Esomeprazole

From Pubdrug

Jump to: navigation, search
Certified
You are reading a certified PubDrug document. This document is complete and accurate to the best of the knowledge of the author and reviewer. This document cannot be edited without being unlocked by the PubDrug admin. Edits or updates may be recommended under the Discussion tab for this document.

Authored by: Mldutka

Certified by: ty7 14:58, 24 April 2007 (PDT)


Esomeprazole Quick Reference
Esomeprazole
IUPAC Name
(S)-5-methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)

methylsulfinyl]-3H-benzoimidazole

Chemical Information
Empirical Formula C17H19N3O3S
Molecular Weight 345.417
General Drug Information
Classification Proton Pump Inhibitor (PPI)
Schedule Legend
How Supplied Oral Capsules: Delayed-Release 20mg, Delayed-Release 40mg; Unit dose packages of 20 and 40mg for oral suspension; 20 and 40mg powder for intravenous injection
Trade Names Nexium
Pregnancy Category B
Breast Feeding Concentrations of esomeprazole have been found in breast milk. Caution should be used.
Generic Availability Generic not available
Patent Expiration Date April 19, 2007
Administration Information
Routes Oral, Nasogastric/Gastric Tube, Intravenous
Method Oral: taken once daily one hour before meals

Nasogastric/ Gastric tube: given once daily

Intravenous injection: infused once daily for 3-30 minutes with or without food for 5 days

Pharmacokinetic Information
Absorption F = 64% (single dosing)
F = 90% (multiple dosing)
F = 100% (Intravenous dosing)
Cmax = 4.7-2.1 hours (Oral dosing)
Cmax = 3.9-7.5 hours (Intravenous dosing)
tmax = 1.5 hours (Oral dosing)
Distribution Vd = 16 L (Oral and Intravenous dosing)
Protein binding ~ 98%
Metabolism Hepatic via CYP2C19 and 3A4 enzymes to hydroxy, desmethyl, and sulfone metabolites (all inactive)
Excretion T1/2 = 1_1.5 hours (Oral and Intravenous dosing)
80% Urine

20% Feces

Contents

Brand/Trade Names of Drug

Nexium

Generic Name of Drug

Esomeprazole magnesium (es oh ME pray zol)

Esomeprazole Pronunciation

Back to top

Description

Esomeprazole belongs to a class of medications know as Proton Pump Inhibitors (PPI's). PPI's, via the inhibition of H+/K+ ATPase enzyme pumps located in the gastric lumen, decrease the amount of gastric acid produced. Esomeprazole consists only of the active isomer (S-isomer), whereas its counterpart, Omeprazole contains the active and in-active isomers (R and S-isomers).[1]

Studies have shown that a decrease in the amount of gastric acid produced was beneficial for patients with Erosive Esophagitis, Symptomatic Gastroesophageal Reflux Disease (GERD), NSAID-Associated Gastric Ulcers, Heliocobacter pylori (H. pylori) infections, and Zollinger-Ellison Syndrome.[2] In patients with gastro-esophageal reflux disease (GERD), PPI_s have been shown to relieve patients of GERD symptoms. In other cases, such as patients with h. pylori infections or the development of ulcers with the use of NSAID_s, PPI_s have again proven to be efficacious in symptomatic and gastric damage relief.[3][4]


Back to top

Mechanism of action

Esomeprazole, like other PPI's, is a prodrug that is activated in an acidic environment to it's active form (sulfenamide). The active form of the prodrug creates a covalent bond to H+/K+ ATPase pumps located on parietal cells in the gastric lumen. H+/K+ ATPase pumps are involved in the final step of the acid secretion pathway. This bond irreversibly inhibits the subsequent release of hydrogen ions. Inhibition of acid production is maintained until new H+/K+ ATPase pumps are regenerated (~18 hours).[3][1]


Back to top

Time Required for Therapeutic Response

  • Initial: ~1 day[5]
  • Maximum: ~7 days[5]


Back to top

Pharmacokinetics

Absorption

Esomeprazole, intended for the oral route of administration, is formulated with an enteric coating to prevent rapid dissolution in the acidic environment of the gastric cavity. The different strengths of oral esomeprazole (20mg and 40mg) create the ranges seen in Cmax, Tmax and AUC. A single 40mg oral dose, taken without food, reaches its peak of 4.7 _mol/L (Cmax) within 1.5 hours (Tmax) with a bioavailability of 64%. The plasma concentration-time curve (AUC) for this single dose is 4.32 _mol*h/L. After multiple doses in fasting conditions, bioavailability increases to ~90% and the AUC increases to 11.2 _mol*h/L. The AUC decreases by 43-53% when a single dose is taken with food.[1][2] Due to the differences in isomeric composition, the AUC of Esomeprazole is 80% higher that that of Omeprazole. This is due to a decrease in the clearance and first-pass metabolism of the S-isomer.[1]

