Contraceptives, Oral

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Contraceptives, Oral (Combination Products)

Pronouncation: (kon-tra-SEP-tiv, OR-al)
Class: Hormone, Contraceptive

Trade Names:
Alesse
- Tablets 20 mcg ethinyl estradiol/0.1 mg levonorgestrel

Trade Names:
Apri
- Tablets 30 mcg ethinyl estradiol/0.15 mg desogestrel

Trade Names:
Aviane
- Tablets 20 mcg ethinyl estradiol/0.1 mg levonorgestrel

Trade Names:
Brevicon
- Tablets 35 mcg ethinyl estradiol/0.5 mg norethindrone

Trade Names:
Cryselle
- Tablets 30 mcg ethinyl estradiol/0.3 mg norgestrel

Trade Names:
Cyclessa
- Tablets Phase 1: 0.1 mg desogestrel/25 mcg ethinyl estradiol. Phase 2: 0.125 mg desogestrel/25 mcg ethinyl estradiol. Phase 3: 0.15 mg desogestrel/25 mcg ethinyl estradiol.

Trade Names:
Demulen 1/35
- Tablets 35 mcg ethinyl estradiol/1 mg ethynodiol diacetate

Trade Names:
Demulen 1/50
- Tablets 50 mcg ethinyl estradiol/1 mg ethynodiol diacetate

Trade Names:
Desogen
- Tablets 30 mcg ethinyl estradiol/0.15 desogestrel

Trade Names:
Enpresse
- Tablets Phase 1: 0.05 mg levonorgestrel/30 mcg ethinyl estradiol. Phase 2: 0.075 mg levonorgestrel/40 mcg ethinyl estradiol. Phase 3: 0.125 mg levonorgestrel/30 mcg ethinyl estradiol.

Trade Names:
Estrostep 21
- Tablets Phase 1: 1 mg norethindrone acetate/20 mcg ethinyl estradiol. Phase 2: 1 mg norethindrone acetate/30 mcg ethinyl estradiol. Phase 3: 1 mg norethindrone acetate/35 mcg ethinyl estradiol.

Trade Names:
Estrostep Fe
- Tablets Phase 1: 1 mg norethindrone acetate/20 mcg ethinyl estradiol. Phase 2: 1 mg norethindrone acetate/30 mcg ethinyl estradiol. Phase 3: 1 mg norethindrone acetate/35 mcg ethinyl estradiol.

Trade Names:
Jenest-28
- Tablets Phase 1: 0.5 mg norethindrone/35 mcg ethinyl estradiol. Phase 2: 1 mg norethindrone/35 mcg ethinyl estradiol

Trade Names:
Kariva
- Tablets 20 mcg ethinyl estradiol (white tablets)/10 mcg ethinyl estradiol (lt. blue tablets)/0.15 mg desogestrel (white tablets only)

Trade Names:
Lessina
- Tablets 20 mcg ethinyl estradiol/0.1 mg levonorgestrel

Trade Names:
Levlen
- Tablets 30 mcg ethinyl estradiol/0.15 mg levonorgestrel

Trade Names:
Levlite
- Tablets 20 mcg ethinyl estradiol/0.1 mg levonorgestrel

Trade Names:
Levora 0.15/30
- Tablets 30 mcg ethinyl estradiol/0.15 mg levonorgestrel

Trade Names:
Loestrin 21 1/20
- Tablets 20 mcg ethinyl estradiol/1 mg norethindrone acetate

Trade Names:
Loestrin 21 1.5/30
- Tablets 30 mcg ethinyl estradiol/1.5 mg norethindrone acetate

Trade Names:
Loestrin Fe 1/20
- Tablets 20 mcg ethinyl estradiol/1 mg norethindrone acetate

Trade Names:
Loestrin Fe 1.5/30
- Tablets 30 mcg ethinyl estradiol/1.5 mg norethindrone acetate

Trade Names:
Lo/Ovral
- Tablets 30 mcg ethinyl estradiol/0.3 mg norgestrel

Trade Names:
Low-Ogestrel
- Tablets 30 mcg ethinyl estradiol/0.3 mg norgestrel

Trade Names:
Microgestin Fe 1/20
- Tablets 20 mcg ethinyl estradiol/1 mg norethindrone acetate

Trade Names:
Microgestin Fe 1.5/30
- Tablets 30 mcg ethinyl estradiol/1.5 mg norethindrone acetate

Trade Names:
Mircette
- Tablets Phase 1: 0.15 mg desogestrel/20 mcg ethinyl estradiol. Phase 2: 0.01 mg ethinyl estradiol.

