Names and pronunciation
Delestrogen
Source page 517
Loading InternPractice…
Individual generic drug information
Extracted information for estradiol valerate only.
Delestrogen
Source page 517
Func. class.: Estrogen, progestins
Source page 517
ACTION: Needed for adequate func- tioning of female reproductive system; affects release of pituitary gonadotropins; inhibits ovulation; adequate calcium use in bone
Source page 517
USES: Vasomotor symptoms (meno- pause), inoperable breast cancer (selected cases), prostatic cancer, atrophic vaginitis, kraurosis vulvae, hypogonadism, primary ovarian failure, prevention of osteoporosis, castration
Source page 517
Extracted information for estradiol valerate only.
CONTRAINDICATIONS: Preg- nancy, breastfeeding, reproductive cancer, genital bleeding (abnormal, undiagnosed), protein S or C deficiency, antithrombin deficiency, angioedema, MI, stroke
Source page 517
Black Box Warning: Breast/endometrial cancer, thromboembolic disorders, MI, stroke Precautions: Hypertension, asthma, blood dyscrasias, gallbladder/bone/renal/ hepatic disease, HF, diabetes mellitus, depression, migraine headache, sei- zure disorders, family history of cancer of breast or reproductive tract, smoking, uter- ine fibroids, vaginal irritation/infection, his- tory of angioedema, cardiac disease Black Box Warning: dementia, acciden- tal exposure pets/children (topical) Black Box Warning: For previous breast/ endometrial cancer, thromboembolic disorders, MI, stroke, dementia; use ad- equate screening for these conditions, estrogen increases the risk • Blood glucose of diabetic patient; hy- perglycemia may occur • Weight daily; notify prescriber of weekly weight gain >5 lb; if increase, diuretic may be ordered • B/P q4hr; watch for increase caused by water and sodium retention • I&O ratio; decreasing urinary output, increasing edema, report changes E • Hepatic studies, including AST, ALT, bilirubin, alkaline phosphatase at baseline, periodically; periodic folic acid level • Hypertension, cardiac symptoms, jaundice, hypercalcemia • Mental status: affect, mood, behav- ioral changes, aggression • Female patient for intact uterus; if so, progesterone should be added to estro- gen therapy to decrease risk of endome- trial cancer • Beers: avoid oral and topical patch in older adults; evidence of carcinogenic potential (breast, endometrial) • Pregnancy/breastfeeding: do not use in pregnancy; estrogens decrease milk production; use only if needed
Source pages 517, 518, 519
SIDE EFFECTS CNS: Dizziness, headache, migraines, depression, seizures CV: Hypertension, thrombophlebitis, edema, thromboembolism, stroke, pulmo- nary embolism, MI, chest pain EENT: Contact lens intolerance, increased myopia, astigmatism, throat swelling, eyelid edema GI: Nausea, vomiting, diarrhea, anorexia, pancreatitis, cramps, constipation, increased appetite, increased weight, cholestatic jaundice, hepatic adenoma GU: Amenorrhea, cervical erosion, break- through bleeding, dysmenorrhea, vaginal candidiasis, breast changes, gynecomas- tia, testicular atrophy, impotence, increased risk of breast cancer, endome- trial cancer, changes in libido; toxic shock, vaginal wall ulceration/erosion (vag ring) INTEG: Rash, urticaria, acne, hirsutism, alopecia, oily skin, seborrhea, purpura, erythema, pruritus, melasma; site irrita- tion (transdermal) META: Folic acid deficiency, hypercalce- mia, hyperglycemia
Source pages 518, 519
INTERACTIONS Increase: action of corticosteroids, tricyclics Increase: toxicity—cycloSPORINE, dantrolene Decrease: action of anticoagulants, oral hypoglycemics, tamoxifen Decrease: estradiol action—anticon- vulsants, barbiturates, phenylbutazone, rifAMPin, calcium Drug/Herb • Altered estrogen effect: black cohosh, DHEA Decrease: estrogen effect—saw pal- metto, St. John’s wort Drug/Food Increase: estrogen level—grapefruit juice Drug/Lab Test Increase: BSP retention test, PBI, T4, serum sodium, platelet aggregation, thy- roxine-binding globulin (TBG), prothrom- bin; factors VII, VIII, IX, X; triglycerides Decrease: serum folate, serum triglyceride, T3 resin uptake test, glucose tolerance test, antithrombin III, pregnanediol, metyra- pone test False positive: LE prep, ANA
Source page 519
Extracted information for estradiol valerate only.
