Triptorelin Acetate (GnRH) Complete Profile, Dosage, and Other Relevant Information

Table of Content:

  1. Fundamentals of Triptorelin Acetate

  2. Triptorelin Acetate Structure

  3. What is Triptorelin Acetate?

  4. How Does it Work in Human Body?

  5. Why is Triptorelin Acetate Prescribed?

  6. Other Medical Uses of Triptorelin Acetate

  7. Dosage and Administration Protocol

  8. Storage, Stability and Disposal

  9. Benefits Associated with Triptorelin Acetate

  10. Side-Effects Associated with Triptorelin Acetate

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Fundamentals of Triptorelin Acetate

Sequence: Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2 acetate salt

Molecular Formula: C64H82N18O13

Molecular Weight: 1311.473 g/mol

Synonyms: Decapeptyl, TRP (6)-LHRH, Triptoreline, Trelstar, Gonapeptyl, Triptodur

Type: Small Molecule

Triptorelin Acetate Structure

What is Triptorelin Acetate?

Triptorelin is a decapeptide homolog of luteinizing releasing hormone - LHR. it is commonly used for the treatment and maintenance of sex hormone-related tumours. Triptorelin Acetate helps to minimize the secretion of luteinizing hormone and follicle-stimulating hormone FSH to substantially reduce the levels of testosterone production and accumulation. This comes up with the outcome of shrinking or slowing down the growth of cancer in the human body. The pharmacokinetics of this compound follows a 3-compartment model. The half-lives are estimated to be 6 minutes, 45 minutes, and 3 hours respectively.

How Does it Work in Human Body?

Triptorelin Acetate is a gonadotropin-releasing hormone agonist (GnRH agonist) which is used to enhance fertility in adults, treat prostate cancer and also treat the central precocious condition in children. It acts on the hypothalamus in the brain to maintain and control hormones secretions and functions in both males and females. GnRH then instructs the pituitary gland in the brain to secrete luteinizing hormone (LH) that assists in testosterone production or follicle-stimulating hormone (FSH) that aids in sperm production.

The main function of Triptorelin Acetate in this process is that it stimulates the hypothalamus to secrete more GnRH, thus sending a message to the pituitary to secrete LH and FSH, therefore more testosterone production occurs.

Triptorelin Acetate is also known under the brand name Diphereline, Trelstar, Decapeptyl, and Gonapeptyl.

Why is Triptorelin Acetate Prescribed?

By injecting Triptorelin Acetate, Central Precocious Puberty (CPP) is been treated. CPP is a condition that occurs in children. This causes them to hit puberty before the time, it results in abnormal bone growth and development of sexual features in children of 2 years or older.

Triptorelin Acetate injection is in a class of medications called GnRH agonists. It functions by minimizing the number of specific hormones in the human body.

Other Medical Uses of Triptorelin Acetate

This compound is also used for the treatment of prostate cancer as part of androgen deprivation therapy.

Another common use of triptorelin acetate is hormone replacement therapy to restrain testosterone or estrogen levels in the transgender community. Triptorelin works as a castration agent which helps to reduce sexual urges in sex offenders. It can also be used to treat breast cancer, endometriosis and uterine fibroids.

Dosage and Administration Protocol

Lyophilized form of triptorelin acetate is first reconstituted in sterile water and no other diluent should be used. It is then administered subcutaneously through injection into the muscle of either thigh or buttock. The image below is representing how subcutaneous injection is administered. 

For Prostate Cancer in Adults:

  • 75 mg triptorelin acetate given every 4 weeks
  • 25 mg of triptorelin acetate given every 12 weeks
  • 5 mg of triptorelin acetate given every 24 weeks

For Central Precocious Puberty in Children:

  • 5 mg of triptorelin acetate given every 2 weeks.

Before receiving the triptorelin acetate injection, must inform your doctor or pharmacist if you are allergic to any drug or using any other medication already. Your healthcare provider will monitor you closely to take care of any new or problematic symptoms because this peptide therapy may cause a rise in certain hormones in the initial weeks after administration. It is advisable to start with 50 micrograms of triptorelin acetate at first to see the variations it is causing in testosterone levels.

Storage, Stability and Disposal

Triptorelin acetate is a hygroscopic compound hence it must be protected from direct light. This peptide is guaranteed one year from the date of delivery. The lyophilized form of triptorelin acetate is stable at room temperature for about 3 weeks, if desiccated it must be stored below -18°C to -20°C (freezer). Avoid freezing it after the reconstitution.