Trade Names:
Modicon
- Tablets 35 mcg ethinyl estradiol/0.5 mg norethindrone

Trade Names:
Mononessa
- Tablets 35 mcg ethinyl estradiol/0.25 mg norgestimate

Trade Names:
Necon 0.5/35
- Tablets 35 mcg ethinyl estradiol/0.5 mg norethindrone

Trade Names:
Necon 1/35
- Tablets 35 mcg ethinyl estradiol/1 mg norethindrone

Trade Names:
Necon 1/50
- Tablets 50 mcg mestranol/1 mg norethindrone

Trade Names:
Necon 10/11
- Tablets Phase 1: 0.5 mg norethindrone/35 mcg ethinyl estradiol. Phase 2: 1 mg norethindrone/35 mcg ethinyl estradiol.

Trade Names:
Nordette
- Tablets 30 mcg ethinyl estradiol/0.15 mg levonorgestrel

Trade Names:
Norinyl 1 + 35
- Tablets 35 mcg ethinyl estradiol/1 mg norethindrone

Trade Names:
Norinyl 1 + 50
- Tablets 50 mcg mestranol/1 mg norethindrone

Trade Names:
Nortrel 0.5/35
- Tablets 35 mcg ethinyl estradiol/ 0.5mg norethindrone

Trade Names:
Nortrel 1/35
- Tablets 35 mcg ethinyl estradiol/ 1 mg norethindrone

Trade Names:
Ogestrel 0.5/50
- Tablets 50 mcg ethinyl estradiol/0.5 mg norgestrel

Trade Names:
Ortho-Cept
- Tablets 30 mcg ethinyl estradiol/0.15 mg desogestrel

Trade Names:
Ortho-Cyclen
- Tablets 35 mcg ethinyl estradiol/0.25 mg norgestimate

Trade Names:
Ortho-Novum 1/50
- Tablets 50 mcg mestranol/1 mg norethindrone

Trade Names:
Ortho-Novum 1/35
- Tablets 35 mcg ethinyl estradiol/1 mg norethindrone

Trade Names:
Ortho-Novum 7/7/7
- Tablets Phase 1: 0.5 mg norethindrone/35 mcg ethinyl estradiol. Phase 2: 0.75 mg norethindrone/35 mcg ethinyl estradiol. Phase 3: 1 mg norethindrone/35 mcg ethinyl estradiol.

Trade Names:
Ortho-Novum 10/11
- Tablets Phase 1: 0.5 mg norethindrone/35 mcg ethinyl estradiol. Phase 2: 1 mg norethindrone/35 mcg ethinyl estradiol.

Trade Names:
Ortho Tri-Cyclen
- Tablets Phase 1: 0.18 mg norgestimate/35 mcg ethinyl estradiol. Phase 2: 0.215 mg norgestimate/35 mcg ethinyl estradiol. Phase 3: 0.25 mg norgestimate/35 mcg ethinyl estradiol.

Trade Names:
Ortho Tri-Cyclen Lo
- Tablets Phase 1: 0.18 mg norgestimate/25 mcg ethinyl estradiol. Phase 2: 0.215 mg norgestimate/25 mcg ethinyl estradiol. Phase 3: 0.25 mg norgestimate/25 mcg ethinyl estradiol.

