Drug Q&A

Esomeprazole

A: Nexium is a proton pump inhibitior which means it blocks the stomach secretion of acid. It is not an antibiotic and contains no penicillin, so you are okay.

Q: I need synthesis of Esomeprazole on R & D level and on production as well.?
I have some part of synthesis but dont know the starting material. I need steps before pyridylmethyl chloride. It involves Boekelheide reaction. Plz reply ASAP!!!

A: You need to go to the literature or to hire a consultant. You shouldn’t be designing industrial production on the basis of suggestions from anonymous strangers.

Q: critique of Esomeprazole compared with Lansoprazole in the treament of Erosive Esophagitis?

A: causes cancer, have the nissen fundoplication surgery done, it is laproscopic and works the best, had it done 12yrs ago and feel great

Q: esomeprazole and lansoprazole and all ‘zole’ s r degrading in answer environ itself…reason?

A: Not sure why this is in geography, but here goes:
Any medication ending in “zole” is a proton pump inhibitor (PPI) used for treatment of acid reflux (GURD). Proton pump inhibitors act by irreversibly blocking the hydrogen/potassium adenosine triphosphatase enzyme system (the H+/K+ ATPase, or more commonly just gastric proton pump) of the gastric parietal cell. The proton pump is the terminal stage in gastric acid secretion, being directly responsible for secreting H+ ions into the gastric lumen, making it an ideal target for inhibiting acid secretion. Targeting the terminal-step in acid production, as well as the irreversible nature of the inhibition, result in a class of drugs that are significantly more effective than H2 antagonists and reduce gastric acid secretion by up to 99%.

Q: What does increased concentration in the blood mean?
I take diazepam every now and then prescribed by my doctor and she has now prescribed Esomeprazole. I have read on a medical website that Esomeprazole can increases the concentration in blood of diazepan What does it mean? Am I safe? ‘DRUG INTERACTIONS: Esomeprazole potentially can increase the concentration in blood of diazepam (Valium) by decreasing the elimination of diazepam in the liver.’

A: Normally, Diazepam is eliminated/metabolised in the liver. When you take Esomeprazole, it may reduces the rate of elimination of Diazepam in the liver. This is due to the fact that Esomeprazole and Diazepam are both metabolised by CYP2C19.

As it now takes longer time to metabolise the Diazepam, the amount of Diazepam that remains in your blood stream will be higher than when you don’t take Esomeprazole. That’s what it means by increasing the concentration in blood of Diazepam.

See it like, you have 2 bags full of large A3 papers to be shredded. There used to be only 1 bag, and the shredder works exlusively to shred the papers from bag A. But now there is a bag B of paper of the same size that can be shredded only by this shredder (A4 shredder is too small for shredding A3 papers) so it’s going to take longer time to finish shredding papers from bag A since some of the papers from bag B are also being shredded at the same time.

Is this helpful to clarify the question for you?

The warning mentions “potentially”, and it is not because any mechanism changes. It’s more dependent on individuals. Some people have more of the cytochrome molecules to run around for metablism, some people have less. Those with more would probably not notice any effect while those with a less efficient system will feel the effect from the interaction. Drug interactions is a very dynamic thing.

Q: Lansoprazole or Esomeprazole?
Please let me know which one of them is more powerful and more effective. I;ve been taking nexium ( Esomeprazole ) for 4 months and now when I visited another doctor he gave me Lansoprazole 30 mg twice daily. ???am confused.,….I need a simple answer…Dont Blunder….
Sorry forgot to add..My endoscopy shows….Small Hiatus Hernia and Moderate Peristalsis and yeah NORMAL DUODENUM

A: Lansoprazole and esomeprazole are generic names. Don’t capitalize them. Lansoprazole is generic for Prevacid. Esomaprazole is generic for Nexium. Nexium is a brand name. Capitalize it. Lansoprazole (Prevacid) is a more potent in vitro inhibitor than esomeprazole (Nexium).

Q: omeprazole vs. esomeprazole?
if omeprazole is a racemic mixture of steroisomers and esomeprazole is the isolated active isomer, why is standard daily dose of omeprazole 20mg and esomeprazole 40mg?
it seems to me that the purified isomer would be approximately twice as potent(based on the distribution of racemic mixtures). is this a chemical or pharmacotherapeutic issue?

A: You are correct – omeprazole is the racemic mixture and esomeprazole is the L-isomer. There is some evidence that esomeprazole (nexium) is more effective. The typical dose of both usually starts at 20mg daily, but you can use up to 80mg per day (typically 40 mg twice daily in this situation). Additionally, esomeprazole comes in an IV formulation as well while, to the best of my knowledge, omeprazole does not.

