Name of the Hormonal Contraceptives-Oral Pills
- Norgestrel(0.5mg) + Ethinylestradiol(50μg
- Levonorgestrel
- Desogestrel
- Norethindrone
- medroxy progesterone
1. Norgestrel (0.5mg) + Ethinylestradiol(50μg)
| Norgestrel(0.5mg) + Ethinylestradiol(50μg) |
| Availability Transdermal patch: 6 mg norelgestromin and 0.75 mg ethinyl estradiol (releases 150 mcg norelgestromin and 20 mcg ethinyl estradiol q 24 hours) |
| Indications and dosages ➣To prevent pregnancy Adults: Apply patch on day 1 of menstrual cycle (or first Sunday after period begins). Change patch weekly thereafter for 3 weeks (on same day each week) and then remove patch for fourth week. Repeat q month. |
Mechanism of Action
Progestin-only oral contraceptives prevent conception by suppressing ovulation in approximately half of users, thickening the cervical mucus to inhibit sperm penetration, lowering the mid-cycle luteinizing hormone and follicle-stimulating hormone peaks, slowing the movement of the ovum through the fallopian tubes, and altering the endometrium
Administration
- Apply patch to clean, dry, intact skin on buttock, abdomen, upper torso, or upper outer arm.
- Change patch on same day each week (except for fourth week, when patch is removed).
Contraindications
- Hypersensitivity to drug or its components
- Undiagnosed abnormal genital bleeding
- Known or suspected breast cancer or history of such cancer
- Endometrial carcinoma or other known or suspected estrogendependent neoplasia
- Thromboembolism, history of thromboembolic disease, known thrombophilic conditions
- Current or past cerebrovascular or coronary artery disease
- Valvular heart disease with complications
- Diabetes with vascular involvement
- Persistent blood pressure values at or above 160 mm Hg systolic or 100 mm Hg diastolic
- Headache with focal neurologic symptoms
- Cholestatic jaundice of pregnancy, jaundice with previous hormonal contraceptive use
- Acute or chronic hepatic disease with abnormal liver function
- Hepatic adenomas or carcinomas
- Major surgery with prolonged immobilization
- Known or suspected pregnancy
Precautions:
- Cardiovascular disease, renal disease, asthma, bone disease, migraine, lipid disorders, fibrocystic breasts, increased risk for endometrial cancer, sexually transmitted diseases
- Family history of breast or genital tract cancer
- Abnormal mammogram
- Elderly patients (use not indicated)
- Women with body weight at or above198 lb (90 kg)
- Breastfeeding patients
- Children before menarche (use not indicated).
Adverse reactions
- CNS: headache, dizziness, lethargy, depression, emotional lability, increased risk of cerebrovascular accident
- CV: edema, hypertension, myocardial infarction, thromboembolism
- EENT: contact lens intolerance, worsening of myopia or astigmatism
- GI: nausea, vomiting, jaundice, abdominal cramps, bloating, anorexia, gallbladder disease, pancreatitis
- GU: amenorrhea, dysmenorrhea, breakthrough bleeding, cervical erosion, vaginal candidiasis, breast tenderness, breast enlargement or secretion, menstrual cramps, libido loss, increased risk of breast or endometrial cancer
- Hepatic: cholestatic jaundice, hepatic adenoma
- Metabolic: hyperglycemia, hypercalcemia, sodium and water retention
- Musculoskeletal: leg cramps
- Respiratory: upper respiratory infection, pulmonary embolism
- Skin: acne, oily skin, increased pigmentation, urticaria, patch site reaction
- Other: increased appetite, weight changes
Patient monitoring
- Evaluate menstrual pattern.
- Monitor blood pressure. Watch for signs and symptoms of thromboembolic disease (swelling or warmth in calf, sudden chest pain, shortness of breath).
- Check blood glucose level in diabetic patient.
Patient teaching
- Instruct patient to start using patch on first day of menstrual period or on first Sunday after period starts. Advise her to use calendar to keep track of which day each week to change patch.
- Tell patient to remove patch during fourth week of each cycle. Explain that she will have bleeding that week.
- Advise patient to check daily to ensure that patch is attached firmly to skin. Explain that if patch is detached for 1 day or less, she should try to reattach it more firmly. If patch is detached for more than 1 day or for an unknown length of time, she should start with new patch and new calendar.
