Loestrin 1/20 Tablets 21s

Manufacturer TEVA/WOMENS HEALTH Active Ingredient Ethinyl Estradiol and Norethindrone Tablets(ETH in il es tra DYE ole & nor eth IN drone) Pronunciation LO-es-trin (Ethinyl Estradiol: ETH-in-il es-tra-DYE-ole; Norethindrone: nor-ETH-in-drone)
WARNING: Smoking cigarettes while using this drug raises the chance of severe heart and blood-related side effects. This chance is raised with age (mainly older than 35 years of age). It is also raised with the number of cigarettes smoked. It is strongly advised not to smoke. Do not use this drug if you smoke and are older than 35 years of age. @ COMMON USES: It is used to prevent pregnancy.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Contraceptive
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Pharmacologic Class
Estrogen and Progestin Combination
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Pregnancy Category
Category X
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FDA Approved
Jun 1976
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Loestrin 1/20 is a birth control pill that contains two female hormones, estrogen (ethinyl estradiol) and progestin (norethindrone). It works by preventing ovulation (the release of an egg from the ovary) and by making it harder for sperm to reach the egg and for a fertilized egg to implant in the womb. It is used to prevent pregnancy.
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How to Use This Medicine

Taking Your Medication Correctly

To use this medication effectively, follow your doctor's instructions and read all the information provided. Take your medication at the same time every day, with or without food. If you experience stomach upset, take it with food to help alleviate discomfort.

If you are also taking colesevelam, be sure to take it at least 4 hours before or after taking this medication. After starting this medication, you may need to use a non-hormone form of birth control, such as condoms, to prevent pregnancy for a certain period. Follow your doctor's guidance on using non-hormone birth control.

It is essential to take your medication as directed, even if you do not have sex frequently. Do not skip doses, as this can reduce the medication's effectiveness in preventing pregnancy. If you vomit or have diarrhea, the medication may not work as well. If this occurs within 3 to 4 hours after taking an active tablet, take another tablet as soon as possible. If vomiting or diarrhea persists for more than a day, use an additional form of birth control and consult your doctor. If you are unsure what to do, call your doctor for guidance.

If you miss two periods in a row, take a pregnancy test before starting a new cycle of medication.

Storing and Disposing of Your Medication

Store your medication at room temperature, protected from light, and in a dry place. Avoid storing it in a bathroom.

What to Do If You Miss a Dose

If you miss a dose, refer to the package insert or consult your doctor for instructions. If you are using this medication to prevent pregnancy, you may need to use a non-hormone form of birth control, such as condoms, for a certain period to prevent pregnancy.
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Lifestyle & Tips

  • Do not smoke, especially if you are over 35 years old, as smoking significantly increases the risk of serious side effects like blood clots, heart attack, and stroke.
  • Report any unusual or severe symptoms immediately to your doctor (e.g., severe leg pain, chest pain, sudden severe headache, vision changes).
  • Maintain regular check-ups, including blood pressure monitoring.
  • This medication does not protect against HIV/AIDS or other sexually transmitted infections (STIs). Use condoms to prevent STIs.
  • If you experience persistent nausea, vomiting, or diarrhea, the effectiveness of the pill may be reduced; use a backup contraceptive method.

Dosing & Administration

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Adult Dosing

Standard Dose: One tablet orally once daily for 21 consecutive days, followed by 7 days of inactive tablets. Begin new pack on the 8th day.

Condition-Specific Dosing:

first_start: Take the first active tablet on the first day of menstrual bleeding (Day 1 Start) or on the first Sunday after the period begins (Sunday Start). Use a non-hormonal backup method for the first 7 days if using Sunday Start.
missed_dose: Refer to package insert for specific instructions based on number of missed pills and week in cycle. Generally, take missed pill as soon as remembered, even if it means taking two pills in one day. Use backup contraception if multiple pills are missed.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Dosing is the same as for adults once menstruation has begun and contraception is desired.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment needed.
Moderate: No specific adjustment needed.
Severe: Use with caution; monitor for fluid retention. No specific dose adjustment guidelines.
Dialysis: Not available; use with caution.

Hepatic Impairment:

Mild: Use with caution; monitor for adverse effects.
Moderate: Contraindicated.
Severe: Contraindicated.

