Monday, January 7, 2008

What kinds of operations are likely to cause massive bleeding?

Surgeries of the lung, heart, pancreas, prostate gland, uterus, spleen, kidney, breast cancer, etc., which often enhance fibrinolysis, are likely to cause massive bleeding.

Why does patient bleed easily during operation?

Because the fibrinolysis is accentuated by stress associated with invasive surgical procedure. There are a lot of stimuli such as anxiety, anesthesia, blood loss, irradiation, administration of anticancer drugs, etc. Those stimuli and various conditions such as weakness of the patient may combine to abnormal bleeding

What is the mechanism of the fibrinolytic system?

The fibrinolytic system is a physiological reaction that is invoked at the final stage of the hemostatic mechanism. It decomposes fibrin, the end product of the coagulation system, which is therefore called “fibrinolytic system”. There is plasminogen in the plasma, and it is converted to the active enzyme plasmin as often as required. Plasmin is a strong protease which effectively decomposes fibrin in blood. Plasminogen is activated by serine protease called plasminogen activator (PA). There are two types of plasminogen activator in the living body : urokinase PA (u-PA or UK) and tissue PA (t-PA). On the other hand, alpha 2 plasmin inhibitor (α 2-PI) and PA inhibitor (PAI) inhibit activation of plasmin and PA, respectively thus controlling activation of the fibrinolytic system.

What kinds of blood coagulation factors are there?

More than 10 kinds of blood coagulation factors are involved in coagulating blood. If any one of the coagulation factors dose not work well, it takes long before blood coagulates, or if it coagulates, the coagulation is not firm enough. Hemophilia, known as a typical disease with bleeding problems, is caused by factor VIII or factor IX deficiency.

What is the mechanism of blood coagulation?

When endothelial cells in a vessel are injured, platelets gather around the site (coagulation), adhere to each other changing their forms (adhesion), and block the broken vessel temporarily. This triggers blood coagulation. Injured endothelial cells and platelets act on blood coagulation factors in blood plasma, and fibrinogen transforms into filiform fibrins, causing blood coagulation. The process of blood coagulation is attributable to two types of actions : autogenous action mainly by constituents of blood and exogenous action associated with components in the injured tissue.

What is the mechanism of blood coagulation?

When endothelial cells in a vessel are injured, platelets gather around the site (coagulation), adhere to each other changing their forms (adhesion), and block the broken vessel temporarily. This triggers blood coagulation. Injured endothelial cells and platelets act on blood coagulation factors in blood plasma, and fibrinogen transforms into filiform fibrins, causing blood coagulation. The process of blood coagulation is attributable to two types of action: autogenous action mainly by constituents of blood and exogenous action associated with components in the injured tissue

What is the minimum amount of bleeding which may require blood transfusion?

A person may not have significant symptoms as long as the amount of bleeding is up to 15% of the circulating blood owing to the compensatory effect of the living body. When the amount of bleeding is 20% to 30%, it’s impact is significant and blood transfusion is required. It is said that hemorrhagic shock occurs in no time, when more than 30% of circulating blood is lost.

What is the blood volume of a human?

The blood volume of a human is one 13th of the body weight, that is, the blood volume (amount of circulating blood) of an adult is approximately 5 liters. 1 liter is in capillary vessels of the lung, 2 liters in vessels of the venous system, and 1 liter each in the heart, vessels of the arterial system, and capillary vessels.

What are precautions for administration of Transamin to patients with chronic renal failure?

Because Transamin is excreted via the kidney, care must be taken not to administer it at high doses for long periods. The drug has a wide range of doses, it should be administered to such patients at lower doses while observing patient’s conditions.

What are precautions for intravenous injection of Transamin?

