Levonorgestrel (Aftera) tablets are used for emergency contraception following unprotected intercourse or after suspected contraceptive failure. It should be used within 72 hours as it does not prevent pregnancy once implantation has occurred.
Levonorgestrel Uses:
-
Emergency contraception:
- Used to prevent pregnancy following unprotected intercourse or possible contraceptive failure
Levonorgestrel (Aftera) Dose in Adults:
Levonorgestrel (Aftera) Dose for Emergency Contraception:
-
Females: Oral:
-
May be used at any time during the menstrual cycle:
-
Two-dose regimen:
- 1 tab 0.75 mg should be taken as soon as possible within 72 hours of unprotected sexual intercourse; a 2nd tab 0.75 mg, 12 hours after the first dose should be taken.
-
Single-dose regimen:
- 1 tab 1.5 mg should be taken as soon as possible within 72 hours of unprotected sexual intercourse.
-
-
Note:
- In case of emergency contraception treatment should begin as soon as possible; however, if used within 5 days treatment is still moderately effective & should be made available to women up to 5 days after unprotected or inadequately protected intercourse.
- The 2nd dose is equally effective if taken 12 to 24 hours after the first when the two-dose emergency contraceptive regimen is used.
Levonorgestrel (Aftera) Dose in Childrens:
Levonorgestrel (Aftera) Dose as an emergency contraceptive pill in adolescents:
-
Females:
- Refer to adult dosing. Not to be used prior to menarche.
Levonorgestrel Pregnancy Risk Category: X
- Women who are already pregnant should not use this product.
- No adverse effects on the mother or foetus were observed after accidental exposure during pregnancy.
- Levonorgestrel can still be used as an emergency contraceptive agent in women who have contraindications to hormonal contraceptives (eg, heart disease, migraines, liver disease)
- A rapid return to fertility can be expected after emergency contraception is used.
- Routine contraceptive measures must be taken to prevent pregnancy.
- One can immediately start using any regular contraceptive method after taking levonorgestrel; however, for a period of seven days, a barrier method (or abstinence form sexual intercourse) may be required.
Levonorgestrel use during breastfeeding:
- Breast milk contains levonorgestrel.
- The relative infant dose (RID), of levonorgestrel, is calculated by using the highest breastmilk concentration and comparing it to a single maternal dose of 1.5m.
- When the RID of your medication is less than 10%, breastfeeding is considered acceptable.
- Calculating the RID of levonorgestrel using a milk content of 10.7ng/mL yielded an estimated daily infant dose via breastmilk of 1,605ng/kg/day.
- This was achieved by giving a maternal dose of 1.5 mg of levonorgestrel 1.5mg to 12 women, who were nearly 11 weeks postpartum.
- Peak breast milk concentrations were observed between 2 and 4 hours following the dose. Then, over the next 12 hours, a rapid drop was observed.
- Levonorgestrel's breast milk half-life was 26 hours.
- Although breast milk concentrations were similar to maternal serum concentrations, they were consistently lower.
- Actual milk concentration was determined by the administration route and dosage.
- SHBG capacity also determined maternal plasma levels of levonorgestrel.
- SHBG can be enhanced by concurrent administration with estrogen and mother's postpartum status.
- Levonorgestrel can also be detected in breastmilk infants after oral administration.
- There have not been any adverse effects on the development or growth of infants. Some reports have reported isolated instances of decreased milk production.
- Levonorgestrel can be used by breastfeeding women as an emergency contraceptive.
Dose in Kidney Disease:
No dosage adjustments are provided in the manufacturer’s labeling (Use has not been studied).
Dose in Liver disease:
No dosage adjustments are provided in the manufacturer’s labeling (Use has not been studied).
Common Side Effects of Levonorgestrel (Aftera):
-
Central nervous system:
- Fatigue
-
Endocrine & metabolic:
- Hypermenorrhea
-
Gastrointestinal:
- Nausea
- Abdominal pain
Less Common Side Effects of Levonorgestrel (Aftera):
-
Central nervous system:
- Dizziness
- Headache
-
Endocrine & metabolic:
- Suppressed menstruation
-
Genitourinary:
- Breast tenderness
Contraindications to Levonorgestrel (Aftera):
- OTC labeling
- If you are pregnant, or for regular birth control, self-medication is not recommended.
Canadian labeling:
- It is not known if there are any contraindications to long-term progestin-only contraceptives if they are used in conjunction with levonorgestrel emergency contraception regimens.
