OptoP: Ocular Medications - Weeks 6 and 7 Flashcards

1
Q

When an optometrist diagnoses glaucoma and starts anti-glaucoma therapy: within what time period should a referral be made to an ophthalmologist?

A

Within 4 months of starting treatment

(referral can be for either: a second opinion or to consider a surgical option)

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2
Q

What condition is the majority of optometry drug prescriptions for?

A

Glaucoma (45.4% of drug prescriptions)

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3
Q

What route of drug administration is best suited for a superficial eye condition?

A

Topical

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4
Q

What route of drug administration is best suited for a deep eye condition?

A

Oral or injection

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5
Q

Between topical vs oral and injection, which route of drug administration is more likely to produce adverse effects (AEs)?

A

Oral and injection route (because they are non-targeted)

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6
Q

Rate the timing of drug availability from fastest to slowest for 3 routes of admin: topical, oral and injection

A

injection>oral>topical

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7
Q

How do oral drugs enter the bloodstream?

A

by absorption over the GI tract. They are also subject to first-pass metabolism in the liver

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8
Q

How do topical drugs enter the bloodstream? (2)

A

by direct absorption across conjunctival blood vessels (~30% of the drug) and by draining via naso-lacrimal duct into nasal cavity and eventually gut (70%)

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9
Q

List the 3 modes of absorption for topical drugs

A

Nasal mucosa (rugae, very fast blood stream)
Cross membrane of olfactory nerve (direct access to CNS (fast). Very potent compared to injection) - e.g. cocaine snorting
Gut (slow)

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10
Q

When may drugs produce systemic effects when in the blood stream?

A

When they are unbound

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11
Q

What binds drugs in the bloodstream? (2) What does this do?

A

Binding is by blood cells and proteins. Binding inactivates drug for metabolic breakdown

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12
Q

What is the “Double-D” rule for minimising the systemic absorption of topical drugs

A

Don’t open eyes (1-2 mins) (minimise conjunctival flow)
Digital occlude puncta (reduce puncta access)

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13
Q

By how much does the Double-D rule reduce concentration of topical drug in the blood?

A

by 65-70%

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14
Q

What features of drugs are required to cross the corneal barrier? (2)

A

To cross the corneal barrier, drugs must be:
- Hydrophilic (to dissolve in tears)
- Lipophilic (to cross cellular membranes)

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15
Q

What is a drug formulary?

A

a list of prescription drugs

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16
Q

What is the best formulary for corneal absorption?

A

Acetate formulary (i.e. acetate formulation)

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17
Q

Describe the features of an acetate formulation in relation to corneal absorption (5) incl.
- rate of absorption
- degree of toxicity
- speed and duration of effect

A

rapid absorption
borders on toxicity
at a lower dose avoids toxicity (dotted line on graph)
effect = fast but short lived
good to load with multiple drops

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18
Q

Describe the features of a phosphate formulation in relation to corneal absorption (3) incl.
- speed of absorption
- duration of effect
- degree of toxicity

A

slower absorption than acetate
longer duration than acetate
non-toxic therapuetic

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19
Q

Describe the features of a phosphate OINTMENT formulation in relation to corneal absorption (2) incl.
- speed of release (in comparison to phosphate and acetate)
- therapeutic duration (in comparison to phosphate and acetate)

A

Slowest speed of release
Longest therapeutic duration

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20
Q

Describe the steroid potency, penetrance, and capacity to raise IOP of the following drugs in the eye:
- Hydrocortisone alcohol and Hydrocortisone acetate

A

Low

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21
Q

Describe the steroid potency, penetrance, and capacity to raise IOP of the following drugs in the eye:
- Fluorometholone alcohol and Prednisolone phosphate

A

Mid

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22
Q

Describe the steroid potency, penetrance, and capacity to raise IOP of the following drugs in the eye:
- Fluoromethalone acetate

A

High

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23
Q

Describe the steroid potency, penetrance, and capacity to raise IOP of the following drugs in the eye:
- Prednisolone acetate

A

Very High (highest penetrance of the group of steroids mentioned)

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24
Q

Describe the steroid potency, penetrance, and capacity to raise IOP of the following drugs in the eye:
- Dexamethasone alcohol

A

Very Very High (however penetrance only mid-high)

25
Q

What is the rule of thumb for steroid eye drops potency, penetrance, and capacity to raise IOP?

A

Acetate > Alcohol&raquo_space; Phosphate

26
Q

Name the 6 drug classes for optometrists

A

Allergy
Anti-inflammatory
Analgesics
Anti-biotics
Anti-virals
Anti-glaucoma

27
Q

What 3 classes of response occur in response to mast cell degranulation (i.e. allergic respones)? What do each of these responses result in? (2, 3, 1)

A

Histamine response: results in red, itchy eye
Cytokine response: results in chemosis, swelling and mucous production in the eye
Cellular response: results in inflammation

28
Q

When does the cellular response occur after mast cell degranulation?

