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Triptorelin acetate im and sc injection 3mg and 3.75mg

Presentation

Injections of triptorelin acetate.

Drugs List

  • DECAPEPTYL SR 3mg powder for suspension for injection
  • GONAPEPTYL DEPOT 3.75mg powder for suspension for injection
  • triptorelin acetate 3.75mg powder for prolonged release injection suspension
  • triptorelin acetate 3mg powder for suspension for injection
  • Therapeutic Indications

    Uses

    Adjunctive treatment of early stage breast cancer in premenopausal women
    Advanced prostate cancer: adjuvant to radiotherapy
    Locally advanced non metastatic prostate cancer
    Metastatic prostate cancer
    Precocious puberty in boys under 10 years of age : treatment
    Precocious puberty in girls under 9 years of age : treatment
    Treatment of endometriosis
    Uterine fibroids

    Locally advanced, non-metastatic prostate cancer, as an alternative to surgical castration Metastatic prostate cancer
    Endometriosis
    Uterine fibroids prior to surgery or when surgery is not appropriate
    Precocious puberty (onset before 8 years in girls and 10 years in boys) As adjuvant treatment:
    To radiotherapy in patients with high-risk localised or locally advanced prostate cancer Prior to radiotherapy in patients with high-risk localised or locally advanced prostate cancer To radical prostatectomy in patients with locally advanced prostate cancer at high risk of disease progression
    In combination with tamoxifen or an aromatase inhibitor, of endocrine responsive early stage breast cancer in women at high risk of recurrence who are confirmed as premenopausal after completion of chemotherapy

    Dosage

    This is the monograph for triptorelin as acetate.

    For information relating to other forms of triptorelin, for example triptorelin as embonate, please consult the separate product information.

    Adults

    Prostate cancer
    One 3mg intramuscular injection every 4 weeks (28 days)
    or
    One 3.75mg deep intramuscular or subcutaneous injection every 4 weeks (28 days)

    Treatment is usually continued in patients treated with gonadotrophin-releasing hormone (GnRH) analogues for metastatic prostate cancer where there has been a development of castrate-resistant prostate cancer.

    Endometriosis and uterine fibroids
    One 3mg intramuscular injection every 4 weeks (28 days)
    or
    One 3.75mg deep intramuscular or subcutaneous injection every 4 weeks (28 days)

    Treatment should commence during the first 5 days of the menstrual cycle.
    For patients with uterine fibroids, the treatment should continue for a minimum of 3 months.
    Maximum duration of treatment is 6 months. A second course of triptorelin or any other GnRH should not be undertaken due to concerns about bone density losses. Normally, maximum results are achieved after 3 to 4 injections.

    Breast cancer
    One 3mg intramuscular injection every 4 weeks in combination with tamoxifen or an aromatase inhibitor.
    Triptorelin should be commenced after completion of chemotherapy and after pre-menopausal status has been determined.
    Triptorelin therapy should be initiated 6 to 8 weeks before starting aromatase inhibitor treatment. A minimum of 2 injections, with a 4 week interval, should be administered before commencing aromatase inhibitor treatment.

    During treatment with the aromatase inhibitor, triptorelin should not be interrupted to avoid a rebound increase in circulating oestrogens. Suggested treatment duration for adjuvant treatment in combination with other hormonotherapy is up to 5 years.

    Children

    Triptorelin 3mg injection
    Contraindicated.

    Triptorelin 3.75mg injection
    Precocious Puberty
    Bodyweight more than 30kg
    One injection of 3.75mg on days 0, 14 and 28, then one injection of 3.75mg every 4 weeks. To be injected subcutaneously or deep intramuscularly.

    Bodyweight 20kg to 30kg
    One injection of 2.5mg on days 0, 14 and 28, then one injection of 2.5mg every 4 weeks. To be injected subcutaneously or deep intramuscularly.

    Bodyweight less than 20kg
    One injection of 1.875mg on days 0, 14 and 28, then one injection of 1.875mg every 4 weeks. To be injected subcutaneously or deep intramuscularly.

    Should the effect be insufficient, one injection may be given every 3 weeks.

    Treatment should be stopped if a bone maturation of older than 12 years in girls and 13 years in boys has been achieved.

    Administration

    The injection site should be changed each time.

    Triptorelin (as acetate) 3mg injection: by intramuscular injection only.

    Triptorelin (as acetate) 3.75mg injection: by intramuscular or subcutaneous injection.