After reconstitution, triptorelin acetate should be stored at 4°C for 2-7 days (refrigerated). For a long duration of storage, it is advisable to add a carrier protein (0.1% HSA or BSA). Kindly avoid it from the free-thaw cycle. Peptides are stable in a cold atmosphere. To prevent peptide bond collapse, keep peptide vials in the refrigerator at all times. When handled carefully, most peptides, especially those that are shorter, can be preserved for weeks.

Following reconstitution, aliquot and store at -20°C.

Before administering, always swab the top lid of the vial with the help of an alcohol wipe or 95% ethanol. The powdered form should be reconstituted only with sterile bacteriostatic water. Bacteriostatic water must be pure and sterile in order to avoid contamination and maintain the shelf life of dissolved peptides. By inserting the pin at an angle through the rubber stopper, you can inject the bacteriostatic water towards the vial's interior wall rather than directly onto the powder.

Never shake a vial to mix because the stability of proteins in the compound suffers when there are air bubbles present.

Benefits Associated with Triptorelin Acetate

Triptorelin Acetate is a well-known substance that enhances fertility in adults. When the peptide stimulates the secretion of Follicle-Stimulating Hormone and Luteinizing Hormone from the pituitary glands, it manages the testosterone levels accordingly and also increases the sperm count in adult males or eggs in females.

Sex hormones like estrogen and testosterone production increase by triptorelin acetate consumption. It is becoming more apparent to researchers that triptorelin peptide has several functions and benefits for people. Some of them are listed below:

  • Prostate cancer treatment
  • Castration with chemicals
  • Treatment of breast cancer
  • Cure for endometriosis.
  • Managing early puberty.
  • Treatment for fibroids in the uterus.

15ml Nasal Spray contains 2mg Triptorelin
30ml Nasal Spray contains 4mg Triptorelin

As triptorelin acetate stimulates the secretion of hormones like testosterone, it results in the development of lean muscle mass. This helps in muscle growth as well. Testosterone is a very essential hormone for males and a good level of testosterone can help to grow muscle mass, increases libido, manages sexual dysfunction, enhances energy, and eliminates the risk of heart disease.

Moreover, it helps in women's health, as premenopausal women with early-stage breast cancer may benefit from this peptide, according to a study. It maintains ovarian function.

Side-Effects Associated with Triptorelin Acetate

Triptorelin Acetate injection can cause adverse effects. Some of them can be headaches, heartburn, constipation, mood changes, leg or joint pain, breast pain, depression, insomnia, rash, hives, itching and seizure as well.

Other side effects can be:

  • hot flashes (a sudden wave of intense body heat), or sweating
  • disturbed sexual desire
  • swelling, or redness at the place where an injection was given
  • cough
  • nausea
  • vomiting
  • blurred vision

Some adverse effects can be very harmful. Call your doctor right away if you encounter any of these symptoms, or seek emergency care:

  • Difficulty breathing or swallowing
  • Swelling of the whole face
  • Hoarseness
  • Seizures
  • Chest pain
  • Pain in body
  • Difficult speech
  • Dizziness or fainting
  • Weakness or numbness of an arm or leg
  • Bone pain
  • Painful or difficult urination
  • Blood in urine
  • Frequent urination
  • Extreme thirst
  • Decreased consciousness

General side effects can include:

  • Anaphylaxis
  • Arthralgia
  • Asthenia
  • Asthma
  • Breast tenderness (males and females)
  • Changes in blood pressure
  • Changes in breast size
  • Ovarian cysts
  • Weight changes

During the first few weeks of treatment, it is possible for children receiving triptorelin injection (Triptodur) for central precocious puberty to experience new or worsened sexual development symptoms. In girls, the first two months of this medication may see the commencement of menstruation or spotting (light vaginal bleeding). Call your doctor for advice if bleeding persists after the second month.

Triptorelin must not be used by women who are pregnant or who are able to get pregnant. Inform your doctor if you are nursing a baby, intend to get pregnant, or are already pregnant. Call your doctor as soon as you suspect pregnancy if you are using a triptorelin injection. The fetus could be harmed by a triptorelin injection. Ask your doctor or chemist for more details if you think this drug may be prescribed for other conditions.

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