It needs to be injected slowly in the same manner for injection of calcium preparations. Although Transamin is an easy-to-use drug which rarely entails adverse reactions, it may cause nausea, vomiting, or transient decrease in blood pressure when injected rapidly. If any of these adverse reactions occured, the injection should be discontinued to give the patient a rest. These adverse reactions are just transient ones and patients will recover from them soon. When the relationship between the incidence of nausea/vomitting and injection of Transamin was investigated using dog models, the injection speed had a larger influence on the incidence of nausea than the concentration of the drug. When 30 mg/kg of Transamin was intravenously injected into normal healthy dogs, there was no effect. When it was injected in a dose of 40 to 300 mg/kg, however, a vomitory effect was observed depending on the dose. It was found that induction of vomiting could be relieved by reducing the injection speed.

What is the initial dose of Transamin injection for bleeding?

The adequate dose of the drug is 10 to 30 mg per kilogram of body weight. Normally, 20 mg/kg is used. For example, the average dose of the drug for a patient who weighs 50 kg is 1,000 mg, but it can be increased according to the amount of bleeding.

Why is it necessary to administer Transamin before surgery?

Abnormal bleeding may occur suddenly during or after operation. Although Transamin is a quick-acting medicine for abnormal bleeding, it is administered before operation to prevent the risk of bleeding beforehand. Doctors used to administer hemostatic drugs after abnormal bleeding occured, but it is an old custom whose time has passed. As preoperative therapy, Transamin is often orally administered. When oral administration is not possible, the drug is injected.

What kinds of diseases are the main targets of Transamin?

Transamin is effective for systemic diseases and diseases possibly associated with the accentuation of local fibrinolysis.

Typical diseases or conditions which possibly enhance fibrinolysis

Transient accentuation of fibrinolysis

Injection of adrenalin, pyrogenic substances, stress, transfusion-associated shock, and surgery of the uterus, lung, pancreas, or prostate gland

Persistent accentuation of fibrinolysis

Liver cirrhosis, leukemia, aplastic anemia, thrombocytopenia, idiopathic renal hemorrhage, prostate cancer, prostatic hypertroph, systemic metastasis of cancer, pancreatic diseases, thyroid diseases, pneumonia, pulmonary suppuration, lung tumor, burn injury, and allergic reaction

Secondary accentuation of fibrinolysis

Early separation of the placenta, dead fetus in uterus, amniotic fluid embolism, acute promyelocytic leukemia, systemic metastasis of stomach cancer, purpura fulminans, thrombolytic purpura, and disseminated intravascular coagulation syndrome (DIC)

What kinds of diseases are the main targets of Transamin?

Transamin is effective for systemic diseases and diseases possibly associated with the accentuation of local fibrinolysis.

Typical diseases or conditions which possibly enhance fibrinolysis

Transient accentuation of fibrinolysis

Injection of adrenalin, pyrogenic substances, stress, transfusion-associated shock, and surgery of the uterus, lung, pancreas, or prostate gland

Persistent accentuation of fibrinolysis

Liver cirrhosis, leukemia, aplastic anemia, thrombocytopenia, idiopathic renal hemorrhage, prostate cancer, prostatic hypertroph, systemic metastasis of cancer, pancreatic diseases, thyroid diseases, pneumonia, pulmonary suppuration, lung tumor, burn injury, and allergic reaction

Secondary accentuation of fibrinolysis

Early separation of the placenta, dead fetus in uterus, amniotic fluid embolism, acute promyelocytic leukemia, systemic metastasis of stomach cancer, purpura fulminans, thrombolytic purpura, and disseminated intravascular coagulation syndrome (DIC)

What is the pharmacokinetic of Transamin after administration?

Pharmacokinetic parameters of Transamin after oral administration or injection are follows :

Tranexamic acid is rapidly absorbed when orally administered to healthy adult volunteers in a single dose of 250 or 500 mg, intramuscularly administered in a dose of 500 mg, or intravenously administered in a dose of 1,000 mg. Approximately 40 to 70% (when orally administered in a dose of 250 or 500 mg) or 80% and 76% (when intramuscularly administered in a dose of 500 mg and intravenously administered in a dose of 1,000 mg) respectively) of the drug are excreted into urine as unchanged compounds within 24 hours after administration.