A

Occurs after the histamine and cytokine response once the allergic response has been going on for some time

29
Q

What does the cellular response to mast cell degranulation involve? (2)

A

Eosinophils and Neutrophils undergo chemotaxis to the site of degranulation via Eosinophil Chemotactic Factor (ECF) and Neutrophil Chemotactic Factor (NCF) respectively

Once there, they cause inflammation

30
Q

Name 3 cytokines involved in the cytokine response to mast cell degranulation and state what they do

A

Heparin: anti-coagulant
Tryptase: COX-2, PG production + fibroblast proliferation
Chymase: increases vascular permeability via angiotensin II

31
Q

Which cytokine in response to mast cell degranulation is responsible for mucous production?

A

Tryptase

32
Q

Which cytokine in response to mast cell degranulation is responsible for chemosis?

A

All 3 of them

33
Q

How long once the allergic response has begun does the cellular response take to kick in/start?

A

usually about a week

34
Q

How can we manage the cellular response to mast cell degranulation? (4)

A

Use anti-metabolites: cyclosporin and tacrolimus
Also can use steroids (affects early in cellular response)

35
Q

How long do anti-metabolites take to act to manage allergic response? Why is this?

A

a long time. At least 2 or 3 months before they have an effect. This is because they affect the cellular response which itself takes a while to start (although that only takes 1 week)

36
Q

How can we manage the histamine response to mast cell degranulation? (2)

A

Lubricants
Antihistamines

37
Q

How can we manage the cytokine response to mast cell degranulation? (2)

A

Steroids (for all cytokines)
NSAIDs (for use against tryptase)

38
Q

How can we manage allergic response by acting on the mast cell?

A

Mast cell stabilizer.

39
Q

When should you use a mast cell stabilizer? Why might this be an issue?

A

Before it degranulates. This is an issue because generally the patient won’t come in to treat allergies before it degranulates (instead they come in when they already have symptoms)

40
Q

How are mast cell stabilizers suggested to be used to patients?

A

If patient has hayfever, start using the mast cell stabilizer one month before hayfever season starts

41
Q

What condition is cyclosporin particularly useful for?

A

dry eye disease (for the cellular responses in dry eye disease)

42
Q

Name 8 kinds of anti-allergy medications

A

Ocular lubricants
Vasoconstrictors
Astringents
Anti-histamines
Mast cell stabilisers (MCS + AH)
NSAIDS
Corticosteroids
Anti-metabolites

43
Q

What can you use ocular lubricants for? (4)

A

Mild ocular surface irritation (incl. SPK)
Dry eye
Neurotrophic keratitis
Adjunct in severe inflammation

44
Q

What allergic conditions are vasoconstrictors used for? (2)

A

Mild allergic conjunctivitis
Other mild non-specific hyperaemia

45
Q

What type of agents are anti-allergy vasoconstrictors?

A

Alpha adrenergic agents

46
Q

What is the role of astringents in anti-allergy treatment?

A

Reduce mucoid discharge in allergic surface disease

47
Q

Name 1 chemical compound that astringents contain

A

Zinc sulphate

48
Q

Which histamine receptor are anti-histamines selective for?

A

H1 receptor

49
Q

Are mast cell stabilisers H1 selective?

A

Yes. So they also have an anti-histamine effect

50
Q

What is the mechanism of NSAIDs?

A

Inhibit COX, which decreases prostaglandin synthesis and prostaglandin-mediated inflammation

51
Q

What is the mechanism of corticosteroids? (3)

A

Intracellular receptor-mediated inhibition of inflammatory cascade, fibroblast and keratocyte activity

52
Q

What type of drug administration may be required if inflammation is deeper than the iris? (4)

A

Either:
Oral, or
Intraocular/sub-conj./sub-Tenon’s injection may be required

53
Q

What is the sub-tenon’s space?

A

A space between the capsule and the sclera

54
Q

What effect does injection of NSAIDs into the eye have on the hypothalamic axis?

A

Suppresses it

55
Q

Do NSAIDs perform inhibition on the anterior or posterior eye?

A

Anterior. They inhibit Cox anteriorly

56
Q

How does topical use of NSAIDs affect the posterior pole?

A

Reduce overall ocular PG load at posterior pole

57
Q

What is the typical dose of an oral steroid?

A

40mg po bd, 2d to 7d then taper over 2-4wks

58
Q

Name 3 side effects of topical steroid treatment

A

Promotes microbial activity
Masks clinical signs
Delays wound healing