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Tripelennamine
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(tri pel EN a meen)

U.S. Brand Names
PBZ®; PBZ-SR®

Generic Available

Yes


Synonyms
Tripelennamine Citrate; Tripelennamine Hydrochloride

Pharmacological Index

Antihistamine


Use

Perennial and seasonal allergic rhinitis and other allergic symptoms including urticaria


Pregnancy Risk Factor

B


Contraindications

Hypersensitivity to tripelennamine or any component


Warnings/Precautions

Use with caution in patients with narrow-angle glaucoma, bladder neck obstruction, symptomatic prostate hypertrophy, asthmatic attacks, and stenosing peptic ulcer


Adverse Reactions

>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


Overdosage/Toxicology

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.


Drug Interactions

Increased effect/toxicity with alcohol, CNS depressants, MAO inhibitors


Mechanism of Action

Competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract


Pharmacodynamics/Kinetics

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


Usual Dosage

Oral:

Adults: 25-50 mg every 4-6 hours, extended release tablets 100 mg morning and evening up to 100 mg every 8 hours


Dietary Considerations

Alcohol: Additive CNS effect, avoid use


Mental Health: Effects on Mental Status

Drowsiness is common; may cause nervousness or dizziness; may rarely cause insomnia, depression, or paradoxical excitement


Mental Health: Effects on Psychiatric Treatment

Concurrent use with psychotropics may produce additive sedation


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

Chronic use of antihistamines will inhibit salivary flow, particularly in elderly patients; this may contribute to periodontal disease and oral discomfort


Patient Information

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.


Nursing Implications

Raise bed rails, institute safety measures, assist with ambulation


Dosage Forms

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


References

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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