How Transamin has the hemostatic effect?

Tranexamic acid firmly binds to the lysine binding site (LBS), which is the fibrin affinity site of plasmin or plasminogen, and prevents access of plasmin or plasminogen to the fibrin molecule. Therefore, degradation of fibrin by plasmin is strongly inhibited. Tranexamic acid is considered to stop bleeding by blocking the degradation of fibrin.

What is FDP?

FDP is an abbreviation of fibrinogen/fibrin degradation products. In the broad sense, it is a product of fibrinogen or fibrin decomposed by plasmin, which is a typical marker of accentuation of fibrinolysis. FDP is a generic name which covers primary fibrinolysis, i.e., fibrinogen degradation products (FgDP), and secondary fibrinolysis, i.e., degradation products derived from fibrin (FDP in a narrow sense). If the FDP value is high, the patient is suspected of having primary or secondary enhancement of fibrinolysis, disseminated intravascular coagulation syndrome (DIC), thrombosis, hemorrhage, malignant tumor, or megadoses of urokinase

What is oozing?

Oozing is exudative bleeding caused by accentuated fibrinolysis. It is said that oozing easily occurs when adhesions are lysed, cancerous lesions are removed, or organs such as the lung, kidney, liver, prostate gland, and uterus are removed. To treat oozing, firm pressure may be applied using gauze moistened with warm physiological saline. If fibrinolysis has progressed, however, bleeding does not stop and there will be the need for hemostatic agents. Although bleeding from thick vessels can be stopped using hemostatic forceps of ligation, administration of hemostatic agents may be required to stop bleeding from thin vessels, because it not only makes operative manipulations difficult prolonging the operation time, but also worsens patient’s general conditions increasing the outflow of blood.

What are symptoms of abnormal bleeding associated with hemorhagic diseases such as purpura, aplastic anemia, cancer, and leukemia?

Patients with hemorrhagic disease commonly develop purpura, epistaxis, and/or bleeding from the dental root. Other symptoms are coma, vomiting, shock, etc. caused by intracranial hemorrhage. There are also pain and swelling caused by hemorrhage of joint.

What should we do if a patient exhibits shock symptomps after administering Transamin?

Because all the reports on adverse reactions associated with Transamin have been made voluntarily or in foreign countries, its incidence is unknown. However, it is true that administration of Transamin may cause shock. If such an adverse reaction should occur, it is necessary to discontinue administration and take appropriate measures against shock symptoms.

What kinds of adverse reactions does Transamin involve?

Although the incidence of adverse reactions induced by Transamin is quite low, there are the following precautions on its use.
  • A Patient may complain of gastrointestinal discomfort or loss of appetite after orally taking Transamin. This adverse reaction can be resolved by reducing the dose or discontinuing the administration.
  • When Transamin is intravenously administered, if the injection speed is too fast, a transient decrease in blood pressure, bradycardia, or dizziness may result. The injection speed for Transamin should be as slow as for calcium preparations.

After administering hemocoagulase (Reptilase S), how long should we wait before administering tranexamic acid?

Although we searched for data on pharmacokinetics of Reptilase S, there was no such data. Because the possibility exist that a tendency to form thrombi may be induced when tranexamic acid is administered in combination with hemocoagulase at high doses, caution should be taken in this combination.

Can Transamin be used in combination with hemocoagulase (Reptilase S)?

The antiplasmin effect on tranexamic acid may make fibrin clots formed by hemocoagulase remain for a comparatively long time and make the occlusion persist further. Because the possibility exist that a tendency to form thrombi may be induced when it is administered in combination with hemocoagulase at high doses, caution should be taken in this combination.

Unlike injection drugs, oral drugs are often administered for long periods. Is it possible that it will cause thrombosis?

There is no fear of thrombosis because Transamin does not have action to enhance coagulation factors. When it is administered to patients who have thrombosis or in danger of developing it, such as those with cerebral thrombosis or myocardial infraction, however, caution should be exercised.

