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Antihistamines and Decongestants (Systemic)

This monograph includes information on the following:


Note: Products containing phenylpropanolamine were removed from the U.S. and Canadian Markets in November 2000.{104}

1) Acrivastine and Pseudoephedrine  
2) Azatadine and Pseudoephedrine
3) Brompheniramine and Phenylephrine 
4) Brompheniramine and Pseudoephedrine 
5) Carbinoxamine and Pseudoephedrine  
6) Cetirizine and Pseudoephedrine  
7) Chlorpheniramine and Phenylephrine 
8) Chlorpheniramine, Phenyltoloxamine, and Phenylephrine 
9) Chlorpheniramine and Pseudoephedrine
10) Chlorpheniramine, Pyrilamine, and Phenylephrine 
11) Dexbrompheniramine and Pseudoephedrine
12) Diphenhydramine and Pseudoephedrine
13) Loratadine and Pseudoephedrine
14) Pheniramine and Phenylephrine  *
15) Promethazine and Phenylephrine  
16) Triprolidine and Pseudoephedrine


INN:
Chlorpheniramine— Chlorphenamine

VA CLASSIFICATION
Primary: RE501


Note: Other combinations containing antihistamines and decongestants in addition to other ingredients are found in Antihistamines, Decongestants, and Analgesics (Systemic);Antihistamines, Decongestants, and Anticholinergics (Systemic);and Cough/Cold Combinations (Systemic).



Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).

*Not commercially available in the U.S.

Not commercially available in Canada.



Category:


Antihistaminic (H 1-receptor)-decongestant —

Indications

Accepted

Congestion, nasal (treatment);
Sneezing (treatment); and
Rhinorrhea (treatment)—Antihistamine and decongestant combinations are indicated for the temporary relief of nasal and sinus congestion, sneezing, and rhinorrhea associated with the common cold and both seasonal and perennial{103}allergic rhinitis .

—The therapeutic effectiveness of oral phenylephrine as a nasal decongestant has been questioned, especially at the usual oral dose. {76}

Note: Products containing terfenadine and pseudoephedrine were withdrawn from the U.S. market by the Food and Drug Administration in February 1998.


Note: In November 2000, the Food and Drug Administration (FDA) issued a public health warning regarding phenylpropanolamine (PPA) due to the risk of hemorrhagic stroke. The FDA, supported by the final report of The Hemorrhagic Stroke Project (HSP){102}, requested that manufacturers voluntarily discontinue marketing products that contain PPA and that consumers work with their healthcare providers to select alternative products.{101}{104}



Pharmacology/Pharmacokinetics

Physicochemical characteristics:

Chemical group—
    Ethanolamine derivatives: Bromodiphenhydramine; Carbinoxamine; Clemastine; Diphenhydramine
    Ethylenediamine derivatives: Pyrilamine; Tripelennamine
    Piperidine derivatives: Azatadine; Loratadine; Cetirizine
    Propylamine derivatives (alkylamines): Brompheniramine; Chlorpheniramine; Dexbrompheniramine; Pheniramine; Triprolidine
    Phenothiazine derivative: Promethazine
    Sympathomimetic amines: Phenylephrine; Pseudoephedrine
    Miscellaneous: Phenindamine; Phenyltoloxamine
Molecular weight—
    Brompheniramine maleate: 435.32
    Cetirizine hydrochloride: 461.82
    Chlorpheniramine maleate: 390.87
    Clemastine fumarate: 459.97
    Dexbrompheniramine maleate: 435.32
    Diphenhydramine hydrochloride: 291.82
    Loratadine: 382.89
    Phenylephrine hydrochloride: 203.67
    Promethazine hydrochloride: 320.88
    Pseudoephedrine hydrochloride: 201.70
    Pseudoephedrine sulfate: 428.54
    Pyrilamine maleate: 401.46
    Triprolidine hydrochloride: 332.87

pKa—
    Brompheniramine maleate: 3.59 and 9.12
    Chlorpheniramine maleate: 9.2
    Diphenhydramine hydrochloride: 9
    Pseudoephedrine: 9.4 {76}
    Triprolidine hydrochloride: 3.6 and 9.3

Mechanism of action/Effect:

Antihistaminic (H 1 -receptor)—Antihistamines used in the treatment of allergy act by competing with histamine for H 1-receptor sites on effector cells. They thereby prevent, but do not reverse, responses mediated by histamine alone. The anticholinergic actions of most antihistamines (loratadine has no significant anticholinergic activity) provide a drying effect on the nasal and oral mucosa. {23} {25} {30}

Decongestant—Sympathomimetic amines act on alpha-adrenergic receptors in the mucosa of the respiratory tract to produce vasoconstriction, which temporarily reduces the swelling associated with inflammation of the mucous membranes lining the nasal passages. {76}


Other actions/effects:

Cetirizine—In animal models it has been shown that cetirizine has negligible anticholinergic and antiserotonergic activity. However, in clinical studies, dry mouth was more common with cetirizine than with placebo. Ex-vivo experiments in mice have shown that cetirizine does not significantly occupy cerebral H 1 receptors{103}

Promethazine—Has antiemetic, antivertigo, hypnotic, and sedative actions.

Pseudoephedrine—Has an indirect vasoconstrictor effect; has relatively weaker pressor and cardiac actions than ephedrine; may also produce mild CNS stimulation, especially in patients sensitive to sympathomimetic drugs. {01} {25} {26}

Absorption:

Antihistamines and sympathomimetic amines, except phenylephrine, are well absorbed from the gastrointestinal tract after oral administration. Phenylephrine has reduced bioavailability (about 38%) from gastrointestinal tract because of first pass metabolism by monoamine oxidase in the stomach and liver. {23} {76}

Protein binding:

Cetirizine—Very high (93%) {103}

Chlorpheniramine—High (72%).

Diphenhydramine—Very high (98 to 99%).

Biotransformation:


Antihistamines:

Hepatic (cytochrome P-450 system); some renal. Of the second generation antihistamines, loratadine is metabolized by the hepatic cytochrome P-450 system and have active metabolites. {51} {53} {54} {55} {96}



Sympathomimetic amines:

Phenylephrine: Extensive in the intestinal wall and in the liver. Sulfate conjugates are formed largely in the intestinal wall. Also, undergoes oxidative deamination by monoamine oxidase. {76}

Pseudoephedrine: Incompletely metabolized in the liver; less than 1% by N-demethylation to the active metabolite norpseudoephedrine. {76}


Half-life:


Antihistamines:


Acrivastine—

1.5 to 3.5 hours. {79}



Brompheniramine—

25 hours.



Cetirizine——

Mean elimination half-life is 7.9 hours.{103}



Chlorpheniramine—

21 to 27 hours.



Diphenhydramine—

1 to 4 hours.



Loratadine—

3 to 20 hours (mean, 8.4 hours). {53} {56}



Triprolidine—

3 to 3.3 hours.




Sympathomimetic amines{76}:


Phenylephrine—

2.1 to 3.4 hours.



Pseudoephedrine—

4.5 to 8 hours.

In children—Mean half-life of pseudoephedrine has been reported to be 4.6 hours.



Onset of action:


Antihistamines:

Most first generation antihistamines: 15 to 60 minutes.

