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Pronunciation |
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(tri
pel EN a
meen) |
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U.S. Brand
Names |
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PBZ®; PBZ-SR® |
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Generic
Available |
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Yes |
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Synonyms |
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Tripelennamine Citrate; Tripelennamine Hydrochloride |
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Pharmacological Index |
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Antihistamine |
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Use |
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Perennial and seasonal allergic rhinitis and other allergic symptoms
including urticaria |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to tripelennamine or any component |
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Warnings/Precautions |
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Use with caution in patients with narrow-angle glaucoma, bladder neck
obstruction, symptomatic prostate hypertrophy, asthmatic attacks, and stenosing
peptic ulcer |
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Adverse
Reactions |
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>10%:
Central nervous system: Slight to moderate drowsiness
Respiratory: Thickening of bronchial secretions
1% to 10%:
Central nervous system: Headache, fatigue, nervousness, dizziness
Gastrointestinal: Appetite increase, weight gain, nausea, diarrhea, abdominal
pain, xerostomia
Neuromuscular & skeletal: Arthralgia
Respiratory: Pharyngitis
<1%: Edema, palpitations, hypotension, depression, sedation, paradoxical
excitement, insomnia, angioedema, photosensitivity, rash, urinary retention,
hepatitis, myalgia, paresthesia, tremor, blurred vision, bronchospasm, epistaxis
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Overdosage/Toxicology |
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Symptoms of overdose include CNS stimulation or depression; flushed skin,
mydriasis, ataxia, athetosis, dry mouth
There is no specific treatment for an antihistamine overdose, however, most
of its clinical toxicity is due to anticholinergic effects. For anticholinergic
overdose with severe life-threatening symptoms, physostigmine 1-2 mg (0.5 mg or
0.02 mg/kg for children) I.V., slowly may be given to reverse these effects.
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Drug
Interactions |
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Increased effect/toxicity with alcohol, CNS depressants, MAO
inhibitors |
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Mechanism of
Action |
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Competes with histamine for H1-receptor sites on effector cells in
the gastrointestinal tract, blood vessels, and respiratory
tract |
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Pharmacodynamics/Kinetics |
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Onset of antihistaminic effect: Within 15-30 minutes
Duration: 4-6 hours (up to 8 hours with PBZ-SR®)
Metabolism: Almost completely in the liver
Elimination: In urine |
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Usual Dosage |
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Oral:
Adults: 25-50 mg every 4-6 hours, extended release tablets 100 mg morning and
evening up to 100 mg every 8 hours |
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Dietary
Considerations |
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Alcohol: Additive CNS effect, avoid use |
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Mental Health: Effects
on Mental Status |
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Drowsiness is common; may cause nervousness or dizziness; may rarely cause
insomnia, depression, or paradoxical excitement |
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Mental Health:
Effects on Psychiatric
Treatment |
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Concurrent use with psychotropics may produce additive
sedation |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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Chronic use of antihistamines will inhibit salivary flow, particularly in
elderly patients; this may contribute to periodontal disease and oral
discomfort |
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Patient
Information |
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Take as directed; do not exceed recommended dose. Avoid use of other
depressants, alcohol, or sleep-inducing medications unless approved by
prescriber. You may experience drowsiness or dizziness (use caution when driving
or engaging in tasks requiring alertness until response to drug is known); or
dry mouth, nausea, or abdominal discomfort (frequent small meals, frequent mouth
care, chewing gum, or sucking hard candy may help). Report persistent dizziness,
sedation, or agitation; chest pain, rapid heartbeat, or palpitations; difficulty
breathing; changes in urinary pattern; yellowing of skin or eyes; dark urine or
pale stool; or lack of improvement or worsening or condition. Breast-feeding
precautions: Do not breast-feed. |
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Nursing
Implications |
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Raise bed rails, institute safety measures, assist with
ambulation |
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Dosage Forms |
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Elixir, as citrate: 37.5 mg/5 mL [equivalent to 25 mg hydrochloride] (473 mL)
Tablet, as hydrochloride: 25 mg, 50 mg
Tablet, extended release, as hydrochloride: 100 mg |
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References |
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Monforte JR, Gault R, Smialek J, et al,
"Toxicological and Pathological Findings in Fatalities Involving Pentazocine and Tripelennamine,"
J Forensic Sci, 1983, 28(1):90-101.
Yeh SY, Todd GD, Johnson RE, et al,
"The Pharmacokinetics of Pentazocine and Tripelennamine," Clin Pharmacol
Ther, 1986, 39(6):669-76. |
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