Pharmacology

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Mechanism of Action

Combined oral contraceptives (COCs) primarily act by suppressing gonadotropins. Although the primary mechanism is inhibition of ovulation, other alterations include changes in the cervical mucus (which increases the difficulty of sperm penetration) and changes in the endometrium (which reduce the likelihood of implantation). Ethinyl estradiol provides the estrogenic component, and norethindrone provides the progestational component.
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Pharmacokinetics

Absorption:

Bioavailability: Ethinyl Estradiol: ~40-45%; Norethindrone: ~60-100%
Tmax: Ethinyl Estradiol: ~1-2 hours; Norethindrone: ~1-2 hours
FoodEffect: Food may slightly decrease Cmax for ethinyl estradiol but does not significantly affect bioavailability. No significant clinical impact.

Distribution:

Vd: Ethinyl Estradiol: ~4-15 L/kg; Norethindrone: ~2-4 L/kg
ProteinBinding: Ethinyl Estradiol: ~98% (primarily to albumin); Norethindrone: ~61% (primarily to albumin and sex hormone-binding globulin [SHBG])
CnssPenetration: Limited

Elimination:

HalfLife: Ethinyl Estradiol: ~6-20 hours (terminal); Norethindrone: ~5-14 hours (terminal)
Clearance: Not available
ExcretionRoute: Ethinyl Estradiol: Renal and fecal (as glucuronide and sulfate conjugates); Norethindrone: Renal and fecal (as metabolites)
Unchanged: Ethinyl Estradiol: <5%; Norethindrone: <1%
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Pharmacodynamics

OnsetOfAction: Contraceptive efficacy typically begins after 7 consecutive days of active pill use. Full protection usually achieved after the first full cycle.
PeakEffect: Not applicable for contraceptive effect; refers to steady-state hormone levels.
DurationOfAction: Daily dosing maintains contraceptive effect.

Safety & Warnings

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BLACK BOX WARNING

Cigarette smoking increases the risk of serious cardiovascular side effects from oral contraceptive use. This risk increases with age and with heavy smoking (15 or more cigarettes per day) and is quite marked in women over 35 years of age. Women who use oral contraceptives should be strongly advised not to smoke.
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Side Effects

Serious Side Effects: Seek Medical Help Immediately

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention right away:

Signs of an allergic reaction, such as:
+ Rash or hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems, including:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Signs of high blood pressure, such as:
+ Severe headache or dizziness
+ Passing out
+ Changes in eyesight
Signs of gallbladder problems, including:
+ Pain in the upper right belly area, right shoulder area, or between the shoulder blades
+ Yellow skin or eyes
+ Fever with chills
+ Bloating
+ Severe upset stomach or vomiting
Weakness on one side of the body
Trouble speaking or thinking
Changes in balance
Drooping on one side of the face
Blurred eyesight
Depression or other mood changes
Breast changes, such as:
+ Lump in the breast
+ Breast pain or soreness
+ Nipple discharge
Vaginal itching or discharge
Eyesight changes or loss
Bulging eyes
Changes in how contact lenses feel
Severe or persistent spotting or vaginal bleeding
Fluid retention, which may cause swelling, weight gain, or trouble breathing

If you experience any of these symptoms, contact your doctor immediately.

Other Possible Side Effects

Most people do not experience serious side effects, and many have only minor or no side effects at all. However, if you notice any of the following side effects, contact your doctor or seek medical attention if they bother you or do not go away:

Changes in appetite
Weight gain or loss
Dizziness or headache
Upset stomach or vomiting
Stomach cramps
Bloating
Enlarged or tender breasts
Dark patches of skin on the face (avoid sun exposure and use protective measures)
Changes in menstrual periods, including:
+ Heavy bleeding
+ Spotting
+ Bleeding between cycles

Reporting Side Effects

If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • A: Abdominal pain (severe)
  • C: Chest pain (severe), cough, shortness of breath
  • H: Headaches (severe, sudden, or worse than usual)
  • E: Eye problems (blurred vision, flashing lights, partial or complete loss of vision)
  • S: Severe leg pain (calf or thigh), swelling, warmth, redness
  • Jaundice (yellowing of skin or eyes)
  • Unexplained vaginal bleeding or spotting outside of withdrawal bleed
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following conditions to ensure safe treatment:

Any allergies you have, including allergies to this medication, its components, or other substances. Describe the allergic reaction and its symptoms.
A history of certain health conditions, including:
+ Blood clots or blood clotting disorders
+ Breast cancer or other hormone-sensitive cancers
+ Diseased blood vessels in the brain or heart
+ Heart valve problems or heart disease
+ Abnormal heart rhythms, such as atrial fibrillation
+ Angina (chest pain) or a history of heart attack
+ Stroke or high blood pressure
+ Liver tumors or other liver problems
+ Severe headaches or migraines
+ Diabetes
A history of endometrial cancer, cervical cancer, vaginal cancer, or unexplained vaginal bleeding.
Hereditary angioedema, a condition characterized by recurring episodes of severe swelling.
Dark skin patches (chloasma) or increased sensitivity to sunlight or radiation.
Recent use (within the past 2 weeks) of ombitasvir, paritaprevir, and ritonavir (with or without dasabuvir).
Current use of glecaprevir and pibrentasvir.
Pregnancy or suspected pregnancy. Do not take this medication if you are pregnant.
Breastfeeding or plans to breastfeed.
A history of jaundice (yellowing of the skin and eyes) during pregnancy or with estrogen use, such as hormonal birth control.

