Optilast Actions

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Actions of Optilast in details

The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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Optilast, a phthalazinone derivative, exhibits histamine H1-receptor antagonist activity in isolated tissues, animal models, and humans. Optilast 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.

How should I take Optilast?

Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.

Use Optilast 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.

Optilast usually comes with patient information insert. Read and follow the instructions carefully. Ask your doctor if you have any questions.

Optilast 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 Optilast for any other nose problem without checking with your doctor first.

To use the spray:

Dosing

The dose of Optilast 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 Optilast. 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.

Missed Dose

If you miss a dose of Optilast, 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.

Storage

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.

Optilast pharmacology

Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
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Mechanism of Action

Optilast, a phthalazinone derivative, exhibits histamine H1-receptor antagonist activity in isolated tissues, animal models, and humans. Optilast 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.

Pharmacodynamics

Cardiac Electrophysiology:

In a placebo-controlled study (95 subjects with allergic rhinitis), there was no evidence of an effect of Optilast 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 Optilast 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 Optilast 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, Optilast does not prolong the QTc interval to any clinically relevant extent.

Pharmacokinetics

Absorption: After intranasal administration, the systemic bioavailability of Optilast is approximately 40%. Maximum plasma concentrations (Cmax) are achieved in 2-3 hours.

Optilast 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 Optilast.

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 Optilast and its metabolite, desmethylAzelastine, are approximately 88% and 97%, respectively.

Metabolism: Optilast is oxidatively metabolized to the principal active metabolite, desmethylAzelastine, by the cytochrome P450 enzyme system. The specific P450 isoforms responsible for the biotransformation of Optilast have not been identified. After intranasal dosing of Optilast to steady-state, plasma concentrations of desmethylAzelastine range from 20-50% of Optilast concentrations. Limited data indicate that the metabolite profile is similar when Optilast 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 Optilast was excreted in the feces with less than 10% as unchanged Optilast.

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 Optilast (4 mg twice daily) with erythromycin (500 mg three times daily for 7 days). In this study, co-administration of orally administered Optilast with erythromycin resulted in Cmax of 5.36 ± 2.6 ng/mL and AUC of 49.7 ± 24 ng∙h/mL for Optilast, whereas, administration of Optilast alone resulted in Cmax of 5.57 ± 2.7 ng/mL and AUC of 48.4 ± 24 ng∙h/mL for Optilast.

Cimetidine and Ranitidine: In a multiple-dose, steady-state drug interaction trial in healthy subjects, cimetidine (400 mg twice daily) increased orally administered mean Optilast (4 mg twice daily) concentrations by approximately 65%. No pharmacokinetic interaction was observed with co-administration of orally administered Optilast (4 mg twice daily) with ranitidine hydrochloride (150 mg twice daily).

Oral co-administration of Optilast with ranitidine resulted in Cmax of 8.89 ±3.28 ng/mL and AUC of 88.22 ± 40.43 ng∙h/mL for Optilast, whereas, Optilast when administered alone resulted in Cmax of 7.83 ± 4.06 ng/mL and AUC of 80.09 ± 43.55 ng∙h/mL for Optilast.

Theophylline: No significant pharmacokinetic interaction was observed with the co-administration of an oral 4 mg dose of Optilast twice daily and theophylline 300 mg or 400 mg twice daily.


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References

  1. EPA DSStox. "Azelastine: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).

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Information checked by Dr. Sachin Kumar, MD Pharmacology

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