Dipherelin - Instructions For Use, 3.75 Mg, Price, Reviews, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Diphereline

Dipherelin: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Drug interactions
11. 11. Analogs
12. 12. Terms and conditions of storage
13. 13. Terms of dispensing from pharmacies
14. 14. Reviews
15. 15. Price in pharmacies

Latin name: Diphereline

ATX code: L02AE04

Active ingredient: triptorelin (triptorelin)

Producer: Beaufour Ipsen Pharma (France)

Description and photo update: 2019-13-08

Prices in pharmacies: from 1650 rubles.

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Diphereline is a drug with antitumor activity.

Release form and composition

Diphereline is available in the following dosage forms:

• Lyophilisate for the preparation of a solution for subcutaneous administration: almost white, dispersed in the supplied solvent, followed by the formation of a practically free of particles, transparent solution; solvent - a colorless transparent solution (in colorless glass vials, 7 vials in a cardboard box, complete with solvent (in 1 ml ampoules, 7 ampoules in a package));
• Lyophilisate for the preparation of a suspension for intramuscular administration of prolonged action: white with a creamy (3.75 mg each) or yellowish (11.25 mg each) shade or white, dispersed in the supplied solvent to form a suspension of white with creamy (3.75 mg each)) either yellowish (11.25 mg each) or white (in slightly darkened glass bottles, 1 bottle in a cardboard box, complete with a disposable polypropylene syringe, solvent (in 2 ml ampoules, 1 ampoule per package), needles for injection (2 pcs.)).

The composition of 1 bottle with a lyophilisate for the preparation of a solution for subcutaneous administration of Dipherelin includes:

• Active ingredient: triptorelin - 0.1 mg (in the form of triptorelin acetate);
• Auxiliary component: mannitol - 10 mg.

Solvent: sodium chloride - 9 mg, water for injection - up to 1000 mg.

The composition of 1 bottle with a lyophilisate for the preparation of a suspension for intramuscular administration of prolonged action of Dipherelin includes:

• Active substance: triptorelin - 3.75 or 11.25 mg (in the form of triptorelin acetate; to ensure the administration of an effective dose, an excess of the substance is included in the preparation);
• Auxiliary components (respectively 3.75 / 11.25 mg): copolymer of D, L-lactic and glycolic acids - about 160/250 mg, mannitol - 85/85 mg, sodium carmellose - 30/30 mg, polysorbate 80 - 2 / 2 mg.

Solvent: mannitol - 16 mg, water for injection - up to 2000 mg.

Pharmacological properties

Diphereline is a hormonal drug considered to be analogous to the natural gonadotropin-releasing hormone.

Pharmacodynamics

Triptorelin belongs to synthetic decapeptides. Immediately after entering the body, it stimulates the gonadotropic function of the pituitary gland for a short period of time, after which inhibition of the secretion of gonadotropins is observed, followed by inhibition of the function of the ovaries and testicles. At the initial stage of using Dipherelin, the level of follicle-stimulating (FSH) and luteinizing (LH) hormones in the blood temporarily increases, which causes an increase in the concentration of estradiol in women and testosterone in men ("flash"). With long-term treatment with triptorelin, the concentration of FSH and LH decreases, which contributes to a decrease in the content of estradiol (to values corresponding to the state of postovariectomy) and testosterone (to values corresponding to the state after testiculectomy). A similar phenomenon is observed approximately on the 20th day after the first injection of Dipherelin. In the future, the concentration of hormones remains unchanged throughout the entire period of therapy.

Long-term use of triptorelin reduces the production of estradiol in women and, accordingly, prevents the development of endometrioid ectopias.

Triptorelin inhibits the gonadotropic hyperfunction of the pituitary gland during premature puberty in both boys and girls, which is expressed in suppressing the secretion of testosterone or estradiol, reducing the maximum concentration of LH and improving the ratio of bone and calendar ages.

Pharmacokinetics

With intramuscular injection of Dipherelin at a dose of 11.25 mg, the maximum concentration of its active component in the blood plasma is determined approximately 3 hours after injection. The duration of the phase of gradual decrease in concentration is 1 month after the start of treatment, after which, until the 90th day, the content of circulating triptorelin remains stable: about 0.04‒0.05 ng / ml - in the treatment of endometriosis, about 0.1 ng / ml - with treatment of prostate cancer.

Indications for use

Solution for subcutaneous administration

According to the instructions, Dipherelin is prescribed for the treatment of female infertility: to stimulate the ovaries together with gonadotropins (human menopausal gonadotropin (hMG), human chorionic gonadotropin (hCG), follicle-stimulating hormone (FSH)) in in vitro fertilization and embryo transfer programs assisted reproductive technologies.

