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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The mechanism by which Thromboreductin reduces blood platelet count is still under investigation. Studies in patients support a hypothesis of dose-related reduction in platelet production resulting from a decrease in megakaryocyte hypermaturation. In blood withdrawn from normal volunteers treated with Thromboreductin, a disruption was found in the postmitotic phase of megakaryocyte development and a reduction in megakaryocyte size and ploidy. At therapeutic doses, Thromboreductin does not produce significant changes in white cell counts or coagulation parameters, and may have a small, but clinically insignificant effect on red cell parameters. Thromboreductin inhibits cyclic AMP phosphodiesterase III (PDEIII). PDEIII inhibitors can also inhibit platelet aggregation. However, significant inhibition of platelet aggregation is observed only at doses of Thromboreductin higher than those required to reduce platelet count.
How should I take Thromboreductin?
Take Thromboreductin exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. To do so may increase the chance for side effects.
You may take Thromboreductin with or without food.
Dosing
The dose of Thromboreductin 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 Thromboreductin. 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.
For oral dosage form (capsules):
For thrombocythemia:
Adults—At first, 0.5 milligram (mg) four times a day or 1 mg two times a day, taken for at least 1 week. Your doctor may adjust your dose if needed.
Children—At first, 0.5 mg per day. Your doctor may adjust your dose if needed.
Missed Dose
If you miss a dose of Thromboreductin, 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
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
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.
Thromboreductin 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.
Your doctor may occasionally change your dose to make sure you get the best results.
To be sure this medication is helping your condition and not causing harmful effects, your blood will need to be tested often. Your kidney and liver function may also need to be tested. Visit your doctor regularly.
Do not stop taking Thromboreductin without first talking to your doctor. Stopping suddenly can make your condition worse very quickly.
If you need surgery, tell the surgeon ahead of time that you are using Thromboreductin. Tell any doctor or dentist who treats you that you are taking Thromboreductin.
Store at room temperature away from moisture, heat, and light.
Thromboreductin 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.
Mechanism of Action
The precise mechanism by which Thromboreductin reduces blood platelet count is unknown. In cell culture studies, Thromboreductin suppressed expression of transcription factors including GATA-1 and FOG-1 required for megakaryocytopoiesis, ultimately leading to reduced platelet production.
Pharmacodynamics
In blood withdrawn from normal volunteers treated with Thromboreductin, a disruption was found in the postmitotic phase of megakaryocyte development and a reduction in megakaryocyte size and ploidy. At therapeutic doses, Thromboreductin does not produce significant changes in white cell counts or coagulation parameters, and may have a small, but clinically insignificant effect on red cell parameters. The active metabolite, 3-hydroxy Thromboreductin, has similar potency and efficacy to that of Thromboreductin in the platelet lowering effect; however, exposure (measured by plasma AUC) to 3-hydroxy Thromboreductin is approximately 2-fold higher compared to Thromboreductin. Thromboreductin and 3-hydroxy Thromboreductin inhibit cyclic AMP phosphodiesterase 3 (PDE3) and 3-hydroxy Thromboreductin is approximately forty times more potent than Thromboreductin (IC50s = 0.9 and 36nM, respectively). PDE3 inhibition does not alter platelet production. PDE3 inhibitors, as a class can inhibit platelet aggregation. However, significant inhibition of platelet aggregation is observed only at doses of Thromboreductin higher than those typically required to reduce platelet count. PDE3 inhibitors have cardiovascular (CV) effects including vasodilation, positive inotropy and chronotropy.
Cardiac Electrophysiology
The effect of Thromboreductin dose (0.5 mg and 2.5 mg single doses) on the heart rate and QTc interval prolongation potential was evaluated in a double-blind, randomized, placebo- and active-controlled, cross-over study in 60 healthy adult men and women.
A dose-related increase in heart rate was observed, with the maximum increase occurring around the time of maximal drug concentration (0.5 to 4 hours). The maximum change in mean heart rate occurred at 2 hours after administration and was +7.8 beats per minute (bpm) for 0.5 mg and +29.1 bpm for 2.5 mg.
