Zymar

gatifloxacin

Dosage Form: ophthalmic solution
Zymar®

(gatifloxacin ophthalmic solution) 0.3%

sterile

Zymar Description

Zymar® (gatifloxacin ophthalmic solution) 0.3% is a sterile ophthalmic solution. It is an 8-methoxy fluoroquinolone anti-infective for topical ophthalmic use.

Structure and Empirical Formula:

Chemical Name: (±) - 1 - Cyclopropyl - 6 - fluoro - 1,4 - dihydro - 8 - methoxy - 7 - (3 - methyl - 1 - piperazinyl) - 4 - oxo - 3 - quinolinecarboxylic acid, sesquihydrate

Contains: Active: gatifloxacin 0.3% (3 mg/mL). Preservative: benzalkonium chloride 0.005%. Inactives: edetate disodium; purified water and sodium chloride. May contain hydrochloric acid and/or sodium hydroxide to adjust pH to approximately 6.

Zymar® is a sterile, clear, pale yellow colored isotonic unbuffered solution. It has an osmolality of 260-330 mOsm/kg.

Zymar - Clinical Pharmacology

Pharmacokinetics: Gatifloxacin ophthalmic solution 0.3% or 0.5% was administered to one eye of 6 healthy male subjects each in an escalated dosing regimen starting with a single 2-drop dose, then 2 drops 4 times daily for 7 days and finally 2 drops 8 times daily for 3 days. At all time points, serum gatifloxacin levels were below the lower limit of quantification (5 ng/mL) in all subjects.

Microbiology: Gatifloxacin is an 8-methoxyfluoroquinolone with a 3-methylpiperazinyl substituent at C7. The antibacterial action of gatifloxacin results from inhibition of DNA gyrase and topoisomerase IV. DNA gyrase is an essential enzyme that is involved in the replication, transcription and repair of bacterial DNA.

Topoisomerase IV is an enzyme known to play a key role in the partitioning of the chromosomal DNA during bacterial cell division.

The mechanism of action of fluoroquinolones including gatifloxacin is different from that of aminoglycoside, macrolide, and tetracycline antibiotics. Therefore, gatifloxacin may be active against pathogens that are resistant to these antibiotics and these antibiotics may be active against pathogens that are resistant to gatifloxacin. There is no cross-resistance between gatifloxacin and the aforementioned classes of antibiotics. Cross resistance has been observed between systemic gatifloxacin and some other fluoroquinolones.

Resistance to gatifloxacin in vitro develops via multiple-step mutations. Resistance to gatifloxacin in vitro occurs at a general frequency of between 1 x 10-7 to 10-10.

Gatifloxacin has been shown to be active against most strains of the following organisms both in vitro and clinically, in conjunctival infections as described in the INDICATIONS AND USAGE section.

Aerobes, Gram-Positive:

Corynebacterium propinquum*

Staphylococcus aureus

Staphylococcus epidermidis

Streptococcus mitis*

Streptococcus pneumoniae

Aerobes, Gram-Negative:

Haemophilus influenzae

* Efficacy for this organism was studied in fewer than 10 infections.

The following in vitro data are available, but their clinical significance in ophthalmic infections is unknown. The safety and effectiveness of Zymar® in treating ophthalmic infections due to the following organisms have not been established in adequate and well-controlled clinical trials.

The following organisms are considered susceptible when evaluated using systemic breakpoints. However, a correlation between the in vitro systemic breakpoint and ophthalmological efficacy has not been established.

The following list of organisms is provided as guidance only in assessing the potential treatment of conjunctival infections. Gatifloxacin exhibits in vitro minimal inhibitory concentrations (MICs) of 2 μg/mL or less (systemic susceptible breakpoint) against most (≥ 90%) strains of the following ocular pathogens.

Aerobes, Gram-Positive:

Listeria monocytogenes

Staphylococcus saprophyticus

Streptococcus agalactiae

Streptococcus pyogenes

Streptococcus viridans Group

Streptococcus Groups C, F, G

Aerobes, Gram-Negative:

Acinetobacter lwoffii

Enterobacter aerogenes

Enterobacter cloacae

Escherichia coli

Citrobacter freundii

Citrobacter koseri

Haemophilus parainfluenzae

Klebsiella oxytoca

Klebsiella pneumoniae

Moraxella catarrhalis

Morganella morganii

Neisseria gonorrhoeae

Neisseria meningitidis

Proteus mirabilis

Proteus vulgaris

Serratia marcescens

Vibrio cholerae

Yersinia enterocolitica

Other Microorganisms:

Chlamydia pneumoniae

Legionella pneumophila

Mycobacterium marinum

Mycobacterium fortuitum

Mycoplasma pneumoniae

Anaerobic Microorganisms:

Bacteroides fragilis

Clostridium perfringens

Clinical Studies: In a randomized, double-masked, multicenter clinical trial, where patients were dosed for 5 days, Zymar® solution was superior to its vehicle on day 5-7 in patients with conjunctivitis and positive conjunctival cultures. Clinical outcomes for the trial demonstrated clinical cure of 77% (40/52) for the gatifloxacin-treated group versus 58% (28/48) for the placebo-treated group. Microbiological outcomes for the same clinical trial demonstrated a statistically superior eradication rate for causative pathogens of 92% (48/52) for gatifloxacin vs. 72% (34/48) for placebo. Please note that microbiological eradication does not always correlate with clinical outcome in anti-infective trials.

Indications and Usage for Zymar

Zymar® solution is indicated for the treatment of bacterial conjunctivitis caused by susceptible strains of the following organisms:

Aerobic Gram-Positive Bacteria:

Corynebacterium propinquum*

Staphylococcus aureus

Staphylococcus epidermidis

Streptococcus mitis*

Streptococcus pneumoniae

Aerobic Gram-Negative Bacteria:

Haemophilus influenzae

* Efficacy for this organism was studied in fewer than 10 infections.

Contraindications

Zymar® solution is contraindicated in patients with a history of hypersensitivity to gatifloxacin, to other quinolones, or to any of the components in this medication.

Warnings

NOT FOR INJECTION.

Zymar® solution should not be injected subconjunctivally, nor should it be introduced directly into the anterior chamber of the eye.

In patients receiving systemic quinolones, including gatifloxacin, serious and occasionally fatal hypersensitivity (anaphylactic) reactions, some following the first dose, have been reported. Some reactions were accompanied by cardiovascular collapse, loss of consciousness, angioedema (including laryngeal, pharyngeal or facial edema), airway obstruction, dyspnea, urticaria, and itching. If an allergic reaction to gatifloxacin occurs, discontinue the drug. Serious acute hypersensitivity reactions may require immediate emergency treatment. Oxygen and airway management should be administered as clinically indicated.