Acrivastine: 0.5 hour. {79}

Cetirizine: within 1 hour.{103}

Loratadine: 1 hour. {78}

Promethazine: 20 minutes.



Sympathomimetic amines:

Pseudoephedrine: 30 minutes.


Time to peak concentration:


Antihistamines:

Acrivastine: 0.8 to 1.7 hours. {79}

Brompheniramine: 2 to 5 hours.

Cetirizine: 2.2 hours.{103}

Chlorpheniramine: 2 to 6 hours.

Diphenhydramine: 1 to 4 hours.

Triprolidine: 2 hours.



Sympathomimetic amines{76}:

Phenylephrine: 0.75 to 2 hours (to achieve peak levels ranging from 0.9 to 298 ng/mL, respectively).

Pseudoephedrine: 1.97 hours (to achieve a concentration of 422 ng/mL).


Time to peak effect:


Antihistamines:

Brompheniramine: 3 to 9 hours.

Chlorpheniramine: 6 hours.

Triprolidine: 2 to 3 hours.


Duration of action:


Antihistamines {01} {31}:


Ethanolamine derivatives—

6 to 8 hours.



Ethylenediamine derivatives—

Pyrilamine—8 hours.



Piperidine derivatives—

Cetirizine—At least 24 hours.{103}

Loratadine—At least 24 hours. {78}



Propylamine derivatives—

4 to 8 hours.

Acrivastine: 6 to 8 hours. {79}




Sympathomimetic amines:


Pseudoephedrine—

3 to 4 hours.




Promethazine and pseudoephedrine combination:

4 to 6 hours.


Elimination:


Antihistamines—
        Renal . Most of the antihistamines studied are excreted as metabolites within 24 hours.
        Promethazine: Renal; slow; mainly as inactive metabolites.



Sympathomimetic amines—
        Renal.
        Phenylephrine: 2.6% of the administered oral dose is excreted unchanged. Eighty to 86% of unchanged phenylephrine and metabolites are recovered in 48 hours after oral administration. {76}
        Pseudoephedrine: Forty-three to 96% is excreted unchanged in urine within 24 hours. Clearance of pseudoephedrine is more rapid in children than in adults. {76}



Precautions to Consider

Cross-sensitivity and/or related problems

Patients sensitive to other antihistamines or other sympathomimetics (for example, amphetamines, ephedrine, epinephrine, isoproterenol, metaproterenol, norepinephrine, terbutaline) may be sensitive to these medications also.

Carcinogenicity/Mutagenicity

Long-term animal studies to evaluate carcinogenic or mutagenic potential have not been performed.

Loratadine—In carcinogenicity studies, AUC data demonstrated that the exposure of mice given loratadine 40 mg/kg was 3.6 (loratadine) and 18 (active metabolite) times higher than a human given 10 mg/day. Exposure of rats given 25 mg/kg was 28 (loratadine) and 67 (active metabolite) times higher than a human given 10 mg/day. Male mice given 40 mg/kg had a significantly higher incidence of hepatocellular tumors (combined adenomas and carcinomas) than concurrent controls. In rats, a significantly higher incidence of hepatocellular tumors (combined adenomas and carcinomas) was observed in males given 10 mg/kg and males and females given 25 mg/kg. The clinical significance of these findings during long-term use of loratadine is not known. {78}

Pregnancy/Reproduction

Pregnancy—
Although the occasional use at the recommended doses of antihistamine and decongestant combinations during pregnancy is not likely to result in adverse effects on the fetus or newborn infant, the following information should be considered in the event of high-dose and/or long-term usage.


Azatadine and pseudoephedrine

Studies in humans have not been done.

Some studies in animals have shown that azatadine and pseudoephedrine combination administered to pregnant rabbits at multiples of the human dose caused retarded fetal development, hyoid wings in the offspring, and increased incidence of resorption. When administered to rats at multiples of the human dose, the fetal survival rate was decreased.

FDA Pregnancy Category C.

Carbinoxamine and pseudoephedrine;

Chlorpheniramine and pseudoephedrine;

Chlorpheniramine, pyrilamine, and phenylephrine; and

Studies have not been done in humans.

Studies have not been done in animals.

FDA Pregnancy Category C.

Cetirizine and pseudoephedrine Studies have not been done in humans.

Studies in rats with the combination of cetirizine and pseudoephedrine caused developmental toxicity when administered orally at doses of approximately 5 times the maximum recommended daily dose in adults on a mg/m 2 basis. When rats were doses through pregnancy with oral doses of cetirizine/pseudoephedrine, 6/154 mg/kg increased the number of fetal skeletal malformations (rib distortions) and variants (unossified sternebrae). {103}
FDA Pregnancy Category C{103}


Triprolidine and pseudoephedrine: Studies in humans have not been done.

Studies in rats and rabbits at doses up to 933 and 560 times the human dose, respectively, of clemastine alone, and doses up to 70 times the human dose of triprolidine and pseudoephedrine have not shown that these combinations cause adverse effects on the fetus.

FDA Pregnancy Category B.

Phenothiazines: Phenothiazines have been reported to cause jaundice and extrapyramidal symptoms in infants whose mothers received these medications during pregnancy. Adequate and well-controlled studies in humans have not been done with promethazine. However, promethazine taken within 2 weeks prior to delivery may inhibit platelet aggregation in the newborn.

Studies in rats given doses 2.1 to 4.2 times the maximum recommended human daily dose have not shown that promethazine causes adverse effects on fetal development.

Promethazine and pseudoephedrine —Studies have not been done with this combination in humans.

Studies have not been done in animals.

FDA Pregnancy Category C.


Breast-feeding


Antihistamines:

Small amounts of antihistamines are distributed into breast milk; use is not recommended in nursing mothers because of the risk of antihistamines causing excitement or irritability in infants. Antihistamines (except loratadine ) may inhibit lactation because of their anticholinergic action. {15}

Cetirizine and Pseudoephedrine Because cetirizine and pseudoephedrine are distributed into breast milk its use in nursing mothers is not recommended {103}

When pseudoephedrine was administered alone, 0.4 to 0.7% of the dose has been reported to be distributed into human breast milk.{103}

When cetirizine is administered alone, it has been reported to be excreted in human breast milk.{103}

In animal studies with rats, when dosing of 6 mg per kg of cetirizine and 154 mg per kg of pseudoephedrine combined, which is approximately 5 times the maximum recommended daily dose in adults, was continued throughout lactation, the viability and weight gain of the offspring decreased. This effect was not found when doses equivalent to maximum recommended daily doses in adults where given{103}.

