Lecture 22 - Oral versus parenteral management of CVD / Enzymology Flashcards

1
Q

What are the advantages of parenteral drug administration?

A
  • Drug not broken down in GI tract
  • 100% bioavailability
  • Localised effect – eg injections into joint, ocular, intradermal
  • Systemic effect – IV injection drug delivered directly into circulation
  • Rapid onset of effect (iv injection)
  • Drug administered in unconscious patient
  • Delayed onset of effect of effect/ few dosing (IM injection once a month)
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2
Q

What are the disadvantages of parenteral drug administration?

A

-Use of needle (needle phobia, needlestick injury)
- Painful
- Preparation needs to meet stringent specifications (expensive)
- Limited self-administration

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3
Q

What is an intravenous injection?

A

Administration into easily accessible vein

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4
Q

What is the volume of an IV injection?

A

1ml

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5
Q

What is the volume of IV infusion?

A

Several litres

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6
Q

What is thrombophlebitis?

A

Damage to vein

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7
Q

How is thrombophlebitis minimized?

A

With the use of a central line

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8
Q

What causes damage to veins?

A
  • Drugs with high/ low pH
  • Hypertonic solutions
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9
Q

How is thrombophelitis minimised?

A

With the use of a central line

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10
Q

Can suspensions be administered via central line?

A

No - particles block capillaries

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11
Q

What is required for central dosing?

A

Emulsion

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12
Q

How are most paranteral drugs administered?

A

IV

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13
Q

What is intracardiac administertration?

A

Drug administration directly into the heart

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14
Q

When is intracardiac administration used?

A

Only for life threatening emergancy

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15
Q

What is the injection volume for intradermal administartion?

A

0.2ml

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16
Q

What is intradermal administration typically used for?

A

Vaccination

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17
Q

What angle is intradermal administered at?

A

10 to 15 degreeds

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18
Q

What angle is subcutaneous administered at?

A

45 degrees

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19
Q

What angle is intramuscular administered at?

A

90 degrees

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20
Q

What layer is intradermal administered into?

A

Dermis

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21
Q

What layer is subcutaneous administered into?

A

Subcutaneous tissue

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22
Q

What layer is instramuscular administered into?

A

Muscle

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23
Q

What is subcutanous also known as?

A

Hypodermic

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24
Q

Where are subcutanous injections administed into?

A

Subcutaneous fat

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25
Q

What is the injection volume for subcutaneous administration?

A

1ml

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26
Q

What are the advantages for subcutanous administration?

A
  • Quite fast administration
  • Predictable eg insulin
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27
Q

What formulation are subcutaneous injections?

A
  • Aqueous solutions
  • Suspensions
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28
Q

Where are intramuscular injections administered?

A
  • Buttock
  • Thigh
  • Shoulder muscle
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29
Q

What is the volume of intramuscular injections?

A

Up to 4ml

30
Q

Is intramuscular administration faster or slower than subcutaneous administration

A

Slower

31
Q

What is the injection volume of intrathecal injections?

A

Up to 10ml

32
Q

What formulation are intrathecal injections?

A

Aqueous solutions

33
Q

Where are intrathecal drugs administered?

A

Into cerebrospinal fluid

34
Q

What are the two intermost protective membranes of spinal chord?

A
  • Arachnoid mater
  • Pia mater
35
Q

Where is the cerebrospinal fluid?

A

In the subarachnoid space between arachnoid mater and pia mater

36
Q

What are intrathecal drugs used for?

A

To introduce drugs that cannot cross the blood brain barrier eg antibiotics to treat menengitis or anticancer agents

37
Q

Where are epidural injectios administered?

A

Into epidural space eg spinal anaesthesia

38
Q

Where are intra articular injections delivered?

A

Into synovial fluid of jount cavities

39
Q

What drugs are usually given via intra-articular injections?

A

Anti-inflammatory drugs to treat arthritic conditions

40
Q

Where are opthalmic injections administered?

A

Around on into the eye

41
Q

What is the volume of ophthalmic injections?

A

1ml

42
Q

Where are intracameral injections administered?

A

Into anterior chamber of the eye - infront of lens

43
Q

What is the maximal volume of ophthlamic injections?

A

0.1ml

44
Q

What happens if ophthalmic injections exceed the maximum volume?

A

Rise in intra ocular pressure

45
Q

What are the pharmacopoeial requirements for injections?

A
  • Sterility
  • Excipients
  • Containers - transparent to permit inspection of contents
  • Free from endotoxin and pyrogens
  • Free of particles
  • For emulsions for IV injection droplet less than 3nm to prevent oil embolism
46
Q

What can injections be?

A
  • Solutions
  • Emulsions
  • Suspensions
47
Q

What injections are used for local action?

A
  • Intra articular
  • Intra ocular
48
Q

What injections need to be absorbed for systemic effect?

A
  • Intramuscular
  • Subcutaneous
49
Q

How long do IM and SC injections of solutions usually take to absorb?

A

Within 30 mins

50
Q

How long do IM injections of suspensions take to act?

A

1 - 7 days

51
Q

How long do IM oily injections take to act?

A

Up to 4 weeks

52
Q

How long do intra-articular injections of suspensions take to act?

A

Act over many weeks

53
Q

What are three vehicles for injections?

A
  • Water for injections (highly purified water)
  • Solubelising agents (eg cyclodextrins)
  • Oils
54
Q

Give examples of oils used for injections

A
  • Lecithin
  • Sorbitan fatty acids
  • Arachis oil
  • Sesame oil
55
Q

What is the pH of plasma?

A

7.4

56
Q

What pH can injections be?

A

Between 3 and 9

57
Q

What is used to adjust the tonicity of injections?

A
  • Dextrose
  • Mannitol
58
Q

What is the purpose of enzymes?

A
  • Powerful catalysts
59
Q

What do catalysts do?

A

Increase the rate of a reaction by up to 1 million fold but don’t change the equillibrium of the reaction

60
Q

How do catalysts accelerate reactions?

A

By stabilising the transition state

61
Q

Describe the transition state?

A
  • Highly unstable
  • Energetically unfavourable
  • Reaction intermediate
62
Q

How do enzymes affect the activation energy?

A

Lower the activation energy of a reaction but G stats the same

63
Q

What is the reaction surface for enzyme catalysis?

A

The active site

64
Q

What is a suitable environment for enzyme catalysis?

A

Hydrophobic

65
Q

What is the active site?

A

Small hyrdrophobic hollow or cleft on the enzyme surface

66
Q

What does the active site contain?

A

Amino acids

67
Q

What do amino acids in the active site do?

A
  • Bind reactants (substrates and cofactors)
  • Catalyse the reaction
68
Q

What are the models of active site binding?

A
  • Lock and key
  • Induced fit
69
Q

What is induced fit?

A
  • The active site is nearly the correct shape for substrate.
  • Binding alters the shape of the enzyme
  • Strains bonds in substrate: involves intramolecular bonds between function groups in substrate and active site
70
Q

What are the strongest bonding forces?

A

Ionic

71
Q

What are the weakest bonding forces?

A

Van der waals