Sunday, April 12, 2009

Salticin




Salticin may be available in the countries listed below.


Ingredient matches for Salticin



Gentamicin

Gentamicin sulfate (a derivative of Gentamicin) is reported as an ingredient of Salticin in the following countries:


  • Indonesia

International Drug Name Search

Friday, April 10, 2009

Aludex




Aludex may be available in the countries listed below.


In some countries, this medicine may only be approved for veterinary use.

Ingredient matches for Aludex



Amitraz

Amitraz is reported as an ingredient of Aludex in the following countries:


  • Ireland

  • United Kingdom

International Drug Name Search

Micardis HCT




In the US, Micardis HCT (hydrochlorothiazide/telmisartan systemic) is a member of the drug class antihypertensive combinations and is used to treat High Blood Pressure.

US matches:

  • Micardis HCT

Ingredient matches for Micardis HCT



Hydrochlorothiazide

Hydrochlorothiazide is reported as an ingredient of Micardis HCT in the following countries:


  • United States

Telmisartan

Telmisartan is reported as an ingredient of Micardis HCT in the following countries:


  • United States

International Drug Name Search

Thursday, April 9, 2009

Buflomed




Buflomed may be available in the countries listed below.


Ingredient matches for Buflomed



Buflomedil

Buflomedil is reported as an ingredient of Buflomed in the following countries:


  • Argentina

Buflomedil hydrochloride (a derivative of Buflomedil) is reported as an ingredient of Buflomed in the following countries:


  • Austria

International Drug Name Search

Monday, April 6, 2009

Darifenacin Hydrobromide


Class: Genitourinary Smooth Muscle Relaxants
Chemical Name: (S)-1-[2-(2,3-Dihydro-5-benzofuranyl)ethyl]-α,α-diphenyl-3-pyrrolidineacetamide
Molecular Formula: C28H30N2O2
CAS Number: 133099-04-4
Brands: Enablex

Introduction

Genitourinary antispasmodic agent; an antimuscarinic agent.1


Uses for Darifenacin Hydrobromide


Overactive Bladder


Relief of symptoms associated with voiding (e.g., urge urinary incontinence, urgency, frequency).1


Extended-release darifenacin (15 mg once daily) may be as effective as immediate-release oxybutynin (5 mg 3 times daily).5


Darifenacin Hydrobromide Dosage and Administration


Administration


Oral Administration


Administer orally once daily with liquids without regard to meals.1


Swallow tablets whole; do not chew, divide, or crush.1


Dosage


Available as darifenacin hydrobromide; dosage expressed in terms of darifenacin.1


Adults


Overactive Bladder

Oral

Initially, 7.5 mg once daily.1 May increase after 2 weeks to 15 mg once daily according to response.1


Prescribing Limits


Adults


Overactive Bladder

Oral

Maximum 15 mg daily.1


Special Populations


Hepatic Impairment


No dosage adjustment required in patients with mild hepatic impairment (Child-Pugh class A).1


Maximum 7.5 mg daily in patients with moderate hepatic impairment (Child-Pugh class B).1


Use not recommended in patients with severe hepatic impairment (Child-Pugh class C).1 (See Distribution: Special Populations, under Pharmacokinetics.)


Renal Impairment


No dosage adjustment required.1 8


Geriatric Patients


No dosage adjustment required.1


Cautions for Darifenacin Hydrobromide


Contraindications



  • Urinary retention, gastric retention, or uncontrolled angle-closure glaucoma or risk of these conditions.1




  • Known hypersensitivity to darifenacin or any ingredient in the formulation.1



Warnings/Precautions


Major Toxicities


GU Effects

Severe acute urinary retention requiring treatment reported in some patients receiving higher than recommended dosages (e.g., 30 mg daily) and in patients with detrusor hyperreflexia secondary to a stroke, benign prostatic hypertrophy, or irritable bowel syndrome.1 Acute urinary retention requiring bladder catheterization for 1–2 days also reported at therapeutic dosages.1


Use with caution in patients with clinically important bladder outflow obstruction.1


General Precautions


Decreased GI Motility

May decrease GI motility; use with caution in patients with severe constipation, ulcerative colitis, or myasthenia gravis.1 Severe constipation reported.1


Risk of gastric retention; use with caution in patients with obstructive GI disorders.1


Controlled Angle-closure Glaucoma

In patients being treated for angle-closure glaucoma, use only if potential benefits outweigh risks.1 (See Contraindications under Cautions.)


Specific Populations


Pregnancy

Category C.1


Lactation

Distributed into milk in rats; not known whether distributed into human milk.1 Use caution.1


Pediatric Use

Safety and efficacy not established in pediatric patients.1


Geriatric Use

No substantial differences in safety and efficacy relative to younger adults.1 (See Geriatric Patients under Dosage and Administration and see Elimination: Special Populations, under Pharmacokinetics.)