Precautions

General: As with other anti-infectives, prolonged use may result in overgrowth of nonsusceptible organisms, including fungi. If superinfection occurs, discontinue use and institute alternative therapy. Whenever clinical judgment dictates, the patient should be examined with the aid of magnification, such as slit lamp biomicroscopy and, where appropriate, fluorescein staining.

Patients should be advised not to wear contact lenses if they have signs and symptoms of bacterial conjunctivitis.

Information for Patients: Avoid contaminating the applicator tip with material from the eye, fingers or other source.

Systemic quinolones, including gatifloxacin, have been associated with hypersensitivity reactions, even following a single dose. Discontinue use immediately and contact your physician at the first sign of a rash or allergic reaction.

Drug Interactions: Specific drug interaction studies have not been conducted with Zymar® ophthalmic solution. However, the systemic administration of some quinolones has been shown to elevate plasma concentrations of theophylline, interfere with the metabolism of caffeine, and enhance the effects of the oral anticoagulant warfarin and its derivatives, and has been associated with transient elevations in serum creatinine in patients receiving systemic cyclosporine concomitantly.

Carcinogenesis, Mutagenesis, Impairment of Fertility:

There was no increase in neoplasms among B6C3F1 mice given gatifloxacin in the diet for 18 months at doses averaging 81 mg/kg/day in males and 90 mg/kg/day in females. These doses are approximately 2000-fold higher than the maximum recommended ophthalmic dose of 0.04 mg/kg/day in a 50 kg human.

There was no increase in neoplasms among Fischer 344 rats given gatifloxacin in the diet for 2 years at doses averaging 47 mg/kg/day in males and 139 mg/kg/day in females (1000 and 3000-fold higher, respectively, than the maximum recommended ophthalmic dose). A statistically significant increase in the incidence of large granular lymphocyte (LGL) leukemia was seen in males treated with a high dose of approximately 2000-fold higher than the maximum recommended ophthalmic dose. Fischer 344 rats have a high spontaneous background rate of LGL leukemia and the incidence in high-dose males only slightly exceeded the historical control range established for this strain.

In genetic toxicity tests, gatifloxacin was positive in 1 of 5 strains used in bacterial reverse mutation assays; Salmonella strain TA102. Gatifloxacin was positive in in vitro mammalian cell mutation and chromosome aberration assays. Gatifloxacin was positive in in vitro unscheduled DNA synthesis in rat hepatocytes but not human leukocytes. Gatifloxacin was negative in in vivo micronucleus tests in mice, cytogenetics test in rats, and DNA repair test in rats. The findings may be due to the inhibitory effects of high concentrations on eukaryotic type II DNA topoisomerase.

There were no adverse effects on fertility or reproduction in rats given gatifloxacin orally at doses up to 200 mg/kg/day (approximately 4500-fold higher than the maximum recommended ophthalmic dose for Zymar®).

Pregnancy: Teratogenic Effects. Pregnancy Category C:

There were no teratogenic effects observed in rats or rabbits following oral gatifloxacin doses up to 50 mg/kg/day (approximately 1000-fold higher than the maximum recommended ophthalmic dose). However, skeletal/craniofacial malformations or delayed ossification, atrial enlargement, and reduced fetal weight were observed in fetuses from rats given ≥150 mg/kg/day (approximately 3000-fold higher than the maximum recommended ophthalmic dose). In a perinatal/postnatal study, increased late post-implantation loss and neonatal/perinatal mortalities were observed at 200 mg/kg/day (approximately 4500 times the maximum recommended ophthalmic dose).

Because there are no adequate and well-controlled studies in pregnant women, Zymar® solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers: Gatifloxacin is excreted in the breast milk of rats. 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 gatifloxacin is administered to a nursing woman.

Pediatric Use: Safety and effectiveness in infants below the age of one year have not been established.

Geriatric Use: No overall differences in safety or effectiveness have been observed between elderly and younger patients.

Adverse Reactions

Ophthalmic Use: The most frequently reported adverse events in the overall study population were conjunctival irritation, increased lacrimation, keratitis, and papillary conjunctivitis. These events occurred in approximately 5-10% of patients. Other reported reactions occurring in 1-4% of patients were chemosis, conjunctival hemorrhage, dry eye, eye discharge, eye irritation, eye pain, eyelid edema, headache, red eye, reduced visual acuity and taste disturbance.

Zymar Dosage and Administration

The recommended dosage regimen for the treatment of bacterial conjunctivitis is:

Days 1 and 2: Instill one drop every two hours in the affected eye(s) while awake, up to 8 times daily.

Days 3 through 7: Instill one drop up to four times daily while awake.

How is Zymar Supplied

Zymar® (gatifloxacin ophthalmic solution) 0.3% is supplied sterile in a white, low density polyethylene (LDPE) bottle with a controlled dropper tip and a tan, high impact polystyrene (HIPS) cap in the following size:

              5 mL in 10 mL bottle - NDC 0023-9218-05

Note: Store at 15°-25°C (59°-77°F). Protect from freezing.

Animal Pharmacology

Quinolone antibacterials have been shown to cause bone or cartilage changes in immature animals. There was no evidence of bone cartilage changes following ocular administration of gatifloxacin in rabbits or dogs.

Rx only

Revised: 01/2010

© 2010 Allergan, Inc.

Irvine, CA 92612, U.S.A.

® marks owned by Allergan, Inc.

Licensed from Kyorin Pharmaceuticals Co., Ltd.

U.S. Patents 5,880,283 and 6,333,045

Made in the U.S.A.

71706US13B

Bottle Label – 5 mL

ALLERGAN

NDC 0023-9218-05 Rx Only

Zymar®

(gatifloxacin ophthalmic solution) 0.3%

5 mL sterile

Carton Label – 5 mL

NDC 0023-9218-05

Zymar®

(gatifloxacin ophthalmic solution) 0.3%

5 mL

Rx only sterile

ALLERGAN

Zymar  gatifloxacin  solution/ drops

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0023-9218 Route of Administration OPHTHALMIC DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength gatifloxacin (gatifloxacin) gatifloxacin 3 mg  in 1 mL

Inactive Ingredients Ingredient Name Strength edetate disodium   water   sodium chloride   benzalkonium chloride   hydrochloric acid   sodium hydroxide

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 0023-9218-05 1 BOTTLE In 1 CARTON contains a BOTTLE, DROPPER 1 5 mL In 1 BOTTLE, DROPPER This package is contained within the CARTON (0023-9218-05)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
NDA	NDA021493	04/11/2003

Labeler - Allergan, Inc. (144796497)

Establishment
Name	Address	ID/FEI	Operations
Allergan, Inc.		362898611	MANUFACTURE

Revised: 02/2011Allergan, Inc.

