author: kimberly mulcahy, pharmd, bcps editor: …samples.jbpub.com/9781284110401/chapter_1.pdf ·...

AntihistaminesAuthor: Kimberly Mulcahy, PharmD, BCPS

Editor: Claudia Lee, RPh, MD

Learning Objectives■■ Identify current pharmacologic agents that are appropriate for each condition/diagnosis.■■ Recommend optimal pharmacologic interventions based on patient-specific characteristics.■■ Provide appropriate patient-specific counseling points and optimal overall medication management.

Key Terms: antihistamines, histamine, first-generation antihistamines (ethanolamine derivatives, ethylenediamine derivatives, phenothiazine derivatives, piperazine derivatives, propylamine derivatives, miscellaneous), second- generation antihistamines, allergy, anaphylaxis, antibody, anticholinergic, antigen, anxiolytic, central nervous system, congestion, conjunctivitis, dermatoses, drowsiness, gastric acid, hay fever, insomnia, motion sickness, nausea, rhini-tis, rhinorrhea, sedating, somnolence, urticaria, vomiting

Overview of AntihistaminesAntihistamines are commonly utilized, predominantly over-the-counter (OTC) medications for treatment of aller-gic conditions. Histamine is found throughout the body, including within the vesicles of mast cells or basophils, and is abundant in the mast cells in areas particularly susceptible to tissue injury, such as the nose, mouth, feet, internal body surfaces, and blood vessels. While intracellular histamine is inert, it is released and becomes activated when a noxious antigen is detected by sensitized antibodies. Histamine that is not found within mast cells functions as a neurotransmitter in the brain and is involved with neuroendocrine control, cardiovascular functions, thermal and weight regulation, and sleep and arousal balance. The enterochromaffin-like (ECL) cells of the stomach release hista-mine, which is one of the main factors that stimulates the stomach mucosal parietal cells to produce gastric acid for digestion.

Four different histamine receptors have been identified. Each of these receptors is distributed in a different area of the body and elicits a different response to histamine agonism or antagonism. H1 receptors are found on smooth muscle cells, the endothelium, and the brain; H2 receptors are distributed in the gastric mucosa, cardiac muscle, mast cells, and the brain; H3 receptors are located in the brain; and H4 receptors are predominantly found on eosinophils, neutrophils, and T cells. When histamine stimulates the H1 receptor, the reaction produces the allergic response commonly observed with insect stings and contact with other allergens, including symptoms such as bronchoconstriction, pain, and itching. H2 receptors, when exposed to histamine, cause the contraction of gastrointestinal smooth muscles and the release of gastric acid. H3 receptors in the brain are responsible for the release of many neurotransmitters and may also have an effect on satiety. H4 receptors on blood cells produce inflammation and other allergic responses

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Chapter 1

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when histamine is present. Currently available antihistamine agents affect the H1 and H2 receptors; no antihistamines are approved for use that affect the H3 and H4 receptors, but there is a potential for these receptors to be drug targets in treatments for sleeping disorders, attention-deficit/hyperactivity disorder (ADHD), and obesity, to name a few conditions.

H1 antihistamines are typically the first drugs used to treat the symptoms of an allergic reaction or allergic rhi-nitis, but when used intranasally they are considered secondary agents, to be used after glucocorticoids. These anti-histamines are also the drugs of choice for managing urticaria (itching) associated with an allergic response; they are effective in this indication even if given prior to an anticipated exposure. If allergic rhinitis (hay fever) presents with nasal congestion, antihistamines are not as efficacious as nasal decongestants, such as pseudoephedrine, or combi-nation antihistamine‒decongestants (frequently named with a “D” added after the drug name, such as loratidine-D). H1 antihistamines are not effective for bronchial asthma and antihistamines are used only as adjuvant treatment for patients experiencing systemic anaphylaxis (epinephrine is the mainstay of treatment).

Many antihistamine formulations are also available for topical administration in the eye and nose. When oph-thalmic preparations are used, contact lenses should be removed prior to application, and can be reinserted 10‒15 minutes after administration, unless otherwise specified. Do not reinsert the lenses if the eyes are red, and separate administration of other ophthalmic topical agents by 5 minutes. With nasal preparations, the nasal spray must be primed prior to first use until a fine mist appears. Repriming is necessary when the product is unused for a number of days specified by the certain manufacturer.

1.1 First-Generation AntihistaminesFirst-generation antihistamines are H1 antagonists and are known for their strong sedating properties due to the easy penetration of the central nervous system (CNS). Since the sedating effect is so powerful with some agents, they are commonly used as sleep aids. However, children and some adults (though rare) may experience an excitation effect. Some medications in this class have antinausea and antiemetic effects and can be used to prevent motion sickness (though they are not as effective if used to treat an active episode). Some H1 antagonists—predominantly diphen-hydramine—can suppress extrapyramidal symptoms caused by antipsychotic use. The ethanolamine and ethylenedi-amine agent subgroups have antimuscarinic actions, which may help patients with non-allergic rhinorrhea, but also cause undesirable side effects of urinary retention and blurred vision.

First-generation antihistamines are largely anticholinergic and can cause dry mouth, dry eyes, urinary retention, constipation, and cognitive disturbances. Patients with a diagnosis of closed-angle glaucoma, urinary retention, peptic ulcer disease, or uncontrolled asthma should not use first-generation antihistamines. Anticholinergic side effects can be further exacerbated by other anticholinergic medications, such as tricyclic antidepressants (TCAs). Because monoamine oxidase inhibitors (MAOIs) can also exacerbate anticholinergic side effects, first-generation antihistamines should not be used during treatment or within 2 weeks of MAOI discontinuation.

Toxicities of the first-generation antihistamines include convulsions, postural hypotension (increasing the risk of falls in patients, especially the elderly), and cardiac arrhythmias. Central nervous system depression can be additive if first-generation antihistamines are combined with other medications with sedative properties or alcohol. Patients should be cautioned about driving and operating machinery while using these medications. There is also a potential for sedative properties to still be present the following morning if these agents are used for sleep. First-generation an-tihistamines are on the Beers list and are considered potentially harmful in elderly patients; other medication options should be explored if possible.

