Friday, 28 September 2012

H-C Tussive


Generic Name: chlorpheniramine, hydrocodone, and phenylephrine (KLOR fe NEER a meen, HYE droe KOE done, FEN il EFF rin)

Brand Names: B-Tuss, Coughtuss, Cytuss HC, De-Chlor HC, DroTuss-CP, Ed-TLC, Ed-Tuss HC, Endal-HD Plus, H-C Tussive, Histussin-HC, Hydro-PC II, Hydro-PC II Plus, Hydron CP, Liquicough HC, Maxi-Tuss HCX, Mintuss MS, Neo HC, Poly-Tussin, Poly-Tussin HD, Relacon-HC, Relacon-HC NR, Relasin-HC, Rindal HD Plus, Rindal-HD, Triant-HC, Tusana-D, Z-Cof HC


What is H-C Tussive (chlorpheniramine, hydrocodone, and phenylephrine)?

Chlorpheniramine is an antihistamine that reduces the natural chemical histamine in the body. Histamine can produce symptoms of sneezing, itching, watery eyes, and runny nose.


Hydrocodone is a narcotic cough medicine.


Phenylephrine is a decongestant that shrinks blood vessels in the nasal passages. Dilated blood vessels can cause nasal congestion (stuffy nose).


The combination of chlorpheniramine, hydrocodone, and phenylephrine is used to treat runny or stuffy nose, sinus congestion, and cough caused by the common cold or flu.


Chlorpheniramine, hydrocodone, and phenylephrine may also be used for purposes not listed in this medication guide.


What is the most important information I should know about H-C Tussive (chlorpheniramine, hydrocodone, and phenylephrine)?


Do not take this medication if you have used an MAO inhibitor such as furazolidone (Furoxone), isocarboxazid (Marplan), phenelzine (Nardil), rasagiline (Azilect), selegiline (Eldepryl, Emsam, Zelapar), or tranylcypromine (Parnate) in the last 14 days. Serious, life threatening side effects can occur if you use chlorpheniramine, hydrocodone, and phenylephrine before the MAO inhibitor has cleared from your body. Chlorpheniramine, hydrocodone, and phenylephrine may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert. Drinking alcohol can increase certain side effects of chlorpheniramine, hydrocodone, and phenylephrine. Before using this medication, tell your doctor if you regularly use other medicines that make you sleepy (such as cold or allergy medicine, sedatives, narcotic pain medicine, sleeping pills, muscle relaxers, and medicine for seizures, depression, or anxiety). They can add to sleepiness caused by chlorpheniramine, hydrocodone, and phenylephrine. Hydrocodone may be habit-forming and should be used only by the person it was prescribed for. Never share hydrocodone with another person, especially someone with a history of drug abuse or addiction. Keep the medication in a place where others cannot get to it.

What should I discuss with my healthcare provider before taking H-C Tussive (chlorpheniramine, hydrocodone, and phenylephrine)?


Do not take this medication if you have used an MAO inhibitor such as furazolidone (Furoxone), isocarboxazid (Marplan), phenelzine (Nardil), rasagiline (Azilect), selegiline (Eldepryl, Emsam, Zelapar), or tranylcypromine (Parnate) in the last 14 days. Serious, life threatening side effects can occur if you use chlorpheniramine, hydrocodone, and phenylephrine before the MAO inhibitor has cleared from your body. You should not use chlorpheniramine, hydrocodone, and phenylephrine if you are allergic to it.

To make sure you can safely take this medication, tell your doctor if you have any of these other conditions:



  • asthma, COPD, sleep apnea, or other breathing disorder;



  • liver or kidney disease;


  • heart disease or high blood pressure;




  • diabetes;




  • a thyroid disorder;




  • curvature of the spine;




  • a history of head injury or brain tumor;




  • epilepsy or other seizure disorder;




  • low blood pressure;




  • glaucoma;




  • gallbladder disease;




  • Addison's disease or other adrenal gland disorders;




  • enlarged prostate, urination problems;




  • mental illness; or




  • a history of drug or alcohol addiction.




Hydrocodone may be habit-forming and should be used only by the person it was prescribed for. Never share hydrocodone with another person, especially someone with a history of drug abuse or addiction. Keep the medication in a place where others cannot get to it. FDA pregnancy category C. It is not known whether chlorpheniramine, hydrocodone, and phenylephrine will harm an unborn baby. Hydrocodone may cause addiction or withdrawal symptoms in a newborn if the mother takes the medication during pregnancy. Tell your doctor if you are pregnant or plan to become pregnant while using chlorpheniramine, hydrocodone, and phenylephrine. It is not known whether chlorpheniramine, hydrocodone, and phenylephrine passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

How should I take H-C Tussive (chlorpheniramine, hydrocodone, and phenylephrine)?


Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.


You may take this medication with or without food.


Measure liquid medicine with a special dose-measuring spoon or cup, not a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.


Store at room temperature away from moisture and heat. Keep track of the amount of medicine used from each new bottle. Hydrocodone is a drug of abuse and you should be aware if anyone is using your medicine improperly or without a prescription.

What happens if I miss a dose?


Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.


What happens if I overdose?


Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. An overdose of hydrocodone can be fatal.

Overdose symptoms may include extreme drowsiness, feeling restless or nervous, vomiting, stomach pain, warmth or tingly feeling, seizure (convulsions), pinpoint pupils, confusion, cold and clammy skin, weak pulse, shallow breathing, fainting, or breathing that stops.


What should I avoid while taking H-C Tussive (chlorpheniramine, hydrocodone, and phenylephrine)?


Chlorpheniramine, hydrocodone, and phenylephrine may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert. Drinking alcohol can increase certain side effects of chlorpheniramine, hydrocodone, and phenylephrine.

H-C Tussive (chlorpheniramine, hydrocodone, and phenylephrine) side effects


Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using this medication and call your doctor at once if you have a serious side effect such as:

  • severe dizziness, anxiety, restless feeling, or nervousness;




  • fast, pounding, or uneven heartbeats;




  • shallow breathing, slow heartbeat;




  • confusion, hallucinations, unusual thoughts or behavior;




  • feeling like you might pass out;




  • urinating less than usual or not at all;




  • easy bruising or bleeding, unusual weakness, fever, chills, body aches, flu symptoms;




  • dangerously high blood pressure (severe headache, blurred vision, buzzing in your ears, chest pain, shortness of breath, seizure); or




  • upper stomach pain, itching, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).



Less serious side effects may include:



  • nausea, vomiting, upset stomach, constipation;




  • dry mouth;




  • blurred vision;




  • dizziness, drowsiness;




  • problems with memory or concentration;




  • sleep problems (insomnia);




  • ringing in your ears;




  • warmth, tingling, or redness under your skin; or




  • skin rash or itching.



This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.


What other drugs will affect H-C Tussive (chlorpheniramine, hydrocodone, and phenylephrine)?


Before using this medication, tell your doctor if you regularly use other medicines that make you sleepy (such as cold or allergy medicine, sedatives, narcotic pain medicine, sleeping pills, muscle relaxers, and medicine for seizures, depression, or anxiety). They can add to sleepiness caused by chlorpheniramine, hydrocodone, and phenylephrine.

