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Pharmaceutical factors Flashcards

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1
Q

What is a double blind clinical trial?

A

Neither the participants nor the experimenters know who is receiving treatment

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2
Q

What is the MCC?

A

Medicine controls council

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3
Q

What is triptorelin?

A

An LHRH agonist

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4
Q

What is rifapentine?

A

Anti-TB drug

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5
Q

Name obstacles in the international pharmaceutical industry

A 
Patents 
Payor pressure
Generic competition
Safety concerns
Reputation
Earnings pressure
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6
Q

Which experimental heart pill created by Pfizer failed?

A

Torcetrapib

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7
Q

What is torcetrapib?

A

Cholesteryl ester transfer protein (CETP) inhibitor

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8
Q

What are pharmacokinetics?

A

Study of time course of drug concentration in the body

“What body does to the drug”

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9
Q

Name the aspects of drug input and output

A 
LADMET
Liberation
Absorption
Distribution
Metabolism
Excretion
Toxicity
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10
Q

Which pharmacokinetic factors are most important to determine dose?

A

Volume of distribution (Vd)
Half life (t1/2)
Clearance (CL)

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11
Q

What is absorption?

A

Movement of drug from site of administration to target site

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12
Q

What is distribution?

A

Diffusion/transport of drug from intravascular space to extravascular space

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13
Q

What is metabolism?

A

Chemical conversion/transformation of drugs into compounds for easier elimination

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14
Q

What is excretion?

A

Elimination of unchanged drug/metabolite from body via excretory system

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15
Q

What is bioavailability?

A

The fraction of administered dug that reaches the systemic circulation unchanged

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16
Q

What is the formula for bioavailability and why?

A

AUCoral/AUCIV

Because IV is always 100% bioavailable

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17
Q

Which factors affect bioavailability and how?

A

All ADME processes
Poor absorption = low bioavailability
High first-pass metabolism = low bioavailability

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18
Q

When is steady state achieved?

A

Rate of drug absorption = drug elimination

Cp plateaus

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19
Q

Which drugs will a missed dose affect?

A

Narrow therapeutic index drugs

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20
Q

How do you calculate Vd?

A

Total amount of drug in body (mg)/drug Cp (mg/L)

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21
Q

What is Vd an indication of?

A

Lipophilicity

Plasma protein binding

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22
Q

What is the relationship between Vd and Cp?

A

Inverse

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23
Q

What is the relationship between Vd and half life?

A

Direct

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24
Q

As Cp increases, what happens to Vd?

