Estrogen Patch Canada
Climara Pro- Patch, transdermal estradiol 0.045 mg/levonorgestrel 0.015 mg per 24 hCombiPatch- Patch, transdermal estradiol 0.05 mg/norethindrone 0.14 mg per 24 h- Patch, transdermal estradiol 0.05 mg/norethindrone 0.25 mg per 24 hPharmacologyEstrogens act to reduce the elevated levels of gonadotropins, luteinizing hormone, and follicle-stimulating hormone seen in postmenopausal women. Progestins counteract the proliferative effects of estrogens on the endometrium. Indications and UsageModerate to severe vasomotor symptoms associated with menopause; moderate to severe symptoms of vulvar and vaginal atrophy associated with menopause ( CombiPatch only); hypoestrogenism due to hypogonadism, castration, or primary ovarian failure ( CombiPatch only); prevention of postmenopausal osteoporosis ( Climara Pro only).
ContraindicationsUndiagnosed abnormal genital bleeding; known, suspected, or history of cancer of the breast; known or suspected estrogen-dependent neoplasia; active deep vein thrombosis, pulmonary embolism, or history of these conditions; active or recent (eg, within past year) arterial thromboembolic disease (eg, MI, stroke); liver dysfunction or disease; known or suspected pregnancy; hypersensitivity to any component of the product. Dosage and Administration Adults Transdermal Climara ProApply 1 patch to the lower abdomen; apply new patch once weekly.
CombiPatchApply 1 patch to the lower abdomen; apply new patch twice weekly. For continuous combined regimen, use regimen continuously. For continuous sequential regimen, use estradiol 0.05 mg/day patch for days 1 to 14 and use CombiPatch for days 15 to 28.
General Advice. Application site should be a smooth (fold-free), clean, dry area of the skin on the lower abdomen. Do not apply on the waistline, to or near the breasts, or to areas where sitting could dislodge the patch.
Ensure selected area is not oily, damaged, or irritated. Rotate application site, with an interval of at least 1 wk allowed between applications to the same site. If patch falls off, the same patch may be reapplied to another area of the lower abdomen. If necessary, a new patch may be applied and the original treatment schedule should be continued. A dose of estradiol 0.05 mg/norethindrone 0.25 mg may be used if a greater progestin dose is desired.Storage/Stability Climara ProStore between 59° and 86°F. CombiPatchPrior to dispensing, store between 36° and 46°F. After dispensing, store below 77°F for up to 6 mo.
Drug Interactions AcitretinAcitretin may interfere with the pharmacologic effects of progestins. AprepitantEstrogen/progestin plasma concentrations and pharmacologic effects may be decreased by aprepitant, reducing the efficacy. Beta-blockers (eg, metoprolol, propranolol)The pharmacologic effects of beta-blockers may be increased.
Monitor patient response; adjust the beta-blocker dose as needed. Corticosteroids (eg, prednisolone)Corticosteroid plasma concentrations may be elevated, increasing the pharmacologic effects and risk of toxicity.
Monitor for signs of corticosteroid toxicity (cushingoid facies, weight gain, fluid retention); reduce the corticosteroid dose if necessary. CyclosporineCyclosporine plasma concentrations may be elevated, increasing the pharmacologic effects and risk of toxicity (eg, nephrotoxicity). Monitor serum cyclosporine concentrations, as well as renal and liver function, for evidence of cyclosporine toxicity. Adjust the cyclosporine dose as needed. CYP3A4 inducers (eg, barbiturates eg, phenobarbital, carbamazepine, efavirenz, modafinil, rifampin, rufinamide, St.
John's wort)Coadministration may reduce plasma concentrations of estrogens, possibly resulting in a decrease in therapeutic effects and/or changes in the uterine bleeding profile. CYP3A4 inhibitors (eg, azole antifungals eg, itraconazole, ketoconazole, grapefruit juice, macrolide antibiotics eg, clarithromycin, erythromycin, protease inhibitors eg, ritonavir)Coadministration may increase plasma concentrations of estrogens, increasing the risk of adverse reactions.
