Allergic Rhinitis - Drug Classes

Front 1

ORAL 1ST GENERATION ANTIHISTAMINES - Diphenhydramine
(Benadryl)

Back 1

Sedative +++
Anticholinergic +++
Antiemetic ++/+++
Antihistaminic +/++

OTC; most sedating.

Comments

Front 2

ORAL 1ST GENERATION ANTIHISTAMINES - Tripelennamine

Back 2

Sedative ++
Anticholinergic +-
Antiemetic --
Antihistaminic +/++

Most GI upset.

Front 3

ORAL 1ST GENERATION ANTIHISTAMINES - Brompheniramine

Back 3

Sedative +
Anticholinergic ++
Antiemetic --
Antihistaminic +++

OTC; least sedating.

Front 4

ORAL 1ST GENERATION ANTIHISTAMINES - Chlorpheniramine

Back 4

Sedative +
Anticholinergic ++
Antiemetic --
Antihistaminic ++

OTC; least sedating.

Front 5

ORAL 1ST GENERATION ANTIHISTAMINES - Hydroxyzine
(Atarax)

Back 5

Sedative ++++
Anticholinergic ++
Antiemetic +++
Antihistaminic ++/+++

Best for urticaria.

Front 6

ORAL 1ST GENERATION ANTIHISTAMINES - Cyproheptadine
(Periactin)

Back 6

Sedative ++
Anticholinergic ++
Antiemetic --
Antihistaminic ++

Most weight gain.

Front 7

INTRANASAL 1ST GENERATION ANTIHISTMINES - Azelastine
(Astelin)

Back 7

Sedative +-
Anticholinergic +-
Antiemetic --
Antihistaminic ++/+++

Most weight gain.

Front 8

ORAL 2nd GENERATION ANTIHISTAMINES - Cetirizine
(Zyrtec)

Back 8

Sedative +
Anticholinergic +-
Antiemetic --
Antihistaminic ++/+++

OTC

Front 9

ORAL 2nd GENERATION ANTIHISTAMINES - Loratadine
(Claritin)

Back 9

Sedative +-
Anticholinergic +-
Antiemetic --
Antihistaminic ++/+++

OTC

Front 10

ORAL 2nd GENERATION ANTIHISTAMINES - Fexofenadine
(Allegra)

Back 10

Sedative +-
Anticholinergic +-
Antiemetic --
Antihistaminic ++/+++

Rx

Front 11

ORAL 2nd GENERATION ANTIHISTAMINES - Desloratadine
(Clarinex)

Back 11

Sedative +-
Anticholinergic +-
Antiemetic --
Antihistaminic ++/+++

Rx

Front 12

OCULAR 2nd GENERATION ANTIHISTAMINES - Olopatadine (Patanol)

Back 12

Sedative +-
Anticholinergic +-
Antiemetic --
Antihistaminic ++/+++

Rx

Front 13

OCULAR 2nd GENERATION ANTIHISTAMINES - Azelastine (Optivar)

Back 13

Sedative +-
Anticholinergic +-
Antiemetic --
Antihistaminic ++/+++

Rx

Front 14

Antihistamine - Points to Consider I

Back 14

• Competitive histamine antagonists (need to be at receptor to compete with histamine)

• For symptomatic relief only; adherence essential; scheduled not PRN; should start 1-2
weeks before season

• Ocular antihistamines have a quicker onset and may be more effective for
ocular symptoms but have little effect on systemic symptoms

•  compliance w/ sustained release drugs

• Do not take if pregnant; do not breast feed

• Children and elderly may have paradoxical excitation

• Side effects depend on route of administration and pharmacologic properties

Front 15

Antihistamine - Points to Consider II

Back 15

Anticholinergic: dry eyes, mouth, nose; blurred vision; urinary retention, HR, irritability
CNS: sedation, impaired motor/mental performance
GI: nausea, vomiting, anorexia

Note: The “third-generation” antihistamines (fexofenadine, desloratadine) are active metabolites of previously marketed antihistamines and have better cardiovascular safety

Note: Using a nonsedating antihistamine in the morning and a sedating antihistamine at night is not recommended (patients are impaired the next day though subjectively may not feel impaired)

Front 16

Antihistamine - Points to Consider III

Back 16

• Nasal antihistamines taste bitter

• Drug interactions depend on the pharmacologic activity (e.g., 1st generation antihistamines have additive anticholinergic effects with drugs that have anticholinergic activity (MAOIs, TCAs)

• Use with caution in patients with CV disease, prostatic hypertrophy, asthma,
untreated glaucoma, cognitive dysfunction

• Avoid alcohol or drugs w/ sedative activity

• Must be discontinued far enough in advance of allergen skin testing to be
cleared from body at time of skin testing (check the half-life of the drug to
estimate when to discontinue)

Front 17

Selected Decongestants - Ephedrine, naphazoline, phenylephrine, tetrahydrazoline

Back 17

Nasal sprays and solutions

Short-acting (4-6 hours); not recommended for AR

Front 18

Selected Decongestants - Xylometazoline

Back 18

Nasal sprays and solutions

Intermediate-acting (8-10 hours)