More Zymar resources

• Zymar Side Effects (in more detail)
• Zymar Dosage
• Zymar Use in Pregnancy & Breastfeeding
• Zymar Support Group
• 6 Reviews for Zymar - Add your own review/rating

• Zymar eent Monograph (AHFS DI)


• Zymar Advanced Consumer (Micromedex) - Includes Dosage Information


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• Conjunctivitis
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• Ophthalmic Surgery

Mexitil

Generic Name: Mexiletine Hydrochloride
Class: Class Ib Antiarrhythmics
VA Class: CV300
Chemical Name: 1-(2,6-Dimethylphenoxy)-2-propanamine hydrochloride
Molecular Formula: C₁₁H₁₇NO•HCl
CAS Number: 5370-01-4

Introduction

Antiarrhythmic agent; a local anesthetic-type, class 1B agent.^{1 8 10 11 12 24 34}

Uses for Mexitil

Ventricular Arrhythmias

Treatment of documented life-threatening ventricular arrhythmias (e.g., sustained ventricular tachycardia).^{1 20 34} Use for less severe arrhythmias is notrecommended.^{1 34 44}

Can reduce ventricular premature contractions (VPCs)†, paired VPCs†, and nonsustained ventricular tachycardia† and can suppress the recurrence of ventricular tachycardia and/or fibrillation in patients with ventricular tachycardia and/or fibrillation†.^{1 10 12 13 14 15 16 17 18 19 20 34} Avoid treatment of asymptomatic VPCs.^{1 34}

Has been effective in some patients for the treatment of ventricular arrhythmias unresponsive to other antiarrhythmic agents†.^{10 11 12 13 16 19 20} However, not a recommended or alternative agent for the management of arrhythmias in ACLS.⁴³

Diabetic Neuropathy

Has been used with equivocal results in the management of painful diabetic neuropathy†;^{26 27 28 29 30 31 32 39 45 46} pending further accumulation of data from well-designed studies, use only in patients who do not respond to or cannot tolerate more established therapies.^{32 39}

Mexitil Dosage and Administration

General

Ventricular Arrhythmias

• 
  

  Individualize dosage carefully according to individual response, tolerance, general condition, and cardiovascular status.^{1 12 17 34 44 46}

  
  


• 
  

  Clinical and ECG evaluation (e.g., Holter monitoring) is recommended to determine whether the desired antiarrhythmic effect has been achieved and to guide dosage titration and adjustment.^{1 12 14 17 18 34 44}

  
  


• 
  

  Initiate therapy in a hospital.^{1 34} Patients at high risk for developing life-threatening arrhythmias after discontinuance of existing antiarrhythmic therapy should be hospitalized.^{1 34}

  
  

Administration

Oral Administration

Administer orally, generally every 8 hours.^{1 10 12 15}

Administer with food or antacids to minimize adverse GI effects.^{1 10 11 12 34 44 46}

Dosage

Available as mexiletine hydrochloride; dosage expressed in terms of the salt.¹

Adults

Ventricular Arrhythmias

Oral

If rapid control of arrhythmia is essential, 400-mg loading dose followed by 200 mg in 8 hours.^{1 12 13 15 34} If rapid control of arrhythmia is not essential, initial dosage of 200 mg every 8 hours.^{1 17 20 34}

If necessary, adjust dosage at intervals of at least 2–3 days in increments or decrements of 50 or 100 mg.^{1 13 34} 200–300 mg every 8 hours usually results in satisfactory control of arrhythmias.^{1 10 17 34} If satisfactory control is not achieved and patient tolerates 300 mg every 8 hours, increase dosage to 400 mg every 8 hours.^{1 11 17 34}

If adequate control of arrhythmia has been achieved at doses ≤300 mg every 8 hours, total dosage may be administered twice daily (every 12 hours) with close monitoring of degree of ventricular ectopy suppression.^{1 34}

Switching from Another Class I Antiarrhythmic Agent

Oral

200 mg as a single dose, administered 6–12 hours after last dose of quinidine sulfate or disopyramide, 3–6 hours after last dose of procainamide, or 8–12 hours after last dose of tocainide.^{1 34} Adjust subsequent doses according to individual requirements.^{1 34}

When switching to mexiletine from IV lidocaine, discontinue lidocaine infusion at the time of administration of the first dose of mexiletine; however, keep infusion line open until arrhythmia appears to be satisfactorily suppressed.^{1 34} Closely monitor patient.^{1 34}

Diabetic Neuropathy†

Oral

Initial dosage of 200 mg once daily has been used;^{31 32 39 44 46} dosage increased at 2-day intervals to 200 mg twice daily and then 200 mg 3 times daily.^{32 39 46}

Prescribing Limits

Adults

Ventricular Arrhythmias

Oral

Maximum 400 mg every 8 hours^{1 11 17 34} (1.2 g daily).^{1 13 34 46}

If given twice daily, maximum 450 mg every 12 hours.^{1 34}

Diabetic Neuropathy†

Oral

Dosage generally should not exceed 1.2 g daily.^{32 39 46}

Special Populations

Hepatic Impairment

Consider dosage reduction in patients with hepatic impairment (including those with hepatic dysfunction secondary to CHF).^{1 8 12 34 44}

Renal Impairment

Dosage adjustment not required.^{1 8 12 21 34}

Cautions for Mexitil

Contraindications

• 
  

  Second- or third-degree AV block (unless a cardiac pacemaker is in place).^{1 34 46}

  
  


• 
  

  Cardiogenic shock.^{1 34 46}

  
  

Warnings/Precautions

Warnings

Mortality

In CAST study, excessive rate of mortality and nonfatal cardiac arrest reported in patients with asymptomatic, non-life-threatening ventricular arrhythmias and recent MI (>6 days but <2 years previously) who were receiving encainide or flecainide compared with placebo.^{1 2 3 4 5 34}

Limit use of mexiletine in patients with ventricular arrhythmias to those with life-threatening arrhythmias^{1 34} due to mexiletine’s arrhythmogenic potential (see Cardiovascular Effects under Cautions) and the lack of evidence for improved survival for class I antiarrhythmic agents.^{33 34 40 41 42} Use for treatment of less severe arrhythmias currently is not recommended; avoid treatment of asymptomatic VPCs.^{1 34}

Major Toxicities

Cardiovascular Effects

Possible development or exacerbation of arrhythmias; clinical and ECG evaluations are essential prior to and during therapy.^{1 34} Initiate therapy in a hospital.^{1 34}

Use with caution in patients with preexisting first-degree AV block, sinus node dysfunction, or intraventricular conduction disturbances.^{1 34} Continuous monitoring recommended for patients with second- or third-degree AV block and an operative ventricular pacemaker.^{1 34} (See Contraindications under Cautions.)