Intravenous forms of esomeprazole have a slightly different pharmacokinetic profile than the oral forms. The different strengths of IV esomeprazole (20mg and 40mg) create the ranges seen in Cmax and AUC. After the IV administration of a 40mg dose, given once daily for a total of 5 days, the AUC is 16.2 _mol*h/L with a peak concentration (Cmax) of 7.51 _mol/L.[6][7]

Distribution

Esomeprazole as an apparent volume of distribution of 16 L. Additionally, esomeprazole is approximately 97% protein bound. This applies to both the oral and intravenous forms.

Metabolism

Esomeprazole metabolism is mediated via the cytochrome P450 enzyme system (CYP450). The hydroxyl and desmethyl metabolites are formed by the CYP219 isoenzyme, while the sulphone metabolite is formed via the CYP3A4 enzyme. All metabolites formed are inactive.[2][1]

Excretion

The inactive metabolites of esomeprazole are mainly renally excreted (80%) with some fecal elimination (20%). A minimal amount of the active parent drug is excreted in the urine (1%). The elimination half life for both the oral and intravenous forms ranges from 1-1.5 hours, with a slightly longer half life with the oral forms of esomeprazole. Elimination is complete with no accumulation of drug.[8][2]


Back to top

Special Population Pharmacokinetics

  • Renal Insufficiency

Due to the insignificant amount of renal elimination of active esomeprazole, there are expected to be no differences between healthy and renally impaired patients. No dosage adjustments are necessary.[2]

  • Hepatic Insufficiency

Patients with sever hepatic insufficiency (Child Pugh Class C) have been shown to have a 2-3 times higher AUC of esomeprazole than those with normal hepatic function. Those with mild-moderate hepatic insufficiency (Child Pugh Class A and B) reported no change in AUC.[2][9]

  • Hemodialysis

Unavailable

  • Geriatric

Both AUC and Cmax were higher in elderly patients, but this was without any significance. No dosage adjustments necessary.[2]

  • Pediatric

Any changes in patients ages 12-17 years old were similar to the changes seen in adult patients. No dosage changes are necessary.[2]

  • Gender

In female patients, AUC and Cmax were slightly higher than males, but without any significance. No dosage changes are necessary.[2]


Back to top

Indications/Dosage

FDA Approved Indications (Oral)


Back to top

FDA Approved Indications (Intravenous)


Back to top

Dosage

Note: The use of 40mg over 20mg has no proven benefit.[2]


Back to top

Oral

  • Gastro-esophageal Reflux Disease (GERD) with or without Erosive Esophagitis[2]
    • Healing/Symtomatic Relief 20-40mg once daily for 4-8 weeks. An additional 4-8 weeks of therapy if initial 4-8 weeks was ineffective.
    • Maintenance 20-40mg once daily for up to 6 months. Studies have not been carried out past 6 months.
  • NSAID-associated Gastric Ulcer Prophylaxis[2]
    • 20-40mg once a day. Studies have been done for up to 26 weeks of use.
  • Heliocobacter pylori (H.pylori) Eradication for Ulcer Prophylaxis
    • 40mg once a day for ~4weeks. Eradication of H.pylori is seen when esomeprazole is used in combination with amoxicillin and clarithromycin.
  • Zollinger-Ellison Syndrome[2]
    • Typical dose is 40mg twice daily. Patients have been show to see therapeutic results with daily dosages ranging from 80-240mg.
  • Duodenal Ulcer[1]
    • 40mg once a day for ~4weeks. Eradication of H.pylori is seen when esomeprazole is used in combination with amoxicillin and clarithromycin.


