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Acrivastine and Pseudoephedrine
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
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
Dosage Forms
References

Pronunciation
(AK ri vas teen & soo doe e FED rin)

U.S. Brand Names
Semprex®-D

Generic Available

No


Synonyms
Pseudoephedrine and Acrivastine

Pharmacological Index

Antihistamine


Use

Temporary relief of nasal congestion, decongest sinus openings, running nose, itching of nose or throat, and itchy, watery eyes due to hay fever or other upper respiratory allergies


Pregnancy Risk Factor

B


Contraindications

MAO inhibitor therapy within 14 days of initiating therapy, severe hypertension, severe coronary artery disease, hypersensitivity to pseudoephedrine, acrivastine (or other alkylamine antihistamines), or any component, renal impairment (Clcr <48 mL/minute)


Warnings/Precautions

Use with caution in patients >60 years of age; use with caution in patients with high blood pressure, ischemic heart disease, diabetes, increased intraocular pressure, GI or GU obstruction, asthma, thyroid disease, or prostatic hypertrophy; not recommended for use in children


Adverse Reactions

>10%: Central nervous system: Drowsiness, headache

1% to 10%:

Cardiovascular: Tachycardia, palpitations

Central nervous system: Nervousness, dizziness, insomnia, vertigo, lightheadedness, fatigue

Gastrointestinal: Nausea, vomiting, xerostomia, diarrhea

Genitourinary: Dysuria

Neuromuscular & skeletal: Weakness

Respiratory: Pharyngitis, cough increase

Miscellaneous: Diaphoresis

<1%: Dysmenorrhea, dyspepsia


Overdosage/Toxicology

Symptoms of overdose include trembling, tachycardia, stridor, loss of consciousness, and possible convulsions

There is no specific antidote for pseudoephedrine intoxication, and the bulk of the treatment is supportive. Hyperactivity and agitation usually respond to reduced sensory input, however, with extreme agitation haloperidol (2-5 mg I.M. for adults) may be required.

Hyperthermia is best treated with external cooling measures, or when severe or unresponsive, muscle paralysis with pancuronium may be needed. Hypertension is usually transient and generally does not require treatment unless severe. For diastolic blood pressure >110 mm Hg, a nitroprusside infusion should be initiated. Seizures usually respond to diazepam I.V. and/or phenytoin maintenance regimens.


Drug Interactions

Decreased effect of guanethidine, reserpine, methyldopa, and beta-blockers

Increased toxicity with MAO inhibitors (hypertensive crisis), sympathomimetics, CNS depressants, alcohol (sedation)


Mechanism of Action

Refer to Pseudoephedrine monograph; acrivastine is an analogue of triprolidine and it is considered to be relatively less sedating than traditional antihistamines; believed to involve competitive blockade of H1-receptor sites resulting in the inability of histamine to combine with its receptor sites and exert its usual effects on target cells


Pharmacodynamics/Kinetics

Onset of action: Within 30 minutes

Duration: 12 hours

Absorption: Not affected by food

Protein binding: 50%

Metabolism: Hepatic to an active metabolite

Half-life: 1.4-2.5 hours

Elimination: Renal (65% eliminated unchanged)


Usual Dosage

Adults: 1 capsule 3-4 times/day


Mental Health: Effects on Mental Status

Drowsiness is common; may produce anxiety and insomnia


Mental Health: Effects on Psychiatric Treatment

Hypertensive crisis may result with MAOI; effects of CNS depressants may be lessened


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

Use with caution since pseudoephedrine is a sympathomimetic amine which could interact with epinephrine to cause a pressor response


Dental Health: Effects on Dental Treatment

Up to 10% of patients could experience tachycardia, palpitations, and dry mouth; use vasoconstrictor with caution


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 hazardous activity until response to drug is known); or dry mouth, nausea or vomiting (frequent small meals, frequent mouth care, chewing gum, or sucking lozenges may help). Report persistent dizziness, sedation, or agitation; chest pain, rapid heartbeat, or palpitations; difficulty breathing or increased cough; changes in urinary pattern; muscle weakness; or lack of improvement or worsening or condition. Breast-feeding precautions: Do not breast-feed.


Dosage Forms

Capsule: Acrivastine 8 mg and pseudoephedrine hydrochloride 60 mg


References

Brogden RN and McTavish D, "Acrivastine: A Review of Its Pharmacological Properties and Therapeutic Efficacy in Allergic Rhinitis, Urticaria, and Related Disorders," Drugs, 1991, 41(6):927-40.

Levien TL and Baker DE, "Reviews of Acrivastine and Midotrine," Hosp Pharm, 1995, 30(3):229-35.


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