Possible exacerbation of hypotension and CHF; use with caution in patients with these conditions.^{1 34}

Hepatic Effects

Possible abnormal liver function test results (AST elevations ≥3 times the ULN),^{1 34 44} especially during initial weeks of therapy in patients with CHF or AMI and/or patients who have received blood transfusions or other drug therapies.^{1 34} Discontinuance of therapy usually is not required.^{1 34} Severe hepatic injury, including hepatic necrosis, reported rarely.^{1 34}

Carefully evaluate patients who develop elevated serum concentrations of hepatic enzymes and those with signs or symptoms suggestive of liver dysfunction; consider discontinuance of therapy if enzyme elevations are persistent or increasing.^{1 34}

Hematologic Effects

Possible leukopenia, agranulocytosis, and thrombocytopenia, ^{1 34} especially in severely ill patients receiving concurrent therapy with drugs known to cause adverse hematologic effects (e.g., procainamide, vinblastine).^{1 34}

Carefully evaluate patients in whom substantial hematologic changes occur; consider discontinuing therapy.^{1 34} Blood cell counts generally return to normal within 1 month following discontinuance.^{1 34}

General Precautions

Seizures

Seizures reported rarely; discontinuance of therapy may be necessary.^{1 34} Use with caution in patients with a history of seizure disorder.^{1 34}

Effects on Urinary Excretion

Substantial changes in urinary pH may affect urinary excretion of mexiletine; avoid concomitant drug therapy or dietary regimens that may markedly affect urinary pH.^{1 11 12 21 34}

Specific Populations

Pregnancy

Category C.¹

Lactation

Distributed into milk.^{1 21 34} Discontinue nursing or the drug.^{1 34}

Pediatric Use

Safety and efficacy not established.^{1 34 44 47}

Hepatic Impairment

Possible prolonged elimination.^{1 8 9 12 13 34} Careful monitoring recommended (including in those with hepatic impairment secondary to CHF).^{1 8 9 34} Consider dosage reduction.^{1 8 12 34 44}

Common Adverse Effects

Nausea,^{1 14 18 19 20 34} vomiting,^{1 18 19 20 34} heartburn,^{1 14 20 34} dizziness^{1 5 18 19 34} or lightheadedness,^{1 34} tremor,^{1 18 20 34} nervousness,^{1 34} chest pain, ^{1 34} coordination difficulties,^{1 34} headache,^{1 15 34} blurred vision/visual disturbances.^{1 20 34}

Interactions for Mexitil

Metabolized by various CYP isoenzymes,^{1 9} principally by CYP2D and CYP1A2.³⁹

Drugs Affecting Hepatic Microsomal Enzymes

Hepatic enzyme inducers: Potential pharmacokinetic interaction (decreased plasma mexiletine concentrations).^{1 8 9 10 11 12 13 21 25 34}

Hepatic enzyme inhibitors: Potential pharmacokinetic interaction (decreased mexiletine clearance).^{1 49 50}

Drugs Affecting Gastric Emptying

Drugs that delay gastric emptying may reduce rate of mexiletine absorption^{1 34} (since mexiletine is absorbed in the small intestine^{1 11 12 13 21 34} ); conversely, drugs that accelerate gastric emptying may increase rate of mexiletine absorption.^{1 10 11 21 34}

Drugs Affecting Urinary pH

Drugs that markedly alter urinary pH may affect elimination of mexiletine; urinary acidification accelerates elimination; alkalinization slows elimination.¹ Avoid concomitant drug therapy that markedly affects urinary pH.^{1 11 12 21 34}

Specific Drugs

Drug	Interaction	Comments
Antacids (aluminum- and magnesium-containing)	Possible decreased rate of absorption of mexiletine1 10 11 21 34
Antianginal agents	Adverse pharmacokinetic interactions not reported1 34
Antiarrhythmic agents (e.g., quinidine, propranolol)	Possible improved control of ventricular ectopy;1 34 prolongation of PR and QT intervals or QRS complex not reported with concomitant propranolol use1 10 11 12 34
Anticoagulants	Adverse pharmacokinetic interactions not reported1 34
Antihypertensive agents	Adverse pharmacokinetic interactions not reported1 34
Atropine	Possible decreased rate of absorption of mexiletine1 10 11 21 34
Benzodiazepines	Pharmacokinetic interactions not reported1 34
Cimetidine	Possible increased, decreased, or unchanged plasma mexiletine concentrations1 8 11 12 34	Closely monitor plasma mexiletine concentrations1 34
Digoxin	Prolongation of PR and QT intervals or QRS complex not reported1 10 11 12 34
Diuretics	Prolongation of PR and QT intervals or QRS complex not reported1 10 11 12 34
Fluvoxamine	Reduced mexiletine clearance49 50	Monitor patient closely and monitor serum mexiletine concentrations 49 50
Lidocaine	Potential additive adverse effects1 34	Close monitoring recommended when patients are switched from IV lidocaine to mexiletine1 34
Methylxanthines (caffeine, theophylline)	Possible decreased methylxanthine clearance and increased plasma theophylline concentrations1 34	Monitor plasma theophylline concentrations; adjust theophylline dosage if necessary1 34
Metoclopramide	Possible increased rate of absorption of mexiletine1 10 11 21 34
Opiate agonists	Possible decreased rate of absorption of mexiletine1 10 11 21 34
Phenobarbital	Possible decreased plasma mexiletine concentrations1 8 9 10 11 12 13 21 25 34	Closely monitor plasma mexiletine concentrations1 34
Phenytoin	Possible decreased plasma mexiletine concentrations1 8 9 10 11 12 13 21 25 34	Closely monitor plasma mexiletine concentrations1 34
Propafenone	Possible increased plasma mexiletine concentrationsa b
Rifampin and rifapentine	Possible decreased plasma mexiletine concentrations1 8 9 10 11 12 13 21 25 34	Closely monitor plasma mexiletine concentrations1 34

Mexitil Pharmacokinetics

Absorption

Bioavailability

About 90% absorbed following oral administration, with peak plasma concentrations attained in 2–3 hours.¹ Undergoes low first-pass metabolism.^{1 34}

Onset

Onset of action is usually within 30–120 minutes.^{1 34}

Plasma Concentrations

Plasma mexilitine concentrations of ≥0.5 mcg/mL generally required to suppress ventricular arrhythmias; concentrations >2 mcg/mL associated with adverse CNS effects.¹

Special Populations

Decreased rate of absorption in patients with AMI or other conditions that delay gastric emptying.¹

Distribution

Plasma Protein Binding

50–60%.¹

Elimination

Metabolism

Extensively metabolized in the liver^{1 9 10 34} by various CYP isoenzymes,⁹ including CYP2D and CYP1A2.³⁹ Pharmacologic activity results principally from the parent drug.^{9 10}