    Contraindications

    Breastfeeding
    Long QT syndrome
    Pregnancy
    Torsade de pointes

    Precautions and Warnings

    Children with progressive brain neoplasm
    Family history of long QT syndrome
    Major risk factors for decreased bone mineral content
    Cardiovascular disorder
    Depression
    Electrolyte imbalance
    History of torsade de pointes
    Metabolic disorder
    Osteoporosis
    Spinal cord compression
    Spinal metastasis
    Urinary obstruction

    Correct electrolyte disorders before treatment
    Not effective following surgical removal of testes
    Advise ability to drive/operate machinery may be affected by side effects
    Breast ca:Administer for 6-8 weeks prior to addition of aromatase inhibitor
    Not all available brands are licensed for all age groups
    Not all available brands are licensed for all routes of administration
    Not all available strengths are licensed for all indications
    Prostate cancer: Prophylaxis of flare with anti-androgen is recommended
    Treatment to be prescribed under the supervision of a specialist
    Vary injection site during prolonged therapy
    Exclude pregnancy prior to initiation of treatment
    Measure bone density in at risk patients prior to therapy
    Consider monitoring ECG in patients at risk of QT prolongation
    If metrorrhagia occurs measure plasma estradiol levels
    Monitor closely patient with depression
    Monitor serum electrolytes
    Monitor size of uterus and myomas regularly
    Prostate cancer: Disease flare may occur at beginning of treatment
    Advise patient to report sudden headache, vomiting or visual disturbances
    Fast reduction of uterus size compared to myoma may lead to bleeding/sepsis
    May cause loss of bone mineral density
    Spinal cord compression may occur
    Treatment or prophylaxis of osteoporosis should be started as appropriate
    Ureteric obstruction may occur
    May affect results of some laboratory tests
    Endometriosis: Maximum treatment duration 6 months
    Uterine fibroids: Maximum treatment duration 6 months
    Female: Non-hormonal contraception required during and after treatment
    Advise patient to report regular menstruation if it persists during therapy
    Menstruation stops during treatment
    Pubertal development will resume after cessation of therapy

    Use may be associated with bone loss, and can lead to osteoporosis, with an increased risk of fractures. Use with caution in patients with metabolic bone disease or other risk factors for osteoporosis. Consider treatment or prophylaxis of osteoporosis where appropriate.
    Use of a bisphosphonate in men, in combination with triptorelin may reduce bone loss. In women, most patients will recover bone loss after cessation of treatment. Peak bone mass in adolescence does not seem to be affected by treatment. Consider additional measures to counteract loss of bone mineral density.

    In rare cases treatment with triptorelin may unmask a pituitary cell adenoma. Patients may present with symptoms of pituitary apoplexy (sudden headache, vomiting, visual impairment and ophthalmoplegia).

    Patients at a high risk of metabolic or cardiovascular disease should be carefully monitored before and regularly during treatment.

    Prostate cancer
    Triptorelin causes a transient increase in serum testosterone levels. As a result, symptoms of prostate cancer may worsen. During initial phase of treatment consider administering an additional anti-androgen.

    Small number of patients may experience an increase in cancer related pain. This can be managed symptomatically.

    Spinal cord compression or urethral obstruction have been observed with the use of gonadotrophin-releasing hormone (GnRH) agonists. Treatment for such complications should continue as normal. In extreme cases, surgical castration should be considered. After surgical castration, triptorelin will not contribute to further decreases in serum testosterone.

    Breast cancer
    Confirm premenopausal status following chemotherapy and before triptorelin therapy by blood concentrations of oestradiol and FSH within ranges for premenopausal women. Once triptorelin therapy has started, confirm ovarian suppression by assessment of FSH, and oestradiol if the patient is to be considered for therapy containing an aromatase inhibitor. Regular assessment of circulating FSH and oestrogen levels should be considered every 3 months during combined therapy with an aromatase inhibitor. Circulating FSH levels are lowered in response to induced menopause compared to a natural menopause where FSH levels are elevated.

    The aromatase inhibitor should be discontinued within 1 month of withdrawing triptorelin.

    Premenopausal women being administered with both triptorelin and exemestane or triptorelin and tamoxifen should undergo monitoring of cardiovascular risk factors and blood pressure. Diabetes has been reported in patients taking the combination of triptorelin and either exemestane or tamoxifen. Consequently, monitoring of blood glucose level is recommended and anti-diabetic treatment should be given if considered necessary.

    Precocious Puberty
    Exclude pseudo-precocious puberty (e.g. gonadal or adrenal tumour or hyperplasia) and gonadotrophin-independent precocious puberty (testicular toxicosis, familial Leydig cell hyperplasia) before treatment.

    In girls at initiation of treatment, ovarian stimulation followed by oestrogen withdrawal will occur. This may lead to mild to moderate vaginal bleed in the first month.

    After finalising therapy, development of puberty characteristics will occur. Information with regard to future fertility is still limited. In most girls, menses will start on average one year after discontinuing therapy.

