General Articles

Acrivastine and pseudoephedrine

U.S. BRAND NAMES — Semprex®-D

PHARMACOLOGIC CATEGORY
Alpha/Beta Agonist
Histamine H1 Antagonist
Histamine H1 Antagonist, Second Generation

DOSING: ADULTS — Rhinitis, nasal congestion, allergic symptoms: Oral: 1 capsule 3-4 times/day

DOSING: ELDERLY — Refer to adult dosing.

DOSING: RENAL IMPAIRMENT — Do not use.

DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule:
Semprex®-D: Acrivastine 8 mg and pseudoephedrine hydrochloride 60 mg

DOSAGE FORMS: CONCISE
Capsule:
Semprex®-D: Acrivastine 8 mg and pseudoephedrine 60 mg

GENERIC EQUIVALENT AVAILABLE — No

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

ADVERSE REACTIONS SIGNIFICANT
>10%: Central nervous system: Drowsiness, headache

1% to 10%:
Cardiovascular: Tachycardia, palpitation
Central nervous system: Nervousness, dizziness, insomnia, vertigo, lightheadedness, fatigue
Gastrointestinal: Nausea, vomiting, xerostomia, diarrhea
Genitourinary: Dysuria
Neuromuscular & skeletal: Weakness
Respiratory: Pharyngitis, cough increased
Miscellaneous: Diaphoresis

CONTRAINDICATIONS — Hypersensitivity to pseudoephedrine, acrivastine (or other alkylamine antihistamines), or any component of the formulation; MAO inhibitor therapy within 14 days of initiating therapy; severe hypertension, severe coronary artery disease; renal impairment (Clcr ≤ 48 mL/minute)

WARNINGS / PRECAUTIONS
Concerns related to adverse effects: CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).

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Disease-related concerns: Cardiovascular disease: Use with caution in patients with cardiovascular disease (including hypertension and ischemic heart disease); contraindicated with severe disease. Diabetes: Use with caution in patients with diabetes mellitus. Increased intraocular pressure/glaucoma: Use with caution in patients with increased intraocular pressure or glaucoma. Prostatic hyperplasia/urinary obstruction: Use with caution in patients with prostatic hyperplasia and/or GU obstruction. Pyloroduodenal obstruction: Use with caution in patients with pyloroduodenal obstruction (including stenotic peptic ulcer). Renal impairment: Use with caution in patients with renal impairment; contraindicated if Clcr ≤ 48 mL/minute. Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.

Concurrent drug therapy issues: Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.

Special populations: Elderly: Use with caution in the elderly; may be more sensitive to adverse effects. Pediatrics: Safety and efficacy have not been established in children <12 years of age. DRUG INTERACTIONS
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy

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Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy

Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy

Antacids: May decrease the excretion of Alpha-/Beta-Agonists. Exceptions: Aluminum Hydroxide. Risk C: Monitor therapy

Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Paliperidone. Risk C: Monitor therapy

Atomoxetine: May enhance the hypertensive effect of Sympathomimetics. Atomoxetine may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy

Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy

Bromocriptine: Alpha-/Beta-Agonists may enhance the adverse/toxic effect of Bromocriptine. Including increased blood pressure, ventricular arrhythmias, and seizure. Risk C: Monitor therapy

Cannabinoids: May enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy

Carbonic Anhydrase Inhibitors: May decrease the excretion of Alpha-/Beta-Agonists. Exceptions: Brinzolamide; Dorzolamide. Risk C: Monitor therapy

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy

Iobenguane I 123: Sympathomimetics may diminish the therapeutic effect of Iobenguane I 123. Risk X: Avoid combination

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MAO Inhibitors: May enhance the hypertensive effect of Alpha-/Beta-Agonists (Indirect-Acting). Risk X: Avoid combination

Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification

Serotonin/Norepinephrine Reuptake Inhibitors: May enhance the tachycardic effect of Alpha-/Beta-Agonists. Serotonin/Norepinephrine Reuptake Inhibitors may enhance the vasopressor effect of Alpha-/Beta-Agonists. Risk D: Consider therapy modification

Spironolactone: May diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Risk C: Monitor therapy

Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Risk C: Monitor therapy

ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Avoid ethanol (may increase sedation)

PREGNANCY RISK FACTOR — B (show table)

LACTATION — Enters breast milk/contraindicated

PRICING — (data from drugstore.com)
Capsules (Semprex-D)
8-60 mg (30): $62.39

INTERNATIONAL BRAND NAMES — Duact (DK, FI)

MECHANISM OF ACTION — Refer to Pseudoephedrine; 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
Pseudoephedrine: See Pseudoephedrine.

Acrivastine:
Metabolism: Minimally hepatic
Time to peak: ~1.1 hours
Excretion: Urine (84%); feces (13%)