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Ocular Pharmacology > Antihistaminics and Decongestants > Flashcards

Antihistaminics and Decongestants Flashcards

1
Q

What is the number 1 site of ocular allergy?

A

conjunctiva (can also be lids and lashes)

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2
Q

What is innate immunity?

A

(<12 hours) non-specific acute response (first-line) that lacks immunological memory

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3
Q

what are the key cells associated with innate immunity?

A

humoral and cell mediated: killer T cells and macrophages

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4
Q

What is adaptive immunity?

A

(1-2 weeks) occurs after prior exposure to an antigen and has specificity and memory

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5
Q

what are the key cells associated with the adaptive immune response?

A

humoral and cell mediated: memory B and T cells

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6
Q

what is an antigen?

A

a foreign/endogenous substance having the capacity to evoke an immunological response

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7
Q

what is hypersensitivity or an allergic reaction?

A

exaggerated immune responses to an innate or foreign innocuous antigen = allergen (environmental, biological, chemical based)

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8
Q

what are the 2 types of hypersensitivity responses that are most commonly associated with ocular reactions?

A

types 1 and 4

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9
Q

what is a type 1 hypersensitivity reaction?

A

IgE based (only one) - activation of mast cells or basophils (allergy)

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10
Q

what are 3 examples of a type 1 response?

A

atopy, asthma, anaphylaxis

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11
Q

what is a type 2 hypersensitivity reaction?

A

(antibody mediated or cytotoxic) non-systemic/local IgM or IgG based attack = local inflammation

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12
Q

what are 3 examples of a type 2 response?

A

graves disease, myasthenia gravis or autoimmune diseases

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13
Q

what is a type 3 hypersensitivity reaction?

A

(immune complex) circulating or systemic IgM or IgG based immune complexes (originate in circulation but can land locally)

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14
Q

what are 4 examples of a type 3 response?

A

arthritis, nephritis, vasculitis, lupus

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15
Q

what is a type 4 hypersensitivity reaction?

A

(delayed type CD4 and/or cell-mediated CD8) T-cell based reactions that lead to macrophage activation and/or cell lysis = inflammation

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16
Q

what are some examples of a type 4 response?

A

IDDM, MS, RA, contact dermatitis, conjunctivitis medicamentosa

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17
Q

how quickly does a type 1 hypersensitivity reaction occur?

A

5-30 min

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18
Q

what are the 5 steps of a type 1 hypersensitivity reaction?

A
  1. B-cell + antigen
  2. B-cell + IgE synthesis
  3. Mast cell/basophil + surface IgE
  4. Mast cell/basophil + Ag = Ca++ entry
  5. Degranulation = histamine release
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19
Q

what cell is local - mast cells or basophils?

A

mast cells are local (at tissue) and basophils are in blood circulating

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20
Q

what 2 things does Ca++ trigger when it enters a mast cell/basophil?

A

triggers phospholipase A2 and mast cell degranulation = histamine (pre-formed)

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21
Q

what is phospholipase A2 involved in?

A

inflammatory cascade

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22
Q

how long does it take for a type 4 response?

A

2-3 days for development (much faster than adaptive immune response)

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23
Q

what triggers a type 4 response?

A

re-exposure (memory) response = TB testing, MS, chronic transplant rejection

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24
Q

How is type 4 different than types 1-3?

A

T-cell based (unlike 1-3) and antibody independent

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25
Q

Does a type 4 response use histamine?

A

no - cytokines are released upon antigen re-exposure and activate macrophages = phagocytic and lytic enzymes

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26
Q

when might you use an antihistamine with a steroid?

A

if symptoms include itch and other significant ocular allergy signs (redness, chemosis, eyelid edema) –> involves inflammation (PGs) as well as mast cells

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27
Q

Is itch always a sign of ocular allergy?

A

no - mast cells can degranulate by scratching and histamine is released

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28
Q

what are 5 allergy therapies?

A

decongestants, antihistamines, mast cell stabilizers, NSAIDS, steroids

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29
Q

would you advise patients with ocular allergies to use a warm or cold compress?

A

cold compress - constriction of vessels = less redness and leakage (swelling)

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30
Q

what are 4 adrenergic agonists used for decongestants?

A

phenylephrine, naphazoline, oxymeazoline, tetrahydrozoline

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31
Q

what are the actions of decongestants?

A

vasoconstriction - reduces hyperemia and edema (palliative therapy)

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32
Q

How can decongestants differentially diagnose episcleritis?

A

if the decongestant blanches the conjunctiva (makes it white) - the redness was superficial and was episcleritis vs. scleritis

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33
Q

why are naphazoline, oxymetazoline, tetrahydrozoline less likely to induce mydriasis?

A

lack a saturated benzene ring = predominantly alpha-adrenergic stimulation

34
Q

when would you use a decongestant?

A

allergy induced hyperemia and injection

35
Q

why is phenylephrine not commonly used as a decongestant?

A

due to its predilection to produce rebound congestion and with chronic use = conjunctival medicamentosa (need to keep using drop to keep eyes white)

36
Q

what are the dosing conditions for ocular decongestants?

A

BID to QID

37
Q

what are some general reactions to decongestants?

A

blur, epithelial erosions, rebound congestion, upper lid retraction, mydriasis, elevated/reduced IOP

38
Q

which decongestants could cause mydriasis?

A

phenylephrine and naphazoline

39
Q

which decongestant elevates IOP?

A

naphazoline

40
Q

which decongestant reduces IOP?

A

tetrahydrozoline

41
Q

what are the contraindications for decongestants?

A

patients with angle closure glaucoma or narrow angles

42
Q

which histamine receptor is involved in immediate hypersensitivity?