- Instruct patient to use alternative contraception during first week of patch use.
- Inform patient that smoking while using patch increases risk of thromboembolic disease and other serious cardiovascular reactions. Stress importance of not smoking. Tell her to immediately report swelling or warmth in calf, chest pain, or shortness of breath.
- Advise breastfeeding patient to use other forms of contraception until she has completely weaned her infant.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, herbs, and behaviors mentioned above.
2.Levonorgestrel
| Levonorgestrel |
| Availability Intrauterine system (Mirena): 52 mg levonorgestrel Tablets (Plan B): 1.5 mg |
| Indications and dosages ➣ Intrauterine contraception for up to 5 years; heavy menstrual bleeding for women who choose to use intrauterine contraception Adults: One intrauterine system (Mirena) inserted into uterus for up to 5 years ➣ Emergency contraception to prevent pregnancy Adults: 1.5 mg (Plan B) P.O. as soon as possible within 72 hours after unprotected intercourse |
Mechanism of Action
Synthetic progestin, ovulation is inhibited from a negative feedback mechanism on hypothalamus, leading to reduced secretion of FSH and LH
Pharmacokinetics
- Peak Plasma Time: 1.4-2.5 hr
- Protein Bound: 50%
- Metabolized in liver
- Half-Life: 11-45 hr
- Excretion: Urine (40-50%), feces (32%
Administration
- Know that Mirena should be inserted under aseptic conditions by health care professional familiar with procedure.
- Verify that patient isn’t pregnant before Mirena insertion.
- Know that Plan B should be given as soon as possible within 72 hours of unprotected sexual intercourse. Drug isn’t suitable as long-term contraceptive.
Contraindications
- Mirena—
- Hypersensitivity to drug or its components
- Known or suspected pregnancy
- Congenital or acquired uterine anomaly
- Acute pelvic inflammatory disease (PID) or history of PID (unless patient had subsequent intrauterine pregnancy)
- Postpartum endometritis or infected abortion within past 3 months
- Known or suspected uterine or cervical neoplasia or unresolved abnormal Papanicolaou (Pap) test
- Untreated acute cervicitis or vaginitis
- Acute hepatic disease or hepatic tumor (benign or malignant)
- Genital bleeding of unknown cause
- Conditions associated with increased risk of infection
- Genital actinomycosis
- Previously inserted intrauterine device that has not been removed
- Known or suspected breast cancer
- History of ectopic pregnancy or conditions that predispose to it
Plan B —
- Hypersensitivity to drug or its components
- Known or suspected pregnancy
- Undiagnosed abnormal genital bleeding
Precautions:
- Diabetes mellitus
- Breastfeeding patients. Use Plan B cautiously in:
- Coagulopathy
- Diabetes mellitus
- Patients receiving anticoagulants concurrently.
Adverse reactions
- CNS: headache (Mirena, Plan B), fatigue, dizziness (Plan B), severe headache, migraine, nervousness, depression (Mirena) CV: hypertension (Mirena)
- EENT: sinusitis (Mirena)
- GI: nausea, vomiting, abdominal pain (Mirena, Plan B), diarrhea (Plan B), intestinal perforation or obstruction (Mirena)
- GU: breast tenderness (Mirena, Plan B); lighter or heavier menstrual bleeding (Plan B); breast pain; increased progesterone levels; ovarian cysts; dysmenorrhea; amenorrhea; spotting; erratic or prolonged menstrual bleeding; pelvic infection; vaginitis; cervicitis; dyspareunia; leukorrhea; decreased libido; abnormal Pap smear; expulsion, embedment in myometrium, adhesions, cervical or ureteral perforation (Mirena)
- Hematologic: anemia (Mirena)
- Hepatic: jaundice (Mirena)
- Musculoskeletal: back pain (Mirena)
- Respiratory: upper respiratory tract infection (Mirena)
- Skin: skin disorder, acne, eczema, hair loss (Mirena)
- Other: water retention, weight gain, sepsis (Mirena)
Patient monitoring
- Monitor blood pressure.
- Watch for adverse reactions, especially changes in menstrual bleeding.
- Monitor blood glucose level in diabetic patients.
- Check liver function tests frequently
Patient teaching
- Tell patient taking either product that drug does not prevent HIV or other sexually transmitted diseases.