A

Decrease

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25
As Cp decreases, what happens to Vd?
Increases
26
As half life increases, what happens to Vd?
Increases
27
As half life decreases, what happens to Vd?
Decreases
28
What if half life?
The time necessary for the drug's plasma concentration to decrease by 1/2
29
What is the therapeutic range?
Above minimum therapeutic concentration | Below minimum toxic concentration
30
What does half life provide an index for?
Time-course of drug accumulation Time-course of drug elimination Dosing interval
31
Which factors influence half life?
Elimination rate Vd Patient factors
32
What effect does a higher clearance have on half life?
Decreased half life
33
What is the effect of a short half life on duration of action, dosing frequency, compliance, steady state and side effects
``` Short duration Increased dosing Lower compliance Earlier steady state Quicker side effects ```
34
What is the effect of a short long life on duration of action, dosing frequency, compliance, steady state and side effects
``` Long duration Decreased dosing Higher compliance Later steady state Longer side effects ```
35
What are first order kinetics?
The constant fraction of drug eliminated per unit of time
36
In first order-kinetics, half life is constant/variable?
Constant
37
In first-order kinetics, half life is concentration dependent/independent
Concentration independent
38
What are zero order kinetics?
The constant amount of drug eliminated per unit of time
39
In zero-order kinetics, half life is constant/variable?
Variable
40
In zero-order kinetics, half life is concentration dependent/independent?
Independent
41
Name drugs that undergo zero-order kinetics
Phenytoin Warfarin Alcohol
42
Name rate-limiting factors
Absorption Distribution Metabolism Excretion
43
What is clearance (CL)?
Volume of plasma cleared of drug per unit time
44
What is the equation for clearance?
Rate of elimination/drug Cp
45
How do you determine clearance in IV dosing?
dose/AUC
46
How do you determine clearance in oral dosing?
bioavailability x dose/AUC
47
How do you determine clearance in with Vd and half life?
0.693 x Vd/half life
48
How do you calculate maintenance dose rate?
CL x Css
49
When is steady state reached with every single drug?
4-5 x t1/2
50
A drug with a Vd <15L is likely...?
Hydrophilic
51
A drug with a Vd >40L is likely...?
Lipophilic
52
Name reasons for polypharmacy
Multiple diseases Combination therapy Complementary therapy
53
What does terfenadine interact with and why was it withdrawn?
Macrolides Grapefruit juice -> fatal arrythmias
54
What is terfenadine?
An antihistamine
55
What does astemizole interact with and why was it withdrawn?
Macrolides Grapefruit juice -> fatal arrythmias
56
What is astemizole?
An antihistamine
57
What does mibefradil interact with and why was it withdrawn?
Beta blockers | -> cardiogenic shock
58
What is mibefradil?
Non-selective calcium channel blocker
59
What does it mean if a drug has a narrow therapeutic index?
Therapeutic effects is close to the adverse effect threshold
60
What factors make a drug most suceptible to drug interactions?
Narrow therapeutic index High 1st pass metabolism Single route of elimination
61
Name the two types of drug interactions
Pharmacodynamic | Pharmacokinetic
62
Name the kinds of pharmacodynamic interactions
Additive (sum of) Synergistic (>sum of) Antagonistic
63
Give an example of additive/synergistic anticoagulants
Warfarin + aspirin
64
Give an example of antagonistic drugs
Bronchodilator + antihypertensive | Flumazenil + benzodiazepine
65
Why do bronchodilators and antihypertensives result in an antagonistic effect?
``` Bronchodilator = beta adrenergic activation Antihypertensive = beta adrenergic inhibition ```
66
What is a substrate?
Competes for same binding site
67
Name factors that affect drug absorption
``` Drug solubility Gut flora Protein carriers Gut pH Gastric motility Transporter function ```
68
Give an example of how adsorption agents play a role in drug interaction
Activated charcoal -> reduced toxin levels | Tetracycline failure due to dairy/antacids (insoluble complex forms)
69
Give an example of how gut flora plays a role in drug interaction
Macrolide antibiotics kill gut flora -> digoxin-induced toxicity (incr bioavailbility)
70
Give an example of how gut pH plays a role in drug interaction
Antacids -> incr gut pH -> ketoconazole failure
71
Comment on ionized vs unionized drugs crossing plasma membranes
``` Ionized = struggles to cross plasma membrane Uncharged = crosses plasma membrane easily ```
72
Give an example of how gastric motility plays a role in drug interaction
Prokinetic -> metformin antidiabetic effect reduced
73
What are p-gp transporters and why are they important in drug interactions?
P-glycoprotein transporters Protective measure to efflux cytotoxins from intracellular compartment -> extracellular space/gastric lumen Inducing leads to increased efflux and therapeutic failure Blocking leads to higher accumulation and bioavailibility -> adverse effects
74
Give an example of how blocking p-gp transporters plays a role in drug interaction
