Biomaterial Database

Influence of acetaminophen-induced hepatic necrosis on the pharmacokinetics of levonorgestrel. 1983

A A Gommaa, and F H Osman

The pharmacokinetics of levonorgestrel in control mice and in mice with induced hepatic necrosis were investigated. Hepatic necrosis was induced by fasting mice for 18 hr and then giving the acetaminophen in a dose of 750 mg/kg i.p. Measurement by radioimmunoassay of plasma levonorgestrel has been used to compare the pharmacokinetic parameters of the drug after oral and intravenous administration in both control and liver-affected animals. The pharmacokinetic parameters of levonorgestrel in control mice showed some similarity to those observed in human subjects, save the systemic bioavailability which was about 67% in mice compared to 100% in humans. The animals with induced hepatic necrosis compared with controls showed: 1 - Similar mean plasma levels; 2 - Increased metabolic clearance; 3 - Shortened elimination half-life; and 4 - No change in volume of distribution, half-life of distribution and systemic bioavailability. The reasons for any change have been discussed and interpreted.

UI	MeSH Term	Description	Entries
D007700	Kinetics	The rate dynamics in chemical or physical systems.
D009644	Norgestrel	A synthetic progestational agent with actions similar to those of PROGESTERONE. This racemic or (+-)-form has about half the potency of the levo form (LEVONORGESTREL). Norgestrel is used as a contraceptive, ovulation inhibitor, and for the control of menstrual disorders and endometriosis.	18,19-Dinorpregn-4-en-20-yn-3-one, 13-ethyl-17-hydroxy-, (17alpha)-(+-)-,DL-Norgestrel,Neogest,Ovrette,Postinor,Wy-3707,DL Norgestrel,Wy 3707,Wy3707
D011863	Radioimmunoassay	Classic quantitative assay for detection of antigen-antibody reactions using a radioactively labeled substance (radioligand) either directly or indirectly to measure the binding of the unlabeled substance to a specific antibody or other receptor system. Non-immunogenic substances (e.g., haptens) can be measured if coupled to larger carrier proteins (e.g., bovine gamma-globulin or human serum albumin) capable of inducing antibody formation.	Radioimmunoassays
D003277	Contraceptives, Oral, Combined	Fixed drug combinations administered orally for contraceptive purposes.	Combined Oral Contraceptive,Contraceptive Agents, Female, Combined,Oral Contraceptives, Combined,Combined Oral Contraceptives,Contraceptive, Combined Oral,Contraceptives, Combined Oral,Oral Contraceptive, Combined
D005260	Female		Females
D000082	Acetaminophen	Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.	Acetamidophenol,Hydroxyacetanilide,Paracetamol,APAP,Acamol,Acephen,Acetaco,Acetominophen,Algotropyl,Anacin-3,Datril,N-(4-Hydroxyphenyl)acetanilide,N-Acetyl-p-aminophenol,Panadol,Tylenol,p-Acetamidophenol,p-Hydroxyacetanilide,Anacin 3,Anacin3
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D001682	Biological Availability	The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action.	Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities
D013237	Stereoisomerism	The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)	Molecular Stereochemistry,Stereoisomers,Stereochemistry, Molecular,Stereoisomer
D016912	Levonorgestrel	A synthetic progestational hormone with actions similar to those of PROGESTERONE and about twice as potent as its racemic or (+-)-isomer (NORGESTREL). It is used for contraception, control of menstrual disorders, and treatment of endometriosis.	18,19-dinorpregn-4-en-20-yn-3-one, 13-ethyl-17-hydroxy-, (17alpha)-(-)-,l-Norgestrel,Capronor,Cerazet,D-Norgestrel,Microlut,Microval,Mirena,NorLevo,Norgeston,Norplant,Norplant-2,Plan B,Vikela,duofem,D Norgestrel,Norplant 2,Norplant2,l Norgestrel