T1 L20 Hormonal drug delivery

Question 1

What are some different dosage forms?

Answer 1

Tablets and capsules
Injections and infusions
Patches
Creams and ointments
Inhalers
Suppositories and pessaries

Question 2

Why do we need different dosage forms?

Answer 2

Some people don't like certain forms
Different clinical conditions
Different types of patients
Different routes of administration
Different physiochemical properties of a drug

Question 3

Give some examples of drug factors to consider when designing dosage forms

Answer 3

Solubility
Partition
Coefficient
pKa
Stability
Molecular weight

Question 4

Give some examples of biopharmaceutical factors to consider when designing dosage forms

Answer 4

Absorption
Bioavailability
Route of administration

Question 5

Give some examples of therapeutic factors to consider when designing dosage forms

Answer 5

Disease
Patient
Route
Local vs systemic delivery

Question 6

Give examples of types of hormones

Answer 6

Modified amino acid derivatives
Peptides and proteins
Steroids
Eicosanoids

Question 7

Give examples of modified amino acid derivatives

Answer 7

Dopamine

Thyroxine

Question 8

What are modified amino acid derivatives derived from?

Answer 8

Tyrosine or tryptophan

Question 9

What are peptides and proteins derived from?

Answer 9

Amino acids

Question 10

Give some examples of peptides and proteins

Answer 10

Neuropeptides - vasopressi
Pituitary hormones - gonadotrophin
GI hormones - insulin

Question 11

What are steroids derived from?

Answer 11

Cholesterol

Question 12

What are some examples of steroids?

Answer 12

Sex hormones - testosteorne

Corticosteroids - hydrocortisone

Question 13

What are eicosanoids derived from?

Answer 13

Lipids

Question 14

What are some examples of eicosanoids?

Answer 14

Prostaglandins

Leukotrienes

Question 15

What is an excipient?

Answer 15

Anything else added that isn’t the drug. Doesn’t have a pharmacological effect

Question 16

Give examples of excipients

Answer 16

Diluents / fillers (lactose, water)
Surfactants (polysorbates)
Lubriants (Mg stearate)
Disintegrants (starch)
Viscosity enhancing agents (cellulose derivatives)
Flavours, colours, perfumes
Sweetening agents
Preservatives

Question 17

when is local delivery used?

Answer 17

Rapid onset of action
Less drug required
Absorption into blood stream isn’t required
Absorption into blood stream can lead to unwanted side effects

Question 18

What are the biopharmaceutical factors of peptide hormones?

Answer 18

Not absorbed after oral administration as enzymatic degradation occurs in lumen of GI tract
Any that survives can’t readily cross GI epithelium into blood as it is too large

Question 19

How do the types of insulin vary?

Answer 19

Onset - how quickly they act
Peak - how quickly they achieve maximum impact
Duration
Route of delivery

Question 20

Describe the adaptions that make the pulmonary route so effective

Answer 20

Large surface area
Thin epithelial barrier
Good blood supply
Avoids harsh environment of GI tract
Avoids first-pass hepatic metabolism

Question 21

What is inhaled insulin?

Answer 21

Rapid-acting inhaled insulin
Taken at beginning of each meal
Used in combination with long-acting injected insulin
Action is prolonged so there could be a risk of late-meal low blood sugars

Question 22

What are some alternatives to the oral route for systemic delivery?

Answer 22

Parental route - IM, injection, implant
Transdermal route - patch or gel
Intranasal route - spray
Buccal route - mucoadhesive system
Vaginal - gel

Question 23

Describe nexplanon

Answer 23

Progestogen-only contraception
Contains etonorgesterel in each flexible rod
Delivered by sub-dermal implantation
Provides effective contraception for up to 3 years
Systemic delivery

Question 24

What are the 2 major types of transdermal delivery system products?

Answer 24

Reservoir - active ingredient is held in a solution or suspension between the backing layer and a rate-controlling membrane
Matrix - solution or suspension dispersed within polymer or cotton pad in direct contact with the skin. Held on the skin by adhesive applied by perimeter of the system

Question 25

What are the advantages of intranasal administration?

Answer 25

Large surface area
Highly vascularised
Avoids first-pass hepatic metabolism
Good availability for low molecular weight compounds

Question 26

What are the disadvantages of intranasal administration?

Answer 26

Mucociliary clearance
Metabolic activity
Poor bioavailability for high molecular weight compounds

Question 27

Describe the mucoadhesive testosterone buccal delivery system

Answer 27

Applied twice daily
Adheres to gum or inner cheek
Sustained release of testosterone through buccal mucosa

Question 28

Describe treatment for hypogonadal males with mucoadhesive testosterone buccal system

Answer 28

Following initial application, serum testosterone rises to a max within 10-12 hours
Steady state levels are obtained after first 2 systems are applied
When removed & not reapplied, serum testosterone levels fall to below normal range in 2-4 hours

Question 29

What are the advantages of intrauterine progestogen-only device?

Answer 29

Uses natural hormone at much lower dose than by other routes
Don’t need to take / administer daily
No oestrogens
T-shaped device for comfort, safety and retention.
Hormonal action confined to uterus