Back to top

Intravenous

  • Gastroesophegeal Reflux Disease (GERD) with a history of Erosive Esophagitis[6][1]
    • 20-40mg once daily infusions given over 3-30 minutes for up to 10 days. Change to oral form if possible after 10 days.
  • Maxium Dosage Limits[1]
    • Adults (PO/IV) 40mg/day
    • Adults (Zollinger-Ellison Syndrome) 240mg/day
    • Elderly (PO/IV) 40mg/day
    • Elderly (Zollinger-Ellison Syndrome) 240mg/day
    • Adolescents > 17 years (PO) 40mg/day
    • Children and Adolescents 12-17 years (PO) 40mg/day
    • Children <12 years Safe and effective use have not been established


Back to top

Administration

  • Capsule[2]
    • Route: Oral
      • Method: Swallow capsule whole with a full glass of water or capsule can be opened and sprinkled/mixed with applesauce. Capsule should be taken once daily and is best if daily dose is taken one hour prior to a meal.
      • Special considerations: Applesauce must be at room temperature and should be administered right after mixing.
    • Route: Nasogastric Tube
      • Method: Open capsule and place granules into a catheter tipped syringe. Add 50ml of water to syringe, replace the plunger and shake contents of syringe for ~15 seconds. Attach syringe to nasogastric tube and inject syringe contents. Flush nasogastric tube with additional water. This should be done once daily.
      • Special considerations: Do not administer contents of syringe if granules are dissolved or disintergrated.
  • Powder for oral solution[2]
    • Route: Oral
      • Method: Mix contents of one packet with 15ml of water, stir and let sit for a couple of minutes to thicken. Drink suspension within 30 minutes of making. If any residual suspension remains, add more water and drink immediately.
    • Route: Nasogastric Tube
      • Method: In a catheter tipped syringe, add the contents of one packet to 15ml of water, shake and let sit for a couple of minutes to thicken. Shake the syringe and inject into nasogastric tube. Refill the syringe with 15ml of water and flush the NG- tube. Suspension must be administered within 30 minutes of making.
  • Powder for Intravenous Injection[6]
    • Route: Intravenous
      • Method: Reconstitute the powder with 5ml of 0.9% Sodium Chloride Injection, USP. Withdraw 5ml of solution and inject intravenously over no less then 3 minutes. This should be stored at room temperature and should be administered within 12 hours of making.
  • Powder for Intravenous Infusion[6]
    • Route: Intravenous
      • Method: Reconstitute the powder with 5ml of 0.9% Sodium Chloride Injection, USP, Lactated Ringer_s Injection, USP or 5% Dextrose Injection, USP. The final admixture should then be diluted to a final volume of 50ml and can then be infused intravenously over 10-30 minutes. This should be stored at room temperature. If using 0.9% Sodium Chloride Injection or Lactated Ringer_s Injection for dilution, the admixture should be administered within 12 hours of making. If using 5% Dextrose Injection for dilution, the admixture should be administered within 6 hours.


Back to top

Monitoring Parameters

  • Liver Function Tests (LFT's)
    • Esomeprazole is hepatically metabolized. The occurrence of changes in liver function tests was seen to be <1%. Monitoring of LFT_s may be reserved for those with suspected hepatic dysfunction.[2]


Back to top

Contraindications/Precautions

Contraindications

  • Benzimidazole hypersensitivity[2]


Back to top

Precautions

  • Gastric Malignancy[1]
  • Pregnancy: Although studies have been done in rats without any teratogenic outcomes, no studies have been performed in pregnant females. Caution is advised with the use of esomeprazole during pregnancy.[2]
  • Breast Feeding: Concentrations of esomeprazole have been found in breast milk. Caution should be used.[2]


Back to top

Pregnancy indications

  • Pregnancy Category: B
    • To date, there have been teratology studies done in rats without any shown harm to the fetus. This study, however, has not been performed in pregnant females but there have been sporadic reports of congenital abnormalities in infants born to mothers receiving esomeprazole therapy.[2]


Back to top

Breast-feeding indications

  • Secretion into breast milk: There are no studies of the secretion of esomeprazole into breast milk, although, concentrations of the drug have been found in breast milk. Because there have been no studies done in nursing females, caution is advised when using esomeprazole in nursing mothers. Discontinuation of the medication should be attempted if the nursing mother has indication to do so.[2]