Trade Names:
Ovcon-35
- Tablets 35 mcg ethinyl estradiol/0.4 mg norethindrone

Trade Names:
Ovcon-50
- Tablets 50 mcg ethinyl estradiol/1 mg norethindrone

Trade Names:
Ovral-28
- Tablets 50 mcg ethinyl estradiol/0.5 mg norethindrone

Trade Names:
Portia
- Tablets 30 mcg ethinyl estradiol/0.15 mg levonorgestrel

Trade Names:
Seasonale
- Tablets 30 mcg ethinyl estradiol/0.15 mg levonorgestrel

Trade Names:
Sprintec
- Tablets 35 mcg ethinyl estradiol/0.25 mg norgestimate

Trade Names:
Tri-Levlen
- Tablets Phase 1: 0.05 mg levonorgestrel/30 mcg ethinyl estradiol. Phase 2: 0.075 mg levonorgestrel/40 mcg ethinyl estradiol. Phase 3: 0.125 mg levonorgestrel/30 mcg ethinyl estradiol.

Trade Names:
Tri-Norinyl
- Tablets Phase 1: 0.5 mg norethindrone/35 mcg ethinyl estradiol. Phase 2: 1 mg norethindrone/35 mcg ethinyl estradiol. Phase 3: 0.5 mg norethindrone/35 mcg ethinyl estradiol.

Trade Names:
Triphasil
- Tablets Phase 1: 0.05 mg levonorgestrel/30 mcg ethinyl estradiol. Phase 2: 0.075 mg levonorgestrel/40 mcg ethinyl estradiol. Phase 3: 0.125 mg levonorgestrel/30 mcg ethinyl estradiol.

Trade Names:
Trivora-28
- Tablets Phase 1: 0.05 mg levonorgestrel/30 mcg ethinyl estradiol. Phase 2: 0.075 mg levonorgestrel/40 mcg ethinyl estradiol. Phase 3: 0.125 mg levonorgestrel/30 mcg ethinyl estradiol.

Trade Names:
Yasmin
- Tablets 30 mcg ethinyl estradiol/3 mg drospirenone

Trade Names:
Yaz
- Tablets 0.02 mg ethinyl estradiol/3 mg drospirenone

Trade Names:
Zovia 1/35E
- Tablets 35 mcg ethinyl estradiol/1 mg ethynodiol diacetate

Trade Names:
Zovia 1/50E
- Tablets 50 mcg ethinyl estradiol/1 mg ethynodiol diacetate

Mechanism of Action

Pharmacology

Inhibits ovulation by suppressing gonadotropins, follicle-stimulating hormone and luteinizing hormone.

Indications and Usage

Prevention of pregnancy.

Unlabeled Uses

Postcoital contraceptive.

Contraindications

Thrombophlebitis; thromboembolic disorders; history of deep vein thrombophlebitis; cerebral vascular disease; MI; coronary artery disease; known or suspected breast carcinoma or estrogen-dependent neoplasia; past or present benign or malignant liver tumors that developed during use of estrogen-containing products; past or present angina pectoris; undiagnosed abnormal genital bleeding; known or suspected pregnancy; cholestatic jaundice of pregnancy or jaundice with prior pill use.

Dosage and Administration

Sunday-Start Packaging
Adults

PO 1 tablet daily beginning on first Sunday after menstruation begins. If menstruation begins on Sunday, take first tablet on that day.

21-day Regimen
Adults

PO 1 tablet daily for 21 days, beginning on day 5 of cycle. Take no tablets for 7 days; then start new course of 21-day regimen.

28-day Regimen
Adults

PO 1 tablet daily.

General Advice

May be given with or without food.

Drug Interactions

Barbiturates, carbamazepine, felbamate, modafinil, oxcarbazine, protease inhibitors, St. John"s wort, hydantoins, rifampin, griseofulvin, penicillin, tetracyclines

Decreased effectiveness of oral contraceptive. Use additional form of birth control during concomitant therapy.

Benzodiazepines, caffeine, corticosteroids, cyclosporine, metoprolol, selegiline, theophylline, tricyclic antidepressants

Effects may be increased by oral contraceptives, increasing the risk of toxicity.

Lamotrigine

Concentration may be decreased, reducing the therapeutic effect.

Laboratory Test Interactions

May cause increases in sulfobromophthalein retention; factors II, VII, VIII, IX, X; plasminogen, fibrinogen; norepinephrine-induced platelet aggregation; thyroid-binding globulin, leading to increased total thyroid hormone measurements; transcortin; corticosteroid levels; triglycerides and phospholipids; ceruloplasmin; aldosterone; amylase; gamma-glutamyl transpeptidase; iron-binding capacity; transferrin; prolactin; renin activity; vitamin A. May cause decreases in anti-thrombin III; free T 3 resin uptake; pregnanediol excretion; response to metyrapone test; folate; glucose tolerance; albumin; cholinesterase; haptoglobin; zinc; vitamin B 12 .