First-Generation Antihistamines

BrompheniramineCarbinoxamineChlorpheniramineClemastineCyproheptadine

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DiphenhydramineDoxylaminePromethazineTriprolidineDimenhydrinate (See also the Antiemetics section in the Gastrointestinal Agents chapter)Hydroxyzine (See also the Anxiolytics, Sedatives, and Hypnotics section in the Central Nervous System chapter)Meclizine (See also the Antiemetics section in the Gastrointestinal Agents chapter)

Case Studies and Conclusions

Joanne was doing yard work over the weekend and is now covered in an itchy rash on both arms. She states she has not been able to sleep at night because she cannot stop scratching.

1. Which of the following would be the best option to manage Joanne’s allergic reaction?

a. Fexofenadineb. Epinephrinec. Diphenhydramined. Ranitidine

Answer C is correct. Fexofenadine is a nonsedating second-generation antihistamine; this patient would benefit from a first-generation antihistamine to increase sedation at night. Epinephrine is used in cases of anaphylaxis, but this patient presents with a local rash. Ranitidine is an H2 antihistamine that is used for gastrointestinal disorders, not allergies.

It has been a few days, and Joanne’s rash has improved and has almost disappeared. She states that she is going on a cruise next week and is afraid she will get motion sickness. She wants a recommendation for an OTC product.

2. What is an OTC formulation of an antihistamine that can be used to prevent nausea?

a. Doxylamineb. Promethazinec. Diphenhydramined. Cetirizine

Answer C is correct. Doxylamine and cetirizine are not indicated for the treatment of nausea. Promethazine is a prescrip-tion-only medication. Diphenhydramine is OTC and has indications for nausea and vomiting as well as helping with the uti-caria and insomnia.

Joanne returned from her cruise and came home just in time for allergy season. She states that she would like to take a first-generation antihistamine to manage her seasonal allergies.

3. Which of the following statements is FALSE?

a. Counsel the patient about the morning “hangover” that may occur if she takes a first-generation antihis-tamine at bedtime.

b. A common side effect with frequent use of a first-generation antihistamine is diarrhea.c. Many of the first-generation antihistamines should be used with caution in geriatric patients.d. First-generation antihistamines should not be used within 2 weeks of use of an MAOI.

Answer B is correct. First-generation antihistamines can cause daytime sleepiness, so patients should be warned about driving or operating machinery. The most common side effects with these drugs are anticholinergic, such as constipation, urinary retention, dry eyes, and dry mouth. First-generation antihistamines are on the Beers list, so second-generation antihistamines should be used instead if possible. The combination of MAOIs and first- generation antihistamines has the potential to cause hypertensive crisis due to the antihistamine’s concurrent effects on neurotransmitters.

ChAPter 1 Antihistamines 3

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George is a 68-year-old patient being seen for his annual physical examination appointment. He mentions that he experiences seasonal allergies and in the past had success with diphenhydramine. His medical history includes depression, hypertension, dyslipidemia, and type 2 diabetes mellitus.

1. What is a concern with using a first-generation antihistamine in George?

a. Many first-generation antihistamines are Beers list medications and may not be safe for all patients.b. First-generation antihistamines may cause excitation in geriatric patients instead of sedation.c. Use of antihistamines may exacerbate George’s diabetes.d. All of the above are true.

Answer A is correct. First-generation antihistamines are on the Beers list, and alternative options for therapy should be explored if possible. In George’s case, it would be appropriate to try a second-generation antihistamine first. Excitation—as opposed to sedation—is a possible side effect when first-generation antihistamines are used in pediatric patients. These antihistamines have anticholinergic properties and could exacerbate closed-angle glaucoma, urinary retention, and prostatic hypertrophy.

Despite your suggestion that a first-generation antihistamine may not be the best option, George says that he is used to these products and would rather take something with which he has had prior experience. George is currently being treated with fluoxetine (a selective serotonin reuptake inhibitor [SSRI]) for his depression.

2. Which of the following statements is true regarding possible drug interactions between the SSRI and first-generation antihistamines?

a. George must wait 2 weeks between his last dose of fluoxetine and brompheniramine.b. Fluoxetine will exacerbate the anticholinergic side effects of the first-generation antihistamines.c. Fluoxetine may worsen the drowsiness/sedative effects of the first-generation antihistamines.d. Use of antidepressants is contraindicated with the first-generation antihistamines.

Answer C is correct. Use of MAOIs should be avoided when a patient is taking brompheniramine, with a 2-week washout period being recommended. TCAs have the potential to exacerbate anticholinergic side effects of the first-generation antihistamines; some SSRIs have the potential to cause anticholinergic effects, although this is not a common side effect of fluoxetine. Medications that have the potential to lead to CNS depression (including antidepressants) may also worsen the drowsiness and sedative effects of the first-generation antihistamines. Although use of antidepressants is not contraindicated with the first- generation antihistamines, MAOIs, TCAs, and other antidepressants with anticholinergic side effects should be used with caution.

George states that his biggest complaint about his allergies occurs when he is working in his garden. On top of the typical “hay fever”‒like symptoms, he says that he almost always manages to come in contact with poison ivy or poison oak and breaks out in a rash.

3. Which product would be best to manage this patient’s allergic rhinitis and the contact allergic reaction?

a. Meclizineb. Chlorpheniraminec. Doxylamined. Diphenhydramine

Answer D is correct. Meclizine is approved as an antiemetic drug. Chlorpheniramine will treat the allergic rhinitis but does not have contact allergic reactions as a labeled indication. Doxylamine is used for insomnia or allergic rhinitis. Diphenhydramine would manage both allergic rhinitis and the contact allergic reaction.