- Teach patient using Mirena how to check (after menstrual period) to make sure thread still protrudes from cervix. Caution her not to pull on thread, because this could cause displacement.
- Instruct patient using Mirena to immediately report fever, chills, unusual vaginal discharge, or abdominal or pelvic pain or tenderness.
- Explain that for maximum efficacy, patient should take Plan B as soon as possible after unprotected sex.
- Inform patient that Plan B isn’t intended for routine contraception and doesn’t terminate existing pregnancy.
- Tell patient to report adverse reactions.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.
3.Desogestrel
| Desogestrel |
| Availability tablet, monophasic 0.15mg/0.03mg tablet, biphasic 0.15mg/0.02mg x 21 days, then inert tabs x 2 days, then 0mg/0.01mg x 5 days tablet, triphasic 0.1mg/0.025mg (7 tabs), plus 0.125mg/0.025mg (7 tabs), plus 0.15mg/0.025mg (7 tabs) |
| Indications and dosages Contraception Monophasic (Apri, Cyred, Cyred EQ, Desogen, Emoquette, Enskyce, Isibloom, Juleber, Ortho-Cept, Reclipsen, Solia) 1 tablet PO qDay for 28 days, then start new pack Days 1-21: Each tablet contains desogestrel 0.15 mg/ethinyl estradiol (EE) 0.03 mg Days 22-28: Inactive tablets Biphasic (Azurette, Bekyree, Kariva, Kimidess, Mircette, Pimtrea, Viorele) 1 tablet PO qDay for 28 days in order indicated on package, then start new pack Days 1-21, Each tablet contains 0.15 mg desogestrel/0.02 mg EE Days 22-23: Inactive tablets Days 24-28: Each tablet contains 0.01 mg ethinyl estradiol Triphasic (Cyclessa, Velivet, Caziant) 1 tablet PO qDay for 28 days in order indicated on package, then start new pack Day 1-7, each tablet contains 0.025 mg ethinyl estradiol and 0.1 mg desogestrel Days 8-14, each tablet contains 0.025 mg ethinyl estradiol and 0.125 desogestrel Days 15-21, each tablet contains 0.025 mg ethinyl estradiol and 0.15 desogestrel Days 22-28: Inactive tablets |
Mechanism of Action
Ethinyl estradiol (EE): Reduces LHRH release from hypothalamus, reduces gonadotropin release from pituitary; increase synthesis of DNA, RNA, and various proteins in target tissues
Desogestrel: Progestin; inhibits gonadotropin secretion from pituitary; prevents follicular maturation & ovulation, stimulates growth of mammary tissues
Pharmacokinetics
- Peak plasma time: Etonogestrel 1-1.5 hr; EE 1-1.5 hr
- Protein Bound: Etonogestrel 98% bound to SHBG; EE extensively bound to serum albumin
- Desogestrel: Metabolized by hepatic P450 enzyme CYP2C9 to etonogestrel (active metabolite)
- EE: Metabolized by hepatic CYP3A4 to estriol, estrone
- Half-Life: Etonogestrel: 38 hr; EE: 28 hr
- Excretion: Urine, feces
Contraindications
- Documented hypersensitivity
- Active or history of breast cancer
- Arterial thromboembolic disease (stroke, MI), thrombophlebitis, DVT/PE, thrombogenic valvular disease
- Estrogen-dependent neoplasia
- Liver disease, liver tumors
- Undiagnosed abnormal vaginal bleeding
- Uncontrolled hypertension (ie, persistent BP values >160 mm Hg systolic or >100 mg Hg diastolic)
- Diabetes mellitus with vascular involvement, jaundice with prior oral contraceptive use
- Inherited or acquired hyper coagulopathies
- Smoke, if age >35 years
- Receiving hepatitis C drug combinations containing ombitasvir/paritaprevir/ritonavir, with or without dasabuvir, due to potential for ALT elevations
Side –Effects
- Serious cardiovascular events and stroke
- Vascular events
- Liver disease
- Depressed mood, mood altered
- Headache
- Nausea, abdominal pain
- Breast tenderness, breast pain
- Weight increased
4.Norethindrone
| Norethindrone |
| Availability Tablets: 0.35 mg, 5 mg |
| Indications and dosages ➣ Endometriosis Adults: 5 mg Aygestin P.O. daily for 2 weeks, increased in increments of 2.5 mg/day q 2 weeks until 15 mg daily is reached ➣ Amenorrhea; abnormal uterine bleeding Adults: 2.5 to 10 mg Aygestin P.O. daily starting on day 5 of menstrual cycle |
Mechanism of Action
Progestin; inhibits secretion of gonadotropins from pituitary gland; prevents follicular maturation & ovulation, stimulates growth of mammary tissues
Pharmacokinetics
- Bioavailability: 64%
- Peak Plasma Time: 1-2 hr
- Protein Bound: 61%
- Metabolism: Liver
- Half-Life: 4-13 hr
- Excretion: Urine 33-81%; feces 35-43%
Administration
- Give with or without food.