Hepatic Impairment

Use not evaluated and not recommended in patients with severe hepatic impairment (Child-Pugh class C).1 (See Hepatic Impairment under Dosage and Administration and see Distribution: Special Populations, under Pharmacokinetics.)


Common Adverse Effects


Dry mouth, constipation.1


Interactions for Darifenacin Hydrobromide


Metabolized principally by CYP2D6 and CYP3A4.1 May inhibit CYP2D6 and CYP3A4; not expected to inhibit CYP1A2 and CYP2C9.1


Drugs Affecting Hepatic Microsomal Enzymes


Inhibitors of CYP3A4: Potential pharmacokinetic interaction (increased plasma darifenacin concentrations).1 7 Do not exceed 7.5 mg daily when used concomitantly with potent inhibitors of CYP3A4.1 No dosage adjustment required when used concomitantly with moderate CYP3A4 inhibitors.1 (See Specific Drugs under Interactions.)


Inhibitors of CYP2D6: Potential pharmacokinetic interaction (increased plasma darifenacin concentrations).1 However, no dosage adjustment required.1


Mixed inhibitors of CYP isoenzymes: Potential pharmacokinetic interaction (increased plasma darifenacin concentrations).1 However, no dosage adjustment required.8


Inducers of CYP3A4: Potential pharmacokinetic interaction1 (altered plasma darifenacin concentrations).1 8


Drugs Metabolized by Hepatic Microsomal Enzymes


Substrates of CYP3A4: Potential pharmacokinetic interaction (increased plasma substrate concentrations).1


Substrates of CYP2D6: Potential pharmacokinetic interaction (increased plasma substrate concentrations).1 Caution advised when used concomitantly with CYP2D6 substrates that have a narrow therapeutic index.1


Substrates of CYP1A2 or CYP2C9: Pharmacokinetic interaction not expected at therapeutic dosages.8


Drugs Affected by GI Motility


Potential pharmacokinetic interaction (altered absorption because of decreased GI motility).1 (See Decreased GI Motility under Cautions.)


Specific Drugs





































































Drug



Interaction



Comments



Anticholinergic agents



Possible additive anticholinergic effects (e.g., decreased GI motility; altered absorption of other drugs)1



Antidepressants, tricyclics



Possible increased concentrations of tricyclic antidepressant1



Use concomitantly with caution1



Cimetidine



Increased plasma darifenacin concentrations1



No dosage adjustment required1



Clarithromycin



Possible increased plasma darifenacin concentrations1



Do not exceed a darifenacin dosage of 7.5 mg daily1



Digoxin



Increased digoxin exposure1



Continue routine monitoring of digoxin therapy1



Diltiazem



Possible increased plasma darifenacin concentrations1



No dosage adjustment required1



Erythromycin



Increased plasma darifenacin concentrations1



No dosage adjustment required1



Flecainide



Possible increased flecainide concentrations1



Use concomitantly with caution1



Fluconazole



Increased plasma darifenacin concentrations1



No dosage adjustment required1



Hormonal contraceptives



Pharmacokinetic interaction unlikely with oral contraceptives containing ethinyl estradiol and levonorgestrel1



Imipramine



Increased plasma concentrations of imipramine and desipramine1



Itraconazole



Possible increased plasma darifenacin concentrations1



Do not exceed a darifenacin dosage of 7.5 mg daily1



Ketoconazole



Increased plasma darifenacin concentrations1



Do not exceed a darifenacin dosage of 7.5 mg daily1



Midazolam



Increased midazolam concentrations1



Nefazodone



Possible increased plasma darifenacin concentrations1



Do not exceed a darifenacin dosage of 7.5 mg daily1



Nelfinavir



Possible increased plasma darifenacin concentrations1



Do not exceed a darifenacin dosage of 7.5 mg daily1



Paroxetine



Increased plasma darifenacin concentrations1



No dosage adjustment required1



Ritonavir



Possible increased plasma darifenacin concentrations1



Do not exceed a darifenacin dosage of 7.5 mg daily1



Thioridazine



Possible increased thioridazine concentrations1



Use concomitantly with caution1



Verapamil



Possible increased plasma darifenacin concentrations1



No dosage adjustment required1



Warfarin



No substantial effect on PT1



Continue routine monitoring of PT1


Darifenacin Hydrobromide Pharmacokinetics


Absorption


Bioavailability


Mean oral bioavailability at steady-state is approximately 15 or 19% for the 7.5- or 15-mg tablets, respectively.1 7


Peak plasma concentrations achieved approximately 7 hours after multiple dosing.1


Onset


Symptomatic improvement (i.e., reduction in number of urge incontinence episodes) observed within first 2 weeks of therapy.1 6


Food


Food does not affect darifenacin pharmacokinetics.1


Special Populations


Darifenacin exposure is 40 or 90% higher in CYP2D6 heterozygote-extensive metabolizers or poor metabolizers, respectively, and 56% lower in Japanese males.7


Distribution


Extent


Distributed into milk in rats; not known whether distributed into human milk.1


Plasma Protein Binding


Approximately 98% (mainly to α1-acid glycoprotein).1


Special Populations


In patients with moderate hepatic impairment (Child-Pugh class B), decreased protein binding resulting in increased darifenacin exposure observed.1 (See Hepatic Impairment under Dosage and Administration.)


