Trospium Chloride

Class: Genitourinary Smooth Muscle Relaxants
VA Class: GU201
Chemical Name: spiro[8-azoniabicyclo[3,2,1]octane-8,1’-pyrrolidinium]-3-[(hydroxydiphenyl-acetyl)- oxy]chloride,(1α, 3β, 5α)
Molecular Formula: C₂₅H₃₀C_lNO₃
CAS Number: 10405-02-4
Brands: Sanctura

Introduction

Genitourinary antispasmodic; quaternary ammonium antimuscarinic.^{1 3}

Uses for Trospium Chloride

Overactive Bladder

Management of overactive bladder for the relief of symptoms associated with voiding (e.g., urge urinary incontinence, urgency, frequency).^{1 3 5}

Appears to be as effective as immediate-release preparations of oxybutynin or tolterodine in decreasing urinary frequency;^{2 4 5 6} may be more effective than immediate-release preparations of tolterodine in decreasing urgency incontinence.^{5 6}

May offer no advantage over extended-release anticholinergic preparations for the treatment of overactive bladder.³

Trospium Chloride Dosage and Administration

Administration

Oral Administration

Administer orally twice daily, at least 1 hour before meals or on an empty stomach.¹

Dosage

Available as trospium chloride; dosage expressed in terms of the salt.¹

Adults

Overactive Bladder

Oral

20 mg twice daily.¹

Special Populations

Hepatic Impairment

Use caution in patients with moderate or severe hepatic impairment.¹ (See Special Populations under Pharmacokinetics.)

Renal Impairment

In patients with severe renal impairment (Cl_cr <30 mL/minute), decrease dosage to 20 mg once daily at bedtime.¹

Geriatric Patients

In geriatric patients ≥75 years of age, may decrease dosage to 20 mg once daily based on patient tolerance.¹ (See Geriatric Use under Cautions.)

Cautions for Trospium Chloride

Contraindications

• 
  

  Presence or risk of urinary retention.¹

  
  


• 
  

  Presence or risk of gastric retention.¹

  
  


• 
  

  Presence or risk of risk of uncontrolled angle-closure glaucoma.¹

  
  


• 
  

  Known hypersensitivity to trospium or any ingredient in the formulation.¹

  
  

Warnings/Precautions

General Precautions

Urinary Retention

Risk of urinary retention; use with caution in patients with clinically important bladder outflow obstruction.¹

Decreased GI Motility

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

May decrease GI motility; use with caution in patents with ulcerative colitis, intestinal atony, or myasthenia gravis.¹

Controlled Angle-closure Glaucoma

Use only if potential benefits outweigh the risks; use with caution and monitor carefully.¹

Specific Populations

Pregnancy

Category C.¹

Lactation

Distributed into milk in rats; not known whether distributed into human milk.¹ Use with caution and only if potential benefit justifies the risk to the infant.¹

Pediatric Use

Safety and efficacy not established.¹

Geriatric Use

In patients ≥75 years of age, possible increased incidence of adverse anticholinergic effects compared with younger adults.¹ (See Geriatric Patients under Dosage and Administration.)

Hepatic Impairment

Use with caution in patients with moderate or severe hepatic impairment.¹ (See Special Populations under Pharmacokinetics.)

Renal Impairment

Dosage reduction necessary in patients with severe renal impairment (Cl_cr<30 mL/per minute); not studied in patients with mild or moderate renal impairment¹ (See Renal Impairment under Dosage and Administration and see Special Populations under Pharmacokinetics.) ¹

Common Adverse Effects

Dry mouth,^{1 2 3} constipation.^{1 2}

Interactions for Trospium Chloride

Minimally metabolized by CYP isoenzymes; does not inhibit CYP1A2, 3A4, 2A6, 2C9, 2C19, 2D6, or 2E1 in vitro.^{1 2 7} Pharmacokinetic interactions unlikely with drugs metabolized by CYP isoenzymes or with CYP enzyme inducers or inhibitors.^{1 2 7}

Drugs Eliminated by Active Tubular Secretion

Possible competition for renal secretion, decreased renal elimination, and increased serum concentrations of trospium and/or other drug.¹ Use concomitantly with caution; monitor carefully.¹

Drugs Affected by GI Motility

Potential for altered absorption because of decreased GI motility.¹

Specific Drugs

Drug	Interaction	Comment
Alcohol	Potential for additive sedative effects1
Anticholinergic agents	Potential for additive anticholinergic effects1
Digoxin	Potential for decreased renal elimination and increased serum concentrations of trospium and/or digoxin1 3	Use concomitantly with caution; monitor carefully1
Metformin	Potential decreased renal elimination and increased serum concentrations of trospium and/or metformin1 3	Use concomitantly with caution; monitor carefully1
Morphine	Potential for decreased renal elimination and increased serum concentrations of trospium and/or morphine 1 3	Use concomitantly with caution; monitor carefully1
Pancuronium	Potential for decreased renal elimination and increased serum concentrations of trospium and/or pancuronium1	Use concomitantly with caution; monitor carefully1
Procainamide	Potential for decreased renal elimination and increased serum concentrations of trospium and/or procainamide1 3	Use concomitantly with caution; monitor carefully1
Tenofovir	Potential for decreased renal elimination and increased serum concentrations of trospium and/or tenofovir1	Use concomitantly with caution; monitor carefully1
Vancomycin	Potential for decreased renal elimination and increased serum concentrations of trospium and/or vancomycin1	Use concomitantly with caution; monitor carefully1

Trospium Chloride Pharmacokinetics

Absorption

Bioavailability

Absorption from GI tract is incomplete.^{1 3 5 7}

Mean absolute oral bioavailability is about 9.6%.¹

Food

High-fat meal reduces AUC and peak plasma concentrations by about 70–80%.^{1 3}

Distribution

Extent

In blood, plasma to whole blood ratio is 1.6 to 1.¹

Hydrophilic; theoretically should not cross the blood-brain barrier.^{5 7}

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

Plasma Protein Binding

50–85%.¹

Elimination

Metabolism

Metabolism not fully elucidated;^{1 2 7} major pathway may be ester hydrolysis and subsequent glucuronidation to form inactive metabolites.^{1 7} Minimally metabolized by CYP isoenzymes.^{1 2 7}

Elimination Route

Excreted principally in feces (about 85%) and in urine (5.8%), mainly as unchanged drug.^{1 2 3 5 7}

Active tubular secretion is a major elimination route.¹

Half-life

About 20 hours.^{1 7}

Special Populations

In patients with severe renal impairment (Cl_cr<30 mL/per minute), peak plasma concentrations and AUC increased 2-fold and 4.5-fold, respectively, and an additional elimination phase (half-life of about 33 hours) occurred.^{1 7}

In patients with mild or moderate hepatic impairment, peak plasma concentrations increased (12 or 63%, respectively); AUC was similarly increased.¹

Stability

Storage

Oral

Tablets

20–25°C.¹

ActionsActions

• 
  

  Antagonizes acetylcholine at muscarinic receptors in cholinergically innervated organs.^{1 3 5}

