Delora stop Actions

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Actions of Delora stop 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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Pharmacology: Delora stop is the orally active, nonsedating, active metabolite of loratadine, with a sustained duration of action that allows once-daily dosing in clinical use.

Mechanism of Action: Delora stop is a new, selective peripheral histamine H1-receptor antagonist with more potent antiallergenic properties than loratadine itself. It also has anti-inflammatory activity. Delora stop acts by inhibiting the release of pro-inflammatory mediators from human mast cells/basophils.

Delora stop was more potent than loratadine with respect to in vivo inhibition of histamine-induced wheal and flare. It does not readily penetrate the central nervous system.

Delora stop demonstrates H1-receptor specificity including 15- to 50-fold lower affinity for muscarinic receptors compared with H1-receptors.

Clinical studies have demonstrated that Delora stop has a lack of clinically significant cardiovascular toxicity, and unlike most other antihistamines, has decongestant effects.

Pharmacokinetics: After oral administration, Delora stop is rapidly and almost completely absorbed. Peak plasma concentrations are reached within about 3 hrs; the terminal elimination half-life of Delora stop is averaged 24-27 hrs, indicating that Delora stop is suitable for once-daily administration. The pharmacokinetics of Delora stop is linear and exhibits dose proportionality. With daily administration of 5 mg of Delora stop, steady-state serum concentrations are achieved within 7 days.

Delora stop is rapidly metabolised by hydroxylation to 3-hydroxydesloratadine and excreted mainly in the urine.

Because the bioavailability and absorption of Delora stop are not significantly affected by food, Delora stop may be administered with or without meals.

Pharmacokinetic studies with Delora stop in the elderly and in patients with renal dysfunction are not yet available. The available data for loratadine indicate that the elimination half-life of Delora stop may be increased in patients with chronic renal failure. However, dosage reduction in mild to moderate renal impairment is probably not necessary.

Limited pharmacokinetic data suggest that Delora stop 5 mg daily is likely to be safe in patients with hepatic dysfunction.

How should I take Delora stop?

Take Delora stop exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Delora stop is usually taken once per day. Follow your doctor's instructions.

Do not crush, chew, or break the regular Delora stop tablet. Swallow the pill whole.

Measure the liquid form of Delora stop with a special dose-measuring spoon or cup, not a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.

To take Delora stop orally disintegrating tablet (Delora stop RediTabs):

Call your doctor if your symptoms do not improve.

Store Delora stop at room temperature away from moisture and heat.

Delora stop administration

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.
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Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Delora stop is usually taken once per day. Follow your doctor's instructions.

Do not crush, chew, or break the regular Delora stop tablet. Swallow the pill whole.

Measure the liquid form of Delora stop with a special dose-measuring spoon or cup, not a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.

To take Delora stop orally disintegrating tablet (Delora stop RediTabs):

Store at room temperature away from moisture and heat.

Call your doctor if your symptoms do not improve.

Delora stop 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

Delora stop is a long-acting tricyclic histamine antagonist with selective H1-receptor histamine antagonist activity. Receptor binding data indicates that at a concentration of 2–3 ng/mL (7 nanomolar), Delora stop shows significant interaction with the human histamine H1-receptor. Delora stop inhibited histamine release from human mast cells in vitro. Results of a radiolabeled tissue distribution study in rats and a radioligand H1-receptor binding study in guinea pigs showed that Delora stop did not readily cross the blood brain barrier. The clinical significance of this finding is unknown.

Pharmacodynamics

Wheal and Flare: Human histamine skin wheal studies following single and repeated 5-mg doses of Delora stop have shown that the drug exhibits an antihistaminic effect by 1 hour; this activity may persist for as long as 24 hours. There was no evidence of histamine-induced skin wheal tachyphylaxis within the Delora stop 5-mg group over the 28-day treatment period. The clinical relevance of histamine wheal skin testing is unknown.

Effects on QTc: Single daily doses of 45 mg were given to normal male and female volunteers for 10 days. All ECGs obtained in this study were manually read in a blinded fashion by a cardiologist. In Delora stop-treated subjects, there was an increase in mean heart rate of 9.2 bpm relative to placebo. The QT interval was corrected for heart rate (QTc) by both the Bazett and Fridericia methods. Using the QTc (Bazett) there was a mean increase of 8.1 msec in Delora stop-treated subjects relative to placebo. Using QTc (Fridericia) there was a mean increase of 0.4 msec in Delora stop-treated subjects relative to placebo. No clinically relevant adverse events were reported.

Pharmacokinetics

Absorption

Following oral administration of a Delora stop 5-mg tablet once daily for 10 days to normal healthy volunteers, the mean time to maximum plasma concentrations (Tmax) occurred at approximately 3 hours post dose and mean steady state peak plasma concentrations (Cmax) and AUC of 4 ng/mL and 56.9 ng∙hr/mL were observed, respectively. Neither food nor grapefruit juice had an effect on the bioavailability (Cmax and AUC) of Delora stop.