Are there any interactions when Transamin is used in combination with antibiotics?

No.

Are there any interactions when Transamin is used in combination with aspirin?

There is no interaction, because Transamin acts only on the fibrinolytic system and aspirin acts on platelets.

Please tell us about the pediatric doses of Transamin

The pediatric doses of Transamin Capsule and Tablet are as follows :

For age 0 to 1 years : 75 to 200 mg

For age 2 to 3 years : 150 to 350 mg

For age 4 to 6 years : 250 to 650 mg

For age 7 to 14 years : 400 to 1,000 mg

The pediatric doses of Transamin Injection are as follows

For age 1 year : 100 mg

For age 3 years : 150 mg

For age 7.5 years : 200 mg

For age 12 years : 250 mg

What is the optimum concentration of Transamin injection when it is prepared for intravenous infusion? Is it stable?

There have been a lot of reports that Transamin was diluted with 5% or 10% glucose. Although there are no data on the optimum concentration of Transamin, a dilution rate that is too low is not recommended, because the blood concentration needs to be maintained at a specified level. Transamin injection is a very stable drug.

Are there any data on the optimum dilution rate of Transamin for drip infusion?

There are no data on the optimum dilution rate of Transamin for drip infusion.

What kinds of urogical diseases are likely to involve bleeding?

There are bleeding disorders such as cystitis, urethritis, ureteral calculus, vesical calculus, and bladder cancer.

Anderson et al. studied the effect of treatment with Transamin on urinary tract bleeding in patients suffering various urological diseases. Transamin was given orally (500 mg or 1,000 mg three-times dailly) or by intravenously (10 mg/kg). The treatment of Transamin showed favorable effects in 71 patients with from lower urinary tract without evidence of abnormal fibrinolytic activity in the plasma, 11 patients with renal hematuria showing no generalized fibrinolysis, 87 patients with bleeding following prostatic surgery and 28 patients with generalized fibrinolysis. Abnormally high fibrinolytic activities in plasma in some patients were restored to normal values after oral (1.5 g) or intravenous (10 mg/kg) administration of Transamin.

Can it be administered to lactating women?

In Japan, tranexamic acid in the form of syrup is used, that is, it is administered to infants. Therefore, there is no problem regarding administration of the drug to lactating women. The concentration of the drug in milk is about 1/100 of that in blood. For example, when it is administered in a dose of 500 mg, its concentration in milk is about 0.06 μg/ml. If the milk consumption of a infant is 1 liter a day, the concentration is 60 μg at most. Because the daily dose of the drug for infants aged 1 and under is 75 to 200 mg, there is no problem.

Does Transamin have an impact on pregnancy? Are there any precautions for its use in pregnant women?

Among drugs to be used for pregnant women, hemostatic drugs tend to be used frequently. Although tranexamic acid is a kind of drug that rarely involves adverse reactions, rapid intravenous infusion should be avoided, because the possibility exists that a change in the ECG or significant decrease in blood pressure may occur.

At the present, there is no particular report on disorder associated with tranexamic acid. Therefore, it is speculated that the use of tranexamic acid (antiplasmin drug) during pregnancy does not have a great influence on fetuses. However, it is recommended that caution should be exercised in its use during beginning pregnancy just in case.

Does Transamin have an impact on menstruation (delay or the amount of bleeding)?

Because the mechanism of menstruation is closely related to the fibrinolytic system of the uterine endometrium, it is possible that Transamin decreases the amount of bleeding, but it is likely that it will delay menstruation.

What is the dosage/administation of Transamin when used for treatment of dysfunctional uterine bleeding?

One or two Transamin Tablets (250 mg) are administered 3 to 4 times a day.