- Pregnancy known or suspected
- Hypersensitivity to levonorgestrel and any other component of the formulation
- PV bleed(undiagnosed)
Warnings and precautions
-
Bleeding irregularities:
- After use, you may notice spotting
- Consider the possibility of pregnancy if menstruation is not completed within 7 days.
-
Ectopic pregnancy
- An ectopic pregnancy history is not a contraindication for emergency contraceptives.
- Patients with lower abdominal pain should be aware of the possibility for ectopic pregnancy.
- Especially if it is associated with missed periods or PV bleeding in women who have had amenorrhea.
Levonorgestrel (systemic): Drug Interaction
|
Antidiabetic Agents |
Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents. |
|
C1 inhibitors |
Progestins may enhance the thrombogenic effect of C1 inhibitors. |
|
CYP3A4 Inducers (Moderate) |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Deferasirox |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Elexacaftor |
Hormonal Contraceptives may enhance the adverse/toxic effect of Elexacaftor. Specifically, the risk for rash may be increased. |
|
Erdafitinib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Flibanserin |
Progestins (Contraceptive) may increase the serum concentration of Flibanserin. |
|
Herbs (Progestogenic Properties) (eg, Bloodroot, Yucca) |
May enhance the adverse/toxic effect of Progestins. |
|
LamoTRIgine |
May decrease the serum concentration of Progestins (Contraceptive). |
|
Metreleptin |
May decrease the serum concentration of Progestins (Contraceptive). Metreleptin may increase the serum concentration of Progestins (Contraceptive). |
|
Sarilumab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Selegiline |
Progestins (Contraceptive) may increase the serum concentration of Selegiline. |
|
Siltuximab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Thalidomide |
Progestins (Contraceptive) may enhance the thrombogenic effect of Thalidomide. |
|
Tocilizumab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Triazolam |
Hormonal Contraceptives may increase the serum concentration of Triazolam. |
|
Voriconazole |
May increase the serum concentration of Progestins (Contraceptive). Progestins (Contraceptive) may increase the serum concentration of Voriconazole. |
|
Risk Factor D (Consider therapy modification) |
|
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Acitretin |
May diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible. Management: Given the potential for progestin-only preparations to fail to prevent pregnancy during acitretin therapy, such products should not be relied upon. Alternative, nonhormonal forms of contraception must be employed during acitretin therapy. |
|
Anticoagulants |
Progestins may diminish the therapeutic effect of Anticoagulants. More specifically, the potential prothrombotic effects of some progestins and progestin-estrogen combinations may counteract anticoagulant effects. Management: Carefully weigh the prospective benefits of progestins against the potential increased risk of procoagulant effects and thromboembolism. Use is considered contraindicated under some circumstances. Refer to related guidelines for specific recommendations. |
|
Aprepitant |
May decrease the serum concentration of Progestins (Contraceptive). Management: Alternative or additional methods of contraception should be used both during treatment with aprepitant or fosaprepitant and for at least one month following the last aprepitant/fosaprepitant dose. |
|
Artemether |
May decrease the serum concentration of Progestins (Contraceptive). Management: Consider the use of an alternative (i.e., non-hormonal) means of contraception in all women of childbearing potential who are using artemether. |
|
Atazanavir |
May increase the serum concentration of Progestins (Contraceptive). However, atazanavir may lead to decreased ethinyl estradiol concentrations and decreased effectiveness of oral contraceptive products. Management: Consider an alternative or additional method of contraception, particularly with combined estrogen/progestin products. Depot medroxyprogesterone acetate may be used without a need for additional contraception. |
|
Barbiturates |
May diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible. Management: Use of alternative, nonhormonal contraceptives is recommended. |
|
Bexarotene (Systemic) |
May decrease the serum concentration of Progestins (Contraceptive). Management: Women of childbearing potential receiving bexarotene should use two reliable forms of contraception (including at least one nonhormonal form). |
|
Bile Acid Sequestrants |
May decrease the serum concentration of Progestins (Contraceptive). Management: Administer oral progestin-containing contraceptives at least 1 to 4 hours prior to or 4 to 6 hours after administration of a bile acid sequestrant. |
|
Bosentan |
May decrease the serum concentration of Progestins (Contraceptive). Management: Use an alternative (i.e., non-hormonal) means of contraception for all women of childbearing potential who are using bosentan, and do not rely on hormonal contraceptives alone. |
|
Brigatinib |
May decrease the serum concentration of Progestins (Contraceptive). Management: Females of childbearing potential should use an alternative, non-hormonal contraceptive during brigatinib therapy and for at least 4 months after the final brigatinib dose. |