  
  


• 
  

  Parasympatholytic action reduces the tonus of smooth muscle in the urinary bladder.^{1 3}

  
  


• 
  

  Increases maximum cystometric capacity and volume at first detrusor contraction in patients with involuntary detrusor contractions.^{1 5}

  
  


• 
  

  Little or no affinity for nicotinic receptors compared with muscarinic receptors at concentrations achieved following usual therapeutic doses.^{1 7}

  
  

Advice to Patients

• 
  

  Importance of informing patients of potential adverse anticholinergic effects (e.g., dizziness, blurred vision, heat prostration when used in a hot environment).¹

  
  


• 
  

  Importance of taking trospium chloride on an empty stomach or at least 1 hour before meals, and if a dose is skipped, taking the next scheduled dose at least 1 hour before the next meal.¹

  
  


• 
  

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

  
  


• 
  

  Importance of using alcohol with caution, since it may enhance drowsiness caused by trospium.¹

  
  


• 
  

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

  
  


• 
  

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

  
  

Preparations

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

Trospium Chloride

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets	20 mg	Sanctura	Odyssey

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.

Sanctura 20MG Tablets (ALLERGAN DERMATOLOGICS): 30/$85.94 or 90/$242.47

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 October 2005. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Odyssey Pharmaceuticals. Sanctura™ (trospium chloride) tablets prescribing information. East Hanover, NJ; 2004. From Sanctura website (http://www.sanctura.com/Sanctura_Prescribing_Information.pdf).

2. Zinner N, Gittelman M, Harris R et al. Trospium chloride improves overactive bladder symptoms: a multicenter phase II trial. J Urol. 2004; 171:2311-5. [IDIS 519949] [PubMed 15126811]

3. Anon. Trospium Chloride (Sanctura): Another anticholinergic for overactive bladder. Med Lett Drugs Ther. 2004; 46:63-4. [PubMed 15289745]

4. Halaska M, Ralph G, Wiedemann A et al. Controlled, double-blind, multicentre clinical trial to investigate long-term tolerability and efficacy of trospium chloride in patients with detrusor instability. World J Urol. 2003; 20:392-9. [IDIS 519866] [PubMed 12811500]

5. Hashim H, Abrams P. Drug treatment of overactive bladder. Efficacy, cost and quality-of-life considerations. Drugs. 2004; 64:1643-56. [PubMed 15257626]

6. UK Medicines Information Pharmacists Group. Trospium. New Medicines on the market. Evaluated Information for the NHS. 2002 Feb. From UKMi website (http://www.ukmi.nhs.uk/NewMaterial/html/docs/trospium.pdf)

7. Rovner ES. Trospium chloride in the management of overactive bladder. Drugs. 2004; 64:2433-2446. [PubMed 15482001]

More Trospium Chloride resources

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

• Sanctura Prescribing Information (FDA)


• Sanctura Advanced Consumer (Micromedex) - Includes Dosage Information


• Sanctura Consumer Overview


• Sanctura MedFacts Consumer Leaflet (Wolters Kluwer)


• Sanctura XR Prescribing Information (FDA)


• Sanctura XR Extended-Release Capsules MedFacts Consumer Leaflet (Wolters Kluwer)

Compare Trospium Chloride with other medications

• Interstitial Cystitis
• Overactive Bladder
• Urinary Incontinence

Sotacor Tablets

1. Name Of The Medicinal Product

SOTACOR 80 MG TABLETS

2. Qualitative And Quantitative Composition

Each tablet contains 80mg sotalol hydrochloride.

Excipient: Each tablet contains 53.8 mg of lactose (as lactose monohydrate)

For a full list of excipients, see section 6.1.

3. Pharmaceutical Form

Tablets

Round, biconvex, white tablets with a break bar on each side..

The tablet can be divided into equal halves.

4. Clinical Particulars

4.1 Therapeutic Indications

SOTACOR tablets are indicated for:

Ventricular arrhythmias:

- Treatment of life-threatening ventricular tachyarrhythmias;

- Treatment of symptomatic non-sustained ventricular tachyarrhythmias;

Supraventricular arrhythmias:

- Prophylaxis of paroxysmal atrial tachycardia, paroxysmal atrial fibrillation, paroxysmal A-V nodal re-entrant tachycardia, paroxysmal A-V re-entrant tachycardia using accessory pathways, and paroxysmal supraventricular tachycardia after cardiac surgery;

- Maintenance of normal sinus rhythm following conversion of atrial fibrillation or atrial flutter.

4.2 Posology And Method Of Administration

The initiation of treatment or changes in dosage with SOTACOR should follow an appropriate medical evaluation including ECG control with measurement of the corrected QT interval, and assessment of renal function, electrolyte balance, and concomitant medications (see section 4.4 Special warnings and precautions).

As with other antiarrhythmic agents, it is recommended that SOTACOR be initiated and doses increased in a facility capable of monitoring and assessing cardiac rhythm. The dosage must be individualized and based on the patient's response. Proarrhythmic events can occur not only at initiation of therapy, but also with each upward dosage adjustment.

In view of its β-adrenergic blocking properties, treatment with SOTACOR should not be discontinued suddenly, especially in patients with ischaemic heart disease (angina pectoris, prior acute myocardial infarction) or hypertension, to prevent exacerbation of the disease (see section 4.4 Special warnings and precautions).

The following dosing schedule can be recommended:

The initial dose is 80 mg, administered either singly or as two divided doses.

Oral dosage of SOTACOR should be adjusted gradually allowing 2-3 days between dosing increments in order to attain steady-state, and to allow monitoring of QT intervals. Most patients respond to a daily dose of 160 to 320 mg administered in two divided doses at approximately 12 hour intervals. Some patients with life-threatening refractory ventricular arrhythmias may require doses as high as 480 - 640 mg/day. These doses should be used under specialist supervision and should only be prescribed when the potential benefit outweighs the increased risk of adverse events, particularly proarrhythmias (see section 4.4 Special warnings and precautions).

Children

SOTACOR is not intended for administration to children.

Dosage in renally impaired patients

Because SOTACOR is excreted mainly in urine, the dosage should be reduced when the creatinine clearance is less than 60 ml/min according to the following table:

Creatinine clearance (ml/min)	Adjusted doses
> 60	Recommended SOTACOR Dose
30-60	½ recommended SOTACOR Dose
10-30	¼ recommended SOTACOR Dose
< 10	Avoid

The creatinine clearance can be estimated from serum creatinine by the Cockroft and Gault formula:

When serum creatinine is given in µmol/l, divide the value by 88.4 (1mg/dl = 88.4 µmol/l).

Dosage in hepatically impaired patients

No dosage adjustment is required in hepatically impaired patients.

4.3 Contraindications

SOTACOR should not be used where there is evidence of sick sinus syndrome; second and third degree AV heart block unless a functioning pacemaker is present; congenital or acquired long QT syndromes; torsades de pointes; symptomatic sinus bradycardia; uncontrolled congestive heart failure; cardiogenic shock; anaesthesia that produces myocardial depression; untreated phaeochromocytoma; hypotension (except due to arrhythmia); Raynaud's phenomenon and severe peripheral circulatory disturbances; history of chronic obstructive airway disease or bronchial asthma (a warning will appear on the label); hypersensitivity to any of the components of the formulation; metabolic acidosis; renal failure (creatinine clearance < 10 ml/min).