Elimination


Metabolism


Extensively metabolized in the liver, mainly via CYP2D6 and CYP3A4.1


Elimination Route


Excreted in urine (60%) and in feces (40%); unchanged drug accounts for about 3% of recovered radioactivity.1


Half-life


Approximately 13–19 hours following long-term administration.1


Special Populations


In patients with poor metabolizer CYP2D6 phenotypes (approximately 7% of Caucasians and 2% of African Americans), darifenacin is metabolized principally via CYP3A4; decreased clearance observed.1 7 Steady-state plasma concentrations following 15-mg daily dosage approximately 1.7–1.9 times higher in poor metabolizers than in extensive metabolizers.1


In geriatric patients, possible decreased clearance (decreases about 6% per decade beginning at 44 years of age).1


In patients with renal impairment, no clear relationship between extent of impairment and darifenacin clearance observed in patients with Clcr 10–136 mL/minute.1 (See Renal Impairment under Dosage and Administration.)


Stability


Storage


Oral


Extended-release Tablets

25°C (may be exposed to 15–30°C).1 Protect from light.1


ActionsActions



  • Potent and selective antimuscarinic agent.1




  • Inhibits binding of acetylcholine to muscarinic receptors in cholinergically innervated organs.8




  • Demonstrates substantially greater binding affinity for muscarinic M3 receptors (which are involved in contraction of detrusor muscle of bladder and GI smooth muscle, saliva production, and iris sphincter function) in vitro than for other muscarinic receptor subtypes.1 3 8 Exhibits functional selectivity for urinary bladder over secretory (e.g., salivary) glands.2 3




  • Increases bladder capacity and diminishes frequency of unstable contractions of detrusor muscle in patients with involuntary detrusor contractions.1



Advice to Patients



  • Risk of constipation, urinary retention, blurred vision, and heat prostration (when used in a hot environment).1 4 Use caution when driving or performing dangerous activities until effects on vision are known.4




  • Importance of taking tablets with liquids and swallowing whole; do not chew, divide, or crush.1 4 If a dose is skipped, resume therapy the next day; do not take 2 doses in the same day.4




  • Importance of reading manufacturer’s patient information leaflet before initiating therapy.1




  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1




  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.1




  • Importance of advising patients of other important precautionary information.1 (See Cautions.)



Preparations


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.


















Darifenacin Hydrobromide

Routes



Dosage Forms



Strengths



Brand Names



Manufacturer



Oral



Tablets, extended-release



7.5 mg (of darifenacin)



Enablex



Novartis



15 mg (of darifenacin)



Enablex



Novartis


Comparative Pricing


This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.


Enablex 15MG 24-hr Tablets (WARNER CHILCOTT PROF PROD DIV): 30/$152.38 or 90/$435.37


Enablex 7.5MG 24-hr Tablets (WARNER CHILCOTT PROF PROD DIV): 30/$146.34 or 90/$420.87



Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.


The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions June 2005. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.




References



1. Novartis. Enablex (darifenacin hydrobromide) extended-release tablets prescribing information. East Hanover, NJ; 2004 Dec.



2. Miyamae K, Yoshida M, Murakami S et al. Pharmacological effects of darifenacin on human isolated urinary bladder. Pharmacology. 2003; 69:205-11. [PubMed 14624061]



3. Croom KF, Keating GM. Darifenacin in the treatment of overactive bladder. Drugs Aging. 2004; 21:885-92. [PubMed 15493952]



4. Novartis. Enablex (darifenacin hydrobromide) extended-release tablets patient information. East Hanover, NJ; 2004 Dec.



5. Zinner N, Tuttle J, and Marks L. Efficacy and tolerability of darifenacin, a muscarinic M3 selective receptor antagonist, compared with oxybutynin in the treatment of patients with overactive bladder. Joint Meeting of the International Continence Society and the International Urogynecological Association. Paris: 2004. Abstract No. 378. From The International Continence Society website ()



6. Haab F, Stewart L, and Dwyer P. Darifenacin, an M3 selective receptor antagonist, is an effective and well-tolerated once-daily treatment for overactive bladder. Eur Urol. 2004; 45:420-9. [PubMed 15041104]



7. Kerbusch T, Wahlby U, Milligan PA et al. Population pharmacokinetic modeling of darifenacin and its hydroxylated metabolite using pooled data, incorporating saturable first-pass metabolism, CYP2D6 genotype and formulation-dependent bioavailability. Br J Clin Pharmacol. 2003; 56:639-52. [IDIS 508556] [PubMed 14616424]



