This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.
Identification
- Summary
Norethindrone enanthate is a synthetic progestogen indicated for contraceptive therapy.
- Generic Name
- Norethindrone enanthate
- DrugBank Accession Number
- DB14678
- Background
Not Available
- Type
- Small Molecule
- Groups
- Experimental
- Structure
- Weight
- Average: 410.598
Monoisotopic: 410.282095084 - Chemical Formula
- C27H38O3
- Synonyms
- Norethisterone enanthate
- Norethisterone oenanthate
- External IDs
- LG 202
- SH 393
- SH-8.0393
- ZK-5410
Pharmacology
- Indication
Not Available
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- Associated Therapies
- Contraindications & Blackbox Warnings
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- Pharmacodynamics
Not Available
- Mechanism of action
- Not Available
- Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Norethindrone enanthate can be increased when it is combined with Abametapir. Abciximab The risk or severity of adverse effects can be increased when Norethindrone enanthate is combined with Abciximab. Acenocoumarol The risk or severity of adverse effects can be increased when Norethindrone enanthate is combined with Acenocoumarol. Acetaminophen The metabolism of Norethindrone enanthate can be increased when combined with Acetaminophen. Acetazolamide The metabolism of Norethindrone enanthate can be increased when combined with Acetazolamide. Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Norethindrone enanthate. Alpelisib The metabolism of Norethindrone enanthate can be increased when combined with Alpelisib. Alteplase The risk or severity of adverse effects can be increased when Norethindrone enanthate is combined with Alteplase. Aminoglutethimide The metabolism of Norethindrone enanthate can be increased when combined with Aminoglutethimide. Amiodarone The metabolism of Norethindrone enanthate can be decreased when combined with Amiodarone. Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- Not Available
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Active Moieties
Name Kind UNII CAS InChI Key Norethisterone prodrug T18F433X4S 68-22-4 VIKNJXKGJWUCNN-XGXHKTLJSA-N - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image MESIGYNA KULLANIMA HAZIR ENJEKTOR 1X1 ML, 1 ADET Norethindrone enanthate (50 mg/ml) + Estradiol valerate (5 mg/ml) Injection, solution Intramuscular BAYER TÜRK KİMYA SAN. LTD. ŞTİ. 2020-08-14 Not applicable Turkey MESIGYNA® Norethindrone enanthate (50 mg) + Estradiol valerate (5 mg) Solution Intramuscular BAYER A.G. 2006-11-10 2021-04-01 Colombia
Categories
- Drug Categories
- Adrenal Cortex Hormones
- Contraceptive Agents, Female
- Contraceptive Agents, Hormonal
- Contraceptives, Oral
- Contraceptives, Oral, Synthetic
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Fused-Ring Compounds
- Hormonal Contraceptives for Systemic Use
- Norpregnanes
- Norpregnenes
- Norsteroids
- Progesterone Congeners
- Progestins
- Reproductive Control Agents
- Steroids
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- HY3S2K0J0F
- CAS number
- 3836-23-5
- InChI Key
- APTGJECXMIKIET-WOSSHHRXSA-N
- InChI
- InChI=1S/C27H38O3/c1-4-6-7-8-9-25(29)30-27(5-2)17-15-24-23-12-10-19-18-20(28)11-13-21(19)22(23)14-16-26(24,27)3/h2,18,21-24H,4,6-17H2,1,3H3/t21-,22+,23+,24-,26-,27-/m0/s1
- IUPAC Name
- (1R,3aS,3bR,9aR,9bS,11aS)-1-ethynyl-11a-methyl-7-oxo-1H,2H,3H,3aH,3bH,4H,5H,7H,8H,9H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-1-yl heptanoate
- SMILES
- [H][C@@]12CC[C@@](OC(=O)CCCCCC)(C#C)[C@@]1(C)CC[C@]1([H])[C@@]3([H])CCC(=O)C=C3CC[C@@]21[H]
References
- General References
- NPRA Product Information: NORISTERAT (norethindrone enanthate) intramuscular injection [Link]
- External Links
- KEGG Compound
- C14486
- ChemSpider
- 199613
- 31984
- ChEBI
- 34894
- ChEMBL
- CHEMBL3187229
- ZINC
- ZINC000004217172
- Wikipedia
- Norethisterone_enanthate
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Prevention Bacterial Vaginosis (BV) / Human Immunodeficiency Virus (HIV) Infections 1 Not Available Not Yet Recruiting Health Services Research Contraception Behavior / Contraceptive Usage 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Intramuscular Injection Intramuscular 200 mg/ml Injection, solution Intramuscular Solution Intramuscular; Parenteral Solution Intramuscular 50 mg Solution Intramuscular - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Not Available
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.00148 mg/mL ALOGPS logP 5.43 ALOGPS logP 6.14 ChemAxon logS -5.4 ALOGPS pKa (Strongest Acidic) 18.25 ChemAxon pKa (Strongest Basic) -4.7 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 2 ChemAxon Hydrogen Donor Count 0 ChemAxon Polar Surface Area 43.37 Å2 ChemAxon Rotatable Bond Count 7 ChemAxon Refractivity 119.61 m3·mol-1 ChemAxon Polarizability 49.66 Å3 ChemAxon Number of Rings 4 ChemAxon Bioavailability 1 ChemAxon Rule of Five No ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule Yes ChemAxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Enzymes
1. DetailsCytochrome P450 3A4
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Zhang N, Shon J, Kim MJ, Yu C, Zhang L, Huang SM, Lee L, Tran D, Li L: Role of CYP3A in Oral Contraceptives Clearance. Clin Transl Sci. 2018 May;11(3):251-260. doi: 10.1111/cts.12499. Epub 2017 Oct 6. [Article]
Drug created at September 05, 2018 17:00 / Updated at May 14, 2021 01:07