4.4 Special Warnings And Precautions For Use

Abrupt Withdrawal Hypersensitivity to catecholamines is observed in patients withdrawn from beta-blocker therapy. Occasional cases of exacerbation of angina pectoris, arrhythmias, and in some cases, myocardial infarction have been reported after abrupt discontinuation of therapy. Patients should be carefully monitored when discontinuing chronically administered SOTACOR, particularly those with ischaemic heart disease. If possible the dosage should be gradually reduced over a period of one to two weeks, if necessary at the same time initiating replacement therapy. Abrupt discontinuation may unmask latent coronary insufficiency. In addition, hypertension may develop.

Proarrhythmia The most dangerous adverse effect of Class I and Class III antiarrhythmic drugs (such as sotalol) is the aggravation of pre-existing arrhythmias or the provocation of new arrhythmias. Drugs that prolong the QT-interval may cause torsades de pointes, a polymorphic ventricular tachycardia associated with prolongation of the QT-interval. Experience to date indicates that the risk of torsades de pointes is associated with the prolongation of the QT-interval, reduction of the heart rate, reduction in serum potassium and magnesium, high plasma sotalol concentrations and with the concomitant use of sotalol and other medications which have been associated with torsades de pointes (see section 4.5 Interactions with other medicinal products). Females may be at increased risk of developing torsades de pointes.

The incidence of torsades de pointes is dose dependent. Torsades de pointes usually occurs within 7 days of initiating therapy or escalation of the dose and can progress to ventricular fibrillation.

In clinical trials of patients with sustained VT/VF the incidence of severe proarrhythmia (torsades de pointes or new sustained VT/VF) was <2% at doses up to 320 mg. The incidence more than doubled at higher doses.

Other risk factors for torsades de pointes were excessive prolongation of the QT_C and history of cardiomegaly or congestive heart failure. Patients with sustained ventricular tachycardia and a history of congestive heart failure have the highest risk of serious proarrhythmia (7%).

Proarrhythmic events must be anticipated not only on initiating therapy but with every upward dose adjustment. Initiating therapy at 80 mg with gradual upward dose titration thereafter reduces the risk of proarrhythmia. In patients already receiving SOTACOR caution should be used if the QT_C exceeds 500msec whilst on therapy, and serious consideration should be given to reducing the dose or discontinuing therapy when the QT_C-interval exceeds 550 msec. Due to the multiple risk factors associated with torsades de pointes, however, caution should be exercised regardless of the QT_C-interval.

Electrolyte Disturbances SOTACOR should not be used in patients with hypokalaemia or hypomagnesaemia prior to correction of imbalance; these conditions can exaggerate the degree of QT prolongation, and increase the potential for torsades de pointes. Special attention should be given to electrolyte and acid-base balance in patients experiencing severe or prolonged diarrhoea or patients receiving concomitant magnesium- and/or potassium-depleting drugs.

Congestive Heart Failure Beta-blockade may further depress myocardial contractility and precipitate more severe heart failure. Caution is advised when initiating therapy in patients with left ventricular dysfunction controlled by therapy (i.e. ACE Inhibitors, diuretics, digitalis, etc); a low initial dose and careful dose titration is appropriate.

Recent MI In post-infarction patients with impaired left ventricular function, the risk versus benefit of sotalol administration must be considered. Careful monitoring and dose titration are critical during initiation and follow-up of therapy. SOTACOR should be avoided in patients with left ventricular ejection fractions <40% without serious ventricular arrhythmias.

Electrocardiographic Changes Excessive prolongation of the QT-interval,>500 msec, can be a sign of toxicity and should be avoided (see Proarrhythmias above). Sinus bradycardia has been observed very commonly in arrhythmia patients receiving sotalol in clinical trials. Bradycardia increases the risk of torsades de pointes. Sinus pause, sinus arrest and sinus node dysfunction occur in less than 1% of patients. The incidence of 2nd- or 3rd-degree AV block is approximately 1%.

Anaphylaxis Patients with a history of anaphylactic reaction to a variety of allergens may have a more severe reaction on repeated challenge while taking beta-blockers. Such patients may be unresponsive to the usual doses of adrenaline used to treat the allergic reaction.

Anaesthesia As with other beta-blocking agents, SOTACOR should be used with caution in patients undergoing surgery and in association with anaesthetics that cause myocardial depression, such as cyclopropane or trichloroethylene.

Diabetes Mellitus SOTACOR should be used with caution in patients with diabetes (especially labile diabetes) or with a history of episodes of spontaneous hypoglycaemia, since beta-blockade may mask some important signs of the onset of acute hypoglycaemia, e.g. tachycardia.

Thyrotoxicosis Beta-blockade may mask certain clinical signs of hyperthyroidism (e.g., tachycardia). Patients suspected of developing thyrotoxicosis should be managed carefully to avoid abrupt withdrawal of beta-blockade which might be followed by an exacerbation of symptoms of hyperthyroidism, including thyroid storm.

Renal Impairment As sotalol is mainly eliminated via the kidneys the dose should be adjusted in patients with renal impairment (see section 4.2 Posology and method of administration).

Psoriasis Beta-blocking drugs have been reported rarely to exacerbate the symptoms of psoriasis vulgaris.

This product contains lactose, patients with rare hereditary problems of galactose intolerance, the Lapp-lactase deficiency or glucose-galactose malabsorption should not take this medicinal product.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

Antiarrhythmics Class 1a antiarrhythmic drugs, such as disopyramide, quinidine and procainamide and other antiarrhythmic drugs such as amiodarone and bepridil are not recommended as concomitant therapy with SOTACOR, because of their potential to prolong refractoriness (see section 4.4 Special warnings and precautions). The concomitant use of other beta-blocking agents with SOTACOR may result in additive Class II effects.

Other drugs prolonging the QT-interval SOTACOR should be given with extreme caution in conjunction with other drugs known to prolong the QT-interval such as phenothiazines, tricyclic antidepressants, terfenadine and astemizole. Other drugs that have been associated with an increased risk for torsades de pointes include erythromycin IV, halofantrine, pentamidine, and quinolone antibiotics.

Floctafenine beta-adrenergic blocking agents may impede the compensatory cardiovascular reactions associated with hypotension or shock that may be induced by Floctafenine.

Calcium channel blocking drugs Concurrent administration of beta-blocking agents and calcium channel blockers has resulted in hypotension, bradycardia, conduction defects, and cardiac failure. Beta-blockers should be avoided in combination with cardiodepressant calcium-channel blockers such as verapamil and diltiazem because of the additive effects on atrioventricular conduction, and ventricular function.

Potassium-Depleting Diuretic : Hypokalaemia or hypomagnesaemia may occur, increasing the potential for torsade de pointes (see section 4.4 Special warnings and precautions ).

