Magnesium Sulfate

Class: Anticonvulsants, Miscellaneous
VA Class: CN400
CAS Number: 10034-99-8

Introduction

Anticonvulsant parenterally; electrolyte; required cofactor for numerous human enzyme systems.^{a h}

Uses for Magnesium Sulfate

Prevention and Control of Seizures

Injection mainly used as an anticonvulsant for the prevention and control of seizures in toxemia (preeclampsia or eclampsia) of pregnancy, acute nephritis (in children), and in various other conditions.⁶⁷

Toxemias of Pregnancy

Generally considered the anticonvulsant drug of choice for the prevention and control of seizures in severe preeclampsia or in eclampsia,^{58 59 60 61} and appears to be more effective than phenytoin.^{58 60 61 d}

Opinions differ regarding the role for prophylactic use in preventing seizures in mild preeclampsia or gestational hypertension†.^d

Also used in the management of uterine tetany, especially that associated with the use of oxytocic agents.^a

Acute Nephritis in Children

Has been used to control seizures, encephalopathy, and hypertension associated with acute nephritis in children.⁶⁷ However, other agents (e.g., barbiturates, reserpine, hydralazine) should be tried first.⁶⁷

Some clinicians caution not to use parenteral magnesium sulfate to control seizures unless hypomagnesemia has been confirmed, and to monitor serum magnesium concentration when administered.^a

Reserve IV use for immediate control of life-threatening seizures.^a

Other Seizure Etiologies

Parenterally, may be useful to control seizures associated with epilepsy, glomerulonephritis, or hypothyroidism, since low plasma concentrations of magnesium may be a contributing cause of seizures in these conditions.^a

Prevention and Treatment of Hypomagnesemia

Injection is added to total parenteral nutrition admixtures to correct or prevent hypomagnesemia.⁶⁷

Treatment of acute hypomagnesemia associated with clinical conditions including malabsorption syndromes, alcoholism, cirrhosis of the liver, acute pancreatitis, or prolonged IV therapy with magnesium-free fluids.^{a 70}

Especially effective in the treatment of acute hypomagnesemia accompanied by signs of tetany similar to those of hypocalcemia;⁶⁷ usually, serum magnesium concentrations are below the lower limits of normal (1.5–2.5 or 3 mEq/L), and serum calcium concentrations are either normal (4.3–5.3 mEq/L) or elevated in such cases.⁶⁷

Preterm Labor

Has been used to inhibit uterine contractions in preterm labor (tocolysis)† and prolong gestation when beneficial.^{13 14}

Previously, the American College of Obstetricians and Gynecologists (ACOG) considered magnesium sulfate a first-line tocolytic agent of choice; currently, ACOG states that there is no clear first-line tocolytic agent.⁶⁹

May be contraindicated by maternal or fetal conditions.¹³ (See Contraindications under Cautions.)

Following successful cessation of uterine contractions, oral maintenance therapy with other magnesium salts (e.g., oxide or gluconate) has not been consistently beneficial.^{13 20}

Combination therapy with another tocolytic agent may be more effective than single-agent therapy, but may increase risk of maternal morbidity, and safety and efficacy have not been established; use with caution.^{13 19 24 25 27 69}

Concurrent use of magnesium sulfate and nifedipine may be particularly risky (e.g., development of severe hypotension and neuromuscular blockade).^{13 32 69}

Arrhythmias

Used IV successfully for the treatment of life-threatening arrhythmias such as atypical VT† (torsades de pointes).^{h 8 9 10}

Considered one of several preferred drugs in the treatment of polymorphic VT suspected of being torsades de pointes† in patients in whom initial attempts at correcting or managing potential precipitating factors (e.g., ischemic cardiac events, electrolyte imbalance, drugs known to prolong the QT interval) have not been successful.^{h 64 66 70}

Not recommended in the treatment of cardiac arrest except when the ECG monitoring shows torsades de pointes.⁷⁰

Drug-induced cardiovascular emergencies or altered vital signs: May consider use in VT associated with tricyclic antidepressant toxicity; however, use may aggravate drug-induced hypotension.⁷⁰ Anecdotal evidence suggests that magnesium sulfate also may be an effective treatment in antiarrhythmic drug-induced torsades de pointes even in the absence of magnesium deficiency.^{66 70}

Has been used IV in the management of paroxysmal atrial tachycardia† when other measures have failed and when there is no evidence of myocardial damage.^a

May consider use in atrial fibrillation with a rapid ventricular response† for rate control.⁷⁰

AMI

Has been administered IV adjunctively to reduce cardiovascular morbidity and mortality (e.g., through reduction in ventricular arrhythmias and/or limitation of infarct size and reperfusion injury) associated with AMI†;^{2 6 7 34 35 36 37 38 39 64} however, evidence of benefit is contradictory and the precise role remains unclear.^{34 44 45 46 47 64}

Routine magnesium prophylaxis in AMI no longer recommended.^{64 70}

Instead, ACC and AHA currently recommend that magnesium in AMI be reserved for patients with documented magnesium and/or potassium deficits, especially in patients receiving diuretics prior to infarction.⁶⁴

ACC/AHA state that it is sound clinical practice to maintain magnesium concentrations >2 mEq/L in patients with AMI.^{64 66 70}

Recommended by ACC/AHA in AMI for episodes of torsades de pointes-type VT.^{64 66}

Recommended by ACC/AHA for consideration in high-risk patients such as geriatric patients and/or those for whom reperfusion therapy is not suitable.

ACC/AHA state that mortality reduction may be possible with magnesium use in certain high-risk patients with AMI (e.g., geriatric patients, those who are not eligible for reperfusion therapy) if they receive the drug as soon as possible after symptom onset (within 6 hours); however, conflicting evidence and/or divergence of opinion about usefulness/efficacy.^{64 66}

Acute Asthma

May modestly improve pulmonary function and reduce hospital admissions when combined with nebulized β-adrenergic agents and corticosteroids, particularly in patients with severe exacerbations of asthma†.⁷⁰

Barium Poisoning

Administered IV to counteract the intense muscle stimulating effects of barium poisoning.

Also may administer by gastric lavage or oral solution to precipitate and remove unabsorbed barium.^a (See Dosage under Dosage and Administration.)

