Administering drugs topically Flashcards

(42 cards)

1
Q

Why are some drugs NOT administered orally?

A

Due to biological and chemical properties = the drugs may be destroyed and thus, not carry out the purpose its was created to do.
Due to risk of systemic side effects = whole spread side effects.

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2
Q

Which two effects are demonstrated when drugs are administered?

A
  • Systemic Effect

- Local Effect

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3
Q

Which three routes are used via the systemic administration?

A
Enteral = Oral  
Parenteral = Injections ( IV / IM / SC / IA / ID )  
Topical = Sub - lingual / Transdermal Patch / Inhalation / Rectal
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4
Q

Which route is used via the local administration?

A

Topical = Creams / Intranasal Sprays / Occular Drops

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5
Q

Explain topical administration in terms of producing a local effect.

A

The drug is applied to a localised area of body surface in order to minimise systemic side effects and systemic absorption.

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6
Q

Explain topical administration in terms of producing a systemic effect.

A

Thee drug is applied to the body surface in order tot provide an alternative / convenient route into the blood.

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7
Q

What happens when a drug is administered via oral tablet?

A

First pass metabolism in the liver occurs = therefore, the drug enters the liver first.

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8
Q

What happens when a drug is administered via IV?

A

Enters the blood directly. (DIRECT ACCESS)

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9
Q

How can you bypass first pass liver metabolism?

A

Increase the dosage of the drug

Administer the drug via another route.

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10
Q

What happens when a drug is administered via buccal?

A

Reaches the body first and then the liver.

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11
Q

What happens when a drug is administered via topical?

A

Reaches the body site DIRECTLY.
Absorption via the skin and thus, systemic action occurs.
Results in stable blood levels.

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12
Q

What conditions is the topical local administration used for?

A
Skin = Eczema  
Eye = Conjunctivitis
Nose = Hay - Fever
Lung = Asthma
Vagina = Thrush
Rectum = Constipation
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13
Q

What conditions is the topical systemic administration used for?

A

Skin = Contraception

Mouth (mucosal membranes) = Chest Pain

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14
Q

What formulation is used to deliver drugs administered topically for the skin?

A
Cream 
Ointments
Powder
Lotions
Gels
Transdermal Patch
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15
Q

What formulation is used to deliver drugs administered topically for the nose and lungs?

A

Solutions and Powders

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16
Q

What formulation is used to deliver drugs administered topically for the eye or ear?

A

Solutions
Ointments
Creams

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17
Q

What formulation is used to deliver drugs administered topically for the rectum / colon?

A

Foams
Enemas
Suppositories

18
Q

What formulation is used to deliver drugs administered topically for the vagina?

A

Creams

Pessaries

19
Q

How are drugs are absorbed into the skin?

A

Drugs diffuse from the stratum corneum in to the epidermis into the dermis.
From the dermis it enters the capillary microcirculation.
Then from there, it enters the systemic circulation.

20
Q

What is the stratum corneum?

A

Outer layer of the epidermis.

The permeability barrier of the skin.

21
Q

What does lipophilic drug mean?

A

Utilises the intracellular route (crosses the cell wall)

= Goes THROUGH the cells.

22
Q

What does hydrophilic drug mean?

A

Utilises the intracellular route (diffusing in fluid filled spaces between the cells)
= Goes AROUND the cells.

23
Q

What layer does the drug have to pass in order to reach the site of action?

A

Epidermis Layer.

24
Q

What is the partition coefficient?

A

Ratio of concentrations of compounds in mixture of 2 substances = This mixture is IMMISCIBLE.

25
What are the 2 types of ointments?
Non - Emulsifying = Lipophilic | Water Soluble = Lipophilic and Hydrophilic
26
What are non - emulsifying ointments like?
Contains beeswax and paraffin = Contains few preservatives. Messy and inconvenient.
27
What are water soluble ointments like?
Allows passage of drugs into the skin. | Easily washed off = promotes hydration.
28
What is the formula like for creams?
Either lipophilic or hydrophilic. | This penetrates the stratum corneum and allows the substance to rub in well.
29
What is the disadvantage of using creams?
Contains preservatives = risk of immunological sensitisation.
30
Why is formulation base essential and to not change medication?
Potency for medication can change if the medication is changed. The ones with a fatter component = ABSORBS BETTER.
31
How can you tell which ointment is fattier?
The one with MORE beeswax.
32
What are the key points of formulations?
Target Site = Is the formulation appropriate to the site? Drug Properties = Is the active ingredient of the drug stable in a particular formulation? Acceptability to patient = Is the cream easy to apply?
33
How do drugs administered orally enter the body?
Pass into the systemic circulation / ESCAPES the first pass metabolism.
34
Examples of topical application for a systemic effect?
Inhaled Anaesthetics Buccal Midazolam Sublingual GTN tablet Transdermal nicotine patch
35
What is transdermal application?
Delivery system which releases the drug through a rate controlling membrane into the skin = systemic circulation.
36
What are the key features of transdermal application?
Time relapsed delivery | Lipid Soluble drugs
37
How does transdermal application work?
Polymer matrix = Adhesive which covers the whole patch. | The active compound is released via diffusion and through the membrane which covers the patch.
38
What is a drug reservoir?
Drug layer has 'liquid compartment' which contains the drug solution. Often this reservoir is encapsulated in a shallow mould.
39
What are the benefits of a transdermal application?
Avoids fluctuation in plasma concentration. Easy to administer and acceptable to patients. Can be stopped easily. There is prolonged drug action.
40
What are the disadvantages of a transdermal application?
Only small enough molecules can penetrate the skin this way. Local side effects. Slow to initiate effect. Not applying the patch properly will affect the dosage.
41
What are the advantages of topical administration?
Targets the intended site of action. Reduced risk of systemic side effects. High drug concentration can be achieved. Generally accepted by patients.
42
What are the disadvantages of the topical route?
Still some systemic absorption of drugs. Local side effect (stinging). May be messy or inconvenient. Rapid clearance = requires regular administration.