Other potassium-depleting drugs Amphotericin B (IV route), corticosteroids (systemic administration), and some laxatives may also be associated with hypokalaemia; potassium levels should be monitored and corrected appropriately during concomitant administration with SOTACOR.

Clonidine Beta-blocking drugs may potentiate the rebound hypertension sometimes observed after discontinuation of clonidine; therefore, the beta-blocker should be discontinued slowly several days before the gradual withdrawal of clonidine.

Digitalis glycosides Single and multiple doses of SOTACOR do not significantly affect serum digoxin levels. Proarrhythmic events were more common in sotalol treated patients also receiving digitalis glycosides; however, this may be related to the presence of CHF, a known risk factor for proarrhythmia, in patients receiving digitalis glycosides. Association of digitalis glycosides with beta-blockers may increase auriculo-ventricular conduction time.

Catecholamine-depleting agents Concomitant use of catecholamine-depleting drugs, such as reserpine, guanethidine, or alpha methyldopa, with a beta-blocker may produce an excessive reduction of resting sympathetic nervous tone. Patients should be closely monitored for evidence of hypotension and/or marked bradycardia which may produce syncope.

Insulin and oral hypoglycaemics Hyperglycaemia may occur, and the dosage of antidiabetic drugs may require adjustment. Symptoms of hypoglycaemia (tachycardia) may be masked by beta-blocking agents.

Neuromuscular blocking agents like Tubocurarin The neuromuscular blockade is prolonged by beta-blocking agents.

Beta-2-receptor stimulants Patients in need of beta-agonists should not normally receive SOTACOR. However, if concomitant therapy is necessary beta-agonists may have to be administered in increased dosages .

Drug/Laboratory interaction The presence of sotalol in the urine may result in falsely elevated levels of urinary metanephrine when measured by photometric methods. Patients suspected of having phaeochromocytoma and who are treated with sotalol should have their urine screened utilizing the HPLC assay with solid phase extraction.

4.6 Pregnancy And Lactation

Pregnancy Animal studies with sotalol hydrochloride have shown no evidence of teratogenicity or other harmful effects on the foetus. Although there are no adequate and well-controlled studies in pregnant women, sotalol hydrochloride has been shown to cross the placenta and is found in amniotic fluid. Beta-blockers reduce placental perfusion, which may result in intrauterine foetal death, immature and premature deliveries. In addition, adverse effects (especially hypoglycaemia and bradycardia) may occur in foetus and neonate. There is an increased risk of cardiac and pulmonary complications in the neonate in the postnatal period. Therefore, SOTACOR should be used in pregnancy only if the potential benefits outweigh the possible risk to the foetus. The neonate should be monitored very carefully for 48 - 72 hours after delivery if it was not possible to interrupt maternal therapy with SOTACOR 2-3 days before the birthdate.

Lactation

Most beta-blockers, particularly lipophilic compounds, will pass into breast milk although to a variable extent. Breast feeding is therefore not recommended during administration of these compounds.

4.7 Effects On Ability To Drive And Use Machines

There are no data available, but the occasional occurrence of side-effects such as dizziness and fatigue should be taken into account (see section 4.8 Undesirable effects).

4.8 Undesirable Effects

The most frequent adverse effects of sotalol arise from its beta-blockade properties. Adverse effects are usually transient in nature and rarely necessitate interruption of, or withdrawal from treatment. If they do occur, they usually disappear when the dosage is reduced. The most significant adverse effects, however, are those due to proarrhythmia, including torsades de pointes (See Warnings).

The following are adverse events considered related to therapy, occurring in 1% or more of patients treated with SOTACOR.

Cardiovascular Bradycardia, dyspnoea, chest pain, palpitations, oedema, ECG abnormalities, hypotension, proarrhythmia, syncope, heart failure, presyncope.

Dermatologic Rash.

Gastro-intestinal Nausea/vomiting, diarrhoea, dyspepsia, abdominal pain, flatulence.

Musculoskeletal Cramps.

Nervous/psychiatric Fatigue, dizziness, asthenia, lightheadedness, headache, sleep disturbances, depression, paraesthesia, mood changes, anxiety.

Urogenital Sexual dysfunction.

Special Senses Visual disturbances, taste abnormalities, hearing disturbances.

Body as a whole Fever.

In trials of patients with cardiac arrhythmia, the most common adverse events leading to discontinuation of SOTACOR were fatigue 4%, bradycardia ( <50 bpm) 3%, dyspnoea 3%, proarrhythmia 2%, asthenia 2%, and dizziness 2%.

Cold and cyanotic extremities, Raynaud's phenomenon, increase in existing intermittent claudication and dry eyes have been seen in association with other beta-blockers.

4.9 Overdose

Intentional or accidental overdosage with SOTACOR has rarely resulted in death. Haemodialysis results in a large reduction of plasma levels of sotalol.

Symptoms and treatment of overdosage: The most common signs to be expected are bradycardia, congestive heart failure, hypotension, bronchospasm and hypoglycaemia. In cases of massive intentional overdosage (2-16 g) of SOTACOR the following clinical findings were seen: hypotension, bradycardia, prolongation of QT-interval, premature ventricular complexes, ventricular tachycardia, torsades de pointes.

If overdosage occurs, therapy with SOTACOR should be discontinued and the patient observed closely. In addition, if required, the following therapeutic measures are suggested:

Bradycardia Atropine (0.5 to 2 mg IV), another anticholinergic drug, a beta-adrenergic agonist (isoprenaline, 5 microgram per minute, up to 25 microgram, by slow IV injection) or transvenous cardiac pacing.

Heart Block (second and third degree) Transvenous cardiac pacing.

Hypotension Adrenaline rather than isoprenaline or noradrenaline may be useful, depending on associated factors.

Bronchospasm Aminophylline or aerosol beta-2-receptor stimulant.

Torsades de pointes DC cardioversion, transvenous cardiac pacing, adrenaline, and/or magnesium sulphate.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

D,l-sotalol is a non-selective hydrophilic β-adrenergic receptor blocking agent, devoid of intrinsic sympathomimetic activity or membrane stabilizing activity.

SOTACOR has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. Sotalol has no known effect on the upstroke velocity and therefore no effect on the depolarisation phase.

Sotalol uniformly prolongs the action potential duration in cardiac tissues by delaying the repolarisation phase. Its major effects are prolongation of the atrial, ventricular and accessory pathway effective refractory periods.

The Class II and III properties may be reflected on the surface electrocardiogram by a lengthening of the PR, QT and QT_C (QT corrected for heart rate) intervals with no significant alteration in the QRS duration.

The d- and l-isomers of sotalol have similar Class III antiarrhythmic effects while the l-isomer is responsible for virtually all of the beta-blocking activity. Although significant beta-blockade may occur at oral doses as low as 25 mg, Class III effects are usually seen at daily doses of greater than 160 mg.