When cetirizine was administered alone, in animal studies it was reported that approximately 3% of the dose is distributed into breast milk.{103}

Loratadine: Loratadine and its metabolite descarboethoxyloratadine are distributed into breast milk, achieving concentrations equivalent to plasma levels. In one study, approximately 0.03% of the administered dose was distributed into breast milk over 48 hours after maternal ingestion of a single oral dose of 40 mg. {53}

Promethazine: Use is not recommended in nursing mothers since promethazine may be distributed into the breast milk. Some studies have indicated that the use of promethazine in children up to 2 years of age may be associated with the sudden infant death syndrome (SIDS) and an increase in sleep apnea, thus possibly increasing the risk to the nursing infant. However, more studies are needed to confirm these findings. {15} {59} {60} {61}



Sympathomimetic amines:

Small amounts of sympathomimetic amines are distributed into breast milk; use is not recommended in nursing mothers because of the high risk for infants from sympathomimetic amines. {27}

Pseudoephedrine: Approximately 0.5% of an oral dose is distributed into breast milk over 24 hours. {76}


Pediatrics


Antihistamines:

Use of antihistamines is not recommended in newborn or premature infants. This age group may be at a higher risk than other age groups because of an increased susceptibility to anticholinergic effects, such as CNS excitation, and an increased tendency toward convulsions. {28}

In children taking antihistamines, a paradoxical reaction characterized by hyperexcitability may occur.

Promethazine: Some studies have associated the use of promethazine with sudden infant death syndrome (SIDS) and with an increase in infant sleep apnea. Until more studies have been performed to confirm this potential risk, promethazine should not be used in children up to 2 years of age. {15}



Sympathomimetic amines:

Very young children may be more sensitive to the effects, especially the vasopressor effects, of sympathomimetic amines. {07}



Geriatrics



Antihistamines:

Confusion, dizziness, sedation, hypotension, hyperexcitability, and anticholinergic side effects, such as dryness of mouth and urinary retention (especially in males), may be more likely to occur in geriatric patients taking antihistamines. If the anticholinergic side effects occur and continue or are severe, medication should probably be discontinued.



Sympathomimetic amines:

Confusion, hallucinations, seizures, and CNS depression may be more likely to occur in geriatric patients taking sympathomimetics. {29} Geriatric patients may also be more sensitive to the effects, especially to the vasopressor effects, of sympathomimetic amines.



Dental

Prolonged use of antihistamines (except loratadine ) may decrease or inhibit salivary flow, especially in middle-aged or elderly patients, thus contributing to the development of caries, periodontal disease, oral candidiasis, and discomfort.

Promethazine: Involuntary orofacial muscle movement may result from extrapyramidal effects. These involuntary movements may result in occlusal adjustments and bite registrations being less reliable. In addition, treatment for bruxism may be less effective. {50}

Drug interactions and/or related problems
The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):


Note: It is not likely that the combinations containing loratadine will interact with the medications that exacerbate anticholinergic or CNS depressant effects since loratadine lacks significant anticholinergic and CNS actions. {40}
Combination products containing any of the following medications, depending on the amount present, may also interact with this medication.

» Alcohol or
» CNS depression–producing medications, other (See Appendix II)    (concurrent use may potentiate the CNS depressant effects of either these medications or antihistamines {01})


Anesthetics, hydrocarbon inhalation, such as:
Chloroform
Cyclopropane
Enflurane
Halothane
Isoflurane
Methoxyflurane
Trichloroethylene or
Digitalis glycosides    (cardiac arrhythmias may occur when phenylephrine, and pseudoephedrine are used prior to anesthesia or concurrently with digitalis glycosides, since these medications may sensitize the myocardium to the effects of the sympathomimetics {32})


» Anticholinergics or other medications with anticholinergic activity (See Appendix II)    (anticholinergic effects may be potentiated when these medications are used concurrently with antihistamines; patients should be advised to report occurrence of gastrointestinal problems promptly, since paralytic ileus may occur with concurrent therapy)


» Antidepressants, tricyclic or
» Maprotiline    (concurrent use with antihistamines may potentiate the anticholinergic and/or CNS depressant effects of either these medications or the antihistamine contained in these combinations)

    (tricyclic antidepressants may potentiate the response to sympathomimetic amines by blocking the reuptake of biogenic amines by nerve terminals {19} {32} {35})


Antihypertensives or
Diuretics used as antihypertensives    (antihypertensive effects may be reduced when these medications are used concurrently with sympathomimetic amines; the patient should be carefully monitored to confirm that the desired effect is being obtained {01} {32} {33} {35})


» Beta-adrenergic blocking agents    (concurrent use with sympathomimetic amines may result in significant hypertension and excessive bradycardia with possible heart block; concurrent use requires careful monitoring {19} {22} {32} {33})


» CNS stimulation–producing medications, other (See Appendix II )    (concurrent use with pseudoephedrine may result in additive CNS stimulation to excessive levels, which may cause unwanted effects, such as nervousness, irritability, insomnia, or possibly convulsions or cardiac arrhythmias {21})


» Digitalis glycosides    (concurrent administration with pseudoephedrine can result in increased ectopic pacemaker activity.{103})


Doxapram    (concurrent use may increase the pressor effects of either doxapram or the sympathomimetic amine)


Fluconazole or
» Itraconazole or
» Ketoconazole or
Metronidazole or
Miconazole    (concurrent use with ketoconazole or itraconazole may increase plasma levels of loratadine because of inhibition of the P450 metabolic pathways by these antifungals; there are no reports to date of serious ventricular arrhythmias associated with increased plasma levels of loratadine; {51} {54} {63} {64} {65} {68} {72} {73} {74} {78}; {97})


» Monoamine oxidase (MAO) inhibitors, including furazolidone and procarbazine    (concurrent use with antihistamines may prolong and intensify the anticholinergic and CNS depressant effects of antihistamines; concurrent use is not recommended )

    (concurrent use with sympathomimetic amines may prolong and intensify cardiac stimulant and vasopressor effects [including headache, cardiac arrhythmias, vomiting, sudden and severe hypertensive and hyperpyretic crises] of phenylephrine, and pseudoephedrine because of release of catecholamines, which accumulate in intraneuronal storage sites during MAO inhibitor therapy; these medications should not be administered during or within 14 days following the administration of a MAO inhibitor {01} {32} {35} {37} {76})


Ototoxic medications (See Appendix II )    (concurrent use with antihistamines may mask the symptoms of ototoxicity such as tinnitus, dizziness, or vertigo {30})


» Rauwolfia alkaloids    (concurrent use of rauwolfia alkaloids may inhibit the indirect-acting sympathomimetic action of pseudoephedrine by depleting catecholamine stores, and may theoretically prolong the action of direct-acting sympathomimetics, such as phenylephrine, by preventing uptake into storage granules)


Sympathomimetics, other    (concurrent use may increase the cardiovascular effects of either the other sympathomimetics or pseudoephedrine and the potential for side effects.{103})


Theophylline    (concurrent administration of theophylline (400 mg once a day for 3 days) with cetirizine has resulted in a 16% decrease in cetirizine clearance{103})



Laboratory value alterations
The following have been selected on the basis of their potential clinical significance (possible effect in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):

With diagnostic test results

For all antihistamines:
Skin tests using allergen extracts    (may inhibit the cutaneous histamine response thus producing false-negative results; it is recommended that antihistamine-containing medication be discontinued at least 72 hours before testing begins [at least 1 week with loratadine and cetrizine{106}])


For cetirizine:
Transaminase and
bilirubin    ( reversible hepatic transaminase elevations and elevated bilirubin has been associated with the use of cetirizine{103})


For promethazine:
Glucose tolerance test    (an increase in glucose tolerance has been reported)


Immunologic urine pregnancy tests    (may produce false-positive or false-negative results, depending on the test used)


Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Except under special circumstances, this medication should not be used when the following medical problem exists:

Risk-benefit should be considered when the following medical problems exist
» Bladder neck obstruction or
» Urinary retention, predisposition to    (anticholinergic effects of antihistamines, and sympathomimetic amines stimulation of alpha-adrenergic receptors on the trigone and sphincter muscles of the bladder, may precipitate or aggravate urinary retention {01} {77})


» Cardiovascular disease    (pressor effects and increase in heart rate may be exacerbated due to sympathomimetic amine–induced cardiovascular effects {35})


» Diabetes mellitus    (sympathomimetic amines may increase risk of developing cardiovascular disease {01})


» Glaucoma, angle-closure, narrow-angle or predisposition to    (increased intraocular pressure may precipitate an acute attack of angle-closure glaucoma {01}{103})


Glaucoma, open angle    (mydriatic effect of antihistamines may cause a slight increase in intraocular pressure; glaucoma therapy may need to be adjusted)


» Hepatic function impairment {100}    (reduced clearance of loratadine; avoidance of loratadine is recommended by the manufacturer)

    (hepatic impairment results in a 50% increase in half-life of cetirizine along with a corresponding 40% decrease in clearance.{103})


» Hypertension    (vasoconstrictive properties of sympathomimetic amines may exacerbate condition {01})


» Hypertension, severe    (pressor effect of sympathomimetic amines may precipitate a hypertensive crisis {01})


» Hyperthyroidism    (characterized by tachycardia, which may be increased due to cardiac stimulant properties of sympathomimetic amines {01})


» Prostatic hypertrophy, symptomatic    (reduction in tone of urinary bladder may lead to complete urinary retention {01})


» Renal function impairment {100}    (reduced clearance elimination of loratadine; dosage reduction is recommended by the manufacturer)


» Sensitivity to the antihistamine or decongestant in the combination used
» Urinary retention    (condition may be exacerbated due to sympathomimetic activity of pseudoephedrine{103})


Caution is recommended when promethazine is used, since signs of intestinal obstruction, brain tumor, or overdosage of toxic drugs may be obscured by its antiemetic action.


Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention
Incidence rare
—more frequent with high doses    
Anaphylaxis (skin rash or hives; troubled breathing; swollen mouth or throat){103}
    
Blood dyscrasias (fever; sore throat; unusual bleeding or bruising; unusual tiredness or weakness)
    
cardiac arrhythmias (fast or irregular heartbeat)
    
cholestasis ( stomach pain; light-colored stools; dark urine; diarrhea; fever; vomiting of blood; yellow eyes or skin){103}
    
glomerulonephritis (bloody or cloudy urine; increased blood pressure; sudden decrease in amount of urine; swelling of face, fingers, feet, and/or lower legs; rapid weight gain){103}
    
hemolytic anemia (back, leg, or stomach pains; bleeding gums; dark urine; fatigue; fever; general body swelling; nosebleeds; pale or yellow skin or eyes){103}
    
hepatitis (dark urine; general tiredness and weakness; light-colored stools; nausea and vomiting; upper right abdominal pain; yellow eyes and skin){103}
    
hypotension, severe ( blurred vision; confusion; dizziness, faintness, or lightheadedness when getting up from a lying or sitting position; sudden sweating; unusual tiredness or weakness){103}
    
mood or mental changes (psychotic episodes, usually associated with previous history of psychiatric illness)
    
orofacial dyskinesia (twitching, twisting, or uncontrolled repetitive movements of face ){103}
    
stillbirth {103}
    
thrombocytopenia (black, tarry stools; chest pain; chills; swollen glands; unusual bleeding or bruising){103}
    
tightness in chest

Symptoms of overdose
    
Anticholinergic effects (clumsiness or unsteadiness; severe dryness of mouth, nose, or throat; flushing or redness of face; shortness of breath or troubled breathing)
    
cardiac arrhythmias (fast or irregular heartbeat)
    
CNS stimulation (hallucinations; seizures; trouble in sleeping)
    
drowsiness, severe
    
extrapyramidal effects (muscle spasms, especially of neck and back; restlessness; shuffling walk; tic-like [jerky] movements of head and face; trembling and shaking of hands)— for promethazine only
    
hypertension (headache, continuing; slow or fast heartbeat)
Note: Anticholinergic and CNS depressant effects are not clinically significant with loratadine. {40} {41}





Those indicating need for medical attention only if they continue or are bothersome
Incidence more frequent
    
Drowsiness —more pronounced with antihistamine ethanolamine derivatives; less pronounced with the propylamine (alkylamine) derivatives, loratadine
    
thickening of bronchial secretions

Incidence less frequent
—more frequent with high doses    
Blurred vision
    
confusion
    
difficult or painful urination
    
dizziness
    
dryness of mouth, nose, or throat
    
headache
    
loss of appetite
    
paradoxical reaction (nightmares; unusual excitement, nervousness, restlessness, or irritability)
    
pounding heartbeat
    
ringing or buzzing in ears
    
skin rash
    
Somnolence (sleepiness or unusual drowsiness; extreme tiredness ){103}
    
stomach upset or pain —more frequent with antihistamine ethylenediamine derivatives





Overdose

Treatment of overdose
Since there is no specific antidote for overdose with antihistamine and decongestant combinations, treatment is symptomatic and supportive with possible utilization of the following:    • Induction of emesis (syrup of ipecac recommended); however, precaution against aspiration necessary, especially in infants and children.
   • Gastric lavage (isotonic or 0.45% sodium chloride solution) if patient unable to vomit within three hours of ingestion.
   • Saline cathartics (milk of magnesia) are sometimes used.
   • Vasopressors to treat hypotension; however, epinephrine should not be used since it may further lower blood pressure.
   • Oxygen and intravenous fluids.
   • Precaution against use of stimulants (analeptic agents) because they may cause seizures.



Patient Consultation

Note: Products containing phenylpropanolamine were removed from the U.S. and Canadian Markets in November 2000.

As an aid to patient consultation, refer to Advice for the Patient, Antihistamines and Decongestants (Systemic) .

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Sensitivity to any of the antihistamines or sympathomimetic amines

Pregnancy—Studies in animals have shown that cetirizine and pseudoephedrine causes skeletal malformities and variants.{103}

Concern for the fetus and/or newborn infant only with high doses and long-term therapy;





Breast-feeding—Antihistamines may cause excitement or irritability in nursing infants; high risk for infants from sympathomimetic amines





Use in children—Increased susceptibility to anticholinergic effects of antihistamines and to vasopressor effects of sympathomimetic amines;






Use in the elderly—Anticholinergic and CNS stimulant effects more likely to occur
Other medications, especially anticholinergics; medicine for high blood pressure or depression; alcohol or CNS depression-producing medications, digitalis glycosides, and monoamine oxidase inhibitors (with cetirizine and pseudoephedrine).
Other medical problems, especially cardiovascular disease, diabetes, hepatic function impairment, hypertension, hyperthyroidism, increased intraocular pressure, narrow angle glaucoma, prostatic hypertrophy, renal function impairment, or urinary retention

Proper use of this medication
» Importance of not taking more medication than the amount recommended

Taking with food, water, or milk to minimize gastric irritation

Swallowing extended-release dosage form whole

» Proper dosing
Missed dose: If on scheduled dosing regimen—Taking as soon as possible; not taking if almost time for next dose; not doubling doses

» Proper storage

Precautions while using this medication
Caution if skin tests using allergens required; possible interference with test results

May mask ototoxic effects of large doses of salicylates

» Avoiding use of alcohol or other CNS depressants

» Caution if drowsiness or dizziness occurs

» Caution if taking appetite suppressants

» Possible insomnia; taking the medication a few hours before bedtime

Possible dryness of mouth; using sugarless gum or candy, ice, or saliva substitute for relief; checking with dentist if dry mouth continues for more than 2 weeks.

