A1,
A2,
B,
C1,
C2,
D,
E,
F,
G-H,
I-K,
L,
M,
N,
O,
P1,
P2,
Q-R,
S,
T,
U-V,
W-Z
Zyrtec Side Effects, and Drug Interactions - Cetirizine
Zyrtec Side Effects, and Drug Interactions - Cetirizine
SIDE EFFECTS
Controlled and uncontrolled clinical
trials conducted in the United States and Canada included more than 6000
patients aged 12 years and older,
with more than 3900 receiving cetirizine at doses of 5 to 20 mg
per day. The duration
of treatment ranged from
1 week to 6 months, with a mean
exposure of 30 days.
Most adverse reactions reported during therapy with cetirizine were mild
or moderate. In placebo-controlled
trials, the incidence of
discontinuations due to adverse reactions in patients receiving cetirizine
5 or 10 mg was not significantly
different from placebo (2.9%
vs. 2.4%, respectively).
The most common adverse reaction
in patients aged 12 years and
older that occurred more frequently on cetirizine than placebo
was somnolence. The incidence
of somnolence associated
with cetirizine was dose related,
6% in placebo, 11% at 5 mg and
14% at 10 mg. Discontinuations due to somnolence for cetirizine were uncommon
(1.0% on cetirizine vs. 0.6% on placebo). Fatigue and dry mouth
also appeared to be treatment-related adverse reactions. There were no
differences by age, race, gender
or by body weight with regard
to the incidence of adverse
reactions.
TABLE 1 lists adverse experiences in patients aged
12 years and older which were reported for cetirizine 5 and 10 mg
in controlled clinical trials
in the United States and that were more common with cetirizine than placebo.
| TABLE 1 Adverse Experiences Reported
in Patients Aged 12 Years and Older in Placebo-Controlled United
States Cetirizine Trials (Maximum Dose of 10 mg) at Rates of 2%
or Greater (Percent Incidence) |
| Adverse Experience |
Cetirizine (N=2034) |
Placebo (N=1612) |
| Somnolence |
13.7 |
6.3 |
| Fatigue |
5.9 |
2.6 |
| Dry Mouth |
5.0 |
2.3 |
| Pharyngitis |
2.0 |
1.9 |
| Dizziness |
2.0 |
1.2 |
In addition, headache and
nausea occurred in more than
2% of the patients, but were more common in placebo
patients.
Pediatric studies were also conducted with
cetirizine. More than 1300 pediatric patients aged 6 to 11 years with more
than 900 treated with cetirizine at doses of 1.25 to 10 mg per day were
included in controlled and uncontrolled clinical trials conducted in the
United States. The duration of treatment ranged from 2 to 12
weeks. Placebo-controlled trials up to
4 weeks duration included 168 pediatric patients aged 2 to 5 years who received
cetirizine, the majority
of whom received single daily doses of 5 mg. A
placebo-controlled trial 18 months in duration
included 399 patients aged 12 to 24 months treated with cetirizine (0.25
mg/kg bid), and another placebo-controlled trial
of 7 days duration included 42 patients
aged 6 to 11 months who were treated with cetirizine
(0.25 mg/kg bid).
The majority of adverse reactions reported in pediatric
patients aged 2 to 11 years with cetirizine were mild or moderate. In
placebo-controlled trials, the incidence
of discontinuations due to adverse reactions in pediatric patients receiving
up to 10 mg of cetirizine was uncommon
(0.4% on cetirizine vs. 1.0% on placebo).
TABLE 2 lists adverse experiences which were reported for cetirizine
5 and 10 mg in pediatric
patients aged 6 to 11 years in
placebo-controlled clinical trials in the United States and were more
common with cetirizine than placebo. Of these, abdominal
pain was considered treatment-related
and somnolence appeared
to be dose-related, 1.3% in placebo, 1.9% at 5 mg and 4.2% at 10 mg. The
adverse experiences reported in pediatric
patients aged 2 to 5 years in placebo-controlled trials were qualitatively
similar in nature and generally similar in frequency to those reported
in trials with children aged
6 to 11 years.
In the placebo-controlled trials of pediatric
patients 6 to 24 months of age, the incidences of adverse experiences,
were similar in the cetirizine and placebo treatment groups in each study.
Somnolence occurred with essentially the same frequency in patients who received cetirizine and patients
who received placebo. In a study
of 1 week duration in children 6-11
months of age, patients who received cetirizine exhibited greater irritability/fussiness
than patients on placebo. In a study of
18 months duration in
patients 12 months
and older, insomnia occurred more frequently in patients who received cetirizine compared to patients who received
placebo (9.0% v. 5.3%). In
those patients who received 5 mg or more per day of
cetirizine as compared to patients who received placebo, fatigue (3.6% v.
1.3%) and malaise (3.6% v.