Q: Is Esomeprazole and Pantoprazole INN product?
If no, then are this BP Product or USP product?

A: both of this drugs are PPI’s, and you can find any information about them by simply googling them separately, if by USP you mean United States Pharmacopeia, I believe you cn find both there, if BP stands for Brithish Pharmacopeia also both may be able to be found there, depending on if they have been licensed in that country or not, as for INN that I do not know.
both drugs are used to decrease the amount of acid in GERD (Gastro Esophageal Reflux Disease)

Q: Would a prolonged low grade fever of 99.9 be a symptom of uncontrolled high blood pressure?
I am 24 years old I have had high blood pressure since I was 18 years both parents have it also. For the last three months I have been having chest pain and they have not been able to get the pressure down. I have been hospitalized three times one time being in the ICU. The only test they have done are two different stress test and some EKGs. They have told me that the reason that I have chest pain is because when my blood pressure gets to high the artiries contract causeing pain. I am now taking 9 med which are Telmisartan 80mg, Isosrbide Mononit 60mg, Esomeprazole 40mg, Lisinopril/ HCT 20/12.5mg, Amlodipine10mg, Methyldopa 250mg, Furosemide 40mg, Simvastatn/Ezetimib 20/10mg,Colnidine 0.2mg, and I also take QuickNitro. With all these meds you would think my pressure would below but it is not. My PCP has me come and see him every two weeks while the Cardiac doctors tells me that it is going to take time to find out whats wrong. I also have some leakey valves there not the cause i hope.

A: probably not, possible symptoms of high blood pressure vary from person to person. These symptoms could also be symptoms of other health problems. Most doctors say that if you’re having symptoms such as:

Headaches

Heart palpitations

A tough time catching your breath after exertion

Fatigue

A flushed face

Blurry vision

Nosebleeds

A strong need to urinate often (especially during the night)

Tinnitus (a ringing or buzzing in the ears)

Vertigo (feelings that you or the world is spinning dizzily)

with the above symptoms they say to get checked for HTN

with a low grade fever, it’s usually around 101 degrees fahrenheit and It is a non-specific finding, but occurs in many diseases, ranging from infectious (viral infections or infective endocarditis) to autoimmune to malignant causes.

A persistent low grade fever can be a sign of many sicknesses.

you should definitely get a second opinion and get some blood work done. maybe the cause of your HTN is due to a virus. normally a virus makes itself and breaks itself and lasts around 10-14 days, some viruses can last months depending on your immune system. you need to get at LEAST a CBC with differential done among other new tests and blood work. good luck.

endocarditis is a possiblity and i would suggest you look into that, i am not a doctor but upon research found this could possibly be a concern.

http://en.wikipedia.org/wiki/Endocarditis#Diagnosis

Q: drugfinder esomeprazole/Nexium?
I want a full explanation & discription of this drug

A: Purplepill.com is on the web site by the company that makes the drug.

The following information is from Gold Standard, part of a pharmaceutical company which provides information on almost every drug “out there”, and supposedly doesn’t have any financial interest in profits from any individual drug.
[Gold Standard, is not freely available on the Internet as far as I know...I was able to access it through our medical college library which has a subscription to it ]

Here goes…
——————–
Patient education portion:

Esomeprazole capsules

What are esomeprazole capsules?
ESOMEPRAZOLE (Nexium®) prevents the production of acid in the stomach. It is used to treat gastroesophageal reflux disease (GERD), ulcers, certain bacteria in the stomach, too much acid in the stomach, and inflammation of the esophagus. It can also be used to prevent ulcers in patients taking medicines called NSAIDs.

What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•liver disease
•an unusual or allergic reaction to esomeprazole, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I take this medicine?
Take esomeprazole capsules by mouth. Follow the directions on the prescription label. Swallow the capsules whole with a drink of water; do not crush, break or chew. The capsules can be opened and the contents sprinkled on applesauce or yogurt, given with fruit juices, or swallowed immediately with water. Do not crush the contents into the food. Esomeprazole works best if taken on an empty stomach at least one hour before a meal. Take your doses at regular intervals. Do not take your medicine more often than directed.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What if I miss a dose?
If you miss a dose, just take your next scheduled dose when it is due. Do not use double or extra doses.

