Lecture 19 Flashcards

(55 cards)

1
Q

____ is a potential for drug-receptor binding

A

Affinity

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2
Q

____ is a binding site with biological effect.

A

Receptor

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3
Q

This deals with the capacity to produce a biological effect

A

Intrinsic activity

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4
Q

These are substances that stimulate a receptor to produce a physiologic reaction and have intrinsic activity and affinity

A

Agonist

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5
Q

These are substances that oppose with the activity of a receptor and its endogenous substrate without producing a physiologic effect itself.

A

Antagonist

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6
Q

Antagonists have ____ but lack

A

affinity; intrinsic activity

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7
Q

What is the equation for efficacy

A

affinity x intrinsic activity

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8
Q

What does EC50 stand for. Where is it tested?

A

Effective concentration in 50% of subject. Tested in labs

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9
Q

What does ED50 stand for? Where is it tested?

A

Effective dose in 50% of subjects. More real world..tested in doses

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10
Q

What results in chronic antagonism

A

Hypersensitivity

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11
Q

This refers to a minimum amount of drug producing a maximum therapeatic effect

A

Maximum dose

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12
Q

a partial agonist has ____ intrinsic activity with potency and affinity within therapeutic range.

A

low

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13
Q

Pharmacodynamics deals with ____ on ____

A

drug; body

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14
Q

Pharmacokinetics deals with ____ on ____

A

body; drug

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15
Q

Potency is ____ related to EC50 for ____

A

inversely; agonists; The lower the EC50, the higher the potency

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16
Q

Potency is inversely related to ______ for drug antagonists

A

IC50; The lower the IC50, the higher the potency

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17
Q

What refers to the science of drug dosing

A

Posology

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18
Q

What is a biological response to a given dose

A

Potency

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19
Q

This deals with loss of pharmacological effect

A

Resistance

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20
Q

This is the ability to produce a desired effect vs adverse effect

A

Selectivity

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21
Q

This is the ability to act a specific receptor

A

specificity

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22
Q

This refers to rapidly decreasing therapeutic response

A

tachyphylaxis

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23
Q

This deals with congenital malformation

A

teratogenesis

24
Q

This is the amount of active drug reaching target tissue

A

bioavailability

25
_____ therapeutic indices are the safest
High
26
______ explains side effects. Lack of this deals with complications that has nothing to do with the region your targeting
Specificity
27
What are the six drug types
1. Supplemental; normally produced in body but in low amounts 2. Supportive: Helping pts cope with symptoms rather than cure 3. Symptomatic: Pt goes in with symptom and is looking for a relief 4. Diagnostic: No therapeutic benefit. 5. Therapeutic: Pt's are looking for a cure 6. Prophylactic: Protect
28
What are the different types of receptor motifs
1. Nuclear: steroids, hormones 2. G protein coupled: AChm, rhodopsin 3. Ion channels: GABA, glutamate, AChn 4. Enzymatic: insulin, epidermal growth factor 5. Calcium release: nitric oxide synthase
29
What are the different types of agonists
1. Direct: isoproterenol 2. Indirect: cocaine 3. Partial: Buspritone 4. Mixed: Tamoxifen 5. Inverse: Ro1545
30
____ _____ don't produce full biological effect. They demonstrate less dependency and withdrawal effects
Partial agonists
31
What are the types of binding selectivity for antagonists
1. Competitive 2. Non competitive 3. Uncompetitive
32
Describe non competitive antagonists
Not competing for same site as agonists; it has its own binding site and it doesn't matter if agonist is available or not its a matter of who reaches site first.
33
Describe uncompetitive antagonist
Requires the presence of an agonist
34
What is absorption influenced by
1. first pass metabolism | 2. patients age, gender, weight, pregnancy, health
35
What is volume of distribution
dose/drug in plasma | *influenced by route of administration
36
what is drug clearance
drug volume eliminated + time
37
What does a high volume of distribution mean
The drug does not readily remain in the bloodstream; which can expose patients to toxicity.
38
What does dehydration cause
A low volume of distribution because the lower plasma volume artificially enhaces drug plasma concentration
39
____ ____ is where there is a free exchange of substances into blood vessels that are close to mucous membranes.
mucous membranes
40
What are two key barriers to drug passage in the eye
RPE and corneal epithelium
41
What is the site of greatest administration of drugs administered topically
ciliary body
42
What are ocular drug barriers
1. Tear film 2. Cornea 3. Conjunctiva and sclera 4. Iris
43
Cornea and conjunctiva have outer ____ charges
negative
44
A dark iris is more ____
lipophilic; require more drops bc of more pigment and lasting effect is bound to be more sustained
45
Basal tear flow ranges from ____ to _____ul/min
0.5 = 2.2
46
If you have 10 ul of tear film on eye how long does it take to replenish that?
20 mins. 10/0.5
47
Entire tear volume is replaced between ____ and 20 mins
5
48
Normeal tear pH is around ___ to ___
7.1-7.6 (slightly basic)
49
A charged state _____ metabolism
reduces
50
Charged drugs accumulate in _____ media
aqueous
51
What are some drug barriers in the eye
1. Anterior chamber aqueous humor 2. Crystalline lens 3. Ciliary body 4. Vitreous 5. Blood retinal barrier
52
Chroidal and ____ blood flow is responsbile for bringing systemic drugs into the eye.
uveal
53
____ order is concentration independent. There is constant amount of clearance. Elimination per unit time is ____
Zero; linear
54
Most drugs are ____ order and they are concentration ____. There is a ____ ____ carrier. There is a constant proportion of ____ and constant ____ ___. Elimination per unit time is ______.
First; dependent; non saturable; clearance; half life; exponential
55
____ order means there is a saturable carrier at high concentrations only
Mixed