1.8%) occurred more frequently.
| TABLE 2 Adverse Experiences Reported in Pediatric
Patients Aged 6 to 11 Years in Placebo-Controlled United States
Cetirizine Trials (5 or 10 mg
Dose) Which Occurred at a Frequency of ³2%
in Either the 5-mg or the 10-mg Cetirizine Group, and More Frequently
Than in the Placebo Group |
| |
|
Cetirizine |
| Adverse Experiences |
Placebo (N=309) |
5 mg (N=161) |
10 mg (N=215) |
| Headache |
12.3% |
11.0% |
14.0% |
| Pharyngitis |
2.9% |
6.2% |
2.8% |
| Abdominal Pain |
1.9% |
4.4% |
5.6% |
| Coughing |
3.9% |
4.4% |
2.8% |
| Somnolence |
1.3% |
1.9% |
4.2% |
| Diarrhea |
1.3% |
3.1% |
1.9% |
| Epistaxis |
2.9% |
3.7% |
1.9% |
| Bronchospasm |
1.9% |
3.1% |
1.9% |
| Nausea |
1.9% |
1.9% |
2.8% |
| Vomiting |
1.0% |
2.5% |
2.3% |
The following events were observed infrequently (less than 2%), in either
3982 adults and children 12 years and older or in 659 pediatric
patients aged 6 to 11 years who received cetirizine in U.S. trials, including
an open adult study of six months
duration. A causal relationship of these infrequent events with cetirizine
administration has
not been established.
Autonomic Nervous System: Anorexia, flushing, increased
salivation, urinary retention.
Cardiovascular: Cardiac failure, hypertension, palpitation,
tachycardia.
Central and Peripheral Nervous Systems: Abnormal coordination,
ataxia, confusion, dysphonia, hyperesthesia, hyperkinesia, hypertonia,
hypoesthesia, leg cramps, migraine,
myelitis, paralysis, paresthesia, ptosis, syncope, tremor, twitching,
vertigo, visual field
defect.
Gastrointestinal: Abnormal hepatic
function, aggravated tooth caries, constipation, dyspepsia, eructation,
flatulence, gastritis, hemorrhoids, increased appetite, melena, rectal
hemorrhage, stomatitis including ulcerative
stomatitis, tongue discoloration,
tongue edema.
Genitourinary: Cystitis, dysuria, hematuria, micturition
frequency, polyuria, urinary incontinence, urinary tract
infection.
Hearing and Vestibular: Deafness, earache, ototoxicity,
tinnitus.
Metabolic/Nutritional: Dehydration, diabetes
mellitus, thirst.
Musculoskeletal: Arthralgia, arthritis, arthrosis, muscle
weakness, myalgia.
Psychiatric: Abnormal thinking, agitation, amnesia, anxiety,
decreased libido, depersonalization, depression, emotional lability, euphoria,
impaired concentration, insomnia, nervousness, paroniria, sleep
disorder.
Respiratory System: Bronchitis, dyspnea, hyperventilation,
increased sputum, pneumonia, respiratory disorder, rhinitis, sinusitis,
upper respiratory tract infection.
Reproductive: Dysmenorrhea, female
breast pain, intermenstrual
bleeding, leukorrhea, menorrhagia, vaginitis.
Reticuloendothelial: Lymphadenopathy.
Skin: Acne, alopecia, angioedema, bullous
eruption, dermatitis, dry skin, eczema, erythematous rash, furunculosis,
hyperkeratosis, hypertrichosis, increased sweating, maculopapular
rash, photosensitivity reaction, photosensitivity toxic reaction, pruritus,
purpura, rash, seborrhea, skin
disorder, skin nodule, urticaria.
Special Senses: Parosmia, taste
loss, taste perversion.
Vision: Blindness, conjunctivitis, eye
pain, glaucoma, loss of accommodation, ocular
hemorrhage, xerophthalmia.
Body as a Whole: Accidental injury, asthenia, back
pain, chest pain, enlarged abdomen, face
edema, fever, generalized edema, hot flashes, increased weight, leg
edema, malaise, nasal polyp,
pain, pallor, periorbital edema, peripheral
edema, rigors.
Occasional instances of transient, reversible
hepatic transaminase
elevations have occurred during cetirizine therapy. Hepatitis with significant
transaminase elevation and elevated bilirubin
in association with the
use of cetirizine HCl has been reported.
Post-Marketing Experience
In the
post-marketing period, the following additional rare, but potentially severe
adverse events have been reported: aggressive reaction, anaphylaxis, cholestasis, convulsions,
glomerulonephritis, hallucinations, hemolytic anemia, hepatitis, orofacial
dyskinesia, severe hypotension,
stillbirth, suicidal ideation, suicide and thrombocytopenia.
DRUG ABUSE AND DEPENDENCE
There is no information to indicate that abuse
or dependency occurs with cetirizine.
DRUG INTERACTIONS
Pharmacokinetic interaction studies with cetirizine in adults were conducted
with pseudoephedrine, antipyrine, ketoconazole, erythromycin
and azithromycin. No interactions were observed. In
a multiple dose
study of theophylline (400 mg once
daily for 3 days) and cetirizine (20 mg
once daily for 3 days), a 16% decrease in the clearance
of cetirizine was observed. The disposition of theophylline
was not altered by concomitant
cetirizine administration.
Drug-Drug Interactions: No clinically significant
drug interactions have been found with theophylline
at a low dose, azithromycin, pseudoephedrine, ketoconazole, or erythromycin.
There was a small decrease in the clearance
of cetirizine caused by a 400-mg dose
of theophylline; it is possible that larger theophylline
doses could have a greater effect.
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