Its β-adrenergic blocking activity causes a reduction in heart rate (negative chronotropic effect) and a limited reduction in the force of contraction (negative inotropic effect). These cardiac changes reduce myocardial oxygen consumption and cardiac work. Like other β-blockers, sotalol inhibits renin release. The renin-suppressive effect of sotalol is significant both at rest and during exercise. Like other beta adrenergic blocking agents, SOTACOR produces a gradual but significant reduction in both systolic and diastolic blood pressures in hypertensive patients. Twenty-four-hour control of blood pressure is maintained both in the supine and upright positions with a single daily dose.

5.2 Pharmacokinetic Properties

The bioavailability of oral sotalol is essentially complete (greater than 90%). After oral administration, peak levels are reached in 2.5 to 4 hours, and steady-state plasma levels are attained within 2-3 days. The absorption is reduced by approximately 20% when administered with a standard meal, in comparison to fasting conditions. Over the dosage range 40-640 mg/day SOTACOR displays dose proportionality with respect to plasma levels. Distribution occurs to a central (plasma) and a peripheral compartment, with an elimination half-life of 10-20 hours. Sotalol does not bind to plasma proteins and is not metabolised. There is very little inter-subject variability in plasma levels. Sotalol crosses the blood brain barrier poorly, with cerebrospinal fluid concentrations only 10% of those in plasma. The primary route of elimination is renal excretion. Approximately 80 to 90% of a dose is excreted unchanged in the urine, while the remainder is excreted in the faeces. Lower doses are necessary in conditions of renal impairment (see Dosage and Administration in patients with renal dysfunction). Age does not significantly alter the pharmacokinetics, although impaired renal function in geriatric patients can decrease the excretion rate, resulting in increased drug accumulation.

5.3 Preclinical Safety Data

No further particulars.

6. Pharmaceutical Particulars

6.1 List Of Excipients

Colloidal anhydrous silica, lactose monohydrate, magnesium stearate, maize starch, microcrystalline cellulose, stearic acid.

6.2 Incompatibilities

There are no known incompatibilities.

6.3 Shelf Life

Three years.

6.4 Special Precautions For Storage

Do not store above 25°C. Protect from light.

6.5 Nature And Contents Of Container

Original packs of 28 or 30 tablets: blister strips of 2x 14 tablets or 3 x 10 tablets, respectively to a carton.

Not all pack sizes may be marketed

6.6 Special Precautions For Disposal And Other Handling

No special requirements

7. Marketing Authorisation Holder

Bristol-Myers Squibb Holdings Limited

t/a Bristol-Myers Pharmaceuticals

Uxbridge Business Park

Sanderson Road

Uxbridge

Middlesex UB8 1DH

8. Marketing Authorisation Number(S)

0125/0076

9. Date Of First Authorisation/Renewal Of The Authorisation

9th June 1976 / 19th August 1997

10. Date Of Revision Of The Text

June 2010

Tri-Sprintec

Pronunciation: nor-JES-ti-mate/ETH-in-il ess-tra-DYE-ole
Generic Name: Norgestimate and Ethinyl Estradiol
Brand Name: Examples include Ortho-Cyclen and Tri-Sprintec

Smoking cigarettes while using Tri-Sprintec increases your chance of having heart problems. Do not smoke while using Tri-Sprintec. Women older than 35 years of age and women who smoke 15 or more cigarettes per day are at a greater risk for heart problems.

Tri-Sprintec is used for:

Preventing pregnancy. It may also be used to regulate the menstrual cycle, treat symptoms of menopause, or treating conditions as determined by your doctor.

Tri-Sprintec is an estrogen and progestin combination. It works by increasing levels of estrogen and progesterone, which inhibits ovulation, changes the cervical mucus (which makes it more difficult for sperm to enter the uterus), and changes the endometrium (which reduces the likelihood of implantation by the fertilized egg).

Do NOT use Tri-Sprintec if:

• you are allergic to any ingredient in Tri-Sprintec


• you are pregnant


• you have a history of problems with the blood vessels in the brain or heart, heart valve problems, heart attack, uncontrolled high blood pressure, abnormal or undiagnosed vaginal bleeding, certain cancers (including breast cancer or endometrial cancer), serious liver problems, blood clots, or have had a stroke


• you are taking troleandomycin

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

Before using Tri-Sprintec:

Some medical conditions may interact with Tri-Sprintec. 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 smoke cigarettes


• if you have cancer, diabetes, headaches or migraines, endometriosis, epilepsy, high cholesterol or triglyceride levels in the blood, high blood pressure, recent surgery, breast nodules or abnormal mammogram, depression, gallbladder or kidney disease, irregular menstrual periods, urinary tract bleeding, or obesity


• if you have heart problems, elevated calcium in the blood, yellowing of the skin or eyes, pancreatitis, or tumors in the uterus

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

• Azole antifungals (eg, ketoconazole), aprepitant, bosentan, barbiturates (eg, phenobarbital), carbamazepine, felbamate, griseofulvin, HIV protease inhibitors (eg, ritonavir), hydantoins (eg, phenytoin), modafinil, nevirapine, penicillins, rifampin, St. John's wort, tetracyclines (eg, doxycycline), topiramate, or troglitazone because they may decrease Tri-Sprintec's effectiveness


• Beta-blockers (eg, metoprolol), corticosteroids (eg, hydrocortisone), cyclosporine, theophyllines, or troleandomycin because the risk of their side effects may be increased by Tri-Sprintec


• Lamotrigine because its effectiveness may be decreased by Tri-Sprintec

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

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

• Take Tri-Sprintec by mouth with or without food.


• Tri-Sprintec can be started either on the first day of your menstrual flow or the first Sunday after the start of your menstrual flow. A second form of birth control should be used during the first month of use.


• Tri-Sprintec works best if it is taken at the same time each day, not more than 24 hours apart.


• If you miss a dose of Tri-Sprintec, take it as soon as you remember. Take your next dose at the regular time. This means you may take 2 doses on the same day. If you miss more than 1 dose of Tri-Sprintec, refer to the patient information that came with Tri-Sprintec.

Ask your health care provider any questions you may have about how to use Tri-Sprintec.

Important safety information:

• Discontinuing Tri-Sprintec while taking lamotrigine may increase the blood levels of lamotrigine and lead to increased side effects such as nausea, dizziness, and visual disturbances.


• Tri-Sprintec may increase the risk of stroke, heart attack, blood clots, high blood pressure, or similar problems. The risk may be greater if you smoke.


• If you have vomiting or diarrhea for any reason, your medicine may not work as well.


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


• If you wear contact lenses and you develop problems with them, contact your doctor.


• Tri-Sprintec may cause dark skin patches on your face. Avoid the sun, sunlamps, or tanning booths until you know how you react to Tri-Sprintec. Use a sunscreen or wear protective clothing if you must be outside for more than a short time.


• Use of Tri-Sprintec will not prevent the spread of sexually transmitted diseases (STDs).


• Taking certain antibiotics, anticonvulsants, and other medicines while you are using Tri-Sprintec may decrease the effectiveness of Tri-Sprintec. To prevent pregnancy, use an extra form of birth control (eg, condoms).


• Tri-Sprintec should not be used in CHILDREN before menstruation has begun.