Tell your doctor about all other medications you use, especially:



  • blood pressure medication;




  • cimetidine (Tagamet);




  • rifampin (Rifadin, Rifater, Rifamate, Rimactane);




  • zidovudine (Retrovir, AZT);




  • an antidepressant;




  • a diuretic (water pill);




  • medication to treat irritable bowel syndrome;




  • bladder or urinary medications such as oxybutynin (Ditropan, Oxytrol) or tolterodine (Detrol);




  • aspirin or salicylates (such as Disalcid, Doan's Pills, Dolobid, Salflex, Tricosal, and others);




  • seizure medication such as phenytoin (Dilantin) or phenobarbital (Luminal, Solfoton);




  • a beta-blocker such as atenolol (Tenormin), carteolol (Cartrol), metoprolol (Lopressor, Toprol), nadolol (Corgard), propranolol (Inderal), sotalol (Betapace), timolol (Blocadren), and others; or




  • medicines to treat psychiatric disorders, such as chlorpromazine (Thorazine), haloperidol (Haldol), mesoridazine (Serentil), pimozide (Orap), or thioridazine (Mellaril).



This list is not complete and other drugs may interact with chlorpheniramine, hydrocodone, and phenylephrine. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.



More H-C Tussive resources


  • H-C Tussive Side Effects (in more detail)
  • H-C Tussive Use in Pregnancy & Breastfeeding
  • H-C Tussive Drug Interactions
  • H-C Tussive Support Group
  • 0 Reviews for H-C Tussive - Add your own review/rating


  • Chlorpheniramine/Hydrocodone/Phenylephrine Liquid MedFacts Consumer Leaflet (Wolters Kluwer)



Compare H-C Tussive with other medications


  • Cough and Nasal Congestion


Where can I get more information?


  • Your pharmacist can provide more information about chlorpheniramine, hydrocodone, and phenylephrine.

See also: H-C Tussive side effects (in more detail)


Thursday, 20 September 2012

Noroxin


Generic Name: Norfloxacin
Class: Quinolones
VA Class: AM900
Chemical Name: 1-Ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid
CAS Number: 70458-96-7



  • Fluoroquinolones, including norfloxacin, are associated with an increased risk of tendinitis and tendon rupture in all age groups.1 372 373 This risk is further increased in older adults (usually those >60 years of age), individuals receiving concomitant corticosteroids, and kidney, heart, or lung transplant recipients.1 372 373 (See Tendinopathy and Tendon Rupture under Cautions.)



REMS:


FDA approved a REMS for norfloxacin to ensure that the benefits of a drug outweigh the risks. The REMS may apply to one or more preparations of norfloxacin and consists of the following: medication guide. See the FDA REMS page () or the ASHP REMS Resource Center ().



Introduction

Antibacterial; fluoroquinolone.1 17 18 20


Uses for Noroxin


Urinary Tract Infections (UTIs) and Prostatitis


Treatment of uncomplicated UTIs (including cystitis) caused by susceptible Citrobacter freundii, Enterobacter aerogenes, E. cloacae, Escherichia coli, Klebsiella pneumoniae, Morganella morganii, Proteus mirabilis, P. vulgaris, Providencia rettgeri, Pseudomonas aeruginosa, or Serratia marcescens.1 107 114 115 116 117 118 123 124 127 128 129 134 135 201 230 231 280 283 309 Also used for treatment of uncomplicated UTIs caused by susceptible Staphylococcus aureus, S. epidermidis, S. saprophyticus, or Streptococcus agalactiae (group B streptococci), or Enterococcus faecalis.1 107 116 117 118 124 127 129 134 135 201 230 231


Treatment of complicated UTIs caused by susceptible E. coli, K. pneumoniae, P. mirabilis, Ps. aeruginosa, S. marcescens, or E. faecalis.1


Treatment of prostatitis caused by E. coli.1


Usually reserved for treatment of complicated UTIs, especially those caused by multidrug-resistant bacteria; generally not recommended for uncomplicated UTIs (e.g., acute cystitis) unless more commonly employed urinary anti-infectives are contraindicated or not tolerated.111 251 253


GI Infections


Treatment of gastroenteritis caused by susceptible enterotoxigenic E. coli,71 193 232 Aeromonas hydrophila,193 232 Plesiomonas shigelloides,71 Salmonella,71 193 232 or Shigella (including Sh. boydii,71 Sh. dysenteriae,36 71 131 193 Sh. flexneri,71 193 Sh. sonnei).71


Treatment of cholera, including infections caused by Vibrio cholerae serotypes 01 or 0139.310 311 341 344 Tetracyclines generally are drugs of choice when an anti-infective is indicated as an adjunct to fluid and electrolyte replacement;43 309 311 334 alternative agents for V. cholerae resistant to tetracyclines include co-trimoxazole, fluoroquinolones, or furazolidone.43 309 311 334 341


Treatment of travelers’ diarrhea.210 301 304 305 306 335 374 Replacement therapy with oral fluids and electrolytes may be sufficient for mild to moderate disease.210 304 305 335 Generally self-limited and may resolve within 3–4 days without anti-infective treatment;210 304 305 334 if diarrhea is moderate or severe, persists for >3 days, or is associated with fever or bloody stools, short-term (1–3 days) anti-infective treatment may be indicated.210 304 305 334 374 Fluoroquinolones (ciprofloxacin, levofloxacin, norfloxacin, ofloxacin) usually drugs of choice when treatment, including self-treatment, is indicated.304 305 312 335 337 374 Azithromycin is a treatment alternative for those who should not receive fluoroquinolones (e.g., children, pregnant women) and may be a drug of choice for travelers in areas with a high prevalence of fluoroquinolone-resistant Campylobacter (e.g., Thailand, India) or those who have not responded after 48 hours of fluoroquinolone treatment.304 305 334 374 Rifaximin is another alternative for treatment of travelers' diarrhea caused by noninvasive E. coli.304 305 374


Prevention of travelers’ diarrhea in individuals traveling for relatively short periods to areas where enterotoxigenic E. coli and other causative bacterial pathogens (e.g., Shigella) are known to be susceptible to the drug.109 131 193 301 304 307 308 335 337 374 CDC and others do not recommend anti-infective prophylaxis in most individuals traveling to areas of risk;210 304 305 308 312 334 374 the principal preventive measures are prudent dietary practices.210 304 329 330 If anti-infective prophylaxis is used (e.g., in immunocompromised individuals such as those with HIV infection), a fluoroquinolone (ciprofloxacin, levofloxacin, ofloxacin, norfloxacin) is recommended for nonpregnant adults,304 305 374 although the increasing incidence of quinolone resistance in pathogens that cause travelers' diarrhea (e.g., Campylobacter) should be considered.304 305


Gonorrhea and Associated Infections


Has been used for treatment of uncomplicated urethral, endocervical, or rectal gonorrhea caused by susceptible Neisseria gonorrhoeae.1 17 18 21 71 111 119 132 193 195 196 229 297 298 301 319


Although fluoroquinolones (ciprofloxacin, levofloxacin, ofloxacin) were previously considered drugs of choice for treatment of uncomplicated gonorrhea,319 358 CDC currently states that fluoroquinolones should not be used for treatment of gonorrhea or any associated infections involving N. gonorrhoeae (e.g., pelvic inflammatory disease [PID], epididymitis).328 358 359 360


Quinolone-resistant N. gonorrhoeae (QRNG) has been reported with increasing frequency worldwide and is widespread in the US.319 320 328 338 358 359 360 (See Resistance in Neisseria gonorrhoeae under Cautions.)


For treatment of uncomplicated cervical, urethral, or rectal gonorrhea, CDC and others recommend IM ceftriaxone or oral cefixime; IM ceftriaxone is drug of choice for pharyngeal infections.319 328 358 359


Noroxin Dosage and Administration


Administration


Oral Administration


Administer orally.1


Give tablets with a glass of water at least 1 hour before or at least 2 hours after a meal or dairy products (e.g., milk, yogurt).1 2 (See Pharmacokinetics.)


