Chemical formula: C₆₀H₈₆N₁₆O₁₃ Molecular mass: 1,239.447 g/mol
Buserelin interacts in the following cases:
Since androgen deprivation treatment may prolong the QT interval, the concomitant use of buserelin 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.
During treatment with buserelin, the effect of antidiabetic agents may be attenuated.
During treatment with buserelin, the effect of antidiabetic agents may be attenuated.
Androgen deprivation therapy may prolong the QT interval. In patients with a history of or risk factors for QT prolongation and in patients receiving concomitant medicinal products that might prolong the QT interval physicians should assess the benefit risk ratio including the potential for Torsade de pointes prior to initiating buserelin.
In patients with hypertension, blood pressure must be monitored regularly (risk of deterioration of blood pressure levels).
The use of LHRH-agonists may be associated with decreased bone density and may lead to osteoporosis and an increased risk of bone fracture. Particular caution is necessary in patients with additional risk factors for osteoporosis (e.g. chronic alcohol abuse, smokers, long-term therapy with anticonvulsants or corticosteroids or a family history of osteoporosis) It is recommended to periodically monitor bone mineral density (BMD) and use preventative measures during therapy to prevent osteopenia/osteoporosis.
In some patients treated with GnRH-agonists, change in glucose tolerance is observed. In diabetic patients blood glucose levels must be checked regularly (risk of deterioration of metabolic control).
Buserelin is contraindicated in pregnancy. It is intended for the treatment of advanced prostatic carcinoma, it should not be used in pregnant or lactating women.
Buserelin passed into breast milk in small amounts. Although negative effects on the infant have not been observed, it is recommended that breast-feeding be avoided during treatment with Suprefact in order to prevent the infant from ingesting small quantities of buserelin with breast milk.
Certain adverse effects (eg. dizziness) may impair the ability to concentrate and react, and therefore constitute a risk in situations where these abilities are of special importance (eg. operating a vehicle or machinery).
The following CIOMS frequency rating is used: Very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1000 to <1/100); rare (≥1/10 000 to <1/1000); very rare (<1/10 000), not known (cannot be estimated from the available data).
In isolated cases severe hypersensitivity reactions with shock can occur. These may become manifest as reddening of the skin, itching, skin rashes (including urticaria) and allergic asthma with dyspnoea as well as, in isolated cases leading to anaphylactic/anaphylactoid shock.
After administration of the injection, pain or local reaction at the injection site is possible.
At the beginning of treatment, a transient rise in the serum testosterone level usually develops and may lead to temporary activation of the tumour with secondary reactions such as:
Such reactions can be largely avoided when an anti-androgen is given concomitantly in the initial phase of buserelin treatment. However, even with concomitant anti-androgen therapy, a mild but transient increase in tumour pain as well as a deterioration in general well being may develop in some patients.
Buserelin treatment may also lead to:
Neoplasms benign and malignant: Very rare cases of pituitary adenomas were reported during treatment with LH-RH agonists, including buserelin.
Blood disorders: Very rare cases of thrombocytopenia or leucopenia.
Metabolism and nutrition disorders: Frequent increase or decrease in weight Occasional changes in appetite and increased thirst. Rarely increase or decrease in blood lipid levels. Very rarely, reduction in glucose tolerance which may lead to the worsening of metabolic control in diabetics.
Psychiatric disorders: Frequent nervousness, emotional instability. Occasional anxiety, depression or worsening of existing depression.
Mood changes, depression. Frequency:
Long term use: Common
Short term use: Uncommon
Nervous system disorders: Dizziness, headache, sleep disturbances, tiredness, drowsiness. Occasional paraesthesia (especially in the arms or legs), disturbances of memory and concentration.
Eye disorders: Occasional dry eyes (possibly leading to eye irritations in people who wear contact lenses), impaired vision (eg blurred vision), feeling of pressure behind the eyes.
Ear and labyrinth disorders: Rare cases of tinnitus, hearing disorders found.
Cardiac disorders: Frequent palpitations.
Frequency unknown: QT prolongation
Vascular disorders: Occasional oedema (of face and extremities) and hot flushes. Very rare cases of a deterioration of blood pressure levels in patients with hypertension.
Gastrointestinal disorders: Frequent lower abdominal pain, stomach ache, nausea, vomiting, diarrhoea, constipation.
Hepato-biliary disorders: Occasional, increase in serum liver enzyme levels (e.g. transaminases), increase in serum bilirubin.
Skin and subcutaneous tissue disorders: Frequent dry skin, acne, increase or decrease in scalp hair (alopecia, hirsutism). Occasional increase or decrease in body hair, splitting nails.
Musculoskeletal and bone disorders: Frequent musculoskeletal discomfort and pain (including shoulder pain/stiffness). The use of LHRH-agonists may be associated with decreased bone density and may lead to osteoporosis and an increased risk of bone fracture. The risk of skeletal fracture increases with the duration of therapy.
Reproductive system and breast disorders: Occasional gynaecomastia (increase in breast size) which is usually painless, atrophy of the testes, decrease in libido and potency (in most patients; result of hormone deprivation).
Most of the effects listed above are directly or indirectly related to the suppression of testosterone by buserelin (symptoms of androgen deficiency).
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