Tranexamic acid

Tranexamic acid is an Antihemorrhagic agent belonging to the pharmacological class of Antifibrinolytics.

Tranexamic acid has been approved to relieve symptoms and also for the treatment and maintenance of Nonacute Abnormal Uterine Bleeding, Dental Procedures for Patients on Oral Anticoagulant Therapy, Treatment of Hemoptysis, Long-term Prophylaxis for Hereditary Angioedema, Management of Epistaxis or Bleeding in Hereditary Hemorrhagic Telangiectasia, Intracranial Hemorrhage in the Setting of Thrombolytic Treatment, Perioperative Prevention of Blood Loss and Transfusion, Prevention of Postpartum Hemorrhage, Treatment of Postpartum Hemorrhage, Tooth Extraction in Patients with Hemostatic Defects, Management of Trauma-Associated Hemorrhage or Traumatic Brain Injury.

In humans, tranexamic acid is taken orally and has a bioavailability of around 30-50% of the amount ingested. Its absorption is not affected by food intake. The initial volume of distribution of tranexamic acid is 0.18 L/kg and the steady-state volume is 0.39 L/kg. The drug is distributed into the cerebrospinal fluid and aqueous humor of the eye at concentrations around 1/10th of typical plasma levels. The metabolism of tranexamic acid is not well understood, but it does not seem to play a significant role in drug elimination. Only a small portion (about 1% and 0.5%) of an orally administered dose is excreted as a dicarboxylic acid and an acetylated metabolite, respectively. Urinary excretion is the primary route of elimination, with over 95% of the administered dose excreted unchanged in the urine. The rate of excretion depends on the route of administration, with around 90% of an intravenously administered dose being excreted within 24 hours, while only 39% of an orally administered dose is excreted within the same time frame.

The common side effects of Tranexamic acid include Nausea, Diarrhea, Vomiting, Headache, Dizziness, Fatigue, Muscle pain, Joint pain, Nasal stuffiness or runny nose, Changes in color vision.

Tranexamic acid is available in the form of Tablets, Injectable Solutions.

Tranexamic acid is approved in Germany, Japan, Malaysia, India, the U.K., the U.S., and China.

Tranexamic acid, belonging to the pharmacological class of Antifibrinolytics, acts as an Antihemorrhagic agent.

Tranexamic acid exerts its inhibitory effect on plasminogen activation through competitive and reversible binding at various sites, including four or five low-affinity sites and one high-affinity site. The high-affinity site, specifically involved in its binding to fibrin, plays a crucial role in the process of fibrinolysis. By occupying these essential binding sites, tranexamic acid hinders the dissolution of fibrin, leading to clot stabilization and prevention of haemorrhage.

Tranexamic acid has been approved to relieve symptoms and also for the treatment and maintenance of Nonacute Abnormal Uterine Bleeding, Dental Procedures for Patients on Oral Anticoagulant Therapy, Treatment of Hemoptysis, Long-term Prophylaxis for Hereditary Angioedema, Management of Epistaxis or Bleeding in Hereditary Hemorrhagic Telangiectasia, Intracranial Hemorrhage in the Setting of Thrombolytic Treatment, Perioperative Prevention of Blood Loss and Transfusion, Prevention of Postpartum Hemorrhage, Treatment of Postpartum Hemorrhage, Tooth Extraction in Patients with Hemostatic Defects, Management of Trauma-Associated Hemorrhage or Traumatic Brain Injury.

After administering multiple oral doses of Tranexamic acid (1300 mg three times daily for five days), the maximum plasma concentration (Cmax) of the drug was measured at 16.41 mcg/mL, and it reached its peak time (Tmax) of 2.5 hours.

Tranexamic acid is found to be available in the form of Tablets, Injectable Solutions.

