Triptorelin for Sale – Buy the Best!

triptorelin for saleComposition and form of release

Lyophilisate for preparation of solution for injection and local use – 1 vial:

  • Active ingredients: triptorelin acetate 3.92 mg (4.12 mg) in terms of triptorelin 3.75 mg (3.94 mg);
  • Excipients: DL – lactic and glycolic acid copolymer (1: 1) 200 mg, D – mannitol 85 mg, sodium carmellose 30 mg, polysorbate-80 2 mg.

Solvent for suspension preparation: mannitol, 0.8% solution – 1 ml:

D – mannitol 8.0 mg, water for injection up to 1.0 ml.

1 bottle with 10 ml of the drug, 1 ampoule with 2 ml of solvent. >>BUY TRIPTORELIN FROM PEPTIDE SCIENCES<<

Description of the dosage form

Lyophilisate: lyophilized powder (brittle lyophilisate) or a porous mass of white or white with a yellowish tinge compacted into a tablet.

Solvent: clear, colorless liquid.

Reconstituted suspension: homogeneous suspension of white or white with a yellowish sheen. On standing, the suspension settles, but easily resuspended with shaking. The suspension should pass freely into the syringe through the # 0840 needle.

Where to Find Triptorelin for Sale

Bioavailability after intramuscular and subcutaneous administration is 38.8 and 69%, respectively. Microsomal liver enzymes (in particular, cytochromes P450) are not involved in metabolism; the role of other enzymes that metabolize the drug is unknown. The half-life (after intravenous administration at a dose of 0.5 mg) is 2.81 hours (in men with normal renal function and creatinine clearance – 150 ml / min). Eliminated (after intravenous administration at a dose of 0.5 mg) with bile and kidneys (42% – in the form of unchanged substance, up to 62% – with a decrease in creatinine clearance and liver failure).

Pharmacodynamics Triptorelin indication

A synthetic analogue of the LH-releasing factor. Like the natural gonadotropin-releasing hormone produced by the hypothalamus, it stimulates the release of LH and FSH from the anterior pituitary gland. With prolonged use, it leads to a complete blockade of the gonadotropic function of the pituitary gland with the suppression of the secretion of lutropin and FSH (chemical castration). In prostate cancer, the release of FSH and lutropin alpha causes a transient increase in the concentration of testosterone, but after suppression of the secretion of FSH and LH (within 4 weeks from the start of treatment), the concentration of testosterone in the blood decreases to post-castration.

In women (with endometriosis, breast cancer), the initial release of FSH and LH leads to a transient increase in the concentration of estradiol, but after suppression of their production, a decrease in the size and suppression of ovarian functions occurs, a decrease in the size of the uterus and mammary glands, inactivation and atrophy of the endometrium (including ectopic), as well as regression of hormone-dependent tumors. Amenorrhea usually develops within 4 to 8 weeks after starting treatment. The maximum effect develops in the 3rd week and lasts throughout the entire period of treatment (reversible after its termination). Menstruation usually occurs no earlier than 3 months after the final injection.

Instructions Triptorelin indication

Rules for the preparation of the suspension and the administration of the drug.