- When administering for endometriosis, amenorrhea, or abnormal uterine bleeding, know that therapy may continue for 6 to 9 months or until breakthrough bleeding necessitates a temporary halt.
When administering for prevention of pregnancy, know that drug must be given continuously every day at the same time with no interruptions between pill packs.
Contraindications
- Hypersensitivity to drug
- Impaired liver function or liver disease
- Thromboembolic disorders
- Known or suspected breast cancer
- Undiagnosed vaginal bleeding
- Known or suspected pregnancy
- As a diagnostic test for pregnancy
Precautions:
- Hypertension, blood dyscrasias, bone marrow disease, hepatic or renal disease, gallbladder disease, heart failure, diabetes mellitus, depression, migraine, asthma, seizure disorder
- Family history of breast or reproductive tract cancer
- Breastfeeding patients.
Adverse reactions
- CNS: migraine, depression, insomnia, drowsiness
- EENT: retinal vascular lesions, sudden partial or complete vision loss, proptosis, diplopia, papilledema
- GI: nausea
- GU: breakthrough bleeding, menstrual flow changes, amenorrhea, changes in cervical erosion and secretions, breast tenderness and secretion
- Hepatic: cholestatic jaundice
- Metabolic: fluid retention, decreased glucose tolerance
- Skin: rash, urticaria, acne, hirsutism, chloasma
- Other: edema, weight gain or loss, fever
Patient monitoring
- Monitor pretreatment and annual physical exams to check blood pressure, breasts, abdomen, pelvic organs, and Pap smear results.
- Assess for signs and symptoms of depression, especially in patients with history of depression. Stop giving drug if significant depression recurs.
- Check blood glucose level in diabetic patients.
Patient teaching
- Instruct patient to avoid pregnancy or to discontinue drug if she gets pregnant (may cause serious fetal anomalies or fetal death).
- Advise patient to discontinue drug and consult prescriber if she experiences sudden partial or complete vision loss.
- If patient is receiving drug to treat amenorrhea, tell her to mark administration days on calendar.
- Instruct patient taking drug to prevent pregnancy to take drug every day at the same time without interruption between pill packs.
- Tell diabetic patient to monitor blood glucose level closely and to watch for hyperglycemia.
- Instruct patient to report breakthrough bleeding, spotting, change in menstrual flow, or amenorrhea.
- Caution patient not to smoke during therapy.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.
