

strategies to increase stability (instability due to hydrolysis)

A

remove water - add a desiccant or change solvent
Lower water activity - add cosolvent
Reduce hygroscopic nature - change salt
Formulate as a solid - powder for reconstitution

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5
Q

strategies to increase stability (instability due to oxidation)

A

remove oxygen-store, and the nitrogen, carbon dioxide or helium

Buffer at PH3 to 4-oxidation is enhanced by anions

add an antioxidant-sodium metabisulphite

chelate metal ions-edetate disodium

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6
Q

strategies to increase stability (instability due to photo lysis)

A

Protect from light (packaging)

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7
Q

Strategies to increase stability (PH)

A

Store at a pH minimum

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8
Q

strategies to increase stability (temperature effects)

A

Store in cold places less than 15°C

Refrigerate (4°C)

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9
Q

Pharmacokinetic considerations in absorption rate

A

aqueous solutions are the best dosage form for rapid and predictable drug absorption from the gastrointestinal tract

But we need to consider solubility, stability, taste, and economic issues

Most patients still prefer solid dosage forms

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10
Q

give some examples of excipients in the formulation of solutions

A

Solvents
chelating agents
Colouring
Preservatives
Sweetening agents
Antioxidants
Clarification agents
Flavourings
Solubilising agents
Viscosity modifiers

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11
Q

Give examples of solvent from aqueous systems

A

water
Ethanol
Iso propanol
Polyethylene glycol
Propylene glycol
Glycerin

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12
Q

Give some examples of solvent for oily systems

A

isopropyl myristate
Mineral oil
Peanut oil
Corn oil
Cottonseed oil
Sesame oil

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13
Q

what are examples of antioxidants for aqueous systems

A

sodium metabisulphite
Ascorbic acid
Citric acid
Malic acid

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14
Q

Give examples of antioxidants for oily systems

A

butylated hydroxyanisole
butylated hydroxytoluene

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15
Q

give examples of chalating agents

A

edetate disodium

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16
Q

give examples of clarifying agents

A

bentonite

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17
Q

give examples of flavouring agents

A

bitter
sour
salty
sweet
anaesthetic: methanol/ peppermint oil

indigestion remedies associated with mint

may use flavour enhancers eg. citric acid for citrus fruits

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18
Q

What do you need to ensure when choosing a preservative?

A

that there is no adsorption of a preservative onto the container

efficiency is not impaired by the pH or other exceptions

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19
Q

What are solubilising agents?

A

use surface acting agents to form micelles

Surfactant concentration is key (toxicity or insufficient solubilisation)

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20
Q

What is the most widely used as a sweetener agent?

A

Low, molecular weight carbohydrates (sucrose)

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21
Q

What is the benefit of using viscosity modifiers?

A

they are especially useful for topical solution is placed on the skin, or in the eyes

Low concentrations of gelling agents can be used to increase the viscosity of the solution

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22
Q

what will parental solutions require?

A

Some specific excipients
buffers
Tonicity modifiers

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23
Q

What to do eyedrops require?

A

To be sterile

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24
Q

what is it important for nasal and ear products to be?

A

their viscosity is important

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25
Q

what is important for mouthwashes and gargles

A

taste

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26
Q

What is the importance of carbohydrates?

A

they are distributed widely in nature
They are key intermediate of metabolism (sugar)
They provide a range of cellular markers
Some are used as excipients

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27
Q

How many oxygen and carbons do carbohydrates roughly have

A

roughly equal number of each

28
Q

3 carbons

A

trioses

29
Q

4 carbons

A

tetroses

30
Q

5 carbons

A

pentoses

31
Q

6 carbons

A

hexoses

32
Q

7 carbons

A

heptoses

33
Q

what is the fischer projection

A

D or L configuration at the bottom

most oxidised group- CHO top, X-OH bottom

vertical substituents are away, horizontal, substituents are towards

34
Q

what’s aldose

A

contains an aldehyde and is a monosaccharide

35
Q

what is ketose

A

contains a ketone and is a monosaccharide

36
Q

what are the consequences of monosaccharide asymmetry

A

A carbon have in four different groups attached is asymmetric (Chiral)

Transporting any two of the groups on a chiral carbon results in a different compound with different physical properties