Patients receiving norfloxacin should be well hydrated and should be instructed to drink fluids liberally.1 240 (See Renal Effects under Cautions.)


Dosage


Adults


Urinary Tract Infections (UTIs) and Prostatitis

Uncomplicated UTIs

Oral

400 mg every 12 hours.1 17 114 116 117 118 124 127 128 201 205 Usual duration is 3 days for treatment of uncomplicated UTIs caused by susceptible E. coli, K. pneumoniae, or P. mirabilis or 7–10 days for treatment of uncomplicated UTIs caused by other susceptible bacteria.1


Complicated UTIs

Oral

400 mg every 12 hours.1 17 114 116 128 135 201 205 Usual duration is ≥10–21 days.1 17 135


Acute or Chronic Prostatitis Caused by E. coli

Oral

400 mg every 12 hours for 28 days.1


GI Infections

Gastroenteritis Caused by Susceptible Bacteria

Oral

400 mg twice daily for 5 days.36 71 131 193 A duration of 3 days may be sufficient for some infections, including shigellosis or some E. coli infections.43


Cholera

Oral

400 mg twice daily for 3 days in conjunction with fluid and electrolyte replacement.341 344 A single 800-mg dose has been used in adults, but there is some evidence that a multiple-dose regimen is more effective than a single-dose regimen for treatment of severe cholera caused by V. cholerae 0139.341


Treatment of Travelers’ Diarrhea

Oral

400 mg twice daily for 1–3 days.305 306 374


Prevention of Travelers’ Diarrhea

Oral

400 mg once daily.305 329 330 335 374


Although anti-infective prophylaxis generally is discouraged,210 304 305 308 312 334 337 374 some clinicians state that it can be given during the period of risk (for ≤3 weeks) beginning the day of travel and continuing for 1 or 2 days after leaving the area of risk.329 330 335 374


Gonorrhea

Uncomplicated Urethral, Endocervical, or Rectal Gonorrhea

Oral

A single 800-mg dose.1 319


Because of increased prevalence of quinolone-resistant Neisseria gonorrhoeae (QRNG), CDC no longer recommends fluoroquinolones for treatment of gonorrhea or any associated infections involving N. gonorrhoeae (e.g., PID, epididymitis).328 358 359 360 (See Gonorrhea and Associated Infections under Uses.)


Unless the presence of coexisting chlamydial infection has been excluded by appropriate testing, patients being treated for gonorrhea should also receive an anti-infective regimen effective for presumptive treatment of chlamydia (e.g., a single dose of oral azithromycin or a 7-day regimen of oral doxycycline).319


Prescribing Limits


Adults


Oral

Maximum 400 mg twice daily because of the risk of crystalluria.1


Special Populations


Renal Impairment


Dosage adjustments necessary in patients with severe renal impairment.1 2 7 8 17 143


Adults with Clcr ≤30 mL/minute per 1.73 m2 should receive 400 mg once daily.1


Geriatric Patients


No dosage adjustments except those related to renal impairment.1 (See Renal Impairment under Dosage and Administration.)


Select dosage with caution because of possible age-related decreases in renal impairment.1


Cautions for Noroxin


Contraindications



  • Hypersensitivity to norfloxacin or any quinolone.1 240




  • History of tendinitis or tendon rupture with norfloxacin or any quinolone.1



Warnings/Precautions


Warnings


Tendinopathy and Tendon Rupture

Fluoroquinolones, including norfloxacin, are associated with increased risk of tendinitis and tendon rupture in all age groups.1 372 373 This risk is further increased in older adults (usually those >60 years of age), individuals receiving concomitant corticosteroids, and kidney, heart, or lung transplant recipients.1 372 373


Other factors that may independently increase risk of tendon rupture include strenuous physical activity, renal failure, and previous tendon disorders such as rheumatoid arthritis.1 372 373 Tendinitis and tendon rupture have been reported in patients receiving fluoroquinolones who did not have any of these risk factors.1


Fluoroquinolone-associated tendinitis and tendon rupture most frequently involve the Achilles tendon and may require surgical repair.1 Tendinitis and tendon rupture in the rotator cuff (shoulder), hand, biceps, thumb, and other tendon sites also reported.1


Tendon rupture can occur during or following fluoroquinolone therapy and has been reported up to several months after completion of therapy.1


Discontinue if pain, swelling, inflammation, or rupture of a tendon occurs.1 372 373 Advise patients to rest and refrain from exercise and contact a clinician at the first sign of tendinitis or tendon rupture (e.g., pain, swelling, or inflammation of a tendon or weakness or inability to use a joint).1 372 373 (See Advice to Patients.)


Musculoskeletal Effects

Fluoroquinolones, including norfloxacin, cause arthropathy and osteochondrosis in immature animals of various species.1 2 233 240 362 363 364 365 366 369 370 Relevance of these adverse effects in immature animals to use in humans unknown.213 241 361 367 368 369 Safety and efficacy of norfloxacin not established in children and adolescents <18 years of age (see Pediatric Use under Cautions) or in pregnant or lactating women (see Pregnancy and see Lactation under Cautions).1


CNS Effects

Possibility of seizures, increased intracranial pressure, toxic psychoses, and CNS stimulation leading to tremors, restlessness, lightheadedness, confusion, and hallucinations.1 21 233 240 257 258


Use with caution in patients with known or suspected CNS disorders that may predispose to seizures or lower seizure threshold (e.g., severe cerebral arteriosclerosis, epilepsy).1


If a severe adverse CNS reaction (e.g., seizures, increased intracranial pressure, CNS stimulation, toxic psychosis) occurs, discontinue the drug and institute appropriate therapeutic measures.1


Peripheral Neuropathy

Sensory or sensorimotor axonal polyneuropathy affecting small and/or large axons resulting in paresthesias, hypoesthesias, dysesthesias, and weakness reported with quinolones, including norfloxacin.1


To prevent development of an irreversible condition, discontinue norfloxacin if symptoms of neuropathy (e.g., pain, burning, tingling, numbness, and/or weakness) occur or if there are deficits in light touch, pain, temperature, position sense, vibratory sensation, and/or motor strength.1


Superinfection/Clostridium difficile-associated Diarrhea and Colitis (CDAD)

Possible emergence and overgrowth of nonsusceptible bacteria or fungi.1 Institute appropriate therapy if superinfection occurs.1


Treatment with anti-infectives alters normal colon flora and may permit overgrowth of Clostridium difficile.1 345 346 347 348 349 354 C. difficile-associated diarrhea and colitis (CDAD; also known as antibiotic-associated diarrhea and colitis or pseudomembranous colitis) has been reported with nearly all anti-infectives, including norfloxacin, and may range in severity from mild diarrhea to fatal colitis.1 242 267 345 346 347 348 349 351 355 356 Outbreaks of severe CDAD caused by fluoroquinolone-resistant C. difficile have been reported with increasing frequency over the last several years.350 351 352 353 355 Hyper toxin-producing strains of C. difficile are associated with increased morbidity and mortality since they may be refractory to anti-infectives and colectomy may be required.1


Consider CDAD if diarrhea develops during or after therapy and manage accordingly.1 345 346 347 348 349 354 Careful medical history is necessary since CDAD has been reported to occur as late as 2 months or longer after anti-infective therapy is discontinued.1 345 346 347 348 349


