T1 L20 Hormonal drug delivery Flashcards

1
Q

What are some different dosage forms?

A
Tablets and capsules
Injections and infusions
Patches
Creams and ointments
Inhalers
Suppositories and pessaries
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2
Q

Why do we need different dosage forms?

A
Some people don't like certain forms
Different clinical conditions
Different types of patients
Different routes of administration
Different physiochemical properties of a drug
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3
Q

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

A
Solubility
Partition
Coefficient
pKa
Stability
Molecular weight
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4
Q

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

A

Absorption
Bioavailability
Route of administration

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5
Q

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

A

Disease
Patient
Route
Local vs systemic delivery

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6
Q

Give examples of types of hormones

A

Modified amino acid derivatives
Peptides and proteins
Steroids
Eicosanoids

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7
Q

Give examples of modified amino acid derivatives

A

Dopamine

Thyroxine

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8
Q

What are modified amino acid derivatives derived from?

A

Tyrosine or tryptophan

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9
Q

What are peptides and proteins derived from?

A

Amino acids

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10
Q

Give some examples of peptides and proteins

A

Neuropeptides - vasopressi
Pituitary hormones - gonadotrophin
GI hormones - insulin

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11
Q

What are steroids derived from?

A

Cholesterol

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12
Q

What are some examples of steroids?

A

Sex hormones - testosteorne

Corticosteroids - hydrocortisone

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13
Q

What are eicosanoids derived from?

A

Lipids

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14
Q

What are some examples of eicosanoids?

A

Prostaglandins

Leukotrienes

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15
Q

What is an excipient?

A

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

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16
Q

Give examples of excipients

A
Diluents / fillers (lactose, water)
Surfactants (polysorbates)
Lubriants (Mg stearate)
Disintegrants (starch)
Viscosity enhancing agents (cellulose derivatives)
Flavours, colours, perfumes
Sweetening agents
Preservatives
17
Q

when is local delivery used?

A

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

18
Q

What are the biopharmaceutical factors of peptide hormones?

A

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

19
Q

How do the types of insulin vary?

A

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

20
Q

Describe the adaptions that make the pulmonary route so effective

A
Large surface area
Thin epithelial barrier
Good blood supply
Avoids harsh environment of GI tract
Avoids first-pass hepatic metabolism
21
Q

What is inhaled insulin?

A

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

22
Q

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

A
Parental route - IM, injection, implant
Transdermal route - patch or gel
Intranasal route - spray
Buccal route - mucoadhesive system
Vaginal - gel
23
Q

Describe nexplanon

A

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

24
Q

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

A

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

25
What are the advantages of intranasal administration?
Large surface area Highly vascularised Avoids first-pass hepatic metabolism Good availability for low molecular weight compounds
26
What are the disadvantages of intranasal administration?
Mucociliary clearance Metabolic activity Poor bioavailability for high molecular weight compounds
27
Describe the mucoadhesive testosterone buccal delivery system
Applied twice daily Adheres to gum or inner cheek Sustained release of testosterone through buccal mucosa
28
Describe treatment for hypogonadal males with mucoadhesive testosterone buccal system
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
29
What are the advantages of intrauterine progestogen-only device?
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