OptoP: Ocular Analgesics - Week 10 Flashcards by Alexander Bowden

How many Drug schedules are there? Describe 3 of them

9 in total.
Schedule 2: therapeutic use available for supply by pharmacists or appropriately licensed persons
Schedule 3: therapeutic use but are dangerous or liable to abuse so as to restrict supply by pharmacists etc.
Schedule 4: prescription only substances intended for therapeutic use but the safety or efficacy requires further evaluation

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For currently listed S2 drugs for optometrists:

- name 2 anti-infectives

dibromopropamidine

- propamidine

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For currently listed S2 drugs for optometrists:

- name 2 anti-inflammatories

antazoline
azelastine
ketotifen
levocabastine

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For currently listed S2 drugs for optometrists:

- name 2 decongestants/analgesics

lodoxamide
naphazoline
pheniramine
sodium cromoglycate

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For currently listed S2 drugs for optometrists:

name 1 drug for miotic, mydriatic or cycloplegia
what schedule of drug do other drugs that have this effect typically fall under?

phenylephrine

other drugs fall under S4 generally (prescription only)

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What class and schedule of drug does chloramphenicol fall under?

S3 drug and is an anti-infective

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What schedule of drug for optometry use is the most common for the following?
- anti-infectives, anti-inflammatories, anti-glaucoma, miotic, mydriatic, cycloplegic, local anaesthetics

In fact, anti-glaucoma and local anaesthetics for optometrists are all S4 (and have no drugs in S2 or 3)

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Name 3 characteristics of a not so serious red eye

tired, drinking
vasodilation of blood vessels
usually associated soreness

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Name 1 characteristic of a more serious red eye

persistent red-eye

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What actions should you take when you see a more serious red eye (2)

identify cause

- decide on best option (understand mediators involved)

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What type of drug is usually adequate to treat a not so serious red eye?

S2 vasoconstrictors (alpha-adrenoceptor agonists) usually adequate

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What 2 drug classes might be used to treat a more serious red eye?

Anti-inflammatory: if irritation due to foreign particles or allergic conditions
Anti-infective: if bacterial, viral, or fungal cause

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What is the vascular response and cellular response to inflammation? What is the primary defence mechanism in inflammation?

Vascular: vasodilation
Cellular: cell migration (WBCs, mast cells)

Primary defence mechanism = pain

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Name the 5 mediators of inflammation and rate how much they contribute to the following: 
A: dilatation
B: vascular permeability
C: chemotaxis
D: pain

A    B    C     D
Histamine      ++  +++   -     -
Serotonin      +/-    +     -     - 
Bradykinin    +++   +     -    +++ 
Prostanoids  +++   +    +++  +
Leukotrienes  -    +++  +++  -

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Which mediators of inflammation have the largest effect on dilatation? (2)

Bradykinin and Prostanoids (closely followed by histamines)

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Which mediators of inflammation have the largest effect on vascular permeability? (2)

Histamine and Leukotrienes

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Which mediators of inflammation have the largest effect on chemotaxis? (2)

Prostanoids and Leukotrienes

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Which mediator of inflammation has the largest effect on pain? (1) Are there any other mediators that cause pain?

Bradykinin. (prostanoids cause slight pain)

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How does pain intensity and duration correlate with the use of the following:
A: Prostaglandin (PGE2)
B: Bradykinin
C: PGE2 + Bradykinin

A: slight pain
B: slightly more pain
C: a lot more pain

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How can we reduce the pain intensity of PGE2 + Bradykinin?

By blocking the action of one of this synergistic pair - this may be sufficient to inhibit the overall pain response
e.g. prostaglandin synthesis inhibitors

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Describe the Arachidonic Acid (AA) pathway and how it branches out in 2 steps

Lipid Membrane produces A.A via phospholipase

2. A.A differentiates into either prostanoids (via cyclooxygenase) or Leukotrienes (via lipoxygenase)

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Name 2 types of prostanoids and describe their effects (4 effects for 1 type and 1 effect for the other)

Prostaglandins:
- hyperalgesia, vasodilation, vasc. permeability (leukocyte trapping)
Thromboxane A2:
- aggregation of platelets

Name 2 prostaglandins

Prostaglandins:

PGE2
PGI2

Name 1 leukotriene and describe its effects (2)

LTB4:

chemoattraction
neutrophil function (phagocytosis)

What class of molecule are prostanoids and leukotrienes?

Eicosanoids

In regards to NSAIDS, describe the following: A: What pathways do they inhibit? B: What treatment are they accepted as an alternative for?

