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Pharmaceutics > Parenterals Route > Flashcards

Parenterals Route Flashcards

1
Q

What is parenterals route commonly referred as?

A

Drug administration by injection

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2
Q

What are the different routes?

A 
Intravenous
Intrathecal, epidural + intraspinal
Intra-arterial + intracardiac 
Intradermal
Subcutaneous
Intramuscular
Intra-articular
Intra-ocular
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3
Q

What are the advantages?

A

Rapid onset of action
Delayed onset possible through intramuscular
Infusion of drugs for prolonged period
Avoids 1st-pass metabolism
Unconscious patients
Allows higher conc of drug in system/local

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4
Q

Why is it good that infusion of drugs is for prolong period?

A

Maintain steady-state plasma levels

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5
Q

Why is it good it avoids 1st-pass metabolism?

A

Improves bioavailability

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6
Q

What are the disadvantages?

A 
Require professionals
Potential risk
Needle-stick injuries
Poor patient acceptability
Formulation + manufacture cost high
Shelf-life shorter than oral
Refrigerated = extra cost
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7
Q

Describe intravenous (IV)

A

Surface vein
1ml to several litres for infusion
Increases plasma drug conc
100% drug absorption

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8
Q

What is the infusion for intravenous?

A

Diluted in a bag = produces slow + controlled drug release rate

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9
Q

What emulsions cannot be used for IV?

A

W/O = block blood vessels

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10
Q

What do hypertonic/extreme drug pH solutions cause in IV?

A

Inflammation + pain at injection site

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11
Q

How is IV infused?

A

Central line into major vessel

= allows rapid diffusion by large blood vol

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12
Q

Describe intra-arterial

A

Like IV except via artery
More invasive + less accessible
Only used when no IV access

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13
Q

When may there be no IV access?

A

Premature babies

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14
Q

When is intracardiac used + why?

A

Only used life-threatening emergencies

= to produce rapid, local effect in heart

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15
Q

Describe intradermal

A

Inject into skin between epidermis + dermis
Up to 0.2ml
Absorption slow

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16
Q

Why is absorption slow in intradermal?

A

Little interstitial fluid to facilitate drug diffusion at injection site
= not-well perfused by blood

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17
Q

What is intradermal used for?

A

Immunological diagnostic tests + vaccinations

eg. BCG

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18
Q

Describe subcutaneous

A

Hypodermic injections

Inject into loose connective + adipose tissues below dermal skin layer

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19
Q

Where is subcutaneous injected + why?

A

Abdomen, upper arms/legs

= highly vascularised = absorption rapid + predictable

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20
Q

What can be injected subcutaneously?

A

Aq solutions or suspensions

Up to 1ml

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21
Q

What is an example of subcutaneous injection?

A

Insulin

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22
Q

Describe intramuscular

A

Into tissue of relaxed muscle = butt, thigh or shoulder
Up to 4ml
Slower than SC

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23
Q

What can be injected intramuscularly?

A

Aq or oily solutions or suspensions

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24
Q

What are the 2 intra-spinal routes?

A

Intrathecal

Epidural

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25
Q

Describe intrathecal

A

Cerebrospinal fluid (CSF) in subarachnoid space or spinal canal
100% absorption in CSF
Vol up to 10ml

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26
Q

What does intrathecal route allow drugs to do?

A

Bypass BBB

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27
Q

What are examples of intrathecal route into CSF?

A

Anticancer drugs
Antibiotics for meningitis
Analgesic

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28
Q

Describe epidural

A

Space between dura mater + vertebrae
Must be aq isotonic
Cannot include preservatives

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29
Q

What are examples of epidural?

A

Spinal anaesthesia - long-acting steroid

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30
Q

Describe intra-articular

A

Into synovial fluid of joint cavities

100% drug absorption at site of action

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31
Q

What is intra-articular suitable for?

A

Aq solutions/suspensions

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32
Q

What is an example of intra-articular route?

A

Anti-inflammatory drugs to treat arthritic conditions or sport injuries

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33
Q

What are the 2 routes for intraocular?