What drug(s) may interact with esomeprazole?
•ampicillin
•diazepam
•digoxin
•iron salts
•itraconazole, ketoconazole, voriconazole, or other prescription medicines for fungus or yeast infections
•phenytoin
•warfarin

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What side effects may I notice from taking esomeprazole?
Side effects that you should report to your prescriber or health care professional as soon as possible:
•chest pain or tightness
•dark yellow or brown urine
•shortness of breath
•skin rash
•unusual tiredness or fatigue

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
•headache
•diarrhea or constipation
•flatulence (gas)
•nausea/vomiting
•dry mouth

What should I watch for while taking esomeprazole?
It can take several days of therapy with esomeprazole before your stomach pains improve. Check with your prescriber or health care professional if your condition does not improve, or if it gets worse. You can take antacids for the occasional relief of pain unless your prescriber or health care professional tells you otherwise.

Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Protect from light and moisture. Throw away any unused medicine after the expiration date.

[ Last Revised: 12/4/2006 10:02:00 AM ]

——————

Description: Esomeprazole, the S-isomer of omeprazole, is the first proton pump inhibitor (PPI) synthesized as an optical isomer to become available for clinical use. Esomeprazole was previously known as perprazole in investigational use. Esomeprazole is approved for the healing and maintenance of erosive esophagitis and for the treatment of symptomatic gastroesophageal reflux disease. It is also indicated for use in combination with clarithromycin and amoxicillin to eradicate Helicobacter pylori in patients with active or prior duodenal ulcer disease.[3145] When compared to omeprazole, esomeprazole has similar efficacy in the eradication of H. pylori, can maintain intragastric pH > 4 for a longer period of time, and has a similar time to sustained resolution of heartburn.[3146] [3147] [3148] Esomeprazole has a greater bioavailability compared to omeprazole, which may contribute to higher healing rates reported in studies of erosive esophagitis.[3149] Esomeprazole (Nexium®) capsules were approved by the FDA in February 2001. In November 2004 the FDA approved oral esomeprazole for the prevention of NSAID-associated gastric ulcers; the sNDA for the healing of NSAID-induced gastric ulcers is ‘approvable’. An injectable formulation of esomeprazole (Nexium®) was approved by the FDA in March 2005. Nexium® capsules received FDA approval for the long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison Syndrome, in October 2006. Also in October 2006, a delayed-release oral suspension was FDA-approved for the treatment of GERD, including symptomatic gastroesophageal reflux disease, healing and maintenance of healing of erosive esophagitis (EE), and risk reduction of NSAID-associated gastric (stomach) ulcers.

Mechanism of Action: Esomeprazole is a substituted benzimidazole proton-pump inhibitor (PPI) that suppresses gastric acid secretion by inhibiting the gastric (H+, K+)-ATPase enzyme pump. Following activation in an acidic pH, esomeprazole binds irreversibly to the H+/K+ ATPase pump on the secretory surface of the parietal cell membrane. Subsequently, the secretion of hydrogen ions into the gastric lumen is inhibited. Gastric acid pump inhibitors block the final step of gastric acid production, and inhibit both basal and stimulus-induced acid secretion. Delayed-release doses of 20 mg and 40 mg esomeprazole maintained intragastric pH > 4.0 for 12.7 hours and 16.8 hours, respectively. Significant in vitro activity against Helicobacter pylori (H. Pylori) has been demonstrated for esomeprazole. Esomeprazole monotherapy increases the clearance rate of H. pylori; however, eradication does not occur without appropriate antimicrobial therapy. Similar to omeprazole and other PPIs, hypergastrinemia can occur during esomeprazole therapy. Although prolonged hypergastrinemia has been associated with gastric tumors in rats, long-term studies of proton pump inhibitors do not suggest the development of tumors in humans.

Pharmacokinetics: Esomeprazole is administered orally. Esomeprazole dissolves rapidly in an acidic environment and therefore is formulated as a capsule containing enteric-coated pellets. Multiple dosing at 40 mg/day results in 90% bioavailability versus 64% after a single 40 mg dose. Cmax is reached within 1—3.5 hours. The AUC of esomeprazole (the S-isomer) is 80% higher than with omeprazole (both S- and R-isomer) due to decreased clearance and first-pass elimination of the S-isomer. Clinically this allows more esomeprazole to reach the site of action and may contribute to higher efficacy rates. The AUC of a single 40 mg dose of esomeprazole is decreased by 33—53% after food intake compared to fasting conditions. Esomeprazole is 97% bound to plasma proteins. Metabolism occurs extensively in the liver to inactive metabolites via CYP2C19 and to a lesser extent by CYP3A4.[3149] The plasma elimination half-life of esomeprazole is approximately 1.5 hours. Less than 1% of parent drug is excreted in the urine with the remainder excreted as inactive metabolites in both the urine and feces.

