Navezole
Navezole Uses, Dosage, Side Effects, Food Interaction and all others data.
Navezole is a substituted benzimidazole, and is also known as PPI due to its property to block the final step of acid secretion by inhibiting H+/K+ ATPase enzyme system in gastric parietal cell. Both basal and stimulated acid are inhibited.
Navezole decreases gastric acid secretion by targeting H+,K+-ATPase, which is the enzyme that catalyzes the final step in the acid secretion pathway in parietal cells. Conveniently, lansoprazole administered any time of day is able to inhibit both daytime and nocturnal acid secretion. The result is that lansoprazole is effective at healing duodenal ulcers, reduces ulcer-related pain, and offers relief from symptoms of heartburn Navezole also reduces pepsin secretion, making it a useful treatment option for hypersecretory conditions such as Zollinger-Ellison syndrome.[F4352]
| Trade Name | Navezole |
| Availability | Rx and/or OTC |
| Generic | Lansoprazole |
| Lansoprazole Other Names | Lansoprazol, Lansoprazole, Lansoprazolum |
| Related Drugs | amoxicillin, omeprazole, famotidine, pantoprazole, metronidazole, Nexium, Pepcid, Protonix, esomeprazole, sucralfate |
| Weight | 30mg |
| Type | Capsule |
| Formula | C16H14F3N3O2S |
| Weight | Average: 369.361 Monoisotopic: 369.075882012 |
| Protein binding | 97% of lansoprazole is plasma protein bound. |
| Groups | Approved, Investigational |
| Therapeutic Class | Proton Pump Inhibitor |
| Manufacturer | Navegal Laboratories |
| Available Country | Pakistan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Navezole is used for:
- Short term treatment of active duodenal ulcer
- Maintenance of healed duodenal ulcers
- Short term treatment of active benign gastric ulcers
- Short term treatment of active erosive esophagitis
- Maintenance of healing of erosive esophagitis
- Pathological hypersecretory conditions including Zollinger- Ellison Syndrome
- H. pylori eradication to reduce the risk of duodenal ulcer recurrence
Navezole is also used to associated treatment for these conditions: Gastro-esophageal Reflux Disease (GERD), Gastrointestinal Bleeding, Helicobacter Pylori Infection, Peptic Ulcer Disease, Hypersecretory conditions
How Navezole works
As a PPI, lansoprazole is a prodrug and requires protonation via an acidic environment to become activated. Once protonated, lansoprazole is able to react with cysteine residues, specifically Cys813 and Cys321, on parietal H+,K+-ATPase resulting in stable disulfides. PPI's in general are able to provide prolonged inhibition of acid secretion due to their ability to bind covalently to their targets.
Dosage
Navezole dosage
Benign gastric ulcer: 30 mg daily in the morning for 8 weeks.
Duodenal ulcer: 30 mg daily in the morning for 4 weeks; maintenance 15 mg.
NSAID-associated duodenal or gastric ulcer: 15-30 mg daily for 4 weeks, followed by a further 4 weeks if not fully healed.
Zollinger-Ellison syndrome (and other hypersecretory conditions): Initially 60 mg once daily adjusted according to response; daily doses of 120 mg or more is given in two divided doses.
Gastroesophageal reflux disease: 30 mg daily in the morning for 4 weeks, followed by a further 4 weeks if not fully healed; maintenance 15-30 mg daily.
Acid-related dyspepsia: 15-30 mg daily in the morning for 2-4 weeks.
Side Effects
Severe or irreversible adverse effects: The possible induction of carcinoid tumors by profound acid suppression, and a rise in serum gastrin may occur. There is a rise in serum gastrin levels in the first 3 months of treatment, which are then maintained though at a lower level than those found in pernicious anaemia. Long term treatment with a proton pump inhibitor in patients with Helicobacter pylori infection may accelerate the development of atrophic gastritis.
