Test 2: Management Of Anti-Histaminic And Anti-Inflammatory Drugs

Front 1

How many mast cells are in each eye?

Back 1

50 million

Front 2

How many receptors are on the surface of mast cells and what binds to them?

Back 2

500,000 receptors for IgE antibodies

Front 3

Describe how Type I (humoral) Hypersensitiviy Reaction work.

Back 3

1. Allergan activates B-lymphocyte; IgE binds to mast cells & basophils (SENSITIZATION)

2. Cell membrane now more permeable to Ca+ ions; Ca+ influx triggers phospholipase A2 in mast cells

3. Mast cell degranulates

Front 4

What gets release when mast cells are degranulated?

Back 4

Histamine
Tryptase
Prostaglandin D2
Leukotrienes
Eosinophilic chemotactic factors
Platelet-activating factors
Proteases
Cytokines IL-4, -5, -6, -8, -13, TNF

Front 5

Result of allergic mediators include...

Back 5

1. itching
2. tearing
3. mucous production
4. conjunctival vasodilation
5. increased vascular permeability
6. papillary hypertrophy

Front 6

When do Type 1 (humoral) reaction occur after exposure to antigen?

Back 6

minutes to hours

immediate phase: 5-30 minutes
late phase: 4-6 hours after exposure; lasts 2 days

Front 7

When do Type IV (delayed, cell-mediated) hypersensitivity reactions occur after exposure to antigen?

Back 7

12-72 hours after allergen exposure, mediated by activated T-cells

Front 8

What are the recommended non-pharmacologic measures that should be taken?

Back 8

1. Keep hands away from eyes
2. Use bed/mattress covers and frequent cleaning of bed and carpets for mites and dander
3. Run AC if mold is a problem
4. Keep windows closed in peak season
5. Shampoo hair before bed
6. Undress in room other than bedroom
7. High Performance AC filters?
8. Freeze toys??
9. Artificial tears
10. Saline Rinse
11. Cool compresses
12. Avoid allergen

Front 9

What are the step approach in the pharmacologic management?

Back 9

1. Decongestants
2. Topical antihistamines
3. Oral antihistamines
4. Mast cell stabilizers
5. NSAIDs
6. Corticosteroids

Front 10

Decongestants are also known as...

Back 10

vasoconstrictors

Front 11

What are the available decongestants?

Back 11

Phenylephrine
Naphazoline
Oxymetazoline
Tetrahydrozaline

Front 12

Side effects of decongestants

Back 12

stinging
pupillary dilation (primarily phenylephrine)
epithelial erosion
rebound congestion
follicular conjunctivitis
possible bradycardia/hypotension

Front 13

Contraindications for decongestants

Back 13

narrow angles
cardiovascular disease

Front 14

Uses for topical antihistamines

Back 14

1. Decrease itching, decrease capillary dilation & permeability, mucus production

2. May or may not decrease other symptoms (burning, pain)

3. Can be very effective in acute reaction (where mast cell stabilizer is not)

4. When histamine-mediated anaphylaxis occurs, antihistamines are too slow-acting (need epi)

Front 15

Name the first generation topical antihistamines.

Back 15

Pheneramine maleate
-Naphcon-A
-Visine-A
-Opcon-A
Antazoline phosphate
-Vasocon-A

Both available only in combo with naphazoline; are OTC

Dosed QID

Front 16

Name the second generation topical antihistamines.

Back 16

Emedastine (Emadine 0.05% sol)
-significant decrease in itching & redness in 10 minutes
-duration 4-6 hours
-dosed qid

selective H1-blockers may also inhibit release of histamine and other mediators from mast cells

Front 17

Name the mast cell-stabilizing antihistamines and their daily dosing.

Back 17

1. Olopatadine
-Patanol 0.1% - BID
-Pataday 0.2% - QD
2. Ketotifen - all BID
-Zaditor 0.025%
-Alaway - generic
-Refresh Eye Itch Relief
3. Azelastine (Optivar 0.05% sol) - BID
4. Epinastine HCl (Elestat) - BID

Front 18

Which mast cell-stabilizing antihistamine can be found over the counter?

Back 18

Ketotifen
- Zaditor 0.025%
- Alaway - generic
- Refresh Eye Itch Relief

Front 19

Side effects of topical antihistamines

Back 19

Burning
Stinging

Front 20

Contraindications of topical antihistamines

Back 20

possible to produce some mydriasis, so contraindicated in narrow angle patients

Front 21

When should oral antihistamines be used?

