Pharmacology Flashcards

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1
Q

What are.. the main routes of drug administration through the skin?

A

Topical
Transdermal
Subcutaneous

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2
Q

What is topical administration?

A

Applying the drug to the surface of the skin

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3
Q

What are two ways that drugs can penetrate the keratin layer?

A

Through the cells (Transcellular) or between them (intercellular)

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4
Q

What route do drugs usually move through the stratum corneum?

A

Intercellular

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5
Q

When are topical skin therapeutics used?

A
Superficial skin disorders
-Psoriasis
-Eczema
Skin infections
Itching
Dry skin
Warts
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6
Q

What is a vehicle?

A

A substance a drug is suspended in

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7
Q

What is the purpose of a vehicle?

A

Get to the site of action quicker

Increase the concentration of a drug at that site

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8
Q

List some vehilcles

A
Tesla 
Ointments
Creams
Gels
Lotions
Pastes
Powders
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9
Q

Does the vehicle have a large effect on the rate and extent of absorption of the drug?

A

Yes

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10
Q

Where does the drug need to dissolve better, the vehicle or the skin?

A

The skin

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11
Q

What is transdermal drug delivery?

A

A passive process driven by diffusion

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12
Q

What is ficks law of diffusion?

A

Rate of absorption = Kp x Concentration of drug in vehicle

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13
Q

What can enhance solubility and absorption of a drug?

A

Addition of excipients

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14
Q

Are topical drugs absorbed well?

A

No

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15
Q

What factors affect the absorption of a topical drug?

A
Hydration of the skin
Inclusion of excipients
Barrier funciton
Nature of skin
Site of application
Integrity of epidermis
Drug preperation
Vehicle
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16
Q

How do glucocorticoids signal?

A

Via nuclear receptors (class 1)

17
Q

Are glucocorticoids lipophillic or lipophobic?

A

Lipophilic

18
Q

How do glucocorticoids enter the cell?

A

Diffusion across the plasma membrane

19
Q

What do glucocorticoids bind to within the cytoplasm?

A

GRa

20
Q

What does the binding of GCs to GRa cause?

A

Dissociation of inhibitory heat shock proteins

21
Q

What happens to the activated GRa receptor?

A

Translocates into the nucleus

22
Q

What aids translocation of GRa receptor into the nucleus?

A

Importins

23
Q

What do activated receptors assemble into in the nucleus?

A

Homodimers

24
Q

What do homodimers bond to?

A

Glucocorticoid response elements (GRE) in the promoter region of specific genes

25
Q

What is the outcome of the homodimers binding to GREs?

A

Transrepression

Transactivation

26
Q

What is subcutaneous administration?

A

When a drug is delivered by a needle into the fatty tissue just beneath the surface of the skin

27
Q

How does a subcutaneous drug reach systemic circulation?

A

Diffusion into the capillaries or lymphatics

28
Q

What are the negatives to subcutaneous administation?

A

Slow absorption
Mainly for protein and oil based drugs
Injection volume limited
Pain?

29
Q

What makes the skin a good site for drug administration?

A

Application is simple and non-sterile
Steady-state plasma concentration
Avoids first pass metabolism
Drug absorption can be terminated rapidly

30
Q

What is transdermal drug delivery?

A

Drug is incorporated into an adhesive patch

31
Q

How is transdermal drug delivery partially controlled?

A

Drug release

32
Q

What type of drug is transdermal delivery most suitable for?

A

LMW drugs
Moderately lipophillic
Potent
Relatively brief half life