• PREGNANCY and BREAST-FEEDING: Do not use Tri-Sprintec if you are pregnant. If you think you may be pregnant, contact your doctor right away. Tri-Sprintec is found in breast milk. If you are or will be breast-feeding while you use Tri-Sprintec, check with your doctor. Discuss any possible risks to your baby.

Possible side effects of Tri-Sprintec:

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:

Nausea; vomiting; weight change; bleeding between menstrual periods; breast tenderness.

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); calf/leg pain or swelling; changes in vision; chest pain; difficulty wearing contact lenses; dizziness or fainting; headache or sudden severe headache; lumps in the breast; missed menstrual period; numbness of an arm or leg; one-sided weakness; persistent or recurrent abnormal vaginal bleeding; severe stomach pain; slurred speech; swelling of fingers or ankles; trouble breathing or shortness of breath; yellowing skin or eyes.

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: Tri-Sprintec 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 nausea; vaginal bleeding; vomiting.

Proper storage of Tri-Sprintec:

Store Tri-Sprintec at room temperature, between 68 to 77 degrees F (20 to 25 degrees C). Store away from heat, moisture, and light. Do not store in the bathroom. Keep Tri-Sprintec out of the reach of children and away from pets.

General information:

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


• Tri-Sprintec 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 Tri-Sprintec. 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 Tri-Sprintec resources

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

• Tri-Sprintec Prescribing Information (FDA)


• MonoNessa Prescribing Information (FDA)


• Ortho Tri-Cyclen Consumer Overview


• Ortho Tri-Cyclen Prescribing Information (FDA)


• Ortho Tri-Cyclen Lo Prescribing Information (FDA)


• Previfem Prescribing Information (FDA)


• Sprintec Prescribing Information (FDA)


• Tri-Lo-Sprintec Prescribing Information (FDA)


• Tri-Previfem Prescribing Information (FDA)


• TriNessa Prescribing Information (FDA)

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• Abnormal Uterine Bleeding
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• Gonadotropin Inhibition
• Ovarian Cysts

Fluorometholone Drops

FLUOROMETHOLONE

ophthalmic suspension, USP 0.1%

sterile

DESCRIPTION

Fluorometholone ophthalmic suspension, USP 0.1% is a sterile topical anti-inflammatory agent for ophthalmic use.

Chemical Name: Fluorometholone: 9-Fluoro-11β,17-dihydroxy-6α-methylpregna-1,4-diene-3,20-dione.

Contains: Active: fluorometholone 0.1%. Preservative: benzalkonium chloride 0.004%. Inactives: edetate disodium; polysorbate 80; polyvinyl alcohol 1.4%; purified water; sodium chloride; sodium phosphate, dibasic; sodium phosphate, monobasic; and sodium hydroxide to adjust the pH. Fluorometholone suspension is formulated with a pH from 6.2 to 7.5. It has an osmolality range of 290-350 mOsm/kg.

Structural Formula:

fluorometholone

CLINICAL PHARMACOLOGY

Corticosteroids inhibit the inflammatory response to a variety of inciting agents and probably delay or slow healing. They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation.

There is no generally accepted explanation for the mechanism of action of ocular corticosteroids. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.

Corticosteroids are capable of producing a rise in intraocular pressure. In clinical studies of documented steroid-responders, fluorometholone demonstrated a significantly longer average time to produce a rise in intraocular pressure than dexamethasone phosphate; however, in a small percentage of individuals, a significant rise in intraocular pressure occurred within one week. The ultimate magnitude of the rise was equivalent for both drugs.

INDICATIONS AND USAGE

Fluorometholone ophthalmic suspension 0.1% is indicated for the treatment of corticosteroidresponsive inflammation of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe.

CONTRAINDICATIONS

Fluorometholone ophthalmic suspension 0.1% is contraindicated in most viral diseases of the cornea and conjunctiva, including epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, and varicella, and also in mycobacterial infection of the eye and fungal diseases of ocular structures. Fluorometholone ophthalmic suspension 0.1% is also contraindicated in individuals with known or suspected hypersensitivity to any of the ingredients of this preparation and to other corticosteroids.

WARNINGS

Prolonged use of corticosteroids may result in glaucoma with damage to the optic nerve, defects in visual acuity and fields of vision, and in posterior subcapsular cataract formation. Prolonged use may also suppress the host immune response and thus increase the hazard of secondary ocular infections.

Various ocular diseases and long-term use of topical corticosteroids have been known to cause corneal and scleral thinning. Use of topical corticosteroids in the presence of thin corneal or scleral tissue may lead to perforation.

Acute purulent infections of the eye may be masked or activity enhanced by the presence of corticosteroid medication.

If this product is used for 10 days or longer, intraocular pressure should be routinely monitored even though it may be difficult in children and uncooperative patients. Steroids should be used with caution in the presence of glaucoma. Intraocular pressure should be checked frequently.

The use of steroids after cataract surgery may delay healing and increase the incidence of bleb formation.

Use of ocular steroids may prolong the course and may exacerbate the severity of many viral infections of the eye (including herpes simplex). Employment of a corticosteroid medication in the treatment of patients with a history of herpes simplex requires great caution; frequent slit lamp microscopy is recommended.

Corticosteroids are not effective in mustard gas keratitis and Sjögren's keratoconjunctivitis.

PRECAUTIONS

General: The initial prescription and renewal of the medication order beyond 20 milliliters of fluorometholone ophthalmic suspension 0.1% should be made by a physician only after examination of the patient with the aid of magnification, such as slit lamp biomicroscopy and, where appropriate, fluorescein staining. If signs and symptoms fail to improve after two days, the patient should be reevaluated.

As fungal infections of the cornea are particularly prone to develop coincidentally with long-term local corticosteroid applications, fungal invasion should be suspected in any persistent corneal ulceration where a corticosteroid has been used or is in use. Fungal cultures should be taken when appropriate.

If this product is used for 10 days or longer, intraocular pressure should be monitored (see WARNINGS).

Information for Patients: If inflammation or pain persists longer than 48 hours or becomes aggravated, the patient should be advised to discontinue use of the medication and consult a physician.

This product is sterile when packaged. To prevent contamination, care should be taken to avoid touching the bottle tip to eyelids or to any other surface. The use of this bottle by more than one person may spread infection. Keep bottle tightly closed when not in use. Keep out of the reach of children.

The preservative in fluorometholone ophthalmic suspension, benzalkonium chloride, may be absorbed by soft contact lenses. Patients wearing soft contact lenses should be instructed to wait at least 15 minutes after instilling fluorometholone ophthalmic suspension to insert soft contact lenses.

Carcinogenesis, mutagenesis, impairment of fertility: No studies have been conducted in animals or in humans to evaluate the possibility of these effects with fluorometholone.