Elimination Route

About 8–15% of a dose is excreted in urine as unchanged drug.^{12 13}

Half-life

10–12 hours.¹

Special Populations

In patients with hepatic impairment, possible decreased metabolism^{1 8 12 34 44} and prolonged elimination.^{1 8 9 12 13 34}

Stability

Storage

Oral

Capsules

20–25°C.¹

ActionsActions

• 
  

  Combines with fast sodium channels within the myocardium and inhibits rapid sodium influx, which decreases the maximal rate of depolarization of phase 0 of the action potential.^{1 8 10 11 12 21 34}

  
  


• 
  

  Inhibits recovery after repolarization in a time- and voltage-dependent manner, which is associated with subsequent dissociation of the drug from the sodium channels.^{35 36 37 39}

  
  


• 
  

  Increases the effective refractory period (ERP) relative to the duration of the action potential (ERP/APD)^{1 8 9 10 12 14 21 34} and reduces ventricular automaticity by raising the threshold for spontaneous firing of ventricular pacemaker cells.¹⁰

  
  


• 
  

  Exhibits electrophysiologic effects characteristic of class IB antiarrhythmic agents,^{8 10 12 35 36 37 38} which rapidly attach to and dissociate from transmembrane sodium channels.^{1 8 9 12 35 36 37}

  
  


• 
  

  Causes little or no prolongation of PR and QT intervals or QRS complex.^{1 8 9 10 12 14 21 34} Has no clinically important effect on heart rate, systemic arterial BP, or myocardial function in healthy individuals or patients with cardiovascular disease.^{1 10 11 12 14 21 34}

  
  

Advice to Patients

• 
  

  Potential for toxicity (e.g., cardiovascular, hepatic).¹

  
  


• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.^{1 34}

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.^{1 34}

  
  


• 
  

  Importance of informing patients of other important precautionary information. (See Cautions.)

  
  

Preparations

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

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Mexiletine Hydrochloride

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Capsules	150 mg*	Mexiletine Hydrochloride Capsules	Roxane, Sandoz, Teva, Watson
			Mexitil (with benzyl alcohol and parabens)	Boehringer Ingelheim
		200 mg*	Mexiletine Hydrochloride Capsules	Roxane, Sandoz, Teva, Watson
			Mexitil (with benzyl alcohol and parabens)	Boehringer Ingelheim
		250 mg*	Mexiletine Hydrochloride Capsules	Roxane, Sandoz, Teva, Watson
			Mexitil (with benzyl alcohol and parabens)	Boehringer Ingelheim

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.

Mexiletine HCl 150MG Capsules (TEVA PHARMACEUTICALS USA): 90/$45.99 or 270/$109.96

Mexiletine HCl 250MG Capsules (TEVA PHARMACEUTICALS USA): 90/$75.99 or 270/$209.99

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 April 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

1. Mexitil (mexiletine hydrochloride) capsules prescribing information. Boehringer Ingelheim Pharmaceuticals, Inc. Ridgefield, CT; 2003 May 30.

2. The Cardiac Arrhythmia Suppression Trial (CAST) investigators. Preliminary report: effect of encainide and flecainide on mortality in a randomized trial of arrhythmia suppression after myocardial infarction. N Engl J Med. 1989; 321:406-12. [IDIS 257848] [PubMed 2473403]

3. Ruskin JN. The Cardiac Arrhythmia Suppression Trial (CAST). N Engl J Med. 1989; 321:386-8. [IDIS 257833] [PubMed 2501683]

4. Echt DC, Liebson PR, Mitchell LB et al. Mortality and morbidity in patients receiving encainide, flecainide, or placebo: the Cardiac Arrhythmia Suppression Trial. N Engl J Med. 1991; 324:781-8. [IDIS 279004] [PubMed 1900101]

5. Food and Drug Administration. Enkaid and Tambocor use in non-life-threatening arrhythmias halted. FDA Talk Paper. Rockville, MD: Food and Drug Administration; 1989 Apr 25.

6. Department of Health and Human Services. Background statement regarding encainide, flecainide, and moricizine. Bethesda, MD: National Institutes of Health, National Heart, Lung, and Blood Institute; 1989 Apr.

7. The Cardiac Arrhythmia Suppression Trial II investigators. Effect of the antiarrhythmic agent moricizine on survival after myocardial infarction. N Engl J Med. 1992; 327:227-33. [IDIS 299111] [PubMed 1377359]

8. Kowey PR. Pharmacological Effects of Antiarrhythmic Drug: Review and Update. Arch Intern Med. 1998; 158: 325-32. [IDIS 401793] [PubMed 9487229]

9. Kowey PR, Marinchak RA, Rials SJ et al. Classification and pharmacology of antiarrhythmic drugs. Am Heart J. 2000;140: 12-20.

10. . Fenster PE, Comess KA. Pharmacology and clinical use of mexiletine. Pharmacotherapy. 1986; 6:1-9. [IDIS 394809] [PubMed 3513138]

11. Campbell RWF. Mexiletine. N Engl J Med. 1987; 316:29-34. [IDIS 223853] [PubMed 3537793]

12. Monk JP, Brogden RN. Mexiletine: a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in the treatment of arrhythmias. Drugs. 1990; 40:374-411. [PubMed 2226221]

13. Mexiletine for arrhythmias. Med Lett Drugs Ther. 1986; 28:65-6.

14. Masotti G, Morettini A, Casolo GC et al. Efficacy of mexiletine in the medium-term treatment of ventricular arrhythmias: a randomized, double-blind, crossover trial against placebo in ambulatory patients. J Int Med Res. 1984; 12:73-80. [PubMed 6202571]

15. Singh JB, Rasul AM, Shah A et al. Efficacy of mexiletine in chronic ventricular arrhythmias compared with quinidine: a single-blind, randomized trial. Am J Cardiol. 1984; 53: 84-7. [IDIS 179626] [PubMed 6362388]

16. Mason JW, for the Electrophysiologic Study versus Electrocardiographic Monitoring Investigators. A comparison of seven antiarrhythmic drugs in patients with ventricular tachyarrhythmias. N Engl J Med. 1993; 329:452-8. [IDIS 318403] [PubMed 8332150]

17. Assey ME, Hudson WM, Hanger KH et al. Comparative study of mexiletine and quinidine in the treatment of ventricular ectopia. South Med J. 1985; 78:565-8. [IDIS 199952] [PubMed 2581322]

18. Frank MJ, Watkins LO, Prisant LM et al. Mexiletine versus quinidine as first-line antiarrhythmia therapy: results from consecutive trials. J Clin Pharmacol. 1991; 31:222-8. [IDIS 279188] [PubMed 2019663]

19. Rutledge JC, Harris F, Amsterdam EA et al. Clinical evaluation of oral mexiletine therapy in the treatment of ventricular arrhythmias. J Am Coll Cardiol. 1985; 6:780-4. [PubMed 4031292]

20. Kerin NZ, Aragon E, Marinescu G et al. Mexiletine: long-term efficacy and side effects in patients with chronic drug-resistant potentially lethal ventricular arrhythmias. Arch Intern Med. 1990; 150:381-4. [IDIS 263330] [PubMed 2302013]

21. Woosley RL, Wang T, Stone W et al. Pharmacology, electrophysiology, and pharmacokinetics of mexiletine. Am Heart J. 1984; 107:1058-65. [IDIS 184957] [PubMed 6326558]

22. Solvay Pharmaceuticals. Luvox (fluvoxamine maleate) tablets prescribing information. Marietta, GA; 2001 Jun.

23. Abbott Laboratories. Norvir (ritonavir) capsules and oral solution prescribing information (dated 2001 Sep). In: Physicians’ desk reference. 57th ed. Montvale, NJ: Medical Economics Company Inc; 2003:482-9.