If CDAD is suspected or confirmed, norfloxacin may need to be discontinued.1 345 346 347 348 349 Some mild cases may respond to discontinuance alone.345 346 347 348 349 Manage moderate to severe cases with fluid, electrolyte, and protein supplementation, appropriate anti-infective therapy active against C. difficile (e.g., oral metronidazole or vancomycin), and surgical evaluation when clinically indicated.1 345 346 347 348 349


Sensitivity Reactions


Hypersensitivity Reactions

Serious and occasionally fatal (anaphylactic) hypersensitivity reactions, which may occur following first dose, reported with some quinolones, including norfloxacin.1 193 293 294 295


Some reactions have been accompanied by cardiovascular collapse, loss of consciousness, tingling, pharyngeal or facial edema, dyspnea, urticaria, and itching.1 293 294 295


In addition, other possible severe and potentially fatal reactions (may be hypersensitivity reactions or of unknown etiology) have been reported, most frequently after multiple doses.1 These include fever, rash or other severe dermatologic reactions (e.g., toxic epidermal necrolysis, Stevens-Johnson syndrome), vasculitis, arthralgia, myalgia, serum sickness, allergic pneumonitis, interstitial nephritis, acute renal insufficiency or failure, hepatitis, jaundice, acute hepatic necrosis or failure, anemia (including hemolytic and aplastic), thrombocytopenia (including thrombotic thrombocytopenic purpura), leukopenia, agranulocytosis, pancytopenia, and/or other hematologic effects.1


Discontinue norfloxacin at first appearance of rash, jaundice, or any other sign of hypersensitivity and institute appropriate therapy as indicated (e.g., epinephrine, corticosteroids, and maintenance of an adequate airway and oxygen).1


Photosensitivity Reactions

Moderate to severe photosensitivity/phototoxicity reactions have been reported with fluoroquinolones, including norfloxacin.1


Phototoxicity may manifest as exaggerated sunburn reactions (e.g., burning, erythema, exudation, vesicles, blistering, edema) on areas exposed to sun or artificial ultraviolet (UV) light (usually the face, neck, extensor surfaces of forearms, dorsa of hands).1


Relative potential of the various fluoroquinolones to cause photosensitivity/phototoxicity unclear.292 Factors that contribute to susceptibility to this adverse effect during fluoroquinolone therapy include patient's skin pigmentation, frequency and duration of exposure to sun and UV light, use of protective clothing and sunscreen, concomitant use of other drugs, and dosage and duration of fluoroquinolone therapy.292


Avoid unnecessary or excessive exposure to sunlight or artificial UV light (tanning beds, UVA/UVB treatment) while receiving norfloxacin.1 If patient needs to be outdoors, they should wear loose-fitting clothing that protects skin from sun exposure and use other sun protection measures (sunscreen).1


Discontinue norfloxacin if photosensitivity or phototoxicity (sunburn-like reaction, skin eruption) occurs.1


General Precautions


Renal Effects

Possible crystalluria;1 2 21 71 138 193 generally associated with alkaline urine and high dosage.21 138 193 221


Adequate fluid intake necessary to ensure proper hydration and adequate urinary output;1 2 240 avoid alkaline urine and do not exceed usual dosage.1 2 240


Hematologic Effects

Hemolytic reactions reported rarely in patients with latent or actual defects in glucose-6-phosphate dehydrogenase (G-6-PD).1


Prolongation of QT Interval

Prolonged QT interval and ventricular arrhythmias (including torsades de pointes) reported with some fluoroquinolones, including norfloxacin.1


Avoid or use with caution in patients receiving class IA (e.g., quinidine, procainamide) or class III (e.g., amiodarone, sotalol) antiarrhythmic agents or other drugs that may affect QT interval (e.g., cisapride [available in the US only under a limited-access protocol], erythromycin, antipsychotic agents, tricyclic antidepressants) and in patients with risk factors for torsades de pointes (e.g., known QT prolongation, uncorrected hypokalemia).1


Myasthenia Gravis Patients

Possible exacerbation of signs of myasthenia gravis, which may lead to life-threatening weakness of respiratory muscles, reported with quinolones, including norfloxacin; use with caution in patients with myasthenia gravis.1


Laboratory Monitoring

Periodically assess organ system functions, including renal, hepatic, and hematopoietic, during prolonged therapy.1


Selection and Use of Anti-infectives

When prescribing a fluoroquinolone, consider potential benefits and risks for the individual patient.372 373 Most patients tolerate the drugs, but serious adverse reactions (e.g., CNS effects, QT prolongation, C. difficile-associated diarrhea and colitis, damage to liver, kidneys, or bone marrow, alterations in glucose homeostatis) may occur rarely.372 373


To reduce development of drug-resistant bacteria and maintain effectiveness of norfloxacin and other antibacterials, use only for treatment or prevention of infections proven or strongly suspected to be caused by susceptible bacteria.1


When selecting or modifying anti-infective therapy, use results of culture and in vitro susceptibility testing.1 In the absence of such data, consider local epidemiology and susceptibility patterns when selecting anti-infectives for empiric therapy.1


Resistance in Neisseria gonorrhoeae

N. gonorrhoeae with decreased susceptibility to norfloxacin and other fluoroquinolones (quinolone-resistant N. gonorrhoeae; QRNG) has been reported with increasing frequency over the past several years.319 320 322 323 324 325 326 327 328 336 358


Recent US data indicate that QRNG has continued to increase among men who have sex with men and among heterosexual males and is now present in all regions of the country.358


CDC states that fluoroquinolones should not be used to treat proven or suspected gonorrhea,328 358 359 360 including infections acquired within the US or acquired while traveling abroad.319


Specific Populations


Pregnancy

Category C.1


Lactation

Not known whether distributed into milk;1 other quinolones are distributed into milk.1 Discontinue nursing or the drug.1


Pediatric Use

Safety and efficacy not established in children and adolescents <18 years of age.1 Norfloxacin causes arthropathy in juvenile animals.1 233 (See Musculoskeletal Effects under Cautions.)


AAP states use of fluoroquinolones may be justified in children <18 years of age in special circumstances after careful assessment of the risks and benefits for the individual patient and after these benefits and risks have been explained to the parents or caregivers.334


Geriatric Use

No substantial differences in safety and efficacy relative to younger adults, but increased risk of some adverse effects cannot be ruled out.1


Risk of severe tendon disorders, including tendon rupture, is increased in geriatric adults >60 years of age.1 372 373 This risk is further increased in those receiving concomitant corticosteroids.1 372 373 (See Tendinopathy and Tendon Rupture under Cautions.) Use caution in geriatric adults, especially those receiving concomitant corticosteroids.1


Risk of QT interval prolongation leading to ventricular arrhythmias may be increased in geriatric patients, especially those receiving concurrent therapy with other drugs that can prolong QT interval (e.g., class IA or III antiarrhythmic agents) or with risk factors for torsades de pointes (e.g., known QT prolongation, uncorrected hypokalemia).1 (See Prolongation of QT Interval under Cautions.)


Substantially eliminated by the kidney and age-related decline in renal function may increase risk of adverse reactions.1


Consider age-related decreases in renal function when selecting dosage; renal function monitoring may be useful.1


Renal Impairment

Increased norfloxacin serum concentrations and prolonged half-life.1 17 18


Dosage adjustments necessary in patients with severe renal impairment.1 2 7 8 17 143 (See Renal Impairment under Dosage and Administration.)