Monitor for estrogen-related adverse reactions. Felbamate, griseofulvin, penicillins (eg, ampicillin), pioglitazone, tetracyclinesThese agents may decrease the pharmacologic effects of estrogen/progestin combinations. Hydantoins (eg, phenytoin)Hydantoins may decrease the pharmacologic effects of estrogen/progestin combinations. In addition, hydantoin concentrations may be altered. Adjust the hydantoin dose as needed.
LamotrigineLamotrigine plasma concentrations may be reduced, decreasing the pharmacologic effects. Adjust the lamotrigine dose as needed. NevirapineNevirapine may decrease the pharmacologic effects of estrogen/progestin combinations.
Estrogen Patch For Men
Coadministration is not recommended. Selegiline, tacrine, tacrolimus, tizanidineEstrogen/progestin combinations may elevate the plasma concentrations of these agents, increasing the pharmacologic effects and risk of adverse reactions. Monitor closely; adjust the dose of these agents as needed. Theophyllines (eg, aminophylline)Theophylline plasma concentrations may be elevated, increasing the pharmacologic effects and risk of toxicity (eg, CV instability, nausea, seizures, vomiting). Monitor theophylline concentrations and the patient for signs of theophylline toxicity; adjust the theophylline dose as needed.
TopiramateCl of estrogen from plasma is increased by topiramate at dosages greater than 200 mg/day. Cl of progestin does not appear to be affected. Tranexamic acidThe risk of estrogen/progestin-related thrombotic events may be increased. Limit coadministration of tranexamic acid with an estrogen/progestin combination to patients with a strong medical need in whom the potential benefits outweigh the increased risk of a thrombotic event. Valproic acidValproic acid plasma concentrations may be reduced, decreasing the pharmacologic effects and increasing the risk of seizures.
Monitor patient and valproic acid concentrations; adjust the valproic acid dose as needed. Laboratory Test InteractionsImpaired glucose tolerance. DecreasedAntithrombin III activity; levels of anti-factor Xa and antithrombin III activity; free hormone concentrations; LDL; response to metyrapone test; T 3 resin uptake. IncreasedPTT, platelet aggregation time, and PT; platelet count; factors II, VII antigen, VIII antigen, VIII coagulation activity, IX, X, XII, VII-X complex, II-VII-X complex, and beta thromboglobulin; levels of fibrinogen and fibrinogen activity; plasminogen antigen and activity; thyroid-binding globulin (TBG) leading to increased circulating total thyroid hormone (as measured by protein-bound iodine, T 4 or T 3 ); corticosteroid binding globulin; sex hormone–binding globulin; angiotensinogen/renin substrate, alpha-1 antitrypsin, ceruloplasmin; HDL, HDL 2, and triglyceride levels. Adverse Reactions CardiovascularHypertension (3%); deep and superficial venous thrombosis, increase in BP, MI, pulmonary embolism, stroke, thrombophlebitis.
CNSHeadache (25%); depression (9%); insomnia (8%); dizziness (7%), nervousness (6%); chorea, dementia, exacerbation of epilepsy, irritability, migraine, mood disturbances. DermatologicApplication-site reaction (41%); rash (6%); acne (5%); chloasma or melasma (may persist when drug is discontinued), erythema multiforme, erythema nodosum, hemorrhagic eruption, hirsutism, loss of scalp hair, pruritus, urticaria.
Estrogen Patch Review
Hormone Replacement Therapy
EENTIntolerance of contact lenses, retinal vascular thrombosis. GIAbdominal pain, diarrhea (14%); nausea (12%); dyspepsia (8%); flatulence (7%); tooth disorder (6%); constipation (5%); abdominal cramps, bloating, cholestatic jaundice, enlargement of hepatic hemangiomas, increased incidence of gallbladder disease, pancreatitis, vomiting.