This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help you determine if it is safe to take this medication with your other treatments. Never start, stop, or change the dose of any medication without consulting your doctor.
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Precautions & Cautions

Important Warnings and Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Your doctor may advise you to stop taking this drug before certain surgical procedures. If you need to stop taking this medication, your doctor will instruct you on when to resume taking it after your surgery or procedure.

If you will be immobile for an extended period, such as during long trips, bedrest after surgery, or illness, discuss this with your doctor. Prolonged immobility may increase your risk of developing blood clots.

If you have diabetes (high blood sugar), consult your doctor, as this medication may affect your blood sugar levels. Monitor your blood sugar as directed by your doctor.

This medication may cause high blood pressure. Have your blood pressure checked regularly, as advised by your doctor.

High cholesterol and triglyceride levels have been associated with this medication. If you have high cholesterol or triglycerides, discuss this with your doctor. Regularly check your blood work and other lab tests as directed by your doctor.

It is crucial to have regular breast exams and gynecology check-ups. Additionally, perform breast self-exams as instructed by your doctor.

If you are allergic to tartrazine (FD&C Yellow No. 5), inform your doctor, as some products contain this ingredient. Also, if you consume grapefruit juice or eat grapefruit frequently, discuss this with your doctor.

This medication may interfere with certain lab tests. Inform all your healthcare providers and lab personnel that you are taking this medication.

Certain medications, herbal products, or health conditions may reduce the effectiveness of hormone-based birth control. Ensure your doctor is aware of all your medications and health issues. You may need to use a non-hormone form of birth control, such as condoms, in addition to this medication.

This medication does not protect against sexually transmitted diseases like HIV or hepatitis. Always use a latex or polyurethane condom during sexual activity. If you have questions, consult your doctor.

This medication may increase the risk of blood clots, stroke, or heart attack. Discuss this with your doctor.

The risk of blood clots is highest during the first year of using this medication and when restarting hormone-based birth control after a break of 4 weeks or more. Consult your doctor about this risk.

Some studies suggest that the risk of cervical cancer may be higher in individuals taking hormone-based birth control, although this may be due to other factors. If you have questions, discuss this with your doctor.

Long-term use of hormone-based birth control may be associated with an increased risk of breast cancer, although not all studies confirm this. If you have questions, consult your doctor.

If you are taking this medication for acne, you must be at least 15 years old. This medication should not be used in children who have not had their first menstrual period.

If you experience any signs of pregnancy or have a positive pregnancy test, contact your doctor immediately.
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Overdose Information

Overdose Symptoms:

  • Nausea
  • Vomiting
  • Withdrawal bleeding (in females)

What to Do:

There are no specific antidotes. Treatment is symptomatic and supportive. In case of suspected overdose, contact a poison control center or emergency medical services. Call 1-800-222-1222.

Drug Interactions

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Contraindicated Interactions

  • Ombitasvir/paritaprevir/ritonavir, with or without dasabuvir (risk of ALT elevations)
  • Glecaprevir/pibrentasvir (risk of ALT elevations)
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Major Interactions

  • Strong CYP3A4 inducers (e.g., Rifampin, Carbamazepine, Phenytoin, Phenobarbital, Topiramate, Oxcarbazepine, Griseofulvin, St. John's Wort) - may decrease contraceptive efficacy and increase breakthrough bleeding.
  • Aromatase inhibitors (e.g., Anastrozole, Letrozole) - may reduce efficacy of aromatase inhibitors.
  • Certain HIV protease inhibitors (e.g., Nelfinavir, Ritonavir) - may alter COC levels.
  • Certain non-nucleoside reverse transcriptase inhibitors (e.g., Efavirenz, Nevirapine) - may alter COC levels.
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Moderate Interactions

  • Lamotrigine - COCs may decrease lamotrigine plasma concentrations, potentially leading to loss of seizure control.
  • Thyroid hormone replacement therapy - COCs may increase thyroid binding globulin, leading to increased thyroid hormone requirements.
  • Cyclosporine - COCs may increase cyclosporine plasma concentrations.
  • Theophylline - COCs may increase theophylline plasma concentrations.
  • Corticosteroids (e.g., Prednisolone) - COCs may increase corticosteroid plasma concentrations.
  • Antibiotics (e.g., Ampicillin, Tetracycline) - theoretical risk of reduced efficacy due to altered enterohepatic circulation, though clinical evidence is limited. Backup method often recommended.
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Minor Interactions

  • Acetaminophen - may increase ethinyl estradiol levels.
  • Ascorbic acid (Vitamin C) - may increase ethinyl estradiol levels.

