Chemical formula: C₅₉H₈₄N₁₆O₁₂ Molecular mass: 1,209.398 g/mol
Leuprorelin interacts in the following cases:
Since androgen deprivation treatment may prolong the QT interval, the concomitant use of 1 month leuprorelin with medicinal products known to prolong the QT interval or medicinal products able to induce Torsade de pointes such as class IA (e.g. quinidine, disopyramide) or class III (e.g. amiodarone, sotalol, dofetilide, ibutilide) antiarrhythmic medicinal products, methadone, moxifloxacin, antipsychotics, etc. should be carefully evaluated.
Leuprorelin is not indicated for use in pregnant women. Safe use of leuprorelin in pregnancy has not been established clinically.
Leuprorelin injection may cause foetal harm when administered to a pregnant woman. Therefore, the possibility exists that spontaneous abortion may occur if the drug is administered during pregnancy.
Studies in animals have shown reproductive toxicity. Before starting treatment with leuprorelin, pregnancy must be excluded. There have been reports of foetal malformation when leuprorelin has been given during pregnancy.
Leuprorelin should not be used in women who are breast-feeding.
Studies in animals have shown reproductive toxicity.
When used 3-monthly at the recommended dose, leuprorelin usually inhibits ovulation and stops menstruation. Contraception is not ensured, however, by taking leuprorelin and therefore patients should use non-hormonal methods of contraception during treatment.
Patients should be advised that if they miss successive doses of leuprorelin, breakthrough bleeding or ovulation may occur with the potential for conception. Patients should be advised to see their physician if they believe they may be pregnant. If a patient becomes pregnant during treatment, the drug must be discontinued. The patient must be apprised of this evidence and the potential for an unknown risk to the foetus.
The ability to drive and use machines may be impaired due to visual disturbances and dizziness.
Adverse reactions seen with PROSTAP 3 are due mainly to the specific pharmacological action, namely increases and decreases in certain hormone levels.
The following lists show adverse reactions with leuprorelin based on experience from clinical trials as well as from post-marketing experience. Adverse reactions are grouped by MedDRA System Organ Classes and frequency classification. Frequencies are defined as: very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000); not known (cannot be estimated from the available data).
In cases where a “tumour flare” occurs after PROSTAP 3 therapy, an exacerbation may occur in any symptoms or signs due to disease, for example, bone pain, urinary obstruction, weakness of the lower extremities and paraesthesia. These symptoms subside on continuation of therapy.
List of adverse reactions:
Not known: anaemia (reported in medicinal products of this class), thrombocytopaenia, leucopenia
Not known: hypersensitivity reactions (including rash, pruritus, urticaria and rarely, wheezing or interstitial pneumonitis, anaphylactic reactions)
Very common: weight fluctuation
Common: decreased appetite
Not known: lipids abnormal, glucose tolerance abnormal
Common: insomnia, depression, mood changes (long-term use)**
Uncommon: mood changes (short term use)**
Common: headache (occasionaly severe)
Uncommon: dizziness, parasthesiae
Very rare: pituitary apoplexy has been reported following initial administration in patients with pituitary adenoma
Not known: paralysis, seizure
Not known: visual impairment
Not known: palpitations, electrocardiogram QT prolonged
Very common: hot flush
Not known: pulmonary embolism, hypertension, hypotension
Common: nausea
Uncommon: diarrhoea, vomiting
Common: hepatic function abnormal, liver function test abnormal (usually transient)
Not known: jaundice
Very common: hyperhydrosis
Very common: muscle weakness, bone pain
Common: arthralgia
Uncommon: myalgia, weakness of lower extremities
Not known: spinal fracture, reduction in bone mass which may occur with the use of GnRH agonists
Not known: interstitial lung disease
Not known: urinary tract obstruction
Very common: libido decreased, erectile dysfunction, testicular atrophy
Common: gynaecomastia
Very common: fatigue, injection site reaction, e.g. induration, erythema, pain, abscesses, swelling, nodules, ulcers and necrosis
Common: oedema peripheral
Not known: pyrexia
** mood changes (long term use: frequency of ‘common’ and short term use: frequency of 'uncommon'
Those adverse events occurring most frequently with PROSTAP 3 are associated with hypo-estrogenism; the most frequently reported are hot flushes, mood swings including depression (occasionally severe), and vaginal dryness. Estrogen levels return to normal after treatment is discontinued.
The induced hypo-estrogenic state results in a small loss in bone density over the course of treatment, some of which may not be reversible.
Vaginal haemorrhage may occur during therapy due to acute degeneration of submucous fibroids.
List of adverse reactions:
Not known: anaemia (reported in medicinal products of this class), thrombocytopaenia, leucopenia
Not known: hypersensitivity reactions (including rash, pruritus, urticaria and rarely, wheezing and interstitial pneumonitis, anaphylactic reactions)
Common: weight fluctuation
Uncommon: decreased appetite, lipids abnormal
Not known: glucose tolerance abnormal, which may affect diabetic control
Very common: insomnia
Common: mood altered depression
Very common: headache (occasionally severe)
Common: parasthesiae, dizziness
Very rare: pituitary haemorrhage has been reported following initial administration in patients with pituitary adenoma
Not known: paralysis, seizure
Uncommon: visual impairment
Uncommon: palpitations
Very common: hot flush
Not known: pulmonary embolism, hypertension, hypotension
Common: nausea
Uncommon: diarrhoea, vomiting
Uncommon: liver function test abnormal (usually transient)
Not known: hepatic function abnormal, jaundice
Uncommon: hair loss
Common: arthralgia, muscle weakness
Uncommon: myalgia
Not known: spinal fracture, reduction in bone mass which may occur with the use of GnRH agonists
Not known: interstitial lung disease
Common: breast tenderness, breast atrophy, vulvovaginal dryness
Not known: vaginal haemorrhage
Common: oedema peripheral, injection site reaction e.g. injection site induration, erythema, pain, abscesses, swelling, nodules, ulcers and necrosis
Uncommon: pyrexia, fatigue
In women with early breast cancer treated with a GnRH agonist, in combination with tamoxifen or an aromatase inhibitor, the most commonly observed adverse reactions included hot flush, musculoskeletal disorders, fatigue, insomnia, hyperhidrosis, vulvovaginal dryness and depression.
In the initial phase of therapy, a short-term increase as flare-up of the sex hormone level occurs, followed by a decrease to values within the pre-pubertal range. Due to this pharmacological effect, adverse events may occur particularly at the beginning of treatment.
List of adverse reactions:
Very rare: hypersensitivity (fever, rash, e.g. itching, anaphylactic reactions)
Common: emotional lability
Common: headache
Very rare: pituitary haemorrhage following initial administration in patients with pituitary adenoma
Not known: seizure
Common: abdominal pain/abdominal cramps, nausea/vomiting
Common: acne
Not known: interstitial lung disease
Common: vaginal haemorrhage, spotting**, vaginal discharge
Common: injection site reactions
** In general, the occurrence of vaginal spotting with continued treatment (subsequent to possible withdrawal bleeding in the first month of treatment) should be assessed as a sign of potential underdosage. The pituitary suppression should then be determined by an LHRH test.
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