Tranexamic acid can be used in the following treatment:

• Nonacute Abnormal Uterine Bleeding
• Dental Procedures for Patients on Oral Anticoagulant Therapy
• Treatment of Hemoptysis
• Long-term Prophylaxis for Hereditary Angioedema
• Management of Epistaxis or Bleeding in Hereditary Hemorrhagic Telangiectasia
• Intracranial Hemorrhage in the Setting of Thrombolytic Treatment
• Perioperative Prevention of Blood Loss and Transfusion
• Prevention of Postpartum Hemorrhage
• Treatment of Postpartum Hemorrhage
• Tooth Extraction in Patients with Hemostatic Defects
• Management of Trauma-Associated Hemorrhage or Traumatic Brain Injury

Tranexamic acid can help to relieve symptoms and also for the treatment and maintenance of Nonacute Abnormal Uterine Bleeding, Dental Procedures for Patients on Oral Anticoagulant Therapy, Treatment of Hemoptysis, Long-term Prophylaxis for Hereditary Angioedema, Management of Epistaxis or Bleeding in Hereditary Hemorrhagic Telangiectasia, Intracranial Hemorrhage in the Setting of Thrombolytic Treatment, Perioperative Prevention of Blood Loss and Transfusion, Prevention of Postpartum Hemorrhage, Treatment of Postpartum Hemorrhage, Tooth Extraction in Patients with Hemostatic Defects, Management of Trauma-Associated Hemorrhage or Traumatic Brain Injury.

Tranexamic acid is approved for use in the following clinical indications:

• Nonacute Abnormal Uterine Bleeding
• Dental Procedures for Patients on Oral Anticoagulant Therapy
• Treatment of Hemoptysis
• Long-term Prophylaxis for Hereditary Angioedema
• Management of Epistaxis or Bleeding in Hereditary Hemorrhagic Telangiectasia
• Intracranial Hemorrhage in the Setting of Thrombolytic Treatment
• Perioperative Prevention of Blood Loss and Transfusion
• Prevention of Postpartum Hemorrhage
• Treatment of Postpartum Hemorrhage
• Tooth Extraction in Patients with Hemostatic Defects
• Management of Trauma-Associated Hemorrhage or Traumatic Brain Injury

1. Abnormal Uterine Bleeding, Nonacute:
1. Lysteda Oral Tablets: 1.3 g 3 times daily for up to 5 days during monthly menstruation.
2. Tranexamic acid [Canadian product] Oral Tablets: 1 to 1.5 g three to four times daily for up to 5 days during menstruation.
2. Dental Procedures in Patients on Oral Anticoagulant Therapy (Off-label use):
1. Oral Rinse (5% solution): Administer 5 to 10 minutes prior to the procedure, rinse mouth for 2 minutes, repeat 2 to 4 times daily for 1 to 2 days after the procedure.
3. Hemoptysis, Treatment (Off-label use):
1. Inhalation for Nebulization: 500 mg (using injectable solution) 3 times daily for up to 5 days.
4. Hereditary Angioedema, Long-term Prophylaxis (Alternative agent, Off-label use):
1. Oral: Initial dose of 500 to 650 mg two to three times daily, titrate gradually based on response and tolerability, usual daily dose: 3 g/day.
5. Hereditary Hemorrhagic Telangiectasia, Epistaxis, or Other Bleeding Sites (Alternative agent, Off-label use):
1. Oral: Initial dose of 1.5 g twice daily or 1 g three times daily for four to tendays; adjust dose as needed to a usual daily dose of 2 to 4.5 g in 2 or 3 divided doses.
6. Intracranial haemorrhage Associated with Thrombolytic Treatment (Alternative agent, Off-label use):
1. IV: 1 g (or 10 to 15 mg/kg) once, administered at a rate not to exceed 100 mg/minute.
7. Perioperative Prevention of Blood Loss and Transfusion:
1. IV: Usual dose of 1 g (or 10 to 30 mg/kg) prior to the procedure, administered at a rate not to exceed 100 mg/minute.
8. Postpartum Hemorrhage, Prevention (Adjunctive agent, Off-label use):
1. IV: 1 g (or 10 to 15 mg/kg) over 10 to 20 minutes may administer before skin incision for cesarean deliveries and after cord clamping for vaginal deliveries.
9. Postpartum Hemorrhage, Treatment (Adjunctive agent, Off-label use):
1. IV: 1 g over 10 to 20 minutes given within threee hours of vaginal birth or cesarean delivery.
10. Tooth Extraction in Patients with Hemostatic Defects (Adjunctive agent):

IV: 10 mg/kg using actual body weight, administered ~2 hours before the procedure at a rate not to exceed 100 mg/minute, then 10 mg/kg three to four times daily for 2 to 8 days.

Oral: 25 mg/kg given 2 hours prior to the procedure, then 25 mg/kg 3 to 4 times daily for up to 7 to 10 days.