1.2 Second-Generation AntihistaminesBoth first and second generations of antihistamines have been found to have equal efficacy in the treatment of allergic responses. Unlike the first-generation antihistamines, however, the second-generation products do not cross the blood‒brain barrier to the same extent and, therefore, do not have the same sedative properties; in addition, they have fewer antimuscarinic and anticholinergic effects. Nevertheless, the second-generation antihistamines may still cause drowsiness in some patients, especially if used concurrently with medications that cause CNS depression or


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alcohol. The second-generation products are most commonly used for chronic allergy symptoms due to their lack of sedation and amenability to daily use. This class is the preferred treatment in geriatric patients and children due to the favorable side-effect profile and minimal CNS penetration.

Second-Generation Antihistamines

AcrivastineCetirizineDesloratadineFexofenadineLevocetirizineLoratadineAzelastine (See also the Antiallergic Agents section in the Eye, Ears, Nose, and Throat Preparations chapter)

Case Studies and Conclusions

Ray is a construction worker and has complaints of seasonal allergies. He says that whenever the pollen level is high, he gets watery and itchy eyes, a runny nose, and persistent sneezing.

1. Which of the following would be the best first-choice option for managing Ray’s allergies?

a. Diphenhydramine by mouthb. Azelastine intranasallyc. Loratadine by mouthd. Cimetidine by mouth

Answer C is correct. Ray is a construction worker, so he presumably operates machinery that requires full attention. Thus di-phenhydramine would be too sedating for him. Azelastine intranasally is not a first-choice option; instead, intranasal antihis-tamines are used after the patient has tried an intranasal glucocorticoid. Cimetidine is an H2 antihistamine and used to treat gastrointestinal upset.

Ray later adds that he typically is very congested, during especially bad pollen days.

2. What would the best advice be for the patient?

a. An antihistamine is sufficient alone to manage nasal congestion.b. Use a combination antihistamine and decongestant.c. Use a decongestant alone.d. Use a combination oral and nasal antihistamine when symptoms are worse.

Answer B is correct. Antihistamines alone are not sufficient to manage nasal congestion with allergy symptoms; combination products with a decongestant, such as pseudoephedrine, are more effective. A decongestant alone would manage Ray’s nasal symptoms, but the antihistamine would be required to help treat his other symptoms, such as watery eyes. While nasal antihistamines are effective for symptom management in patients with nasal congestion, they are not a first-line option and need to be used regularly to achieve their greatest efficacy.

Ray asks whether his medications might also be safe for his 72-year old father, who is having similar reactions.

3. Which of the following statements best summarizes the recommended use of antihistamines in older adults?

a. First-generation antihistamines are a good option for geriatric patients with seasonal allergies because they can cause CNS excitation, which can help give them more energy.

b. Second-generation antihistamines are the best option for geriatric patients with seasonal allergies be-cause of their minimal CNS penetration.

c. Geriatric patients should be offered only intranasal or ophthalmic preparations; oral medications are not recommended in older adults.

d. No antihistamines are safe in geriatric patients under any circumstances.

Answer B is correct. Second-generation antihistamines have less CNS penetration and a safer side-effect profile for geriatric patients.


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Sam presents to his doctor’s appointment with complaints of a runny nose, watery eyes, and nasal congestion. He says that these symptoms occur every year around this time, but he usually just muddles his way through the allergy season without any medications. This year, however, his symptoms are worse than ever, and he would like to explore possible medication options.

1. Which of the following is NOT a benefit of Sam using a second-generation antihistamine as opposed to a first-generation antihistamine?

a. The risk of sedation is less with the first-generation antihistamines, so using the second-generation products could help him sleep better at night.

b. Many second-generation products come in combination products with a decongestant.c. Most second-generation medications are dosed once a day.d. All of the above are true.

Answer A is correct. Second-generation antihistamines are less sedating than the first-generation products. Second- generation antihistamines are available in many different combinations, including with pseudoephedrine, ibuprofen, or acetaminophen. Another appealing aspect of second-generation products is that most require only once-daily dosing, whereas most first-generation antihistamines are dosed multiple times a day.

Sam’s medical history includes hypertension, and he has an extensive family history of cardiovascular disease. His blood pressure at the beginning of this visit was elevated, and he says he often forgets to take his blood pressure medication.

2. Which of the following products would be the least appropriate to recommend to Sam?

a. Acrivastineb. Cetirizinec. Fexofenadined. Loratadine

Answer A is correct. Acrivastine should be avoided in patients with severe hypertension or coronary artery disease. Cetirizine, fexofenadine, and loratidine do not have cardiovascular concerns and would be better recommendations for Sam to use.

Sam states that he frequently consumes alcoholic beverages and would like to avoid an allergy agent that is metabolized via the liver.

3. Which of the following medications requires dose adjustment or dose consideration with hepatic impairment?

a. Cetirizineb. Desloratadinec. Levocetirizined. Loratadine

Answer B is correct. Desloratadine requires dose adjustment for both hepatic and renal impairment (5 mg every other day). Cetirizine, levocetirizine, and loratadine require dose adjustment for renal impairment.

1.3 Other AntihistaminesH2 antihistamines (cimetidine, famotidine, nizatidine, and ranitidine) are used to inhibit the secretion of gastric acid in patients with gastrointestinal (GI) disorders. Intranasal products should be used after a patient has tried an intranasal glucocorticoid. Intranasal antihistamines are most effective when used regularly and do not cause rebound effects as nasal decongestants do.

Bepotastine (See also the Antiallergic Agents section in the Eye, Ears, Nose, and Throat Preparations chapter)Cimetidine (See also the Antiulcer Agents and Suppressants section in the Gastrointestinal Agents chapter)Emedastine (See also the Antiallergic Agents section in the Eye, Ears, Nose, and Throat Preparations chapter)


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Famotidine (See also the Antiulcer Agents and Suppressants section in the Gastrointestinal Agents chapter)Ketotifen (See also the Antiallergic Agents section in the Eye, Ears, Nose, and Throat Preparations chapter)Nizatidine (See also the Antiulcer Agents and Suppressants section in the Gastrointestinal Agents chapter)Olopatadine (See also the Antiallergic Agents section in the Eye, Ear, Nose, and Throat Preparations chapter)Ranitidine (See also the Antiulcer Agents and Suppressants section in the Gastrointestinal Agents chapter)

Common Class Considerations

Anaphylaxis: A life-threatening allergic reaction. Signs and symptoms include an itchy rash, swelling of the tongue, bronchoconstriction, hypotension, and facial edema. Anaphylaxis presents suddenly, typically over a few minutes. Antihistamines alone are not a sufficient treatment, and patients should immediately receive epinephrine. Antihistamines and steroids are added as adjuvant treatments.

