Contraceptives, Hormonal Monophasic Oral Contraceptives

Ethinyl estradiol/desogestrel

Brand Names: Apri 28, Desogen, Ortho-Cept, Reclipsen, Solia

Ethinyl estradiol/drospirenone

Brand Names: Yasmin, Yaz

Ethinyl estradiol/ethynodiol

Brand Names: Kelnor 1/35, Zovia 1/35, Zovia 1/50

Ethinyl estradiol/levonorgestrel

Brand Names: Alesse-28, Aviane-28, Lessina-28, Levlen-28, Levlite-28, Levora-28, Lutera, Nordette-28, Portia-28, Sronyx

Ethinyl estradiol/norethindrone

Brand Names: Balziva, Brevicon, Femcon Fe, Junel 21 1/20, Junel 21 1.5/20, Junel Fe 1/20, Junel Fe 1.5/30, Loestrin 21 1/20, Loestrin 21 1.5/30, Loestrin Fe 1/20, Loestrin Fe 1.5/30, Microgestin Fe 1/20, Modicon, Necon 0.5/35, Necon 1/35, Norethin 1/35E, Norinyl 1 + 35, Nortrel 0.5/35, Nortrel 1/35, Ortho-Novum 1/35, Ovcon 35, Ovcon 50, Zenchant

Ethinyl estradiol/norgestimate

Brand Names: MonoNessa, Ortho-Cyclen, Previfem, Sprintec

Ethinyl estradiol/norgestrel

Brand Names: Cryselle, Lo/Ovral 28, Low-Ogestrel 28, Ogestrel 28

Mestranol/norethindrone

Brand Names: Necon 1/50, Norethin 1/50M, Norinyl 1+50, Ortho-Novum 1/50

Biphasic Oral Contraceptives

Ethinyl estradiol/desogestrel

Brand Names: Kariva, Mircette

Ethinyl estradiol/norethindrone

Brand Names: Necon 10/11, Ortho-Novum 10/11

Triphasic Oral Contraceptives

Ethinyl estradiol/desogestrel

Brand Names: Cesia, Cyclessa, Velivet

Ethinyl estradiol/levonorgestrel

Brand Names: Enpresse, Tri-Levlen, Triphasil 28, Trivora 28

Ethinyl estradiol/norethindrone

Brand Names: Aranelle, Leena, Necon 7/7/7, Nortrel 7/7/7, Ortho-Novum 7/7/7, Tri-Norinyl

Ethinyl estradiol/norgestimate

Brand Names: OrthoTri-Cyclen, OrthoTri-Cyclen Lo, Tri-Nessa, Tri-Previfem, Tri-Sprintec

Extended-Cycle Oral Contraceptive

Ethinyl estradiol/levonorgestrel

Brand Names: Lybrel, Seasonale, Seasonique

Progestin-Only Oral Contraceptives

Norethindrone

Brand Names: Errin, Camila, Jolivette, Micronor, Nor-QD

Progressive Estrogen Oral Contraceptives

Norethindrone/ethinyl acetate

Brand Names: Estrostep, Estrostep Fe

Contraceptive Implant

Etonorgestrel

Brand Names: Implanon

Emergency Contraceptive

Levonorgestrel

Brand Names: Plan B

Injectable Contraceptive

Medroxyprogesterone

Brand Names: Depo-Provera, Depo-subQ Provera 104

Intrauterine Contraceptive

Levonorgestrel

Brand Names: Mirena

Vaginal Ring Contraceptive

Ethinyl estradiol/etonogestrel

Brand Names: NuvaRing

Transdermal Contraceptive

Ethinyl estradiol/norelgestromin

Brand Names: OrthoEvra

Classification of Contraceptives

(The therapeutic classification, which categorizes drugs by the disease state they are used to treat, appears first, followed by the pharmacologic classification, which is based on the drug’s mechanism of action.)

Therapeutic class: contraceptive hormones

Pregnancy Category (pregnancy categories (A, B, C, D, and X) provide a basis for determining a drug’s potential for fetal harm): X

Indications of Contraceptives

(Medications are approved by the FDA for specific disease states. This section identifies the diseases or conditions for which the drug is commonly used and includes significant unlabeled uses as well.)

Prevention of pregnancy. Regulation of menstrual cycle. Emergency contraception (some products). Treatment of premenstrual dysphoric disorder (Yaz, Yasmin). Management of acne in women >14yr who desire contraception, have no health problems, and have failed topical treatment.

Action of Contraceptives

(This section contains a concise description of how the Drug produces the desired therapeutic effect.)