A

Intracameral

Intravitreal

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34
Q

What is the intraocular route?

A

Into eye

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35
Q

Describe intracameral

A

Into anterior chamber (front lens)
0.1-1ml
Antibiotics, local anaesthetics

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36
Q

Describe intravitreal

A

Into vitreous chamber

Treat ocular diseases

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37
Q

What precaution must be taken + why with intravitreal route?

A

Max vol 0.1ml

= minimise risk of rising intraocular pressure + damage

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38
Q

What must all parenteral preparations be?

A

Sterile

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39
Q

Why must be sterile?

A

Drug formulations directly injected into blood/body tissue

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40
Q

Why are excipients used?

A 
Adjust isotonicity 
Adjust pH
\+ drug solubility
\+ drug stability
\+ shelf-life
Preservative
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41
Q

Why does isotonicity need to be adjusted?

A

To match human blood

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42
Q

What should excipients not do?

A

Adversely affect drug action or cause any side effects?toxicity

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43
Q

What are endotoxins?

A

Lipopolysaccharides found in outer membrane of gram-negative bacteria

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44
Q

What are pyrogens?

A

Substances that cause fever, typically produced by bacteria/viruses

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45
Q

What must parenteral preparations be free from?

A

Endotoxins + pyrogens

Particulates

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46
Q

What must all products comply with?

A

Tests for bacterial endotoxins + pyrogens

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47
Q

What can contain particulates?

A

IM
SC
Intra-articular

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48
Q

What happens if there is any suspended particles?

A

Travel through venous system to lung
= prevent blood flow
= pulmonary embolism

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49
Q

Why significantly can’t there be any particles in IV?

A

Droplet size of 3mm, which is equal to diameter of capillary

50
Q

What must containers be?

A 
Transparent
Glass or plastic
Airtight
Effectively sealed
Compatible with formulation
51
Q

Why must a container be transparent?

A

So can inspect for particles

52
Q

Why must container be effectively sealed?

A

To prevent contamination before use

53
Q

What can sterile products be in?

A

Solutions
Suspensions
Emulsions

54
Q

What must solutions be?

A

Clear

Free from particles

55
Q

What must suspensions be?

A

Readily re-suspended on shaking

56
Q

What does shaking suspensions enable?

A

Uniform dose to allow withdrawal

57
Q

What must emulsions not be?

A

Show any signs of creaming or cracking

58
Q

What are aq injections for?

A

Multiple dosing

59
Q

What must aq injections contain?

A

Antimicrobial preservative

60
Q

When can a preservative not be used in aq injection?

A

Dose vol bigger than 15ml

Injecting into eye or spine

61
Q

What are unpreserved injections formulated in?

A

Single-dose containers

= in ampoules or prefilled syringes

62
Q

What are infusions?

A

Sterile aq solutions/emulsions

63
Q

What is the continuous phase as infusions?

A

H2O

64
Q

What is the vol of infusions?

A

100-1000ml

65
Q

Do infusions contain preservatives?

A

NO

66
Q

What is isotonicity in respect with in infusions?

A

Blood

67
Q

What are concentrates for?

A

Injection or infusion after solution

68
Q

What are concentrates diluted with?

A

Saline or H2O for injection

69
Q

How are concentrates administrated?

A

Through infusion bags

70
Q

What are powders?

A

Dry sterile solid in final container for reconstitution

71
Q

What is required for powders?

A

Vol of diluent added prior administration

72
Q

When are powders used?

A

Used for drugs with short shelf-life after dissolved in solution

73
Q

What are suspensions for?

A

SC
IM
Intra-articular

74
Q

What do suspensions allow?

A

Slow + prolonged release = reduce dosing frequency

75
Q

What must happen to suspended drug first?

A

Dissolved before it can be absorbed

76
Q

Why may low aq solubility drugs use IM?

A

Provide prolonged effect

77
Q

How long does benzylpenicillin benzathine IM suspension release over?

A

2-4 weeks

78
Q

How long does hydrocortisone acetate IM suspension release over?

A

2-7 days

79
Q

What are the vehicles for injections?