24. AstraZeneca. EMLA Cream and Anesthetic Disc (lidocaine 2.5% and prilocaine 2.5% cream) prescribing information (dated 2002 Feb). In: Physicians’ desk reference. 57th ed. Montvale, NJ: Medical Economics Company Inc; 2003:599-602.

25. Aventis. Priftin (rifapentine) tablets prescribing information. In: Physicians’ desk reference. 57th ed. Montvale, NJ: Medical Economics Company Inc; 2003:753-6.

26. National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK). Diabetic Neuropathies: the nerve damage of diabetes. From NIDDK website () 2003 Apr 2.

27. Russell D, Stading J. Diabetic Peripheral Neuropathy: minimizing and treating its pain. US Pharmacist. 2002; 27:56-67.

28. Galer BS. Neuropathic pain of peripheral origin: advances in pharmacologic treatment. Neurology. 1995; 45(Suppl 9):S17-25. [IDIS 360673] [PubMed 8538882]

29. Oskarsson P, Ljunggren JG, Lins PE et al. Efficacy and safety of mexiletine in the treatment of painful diabetic neuropathy. Diabetes Care. 1997; 20:1594-7. [IDIS 393128] [PubMed 9314641]

30. Dejgard A, Petersen P, Kastrup J. Mexiletine for treatment of chronic painful diabetic neuropathy. Lancet. 1988; 1:9-11. [IDIS 237595] [PubMed 2891940]

31. Stracke H, Meyer UE, Schumacher HE et al. Mexiletine in the treatment of diabetic neuropathy. Diabetes Care. 1992; 15:1550-5. [PubMed 1468285]

32. Wright JM, Oki JC, Graves L 3rd. Mexiletine in the symptomatic treatment of diabetic peripheral neuropathy. Ann Pharmacother. 1997; 31:116-7. [IDIS 377886] [PubMed 8997478]

33. Hine LK, Laird NM, Hewitt P et al. Meta-analysis of empirical long-term antiarrhythmic therapy after myocardial infarction. JAMA. 1989; 262:3037-40. [IDIS 260965] [PubMed 2509746]

34. Watson. Mexiletine hydrochloride capsules prescribing information. Corona, CA; 2000 May.

35. Vaughan Williams EM. A classification of antiarrhythmic actions reassessed after a decade of new drugs. J Clin Pharmacol. 1984; 24:129-47. [IDIS 186026] [PubMed 6144698]

36. Harrison DC. Antiarrhythmic drug classification: new science and practical applications. Am J Cardiol. 1985; 56:185-7. [PubMed 2409789]

37. Campbell TJ. Kinetics of onset of rate-dependent effects of class I antiarrhythmic drugs are important in determining their effects on refractoriness in guinea-pig ventricle, and provide a theoretical basis for their subclassification. Cardiovasc Res. 1983; 17:344-52. [PubMed 6883410]

38. Harrison DC. Current classification of antiarrhythmic drugs as a guide to their rational clinical use. Drugs. 1986; 31:93-5. [IDIS 212454] [PubMed 3948737]

39. Jarvis B, Coukell AJ. Mexiletine: a review of its therapeutic use in painful diabetic neuropathy. Drugs. 1998; 56:691-707. [PubMed 9806111]

40. Anon. Drugs for cardiac arrhythmias. Med Lett Drugs Ther. 1989; 31:35-40. [PubMed 2565011]

41. Teo KK, Yusuf S, Furberg CD. Effects of prophylactic antiarrhythmic drug therapy in acute myocardial infarction. JAMA. 1993; 270:1589-95. [IDIS 320343] [PubMed 8371471]

42. Pratt CM, Moye L. The Cardiac Arrhythmia Suppression Trial: implications for antiarrhythmic drug development. J Clin Pharmacol. 1990; 30:967-74. [IDIS 274583] [PubMed 2122983]

43. The American Heart Association in Collaboration with the International Liaison Committee on Resuscitation. Guidelines 2000 for cardiopulmonary resuscitation and emergency cardiovascular care. Part 6: Advanced cardiovascular life support. Circulation. 2000; 102(Suppl I): I-86-171.

44. Reviewers’ comments (personal observations).

45. Vinik AI. Diagnosis and management of diabetic neuropathy. Clin Geriatr Med. 1999; 2:293-320.

46. Guay DRP.Adjunctive agents in the management of chronic pain. Pharmacotherapy. 2001; 9: 1070-81.

47. Boehringer Ingelheim Pharmaceuticals, Inc. Ridgefield, CT: Personal communication.

49. Barr Laboratories, Inc. Fluvoxamine maleate tablets prescribing information. Pomona, NY; 2005 Jan.

50. Kusumoto M, Ueno K, Oda A et al. Effect of fluvoxamine on the pharmacokinetics of mexiletine in healthy Japanese men. Clin Pharmacol Ther. 2001; 69:104-7. [IDIS 461192] [PubMed 11240973]

a. Libersa C, Caron J, Broly F et al. Interaction of propafenone and mexiletine. J Am Coll Cardiol. 1993; 22:2061. [PubMed 8245368]

b. Yeung-Lai-Wah JA, Murdock CJ, Boone J et al. Propafenone-mexiletine combination for the treatment of sustained ventricular tachycardia. J Am Coll Cardiol. 1992; 20:547-51.

More Mexitil resources

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

• Mexitil Prescribing Information (FDA)


• Mexitil MedFacts Consumer Leaflet (Wolters Kluwer)


• Mexitil Concise Consumer Information (Cerner Multum)


• Mexitil Advanced Consumer (Micromedex) - Includes Dosage Information


• Mexiletine Prescribing Information (FDA)

Compare Mexitil with other medications

• Arrhythmia
• Diabetic Nerve Damage
• Ventricular Tachycardia

FA-8

Pronunciation: FOE-lik ASS-id
Generic Name: Folic Acid
Brand Name: FA-8

FA-8 is used for:

Treating certain types of anemia. It may also be used for other conditions as determined by your doctor.