Excitation: In children, normal doses of first-generation antihistamines often result in an excitatory effect instead of a sedative effect. This phenomenon has also been infrequently reported in some adult cases at ther-apeutic doses, but is more common in overdose and toxic situations.

Sedation/somnolence: Increased sedation and somnolence are frequently reported with use of the first- generation antihistamines. When taken at bedtime, these drugs may also lead to a daytime “hangover” of drowsiness and somnolence. Second-generation antihistamines are referred to as “nonsedating” and have similar incidence of sedation as placebo in studies.

Toxicity: Toxicity of antihistamines has been reported in incidents of overdose or interactions with liver metabolism enzymes (CYP)-inhibiting medications (predominately macrolides and azole a ntifungal drugs), with patients experiencing higher than intended circulating antihistamine levels. Signs and symptoms of toxicity include hallucinations, incoordination, convulsions, cardiac arrhythmias, and fever.

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Tips from the Field

1. Make sure your patients understand the difference between antihistamines and decongestants. Decongestants constrict nasal blood vessels, resulting in an improvement in nasal stuffiness but they do not affect histamine and won’t impact any of the other symptoms associated with hay fever, such as sneezing, runny nose, and itching. Caution patients that if they use nasal spray deconges-tants for more than a few days, these agents can produce a rebound swelling of the nasal tissues, resulting in even greater congestion.

2. Suggest use of OTC products, such as Claritin D, which contain both an antihistamine and a decon-gestant if symptoms warrant use. Make sure they understand the side effects associated with this combination.

3. Help patients determine the right antihistamine for them, for example, daytime use avoid s edating agents like diphenhydramine (Benadryl). Newer generation antihistamines, such as loratadine (Claritin), fexofenadine (Allegra), and cetirizine (Zyrtec), are generally a better choice since they are less sedating.

4. Note that even the newer nonsedating generation antihistamines can cause drowsiness and other symptoms in some people, especially older adults, particularly if they take them at higher doses. Make sure they understand importance of starting the drug at the lowest dose and evaluate its effectiveness.

5. Most of these agents can be purchased OTC and there is no difference between the generic brand ver-sus the name brand.


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6. Explain to your elderly patients that antihistamines can cause other central nervous system effects, in-cluding coordination problems, fatigue, and temporary cognitive impairment. Research has shown an increased risk of long-term cognitive decline in older people who take the drugs regularly.

7. First-generation antihistamines are also more likely than the newer products to cause serious side ef-fects, such as a rapid heart rate or urinary retention (which can be especially problematic in men who have BPH).

8. Several first-generation antihistamines can reduce motion sickness such as diphenhydramine, doxyl-amine, dimenhydrinate (as found in Dramamine), and meclizine (the active ingredient in Bonine) These are all OTC and are the most commonly used motion sickness medications. Make sure they understand that it can take at least 30 minutes for them to take effect.

9. People suffering closed or narrow-angle glaucoma, COPD (chronic obstructive pulmonary disease), kidney disease, prostate problems, hypertension, heart disease, and thyroid problems should not take any OTC antihistamines without first consulting with their provider.

10. The FDA Nonprescription Drug Advisory Committee and the Pediatric Advisory Committee has recommended that nonprescription cough and cold products should not be used in children less than 2 years of age and an official ruling regarding the use of these products in children older than 2 has not yet been announced. Refer to pediatric drug references for additional information (FDA, 2008).

References

American Geriatrics Society. Updated Beers criteria for potentially inappropriate medication use in older adults. J Am Geriatr Soc. 2015;63:2227-2246.

Haas HL, Sergeeva OA, Selbach O. Histamine in the nervous system. Physiol Rev. 2008;88:1183-1241.

Holgate ST, Canonica GW, Simons FE, et al. Consensus Group on New-Generation Antihistamines (CONGA): present status and recom-mendations. Clin Exp Allergy. 2003;33:1305-1324.

McEvoy GK, ed. AHFS: Drug Information. Bethesda, MD: American Society of Health-System Pharmacists; 2016.

Richardson GS, Roehrs TA, Rosenthal L, Koshorek G, Roth T. Tolerance to daytime sedative effects of H1 antihistamines. J Clin Psychopharmacol. 2002;22:511-515.

Skidgel RA, Kaplan AP, Erdös EG. Histamine, bradykinin, and their antagonists. In: Brunton LL, Chabner BA, Knollmann BC, eds. Goodman & Gilman’s The Pharmacological Basis of Therapeutics. 12th ed. New York, NY: McGraw-Hill; 2011:911-936.

U.S. Food and Drug Administration (FDA). Public health advisory: FDA recommends that over-the-counter (OTC) cough and cold products not be used for infants and children under 2 years of age 2008. http://www.fda.gov/NewsEvents/Newsroom / PressAnnouncements/2008/ucm051137.htm


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that

thes

e re

pro

duct

ive

risks

may

als

o ex

tend

to m

ales

.

•Br

and

nam

es a

re p

rovi

ded

for t

hose

age

nts

still

ava

ilab

le o

n th

e m

arke

t. D

ue to

the

ever

-cha

ngin

g p

rodu

ct a

vaila

bili

ty, r

efer

to F

ood

and

Dru

g A

dmin

istr

atio

n (F

DA

) res

ourc

es to

con

firm

the

actu

al b

rand

s av

aila

ble

Thi

s dr

ug s

umm

ary

is fo

r edu

catio

nal p

urp

oses

onl

y. P

resc

ribin

g de

cisi

ons

shou

ld b

e b

ased

on

real

-tim

e co

mp

rehe

nsiv

e dr

ug d

atab

ases

that

are

up

date

d on

a re

gula

r bas

is.