For promethazine
Possible interference with diagnosis of intestinal obstruction, brain tumor, or overdosage of toxic drugs; need to inform physician of use


Side/adverse effects
Signs of potential side effects, especially anaphylaxis, blood dyscrasias, cardiac arrhythmias, cholestasis, glomerulonephritis, hemolytic anemia, hepatitis, severe hypotension, orofacial dyskinesia, psychotic episodes, stillbirth, thrombocytopenia and tightness in chest


General Dosing Information

Diet/Nutrition
This medication may be taken with food, water, or milk to lessen gastric irritation. However, gastric irritation occurs rarely with the extended-release capsules.

ANTIHISTAMINES AND DECONGESTANTS


Oral Dosage Forms

Table 1. Oral Dosage Forms


Note: Products containing phenylpropanolamine were removed from the U.S. and Canadian Markets in November 2000.{104}


Note: Content per capsule, tablet, or 5 mL, unless otherwise stated.



Brand or
generic name
[availability]
Antihistamines
Decongestants
Other
content
information
as per product
label
Usual adult
and adolescent
dose *
prn
Usual
pediatric
dose prn
Packaging,
storage, and
auxiliary
labeling
Allerest Maximum Strength Tablets (OTC) [U.S.]
Chlorpheniramine
maleate 2 mg
Pseudoephedrine HCl
30 mg
  2 tabs
q 4–6 hr
(max 8 tabs/
day)
6–12 yrs:
1 tab
q 4–6 hr
(max 4 tabs/
day)
a
 
Allerphed Syrup USP (OTC)
[U.S.]
Triprolidine HCl
1.25 mg
Pseudoephedrine HCl
30 mg
  10 mL
q 4–6 hr
(max 40 mL/
day)
6–12 yrs:
5 mL
q 4–6 hr
b, e, f, g
 
Atrohist Pediatric Extended-release
Capsules (Rx)
[U.S.]
Chlorpheniramine
maleate 4 mg
Pseudoephedrine HCl
60 mg
  2 caps q 12 hr
6–12 yrs:
1 cap q 12 hr
b, g
 
Atrohist Pediatric Suspension Dye Free Oral Suspension
(Rx)
[U.S.]
Chlorpheniramine
tannate 2 mg,
Pyrilamine
tannate 12.5 mg
Phenylephrine
tannate 5 mg
  Intended
for
pediatric
use
2–6 yrs:
2.5–5 mL,
6–12 yrs:
5–10 mL,
q 12 hr
a, e, g, i
 
Benadryl Allergy Decongestant Liquid Medication Oral Solution (OTC)
[U.S.]
Diphenhydramine
HCl 12.5 mg
Pseudoephedrine HCl
30 mg
Alcohol free
Sugar free
10 mL
q 4–6 hr
(max 40 mL
/day)
6–12 yrs: 5 mL
q 4–6 hr
(max 20 mL/
day)
c, e, g
 
Brofed Liquid Oral Solution (Rx)
[U.S.]
Brompheniramine
maleate 4 mg
Pseudoephedrine HCl
30 mg
  10 mL q 8 hr
(max 3 doses/
day)
2–6 yrs:
2.5 mL,
6–12 yrs:
5 mL,
q 8 hr
(max 3 doses/
day)
a, e, f, g
 
Bromadrine TR Extended-release
Capsules (Rx) [U.S.]
Brompheniramine
maleate 12 mg
Pseudoephedrine HCl
120 mg
  1 cap q 12 hr
  b, g
 
Bromfed Extended-release
Capsules (Rx) [U.S.]
Brompheniramine
maleate 12 mg
Pseudoephedrine HCl
120 mg
  1 cap q 12 hr
  a, g
 
Syrup (OTC)
[U.S.]
Brompheniramine
maleate 2 mg
Pseudoephedrine HCl
30 mg
Alcohol free
10 mL
q 4–6 hr
(max 40 mL/
day)
6–12 yrs: 5 mL
q 4–6 hr
(max 20 mL/
day)
b, e, f, g
 
Tablets (Rx)
[U.S.]
Brompheniramine
maleate 4 mg
Pseudoephedrine HCl
60 mg
Scored
1 tab q 4 hr
(max 6 tabs/
day)
6–12 yrs:
1/2 tab q 4 hr
(max 3 tabs/
day)
a, g
 
Bromfed-PD Extended-release
Capsules (Rx) [U.S.]
Brompheniramine
maleate 6 mg
Pseudoephedrine HCl
60 mg
  1–2 caps
q 12 hr
6–12 yrs: 1 cap
q 12 hr
b, g
 
Bromfenex Extended-release
Capsules (Rx)
[U.S.]
Brompheniramine
maleate 12 mg
Pseudoephedrine HCl
120 mg
  1 cap q 12 hr
  a, g
 
Bromfenex PD Extended-release
Capsules (Rx)
[U.S.]
Brompheniramine
maleate 6 mg
Pseudoephedrine HCl
60 mg
  1–2 caps
q 12 hr
6–12 yrs:
1 cap q 12 hr
a, g
 
Brompheniramine
Maleate and
Pseudoephedrine HCl
Extended-release
Capsules (Rx) [U.S.]
Brompheniramine
maleate 6 mg
Pseudoephedrine HCl
60 mg
  1–2 caps
q 12 hr
6–12 yrs:
1 cap q 12 hr
a, g
 
  Brompheniramine
maleate 12 mg
Pseudoephedrine HCl
120 mg
  1 cap q 12 hr
  a, g
 
Chlordrine S.R. Extended-release
Capsules (Rx) [U.S.]
Chlorpheniramine
maleate 8 mg
Pseudoephedrine HCl
120 mg
  1 cap q 12 hr
  a, g
 
Chlorfed-A Extended-release
Capsules (Rx) [U.S.]
Chlorpheniramine
maleate 8 mg
Pseudoephedrine HCl
120 mg
  1 cap q 12 hr
  a, g
 
Chlorpheniramine
Maleate and
Pseudoephedrine HCl
Extended-release
Capsules (Rx)
[U.S.]
Chlorpheniramine
maleate 8 mg
Pseudoephedrine HCl
120 mg
  1 cap q 12 hr
  a, g
 
Chlor-Trimeton 4 Hour Relief Tablets (OTC)
[U.S.]
Chlorpheniramine
maleate 4 mg
Pseudoephedrine
sulfate 60 mg
Lactose
1 tab
q 4–6 hr
(max 4 tabs/
day)
6–12 yrs: 1/2 tab
q 4–6 hr
(max 2 tabs/
day)
c, g
 
