Abortifacient Agents, Nonsteroidal Dinoprost tromethamine CAS NO.38562-01-5

Dinoprost tromethamine(Prostaglandin F2alpha)

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Process

Prostaglandin F_2α (PGF_2α in prostanoid nomenclature), pharmaceutically termed dinoprost (INN),

is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient.

In domestic mammals, it is produced by the uterus when stimulated by oxytocin, in the event that there

has been no implantation during the follicular phase. It acts on the corpus luteum to cause luteolysis,

forming a corpus albicans and stopping the production of progesterone. Action of PGF_2α is dependent

on the number of receptors on the corpus luteum membrane.The PGF_2α isoform 8-iso-PGF_2α was found

in significantly increased amounts in patients with endometriosis, thus being a potential causative link

in endometriosis-associated oxidative stress

Mechanism of action

Further information: Prostaglandin F2alpha receptor

PGF2alphaacts by binding to the prostaglandin F2alpha receptor.

Synthesis In 2012 a concise and highly stereoselective total synthesis of PGF2alpha was described.The synthesis requires only seven steps, a huge improvement on the original 17-steps synthesis of Corey and Cheng,and uses 2,5-dimethoxytetrahydrofuran as a starting reagent, with S-proline as an asymmetric catalyst.

Analogs The following medications are analogs of prostaglandin F2alpha:

Latanoprost

Bimatoprost

Travoprost

Carboprost

Dinoprost tromethamine(Prostaglandin F2alpha)

• Abortifacient Agents, Nonsteroidal
• Oxytocics
• Diagnostic aid (angiography)
• Uterine stimulants

Dosage Forms

• Liquid
• Powder
• Solution
• Tablet

Brands / Synonyms

Dinolytic; Dinoprost tromethamine [USAN:JAN]; Dinoprost, trometamol salt; Ensaprost; Lutalyse; Panacelan F tromethamine salt; PGF2-alpha THAM; PGF2alpha THAM; Pronalgon F; Prostaglandin F2-alpha THAM; Prostaglandin F2a tromethamine; Prostaglandin F2alpha tham; Prostalmon F; Prostin F2 Alpha; Tham; Zinoprost

Indications

Used for aborting second-trimester pregnancy (between the twelfth to eighteenth week of gestation) and in incomplete abortion or for therapeutic abortion in cases of intrauterine fetal death and congenital abnormalities incompatible with life. Also used at low-doses for medically indicated induction of labor at term. Also injected intra-arterially for use as a vasodilator to assist in angiography.

Pharmacology

Dinoprost tromethamine is the tromethamine (THAM) salt of the naturally occurring prostaglandin F2alpha. Prostaglandin F2alpha has several pharmacologic effects on the female reproductive system, including stimulation of myometrial activity, relaxation of the cervix, inhibition of steroidogenesis by corpora lutea, and can potentially lyse corpora lutea.

Mechanism of Action

Dinoprost tromethamine appears to act directly on the myometrium, but this has not been completely established. Dinoprost stimulates myometrial contractions in the gravid uterus that are similar to the contractions that occur in the term uterus during labor. These contractions are usually sufficient to cause abortion. Uterine response to prostaglandins increases gradually throughout pregnancy. Dinoprost also facilitates cervical dilatation and softening.

Absorption

Slowly absorbed from the amniotic fluid into systemic circulation.

Toxicity

Although overdose by intra-amniotic administration of dinoprost has not been reported, exaggeration of the nausea, vomiting, and diarrhea that occur with normal doses would be expected.

Biotrnasformation / Drug Metabolism

Enzymatic dehydrogenation primarily in the maternal lungs and also in the liver.

Contraindications

Allergy or intolerance to dinoprost or other oxytocics, asthma - or history of (increased risk of bronchoconstriction), cephalopelvic disproportion, pelvic inflammatory disease, pulmonary disease - active, and ruptured membranes — intra-amniotic or extra-amniotic route (increased risk of intravascular absorption of dinoprost) .

Drug Interactions

Oxytocin or other oxytocics (concurrent use with dinoprost may result in uterine hypertonus, possibly causing uterine rupture or cervical laceration, especially in the absence of adequate cervical dilatation; although combinations are sometimes used for therapeutic advantage, when used concurrently, patient should be closely monitored.

Packaging 

The packaging can be customized, normally, 1kgs/Tin, or 5kgs/Tin or per drums

Company Introduction

Top Pharm Chemical Group is specialized in the New Drug Researching and Developing, and mainly manufacture Chemical Intermediates,  Pharmaceutical APIs and Pilot Production. To meet customers regulatory needs, we can offer products from gram to kilo and tons scale, and we can also support our customers with the DMF and other documents to Complete the registration.  

Our Targets:

"Best Technic; Better Quality; Better Price; Better Service"

Main Products:

Anidulafungin,Micafungin,Caspofungin,Posaconazole etc. (Anti-Infective)

Ixabepilone, Argatroban, Decitabine, Everolimus etc. (Anti-Tumor)

Epothilone B, Tacrolimus, Rapamycin,Temsirolimus etc. (Fermentation)

Bimatoprost, Latanoprost, Travoprost, Cloprostenol etc.(Prostaglandins)