Firs

t-G

ener

atio

n A

ntih

ista

min

esU

nive

rsal

pre

scrib

ing

aler

ts:

•C

entr

al n

ervo

us d

epre

ssio

n ca

n b

e ad

ditiv

e if

first

-gen

erat

ion

antih

ista

min

es a

re c

omb

ined

with

oth

er m

edic

atio

ns w

ith s

edat

ive

pro

per

ties

or a

lcoh

ol; p

atie

nts

shou

ld b

e ca

utio

ned

abou

t driv

ing

and

oper

atin

g m

achi

nery

whi

le u

sing

thes

e m

edic

atio

ns.

•Fi

rst-

gene

ratio

n an

tihis

tam

ines

are

larg

ely

antic

holin

ergi

c ag

ents

and

can

cau

se d

ry m

outh

, dry

eye

s, u

rinar

y re

tent

ion,

con

stip

atio

n, a

nd c

ogni

tive

dist

urb

ance

s;

thei

r use

sho

uld

be

avoi

ded

in p

atie

nts

with

und

erly

ing

clos

ed-a

ngle

gla

ucom

a, u

rinar

y re

tent

ion,

pep

tic u

lcer

dis

ease

, and

unc

ontr

olle

d as

thm

a. A

ntic

holin

ergi

c si

de e

ffec

ts c

an b

e fu

rthe

r exa

cerb

ated

by

othe

r ant

icho

liner

gic

med

icat

ions

, suc

h as

tric

yclic

ant

idep

ress

ants

and

mon

oam

ine

oxid

ase

inhi

bito

rs (M

AO

Is).

•Fi

rst-

gene

ratio

n an

tihis

tam

ines

sho

uld

not b

e us

ed w

ithin

2 w

eeks

of M

AO

Is.

•Th

ere

is a

pot

entia

l for

sed

ativ

e p

rop

ertie

s to

stil

l be

pre

sent

the

follo

win

g m

orni

ng if

thes

e ag

ents

are

use

d fo

r sle

ep.

•Fi

rst-

gene

ratio

n an

tihis

tam

ines

are

on

the

Beer

s lis

t and

are

con

side

red

pote

ntia

lly h

arm

ful i

n el

derly

pat

ient

s; ot

her m

edic

atio

n op

tions

shou

ld b

e ex

plor

ed if

pos

sibl

e.


9781284110562_CH01_Pass01.indd 9 25/11/16 8:03 PM


Dru

g N

ame

FDA

-Ap

pro

ved

Ind

icat

ion

sD

osa

ge

Ran

ge

Prec

auti

on

s an

d C

linic

al P

earl

s

Gen

eric

Nam

e

Brom

phe

nira

min

e m

alea

te

Bra

nd

Nam

e

J-Ta

n PD

Resp

a-BR

Brom

ax

LoH

ist

QT BL PD GD

QT BL PD GD

Alle

rgic

rhin

itis

Com

mon

col

d

Dos

e va

ries

dep

endi

ng

on p

rodu

ct s

elec

ted

Illu

stra

tive

ora

l do

se

(mal

eate

):

6 to

12

mg

ever

y

12 h

ours

•Ta

ke w

ith fo

od, w

ater

, or m

ilk to

min

imiz

e ga

stric

irrit

atio

n

•D

exb

rom

phe

nira

min

e m

alea

te is

a c

hem

ical

ly re

late

d in

gred

ient

•U

se is

gen

eral

ly “a

s ne

eded

”

•So

me

bro

mp

heni

ram

ine

cont

aini

ng p

rodu

cts

are

OTC

and

oth

ers

requ

ire a

pre

scrip

tion

•D

iffer

ent s

alt f

orm

s ar

e av

aila

ble

(mal

eate

and

tann

ate)

requ

iring

di

ffer

ent d

ose

sche

dule

s.

Ava

ilab

le in

mul

tiple

com

bin

atio

n p

rodu

cts.

Ple

ase

see

indi

vidu

al p

rodu

ct

for i

ndic

atio

ns, d

osin

g, a

nd n

ame

bra

nd.

Gen

eric

Nam

e

Car

bin

oxam

ine

mal

eate

Bra

nd

Nam

e

Arb

inox

a

Karb

inal

ER

QT BL PD GD

QT BL PD GD

Alle

rgie

s an

d re

late

d sy

mp

tom

s su

ch a

s rh

initi

s,

pru

ritus

, rhi

norr

hea

and

urtic

aria

Usu

al o

ral d

ose

:

IR: 4

to 8

mg

3 to

4

times

dai

ly

ER: 6

to 1

6 m

g ev

ery

12

hou

rs (n

ot to

exc

eed

32 m

g da

ily)

•Ta

ke o

n an

em

pty

sto

mac

h w

ith w

ater

•A

vaila

ble

by

pre

scrip

tion

only

•Ex

tend

ed re

leas

e an

d im

med

iate

rele

ase

pro

duct

dos

ing

sche

dule

s ar

e di

ffer

ent,

revi

ew d

irect

ions

prio

r to

use

Gen

eric

Nam

e

Chl

orp

heni

ram

ine

mal

eate

Bra

nd

Nam

e

Alle

r-C

hlor

Chl

or-T

rimet

on A

llerg

y

Chl

or-T

rimet

on

Chl

orp

hen

Ed C

hlor

Ped

Ed-C

hlor

tan

Phar

bec

hlor

QT BL PD GD

QT BL PD GD

Alle

rgic

rhin

itis,

pru

ritus

, rh

inor

rhea

, and

urt

icar

iaD

ose

varie

s de

pen

ding

on

pro

duct

sel

ecte

d

Illu

stra

tive

ora

l do

se

imm

edia

te r

elea

se:

4 m

g ev

ery

4 to

6 h

ours

(m

axim

um d

aily

dos

e [M

DD

]: 24

mg)

•D

exch

lorp

heni

ram

ine

mal

eate

is a

che

mic

ally

rela

ted

ingr

edie

nt

•O

TC a

nd p

resc

riptio

n (h

ighe

r dos

es) a

re a

vaila

ble

•Ex

tend

ed re

leas

e an

d im

med

iate

rele

ase

pro

duct

dos

ing

sche

dule

s ar

e di

ffer

ent,

revi

ew d

irect

ions

prio

r to

use

Ava

ilab

le in

mul

tiple

com

bin

atio

n p

rodu

cts.