It is effective to intravenously inject 5 ml of 5% Transamin Injections at the time of visit. Among dysfuctional uterine bleedings involving ovulations is hypermenorrhea. Many of patients with hypermenorrhea. Many of patients with hypermenorrhea are women aged 35 to 45. Transamin is effective in decreasing the amount of bleeding in such patients. Transamin dose not entail any adverse reaction that will inhibit ovulation. For treatment of hypermenorrhea, Transamin is administrered from the first day of each menstrual period for 5 to 7 days.

What is dysfunctional uterine bleeding (DUB)?

Dysfunctional uterine bleeding means irregular or excessive bleeding during a menstrual or intermenstrual period.

It is dysfunctional uterine bleeding without any organic abnormalities such as pregnancy, tumor, and inflammation. The causes of dysfunctional uterine bleeding are complicated. It is also classified into cyclic ovulation bleeding and cyclic anovulatory bleeding. It is said that many of patients with cyclic anovulatory bleeding are younger or postmenopausal women.

In the light of findings in endometrial tissues, when an ovarian follicle exists without ovulating, secretion of estrogen is maintained, which is followed by bleeding caused by thickening of the uterine endometrium. This type of bleeding is regarded as dysfunctional uterine bleeding. When dysfuctional uterine bleeding occurs, enhancement of fibrinolytic phenomena in the uterine endometrium, especially an increase in plasminogen activators, is noted. As medication for dysfunctional uterine bleeding, hormone pills (estrogenic hormon, corpus luteum hormone, and ambisextrous hormone) and antiplasmin drugs (epsilon and transamin) are used.

What is atypical genital bleeding?

Atypical genital bleeding means irregular genital bleeding which has no relationship with menstruation. Except for intermenstrual bleeding (ovulation bleeding), most of atypical genital bleedings are pathologic ones. In the field of obstetrics and gynecology, atypical genital bleeding is the chief complaint that is most frequently seen. For diagnosis of such bleedings, it is important to locate the site of bleeding and identify the underlying cause. In general, it is recommended that atypical genital bleedings should be classified into two types: gynecological bleeding which has no relationship with pregnancy and obstetric bleeding associated with pregnancy.

What is the minimum amount of bleeding during a delivery that is treated as abnormal bleeding?

The amount of bleeding during a delivery mainly means the total amount of bleeding during the period from a delivery to 2 hours after that. In general, when the amount of bleeding is 500 ml or more, it is defined as abnormal bleeding.

During a delivery, bleeding occurs from the separation of the placenta and from the injured area of soft birth canal. The greater part of the bleeding is from the separation of the placenta. Because there are plenty of plasminogen activators associated with fibrinolysis in the uterus, Transamin, an antiplasminic agent that inhibits the action of the plasminogen activators, is effective.

Major treatments for afterbirth bleeding (third stage of labor) are classified into two types : mechanical, surgical method and pharmacological, medical method. Among pharmacological, medical treatments are administration of a uterotonic (quick-acting), administration of a hemostatic agent, and blood transfusion. Uterotonic agents have a strong hemostatic effect and used routinely.

Oral administration of Transamin before childbirth or intravenous injection of Transamin immediately before the third stage of labor is effective in inhibiting the amount of bleeding and preventing abnormal bleeding.

What kinds of hemorrhages are most frequently seen in the field of obstetrics and gynecology?

Bleeding from the female productive organs is most frequently seen. Because abnormal bleeding during childbirth is often associated with great loss of blood, caution must be exercised. It is said that many of hemorrhages in the field of gynecology are caused by a disorder of physiological functions such as dysfunctional uterine bleeding (DUB) and menorrhagia.

Does Transamin contain materials derived from cows?

Some of hemostatic drugs use materials derived from cows. Up to the present, there is no report that a human is infected with BSE through drugs, etc. in Japan and other countries. In April of 1996, a notification from the Japanese government invited people’s attention to BSF, based on the incidence of BSE in England

Hemostatic drugs containing materials derived from cows

Aprotinin, thrombin, gelatin, collagen, etc.

Unlike these drugs, tranexamic acid, as an igredient of Transamin, is completely free from materials derived from cows.

