Hemostan Actions

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Actions of Hemostan 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: Pharmacodynamics: Hemostan is a competitive inhibitor of plasminogen activation, and at much higher concentrations, a noncompetitive inhibitor of plasmin, ie, actions similar to aminocaproic acid. Hemostan is about 10 times more potent in vitro than aminocaproic acid.

Hemostan binds more strongly than aminocaproic acid to both the strong and weak receptor sites of the plasminogen molecule in a ratio corresponding to the difference in potency between the compounds. Hemostan in a concentration of 1 mg/mL does not aggregate platelets in vitro.

Hemostan in concentrations up to 10 mg/mL blood has no influence on the platelet count, the coagulation time or various coagulation factors in whole blood or citrated blood from normal subjects. However, Hemostan in concentrations of 10 mg/mL and 1 mg/mL blood prolongs the thrombin time.

Pharmacokinetics: The plasma protein-binding of Hemostan is about 3% at therapeutic plasma levels and seems to be fully accounted for by its binding to plasminogen. Hemostan does not bind to serum albumin.

After an IV dose of 1 g, the plasma concentration time curve shows a triexponential decay with a t½ of about 2 hrs for the terminal elimination phase. The initial volume of distribution is about 9-12 L. Urinary excretion via glomerular filtration is the main route of elimination. Overall renal clearance is equal to overall plasma clearance (110-116 mL/min) and >95% of the dose is excreted in the urine as the unchanged drug. Excretion of Hemostan is about 90% at 24 hrs after IV administration of 10 mg/kg body weight.

An anti-fibrinolytic concentration of Hemostan remains in different tissues for about 17 hrs, and in the serum, up to 7 or 8 hrs.

Hemostan passes through the placenta. The concentration in cord blood after an IV injection of 10 mg/kg to pregnant women is about 30 mg/L, as high as in the maternal blood.

Hemostan diffuses rapidly into joint fluid and the synovial membrane. In the joint fluid the same concentration is obtained as in the serum. The biological t½ of Hemostan in the joint fluid is about 3 hrs.

The concentration of Hemostan in a number of other tissues is lower than in blood. In breast milk, the concentration is about 1/100 of the serum peak concentration. Hemostan concentration in cerebrospinal fluid is about 1/10 of that of the plasma. The drug passes into the aqueous humor, the concentration being about 1/10 of the plasma concentration.

Hemostan has been detected in semen where it inhibits fibrinolytic activity but does not influence sperm migration.

Toxicology: Preclinical Safety Data: An increased incidence of leukemia in male mice receiving Hemostan in food at a concentration of 4.8% (equivalent to doses as high as 5 g/kg/day) may have been related to treatment. Female mice were not included in this experiment.

Hyperplasia of the biliary tract and cholangioma and adenocarcinoma of the intrahepatic biliary system have been reported in 1 strain of rats after dietary administration of doses exceeding the maximum tolerated dose for 22 months. Hyperplastic, but not neoplastic, lesions were reported at lower doses. Subsequent long-term dietary administration studies in a different strain of rat, each with an exposure level equal to the maximum level employed in the earlier experiment, have failed to show such hyperplastic/neoplastic changes in the liver. No mutagenic activity has been demonstrated in several in vitro and in vivo genotoxicity testing systems.

In published, preclinical animal studies, epileptic activities were induced by topical application of Hemostan to the cortex of anesthetized cats. Similarly, IV infusion of high doses (500-600 mg/kg) of Hemostan induced seizure-like activity in conscious cats. Severe hind limb spasms developed into generalized convulsions in a rat model following application of Hemostan to the lumbar spinal cord. Hemostan within a fibrin sealant similarly induced limb spasms and convulsions in this rat model. Fibrin sealant containing Hemostan evoked generalized seizures in rats following application to the cerebral cortex of anesthetized rats. Central nervous system hyperexcitability may be the result of antagonism of γ-aminobutyric acidA receptors by Hemostan.

How should I take Hemostan?

Take Hemostan only 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 of side effects.

Do not take Hemostan when you do not have your period. You should wait until your monthly period has started before taking Hemostan.

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

You may take Hemostan with or without food.

Swallow the tablet whole with liquids. Do not break, crush, or chew it.

Dosing

The dose of Hemostan 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 Hemostan. 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 Hemostan, 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.

If you take a dose that is late, wait at least 6 hours before you take your next dose.

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.

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

Hemostan is injected into a vein through an IV just before your tooth is pulled. You may need to keep using the medication for up to 8 days afterward.

You may be shown how to use an IV at home. Do not self-inject Hemostan if you do not fully understand how to give the injection and properly dispose of used needles, IV tubing, and other items used to inject the medicine.