Ple

ase

see

indi

vidu

al p

rodu

ct

for i

ndic

atio

ns, d

osin

g, a

nd n

ame

bra

nd.


9781284110562_CH01_Pass01.indd 10 25/11/16 8:03 PM


Gen

eric

Nam

e

Cle

mas

tine

fum

arat

e

Bra

nd

Nam

e

Day

hist

Alle

rgy

12 H

our

Relie

f

Tavi

st A

llerg

yQT BL PD GD

QT BL PD GD

Alle

rgic

rhin

itis,

pru

ritus

, ur

ticar

ia, s

ymp

tom

s of

th

e co

mm

on c

old

and

angi

oede

ma

Dos

e va

ries

dep

endi

ng

on p

rodu

ct s

elec

ted

Illu

stra

tive

OTC

ora

l d

ose

: 1.3

4 m

g tw

ice

daily

(MD

D 8

.04

mg

incl

udin

g p

resc

riptio

n do

sing

)

•Ta

ke w

ith fo

od o

r milk

if p

atie

nt e

xper

ienc

es s

tom

ach

upse

t

•Pr

escr

iptio

n p

rodu

cts

avai

lab

le fo

r use

at h

ighe

r dos

es

Ava

ilab

le in

mul

tiple

com

bin

atio

n p

rodu

cts.

Ple

ase

see

indi

vidu

al p

rodu

ct

for i

ndic

atio

ns, d

osin

g, a

nd n

ame

bra

nd.

Gen

eric

Nam

e

Cyp

rohe

pta

dine

hy

droc

hlor

ide

QT BL PD GD

QT BL PD GD

Illu

stra

tive

ind

icat

ion

s fo

r u

se:

Alle

rgic

rhin

itis,

pru

ritus

, ur

ticar

ia, a

nd a

ngio

edem

a

Usu

al o

ral d

ose

:

4 to

20

mg

daily

in

divi

ded

dose

s (M

DD

0.

5 m

g/kg

per

day

or

32 m

g w

hich

ever

is le

ss)

•H

epat

ic im

pai

rmen

t dos

e ad

just

men

t rec

omm

ende

d, h

owev

er, n

o sp

ecifi

c do

se s

ugge

stio

n p

rovi

ded

by m

anuf

actu

rer

Gen

eric

Nam

e

Dip

henh

ydra

min

e hy

droc

hlor

ide

Bra

nd

Nam

e

Bena

dryl

and

var

ious

ot

hers

QT BL PD GD

QT BL PD GD

QT BL PD GD

QT BL PD GD

QT BL PD GD

Illu

stra

tive

ind

icat

ion

s fo

r u

se:

Alle

rgic

rhin

itis,

con

tact

de

rmat

itis,

ant

ituss

ive,

dru

g-in

duce

d EP

S, P

arki

nson

ian

synd

rom

es, i

nsom

nia,

mot

ion

sick

ness

, adj

unct

trea

tmen

t of

anap

hyla

xis

Dos

e va

ries

dep

endi

ng

on c

omb

inat

ion

pro

duct

sel

ecte

d

Illu

stra

tive

ora

l do

se:

25 to

50

mg

ever

y 4

to 8

ho

urs

(max

300

mg

per

24

hou

rs)

Usu

al p

aren

tera

l do

se:

IM/I

V:1

0 to

50

mg

per

do

se

(max

100

mg

per

dos

e;

max

400

mg

per

day

)

•To

pic

al a

pp

licat

ion

can

caus

e an

alle

rgic

-typ

e co

ntac

t der

mat

itis

•D

rug

inte

ract

ions

may

requ

ire d

ose

adju

stm

ents

Ava

ilab

le in

mul

tiple

com

bin

atio

n p

rodu

cts.

Ple

ase

see

indi

vidu

al p

rodu

ct

for i

ndic

atio

ns, d

osin

g, a

nd n

ame

bra

nd.

Gen

eric

Nam

e

Dox

ylam

ine

succ

inat

e

Bra

nd

Nam

e

Dox

ytex

Nite

time

Slee

p-A

id

Slee

p A

id

Uni

som

QT BL PD GD

QT BL PD GD

QT BL PD GD

Alle

rgic

rhin

itis,

inso

mni

aD

ose

varie

s de

pen

ding

on

pro

duct

sel

ecte

d

Illu

stra

tive

ora

l do

se:

25 m

g da

ily o

r at

bed

time

•O

ptim

al d

ose

sche

dule

for i

nsom

nia

is ta

ke d

ose

30 m

inut

es p

rior t

o p

lann

ed 8

-hou

r sle

ep (b

edtim

e)

Ava

ilab

le in

mul

tiple

com

bin

atio

n p

rodu

cts.

Ple

ase

see

indi

vidu

al p

rodu

ct

for i

ndic

atio

ns, d

osin

g, a

nd n

ame

bra

nd.


9781284110562_CH01_Pass01.indd 11 25/11/16 8:03 PM


Gen

eric

Nam

e

Prom

etha

zine

hy

droc

hlor

ide

Bra

nd

Nam

e

Phen

adoz

Phen

erga

n

Prom

ethe

gan

QT BL PD GD

QT BL PD GD

QT BL PD GD

QT BL PD GD

Alle

rgic

con

ditio

ns, m

otio

n si

ckne

ss, a

ntie

met

ic, s

edat

ive

Dos

e va

ries

dep

endi

ng

on p

rodu

ct s

elec

ted

Illu

stra

tive

ora

l do

se

for

nau

sea/

vom

itin

g:

12.5

mg

bef

ore

mea

ls

and

HS

Illu

stra

tive

rec

tal d

ose

fo

r n

ause

a/vo

mit

ing

:

12.5

to 2

5 m

g ev

ery

4 to

6

hour

s as

nee

ded

Illu

stra

tive

IM d

ose

for

nau

sea/

vom

itin

g:

12.5

to 2

5 m

g ev

ery

4 to

6

hour

s as

nee

ded

•M

ild to

mod

erat

e ak

athi

sia

and

extr

apyr

amid

al s

ymp

tom

s p

ossi

ble

aft

er

inje

ctio

n or

long

-ter

m u

se

•U

se is

ass

ocia

ted

with

QT

pro

long

atio

n

•D

rug

inte

ract

ions

may

requ

ire d

ose

adju

stm

ent

•W

hen

trea

ting

naus

ea/v

omiti

ng; a

dmin

iste

r bef

ore

mea

ls o

r sna

ck

•D

eep

IM in

ject

ion

pre

ferr

ed ro

ute

of p

aren

tera

l adm

inis

trat

ion

Ass

ocia

ted

with

:

•In

ject

ion

can

caus

e se

vere

tiss

ue in

jury

•Su

bcu

tane

ous

and

intr

a-ar

teria

l adm

inis

trat

ion

•U

se in

pat

ient

s in

a c

oma

•U

se in

pat

ient

s w

ith a

sthm

a

Ava

ilab

le in

mul

tiple

com

bin

atio

n p

rodu

cts.

Ple

ase

see

indi

vidu

al p

rodu

ct

for i

ndic

atio

ns, d

osin

g, a

nd n

ame

bra

nd.

Gen

eric

Nam

e

Trip

rolid

ine

hydr

ochl

orid

e

Bra

nd

Nam

e

His

tex

PD

His

tex

QT BL PD GD

QT BL PD GD

Alle

rgie

s, rh

initi

s, u

rtic

aria

Dos

e va

ries

dep

endi

ng

on p

rodu

ct s

elec

ted

Illu

stra

tive

ora

l do

se:

2.5

mg

ever

y 4

to 6

ho

urs

(max

10

mg

per

24

hou

rs)

•M

ay b

e ad

min

iste

red

with

out r

egar

d to

mea

ls, h

owev

er m

ay ta

ke w

ith

food

or m

ilk to

min

imiz

e st

omac

h up

set

Ava

ilab

le in

mul

tiple

com

bin

atio

n p

rodu

cts.

Ple

ase

see

indi

vidu

al p

rodu

ct

for i

ndic

atio

ns, d

osin

g, a

nd n

ame

bra

nd.

Dim

enhy

drin

ate

QT BL PD GD

Refe

r to

the

Gas

troi

ntes

tinal

Age

nts c

hapt

er.

Hyd

roxy

zine

QT BL PD GD

Refe

r to

the

Cent

ral N

ervo

us S

yste

m c

hapt

er.

Mec

lizin

e

QT BL PD GD

Refe

r to

the

Gas

troi

ntes

tinal

Age

nts c

hapt

er.


9781284110562_CH01_Pass01.indd 12 25/11/16 8:03 PM


Seco

nd

-Gen

erat

ion

Ant

ihis

tam

ines

•U

nive

rsal

pre

scrib

ing

aler

ts:

Man

y of

thes

e se

cond

-gen

erat

ion

agen

ts c

ause

CN

S de

pre

ssio

n (a

lbei

t not

to th

e sa

me

exte

nt a

s th

e fir

st-g

ener

atio

n an

tihis

tam

ines

). Pa

tient

s sh

ould

use

cau

tion

whe

n p

erfo

rmin

g ta

sks

that

requ

ire m

enta

l ale

rtne

ss.

Dru

g N

ame

FDA

-Ap

pro

ved

Ind

icat

ion

sD

osa

ge

Ran

ge

Prec

auti

on

s an

d C

linic

al P

earl

s

Gen

eric

Nam

e

Acr

ivas

tine

Bra

nd

Nam

e

Sem

pre

x-D

Alle

rgic

rhin

itis,

nas

al

cong

estio

nU

sual

ora

l do

se:

8 m

g ev

ery

4 to

6 h

ours

(32

mg

max

imum

per

da

y)

•A

void

use

in p

atie

nts

with

CrC

l les

s th

an 4

8 m

L/m

in

•U

se in

cau

tion

in p

atie

nts

with

dia

bet

es o

r thy

roid

dys

func

tion

•A

vaila

ble

in c

omb

inat

ion

with

pse

udoe

phe

drin

e on

ly

•8

mg

acriv

astin

e ta

ble

ts a

lso

cont

ain

60 m

g p

seud

oep

hedr

ine

•Re

com

men

ded

for u

se a

s ne

eded

up

to 1

4 da

ys

Con

trai

ndic

atio

ns:

•C

oron

ary

arte

ry d

isea

se

•U

ncon

trol

led

hyp

erte

nsio

n

•D

rug

inte

ract

ions

may

pre

clud

e us

e (i.

e., M

AO

Is)

Gen

eric

Nam

e

Cet

irizi

ne h

ydro

chlo

ride

Bra

nd

Nam

e

All

Day

Alle

rgy

Zyrt

ec

QT BL PD GD

QT BL PD GD

QT BL PD GD

Alle

rgie

s, rh

initi

s, u

rtic

aria

Dos

e va

ries

dep

endi

ng

on p

rodu

ct s

elec

ted

Illu

stra

tive

ora

l do

se:

5 to

10

mg

daily

•C

etiri

zine

is n

ot re

mov

ed w

ith h

emod

ialy

sis

•IS

MP

safe

ty a

lert

(may

sou

nd li

ke o

r loo

k lik

e ot

her m

edic

atio

ns, t

hus

mis

take

s m

ay b

e m

ore

com

mon

with

this

dru

g)

Ava

ilab

le in

mul

tiple

com

bin

atio

n p

rodu

cts.

Ple

ase

see

indi

vidu

al p

rodu

ct

for i

ndic

atio

ns, d

osin

g, a

nd n

ame

bra

nd.