Magnesium Sulfate Dosage and Administration

Administration

Administer IV or IM.^{a 70}

For ACLS during CPR, may be administered by intraosseous infusion† when IV injection is not possible.⁷⁰

IV Administration

Generally, concentration should not be >200 mg/mL (20%).^a

Rate of Administration

Risk of vasodilation or hypotension if administered rapidly.⁷⁰

Usually, do not exceed 150 mg/minute (e.g., 1.5 mL/minute of a 10% concentration or equivalent) except in patients with seizures associated with severe eclampsia (e.g., up to 1.33 g/minute for loading dose), preterm labor (e.g., 300 mg/minute for loading dose), or arrhythmias (e.g., 1–6 g over several minutes; 3–4 g over 30 seconds with extreme caution).⁶⁷

IM Administration

Generally, use concentrations of 250 mg/mL (25%) or 500 mg/mL (50%).^a

Infants and children: Usually, use concentration ≤200 mg/mL (20%).^a However, higher concentrations (e.g., 50%) have been used.^{a c}

Intraosseous Administration

When IV administration is not possible, magnesium sulfate may be given by intraosseous infusion† for CPR.⁷⁰

Dosage

Adjust dosage carefully according to individual requirements and response; discontinue as soon as the desired effect is obtained.^a

Pediatric Patients

PALS in CPR

Torsades de Pointes† or Suspected Hypomagnesemia

IV or Intraosseous

Infuse 25–50 mg/kg (up to 2 g) over 10–20 minutes.⁷⁰

Infuse more rapidly (over several minutes) in torsades de pointes†.⁷⁰

Prevention and Control of Seizures

Acute Nephritis in Children

IM

To control seizures, encephalopathy, and hypertension: 100 mg/kg (0.8 mEq/kg or 0.2 mL/kg of a 50% solution) every 4–6 hours as needed.^a

Alternatively to control seizures: 20–40 mg/kg (0.16–0.32 mEq/kg or 0.1–0.2 mL/kg of a 20% solution) as needed.⁶⁷

IV

If symptoms are severe, may administer a 1–3% solution in a dosage of 100–200 mg/kg.^a

Administer slowly; closely monitor BP.^a

Administer total dose within 1 hour, with ½ the dose administered in the first 15–20 minutes.^a

Hypomagnesemia

Prevention

Additive in Total Parenteral Infusion

Infants: Usually, 0.25–0.6 mEq/kg daily.⁶⁷

Maintenance requirements not precisely known.⁶⁷

Treatment

IM

Older children: For deficiency that is not severe, manufacturers recommend 1 g (2 mL of 50% solution) once or twice daily; use serum magnesium values as guide to continued dosage.^c

Adults

Prevention and Control of Seizures

Toxemias of Pregnancy

For the management of preeclampsia or eclampsia, dilute (1–8%) solutions are often given by IV infusion in combination with IM injections using 50% magnesium sulfate.⁶⁸

IV with IM

Severe preeclampsia or eclampsia: Initially, IV infusion of 4–5 g (32.4–40.5 mEq) diluted in 250 mL of 5% dextrose injection or 0.9% sodium chloride injection, in combination with IM injection of up to 10 g (10 mL of undiluted 50% solution administered into each buttock).⁶⁷ Alternatively, after the initial 4- to 5-g IV dose, constant IV infusion of 1–3 g/hour has been recommended.^a Total initial dose: 10–14 g (81–113.4 mEq).^{67 68}

Alternatively, 8–15 g IV initially, depending on weight (8 g for a 45-kg patient to 15 g for a 90-kg patient); 4 g (undiluted or diluted in 5% dextrose injection); give remainder of initial dose IM using undiluted 50% injection.^a Base dosage for the next 24 hours on the serum magnesium concentration and urinary excretion after the initial dose.^a Subsequent doses should be sufficient to replace the magnesium excreted in the urine and will be approximately 65% of the initial dose administered IM at 6-hour intervals.^a

Alternatively, the manufacturer recommends that an initial dose of 4 g (32.4 mEq) be given IV by diluting the 50% solution to 10 or 20% concentration; may then inject 40 mL of a 10% solution or 20 mL of a 20% solution IV over 3–4 minutes.⁶⁷ Administer subsequent 4- to 5-g doses (32.4–40.5 mEq or 8–10 mL of the undiluted 50% injection) IM into alternate buttocks every 4 hours as needed, depending on the continuing presence of the patellar reflex and adequate respiratory function.⁶⁷

Continue therapy until paroxysms cease.⁶⁷

Serum magnesium concentration of 6 mg/dL is considered optimal for seizure control.⁶⁷

IV

For eclampsia, ACOG currently recommends 4–6 g in 100 mL of IV fluid over 15–20 minutes, followed by 2 g per hour continuous IV infusion; use antihypertensive agents for women with DBP ≥105–110 mm Hg.^d

Other Seizure Etiologies

IM or IV

For seizures associated with epilepsy, glomerulonephritis, or hypothyroidism: Usually, 1 g.^a

Hypomagnesemia

Prevention

IV Infusion

Additive in total parenteral nutrition: Usually, 5–8 mEq daily.⁶⁷

Maintenance requirements are not precisely known.⁶⁷

Treatment

Use caution to prevent exceeding the renal excretory capacity.^a

IM

Mild deficiency: Usually, 1 g (8.12 mEq or 2 mL of the 50% solution) every 6 hours for 4 doses.⁶⁷

Alternatively, for deficiency that is not severe, 1 g (2 mL of 50% solution) once or twice daily; use serum magnesium concentrations as guide to continued dosage.^c

Severe deficiency: If necessary, may administer up to 250 mg (about 2 mEq or 0.5 mL of the 50% solution) per kg of body weight within a 4-hour period.^{a f}

Alternatively, for severe hypomagnesemia: 1–5 g (2–10 mL of 50% solution) daily in divided doses; repeat daily until serum levels are normal.^c

Oral

For mild deficiency: 3 g every 6 hours for 4 doses.^a

IV infusion

For severe deficiency: 5 g (approximately 40 mEq) added to 1 L of 5% dextrose injection or 0.9% sodium chloride injection over 3 hours.^{67 f}

Alternatively, for severe or symptomatic hypomagnesemia, 1–2 g over 5–60 minutes.⁷⁰ If seizures are present, administer 2 g over 10 minutes.⁷⁰