A

H2O = most common
Saline
Solubilising agents
Co-solvents

80
Q

What type of H2O is vehicle for injection?

A

Highly purified grade

81
Q

Describe saline

A

Up to 0.9% w/v

Commonly used as infusion vehicle

82
Q

Why are solubilising agents added?

A

To aid dissolution

83
Q

What is an example of solubilising agent?

A

Polyoxyethylene castor oil derivatives can solubilise hydrophobic drugs lie diazepam

84
Q

What are examples of co-solvents?

A

Ethanol
Glycerol
Propylene glycol

85
Q

Why are preservatives used?

A

Antimicrobial protection used in multi-dose

86
Q

What are some common preservatives?

A 
Benzalkonium chloride (0.01% w/v)
Benzoic acid (0.17% w/v)
Benzyl alcohol (1-2% w/v)
87
Q

What do co-solvents do?

A

Aid dissolution + antimicrobial effect

88
Q

What do antioxidants do?

A

Reduce drug degradation by oxidation = extend shelf-life

89
Q

How do antioxidants work?

A

N2 gas bubbled through solution to displace O2

90
Q

What can N2 be used for?

A

Fill container headspace

91
Q

What is the physiological pH?

A

7.4

92
Q

What is the pH range for injectables?

A

pH 3-9

93
Q

What happens if pH is out of injectables range?

A

Too corrosive = tissue damage

94
Q

What can adjust pH?

A

Acidifying + alkalizing agents

95
Q

What maintains pH?

A

Buffers

96
Q

When do buffers work best?

A

When pH is close to pKa of WA/WB

97
Q

What is blood osmolarity?

A

275-295m Osm/kg

98
Q

What is hypotonic?

A

Cells swell = burst

99
Q

What is hypertonic?

A

Cells lose H2O = shrivel

100
Q

What must IV infusions be?

A

Isotonic

101
Q

What must also be ideally isotonic?

A 
SC
IM
Intradermal
CSF
Intra-ocular
102
Q

What is added to hypotonic?

A

NaCl
Dextrose
Mannitol

103
Q

What can make it hypertonic?

A

Dilution prior administration

104
Q

When are suspending agents used?

A

Used in suspensions to ensure drug can be readily re-suspended (by shaking) prior to use

105
Q

What are examples of suspending agents?

A

Methylcellulose + polysorbates

106
Q

How is a suspension re-suspended?

A

Shaking

107
Q

What is the vol of glass ampoule containers?

A

1-10ml

108
Q

What are glass ampoule containers used for?

A

Single-use unpreserved product

109
Q

What glass is used for glass ampoule containers + why?

A

Type 1

= little interaction with formulation

110
Q

What is problem with Type 1 glass?

A

Fragile = safety risk when opening

= deposition of glass particles when opening

111
Q

What are advantages of plastic ampoule containers?

A

More robust
Safer to use
Fewer particles generated on opening

112
Q

What are disadvantages of plastic ampoule containers?

A

More costly

More prone to drug interaction

113
Q

What are vials made from?

A

Type 1 glass with re-usable synthetic drug closure

114
Q

What is vol of vials?

A

5-100ml

115
Q

What is the closure on vial?

A

Rubber closure held in place by aluminium cover seal

116
Q

What are pros of rubber closure on vial?

A

Dust protection
Security measure
Self-sealing
Coated in Teflon = minimise drug interaction

117
Q

What is the negative of rubber closer on vial?

A

Allows few punctures

118
Q

What is vol of infusion bag?

A

100-1000ml
OR
3000ml

119
Q

Describe collapsible infusion bag

A

Made from PVC or poly-olefin plastic
Have additive port = injectable drugs added
Air inlet not needed

120
Q

Describe semi-rigid plastic bottle

A

Made of polyethene

Air equilibration may be required

121
Q

Describe glass bottles

A

Less commonly used now

122
Q

What different containers are used?

A 
Glass ampoules
Plastic ampoules
Vials
Infusion bags - collapsible
Semi-rigid plastic bottles
Glass bottles

Pharmaceutics (21 decks)

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