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PART ONE REVISION. > PHARMACOLOGY - Clinical (IOP, Steroids, Immunosuppressors etc) > Flashcards

PHARMACOLOGY - Clinical (IOP, Steroids, Immunosuppressors etc) Flashcards

1
Q

What are the most frequent side effects for prostaglandin analogues? (7)

A
  1. Increased iris pigmentation
  2. Iris cyst formation
  3. Increased peri-ocular skin pigmentation
  4. Eyelash hypertrichosis
  5. Iritis
  6. Peri-orbital fat atrophy
  7. CMO
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2
Q

What is ciclosporin’s main side effect?

A

nephrotoxicity, does not cause bone marrow suppression

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3
Q
  1. What are the main HIV medications?
  2. What are their main side effects?
A
  1. Ritonavir - nausea and diarrhoea
  2. Zidovudine - cytopaenia
  3. Zalcitabine - peripheral neuropathy
  4. Didanosine - pancreatitis

dida goalkeeper - brown - pancreatitis
zido/zico - is white - cytopaenia

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4
Q

Ribosomes are inhibited by which drug?

A

Chloramphenicol

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5
Q

What is the mechanism of action of fluoroquinolones?

A

Inhibit DNA replication by action on bacterial DNA gyrase

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6
Q

what is the mechanism of action of the imidazole antimicrobial?

A

inhibit cell membrane synthesis by inhibiting synthesis of sterols (important constiutent of fungal cell membranes)

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7
Q

What is the mechanism of action of aciclovir?

A

aciclovir inhibits DNA polymerase - an acyclic analogue of guanosine –> works better in infected cells.

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8
Q

Which drug can cause xanthopsia (yellow-blue discoloration), photopsia and pain on eye movements?

A

digoxin

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9
Q

What are the main side effects of carbonic anhydrase inhibitors (9) (-AMIDES)

A
  1. Paraesthesia
  2. Malaise complex (fatigue, weight loss)
  3. GI complex: diarrhoea, nausea, cramps due to potassium depletion
  4. Renal stone formation (calcium oxalate/phosphate)
  5. Steven-Johnson’s
  6. Bone marrow suppression/aplastic anaemia/agranulocytosis
  7. Thrombocytopaenia
  8. use in caution in patients with corneal endothelial dysfunction - affects endothelial pump mechanism

9, Teratogenic

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10
Q

What type of beta blocker is betoxalol? What is its protective effect?

A

Cardioselective (greater effect on B1 on myocardium vs B2 on respiratory/ocular system)

Protective effect on VF preservation due to effects on microperfusion of optic disc

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11
Q

What are the effects of betoxalol? (2)

A
  1. Less oculohypotensive effect than timolol
  2. Greater effect on visual field preservation due to effects on microperfusion of optic disc
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12
Q

Which immunosuppressant has an enhanced effect with allopurinol?

A

azathioprine –> patients need reduced dose on this

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13
Q

What is the mechanism of action of apraclonidine?

A

alpha-2-adrenergic agonist (partial) –> potent systemic anti-hypertensive –> causes mydriasis

Acts on the presynaptic nerve endings and are inhibitory –> prevent further release of neurotransmitter

Has very little alpha-1 activity

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14
Q

What are the effects of apraclonidine? (3)

A
  1. Mydriasis
  2. Eyelid retraction
  3. Conjunctival blanching
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15
Q

What are the optic side effects of vigabatrin? (3)

A
  1. Optic Nerve Pallor
  2. RNFL atrophy
  3. Concentric peripheral field loss (binasal field defect with macula sparing- affects males more than females)
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16
Q

What is the mechanism of action of dorzolamide or brinzolamide?

A

carbonic anhydrase inhibitor

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17
Q

Which class of IOP lowering agents is most chemically similar to sulphonamides?

A

Carbonic anhydrase inhibitors

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18
Q

What drugs can cause corneal verticillata / vortex keratopathy? (5 + 1)

A
  1. Chloroquine
  2. Hydroxychloroquine
  3. Amiodarone
  4. Indomethacin
  5. Phenothiazines
  6. Fabry’s disease
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19
Q

What is the mechanism of action of prostaglandins?

Bimatoprost additionally does what?

A

Increase uveoscleral outflow –> increased aqueous outflow.

Bimatoprost enhances trabecular outflow.

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20
Q

Which beta blocker will induce less bradycardia and postural hypotension than the others?

A

Carteolol - has intrinsic sympathetic activity.

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21
Q

What are the main complications of overtreatment with topical antivirals for HSK? (3)

A
  1. Follicular conjunctivitis
  2. Punctate keratitis with photophobia
  3. Sterile corneal ulceration
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22
Q

What is the main ocular side effects of brimonidine / apraclonidine?