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CarBAMazepine |
May diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible. Management: Use of alternative, nonhormonal contraceptives is recommended. |
|
Carfilzomib |
May enhance the thrombogenic effect of Progestins (Contraceptive). Management: Consider alternative, non-hormonal methods of contraception in patients requiring therapy with carfilzomib. |
|
Cenobamate |
May decrease the serum concentration of Hormonal Contraceptives. Management: Women should use additional or alternative non-hormonal birth control while taking cenobamate. |
|
Cladribine |
May diminish the therapeutic effect of Hormonal Contraceptives. Management: Women using systemically acting hormonal contraceptives should add a barrier method during cladribine dosing and for at least 4 weeks after the last dose in each treatment course. |
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CloBAZam |
May decrease the serum concentration of Progestins (Contraceptive). |
|
Cobicistat |
May increase the serum concentration of Progestins (Contraceptive). Management: Consider an alternative, nonhormone-based contraceptive in patients receiving cobicistatcontaining products. Drospirenone is specifically contraindicated with atazanavir and cobicistat. |
|
CYP3A4 Inducers (Strong) |
May increase the metabolism of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. |
|
Dabrafenib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). |
|
Dabrafenib |
May decrease the serum concentration of Progestins (Contraceptive). Management: Females of reproductive potential should use an alternative, highly effective, non-hormonal means of contraception during and at least 2 weeks (dabrafenib alone) or 4 months (dabrafenib + trametinib) after discontinuation of dabrafenib treatment. |
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Darunavir |
May decrease the serum concentration of Progestins (Contraceptive). Management: Consider using an alternative or additional means of contraception. Injected depot medroxyprogesterone acetate may be used without a need for additional contraception. |
|
Efavirenz |
May decrease the serum concentration of Progestins (Contraceptive). Management: Use an alternative or additional method of contraception due to possibly decreased contraceptive effectiveness. Injected depot medroxyprogesterone acetate does not appear to participate in this interaction. |
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Enzalutamide |
|
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Eslicarbazepine |
May decrease the serum concentration of Progestins (Contraceptive). Management: Alternative, non-hormonal means of birth control should be considered for women of child-bearing potential. |
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Exenatide |
May decrease the serum concentration of Progestins (Oral Contraceptive). Management: Administer oral contraceptives at least one hour prior to exenatide. |
|
Felbamate |
May decrease the serum concentration of Progestins (Contraceptive). Management: Contraceptive failure is possible. Use of an alternative, nonhormonal method of contraception is recommended. |
|
Fosamprenavir |
Progestins (Contraceptive) may decrease serum concentrations of the active metabolite(s) of Fosamprenavir. Fosamprenavir may decrease the serum concentration of Progestins (Contraceptive). Management: Consider using an alternative or additional means of contraception. Injected depot medroxyprogesterone acetate may be used without a need for additional contraception. |
|
Fosaprepitant |
May decrease the serum concentration of Progestins (Contraceptive). The active metabolite aprepitant is likely responsible for this effect. Management: Alternative or additional methods of contraception should be used both during treatment with aprepitant or fosaprepitant and for at least one month following the last aprepitant/fosaprepitant dose. |
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Fosphenytoin |
May diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible. Management: Contraceptive failure is possible. Use of an alternative, nonhormonal contraceptive is recommended. |
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Ivosidenib |
May decrease the serum concentration of Progestins (Contraceptive). Management: Consider alternative methods of contraception (ie, non-hormonal) in patients receiving ivosidenib. |
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Lesinurad |
May decrease the serum concentration of Progestins (Contraceptive). Management: Use of an additional, nonhormonal contraceptive is recommended in patients being treated with lesinurad who desire effective contraception. |
|
Lixisenatide |
May decrease the serum concentration of Progestins (Contraceptive). Management: Administer oral contraceptives 1 hour before or at least 11 hours after administration of lixisenatide. |
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Lopinavir |
May decrease the serum concentration of Progestins (Contraceptive). Lopinavir may increase the serum concentration of Progestins (Contraceptive). Management: Consider using an alternative or additional means of contraception. Injected depot medroxyprogesterone acetate and etonogestrel implants may be used without a need for additional contraception. |