The pharmacokinetic profile of Delora stop

Oral Solution was evaluated in a three-way crossover study in 30 adult volunteers. A single dose of 10 mL of Delora stop

Oral Solution containing 5 mg of Delora stop was bioequivalent to a single dose of 5-mg Delora stop Tablet. Food had no effect on the bioavailability (AUC and Cmax) of Delora stop

Oral Solution.

The pharmacokinetic profile of Delora stop RediTabs Tablets was evaluated in a three-way crossover study in 24 adult volunteers. A single Delora stop RediTabs Tablet containing 5 mg of Delora stop was bioequivalent to a single 5-mg Delora stop RediTabs Tablet (original formulation) for both Delora stop and 3-hydroxydesloratadine. Food and water had no effect on the bioavailability (AUC and Cmax) of Delora stop RediTabs Tablets.

Distribution

Delora stop and 3-hydroxydesloratadine are approximately 82% to 87% and 85% to 89% bound to plasma proteins, respectively. Protein binding of Delora stop and 3-hydroxydesloratadine was unaltered in subjects with impaired renal function.

Metabolism

Delora stop (a major metabolite of loratadine) is extensively metabolized to 3-hydroxydesloratadine, an active metabolite, which is subsequently glucuronidated. The enzyme(s) responsible for the formation of 3-hydroxydesloratadine have not been identified. Data from clinical trials indicate that a subset of the general population has a decreased ability to form 3-hydroxydesloratadine, and are poor metabolizers of Delora stop. In pharmacokinetic studies (n=3748), approximately 6% of subjects were poor metabolizers of Delora stop (defined as a subject with an AUC ratio of 3-hydroxydesloratadine to Delora stop less than 0.1, or a subject with a Delora stop half-life exceeding 50 hours). These pharmacokinetic studies included subjects between the ages of 2 and 70 years, including 977 subjects aged 2 to 5 years, 1575 subjects aged 6 to 11 years, and 1196 subjects aged 12 to 70 years. There was no difference in the prevalence of poor metabolizers across age groups. The frequency of poor metabolizers was higher in Blacks (17%, n=988) as compared to Caucasians (2%, n=1,462) and Hispanics (2%, n=1,063). The median exposure (AUC) to Delora stop in the poor metabolizers was approximately 6-fold greater than in the subjects who are not poor metabolizers. Subjects who are poor metabolizers of Delora stop cannot be prospectively identified and will be exposed to higher levels of Delora stop following dosing with the recommended dose of Delora stop. In multidose clinical safety studies, where metabolizer status was identified, a total of 94 poor metabolizers and 123 normal metabolizers were enrolled and treated with Delora stop

Oral Solution for 15–35 days. In these studies, no overall differences in safety were observed between poor metabolizers and normal metabolizers. Although not seen in these studies, an increased risk of exposure-related adverse events in patients who are poor metabolizers cannot be ruled out.

Elimination

The mean plasma elimination half-life of Delora stop was approximately 27 hours. Cmax and AUC values increased in a dose proportional manner following single oral doses between 5 and 20 mg. The degree of accumulation after 14 days of dosing was consistent with the half-life and dosing frequency. A human mass balance study documented a recovery of approximately 87% of the 14C-Delora stop dose, which was equally distributed in urine and feces as metabolic products. Analysis of plasma 3-hydroxydesloratadine showed similar Tmax and half-life values compared to Delora stop.

Special Populations

Geriatric Subjects: In older subjects (≥65 years old; n=17) following multiple-dose administration of Delora stop Tablets, the mean Cmax and AUC values for Delora stop were 20% greater than in younger subjects (<65 years old). The oral total body clearance (CL/F) when normalized for body weight was similar between the two age groups. The mean plasma elimination half-life of Delora stop was 33.7 hr in subjects ≥65 years old. The pharmacokinetics for 3-hydroxydesloratadine appeared unchanged in older versus younger subjects. These age-related differences are unlikely to be clinically relevant and no dosage adjustment is recommended in elderly subjects.

Pediatric Subjects: In subjects 6 to 11 years old, a single dose of 5 mL of Delora stop

Oral Solution containing 2.5 mg of Delora stop, resulted in Delora stop plasma concentrations similar to those achieved in adults administered a single 5-mg Delora stop Tablet. In subjects 2 to 5 years old, a single dose of 2.5 mL of Delora stop

Oral Solution containing 1.25 mg of Delora stop, resulted in Delora stop plasma concentrations similar to those achieved in adults administered a single 5-mg Delora stop Tablet. However, the Cmax and AUC of the metabolite (3-hydroxydesloratadine) were 1.27 and 1.61 times higher for the 5-mg dose of

Oral Solution administered in adults compared to the Cmax and AUC obtained in children 2 to 11 years of age receiving 1.25–2.5 mg of Delora stop

Oral Solution.

A single dose of either 2.5 mL or 1.25 mL of Delora stop

Oral Solution containing 1.25 mg or 0.625 mg, respectively, of Delora stop was administered to subjects 6 to 11 months of age and 12 to 23 months of age. The results of a population pharmacokinetic analysis indicated that a dose of 1 mg for subjects aged 6 to 11 months and 1.25 mg for subjects 12 to 23 months of age is required to obtain Delora stop plasma concentrations similar to those achieved in adults administered a single 5-mg dose of Delora stop

Oral Solution.