Sustained-release suspension for intramuscular administration

• Prostate cancer (locally advanced (either as monotherapy or as an adjuvant against the background of radiation therapy), metastatic);
• Premature puberty;
• Endometriosis (extragenital and genital);
• Fibroids of the uterus (before surgery);
• Female infertility (in in vitro fertilization programs).

Contraindications

• Hormone-independent prostate cancer, conditions after surgical testiculectomy;
• Pregnancy and breastfeeding period;
• Hypersensitivity to the components of the drug and other analogs of gonadotropin-releasing hormone (GnRH).

Suspension Dipherelin 3.75 mg and 11.25 mg should be prescribed with caution in osteoporosis and polycystic ovary syndrome.

Instructions for the use of Dipherelin: method and dosage

Solution for subcutaneous administration

Diphereline is administered subcutaneously.

One of 2 courses of treatment is possible:

• Short: daily, 0.1 mg per day, starting on the second day of the cycle (at the same time starting to conduct ovarian stimulation). The therapy is completed 1 day before the scheduled administration of human chorionic gonadotropin. The duration of the course is 10-12 days;
• Long-term: daily, 0.1 mg per day, starting from the second day of the cycle. When the pituitary gland is desensitized (E2 is less than 50 pg / ml, i.e., approximately on the fifteenth day after the start of therapy), stimulation of the ovaries with gonadotropins begins, continuing subcutaneous injections at the same dose. The course is completed 1 day before the scheduled administration of human chorionic gonadotropin. The doctor determines the duration of treatment individually.

To prepare the solution, the supplied solvent must be introduced into the vial with the lyophilisate, and then shaken until completely dissolved.

Sustained-release suspension for intramuscular administration

Diphereline is injected only intramuscularly, into the gluteus muscle.

The dosage regimen depends on the indications:

• Prostate cancer: long-term, 3.75 mg (1 injection) every 4 weeks or every 3 months, 11.25 mg. When treating simultaneously with radiation therapy, long-term antiandrogen therapy (3 years) is preferable to short-term (6 months);
• Premature puberty: every 28 days, 1.875 mg (with a body weight of up to 20 kg) or 3.75 mg (with a body weight of 20 kg);
• Endometriosis: once every 4 weeks at 3.75 mg or once every 3 months at 11.25 mg; the injection must be carried out in the first 5 days of the menstrual cycle. The duration of the course is up to 6 months. The duration of therapy is determined by the severity of endometriosis and the clinical picture (anatomical and functional changes) during therapy. Repeated treatment with triptorelin or another GnRH analog is not recommended;
• Female infertility: 1 injection of 3.75 mg on the second day of the cycle. The connection with gonadotropins should be monitored after desensitization of the pituitary gland (the concentration of estrogen in the blood plasma is less than 50 pg / ml is usually determined 15 days after the administration of Dipherelin);
• Fibroids of the uterus: every 4 weeks, 3.75 mg. The suspension must be administered in the first 5 days of the menstrual cycle. For patients preparing for surgery, the duration of the course of treatment is 3 months.

A suspension for intramuscular administration is prepared immediately before the procedure by dissolving the lyophilisate in the supplied solvent.

Side effects

Solution for subcutaneous administration

At the beginning of the use of Dipherelin, when combined with gonadotropins, disorders of the reproductive system may occur in the form of ovarian hyperstimulation (abdominal pain, an increase in the size of the ovaries).

During therapy, the following side effects may develop:

• Reproductive system: very often - vaginal dryness, sudden flushes, dyspareunia and decreased libido associated with pituitary-ovarian blockade;
• Digestive system: vomiting, nausea, increased activity of hepatic transaminases;
• Central and peripheral nervous system: visual impairment, emotional lability, headache;
• Musculoskeletal system: joint and muscle pain; with prolonged therapy with GnRH analogs - bone demineralization, the risk of osteoporosis (this violation is not observed with short-term use of Dipherelin at a dose of 0.1 mg);
• Cardiovascular system: increased blood pressure;
• Allergic reactions: skin rash, hives, itching; rarely - Quincke's edema;
• Local reactions: pain at the injection site;
• Others: weight gain.

Sustained-release suspension for intramuscular administration

• Musculoskeletal system: with prolonged therapy - bone demineralization, which is a risk factor for the development of osteoporosis. At the beginning of therapy for prostate cancer, patients may experience a temporary increase in pain in the bones affected by metastases (symptomatic treatment is indicated). In some cases - obstruction of the ureters and the appearance of signs associated with compression by metastases of the spinal cord (disappear in 7-14 days). Also at this time, there may be a short increase in the activity of acid phosphatase in the blood plasma;
• Cardiovascular system: in isolated cases - a feeling of hot flashes, arterial hypertension;
• Central nervous system: in isolated cases - visual impairment, increased emotional lability;
• Reproductive system: men - decreased potency; women - depression, headache, change in libido, sweating, change in the size of the mammary glands, dryness of the vaginal mucosa, dyspareunia; with simultaneous use with gonadotropins - the development of ovarian hyperstimulation syndrome; in the treatment of premature puberty in girls - spotting from the vagina; with prolonged treatment - hypogonadotropic amenorrhea;
• Digestive system: in isolated cases - vomiting, nausea;
• Allergic reactions: rash, hives, itching; very rarely - Quincke's edema;
• Local reactions: in isolated cases - pain at the injection site of the suspension;
• Others: in isolated cases - an increase in body temperature, an increase in body weight.