Preterm Labor†

Carefully adjust rate and duration of infusion according to the patient’s response as indicated (by uterine response, maternal and fetal tolerance).^{13 14 15 16 17 18}

Monitoring of serum magnesium concentrations may be useful to minimize the risk of toxicity (e.g., respiratory depression, cardiotoxicity, maternal tetany, muscular paralysis, hypotension) and to determine the maximum safe infusion rate.^{13 33}

Monitor amount and rate of IV fluid administration to avoid circulatory overload.¹³

Observe for signs and symptoms of pulmonary edema.¹³

IV Infusion

Acute tocolytic therapy: Loading dose of 4–6 g over 20 minutes; after contractions cease, follow with maintenance infusions of 2–4 g/hour for 12–24 hours as tolerated.^{13 14 15 16 17 18 e}

Arrhythmias

Atypical VT (Torsades de Pointes)†

IV

1–6 g over several minutes, occasionally followed by approximately 3–20 mg/minute by IV infusion for 5–48 hours, depending on response and serum magnesium concentrations.^{8 9 10 64}

Alternatively, for torsades de pointes associated with cardiac (pulseless) arrest†, 1–2 g in 10 mL 5% dextrose injection over 5–20 minutes.⁷⁰

Alternatively, for torsades de pointes in a patient with pulses†, give a loading dose of 1–2 g (8–16 mEq) in 50–100 mL 5% dextrose injection over 5–60 minutes.⁷⁰

Intraosseous

Torsades de pointes associated with cardiac (pulseless) arrest†: 1–2 g in 10 mL 5% dextrose injection over 5–20 minutes.⁷⁰

Paroxysmal Atrial Tachycardia†

IV

Usually, 3–4 g (e.g., 30–40 mL of a 10% solution) over 30 seconds with extreme caution.

AMI†

IV

Optimum dosage not established.

2-g over 5–15 minutes, followed by 18 g over 24 hours (approximately 12.5 mg/minute).⁶⁴

Timing appears to be an important prognostic factor;^{34 56 57 64} initiate administration as soon as possible (preferably no later than 6 hours) after symptom onset.⁶⁴

Acute Asthma†

IV

Usually, 1.2–2 g over 20 minutes.⁷⁰

Barium Poisoning

IV

Usually, 1–2 g to counteract the intense muscle stimulating effects of barium.^a

Gastric Lavage or Oral

May administer 2–5% magnesium sulfate (or sodium sulfate) solution by gastric lavage to precipitate and remove unabsorbed barium remaining in the GI tract.^a

Alternatively, may administer 5–10% magnesium sulfate (or sodium sulfate) solution (up to 60 g) orally to precipitate barium and produce catharsis.^a

Prescribing Limits

Pediatric Patients

PALS in CPR

Torsades de Pointes† or Suspected Hypomagnesemia

IV or Intraosseous

Maximum 2 g, as a single dose.⁷⁰

Adults

Prevention and Control of Seizures

Toxemias of Pregnancy

IV with IM

Do not exceed total daily dosage of 30–40 g.^a

Special Populations

Renal Impairment

Prevention and Control of Seizures

Toxemias of Pregnancy

IV with IM

Maximum 20 g/48 hours in severe renal impairment.^a

Geriatric Patients

Often require reduced dosage because of impaired renal function.^f Maximum 20 g/48 hours in severe renal impairment.^f

Cautions for Magnesium Sulfate

Contraindications

• 
  

  Parenteral administration in heart block or myocardial damage.^{a c}

  
  


• 
  

  Tocolytic therapy in general may be contraindicated by some maternal or fetal conditions (e.g., acute fetal distress other than intrauterine resuscitation, chorioamnionitis, fetal demise [singleton], fetal maturity, maternal hemodynamic instability).¹³

  
  


• 
  

  Tocolytic therapy may be contraindicated by hypocalcemia, myasthenia gravis, renal failure.¹³

  
  


• 
  

  In toxemia of pregnancy during 2 hours prior to delivery.^{67 68}

  
  

Warnings/Precautions

Warnings

Toxicity

Principal hazard is hypermagnesemia, most immediate life-threatening effect is respiratory depression; have IV calcium (e.g., calcium gluconate) readily available for use as antidote.^{a c 70}

Adverse effects of parenteral therapy are caused by magnesium intoxication.^a

Toxic manifestations (may begin at serum magnesium concentrations of 4 mEq/L) include neurologic symptoms (e.g., muscular weakness, flaccid paralysis, ataxia, drowsiness, confusion, depression of reflexes), flushing, sweating, vasodilation, hypotension, hypothermia, depression of cardiac function, bradycardia, cardiac arrhythmias, circulatory collapse, hypoventilation, and CNS depression (depressed level of consciousness); can proceed to fatal respiratory paralysis.^{a 70}

Observe carefully, and monitor serum magnesium concentrations to avoid overdosage and toxicity.^a

During tocolytic therapy, observe carefully and monitor serum magnesium concentrations to minimize the risk of toxicity (e.g., respiratory depression, cardiotoxicity, maternal tetany, muscular paralysis, hypotension).^{13 21 22 23}

Hypocalcemia with signs of tetany can occur during tocolytic use.^a

Patellar reflex disappearance is useful to detect intoxication onset.^a Test knee jerk reflexes before each dose; if absent, give no additional magnesium until they return.^a

Make sure respiration rate is ≥16/minute prior to each dose.^a

Do not continue dosage unless urine output is 100 mL or more during the 4 hours preceding each dose.^a

If overdosage occurs, provide artificial ventilation until a calcium salt can be given IV.^a

In adults, IV administration of 5–10 mEq of calcium (e.g., 10–20 mL of 10% calcium gluconate) usually will reverse respiratory depression or heart block caused by magnesium intoxication.^a

Peritoneal dialysis or hemodialysis may be required in extreme cases of hypermagnesemia.^a

Maternal Pulmonary Edema

Risk of maternal pulmonary edema with tocolytic therapy; development during the initial 24 hours is uncommon.¹³

Etiology is unclear;¹³ risk factors include excessive hydration, multiple gestation, occult sepsis, and underlying cardiac disease.¹³

Adjunctive corticosteroid therapy apparently is not an important risk factor .¹³

Reduce risk by limiting fluid intake to 2.5–3 L daily, limiting sodium intake, and maintaining maternal pulse <130 bpm.¹³

Monitor amount and rate of IV fluid administration to avoid circulatory overload; observe carefully for signs/symptoms of pulmonary edema.¹³

Hypocalcemia

Clinically important hypocalcemia with signs of tetany has occurred after use for eclampsia.^a Changes in calcium and phosphorus balance should be anticipated in each case of parenteral magnesium administration.^a

Major Toxicities

Respiratory Depression

See Warnings under Cautions.