A: Inhibits prostanoid pathway only (by reducing amplification of inflammatory signals) B: Accepted alternative/adjucent to steroid treatment

How safe are NSAIDs? List Contraindications (2)

Generally considered Safe. Contraindications: - aspirin/NSAID anaphylactic reaction - bisulphate sensitivity (for Indomethacin only)

List 4 potential adverse effects of NSAIDs

1. burning, stinging or mild discomfort on application 2. ocular irritation, itching and redness 3. delayed epithelial growth and wound healing (Diclofenac only) 4. Potential bleeding risk (local + systemic)

Describe the action of the following classes of drugs on the AA pathway: A: Steroids B: NSAIDS

A: steroids inhibit phospholipase and cyclooxygenase B: NSAIDs inhibit cyclooxygenase

Describe the mechanism of action of 'transactivation' with glucocorticoids (a steroid) (5)

- Glucocorticoids travel through the membrane and bind to the cytosolic GR (glucocorticoid receptor) - The newly formed complex then translocates itself into the cell nucleus, - where it binds GREs (glucocorticoid response elements) in the promoter region of the target genes - resulting in the regulation of gene expression (transactivation) ("these genes turn ON") - result in increase in Lipocortin-1

What is the function of Lipocortin-1?

it is a phosphoprotein that inhibits PLA-2

Describe the mechanism of action of 'transrepression' with glucocorticoids (a steroid) (3)

- the activated GR binds to DNA in the same site where the transcription factor would bind (GR binds nGREs) - this prevents the transcription of genes that are transcribed via the activity of that factor "these genes turn OFF" - results in reduction of cytokines, COX-2 and PLA2

What does nGRE stand for?

Negative Glucocorticoid Response Element

List 12 systemic side effects of steroids (don't really have to know all of these)

- osteoporosis - immunosuppression/risk of infection - hypertension - fat deposition, abdominal, face, neck - thinning skin, arms, legs - muscle wasting - behavioural disturbances - peptic ulceration - growth inhibition - delay/poor wound healing - cataracts

List 3 advantages of topical steroids

- minimise systemic effects - can place where needed - can treat uniocular disease

List 1 disadvantage and 2 sub-disadvantages of topical steroids

- specific local reactions: - may leave white residue, may affect vision

list 4 common ocular side-effects of topical steroids

- ocular hypertension - reduced corneal healing - rebound inflammation - cataract formation

List 6 rare ocular side-effects of topical steroids

- corneal melt - refractive changes - ptosis - lid swelling - exophthalmus - adrenal insufficiency

Name 2 indications for the use of topical steroids

- allergic and selected inflammatory conditions of lids, conjunctiva, cornea, iris and cil. body - post-operative inflammation

Name 1 contra-indication for the use of topical steroids

ocular infection

Name 2 specific considerations for the use of topical steroids

- aggravation of glaucoma | - increase risk of ocular hypertension and cataract

Name 5 topical steroids and rate the following features: A: potency B: penetration C: IOP rise

``` A B C Dexamethasone 4+ 2+ 4+ Fluorometholone 3+ + 3+ Hydrocortisone + + 2+ Medrysone + - + Prednisolone 3+ 3+ 3+ ```

How long should you prescribe topical steroids for? Any exceptions?

No longer than 2 weeks unless you are able to monitor corneal epithelium and measure IOP

In regards to topical cyclosporin, describe the following: A: State it's effect on the immune system B: What does it inhibit or activate? (2)

Cyclosporin is an immunosuppressant that specifically inhibits T-lymphocyte activation and cytokine production

List 5 indications for the use of topical cyclosporin

- dry eye - vernal keratoconjunctivitis - eczema - atopic keratoconjunctivitis - allergic conjunctivitis

Name 3 systemic side effects that are lessened/absent as a consequence of the topical administration of cyclosporin

- IOP increase - delay in wound healing - cataract formation

List 2 contraindications for the use of topical cyclosporin

- known hypersensitivity | - active ocular infections

Name 2 Histamine H1 antagonists and briefly describe them

1. Levocabastine - used for seasonal allergic conjunctivitis; full adverse profile not known 2. Oloptadine - histamine receptor antagonist and mast cell stabiliser

In 2 steps, describe what you should do before removing a foreign particle from the eye

1. ensure no infection | 2. use local anaesthetic

Name drugs that can target the following: A: mediator release (2) B: cell migration (2) C: vascular response (1)

A: NSAIDs (to inhibit prostaglandin formation) and Oloptadine (to inhibit histamine receptor) B: suppress WBCs and mast cells with Steroids, Cyclosporin C: alpha-adrenoceptor agonists

List 3 factors to consider when thinking about the quality use of medicine

1. selecting management options wisely 2. choosing suitable medications 3. using medicines safely and effectively

List 2 factors to consider when thinking about considerations of the patient

1. presentation of signs and symptoms | 2. medical history: other medications, known drug allergies

List 6 factors to consider when thinking about the pharmacology of drug use

1. indications/contraindications 2. normal clinical response expected 3. suitable dosing regimes 4. potential side effects (topical and systemic) 5. interactions with other drugs 6. how such complications can be managed/avoided

Name 4 topical NSAIDs

- Diclofenac - Flurbiprofen - Indomethacin - Ketorolac