Tapros 3M

Tapros 3M

leuprorelin

Manufacturer:

Takeda
Full Prescribing Info
Contents
Leuprorelin acetate.
Description
Each vial contains also contains the following excipients: Powder: Prolactic acid 99.3 mg, mannitol 19.45 mg. Solvent: Sodium carboxymethylcellulose 10 mg, mannitol 100 mg, polysorbate 80 2 mg, water for injection sufficient quantity for 2 mL.
Action
Pharmacology: Leuprorelin is a synthetic nonapeptide analogue of natural Gn-RH. The studies performed in humans as well as in animals have demonstrated that, after an initial stimulation, the prolonged administration of leuprorelin induces a decrease of gonadotropin secretion, consequently suppressing the testicular function in men and inducing an atrophy of the uterine and ectopic endometrial tissue in women. This effect is reversible upon discontinuation of drug therapy.
Through some studies in animals, another mechanism of action has been evoked: A direct effect by the decrease of sensitivity of the gonadotropin receptors.
In humans, after administration of the 1st dose, an increase in circulating levels of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) is induced, leading to an initial increase in levels of the gonadal steroids (testosterone and dihydrotestosterone in men, and oestradiol in women). The pursuit of the treatment leads to a decrease in LH and FSH levels, inducing within 3-4 weeks, to androgen or oestrogen levels equivalent to those obtained after castration or menopause, as long as drug administration continues.
Indications/Uses
Treatment of prostatic cancer with metastases, and endometriosis at genital and extragenital localization (from stage I-IV).
Breast cancer in pre- and peri-menopausal women, provided endocrine treatment is indicated.
The clinical knowledge concerning the endometriosis treatment is limited to women >18 years.
The duration of treatment is limited to 6 months. It is not recommended to start a 2nd treatment period with Tapros 3M or with another Gn-RH analogue.
Dosage/Direction for Use
Prostatic & Breast Cancer: 1 SC/IM inj renewed every 3 months.
Endometriosis: Start treatment during the 1st 5 days of menstrual cycle. 1 SC/IM inj renewed every 3 months. Duration: No more than 6 months whatever is the stage.
Contraindications
Hypersensitivity to Gn-RH, Gn-RH analogues or to any of the components of Tapros 3M.
Vaginal bleedings of undetermined origin.
Use in pregnancy & lactation: Do not use when pregnant. Women must be confirmed not pregnant before the start of treatment. Because of the lack of data regarding Tapros 3M's excretion in milk and its potential effects on nursing babies, this product should not be used during breastfeeding.
Warnings
Since Tapros 3M is a sustained-release preparation with its action lasting 12 weeks, administration at an interval exceeding 12 weeks may lead to the recurrence of an increase in the serum level of gonadotropic hormone due to the pituitary-gonad system stimulating effect of this drug, resulting in a transient aggravation of the clinical condition. Therefore, the method of administering once every 12 weeks should be observed.
Endometriosis: The incidence of adverse reactions generally tends to increase with an increase in dose. Thus, in selling the dose, careful attention should be paid to the body weight.
Before any prescription of Tapros 3M, it is mandatory to verify that the patient is not pregnant. During the period of the treatment, the patient should be instructed to prevent conception with the use of nonhormonal methods.
It is advised, as for every other Gn-RH analogues, to monitor the patients suffering from osteoporosis when prolonged use.
A decrease in bone mass may occur owing to estrogen reducing effect of Tapros 3M. Therefore, as a rule, this drug should not be administered to patients with endometriosis or uterine myoma for >6 months. The safety of administration for >6 months has not been established. When it is inevitable to administer this drug for a long period or to resume its administration, it should be carefully administered after the bone mass is examined as far as possible.
Breast Cancer: When starting treatment with Tapros 3M, absence/presence of hormone receptor expression should be confirmed as a rule. When hormone receptor expression is confirmed to be negative, Tapros 3M should not be used.
Before starting treatment, it should be confirmed that the patient is not pregnant. During the period of treatment with Tapros 3M, the patient should be instructed to prevent conception with the use of a nonhonmonal method.
A decrease in bone mass may occur owing to estrogen reducing effect of Tapros 3M. Therefore, when this drug is administered for a long period, it should be carefully administered after bone mass is examined as far as possible.
Prostate Cancer: Patient who have already had renal dysfunction due to spinal cord compression or urethral obstruction or those may be at risk of developing such manifestation. There is a possibility that the symptoms or underlying disease are aggravated with the elevation of serum testosterone level in the early period after the 1st administration.
Special Precautions
Endometriosis: In administration of Tapros 3M, care should be taken to differentiate a similar disease (malignant tumor, etc) from endometriosis, uterine myoma. If during administration of Tapros 3M, any growing phyma is found or no improvement is seen in the clinical symptom, the administration should be discontinued.