•Special Populations: Data in patients with hepatic cirrhosis showed that the mean AUC of esomeprazole was 76% higher and the half-life was 29% longer compared with GERD patients with no hepatic dysfunction. However, cirrhotic patients with mild to moderate liver dysfunction exhibited similar pharmacokinetic parameters to otherwise healthy GERD patients.[3149] Cirrhotic patients with severe hepatic insufficiency exhibited AUCs 2—3 times higher than those with normal liver function. The AUC and Cmax of esomeprazole were both elevated in the elderly compared to younger patients, but dose adjustments based on age are not needed. Three percent of Caucasians and 15—20% of Asians lack CYP2C19 and are poor metabolizers of esomeprazole. The AUC ratio of esomeprazole in poor metabolizers compared to the AUC of the normal population is approximately 2. The pharmacokinetic parameters of esomeprazole are not altered in renal insufficiency. Esomeprazole pharmacokinetic parameters in adolescents and children age 12 to 17 years were similar to those observed in adult patients with symptomatic GERD.

References

3145. Laine L , Fennerty MB, Osato M et al. Esomeprazole-based Helicobacter pylori eradication therapy and the effect of antibiotic resistance: results of three US multicenter, double-blind trials. Am J Gastroenterol 2000;95:3393—8.
3146. Veldhuyzen VZ, Lauritsen K, Delchier JC et al. One-week triple therapy with esomeprazole provides effective eradication of Helicobacter pylori in duodenal ulcer disease. Aliment Pharmacol Ther 2000;14:1605—11.

3147. Lind T, Rydberg L, Kyleback A et al. Esomeprazole provides improved acid control vs. omeprazole in patients with symptoms of gastro-oesophageal reflux disease. Aliment Pharmacol Ther 2000;14:861—67.

3148. Kahrilas PJ, Falk GW, Johnson DA. Esomeprazole improves healing and symptom resolution as compared with omeprazole in reflux oesophagitis patients: a randomized controlled trial. Aliment Pharmacol Ther 2000;14:1249—58.)

3149. Thitiphuree S, Talley NJ. Esomeprazole, A new proton pump inhibitor: Pharmacological characteristics and clinical efficacy. Int J Clin Pract 2000;54:537—41.)

[ Revised 12/4/2006 10:03:00 AM ]

Drug Information Provided by
Gold Standard, Inc. © 2006
——-
Indications/Dosage
Indications…Dosage

For the short-term treatment of frequent pyrosis (heartburn)† that occurs >= 2 times per week:
Oral dosage:
Adults, including the elderly: 20 mg PO once daily for up to 14 days. Full relief may take 1—4 days. If frequent heartburn returns soon after the initial 14-day treatment regimen, patients should contact their health care provider.
Children: Safe and effective use have not been established.

For the treatment of symptomatic gastroesophageal reflux disease (GERD) including erosive esophagitis:
Oral dosage:
Adults, including the elderly, and Adolescents > 17 years: For GERD with no esophageal lesions, 20 mg PO once daily, taken 1 hour before meals, for up to 4 weeks. For erosive esophagitis, 20—40 mg PO once daily for 4—8 weeks. For no response to initial course or for recurrences, consider an additional 4—8 week course. To prevent relapse, chronic maintenance therapy may be necessary; give 20 mg PO once daily. Maintenance studies have not extended beyond 6 months. In one study, 40 mg/day was no more effective than 20 mg/day for maintenance treatment; however, mean time to first recurrence was longer with the 40 mg/day dose (163 days) vs. the 20 mg/day dose (115 days). At month 6, greater than 70% of patients using either dose remained heartburn-free.[3150] In a comparative study, the percent of patients with healed esophagitis was significantly greater with esomeprazole 40 mg/day vs. omeprazole 20 mg/day. The incidence of symptomatic relief was higher and relief occurred sooner with esomeprazole 40 mg/day vs. the other treatment groups.[3148]
Adolescents and Children 12—17 years: 20 mg or 40 mg PO once daily, taken 1 hour before meals, for up to 8 weeks.
Children < 12 years: Safe and effective use have not been established.
•for the short-term treatment of gastric esophageal reflux (GERD) associated with a history or erosive esophagitis in patients unable to take oral therapy:
Intravenous dosage:
Adults, including the elderly, and Adolescents > 17 years: 20 or 40 mg IV once daily for up to 10 days. The IV formulation is indicated as an alternative to oral therapy for the short-term treatment (up to 10 days) of GERD. Switch to oral therapy when feasible.
Adolescents <= 17 years and Children: Safe and effective use have not been established.