Chlor-Trimeton 12 Hour Relief Extended-release
Tablets (OTC)
[U.S.]
Chlorpheniramine
maleate 8 mg
Pseudoephedrine
sulfate 120 mg
Lactose
1 tab
q 12 hr
(max 2 tabs/
day)
  c, g
 
Chlor-Trimeton Allergy-D 12 Hour {99} Extended-release
Tablets (OTC)
[U.S.]
Chlorpheniramine
maleate 8 mg
Pseudoephedrine
sulfate 120 mg
Lactose
1 tab
q 12 hr
(max 2 tabs/
day)
  c, g
 
Claritin-D 12 Hour Extended-release
Tablets (Rx)
[U.S.]
Loratadine
5 mg
Pseudoephedrine
sulfate 120 mg
  1 tab q 12 hr
(In renal function impairment
[creatinine clearance
<30 mL/min]:
1 tab q 24 hr {100})
  d
 
Claritin-D 24 Hour Extended-release
Tablets (Rx)
[U.S.]
Loratadine
10 mg
Pseudoephedrine
sulfate 240 mg
  1 tab q 24 hr
(In renal function impairment
[creatinine clearance
<30 mL/min]:
1 tab q 48 hr {100})
  d
 
Claritin Extra Extended-release
Tablets (OTC)
[Canada]
Loratadine
5 mg
Pseudoephedrine
sulfate 120 mg
  1 tab q 12 hr
  a
 
Colfed-A Extended-release
Capsules (Rx) [U.S.]
Chlorpheniramine
maleate 8 mg
Pseudoephedrine HCl
120 mg
  1 cap q 12 hr
  a, g
 
Comhist Tablets (Rx)
[U.S.]
Chlorpheniramine
maleate 2 mg,
Phenyltoloxamine
citrate 25 mg
Phenylephrine HCl
10 mg
Scored
1–2 tabs
q 8 hr
  a, g
 
CP Oral Oral Solution (Rx)
[U.S.]
Carbinoxamine
maleate 2 mg/mL
Pseudoephedrine HCl
25 mg/mL
  Intended for
pediatric use
1–3 mos: 1/4 mL,
3–6 mos: 1/2 mL,
6–9 mos: 3/4 mL,
9–18 mos: 1 mL,
q 6 hr
a, e
 
Dallergy Jr. Extended-release
Capsules (Rx) [U.S.]
Brompheniramine
maleate 6 mg
Pseudoephedrine HCl
60 mg
  2 caps q 12 hr
(max 2 doses/
day)
6–12 yrs:
1 cap q 12 hr
(max 2 doses/
day)
a, g
 
Deconamine Syrup (Rx)
[U.S.]
Chlorpheniramine
maleate 2 mg
Pseudoephedrine HCl
30 mg
Alcohol free
Dye free
5–10 mL
q 6–8 hr
2–6 yrs: 2.5 mL,
6–12 yrs:
2.5–5 mL,
q 6–8 hr
b, g
 
Tablets (Rx)
[U.S.]
Chlorpheniramine
maleate 4 mg
Pseudoephedrine HCl
60 mg
Dye free
Scored
1 tab q 6–8 hr
Not
recommended
See Deconamine Syrup and Chewable Tablets
b, g
 
Deconamine SR Extended-release
Capsules (Rx) [U.S.]
Chlorpheniramine
maleate 8 mg
Pseudoephedrine HCl
120 mg
  1 cap q 12 hr
Not
recommended
See Deconamine Syrup and Chewable Tablets
b, g
 
Deconomed SR Extended-release
Capsules (Rx) [U.S.]
Chlorpheniramine
maleate 8 mg
Pseudoephedrine HCl
120 mg
  1 cap q 12 hr
  a, f, g
 
Dexaphen SA Extended-release
Tablets (Rx)
[U.S.]
Dexbrompheniramine
maleate 6 mg
Pseudoephedrine
sulfate 120 mg
  1 tab q 12 hr
  a, g
 
Disobrom Extended-release
Tablets (Rx) [U.S.]
Dexbrompheniramine
maleate 6 mg
Pseudoephedrine
sulfate 120 mg
  1 tab q 12 hr
  a, g
 
Disophrol Chronotabs Extended-release
Tablets (OTC) [U.S.]
Dexbrompheniramine
maleate 6 mg
Pseudoephedrine
sulfate 120 mg
Sugar coated
1 tab q 12 hr
(max 2 tabs/
day)
  c, g
 
Drixomed Extended-release
Tablets (OTC)
[U.S.]
Dexbrompheniramine
maleate 6 mg
Pseudoephedrine
sulfate 120 mg
  1 tab
q 12 hr
(max 2 tabs/
day)
  c, f, g
 
Drixoral Extended-release
Tablets (OTC)
[Canada]
Dexbrompheniramine
maleate 6 mg
Pseudoephedrine
sulfate 120 mg
Sugar coated
1 tab
q 8–12 hr
  c, g
Drixoral Cold and Allergy Extended-release
Tablets (OTC)
[U.S.]
Dexbrompheniramine
maleate 6 mg
Pseudoephedrine
sulfate 120 mg
Lactose
1 tab q 12 hr
(max 2 tabs/
day)
  c, g
 
Drixoral Night Tablets (OTC)
[Canada]
Dexbrompheniramine
maleate 2 mg
Pseudoephedrine
sulfate 120 mg
Tartrazine free
Available in a
dual package
that also
contains
Drixoral N.D.
1 tab hs
  a, g
 
Drixtab Tablets (OTC)
[Canada]
Dexbrompheniramine
maleate 2 mg
Pseudoephedrine
sulfate 60 mg
Tartrazine free
1 tab q 6–8 hr
6–12 yrs: 1/2 tab
q 6–8 hr
a, g
 
Dura-Tap PD Extended-release
Capsules (Rx) [U.S.]
Chlorpheniramine
maleate 4 mg
Pseudoephedrine HCl
60 mg
  2 caps q 12 hr
6–12 yrs:
1 cap q 12 hr
b, g
 
Ed A-Hist Oral Solution (Rx)
[U.S.]
Chlorpheniramine
maleate 4 mg
Phenylephrine HCl
10 mg
Alcohol 5%
5 mL
q 6–8 hr
2–5 yrs:
1.25 mL,
6–12 yrs:
2.5 mL,
q 6–8 hr
a, f, g
Extended-release
Tablets (Rx) [U.S.]
Chlorpheniramine
maleate 8 mg
Phenylephrine HCl
20 mg
  1 tab q 12 hr
  a, g
 
Hayfebrol Oral Solution (OTC)
[U.S.]
Chlorpheniramine
maleate 2 mg
Pseudoephedrine HCl
30 mg
Alcohol free
Sugar free
Dye free
10 mL q 6 hr
2–6 yrs:
2.5 mL,
6–12 yrs:
5 mL,
q 6 hr
a, e, g
 
Histatab Plus Tablets (OTC)
[U.S.]
Chlorpheniramine
maleate 2 mg
Phenylephrine HCl
5 mg
  2 tabs initially,
then 1 tab
q 4 hr
  a, g
 
