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week 17 > the medicine > Flashcards

the medicine Flashcards

(67 cards)

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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
what is important for mouthwashes and gargles
taste
26
What is the importance of carbohydrates?
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
27
How many oxygen and carbons do carbohydrates roughly have
roughly equal number of each
28
3 carbons
trioses
29
4 carbons
tetroses
30
5 carbons
pentoses
31
6 carbons
hexoses
32
7 carbons
heptoses
33
what is the fischer projection
D or L configuration at the bottom most oxidised group- CHO top, X-OH bottom vertical substituents are away, horizontal, substituents are towards
34
what’s aldose
contains an aldehyde and is a monosaccharide
35
what is ketose
contains a ketone and is a monosaccharide
36
what are the consequences of monosaccharide asymmetry
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
what are epimers
sugars that differ at a single asymmetric centre
38
what are enantiomers
sugars that differ at all of that asymmetric centres and are mirror images
39
what are diastereoisomers
sugars that differ at one or more chiral centres. And that are not enantiomers
40
what are aldotetroses
they have two chiral centres
41
what is cyclisation
a chemical reaction where a molecule undergoes a ring closing reaction
42
what does pentose cyclisation form
pyranose rings
43
what does hexoses cyclisation form
furanose
44
what are anomers
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
alpha monosaccharides
Hydroxyl group sits below the plane of the Ring (carbon one)
46
Beta monosaccharides
Hydroxyl group sits above the plane of the Ring (carbon one)
47
what is mutarotation
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
what is mannitol
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
what is sorbitol
it is a laxative It is used to treat constipation
50
what is a glycosidic bond
carbohydrates are joined to alcohols and amines at the anomeric centre by glycosidic bonds
51
what is a disaccharide
combines a hydroxyl of one monosaccharide and an acetyl linkage with another monosaccharide C1 and C4
52
what is lactose
a disaccharide that occurs naturally in milk it is a reducing sugar exhibits mutarotation cleaved in digestion to glucose and galactose
53
why is lactose a common excipient
used to help form tablets because it has excellent compress ability properties It is used to formate diluent powder for dry powder inhalations
54
what is mannose
a common excipient
55
what is maltose
a common excipient
56
what is sucrose
‘table sugar’ pure sucrose, a disaccharide that hydrolyses to glucose and fructose does not undergo mutarotation
57
what is glycogen
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
what are amino sugars
they are found in antibiotics occurs in cartilage
59
what are grooves in DNA
the strands of the DNA double helix create two continuous grooves major and minor major groove is wider and deeper
60
what is aciclovir
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
what is a chain terminator
nucleoside analogues which interfere with or halt DNA replication eg Aciclovir
62
what is interstrand
crosslinking can occur between two complementary strands of DNA
63
what is intrastrand
crosslinking happening between a single strand of DNA (within a strand) as generated by cisplatin
64
what is temozolomide
a pro drug against brain tumours discovered at aston crossed the Blood brain barrier undergoes chemical transformation to yield the reactive methylating agent
65
what is doxorubicin
an example of a DNA intercalator
66
what is a DNA intercalator
they are molecules capable of fitting between nucleic acid base pairs
67
what is the therapeutic difference between citerazine hydrochloride and di hydrochloride
There’s no therapeutic different apart from they are both stereoisomers

week 17 (3 decks)

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