Monophasic Oral Contraceptives: Provide a fixed dosage of estrogen/progestin over a 21 -day cycle. Ovulation is inhibited by suppression of follicle-stimulating hormone (FSH) and luteinizing hormone (LH). May alter cervical mucus and the endometrial environment, preventing penetration by sperm and implantation of the egg.

Biphasic Oral Contraceptives: Ovulation is inhibited by suppression of FSH and LH. May alter cervical mucus and the endometrial environment, preventing penetration by sperm and implantation of the egg. In addition, smaller dose of progestin in phase 1 allows for proliferation of endometrium. Larger amount in phase 2 allows for adequate secretory development.

Triphasic Oral Contraceptives: Ovuktion is inhibited by suppression of FSH and LH. May alter cervical mucus and the endometrial environment, preventing penetration by sperm and implantation of the egg. Varying doses of estrogen/progestin may more closely mimic natural hormonal fluctuations.

Extended-cycle Oral Contraceptives: Provides continuous estrogen/progestin for 84 days (365 days for Lybrel), then off for 7 days, resulting in 4 menstrual periods/year (no periods/year for Lybrel). Progressive Estrogen Oral Contraceptives: Contains constant amount of progestin with 3 progressive doses of estrogen.

Progestin-Only Contraceptives/Contraceptive Implant/Intrauterine Levonorgestrel/Medroxyprogesterone Injection: Mechanism not clearly known. May alter cervical mucus and the endometrial environment, preventing penetration by sperm and implantation of the egg. Ovulation may also be suppressed.

Emergency Contraceptive Pills (ECPs): Inhibit ovulation/fertilization; may also alter tubal transport of sperm/egg and prevent implantation.

Vaginal Ring, Transdermal Patch: Inhibits ovulation, decreases sperm entry into uterus, and decreases likelihood of implantation. Anti-acne effect Combination of estrogen/progestin may increase sex hormone binding globulin (SHBG) resulting in decreased unbound testosterone, which may be a cause of acne.

Therapeutic Effects of Drug: Prevention of pregnancy. Decreased severity of acne. Decrease in premenstrual disphoric disorder.

Pharmacokinetics

(Pharmacokinetics refers to the way the body processes a medication by absorption, distribution, metabolism, and excretion. Also includes information on the drug’s half-life.)

Absorption: Ethinyl estradiol — rapidly absorbed; norethindrone — 65% absorbed; Desogesrtrel and levonorgestrel — 100% absorbed. Others are well absorbed after oral administration. Slowly absorbed from implant, subcutaneous, or intramuscular injection. Some absorption follows intrauterine implantation.

Distribution: Unknown.

Protein Binding: Ethinyl estradiol — 97-98%. Drospirenone — 97%

Metabolism and Excretion: Ethinyl estradiol andn orethindrone — undergo extensive first-pass hepatic metabolism. Mestranol — is rapidly converted to ethinyl estradol. Desogestrel — is rapidly metabolized to 3-keto-desogestgrel, the active metabolite. Most agents are metabolized by the liver.

Half-life: Ethinyl estradiol — 6-20 hours; Levonorgestrel — 45 hours; Norethindrone — 5-14 hours; Desogestrel (metabolite) — 38 ± 20 hours; Dros-pirenone — 30 hours; Norgestimate (metabolite) — 12-20 hours; others — unknown.

Time/Action Profile (the table provides the onset of Drug action, its peak effect, and its duration of activity) (prevention of pregnancy)

Route Onset Peak Duration
PO 1 month 1 month 1 month *
Implant 1 month 1 month 5 year
Intrauterine system 1 month 1 month 3 year
IM 1 month 1 month 3 month
SC Unk 1 wk 3 month

* Only during month of taking contraceptive

Contraindications/Precautions

(Situations in which Drug use should be avoided or alternatives strongly considered are listed as contraindications. In general, most drugs are contraindicated in pregnancy or lactation. The precautions portion includes disease states or clinical situations in which drug use involves particular risks or in which dosage modification may be necessary.)

Contraindicated in: Pregnancy; History of thromboembolic disease (e.g., deep vein thrombosis, PE, myocardial infarction (MI), stroke); Valvular heart disease; Major surgery with extended periods of immobility; Diabetes with vascular involvement; Headache with focal neurological symptoms; Uncontrolled hypertension; History of breast, endometrial, or estrogen-dependent cancer; Abnormal genital bleeding; Liver disease; Hypersensitivity to parabens (injectable only); Intrauterine levonorgestrel only — Intrauterine anomaly, postpartum endometriosis, multiple sexual partners, pelvic inflammatory disease, liver disease, genital actinomycosis, immunosuppression, intravenous (IV) drug abuse, untreated genitourinary infection, history of ectopic pregnancy; Some products contain tartrazine and should be avoided in patients with known hypersensitivity intolerance; Lactation: Avoid use.

