Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

PHARMACOLOGY - 1 > 10 – Biopharmaceutics & Drug Types > Flashcards

10 – Biopharmaceutics & Drug Types Flashcards

1
Q

Drug product is comprised of different components

A
  • Active pharmaceutical ingredients (API)=’drug substance’
  • Everything else (‘excipients’)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Oral route: dosage forms

A
  • Solid
  • Semi-solid
  • Oral solution
  • Feed premix
    *usually have longer expiry dates
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Capsule vs. pill/tablet

A
  • Tablets can be split
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Parenteral (‘injectable w/needle’) (IM/SC/IV) route: dosage forms

A
  • Usually solution (water-soluble)
  • Sometimes non-aqueous (ex. oil)
    **needs to be sterile
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Topical (stay on skin) vs. transdermal (through the skin) route: dosage forms

A
  • Cream
  • Liquid
  • Gels
  • Patches
    **intended for local effect
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Intra-mammary (IMM) route: dosage forms

A
  • Suspension
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Intranasal (IN) route: dosage forms

A
  • Liquid
  • Aerosolize/nebulize (convert liquid to fine particles)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Rectal route: dosage forms

A
  • Suppository
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Buccal route: dosage form

A
  • Fast dissolving tablet or paste
    **avoids first pass (hepatic) metabolism (BUT make sure it isn’t swallowed)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Why not just administer the active pharmaceutical?

A
  • Just dosing API probably won’t MAXIMIZE its efficacy or safety
  • Ex. how much reaches systemic circulation, stability, taste
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

If use a drug product with a delayed absorption what changes?

A
  • Usually C max
  • Tmax
  • AUC (elimination half-life)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Oral administration excipients

A
  • Binding agent
  • Coating or capsule
  • Flavouring agent
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Oral administration: binding agent

A
  • Delays DISAGGREGATION (break down tablet) and DISSOLUTION (solubilizes API)
  • *both necessary to permeate intestinal cell
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Oral administration: coating capsule

A
  • Protect API from acid in stomach
  • Decrease irritation in proximal GIT
  • Delay timing of absorption
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Parenteral injection (IM, SC, IV) excipients

A
  • pH adjuster
  • salt or chelating agent
  • preservative
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Parenteral injection: pH adjuster

A
  • makes injection less irritating
  • increase solubility of API
  • enhance stability of API in solution
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Parenteral injection: salt or chelating agent

A
  • alters API solubility
  • determines how long before API is released
  • vasoconstriction: impact on absorption?
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Parenteral injection: preservative

A
  • maintain sterility
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Long story short of biopharmaceutics

A
  • formulation matters
  • different forms of same API can have BIG differences
  • messing with formulation changes the drug product
20
Q

Pioneer drug product

A
  • innovator
  • first one that came to market
21
Q

Generic drug product

A
  • copy of the pioneer
22
Q

Compounded drug product

A
  • making up a drug product in the clinic, but not approved
23
Q

What is the point of generic drugs?

A
  • More drug product availability
  • More competition = decrease prices
  • Only once pioneer drug patent has expired
24
Q

How come pioneer drugs are more expensive?

A
  • High costs for initial drug approval
  • Patents allow for exclusive market ($$$)
  • When patent runs out=price typically drops
25
Q

How come generic drugs are cheaper?

A
  • ‘proven’ safety and efficacy of pioneer drug
  • NOT required to reproduce efficacy and safety studies that pioneer did
26
Q

What do generic drugs need to be approved?