Adverse Reactions

Cardiovascular

Coronary thrombosis; MI; hypertension.

CNS

Cerebral thrombosis; cerebral hemorrhage; migraine; mental depression.

Dermatologic

Melasma; rash; photosensitivity.

EENT

Steepening of corneal curvature; contact lens intolerance.

GI

Nausea and vomiting; abdominal cramps; bloating; mesenteric thrombosis.

Genitourinary

Renal artery thrombosis; break-through bleeding; spotting; change in menstrual flow; dysmenorrhea; amenorrhea; temporary infertility after discontinuation; change in cervical erosion and cervical secretions; endocervical hyperplasia; increase in size of uterine leiomyomata; vaginal candidiasis.

Hematologic

Thrombophlebitis and thrombosis; arterial thromboembolism.

Hepatic

Cholestatic jaundice; gallbladder disease.

Respiratory

Pulmonary embolism.

Miscellaneous

Raynaud disease; congenital anomalies; liver tumors; hepatocellular carcinoma; breast tenderness, enlargement, secretion, diminished lactation; edema; weight change; reduced carbohydrate tolerance; prolactin-secreting pituitary tumors; increased prevalence of cervical chlamydia trachomatous.

Precautions

Warnings

Smoking

Cigarette smoking increases the risk of serious cardiovascular side effects. The risk increases with age (older than 35 yr) and heavy smoking (at least 15 cigarettes/day). Smoking is not recommended during therapy.


Monitor

Blood glucose

Monitor blood glucose levels in patients with diabetes.


Pregnancy

Category X .

Lactation

Excreted in breast milk. Defer use until infant weaned.

Tartrazine Sensitivity

Some products may contain tartrazine, which may cause allergic-type reaction in susceptible individuals.

Acute intermittent porphyria

May be precipitated by estrogen therapy in susceptible individuals.

Carbohydrate and lipid metabolism

Glucose tolerance may decrease; triglycerides and total phospholipids may increase. Progestins may elevate LDL levels.

Depression

Use drug with caution in patients with history of depression.

Fibroids

Oral contraceptives may cause an increase in size of preexisting uterine leiomyomata (fibroids).

Fluid retention

Use drug with caution in patients with hypertension; convulsive disorders; migraines; asthma; cardiac, hepatic, or renal dysfunction.

Liver dysfunction

May impair metabolism of oral contraceptives.

Pyridoxine deficiency

May occur due to disturbance in normal tryptophan metabolism.

Serum folate

May be depressed by oral contraceptive therapy.

Overdosage

Symptoms

Withdrawal bleeding.

Patient Information

  • Advise patient to use additional method of birth control until after first week of administration in initial cycle.
  • Advise patient what to do if dose is missed: (1) if missed 1, take when remember or take 2 the next day; (2) if missed 2, take 2 on 2 consecutive days; (3) if missed at least 3, stop pills; (4) use alternative form of birth control in all cases.
  • Advise patient to take multiple daily vitamin.
  • Encourage patient who smokes to stop. Cardiovascular dysfunction and thromboembolic disease have been associated with use of oral contraceptives in patients who smoke.
  • Advise patient that oral contraceptives may change the fit of rigid contact lenses.
  • Caution patient to avoid prolonged exposure to sunlight, and to use sunscreen or wear protective clothing to avoid photosensitivity reaction.
  • Advise patient to wait at least 3 mo after discontinuing oral contraceptives to try to become pregnant.
  • Caution patient that antibiotics may decrease effectiveness of oral contraceptives and to use a nonhormonal form of contraception while taking antibiotics and for 7 days after stopping antibiotics.
  • Instruct patient to report symptoms of blood clots (eg, pain, numbness, shortness of breath, visual disturbances).
  • Teach patient routine breast self-examination technique.
  • Warn patient that side effects such as nausea and breakthrough bleeding are common at first.




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