Back to top

Drug-Drug Interactions

Esomeprazole Drug/Drug Interaction Chart
Severity Level Click here to see Severity Level Legend Increased Effect/Toxicity Decreased Effect
4 None Known atazanavir [10] Esomeprazole has been shown to decrease the AUC of atazanavir when given with ritonavir.
3 cilostazol[11] Bioavailability of these drugs is increased with CYP2C19 inhibition. Cilostazole dosage should be reduced by 50%. ampicillin[8] These medications require an acidic environment for absorption. With certain formulations, absorption of these drugs are decreased due to the resultant increase in gastric pH levels with PPI use. , delavirdine[12] These medications require an acidic environment for absorption. With certain formulations, absorption of these drugs are decreased due to the resultant increase in gastric pH levels with PPI use. , iron salts[2] These medications require an acidic environment for absorption. With certain formulations, absorption of these drugs are decreased due to the resultant increase in gastric pH levels with PPI use. , itraconazole[2] These medications require an acidic environment for absorption. With certain formulations, absorption of these drugs are decreased due to the resultant increase in gastric pH levels with PPI use. , ketoconazole[2] These medications require an acidic environment for absorption. With certain formulations, absorption of these drugs are decreased due to the resultant increase in gastric pH levels with PPI use. , H2 Blockers[13] decreases the effectiveness of PPI's because PPI's only work on active hydrogen pumps.
2 alendronate[14] The risk of having upper GI side effects is increased when alendronate is co-administered with PPI's or H2 receptor blockers by affecting the bioavailability of alendronate. , fluvoxamine[2] Has the potential to inhibit CYP2C19 enzymes thereby theoretically increasing the concentrations of drugs metabolized by this enzyme. , naproxen[15] Enteric coating of medications serves as a barrier to prevent exposure of the medication to acidic pH levels. PPI's increase the pH of the gastric cavity and will therefore increase the exposure of enteric coated medications to this area. By doing so, some adverse events such as gastric irritation or drug degradation/stability changes will occur. , voriconazole[2] Because esomeprazole is a CYP2C19 inhibitor, there is a potential for the concentrations of drugs metabolized by CYP2C19 to increase. This is only a potential and is not definite. Monitoring with the use of esomeprazole and narrow therapeutic index drugs may be advised. , warfarin[2] Because esomeprazole is a CYP2C19 inhibitor, there is a potential for the concentrations of drugs metabolized by CYP2C19 to increase. This is only a potential and is not definite. Monitoring with the use of esomeprazole and narrow therapeutic index drugs may be advised. antimuscarinics[13] Potentially decreases the effectiveness of PPI's because PPI's only work on active hydrogen pumps. , carbamazepine[16] Potentially decreases the effectiveness of PPI's because PPI's only work on active hydrogen pumps. , fluvastatin[17] Potentially decreases the effectiveness of PPI's because PPI's only work on active hydrogen pumps. , diazepam[2] Bioavailability of these drugs is increased with CYP2C19 inhibition. Diazepam dosage may not need to be altered; close monitoring is advised when used with esomeprazole. , gefitinib[18] These medications require an acidic environment for absorption. With certain formulations, absorption of these drugs are decreased due to the resultant increase in gastric pH levels with PPI use.
1 carisoprodol[2] Because esomeprazole is a CYP2C19 inhibitor, there is a potential for the concentrations of drugs metabolized by CYP2C19 to increase. This is only a potential and is not definite. Monitoring with the use of esomeprazole and narrow therapeutic index drugs may be advised. , citalopram[2] Because esomeprazole is a CYP2C19 inhibitor, there is a potential for the concentrations of drugs metabolized by CYP2C19 to increase. This is only a potential and is not definite. Monitoring with the use of esomeprazole and narrow therapeutic index drugs may be advised. , clomipramine[2] Because esomeprazole is a CYP2C19 inhibitor, there is a potential for the concentrations of drugs metabolized by CYP2C19 to increase. This is only a potential and is not definite. Monitoring with the use of esomeprazole and narrow therapeutic index drugs may be advised. , escitalopram[2] Because esomeprazole is a CYP2C19 inhibitor, there is a potential for the concentrations of drugs metabolized by CYP2C19 to increase. This is only a potential and is not definite. Monitoring with the use of esomeprazole and narrow therapeutic index drugs may be advised. , mipramine[2] Because esomeprazole is a CYP2C19 inhibitor, there is a potential for the concentrations of drugs metabolized by CYP2C19 to