8. Novartis, East Hanover, NJ: Personal communication.



9. Steers W, Corcos J, Foote J et al. An investigation of dose titration with darifenacin, an M3-selective receptor antagonist. BJU Int. 2005; 95:580-6. [PubMed 15705084]



More Darifenacin Hydrobromide resources


  • Darifenacin Hydrobromide Side Effects (in more detail)
  • Darifenacin Hydrobromide Dosage
  • Darifenacin Hydrobromide Use in Pregnancy & Breastfeeding
  • Darifenacin Hydrobromide Drug Interactions
  • Darifenacin Hydrobromide Support Group
  • 12 Reviews for Darifenacin Hydrobromide - Add your own review/rating


Compare Darifenacin Hydrobromide with other medications


  • Overactive Bladder
  • Urinary Incontinence

Saturday, April 4, 2009

Blephamide S.O.P. Ointment


Pronunciation: pred-NISS-oh-lone/sul-fa-SEE-ta-mide
Generic Name: Prednisolone/Sulfacetamide
Brand Name: Blephamide S.O.P.


Blephamide S.O.P. Ointment is used for:

Treating inflammation (swelling, warmth, redness, pain) of the eyes and eyelids when infection or risk of infection is present.


Blephamide S.O.P. Ointment is an antibacterial and corticosteroid combination. It works by reducing the itching, redness, and swelling of the eye. It also works to stop the growth of certain bacteria that cause eye infections.


Do NOT use Blephamide S.O.P. Ointment if:


  • you are allergic to any ingredient in Blephamide S.O.P. Ointment, to other corticosteroids (eg, dexamethasone), or to other sulfonamides (eg, acetazolamide, celecoxib, hydrochlorothiazide, glyburide, probenecid, sulfamethoxazole, valdecoxib, zonisamide)

  • you have a viral eye infection (eg, herpes simplex, vaccinia, chickenpox), tuberculosis eye infection, or fungal infection of the eye or eye structures

  • you have thinning of the cornea of the eye

Contact your doctor or health care provider right away if any of these apply to you.



Before using Blephamide S.O.P. Ointment:


Some medical conditions may interact with Blephamide S.O.P. Ointment. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:


  • if you are pregnant, planning to become pregnant, or are breast-feeding

  • if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement

  • if you have allergies to medicines, foods, or other substances

  • if you have thinning of the eye tissues (eg, cornea, sclera), other eye problems (eg, glaucoma, cataracts, nerve damage), severe dry eyes, or diabetes

  • if you have recently had cataract surgery

Some MEDICINES MAY INTERACT with Blephamide S.O.P. Ointment. Tell your health care provider if you are taking any other medicine, especially any of the following:


  • Silver-containing medicines (eg, silver nitrate) because the risk of side effects may be increased

This may not be a complete list of all interactions that may occur. Ask your health care provider if Blephamide S.O.P. Ointment may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.


How to use Blephamide S.O.P. Ointment:


Use Blephamide S.O.P. Ointment as directed by your doctor. Check the label on the medicine for exact dosing instructions.


  • Blephamide S.O.P. Ointment may be used around the eye or in the eye. To use Blephamide S.O.P. Ointment in the eye, first, wash your hands. Using your index finger, pull the lower eyelid away from your eye to form a pouch. Squeeze a thin strip of ointment into the pouch. After using Blephamide S.O.P. Ointment, gently close your eyes for 1 to 2 minutes. Wash your hands to remove any medicine that may be on them. Wipe the applicator tip with a clean, dry tissue.

  • To prevent germs from contaminating your medicine, do not touch the applicator tip to any surface, including the eye. Keep the container tightly closed.

  • To clear up your infection completely, use Blephamide S.O.P. Ointment for the full course of treatment. Keep using it even if you feel better in a few days.

  • Do not use Blephamide S.O.P. Ointment if it is dark brown or has darkened since you began using it. Contact your doctor or pharmacist if you have questions about whether you should use Blephamide S.O.P. Ointment.

  • Do not wear contact lenses while you are using Blephamide S.O.P. Ointment. Take care of your contact lenses as directed by the manufacturer. Check with your doctor before you use them.

  • If you miss a dose of Blephamide S.O.P. Ointment, use it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not use 2 doses at once.

Ask your health care provider any questions you may have about how to use Blephamide S.O.P. Ointment.



Important safety information:


  • Blephamide S.O.P. Ointment may cause blurred vision. These effects may be worse if you take it with alcohol or certain medicines. Use Blephamide S.O.P. Ointment with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.

  • If your symptoms do not get better within 2 days or if they get worse, check with your doctor.