The number of allison this is 2^n where n is the number of asymmetric carbons

most sugars are therefore optically active
(can rotate a beam of plane polarised light)

37
Q

what are epimers

A

sugars that differ at a single asymmetric centre

38
Q

what are enantiomers

A

sugars that differ at all of that asymmetric centres and are mirror images

39
Q

what are diastereoisomers

A

sugars that differ at one or more chiral centres. And that are not enantiomers

40
Q

what are aldotetroses

A

they have two chiral centres

41
Q

what is cyclisation

A

a chemical reaction where a molecule undergoes a ring closing reaction

42
Q

what does pentose cyclisation form

A

pyranose rings

43
Q

what does hexoses cyclisation form

A

furanose

44
Q

what are anomers

A

intermolecular nucleophillic addition creates cyclic hemiacetals in sugars

formation of the cyclic hemiacetal creates an additional chiral centre giving two diastereoisomeric forms alpha and beta

these diastereoisomers are called anomers

45
Q

alpha monosaccharides

A

Hydroxyl group sits below the plane of the Ring (carbon one)

46
Q

Beta monosaccharides

A

Hydroxyl group sits above the plane of the Ring (carbon one)

47
Q

what is mutarotation

A

where the cyclic structure of a sugar molecule undergoes a rapid equilibrium between the alpha and beta anomers in aqueous solution

occurs due to the hydroxyl groups next to it rotate freely. therefore equilibrium can be shifted by external factors eg. them, pH, and []

48
Q

what is mannitol

A

it is used to prevent or treat excess body water in certain kidney conditions

Reduces swelling of the brain

Reduces pressure in the eye

It is an osmotic diuretic, it works by increasing the amount of fluid excreted by the kidneys, and helps the body to decrease pressure in the brain and eyes.

49
Q

what is sorbitol

A

it is a laxative

It is used to treat constipation

50
Q

what is a glycosidic bond

A

carbohydrates are joined to alcohols and amines at the anomeric centre by glycosidic bonds

51
Q

what is a disaccharide

A

combines a hydroxyl of one monosaccharide and an acetyl linkage with another monosaccharide C1 and C4

52
Q

what is lactose

A

a disaccharide that occurs naturally in milk

it is a reducing sugar

exhibits mutarotation

cleaved in digestion to glucose and galactose

53
Q

why is lactose a common excipient

A

used to help form tablets because it has excellent compress ability properties

It is used to formate diluent powder for dry powder inhalations

54
Q

what is mannose

A

a common excipient

55
Q

what is maltose

A

a common excipient

56
Q

what is sucrose

A

‘table sugar’
pure sucrose, a disaccharide that hydrolyses to glucose and fructose

does not undergo mutarotation

57
Q

what is glycogen

A

a polysaccharide that serves the same energy stronger function in animals that starch serves in plants

highly branched and larger than amylopectin

up to 100,000 glucose units

58
Q

what are amino sugars

A

they are found in antibiotics

occurs in cartilage

59
Q

what are grooves in DNA

A

the strands of the DNA double helix create two continuous grooves major and minor

major groove is wider and deeper

60
Q

what is aciclovir

A

a purine based antiviral drug acting against herpes
guanine base

the acyclic hydroxy ether substitutet mimics the sugar of the natural nucleoside

achiral - cheaper to make

acts as a chain terminator in viral DNA replication

61
Q

what is a chain terminator

A

nucleoside analogues which interfere with or halt DNA replication

eg Aciclovir

62
Q

what is interstrand

A

crosslinking can occur between two complementary strands of DNA

63
Q

what is intrastrand

A

crosslinking happening between a single strand of DNA (within a strand) as generated by cisplatin

64
Q

what is temozolomide

A

a pro drug against brain tumours discovered at aston

crossed the Blood brain barrier

undergoes chemical transformation to yield
the reactive methylating agent

65
Q

what is doxorubicin

A

an example of a DNA intercalator

66
Q

what is a DNA intercalator

A

they are molecules capable of fitting between nucleic acid base pairs

67
Q

what is the therapeutic difference between citerazine hydrochloride and di hydrochloride

A

There’s no therapeutic different apart from they are both stereoisomers

week 17 (3 decks)

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