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Eyedocs pharmacology Flashcards

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1
Q

What are the actions of the parasympathetic pathway? (4)

A
  1. Ciliary muscle contaction –> accomodation
  2. Sphincter muscle constriction –> dilation
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2
Q

What are the actions of the sympathetic pathway?

A
  1. Ciliary muscle relaxation
  2. Sphincter pupillae action –> pupil miosis
  3. Upper lid retraction (Dalrymple sign)
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3
Q

What neurotransmitter is secreted in the sympathetic pathway?

A

Acetylcholine

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4
Q

What are the mechanism of pilocarpine? (6)

A

sympathetic agonist - acts on muscarinic / Ach receptor

  1. Iris sphincter contraction - pupil miosis
  2. Ciliary muscle contraction - accomodative spasm (can treat accomodative esotropia by reducing drive for convergence)
  3. Ciliary muscle contraction –> lens thickening and move forward –> iris moving forward –> narrow anterior chamber angle –> COAG
  4. Ciliary muscle contraction –> increases tension on scleral spur –> opening of trabecular meshwork (conventional route) –> reduce IOP
  5. Ciliary muscle contraction –> myopia
    6 –> increased vascular permeability (should be avoided in uveitis)
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5
Q

Which drugs can reverse atropine mydriasis?

Which drugs can reverse phenylephrine mydriasis?

A
  1. Pilocarpine
  2. Pilocarpine, thymoxamine (more effective)
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6
Q

Which HIV drugs are reverse transcriptase inhibitors?

Which HIV drugs are protease inhibitors?

A

Didanosine, Zidovudine, Zalcitabine

Ritonavir

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7
Q

What are the main side effects of carbonic anhydrase inhibitors (6)

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

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

A

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

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

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9
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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10
Q

Which immunosuppressant has an enhanced effect with allopurinol?

A

azathioprine –> patients need reduced dose on this

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11
Q

What is the mechanism of action of botox?

A

inhibition of release of ACh from presynaptic nerve terminals

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12
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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13
Q

What are the effects of apraclonidine? (3)

A
  1. Mydriasis
  2. Eyelid retraction
  3. Conjunctival blanching
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14
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)
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15
Q

What is the mechanism of action of dorzolamide or brinzolamide?

A
  1. Transient bitter taste
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16
Q

What compounds are most likely to penetrate the cornea to reach the anterior chamber (ie biphasic - both hydrophilic and hydrophobic) (3)

A
  1. Acetate (most)
  2. Alcohol
  3. Phosphate (least)
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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?

A

Increase uveoscleral outflow –> increased aqueous 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

What is the mechanism of action of quinolones?

