Drug information of Follitropin alfa

Follitropin alfa

Drug group:

Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin. Follitropin is important in the development of follicles produced by the ovaries.

Mechanism of effect

Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor.

 Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells.

Pharmacodynamic

Used for the treatment of female infertility, Follitropin or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin is the primary hormone responsible for follicular recruitment and development.

Pharmacokinetics

  • Onset: 2.7-18 months (spermatogenesis); within cycle (females)
  • Vd: 10 L
  • Bioavailability: 66-76% (healthy female volunteers)
  • Half-life: 50 hr (IM in healthy female volunteers); 24 hr (SC in healthy female volunteers)
  • Peak plasma time: 8-16 hr (SC in females); 25 hr (IM in females); 11-20 hr (IM in males)

Dosage

Adult

Ovulation Induction

Initial dose of first cycle: 75 IU SC qDay; after 14 days, increase dose by increments of up to 37.5 IU; further dose increases, as necessary every 7 days

Dose based on effect, with lowest effective dose; maximum recommended dose 300 International Units qDay

To complete follicular development in absence of endogenous LH surge, give chorionic gonadatropin (hCG)- 5000 units 1 day after last dose

Withhold if serum estradiol >2,000 pg/mL or if abnormal ovarian enlargement/abdominal pain

Initial dose in subsequent cycles based on response in previous cycle

Advise daily intercourse beginning on day prior to hCG until ovulation apparent from lab tests

Initial dose on cycle day 2 or 3: 150 IU SC qDay until sufficient follicular development; typically does not exceed 10 days

If endogenous gonadotropin levels are suppressed, should be started at 225 IU qDay

Continue until adequate follicular development based on ultrasound and serum estradiol levels; dose adjustments of 75-150 IU may be made q3-5Days

Maximum recommended dose 450 IU qDay

Male Patients with Hypogonadotropic Hypogonadism (Gonal-f Only)

Pretreat with hCG (1,000- 2,250 USP IU 2-3 x/week) until serum testosterone within normal range (may require 3-6 months of treatment)

Treatment consists of Gonal-f 150 IU SC 3 times/week used in conjunction with hCG

hCG 1000 USP Units (or dose to maintain normal serum testosterone levels) 3 x/week

If azoospermia persists, may increase dose to 300 IU 3 x/week

May need to administer for up to 18 months for adequate response

Pediatric

Safety and efficacy not established

Interactions

Buserelin , Ganirelix

Alerts

May cause Ovarian Hyperstimulation Syndrome (OHSS, dramatic increase in vascular permeability which can result in rapid fluid accumulation in peritoneal cavity, thorax and pericardium; accompanied by severe pelvic pain, nausea, vomiting and weight gain) in women with or without pulmonary or vascular complications

If ovaries are abnormally enlarged on last day of GONAL-f therapy, do not administer hCG

Pulmonary conditions (atelactasis, ARDS, & asthma exacerbation) have been reported

Possibility of multiple births (range 12.3%-44.0% live births)

A thorough gynecologic & endocrinological evaluation should be conducted prior to treatment to rule out primary ovarian failure, early pregnancy & partner's fertility potential

Points of recommendation

  • This medicine may raise the chance of very bad side effects like blood clots and lung problems. Rarely, these effects have been deadly. Talk with the doctor.

Women:

  • This medicine may raise the chance of getting pregnant with more than one baby.
  • Limit working out while undergoing ovarian stimulation. Talk with your doctor.
  • The rate of pregnancy loss (miscarriage) is higher in women using drugs like this one than in women who have a natural pregnancy. Talk with the doctor.
  • If you have used drugs like this one more than 1 time to get pregnant, the chance of having tumors in your ovaries may be raised. Talk with your doctor.
  • This medicine may cause harm to the unborn baby if you take it while you are pregnant. If you are pregnant or you get pregnant while taking follitropin alfa, call your doctor right away.

Pregnancy level

X


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