Trauma-Associated Hemorrhage or Traumatic Brain Injury (Off-label use):

IV: Loading dose of 1 g over 10 minutes started within 3 hours of injury, followed by 1 g over the next eight hours as a continuous infusion.

Tranexamic acid is available in the following dosage forms and strengths:

Tablets 250 mg 500mg 650 mg and 1.3 g injection 100mg/ml.

Tablets, Injectable Solutions.

• Dosage Adjustments in Kidney Patients:

Patients with renal impairment need to have their tranexamic acid dosage adjusted to avoid drug accumulation. The dosage adjustments required may vary depending on the severity of the impairment, so it is important to seek personalized dosing recommendations from a healthcare professional. Typically, for individuals with moderate to severe renal impairment (creatinine clearance <50 mL/min), the tranexamic acid dose should be reduced.

• Dosage Adjustments in Hepatic Impairment Patients:

There are found to be no dosage adjustments in the manufacturer's labelling.

• Dosage Adjustments in Pediatric Patients:

Treatment of Diffuse Alveolar Hemorrhage (intractable):

• Children ≤25 kg: Inhaled: 250 mg every 6 hours for 3 to 4 doses (18 to 24 hours); if a response occurs, continue treatment for another 2 to 3 doses after bleeding completely stops; if no or minimal response or bleeding worsens, add inhaled recombinant factor VIIa; maximum duration of inhaled therapy: 3 days.
• Children >25 kg and Adolescents: Inhaled: 500 mg inhaled every 6 hours for 3 to 4 doses (18 to 24 hours); if response occurs, continue treatment for another 2 to 3 doses after bleeding completely stops; if no or minimal response or bleeding worsens, add inhaled recombinant factor VIIa; maximum duration of inhaled therapy: 3 days.

Hereditary Angioedema (HAE) Prophylaxis:

• Long-term prophylaxis: Children and Adolescents: Oral: 20 to 50 mg/kg/day in 2 to 3 divided doses; doses up to 75 mg/kg/day have been reported; maximum daily dose range: 3,000 to 6,000 mg/day; may consider alternate-day regimen or twice-weekly regimen when the frequency of attacks reduces.

Prevention of Bleeding Associated with Tooth Extraction in Hemophilic Patients:

• Infants, Children, and Adolescents: IV: 10 mg/kg immediately before surgery, then 10 mg/kg/dose 3 to 4 times daily for 2 to 8 days.

Prevention of Perioperative Bleeding:

• General dosing (non-cardiac): Infants, Children, and Adolescents: IV: Loading dose: 10 to 30 mg/kg followed by a continuous IV infusion at 5 to 10 mg/kg/hour.
• Cardiac surgery with cardiopulmonary bypass: Infants, Children, and Adolescents: Various dosing regimens based on weight, ranging from low dose to high dose, depending on the target serum concentration.

Trauma, Hemorrhagic (Acute Traumatic Coagulopathy):

• Children <12 years: IV: Loading dose: 15 mg/kg over 10 minutes given within 3 hours of injury (maximum dose: 1,000 mg/dose), followed by continuous IV infusion at 2 mg/kg/hour for ≥8 hours or until the bleeding stops.
• Children ≥12 years and Adolescents: IV: Loading dose: 1,000 mg over 10 minutes given within 3 hours of injury, followed by 1,000 mg infused over 8 hours.

Traumatic Hyphema:

• Children and Adolescents: Oral: 25 mg/kg/dose every 8 hours for 5 to 7 days. Note: This regimen may also be used for secondary haemorrhage after an initial traumatic hyphema event.

There are no specific dietary requirements for tranexamic acid. It is typically prescribed as a medication and is not affected by food intake.

Tranexamic acid may be contraindicated under the following conditions:

• Intrathecal and Epidural Administration: Avoid administering tranexamic acid intrathecally or epidurally.
• History or Risk of Thrombosis: Patients with a history or risk of thrombosis should not receive Tranexamic acid unless concomitant treatment with anticoagulants is possible.
• Acquired Disturbances of Color Vision: It is advised that Tranexamic acid should not be given to patients with acquired disturbances of color vision. If visual disturbances occur during treatment, discontinue the use of the medication.
• Active Thromboembolic Disease: Patients with active thromboembolic conditions like deep vein thrombosis, pulmonary embolism, and cerebral thrombosis should not use Tranexamic acid.
• Subarachnoid Hemorrhage: Limited clinical experience suggests that the reduced risk of re-bleeding is offset by an increased rate of cerebral ischemia in patients with subarachnoid haemorrhage.
• Haematuria: Caution is advised in patients with haematuria (blood in urine).
• Hypersensitivity: Tranexamic acid is contraindicated in patients who are hypersensitive to tranexamic acid or any ingredient in the formulation, including non-medicinal ingredients or container components.

