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Pronunciation |
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(AK
ri vas teen & soo doe e FED
rin) |
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U.S. Brand
Names |
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Semprex®-D |
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Generic
Available |
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No |
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Synonyms |
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Pseudoephedrine and Acrivastine |
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Pharmacological Index |
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Antihistamine |
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Use |
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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 |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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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) |
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Warnings/Precautions |
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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 |
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Adverse
Reactions |
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>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 |
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Overdosage/Toxicology |
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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. |
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Drug
Interactions |
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Decreased effect of guanethidine, reserpine, methyldopa, and beta-blockers
Increased toxicity with MAO inhibitors (hypertensive crisis),
sympathomimetics, CNS depressants, alcohol (sedation) |
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Mechanism of
Action |
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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 |
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Pharmacodynamics/Kinetics |
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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) |
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Usual Dosage |
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Adults: 1 capsule 3-4 times/day |
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Mental Health: Effects
on Mental Status |
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Drowsiness is common; may produce anxiety and insomnia |
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Mental Health:
Effects on Psychiatric
Treatment |
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Hypertensive crisis may result with MAOI; effects of CNS depressants may be
lessened |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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Use with caution since pseudoephedrine is a sympathomimetic amine which could
interact with epinephrine to cause a pressor response |
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Dental Health:
Effects on Dental Treatment |
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Up to 10% of patients could experience tachycardia, palpitations, and dry
mouth; use vasoconstrictor with caution |
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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 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. |
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Dosage Forms |
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Capsule: Acrivastine 8 mg and pseudoephedrine hydrochloride 60
mg |
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References |
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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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