increase. This is only a potential and is not definite. Monitoring with the use of esomeprazole and narrow therapeutic index drugs may be advised. , mephenytoin[2] Because esomeprazole is a CYP2C19 inhibitor, there is a potential for the concentrations of drugs metabolized by CYP2C19 to increase. This is only a potential and is not definite. Monitoring with the use of esomeprazole and narrow therapeutic index drugs may be advised. , Phenytoin(fosphenytoin)[2] Because esomeprazole is a CYP2C19 inhibitor, there is a potential for the concentrations of drugs metabolized by CYP2C19 to increase. This is only a potential and is not definite. Monitoring with the use of esomeprazole and narrow therapeutic index drugs may be advised. , proguanil[2] Because esomeprazole is a CYP2C19 inhibitor, there is a potential for the concentrations of drugs metabolized by CYP2C19 to increase. This is only a potential and is not definite. Monitoring with the use of esomeprazole and narrow therapeutic index drugs may be advised. , sertraline[2] Because esomeprazole is a CYP2C19 inhibitor, there is a potential for the concentrations of drugs metabolized by CYP2C19 to increase. This is only a potential and is not definite. Monitoring with the use of esomeprazole and narrow therapeutic index drugs may be advised. , bortezomib[19] Has the potential to inhibit CYP2C19 enzymes thereby theoretically increasing the concentrations of drugs metabolized by this enzyme. , budesonide[20] Enteric coating of medications serves as a barrier to prevent exposure of the medication to acidic pH levels. PPI's increase the pH of the gastric cavity and will therefore increase the exposure of enteric coated medications to this area. By doing so, some adverse events such as gastric irritation or drug degradation/stability changes will occur. ,ceftibuten[21] Based on studies that analyzed the co-administration with ranitidine, there is a potential to have increase in both AUC and Cmax with the use of esomeprazole. , Combination therapy with clarithromycin and amoxicillin[2] The combination of the three drugs together, when used to eradicate h.pylori infections, has been shown to result in an increase in esomeprazole concentraions. , dexmethylphenidate [22] The dissolution of dexmethylphenidate long acting formulations is alterd by various pH levels. The elevated pH levels created by PPI_s leads to an increased rate of dissolution for this medication and therefore diminishes it's long acting effects, but may increase adverse events/drug concentrations. , digoxin[23] Alterations in gastric pH may effect the AUC of this drug. An increased pH with the use of omeprazole has been shown to cause an increase in digoxin AUC by about 10%. There is a potential for the same to occur with the use of esomeprazole. Monitoring is advised as a precautionary measure. , efavirenz[24] Has the potential to inhibit CYP2C19 enzymes thereby theoretically increasing the concentrations of drugs metabolized by this enzyme. , felbamate Has the potential to inhibit CYP2C19 enzymes thereby theoretically increasing the concentrations of drugs metabolized by this enzyme. , fluconazole Has the potential to inhibit CYP2C19 enzymes thereby theoretically increasing the concentrations of drugs metabolized by this enzyme. , fluoxetine Has the potential to inhibit CYP2C19 enzymes thereby theoretically increasing the concentrations of drugs metabolized by this enzyme. , imipramine[2] Because esomeprazole is a CYP2C19 inhibitor, there is a potential for the concentrations of drugs metabolized by CYP2C19 to increase. This is only a potential and is not definite. Monitoring with the use of esomeprazole and narrow therapeutic index drugs may be advised. , isoniazid Has the potential to inhibit CYP2C19 enzymes thereby theoretically increasing the concentrations of drugs metabolized by this enzyme. , methylphenidate [22] The dissolution of dexmethylphenidate long acting formulations is alterd by various pH levels. The elevated pH levels created by PPI_s leads to an increased rate of dissolution for this medication and therefore diminishes it's long acting effects, but may increase adverse events/drug concentrations. , ticlopidine Has the potential to inhibit CYP2C19 enzymes thereby theoretically increasing the concentrations of drugs metabolized by this enzyme. Cyanocobalamin (vitamin B12)[25] Cyanocobalamin requires an acidic environment in order to be released from its dietary source. Effects with esomeprazole are based on those observed with omeprazole. , misoprostol[13] Potentially decreases the effectiveness of PPI's because PPI's only work on active hydrogen pumps. , octreotide[13] Potentially decreases the effectiveness of PPI's because PPI's only work on active hydrogen pumps. , sucralfate[26] Based on an interaction with lansoprazole, there is a potential for sucralfate to decrease the bioavailability of esomeprazole.