General Precautions

Use with caution if flushing and sweating occur.^c

CNS Depressants

Adjust dosage carefully with concomitant use; have IV calcium (e.g., calcium gluconate) readily available for use as antidote for magnesium toxicity.^{a c} (See CNS Depressants under Interactions.)

Laboratory Tests

Confirm hypomagnesemia, monitor serum magnesium concentration.^c (See Warnings under Cautions.)

Specific Populations

Pregnancy

Category A or B.^{67 68 f}

Although one manufacturer states category D and that parenteral magnesium may cause fetal harm in pregnant women or those becoming pregnant during use,^c most experts consider the drug category B and state that maternal anticonvulsant or tocolytic use usually does not pose fetal or neonatal risk except with prolonged IV infusions.^b

Increased possibility of neonatal toxicity (including neuromuscular or respiratory depression) with prolonged continuous IV infusion before delivery (especially for >24 hours); IM use does not usually compromise neonate.^{a b}

Do not give IV during the 2 hours preceding delivery.^a

Neonatal hypermagnesemia management may require resuscitation and assisted ventilation via endotracheal intubation and/or intermittent positive-pressure ventilation, as well as IV calcium.^a

Lactation

Distributed into milk.^{a b} Caution if used in nursing women,^a but generally considered compatible with breast-feeding.^b

Milk magnesium concentrations increased for only about 24 hours after discontinuance of parenteral magnesium; amount ingested by a nursing infant during this period is probably too small to be of clinical importance.^{a b}

Pediatric Use

Although one manufacturer states safety and efficacy not established in children,^c other manufacturers make no pediatric restrictions.^{67 68 f g}

Included in current CPR guidelines for pediatric advanced life support (PALS).^{70 64}

Geriatric Use

Often requires reduced dosage because of impaired renal function.^f (See Geriatric Use under Dosage and Administration.)

Renal Impairment

Administer with caution in renal impairment; danger of magnesium intoxication.^{a c f}

Reduce dosage and obtain frequent serum magnesium concentrations in severe renal impairment.^a (See Renal Impairment under Dosage and Administration.)^a

Common Adverse Effects

Flushing, sweating, hypotension, depression of reflexes, flaccid paralysis, hypothermia, circulatory collapse, depression of cardiac function, CNS depression.^a

Interactions for Magnesium Sulfate

Specific Drugs

Drug	Interaction	Comments
CNS depressants (e.g., barbiturates, opiates, general anesthetics)	Additive central depressant effects with concomitant usea	Adjust dosage carefullya Have IV calcium (e.g., calcium gluconate) preparation readily available for use as antidotec
Digoxin	Serious changes in cardiac conduction; may cause heart block if IV calcium is required to treat magnesium toxicitya	Use with extreme caution in digitalized patientsa
Neuromuscular blocking agents	Excessive neuromuscular blockade a	Use concomitantly with cautiona

Magnesium Sulfate Pharmacokinetics

Absorption

Onset

IV administration: Immediate onset.^a

IM administration: About 1 hour.^a

Duration

IV administration: About 30 minutes.^a

IM administration: 3–4 hours.^a

Plasma Concentrations

Effective anticonvulsant serum magnesium concentrations: 2.5–7.5 mEq/L.^a

Monitor for hypermagnesemia (serum concentrations >2.5 mEq/L); toxic effects (e.g., depression of deep-tendon reflexes) may begin at 4 mEq/L.^a

At 10 mEq/L, deep-tendon reflexes disappear and respiratory paralysis may occur; complete heart block can occur at about 10 mEq/L.^a

Serum magnesium >12 mEq/L may be fatal.

Distribution

Extent

Crosses the placenta.^{a b}

Distributes into milk.^{a b}

Elimination

Elimination Route

Excreted by the kidneys; interindividual variability in rate but directly proportional to serum concentration and glomerular filtration.^{a h}

Stability

Storage

Parenteral

Injection

15–30°C.^{67 f g}

Magnesium Sulfate in 5% Dextrose Injection

25°C (may expose to up to 40°C).⁶⁷ Avoid freezing.^a

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Incompatible with alkali hydroxides (forming insoluble magnesium hydroxide), with alkali carbonates (forming basic carbonates), and with salicylates (forming basic salicylates).^a

Reacts with arsenates, phosphates, and tartrates, precipitating the corresponding magnesium salts.^a

Lead, barium, strontium, and calcium react with magnesium sulfate resulting in precipitation of the respective sulfates.^a

Parenteral

Solution Compatibility^HID

Compatible
Dextrose 5% in water
Ringer’s injection, lactated
Sodium chloride 0.9%
Incompatible
Fat emulsion 10%, IV

Drug Compatibility

Admixture CompatibilityHID

Compatible
Chloramphenicol sodium succinate
Cisplatin
Heparin sodium
Hydrocortisone sodium succinate
Isoproterenol HCl
Linezolid
Meropenem
Methyldopate HCl
Norepinephrine bitartrate
Penicillin G potassium
Potassium chloride
Potassium phosphates
Verapamil HCl
Incompatible
Amphotericin B
Cyclosporine
Dobutamine HCl
Polymyxin B sulfate
Procaine HCl
Sodium bicarbonate
Variable
Calcium chloride
Calcium gluconate