DOSAGE AND ROUTES Hormone replacement/menopause symptoms • Adult: TRANSDERMAL 1 patch deliv- ering 0.025, 0.0375, 0.05, 0.075, or 0.1 mg/day 2×/wk (Alora, Estraderm, Viv- elle-Dot); 1 patch delivering 0.025, 0.0375, 0.05, 0.06, 0.075, or 0.1 mg/day replace q7days (Climara); GEL apply entire unit-dose packet to 5 × 7-inch area of upper thigh/day, alternate thighs; SPRAY (Evamist) 1 spray to inner sur- face of forearm/day in AM Menopause/hypogonadism/ castration/ovarian failure • Adult: PO 0.5-2 mg/day, 3 wk on, 1 wk off or continuously; IM (cypionate) 1-5 mg q3-4wk; (valerate) 10-20 mg q4wk • Adult: TOPICAL (Estraderm) 0.05 mg/24 hr applied 2×/wk; (Climara) 0.05 mg/hr applied 1×/wk in cyclic regimen; women with hysterectomy may use con- tinuously Postmenopausal osteoporosis, prophylaxis • Adult female: PO 0.5 mg/day × 23 days of a 28-day cycle; TRANSDERMAL (Al- ora, Minivelle, Vivelle-Dot) 0.025 mg/day applied to skin 2×/wk; adjust as needed based on clinical response, bone mineral TRANSDERMAL density; (Climara) 0.025 mg/day applied to skin weekly Prostatic cancer (inoperable) • Adult: IM (valerate) 30 mg q1-2wk; PO (oral estradiol) 1-2 mg bid-tid Breast cancer (palliative treatment) • Adult: PO 10 mg tid × 3 mo or longer Atrophic vaginitis/kraurosis vulvae • Adult: VAG CREAM 2-4 g/day × 1-2 wk, then 1 g 1-3×/wk cycled; VAG TAB- LET 1/day × 2 wk, maintenance 1 tab 2×/wk; VAG RING inserted, left in place continuously for 3 mo Vasomotor symptoms • Adult: TOPICAL after cleaning and drying skin on left thigh, calf, rub in contents of pouch using both hands until completely absorbed; wash hands
Source page 518
Available forms: Estradiol: tablets 0.5, 1, 2 mg; valerate: injection 10, 20, 40 mg/ mL; transdermal: 0.014, 0.025, 0.0375, 0.05, 0.075, 0.1 mg/24 hr release rate; vag cream: 100 mcg/g; vag tablet: 10 mcg; vag ring: 2 mg/90 days; topical emulsion: 2.5 mg; gel (Divigel) 0.06%, 0.1%; spray (Evamist) 1.53 mg/actuation
Source page 518
Administer: • Titrated dose; use lowest effective dose • IM inject deeply in large muscle mass PO route • With food or milk to decrease GI symptoms Transdermal route • May contain aluminum or other met- als in backing of patch, can overheat in MRI scan and burn patients • Apply to trunk of body 2×/wk; press firmly, hold in place for 10 sec to ensure good contact; do not apply to breasts • On intermittent cycle schedule: 3 wk on, then 1 wk off; if patch falls off, reapply Topical route • Use Evamist daily; spray to inner up- per arm; may increase to 2-3×/day based on response; allow to dry for 2 min, avoid secondary exposure to children, pets, caregivers Vaginal route • Use a new applicator daily, provided
Source page 518
Extracted information for estradiol valerate only.