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Lorlatinib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Avoid concurrent use of lorlatinib with any CYP3A4 substrates for which a minimal decrease in serum concentrations of the CYP3A4 substrate could lead to therapeutic failure and serious clinical consequences. |
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Lumacaftor |
May decrease the serum concentration of Progestins (Contraceptive). Management: Do not rely on hormone-based contraceptives with concurrent use of lumacaftor/ivacaftor; an alternative, non-hormonal, method of contraception should be used if this combination is required. |
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MiFEPRIStone |
May diminish the therapeutic effect of Progestins (Contraceptive). MiFEPRIStone may increase the serum concentration of Progestins (Contraceptive). Management: Women of childbearing potential should use an effective, nonhormonal means of contraception during and 4 weeks following mifepristone treatment. |
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Mitotane |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. |
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Mycophenolate |
May decrease the serum concentration of Progestins (Contraceptive). Management: Use of an additional or alternative (nonhormonal) method of contraception should be considered. |
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Nelfinavir |
May decrease the serum concentration of Progestins (Contraceptive). Management: Use an alternative or additional method of contraception due to possibly decreased contraceptive effectiveness. Injected depot medroxyprogesterone acetate does not appear to participate in this interaction. |
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Oxcarbazepine |
May decrease the serum concentration of Progestins (Contraceptive). Management: Contraceptive failure is possible. Use of an additional or alternative, nonhormonal method of contraception is recommended. |
|
Perampanel |
May decrease the serum concentration of Progestins (Contraceptive). Management: Patients should use an alternative, nonhormonal-based form of contraception both during the concurrent use of perampanel and for 1 month after discontinuing perampanel. |
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Phenytoin |
May diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible. Management: Contraceptive failure is possible. Use of an alternative, nonhormonal contraceptive is recommended. |
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Pitolisant |
May decrease the serum concentration of Hormonal Contraceptives. Management: Patients using hormonal contraception should be advised to use an alternative non-hormonal contraceptive method during treatment with pitolisant and for at least 21 days after discontinuation of pitolisant treatment. |
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Pomalidomide |
Progestins may enhance the thrombogenic effect of Pomalidomide. Management: Canadian pomalidomide labeling recommends caution with use of hormone replacement therapy and states that hormonal contraceptives are not recommended. US pomalidomide labeling does not contain these specific recommendations. |
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Primidone |
May diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible. Management: Use of alternative, nonhormonal contraceptives is recommended. |
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Retinoic Acid Derivatives |
May diminish the therapeutic effect of Progestins (Contraceptive). Retinoic Acid Derivatives may decrease the serum concentration of Progestins (Contraceptive). Management: Two forms of effective contraception should be used in patients receiving retinoic acid derivatives. Microdosed progesterone-only preparations (ie, minipills that do not contain estrogen) are considered an inadequate method of contraception. Exceptions: Adapalene; Alitretinoin (Topical); Bexarotene (Topical); Tretinoin (Topical). |
|
Rifamycin Derivatives |
May decrease the serum concentration of Progestins (Contraceptive). Contraceptive failure is possible. Management: Contraceptive failure is possible. Use of an alternative, nonhormonal contraceptive is recommended. |
|
Saquinavir |
May decrease the serum concentration of Progestins (Contraceptive). Management: Use an alternative or additional method of contraception due to possibly decreased contraceptive effectiveness. Injected depot medroxyprogesterone acetate does not appear to participate in this interaction. |
|
St John's Wort |
May diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible. Management: Consider using a product other than St John's wort. Contraceptive failure is possible. Use of an alternative, nonhormonal contraceptive is recommended. |
|
Sugammadex |
May decrease the serum concentration of Progestins (Contraceptive). Management: Patients receiving any hormonal contraceptive (oral or non-oral) should use an additional, nonhormonal contraceptive method during and for 7 days following sugammadex treatment. |
|
Tetrahydrocannabinol and Cannabidiol |