  • The drug is administered only intramuscularly;
  • a suspension for intramuscular injection is prepared immediately before administration using the supplied solvent;
  • the drug should be prepared and administered only by specially trained medical personnel;
  • Hold the bottle with Triptorelin-Long strictly vertically. By tapping lightly on the bottle, make sure that all the drug is at the bottom of the bottle;
  • open the syringe, attach the supplied 0.8 mm x 40 mm needle to it to take the solvent;
  • open the ampoule with the solvent and draw the entire contents of the ampoule into the syringe, set the syringe to the 2 ml level;
  • remove the plastic cap from the vial containing the drug. Disinfect the rubber stopper of the bottle with a swab dipped in alcohol. Insert the needle into the vial with the drug through the center of the rubber stopper and carefully inject the solvent along the inner wall of the vial, without touching the contents of the vial with the needle;
  • remove the syringe with the needle from the vial;
  • the bottle must remain motionless until the drug is completely saturated with the solvent and a suspension is formed. Without turning the bottle upside down, check for a dry residue at the walls and bottom of the bottle. If you find dry residues of the drug, leave the bottle until completely soaked (for about 3-5 minutes);
  • after you are convinced that there are no residues of the dry preparation, gently stir the contents of the bottle in circular movements for 30-60 seconds until a homogeneous suspension is formed;
  • do not turn or shake the bottle;
  • replace the needle on the syringe with a 1.2 mm x 50 mm needle (for a suspension set). Insert the needle through the rubber stopper into the vial. Then lower the needle cut down and, tilting the bottle at an angle of 45 degrees, slowly draw the suspension completely into the syringe. Do not turn the bottle over while dialing. A small amount of the drug may remain on the sides and bottom of the bottle. The consumption of the residue on the walls and bottom of the bottle is taken into account;
  • remove the needle immediately after drawing the suspension into the syringe. Replace with a 1.1 mm x 40 mm needle, gently invert the syringe and remove air from the syringe;
  • enter the suspension of the drug immediately after preparation;
  • use an alcohol swab to disinfect the injection site. Insert the needle deep into the gluteus muscle, then pull the syringe plunger back slightly to make sure there is no damage to the vessel. Inject the suspension slowly with constant pressure on the syringe plunger. If the needle becomes clogged, replace it with another needle of the same diameter;
  • dispose of needles in sharps containers;
  • with repeated injections, the left and right gluteal muscles should be alternated;
  • the cases of incomplete injection, leading to the loss of a large amount of suspension, must be reported to the attending physician.

Indications for use of Triptorelin-Long

Treatment of locally advanced prostate cancer in monotherapy or as an adjuvant treatment with radiation therapy.

Treatment of metastatic prostate cancer.

Genital and extragenital endometriosis (stages I-IV).

Contraindications to the use of Triptorelin-Long

Hypersensitivity to triptorelin and other analogs of gonadotropin releasing factors.

Hormone-independent prostate cancer.

Condition after surgical castration (for prostate cancer).

Pregnancy, breastfeeding.

Clinically pronounced osteoporosis or a high risk of developing it in women.

Triptorelin-Long Use in pregnancy and children

Pregnancy must be excluded before starting treatment. Human studies have not been conducted. In view of the potential threat to the fetus, women of childbearing age are recommended to use non-hormonal contraception methods during the first month of triptorelin treatment. There is no evidence of penetration into breast milk. Due to the potential risk of adverse effects on the child during treatment with triptorelin, breastfeeding is recommended to be discontinued.

Triptorelin-long Side effects

Adverse reactions in men.

Adverse reactions when using triptorelin are associated with its expected pharmacological effects: an initial increase in testosterone concentration, and then an almost complete suppression of testosterone synthesis.

The frequency of adverse reactions that can occur during therapy is given in the following gradation: very often (> 1/10), often (> 1/100, <1/10), infrequently (> 1/1000, <1/100 ), rare (> 1/10000, <1/1000), very rare (<1/10000) and the frequency is unknown (the frequency cannot be determined from the available data).

Infectious and parasitic diseases: very rarely – rhinopharyngitis.

Immune system disorders: very rarely – anaphylactic reactions, hypersensitivity.

Metabolic and nutritional disorders: rarely – anorexia, decreased appetite, increased appetite; very rarely – diabetes mellitus; frequency unknown – gout.

Mental disorders: often – mood changes, depression, sleep disturbances, decreased libido; rarely – irritability, insomnia; very rarely – confusion, decreased activity, a feeling of euphoria; frequency unknown – anxiety, loss of libido.

Disturbances from the nervous system: very often – paresthesia of the lower extremities; often – headache; rarely – paresthesia, taste disturbance, drowsiness, astasia (disturbance of the ability to stand, associated with impaired coordination), lethargy; very rarely – memory impairment; frequency unknown – dizziness.

Violations from the organ of vision: very rarely – discomfort in the eyes, blurred vision; frequency unknown – visual impairment.

Hearing disorders and labyrinth disorders: rarely – ringing in the ears; frequency unknown – vertigo.