A
  • Manufacturing and chemistry (PRODUCT QUALITY)
    o Potency
    o Purity
    o Stability, sterility, etc
  • Clinical efficacy and safety
27
Q

Clinical efficacy and safety of generic drugs

A
  • Must be same STRENGTH and DOSAGE FORM
  • Demonstrate BIOEQUIVALANCE with pioneer product
  • *’clinically interchangeable’
28
Q

Bioequivalence

A
  • Rate and extent of absorption is the same between two pharmaceutically equivalent formulations of drugs within ALLOWABLE LIMITS when under similar experimental conditions
  • *assumption: equal plasma concentrations=equal clinical efficacy and safety
  • **Cmax and AUC=same
29
Q

Pharmaceutically equivalent

A
  • Two drugs that contain IDENTICAL AMOUNTS of IDENTICAL MEDICINAL INGREDIENTS in comparable DOSAGE FORMS
  • Ex. if pioneer drug is tablet, generic version cannot be a solution
  • *doesn’t necessarily contain the same non-medicinal ingredients
30
Q

How to PROVE bioequivalence: blood-level study

A
  • Each animal gets both products with a ‘washout period’
    o 10x half life to avoid drug carry over into next period
  • Dosing same animal twice reduces inter-individual variability
  • Collect multiple blood samples over time
  • Determine plasma concentrations (REQUIRES VALIDATED ANALYTICAL METHOD
  • *look at ratio of AUC and Cmax (needs to be between 0.8-1.25=80% confidence intervals)
31
Q

If below 80% CI: blood-level study

A
  • Worried about efficacy
32
Q

If above 80% CI: blood-level study

A
  • Worried about safety
33
Q

Compounding

A
  • Combining or mixing multiple ingredients (at least one is a drug) to create a final product in an appropriate dosing form
34
Q

Why use compound drugs?

A
  1. Available formulations are NOT appropriate for a specific patient (diluted form for very small animals)
  2. Improve client compliance (more palatable oral product, non-oral formulation)
  3. No approved drug product commercially available
    **COST is NOT a valid reason
35
Q

FDA rules on compound drugs

A
  • Used to treat an UNMET therapeutic need or reduce animal suffering
  • Do NOT cause harm to treated animal
  • Do NOT result in therapeutic failures
  • Do NOT result in violative drug residues (food animals)
36
Q

Compounded drug ‘ladder’

A
  • Approved vet drug: on label
  • Approved vet drug: extra-label
  • Approved human drug
  • Compounded drug: vet drug
  • Compounded drug: human drug
  • Compounded drug: active pharmaceutical ingredient
37
Q

Compounding concerns

A
  1. PURITY of compound drug
  2. POTENCY of compounded drug
  3. Stability of compounded formulation
  4. Pharmacokinetic changes due to formulation
38
Q

Purity of compound drug

A
  • ‘quality’ of drug
  • Drug that is present is supposed to be there
  • No other drugs there if not supposed to be
39
Q

Potency of compound drug

A
  • ‘quantity’ of drug
  • ACCURACY with label quantity
  • Manufactured drugs: concentration must be within +/- 10%
40
Q

Meloxicam example: compounding

A
  • Tested compounded products
  • Potency: 37-132% claimed concentration
  • *what batch did you get? You don’t know!
41
Q

Stability of compounded formulation

A
  • Hydrolysis (comes dry=keep it dry)
  • Oxidation (pink or amber colour change)
  • Consistency (precipitates, settling out)
  • Expiry date? (25% of time left on original expiry date)
  • *if say water-based compound good for 3-6months=BS! (usually put 14 days)
42
Q

Compound stability case: in UK with epidural injection

A
  • ‘preservative free’
  • Fungal contamination of ‘sterile’ MPA vials
43
Q

Pharmacokinetic changes due to formulation

A
  • Absorption (oral, transdermal)
  • Bioavailability
44
Q

Compounded transdermal products

A
  • *just because there is a gel or patch with API in it does NOT mean it will be absorbed
  • Some APIs will NOT permeate the skin
  • Results vary BETWEEN and WITHIN patients
  • Products no uniform between pharmacies
45
Q

What to tell your clients about a compound drug product

A
  • Explain why you are prescribing it (SPECIFIC PATIENT, no approved drug available)
  • Have a method of assessing efficacy
  • Get INFORMED CONSENT and DOCUMENTATION IN MEDICAL RECORD
46
Q

What to NOT tell your client about a compound drug product

A
  • Call it a ‘generic version’ or ‘the same thing’
  • Use it strictly because it’s cheaper

PHARMACOLOGY - 1 (12 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions