A synthetic decapeptide analogue of natural GnRH. Diferelin®, after a short initial period of stimulation gonadotropic pituitary function, has an inhibitory effect on gonadotropin secretion followed by suppression of testicular and ovarian function.
Constant application Diferelin® drug inhibits secretion of ovarian estrogen to menopausal status, and reduces testosterone secretion, which can reach concentrations of indicators are observed following surgical castration.
Absorption and distribution
After the / m of slurry comes initial phase of rapid release of the active substance, followed by constant release phase. Thus triptorelin Cmax in plasma is 0.32 ± 0.12 ng / ml, and the average number of released permanently triptorelin was 46.6 ± 7.1 ug / day.
The bioavailability of the drug when administered one time per month is 53%.
Ipsen Pharma, France
1 vial contains:
The active ingredient is:
triptorelin acetate, triptorelin, based on 3.75 mg *
* – taking into account features of the dosage form in the formulation an excess of active agent incorporated for administration of an effective dose.
copolymer of D, L-lactic and glycolic acids – about 160 mg (the number depends on the level of encapsulation),
Mannitol – 85 mg,
carmellose sodium – 30 mg,
Polysorbate 80 – 2 mg.
The solvent :
mannitol – 16 mg,
water d / and – up to 2000 mg.
prostate cancer; genital and extragenital endometriosis; precocious puberty; female infertility (in vitro fertilization); Uterine fibroids (before surgery).
- lactation (breastfeeding);
- hypersensitivity to triptorelin, other ingredients and other GnRH analogues.
Be wary: should be prescribed for osteoporosis.
Allergic reactions: urticaria, rash, pruritus; very rarely – angioedema. On the part of the reproductive system: male – reduced potency; women – headache, depression, sweating and changes in libido, dryness of the vagina, dyspareunia, and change the size of the mammary glands.
When used in combination with gonadotropins reported cases of ovarian hyperstimulation syndrome. In the treatment of precocious puberty in girls may experience bleeding from the vagina. Long term use of the drug can cause hypogonadotropic amenorrhoea.
On the part of the musculoskeletal system: long-term use – demineralization of the bones, that is the risk of developing osteoporosis. At the beginning of treatment for prostate cancer patients may experience a temporary increase in bone pain, metastatic sites (symptomatic treatment). There have been isolated cases of ureteric obstruction and symptoms associated with metastatic spinal cord compression (run 1-2 weeks). Also, a temporary increase in the activity of acid phosphatase in the blood plasma can be observed during this period.
From the digestive system: in rare cases – nausea, vomiting.
From CNS: in rare cases – the increased emotional lability, impaired vision.
Cardio-vascular system: in rare cases – arterial hypertension, feeling the tides.
Local reactions: in single cases – pain at the injection site.
Other: in rare cases – an increase in body weight, increased body temperature.
How to accept, acceptance rate and dosage
The drug is administered only / m.
In prostate cancer Diferelin® administered at a dose of 3.75 mg (1 injection) every 4 weeks long.
In premature puberty drug prescribed to patients weighing more than 20 kg of 3,75 mg every 28 days, patients weighing less than 20 kg – 1,875 mg for every 28 days.
In endometriosis drug is administered in a dose of 3.75 mg 1 every 4 weeks. The injection is carried out in the first 5 days of the menstrual cycle. Duration of treatment – no more than 6 months.
In female infertility drug administered in a dose of 3.75 mg (1 injection) on the 2nd day of the cycle. Communication with gonadotropins should be controlled after pituitary desensitization (plasma concentration of estrogen less than 50 pg / ml generally determined after 15 days after the injection Diferelin®).
When uterine fibroids drug should be administered during the first 5 days of the menstrual cycle. The drug is prescribed to 3.75 mg every 4 weeks. The duration of treatment is 3 months for patients being prepared for operation.
Terms slurry preparation and administration
A suspension for a / m administration is prepared by dissolving the lyophilisate in the attached solvent just prior to administration. Mix the contents of the vial with caution until a homogeneous suspension.
Cases of incomplete injections resulting in the loss of more slurry than is normally left in the syringe for injection, it is necessary to inform the attending physician.
The introduction should be carried out in strict accordance with the instructions.
The patient should be in a prone position. Disinfect the skin of the buttocks.
- Break the ampoule neck (the point on the right side on top).
- Enter the solvent into the syringe with a needle.
- Remove the protective plastic cover from the top of the bottle.
- Drag the solvent into the vial of lyophilisate.
- Pull the needle so that it remains in the bottle, but not touch the suspension.
- Not turning the vial, gently shake the contents until a homogeneous suspension.
- Check the agglomerates before they will type suspension in the syringe (in the absence of agglomerates, stir until homogeneous).
- Not turning the vial into the syringe, type the entire suspension.
- Remove the needle that was used to prepare a suspension, and attach tightly onto the other needle tip of the syringe. Hold only the tip of the color.
- Remove air from the syringe.
- Immediately inject in the gluteal muscle.
- Dispose of the needle in the container for sharp objects.
At temperatures above 25 ° C
Drug interaction Diferelin® preparation is not described.
Early treatment may increase the clinical symptoms, and therefore should be used with caution in Diferelin® prostate cancer patients at risk of developing ureteric obstruction or spinal cord compression. Careful medical supervision in these patients during the first month of therapy.
Prior to initiating therapy Diferelin necessary to confirm the absence of pregnancy.
With careful use of the drug in patients with polycystic ovary syndrome during ovulation stimulation regimens. This is due to the fact that a small number of patients may increase the number of induced follicles.
It is necessary to carefully monitor the level of stimulation in vitro fertilization cycle to identify patients at risk of developing ovarian hyperstimulation syndrome because the frequency and severity of manifestations of the syndrome may be dependent on the dosing regimen of gonadotropin. If necessary, the introduction of human chorionic gonadotropin should be discontinued.
Effects on ability to drive vehicles and other machines that require high concentration of attention
No data available.
Pregnancy and lactation
Diferelin® contraindicated during pregnancy and lactation (breastfeeding).
So far, cases of drug overdose Diferelin® were reported.