Use Cautiously in: History of cigarette smoking or age > 30-3 5 year (increased risk of cardiovascular or thromboembolic phenomenon); Presence of other cardiovascular risk factors (obesity, hyperglycemia, elevated lipids, hypertension) ; History of diabetes mellitus, bleeding disorders, concurrent anticoagulant therapy or headaches; Pediatric: Should not be used before menarche.

Adverse Reactions/Side Effects of Contraceptives

(Although it is not possible to include all reported reactions, major side effects for all drugs are included.)

Central Nervous System (CNS): depression, migraine headache. Eye, Ear, Nose, and Throat: contact lens intolerance, optic neuritis, retinal thrombosis. Cardiovascular: cerebral hemorrhage, cerebral thrombosis, coronary thrombosis, pulmonary embolism, edema, hypertension, Raynaud’s phenomenon, thromboembolic phenomena, thrombophlebitis. Gastrointestinal (GI): abdominal cramps, bloating, cholestatic jaundice, gallbladder disease, liver tumors, nausea, vomiting. Genitourinary: amenorrhea, breakthrough bleeding, dysmenorrhea, spotting. Intrauterine levonorgestrel only — uterine imbedment/uterine rupture. Dermatologic: melasma, rash. Endocrine: hyperglycemia. Musculoskeletal: Injectable medroxyprogesterone only — bone loss. Misc: weight change.

Interactions

(Drug interactions are a significant risk for patients. As the number of medications a patient receives increases, so does the likelihood of drug-drug interactions. This section provides the most important drug-drug interactions and their physiological effects.)

Drug-Drugs: Oral contraceptive efficacy may be reduced by penicillins, chloramphenicol, barbiturates, chronic alcohol use, carbamazepine oxcarbazepine, felbamate, systemic corticosteroids, phenytoin, topiramate, primidone, modafinil, rifampin, rifabutin, some protease inhibitor antiretrovirals (including ritonavir), or tetracyclines. Drug may increase effects/risk of toxicity of some benzodiazepines, betablockers, corticosteroids, cyclosporine, andtheophylline. Drug increases risk of hepatic toxicity with dantrolene (estrogen only). Indinavir, itraconazole, ketoconazole, fluconazole, andatorvastatinmay increase effects/risk of toxicity. Smoking increase risk of thromboembolic phenomena (estrogen only). Drug may reduce levels of acetaminophen, temazepam, lamotrigine, lorazepam, oxazepam, or morphine. Drosperinone — containing products only — concurrent use with nonsteroidal anti-inflammatory drug (NSAIDs), potassium-sparing diuretics, potasssium supplements, ACE (angiotensin-converting enzyme) inhibitors, or angiotensin II receptor antagonists may result in hyperka-lemia.

Drug-Natural Products: Concomitant use with St. John’s wort Drug may reduce contraceptive efficacy and cause breakthrough bleeding and irregular menses.

Dosage / Route of Contraceptives

(Routes of administration are grouped together and include recommended doses for adults, children, and other. Dosage units are expressed in the terms in which they are usually prescribed. Dosing intervals also are provided in the manner in which they are frequently ordered.)

Monophasic Oral Contraceptives

PO (by mouth, orally) (Adults): On 21-day regimen, take first tablet on first Sunday after menses begins (take on Sunday if menses begins on Sunday) for 21 days, then skip 7 days and begin again. Regimen may also be started on first day of menses, continue for 21 days, then skip 7 days and begin again. Some regimens contain 7 placebo tablets, so that 1 tablet is taken every day for 28 days.

Biphasic Oral Contraceptives

PO (Adults): Given in 2 phases. First phase is 10 days of smaller amount of progestin. Second phase is larger amount of progestin. Amount of estrogen remains constant for same length of time (total of 21 days), then skip 7 days and begin again. Some regimens contain 7 placebo tablets for 28-day regimen.

Triphasic Oral Contraceptives

PO (Adults): Progestin amount varies throughout 21-day cycle. Estrogen component stays the same or may vary. Some regimens contain 7 placebo tablets for 28-day regimen.

Extended-cycle Contraceptive

PO (Adults): Seasonale and Seasonique Start taking first active pill on first Sunday after menses start (if first day is Sunday, start then), continue for 84 days of active pill, followed by 7 days of placebo tablets, then resume 84/7 cycle again. For Lybrel, begin taking the first pill during the first day of the menstrual cycle and start the next pack the day after the previous pack ends.

Progestin-Only Oral Contraceptives

PO (Adults): Start on first day of menses. Taken daily and continuously.

Progressive Estrogen Oral Contraceptives

PO (Adults): Estrogen amount increases every 7 days throughout 21 -day cycle. Progestin component stays the same. Some regimens contain 7 placebo tablets for 28-day regimen.

