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Levonorgestrel
Levonorgestrel is a synthetic progestin used in various contraceptive formulations, including emergency contraception (Plan B) and intrauterine devices (IUDs). It should be used with caution in certain patient populations, particularly those with a history of thromboembolic disorders, as progestins, including levonorgestrel, may increase the risk of blood clot formation. Women with a history of deep vein thrombosis (DVT), pulmonary embolism (PE), or stroke should discuss alternative contraceptive options with their healthcare provider.
Levonorgestrel should be used cautiously in women with liver disorders, as hepatic impairment may affect its metabolism, leading to altered drug levels. Close monitoring is recommended for patients with hepatic dysfunction.
Levonorgestrel should be avoided during pregnancy. It is not effective for abortion and can potentially harm a developing fetus. It is classified as a pregnancy category X drug, meaning its use is contraindicated in pregnancy. While it is considered safe during breastfeeding, levonorgestrel may pass into breast milk in small amounts, and caution is advised when used by nursing mothers.
In addition, patients with a history of uterine fibroids or undiagnosed abnormal vaginal bleeding should be evaluated for other underlying conditions before initiating levonorgestrel-containing products.
Levonorgestrel is most commonly used for contraception, both for emergency contraception and long-term use. As an emergency contraceptive, it is effective when taken within 72 hours after unprotected sex or contraceptive failure, such as condom breakage. It works by inhibiting ovulation, preventing fertilization, or altering the endometrium to prevent implantation.
Levonorgestrel is also used in combination with other hormones as part of regular contraceptive pills, often in combination with estrogens. In addition, the levonorgestrel intrauterine system (IUS) is used for long-term contraception, providing a highly effective method of birth control for up to five years.
Other off-label uses include the treatment of menorrhagia (heavy menstrual bleeding) and in combination with estrogen for hormone replacement therapy in postmenopausal women. Levonorgestrel may also be used in certain cases of endometriosis to manage symptoms by suppressing the hormonal fluctuations that trigger the growth of endometrial tissue.
Levonorgestrel is contraindicated in women who are pregnant or who may be pregnant, as it does not terminate an existing pregnancy and may harm the fetus. It is classified as a category X drug for pregnancy, meaning it should not be used during pregnancy under any circumstances.
Levonorgestrel is also contraindicated in women with a known or suspected breast cancer or any other estrogen- or progestin-dependent neoplasms. Women with a history of breast cancer or uterine cancer should avoid levonorgestrel-containing products, as progestins may influence hormone-sensitive cancers.
It is contraindicated in individuals with undiagnosed vaginal bleeding or active liver disease, as it may exacerbate existing conditions. Additionally, women with a history of thrombosis, including DVT, PE, or stroke, should avoid using levonorgestrel-containing products due to the potential for increased risk of thromboembolic events.
Common side effects of levonorgestrel include nausea, vomiting, abdominal pain, dizziness, headache, fatigue, and breast tenderness. These side effects are generally mild and transient, often improving within a few days after use.
Less common but more serious side effects include changes in menstrual bleeding patterns, such as irregular bleeding or spotting, which is most frequently observed in the early months of using levonorgestrel as an emergency contraceptive or as part of an IUS. If bleeding persists or becomes severe, a healthcare provider should be consulted.
Psychiatric side effects such as mood changes, depression, and irritability can occur, particularly in long-term users. Some women may experience emotional side effects, such as depression or mood swings, which should be monitored.
In rare cases, more serious side effects may occur, such as allergic reactions (including rash, swelling, or difficulty breathing) and thromboembolic events (deep vein thrombosis or pulmonary embolism). Women who experience leg swelling, chest pain, or difficulty breathing should seek immediate medical attention.
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Levonorgestrel is a synthetic progestin that exerts its contraceptive effects primarily by inhibiting ovulation, preventing fertilization, and altering the endometrial lining to prevent implantation. Its primary action is the inhibition of ovulation by altering the secretion of gonadotropins (LH and FSH), which are required for ovulation.
Levonorgestrel also thickens the cervical mucus, making it more difficult for sperm to pass through the cervix and reach an egg. Additionally, it alters the endometrial lining, making it less receptive to a fertilized egg, which further contributes to its contraceptive action.
The mode of action of levonorgestrel as an emergency contraceptive is similar, but its effectiveness is most pronounced when taken as soon as possible after unprotected intercourse. It can inhibit or delay ovulation, preventing fertilization from occurring.
Pharmacokinetically, levonorgestrel is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 1–2 hours. It is metabolized in the liver, and its elimination half-life is approximately 30 hours.
Levonorgestrel may interact with several medications, potentially altering its efficacy or leading to increased side effects. Some key interactions include:
- Enzyme-Inducing Drugs: Drugs that induce cytochrome P450 enzymes, such as certain anticonvulsants (e.g., phenytoin, carbamazepine, topiramate) and some antibiotics (e.g., rifampin), may reduce the effectiveness of levonorgestrel. In these cases, alternative or additional contraceptive methods should be considered, as the metabolism of levonorgestrel may be increased, lowering its serum concentration.
- Antifungal Agents: Some antifungal agents, such as ketoconazole, may increase the blood levels of levonorgestrel by inhibiting the metabolism of the drug. This may increase the risk of side effects such as breakthrough bleeding or nausea.
- Other Hormonal Contraceptives: When levonorgestrel is used in combination with other hormonal contraceptives, such as oral contraceptive pills, it can enhance the overall contraceptive effect, but careful monitoring for side effects is necessary, particularly those related to hormonal imbalances like mood changes or irregular bleeding.
- Antibiotics: Although the concern about antibiotics reducing the efficacy of hormonal contraceptives is largely unfounded for most antibiotics, certain antibiotics (such as rifampin) may reduce the efficacy of levonorgestrel. It is advisable to use backup contraception if taking these antibiotics alongside levonorgestrel.
- Food and Alcohol: There are no significant food interactions with levonorgestrel, and it can be taken with or without food. Alcohol does not directly interact with levonorgestrel, but excessive alcohol consumption may impair judgment or adherence to contraceptive regimens, reducing overall efficacy.
For emergency contraception, the typical adult dose of levonorgestrel is a single 1.5 mg tablet taken as soon as possible after unprotected intercourse, ideally within 72 hours. The effectiveness of levonorgestrel decreases as time progresses, and it is most effective when taken within 12 hours after unprotected sex.
For the levonorgestrel IUS, the usual dosage is the insertion of a device containing 52 mg of levonorgestrel, which provides long-term contraception for up to five years. The device is typically inserted by a healthcare provider during a routine office visit.
For the combined oral contraceptive pill containing levonorgestrel, the dose varies depending on the formulation, with typical doses ranging from 0.1 mg to 0.3 mg per tablet, taken once daily.
Levonorgestrel is not typically recommended for children under the age of 16, except under the guidance of a healthcare provider. The use of levonorgestrel as emergency contraception is not approved for children under 12 years of age, and younger adolescents should seek guidance from a healthcare provider to ensure proper management of contraception.
For children and adolescents aged 16 or older, the same dose used for adults (1.5 mg as a single dose) is typically appropriate for emergency contraception. Levonorgestrel should only be used under the supervision of a healthcare professional in these cases.
Levonorgestrel does not require dose adjustments in patients with renal impairment, as it is primarily metabolized by the liver. However, patients with severe renal dysfunction should be monitored closely for any potential changes in drug clearance, particularly if levonorgestrel is used as part of a combination contraceptive regimen.
Not available in a medicine form yet