Back to top

Drug-Food-Herb Interactions

Esomeprazole Drug/Food/Herb Interaction Chart
Severity Level Click here to see Severity Level Legend Increased Effect/Toxicity Decreased Effect
4 None Known None Known
3 None Known None Known
2 None Known None Known
1 None Known None Known


Back to top

Adverse Reactions/Side Effects

Esomeprazole is generally well tolerated. Most adverse events have <1% occurance. It appears that CNS affects (headaches) are more common with IV dosage forms. The most common adverse event for all dosage forms was diarrhea (1-2.5%) and nausea (0-7%). [2][8]


Esomeprazole Adverse Reactions Chart
Incidence Body System Adverse Reactions
> 10 % CNS Headache (IV 11%/oral 3-6%)
2-10% CNS Dizziness (3%)
CV None listed
Dermatologic Injection site reaction (IV 2%)
GI Flatulence (10%), nausea (I.V. 6%/oral 2%), abdominal pain (IV 6%/oral 3-4%), diarrhea (4%), xerostomia (I.V. 4%/oral _1%), dyspepsia (0-6%), constipation (3%)
GU None listed
Neuromuscular & skeletal None listed
Respiratory Sinusitis (I.V. 2%), respiratory infection (IV 1%)
Misc None listed
< 2% All abdominal pain, general/peripheral/facial edema, allergic reaction, back pain, chest pain, asthenia, hot flushes, fatigue, fever, flu-like disorder, malaise, rigors, pain, hypertension, tachycardia, goiter, bowel irregularity, consstipation aggravated, dyspepsia, dysphagia, epigastric pain, erucatation, esophageal disorder, frequent stools, GI hemorrhage, diccup, mouth/rectal/pharynx/tongue disorder, serum gastrin increased, ulcerative stomatitis, vomiting, earache, tinnitus, anemia, cervical lymphoadenopathy, epistaxis, leukocytosis, leudopenia, thrombocytopenia, bilirubinemia, hepatic function abnormal, SGOT/SGPT increased, glycosuria, hyperuricemia, hyponatermia, increase alkaline phosphatase, thirst, vitamin B12 deficiency, weight increase/decrease, arthralgia, arthropathy, cramps, fibromyalgia syndrome, hernia, polymyalgia rheumatica, anorexia, apathy, appetite increased, confusion, depression aggravated, hypertonia, nervousness, hypoesthesia, impotence, insomnia, migraine, paresthesia, somnolence, vertigo, visual field defect, dysmenorrhea, vafinitis, coughing, acne, dermatitis, pruritis, rash, skin inflammation, increased sweating, urticaria, otitis media, taste loss, abnormal urine, albuminuria, cystitis, dysuria, fungal infection, hematuria, micturition frequency, polyuria, conjuctivitis


Back to top

Overdosage Measures

Dosages of around 510 mg/kg were observed to be toxic in rats. Signs of toxicity seen in rats included changes in respiratory frequency, tremor, reduced motor activity, ataxia, and intermittent clonic convulsions. In humans, doses greated than 120 times greater than the recommended dosages created toxicity such as confusion, drowsiness, blurred vision, tachcardia, nausea, flushing, headache and dry mouth. Toxicity was rarely seen when doses were kept within recommended therapeutic ranges. Overall, esomeprazole is well tolerated.[2]


Back to top

Product Information and Distribution

Esomeprazole Product Availability Information
Name Manufacturer Dosage Form Strength Quantity NDC Storage
Nexium[2] AstraZeneca Oral Delayed Release Capsules 20 mg 30 00186-5020-31 25_C (77_F)
100 00186-5022-28
90 00186-0520-54
1000 00186-5020-82
40 mg 30 00186-5040-31
100 00186-5042-28
90 00186-5040-54
1000 00186-5040-82
Delayed-Release Powder for Suspension 20 mg unit dose packages of 30 00186-4020-01
40 mg unit dose packages of 30 00186-4040-01
IV Powder for Injection 20 mg 1 carton of 10 vials (each vial=20mg of esomeprazole) 00186-6020-01
40 mg 1 carton of 10 vials (each vial=40mg of esomeprazole) 00186-6040-01
  • Manufacturers/Distributors
    • AstraZeneca LP, Wilmington, DE
  • Inactive ingredients
    • glyceryl monostearate 40-55, hydroxypropyl cellulose, hypromellose, magnesium stearate, methacrylic acid copolymer type C, polysorbate 80, sugar spheres, talc, and triethyl cirtate [2]