A

H1

43
Q

what does the histamine receptor H2 do?

A

promotes gastric acid production and immune cell activation

44
Q

what does the histamine receptor H3 do?

A

pre-synaptic feedback inhibition (similar to alpha2)

45
Q

what does the histamine receptor H4 do?

A

immuno-modulation, inflammation, and nociception roles

46
Q

what type of histamine receptor does the eye have a lot of?

A

H2

47
Q

what are some systemic effects of histamine?

A

promotes vascular permeability, induces vasodilation (hypotension/tachycardia), causes smooth muscle contraction (bronchoconstriction), stimulates sensory nerves (itching, sneezing)

48
Q

Are antihistaminics antagonists or inverse agonists?

A

inverse agonists

49
Q

when would you use an oral decongestant?

A

deeper ocular involvement = moderate to severe edema and chemosis

50
Q

what is the typical dosing for antihistaminic’s?

A

QD, BID, QID

51
Q

what are 4 broader ophthalmic uses for antihistaminic’s?

A

allergic conjunctivitis, myokymia, allergic rhinitis, intra-operative anti-miotic use

52
Q

why can first generation antihistaminic’s cause drowsiness?

A

they are lipid soluble and can cross the blood brain barrier

53
Q

what are 2 types of antihistaminic’s/decongestants?

A

Vasocon-A and Naphcon-A

54
Q

what are the components of Vasocon-A?

A

antihistaminic = antazoline phosphate
decongestant = naphazoline HCl
dosing = QID
ages 6 and up

55
Q

what are the components of Naphcon-A?

A

Antihistaminic = pheniramine maleate
decongestant = naphazoline HCl
dosing = QID
ages 6 and up

56
Q

what are some general adverse effects of antihistaminic’s?

A

mydriasis, anisocoria, medicmentosa, rebound hyperemia, lacrimation/dry eye, irritation, pain, photophobia, IOP fluctuation, vasoconstriction, suppress accommodation, headache

57
Q

what are some contraindications for antihistaminic’s?

A

hypersensitivity, MAOI, alcohol, CVD, diabetes, narrow chamber angles

58
Q

what are mast cell stabilizers? and when are they used?

A

oral agents that block Ca++ influx to stop degranulation = HALTS type 1 hypersensitivity reaction

59
Q

what are 2 ocular conditions that need mast cell stabilizers?

A

vernal keratoconjunctivitis and giant papillary conjunctivitis

60
Q

what can patients use to prepare for an upcoming allergy season to reduce their chance of allergy reaction?

A

can take a mast cell stabilizer as a prophylactic therapy

61
Q

what are 4 topical mast cell stabilizers for chronic use?

A

permirolast, nedocromil, lodoxamide, cromolyn

62
Q

which mast cell stabilizer is only BID and the most rapid?

A

nedocromil (alocril)

63
Q

what is the mast cell stabilizer that can be used on a 2 year old?

A

lodoxamide (alomide)

64
Q

what is the only over the counter acute antihistaminic/MCS combo drug?

A

alaway (ketoifen) = BID

65
Q

what are some acute antihistaminic/MCS combos you need an Rx for?

A

Bepreve (bepotastine), elestat (epinastine), lastacaft (alcaftadine), optivar (azelastine), pataday (olopatadine)

66
Q

what are the 2 antihistaminic/MCS that are QD instead of BID?

A

lastacaft and pataday

67
Q

what are some adverse effects of antihistaminic/MCS combos?

A

sting/burn, FB sensation, dry eye, itch, headache, flu-like syndrome, rhinitis, taste changes

68
Q

what is a contraindication for antihistaminic/MCS?

A

known hypersensitivity

69
Q

what is an example of an NSAID used for allergy therapy?

A

acular (ketorolac tromethamine) = seasonal allergic conjunctivitis (SAC)

70
Q

what is an example of a steroid used for allergy therapy?

A

Lotemax (loteprednol etabonate) = safe for long term therapy of SAC and VKC

71
Q

what are 4 anti-H2 antihistaminic’s?

A

Tagamet (cimetidine), pepcid (famotidine), axid (nizatidine), zantac (ranitidine)

72
Q

what are 2 mildly sedating first generation antihistaminic’s?

A

brompheniramine and chlorpheniramine

73
Q

what is a moderate sedating first generation antihistaminic?

A

clemastine

74
Q

what are 2 strongly sedating first generation antihistaminic’s?

A

diphenhydramine (benadryl) and promethazine

75
Q

what are 4 contraindications for first generation antihistaminic’s?

A

peptic ulcer, prostatic hypertrophy, bladder obstruction, angle closure glaucoma = anticholinergic effects (stopping rest and digest)

76
Q

what are 4 examples of second generation antihistaminic’s?

A

allergra (fexofenadine), claritin (loratadine), clarinex (desloratadine), zyrtec (cetirizine)

77
Q

which second generation antihistaminic has the least CNS effects?

A

allergra (fexofenadine)

78
Q

which second generation antihistaminic is the most potent (and most sedating)?

A

zyrtec (cetirizine)

79
Q

what is different about second generation antihistaminic’s from first generation?

A

have a longer elimination profile (allow for some QD dosing) and are less sedating - may have potential to decrease histamine release

80
Q

Are mast cell stabilizers more or less effective when combined with antihistaminic’s?

A

the combo drops are more effective

81
Q

which antihistaminic/MCS combo has anti-H2 properties?

A

Elestat (epinastidine)

82
Q

which antihistaminic/MCS combo can cause folliculosis, upper respiratory tract infection?

A

Elestat (epinastidine) - suppressed immune system may promote infections

Ocular Pharmacology (10 decks)

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