Gen

eric

Nam

e

Des

lora

tadi

ne

Bra

nd

Nam

e

Cla

rinex

QT BL PD GD

QT BL PD GD

QT BL PD GD

Alle

rgic

rhin

itis,

chr

onic

id

iop

athi

c ur

ticar

ia, p

rurit

usD

ose

varie

s de

pen

ding

on

pro

duct

sel

ecte

d

Illu

stra

tive

ora

l do

se:

5 m

g da

ily

•D

eslo

rata

dine

is n

ot re

mov

ed b

y he

mod

ialy

sis

Ava

ilab

le in

mul

tiple

com

bin

atio

n p

rodu

cts.

Ple

ase

see

indi

vidu

al p

rodu

ct

for i

ndic

atio

ns, d

osin

g, a

nd n

ame

bra

nd.


9781284110562_CH01_Pass01.indd 13 25/11/16 8:03 PM


Gen

eric

Nam

e

Fexo

fena

dine

hy

droc

hlor

ide

Bra

nd

Nam

e

Alle

gra

QT BL PD GD

QT BL PD GD

Alle

rgic

rhin

itis

Chr

onic

idio

pat

hic

urtic

aria

Dos

e va

ries

dep

endi

ng

on p

rodu

ct s

elec

ted

Illu

stra

tive

ora

l do

se:

60 m

g tw

ice

daily

or

180

mg

once

dai

ly

Ava

ilab

le in

mul

tiple

com

bin

atio

n p

rodu

cts.

Ple

ase

see

indi

vidu

al p

rodu

ct

for i

ndic

atio

ns, d

osin

g, a

nd n

ame

bra

nd.

Gen

eric

Nam

e

Levo

cetir

izin

e di

hydr

ochl

orid

e

Bra

nd

Nam

e

Xyza

l

QT BL PD GD

QT BL PD GD

Alle

rgic

rhin

itis

Chr

onic

idio

pat

hic

urtic

aria

Usu

al o

ral d

ose

:

5 m

g on

ce d

aily

•D

iarr

hea

and

cons

tipat

ion

com

mon

adv

erse

eff

ects

Con

trai

ndic

atio

ns:

•En

d-st

age

rena

l dis

ease

•U

se o

f lev

ocet

irizi

ne in

pat

ient

s un

derg

oing

dia

lysi

s

Gen

eric

Nam

e

Lora

tadi

ne

Bra

nd

Nam

e A

lave

rt

Alle

rgy

Cla

ritin

Lora

dam

ed

QT BL PD GD

QT BL PD GD

QT BL PD GD

QT BL PD GD

Alle

rgic

rhin

itis,

urt

icar

ia,

pru

ritus

Dos

e va

ries

dep

endi

ng

on p

rodu

ct s

elec

ted

Illu

stra

tive

ora

l do

se:

10 m

g on

ce d

aily

or

5 m

g tw

ice

daily

•H

eada

che

is th

e m

ost c

omm

on s

ide

effe

ct

•O

rally

dis

solv

able

tab

lets

are

ava

ilab

le (t

able

t dis

inte

grat

es w

ith o

r w

ithou

t wat

er)

•Lo

rata

dine

is n

ot re

mov

ed b

y he

mod

ialy

sis

•Br

and

nam

e C

larit

in o

ral p

rodu

cts

do n

ot c

onta

in th

e sa

me

ingr

edie

nt a

s C

larit

in e

ye p

rodu

cts

(ket

otife

n fu

mar

ate)

—us

e ca

re w

hen

pre

scrib

ing

Ava

ilab

le in

mul

tiple

com

bin

atio

n p

rodu

cts.

Ple

ase

see

indi

vidu

al p

rodu

ct

for i

ndic

atio

ns, d

osin

g, a

nd n

ame

bra

nd.

Gen

eric

Nam

e

Aze

last

ine

Bra

nd

Nam

e

Vario

us b

ased

on

pro

duct

se

lect

ed a

nd a

rea

of

app

licat

ion

QT BL PD GD

Refe

r to

the

Eye,

Ear

s, N

ose,

and

Thr

oat P

repa

ratio

ns c

hapt

er.


9781284110562_CH01_Pass01.indd 14 25/11/16 8:03 PM


Oth

er A

ntih

ista

min

esU

nive

rsal

pre

scrib

ing

aler

ts:

•In

tran

asal

ant

ihis

tam

ines

are

mos

t eff

ectiv

e w

hen

used

regu

larl

y an

d do

not

cau

se re

bou

nd e

ffec

ts a

s na

sal d

econ

gest

ants

do.

Dru

g N

ame

FDA

-Ap

pro

ved

Ind

icat

ion

sD

osa

ge

Ran

ge

Prec

auti

on

s an

d C

linic

al P

earl

s

Bep

otas

tine

QT BL PD GD

Refe

r to

the

Eye,

Ear

s, N

ose,

and

Thr

oat P

repa

ratio

ns c

hapt

er.

Cim

etid

ine

QT BL PD GD

Refe

r to

the

Gas

troi

ntes

tinal

Age

nts c

hapt

er.

Emed

astin

e

QT BL PD GD

Refe

r to

the

Eye,

Ear

s, N

ose,

and

Thr

oat P

repa

ratio

ns c

hapt

er.

Fam

otid

ine

QT BL PD GD

Refe

r to

the

Gas

troi

ntes

tinal

Age

nts c

hapt

er.

Keto

tifen

QT BL PD GD

Refe

r to

the

Eye,

Ear

s, N

ose,

and

Thr

oat P

repa

ratio

ns c

hapt

er.

Niz

atid

ine

QT BL PD GD

Refe

r to

the

Gas

troi

ntes

tinal

Age

nts c

hapt

er.

Olo

pat

adin

e

QT BL PD GD

Refe

r to

the

Eye,

Ear

s, N

ose,

and

Thr

oat P

repa

ratio

ns c

hapt

er.

Rani

tidin

e

QT BL PD GD

Refe

r to

the

Gas

troi

ntes

tinal

Age

nts c

hapt

er.


9781284110562_CH01_Pass01.indd 15 25/11/16 8:03 PM


9781284110562_CH01_Pass01.indd 16 25/11/16 8:03 PM


author: kimberly mulcahy, pharmd, bcps editor: …samples.jbpub.com/9781284110401/chapter_1.pdf ·...

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