Back to top

Pharmacogenomic Information

Esomeprazole Pharmacogenomic Information


Back to top

References

  1. _ 1.0_1.1_1.2_1.3_1.4_1.5_1.6_1.7_1.8 Clinical Pharmacology: Nexium Monograph. Available at: www.clinicalpharmacology.com
  2. _ 2.00_2.01_2.02_2.03_2.04_2.05_2.06_2.07_2.08_2.09_2.10_2.11_2.12_2.13_2.14_2.15_2.16_2.17_2.18_2.19_2.20_2.21_2.22_2.23_2.24_2.25_2.26_2.27_2.28_2.29_2.30_2.31_2.32_2.33_2.34_2.35_2.36_2.37_2.38_2.39_2.40_2.41_2.42 Nexium(esomeprazole magnesium)package insert for PO use Wilmington,DE; AstraZeneca; 2006 October.
  3. _ 3.0_3.1 Integrative Inflammation Pharmacology: Peptic Ulcer Disease. Eds: Golan DE., et al. Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy. pgs: 389-69. Baltimore, Lippincott Williams & Wilkins.
  4. _ Yeomans, Neville D.; Tulassay, Zsolt; Juhasz, Laszlo; Racz, Istvan; Howard, John M.; van Rensburg, Christoffel J.; Swannell, Anthony J.; Hawkey, Christopher J. A Comparison of Omeprazole with Ranitidine for Ulcers Associated with Nonsteroidal Antiinflammatory Drugs.N Engl J Med 1998;338:719-726.
  5. _ 5.0_5.1 Simon,B; M_ller, P; Pascu, O. Intra-oesophageal pH profiles and pharmacokinetics of pantoprazole and esomeprazole: a crossover study in patients with gastro-oesophageal reflux disease. European Journal of Gastroenterology & Hepatology. Volume 15(7), July 2003, pp 791-799.
  6. _ 6.0_6.1_6.2_6.3 Nexium(esomeprazole magnesium)package insert for IV use. Wilmington,DE; AstraZeneca; 2006 October.
  7. _ Wilder-Smith,C; Bondarov,P; Lundgren,M. Intravenous esomeprazole (40 mg and 20 mg) inhibits gastric acid secretion as effectively as oral esomeprazole: results of two randomized clinical studies.European Journal of Gastroenterology & Hepatology. Volume 17(2), February 2005, pp 191-197.
  8. _ 8.0_8.1_8.2 Lexi-Comp (2003). Drug Information Handbook. 11th Edition., APhA
  9. _ Sj_vall,H; Bj_rnsson,E; Holmberg,J; Hasselgren,G; Pharmacokinetic study of esomeprazole in patients with hepatic impairment. European Journal of Gastroenterology & Hepatology. Volume 14(5), May 2002, pp 491-496
  10. _ Atazanavir package insert. Princeton,NJ; Bristol-Myers Squibb Company; 2006 August.
  11. _ Pletal (cilostazol) package insert. Tokushima, Japan: Otsuka Pharmaceutical Co., Ltd.; 2004 Feb.
  12. _ Rescriptor (delavirdine) package insert. La Jolla, CA: Agouron Pharmaceuticals; 2006 Feb.
  13. _ 13.0_13.1_13.2_13.3 Soll AH, for the Practice Parameters Committee of the American College of Gastroenterology. Medical Treatment of Peptic Ulcer Disease: Practice Guidelines. JAMA 1996;275:622_9.
  14. _ Fosamax_ (alendronate sodium) package insert. Whitehouse Station, NJ; Merck & Co.Inc; 2006 Nov.
  15. _ EC Naprosyn_ (naproxen delayed-release) package insert. Nutley, NJ: Roche Laboratories, Inc.; 2003 May.
  16. _ Dixit RK, Chawla AB, Kumar N, et al. Effect of omeprazole on the pharmacokinetics of sustained-release carbamazepine in healthy male volunteers. Methods Find Exp Clin Pharmacol 2001;23:37_9.
  17. _ Lescol_ (fluvastatin) package insert. East Hanover, NJ: Novartis Pharmaceuticals Corporation; 2005 Jan.
  18. _ Iressa_ (gefitinib) package insert. Wilmington, DE: AstraZeneca Pharmaceuticals LP; 2003 May.
  19. _ Velcade_ (bortezomib) package insert. Cambridge, MA: Millennium Pharmaceuticals, Inc.; 2006 Dec.
  20. _ Entocort_ EC (budesonide) capsules package insert. Wilmington DE: AstraZeneca Pharmaceuticals LP; 2002 Oct
  21. _ Cedax_(ceftibuten) package insert. Morrisville, NC: Biovail Pharmaceuticals, Inc.; 2002 Mar.
  22. _ 22.0_22.1 Focalin_ XR(dexmethylphenidate extended-release) package insert. East Hanover, NJ: Novartis Pharmaceutical Corp.; 2006 August.
  23. _ Oosterhuis B, Jonkman JH, Andersson T, et al. Minor effect of multiple dose omeprazole on the pharmacokinetics of digoxin after a single oral dose. Br J Clin Pharm 1991;32:569_72.
  24. _ Sustiva_ (efavirenz) package insert. Princeton, NJ: Bristol-Myers Squibb Company; 2007 Jan.
  25. _ Marcuard SP, Albernaz L, Khazanie PG. Omeprazole therapy causes malabsorption of cyanocobalamin (vitamin B12). Ann Intern Med 1994;120:211_5.
  26. _ Prevacid_ (lansoprazole) package insert. Lake Forest, IL:TAP Pharmaceuticals Inc.; 2004 Jun.

