Triptorelin

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2

[edit] MECHANISM OF ACTION

Triptorelin is a synthetic decapeptide analog of naturally occurring gonadotropin-releasing hormone (GnRH or LH-RH).

Normally, the hypothalamus controls the pituitary production of gonadotropins through secretion of GnRH. The hypothalamus releases GnRH in a pulsatile fashion every 90–120 min into the portal circulation connecting the hypothalamus and anterior pituitary. When the pulsatile GnRH binds to the gonadotropes in the anterior pituitary, it stimulates release of LH and FSH into the general circulation.

Triptorelin acts like GnRH by binding to the gonadotropin releasing hormone receptor; following an initial stimulation of gonadotropins release, long-term exposure to constant levels of Triptorelin interrupt the normal pulsatile stimulation of GnRH receptors by GnRH, and thus desensitize the GnRH receptors and indirectly downregulates the secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to hypogonadism and thus a dramatic reduction in estradiol and testosterone levels in both sexes.

This causes the ovaries to enter a state of rest, putting the woman in a temporary “menopausal state” and, in males, androgens are reduced to castrate or pre-pubertal levels. These decreases occur usually 2 to 4 weeks after initiation of therapy and are maintained as long as treatment continues.

This effect is reversible on discontinuation of therapy.

Antiandrogens like Bicalutamide (Casodex) is strongly recommended as adjunctive therapy before starting and during the first weeks of GnRH agonist therapy in order to prevent the initial and temporary rise in serum testosterone (flare up effect)

[edit] INDICATIONS

  • Palliative treatment of advanced Prostate Cancer
  • In assisted reproduction techniques (ART), occasionally ovulation may occur too early, causing a significant reduction in the chance of getting pregnant. Triptorelin is indicated for downregulation and prevention of premature LH surges that might cause a premature release of egg cells. Prevention of the LH surge can reduce the cycle cancellation rate, increases the pregnancy rate and facilitates cycle control

[edit] DOSAGE

  • Prostate Cancer
    • Depot formulations:
      • 3.75 mg administered every month as a single subcutaneous or intramuscular injection
      • 11,25 mg every 3 months as a single subcutaneous or intramuscular injection.
      • 22,5 mg every 6 months as a single subcutaneous or intramuscular injection.
        Triptorelin is entended for long-term administration
  • Assisted Reproduction: The usual dosage is 0,1 mg injection under the skin of the lower abdomen once-daily. Treatment can be started on day 2 or 3 or day 21 to 23 of the menstrual cycle (or 5-7 days before the expected start of menstruation). After 2 to 4 weeks exogenous gonadotropins (e.g. Menopur/Gonal F will be given in order to stimulate follicle growth (egg sac growth). In general, Triptorelin treatment will continue until follicles have reached a suitable size. This will last usually 4 to 7 weeks. If enough egg sacs are present, a single injection of human chorionic gonadotrophin (hCG) to induce ovulation (release of an egg).

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Triptorelin or to other GnRH agonists
  • Pregnancy: Triptorelin may cause fetal harm when administered to a pregnant woman.

[edit] WARNINGS AND PRECAUTIONS

  • Tumor Flare Phenomenon: Transient worsening of tumor symptoms may occur during the first few weeks of treatment in men, which may include bone pain, ureteral obstruction and spinal cord compression.

[edit] DOSAGE FORMS AND STRENGTHS

  • Injectable suspension 0.1 mg/1 ml
  • Injectable sustained release formulation: 3.75mg, 11.25mg, 22.5mg.

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category X (US). Triptorelin is contraindicated in women who are or may become pregnant
  • Triptorelin should not be used by nursing mothers

[edit] SIDE EFFECTS

The most common adverse reactions in men are hot flashes, sexual dysfunction, decreased erections, injection site pain, skeletal pain, edema in legs, testicular atrophy and headache.

Because of the initial and temporary rise in serum testosterone in men, tumor flare can occur on the initiation of Triptorelin.

In Women, common side effects are: hot flushes, headache, abdominal pain, vaginal bleeding/spotting, nausea, inflammation at the injection site

[edit] RELATED LINKS

Hormone Therapy for Prostate Cancer

[edit] BIBLIOGRAPHY

[edit] REFERENCES