1. Visual Disturbances: Be aware of potential visual impairment, blurred vision, and impaired colour vision with tranexamic acid usage. Regular ophthalmic check-ups are advisable during prolonged treatment.
2. Irregular Menstrual Bleeding: Do not use tranexamic acid if experiencing irregular menstrual bleeding until the cause is determined.
3. Menstrual Bleeding Reduction: Consult a doctor if menstrual bleeding is not reduced after three menstrual cycles. Consider alternative treatments if tranexamic acid is ineffective.
4. Thrombosis Risk: Exercise caution in patients at high risk for thrombosis, such as those with a history of thromboembolic events or family history. Use tranexamic acid only if medically necessary and under strict medical supervision.
5. DIC Management: Patients with disseminated intravascular coagulation (DIC) requiring tranexamic acid should be closely monitored by experienced physicians.
6. Haematuria Caused by Renal Parenchymal Diseases: Avoid tranexamic acid therapy in cases of haematuria from renal parenchymal diseases, as it may worsen the condition.
7. Convulsions: Be aware of possible convulsions associated with tranexamic acid treatment.
8. Hormonal Contraceptives: Exercise caution when using hormonal contraception concurrently with tranexamic acid due to potential increased thrombotic risk. Weigh the benefit of treatment against the risk of thrombotic events.
9. Renal Insufficiency: Use caution in patients with renal insufficiency to prevent drug accumulation.
10. Pronounced Haematuria from Upper Urinary Tract: Monitor patients with pronounced haematuria from the upper urinary tract, as obstruction may occur in isolated cases.
11. Specific Patient Populations: Obese and diabetic patients, those with polycystic ovary syndrome or a history of endometrial cancer in a first-degree relative, and women receiving unopposed estrogen or tamoxifen should consult a doctor before starting tranexamic acid treatment. Consider individual risks and benefits in these cases.

Alcohol can sometimes interact with certain medications, affecting their effectiveness or causing adverse effects. Additionally, alcohol may exacerbate certain medical conditions that tranexamic acid is prescribed for, such as blood clotting disorders.

Tranexamic acid is excreted in breast milk at a concentration approximately one hundredth of the levels found in the mother's serum.

Published literature confirms the presence of tranexamic acid in human milk. However, there is currently a lack of data regarding the specific effects of tranexamic acid on the breastfed child or its impact on milk production. It is essential to consider the developmental and health benefits of breastfeeding while also taking into account the mother's clinical requirement for tranexamic acid and any potential adverse effects it may have on the breastfed child, either directly from the medication or due to the underlying maternal condition.

Pregnancy:

Pregnancy category B:

Tranexamic acid crosses the placenta barrier, reaching similar concentrations in the cord blood as in the maternal blood after intravenous injection of 10 mg/kg to pregnant women.

Neonates have a high fibrinolytic activity, and it is uncertain whether reducing this activity in the first hours of life is harmful. However, experienced researchers have not observed any negative effects on infants following the use of tranexamic acid in connection with childbirth.

When considering the use of tranexamic acid during pregnancy, the potential risk to the fetus should always be weighed against the mother's clinical need for the medication.Before making any decisions, the doctor in charge of treatment should perform a thorough risk and benefit

assessment. Currently, there is no conclusive evidence from published studies, case series, or reports on the use of tranexamic acid in pregnant women during the second and third trimesters or at the time of delivery that suggests any risk of miscarriage or adverse outcomes for either the mother or the fetus. Although there have been some cases of fetal structural abnormalities leading to newborn death after administering tranexamic acid during conception or the first trimester, other factors make it difficult to determine the actual risk of major birth defects.

Although some clinical studies have shown potential issues in fetuses and infants exposed to tranexamic acid during pregnancy, such as low Apgar scores, neonatal sepsis, cephalohematoma, and changes in growth,

there have been cases where the use of tranexamic acid has resulted in positive outcomes. For instance, one woman with fibrinolytic bleeding in the fourth month of pregnancy was treated with tranexamic acid for 64 days, leading to a normal delivery and a healthy baby. Another case involved the successful prevention of placental abruption with tranexamic acid, resulting in a healthy baby delivered by Caesarean section.