  • Be sure to use Blephamide S.O.P. Ointment for the full course of treatment. If you do not, the medicine may not clear up your infection completely. The bacteria could also become less sensitive to this or other medicines. This could make the infection harder to treat in the future.

  • Long-term or repeated use of Blephamide S.O.P. Ointment may cause a second infection. Tell your doctor if signs of a second infection occur. Your medicine may need to be changed to treat this.

  • Tell your doctor or dentist that you take Blephamide S.O.P. Ointment before you receive any medical or dental care, emergency care, or surgery.

  • Do not use Blephamide S.O.P. Ointment for future eye problems unless directed by your doctor.

  • Lab tests, including eye pressure, may be performed while you use Blephamide S.O.P. Ointment. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.

  • Blephamide S.O.P. Ointment should be used with extreme caution in CHILDREN younger than 6 years old; safety and effectiveness in these children have not been confirmed.

  • PREGNANCY and BREAST-FEEDING: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Blephamide S.O.P. Ointment while you are pregnant. It is not known if Blephamide S.O.P. Ointment is found in breast milk. Do not breast-feed while using Blephamide S.O.P. Ointment.


Possible side effects of Blephamide S.O.P. Ointment:


All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:



Temporary burning or stinging.



Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); changes in vision; eye pain, itching, redness, swelling, irritation, or sores not present when you began using Blephamide S.O.P. Ointment; fever, chills, or sore throat; red, swollen, or blistered skin; severe or persistent blurred vision; unusual tiredness or weakness; yellowing of the eyes or skin.



This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.


See also: Blephamide S.O.P. side effects (in more detail)


If OVERDOSE is suspected:


Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately.


Proper storage of Blephamide S.O.P. Ointment:

Store Blephamide S.O.P. Ointment at room temperature, between 59 and 77 degrees F (15 and 25 degrees C). Do not freeze. Store away from heat and light. Keep Blephamide S.O.P. Ointment out of the reach of children and away from pets.


General information:


  • If you have any questions about Blephamide S.O.P. Ointment, please talk with your doctor, pharmacist, or other health care provider.

  • Blephamide S.O.P. Ointment is to be used only by the patient for whom it is prescribed. Do not share it with other people.

  • If your symptoms do not improve or if they become worse, check with your doctor.

  • Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Blephamide S.O.P. Ointment. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.



Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Blephamide S.O.P. resources


  • Blephamide S.O.P. Side Effects (in more detail)
  • Blephamide S.O.P. Use in Pregnancy & Breastfeeding
  • Blephamide S.O.P. Drug Interactions
  • Blephamide S.O.P. Support Group
  • 0 Reviews for Blephamide S.O.P. - Add your own review/rating


Compare Blephamide S.O.P. with other medications


  • Blepharitis
  • Conjunctivitis, Bacterial
  • Keratitis
  • Keratoconjunctivitis
  • Uveitis

Friday, April 3, 2009

Divigel Transdermal


Generic Name: estradiol (Transdermal route)

es-tra-DYE-ol

Transdermal route(Emulsion)

Estrogens increase the risk of endometrial cancer; monitor for abnormal vaginal bleeding. Estrogens with or without progestins should not be used for the prevention of cardiovascular disease or dementia. Increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50 to 79 years of age) have been reported. An increased risk of developing probable dementia in postmenopausal women 65 years of age or older has also been reported. Risks should be assumed to be similar for other doses, combinations, and dosage forms of estrogens and progestins. Estrogens, with or without progestins, should be prescribed at the lowest effective doses and for the shortest duration possible .


Transdermal route(Patch, Extended Release)

Estrogens increase the risk of endometrial cancer; monitor for abnormal vaginal bleeding. Estrogens with or without progestins should not be used for the prevention of cardiovascular disease or dementia. Increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50 to 79 years of age) have been reported. An increased risk of developing probable dementia in postmenopausal women 65 years of age or older has also been reported. Risks should be assumed to be similar for other doses, combinations, and dosage forms of estrogens and progestins. Estrogens, with or without progestins, should be prescribed at the lowest effective doses and for the shortest duration possible.


Transdermal route(Gel/Jelly)

Estrogens increase the risk of endometrial cancer; monitor for abnormal vaginal bleeding. Estrogens with or without progestins should not be used for the prevention of cardiovascular disease. Increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50 to 79 years of age) have been reported. Risks should be assumed to be similar for other doses, combinations, and dosage forms of estrogens and progestins. Estrogens, with or without progestins, should be prescribed at the lowest effective doses and for the shortest duration possible .