A

ciprofloxacin

Blocks DNA synthesis by inhibiting DNA gyrase

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25
Which antibiotics inhibit bacterial cell wall synthesis? (3)
Penicillins, cephalosporins (ceftriaxone), vancomycin
26
Where are Beta-2 receptors found? (3)
Lungs, GI tract, vascular smooth muscle
27
What is the systemic effect of leukotrienes? (3)
1. Bronchoconstriction 2. Vasoconstriction 3. Increase vascular permeability --> involved in allergic reactions and inflammation
28
What drugs can induce optic neuropathy? (14)
Anti-Tb: Isoniazid, Ethambutol Antibiotic: erythromycin, streptomycin, quinine, linezolid, dapsone (sulphonamide), chloramphenicol Anti-retrovirals Others: Amiodarine, Clioquinol, Infliximab, Pheniprazine, Suramin
29
Systemically, what can chloramphenicol cause?
aplastic anaemia
30
What are the ocular side effects of pilocarpine? (7)
1. Miosis 2. Induced myopia (myopic shift) 3. Conjunctival vascular congstion 4. Punctal stenosis 5. Cataract formation 6. Retinal detachment 7. Headaches/brow ache
31
Which drugs should be avoided in myaesthenia gravis? (9)
1. Aminoglycosides (gentamicin) 2. Fluoroquinolones (ciprofloxacin, levofloxacin) 3. Macrolides (erythromycin, azithromycin) 4. Beta blockers 5. Chlorpromazine 6. Procainamide 7. Penicillamine 8. Respiratory supplements
32
Which topical steroid is least likely to induce intraocular pressure elevation?
Loteprednol etabonate
33
Which antibiotics inhibit protein synthesis? (5) Which antibiotics inhibit 30S subunit Which antibiotics inhibit 50S subunit
30S: tetracycline, aminoglycosides (messenger RNA) 50S: Macrolides, Lincosamides, Chloramphenicol
34
What antibiotics inhibit cell wall synthesis?
Beta lactam antibiotics - penicillin, cephalosporins
35
What antibiotics inhibit folic acid synthesis?
Sulphonamides Trimethoprim
36
What antibiotics inhibit DNA gyrase and transcription?
Fluoroquinolones
37
What are the ocular effects of tamoxifen? (3)
1. White retinal crystals 2. Retinal lesions 3. Macula oedema
38
What is the mechanism of action of aciclovir?
Inhibits DNA polymerase
39
What is Fick's Law?
rate of diffusion = diffusion coefficient x concentration gradient / membrane thickness
40
What are the ocular side effects of beta blockers? (2) What are the non ocular side effects of beta blockers? (5)
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)
41
Which antibiotic is the most retino-toxic when given intravitreally?
Gentamicin (gram negative cover)
42
What are the ocular side effects of topiramate? (5)
1. Myopia 2. Blurred vision 3. Angle-closure glaucoma 4. Scleritis 5. Suprachoroidal effusion
43
What is the mechanism of action of azathioprine / methotrexate?
Inhibit purine ring biosynthesis - cytotoxic anti-metabolite
44
What are aminoglycosides not effective against?
Streptococcus and strict anaerobes
45
What is the general actions of adrenergic agonists (4)
1. Increase aqueous outflow 2. Ciliary muscle relaxation 3. Contraction of Muller's muscle --> ptosis relief 4. Conjunctival vessel constriction
46
Which drugs are alpha-1 adrenergic agonists? Which drugs are alpha-2 adrenergic agonists?
Alpha-1 : phenylephrine Alpha-2: aproclonidine
47
What are the side effects of acetazolamide? (7) Biochemical (3) Side effects (4)
hyponatraemia, hypokalaemia, metabolic acidosis Renal calculi, paraesthesia of limbs, fatigue, Steven-Johnson's syndrome
48
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?
Rituximab - anti-CD20 protein (B cell surface) Cyclosporin/tacro - anti-IL2 Infliximab/atanercept - anti-TNF
49
Which drug can cause xanthopsia (yellow-blue discoloration), photopsia and pain on eye movements?
digoxin
50
Which antibiotics are known to be associated with IIH?
1. Tetracyclines 2. Fluoroquinolones
51
What factors affect diffusion coefficient? (3)
1. Lipid solubility 2. Ionization 3. Molecular size
52
What happens to drug absorption with increased blink rate?
Reduces by increasing clearance
53
What effect does acidity/alkaninity have on a drug?
1. More unionised and so more lipid soluble to increase corneal absorption 2. Causes irritation/lacrimation --> drug clearance
54
What is the mechanism of action of cocaine?
inhibits reuptake of monoamines at the synaptic space
55
What effect do steroids have on trabecular meshwork?
increase production of myocilin
56
What does Phase 1 drug metabolism involve?
oxidation reactions (carried out by cytochrome P450)
57
What do Phase 2 drug metabolism involve?
conjugation reactions (addition of glucuronate, glutamine and acetate groups) which makes molecules more water soluble for excretion
58
What type of drug is etanercept?
anti-TNF alpha drug
59
What is the mechanism of action of methotrexate?