Y-Site CompatibilityHID

Compatible
Acyclovir sodium
Aldesleukin
Amifostine
Amikacin sulfate
Ampicillin sodium
Aztreonam
Bivalirudin
Cefazolin sodium
Cefotaxime sodium
Cefoxitin sodium
Chloramphenicol sodium succinate
Clindamycin phosphate
Co-trimoxazole
Dexmedetomidine HCl
Dobutamine HCl
Docetaxel
Doxorubicin HCl liposome injection
Doxycycline hyclate
Enalaprilat
Erythromycin lactobionate
Esmolol HCl
Etoposide phosphate
Famotidine
Fenoldopam mesylate
Fludarabine phosphate
Gallium nitrate
Gentamicin sulfate
Granisetron HCl
Heparin sodium
Hetastarch in lactated electrolyte injection (Hextend)
Hydrocortisone sodium succinate
Hydromorphone HCl
Idarubicin HCl
Kanamycin sulfate
Labetalol HCl
Linezolid
Meperidine HCl
Metronidazole
Milrinone lactate
Morphine sulfate
Nafcillin sodium
Nicardipine HCl
Ondansetron HCl
Oxacillin sodium
Oxaliplatin
Paclitaxel
Penicillin G potassium
Piperacillin sodium–tazobactam sodium
Potassium chloride
Propofol
Remifentanil HCl
Sargramostim
Sodium nitroprusside
Thiotepa
Tobramycin sulfate
Vancomycin HCl
Vitamin B complex with C
Incompatible
Amphotericin B cholesteryl sulfate complex
Cefepime HCl
Drotrecogin alfa (activated)
Lansoprazole
Variable
Amiodarone
Ciprofloxacin

ActionsActions

• 
  

  Hypermagnesemia (serum magnesium concentrations >2.5 mEq/L) may depress the CNS and block peripheral neuromuscular transmission, producing anticonvulsant effects.^a

  
  


• 
  

  Exact mechanism is not fully known; excess magnesium appears to decrease the amount of acetylcholine liberated by the motor nerve impulse.^a

  
  


• 
  

  Magnesium ions slow the rate of the SA node impulse formation and prolong conduction time in animals.^a

  
  


• 
  

  IV infusion prolongs PR interval, H (atria-His bundle) interval, antegrade AV nodal effective refractory period, and SA conduction time in humans.^a

  
  


• 
  

  Required cofactor for >300 enzyme systems.^h

  
  


• 
  

  Required for both anaerobic and aerobic energy generation and for glycolysis.^h

  
  


• 
  

  Described as nature’s physiologic calcium-channel blocking agent.^h

  
  


• 
  

  During magnesium depletion, intracellular calcium increases, which can cause muscle cramps, hypertension, and coronary and cerebral vasospasms.^h

  
  


• 
  

  Plays an important role in BP regulation; hypertension may be associated with magnesium deficiency and magnesium may decrease BP in hypertension.^h

  
  


• 
  

  Important role in bone and mineral homeostasis and can directly affect bone cell formation and influence hydroxyapatite crystal formation and growth; deficiency may be risk factor for osteoporosis.^h

  
  


• 
  

  Insulin resistance and impaired insulin secretion with deficiency.^h

  
  

Advice to Patients

• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs as well as any concomitant illnesses.^a

  
  


• 
  

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

  
  


• 
  

  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

Magnesium Sulfate

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Bulk	Crystals
Parenteral	Injection	50%*	Magnesium Sulfate Injection	Abraxis, American Regent, Hospira, IMS
	Injection, for IV use only	4% (4, 20, and 40 g)	Magnesium Sulfate Injection	Hospira
		8% (4 g)	Magnesium Sulfate Injection	Hospira

Magnesium Sulfate in Dextrose

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Parenteral	Injection, for IV use only	1% (1 g) in 5% Dextrose	Magnesium Sulfate in 5% Dextrose Injection	Hospira

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 January 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

2. Abraham AS, Rosenmann D, Kramer M et al. Magnesium in the prevention of lethal arrhythmias in acute myocardial infarction. Arch Intern Med. 1987; 147:753-5. [IDIS 227956] [PubMed 3548627]

6. Rasmussen HS, Norregard P, McNair P et al. Intravenous magnesium in acute myocardial infarction. Lancet. 1986; 1:234-6. [IDIS 210464] [PubMed 2868254]

7. Rasmussen HS, Grnbaek M, Cintin C et al. One-year death rate in 270 patients with suspected acute myocardial infarction, initially treated with intravenous magnesium or placebo. Clin Cardiol. 1988; 11:377-81. [PubMed 3396238]

8. Allen BJ, Brodsky MA, Capparelli EV et al. Magnesium sulfate therapy for sustained monomorphic ventricular tachycardia. Am J Cardiol. 1989; 64:1202-4. [IDIS 305714] [PubMed 2816773]

9. Banai S et al. Magnesium sulfate is the treatment of choice for torsades de pointes if the right dose is given. Am J Cardiol. 1989; 65:266.

10. Tzivoni D, Banai S, Schuger C et al. Treatment of torsade de pointes with magnesium sulfate. Circulation. 1988; 79:392-7.

11. Skobeloff EM, Spivey WH, McNamara RM et al. Intravenous magnesium sulfate for the treatment of acute asthma in the emergency department. JAMA. 1989; 262:1210-3. [IDIS 258000] [PubMed 2761061]

12. Okayama H, Aikawa T, Okayama M et al. Bronchodilating effect of intravenous magnesium sulfate in bronchial asthma. JAMA. 1987; 257:1076-8. [IDIS 225846] [PubMed 3806898]

13. American College of Obstetricians and Gynecologists (AGOG) Committee on Technical Bulletins. Preterm labor. Technical Bulletin No. 206. Washington, DC: American College of Obstetricians and Gynecologists; 1995 Jun:1-10.

14. Morales WJ, Madhav H. Efficacy and safety of indomethacin compared with magnesium sulfate in the management of preterm labor: a randomized study. Am J Obstet Gynecol. 1993; 169:97-102. [IDIS 318916] [PubMed 8333483]

15. Glock JL, Morales WJ. Efficacy and safety of nifedipine versus magnesium sulfate in the management of preterm labor: a randomized study. Am J Obstet Gynecol. 1993; 169:960-4. [IDIS 321360] [PubMed 8238157]

16. Beall MH, Edgar BW, Paul RH et al. A comparison of ritodrine, terbutaline, and magnesium sulfate for the suppression of preterm labor. Am J Obstet Gynecol. 1985; 153:854-9. [IDIS 211026] [PubMed 4073155]

17. Hollander DI, Nagey DA, Pupkin MJ. Magnesium sulfate and ritodrine hydrochloride: a randomized comparison. Am J Obstet Gynecol. 1987; 156:631-7. [IDIS 227015] [PubMed 3548382]

18. Wilkins IA, Lynch L, Mehalek KE et al. Efficacy and side effects of magnesium sulfate and ritodrine as tocolytic agents. Am J Obstet Gynecol. 1988; 159:685-9. [IDIS 246807] [PubMed 3048103]