In the early period after the 1st administration of Tapros 3M, a transient elevation of the serum level of estrogen may occur owing to the stimulating effect of Tapros 3M, as a highly active LH-RH derivative, on the pituitary-gonad system, resulting in a transient aggravation of clinical condition. However, such an aggravation usually disappears in the course of continued administration.
Since a depressed state like climacteric disturbance may occur, the patient's condition should be closely observed.
Prostate Cancer: Since Tapros 3M is an agent for endocrine therapy, use of this drug for prostate cancer should be limited to patients for whom treatment with Tapros 3M is considered appropriate under the supervision of a physician who has adequate knowledge and experience in medication for cancer.
In the earlyy period after the 1st administration ofTapros 3M, a transient elevation of the serum level of testosterone may occur owing to the stimulating effect of Tapros 3M, as a highly active LH-RH derivative, on the pituitary-gonad system, resulting in a transient aggravation of bone pain, etc. In such a case, symptomatic treatment should be given. Since ureteral obstruction or spinal cord compression may occur, this drug should be carefully administered and close observation should be made during the 1st month after initiation of administration, and if any of such symptoms occur, appropriate measures should be taken.
Since a depressed state occur, the patient's condition should be closely observed.
Breast Cancer: Since Tapros 3M is an agent for endocrine therapy, use of this drug for premenopausal breast cancer should be limited to patients for whom treatment with Tapros 3M is considered appropriate under the supervision of a physician who has adequate knowledge and experience in medication for cancer.
In the early period after the 1st administration of Tapros 3M, a transient elevation of the serum level of estrogen may occur owing to the stimuiating effect of Tapros 3M, as a highly active LH-RH derivative, on the pituitary-gonad system, resulting in a transient aggravation of bone pain, etc. In such a case, symptomatic treatment should be given. In antitumor effect is not obtained with Tapros 3M and any progression of the tumor is observed, the administration should be discontinued.
Since a depressed state like climateric disturbance may occur, the patient's condition should be closely observed.
Other Precautions: All Indications: It has been reported that the benign pituitary adenoma was observed in rats in a study in which Tapros 3M was administered SC in doses of 0.8, 3.6 and 16 mg (as leuprorelin acetate)/kg at 4-week intervals for 1 year and another study in which an aqueous injectable solution of leuprorelin acetate was similarly administered in doses of 0.6, 1.5 and 4 mg/kg/day for 2 years.
Endometriosis and Breast Cancer: It has been reported that the administration of Tapros 3M brought about venous thrombosis or pulmonary embolism.
Prostate Cancer: It has been reported that the administration of Tapros 3M brought about cerebral infarction, venous thrombosis or pulmonary embolism.
Use In Pregnancy & Lactation
Do not use when pregnant. Women must be confirmed not pregnant before the start of treatment. Because of the lack of data regarding Tapros 3M's excretion in milk and its potential effects on nursing babies, this product should not be used during breastfeeding.
Adverse Reactions
Clinically Significant Adverse Reaction: Since interstitial pneumonia, accompanied by fever, coughing, dyspnea, abnormal chest X-ray, etc may occur (<0.1%), the patient's condition should be closely observed. If any abnormality is observed, appropriate measures eg, treatment with adrenal cortical hormones, should be taken.
Since anaphylactoid symptoms may occur (<0.1%), careful inquiry should be made and close observation should be made after the administration of Tapros 3M. If any abnormality is observed, appropriate measures should be taken.
Hepatic dysfunction or jaundice, with increased AST (GOT), ALT (GPT) etc may occur (frequency unknown). Therefore, close observation should be made, and if any abnormality is observed, appropriate measures should be taken.
Development or aggravation of diabetes may occur (frequency unknown). If any abnormality is observed, appropriate measures should be taken.
Pituitary apoplexy has been reported in patients with pituitary adenoma (frequency unknown). Therefore, if headache, vision impairment, visual field disorder, etc are observed immediately after the 1st dose of Tapros 3M, appropriate measures eg, surgical treatment, should be taken after conducting examination.
Prostatic Cancer: At the Beginning of Treatment (see Warnings and Precautions): The start of treatment can be sometimes accompanied by some increase of clinical signs and symptoms (flare phenomenon): Bone pain, hematuria, urinary obstruction and weakness of the lower limbs/paresthesia has been reported.
These manifestations are usually transitory, disappearing within 1-2 weeks during the pursuit of the treatment. However, the possibility of potential exacerbations of these symptoms during the 1st few weeks of treatment has to be taken into consideration in patients with neurological disorders or with urinary obstruction.
Hepatic (Close Observation should be Made): ≥5%: Increased LDH; 0.1 to <5%: Jaundice, or increased AST (GOT), ALT (GPT), γ-GTP or ALP.
Endocrine: ≥5%: Hot flushes, warmth feeling; 0.1 to <5%: Headache, facial hot flushes, dizziness, diaphoresis, decreases libido, erectile disturbance, gynecomastia, testicular atrophy or discomfort in the perineal region.