For use in combination with clarithromycin and amoxicillin for the eradication of Helicobacter pylori and to reduce the risk of duodenal ulcer recurrence:
Oral dosage:
Adults, including the elderly: The FDA-approved dosage is esomeprazole 40 mg PO once daily, taken one hour before meals, with clarithromycin (500 mg PO twice daily) and amoxicillin (1 g PO twice daily) for 10 days. In patients who fail therapy, susceptibility testing should be done; resistance will likely be demonstrated. If resistance is found or susceptibility testing is not possible, alternative antimicrobial therapy should be instituted. NOTE: Patients in H. pylori clinical trials had either an active duodenal ulcer or a history of an ulcer. One study notes that after a 7-day course of esomeprazole-based triple therapy, endoscopically confirmed duodenal ulcer healing rates were 91% at 4 weeks.[3151] Recommendations on whether esomeprazole needs to be continued for 2—4 weeks for active ulcer healing after eradication of H. pylori are not currently available. However, expert opinions generally agree that esomeprazole, like other PPIs, will be continued for several weeks following H. pylori eradication to complete ulcer healing, pending further data.
Children: Safe and effective use have not been established.

For NSAID-induced ulcer prophylaxis (gastric):
Oral dosage:
Adults, including the elderly: 20 or 40 mg PO once daily; in clinical trials the 20 and 40 mg dose showed comparable benefits in providing risk reduction. Roughly 95% of patients remained ulcer free for up to 6 months. Studies did not demonstrate significant reduction in the development of NSAID-associated duodenal ulcer due to the low incidence.
Children: Safe and effective use have not been established.

For the treatment of pathological hypersecretion associated with Zollinger-Ellison syndrome:
Oral dosage:
Adults, including the elderly: Initially, 40 mg PO twice daily. Adjust dosage to attain clinical goals. Doses up to 240 mg/day PO have been administered. Patients have been treated for up to 12 months.
Adolescents and children: Safe and effective use has not been established.

Maximum Dosage Limits:
•Adults: 40 mg/day PO/IV; up to 240 mg/day PO for Zollinger-Ellison syndrome.
•Elderly: 40 mg/day PO/IV; up to 240 mg/day PO for Zollinger-Ellison syndrome.
•Adolescents > 17 years: 40 mg/day PO/IV.
•Adolescents <= 17 years: 40 mg/day PO.
•Children >= 12 years: 40 mg/day PO.
•Children < 12 years: Safe and effective use have not been established.

Patients with hepatic impairment:
No dosage adjustment is recommended for mild to moderate hepatic impairment. However, in patients with severe hepatic insufficiency (Child Pugh Class C), do not exceed 20 mg/day.

Patients with renal impairment:
No dosage adjustment is necessary.

Intermittent hemodialysis:
No dosage adjustment is necessary. Due to high protein binding, esomeprazole is not expected to be removed by hemodialysis.

[ Last revised: 10/24/2006 9:50:00 AM ]
——————————
Administration
Indications…Dosage

Patients with renal impairment:
No dosage adjustment is necessary.

Intermittent hemodialysis:
No dosage adjustment is necessary. Due to high protein binding, esomeprazole is not expected to be removed by hemodialysis.

[ Last revised: 10/24/2006 9:50:00 AM ]

—————-
Contraindications/Precautions
Contraindications/Precautions

Esomeprazole is contraindicated in patients with known hypersensitivity to esomeprazole or other substituted benzimidazoles such as omeprazole or lansoprazole (i.e., known proton pump inhibitors (PPIs) hypersensitivity). Although rare, occasionally such reactions can be serious (i.e., result in anaphylaxis or angioedema). There has been evidence of PPI cross-sensitivity in some sensitive individuals in literature reports.

Esomeprazole undergoes extensive hepatic metabolism. Patients with severe hepatic disease should not exceed a dose of 20 mg per day. No dosage adjustment is recommended in patients with mild to moderate hepatic impairment.

Antimicrobials, proton pump inhibitors, and bismuth preparations suppress Helicobacter pylori. Ingestion of these substances within four weeks prior to performing urease or breath-tests for H. pylori detection may lead to false negative results. In the four weeks prior to performing the test, the patient should avoid the use of esomeprazole and other agents which are known to suppress H. pylori.

Symptomatic response to therapy with esomeprazole does not preclude the presence of gastric cancer or other malignancy.