    Slipped capital femoral epiphysis may be seen after withdrawal of treatment.

    Treatment of endometriosis and fibroids
    Non-hormonal contraception should be used through out the treatment and for 1 month after duration of the last injection as ovulation may be triggered by the initial release of gonadotrophins.

    Treatment with triptorelin will cause a persistent hypogonadotropic amenorrhoea. If metrorrhagia occurs, other than in the first month, plasma estradiol levels should be measured. If the level is less than 50 pg/ml, possible associated organic lesions should be sought.
    After withdrawal of treatment, ovarian function resumes, with ovarian function expected to occur approximately 2 to 3 months after the last injection.

    Pregnancy and Lactation

    Pregnancy

    Triptorelin is contraindicated in pregnancy.

    Gonadotrophin-releasing hormone (GnRH) agonists are associated with a theoretical risk of abortion or foetal abnormality.

    At the time of writing, there are no adequate data available on the use of triptorelin in human pregnancy. Limited data available on the inadvertent use of triptorelin during pregnancy did not indicate an increased risk of congenital malformations. However, long term follow up studies on development are far too limited.

    Research conducted in animals has not indicated direct or indirect harmful effects with respect to pregnancy or post-natal development, but there are indications for foetotoxicity and delayed parturition.

    The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

    Lactation

    Triptorelin is contraindicated in breastfeeding.

    The manufacturer suggests triptorelin is not recommended for use in breastfeeding.

    It is not known whether triptorelin is excreted in human breast milk. It is unlikely to be excreted in breast milk due to its high molecular weight.

    Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
    Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

    Side Effects

    Abnormal sensation in eye
    Acne
    Alanine aminotransferase increased
    Alopecia
    Amenorrhoea
    Angioedema
    Anorexia
    Anxiety
    Arthralgia
    Aspartate aminotransferase increased
    Asthenia
    Blurred vision
    Changes in mood
    Changes of blood pressure
    Confusion
    Decrease in bone mineral density
    Depression
    Diabetes mellitus
    Dizziness
    Dry mouth
    Dysmenorrhoea
    Dyspareunia
    Dyspnoea
    Dysstasia
    Dysuria
    Epiphysiolysis at the site of the hip joint
    Epistaxis
    Erectile dysfunction
    Failure of ejaculation
    Fatigue
    Gastro-intestinal symptoms
    Gout
    Gynaecomastia
    Haematuria
    Headache
    Hot flushes
    Hyperhidrosis
    Hypersensitivity reactions including anaphylaxis
    Hypertension
    Impaired memory
    Impotence
    Increase in alkaline phosphatase
    Increase in blood urea or creatinine
    Increased appetite
    Influenza-like symptoms
    Injection site reactions
    Insomnia
    Irritability
    Joint swelling
    Lability of affect
    Lethargy
    Malaise
    Menorrhagia
    Metrorrhagia
    Musculoskeletal disturbances
    Myalgia
    Nasopharyngitis
    Nervousness
    Oedema
    Orthopnoea
    Osteoarthritis
    Osteoporosis
    Ovarian enlargement
    Ovarian hyperstimulation syndrome (OHSS)
    Pain
    Paraesthesia
    Prolongation of QT interval
    Purpura
    Pyrexia
    Rash
    Reduced libido
    Rigors
    Skin reactions
    Sleep disturbances
    Somnolence
    Spinal cord compression
    Sweating
    Testicular atrophy
    Tinnitus
    Tumour flare
    Urinary obstruction
    Vaginal dryness
    Vertigo
    Visual disturbances
    Weakness
    Weight changes

    Effects on Laboratory Tests

    Suppression of the pituitary gonadal system occurs with therapeutic doses of triptorelin, which may give misleading results in relevant diagnostic tests.

    Overdosage

    It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

    The following number will direct the caller to the relevant local centre (0844) 892 0111

    Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

    Further Information

    Last Full Review Date: February 2018

    Reference Sources

    Drugs During Pregnancy and Lactation: Treatment Options and Risk Assessment, 3rd edition (2015) ed. Schaefer, C., Peters, P. and Miller, R. Elsevier, London.

    Medications and Mothers' Milk, Sixteenth Edition (2014) Hale, T and Rowe, H, Hale Publishing, Plano, Texas.

    Summary of Product Characteristics. Decapeptyl SR 3mg. Ipsen Ltd. Revised September 2017.
    Summary of Product Characteristics: Gonapeptyl Depot. Ferring Pharmaceuticals. Revised May 2015.

    The Renal Drug Handbook. Fourth Edition (2014) ed. Ashley, C and Dunleavy, A, Radcliffe Publishing Ltd, London.

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