To be sure this medication is not causing harmful effects, your vision may need to be tested while you are using Hemostan. Follow your doctor's instructions.

Store this medication at room temperature away from moisture and heat.

Hemostan 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

Hemostan is a synthetic lysine amino acid derivative, which diminishes the dissolution of hemostatic fibrin by plasmin. In the presence of Hemostan, the lysine receptor binding sites of plasmin for fibrin are occupied, preventing binding to fibrin monomers, thus preserving and stabilizing fibrin's matrix structure.

The antifibrinolytic effects of Hemostan are mediated by reversible interactions at multiple binding sites within plasminogen. Native human plasminogen contains 4 to 5 lysine binding sites with low affinity for Hemostan (Kd = 750 μmol/L) and 1 with high affinity (Kd = 1.1 μmol/L). The high affinity lysine site of plasminogen is involved in its binding to fibrin. Saturation of the high affinity binding site with Hemostan displaces plasminogen from the surface of fibrin. Although plasmin may be formed by conformational changes in plasminogen, binding to and dissolution of the fibrin matrix is inhibited.

Pharmacodynamics

Hemostan, at in vitro concentrations of 25 - 100 μM, reduces by 20 - 60% the maximal rate of plasmin lysis of fibrin catalyzed by tissue plasminogen activator (tPA).

Elevated concentrations of endometrial, uterine, and menstrual blood tPA are observed in women with heavy menstrual bleeding (HMB) compared to women with normal menstrual blood loss. The effect of Hemostan on lowering endometrial tPA activity and menstrual fluid fibrinolysis is observed in women with HMB receiving Hemostan total oral doses of 2-3 g/day for 5 days.

In healthy subjects, Hemostan at blood concentrations less than 10 mg/mL has no effect on the platelet count, the coagulation time or various coagulation factors in whole blood or citrated blood. Hemostan, however, at blood concentrations of 1 and 10 mg/mL prolongs the thrombin time.

Cardiac Electrophysiology

The effect of Hemostan Tablets on QT interval was evaluated in a randomized, single-dose, 4-way crossover study in 48 healthy females aged 18 to 49 years. Subjects received (1) Hemostan Tablets 1300 mg (two 650 mg tablets), (2) Hemostan Tablets 3900 mg (six 650 mg tablets; three times the recommended single dose), (3) moxifloxacin 400 mg, and (4) placebo. There was no significant increase in the corrected QT interval at any time up to 24 hours after the administration of either dose of Hemostan Tablets. Moxifloxacin, the active control, was associated with a maximum 14.11 msec mean increase in corrected QT interval (moxifloxacin – placebo) at 3 hours after administration.

Pharmacokinetics

Absorption

After a single oral administration of two 650 mg tablets of Hemostan, the peak plasma concentration (Cmax) occurred at approximately 3 hours (Tmax). The absolute bioavailability of Hemostan Tablets in women aged 18-49 is approximately 45%. Following multiple oral doses (two 650 mg tablets three times daily) administration of Hemostan Tablets for 5 days, the mean Cmax increased by approximately 19% and the mean area under the plasma concentration-time curve (AUC) remained unchanged, compared to a single oral dose administration (two 650 mg tablets). Plasma concentrations reached steady state at the 5th dose of Hemostan Tablets on Day 2.

The mean plasma pharmacokinetic parameters of Hemostan determined in 19 healthy women following a single (two 650 mg tablets) and multiple (two 650 mg tablets three times daily for 5 days) oral dose of Hemostan Tablets are shown in Table 3.

Effect of food: Hemostan Tablets may be administered without regard to meals. A single dose administration (two 650 mg tablets) of Hemostan Tablets with food increased both Cmax and AUC by 7% and 16%, respectively.

Distribution

Hemostan is 3% bound to plasma proteins with no apparent binding to albumin. Hemostan is distributed with an initial volume of distribution of 0.18 L/kg and steady-state apparent volume of distribution of 0.39 L/kg.

Hemostan crosses the placenta. The concentration in cord blood after an intravenous injection of 10 mg/kg to pregnant women is about 30 mg/L, as high as in the maternal blood.

Hemostan concentration in cerebrospinal fluid is about one tenth of the plasma concentration.

The drug passes into the aqueous humor of the eye achieving a concentration of approximately one tenth of plasma concentrations.

Metabolism

A small fraction of the Hemostan is metabolized.

Excretion

Hemostan is eliminated by urinary excretion primarily via glomerular filtration with more than 95% of the dose excreted unchanged. Excretion of Hemostan is about 90% at 24 hours after intravenous administration of 10 mg/kg. Most elimination post intravenous administration occurred during the first 10 hours, giving an apparent elimination half-life of approximately 2 hours. The mean terminal half-life of Hemostan Tablets is approximately 11 hours. Plasma clearance of Hemostan is 110-116 mL/min.