Common Adverse Effects


GI effects (nausea, abdominal cramping);1 17 18 21 71 116 124 193 205 233 CNS effects (headache, dizziness, asthenia);1 17 18 21 71 116 124 193 205 233 rash.1


Interactions for Noroxin


Drugs Metabolized by Hepatic Microsomal Enzymes


Inhibits cytochrome P-450 (CYP) isoenzyme 1A2.1 Potential pharmacokinetic interaction with CYP1A2 substrates (e.g., caffeine, clozapine, ropinirole, tacrine, theophylline, tizanidine) resulting in increased drug concentrations if given in usual dosages.1 Carefully monitor patients receiving norfloxacin concomitantly with drugs metabolized by CYP1A2.1


Drugs that Prolong QT Interval


Potential pharmacologic interaction (additive effect on QT interval prolongation).1 Avoid or use with caution in patients receiving class IA (e.g., quinidine, procainamide) or class III (e.g., amiodarone, sotalol) antiarrhythmic agents or other drugs that may affect QT interval (e.g., cisapride, erythromycin, antipsychotic agents, tricyclic antidepressants).1 (See Prolongation of QT Interval under Cautions.)


Specific Drugs






















































Drug



Interaction



Comments



Aminoglycosides



In vitro evidence of additive or synergistic antibacterial effects against some Enterobacteriaceae and Ps. aeruginosa;150 155 177 synergism unpredictable and indifference or antagonism also has been reported48 155



Antacids (aluminum- or magnesium-containing)



Decreased absorption of norfloxacin1 2 18 71 240 266



Administer norfloxacin tablets at least 2 hours before or after such antacids1 219



Anticoagulants, oral (warfarin)



Potential for enhanced warfarin effects1 276 289



Use with caution;276 289 monitor PT or other appropriate coagulation tests1



β-lactam antibiotics



No in vitro evidence of synergism or antagonism against gram-positive or -negative bacteria when used with ampicillin, cefotaxime, or cefoxitin48



Caffeine



Possible prolonged half-life of caffeine with some quinolones (e.g., ciprofloxacin)241 244 269 270 271 272 273



The possibility of exaggerated or prolonged effects of caffeine during concomitant use with a quinolone should be considered244 270



Corticosteroids



Increased risk of tendinitis or tendon rupture, especially in patients >60 years of age1 372 373



Cyclosporine



Possible increased concentrations of cyclosporine1



Monitor cyclosporine concentrations and adjust cyclosporine dosage if needed1



Didanosine



Decreased absorption of norfloxacin with buffered didanosine preparations1



Administer norfloxacin tablets at least 2 hours before or after buffered didanosine preparations (pediatric oral solution admixed with antacid)1



Glyburide



Severe hypoglycemia reported1



Monitor blood glucose1



Iron preparations



Decreased absorption of norfloxacin1



Administer norfloxacin tablets at least 2 hours before or after ferrous sulfate and dietary supplements containing iron1



Multivitamins and mineral supplements



Decreased absorption of norfloxacin1



Administer norfloxacin tablets at least 2 hours before or after supplements containing zinc or iron1



Nitrofurantoin



Some in vitro evidence of antagonism between norfloxacin and nitrofurantoin1



Clinical importance unknown; should not be used concomitantly1



NSAIAs



Increased risk of CNS stimulation and convulsive seizures1


Animal studies suggest norfloxacin may have greater convulsant activity than some other fluoroquinolones (e.g., levofloxacin) and the potential risk associated with concomitant therapy may vary depending on the specific NSAIA357



Use with caution1



Probenecid



Decreased clearance of norfloxacin;1 2 3 139 serum concentrations139 and half-life of norfloxacin generally not affected2 3



Sucralfate



Possible decreased GI absorption of norfloxacin1 333



Some clinicians suggest that concomitant use should be avoided; if used concomitantly, give norfloxacin tablets at least 2 hours before or after sucralfate1 333



Theophylline



Possible increased theophylline concentrations and increased risk of theophylline-related adverse effects1 18 21 205 216 224 225 234 244 245 246 255


Although risk of norfloxacin inducing substantial alterations in theophylline pharmacokinetics appears to be less than with some other quinolones (e.g., ciprofloxacin),244 245 246 255 256 theophylline-related adverse effects have been reported in patients receiving norfloxacin concomitantly1



Some clinicians suggest that the interaction between norfloxacin and theophylline may not be clinically important in most patients;234 255 256 275 287 others suggest that norfloxacin should be used with caution in patients receiving theophylline205 219 244 246 255


Manufacturer of norfloxacin states that consideration should be given to monitoring plasma theophylline concentrations and theophylline dosage should be adjusted as required1


Noroxin Pharmacokinetics


Absorption


Bioavailability


Rapidly, but incompletely, absorbed from GI tract following oral administration.1 2 3 4 17 18 21 22 136 142 205


At least 30–50% of an oral dose is absorbed from GI tract;1 2 4 peak serum concentrations generally attained within 1–2 hours

Hydroquinone Cream




Hydroquinone USP, 4%

  


Skin Bleaching Cream


Rx Only


FOR EXTERNAL USE ONLY


NOT FOR OPHTHALMIC USE



Hydroquinone Cream Description


Each gram of Hydroquinone USP, 4% Skin Bleaching Cream contains 40 mg hydroquinone USP, in a vanishing cream base of glyceryl monostearate, mineral oil, PEG-25 propylene glycol stearate, polyoxyl 40 stearate, propylene glycol, propylparaben, purified water, sodium metabisulfite, squalane and stearic acid. Chemically, hydroquinone is C6H6O2 and has a molecular weight of 110.11. The chemical name is 1,4 dihydroxybenzene, and the structural formula of hydroquinone is:




Hydroquinone Cream - Clinical Pharmacology


Topical application of hydroquinone produces a reversible depigmentation of the skin by inhibition of the enzymatic oxidation of tyrosine to 3,4-dihydroxyphenylalanine (dopa) (Denton, C. et al., 1952)1 and suppression of other melanocyte metabolic processes (Jimbow, K. et al., 1974)2. Exposure to sunlight or ultraviolet light will cause repigmentation of bleached areas (Parrish, J.A. et al., 1978)3.



Indications and Usage for Hydroquinone Cream


Hydroquinone USP, 4% Skin Bleaching Cream is indicated for the gradual bleaching of hyperpigmented skin conditions such as chloasma, melasma, freckles, senile lentigines, and other unwanted areas of melanin hyperpigmentation.



Contraindications


Prior history of sensitivity or allergic reaction to hydroquinone or to any of the ingredients of the product. The safety of topical hydroquinone use during pregnancy or for children (12 years and under) has not been established.



Warnings


Contains sodium metabisulfite, a sulfite that may cause allergic-type reactions including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in certain susceptible people. The overall prevalence of sulfite sensitivity in the general population is unknown and probably low. Sulfite sensitivity is seen more frequently in asthmatic than in non-asthmatic people.


Since this product contains no sunscreen, an effective broad spectrum sun blocking agent should be used and unnecessary solar exposure avoided, or protective clothing should be worn to cover bleached skin in order to prevent repigmentation from occurring.


Hydroquinone may produce exogenous ochronosis, a gradual blue-black darkening of the skin. If this condition occurs, discontinue treatment and consult your physician. The majority of patients developing this condition are Black, but it may also occur in Caucasians and Hispanics.



PRECAUTIONS


(see WARNINGS)



General -


Test for skin sensitivity before using by applying a small amount to an unbroken patch of skin; check within 24 hours. Minor redness is not a contraindication, but where there is itching or vesicle formation or excessive inflammatory response further treatment is not advised. Close patient supervision is recommended.