Vascular disorders: very often – “hot flashes”; infrequently – increased blood pressure, thromboembolism; frequency unknown – lowering blood pressure.

Disturbances from the respiratory system, chest and mediastinal organs: infrequently – bronchial asthma; rarely – shortness of breath; very rarely – nosebleeds, shortness of breath that occurs when lying down.

Disturbances from the gastrointestinal tract: often – nausea; rarely – abdominal pain, constipation, diarrhea, vomiting, bloating, flatulence, dry mouth; frequency unknown – gastralgia.

Violations of the skin and subcutaneous tissues: very often – hyperhidrosis; infrequently – hypotrichosis; rarely – alopecia, acne, itching, rash; very rarely – blisters; frequency unknown – Quincke’s edema, urticaria, purpura.

Musculoskeletal and connective tissue disorders: very often – back pain; often – pain in the limbs; rarely – muscle spasm, muscle weakness, myalgia, arthralgia; very rarely – joint swelling, stiffness of muscles and joints, osteoarthritis; frequency unknown – musculoskeletal pain, joint stiffness, bone pain.

Disorders of the kidneys and urinary tract: very often – dysuria.

Violations of the genital organs and mammary gland: often – erectile dysfunction; rarely – gynecomastia, testicular atrophy, pain in the testicles, engorgement of the mammary glands; frequency unknown – pain in the breast, lack of ejaculation.

General disorders and disorders at the injection site: very often – asthenia; often – increased fatigue, reaction at the injection site, pain at the injection site, redness at the injection site, inflammation at the injection site, edema, irritability; rarely – pain; very rarely – fever, flu-like syndrome; frequency unknown – feeling of discomfort, chest pain, malaise.

Laboratory and instrumental data: infrequently – increased activity of lactate dehydrogenase, gamma-glutamyltransferase, decrease in body weight; rarely – an increase in the activity of alanine aminotransferase, aspartate aminotransferase, an increase in body weight, an increase in the concentration of creatinine, urea in the blood plasma; very rarely – increased plasma alkaline phosphatase activity, hyperthermia; frequency unknown – increased blood pressure.

Triptorelin causes a short-term increase in the concentration of circulating testosterone during the first week after the first injection of the drug. In this regard, there may be a temporary worsening of symptoms of prostate cancer, which is usually manifested by disorders of the urinary tract, increased pain due to metastatic lesions. These symptoms are transient and usually disappear after 1 to 2 weeks.

In isolated cases, obstruction of the urinary tract or metastatic compression of the spinal cord is noted. As a consequence, patients with metastatic lesions of the spinal cord and / or obstruction of the upper or lower urinary tract should be closely monitored for the first few weeks after starting therapy. The use of GnRH agonists for the treatment of prostate cancer may be associated with an increased risk of bone loss, osteoporosis, and an increased risk of bone fractures.

Patients receiving long-term therapy with GnRH analogues in combination with radiation therapy may experience a greater number of adverse reactions, especially from the gastrointestinal tract, which are associated with the course of radiation therapy.

Adverse reactions in women.

As a consequence of a decrease in estrogen concentration, the most common adverse reactions may be: headache, decreased libido, sleep disturbance, mood changes, dyspareunia, dysmenorrhea, vaginal bleeding, ovarian hyperstimulation syndrome, ovarian enlargement, pelvic pain, abdominal pain, dryness the mucous membrane of the vagina and vulva, increased sweating, “hot flashes” and asthenia.

The frequency of adverse reactions that may occur during therapy is given as the following gradation: very often (> 1/10), often (> 1/100, <1/10), infrequently (> 1/1000, <1/100 ), rare (> 1/10000, <1/1000), very rare (<1/10000) and the frequency is unknown (the frequency cannot be determined from the available data).

Immune system disorders: infrequently – anaphylactic reactions; frequency unknown – hypersensitivity.

Mental disorders: very often – decreased libido, mood changes, sleep disturbances; often – depression, depressed mood; frequency unknown – anxiety, confusion.

Nervous system disorders: very often – headache; frequency unknown – dizziness, paresthesia.

Violations of the organ of vision: the frequency is unknown – blurred vision, visual impairment.