FA-8 is a vitamin. It works by helping the body to produce blood cells.

Do NOT use FA-8 if:

• you are allergic to any ingredient in FA-8

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

Before using FA-8:

Some medical conditions may interact with FA-8. 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 a long-term infection, seizure disorder (eg, epilepsy), or liver problems (eg, alcoholic cirrhosis), or if you are on kidney dialysis


• if you drink alcohol regularly


• if you have other types of anemia (eg, anemia due to low vitamin B₁₂ levels)

Some MEDICINES MAY INTERACT with FA-8. Tell your health care provider if you are taking any other medicines, especially any of the following:

• Fluorouracil because its actions and side effects may be increased by FA-8


• Hydantoins (eg, phenytoin) because their effectiveness may be decreased by FA-8


• Barbiturates (eg, phenobarbital), methotrexate, nitrofurantoin, phenytoin, primidone, or pyrimethamine because the effectiveness of FA-8 may be decreased

This may not be a complete list of all interactions that may occur. Ask your health care provider if FA-8 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 FA-8:

Use FA-8 as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• FA-8 may be taken with or without food.


• If you miss a dose of FA-8, 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 FA-8.

Important safety information:

• Check any other vitamin products you may be taking for folic acid content. Tell your doctor or pharmacist if any other medicines that you take contain folic acid.


• LAB TESTS, including red blood cell counts, may be performed to monitor your progress or to check for side effects. Be sure to keep all doctor and lab appointments.

Possible side effects of FA-8:

All medicines may cause side effects, but many people have no, or minor, side effects. When used in small doses, no COMMON side effects have been reported with this product. Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue).

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: FA-8 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 FA-8:

Store FA-8 at room temperature, between 59 and 86 degrees F (15 and 30 degrees C). Store away from heat, moisture, and light. Do not store in the bathroom. Keep FA-8 out of the reach of children and away from pets.

General information:

• If you have any questions about FA-8, please talk with your doctor, pharmacist, or other health care provider.


• FA-8 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 FA-8. 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 FA-8 resources

• FA-8 Side Effects (in more detail)
• FA-8 Use in Pregnancy & Breastfeeding
• FA-8 Drug Interactions
• FA-8 Support Group
• 0 Reviews for FA-8 - Add your own review/rating

• FA-8 Advanced Consumer (Micromedex) - Includes Dosage Information


• FA-8 Concise Consumer Information (Cerner Multum)


• Folic Acid Prescribing Information (FDA)


• Folic Acid Professional Patient Advice (Wolters Kluwer)


• Folic Acid Monograph (AHFS DI)

Compare FA-8 with other medications

• Anemia, Megaloblastic
• Folic Acid Deficiency
• Vitamin/Mineral Supplementation and Deficiency

Shark Cartilage

Pronunciation: Not applicable.
Generic Name: Shark Cartilage
Brand Name: Generics only. No brands available.

Shark Cartilage is used for:

An addition to cancer therapy to lessen pain and improve appetite. Shark cartilage is also claimed to be useful in psoriasis and arthritis. It may also have other uses. Check with your pharmacist for more details regarding the particular brand you use.

Shark Cartilage is finely ground cartilage from sharks. It is thought to work by providing a protein substance that blocks new blood networks from forming. Tumors and certain other diseases are dependent on new blood networks.

Do NOT use Shark Cartilage if:

• you are allergic to any ingredient in Shark Cartilage

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

Before using Shark Cartilage:

Some medical conditions may interact with Shark Cartilage. 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 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 high calcium levels in the blood or a history of liver disease

Some MEDICINES MAY INTERACT with Shark Cartilage. However, no specific interactions are known at this time.

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

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

• Dosing depends on the use and the source of the product.


• Use as directed on the package, unless instructed otherwise by your doctor.


• If you miss taking a dose of Shark Cartilage for 1 or more days, there is no cause for concern. If your doctor recommended that you take it, try to remember your dose every day.

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

Important safety information:

• Check with your doctor before you begin taking any new medicine, either prescription or over-the-counter.


• This product has not been approved by the Food and Drug Administration (FDA) as safe and effective for any medical condition. The long-term safety of dietary supplements is not known. Before using any alternative medicine, talk with your doctor or pharmacist.


• Keep all doctor and laboratory appointments while taking Shark Cartilage.


• PREGNANCY and BREAST-FEEDING: Do not take this product if you are pregnant. Do not breast-feed while taking this product.

Possible side effects of Shark Cartilage:

All medicines may cause side effects, but many people have no, or minor, side effects. 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); behavior changes; hyperactivity; severe mood swings or unusual irritability.

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: Shark Cartilage 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 Shark Cartilage:

Store at room temperature away from heat, moisture, and light unless otherwise directed on the package label. Do not store in the bathroom. Most dietary supplements are not in childproof containers. Keep Shark Cartilage out of the reach of children and away from pets.

General information:

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


• Shark Cartilage 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 Shark Cartilage. 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 Shark Cartilage resources

• Shark Cartilage Side Effects (in more detail)
• Shark Cartilage Use in Pregnancy & Breastfeeding
• Shark Cartilage Support Group
• 0 Reviews for Shark Cartilage - Add your own review/rating

Compare Shark Cartilage with other medications

• Herbal Supplementation

flecainide

Generic Name: flecainide (FLEK a nide)

Brand Names: Tambocor

What is flecainide?

Flecainide is in a group of drugs called Class IC anti-arrhythmics. It affects the way your heart beats.

Flecainide is used in certain situations to prevent serious heart rhythm disorders.

Flecainide may also be used for other purposes not listed in this medication guide.

What is the most important information I should know about flecainide?

You should not use this medication if you are allergic to flecainide, or if you have certain heart conditions, especially "AV block" (unless you have a pacemaker).

Before using flecainide, tell your doctor if you have congestive heart failure, a heart condition called "sick sinus syndrome," an electrolyte imbalance, liver disease, kidney disease, if you have a pacemaker, or if you have had a heart attack within the past 2 years.

You will need to receive your first few doses of flecainide in a hospital setting in case the medication causes serious side effects. Your heart rate will be constantly monitored using an electrocardiograph or ECG (sometimes called an EKG). This machine measures electrical activity of the heart. Call your doctor at once if you have a serious side effect such as weak pulse, slow breathing, fast or uneven heartbeat, feeling like you might pass out, feeling short of breath, swelling, rapid weight gain, confusion, extreme thirst, increased urination, muscle weakness, or jaundice (yellowing of the skin or eyes).

What should I discuss with my healthcare provider before taking flecainide?

You should not use this medication if you are allergic to flecainide, or if you have certain heart conditions, especially "AV block" (unless you have a pacemaker).