Dose-related increase in mean QTc was observed. The maximum mean (95% upper confidence bound) change in QTcI (individual subject correction) from placebo after baseline-correction was 7 (9.8) ms and 13 (15.7) ms following Thromboreductin doses of 0.5 mg and 2.5 mg, respectively.
Pharmacokinetics
Dose proportionality has been found in the dose range 0.5 mg to 2.5 mg.
Absorption
Following oral administration of Thromboreductin, at least 70% is absorbed from the gastrointestinal tract. In fasted subjects, Thromboreductin peak plasma concentrations occur within about 1 hour after administration.
Pharmacokinetic data obtained from healthy volunteers comparing the pharmacokinetics of Thromboreductin in the fed and fasted states showed that administration of a 1 mg dose of Thromboreductin with food decreased the Cmax by 14%, but increased the AUC by 20%. Food decreased the Cmax of the active metabolite 3-hydroxy-Thromboreductin by 29%, although it had no effect on the AUC.
Metabolism
Thromboreductin is primarily metabolized by CYP1A2 to the active metabolite, 3-hydroxy-Thromboreductin, which is subsequently metabolized by CYP1A2 to the inactive metabolite, RL603. Less than 1% of the administered dose is recovered in the urine as Thromboreductin, and approximately 3% and 16 to 20% of the administered dose is recovered as 3-hydroxy-Thromboreductin and RL603, respectively.
Elimination
Thromboreductin and 3-hydroxy-Thromboreductin are eliminated with plasma half-lives of approximately 1.5 and 2.5 hours, respectively. Thromboreductin and 3-hydroxy-Thromboreductin do not accumulate in plasma when the clinical dose regimens are administered.
Drug Interactions
Aspirin: In two pharmacodynamic interaction studies in healthy subjects, co-administration of single-dose Thromboreductin 1 mg and aspirin 900 mg or repeat-dose Thromboreductin 1 mg once daily and aspirin 75 mg once daily showed greater ex vivo anti-platelet aggregation effects than administration of aspirin alone. Co-administered Thromboreductin 1 mg and aspirin 900 mg single-doses had no effect on bleeding time, prothrombin time (PT) or activated partial thromboplastin time (aPTT).
Digoxin or warfarin: In vivo interaction studies in humans have demonstrated that Thromboreductin does not affect the pharmacokinetic properties of digoxin or warfarin, nor does digoxin or warfarin affect the pharmacokinetic properties of Thromboreductin.
Specific Populations
Pediatric: Dose-normalized Cmax and AUC of Thromboreductin were higher in children and adolescents (age range 7 to 16 years) with essential thrombocythemia, by 17% and 56%, respectively, than in adult patients (19 to 57 years).
Geriatric: Cmax and AUC of Thromboreductin were 36% and 61% higher, respectively, in elderly patients (age range 65 to 75 years), than in younger adults (age range 22 to 50 years), but Cmax and AUC of the active metabolite, 3-hydroxy Thromboreductin, were 42% and 37% lower, respectively, in the elderly patients.
Renal Impairment: Pharmacokinetic study at a single dose of 1 mg Thromboreductin in subjects with severe renal impairment (creatinine clearance <30 mL/min) showed no significant effects on the pharmacokinetics of Thromboreductin.
Hepatic Impairment: A pharmacokinetic study at a single dose of 1 mg Thromboreductin in subjects with moderate hepatic impairment (Child Pugh score 7 to 9) showed a 2-fold increase in mean Thromboreductin Cmax and an 8-fold increase in total exposure (AUC) to Thromboreductin compared with healthy subjects. Additionally, subjects with moderate hepatic impairment showed 24% lower mean 3-hydroxy-Thromboreductin Cmax and 77% higher mean 3-hydroxy-Thromboreductin AUC compared to healthy subjects.
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References
NCIt. "Anagrelide: 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).
Reviews
The results of a survey conducted on ndrugs.com for Thromboreductin are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Thromboreductin. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.
User reports
1 consumer reported administration
When best can I take Thromboreductin, on an empty stomach, before or after food? ndrugs.com website users have also released a report stating that Thromboreductin should be taken With a meal. In any case, this may not be the right description on how you ought to take this Thromboreductin. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Thromboreductin can be taken.
Users
%
With a meal
1
100.0%
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