Follitropin Alfa + Lutropin Alfa

Follitropin Alfa + Lutropin Alfa Uses, Dosage, Side Effects, Food Interaction and all others data.

Lutropin alfa is a recombinant human luteinizing hormone produced in yeast with 2 subunits, alpha = 92 residues, beta = 121 residues. It is a heterodimeric glycoprotein made up of monomeric units. Lutropin alfa was the first and only recombinant human form of luteinizing hormone (LH) developed for use in the stimulation of follicular development. Its pharmacological action mimics the biological activity of endogenous LH; an acute rise of LH, or LH surge, in females triggers ovulation and the development of the corpous luteum. In males, LH stimulates Leydig cell to produce testosterone.

Used to facilitate female conception, lutropin alfa performs the same actions as luteinizing hormone (LH), which is normally produced in the pituitary gland. Lutropin is usually given in combination with follitropin alfa. Together they stimulate the development of a follicle to prepare the reproductive tract for implementation and pregnancy. Lutropin alfa also stimulates the theca cells to produce androgens and the secretion of estradiol by the follicles. Lutropin alfa and follitropin alfa are discontinued once ultrasound assessment and serum estradiol concentrations show sufficient follicular maturation. hCG is then administered to complete follicular maturation and induce ovulation. In females, a LH surge about halfway through the menstrual cycle triggers the onset of ovulation. Lutropin alfa substitutes for endogenous LH and induces rupture of the preovulatory ovarian follicle and oocyte expulsion. Lutropin alfa induces and maintains the corpus luteum, which then secretes progesterone.

Follitropin Alfa + Lutropin Alfa
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Follitropin Alfa + Lutropin Alfa
Generic	Follitropin Alfa + Lutropin Alfa
Type
Therapeutic Class	Drugs for Infertility
Manufacturer
Available Country	Bangladesh
Last Updated:	September 24, 2024 at 5:38 am

Uses

This injection is indicated for the stimulation of follicular development in adult women with severe LH and FSH deficiency. In clinical trials, these patients were defined by an endogenous serum LH level < 1.2 IU/L.

Follitropin Alfa + Lutropin Alfa is also used to associated treatment for these conditions: Hypogonadism, Infertility

How Follitropin Alfa + Lutropin Alfa works

Luteinizing hormone binds to a receptor shared with the human chorionic gonadotropin hormone (hCG) on the ovarian theca (and granulosa) cells and testicular Leydig cells. This LH/CG transmembrane receptor is a member of the super-family of G protein-coupled receptors. Adenylate cyclase then activates many other pathways leading to steroid hormone production and other follicle maturation processes.

Dosage

Follitropin Alfa + Lutropin Alfa dosage

In LH and FSH deficient women (hypogonadotrophic hypogonadism), the objective of this injection therapy is to develop a single mature Graafian follicle from which the oocyte will be liberated after the administration of human chorionic gonadotrophin (hCG). This injection should be given as a course of daily injections. Since these patients are amenorrhoeic and have low endogenous oestrogen secretion, treatment can commence at any time.Treatment should be tailored to the individual patient's response as assessed by measuring follicle size by ultrasound and oestrogen response.A recommended regimen commences with one vial of this injection daily. If less than one vial daily is used, the follicular response may be unsatisfactory because the amount of lutropin alfa may be insufficient.If an FSH dose increase is deemed appropriate, dose adaptation should preferably be after 7-14 day intervals and preferably by 37.5-75 IU increments using a licensed follitropin alfa preparation. It may be acceptable to extend the duration of stimulation in any one cycle to up to 5 weeks.When an optimal response is obtained, a single injection of 250 micrograms of r-hCG or 5,000 IU to 10,000 IU hCG should be administered 24-48 hours after the last this injection. The patient is recommended to have coitus on the day of, and on the day following, hCG administration. Alternatively, intrauterine insemination (IUI) may be performed.Luteal phase support may be considered since lack of substances with luteotrophic activity (LH/hCG) after ovulation may lead to premature failure of the corpus luteum.If an excessive response is obtained, treatment should be stopped and hCG withheld. Treatment should recommence in the next cycle at a dose of FSH lower than that of the previous cycle. This injection is intended for subcutaneous administration. The first injection should be performed under direct medical supervision. The powder should be reconstituted immediately prior to use with the solvent provided. Self-administration should only be performed by patients who are well motivated, adequately trained and with access to expert advice.