Hydroquinone is a skin bleaching agent which may produce unwanted cosmetic effects if not used as directed. The physician should be familiar with the contents of this insert before prescribing or dispensing this medication.



Information for Patients -


Sunscreen use is an essential aspect of hydroquinone therapy because even minimal sunlight sustains melanocytic activity. To prevent repigmentation, during treatment and maintenance therapy, sun exposure on treated skin should be avoided by application of a broad spectrum sunscreen (SPF 15 or greater) or by use of protective clothing.


Avoid contact with eyes and mucous membranes.


Keep this and all medications out of reach of children. In case of accidental ingestion, call a physician or a poison control center immediately.



Drug Interactions -


Patients are cautioned on concomitant use of medications that are known to be photosensitizing.



Carcinogenesis, Mutagenesis, Impairment of Fertility -


Studies of hydroquinone in animals have demonstrated some evidence of carcinogenicity. The carcinogenic potential of hydroquinone in humans is unknown.


Published studies have demonstrated that hydroquinone is a mutagen and a clastogen. Treatment with hydroquinone has resulted in positive findings for genetic toxicity in the Ames assay in bacterial strains sensitive to oxidizing mutagens, in in vitro studies in mammalian cells, and in the in vivo mouse micronucleus assay.



Pregnancy:


Teratogenic Effects:

Pregnancy Category C -


Animal reproduction studies have not been conducted with topical hydroquinone. It is also not known whether topical hydroquinone can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Topical hydroquinone should be given to a pregnant woman only if clearly needed.



Nursing Mothers -


It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when topical hydroquinone is administered to a nursing woman.



Pediatric Use -


Safety and effectiveness for pediatric patients below the age of 12 years have not been established.



Adverse Reactions


The following adverse reactions have been reported: dryness and fissuring of paranasal and infraorbital areas, erythema, and stinging. Occasional hypersensitivity (localized contact dermatitis) may develop. If this occurs, the medication should be discontinued and the physician notified immediately.



Overdosage


There have been no systemic reactions reported from the use of topical hydroquinone. However, treatment should be limited to relatively small areas of the body at one time, since some patients experience a transient skin reddening and a mild burning sensation which does not preclude treatment.



Hydroquinone Cream Dosage and Administration


Hydroquinone USP, 4% Skin Bleaching Cream should be applied to affected areas and rubbed in well twice daily, in the morning and before bedtime, or as directed by a physician. If no improvement is seen after 2 months of treatment, use of this product should be discontinued. There is no recommended dosage for pediatric patients under 12 years of age except under the advice and supervision of a physician.



How is Hydroquinone Cream Supplied


Hydroquinone USP, 4% Skin Bleaching Cream is available as follows:


1 oz (28.35 g) tube (NDC 45802-980-64)



Store at 20-25°C (68-77°F) [see USP Controlled Room Temperature].



REFERENCES


1 DENTON C., LERNER A.B., FITZPATRICK T.B.


Inhibition of Melanin Formation by Chemical Agents


Journal of Investigative Dermatology 1952, 18:119-135.


2 JIMBOW K., OBATA H., PATHAK M., FITZPATRICK T.B.


Mechanism of Depigmentation by Hydroquinone


Journal of Investigative Dermatology 1974, 62:436-449.


3 PARRISH J.A., ANDERSON R.R., URBACH F., PITTS D.


UVA, Biological Effects of Ultraviolet Radiation with Emphasis on Human Responses to Longwave Ultraviolet


Plenum Press, New York and London, 1978, p. 151.


Manufactured by


Perrigo


Bronx, NY 10457



Rev. 03/11


7J200 RC J2



Principal Display Panel - 1 oz Carton


Rx Only


Hydroquinone USP, 4%


Skin Bleaching Cream


Hydroquinone USP, 4% Carton Image 1



Hydroquinone USP, 4% Carton Image 2




Principal Display Panel - 1 oz Tube


Rx Only


Hydroquinone USP, 4%


Skin Bleaching Cream


Hydroquinone USP, 4% - 1 oz Tube










HYDROQUINONE 
hydroquinone  cream










Product Information
Product TypeHUMAN PRESCRIPTION DRUGNDC Product Code (Source)45802-980
Route of AdministrationTOPICALDEA Schedule    








Active Ingredient/Active Moiety
Ingredient NameBasis of StrengthStrength
HYDROQUINONE (HYDROQUINONE)HYDROQUINONE40 mg  in 1 g
























Inactive Ingredients
Ingredient NameStrength
GLYCERYL MONOSTEARATE 
MINERAL OIL 
POLYOXYL 40 STEARATE 
PROPYLENE GLYCOL 
PROPYLPARABEN 
WATER 
SODIUM METABISULFITE 
SQUALANE 
STEARIC ACID 
PEG-25 PROPYLENE GLYCOL STEARATE 


















Product Characteristics
ColorWHITE (white to off-white)Score    
ShapeSize
FlavorImprint Code
Contains      














Packaging
#NDCPackage DescriptionMultilevel Packaging
145802-980-641 TUBE In 1 CARTONcontains a TUBE
128.35 g In 1 TUBEThis package is contained within the CARTON (45802-980-64)










Marketing Information
Marketing CategoryApplication Number or Monograph CitationMarketing Start DateMarketing End Date
Unapproved drug other06/17/2008


Labeler - Perrigo New York Inc (078846912)
Revised: 09/2011Perrigo New York Inc

More Hydroquinone Cream resources


  • Hydroquinone Cream Side Effects (in more detail)
  • Hydroquinone Cream Use in Pregnancy & Breastfeeding
  • Hydroquinone Cream Support Group
  • 2 Reviews for Hydroquinone - Add your own review/rating


Compare Hydroquinone Cream with other medications


  • Dermatological Disorders

Wednesday, 19 September 2012

Exemestane


Class: Antineoplastic Agents
VA Class: AN900
Molecular Formula: C20H24O2
CAS Number: 107868-30-4
Brands: Aromasin

Introduction

Antineoplastic agent; irreversible, selective steroidal aromatase inhibitor (type I), structurally related to the natural substrate androstenedione.1 2 3 4 5 6


Uses for Exemestane


Breast Cancer


Treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy.1


Exemestane Dosage and Administration


Administration


Oral Administration


Administer orally after a meal.1


Dosage


Adults


Breast Cancer

Oral

25 mg once daily; continue until tumor progression is evident.1


Prescribing Limits


Adults


Dosages >25 mg daily not shown to provide substantially greater suppression of plasma estrogens but may increase adverse effects.1 2 3


Special Populations


Hepatic Impairment


Dosage adjustment does not appear to be necessary.1 (See Special Populations under Pharmacokinetics.)


Renal Impairment


Dosage adjustment does not appear to be necessary.1 (See Special Populations under Pharmacokinetics.)


Cautions for Exemestane


Contraindications



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



Warnings/Precautions


Warnings


Fetal/Neonatal Morbidity and Mortality

Possible fetal harm; embryotoxic in rats and embryotoxic and abortifacient in rabbits.1 If used during pregnancy, apprise of potential hazard to fetus and potential risk for loss of the pregnancy.1


General Precautions


Premenopausal Women

Not recommended for use in premenopausal women.1 Possible incomplete estrogen suppression and reflex increases in gonadotropin levels (ovarian hyperstimulation syndrome).6


Estrogenic Agents

Do not administer concomitantly with exemestane.1 (See Estrogenic Agents under Interactions.)