19. Lewis DF, Grimshaw A, Brooks GG et al. A comparison of magnesium sulfate and indomethacin to magnesium sulfate only for tocolysis in preterm labor with advanced cervical dilation. Southern Med J. 1995; 88:737-40. [PubMed 7597478]

20. Travis BE, McCullough JM. Pharmacotherapy of preterm labor. Pharmacotherapy. 1993; 13:28-36. [IDIS 311789] [PubMed 8437965]

21. Cox SM, Sherman ML, Leveno KJ. Randomized investigation of magnesium sulfate for prevention of preterm birth. Am J Obstet Gynecol. 1990; 163:767-72. [IDIS 272666] [PubMed 2206069]

22. Elliott JP. Subtherapeutic doses of magnesium sulfate do not inhibit preterm labor. Am J Obstet Gynecol. 1992; 167:568. [IDIS 301174] [PubMed 1497070]

23. Madden C, Owen J, Hauth JC. Magnesium tocolysis: serum levels versus success. Am J Obstet Gynecol. 1990; 162:1177-80. [IDIS 301277] [PubMed 2339717]

24. Kosasa TS, Busse R, Wahl N et al. Long-term tocolysis with combined intravenous terbutaline and magnesium sulfate: a 10-year study of 1000 patients. Obstet Gynecol. 1994; 84:369-73. [IDIS 33

Vertizine

Vertizine may be available in the countries listed below.

Ingredient matches for Vertizine

Cinnarizine

Cinnarizine is reported as an ingredient of Vertizine in the following countries:

• Indonesia

International Drug Name Search

Tusilin

Tusilin may be available in the countries listed below.

Ingredient matches for Tusilin

Ambroxol

Ambroxol is reported as an ingredient of Tusilin in the following countries:

• Turkey

International Drug Name Search

memantine

me-MAN-teen

Commonly used brand name(s)

In the U.S.

• Namenda


• Namenda XR

Available Dosage Forms:

• Capsule, Extended Release


• Tablet


• Solution

Therapeutic Class: Central Nervous System Agent

Pharmacologic Class: N-Methyl-D-Aspartate Receptor Antagonist

Uses For memantine

Memantine is used to treat moderate to severe Alzheimer's disease. Memantine is not a cure for Alzheimer's disease but it can help people with the disease. Memantine will not cure Alzheimer's disease, and it will not stop the disease from getting worse.

memantine is available only with your doctor's prescription.

Before Using memantine

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

Allergies

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

Pediatric

Appropriate studies on the relationship of age to the effects of memantine have not been performed in the pediatric population.

Geriatric

No information is available on the relationship of age to the effects of memantine in geriatric patients.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	B	Animal studies have revealed no evidence of harm to the fetus, however, there are no adequate studies in pregnant women OR animal studies have shown an adverse effect, but adequate studies in pregnant women have failed to demonstrate a risk to the fetus.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

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

• Epilepsy or seizures or


• Urinary tract problems (e.g., bladder problems, difficulty with urination)—Use with caution. May make these conditions worse.

• Kidney disease or


• Liver disease—Use with caution. The effects may be increased because of slower removal of the medicine from the body.

Proper Use of memantine

Take memantine exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered.

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

You may take memantine with or without food.

Swallow the extended-release capsules whole. Do not break, crush, or chew them.

If you cannot swallow the extended-release capsule, you may open it and pour the medicine into a small amount of soft food such as applesauce. Stir this mixture well and swallow it without chewing.

For patients taking the oral liquid:

• Remove the oral dosing syringe along with the cap and plastic tube from the bag and attach to tube to the cap.


• Open the child-resistant cap on the bottle by pushing down on the cap while turning the cap counter-clockwise (to the left) and remove the cap and seal from the bottle.


• Insert the plastic tube fully into the bottle and screw the cap tightly onto the bottle by turning the cap clockwise (to the right).


• Keeping the bottle upright on the table, remove the lid to uncover the opening on the top of the cap. With the plunger fully depressed, insert the tip of the syringe firmly into the opening of the cap.


• While holding the syringe, gently pull the plunger of the syringe up to draw medicine into the syringe.


• Remove the syringe from the cap opening. Invert the syringe (point tip upwards) and slowly press the plunger to a level that pushed out any large air bubbles that may be present. Keep the plunger in this position.


• Re-insert the tip of the syringe into the cap opening. While holding the syringe, continue to gently pull out the plunger until the bottom of the black ring of the plunger reaches the appropriate mark on the syringe that corresponds to the dose prescribed.


• Remove the syringe from the bottle and swallow the oral solution directly from the syringe. Do not mix with any other liquid.


• After use, reseal the bottle by snapping the attached lid closed.


• Rinse the empty syringe by inserting the open end of the syringe into a glass of water, pulling the plunger out to draw in water, and pushing the plunger in to remove the water. Repeat several times. Allow the syringe to air dry.

Dosing

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

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

• For treatment of Alzheimer's disease:
  
  • For oral dosage form (extended-release capsules):
    
    • Adults—At first, 7 milligrams (mg) once a day. Your doctor may gradually increase your dose as needed. However, the dose is usually not more than 28 mg per day.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  
  • For oral dosage form (solution and tablets):
    
    • Adults—At first, 5 milligrams (mg) once a day. Your doctor may gradually increase your dose as needed. However, the dose is usually not more than 10 mg two times a day.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  