Side Effects

Ovarian cysts, mild to severe Inj site reactions, headache, mild to moderate ovarian hyperstimulation syndrome (OHSS), abdominal pain, GI disturbances. Rarely, severe OHSS, ovarian torsion, thromboembolism, mild systemic allergic reactions.

Toxicity

Lutropin alfa is not indicated for people under 16 and over 60, pregnant and lactating women, patients with uncontrolled thyroid and adrenal failure, patients with active, untreated tumours of the hypothalamus and pituitary gland, and in any patient with a condition that makes a normal pregnancy possible such as primary ovarian failure or fibroid tumors of the uterus.

Precaution

This injection contains potent gonadotrophic substances capable of causing mild to severe adverse reactions, and should only be used by physicians who are thoroughly familiar with infertility problems and their management.Gonadotrophin therapy requires a certain time commitment by physicians and supportive health care professionals, as well as the availability of appropriate monitoring facilities. In women, safe and effective use of this injection calls for monitoring of ovarian response with ultrasound, alone or preferably in combination with measurement of serum oestradiol levels, on a regular basis. There may be a degree of interpatient variability in response to FSH/LH administration, with a poor response to FSH/LH in some patients. The lowest effective dose in relation to the treatment objective should be used in women.

Interaction

This injection should not be administered as a mixture with other medicinal products, in the same injection, except follitropin alfa for which studies have shown that co-administration does not significantly alter the activity, stability, pharmacokinetic nor pharmacodynamic properties of the active substances.

Volume of Distribution

The steady state volume of distribution is around 10-14 L.

Elimination Route

Mean absolute bioavailability is 56%, following sub-Q administration, maximum serum concentrations reached after 4–16 hours. Time to peak, serum: 9 hours

Half Life

Biphasic; terminal half-life is approximately 18 hours.

Clearance

2 – 3 L/h [healthy female following subcutaneous administration]

Elimination Route

Total body clearance is approximately 2 to 3 L/h with less than 5 percent of the dose being excreted unchanged renally.

Pregnancy & Breastfeeding use

There is no indication for the use of this injection during pregnancy. Data on a limited number of exposed pregnancies indicate no adverse reactions of follitropin alfa and lutropin alfa on pregnancy, embryonal or foetal development, parturition or postnatal development following controlled ovarian stimulation. No teratogenic effect of such gonadotropins has been reported in animal studies. In case of exposure during pregnancy, clinical data are not sufficient to exclude a teratogenic effect of this injection. This not indicated during breast-feeding.

Contraindication

This injection is contraindicated in patients with: hypersensitivity to the active substances or to any of the excipients tumours of the hypothalamus and pituitary gland ovarian enlargement or ovarian cyst unrelated to polycystic ovarian disease and of unknown origin gynaecological haemorrhages of unknown origin ovarian, uterine or mammary carcinoma This injection must not be used when an effective response cannot be obtained, such as: primary ovarian failure malformations of sexual organs incompatible with pregnancy fibroid tumours of the uterus incompatible with pregnancy

Special Warning

Elderly: There is no relevant indication for the use of this injection in the elderly population. Safety and effectiveness of this medicinal product in elderly patients have not been established.Renal and hepatic impairment: Safety, efficacy, and pharmacokinetics of this medicinal product in patients with renal or hepatic impairment have not been established.Paediatric population: There is no relevant use of this medicinal product in the paediatric population.