Macrolide antibiotics prevent p-gp efflux of digoxin -> digoxin toxicity
75
Why are p-gp transporters important in cancer treatment?
Higher p-gp expression = higher cancer resistance | Block the p-gp -> higher anticancer activity
76
Which plasma protein binds acidic and basic drugs?
Albumin
77
Which plasma protein binds only basic drugs?
Alpha-acid glycoprotein
78
Comment on plasma-bound drugs
Pharmacologically inert Cannot be filtered by kidney Free fraction = bioactive and can be metabolised and removed
79
Give an example of how plasma proteins play a role in drug interaction
Streptozocin induces hypoalbuminaema -> incr adverse effects of other drugs Ibuprofen displaces methotrexate from albumin -> incr methotrexate toxicity
80
What is phase I metabolism?
CYP450 monooxidase system prepares drugs for further chemical conversion
81
What is phase II metabolism?
Inactivation of drug | Increases hydrophilicity
82
Comment on how enzyme induction plays a role in drug interaction
Decr drug plasma concentrations -> treatment failure | Incr pro-drug conversion/toxic metabolite formation -> adverse effects
83
Give an example of how enzyme induction plays a role in drug interaction
Macrolide antibiotics reduce OCP fficacy
84
Comment on how enzyme inhibition plays a role in drug interaction
Higher plasma [ ] -> adverse effects | Decr active metabolites -> treatment failure
85
Give an example of how enzyme inhibition plays a role in drug interaction
Grapefruit juice inhibits CYP3A4 metabolism -> incr diazepam toxicity
86
Which organ is the main excretory organ?
Kidney
87
Which factors affect kidney excretion?
Urinary pH Transporter competition Renal blood flow Active tubular secretion
88
What is the affect of acidic urine on excretion?
Higher weak base excretion
89
What is the affect of alkaline urine on excretion?
Higher weak acid excretion
90
Give an example of how active tubular secretion plays a role in drug interaction
Probenecid excreted > penicillin -> incr penicillin [ ] | Ibuprofen excreted > methotrexate -> incr methorexate [ ]
91
What is the mechanism of drug interaction due to fatty meals and what is the result?
Increased absorption of lipophilic drugs | Increased bioavailibility of griseofulvin
92
Griseofulvin is lipophilic/lipophobic
Lipophilic
93
What is the mechanism of drug interaction due to fibre-rich meals and what is the result?
Increased adsorption of drugs | Decreased bioavailbility of digoxin
94
What is the mechanism of drug interaction due to pressor/tyramine-rich meals and what is the result?
Increased catecholamine release due to tyramine | Hypertensive crisis with selegiline
95
What is the mechanism of drug interaction due to sodium-rich meals and what is the result?
Increased sodium [ ] | Increased absorption of lithium
96
What is the mechanism of drug interaction due to potassium-rich meals and what is the result?
Increased potassium [ ] | Cardiac arrythmias w/ potassium sparing diuretics
97
What is the result of an interaction with alcohol and hepatotoxins?
Increased hepatotoxicity of acetominophen
98
What is the result of an interaction with alcohol and acetaldehyde dehydrogenase inhibitors?
Severe hangover effect with disulfarim
99
What is the result of an interaction with alcohol and NSAIDs?
Increased mucosal damage with aspirin
100
What is the result of an interaction with caffeine-rich drinks and anxiolytics?
Antagonism of diazepam therapeutic effects
101
What is the result of an interaction with caffeine-rich drinks and stimulants?
Stimulant-toxicity with theophylline
102
What is the result of an interaction with grapefruit juice and cyclosporine?
Decreased metabolism of cyclosporine (CYP3A4)
103
What is warfarin?
A vitamin K epoxide reductase inhibitor
104
What is the intended INR with warfarin use?
INR stable 2-4
105
How is warfarin metabolised?
CYP450 metabolism esp CYP2C9
106
What is the mechanism of interaction of warfarin with oral antibiotics and what is the result?
Inhibition of CYP2C9 Kills gut flora Increased bleeding
107
What is the mechanism of interaction of warfarin with NSAIDs and what is the result?
Additive/synergistic anticoagulant effect Increased bleeding
108
What is the mechanism of interaction of warfarin with antiplatelet drugs and what is the result?
Additive/synergistic anticoagulant effect Increased bleeding
109
What is the mechanism of interaction of warfarin with ginger/garlic and what is the result?
Additive/synergistic anticoagulant effect Increased bleeding
110
What is the mechanism of interaction of warfarin with vitamin K and what is the result?
Oversaturates the coagulation cascade Treatment failure -> thromboses
111
What is the mechanism of interaction of warfarin with St John's wort and what is the result?
Induction of CYP3A4 and CYP2C19 Treatment failure -> thromboses
112
What is the mechanism of interaction of macrolides with other drugs?
Potent CYP4A inhibitors | Gut flora destruction
113
What is the mechanism of interaction of macrolides with digoxin and what is the result?
P-gp inhibition Gut flora destruction Digoxin toxicity
114
What is the mechanism of interaction of macrolides with clozapine and what is the result