Assess:
Source page 519
Evaluate: • Therapeutic response: reversal of menopause symptoms; decrease in tumor size in prostatic, breast cancer
Source page 519
CLINICAL CONSIDERATIONS
Source page 519
Patient and caregiver information: • To weigh weekly; to report gain >5 lb • To report breast lumps, vaginal bleeding, edema, jaundice, dark urine, clay-colored stools, dyspnea, headache, blurred vision, abdominal pain, numb- ness or stiffness in legs, chest pain; tenderness, redness, and swelling in extremities; males to report impotence, gynecomastia; to report dermal rash with transdermal patch • To avoid grapefruit or grapefruit juice (PO) • That smoking increases CV condi- tions; encourage to stop • To notify prescriber if pregnancy is planned or suspected; not to become pregnant when using estrogen • To report changes in blood glucose if diabetic HIGH ALERT
Source pages 519, 520
Extracted information for estradiol valerate only.
PHARMACOKINETICS PO/INJECTION/TRANSDERMAL: Degraded in liver, excreted in urine, crosses placenta, excreted in breast milk
Source page 519
Filter the extracted dose blocks for this individual drug.
Hormone replacement/menopause symptoms
• Adult: TRANSDERMAL 1 patch deliv- ering 0.025, 0.0375, 0.05, 0.075, or 0.1 mg/day 2×/wk (Alora, Estraderm, Viv- elle-Dot); 1 patch delivering 0.025, 0.0375, 0.05, 0.06, 0.075, or 0.1 mg/day replace q7days (Climara); GEL apply entire unit-dose packet to 5 × 7-inch area of upper thigh/day, alternate thighs; SPRAY (Evamist) 1 spray to inner sur- face of forearm/day in AM Menopause/hypogonadism/ castration/ovarian failure
Candidate age grouping · source page 518
Hormone replacement/menopause symptoms
• Adult: PO 0.5-2 mg/day, 3 wk on, 1 wk off or continuously; IM (cypionate) 1-5 mg q3-4wk; (valerate) 10-20 mg q4wk
Candidate age grouping · source page 518
Hormone replacement/menopause symptoms
• Adult: TOPICAL (Estraderm) 0.05 mg/24 hr applied 2×/wk; (Climara) 0.05 mg/hr applied 1×/wk in cyclic regimen; women with hysterectomy may use con- tinuously Postmenopausal osteoporosis, prophylaxis
Candidate age grouping · source page 518
Hormone replacement/menopause symptoms
• Adult female: PO 0.5 mg/day × 23 days of a 28-day cycle; TRANSDERMAL (Al- ora, Minivelle, Vivelle-Dot) 0.025 mg/day applied to skin 2×/wk; adjust as needed based on clinical response, bone mineral TRANSDERMAL density; (Climara) 0.025 mg/day applied to skin weekly Prostatic cancer (inoperable)
Candidate age grouping · source page 518
Hormone replacement/menopause symptoms
• Adult: IM (valerate) 30 mg q1-2wk; PO (oral estradiol) 1-2 mg bid-tid Breast cancer (palliative treatment)
Candidate age grouping · source page 518
Hormone replacement/menopause symptoms
• Adult: PO 10 mg tid × 3 mo or longer Atrophic vaginitis/kraurosis vulvae
Candidate age grouping · source page 518
Hormone replacement/menopause symptoms
• Adult: VAG CREAM 2-4 g/day × 1-2 wk, then 1 g 1-3×/wk cycled; VAG TAB- LET 1/day × 2 wk, maintenance 1 tab 2×/wk; VAG RING inserted, left in place continuously for 3 mo Vasomotor symptoms
Candidate age grouping · source page 518
Hormone replacement/menopause symptoms
• Adult: TOPICAL after cleaning and drying skin on left thigh, calf, rub in contents of pouch using both hands until completely absorbed; wash hands
Candidate age grouping · source page 518