Transdermal route(Spray)

Unopposed estrogens increase the risk of endometrial cancer. Adding a progestin will reduce the risk of endometrial hyperplasia, which may be a precursor to endometrial cancer. Diagnostic measures should be undertaken to rule out malignancy in postmenopausal women with undiagnosed persistent or recurring abnormal genital bleeding. Estrogens with or without progestins should not be used for the prevention of cardiovascular disease or dementia. Increased risks of stroke and deep vein thrombosis in postmenopausal women (50 to 79 years of age) using estrogen alone have been reported. Increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50 to 79 years of age) using estrogens combined with progestins have been reported. An increased risk of developing probable dementia in postmenopausal women 65 years of age or older has also been reported in women receiving estrogen alone or estrogen combined with progestins. Risks should be assumed to be similar for other doses, combinations, and dosage forms of estrogens and progestins. Estrogens, with or without progestins, should be prescribed at the lowest effective doses and for the shortest duration possible. Breast budding and breast masses in prepubertal females and gynecomastia and breast masses in prepubertal males have been reported following unintentional secondary exposure. Patients should strictly adhere to recommended instructions for use .



Commonly used brand name(s)

In the U.S.


  • Alora

  • Climara

  • Divigel

  • Elestrin

  • Esclim

  • Estraderm

  • Estrasorb

  • EstroGel

  • Evamist

  • Menostar

  • Vivelle

  • Vivelle-Dot

In Canada


  • Estradot Transdermal

  • Estradot Transdermal Therapeutic System

  • Estradot Transdermal Therapeutic System

  • Oesclim

  • Rhoxal-Estradiol Derm 50

  • Rhoxal-Estradiol Derm 75

  • Roxal-Estradiol Derm 100

  • Vivelle 100 Mcg

  • Vivelle 25 Mcg

  • Vivelle 37.5 Mcg

Available Dosage Forms:


  • Patch, Extended Release

  • Gel/Jelly

  • Spray

  • Emulsion

Therapeutic Class: Endocrine-Metabolic Agent


Pharmacologic Class: Estrogen


Uses For Divigel


Estradiol transdermal spray is used to treat moderate to severe hot flashes and other symptoms of menopause or low amounts of estrogen.


Estradiol is an estrogen hormone. The hormone from the spray is absorbed through your skin into your body. It works by preventing symptoms, such as feelings of warmth in the face, neck, and chest, or sudden strong feelings of heat and sweating ("hot flashes") in women during menopause.


This medicine is available only with your doctor's prescription.


Before Using Divigel


In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:


Allergies


Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.


Pediatric


Use of estradiol transdermal spray is not indicated in the pediatric population. Safety and efficacy have not been established.


Geriatric


Although appropriate studies on the relationship of age to the effects of estradiol transdermal spray have not been performed in the geriatric population, no geriatric-specific problems have been documented to date. However, elderly patients are more likely to have breast cancer, stroke, or dementia, which may require caution in patients receiving estradiol transdermal spray.


Pregnancy








Pregnancy CategoryExplanation
All TrimestersXStudies in animals or pregnant women have demonstrated positive evidence of fetal abnormalities. This drug should not be used in women who are or may become pregnant because the risk clearly outweighs any possible benefit.

Breast Feeding


Studies suggest that this medication may alter milk production or composition. If an alternative to this medication is not prescribed, you should monitor the infant for side effects and adequate milk intake.


Interactions with Medicines


Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are receiving this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.


Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.


  • Isotretinoin

  • Theophylline

  • Tizanidine

  • Tranexamic Acid

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.


  • Alprazolam

  • Amoxicillin

  • Ampicillin

  • Amprenavir

  • Aprepitant

  • Atazanavir

  • Bacampicillin

  • Betamethasone

  • Bexarotene

  • Bosentan

  • Carbamazepine

  • Clarithromycin

  • Colesevelam

  • Cyclosporine

  • Darunavir

  • Delavirdine

  • Doxycycline

  • Efavirenz

  • Etravirine

  • Fosamprenavir

  • Fosaprepitant

  • Fosphenytoin

  • Ginseng

  • Griseofulvin

  • Itraconazole

  • Ketoconazole

  • Lamotrigine

  • Levothyroxine

  • Licorice

  • Minocycline

  • Modafinil

  • Mycophenolate Mofetil

  • Mycophenolic Acid

  • Nelfinavir

  • Nevirapine

  • Oxcarbazepine

  • Oxytetracycline

  • Phenobarbital

  • Phenytoin

  • Pioglitazone

  • Prednisolone

  • Primidone

  • Rifabutin

  • Rifampin

  • Rifapentine

  • Ritonavir

  • Rosuvastatin

  • Rufinamide

  • Selegiline

  • St John's Wort

  • Tacrine

  • Telaprevir

  • Tetracycline

  • Tipranavir

  • Topiramate

  • Troglitazone

  • Troleandomycin

  • Voriconazole

  • Warfarin

Interactions with Food/Tobacco/Alcohol


Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.


Using this medicine with any of the following may cause an increased risk of certain side effects but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.


