Gonadotropin preparations are drug

Drug

A drug, broadly speaking, is any substance that, when absorbed into the body of a living organism, alters normal bodily function. There is no single, precise definition, as there are different meanings in drug control law, government regulations, medicine, and colloquial usage.In pharmacology, a...

s that mimic the physiological effects of gonadotropin

Gonadotropin

Gonadotropins are protein hormones secreted by gonadotrope cells of the pituitary gland of vertebrates. This is a family of proteins, which include the mammalian hormones follitropin , lutropin , placental chorionic gonadotropins hCG and eCG and chorionic gonadotropin , as well as at least two...

s, used therapeutically mainly as fertility medication

Fertility medication

Fertility medication are drugs which enhance reproductive fertility. For women, fertility medication is used to stimulate follicle development of the ovary...

. For example, the so called menotropin

Menotropin

Menotropin is an active substance for the treatment of fertility disturbances. It consists of gonadotropins that are extracted from the urine of postmenopausal women, usually luteinizing hormone and follicle-stimulating hormone...

s consist of LH

Luteinizing hormone

Luteinizing hormone is a hormone produced by the anterior pituitary gland. In females, an acute rise of LH called the LH surge triggers ovulation and development of the corpus luteum. In males, where LH had also been called interstitial cell-stimulating hormone , it stimulates Leydig cell...

 and FSH

Follicle-stimulating hormone

Follicle-stimulating hormone is a hormone found in humans and other animals. It is synthesized and secreted by gonadotrophs of the anterior pituitary gland. FSH regulates the development, growth, pubertal maturation, and reproductive processes of the body. FSH and Luteinizing hormone act...

 extracted from human urine

Urine

Urine is a typically sterile liquid by-product of the body that is secreted by the kidneys through a process called urination and excreted through the urethra. Cellular metabolism generates numerous by-products, many rich in nitrogen, that require elimination from the bloodstream...

 from menopausal women. There are also recombinant variants.

FSH and LH Preparations

hMG (human Menopausal Gonadotrophins), FSH

FSH

FSH may refer to:* Follicle-stimulating hormone* Fox Sports Houston, a regional Fox Sports Net affiliate station for the Houston, Texas area* Facioscapulohumeral muscular dystrophy* International Civil Aviation Organisation code for Flash Airlines...

 and LH

LH

LH, Lh, or lh may stand for:*Laurel and Hardy*Leasehold *Left-handed or left hand*Letterhead, the heading at the top of a sheet of letter paper*lh, a digraph for many languages...

 prepared from human urine collected from postmenopausal women. First extracted in 1953. Injected intra-muscularily (IM) or subcutaneously (SC).

Generic

menotropin

Menotropin

Menotropin is an active substance for the treatment of fertility disturbances. It consists of gonadotropins that are extracted from the urine of postmenopausal women, usually luteinizing hormone and follicle-stimulating hormone...

s for injections, USP

Brands

• Menopur, 5 mL vials containing 75 IU FSH and 75 IU LH.
• Repronex, vials containing either 75 IU FSH and 75 IU LH, or 150 IU FSH and 150 IU LH.

FSH Preparations

There are two types of FSH preparations. Those derived from the urine of menopausal women and recombinant
preparations. The recombinant preparations are more pure and more easily administered, but they are more expensive. The urinary preparations are equally effective and less expensive, but are not as convenient to administer as they are available in vials versus injection pens. One study reported that users of the purified urinary FSH preparation Bravelle experienced less injection stite pain compared to the recombinant preparation Follistim.

Urinary Preparations

Purified urinary FSH (75 IU FSH and ≤ 2 IU of LH)

Generic

urofollitropin

Urofollitropin

Urofollitropin is a purified form of follicle-stimulating hormone that is manufactured by extraction from human urine and then purified to remove various proteins and other substances. FSH is important in the development of follicles produced by the ovaries...

for injection, purified.

Brands

• Bravelle, U.S., (≤ 2 IU LH)
• Metrodin, U.S. and Canada, (≤ 1 IU LH)
• Fertinorm Hp, (Canada)

Highly purified urinary FSH (75 IU FSH and ≤ 0.1 IU LH/1000 IU FSH)

Generic

urofollitropin for injection, (highly) purified.

Dosage

typically 75 - 300, but as high as 600 IU / day

Brands

Fertinex (≤ 0.1 IU LH/1000 IU FSH)

Recombinant Preparations

Follitropin alfa

Generic

Follitropin alfa injection

Brands

Gonal-F

Follitropin beta

Generic

follitropin beta injection

Brands

• Follistim
• Puregon

The package insert for Gonal-F states that based on physio-chemical tests and bioassays that follitropin beta and follitropin alfa are indistinguishable. Two studies showed no difference. However, a more recent study showed there is may be a slight clinical difference, with the alfa form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels.

The package insert for Puregon states that structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (hFSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural hFSH. However, these small differences do not affect the bioactivity compared to natural hFSH.

FSH Analogs

Corifollitropin alfa

Merck received approval on February 15, 2010 from the European Commission for ELONVA (corifollitropin alfa) a long lasting single injection fusion protein lacking LH activity. Only one injection is required for the first seven days, replacing the first seven daily injections of conventional FSH. Initial results demonstrates similar pregnancy rates as daily recombinant FSH injections.

LH (Luteinizing hormone) Preparations

Prepared from recombinant DNA.

Generic

lutropin alfa for injection

Brands

Luveris

hCG (human Chorionic Gonadotropin) Preparations

Used to induce final maturation of follicle and subsequent ovulation. Also used for luteal phase support. Typically a single injection of 10,000 international units is used to induce ovulation. Recent data has shown that subcutaneous injection works as well as intramuscular injection, however this form of administration is not FDA approved.

Urinary Preparations

Derived from the urine of pregnant women.

Generic

(human) chorionic gonadotropin for injection, USP

Brands

• Pregnyl (Merck/Schering-Plough)
• Follutein
• Profasi
• Novarel

Recombinant Preparations

Generic

choriogonadotropin alfa for injection (recombinant human Chorionic Gonadotropin, r-hCG).

Brands

Ovidrel