Musculoskeletal: 0.1 to <5%: Arthralgia, bone pain, pain in the shoulder, low back or limbs, or difficulty in walking; <0.1%: Muscle ache or decreased bone mass.
Dermatologic: 0.1 to <5%: Dermatitis or hair growth on the head.
Urinary: 0.1% to <5%: Poliakiuria, hematuria or increased blood urea nitrogen (BUN).
Cardiovascular: 0.1 to <5%: ECG abnormalities or increased cardiothoracic ratio.
Hematologic: 0.1 to <5%: Anemia or decreased platelet count.
Gastrointestinal: 0.1 to <5%: Nausea, vomiting or anorexia; <0.1%: Diarrhea.
Hypersensitivity: 0.1 to <5%: Rash of pruritus
Administration Site (Close Observation should be Made): 0.1 to <5%: Reactions at the injection site eg, pain, induration and redness; <0.1%: Abscess.
Others: 0.1 to <5%: Edema, pressure sensation of chest, rigor, malaise, numbness of lips or limbs, increased weight, paresthesia, deafness, tinnitus, fever, increased total cholesterol, triglyceride or uric acid, hyperkalemia, or increased blood sugar level; <0.1%: Weakness.
Endometriosis and Breast Cancer: Symptoms Resulting from Decreased Estrogen: ≥5%: Hot flushes, feeling of warmth, feeling of hot flushes, shoulder stiffness, headache, insomnia, dizziness or diaphoresis; 0.1 to <5%: Decreased libido, coldness, visual disturbance or emotional lability.
Female Reproductive: 0.1 to <5%: Metrorrhagia, vaginal dryness, coital pain, vaginitis, increased fluor, ovarian hyperstimulation syndrome, or pain, swelling or atrophy of the breast.
Musculoskeletal: ≥5%: Pains eg, arthralgia and bone pain. 0.1 to <5%: Joint stiffness, lumbar pain, muscle ache, muscular spasm, decreased bone mass, increased serum phosphorus or hypercalcemia.
Dermatologic: 0.1 to <5%: Acne, dry skin, alopecia, hypertrichosis or nail abnormality.
Psychoneurologic: 0.1 to <5%: Sleepiness, irritated feeling, hypomnesia, decreased attentiveness or paresthesia.
Hypersensitivity: 0.1 to <5%: Rash of pruritus.
Hepatic (Close Observation should be Made): 0.1 to <5%: Increased AST (GOT), ALT (GPT), ALP, LDH, γ-GTP or bilirubin; <0.1%: Jaundice.
Gastrointestinal: 0.1 to <5%: Nausea, vomiting, anorexia, abdominal pain, feeling of enlarged abdomen, diarrhea, constipation, stomatitis or thirst.
Cardiovascular: 0.1 to <5%: Palpitation or increased blood pressure.
Hematologic: 0.1 to <5%: Increased red blood cell count, anemia, decreased white blood cell, decreased platelet count or prolonged partial thromboplastin time.
Urinary: 0.1to <5%: Pollakiuria, dysuria or increased BUN.
Administration Site (Close Observation should be Made): 0.1 to <5%: Reactions at the injection site eg, pain, induration and redness; <0.1%: Abscess.
Others: 0.1 to <5%: Fatigue, malaise, weakness, numbness of lips or limbs, carpal tunnel syndrome, tinnitus, deafness, chest discomfort, edema, increased weight, pain of lower extremities, respiratory distress, fever, increased total function cholesterol, LDL cholesterol or triglyceride, or hyperkalemia; <0.1%: Decreased weight, taste abnomiality or abnormal thyroid function.
It has been reported that the administration of leuprorelin acetate brought about cerebral infarction, venous thrombosis or pulmonary embolism.
Drug Interactions
Tapros should be administered with care when co-administered with sex hormone preparations.
Caution For Usage
Tapros 3M should be used only by the SC or IM route (IV injection of Tapros 3M may induce thrombosis).
For SC injection, the following cautions should be exercised: The site for SC injection should be the brachial, abdominal or gluteal region.
The injection site should be changed each time. The repeated injection should not be given at the same site.
The check should be made to see that the needle is not piercing a blood vessel.
The patients should be instructed not to massage the injection site.
Preparation: The injectable soiution should be prepared at the time of use and be used immediately after suspending.
If any sedimentation is noticed in the suspension of vial product, such suspension should be used after swirling gently, avoiding formation of bubbles, to resuspend the particles uniformly.
Use immediately after reconstitution.
Storage
Store below 25°C, avoiding heat. No refrigeration necessary.
ATC Classification
L02AE02 - leuprorelin ; Belongs to the class of gonadotropin releasing hormone analogues. Used in endocrine therapy.
Presentation/Packing
Inj (vial) 11.25 mg x 1's.
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