Lymphocytopenia

Risk of grade 3 or 4 lymphocytopenia; no substantial increase in viral infections and no opportunistic infections observed in clinical studies.1


Specific Populations


Pregnancy

Category D.1 (See Fetal/Neonatal Morbidity and Mortality under Cautions.)


Lactation

Distributed into milk in rats; not known whether distributed into human milk.1 Caution advised if a nursing woman is inadvertently exposed to the drug.1


Pediatric Use

Not indicated; safety and efficacy not established.1


Geriatric Use

No special precautions.1


Hepatic Impairment

Safety of chronic administration not established.1


Renal Impairment

Safety of chronic administration not established.1


Common Adverse Effects


Hot flushes (flashes), nausea, fatigue, increased sweating, excessive weight gain, pain, mental depression, insomnia, anxiety, dyspnea, dizziness, headache, edema, vomiting, flu-like symptoms, abdominal pain, anorexia, coughing, hypertension, constipation.1


Interactions for Exemestane


Metabolized by CYP3A4.1 Does not inhibit CYP1A2, 2C9, 2D6, 2E1, or 3A4.1


Drugs Affecting Hepatic Microsomal Enzymes


Inhibitors or inducers of CYP3A4; potential pharmacokinetic interaction (possible increased or decreased serum exemestane concentrations).1 However, based on experience with concomitant ketoconazole (potent CYP3A4 inhibitor), clinically important interactions with CYP3A4 inhibitors unlikely.1


Estrogenic Agents


Potential antagonistic pharmacologic effects.1


Exemestane Pharmacokinetics


Absorption


Bioavailability


Rapidly absorbed following oral administration, with peak concentrations in women with breast cancer or healthy women attained within about 1.2 or 2.9 hours, respectively.1


Steady-state plasma concentrations achieved in approximately 7 days.1


Food


High-fat meal increases plasma exemestane concentrations by approximately 40%.1


Distribution


Extent


Extensively distributed into tissues.1


Crosses placenta.


Distributed into milk in animals; not studied in pregnant or nursing women.1


Plasma Protein Binding


90% (mainly α1-acid glycoprotein and albumin).1


Elimination


Metabolism


Extensively metabolized via CYP3A4 and aldoketoreductases; metabolites are inactive or inhibit aromatase with decreased potency compared with parent drug.1 One metabolite, 17-hydroexemestane, may have androgenic activity.1


Elimination Route


Excreted similarly (42%) in both urine and feces; <1% excreted as unchanged drug in urine.1


Half-life


Approximately 24 hours.1


Special Populations


In patients with moderate or severe hepatic or renal impairment, AUC is approximately 3 times higher than in healthy individuals.1


Stability


Storage


Oral


Tablets

25°C (may be exposed to 15–30°C).1


ActionsActions



  • Acts as a false substrate and is converted by aromatase to reactive alkylating intermediates that bind covalently to the substrate binding site of the enzyme; this irreversible binding to the active site of aromatase results in its inactivation (i.e., “suicide” inhibition).1 2 4 5 6




  • Selectively inhibits conversion of androgens to estrogens;1 2 4 5 6 resulting reduction in serum and tumor concentrations of estrogen inhibits tumor growth and delays disease progression.1 6




  • Selectively inhibits synthesis of estrogens; does not affect synthesis of adrenal corticosteroid, aldosterone, or thyroid hormone.1 2 3 6




  • Dose-dependent decrease in sex hormone binding globulin (SHBG) observed with dosages ≥ 2.5 mg daily.1 2




  • Slight, dose-independent increases in serum LH and FSH concentrations observed even at low dosages as result of negative feedback on the pituitary gland.1 2 3




  • At dosages ≤25 mg daily, no clinically important effect on circulating concentrations of testosterone, androstenedione, dehydroepiandrostenedione sulfate, or 17-hydroxyprogesterone observed.1 3




  • At dosages ≥200 mg daily, testosterone and androstenedione concentrations are increased.1 3 17-Hydroexemestane, a metabolite, exhibits substantial intrinsic androgenic activity, which may become clinically important at high (e.g., 200 mg daily) dosages.1 2 3



Advice to Patients



  • Importance of adherence to dosing and medical or laboratory appointment schedules.1




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




  • Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed; warn of potential hazard to the fetus in cases of inadvertent exposure of pregnant women to exemestane.1




  • Importance of informing 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.













Exemestane

Routes



Dosage Forms



Strengths



Brand Names



Manufacturer



Oral



Tablets



25 mg



Aromasin



Pfizer


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.


Aromasin 25MG Tablets (PFIZER U.S.): 30/$406.97 or 90/$1189.92



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 May 2004. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.




References



1. Pharmacia & Upjohn Co. Aromasin (exemestane) tablets prescribing information. Kalamazoo, MI; 1999 Oct 20.



2. Johannessen DC, Engan T, Di Salle E et al. Endocrine and clinical effects of exemestane (PNU 155971), a novel steroidal aromatase inhibitor, in postmenopausal breast cancer patients: a phase I study. Clin Cancer Res. 1997; 3:1101-8. [IDIS 389585] [PubMed 9815789]



3. Evans TRJ, Di Salle E, Ornati G et al. Phase I and endocrine study of exemestane (FCE 24304), a new aromatase inhibitor, in postmenopausal women. Cancer Res. 1992; 52:5933-9. [IDIS 304969] [PubMed 1394219]



4. Geisler J, King N, Anker G et al. In vivo inhibition of aromatization by exemestane, a novel irreversible aromatase inhibitor, in postmenopausal breast cancer patients. Clin Cancer Res. 1998; 4:2089-93. [IDIS 410748] [PubMed 9748124]



5. Reddy P. A review of the newer aromatase inhibitors in the management of metastatic breast cancer. J Clin Pharm Ther. 1998; 23:81-90. [IDIS 415373] [PubMed 9786093]



6. Goss PE, Gwyn KMEH. Current perspectives on aromatase inhibitors in breast cancer. J Clin Oncol. 1994; 12:2460-70. [IDIS 338078] [PubMed 7964964]



7. Anker GB, Refsum H, Ueland PM et al. Influence of aromatase inhibitors on plasma total homocysteine in postmenopausal breast cancer patients. Clin Chem. 1999; 45:252-6. [IDIS 424029] [PubMed 9931048]



a. Pharmacia & Upjohn Co. Aromasin (exemestane) tablets prescribing information. Kalamazoo, MI; 2003 Jul.



More Exemestane resources


  • Exemestane Side Effects (in more detail)
  • Exemestane Dosage
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  • Drug Images
  • Exemestane Drug Interactions
  • Exemestane Support Group
  • 10 Reviews for Exemestane - Add your own review/rating


  • Exemestane MedFacts Consumer Leaflet (Wolters Kluwer)

  • Exemestane Professional Patient Advice (Wolters Kluwer)

  • exemestane Advanced Consumer (Micromedex) - Includes Dosage Information

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  • Breast Cancer

Sotalol



Pronunciation: SOE-ta-lol
Generic Name: Sotalol
Brand Name: Betapace

Because Sotalol may sometimes cause an abnormal or irregular heartbeat, patients who begin taking or restart Sotalol should be observed in a hospital or similar setting in which heart and kidney function monitoring may be performed for at least 3 days after starting Sotalol. Close monitoring of your heart or kidney function may also be needed if your dose is changed. Do not change from one brand or generic version of Sotalol to another without consulting your doctor or pharmacist. Sotalol is labeled specifically for ventricular arrhythmias.