Folate antagonist
60
What is the mechanism of action of azathioprine?
Purine analogue
61
What is the mechanism of action of ciclosporin?
IL-2 inhibitor (T-cell inhibitor)
62
what is the mechanism of action of imidazole antifungals?
inhibitr cell membrane synthesis - they inhibit the synthesis of sterols which are an important constituent in fungal cell membranes (anti-mycotics)
63
Which drug relaxes the ciliary body?
atropine
64
What are the main risk factors for steroid-induced raised IOP? (6)
1. POAG 2. Pigmentary glaucoma 3. FH of glaucoma 4. High myopes 5. Diabetics 6. FH of steroid responders
65
Which glaucoma drug is safest in pregnancy?
alpha-2 agonists (brimonidine, apraclonidine)
66
Which drugs can cause a drug-induce myaesthenia? (6)
1. NJ blockers - suxamethonium 2. Resp suppressors - morphine 3. Aminoglycosides 4. Chloropromazine 5. Procainamide 6. Penicillamine
67
Accomodation occurs with parasympathetic or sympathetic control?
parasympathetic control
68
Which drugs are parasympathetic antagonists?
1. Cyclopentolate 2. Tropicamide 3. Atropine 4. Phenothiazine
69
Which drugs are generally avoided in uveitis related ocular hypertension? (2)
1. Prostaglandins --> precipitate uveitic episode of CMO 2. miotics --> increase vascular permeability and induce inflammation, worsen posterior synechiae
70
What are the ocular side effects of topiramate (6)
1. AACG 2. Oculogyric crises 3. Periorbital oedema 4. Scleritis 5. Acute myopia 6. Blepharospasm
71
What is the mechanism of action of botox/
Binds to pre-synaptic receptors on the nerve terminal (motor nerve) inhibiting ACh release
72
Which glaucoma medications decrease aqueous production?
1. Beta blockers 2. Carbonic Anhydrase Inhibitors 3. Alpha-2 agonists (dual mechanism)
73
Which glaucoma medications increase uveoscleral outflow?
1. Alpha-adrenergic agonists 2. Prostaglandins
74
What ocular side effect occurs with prolonged use of ciprofloxacin?
Corneal crystalline precipitates
75
What effect does epinephrine have on intraocular pressure?
Reduces pressure
76
Which drugs can induce a cataract? (6)
1. Chlorpromazine (anterior lens capsule) 2. Corticosteroids 3. Allopurinol 4. Amiodarone 5. Busulphan 6. Gold (anterior capsule deposits)
77
What type of bacteria do tetracyclines target? (3)
Gram +ve Gram -ve Chlamydia
78
What is the mechanism of action of phenylephrine?
Non selective alpha agonist
79
What are the main side effects of dorzolamide?
burning/blurring on instillation bitter/metallic taste in mouth
80
What effects happen with beta-1 blockers? (3)
1. Slow pulse rate 2. Weakens myocardial contraction 3. Reduced exercise tolerance
81
What effects happen with beta-2 blockers?
1. Bronchoconstriction 2. Peripheral arterial constriction 3. Reduced aqeous production from ciliary epithelium
82
What is the difference between lipid soluble and water soluble drugs? (3)
1. Lipid soluble enter BBB so have more CNS effects 2. Water soluble are easier to clear 3. Hepatic drug metabolism converts lipid soluble drug into a water soluble drug
83
What is the mechanism of action of tropicamide?
It is a muscarinic antagonist - blocks parasympathetic pathway.
84
what are the side effects of tropicamide?
1. precipitates angle closure 2. exacerbates ataxic dysarthia 3. cerebellar signs 4. increases risk of seizure
85
Which drug can be used for infections caused by aspergillus and candida?
Topical amphotericin
86
In what instances are alpha-2-agonists contraindicated? (2)
1. Potentiates hypertensive crisis with monoamine oxidase inhibitors 2. WIth TCAs, its IOP effect is removed.
87
What are the most important factors on rate and extent of ocular absorption (5)
PRE-corneal factors 1. Tear volume (7-30ul) 2. Tear turnover time (-.5-2.2ul/min) 3. Blink rate (15-min) all these factors limit drug time in conjunctival sac to 3-5 minutes on average 4. Corneal thickness 5. Conjunctival:corneal surface area (17:1)
88
What is the greatest barrier in the cornea for ocular drug penetration? What route does it go by?
Corneal epithelium (lipophilic layer) Lipophilic drugs --> intracellular route Hydrophilic drugs --> paracellular route
89
Which drugs accumulate in the cornea? (2)
1. NSAIDs 2. Pilocarpine
90
What is the effect of muscarinic agonists, example? (3)
Direct - pilocarpine Indirect - carbachol - inhibits cholinesterase 1. Miosis 2. Accomodation 3. Decreased intraocular pressure
91
What are the main muscarinic agonists and antagonists?
Musacrinic agonist - pilocarpine, carbahol Muscarinic antagonist - atropine
92
What is the order of potency for muscarinic antagonists?
atropine > cyclopentolate > homatropine > tropicamide

Eyedocs revision (7 decks)

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