Hormonal drug delivery Flashcards Preview

203: The endocrine system > Hormonal drug delivery > Flashcards

Flashcards in Hormonal drug delivery Deck (28)
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1

Amino acid derivatives
- Route of administration

Orally route
- Derived from amino acids e.g tyrosine

Example
- Dopamine, thyroxine, hydrocortisone

2

Cmax and Tmax

Cmax
- Max concentration achieved in the plasma after absorption

Tmax
- Time at Cmax

3

AUC

Extent at which a drug is absorbed
- Area under the curve

4

Therapeutic range

Concentration of the drug between the max safe concentration and minimally effective concentration

5

Multiple oral dosing

Giving multiple doses to keep concentration of drug within therapeutic range

Dosage given when concentration starts to decline

6

Amino acid derivatives
- Drug factos

Potent
- Lose dose required

Low dose drug requires bulking
- Excipeients

7

Excipients

Given with small dose of drugs
- Diluents
- Surfactants
- Lubricant
- Disintegrants

8

Local delivery

Site of administration is the site of action
- Rapid onset of action
- Less drug required---> Avoids side effects as it is not absorbed into the blood stream.

9

Local corticosteroids
- Examples

Given locally to avoid systemic side effects

Intrarticular injection- Tennis elbow
Creams- Eczema
Inhaler- Asthma
Eye drop- Inflammation
Suppositories- Haemorrhoids

10

Insulin
- Drug factors
- Biopharmaceutical factors

Large peptide hormone
- Cannot be given orally as it will not be absorbed

11

Differences in insulin

Onset

Peak

Duration

Route
- Inhaled
- Subcutaneous

12

Long and short acting insulin

Long acting
- Solution in syringe
- Precipitates and aggregates in fat then separates in blood stream
- The separation of the particles is the rate limitting step

Short acting
- Rapid analog that is given in its simplest form

13

Insulin pump of rapid analog

Delivers sustained rapid analog throughout the day

14

Pulmonary route
- Systemic

Larger surface area
- High absorption probability

Thin epithelial barrier
- Small diffusion barrier for drugs

Good blood supply
- 100% cardiac output

Avoids GI harsh environment and first pass hepatic metabolism

15

Afrezza

Inhaled insulin

Rapid acting, taken at the start of each meal

Along side long acting insulin injections

16

Sex hormones
- Drug factors
- Biopharmaceutical factors
- Therapeutic factors

Lipophilic

Variable oral administration
- First pass hepatic factors
- Short half life

System effects wanted

17

Systemic delivery of sex hormones

Done to increase bioavailabity and gives sustained release

Examples
- Parenteral [IM injection, implant]
- Transmdermal
- Intranasal spray
- Buccal

18

Oily injections

IM injection- Gives sustained release

Example: testosterone formulation
- Adds ester group to decrease water solubility and deactivates the molecule
- Activated through hydrolysis (pro-drug)

19

Nexplanon

Subdermal implant of etonogestrel
- System delivery

Releases hormone very slowly
- Removed after 3 years

20

Transdermal estradiol patch

Drug diffuses across the skin into the blood stream.

21

Intranasal administration system
- Advantages

Advantages
- Large surface area
- Highly vascularised
- Avoids first pass
- Good bioavailability if LMW

22

Intranasal administration system
- Disadvantages

Mucociliary clearance

Metabolic activity

Poor bioavailability if HMW

23

Buccal administration [sex hormone]
- Systemic

Mucoadhesive testosterone buccal delivery
- Twice daily
- Absorbed in the blood stream of the mouth.
- Gives sustained release

24

Vaginal gel
- Progesterone

Local delivery
- Crinone

Gives sustained release and has good compliance

25

Vaginal ring

Releases estradiol over 90 days
- Acts locally

26

Vaginal pessary

Estradiol given in vaginal tablets
- Local delivery

27

Intra-uterine device

Example: Mirena, Levosert

Inserted into the uterine cavity
- Local action
- Levonorgestrel

28

Eicosanoid hormones

Lipid derivate hormones
- Prostaglandins E2

Routes
- Vaginal gel
- Vaginal pessary