Daily treatment with a gastric acid-suppressing medication such as esomeprazole over a long period of time (e.g., longer than 3 years) may lead to malabsorption of cyanocobalamin and vitamin B12 deficiency caused by hypo- or achlorhydria. Rare reports of cyanocobalamin deficiency occurring with acid-suppression therapy have been reported in the literature (see Adverse Reactions). This possibility should be considered if clinical symptoms consistent with cyanocobalamin deficiency are observed.[162] [6226]

No overall differences in safety and efficacy were observed between the elderly and younger individuals receiving esomeprazole. Other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity for some older individuals cannot be ruled out.

Esomeprazole is classified in FDA pregnancy risk category B. There are no adequate and well-controlled studies in pregnant women. Animal reproductive studies have been conducted in rats and rabbits using doses up to 57 and 35 times, respectively, that of humans based on body surface area; there was no evidence of fetal harm. Although not specifically studied, esomeprazole is expected to cross the human placenta like omeprazole. Since data on human pregnancy exposure to esomeprazole is not available, caution should be observed when administering esomeprazole in pregnancy. If inadvertent exposure does occur during the first trimester, the risk to the fetus appears to be low.[9215]

No reports describing the use of esomeprazole during breast-feeding are available. Warnings with the use of other PPIs exist and may be applicable to esomeprazole. Esomeprazole has a low molecular weight (345) and excretion into breast milk is expected. The manufacturer recommends that a decision should be made whether to discontinue nursing or to discontinue esomeprazole, taking into account the importance of the drug to the mother’s condition.[6265] However, consideration of the dose and drug properties may allow for continued nursing without significant exposure to breast-fed infants for nursing women who require esomeprazole.[9214] If possible, the mother should wait to nurse or pump milk 5—7.5 hours after the daily dose of esomeprazole. Allowing this time should eliminate 97% of the drug from the plasma and would avoid the period when the greatest amount of drug is available to enter the milk. Near the end of the waiting period, breast milk should be expressed and discarded to complete the strategy to limit the infants exposure to esomeprazole.[9214]

The safety and efficacy of esomeprazole in children has not been established.

[ Last revised: 12/4/2006 9:57:00 AM ]

References

162. Marcuard SP, Albernaz L, Khazanie PG. Omeprazole therapy causes malabsorption of cyanocobalamin (vitamin B12). Ann Intern Med 1994;120:211—5.
6226. Protonix® (pantoprazole) package insert. Philadelphia, PA: Wyeth Laboratories; 2005 Dec.

6265. Nexium® (esomeprazole) package insert. Wilmington, DE: AstraZeneca; 2006 Oct.

9214. Briggs, Freeman, Yaffee. Esomeprazole. Update, Drugs in Pregnancy and Lactation 2005:18;19—20.

9215. Richter JE. Review article: the management of heartburn in pregnancy. Aliment Pharmacol Ther 2005;22:749—57.

Symptomatic response to therapy with esomeprazole does not preclude the presence of gastric cancer or other malignancy.

The safety and efficacy of esomeprazole in children has not been established.

[ Last revised: 12/4/2006 9:57:00 AM ]

References

6265. Nexium® (esomeprazole) package insert. Wilmington, DE: AstraZeneca; 2006 Oct.

9214. Briggs, Freeman, Yaffee. Esomeprazole. Update, Drugs in Pregnancy and Lactation 2005:18;19—20.

9215. Richter JE. Review article: the management of heartburn in pregnancy. Aliment Pharmacol Ther 2005;22:749—57.

In general, oral esomeprazole has been well-tolerated in clinical trials (n > 10,000). Greater than 2900 patients have been evaluated in 6—12 month long studies. The types of adverse events are similar with short or long-term use, and have been comparable to placebo rates. The safety profile of esomeprazole is similar to omeprazole.[3148]

The most frequently (>=1%) reported adverse events with oral esomeprazole use were gastrointestinal (GI) in nature, including abdominal pain (3.8%), constipation, diarrhea (4.3%), flatulence (1.8%), nausea/vomiting (3.8%), and xerostomia (dry mouth). A study of 149 adolescents and children (12—17 years of age) with clinically diagnosed GERD reported abdominal pain (2.7%), diarrhea (2%), and nausea (2%). Other notable GI events that occurred in < 1% of patients, but were judged by investigators to be possibly or probably related to esomeprazole include: anorexia, bowel irregularity, dyspepsia, dysphagia, eructation, esophageal disorder, GI hemorrhage, melena, tongue edema, and ulcerative stomatitis. Intravenous esomeprazole has a safety profile similar to that of oral administration. Intravenous (IV) esomeprazole has been associated with injection site reaction (1.7%), including mild focal erythema and itching at the IV insertion site.

