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Parenterals Route Flashcards

(122 cards)

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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
Describe intrathecal
Cerebrospinal fluid (CSF) in subarachnoid space or spinal canal 100% absorption in CSF Vol up to 10ml
26
What does intrathecal route allow drugs to do?
Bypass BBB
27
What are examples of intrathecal route into CSF?
Anticancer drugs Antibiotics for meningitis Analgesic
28
Describe epidural
Space between dura mater + vertebrae Must be aq isotonic Cannot include preservatives
29
What are examples of epidural?
Spinal anaesthesia - long-acting steroid
30
Describe intra-articular
Into synovial fluid of joint cavities | 100% drug absorption at site of action
31
What is intra-articular suitable for?
Aq solutions/suspensions
32
What is an example of intra-articular route?
Anti-inflammatory drugs to treat arthritic conditions or sport injuries
33
What are the 2 routes for intraocular?
Intracameral | Intravitreal
34
What is the intraocular route?
Into eye
35
Describe intracameral
Into anterior chamber (front lens) 0.1-1ml Antibiotics, local anaesthetics
36
Describe intravitreal
Into vitreous chamber | Treat ocular diseases
37
What precaution must be taken + why with intravitreal route?
Max vol 0.1ml | = minimise risk of rising intraocular pressure + damage
38
What must all parenteral preparations be?
Sterile
39
Why must be sterile?
Drug formulations directly injected into blood/body tissue
40
Why are excipients used?
``` Adjust isotonicity Adjust pH + drug solubility + drug stability + shelf-life Preservative ```
41
Why does isotonicity need to be adjusted?
To match human blood
42
What should excipients not do?
Adversely affect drug action or cause any side effects?toxicity
43
What are endotoxins?
Lipopolysaccharides found in outer membrane of gram-negative bacteria
44
What are pyrogens?
Substances that cause fever, typically produced by bacteria/viruses
45
What must parenteral preparations be free from?
Endotoxins + pyrogens | Particulates
46
What must all products comply with?
Tests for bacterial endotoxins + pyrogens
47
What can contain particulates?
IM SC Intra-articular
48
What happens if there is any suspended particles?
Travel through venous system to lung = prevent blood flow = pulmonary embolism
49
Why significantly can't there be any particles in IV?
Droplet size of 3mm, which is equal to diameter of capillary
50
What must containers be?
``` Transparent Glass or plastic Airtight Effectively sealed Compatible with formulation ```
51
Why must a container be transparent?
So can inspect for particles
52
Why must container be effectively sealed?
To prevent contamination before use
53
What can sterile products be in?
Solutions Suspensions Emulsions
54
What must solutions be?
Clear | Free from particles
55
What must suspensions be?
Readily re-suspended on shaking
56
What does shaking suspensions enable?
Uniform dose to allow withdrawal
57
What must emulsions not be?
Show any signs of creaming or cracking
58
What are aq injections for?
Multiple dosing
59
What must aq injections contain?
Antimicrobial preservative
60
When can a preservative not be used in aq injection?
Dose vol bigger than 15ml | Injecting into eye or spine
61
What are unpreserved injections formulated in?
Single-dose containers | = in ampoules or prefilled syringes
62
What are infusions?
Sterile aq solutions/emulsions
63
What is the continuous phase as infusions?
H2O
64
What is the vol of infusions?
100-1000ml
65
Do infusions contain preservatives?
NO
66
What is isotonicity in respect with in infusions?
Blood
67
What are concentrates for?
Injection or infusion after solution
68
What are concentrates diluted with?
Saline or H2O for injection
69
How are concentrates administrated?
Through infusion bags
70
What are powders?
Dry sterile solid in final container for reconstitution
71
What is required for powders?
Vol of diluent added prior administration
72
When are powders used?
Used for drugs with short shelf-life after dissolved in solution
73
What are suspensions for?
SC IM Intra-articular
74
What do suspensions allow?
Slow + prolonged release = reduce dosing frequency
75
What must happen to suspended drug first?
Dissolved before it can be absorbed
76
Why may low aq solubility drugs use IM?
Provide prolonged effect
77
How long does benzylpenicillin benzathine IM suspension release over?
2-4 weeks
78
How long does hydrocortisone acetate IM suspension release over?
2-7 days
79
What are the vehicles for injections?
H2O = most common Saline Solubilising agents Co-solvents
80
What type of H2O is vehicle for injection?
Highly purified grade
81
Describe saline
Up to 0.9% w/v | Commonly used as infusion vehicle
82
Why are solubilising agents added?
To aid dissolution
83
What is an example of solubilising agent?
Polyoxyethylene castor oil derivatives can solubilise hydrophobic drugs lie diazepam
84
What are examples of co-solvents?
Ethanol Glycerol Propylene glycol
85
Why are preservatives used?
Antimicrobial protection used in multi-dose
86
What are some common preservatives?
``` Benzalkonium chloride (0.01% w/v) Benzoic acid (0.17% w/v) Benzyl alcohol (1-2% w/v) ```
87
What do co-solvents do?
Aid dissolution + antimicrobial effect
88
What do antioxidants do?
Reduce drug degradation by oxidation = extend shelf-life
89
How do antioxidants work?
N2 gas bubbled through solution to displace O2
90
What can N2 be used for?
Fill container headspace
91
What is the physiological pH?
7.4
92
What is the pH range for injectables?
pH 3-9
93
What happens if pH is out of injectables range?
Too corrosive = tissue damage
94
What can adjust pH?
Acidifying + alkalizing agents
95
What maintains pH?
Buffers
96
When do buffers work best?
When pH is close to pKa of WA/WB
97
What is blood osmolarity?
275-295m Osm/kg
98
What is hypotonic?
Cells swell = burst
99
What is hypertonic?
Cells lose H2O = shrivel
100
What must IV infusions be?
Isotonic
101
What must also be ideally isotonic?
``` SC IM Intradermal CSF Intra-ocular ```
102
What is added to hypotonic?
NaCl Dextrose Mannitol
103
What can make it hypertonic?
Dilution prior administration
104
When are suspending agents used?
Used in suspensions to ensure drug can be readily re-suspended (by shaking) prior to use
105
What are examples of suspending agents?
Methylcellulose + polysorbates
106
How is a suspension re-suspended?
Shaking
107
What is the vol of glass ampoule containers?
1-10ml
108
What are glass ampoule containers used for?
Single-use unpreserved product
109
What glass is used for glass ampoule containers + why?
Type 1 | = little interaction with formulation
110
What is problem with Type 1 glass?
Fragile = safety risk when opening | = deposition of glass particles when opening
111
What are advantages of plastic ampoule containers?
More robust Safer to use Fewer particles generated on opening
112
What are disadvantages of plastic ampoule containers?
More costly | More prone to drug interaction
113
What are vials made from?
Type 1 glass with re-usable synthetic drug closure
114
What is vol of vials?
5-100ml
115
What is the closure on vial?
Rubber closure held in place by aluminium cover seal
116
What are pros of rubber closure on vial?
Dust protection Security measure Self-sealing Coated in Teflon = minimise drug interaction
117
What is the negative of rubber closer on vial?
Allows few punctures
118
What is vol of infusion bag?
100-1000ml OR 3000ml
119
Describe collapsible infusion bag
Made from PVC or poly-olefin plastic Have additive port = injectable drugs added Air inlet not needed
120
Describe semi-rigid plastic bottle
Made of polyethene | Air equilibration may be required
121
Describe glass bottles
Less commonly used now
122
What different containers are used?
``` Glass ampoules Plastic ampoules Vials Infusion bags - collapsible Semi-rigid plastic bottles Glass bottles ```

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