Symptomatic adverse effect: Dose dependent diarrhoea occurs with an incidence of about 4% at 30 mg per day, rising to 8% at 60 mg per day. Headache occurs in 2-3% of treated patients
Toxicity
The most commonly reported adverse events occurring more frequently in lansoprazole treated patients compared to placebo include abdominal pain, constipation, diarrhea, and nausea. There is a case report of toxic epidermal necrolysis (TEN), which is a rare but very serious cutaneous reaction, caused by lansoprazole. The previously healthy patient presented with symptoms of TEN 15 days after starting lansoprazole to manage peptic disease. Although the use of PPI's is rarely associated with TEN, causation should be considered if a patient presents with TEN shortly after newly commencing a PPI.
In a single case report, a patient ingested 600 mg of lansoprazole and did not experience any adverse effects or symptoms of overdose. Overall, lansoprazole is well tolerated with relatively few adverse effects.
Navezole is classified as Pregnancy Category B. Although there are animal studies that suggest lansoprazole does not cause harm to the fetus, there is still a paucity of human data. Hence, lansoprazole should only be administered to pregnant women if other options with more safety data have been exhausted.
It is unknown if lansoprazole is excreted in human breast milk. It is worth mentioning that lansoprazole has been used safely in infants, and is therefore likely safe to use during breastfeeding.
Precaution
Gastric malignancy should be ruled out. Hepatic impairment. Pregnancy and lactation.
Interaction
Navezole appears to be a selective inhibitor of the cytochrome P-450 monooxygenase system; there may be an effect on hepatic clearance, but there have been no reports to date of clinically relevant interactions. There is some uncertainty over the effect of Navezole on the oral combined contraceptive pill. Further assessment is currently underway. Physiological changes similar to those found with Omeprazole are likely to take place because of the reduction in gastric acid, which is likely to influence the bacterial colonization of the stomach and duodenum and also vitamin B12 absorption.
Food Interaction
- Take before a meal. Take 30-60 minutes before meals.
Navezole Drug Interaction
Moderate: levothyroxine, levothyroxineMinor: aspirin, aspirin, cyanocobalamin, cyanocobalaminUnknown: omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, pregabalin, pregabalin, metoprolol, metoprolol, acetaminophen, acetaminophen, acetaminophen, acetaminophen, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol
Navezole Disease Interaction
Major: C. diffModerate: liver disease, bone fractures, hypomagnesemia
Volume of Distribution
The apparent volume of distribution of lansoprazole is 0.4 L/kg.
Elimination Route
The oral bioavailability of lansoprazole is reported to be 80-90% and the peak plasma concentration(Cmax) is achieved about 1.7 hours after oral dosing. Food reduces the absorption of lansoprazole (both Cmax and AUC are reduced by 50-70%); therefore, patients should be instructed to take lansoprazole before meals.
Half Life
One source reports the half life of lansoprazole to be 0.9 - 1.6 hours, while another source cites 0.9 - 2.1 hours. The general consensus is that lansoprazole has a short half life and is approximately 2 hours or less. These numbers may be misleading since it suggests that lansoprazole has a short duration of action when in practice, lansoprazole can effectively inhibit acid secretion for ~24 hours due to it's mechanism of action.
Clearance
The reported clearance of lansoprazole is 400-650 mL/min.
Elimination Route
A reported 14-23% of a lansoprazole is eliminated in the urine with this percentage range including both conjugated and unconjugated hydroxylated metabolites.
Pregnancy & Breastfeeding use
Navezole should be avoided in pregnancy unless there are compelling reasons.
Contraindication
Navezole is contraindicated in patients with known hypersensitivity to any component of the formulation.
Special Warning
Neonates:There is no relevant human data. The drug is not recommended for use with neonates.
Children: The youngest person to have received Navezole in clinical trials was 13 years old.
The Elderly: No problems have been encoun- tered in clinical use and there has been no increase in adverse drug reaction in the elderly.
Storage Condition
Store at 25° C.
Innovators Monograph
You find simplified version here Navezole
Navezole contains Lansoprazole see full prescribing information from innovator Navezole Monograph, Navezole MSDS, Navezole FDA label
FAQ
What is Navezole used for?
Navezole is used to treat peptic ulcer disease, gastroesophageal reflux disease, and Zollinger–Ellison syndrome. Navezole is also taken to prevent and treat stomach ulcers.
How safe is Navezole?
Most adults and children can take Navezole. Navezole is not suitable for some people. To make sure it's safe for you, tell your doctor before taking Navezole if you have ever had an allergic reaction to lansoprazole or any other medicines.