CYP3A4 inhibition Seizures and disorientation
115
What is the mechanism of interaction of macrolides with midazolam and what is the result
CYP3A4 inhibition Increased hypnotic effect
116
What is the mechanism of interaction of macrolides with theophylline and what is the result
CYP3A4 inhibition Tremors and tachycardia
117
What is the mechanism of interaction of macrolides with quinidine and what is the result
P-gp inhibition CYP3A4 inhibition Prolonged QT interval Ventricular dysrhythmias
118
How do MAO-I increase serotonin concentrations?
Reduce serotonin degradation
119
What is the mechanism of interaction of monoamine oxidase inhibitors with SSRIs and what is the result
Increased serotonin levels Serotonin syndrome
120
What is the mechanism of interaction of monoamine oxidase inhibitors with TCAs and what is the result
Increased catecholamine levels Hypertensive crises Psychoses Serotonin syndrome
121
What is the mechanism of interaction of monoamine oxidase inhibitors with catecholamine releasers/reuptake inhibitors and what is the result
Increased catecholamine levels Hypertensive crises Psychoses Serotonin syndrome
122
What is the mechanism of interaction of monoamine oxidase inhibitors with local anaesthetics and what is the result
Increased blood pressure Hypertensive crises
123
What is the mechanism of interaction of monoamine oxidase inhibitors with tyramine-containing food and what is the result
Increased catecholamine release Hypertensive crises
124
Explain the interaction of tyramine with MOA-I
Tyramine in foods = catecholamine releasing agent -> noradrenaline release Noradrenaline metbaolised by MOA MOA-I -> incr noradrenaline -> advers effects eg incr blood pressure
125
What tyramine intake is enough to interact with a MOA-I?
>6mg
126
What occurs in chronic tyramine intake with MOA-I?
Tyramine releases octopamine and noradrenaline -> less catecholamines -> less adverse effects
127
How do NSAIDs work?
Inhibit COX -> decr prostaglandin synthesis
128
What is the mechanism of interaction of NSAIDs with warfarin and what is the result
Increased anticoagulant effect Increased bleeding
129
What is the mechanism of interaction of NSAIDs with methotrexate and what is the result
Displaced methotrexate from albumin + decrease renal clearance Methotrexate toxicity
130
What is the mechanism of interaction of NSAIDs with digoxin and what is the result
Reduced renal clearance Digoxin toxicity
131
What is the mechanism of interaction of NSAIDs with lithium and what is the result
Reduced renal clearance Tremors and seizures
132
What is the mechanism of interaction of NSAIDs with ACE-I and what is the result
Inhibition of prostaglandin-mediated vasodilation Treatment failure: hypertension
133
What is the mechanism of interaction of NSAIDs with diuretics and what is the result
Salt and water retention Treatment failure: hypertension
134
What is the mechanism of interaction of grapefruit juice with amiodarone and what is the result
CYP3A4 inhibition and reduced mRNA expression Arrythmias
135
What is the mechanism of interaction of grapefruit juice with cyclosporine and what is the result
CYP3A4 inhibition and reduced mRNA expression Immunosuppression
136
What is the mechanism of interaction of grapefruit juice with diazepam and what is the result
CYP3A4 inhibition and reduced mRNA expression Increased sedation
137
What is the mechanism of interaction of grapefruit juice with quitapine and what is the result
CYP3A4 inhibition and reduced mRNA expression Hallucinations Hypotension
138
What is the mechanism of interaction of grapefruit juice with loperamide and what is the result
CYP3A4 inhibition and reduced mRNA expression Severe GI pain
139
What is the mechanism of interaction of grapefruit juice with oxycodone and what is the result
CYP3A4 inhibition and reduced mRNA expression Bradycardia Hallucinations
140
How does grapefruit juice work?
Potent CYP3A4 inhibitor
141
How does St John's wort work?
CYP450 inducer
142
What is St John's wort used for?
Hypericum perforatum preparation -> anxiety and depression
143
What is the mechanism of interaction of St John's wort with warfarin and what is the result
Induction of CYP3A4 and CYP2C19 Treatment failure: increased coagulation
144
What is the mechanism of interaction of St John's wort with cyclosporine and what is the result
Induction of CYP3A4 and CYP2C19 Treatment failure: organ rejection
145
What is the mechanism of interaction of St John's wort with contraceptives and what is the result
Induction of CYP3A4 and CYP2C19 Treatment failure: failed contraception
146
What is the mechanism of interaction of St John's wort with ARVs and what is the result
Induction of CYP3A4 and CYP2C19 Treatment failure: viral replication
147
What is the mechanism of interaction of St John's wort with SSRIs and what is the result
Increased plasma serotonin levels Serotonin syndrome
148
What is the mechanism of interaction of St John's wort with aminolevulinic acid and what is the result
Increased photosensitvity Skin irritation

Pharmacology (32 decks)

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