Can Transamin be used in patients with DIC?

As a rule, the use of Transamin in patients with DIC is contraindicated. From a practical standpoint, however, it is not rare that secondary fibrinolysis occurs as an excessive response, which worsens bleeding or can even endanger patient’s life. To save patients from the life-threating situation caused by bleeding, there may be no choice but to use an antiplasminic agent.

In this case, Transamin is used until bleeding stops, and administration is discontinued as soon as possible after bleeding has stopped. This will minimize tissue damage in the kidney and other organs resulting from intravascular coagulation.

What is DIC?

DIC stands for disseminated intravascular coagulation syndrome or diffuse intravascular coagulation syndrome. It is a sign of bleeding susequent to unadjustable activation of coagulatio factors and fibrinolytic enzymes in small vessels. When DIC occurs, fibrin deposits, and fibrinogen, prothrombin, coagulation factors (Factors V, VIII, XIII), and platelets are consumed in the process of coagulation. Fibrin degradatin products inhibit polumerization of fibrin, which results in tissue necrosis and bleeding.

Are there any data on percutaneous absorption of Transamin?

The absorbtion of Transamin into normal skin is very slow. It is slightly better for the skin from which the horny layer has been peeled off. Wheen Transamin at a concentratio of 96 mg/ml was applied on guinea pigs to examine its percutaneous absorption, the following results were obtained.

How is Transamin used for patients undergoing cardiac surgery with cardiopulmonary bypass?

Patients undergoing cardiac surgery with cardiopulmonary bypass (CPB) are at high risk for postoperative bleeding. Excessive bleeding after CPB is attributable not only to the size of surgical wound required for the operation but also the activation of both coagulation and fibrinolysis by the passage of blood through the CPB bypass. The stimulation of the formation and dissolution of blood clots causes excessive consumption of coagulant factors and predisposes patients to prolonged and excessive bleeding. The severe bleeding complication increases morbidity and mortality and also the need for transfusion, reoperation and costs.

Nakashima et al. evaluated the effect of Transamin on blood loss after CPB in 157 patients who underwent elective valve replacement operations. Transamin was administered in 90 patients (Group TA) at 50 mg/kg just before and after CPB, and every minute during CPB. Remaining 67 patients serve as the control group (Group N). The time required for hemostasis was significantly shorter in Group TA (6.7 + 1.5 hr vs. 6.0 + 1.5 hr, p – 0.006). The amount of chest tube drainage within 12 hr after surgery was significantly reduced and the chest tube could be removed earlier in Grout TA. The total blood loss was significantly smaller than in Group TA (402 + 292 ml) than in Group N (631 + 609 ml, p = 0.003). It was concluded that antifibrinolytic therapy during CPB with Transamin reduces postoperative loss, and shortens the operation time due to an improvement in hemostasis.

What is the dose of Transamin when used to stop bleeding associated with tonsillectomy in pediatric patients?

One of major problems that arise after tonsillectomy is rebleeding. It is recommended that Transamin be used for adults in the following doses. When it is administered to children, the dose is reduced according to the age, etc.

2 hours before operation :

500 mg, intravenous injection

1 day after operation :

250 mg, every 4 hours

2 to 4 days after operation :

500 mg, 3 times a day, oral administration

How is Transamin used for treatment of gastric bleeding?

Upper Gastrointestinal Bleeding has been observed that gastric mucosa is rich in plasminogen activator and fibrinolytic activity is high in gastric venous blood. Therefore, it seems to be rationale to use fibrinolytic drugs in the management of bleeding from gastrointestinal lesion.