Before using flecainide, tell your doctor if you are allergic to any drugs, or if you have:

• 
  

  congestive heart failure;

  
  


• 
  

  a heart condition called "sick sinus syndrome";

  
  


• 
  

  an electrolyte imbalance;

  
  


• 
  

  liver disease;

  
  


• 
  

  kidney disease;

  
  


• 
  

  if you have a pacemaker; or

  
  


• 
  

  if you have had a heart attack within the past 2 years.

  
  

If you have any of these conditions, you may need a dose adjustment or special tests to safely use flecainide.

FDA pregnancy category C. This medication may be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. Flecainide can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

How should I take flecainide?

You will need to receive your first few doses of flecainide in a hospital setting in case the medication causes serious side effects. Your heart rate will be constantly monitored using an electrocardiograph or ECG (sometimes called an EKG). This machine measures electrical activity of the heart.

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

Your doctor may occasionally change your dose to make sure you get the best results from this medication.

To be sure this medication is helping your condition, your blood may need to be tested on a regular basis. Do not miss any scheduled appointments.

Store flecainide at room temperature away from moisture, heat, and light.

See also: Flecainide dosage (in more detail)

What happens if I miss a dose?

Take the missed dose as soon as you remember. If it is almost time for your next dose, wait until then to take the medicine and skip the missed dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention if you think you have used too much of this medicine.

Overdose symptoms may include nausea, vomiting, slow heart rate, feeling like you might pass out, or seizure (convulsions).

What should I avoid while taking flecainide?

Follow your doctor's instructions about any restrictions on food, beverages, or activity while you are using flecainide.

Flecainide 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. Call your doctor at once if you have a serious side effect such as:

• 
  

  slow heart rate, weak pulse, fainting, slow breathing (breathing may stop);

  
  


• 
  

  dizziness, fainting, fast or pounding heartbeat;

  
  


• 
  

  feeling short of breath, even with mild exertion;

  
  


• 
  

  swelling, rapid weight gain;

  
  


• 
  

  low potassium (confusion, uneven heart rate, extreme thirst, increased urination, leg discomfort, muscle weakness or limp feeling);

  
  


• 
  

  high potassium (slow heart rate, weak pulse, muscle weakness, tingly feeling);

  
  


• 
  

  pale skin, easy bruising or bleeding, unusual weakness; or

  
  


• 
  

  jaundice (yellowing of the skin or eyes).

  
  

Less serious side effects may include:

• 
  

  dizziness;

  
  


• 
  

  tremor or shaking;

  
  


• 
  

  headache;

  
  


• 
  

  anxiety or depression;

  
  


• 
  

  vision problems;

  
  


• 
  

  nausea, vomiting, stomach pain;

  
  


• 
  

  diarrhea, constipation; or

  
  


• 
  

  numbness or tingling.

  
  

This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect. You may report side effects to FDA at 1-800-FDA-1088.

Flecainide Dosing Information

Usual Adult Dose for Ventricular Tachycardia:

Initial dose: 100 mg orally every 12 hours.
Maintenance dose: May be increased in increments of 50 mg bid every 4 days until efficacy is achieved. Most patients with SUSTAINED VT do not require more than 150 mg every 12 hours (300 mg/day), and the maximum dose recommended is 400 mg/day.

Usual Adult Dose for Atrial Fibrillation:

Initial dose: 50 mg orally every 12 hours.
Maintenance dose: May be increased in increments of 50 mg bid every 4 days until efficacy is achieved.

Usual Adult Dose for Atrial Flutter:

Initial dose: 50 mg orally every 12 hours.
Maintenance dose: May be increased in increments of 50 mg bid every 4 days until efficacy is achieved.

Usual Adult Dose for Wolff-Parkinson-White Syndrome:

Initial dose: 50 mg orally every 12 hours.
Maintenance dose: May be increased in increments of 50 mg bid every 4 days until efficacy is achieved.

Usual Adult Dose for Paroxysmal Supraventricular Tachycardia:

Initial dose: 50 mg orally every 12 hours.
Maintenance dose: May be increased in increments of 50 mg bid every 4 days until efficacy is achieved.

Usual Pediatric Dose for Supraventricular Tachycardia:

less than 1 month:
Supraventricular tachycardia: Limited data available: Initial: 2 mg/kg/day orally divided every 12 hours; titrate to clinical response, monitor serum concentration; mean dose required to suppress SVT: 3.35 ± 1.35 mg/kg/day in 17 neonates (n=20 treated neonates; mean PNA: 11.5 days; mean GA: 36.8 weeks; mean birthweight: 2.8 kg); study did not report resultant serum concentrations.

1 month or older:
Initial: 1 to 3 mg/kg/day orally or 50 to 100 mg/m2/day orally in 3 divided doses; usual: 3 to 6 mg/kg/day or 100 to 150 mg/m2/day in 3 divided doses; up to 8 mg/kg/day or 200 mg/m2/day for uncontrolled patients with subtherapeutic levels; higher doses have been reported, however they may be associated with an increased risk of proarrhythmias; a review of world literature reports the average effective dose to be 4 mg/kg/day or 140 mg/m2/day.

What other drugs will affect flecainide?

Before taking flecainide, tell your doctor if you are taking any of the following medicines:

• 
  

  cimetidine (Tagamet),

  
  


• 
  

  digoxin (digitalis, Lanoxin);

  
  


• 
  

  a diuretic (water pill);

  
  


• 
  

  verapamil (Verelan, Calan, Isoptin);

  
  


• 
  

  seizure medication such as carbamazepine (Carbatrol, Tegretol), phenobarbital (Solfoton), or phenytoin (Dilantin);

  
  


• 
  

  other heart rhythm medications such as amiodarone (Cordarone), disopyramide (Norpace), or quinidine (Quinaglute, Quinidex); or

  
  


• 
  

  a beta-blocker such as atenolol (Tenormin), labetalol (Normodyne, Trandate), metoprolol (Lopressor, Toprol), propranolol (Inderal, InnoPran), sotalol (Betapace), timolol (Blocadren), and others.

  
  

This list is not complete and there may be other drugs that can interact with flecainide. Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start a new medication without telling your doctor.

More flecainide resources

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

• flecainide Advanced Consumer (Micromedex) - Includes Dosage Information


• Flecainide MedFacts Consumer Leaflet (Wolters Kluwer)


• Flecainide Prescribing Information (FDA)


• Flecainide Acetate Monograph (AHFS DI)


• Tambocor Prescribing Information (FDA)

Compare flecainide with other medications

• Atrial Fibrillation
• Atrial Flutter
• Paroxysmal Supraventricular Tachycardia
• Supraventricular Tachycardia
• Ventricular Tachycardia
• Wolff-Parkinson-White Syndrome

Where can I get more information?

• Your pharmacist can provide more information about flecainide.

See also: flecainide side effects (in more detail)