Pregnancy: Teratogenic effects. Pregnancy Category C: Fluorometholone has been shown to be embryocidal and teratogenic in rabbits when administered at low multiples of the human ocular dose. Fluorometholone was applied ocularly to rabbits daily on days 6-18 of gestation, and dose-related fetal loss and fetal abnormalities including cleft palate, deformed rib cage, anomalous limbs and neural abnormalities such as encephalocele, craniorachischisis, and spina bifida were observed. There are no adequate and well-controlled studies of fluorometholone in pregnant women, and it is not known whether fluorometholone can cause fetal harm when administered to a pregnant woman. Fluorometholone should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers: It is not known whether topical ophthalmic administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in human milk. Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. Because of the potential for serious adverse reactions in nursing infants from fluorometholone, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use: Safety and effectiveness in infants below the age of 2 years have not been established.

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

Adverse Reactions

Adverse reactions include, in decreasing order of frequency, elevation of intraocular pressure (IOP) with possible development of glaucoma and infrequent optic nerve damage, posterior subcapsular cataract formation, and delayed wound healing.

Although systemic effects are extremely uncommon, there have been rare occurrences of systemic hypercorticoidism after use of topical steroids.

Corticosteroid-containing preparations have also been reported to cause acute anterior uveitis and perforation of the globe. Keratitis, conjunctivitis, corneal ulcers, mydriasis, conjunctival hyperemia, loss of accommodation and ptosis have occasionally been reported following local use of corticosteroids.

The development of secondary ocular infection (bacterial, fungal and viral) has occurred. Fungal and viral infections of the cornea are particularly prone to develop coincidentally with long-term applications of steroids. The possibility of fungal invasion should be considered in any persistent corneal ulceration where steroid treatment has been used (see WARNINGS).

Transient burning and stinging upon instillation and other minor symptoms of ocular irritation have been reported with the use of fluorometholone ophthalmic suspension 0.1%. Other adverse events reported with the use of fluorometholone ophthalmic suspension 0.1% include: allergic reactions, visual disturbance (blurry vision), and taste perversion.

DOSAGE AND ADMINISTRATION

Instill one drop into the conjunctival sac two to four times daily. During the initial 24 to 48 hours, the dosage may be increased to one application every four hours. Care should be taken not to discontinue therapy prematurely.

If signs and symptoms fail to improve after two days, the patient should be re-evaluated (see PRECAUTIONS).

The dosing of fluorometholone ophthalmic suspension 0.1% may be reduced, but care should be taken not to discontinue therapy prematurely. In chronic conditions, withdrawal of treatment should be carried out by gradually decreasing the frequency of applications.

HOW SUPPLIED

Fluorometholone ophthalmic suspension, USP 0.1% is supplied sterile in opaque white LDPE plastic bottles with droppers with white high impact polystyrene (HIPS) caps as follows:

5mL in 10mL bottle NDC 60758-880-05

10mL in 15mL bottle NDC 60758-880-10

15mL in 15mL bottle NDC 60758-880-15

Note: Store between 2° and 25°C (36° - 77°F); protect from freezing. Shake well before using.

Rx Only

Revised June 2003

© 2003 Pacific Pharma

Irvine, CA 92612, U.S.A.

4708X

71599PY10M

PACIFIC

PHARMA®

NDC 60758-880-10 Rx Only

FLUOROMETHOLONE

ophthalmic suspension,

USP 0.1%

10 mL Sterile

PACIFIC

PHARMA®

NDC 60758-880-10

FLUOROMETHOLONE

ophthalmic

suspension,

USP 0.1%

10 mL

Sterile

Rx only

FLUOROMETHOLONE  fluorometholone  solution/ drops

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 60758-880 Route of Administration OPHTHALMIC DEA Schedule

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

Inactive Ingredients Ingredient Name Strength benzalkonium chloride   edetate disodium   polysorbate 80   polyvinyl alcohol   water   sodium chloride   sodium phosphate, dibasic   sodium phosphate, monobasic   sodium hydroxide

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 60758-880-05 1 BOTTLE In 1 CARTON contains a BOTTLE, DROPPER 1 5 mL In 1 BOTTLE, DROPPER This package is contained within the CARTON (60758-880-05) 2 60758-880-10 1 BOTTLE In 1 CARTON contains a BOTTLE, DROPPER 2 10 mL In 1 BOTTLE, DROPPER This package is contained within the CARTON (60758-880-10) 3 60758-880-15 1 BOTTLE In 1 CARTON contains a BOTTLE, DROPPER 3 15 mL In 1 BOTTLE, DROPPER This package is contained within the CARTON (60758-880-15)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
NDA authorized generic	NDA016851	10/31/1997

Labeler - Pacific Pharma, Inc. (877645267)

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

Revised: 07/2011Pacific Pharma, Inc.

More Fluorometholone Drops resources

• Fluorometholone Drops Side Effects (in more detail)
• Fluorometholone Drops Use in Pregnancy & Breastfeeding
• Fluorometholone Drops Drug Interactions
• Fluorometholone Drops Support Group
• 1 Review for Fluorometholone - Add your own review/rating

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Gee's Linctus BP (Boots Company plc)

Gee’s Linctus B.P. (Boots Company plc)

(Opium Tincture, Squill Oxymel)

traditional relief from chesty coughs

200 ml e

Read all of this label for full instructions.

What this medicine is for

A linctus for the relief of chesty coughs.

Before you take this medicine

Do not take:

• If you are allergic to any of the ingredients



• If you have heart, liver or kidney problems



• If you have severe breathing problems



• If you have a head injury or a condition where there is raised pressure in the head



• If you suffer from alcoholism or fits



• If you are pregnant or breastfeeding



• If you have an intolerance to some sugars, unless your doctor tells you to (this medicine contains sucrose)

Talk to your pharmacist or doctor:

• If you suffer from colitis



• If you are elderly



• If you are taking monoamine oxidase inhibitors (for depression) or have taken them in the last 14 days



• If you take other medicines – anaesthetics, sedatives, hypnotics, medicines known as phenothiazines (e.g. chlorpromazine)



• If you are on a controlled sodium diet (this medicine contains 157 mg of sodium per 5 ml spoonful)

If you take this medicine continuously for a long time (e.g. 2 weeks or more), you may become dependent on it.

Driving:

This medicine may cause drowsiness. If affected do not drive or operate machinery.

Do not drink alcohol (beer, wine, spirits) when taking this medicine.

This medicine contains 1.5 g of sucrose per 5 ml spoonful. This should be taken into account if you suffer from diabetes.

Each 5 ml spoonful contains 0.8 g of alcohol (ethanol) equivalent to 21 ml of beer or 9 ml of wine. This should be taken into account if given to children. May modify or increase the effects of other medicines.

How to take this medicine

Check the cap seal is not broken before first use. If it is, do not take the medicine.

Adults and children of 12 years and over: One 5 ml spoonful. Swallow this amount 3 or 4 times in 24 hours.

Do not give to children under 12 years.

Warning: Do not exceed the stated dose.

If symptoms do not go away talk to your doctor.

If you take too much: Talk to a doctor straight away.

Possible side effects

Most people will not have problems, but some may get some of these:

• Violent diarrhoea, feeling sick, being sick



• Drowsiness



• Constipation (if used over a long period of time)

If any side effect becomes severe, or you notice any side effect not listed here, please tell your pharmacist or doctor.

