Names and pronunciation
(nor-eth-in′drone) Activelle , Aygestin, Brevicon , Camila, Errin, Estalis , Heather, Incassia, Jencycla, Loestrin , LeLo , Minestrin , Nora-BE
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Drug reference
(nor-eth-in′drone) Activelle , Aygestin, Brevicon , Camila, Errin, Estalis , Heather, Incassia, Jencycla, Loestrin , LeLo , Minestrin , Nora-BE
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Func. class.: Progestogen
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ACTION: Inhibits the secretion of pitu- itary gonadotropins, which prevents follicu- lar maturation and ovulation; stimulates growth of mammary tissue; antineoplastic action against endometrial cancer
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USES: Uterine bleeding (abnormal), amenorrhea, endometriosis, contraception
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CONTRAINDICATIONS: Preg- nancy, breast cancer, hypersensitivity, thromboembolic disorders, reproductive cancer, genital bleeding (abnormal, undi- agnosed), liver tumors, hepatic disease Precautions: Breastfeeding, hypertension, asthma, blood dyscrasias, HF, diabetes mel- litus, depression, migraine headache, sei- zure disorders, bone/gallbladder/renal/ hepatic disease, family history of breast or reproductive tract cancer, smoking, HIV
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SIDE EFFECTS CNS: Dizziness, headache, migraines, depression, fatigue CV: Hypotension, thrombophlebitis, edema, thromboembolism, CVA, stroke, PE, MI EENT: Diplopia GI: Nausea, vomiting, anorexia, cramps, increased weight, cholestatic jaundice GU: Amenorrhea, cervical erosion, breakthrough bleeding, dysmenorrhea, vaginal candidiasis, breast changes, (gynecomastia, testicular atrophy, impo- tence), endometriosis, spontaneous abortion, breast tenderness INTEG: Rash, urticaria, acne, hirsutism, alopecia, oily skin, seborrhea, purpura, melasma META: Hyperglycemia
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INTERACTIONS Decrease: progestin effect—barbitu- rates, carBAMazepine, fosphenytoin, phenytoin, rifampin Drug/Herb Decrease: contraception—St. John’s wort Drug/Food Increase: caffeine level—caffeine Drug/Lab Test Increase: LDL Decrease: GTT, HDL, alk phos
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DOSAGE AND ROUTES Amenorrhea, abnormal uterine bleeding (Aygestin) • Adult: PO 2.5-10 mg/day on days 5-25 N of menstrual cycle Endometriosis (Aygestin) • Adult: PO 5 mg/day × 2 wk, then in- creased by 2.5 mg/day × 2 wk up to 15 mg/day, may continue for 6-9 mo Contraception • Adult: PO 0.35 mg on 1st day of men- ses, then 0.35 mg/day
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Available forms: Tabs 5 mg; tabs 0.35 mg
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Administer: • Titrated dose; use lowest effective dose • One dose in AM; do not interrupt between pill packs; give at roughly same time of day • Without regard to meals • Store in dark area
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Assess: • Weight daily: notify prescriber of weekly weight gain >5 lb • B/P at beginning of treatment and pe- riodically • I&O ratio; be alert for decreasing uri- nary output, increasing edema • Hepatic studies: ALT, AST, bilirubin periodically during long-term therapy • Edema, hypertension, cardiac symp- toms, jaundice, thromboembolism • Mental status: affect, mood, behav- ioral changes, depression • Monitor for hypercalcemia • Monitor Pap smear
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Evaluate: • Therapeutic response: decreased ab- normal uterine bleeding, absence of amenorrhea
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • About cushingoid symptoms (fatigue, weakness, increased thirst/urination, anxiety, weight gain, facial puffiness) • To report vaginal bleeding, amenorrhea, edema, jaundice, dark urine, clay-colored stools, dyspnea, headache, blurred vision, abdominal pain, numbness or stiffness in legs, chest pain; impotence or gyneco- mastia (men) • To take at same time of day; not to in- terrupt between pill packs • Pregnancy: to report suspected preg- nancy immediately; to wait ≥3 mo after stopping product to become pregnant; to use backup contraception methods for 48 hr if treatment is not begun on the first day of menstruation • To avoid smoking; CV reactions may occur • That product does not protect against HIV, STDs • That product may mask onset of meno- pause
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PHARMACOKINETICS Excreted in urine, feces; metabolized in liver, half-life 5-14 hr
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• Adult: PO 2.5-10 mg/day on days 5-25 N of menstrual cycle Endometriosis (Aygestin)
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• Adult: PO 5 mg/day × 2 wk, then in- creased by 2.5 mg/day × 2 wk up to 15 mg/day, may continue for 6-9 mo Contraception
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• Adult: PO 0.35 mg on 1st day of men- ses, then 0.35 mg/day
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