Iofed Extended-release
Capsules (Rx)
[U.S.]
Brompheniramine
maleate 12 mg
Pseudoephedrine HCl
120 mg
  1 cap
q 12 hr
  a, f, g
 
Iofed PD Extended-release
Capsules (Rx)
[U.S.]
Brompheniramine
maleate 6 mg
Pseudoephedrine HCl
60 mg
  1–2 caps
q 12 hr
6–12 yrs:
1 cap
q 12 hr
a, f, g
 
Kronofed-A Jr. Kronocaps Extended-release
Capsules (Rx) [U.S.]
Chlorpheniramine
maleate 4 mg
Pseudoephedrine HCl
60 mg
Dye free
1–2 caps
q 12 hr
6–12 yrs: 1 cap
q 12 hr
a, g
 
Kronofed-A Kronocaps Extended-release
Capsules (Rx)
[U.S.]
Chlorpheniramine
maleate 8 mg
Pseudoephedrine HCl
120 mg
Dye free
1 cap q 12 hr
  a, g
 
Lodrane LD Extended-release
Capsules (Rx)
[U.S.]
Brompheniramine
maleate 6 mg
Pseudoephedrine HCl 60 mg
Dye free
1–2 caps
q 12 hr
  a, g
Lodrane Liquid Oral Solution (Rx)
[U.S.]
Brompheniramine
maleate 4 mg
Pseudoephedrine HCl 60 mg
Dye free
Sugar free
Alcohol free
  2–6 yrs: 1.25 mL
6–12 yrs: 2.5 mL
³12 yrs: 5 mL
q 4–6 hr
b, e, g
 
Mooredec Extended-release
Tablets (Rx) [U.S.]
Carbinoxamine
maleate 8 mg
Pseudoephedrine HCl
120 mg
  1 tab q 12 hr
  a, g
 
Nalex-A Extended-release
Tablets (Rx) [U.S.]
Chlorpheniramine
maleate 4 mg,
Phenyltoloxamine
citrate 40 mg
Phenylephrine HCl
20 mg
Lactose
Scored
1/2–1 tab
q 8–12 hr
6–12 yrs:
1/2 tab
q 8–12 hr
a, f, g
ND Clear T.D. Extended-release
Capsules (Rx)
[U.S.]
Chlorpheniramine
maleate 8 mg
Pseudoephedrine
HCl 120 mg
Dye free
1 cap q 12 hr
  a, g
 
Neo Citran A for Oral Solution
(OTC) [Canada]
Pheniramine
maleate
20 mg/pouch
Phenylephrine HCl
10 mg/pouch
Vitamin C
50 mg/pouch
1 pouch
dissolved in
225 mL of
hot water
q 3–4 hr
  a, g
 
Novafed A Extended-release
Capsules (Rx) [U.S.]
Chlorpheniramine
maleate 8 mg
Pseudoephedrine HCl
120 mg
  1 cap q 12 hr
  b, g
 
PediaCare Cold Formula Oral Solution (OTC)
[U.S.]
Chlorpheniramine
maleate 1 mg
Pseudoephedrine HCl
15 mg
Alcohol free
Saccharin free
Intended for
pediatric use
6–11 yrs: 10 mL
q 4–6 hr
b, e, g
 
Poly Hist Forte Tablets (Rx)
[U.S.]
Chlorpheniramine
maleate 4 mg,
Pyrilamine maleate
25 mg
Phenylephrine HCl
10 mg,
HCl 50 mg
  1 tab q 8–12 hr
6–12 yrs: 1/2 tab
q 8–12 hr
b, f, g
 
Promethazine VC
Phenylephrine HCl
Syrup (Rx)
[U.S.]
Promethazine HCl
6.25 mg
Phenylephrine HCl
5 mg
Alcohol 7%
5 mL q 4–6 hr
2–6 yrs:
1.25–2.5 mL,
6–12 yrs:
2.5–5 mL,
q 4–6 hr
d, e, f, g
 
Promethazine VC Syrup (Rx)
[U.S.]
Promethazine HCl
6.25 mg
Phenylephrine HCl
5 mg
  5 mL q 4–6 hr
(max 20 mL/
day)
2–6 yrs:
1.25–2.5 mL,
6–12 yrs:
2.5–5 mL,
q 4–6 hr
d, e, f, g
Prometh VC Syrup (Rx)
[U.S.]
Promethazine HCl
6.25 mg
Phenylephrine HCl
5 mg
Alcohol 7%
5 mL q 4–6 hr
(max 20 mL/
day)
2–6 yrs:
1.25–2.5 mL,
6–12 yrs:
2.5–5 mL,
q 4–6 hr
d, e, f, g
 
Pseudo-Chlor Extended-release
Capsules (Rx)
[U.S.]
Chlorpheniramine
maleate 8 mg
Pseudoephedrine HCl
120 mg
  1 cap q 12 hr
  a, g
 
Rescon Extended-release
Capsules (Rx)
[U.S.]
Chlorpheniramine
maleate 12 mg
Pseudoephedrine HCl
120 mg
  1 cap q 12 hr
  a, g
 
Rescon-ED Extended-release
Capsules (Rx)
[U.S.]
Chlorpheniramine
maleate 8 mg
Pseudoephedrine HCl
120 mg
  1 cap q 12 hr
  a, g
 
Rescon JR Extended-release
Capsules (Rx) [U.S.]
Chlorpheniramine
maleate 4 mg
Pseudoephedrine HCl
60 mg
Dye free
Intended for
pediatric use
6–12 yrs:
1 cap q 12 hr
a, g
 
Respahist Extended-release
Capsules (Rx)
[U.S.]
Brompheniramine
maleate 6 mg
Pseudoephedrine HCl
60 mg
Dye free
1–2 caps
q 12 hr
6–12 yrs:
1 cap q 12 hr
a, f, g
 
Rhinosyn Oral Solution
(OTC) [U.S.]
Chlorpheniramine
maleate 4 mg
Pseudoephedrine HCl
60 mg
Alcohol 0.45%
5 mL
q 4 hr
  a, e, g
 
Rhinosyn-PD Oral Solution
(OTC) [U.S.]
Chlorpheniramine
maleate 2 mg
Pseudoephedrine HCl
30 mg
Alcohol 1.2%
10 mL
q 4 hr
  a, e, g
 
Rinade B.I.D. Extended-release
Capsules (Rx)
[U.S.]
Chlorpheniramine
maleate 8 mg
Pseudoephedrine HCl
120 mg
Dye free
1 cap q 12 hr
  a, g
 
Tablets (Rx)
[U.S.]
Carbinoxamine
maleate 4 mg
Pseudoephedrine HCl
60 mg
  1 tab q 6 hr
6–12 yrs: 1 tab
q 6 hr
a, g
 
Extended-release
Tablets (Rx)
[U.S.]
Carbinoxamine
maleate 8 mg
Pseudoephedrine HCl
120 mg
  1 tab q 12 hr
  a, g
 
Rondec Syrup (Rx)
[U.S.]
Carbinoxamine
maleate 4 mg
Pseudoephedrine HCl
60 mg
Alcohol free
Sugar Free
5 mL q 6 hr
18 mos–6 yrs:
2.5 mL,
6–12 yrs: 5 mL,
q 6 hr
a, e, g
 
