Hormonal drug delivery Flashcards

1
Q

Amino acid derivatives

- Route of administration

A

Orally route
- Derived from amino acids e.g tyrosine

Example
- Dopamine, thyroxine, hydrocortisone

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2
Q

Cmax and Tmax

A

Cmax
- Max concentration achieved in the plasma after absorption

Tmax
- Time at Cmax

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3
Q

AUC

A

Extent at which a drug is absorbed

- Area under the curve

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4
Q

Therapeutic range

A

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

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5
Q

Multiple oral dosing

A

Giving multiple doses to keep concentration of drug within therapeutic range

Dosage given when concentration starts to decline

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6
Q

Amino acid derivatives

- Drug factos

A

Potent
- Lose dose required

Low dose drug requires bulking
- Excipeients

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7
Q

Excipients

A

Given with small dose of drugs

  • Diluents
  • Surfactants
  • Lubricant
  • Disintegrants
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8
Q

Local delivery

A

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.
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9
Q

Local corticosteroids

- Examples

A

Given locally to avoid systemic side effects

Intrarticular injection- Tennis elbow
Creams- Eczema
Inhaler- Asthma
Eye drop- Inflammation
Suppositories- Haemorrhoids
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10
Q

Insulin

  • Drug factors
  • Biopharmaceutical factors
A

Large peptide hormone

- Cannot be given orally as it will not be absorbed

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11
Q

Differences in insulin

A

Onset

Peak

Duration

Route

  • Inhaled
  • Subcutaneous
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12
Q

Long and short acting insulin

A

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

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13
Q

Insulin pump of rapid analog

A

Delivers sustained rapid analog throughout the day

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14
Q

Pulmonary route

- Systemic

A

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

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15
Q

Afrezza

A

Inhaled insulin

Rapid acting, taken at the start of each meal

Along side long acting insulin injections

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16
Q

Sex hormones

  • Drug factors
  • Biopharmaceutical factors
  • Therapeutic factors
A

Lipophilic

Variable oral administration

  • First pass hepatic factors
  • Short half life

System effects wanted

17
Q

Systemic delivery of sex hormones

A

Done to increase bioavailabity and gives sustained release

Examples

  • Parenteral [IM injection, implant]
  • Transmdermal
  • Intranasal spray
  • Buccal
18
Q

Oily injections

A

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
Q

Nexplanon

A

Subdermal implant of etonogestrel
- System delivery

Releases hormone very slowly
- Removed after 3 years

20
Q

Transdermal estradiol patch

A

Drug diffuses across the skin into the blood stream.

21
Q

Intranasal administration system

- Advantages

A

Advantages

  • Large surface area
  • Highly vascularised
  • Avoids first pass
  • Good bioavailability if LMW
22
Q

Intranasal administration system

- Disadvantages

A

Mucociliary clearance

Metabolic activity

Poor bioavailability if HMW

23
Q

Buccal administration [sex hormone]

- Systemic

A

Mucoadhesive testosterone buccal delivery

  • Twice daily
  • Absorbed in the blood stream of the mouth.
  • Gives sustained release
24
Q

Vaginal gel

- Progesterone

A

Local delivery
- Crinone

Gives sustained release and has good compliance

25
Q

Vaginal ring

A

Releases estradiol over 90 days

- Acts locally

26
Q

Vaginal pessary

A

Estradiol given in vaginal tablets

- Local delivery

27
Q

Intra-uterine device

A

Example: Mirena, Levosert

Inserted into the uterine cavity

  • Local action
  • Levonorgestrel
28
Q

Eicosanoid hormones

A

Lipid derivate hormones
- Prostaglandins E2

Routes

  • Vaginal gel
  • Vaginal pessary