Headache occurred in up to 5.5% of adult patients and 8.1% of adolescents and children (age 12—17) using oral esomeprazole. Other notable, but rare (< 1%) central nervous system adverse events possibly or probably related to esomeprazole include: confusion, depression, dizziness, nervousness, insomnia, and migraine. Psychiatric disturbances such as agitation, aggression, and hallucinations have all been reported in post-marketing experience. Dizziness was reported in 2.5% of patients receiving intravenous esomeprazole during pre-marketing trials.

Post-marketing spontaneous reports during esomeprazole use have included anaphylactic shock or anaphylactoid reactions. Hypersensitivity reactions occurring in < 1% of patients judged by investigators during pre-approval trials as possibly or probably related to esomeprazole included: angioedema, dermatitis, pruritus, rash (unspecified), maculopapular rash, and urticaria. Rare cases of severe generalized skin reactions including toxic epidermal necrolysis (TEN) (some fatal), Stevens-Johnson syndrome and erythema multiforme have occurred. Exfoliative dermatitis has been reported with omeprazole, and could potentially occur with esomeprazole based on the similarity in dermatological reactions reported to date.

Elevated hepatic enzymes (ALT, AST and alkaline phosphatase) and hyperbilirubinemia have been rarely (< 1%) reported, both with esomeprazole and omeprazole. Rarely, hepatic failure and hepatitis with or without jaundice has been reported with esomeprazole. Hepatic encephalopathy has also been reported in post-marketing experience.

Myalgia, alopecia, and blurred vision have been reported during post-marketing experience with esomeprazole. Rare reports of interstitial nephritis and gynecomastia have been reported post-marketing. Rare cardiovascular system adverse reactions with esomeprazole include chest pain, flushing, hypertension, and tachycardia. A reduction in potassium levels was noted in <= 1% of patients, but an association with hypokalemia was not made.

As with omeprazole, rare hematologic abnormalities have been reported with esomeprazole including anemia, leukocytosis, leukopenia, and thrombocytopenia. In a study of healthy volunteers, it was shown that omeprazole caused a significant reduction in cyanocobalamin absorption (vitamin B12 deficiency).[162] Although clinical data in esomeprazole is lacking, it may be prudent to monitor patients for signs of pernicious anemia. Neurological manifestations of pernicious anemia can occur in the absence of hematologic changes. Other potentially serious, but rare adverse events that have also been reported in spontaneous post-marketing reports include agranulocytosis and pancytopenia; however, causality cannot be assessed.

Gastrointestinal infestation with candidiasis have been reported in post-marketing experience with esomeprazole. Pancreatitis has also been reported post-marketing.

Animal and human data have demonstrated a proliferation of enterochromaffin-like cells due to hypergastrinemia, which may be associated with the development of malignant gastric carcinoma during long-term administration of proton pump inhibitors (PPIs). In over 1,000 patients treated with esomeprazole for up to 12 months, the prevalence of ECL cell hyperplasia increased with time and dose, but no patient developed ECL cell carcinoids, dysplasia, or neoplasia in the gastric mucosa. In esomeprazole clinical trials, there were dose-related increases in mean fasting gastrin levels which reached plateaus at 2 to 3 months and returned to baseline 4 weeks after drug discontinuation. According the the manufacturer of esomeprazole, < 1% of patients were reported to have hypergastrinemia or GI dysplasia. Historically, omeprazole has been given for as long as 5 years without concern for the development of gastric neoplasia. The overall risk of carcinoid tumors during therapy with PPIs is low based on cumulative safety experience; monitoring of serum gastrin levels during PPI therapy is generally not necessary.[2859]

Atrophic gastritis, a precursor for gastric cancer, has been noted occasionally in gastric corpus biopsies from patients treated long-term with pantoprazole, particularly in patients who were H. pylori positive.[6226] Other proton pump inhibitors (PPI) have also been implicated. One study compared the long-term effects of omeprazole (20—40 mg once daily) versus funduscopy in the treatment of gastroesophageal reflux. Among H. pylori positive patients treated with omeprazole, 30% developed atrophic gastritis (P < 0.001). In contrast, only 4% of omeprazole-treated patients who were not infected with H. pylori developed atrophic gastritis. No patients in the funduscopy group developed atrophic gastritis during the study period regardless of H. pylori infection status.[9496] Some studies have corroborated these results, while other studies have found no evidence of accelerated progression to atrophic gastritis in this population. Until more data are available, it may be prudent to test and treat baseline H. pylori infections before starting empiric esomeprazole maintenance therapy to avoid the possible increased risk of atrophic gastritis development.[9497]

Other less significant and infrequently (< 1%) reported adverse reactions are detailed in the prescribing literature for oral esomeprazole.

