Acrivastine And Pseudoephedrine
Acrivastine And Pseudoephedrine Uses, Dosage, Side Effects, Food Interaction and all others data.
Acrivastine is a triprolidine analog antihistamine indicated for the treatment of allergies and hay fever. As an H1 receptor antagonist, it functions by blocking the action of histamine at this receptor thereby preventing the symptoms associated with histamine release such as pruritis, vasodilation, hypotension, edema, bronchoconstriction, and tachycardia.
Acrivastine is currently available in combination with pseudoephedrine as the FDA-approved product Semprex-D.
Pseudoephedrine is structurally related to ephedrine but exerts a weaker effect on the sympathetic nervous system. Both drugs naturally occur in in ephedra plant which have a history of use in traditional Eastern medicine and were first researched in the west in 1889. The decongestant effect of pseudoephedrine was described in dogs in 1927.
Pseudoephedrine causes vasoconstriction which leads to a decongestant effect. It has a short duration of action unless formulated as an extended release product. Patients should be counselled regarding the risk of central nervous system stimulation.
| Trade Name | Acrivastine And Pseudoephedrine |
| Generic | Acrivastine + pseudoephedrine |
| Weight | 8mg + 60mg |
| Type | Oral capsule |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Acrivastine is an antihistamine agent used for the symptomatic relief of seasonal allergic rhinitis such as sneezing, rhinorrhea, pruritus, lacrimation, and nasal congestion.
For the relief of symptoms associated with seasonal allergic rhinitis such as sneezing, rhinorrhea, pruritus, lacrimation, and nasal congestion.
Pseudoephedrine is an alpha and beta adrenergic agonist used to treat nasal and sinus congestion, as well as allergic rhinitis.
Pseudoephedrine is a sympathomimetic amine used for its decongestant activity.
Acrivastine And Pseudoephedrine is also used to associated treatment for these conditions: Seasonal Allergic RhinitisAllergic Rhinitis (AR), Allergies, Common Cold, Common Cold Associated With Cough, Common Cold/Flu, Cough, Cough caused by Common Cold, Eye allergy, Fever, Flu caused by Influenza, Headache, Irritative cough, Nasal Allergies, Nasal Congestion, Nasal Congestion caused by Common Cold, Pain, Perennial Allergy, Priapism, Respiratory Allergy, Rhinorrhoea, Seasonal Allergic Rhinitis, Seasonal Allergies, Sinus Congestion, Sinusitis, Sneezing, Sore Throat, Symptoms of Acute Bronchitis Accompanied by Coughing, Throat irritation, Upper Respiratory Tract Infection, Upper respiratory tract congestion, Upper respiratory tract signs and symptoms, Dry cough, Minor aches and pains, Sinus pain, Watery itchy eyes, Airway secretion clearance therapy
How Acrivastine And Pseudoephedrine works
Pseudoephedrine acts mainly as an agonist of alpha adrenergic receptors and less strongly as an agonist of beta adrenergic receptors.[A10896] This agonism of adrenergic receptors produces vasoconstriction which is used as a decongestant and as a treatment of priapism. Pseudoephedrine is also an inhibitor of norepinephrine, dopamine, and serotonin transporters.
The sympathomimetic effects of pseudoephedrine include an increase in mean arterial pressure, heart rate, and chronotropic response of the right atria. Pseudoephedrine is also a partial agonist of the anococcygeal muscle. Pseudoephedrine also inhibits NF-kappa-B, NFAT, and AP-1.
Toxicity
The oral LD50 of pseudoephedrine is 2206mg/kg in rats and 726mg/kg in mice.
Patients experiencing an overdose of pseudoephedrine may present with giddiness, headache, nausea, vomiting, sweating, thirst, tachycardia, precordial pain, palpitations, difficulty urinating, muscle weakness, muscle tension, anxiety, restlessness, insomnia, toxic psychosis, cardiac arrhythmias, circulatory collapse, convulsions, coma, and respiratory failure. Treat overdose with symptomatic and supportive treatment including removal of unabsorbed drug.
Volume of Distribution
0.46 ± 0.05 L/kg
The apparent volume of distribution of pseudoephedrin is 2.6-3.3L/kg.
Elimination Route
Acrivastine was absorbed rapidly from the combination capsule following oral administration and was as bioavailable as a solution of acrivastine. After administration of SEMPREX-D Capsules, maximum plasma acrivastine concentrations were achieved at 1.14 ± 0.23 hour.
A 240mg oral dose of pseudoephedrine reaches a Cmax of 246.3±10.5ng/mL fed and 272.5±13.4ng/mL fasted, with a Tmax of 6.60±1.38h fed and 11.87±0.72h fasted, with an AUC of 6862.0±334.1ng*h/mL fed and 7535.1±333.0ng*h/mL fasted.
Half Life
The mean terminal half-life for acrivastine was 1.9 ± 0.3 hours following single oral doses and increased to 3.5 ± 1.9 hours at steady state. The terminal half-life for the propionic acid metabolite was 3.8 ± 1.4 hours.
The mean elimination half life of pseudoephedrine is 6.0h.
Clearance
2.9 ± 0.7 mL/min/kg
A 60mg oral dose of pseudoephedrine has a clearance of 5.9±1.7mL/min/kg.
Elimination Route
A mass balance study in 7 healthy volunteers showed that acrivastine is primarily eliminated by the kidneys. Over a 72-hour collection period, about 84% of the administered total radioactivity was recovered in urine and about 13% in feces, for a combined recovery of about 97%.
55-75% of an oral dose is detected in the urine as unchanged pseudoephedrine.
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