Hearing disorders and labyrinthine disorders: frequency unknown – vertigo.

Vascular disorders: very often – “hot flashes”.

Disturbances from the respiratory system, chest and mediastinal organs: frequency unknown – shortness of breath.

Disorders from the gastrointestinal tract: very often – abdominal pain; often – nausea, abdominal discomfort; frequency unknown – diarrhea, vomiting.

Violations of the skin and subcutaneous tissues: very often – hyperhidrosis; the frequency is unknown – angioedema, itching, rash, urticaria.

Musculoskeletal and connective tissue disorders: very common – bone pain; often – arthralgia, muscle spasm; infrequently – back pain; frequency unknown – myalgia, muscle weakness, bone resorption.

Violations of the genitals and mammary gland: very often – vaginal bleeding, dryness of the vaginal mucosa, dyspareunia, dysmenorrhea, ovarian hyperstimulation syndrome, an increase in the size of the ovaries, pain in the pelvic region, menorrhagia, metrorrhagia; often – pain in the mammary glands; frequency unknown – amenorrhea.

General disorders and disorders at the injection site: very often – asthenia; often – fatigue, irritability, reactions at the injection site, pain at the injection site, erythema and inflammation at the injection site; frequency unknown – fever, malaise.

Laboratory and instrumental data: often – weight gain; infrequently – an increase in the activity of lactate dehydrogenase, gamma-glutamyltransferase, alanine aminotransferase, aspartate aminotransferase, an increase in cholesterol concentration; the frequency is unknown – an increase in blood pressure, a decrease in body weight.

At the beginning of treatment, during a short-term increase in the concentration of estradiol in the blood plasma, symptoms of endometriosis, including pain in the pelvic region and dysmenorrhea, may worsen. These symptoms are transient and usually disappear after 1 to 2 weeks. Uterine bleeding, including menorrhagia, metrorrhagia may occur within one month after the first injection. There may be an increase in ovarian size, pelvic pain, and / or abdominal pain.

Drug interactions

There have been no controlled clinical studies of the interaction of triptorelin with other drugs. However, the possibility of interaction of triptorelin with other drugs, including drugs that promote the release of histamine, is not excluded.

It is not recommended to prescribe triptorelin simultaneously with drugs that increase the concentration of prolactin in the blood plasma, since these drugs reduce the number of GnRH receptors in the pituitary gland.

It is also necessary to take special precautions and monitor the concentration of sex hormones in the blood plasma when using triptorelin in combination with drugs that affect the secretion of gonadotropins by the pituitary gland.

Prolonged androgen deprivation can prolong the QT interval. It is necessary to assess the risk / benefit ratio before prescribing triptorelin to patients with congenital prolonged QT interval syndrome, electrolyte disturbances or chronic heart failure; or in patients taking drugs that can prolong the QT interval or drugs that can cause the development of bidirectional ventricular fusiform tachycardia, such as class IA antiarrhythmic drugs (eg, quinidine, procainamide) or III (eg, amiodarone, sotalol).

Dosage of Triptorelin-Long

The drug Triptorelin-Long is administered intramuscularly (IM). The injection site should be changed.

The drug Triptorelin-Long should be used only under the supervision of a physician with experience in these indications.

Fibroids of the uterus and endometriosis.

The drug Triptorelin-Long is administered at a dose of 3.75 mg (1 injection) IM 1 time in 28 days. Treatment should be started in the first 5 days of the menstrual cycle.

The duration of treatment depends on the severity of endometriosis and the observed clinical picture (functional and anatomical changes) and changes in the size of uterine fibroids, determined by ultrasound, during therapy. The duration of use of the drug for endometriosis is 4-6 months due to the possible effect on bone density.

The duration of therapy for preoperative treatment of uterine fibroids is no more than 3 months.

Repeated treatment with triptorelin or other GnRH agonists is not recommended.

ART.

The drug Triptorelin-lopg is administered once in a dose of 3.75 mg (1 injection) IM on the 2nd day of the menstrual cycle.

Prostate cancer.