A

After 1 year - allergic conjunctivitis, follicular conjunctivitis

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23
Q

What are the main side effects of topical prostaglandin analogues? (7)

A
  1. Increased iris pigmentation
  2. Iris cyst formation
  3. Increased peri-ocular skin pigmentation
  4. Peri-orbital fat atrophy
  5. Eyelash hypertrichosis
  6. Iritis
  7. CMO
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24
Q

Where are Beta-2 receptors found? (3)

A

Lungs, GI tract, vascular smooth muscle

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25
Q

Which antibiotics are known to be associated with IIH?

A
  1. Tetracyclines
  2. Fluoroquinolones
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26
Q

What drugs can induce optic neuropathy? (14)

A

Anti-Tb: Isoniazid, Ethambutol
Antibiotic: erythromycin, streptomycin, quinine, linezolid, dapsone (sulphonamide), chloramphenicol
Anti-retrovirals
Others: Amiodarone, Clioquinol, Infliximab, Pheniprazine, Suramin, Methotrexate

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27
Q

What are the ocular side effects of pilocarpine? (7)

A
  1. Miosis
  2. Induced myopia (myopic shift)
  3. Conjunctival vascular congestion
  4. Punctal stenosis
  5. Cataract formation
  6. Retinal detachment
  7. Headaches/brow ache
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28
Q

Which drugs should be avoided in myaesthenia gravis? (9)

A
  1. Aminoglycosides (gentamicin)
  2. Fluoroquinolones (ciprofloxacin, levofloxacin)
  3. Macrolides (erythromycin, azithromycin)
  4. Beta blockers
  5. Chlorpromazine
  6. Procainamide
  7. Penicillamine
  8. Respiratory supplements
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29
Q

Which topical steroid is least likely to induce intraocular pressure elevation?

A

Loteprednol etabonate

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30
Q

What are the ocular side effects of beta blockers?
(2)
What are the non ocular side effects of beta blockers?
(5)

A
  1. Reduced aqueous secretions by inhibition of beta-2 receptors on ciliary epithelium, punctate corneal erosions
  2. Local allergy, Bradycardia, Bronchospasm, Hypotension, Weakness (sleep disturbance, fatigue, headache, decreased libido)
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31
Q

What are the ocular side effects of topiramate? (8)

A
  1. Myopia
  2. Blurred vision
  3. Angle-closure glaucoma
  4. Scleritis
  5. Suprachoroidal effusion
  6. Periorbital Oedema
  7. Oculogyric crisis
  8. Blepharospasm
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32
Q

What are the side effects of acetazolamide? (7)
Biochemical (3)
Side effects (5)

A

hyponatraemia, hypokalaemia, metabolic acidosis

Renal calculi, paraesthesia of limbs, fatigue, Steven-Johnson’s syndrome, transient myopia

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33
Q

What is the mechanism of action of rituximab?
What is the mechanism of action of cyclosporin or tacrolimus?
What is the mechanism of action of infliximab and etanercept?

A

Rituximab - anti-CD20 protein (B cell surface)
Cyclosporin/tacro - calcineurin inhibitor –> anti-IL2
Infliximab/atanercept - anti-TNFdi

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34
Q

What effects happen with beta-1 blockers? (3)

What effects happen with beta-2 blockers? (3)

A

beta -1
1. Slow pulse rate
2. Weakens myocardial contraction
3. Reduced exercise tolerance

beta - 2
1. Bronchoconstriction
2. Peripheral arterial constriction
3. Reduced aqeous production from ciliary epithelium

35
Q

What are the main side effects of dorzolamide?

A

burning/blurring on instillation
bitter/metallic taste in mouth

36
Q

Which drugs can induce a cataract? (6)

A
  1. Chlorpromazine (anterior lens capsule)
  2. Corticosteroids
  3. Allopurinol
  4. Amiodarone
  5. Busulphan
  6. Gold (anterior capsule deposits)
37
Q

What effect does epinephrine have on intraocular pressure?

A

Reduces pressure

38
Q

Which glaucoma medications increase uveoscleral outflow?

A
  1. Alpha-adrenergic agonists
  2. Prostaglandins
39
Q

Which glaucoma medications decrease aqueous production? (3)

A
  1. Beta blockers (block adrenergic receptors ciliary body)
  2. Carbonic Anhydrase Inhibitors (inhibit enzyme in ciliary processes)
  3. Alpha-2 agonists (dual mechanism - increase uveoscleral outflow)
40
Q

What is the mechanism of action of botox? What is it used to treat?

A

Binds to pre-synaptic Ca2+ mediated receptors on the nerve terminal (motor nerve) inhibiting ACh release

Cleaves SNARE proteins needed for fusion of neurosecretory vesicles with the plasma membrane and so block ACh exocytosis.