Specific Populations

Pregnancy (Category B)

Hemostan Tablets are not indicated for use in pregnant women. Hemostan is known to cross the placenta and appears in cord blood at concentrations approximately equal to maternal concentration. There are no adequate and well-controlled studies in pregnant women.

Nursing Mothers

Hemostan is present in the mother's milk at a concentration of about one hundredth of the corresponding serum concentrations. Hemostan Tablets should be used during lactation only if clearly needed.

Pediatric Use

Hemostan Tablets are indicated for women of reproductive age and are not intended for use in premenarcheal girls.

In a randomized, single dose, two-way crossover study of two dose levels (650 mg and 1,300 mg [two 650 mg tablets]), pharmacokinetics of Hemostan was evaluated in 20 female adolescents (12 to 16 years of age) with heavy menstrual bleeding. The Cmax and AUC values after a single oral dose of 650 mg in the adolescent females were 32 – 36% less than those after a single oral dose of 1,300 mg in the adolescent females. The Cmax and AUC values after a single oral dose of 1300 mg in the adolescent females were 20 – 25% less than those in the adult females given the same dose in a separate study.

Geriatric Use

Hemostan Tablets are indicated for women of reproductive age and are not intended for use by postmenopausal women.

Renal Impairment

The effect of renal impairment on the disposition of Hemostan Tablets has not been evaluated. Urinary excretion following a single intravenous injection of Hemostan declines as renal function decreases. Following a single 10 mg/kg intravenous injection of Hemostan in 28 patients, the 24-hour urinary fractions of Hemostan with serum creatinine concentrations 1.4 – 2.8, 2.8 – 5.7, and greater than 5.7 mg/dL were 51, 39, and 19%, respectively. The 24-hour Hemostan plasma concentrations for these patients demonstrated a direct relationship to the degree of renal impairment. Therefore, dose adjustment is needed in patients with renal impairment.

Hepatic Impairment

The effect of hepatic impairment on the disposition of Hemostan Tablets has not been evaluated. One percent and 0.5 percent of an oral dose are excreted as a dicarboxylic acid and acetylated metabolite, respectively. Because only a small fraction of the drug is metabolized, no dose adjustment is needed in patients with hepatic impairment.

Drug Interactions

No drug-drug interaction studies were conducted with Hemostan Tablets.

Hormonal Contraceptives

Because Hemostan Tablets are antifibrinolytic, concomitant use of hormonal contraception and Hemostan Tablets may further exacerbate the increased thrombotic risk associated with combination hormonal contraceptives. For this reason, concomitant use of Hemostan Tablets with combination hormonal contraceptives is contraindicated

Factor IX Complex Concentrates or Anti-inhibitor Coagulant Concentrates

Hemostan Tablets are not recommended in patients taking either Factor IX complex concentrates or anti-inhibitor coagulant concentrates because the risk of thrombosis may be increased.

Tissue Plasminogen Activators

Concomitant therapy with tissue plasminogen activators may decrease the efficacy of both Hemostan Tablets and tissue plasminogen activators. Therefore, exercise caution if a patient taking Hemostan Tablets therapy requires tissue plasminogen activators.

All-Trans Retinoic Acid (Oral Tretinoin)

In a study involving 28 patients with acute promyelocytic leukemia who were given either orally administered all-trans retinoic acid plus intravenously administered Hemostan, all-trans retinoic acid plus chemotherapy, or all-trans retinoic acid plus Hemostan plus chemotherapy, all 4 patients who were given all-trans retinoic acid plus Hemostan died, with 3 of the 4 deaths due to thrombotic complications. It appears that the procoagulant effect of all-trans retinoic acid may be exacerbated by concomitant use of Hemostan. Therefore, exercise caution when prescribing Hemostan Tablets to patients with acute promyelocytic leukemia taking all-trans retinoic acid.


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References

  1. DailyMed. "TRANEXAMIC ACID: 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. "Tranexamic Acid: 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. "Tranexamic acid: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).

Reviews

The results of a survey conducted on ndrugs.com for Hemostan 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 Hemostan. 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

2 consumers reported administration

When best can I take Hemostan, on an empty stomach, before or after food?
ndrugs.com website users have also released a report stating that Hemostan should be taken Empty stomach. In any case, this may not be the right description on how you ought to take this Hemostan. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Hemostan can be taken.
Users%
Empty stomach2
100.0%


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Information checked by Dr. Sachin Kumar, MD Pharmacology

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