The drug Triptorelin-Long is administered at a dose of 3.75 mg (1 injection) IM 1 time in 28 days, for a long time.

In patients with locally advanced prostate cancer, when treated in combination with radiation therapy, long-term antiandrogen therapy (3 years) is preferable to short-term antiandrogen therapy (6 months).

Application in selected groups of patients.

No dose adjustment is required in elderly patients and patients with impaired renal function.

Overdose

Cases of triptorelin overdose have not been described.

In case of overdose, symptomatic therapy is indicated.

Precautionary measures

Caution should be observed in patients taking anticoagulants, as a hematoma may develop at the injection site.

Fibroids of the uterus and endometriosis.

Pregnancy must be excluded before starting treatment.

The drug Triptorelin-Long should be prescribed only after an in-depth diagnosis of uterine fibroids and endometriosis (laparoscopy and / or hysteroscopy).

Throughout the entire treatment period, including within 3 months from the last injection, non-hormonal contraceptives should be used.

Due to the possible effect of Triptorelin-Long on bone mineral density, treatment should not be recommended for more than 6 months. It is not recommended to repeat the course of therapy with triptorelin or other GnRH analogues.

Treatment of uterine fibroids should be carried out under ultrasound control, since a rapid decrease in the size of the uterus in some cases can lead to the development of uterine bleeding of varying duration and intensity.

In case of uterine myoma, it is most advisable to combine therapy with Triptorelin-Long, followed by surgical treatment. The appointment of triptorelin leads to a significant decrease in the size of the myomatous uterus, which facilitates the operation technique. It is especially advisable to conduct a course of therapy with triptorelin in young patients in order to preserve reproductive function, when organ-saving surgery can be performed using laparoscopic techniques.

During the first month, vaginal bleeding / spotting of varying intensity and duration is possible. With continued spotting / bleeding after the first month, it is necessary to determine the concentration of estradiol in the blood plasma. With a decrease in the concentration of estradiol less than 50 pg / ml, the presence of other organic lesions is possible.

After stopping triptorelin therapy, ovarian function is restored after 7-12 weeks. Given that menstruation must stop during triptorelin therapy, the patient should be properly instructed on what she should inform her doctor if regular menses persist.

Prostate cancer.

At an early stage, the drug Triptorelin-Long causes a temporary increase in the concentration of testosterone in the blood plasma. As a result, during the first weeks of therapy, the appearance and intensification of clinical symptoms (in particular, bone pain, dysuric disorders), which are of a transient nature, and in which symptomatic therapy should be carried out, may be observed. As with other GnRH agonists, isolated cases of spinal cord compression or urinary tract obstruction may be identified. In case of spinal cord compression or urinary tract obstruction, standard treatment for these complications should be prescribed and orchiectomy (surgical castration) should be performed in case of emergency.

It is necessary to closely monitor patients during the first few weeks of therapy (the concentration of testosterone in the blood plasma should not exceed 1 ng / ml), especially in patients with metastatic lesions of the spinal cord, patients at risk of spinal cord compression or urinary tract obstruction. For the same reason, special attention should be paid at the beginning of treatment to patients with signs of spinal cord compression identified during a preliminary examination.

During the initial phase of therapy, the use of additional antiandrogenic drugs should be considered to prevent an initial increase in plasma testosterone concentration and a worsening of clinical symptoms.

Epidemiological data have shown that metabolic disorders (eg, impaired glucose tolerance) may develop in patients during androgen deprivation therapy; increase the risk of cardiovascular disease. However, prospective data have not confirmed an association between treatment with GnRH agonists and increased mortality from cardiovascular disease.

Patients with a high risk of metabolic and cardiovascular diseases should be carefully evaluated before treatment is prescribed and carefully monitored during androgen deprivation therapy.

At the beginning of therapy, there may be a temporary increase in the activity of acid phosphatase in the blood plasma.

The function of the gonads and pituitary gland.

The use of triptorelin in therapeutic doses leads to suppression of the gonads-pituitary gland system. The normal functioning of the gonads and the pituitary gland is usually restored after discontinuation of therapy. The results of a diagnostic test of gonadotropic function of the pituitary gland, carried out during and after cessation of therapy, may therefore be incorrect.