The Delora stop RediTabs 2.5-mg tablet has not been evaluated in pediatric patients. Bioequivalence of the Delora stop RediTabs Tablet and the original Delora stop RediTabs Tablets was established in adults. In conjunction with the dose-finding studies in pediatrics described, the pharmacokinetic data for Delora stop RediTabs Tablets supports the use of the 2.5-mg dose strength in pediatric patients 6 to 11 years of age.

Renally Impaired: Delora stop pharmacokinetics following a single dose of 7.5 mg were characterized in patients with mild (n=7; creatinine clearance 51–69 mL/min/1.73 m2), moderate (n=6; creatinine clearance 34–43 mL/min/1.73 m2), and severe (n=6; creatinine clearance 5–29 mL/min/1.73 m2) renal impairment or hemodialysis dependent (n=6) patients. In patients with mild and moderate renal impairment, median Cmax and AUC values increased by approximately 1.2- and 1.9-fold, respectively, relative to subjects with normal renal function. In patients with severe renal impairment or who were hemodialysis dependent, Cmax and AUC values increased by approximately 1.7- and 2.5-fold, respectively. Minimal changes in 3-hydroxydesloratadine concentrations were observed. Delora stop and 3-hydroxydesloratadine were poorly removed by hemodialysis. Plasma protein binding of Delora stop and 3-hydroxydesloratadine was unaltered by renal impairment. Dosage adjustment for patients with renal impairment is recommended.

Hepatically Impaired: Delora stop pharmacokinetics were characterized following a single oral dose in patients with mild (n=4), moderate (n=4), and severe (n=4) hepatic impairment as defined by the Child-Pugh classification of hepatic function and 8 subjects with normal hepatic function. Patients with hepatic impairment, regardless of severity, had approximately a 2.4-fold increase in AUC as compared with normal subjects. The apparent oral clearance of Delora stop in patients with mild, moderate, and severe hepatic impairment was 37%, 36%, and 28% of that in normal subjects, respectively. An increase in the mean elimination half-life of Delora stop in patients with hepatic impairment was observed. For 3-hydroxydesloratadine, the mean Cmax and AUC values for patients with hepatic impairment were not statistically significantly different from subjects with normal hepatic function. Dosage adjustment for patients with hepatic impairment is recommended.

Gender: Female subjects treated for 14 days with Delora stop Tablets had 10% and 3% higher Delora stop Cmax and AUC values, respectively, compared with male subjects. The 3-hydroxydesloratadine Cmax and AUC values were also increased by 45% and 48%, respectively, in females compared with males. However, these apparent differences are not likely to be clinically relevant and therefore no dosage adjustment is recommended.

Race: Following 14 days of treatment with Delora stop Tablets, the Cmax and AUC values for Delora stop were 18% and 32% higher, respectively, in Blacks compared with Caucasians. For 3-hydroxydesloratadine there was a corresponding 10% reduction in Cmax and AUC values in Blacks compared to Caucasians. These differences are not likely to be clinically relevant and therefore no dose adjustment is recommended.

Drug Interactions: In two controlled crossover clinical pharmacology studies in healthy male (n=12 in each study) and female (n=12 in each study) volunteers, Delora stop 7.5 mg (1.5 times the daily dose) once daily was coadministered with erythromycin 500 mg every 8 hours or ketoconazole 200 mg every 12 hours for 10 days. In three separate controlled, parallel group clinical pharmacology studies, Delora stop at the clinical dose of 5 mg has been coadministered with azithromycin 500 mg followed by 250 mg once daily for 4 days (n=18) or with fluoxetine 20 mg once daily for 7 days after a 23-day pretreatment period with fluoxetine (n=18) or with cimetidine 600 mg every 12 hours for 14 days (n=18) under steady-state conditions to normal healthy male and female volunteers. Although increased plasma concentrations (Cmax and AUC0-24 hrs) of Delora stop and 3-hydroxydesloratadine were observed, there were no clinically relevant changes in the safety profile of Delora stop, as assessed by electrocardiographic parameters (including the corrected QT interval), clinical laboratory tests, vital signs, and adverse events.

Table 2: Changes in Delora stop and 3-Hydroxydesloratadine Pharmacokinetics in Healthy Male and Female Volunteers
Delora stop 3-Hydroxydesloratadine
Cmax AUC0-24 hrs Cmax AUC0-24 hrs
Erythromycin

(500 mg Q8h)

+ 24% + 14% + 43% + 40%

Ketoconazole

(200 mg Q12h)

+ 45%

+ 39%

+ 43%

+ 72%

Azithromycin

(500 mg day 1,

250 mg QD x 4 days)

+ 15%

+ 5%

+ 15%

+ 4%

Fluoxetine

(20 mg QD)

+ 15%

+ 0%

+ 17%

+ 13%

Cimetidine

(600 mg Q12h)

+ 12%

+ 19%

- 11%

- 3%



References

  1. DailyMed. "DESLORATADINE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
  2. NCIt. "Desloratadine: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
  3. EPA DSStox. "Desloratadine: 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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