Missed Dose

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

Storage

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

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

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

Precautions While Using memantine

It is very important that your doctor check your progress at regular visits to make sure that memantine is working properly and to check for unwanted effects.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

memantine Side Effects

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

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

Less common

• Bloating or swelling of the face, arms, hands, lower legs, or feet


• blurred vision


• dizziness


• headache


• nervousness


• pounding in the ears


• rapid weight gain


• slow or fast heartbeat


• tingling of the hands or feet


• unusual weight gain or loss

Incidence not known

• Abdominal or stomach pain


• agitation


• black, tarry stools


• bleeding gums


• blistering, peeling, or loosening of the skin


• blood in the urine or stools


• chest pain


• coma


• constipation


• continuing vomiting


• convulsions


• dark-colored urine


• decreased urine output


• depression


• fainting


• fast, pounding, or irregular heartbeat or pulse


• general feeling of tiredness or weakness


• high fever


• high or low blood pressure


• hostility


• increased sweating


• indigestion


• infection from breathing foreign substances into the lungs


• itching


• lethargy


• light-colored stools


• lip smacking or puckering


• loss of consciousness


• muscle twitching


• no blood pressure


• no breathing


• no pulse


• numbness or tingling in the face, arms, or legs


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


• pain or swelling in the arms or legs without any injury


• pain, tension, and weakness upon walking that subsides during periods of rest


• pinpoint red spots on the skin


• pounding, slow heartbeat


• puffing of the cheeks


• rapid or worm-like movements of the tongue


• rapid weight gain


• recurrent fainting


• red irritated eyes


• red skin lesions, often with a purple center


• seizures


• severe constipation


• severe headache


• severe muscle stiffness


• severe vomiting


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


• stupor


• sudden severe weakness


• swelling of the face, ankles, or hands


• total body jerking


• trouble with speaking or walking


• troubled breathing


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


• uncontrolled chewing movements


• unusual bleeding or bruising


• unusually pale skin


• vomiting


• yellow eyes and skin

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

More common

• Confusion

Less common

• Anxiety


• back pain


• bladder pain


• bloody or cloudy urine


• change in walking and balance


• chills


• clumsiness or unsteadiness


• cough producing mucus


• coughing


• diarrhea


• difficult, burning, or painful urination


• difficulty with breathing


• difficulty with moving


• discouragement


• dry mouth


• fear


• feeling sad or empty


• fever


• frequent urge to urinate


• general feeling of discomfort or illness


• hyperventilation


• insomnia


• irritability


• joint pain


• loss of appetite


• loss of bladder control


• loss of interest or pleasure


• lower back or side pain


• muscle pain or stiffness


• nausea


• nervousness


• pain


• pain in the joints


• restlessness


• seeing, hearing, or feeling things that are not there


• shortness of breath


• sleepiness or unusual drowsiness


• sore throat


• tightness in the chest


• tiredness


• trouble with concentrating


• trouble with sleeping


• unusual tiredness or weakness


• vomiting


• wheezing

Incidence not known

• Burning feeling in the chest or stomach


• burning, numbness, pain, or tingling in all fingers except smallest finger


• cold sweats


• cool pale skin


• decreased interest in sexual intercourse


• difficulty with swallowing


• general feeling of discomfort or illness


• heartburn


• inability to have or keep an erection


• increased hunger


• large amounts of fat in the blood


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


• nightmares


• shakiness


• slurred speech


• stomach cramps


• stomach upset


• tenderness in the stomach area


• watery or bloody diarrhea

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

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

See also: memantine side effects (in more detail)

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

More memantine resources

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

• Memantine MedFacts Consumer Leaflet (Wolters Kluwer)


• Memantine Hydrochloride Monograph (AHFS DI)


• Namenda Prescribing Information (FDA)


• Namenda Consumer Overview

Compare memantine with other medications

• Alzheimer's Disease

Tykerb

Tykerb is a brand name of lapatinib, approved by the FDA in the following formulation(s):

TYKERB (lapatinib ditosylate - tablet; oral)

• 
  Manufacturer: SMITHKLINE BEECHAM
  
  Approval date: March 13, 2007
  
  Strength(s): EQ 250MG BASE ^[RLD]

Has a generic version of Tykerb been approved?

No. There is currently no therapeutically equivalent version of Tykerb available.

Note: Fraudulent online pharmacies may attempt to sell an illegal generic version of Tykerb. These medications may be counterfeit and potentially unsafe. If you purchase medications online, be sure you are buying from a reputable and valid online pharmacy. Ask your health care provider for advice if you are unsure about the online purchase of any medication.

See also: About generic drugs.

Related Patents

Patents are granted by the U.S. Patent and Trademark Office at any time during a drug's development and may include a wide range of claims.

• 
  Fused heterocyclic compounds as protein tyrosine kinase inhibitors
  Patent 6,391,874
  Issued: May 21, 2002
  Inventor(s): George Stuart; Cockerill & Malcolm Clive; Carter & Stephen Barry; Guntrip & Kathryn Jane; Smith
  Assignee(s): SmithKline Beecham Corporation
  Substituted heteroaromatic compounds of formula (I) and in particular substituted quinolines and quinazolines, are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis, or a salt or solvate thereof; wherein X is N or CH; Y is a group W(CH2), (CH2)W, or W, in which W is O, S(O)m wherein m is 0, 1 or 2, or NRa wherein Ra is hydrogen or a C1-8 alkyl group; R1 represents a phenyl group or a 5- or 6-membered heterocyclic ring containing 1 to 4 heteroatoms selected from N, O or S(O)m, wherein m is as defined above, with the provisos that the ring does not contain two adjacent O or S(O)m atoms and that where the ring contains only N as heteroatom(s) the ring is C-linked to the quinazoline or quinoline ring, R1 being optionally substituted by one or more R3;groups; P&equals;0 to 3; U, R2, R3 are as defined in the application.
  
  Patent expiration dates:
  
  
  • July 11, 2017
    
    ✓ 
    Patent use: TREATMENT OF PATIENTS WITH ADVANCED OR METASTATIC BREAST CANCER WHOSE TUMORS OVEREXPRESS HER2 AND WHO HAVE RECEIVED PRIOR THERAPY INCLUDING ANTHRACYCLINE, A TAXANE AND TRASTUZUMAB
    ✓ 
    Drug substance
    ✓ 
    Drug product
  
  



• 
  Heterocyclic compounds
  Patent 6,713,485
  Issued: March 30, 2004
  Inventor(s): Malcolm Clive; Carter & George Stuart; Cockerill & Stephen Barry; Guntrip & Karen Elizabeth; Lackey & Kathryn Jane; Smith
  Assignee(s): SmithKline Beecham Corporation
  The present invention relates to substituted heteroaromatic compounds, methods for their preparation, pharmaceutical compositions containing them and their use in medicine. Specifically, the invention relates to quinazoline derivatives useful in treating disorders mediated by protein tyrosine kinase activity, in particular erbB-2 and/or EGFR activity.
  