Monitoring

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Baseline Monitoring

Complete medical history (including family history)

Rationale: To identify contraindications, risk factors for cardiovascular disease, and other conditions that may be affected by COC use.

Timing: Prior to initiation

Physical examination (including blood pressure, breast exam, pelvic exam, Pap test)

Rationale: To establish baseline health status and rule out existing conditions.

Timing: Prior to initiation

Lipid profile (optional, consider for high-risk patients)

Rationale: To assess baseline cardiovascular risk.

Timing: Prior to initiation

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Routine Monitoring

Blood pressure

Frequency: Annually

Target: <140/90 mmHg

Action Threshold: Sustained elevation (e.g., >140/90 mmHg) may require discontinuation or change in contraceptive method.

Annual physical examination (including breast exam, pelvic exam, Pap test as per guidelines)

Frequency: Annually

Target: Normal findings

Action Threshold: Abnormal findings require further investigation.

Review of medication list and health changes

Frequency: Annually or at each visit

Target: N/A

Action Threshold: Identify potential drug interactions or new contraindications.

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Symptom Monitoring

  • Severe abdominal pain (A)
  • Severe chest pain, shortness of breath, or coughing up blood (C)
  • Severe headaches (H)
  • Eye problems (e.g., blurred vision, loss of vision) (E)
  • Severe leg pain (calf or thigh), swelling, warmth, or redness (S)
  • Jaundice (yellowing of skin or eyes)
  • Unexplained vaginal bleeding or spotting
  • Mood changes, depression

Special Patient Groups

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Pregnancy

Contraindicated in pregnancy. There is no indication for COC use in pregnancy, and there is no evidence of teratogenicity from inadvertent exposure to COCs during early pregnancy.

Trimester-Specific Risks:

First Trimester: Contraindicated. No increased risk of birth defects reported.
Second Trimester: Contraindicated.
Third Trimester: Contraindicated.
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Lactation

Not recommended during lactation. Estrogens can decrease the quantity and quality of breast milk. Small amounts of contraceptive steroids and/or their metabolites may be excreted in breast milk.

Infant Risk: Potential for adverse effects on the infant (e.g., jaundice, breast enlargement). Consider non-hormonal methods or progestin-only methods if breastfeeding.
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Pediatric Use

Safety and efficacy are established for post-menarcheal adolescents. Use in pre-menarcheal females is not indicated.

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Geriatric Use

Not indicated for use in postmenopausal women for contraception. Increased risk of cardiovascular events in older women.

Clinical Information

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Clinical Pearls

  • Always advise patients to read the patient information leaflet provided with the medication.
  • Emphasize the importance of taking the pill at the same time each day to maintain efficacy.
  • Counsel patients on backup contraceptive methods, especially during the first cycle, when starting after a break, or if pills are missed or if experiencing severe vomiting/diarrhea.
  • Be aware of potential drug interactions, especially with enzyme-inducing medications, which can reduce contraceptive effectiveness.
  • Educate patients on the 'ACHES' warning signs for serious adverse events (Abdominal pain, Chest pain, Headaches, Eye problems, Severe leg pain).
  • This formulation (1 mg norethindrone, 20 mcg ethinyl estradiol) is considered a low-dose COC, which may be associated with less estrogen-related side effects but potentially more breakthrough bleeding compared to higher-dose formulations.
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Alternative Therapies

  • Progestin-only pills (mini-pill)
  • Contraceptive patch (Xulane)
  • Vaginal ring (NuvaRing, Annovera)
  • Contraceptive injection (Depo-Provera)
  • Contraceptive implant (Nexplanon)
  • Intrauterine devices (IUDs - hormonal and non-hormonal)
  • Barrier methods (condoms, diaphragm, cervical cap)
  • Spermicides
  • Sterilization (tubal ligation, vasectomy)
  • Emergency contraception
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Cost & Coverage

Average Cost: $25 - $100 per 28 tablets (1 cycle)
Generic Available: Yes
Insurance Coverage: Tier 1 or 2 (often covered under ACA as preventive care)
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General Drug Facts

If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.