[ Last revised: 9/21/2006 10:52:00 AM ]

References

162. Marcuard SP, Albernaz L, Khazanie PG. Omeprazole therapy causes malabsorption of cyanocobalamin (vitamin B12). Ann Intern Med 1994;120:211—5.
2859. Reilly JP. Safety profile of the proton-pump inhibitors. Am J Health-Syst Pharm 1999;56(Suppl 4):S11—7.

6226. Protonix® (pantoprazole) package insert. Philadelphia, PA: Wyeth Laboratories; 2005 Dec.

9496. Kuipers EJ, Lundell L, Klinkenberg-Knol EC, et al. Atrophic gastritis and Helicobacter pylori infection in patients with reflux esophagitis treated with omeprazole or fundoplication. N Engl J Med 1996;334:1018—22.

9497. Raghunath AS, O’Morain C, McLoughlin RC. Review article: the long-term use of proton-pump inhibitors. Aliment Pharmacol Ther 2005;22(Suppl 1):55—63.

Q: can tegaserod(zelnorm) and nexium(esomeprazole) be taken together to treat IBS(irritible bowel syndrome)?

A: IBS is a farce, there is little medical evidence to prove it exists.. Just take some Tums.

Q: Is it possible to feel severe chest pain because of taking a treatment for helicobacter pylori?
(Esomeprazole 20mg, Amoxicilin 1g, claritromicin 500mg= every 12 hours). Two weeks ago I was taking Nistatin for candida funghi in my mouth.

A: Not really. More likely is pain because you thought you could eat anything since you have a treatment for h. pylori. Not so; even if you’re being treated, you still have to stay away from peppers (even bell peppers) and other ulcer triggers.

Please check with your doctor or medical center, but I’d say the only way you’re having pain associated with the h. pylori is if you’re off-diet/

Q: Is there a non-prescription alternative to Nexium / esomeprazole magnesium?
I take Nexium 20mg and due to a change in how my doctor will do repeats it is going to cost me $50+ for this script. I have stopped taking this tablet until I have symptons and have found I need only to take one tablet once about every 6 days. I am curious as to if I really need this prescription (and it’s associated cost) and can take an over the counter medication instead.

What I am after is recomendations on what to use? Is it as simple as using Quikeze or Mylanta or something stronger. Or should I just suffer the cost and continue the prescription of Nexium?
I am taking this for reflux.

A: There are a lot of OTC meds for this health problem, but none seem to work on me as well as Nexium. You might try some of the others and if they don’t work, you can go back to Nexium. Pepcid, Prilosec, Zantac and probably others.

Q: How long does it take for …….?
I have gastritis & acid reflux and was given Nexium (Esomeprazole) Yesterday evening. I took one yesterday evening, and one this morning. How long does it take for Nexium to block the acid completely & how long on average for my stomach to heal? I’ve been ill for 10 weeks now and cannot take much more of the nausea and discomfort. Thanks x

A: It takes 4-6 weeks to heal but if you are still having nausea you may need a different acid reflux medication. There are several different one. I was on Nexium and it made me sick so I had to be put on Zantac and now I’m on Zegerid (the strongest there is) and I do fine with it. Talk to your Dr if next week you are no better, he may need to change you from Nexium to something else. Like I said Nexium made me sick, it may be making you sick also. My hubby take it and does fine but not me.

Q: what is the rationale why meds like ppi and chloramphenicol are given to a patient with cholecystitis? 10 pts?
the patient’s diagnosis is chronic calculous cholecystitis post cholecystectomy..i want to know why the ppi meds like esomeprazole (nexium) and chloramphenicol which is an antimicrobial is given, intraveneously..what are the reasons/rationale for this?

thanks for your answers!!

A: Your terminology is faulty– how can you have cholecystitis(inflammation of the gall bladder) after the gall bladder has been surgically removed(post cholecystectomy). If you mean chronic calculous choledochal cystitis which means residual calcified stones in the common bile duct it makes more sense. I believe a smoldering infection in the calcified stones or draining bile is the reason for the antibiotic and nexium empties the stomach as part of its function reducing stimulationn of the bile producing system. Quite a mouthful-I hope this helps you.

Medication Q&A

denverurbanforest.com

Drug Q&A

Esomeprazole

Related Posts

Write a comment