  Patent expiration dates:
  
  
  • September 29, 2020
    
    ✓ 
    Patent use: TREATMENT OF PATIENTS WITH ADVANCED OR METASTATIC BREAST CANCER WHOSE TUMORS OVEREXPRESS HER2 AND WHO HAVE RECEIVED PRIOR THERAPY INCLUDING ANTHRACYCLINE, A TAXANE AND TRASTUZUMAB
    ✓ 
    Drug substance
    ✓ 
    Drug product
  
  



• 
  Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors
  Patent 6,727,256
  Issued: April 27, 2004
  Inventor(s): Malcolm Clive; Carter & George Stuart; Cockerill & Stephen Barry; Guntrip & Karen Elizabeth; Lackey & Kathryn Jane; Smith
  Assignee(s): SmithKline Beecham Corporation
  Substituted heteroaromatic compounds of formula (I), wherein X is N or CH; Y is CR1 and V is N; or Y is N and V is CR1; or Y is CR1 and V is CR2; or Y is CR2 and V is CR1; R1 represents a group CH3SO2CH2CH2NHCH2—Ar—, wherein Ar is selected from phenyl, furan, thiophene, pyrrole and thiazole, each of which may optionally be substituted by one or two halo, C1-4alkyl or C1-4alkoxy groups; R2 is selected from the group comprising hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkoxy, C1-4alkylamino and di&lsqb;C1-4alkyl&rsqb;amino; U represents a phenyl, pyridyl, 3H-imidazolyl, indolyl, isoindolyl, indolinyl, isoindolinyl, 1H-indazolyl, 2,3-dihydro-1H-indazolyl, 1H-benzimidazolyl, 2,3-dihydro-1H-benzimidazolyl or 1H-benzotriazolyl group, substituted by an R3 group and optionally substituted by at least one independently selected R4 group; R3 is selected from a group comprising benzyl, halo-, dihalo- and trihalobenzyl, benzoyl, pyridylmethyl, pyridylmethoxy, phenoxy, benzyloxy, halo-, dihalo- and trihalobenzyloxy and benzenesulphonyl, or R3 represents trihalomethylbenzyl or trihalomethylbenzyloxy; or R3 represents a group of formula (a) wherein each R5 is independently selected from halogen, C1-4alkyl, C1-4alkoxy; and n is 0 to 3; each R4 is independently hydroxy, halogen, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, amino, C1-4alkylamino, di&lsqb;C1-4alkyl&rsqb;amino, C1-4alkylthio, C1-4alkylsulphinyl, C1-4alkylsulphonyl, C1-4alkylcarbonyl, carboxy, carbamoyl, C1-4alkoxycarbonyl, C1-4alkanoylamino, N-(C1-4alkyl)carbamoyl, N,N-di(C1-4alkyl)carbamoyl, cyano, nitro and trifluoromethyl; and salts and solvates thereof, are disclosed, as are methods for their preparation, pharmaceutical compositions containing them and their use in medicine.
  
  Patent expiration dates:
  
  
  • January 8, 2019
    
    ✓ 
    Patent use: TREATMENT OF PATIENTS WITH ADVANCED OR METASTATIC BREAST CANCER WHOSE TUMORS OVEREXPRESS HER2 AND WHO HAVE RECEIVED PRIOR THERAPY INCLUDING ANTHRACYCLINE, A TAXANE AND TRASTUZUMAB
    ✓ 
    Drug substance
    ✓ 
    Drug product
  
  



• 
  Heterocyclic compounds
  Patent 6,828,320
  Issued: December 7, 2004
  Inventor(s): George Stuart; Cockerill & Malcolm Clive; Carter & Stephen Barry; Guntrip & Kathryn Jane; Smith
  Assignee(s): SmithKline Beecham Corporation
  Substituted heteroaromatic compounds, and in particular substituted quinolines and quinazolines, are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis.
  
  Patent expiration dates:
  
  
  • July 11, 2017
    
    ✓ 
    Patent use: TREATMENT OF PATIENTS WITH ADVANCED OR METASTATIC BREAST CANCER WHOSE TUMORS OVEREXPRESS HER2 AND WHO HAVE RECEIVED PRIOR THERAPY INCLUDING ANTHRACYCLINE, A TAXANE AND TRASTUZUMAB
  
  



• 
  Quinazoline ditosylate salt compounds
  Patent 7,157,466
  Issued: January 2, 2007
  Inventor(s): McClure; Michael Scott & Osterhout; Martin Howard & Roschangar; Frank & Sacchetti; Mark Joseph
  Assignee(s): SmithKline Beecham (Cork) Limited
  Ditosylate salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorde4rs characterized by aberrant erbB family PTK activity.
  
  Patent expiration dates:
  
  
  • November 19, 2021
    
    ✓ 
    Drug substance
    ✓ 
    Drug product
  
  

Related Exclusivities

Exclusivity is exclusive marketing rights granted by the FDA upon approval of a drug and can run concurrently with a patent or not. Exclusivity is a statutory provision and is granted to an NDA applicant if statutory requirements are met.

• Exclusivity expiration dates:
  • March 13, 2012 - NEW CHEMICAL ENTITY
  
  
  • January 29, 2013 - FOR USE IN COMBINATION WITH LETROZOLE FOR THE TREATMENT OF POSTMENOPAUSAL WOMEN WITH HORMONE RECEPTOR POSITIVE METASTATIC BREAST CANCER THAT OVEREXPRESSES THE HER2 RECEPTOR FOR WHOM HORMONAL THERAPY IS INDICATED
  
  

See also...

• Tykerb Consumer Information (Drugs.com)
• Tykerb Consumer Information (Wolters Kluwer)
• Tykerb Consumer Information (Cerner Multum)
• Tykerb Advanced Consumer Information (Micromedex)
• Tykerb AHFS DI Monographs (ASHP)
• Lapatinib Consumer Information (Wolters Kluwer)
• Lapatinib Consumer Information (Cerner Multum)
• Lapatinib Advanced Consumer Information (Micromedex)
• Lapatinib Ditosylate AHFS DI Monographs (ASHP)

Mecon

Mecon may be available in the countries listed below.

Ingredient matches for Mecon

Meloxicam

Meloxicam is reported as an ingredient of Mecon in the following countries:

• Taiwan

International Drug Name Search

Biluta

Biluta may be available in the countries listed below.

Ingredient matches for Biluta

Bicalutamide

Bicalutamide is reported as an ingredient of Biluta in the following countries:

• Ireland

International Drug Name Search