Emergency Contraceptive

PO (Adults and Adolescents): Given within 72 hours of unprotected intercourse and repeated 12 hours later. Plan B — 1 tablet followed by 1 more tablet 12 hours later; Ovral — 2 white tablets followed by 2 more white tablets 12 hours later; Lo/Ovral — 4 white tablets followed by 4 more white tablets 12 hours later; Levlen, Nordette — 4 light orange tablets followed by 4 more light orange tablets 12 hours later; Triphasil, Tri-Levlen — 4 yellow tablets followed by 4 more yellow tablets 12 hours later.

Injectable Contraceptive

Medroxyprogesterone (Depo-Provera)

Intramuscular (Adults): 150 mg within first 5 days of menses or within 5 days postpartum, if not breastfeeding. If breastfeeding, give 6 week postpartum; repeat every 3 month.

Medroxyprogesterone (Depo-Sub Q Provera 104)

Subcut (Adults): 104 mg within first 5 days of menses or within 5 days postpartum, if not breastfeeding. If breastfeeding, give 6 wkpostpartum; repeat every 12-14 wk.

Vaginal Ring Contraceptive

Vaginal (Adults): One ring inserted on or prior to day 5 of menstrual cycle. Ring is left in place for 3 wk, then removed for 1 wk, then a new ring is inserted.

Transdermal Patch

Transdermal (Adults): Patch is applied on day 1 of menstrual cycle (or convenient day in first week), changed weekly thereafter for 3 weeks. Week 4 is patch-free. Cycle is then repeated.

Acne

PO (by mouth, orally) (Adults): Ortho Tri-Cyclen only, taken daily for 21 days, off for 7 days.

Package & Price of Drug in Pharmacies of the US

(This lists the strengths and concentrations of available dose forms. Such information is useful in planning more convenient regimens (fewer tablets / capsules, less injection volume). General availability and average wholesale prices of commonly prescribed drugs have also been added as an aid to nurses with prescriptive authority.)

Combination Estrogen/Progestin Oral Contraceptives

Oral contraceptive tablets: Usually in monthly packs with enough (21) active tablets to complete a 28-day cycle. Some contain 7 inert tablets to complete the cycle with or without supplemental iron. Drug Cost: Apri — of Drug cost $179-93/6 cydes; Estrostep Fe — of Drug cost $354.26/6 cycles; Femcon Fe — of Drug cost $338.97/6 cycles; Kariva — of Drug cost $259-9/reduce/6 cycles; Levora — of Drug cost $ 151.94/6 cycles; Low-Ogestrel — of Drug cost $151.94/6 cycles; Necon 0.5/35 — of Drug cost $125.95/6 cycles; Ovcon 35 — of Drug cost $322.44/6 cycles; Sprintec — of Drug cost $ 143.10/6 cycles; Tri-Nessa — of Drug cost $137.94/6 cycles; Trivora-28 — of Drug cost $139-94/6 cycles; Yasmin — of Drug cost $299.90/6 cycles; Yaz — of Drug cost $307-96/6 cycles.

Extended-cycle Contraceptive

Drug Tablets: Seasonale- 84 active tablets containing 0.03 mg ethinyl estradiol and 0.15 mg levonorgestrel and 7 inactive tablets, Seasonique-active tablets containing 0.03 mg ethinly estradiol, 0.15 mg levonorgestrel, and 7 inactive tablets containing 0.01 mg ethinyl estradiol, Ly-brel — 28 active tablets containing 0.09 mg levonorgestrel and 0.02 mg ethinyl estradiol. Drug Cost: Lybrel — of Drug cost $49.99/28 tablets; Seasonale — of Drug cost $181.98/91 tablets; Seasonique — of Drug cost $165.98/91 tablets.

Levonorgestrel

Emergency contraceptives: 2 tablets containing 0.75 mg levonorgestrel (Plan B). Implant: Rod contains 68 mg etonogestrel. Intrauterine system: contains 52 mg levonorgestrel (releases 20 meg/day).

Medroxyprogesterone Injectable

Intramuscular (IM): 150 mg/ml. Injectable Subcutaneous: 104 mg/0.65 ml (in prefilled syringes).

Vaginal Ring Contraceptive

Ring: delivers 0.015 mg ethinyl estradiol and 0.120 mg etonogestrel/day. Drug Cost: of Drug cost $289-95/6 rings.

Transdermal Patch

Patch: contains 0.75 mg ethinyl estradiol and 6 mg of norelgestromin; releases 20 mg ethinyl estradiol/150 mg norelgestromin per 24 hours. Drug Cost: of Drug cost $299-95/18 patches.

Nursing Implications for Contraceptives

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