Tablets (Rx)
[U.S.]
Carbinoxamine
maleate 4 mg
Pseudoephedrine HCl
60 mg
Film coated
1 tab q 6 hr
6–12 yrs: 1 tab
q 6 hr
a, g
 
Rondec Chewable {98} Chewable Tablets (Rx)
[U.S.]
{98}
Brompheniramine maleate 4 mg
Pseudoephedrine HCl 60 mg
Aspartame
1 tab q 4 hr (max 6 tabs/day)
6-12 yrs: 1/2 tab q 4 hr (max 6 doses [3 tabs]/day)
a, g, j
 
Rondec Drops Oral Solution (Rx)
[U.S.]
Carbinoxamine
maleate 2 mg/mL
Pseudoephedrine HCl
25 mg/mL
Alcohol free
Intended for
pediatric use
1–3 mos: 1/4 mL,
3–6 mos: 1/2 mL,
6–9 mos: 3/4 mL,
9–18 mos: 1 mL,
q 6 hr
a, e, g
 
Rondec-TR Extended-release
Tablets (Rx)
[U.S.]
Carbinoxamine
maleate 8 mg
Pseudoephedrine HCl
120 mg
Film coated
1 tab q 12 hr
  a, g
 
R-Tannamine Tablets (Rx)
[U.S.]
Chlorpheniramine
tannate 8 mg,
Pyrilamine tannate
25 mg
Phenylephrine
tannate 25 mg
  1–2 tabs
q 12 hr
  a, g
 
R-Tannamine Pediatric Oral Suspension
(Rx) [U.S.]
Chlorpheniramine
tannate 2 mg,
Pyrilamine tannate
12.5 mg
Phenylephrine
tannate 5 mg
  Intended for
pediatric use
2–6 yrs:
2.5–5 mL,
6–12 yrs:
5–10 mL,
q 12 hr
a, e, g, i
 
R-Tannate Tablets (Rx)
[U.S.]
Chlorpheniramine
tannate 8 mg,
Pyrilamine tannate
25 mg
Phenylephrine
tannate 25 mg
  1–2 tabs
q 12 hr
  a, g
Semprex-D Capsules (Rx)
[U.S.]
Acrivastine
8 mg
Pseudoephedrine HCl
60 mg
  1 cap
q 4–6 hr
(max 4 caps/
day)
  a, f, g
 
Silafed Syrup (OTC)
[U.S.]
Triprolidine HCl
1.25 mg
Pseudoephedrine HCl
30 mg
  10 mL
q 4–6 hr
(max 40 mL/
day)
6–12 yrs:
5 mL
q 4–6 hr
(max 20 mL/
day)
b, f, g
 
Tanafed Oral Suspension
(Rx) [U.S.]
Chlorpheniramine
tannate 4.5 mg
Pseudoephedrine
tannate 75 mg
  10–20 mL
q 12 hr
2–6 yrs:
2.5–5 mL
(max 10 mL/
day),
6–12 yrs:
5–10 mL
(max 20 mL/
day),
q 12 hr
b, e, f, g, i
 
Trinalin Repetabs Extended-release
Tablets (Rx)
[U.S./Canada]
Azatadine maleate
1 mg
Pseudoephedrine
sulfate 120 mg
Sugar coated
1 tab q 12 hr
Not
recommended
c, g
 
Triotann Tablets (Rx)
[U.S.]
Chlorpheniramine
tannate 8 mg,
Pyrilamine tannate
25 mg
Phenylephrine
tannate 25 mg
  1–2 tabs
q 12 hr
  a, g
 
Triotann Pediatric Oral Suspension
(Rx) [U.S.]
Chlorpheniramine
tannate 2 mg,
Pyrilamine tannate
12.5 mg
Phenylephrine
tannate 5 mg
  Intended for
pediatric use
2–6 yrs:
2.5–5 mL,
6–12 yrs:
5–10 mL,
q 12 hr
a, e, g, i
 
Triotann-S Pediatric Oral Suspension
(Rx) [U.S.]
Chlorpheniramine
tannate 2 mg,
Pyrilamine tannate
12.5 mg
Phenylephrine
tannate 5 mg
  Intended for
pediatric use
2–6 yrs:
2.5–5 mL,
6–12 yrs:
5–10 mL,
q 12 hr
a, e, g, i
 
Triprolidine HCl and
Pseudoephedrine HCl
Syrup USP
(Rx) (OTC) [U.S.]
Triprolidine HCl
1.25 mg
Pseudoephedrine HCl
30 mg
  10 mL
q 4–6 hr
(max 40 mL/
day)
6–12 yrs: 5 mL
q 4–6 hr
b, e, f, g
 
Tablets USP
(Rx) (OTC) [U.S.]
Triprolidine HCl
2.5 mg
Pseudoephedrine HCl
60 mg
  1 tab q 4–6 hr
6–12 yrs:
1/2 tab q 4–6 hr
b, f, g
 
Tri-Tannate Tablets (Rx)
[U.S.]
Chlorpheniramine
tannate 8 mg,
Pyrilamine
tannate 25 mg
Phenylephrine
tannate 25 mg
  1–2 tabs
q 12 hr
  a, g
 
ULTRAbrom Extended-release
Capsules (Rx)
[U.S.]
Brompheniramine
maleate 12 mg
Pseudoephedrine HCl
120 mg
  1 cap q 12 hr
  a, g
 
ULTRAbrom PD Extended-release
Capsules (Rx)
[U.S.]
Brompheniramine
maleate
6 mg
Pseudoephedrine HCl
60 mg
  1–2 caps
q 12 hr
6–12 yrs:
1 cap q 12 hr
a, g
 
Vasofrinic Oral Solution (OTC)
[Canada]
Chlorpheniramine
maleate 2 mg
Pseudoephedrine HCl
30 mg
  5–10 mL
q 6–8 hr
2–6 yrs:
2.5 mL,
6–12 yrs:
5 mL,
q 6–8 hr
b, e, g
 
Zyrtec-D 12 Hour Extended-release
Tablets (Rx)
[U.S.]
Cetirizine hydrochloride, 5 mg,
Pseudoephedrine hydrochloride, 120 mg
Lactose
Adults and Children 12 years and older:
1 tablet twice daily
  b
 
{105} *  Geriatric patients may be more sensitive to the effects of the usual adult dose.
 For appropriate Packaging and storage and Auxiliary labeling information refer to designated letters as follows:

• a—Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), in a tight container, unless otherwise specified by manufacturer.


• b—Store between 15 and 30 °C (59 and 86 °F), in a tight container, unless otherwise specified by manufacturer.


• c—Store between 2 and 30 °C (36 and 86 °F), in a tight container, unless otherwise specified by manufacturer.


• d—Store below 25 °C (77 °F), in a tight container, unless otherwise specified by manufacturer.


• e—Protect from freezing.


• f—Protect from light.


• g—Auxiliary labeling:    • May cause drowsiness.
   • Avoid alcoholic beverages.



• h—Auxiliary labeling: o May be chewed.


• i—Auxiliary labeling: o Shake well.


• j—Color may change over time from pink to peach. This does not reflect any change in quality or potency of tablets. {98}





Strength(s) usually available
U.S.—
See above table.



Revised: 08/29/2002



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