Henry et al. performed a meta-analysis fo six randomized double-blind placebo controlled trials from UK, Sweden and Australia which investigated the effect of fibrinolytic inhibitors in 1,267 patients in total with upper gastrointestinal bleeding. Most patients were bleeding from peptic ulcers in the stomach and duodenum (43 – 88%) or gastric erosions (4 – 23 %). Transamin 3 – 6 g/day given intravenously for 2 or 3 days followed by 3 – 6 g/day orally for a further 3 to 5 days (four trials) or 4.5 – 12 g/day orally for 2 to 7 days (two trials). Treatment with Transamin was associated with a 20 – 30% reduction in the rate of rebleeding, and a 40% reduction (95% confidence interval 10 – 60 %) in mortality. From the meta-analysis, it was concluded that Transamin might be of value to patients considered to be at risk of dying after an upper gastrointestinal hemorrhage.

Except for pulmonary tubercolosis, what kinds of diseases are the targets of Transamin?

Bleeding from lung cancer (most frequently seen), pneumonia, bronchitis, or severe inflammation of upper respiratory tract.

How is Transamin used for treatment of pulmonary tuberculosis?

Sato et al. administered Transamin to 34 patients with pneumonia, bronchial ectasia, or pulmonary tuberculosis who had bloody sputum or hemoptysis, at a minimum maintenance dose of 250 mg, 3 times a day, to investigate the hemostatic effect of Transamin. The dose was increased to 1,500 mg per day when the amount of bloody sputum was large. Administration of Transamin stopped bleeding in 30 patients (88.2%). In 2 patients (5.9%), bleeding was stopped when the drug was administered, but bloody sputum recurred after a while. In the other 2 patients (5,9%), the drug had almost no effect. The drug can be administered without anxiety about adverse reactions. It is administered at a high dose at early stages, and after bleeding has stopped, the dose is reduced gradually until the administration is discontinued. When it is administered as a preventative treatment from 3 to 4 days before a period in which patients easily have bloody sputum, such as a menstrual period, when a typhoon is approaching, or flu season, it sometimes happens that patients do not have bloody sputum at all.

Sunday, January 6, 2008

What is the dose of Transamin when used for treatment of bleeding associated with the removal of prostate gland or ureteral calculus?

2 hours prior to operation :

500 mg, intravenous injection

1 day after operation :

250 mg, every 4 hours

2 to 4 days after operation :

500 mg, oral administration, 3 times a day

Transamin

Transamin (Tranexamic Acid) is often prescribed for excessive bleeding. It is an antifibrinolytic that competitively inhibits the activation of plasminogen to plasmin, a molecule responsible for the degradation of fibrin. Fibrin is the basic framework for the formation of a blood clot in hemostasis. It has roughly 8 times the antifibrinolytic activity of an older analogue, ε-aminoacaproic acid.

Therapeutic Uses of Transamin

Menstrual bleeding

Transamin is a synthetic derivative of the amino acid lysine. It exerts its antifibrinolytic effect through the reversible blockade of lysine binding sites on plasminogen molecules. It inhibits endometrial plasminogen activator and thus prevents fibrinolysis and the breakdown of clot. Side effects are uncommon. While prolonged treatment may heighten the risk of an increased thrombotic tendency, such as deep vein thrombosis, large scale studies reveal that the incidence of thrombosis in women treated by Transamin is no different from the spontaneous incidence of thrombosis in women.

Transamin is used as firstline nonhormonal treatment of dysfunctional uterine bleeding, and heavy bleeding associated with uterine fibroids.

Haemophilia

Transamin is also useful in the treatment of bleeding as a second line treatment next to factor VIII in haemophilia patients (i.e. Tooth extraction in haemophilia patients.)

Angioedema

In acquired angioedema types I and II and non-histaminergic angioedema, antifibrinolytics such as Transamin may be effective.

Cardiac surgery

Transamin is used in cardiac surgery, e.g. coronary artery bypass surgery, to prevent excessive blood loss.


Orthopedic Surgery


Transamin is used in orthopedic surgery to reduce bloodloss. It is of proven value in clearing the field of surgery and reducing per and postoperative blood loss. Drain and number of transfusion is reduced. However the hidden blood loss is not reduced. Still it is becoming an important tool in the anaesthetist’s arsenal. It is commonly used in joint replacement surgery.