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Ocular Pharm > Lecture 19 > Flashcards

Lecture 19 Flashcards

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
Q

_____ therapeutic indices are the safest

A

High

26
Q

______ explains side effects. Lack of this deals with complications that has nothing to do with the region your targeting

A

Specificity

27
Q

What are the six drug types

A
  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
Q

What are the different types of receptor motifs

A
  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
Q

What are the different types of agonists

A
  1. Direct: isoproterenol
  2. Indirect: cocaine
  3. Partial: Buspritone
  4. Mixed: Tamoxifen
  5. Inverse: Ro1545
30
Q

____ _____ don’t produce full biological effect. They demonstrate less dependency and withdrawal effects

A

Partial agonists

31
Q

What are the types of binding selectivity for antagonists

A
  1. Competitive
  2. Non competitive
  3. Uncompetitive
32
Q

Describe non competitive antagonists

A

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
Q

Describe uncompetitive antagonist

A

Requires the presence of an agonist

34
Q

What is absorption influenced by

A
  1. first pass metabolism

2. patients age, gender, weight, pregnancy, health

35
Q

What is volume of distribution

A

dose/drug in plasma

*influenced by route of administration

36
Q

what is drug clearance

A

drug volume eliminated + time

37
Q

What does a high volume of distribution mean

A

The drug does not readily remain in the bloodstream; which can expose patients to toxicity.

38
Q

What does dehydration cause

A

A low volume of distribution because the lower plasma volume artificially enhaces drug plasma concentration

39
Q

____ ____ is where there is a free exchange of substances into blood vessels that are close to mucous membranes.

A

mucous membranes

40
Q

What are two key barriers to drug passage in the eye

A

RPE and corneal epithelium

41
Q

What is the site of greatest administration of drugs administered topically

A

ciliary body

42
Q

What are ocular drug barriers

A
  1. Tear film
  2. Cornea
  3. Conjunctiva and sclera
  4. Iris
43
Q

Cornea and conjunctiva have outer ____ charges

A

negative

44
Q

A dark iris is more ____

A

lipophilic; require more drops bc of more pigment and lasting effect is bound to be more sustained

45
Q

Basal tear flow ranges from ____ to _____ul/min

A

0.5 = 2.2

46
Q

If you have 10 ul of tear film on eye how long does it take to replenish that?

A

20 mins. 10/0.5

47
Q

Entire tear volume is replaced between ____ and 20 mins

A

5

48
Q

Normeal tear pH is around ___ to ___

A

7.1-7.6 (slightly basic)

49
Q

A charged state _____ metabolism

A

reduces

50
Q

Charged drugs accumulate in _____ media

A

aqueous

51
Q

What are some drug barriers in the eye

A
  1. Anterior chamber aqueous humor
  2. Crystalline lens
  3. Ciliary body
  4. Vitreous
  5. Blood retinal barrier
52
Q

Chroidal and ____ blood flow is responsbile for bringing systemic drugs into the eye.

A

uveal

53
Q

____ order is concentration independent. There is constant amount of clearance. Elimination per unit time is ____

A

Zero; linear

54
Q

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 ______.

A

First; dependent; non saturable; clearance; half life; exponential

55
Q

____ order means there is a saturable carrier at high concentrations only

A

Mixed

Ocular Pharm (12 decks)

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