PUBMED References

Efficacy Trial Articles

  1. Yeomans, Neville D.; Tulassay, Zsolt; Juhasz, Laszlo; Racz, Istvan; Howard, John M.; van Rensburg, Christoffel J.; Swannell, Anthony J.; Hawkey, Christopher J. A Comparison of Omeprazole with Ranitidine for Ulcers Associated with Nonsteroidal Antiinflammatory Drugs.N Engl J Med 1998;338:719-726.
  2. Wilder-Smith,C; Bondarov,P; Lundgren,M. Intravenous esomeprazole (40 mg and 20 mg) inhibits gastric acid secretion as effectively as oral esomeprazole: results of two randomized clinical studies.European Journal of Gastroenterology & Hepatology. Volume 17(2), February 2005, pp 191-197.

Back to top

Therapeutic Class Comparison Articles

  1. Yeomans, Neville D.; Tulassay, Zsolt; Juhasz, Laszlo; Racz, Istvan; Howard, John M.; van Rensburg, Christoffel J.; Swannell, Anthony J.; Hawkey, Christopher J. A Comparison of Omeprazole with Ranitidine for Ulcers Associated with Nonsteroidal Antiinflammatory Drugs.N Engl J Med 1998;338:719-726.
  2. Wilder-Smith,C; Bondarov,P; Lundgren,M. Intravenous esomeprazole (40 mg and 20 mg) inhibits gastric acid secretion as effectively as oral esomeprazole: results of two randomized clinical studies.European Journal of Gastroenterology & Hepatology. Volume 17(2), February 2005, pp 191-197.

Back to top

Pharmacokinetics Articles

  1. Simon B, Muller P, Pascu O, Gatz G, Sander P, Huber R, et al. Intra-oesophageal pH profiles and pharmacokinetics of pantoprazole and esomeprazole: a crossover study in patients with gastro-oesophageal reflux disease. European Journal of Gastroenterology & Hepatology 2003;15(7):791-9.
  2. Sj_vall,H; Bj_rnsson,E; Holmberg,J; Hasselgren,G; Pharmacokinetic study of esomeprazole in patients with hepatic impairment. European Journal of Gastroenterology & Hepatology. Volume 14(5), May 2002, pp 491-496.
  3. Dixit RK, Chawla AB, Kumar N, Garg SK.Effect of omeprazole on the pharmacokinetics of sustained-release carbamazepine in healthy male volunteers.Methods Find Exp Clin Pharmacol. 2001 Jan-Feb;23(1):37-9.
  4. Oosterhuis B, Jonkman JH, Andersson T, et al. Minor effect of multiple dose omeprazole on the pharmacokinetics of digoxin after a single oral dose. Br J Clin Pharm 1991;32:569_72.

Back to top

Drug Interaction Articles

  1. Hurwitz A, Ruhl CE, Kimler BF, Topp EM, Mayo MS.Gastric function in the elderly: effects on absorption of ketoconazole.J Clin Pharmacol. 2003 Sep;43(9):996-1002.
  2. Dixit RK, Chawla AB, Kumar N, Garg SK.Effect of omeprazole on the pharmacokinetics of sustained-release carbamazepine in healthy male volunteers.Methods Find Exp Clin Pharmacol. 2001 Jan-Feb;23(1):37-9.
  3. Oosterhuis B, Jonkman JH, Andersson T, et al. Minor effect of multiple dose omeprazole on the pharmacokinetics of digoxin after a single oral dose. Br J Clin Pharm 1991;32:569_72.
  4. Soll AH, for the Practice Parameters Committee of the American College of Gastroenterology. Medical Treatment of Peptic Ulcer Disease: Practice Guidelines. JAMA 1996;275:622_9.
  5. Marcuard SP, Albernaz L, Khazanie PG. Omeprazole therapy causes malabsorption of cyanocobalamin (vitamin B12). Ann Intern Med 1994;120:211_5.

Back to top


External Links

Back to top

Retrieved from "http://www.smbrower.com/mediawiki/index.php/Esomeprazole"
Personal tools