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|Appearance:||White Crystalline Powder||Quality Standard:||USP|
CAS 797-63-7 Healthy Estrogens Oral Anabolic Steroids Levonorgestrel powder For Hormonal drugs
1. Oral contraception:
At low doses, levonorgestrel is used in monophasic and triphasic formulations of combined oral contraceptive pills, Levonorgestrel is used for promoting the synthesis of protein and reduce the decomposition of amino acid, and for improving muscle hyperplasia, action and enhance male sexual characteristics.
2. Emergency contraception:
Levonorgestrel is used in emergency contraceptive pills (ECPs), both in a combined Yuzpe regimen which includes estrogen, and as a levonorgestrel-only method. The levonorgestrel-only method uses levonorgestrel 1.5 mg (as a single dose or as two 0.75 mg doses 12 hours apart) taken within 3 days of unprotected sex, with one study indicating that beginning as late as 120 hours (5 days) after intercourse could be effective.
3. Intrauterine system:
Levonorgestrel is the active ingredient in the Mirena & Skyla (Jaydess) intrauterine system.The levonorgestrel-only method uses levonorgestrel 1.5mg (as a single dose or as two 0.75mg doses 12 hours apart) taken within 3 days of unprotected sex, with one study indicating that beginning as late as 120 hours (5 days) after intercourse could be effective.
4. Contraceptive implants
Levonorgestrel is the active ingredient in Norplant and Jadelle.
5. Hormone replacement therapy
Levenorgestrel is combined with 17-beta estradiol in the Climara Pro hormonal patch.
At low doses, levonorgestrel is used in monophasicand triphasicformulations of combined oral contraceptive pills, with available monophasic doses ranging from 100-250μg, and triphasic doses of 50μg/75μg/125μg.
At very low daily dose of 30μg, levonorgestrel is used in some progestogen only pillformulations.
Levonorgestrel is used in emergency contraceptive pills(ECPs), both in a combined Yuzpe regimenwhich includes estrogen, and as a levonorgestrel-only method. The levonorgestrel-only method uses levonorgestrel 1.5mg (as a single dose or as two 0.75mg doses 12 hours apart) taken within 3 days of unprotected sex, with one study indicating that beginning as late as 120 hours (5 days) after intercourse could be effective.
The primary mechanism of action of levonorgestrel as a progestogen-only emergency contraceptive pill is, according to FIGO, to prevent fertilization by inhibition of ovulation. The International Federation of Gynecology and Obstetrics(FIGO) has issued a statement that: "review of the evidence suggests that LNG [levonorgestreol] ECPs cannot prevent implantation of a fertilized egg. Language on implantation should not be included in LNG ECP product labeling." In June 2012, a New York Timeseditorial called on the Food and Drug Administration(FDA) to remove from the label the unsupported suggestion that levonorgestrel emergency contraceptive pills inhibit implantation. In November 2013, the European Medicines Agency(EMA) approved a change to the label for HRA Pharma's NorLevo saying it cannot prevent implantation of a fertilized egg. In November 2013, the EMA also approved a change to the label for HRA Pharma's NorLevo saying: "In clinical trials, contraceptive efficacy was reduced in women weighing 75 kg [165 pounds] or more, and levonorgestrel was not effective in women who weighed more than 80 kg [176 pounds]." In November 2013 and January 2014, the FDA and the EMA said they were reviewing whether increased weight and body mass index(BMI) reduce the efficacy of emergency contraceptives.
|Description||: White Or Almost White Crystalline Powder|
|Identification||: A-IR Absorption||Positive|
|: B-Specific rotation & melting range||Positive|
|distinguishing it from Norgestrel.|
|Melting Point||: 232~239°C||236.0~238.8°C|
|Loss On Drying||: 0.5%max||0.04%|
|Specific Rotation||: -30°~ -35°||-32.8°|
|Ethynyl Group||: 7.81~8.18%||7.96%|
|Residue On Ignition||: 0.3%max||0.03%|
|Residual Solvents||: meets the requirements||Confirms
Levonorgestrel Side Effects
After intake of levonorgestrel 1.5 mg in clinical trials, very common effects (reported by 10% or more) included: dizziness, headache, nausea, abdominal pain, uterine pain, delay of menses, heavy menses, uterine bleeding, or fatigue; common effects (reported by 1% to 10%) included diarrhea, vomiting, or painful menses; these effects usually disappeared within 48 hours.
Usage And Synthesis:
Oral contraceptives, levonorgestrel, also known as D- norethindrone, left Kanok ketone, is currently the most widely used oral contraceptives, the racemic optically active part of norethindrone, the activity ratio norethindrone strong double dose can be reduced by half, adverse reactions are also reduced accordingly. Rapid oral absorption, 0.5 ~ 1h, reached the peak. t1 / 2 of 10 ~ 24h.Protein binding rate of 93% to 95%, bioavailability, mainly located in the liver, kidney, ovarian and uterine body's organs and tissues, and its metabolites, mainly in the form of glucuronide and sulfate salts from the urine and feces in vitro. And ethinyl estradiol combination as a short-acting oral contraceptives. Its dual photo and three photo adverse reactions less, closer to women's normal hormone secretion type. Women can be used for emergency contraception, namely failure (condom slippage or breakage, coitus out of control, rhythm miscalculation, etc.) in the same room of post-coital contraception measures unprotected intercourse or other contraceptive methods.
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