May decrease the serum concentration of Hormonal Contraceptives. Management: Women using hormonal contraceptives should consider adding a barrier contraceptive due to the potential for tetrahydrocannabinol and cannabidiol to decrease concentrations and effectiveness of hormonal contraceptives. |
|
Tipranavir |
May increase the serum concentration of Progestins (Contraceptive). Management: Use an alternative or additional method of contraception due to possibly decreased contraceptive effectiveness. Injected depot medroxyprogesterone acetate does not appear to participate in this interaction. |
|
Topiramate |
May decrease the serum concentration of Progestins (Contraceptive). Management: Caution patients that this combination may be associated with reduced contraceptive effectiveness. Consider adding an additional (non-hormonal) contraceptive method. |
|
Vitamin K Antagonists (eg, warfarin) |
Progestins (Contraceptive) may diminish the anticoagulant effect of Vitamin K Antagonists. In contrast, enhanced anticoagulant effects have also been noted with some products. Management: When possible, concomitant hormonal contraceptives and coumarin derivatives should be avoided in order to eliminate the risk of thromboembolic disorders. Consider using an alternative, nonhormonal contraceptive. |
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Risk Factor X (Avoid combination) |
|
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Encorafenib |
May decrease the serum concentration of Progestins (Contraceptive). |
|
Griseofulvin |
May diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible. |
|
Ixazomib |
May decrease the serum concentration of Progestins (Contraceptive). More specifically, use of ixazomib with dexamethasone may decrease the serum concentrations of contraceptive progestins. Management: Patients of childbearing potential should use a nonhormonal barrier contraceptive during and 90 days following ixazomib treatment. |
|
Tranexamic Acid |
Progestins (Contraceptive) may enhance the thrombogenic effect of Tranexamic Acid. |
|
Ulipristal |
Progestins may diminish the therapeutic effect of Ulipristal. Ulipristal may diminish the therapeutic effect of Progestins. Management: Ulipristal for uterine fibroids (Canadian indication): avoid progestins within 12 days of stopping ulipristal; as emergency contraceptive (U.S. indication): avoid progestins within 5 days of stopping ulipristal. |
Monitoring parameters:
If the normal (expected) menstrual period is delayed for more than one week following emergency contraception, or if lower abdominal pain or persistent irregular bleeding develops, evaluation should be done for pregnancy, spontaneous abortion, or ectopic pregnancy.
How to administer Levonorgestrel (Aftera)?
P/O: If vomiting occurs within 2 hours, consider repeating the dose.
Mechanism of action of Levonorgestrel (Aftera):
- There are many ways to prevent pregnancy:
- Sperm survival and passage through the uterus is affected by thickening of cervical mucus.
- The negative feedback mechanism on hypothalamus reduces FSH and LH secretion and inhibits ovulation.
- Modifying the endometrium can affect implantation.
- Once the implantation process is complete, Levonorgestrel will no longer be effective.
- There are many ways to prevent pregnancy:
- Sperm survival and passage through the uterus is affected by thickening of cervical mucus.
- The negative feedback mechanism on hypothalamus reduces FSH and LH secretion and inhibits ovulation.
- Modifying the endometrium can affect implantation.
- Once the implantation process is complete, Levonorgestrel will no longer be effective.
Absorption:
- Rapid and complete with oral administration.
Protein binding:
- Highly albumin binding (~50%) and SHBG (~47%)
Metabolism:
- Forms inactive metabolites in the liver via CYP3A4.
Half-life elimination:
- Almost 27 hours with oral administration.
Time to peak:
- Almost 2 hours with oral administration.
Excretion:
- 45% in Urine & 32% in feces.
International Brand Names of Levonorgestrel:
- Aftera
- EContra EZ
- EContra One-Step
- Fallback Solo
- My Choice
- My Way
- New Day
- Next Choice One Dose
- Opcicon One-Step
- Plan B One-Step
- React
- Take Action
- Afterel
- Afternor
- Chrono 72
- Dopo
- ECEE
- Egianti
- Emcon
- Emergency
- Emerres
- Escapel
- Escapelle
- Estinor
- Galnique
- Glanique
- Hyan
- Indoplant
- Jadelle
- Jadelle Implant
- Lebella
- Levidon
- Levonelle
- Levonelle-2
- Madonna
- Me
- Microlut
- MIcrolut
- Microval
- Mindchange
- Norlevo
- Nulsora
- Oh God
- Ovulol
- PiDaNa
- Pill 72
- Poslov
- Postinor
- Postinor-1
- Postinor-2
- Postpill
- Pozato
- Pregnon
- Prevenelle
- Puill 72
- Ramonna
- Revoke
- Secufem
- Sino Implant II
- Upostelle
- Valenor
- Vikela
Levonorgestrel Brand Names in Pakistan:
Levonorgestrel Tablets 52 mg in Pakistan |
|
| Mirena Ius | Bayer Health Care |
Levonorgestrel Tablets 1.5 mg in Pakistan |
|
| Emkit-Ds | Zafa Pharmaceutical Laboratories (Pvt) Ltd. |
Levonorgestrel Tablets 0.75 mg in Pakistan |
|
| Ecp | Social Marketing Pakistan (Guarantee) Ltd. |
| Emergency Pills | Hansel Pharmacueutical Pvt (Ltd) |
| Emkit | Zafa Pharmaceutical Laboratories (Pvt) Ltd. |
| Medkit | Mediate Pharmaceuticals (Pvt) Ltd |
| Postinor | Medimpex Scientific Office |
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