  • Caffeine

  • Grapefruit Juice

Other Medical Problems


The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:


  • Abnormal or unusual vaginal bleeding or

  • Blood clots (e.g., deep vein thrombosis, pulmonary embolism), active or history of or

  • Breast cancer, known or suspected, or a history of or

  • Heart attack, active or recent (within the past 12 months) or

  • Liver disease or

  • Stroke, active or recent (within the past 12 months) or

  • Surgery with a long period of inactivity or

  • Tumors (estrogen-dependent), known or suspected—Should not be used in patients with these conditions.

  • Asthma or

  • Cancer, history of or

  • Diabetes or

  • Edema (fluid retention or body swelling) or

  • Endometriosis or

  • Epilepsy (seizures) or

  • Gallbladder disease or

  • Heart disease or

  • Hypercalcemia (high calcium in the blood) or

  • Hypertension (high blood pressure) or

  • Hypertriglyceridemia (high triglycerides or fats in the blood) or

  • Hypocalcemia (low calcium in the blood), severe or

  • Hypothyroidism (an underactive thyroid) or

  • Jaundice during pregnancy or from using hormonal therapy in the past or

  • Liver tumors or

  • Migraine headache or

  • Porphyria (an enzyme problem) or

  • Systemic lupus erythematosus (SLE)—Use with caution. May make these conditions worse.

Proper Use of estradiol

This section provides information on the proper use of a number of products that contain estradiol. It may not be specific to Divigel. Please read with care.


It is very important that you use this medicine only as directed by your doctor. Do not use more of it, do not use it more often, and do not use it for a longer time than your doctor ordered. To do so may cause unwanted side effects.


This medicine is for use on the skin only. Do not get it in your eyes, nose, mouth, breast, or vagina. Do not use it on skin areas that have cuts, scrapes, or burns. If it does get on these areas, rinse it off right away with water.


This medicine comes with a patient information insert. Read and follow the instructions in the insert carefully. Ask your doctor if you have any questions.


Wash your hands with soap and water before and after using this medicine.


To use the spray:


  • The spray form of this medicine comes in an applicator that delivers a measured amount of estradiol to the skin with each spray. When using a new spray applicator, prime the pump by holding the spray upright and pumping 3 times. Priming is only necessary the first time you use a new spray applicator; do not prime again.

  • Apply the medicine to clean, dry, and unbroken skin on the inside of the forearm between the elbow and the wrist. Do not apply the medicine directly to your breasts or in or around the vagina.

  • Allow the medicine to dry for at least 2 minutes before dressing, and at least 1 hour before washing.

  • If your doctor tells you to increase your dose, move the applicator to an area of the skin next to your previous application site, before applying the second or third spray.

  • Do not rub Evamist® spray into your skin.

  • Do not allow your child to touch the area of the arm where the medicine was sprayed. If you cannot avoid being close with your child, wear clothes with long sleeves to cover the application site.

  • If your child comes in direct contact with the arm where the medicine was sprayed, wash your child's skin right away with soap and water.

  • Do not allow your pets to lick or touch the arm where the medicine was sprayed.

  • Always place the protective cover back on the applicator of the spray.

  • Do not use the applicator for more than 75 sprays.

  • Apply sunscreen at least 1 hour before applying Evamist®.

The spray contains alcohol and is flammable. Avoid using it near an open flame or while smoking.


Dosing


The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.


The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.


  • For transdermal dosage form (spray):
    • For hot flashes and other symptoms caused by menopause:
      • Adults—At first, one spray once a day, usually in the morning. Your doctor may adjust your dose as needed.

      • Children—Use is not recommended.



Missed Dose


If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.


Do not use Evamist® spray if it has been more than 12 hours since you missed your last dose.


Storage


Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.


Keep out of the reach of children.


Do not keep outdated medicine or medicine no longer needed.


Ask your healthcare professional how you should dispose of any medicine you do not use.


Precautions While Using Divigel


It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly and does not cause unwanted effects. Pelvic exam, breast exam, and mammogram (breast x-ray) may be needed to check for unwanted effects, unless your doctor tells you otherwise.


It is unlikely that a postmenopausal woman may become pregnant. But, you should know that using this medicine while you are pregnant could harm your unborn baby. If you think you have become pregnant while using the medicine, tell your doctor right away.


Using large doses of this medicine over a long period of time may increase your risk of heart attack, stroke, blood clots, dementia, breast cancer, or uterine cancer. Talk with your doctor about this risk. If you still have your uterus (womb), ask your doctor if you should also use a progestin medicine.


Your risk of heart disease or stroke from this medicine is higher if you smoke. Your risk is also increased if you have diabetes or high cholesterol, or if you are overweight. Talk with your doctor about ways to stop smoking. Keep your diabetes under control. Ask your doctor about diet and exercise to control your weight and blood cholesterol level.


Tell the medical doctor or dentist in charge that you are using this medicine before any kind of surgery (including dental surgery) or emergency treatment. Your doctor will decide whether you should continue using this medicine.