It's important to note that the general human population's estimated background risk for major birth defects and miscarriage is unknown, and every pregnancy carries some inherent risk of adverse outcomes.

There are no specific food warnings related to the use of tranexamic acid in the United States. Tranexamic acid is typically taken as an oral medication or administered intravenously for certain medical conditions. It is not known to have any significant interactions with food or dietary restrictions.

The adverse reactions related to Tranexamic acid can be categorized as follows:

Common:

• Nausea
• Diarrhea
• Vomiting
• Headache
• Dizziness
• Fatigue
• Muscle pain
• Joint pain

Less common:

• Nasal stuffiness or runny nose
• Changes in color vision

Rare:

• Allergic reactions such as rash, itching, swelling, severe dizziness, difficulty breathing.
• Blood clots
• Seizures
• Visual disturbances (blurred or double vision)
• Chest pain or pressure
• Shortness of breath
• Unusual bruising or bleeding (including in urine or stools)

The clinically relevant drug interactions of Tranexamic acid is briefly summarized here:

There have been no conducted studies on interactions between tranexamic acid and other drugs. Due to this lack of interaction data, simultaneous treatment with anticoagulants should only occur under the strict supervision of a physician experienced in this field.

There is a possibility of potential drug-drug interactions leading to myocardial infarction when coadministered with hormonal contraceptives, hydrochlorothiazide, desmopressin, sulbactam-ampicillin, carbazochrome, ranitidine, or nitroglycerin.

As tranexamic acid is an antifibrinolytic, the simultaneous use of hormonal contraception and tranexamic acid could potentially exacerbate the increased thrombotic risk associated with combination hormonal contraceptives. Therefore, caution should be exercised in such cases, and appropriate medical advice should be sought.

The following are the side effects involving Tranexamic acid:

• Nausea
• Diarrhea
• Vomiting
• Headache
• Dizziness
• Fatigue
• Muscle pain
• Joint pain
• Nasal stuffiness or runny nose
• Changes in color vision

The use of Tranexamic acid should be prudent in the following group of special populations:

Pregnancy:

Pregnancy category B:

Tranexamic acid crosses the placenta barrier, reaching similar concentrations in the cord blood as in the maternal blood after intravenous injection of 10 mg/kg to pregnant women.

Neonates have a high fibrinolytic activity, and it is uncertain whether reducing this activity in the first hours of life is harmful. However, experienced researchers have not observed any negative effects on infants following the use of tranexamic acid in connection with childbirth.

When considering the use of tranexamic acid during pregnancy, the potential risk to the fetus should always be weighed against the mother's clinical need for the medication. The treating physician should conduct a thorough risk-benefit evaluation to make informed decisions.

Data from published studies, case series, and reports on tranexamic acid use in pregnant women in the second and third trimesters and at the time of delivery have not definitively determined whether there is a drug-associated risk of miscarriage or adverse maternal or the fetal outcomes. While there have been instances of fetal structural abnormalities leading to newborn death after tranexamic acid administration during conception or the first trimester, other confounding factors make the actual risk of major birth defects unclear.

Some clinical studies have reported functional issues in fetuses and infants exposed to tranexamic acid in utero, such as low Apgar scores, neonatal sepsis, cephalohematoma, and alterations to growth, including low birth weight and preterm birth at 22-36 weeks of gestation.

In specific cases, tranexamic acid was used during pregnancy with positive outcomes. One case involved a woman with fibrinolytic bleeding in the fourth month of pregnancy, treated with tranexamic acid for 64 days, resulting in a normal delivery and a healthy infant. Another case described the successful prevention of placental abruption through the administration of tranexamic acid, leading to a healthy baby delivered by Caesarean section.

The estimated background risk for the major birth defects and miscarriage in the general human population is unknown. It is essential to recognize that all pregnancies carry some level of inherent risk of birth defects, loss, or other adverse outcomes.

Lactation

Tranexamic acid is excreted in breast milk at a concentration approximately one hundredth of the levels found in the mother's serum.

Published literature confirms the presence of tranexamic acid in human milk. However, there is currently a lack of data regarding the specific effects of tranexamic acid on the breastfed child or its impact on milk production. It is essential to consider the developmental and health benefits of breastfeeding while also taking into account the mother's clinical requirement for tranexamic acid and any potential adverse effects it may have on the breastfed child, either directly from the medication or due to the underlying maternal condition.