Sotalol is used for:

Treating certain types of irregular heartbeat (ventricular arrhythmias).


Sotalol is an antiarrhythmic medicine. It works by helping the heart beat regularly for a longer period of time.


Do NOT use Sotalol if:


  • you are allergic to any ingredient in Sotalol

  • you have certain types of irregular heartbeat (eg, long QT syndrome, prolonged QT interval), shock caused by serious heart problems, uncontrolled heart failure, low blood potassium or magnesium levels, or certain lung or breathing problems (eg, asthma, chronic bronchitis, emphysema)

  • you have a very slow heartbeat or certain types of irregular heartbeat (sick sinus syndrome, second- or third-degree heart block) and you do not have a permanent pacemaker

  • you are taking certain antiarrhythmics (eg, amiodarone, disopyramide, dofetilide, procainamide, quinidine), bepridil, cisapride, mibefradil, nilotinib, tetrabenazine, a theophylline (eg, aminophylline), a tricyclic antidepressant (eg, amitriptyline), or vardenafil

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



Before using Sotalol:


Some medical conditions may interact with Sotalol. 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 breathing or lung problems (eg, chronic obstructive pulmonary disorder [COPD]); an overactive thyroid; kidney problems; diabetes; blood flow problems; a tumor on your adrenal gland; loss of appetite; increased thirst; or severe or persistent diarrhea, sweating, or vomiting

  • if you have a history of other heart problems (eg, heart failure, slow or irregular heartbeat, a recent heart attack), blood electrolyte problems (eg, low blood potassium or magnesium levels), problems with the acid or base levels in your body, or episodes of low blood sugar

  • if you are on dialysis or you are scheduled for surgery

Some MEDICINES MAY INTERACT with Sotalol. Tell your health care provider if you are taking any other medicines, especially any of the following:


  • Indomethacin because it may decrease Sotalol's effectiveness

  • Calcium channel blockers (eg, diltiazem, verapamil), clonidine, digoxin, diuretics (eg, furosemide, hydrochlorothiazide), guanethidine, mibefradil, or reserpine because the risk of side effects, such as low blood pressure or heart problems, may be increased

  • Antiarrhythmics (eg, dronedarone, propafenone), arsenic, astemizole, bepridil, chloroquine, cisapride, dolasetron, domperidone, droperidol, fingolimod, fluconazole, halofantrine, haloperidol, iloperidone, ketanserin, macrolides and ketolides (eg, erythromycin), maprotiline, mefloquine, methadone, nilotinib, oseltamivir, paliperidone, pentamidine, phenothiazines (eg, chlorpromazine, thioridazine), pimozide, quinolones (eg, ciprofloxacin), romidepsin, saquinavir, terfenadine, tetrabenazine, tricyclic antidepressants (eg, amitriptyline), tyrosine kinase inhibitors (eg, dasatinib), vardenafil, or ziprasidone because the risk of abnormal heart rhythms may be increased

  • Epinephrine, insulin, lidocaine, meglitinide antidiabetics (eg, nateglinide), or quinazolines (eg, prazosin) because the risk of their side effects may be increased by Sotalol

  • Beta-agonists (eg, albuterol) or theophyllines (eg, aminophylline) because their effectiveness may be decreased by Sotalol

This may not be a complete list of all interactions that may occur. Ask your health care provider if Sotalol 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 Sotalol:


Use Sotalol as directed by your doctor. Check the label on the medicine for exact dosing instructions.


  • Take Sotalol by mouth with or without food. Try to take it the same way (either with food or without food) each time you take your dose. Check with your doctor or pharmacist if you have questions about taking Sotalol with food.

  • Do not take an antacid that has aluminum or magnesium in it within 2 hours before or after you take Sotalol.

  • Sotalol works best if it is taken at the same time each day. Taking Sotalol at the same time each day will also help you remember to take it.

  • Continue to use Sotalol even if you feel well. Do not miss any doses.

  • If you miss a dose of Sotalol, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Sotalol.



Important safety information:


  • Sotalol may cause dizziness or lightheadedness. These effects may be worse if you take it with alcohol or certain medicines. Use Sotalol with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.

  • Sotalol may cause dizziness, lightheadedness, or fainting; alcohol, hot weather, exercise, or fever may increase these effects. To prevent them, sit up or stand slowly, especially in the morning. Sit or lie down at the first sign of any of these effects.

  • Do NOT take more than the recommended dose or change your dose without checking with your doctor.

  • Tell your doctor or dentist that you take Sotalol before you receive any medical or dental care, emergency care, or surgery.

  • Do not suddenly stop taking Sotalol. Sharp chest pain, irregular heartbeat, and, sometimes, heart attack may occur if you suddenly stop Sotalol. The risk may be greater if you have certain types of heart disease. Heart disease is common and you may not know you have it. Your doctor should slowly lower your dose over several weeks if you need to stop taking it. Limit physical activity while you are lowering your dose. If new or worsened chest pain or other heart problems occur, contact your doctor right away. You may need to start taking Sotalol again.

  • Diabetes patients - Sotalol may affect your blood sugar. Check blood sugar levels closely. Ask your doctor before you change the dose of your diabetes medicine.

  • Diabetes patients - Sotalol may hide signs of low blood sugar, such as rapid heartbeat. Be sure to watch for other signs of low blood sugar. Low blood sugar may make you anxious, sweaty, weak, dizzy, drowsy, or faint. It may also make your vision change; give you a headache, chills, or tremors; or make you more hungry. Check blood sugar levels closely. Ask your doctor before you change the dose of your diabetes medicine.

  • If you have a history of any severe allergic reaction, talk with your doctor. You may be at risk of an even more severe allergic reaction if you come into contact with the substance that caused your allergy. Some medicines used to treat severe allergies may also not work as well while you are taking Sotalol.

  • Sotalol may interfere with certain lab tests. Be sure your doctor and lab personnel know you are taking Sotalol.

  • Lab tests, including heart and kidney function, and blood pressure monitoring, may be performed while you take Sotalol. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.

  • PREGNANCY and BREAST-FEEDING: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of taking Sotalol while you are pregnant. Sotalol is found in breast milk. Do not breast-feed while taking Sotalol.


Possible side effects of Sotalol:


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:



Dizziness; headache; lightheadedness; mild diarrhea or nausea; tiredness; trouble sleeping.



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); abnormally fast, slow, or irregular heartbeat; changes in vision; chest pain; decreased appetite; excessive thirst; fainting; numbness of an arm or leg; severe or persistent tiredness; severe or persistent nausea, vomiting, or diarrhea; severe stomach pain; shortness of breath; sudden leg pain; sudden, severe headache, vomiting, or dizziness; unusual sweating.



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: Sotalol 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. Symptoms may include difficulty breathing; dizziness; fainting; fatigue; severe weakness; slow heartbeat.


Proper storage of Sotalol:

Store Sotalol at 77 degrees F (25 degrees C). Brief storage at temperatures between 59 and 86 degrees F (15 and 30 degrees C) is permitted. Store away from heat, moisture, and light. Do not store in the bathroom. Keep Sotalol out of the reach of children and away from pets.


General information:


  • If you have any questions about Sotalol, please talk with your doctor, pharmacist, or other health care provider.

  • Sotalol 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 Sotalol. 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 Sotalol resources


  • Sotalol Side Effects (in more detail)
  • Sotalol Use in Pregnancy & Breastfeeding
  • Drug Images
  • Sotalol Drug Interactions
  • Sotalol Support Group
  • 9 Reviews for Sotalol - Add your own review/rating


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