Used to treat Blepharospasm

41
Q

Which drugs are generally avoided in uveitis related ocular hypertension? (2)

A
  1. Prostaglandins –> precipitate uveitic episode of CMO
  2. miotics –> increase vascular permeability and induce inflammation, worsen posterior synechiae
42
Q

How do topical anaesthetics inhibit wound healing?

A

disrupt tight junctions between cells and interfere with corneal epithelial metabolism

43
Q

What are the ocular manifestations of chloroquine use? (3)

A
  1. Corneal deposition
  2. Anterior subcapsular cataract
  3. Bull’s eye maculopathy
44
Q

Which drug can cause xanthopsia (yellow-blue discoloration), photopsia and pain on eye movements?

A

digoxin

45
Q

What are the main anti-inflammatory pathways of steroids (5)

A
  1. Inhibit enzymes for eicosanoid and phospholipase A2 synthesis
  2. Inhibit histamine release
  3. Inhibit numbers of PMLs, lymphocytes and macrophages
  4. Inhibit cytokine gene transcription in lymphocytes and Antigen-presenting complexes (APCs)
  5. Induce ACE and neuronal endopeptidases –> degradation of bradykinin, a vasoactive inflammatory mediator
  6. increase production of leukotrienes
46
Q

What is the mechanism of action of edrophonium? What is it used for?

A

Reversible acetylinesterase inhibitor used in the tensilon test to test for myaesthenia gravis

47
Q

What are the main side effects of ciclosporin? (5)

A

Nephrotoxicity
hepatotoxicity
gingival hyperplasia
hypertrichosis
hypertension

48
Q

What drugs can cause optic neuropathies?

A
49
Q

What drug is used to aid diagnosis in Adie’s pupil?

A

Low dose pilocarpine (0.125%) constricts the abnormal dilated eye - there is supersensitive iris sphincter caused by loss of post-ganglionic nerve fibres.

50
Q

Which pressure control drops have teratogenic side effects?

Which pressure control drops should be avoided when breastfeeding?

A
  1. Prostaglandins, carbonic anhydrase inhibitors and beta blockers - alpha-2 agonists are safe (apraclonidine, brimonidine)
  2. Alpha-2-agonists.
51
Q

What are the main side effects of glucocorticoids / steroids? (4)

A
  1. Cataract (typically if 15mg daily prednisolone)
  2. Increased risk of bacterial infection
  3. Reactivation of viral keratitis
  4. Steroid induced IOP rise via GAG and water accumulation in the trabecular meshwork reducing outflow (30% are steroid responsive)
52
Q

What are the risk factors to being a steroid responder? (8)

A
  1. POAG
  2. Pigmentary glaucoma
  3. FHx of glaucoma
  4. FHx of steroid response
  5. High myopes
  6. Diabetics (type 1)
  7. Traumatic glaucoma
  8. Fuch’s / keratoconus / keratoplasty
53
Q

What is the mechanism of action of ciclosporin A?

A

Caclineurin inhibitor and inhibits nuclear factor of activated T cells (NFAT) which leads to reduced production of IL-2

54
Q

What is the mechanism of action of azathioprine?

What is it metabolised by?

What is it metabolised to?

A

purine antagonist which blocks RNA and DNA synthesis.

Azathioprine is metabolised by thiopurine methyltransferase

It is metabolised to 6-mercaptopurine

55
Q

What is the mechanism of action of methotrexate?

A

Folic acid antagonist - inhibits dihydrofolate reductase to suppress DNA synthesis

56
Q

What are the side effects of azathioprine?

What are the side effects of methotrexate?

A

SAME: bone marrow suppression, hepatotoxicity (LFT monitoring)

DIFFERENCE:
Methotrexate: oral ulceration, myalgia, pneumonitis

57
Q

What is the mechanism of action of cyclophosphamide?

A

Alkylating agent that cross-links between DNA strands to prevent transcription of mRNA

58
Q

What is the mechanism of action of infliximab / etanercept

A

Anti-TNF alpha agents.

59
Q

How do topical anaesthetics impair wound healing?

A

disrupt tight junctions between cells and interefore with corneal epithelial metabolism

60
Q

What is the difference between unfractionated heparin and low-molecular weight heparin?

A

unfractionated heparin : potentiates anti-thrombin which inactivates thrombin and factor Xa –> inhibition of platelet aggregation

LMWH preferentially affects factor Xa.