5.Medroxy progesterone
| Medroxy progesterone |
| Availability Suspension for depot injection: 150 mg/ ml, 400 mg/ml Suspension for depot subcutaneous injection: 104 mg/0.65 ml in prefilled single-use syringes Tablets: 2.5 mg, 5 mg, 10 mg |
| Indications and dosages ➣ Secondary amenorrhea Adults: 5 to 10 mg/day P.O. for 5 to 10 days, starting at any time during menstrual cycle ➣ Dysfunctional uterine bleeding; menses induction Adults: 5 to 10 mg/day P.O. for 5 to 10 days, starting on day 16 or 21 of menstrual cycle ➣ To prevent estrogen-related endometrial changes in postmenopausal women Adults: 2.5 to 5 mg/day P.O. given with 0.625 mg conjugated estrogens P.O. (monophasic regimen); or 5 mg/day P.O. on days 15 to 28 of cycle, given with 0.625 mg conjugated estrogens P.O. daily throughout cycle (biphasic regimen) ➣ Management of endometriosis associated pain Adults: 104 mg (Depot-subcutaneousProvera) in anterior thigh or abdomen q 12 to 14 weeks ➣ To prevent pregnancy Adults: 150 mg (Depo-Provera) deep I.M. injection q 13 weeks or 104 mg (Depot-subcutaneousProvera) in anterior thigh or abdomen q 12 to 14 weeks. Give first injection during first 5 days of normal menstrual period or first 5 postpartal days if patient isn’t breastfeeding, or during sixth postpartal week if patient is breastfeeding exclusively. ➣ Renal or endometrial cancer Adults: 400 to 1,000 mg I.M.; may repeat weekly. If improvement occurs, decrease to 400 mg q month. |
Mechanism of Action
Progestin inhibits the secretion of gonadotropins, which primarily prevents follicular maturation and ovulation and causes thickening cervical mucus; these actions contribute to its contraceptive effects
Suppression of serum estradiol concentrations is likely to be responsible for the therapeutic effect on endometriosis-associated pain
Pharmacokinetics
Protein bound: ~90%
Metabolism
Following oral dosing, MPA is extensively metabolized in the liver via hydroxylation, with subsequent conjugation and elimination in the urin
Half-life
- Oral (single dose): 12.1 hr (2 x 10-mg doses); 11.6 hr (8 x 2.5-mg doses)
- Oral (multiple doses): 16.6 ng/mL (10-mg dose)
Administration
- Before starting therapy, obtain thorough history and physical examination, with emphasis on breast and pelvic organs. Also obtain Pap smear and repeat annually during therapy.
- With contraceptive use, rule out pregnancy before first dose and when more than 14 weeks have passed since previous dose.
- For I.M. injection, inject deep into gluteal, deltoid, or anterior thigh muscle. Rotate injection sites.
- Be aware that when drug is used to prevent estrogen-related endometrial changes in postmenopausal women, lowest dosage should be used for shortest time, because treatment exceeding 1 year correlates with cancer. (Some combination products have 0.3 mg estrogen/1.5 mg progesterone or 0.45 mg estrogen/1.5 mg progesterone.)
Contraindications
- Hypersensitivity to drug or its components
- Cerebrovascular or thromboembolic disease
- Hepatic dysfunction or disease
- Breast or genital cancer
- Undiagnosed vaginal bleeding
- Known or suspected pregnancy
Precautions:
- Seizure disorder, renal or cardiovascular disease, asthma, diabetes mellitus, depression, migraine
- History of hepatic disease.
Adverse reactions
- CNS: insomnia, migraine, nervousness, drowsiness, dizziness, fatigue, depression, mood changes
- CV: thrombophlebitis, thromboembolism
- EENT: diplopia, proptosis, retinal vascular lesions, papilledema
- GI: abdominal pain, bloating
- GU: amenorrhea, leukorrhea, spotting, cervical secretions, galactorrhea, breast tenderness and secretion, cervical erosions, pelvic pain, infertility
- Hepatic: jaundice
- Metabolic: fluid retention, hyperglycemia
- Musculoskeletal: leg cramps, back pain
- Respiratory: pulmonary embolism
- Skin: pruritus, urticaria, rash, acne, alopecia, hirsutism, chloasma, melasma, sterile abscesses, induration at I.M. site Other: weight and appetite changes, edema, angioedema, allergic reactions including anaphylaxis
Patient monitoring
- Monitor patient for fluid retention and for signs and symptoms of thrombophlebitis, including pain, swelling, and redness of lower legs.
- Assess for visual disturbances and headache. If ocular exam shows papilledema or retinal vascular lesions, drug should be discontinued.
- Evaluate liver function tests.
- Watch for abdominal pain, fever, malaise, jaundice, darkened urine, and clay-colored stools
Patient teaching
- Advise patient that drug may cause nausea, vomiting, headache, abdominal pain, painful breast swelling, and abnormal bleeding pattern. Instruct her to report these effects if pronounced.
- Tell patient to promptly report bloating, swelling, appetite loss, rash, yellowed skin, mood changes or depression, nervousness, dizziness, chest pain, shortness of breath, visual disturbances, or severe headache.
- Teach patient how to perform breast self-exams.
- Tell patient she must undergo yearly physical examinations with Pap smear.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above.
REFERENCES
- Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
- McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
- April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
- Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
- Nursebro.com, Search – Nursebro
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