Overdose

There are no reports of overdose cases of Dipherelin at the moment. In the course of experiments on animals, results were obtained that suggest the effect of triptorelin in very high doses on the level of sex hormones and, accordingly, on the state of the reproductive system. In case of an overdose of the drug, symptomatic therapy is prescribed, if necessary.

special instructions

Before starting to use Dipherelin, pregnancy must be excluded.

Solution for subcutaneous administration

The response of the ovaries to the subcutaneous administration of the solution simultaneously with gonadotropins in predisposed patients may increase significantly, in particular, with polycystic ovaries.

The response of the ovaries to the introduction of Dipherelin together with gonadotropins in different patients may differ, even in the same women with different cycles, the response may be different.

Stimulation of ovulation must be carried out under the supervision of a physician, carrying out regular analyzes using clinical and biological methods: ultrasound echography and an increase in the content of estrogen in the plasma. If there is an excessive ovarian response, it is recommended to interrupt the stimulation cycle by stopping the injection of gonadotropin.

Since, in some cases, visual impairment may occur during therapy, caution should be exercised when driving vehicles and performing potentially hazardous types of work that require a high concentration of attention and quick psychomotor reactions.

Sustained-release suspension for intramuscular administration

At the beginning of therapy, an increase in clinical signs is possible, which is why Dipherelin should be prescribed with caution to patients with prostate cancer who are at risk of developing spinal cord compression or ureteral obstruction. During the first month of therapy, the condition of such patients requires careful medical supervision.

Against the background of polycystic ovary disease, when carrying out ovulation stimulation schemes, Diphereline should be used with caution, since this can lead to an increase in the number of induced follicles.

With in vitro fertilization, it is necessary to carefully monitor the level of cycle stimulation (to identify patients at risk of developing ovarian hyperstimulation syndrome). If necessary, the introduction of human chorionic gonadotropin should be discontinued.

Application during pregnancy and lactation

During pregnancy, the administration of triptorelin is contraindicated, since such treatment can provoke an abortion or the appearance of intrauterine malformations in the fetus. Before starting treatment in patients of reproductive age, pregnancy should be excluded by conducting a thorough examination. During the course of therapy with Dipherelin, it is necessary to use non-hormonal methods of contraception until the menstrual cycle is restored.

During lactation, the use of Dipherelin is strictly prohibited.

Drug interactions

There are no data on the interaction of Dipherelin with other drugs.

Analogs

The analogue of Dipherelin is Decapeptyl Depot.

Terms and conditions of storage

Keep out of reach of children at temperatures up to 25 ° C.

Shelf life:

• Lyophilisate for preparation of solution for subcutaneous administration - 2 years;
• Lyophilisate for preparing a suspension for intramuscular injection: 3.75 mg - 2 years, 11.25 mg - 3 years; solvent - 5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews of Diphereline

Almost all reviews about Dipherelin left by gynecologists are positive. They recommend using the drug only as directed by a specialist and in accordance with the instructions. Among patients, there are negative opinions about the drug, which may be due to the individual body's response to triptorelin. After adjusting the dose of Dipherelin and the duration of treatment, side effects are usually not observed.

Price for Diphereline in pharmacies

The approximate price for Dipherelin in the form of a lyophilisate for the preparation of a solution for subcutaneous administration is 2576-2744 rubles. It is possible to purchase a lyophilisate for the preparation of a suspension for intramuscular administration of prolonged action of Dipherelin 3.75 mg for 6,694 - 7,500 rubles, and Dipherelin 11.25 mg for 19,582 - 21,998 rubles.

Differelin: prices in online pharmacies

Drug name Price Pharmacy

Diphereline 0.1 mg lyophilisate for preparation of a solution for subcutaneous administration complete with a solvent 7 pcs. 1650 RUB Buy

Diphereline 3.75 mg lyophilisate for preparation of a suspension for intramuscular administration of prolonged action complete with a solvent 1 pc. 4392 RUB Buy

Diphereline pore. d / inv. suspension fl. 3.75mg (complete with solution, amp., Disposable syringe and 2 needles) 6299 RUB Buy

Diphereline 11.25 mg lyophilisate for preparation of a suspension for intramuscular administration of prolonged action complete with a solvent 1 pc. RUB 14800 Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!