Front 19

Selected Decongestants - Oxymetazoline

Back 19

Nasal sprays and solutions

Long-acting (12-24 hours)

Front 20

Selected Decongestants - Propylhexedrine, desoxyephedrine

Back 20

Nasal inhalers

Not recommended for any indication (high abuse potential; rapidly evaporate)

Front 21

Selected Decongestants - Epinephrine, phenylephrine, oxymetazoline, naphazoline, tetrahydrozoline

Back 21

Ocular drops

Not recommended for AR; cosmetic only (limit use to 10 or fewer days)

Front 22

Selected Decongestants - Pseudoephedrine, phenylephrine

Back 22

Tablets, syrups

Pseudoephedrine is BTC; phenylephrine is OTC

Front 23

Decongestants - Points to Consider

Back 23

• Alpha-adrenergic agonists

• Side effects include  HR,  BP,  IOP, irregular HR, insomnia, tremor, nervousness, urinary retention, pupillary dilation, rhinitis medicamentosa (intranasal)

• Oral drugs preferred; do not use intranasal decongestants for > than 3 days

• Drug interactions: MAOIs

• SR preferred

• Use only w/ physician advice if HTN, DM, arrhythmias, glaucoma, prostatic hypertrophy, hyperthyroidism

• Do not take if pregnant, do not breast feed.

• Considered “doping” – check sanctioned drug lists before athletic events.

Front 24

Selected Corticosteroids - Prednisone, methylprednisolone (Medrol), cortisone, dexamethasone (Decadron)

Back 24

Tablets

Limited to 3-7 day courses

Front 25

Selected Corticosteroids - Beclomethasone (Beconase), busedonide (Rhinocort), flunisolide (Nasalide), fluticasone (Flonase), triamcinolone (Nasacort), mometasone (Nasonex), ciclesonide (Omnaris)

Back 25

Nasal sprays

Similar efficacy; differences pertain to bioavailability, lipophilicity, aqueous vs. alcohol-based solution

Front 26

Selected Corticosteroids -
Loteprednol (Alrex)

Back 26

Ocular

For more severe disease (increased risk for cataracts, incr. IOP, 2degree infections); onset in about 2 hrs w/ maximum benefit in about 2 weeks

Front 27

Corticosteroids - Points to Consider

Back 27

• Side effects associated with nasal administration include drying, stinging, burning, irritation, sneezing, epistaxis; decreased growth (children)

• Nasal: Takes 1-2 weeks of regular use to see benefit. Use on a schedule (not PRN).

• Do not spray nasal solutions in eyes.

• May aggravate viral or bacterial infections.

• Systemic: Follow directions exactly.

• Aqueous nasal solutions are better tolerated than alcohol-based solutions (propylene glycol) that can sting and burn

• Nasal solutions are minimally absorbed (advantageous in terms of long-term
safety but are ineffective treatment of systemic symptoms

Front 28

Other Drugs - Cromones

Back 28

Cromolyn (Nasalcrom; Opticrom)

Nasal spray; ocular drops

OTC; weak anti-inflammatory; requires regular use (QID) for at least 4 weeks; also used preventively prior to exposure

Front 29

Other drugs - Anticholinergics

Back 29

Ipratropium (Atrovent)

Nasal spray

Rx; expensive

Front 30

Other Drugs - Antileukotrienes

Back 30

Montelukast (Singulair)

Oral tablet

Rx; weak anti-inflammatory; FDA-approved for SAR > 2 yrs old

Front 31

Other Drugs - NSAID

Back 31

Ketorolac (Acular)

Ocular drops

Rx; limited use for temporary relief of itching

Front 32

Other Drugs - IgE blocker

Back 32

Omalizumab

Subcutaneous injections

Investigational for AR; $$$$$

Front 33

Leukotriene receptor antagonists - Points to Consider

Back 33

MOA : Anti-inflammatory

SE: GI (nausea, dyspepsia, pain); Incr. AST and ALT

DI: Phenobarbital, rifampin

PRODUCT SELECTION:

PATIENT COUNSELING: Take regularly.
6/09 – FDA requested labeling change for neuropsych events (behavior and mood changes); all LTRA’s

Front 34

Cromones - Points to Consider

Back 34

MOA : Anti-inflammatory

SE: Transient burning and stinging

DI:

PRODUCT SELECTION:

PATIENT COUNSELING:
Takes 1-2 weeks of regular use (QID) to see benefit. Use on a schedule (not PRN).

Front 35

Anticholinergics - Points to Consider

Back 35

MOA : Inhibit cholinergic-mediated mucus production

SE: Transient burning and stinging

DI:

PRODUCT SELECTION:
Caution w/ glaucoma, prostatic hypertrophy; bladder outlet obstruction

PATIENT COUNSELING:
Use on a schedule (not PRN).
Do not spray in eyes.