This medicine may also increase your risk of certain types of cancer. Talk to your doctor if you have concerns about this risk.


Using this medicine alone may increase your risk of getting cancer of the uterus (womb). Check with your doctor right away if you have unusual vaginal bleeding while you are using this medicine.


Stop using this medicine and check with your doctor immediately if severe headache or sudden loss of vision or any other change in vision occurs while you are using this medicine. Your doctor may want you to have your eyes checked by an ophthalmologist (eye doctor).


Check with your child's doctor right away if your child starts to have the following symptoms: nipple or breast swelling or tenderness in females, or enlargement of the breasts in males. Your child may have been exposed to this medicine.


Do not allow your pets to lick or touch the arm where this medicine was applied. Small pets may be sensitive to this medicine. Call your pet's veterinarian if your pet starts to have the following symptoms: nipple or breast enlargement, swelling of the vulva, or any signs of illness.


Before you have any medical tests, tell the medical doctor in charge that you are taking this medicine. The results of some tests may be affected by this medicine.


Do not take other medicines or drink grapefruit juice unless you discuss it with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal (e.g., St. John's wort) or vitamin supplements.


Divigel Side Effects


Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.


Check with your doctor immediately if any of the following side effects occur:


Incidence not known
  • Abdominal or stomach cramps or pain

  • acid or sour stomach

  • anxiety

  • backache

  • belching

  • blistering, peeling, or loosening of the skin

  • bloating

  • blurred vision

  • breast tenderness, enlargement, pain, or discharge

  • change in vaginal discharge

  • changes in skin color

  • changes in vision

  • chest pain or discomfort

  • chills

  • clay-colored stools

  • clear or bloody discharge from the nipple

  • confusion

  • constipation

  • convulsions

  • cough

  • darkening of the urine

  • diarrhea

  • difficulty with breathing

  • difficulty with swallowing

  • dimpling of the breast skin

  • dizziness or lightheadedness

  • double vision

  • fainting

  • fast heartbeat

  • fever

  • fluid-filled skin blisters

  • full or bloated feeling or pressure in the stomach

  • headache

  • headache, severe and throbbing

  • heartburn

  • hives

  • indigestion

  • inverted nipple

  • irregular heartbeats

  • itching of the skin

  • itching of the vagina or genital area

  • joint or muscle pain

  • large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs

  • light-colored stools

  • loss of appetite

  • loss of bladder control

  • lump in the breast or under the arm

  • migraine headache

  • mood or mental changes

  • muscle cramps in the hands, arms, feet, legs, or face

  • muscle spasm or jerking of all extremities

  • nausea

  • noisy breathing

  • numbness and tingling around the mouth, fingertips, or feet

  • pain during sexual intercourse

  • pain in the ankles or knees

  • pain or discomfort in the arms, jaw, back, or neck

  • pain or feeling of pressure in the pelvis

  • pain, redness, or swelling in the arm, foot, or leg

  • painful, red lumps under the skin, mostly on the legs

  • pains in the stomach, side, or abdomen, possibly radiating to the back

  • persistent crusting or scaling of the nipple

  • poor insight and judgment

  • problems with memory or speech

  • puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue

  • rash

  • red, irritated eyes

  • redness or swelling of the breast

  • sensitivity to the sun

  • shortness of breath

  • skin thinness

  • sore on the skin of the breast that does not heal

  • sore throat

  • sores, ulcers, or white spots in the mouth or on the lips

  • stomach discomfort, upset, or pain

  • sudden loss of consciousness

  • sudden shortness of breath or troubled breathing

  • sweating

  • swelling

  • swelling of the abdominal or stomach area

  • thick, white vaginal discharge with no odor or with a mild odor

  • tightness in the chest

  • tremor

  • trouble recognizing objects

  • trouble thinking and planning

  • trouble walking

  • unexpected or excess milk flow from the breasts

  • unpleasant breath odor

  • unusual tiredness or weakness

  • unusually heavy or unexpected menstrual bleeding

  • vaginal bleeding or spotting

  • vomiting

  • vomiting of blood

  • wheezing

  • yellow eyes or skin

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:


Less common
  • Back pain

  • difficulty with moving

  • muscle aches

  • muscle pain or stiffness

  • stuffy or runny nose

Incidence not known
  • Decreased interest in sexual intercourse

  • heavy bleeding

  • hives or welts

  • inability to have or keep an erection

  • increased hair growth, especially on the face

  • increased in sexual ability, desire, drive, or performance

  • increased interest in sexual intercourse

  • irritability

  • leg cramps

  • loss in sexual ability, desire, drive, or performance

  • loss of scalp hair

  • mental depression

  • mood disturbances

  • patchy brown or dark brown discoloration of the skin

  • redness of the skin

  • twitching, uncontrolled movements of the tongue, lips, face, arms, or legs

  • weight changes

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.


Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.



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