Osteoporosis.

The use of GnRH agonists can cause a decrease in bone mineral density (BMD).

In men, prolonged androgen deprivation with bilateral orchiectomy or with GnRH analogues may be associated with an increased risk of bone loss and may lead to osteoporosis and an increased risk of bone fracture.

Preliminary evidence suggests that the use of bisphosphonates in combination with GnRH may reduce BMD loss. Particular attention should be paid to patients with risk factors for the development of osteoporosis (for example: chronic alcohol dependence; smoking; long-term therapy with drugs that reduce BMD, such as anticonvulsant drugs or glucocorticosteroids; a history of hereditary osteoporosis; malnutrition or malnutrition).

In women, the use of GnRH agonists may be the cause of a decrease in BMD by an average of 1% per month for six months of treatment. Every 10% decrease in BMD leads to an increase in the risk of bone fracture approximately 2-3 times.

In most women, BMD is restored after stopping therapy.

There are no data available on the use of triptorelin in patients with established osteoprosis or with risk factors for osteoporosis (for example: chronic alcohol dependence; smoking; long-term therapy with drugs that reduce BMD, such as anticonvulsants or glucocorticosteroids; a history of hereditary osteoporosis; insufficiency or eating disorders, for example, anorexia neurosis). Given that a decrease in BMD is more likely in these patients, triptorelin treatment should be prescribed on an individual basis and can only be started if the benefits obtained from the treatment outweigh the risk. The possibility of additional examination should be considered to avoid loss of BMD.

Pituitary tumor.

Rarely, the use of GnRH agonists can reveal the presence of a previously undiagnosed gonadotropic pituitary adenoma. Pituitary hemorrhage is characterized by sudden headache, visual disturbances, and ophthalmoplegia.

Depression.

There is an increased risk of depression (which can be severe) in patients receiving triptorelin therapy. Patients should be informed of the possible development of depression and should receive appropriate therapy if depression develops. Patients with known depression should be closely monitored during therapy.

Prolongation of the QT interval.

Prolonged androgen deprivation can prolong the QT interval. It is necessary to assess the risk / benefit ratio before prescribing triptorelin to patients with congenital prolonged QT interval syndrome, electrolyte disturbances or chronic heart failure; or in patients taking drugs that can prolong the QT interval or drugs that can cause bidirectional ventricular fusiform tachycardia, such as class IA antiarrhythmic drugs (eg, quinidine, procainamide) or III (eg, amiodarone, sotalol).

Conducting ovulation induction in the framework of ART.

When treating infertility with IVF, Triptorelin-Long should be used only under the supervision of a specialist with experience in this field. During IVF, Triptorelin-Long is used to stabilize the concentration of endogenous sex hormones, followed by the administration of gonadotropins to stimulate follicular growth. The use of triptorelin allows you to avoid premature spontaneous ovulation of stimulated follicles, which increases the effectiveness of the IVF program in general.

It is recommended to use the drug Triptorelin-Long with caution during IVF in patients with polycystic ovary syndrome, because stimulation of a large number of follicles is possible.

Due to the fact that the use of the drug Triptorelin-Long can lead to the development of ovarian hyperstimulation syndrome, regular clinical monitoring is necessary, including an ultrasound of the ovaries.

It is required to determine the concentration of estradiol in the blood plasma in order to control the ovarian response during ovulation induction within the framework of ART (interruption of the ovulation stimulation cycle with an excessive ovarian response and cessation of gonadotropin injections) and clinical manifestations of ovarian hyperstimulation syndrome.

Dose adjustment.

It is necessary to adjust the dose of anti-hypertensive drugs when used together with Triptorelin-Long.

Influence on the ability to drive vehicles and mechanisms

Currently, there are no data on the possible effect of Triptorelin-Long on the ability to drive vehicles and mechanisms. Nevertheless, the use of the drug can lead to the development of such undesirable reactions as headache, decreased vision, drowsiness, which can negatively affect the ability to drive vehicles and perform potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions. If you experience the above symptoms, you should refrain from driving vehicles and mechanisms.

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