61
Q

What are the side effects of heparin ? (5)

A
  1. Bleeding
  2. Thrombocytopaenia (paradoxical thrombosis)
  3. Osteoporosis
  4. Hypoaldosteronism
  5. Hyperkalaemia
62
Q

What drugs cause drug-induced myopia? (4)

A
  1. Acetazolamide
  2. Oral contraceptive
  3. Tetracycline
  4. Topiramate (can also cause suprachoroidal effusion, angle-closure, scleritis).
63
Q

What drugs cause optic neuropathy? (8)

A
  1. Anti - TB : ethambutol, isoniazid
  2. Chloramphenicol
  3. hydroxycholorquine
  4. Amiodarone
  5. Cisplatin
  6. Vincristine
  7. Streptomycin
64
Q

What drugs can cause raised intracranial pressure (drug-induced IIH)?

A
  1. Tetracycline
  2. Fluoroquinolones
  3. Retinoids (vitamin A)
  4. Progesterones
  5. Amiodarone
  6. Lithium
  7. Phenytoin
  8. Tamoxifen
65
Q

What is the difference bewteen the mechanism of action of 5-FU and MMC? Active stage?

A

5-FU : inhibits thymidylate synthetase in S phase/G2 cells –> inhibition of DNA synthesis. Active stage –> S Phase and G2

MMC: alkylating agent which cross links DNA. Active stage –> any stage

66
Q

What are the adverse/side effects of 5-FU? (5)

A
  1. Corneal epithelium toxicity
  2. Hypotonous maculopathy
  3. Suprachoroidal haemorrhage
  4. Conjunctival wound leak
  5. Ischaemic blebs.
67
Q

Acetazolamide is derived from…

A

sulphonamides so cannot be given to someone with sulphonamide allergy

68
Q

What is the mechanism of action of carbonic anhydrase?

A

Carbonic anhydrase catalyses the reversible reaction H + HC03 –> H2C03. It stimulates aqueous production in non-pigmented ciliary epithelium by increasing availability of bicarbonate ions.

69
Q

What is the mechanism of action of glucocorticoids?

How long does this process take?

A

Binds to cytoplasmic receptor proteins –> change in steroid rceptor complex to allow migration into nucleus –> binds to glucocorticoid response elements (GRE) on chromatin –> promoting transcription of specific mRNA and regulation of protein synthesis

Takes at least 30-60 minutes.

70
Q

Why is apraclonidine contraindicated in children less than two?

A

Can pass blood brain barrier and cause CNS depression in children.

71
Q

What type of IOP lowering drugs work on the…
1) trabecular meshwork
2) Uveoscleral pathway
3) Blockage of aqueous humor

A

See diagram.

72
Q

What is the mechanism of action of mycophenolate mofetil?

A

Inhibits activity of inosine (de novo purine) monophosphate dehydrogenase (anti-metabolite M)

73
Q

What are the side effects of cyclosporin? (6)

A
  1. Nephrotoxicity
  2. Hepatotoxicity
  3. Malignancy
  4. Hypertension
  5. Hyperkalaemia
  6. Thrombosis microangiopathy
74
Q

What are the drugs that cause crystalline retinopathy? (4)

A
  1. Tamoxifen (fine yellow deposits)
  2. Nitrofurantoin (circinate pattern)
  3. Canthaxanthin
  4. Methoxyflurane (anaesthetic - calcium oxalate crystals)
75
Q

Table which cause toxic optic neuropathy

A
76
Q

What are the side effects of anti-cholinesterases?

A
  1. cyst proliferation of iris pigment epithelium at pupillary margin in children
  2. Cataracts in adults
77
Q

Which anaesthetic can result in corneal epithelial toicity?

A

tetracaine

78
Q

Which drug is a combined H1 blocker and mast cell stabiliser? (2)

A
  1. Opatanol
  2. Nedocromil
79
Q

Which are the two main hyperosmotic drugs used in ophthalmology?

A

Mannitol and Glycerin

80
Q

What is the order of potency of topical steroids (5)

A
  1. prednisolone acetate 1% (most potent)
  2. dexamethasone 0.1%
  3. betamethasone 0.1%
  4. prednisolone sodium phosphate 0.5%
    f5. luorometholone 0.1% (least potent)
81
Q

Which ocular surface disease is linked to these tear film deficiencies:
1. Aqueous deficiency
2. Mucin deficiency
3. Lipid deficiency

A
  1. Aqueous - Sjogren’s syndrome
  2. Mucin - cicatriacal conjunctival disease and hyovitaminosis A
  3. Lipid - chronic meibomian gland inflammation
82
Q

What is the difference in washout periods between dorzolamide, timolol, brimonidine and latanoprost?

A

dorzolamide - 7 days
timolol - 4 weeks
brimonidine - 5 weeks
latanoprost - 8 weeks

83
Q

What is the mechanism of action of tolicizumab?

A

Monoclonal antibody against IL-6 receptor - used for treatment against RA, refactory GCA and rare uveitis.

84
Q

Which drug causes of binasal visual field defect?

A

Vigabatrin

PART ONE REVISION. (84 decks)

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