How does Navezole work?
Navezole prevents proton pumps from working properly. This reduces the amount of acid the stomach makes.
What are the common side effects of Navezole?
Common side effects of Navezole are include:
- headaches
- feeling sick
- diarrhoea or being sick (vomiting)
- stomach pain
- constipation
- wind
- itchy skin rashes
- feeling dizzy or tired
- dry mouth or throat
Is Navezole safe during pregnancy?
Navezole is not usually recommended if you're pregnant because there is little information about its use during pregnancy. Your doctor may recommend a similar medicine called omeprazole instead as there is more safety information available.
Is Navezole safe during breastfeeding?
If your doctor or health visitor says your baby is healthy, it's safe to take Navezole while you're breastfeeding.It is not known how much passes into breast milk but it's likely to be a very small amount and your baby will not absorb a lot into their body from the breast milk.
Can I drink alcohol with Navezole?
Yes, you can drink alcohol with Navezole. But it's best not to drink too much, because drinking alcohol makes your stomach produce more acid than normal. This can irritate your stomach lining and make your symptoms worse.
Can I drive or ride a bike?
Navezole can make you feel dizzy, sleepy, or get blurred vision. If this happens to you, do not drive, cycle or use machinery or tools until you feel better. It's an offence to drive a car if your ability to drive safely is affected. It's your responsibility to decide if it's safe to drive. If you're in any doubt, do not drive.
When should be taken of Navezole?
You'll usually take Navezole once a day, first thing in the morning.If you take Navezole twice a day, take 1 dose in the morning and 1 dose in the evening.
How to take Navezole?
Swallow the tablets or capsules whole with a drink of water or juice.
If you have problems swallowing capsules, you can open Navezole capsules and mix the granules inside with a little water or fruit juice, or sprinkle them onto soft food, such as yogurt or apple puree, to help you swallow them.
How long can I take Navezole?
Depending on your condition, you may only need to take Navezole for a few weeks or months. Sometimes you might need to take it for longer, even many years.
What happen if I take too much Navezole?
It is very unlikely that taking 1 or 2 extra doses of Navezole will cause any problems.
If you take an extra dose, you might get some of the common side effects. If this happens or you're concerned, contact your doctor.
What happen If I missed dose of Navezole?
If you miss the dose;
- once a day, take the missed dose as soon as you remember, unless it is within 12 hours of your next dose in which case skip the missed dose and take the next one at the usual time
- twice a day, take the missed dose as soon as you remember, unless it is within 4 hours of your next dose in which case skip the missed dose and take the next one at the usual time.
How should I stop taking Navezole ?
Usually, you can stop taking Navezole without reducing the dose first. But if you've taken Navezole for a long time, speak to your doctor before you stop taking it.
What happens If I suddenly stop taking Navezole?
Stopping the medicine suddenly could make your stomach produce a lot more acid, and make your symptoms return.Reducing the dose gradually before stopping completely will prevent this happening.
Will Navezole affect my fertility?
There's no evidence to suggest that taking Navezole will reduce fertility in either men or women.
However, speak to a pharmacist or your doctor if you're trying to get pregnant as they may want to review your treatment.
When will I feel better?
You should start to feel better within 2 to 3 days. However, it may take up to 4 weeks for Navezole to work properly so you may still have some acid symptoms during this time.
Do I have to take Navezole on an empty stomach?
Navezole works best if taken on an empty stomach 30 to 60 minutes before food.
Does Navezole raise blood pressure?
Navezole had no effect on blood pressure and electrocardiogram of anesthetized rat.
Can Navezole affect my kidney?
Navezole may cause kidney damage, which can occur at any time during the treatment. Call your doctor if you have blood in your urine, flank pain or changes in urination during the treatment.
Can Navezole effects my liver?
Navezole therapy is associated with a low rate of transient and asymptomatic serum aminotransferase elevations and is a reported, but very rare cause of clinically apparent liver injury.
Who should not take Navezole?
Navezole is not recommended for use in children younger than 1 year due to an increased risk of serious side effects.
Can Navezole cause heart palpitations?
It's unlikely that acid reflux will cause heart palpitations directly.