Keep all medicines out of the sight and reach of children.

Use by the date on the label edge.

Active ingredients

Each 5 ml of oral liquid contains Opium Tincture 0.084 ml, Squill Vinegar for Oxymel 0.5 ml.

Also contains: honey (containing sodium), liquid sugar (sucrose), purified water, ethanol (19.7 vol %), benzoic acid (E210), tragacanth, flavours (tolu, camphor, star anise oil).

PL 00014/5721

P

Text prepared 10/07

Manufactured by the Marketing Authorisation holder

The Boots Company PLC

Nottingham

NG2 3AA

If you need more advice ask your pharmacist.

BTC13949 vF 02/07/08

Mirapex ER Extended-Release Tablets

Pronunciation: PRAM-i-PEX-ole
Generic Name: Pramipexole
Brand Name: Mirapex ER

Mirapex ER Extended-Release Tablets are used for:

Treating the signs and symptoms of early Parkinson disease. It may also be used for other conditions as determined by your doctor.

Mirapex ER Extended-Release Tablets are a dopamine agonist. Exactly how Mirapex ER Extended-Release Tablets works is unknown. It may increase the action of certain chemical receptors in the brain.

Do NOT use Mirapex ER Extended-Release Tablets if:

• you are allergic to any ingredient in Mirapex ER Extended-Release Tablets


• you have severe kidney problems or are on dialysis


• you are taking another medicine that has pramipexole in it

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

Before using Mirapex ER Extended-Release Tablets:

Some medical conditions may interact with Mirapex ER Extended-Release Tablets. 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 kidney problems, low blood pressure, lightheadedness when you sit or stand up, or daytime sleepiness


• if you drink alcohol or have a history of compulsive behavior (eg, eating, gambling, shopping)


• if you have trouble controlling your muscles

Some MEDICINES MAY INTERACT with Mirapex ER Extended-Release Tablets. Tell your health care provider if you are taking any other medicines, especially any of the following:

• Cimetidine because it may increase the risk of Mirapex ER Extended-Release Tablets's side effects


• Butyrophenones (eg, haloperidol), metoclopramide, phenothiazines (eg, chlorpromazine), or thioxanthenes (eg, thiothixene) because they may decrease Mirapex ER Extended-Release Tablets's effectiveness


• Levodopa because the risk of its side effects may be increased by Mirapex ER Extended-Release Tablets

This may not be a complete list of all interactions that may occur. Ask your health care provider if Mirapex ER Extended-Release Tablets 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 Mirapex ER Extended-Release Tablets:

Use Mirapex ER Extended-Release Tablets as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• An extra patient leaflet is available with Mirapex ER Extended-Release Tablets. Talk to your pharmacist if you have questions about this information.


• Take Mirapex ER Extended-Release Tablets by mouth with or without food. If stomach upset occurs, take with food to reduce stomach irritation.


• Swallow Mirapex ER Extended-Release Tablets whole. Do not break, crush, or chew before swallowing.


• Your dose will be started low and gradually increased to achieve the best results. Do not change your dose sooner than recommended.


• Do not suddenly stop taking Mirapex ER Extended-Release Tablets without checking with your doctor. Severe side effects, including fever, mental or mood changes, and stiff muscles, may occur.


• If you miss a dose of Mirapex ER Extended-Release Tablets, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once. If you miss several doses, contact your doctor before you start to take Mirapex ER Extended-Release Tablets again.

Ask your health care provider any questions you may have about how to use Mirapex ER Extended-Release Tablets.

Important safety information:

• Mirapex ER Extended-Release Tablets may cause drowsiness or dizziness. These effects may be worse if you take it with alcohol or certain medicines. Use Mirapex ER Extended-Release Tablets with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.


• Do not drink alcohol while you are using Mirapex ER Extended-Release Tablets.


• Check with your doctor before you use medicines that may cause drowsiness (eg, sleep aids, muscle relaxers) while you are using Mirapex ER Extended-Release Tablets; it may add to their effects. Ask your pharmacist if you have questions about which medicines may cause drowsiness.


• Mirapex ER Extended-Release Tablets 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.


• Some patients who take Mirapex ER Extended-Release Tablets have reported suddenly falling asleep while performing daily activities (eg, driving, eating, conversing). Many patients reported drowsiness before falling asleep; however, some patients did not experience drowsiness and felt that they were alert immediately before suddenly falling asleep. Use caution when driving, operating machinery, or performing other activities that could be dangerous. Inform your doctor if you experience unusual drowsiness or sleepiness while using Mirapex ER Extended-Release Tablets.


• Some people have experienced new, unusual, or increased urges (eg, gambling, sexual urges) while using Mirapex ER Extended-Release Tablets. Tell your doctor right away if you notice such effects.


• Patients with Parkinson disease may have an increased risk of developing a certain type of skin cancer (melanoma). It is not known if Mirapex ER Extended-Release Tablets also increases the risk of melanoma. You may need to have skin exams while you are using Mirapex ER Extended-Release Tablets. Discuss any questions or concerns with your doctor.


• Lab tests, including blood pressure or skin checks, may be performed while you use Mirapex ER Extended-Release Tablets. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.


• Use Mirapex ER Extended-Release Tablets with caution in the ELDERLY; they may be more sensitive to its effects, especially hallucinations.


• Mirapex ER Extended-Release Tablets should be used with extreme caution in CHILDREN; safety and effectiveness in children have not been confirmed.


• PREGNANCY and BREAST-FEEDING: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Mirapex ER Extended-Release Tablets while you are pregnant. It is not known if Mirapex ER Extended-Release Tablets are found in breast milk. Do not breast-feed while taking Mirapex ER Extended-Release Tablets.

Possible side effects of Mirapex ER Extended-Release Tablets:

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:

Constipation; cough; dizziness; drowsiness; dry mouth; muscle spasms; nausea; stomach pain or upset; tiredness; vomiting.

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); abnormal thinking; balance problems; change in behavior, mood, or emotions; chest pain; confusion; decreased sexual ability; difficulty walking; fainting; hallucinations; increased urination; memory loss; muscle pain, tenderness, or weakness; new or unusual skin growths; severe or persistent drowsiness or sleepiness; shortness of breath; sudden irresistible urge to sleep or suddenly falling asleep at unusual times; swelling of the arms or legs; trouble swallowing; unusual or intense urges (eg, gambling, sexual urges); unusual twitching or muscle movements; vision changes; vivid dreams or daydreams.

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: Mirapex ER 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 agitation; chest pain; confusion; decrease in blood pressure; difficulty moving; drowsiness; nausea; sedation; vomiting.

Proper storage of Mirapex ER Extended-Release Tablets:

Store Mirapex ER Extended-Release Tablets 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 Mirapex ER Extended-Release Tablets out of the reach of children and away from pets.

General information:

• If you have any questions about Mirapex ER Extended-Release Tablets, please talk with your doctor, pharmacist, or other health care provider.


• Mirapex ER Extended-Release Tablets are 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 Mirapex ER Extended-Release Tablets. 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.

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