Back 21

Appropriate when other signs and symptoms are present

May actually exacerbate ocular symptoms (especially more sedating ones)

Front 22

What is different between the first generation and second generation classes of oral antihistamines?

Back 22

First Generation
- "sedating"
- "CNS depression/stimulation"
- Anticholinergic effects

Second Generation
- "less" or "non-sedating"
- less dry mouth, blurred vision
- longer elimination time (less frequent dosing)

Front 23

Clinical uses of antihistamines.

Back 23

- nasal and conjunctival itching, sneezing, coughing
- rhinitis
- eyelid edema

- Topical: more direct and rapid effect on ocular surface

Front 24

Name the first generation oral antihistamines.

Back 24

Mildly sedating - cold meds
- chlorpheniramine

Moderately sedating - some cold meds, some motion sickness meds
- clemastine

Strongly sedating
- diphenhydramine
- promethazine

Front 25

Name the second generation oral antihistamines.

Back 25

Fexofenadine (Allegra)
Cetirizine HCl (Zyrtec) ** most potent
Desloratadine (Clarinex)
Loratadine (Claritin)

Front 26

What is the dosing for Fexofenadine (Allegra)?

Back 26

Children and Adults aged 12+
- 60mg BID or 180mg QD

Children 2-11
- 30mg BID

Children 6 months - under 2 years
- 15mg BID

Available forms:
- 30, 60, and 180 mg tabs
- 30mg/5ml oral suspension

**Decreased concentration when taken with grapefruit, orange, or apple juice

Front 27

What is the dosing for Cetirizine HCl (Zyrtec)?

Back 27

Adults and Children 12+
- 5 mg/day or 10 mg/day

Children 6-11 years
- 5 mg/day or 10 mg/day

Children 6 mos - under 2 years
- 2.5 mg/day
-MAXIMUM 5 mg/day (single or divided)

Available forms:
- 5 mg, 10 mg tablets
- 5 mg, 10 mg chewable tablets
- 1 mg/ml oral syrup

**Zyrtec-D (age 12 and older ONLY; BID)

Front 28

What is the dosing for Desloratadine (Clarinex)?

Back 28

Adults and Children 12+ years
- 5 mg QD

Children 6 - 11 years
- 2.5 mg QD

Children 12 mos - 5 years
- 1.25 mg QD

Infants 6 - 11 months
- 1 mg QD

Available forms:
- 5 mg tabs
- 5 mg, 2.5 mg redi-tabs
- Syrup 2.5 mg/5 ml
- Available with pseudoephedrine

Front 29

What is the dosing for Loratadine (Claratin)

Back 29

OTC
Once Daily
Approved for children 2 years and up

Available forms:
- tablets
- syrup
- Adult and Children's Redi-Tabs
- Available with pseudoephedrine (Claratin-D)

Front 30

Side effects of oral antihistamines

Back 30

1. sedation (worse with alcohol)
2. palpitations
3. drying of secretions
4. GI disturbance
5. dry eyes
6. mydriasis
7. decreased accommodation

Front 31

Contraindications of oral antihistamines

Back 31

1. 1st and 3rd trimester pregnancy
2. nursing mother
3. strong anticholinergic H1 blockers:
- peptic ulcer disease
- prostate hypertrophy
- bladder obstruction
- narrow angles

Front 32

Name the drugs for Mast Cell Stabilizers and their dosing.

Back 32

1. Cromolyn sodium (Crolom, Opticrom) - QID

2. Iodoxamide (Alomide) - QID
*** 2500x more potent

3. Pemirolast (Alamast) - BID, may load QID

4. Nedocromil (Alocril) - BID
- multicellular action
- quick decrease in symptoms
- yellow color

Front 33

Name the NSAID drugs.

Back 33

1. Ketorotac tromethamine (Acular)
- Acular
- Acular LS
- Acular PF

2. Diclofenac sodium (Voltaren)

3. Bromfenac (Xibrom) - BID

4. Nepafenac (Nevanac)

Front 34

Name the corticosteroid drugs

Back 34

Loteprednol etabonate 0.2% (Alrex) is the only topical corticosteroid with FDA approval for ocular allergy