Pediatric

Health Canada has reviewed the submitted data and established the safety and efficacy of Tranexamic acid for pediatric patients in the treatment of hereditary angioneurotic oedema and increased local fibrinolysis when hyperfibrinolysis is diagnosed. Specific data is available for surgical patients undergoing cardiac and orthopedic surgeries. As a result, Health Canada has granted authorization for the use of Tranexamic acid in these indications for pediatric patients.

However, for menorrhagia (hypermenorrhea), there is limited data available to Health Canada. Clinical experience with Tranexamic acid in children under 18 years of age with menorrhagic (hypermenorrhea) is not available. Therefore, Health Canada has not authorized Tranexamic acid for pediatric use in this indication.

Geriatric Use

The clinical trials involving Tranexamic acid did not enroll enough participants aged 65 and above to establish if they exhibit different responses compared to younger subjects. However, other clinical observations have not revealed any notable differences in the reactions between elderly and younger patients. When prescribing for elderly individuals, it is advisable to exercise caution in dose selection, typically initiating treatment at the lower end of the dosing range. This approach takes into account the higher occurrence of reduced hepatic, renal, or cardiac function, as well as the potential for concomitant diseases or drug therapies in this age group.

The physician should be vigilant about the knowledge pertaining to the identification and treatment of overdosage of Tranexamic acid.

There have been no reported cases of overdosage of Tranexamic acid in humans. If an overdose were to occur, potential symptoms may include nausea, diarrhea, dizziness, headache, convulsions, vomiting, orthostatic symptoms, and hypotension. In such a situation, treatment would involve inducing vomiting, performing gastric lavage, administering charcoal therapy, and providing symptomatic care. Maintaining sufficient diuresis is also important.

An incident involving a seventeen-year-old showed that mild intoxication occurred after the ingestion of 37 g of tranexamic acid. Gastric lavage was performed in this case to address the situation.

Pharmacodynamics:

Tranexamic acid is a medication that prevents the activation of plasminogen to plasmin, which is involved in the breakdown of blood clots. It works as an competitive inhibitor of plasminogen and as a noncompetitive inhibitor of plasmin at higher concentrations. Another similar medication is aminocaproic acid, which is less potent than tranexamic acid. However, tranexamic acid has a stronger binding to both strong and weak receptor sites of the plasminogen molecule, which makes it more potent. In patients with hereditary angioedema, tranexamic acid can help prevent attacks by reducing plasmin-induced activation of the first complement protein (C1).

However, it's worth noting that off-target antagonism of GABA(A) receptors may lead to the development of convulsions and hyperexcitability after administering tranexamic acid, particularly if improperly administered or during cardiovascular surgery. Therefore, EEG monitoring should be considered for patients with a history of seizures.

Pharmacokinetics:

Absorption:

● Absorption from the human gastrointestinal tract is not complete, with approximately 40% of the drug being absorbed.

● 3 hours after a single oral dose of 25 mg per kg body weight, the peak serum level was 15.4 mg per L, and the aqueous humor level was 1.6 mg per L.

Distribution:

● Intravenous administration of 10 mg per kg body weight resulted in plasma concentrations of 18.3 μg, 9.6 μg, and 5 μg per mL at one, three, and five hours after the injection.

● Tranexamic acid has the ability to cross the blood-brain barrier, as demonstrated when administered to patients with ruptured intracranial aneurysms.

● The drug diffuses rapidly to the joint fluid and the synovial membrane, with the joint fluid reaching the same concentration as in the serum. The biological half-life in the joint fluid was approximately 3 hours.

Metabolism:

● Possible routes of biotransformation for tranexamic acid are acetylation or deamination followed by oxidation or reduction.

Elimination:

● After intravenous administration of ten mg per kg body weight, tranexamic acid is eliminated through glomerular filtration. At one hour, approximately 30% of the drug is excreted, with 55% excreted at three hours and 90% at 24 hours. For oral administration of 10-15 mg per kg body weight, 1% of the drug is excreted after one hour, with 7% excreted after three hours and 39% excreted at 24 hours.

● Following oral administration, around 50% of the parent compound, 2% of the deaminated dicarboxylic acid, and 0.5% of the acetylated product are excreted.

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