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Otrivin Heuschnupfen Actions |
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Otrivin Heuschnupfen hydrochloride, a phthalazinone derivative, exhibits histamine H1-receptor antagonist activity in isolated tissues, animal models, and humans. Otrivin Heuschnupfen hydrochloride nasal solution (nasal spray) is administered as a racemic mixture with no difference in pharmacologic activity noted between the enantiomers in in vitro studies. The major metabolite, desmethylAzelastine, also possesses H1-receptor antagonist activity.
Use Otrivin Heuschnupfen only as directed by your doctor. Do not use more of it and do not use it more often than your doctor ordered. To do so may increase the chance of side effects.
Otrivin Heuschnupfen usually comes with patient information insert. Read and follow the instructions carefully. Ask your doctor if you have any questions.
Otrivin Heuschnupfen is for use only in the nose. Do not get any of it in your eyes or on your mouth. If it does get on these areas, rinse it off with water and call your doctor right away.
Do not use Otrivin Heuschnupfen for any other nose problem without checking with your doctor first.
To use the spray:
The dose of Otrivin Heuschnupfen will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Otrivin Heuschnupfen. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
If you miss a dose of Otrivin Heuschnupfen, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Ask your healthcare professional how you should dispose of any medicine you do not use.
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Store the bottle upright with the pump tightly closed.
Otrivin Heuschnupfen hydrochloride, a phthalazinone derivative, exhibits histamine H1-receptor antagonist activity in isolated tissues, animal models, and humans. Otrivin Heuschnupfen hydrochloride nasal solution (nasal spray) is administered as a racemic mixture with no difference in pharmacologic activity noted between the enantiomers in in vitro studies. The major metabolite, desmethylAzelastine, also possesses H1-receptor antagonist activity.
Cardiac Electrophysiology:
In a placebo-controlled study (95 subjects with allergic rhinitis), there was no evidence of an effect of Otrivin Heuschnupfen hydrochloride nasal solution (nasal spray) (2 sprays per nostril twice daily for 56 days) on cardiac repolarization as represented by the corrected QT interval (QTc) of the electrocardiogram. Following multiple dose oral administration of Otrivin Heuschnupfen 4 mg or 8 mg twice daily, the mean change in QTc was 7.2 msec and 3.6 msec, respectively.
Interaction studies investigating the cardiac repolarization effects of concomitantly administered oral Otrivin Heuschnupfen hydrochloride and erythromycin or ketoconazole were conducted. These drugs had no effect on QTc based on analysis of serial electrocardiograms. At a dose approximately 8 times the maximum recommended dose, Otrivin Heuschnupfen hydrochloride does not prolong the QTc interval to any clinically relevant extent.
Absorption: After intranasal administration, the systemic bioavailability of Otrivin Heuschnupfen hydrochloride is approximately 40%. Maximum plasma concentrations (Cmax) are achieved in 2-3 hours.
Otrivin Heuschnupfen hydrochloride administered intranasally at doses above two sprays per nostril twice daily for 29 days resulted in greater than proportional increases in Cmax and area under the curve (AUC) for Otrivin Heuschnupfen.
Distribution: Based on intravenous and oral administration, the steady-state volume of distribution is 14.5 L/kg. In vitro studies with human plasma indicate that the plasma protein binding of Otrivin Heuschnupfen and its metabolite, desmethylAzelastine, are approximately 88% and 97%, respectively.
Metabolism: Otrivin Heuschnupfen is oxidatively metabolized to the principal active metabolite, desmethylAzelastine, by the cytochrome P450 enzyme system. The specific P450 isoforms responsible for the biotransformation of Otrivin Heuschnupfen have not been identified. After intranasal dosing of Otrivin Heuschnupfen hydrochloride to steady-state, plasma concentrations of desmethylAzelastine range from 20-50% of Otrivin Heuschnupfen concentrations. Limited data indicate that the metabolite profile is similar when Otrivin Heuschnupfen hydrochloride is administered via the intranasal or oral route.
Elimination: Based on intravenous and oral administration, the elimination half-life and plasma clearance are 22 hours and 0.5 L/h/kg, respectively. Approximately 75% of an oral dose of radiolabeled Otrivin Heuschnupfen hydrochloride was excreted in the feces with less than 10% as unchanged Otrivin Heuschnupfen.
Special Populations:
Hepatic Impairment: Following oral administration, pharmacokinetic parameters were not influenced by hepatic impairment.
Renal Impairment: Based on oral, single-dose studies, renal insufficiency (creatinine clearance <50 mL/min) resulted in a 70-75% higher Cmax and AUC compared to normal subjects. Time to maximum concentration was unchanged.
Age: Following oral administration, pharmacokinetic parameters were not influenced by age.
Gender: Following oral administration, pharmacokinetic parameters were not influenced by gender.
Race: The effect of race has not been evaluated.
Drug-Drug Interactions:
Erythromycin: No significant pharmacokinetic interaction was observed with the co-administration of orally administered Otrivin Heuschnupfen (4 mg twice daily) with erythromycin (500 mg three times daily for 7 days). In this study, co-administration of orally administered Otrivin Heuschnupfen with erythromycin resulted in Cmax of 5.36 ± 2.6 ng/mL and AUC of 49.7 ± 24 ng∙h/mL for Otrivin Heuschnupfen, whereas, administration of Otrivin Heuschnupfen alone resulted in Cmax of 5.57 ± 2.7 ng/mL and AUC of 48.4 ± 24 ng∙h/mL for Otrivin Heuschnupfen.
Cimetidine and Ranitidine: In a multiple-dose, steady-state drug interaction trial in healthy subjects, cimetidine (400 mg twice daily) increased orally administered mean Otrivin Heuschnupfen (4 mg twice daily) concentrations by approximately 65%. No pharmacokinetic interaction was observed with co-administration of orally administered Otrivin Heuschnupfen (4 mg twice daily) with ranitidine hydrochloride (150 mg twice daily).
Oral co-administration of Otrivin Heuschnupfen with ranitidine resulted in Cmax of 8.89 ±3.28 ng/mL and AUC of 88.22 ± 40.43 ng∙h/mL for Otrivin Heuschnupfen, whereas, Otrivin Heuschnupfen when administered alone resulted in Cmax of 7.83 ± 4.06 ng/mL and AUC of 80.09 ± 43.55 ng∙h/mL for Otrivin Heuschnupfen.
Theophylline: No significant pharmacokinetic interaction was observed with the co-administration of an oral 4 mg dose of Otrivin Heuschnupfen hydrochloride twice daily and theophylline 300 mg or 400 mg twice daily.
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Information checked by Dr. Sachin Kumar, MD Pharmacology
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