Last Updated on June 3, 2023
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What is Ranitidine?
The blocker of histamine H2-receptors. Suppresses the basal and stimulated by histamine, gastrin and acetylcholine (to a lesser extent) the secretion of hydrochloric acid. It increases the pH of gastric contents and reduces the activity of pepsin. The duration of action ranitidine with a single admission – 12 hours. The active ingredient Ranitidine is one of the drugs to treat heartburn and peptic ulcers. Because it is not as potent as other drugs against these diseases, Ranitidine is used only as a means of second choice. Children and pregnant women should not take the drug after a detailed medical examination. Here you can read everything about Ranitidine.
How Ranitidine works?
Once inside, ranitidine is rapidly absorbed from the digestive tract. Food intake and antacids slightly affect the degree of absorption. Exposed to the effect of “first passage” through the liver. Cmax in plasma is achieved 2 hours after a single oral intake. After the / m introduction quickly and almost completely absorbed from the injection site. Cmax is reached after 15 minutes.
Binding to proteins – 15%. Vd – 1.4 l / kg. Ranitidine is excreted in breast milk.
T1 / 2 is 2-3 hours. About 30% of the dose is excreted unchanged in the urine. The rate of excretion is reduced if the liver or kidney function is impaired.
Especially in the fasting state, the gastric environment is very acidic. This is important, since the ingested food must meet a mix of acid and enzymes to ensure a first digestion and bacterial killing. In order to maintain this environment, the body has a complex control mechanism, to which various neurotransmitters such as histamine and acetylcholine (acid-stimulating) and prostaglandins (acid-resistant) are involved.
Normally, the aggressive gastric acid would attack the wall of the stomach, if it were not protected. That protection is an acid-neutralizing mucus is mainly involved, which is like a film on the stomach inner wall.
In some cases, however, this protection could be affected or are inadequate. The acid can then cause by attacking the stomach wall an ulcer. In addition, when it comes to heartburn regurgitation: Acid stomach contents rise up (reflux) and comes with the unprotected esophageal mucosa in contact. An inflammation of the esophagus is the possible consequence (reflux oesophagitis).
Ranitidine belongs to the so-called H 2antihistamines and inhibits the production of acid in specific cells (parietal cells) of the stomach. There, the active agent blocks the docking sites (receptors) from the acid-stimulating histamine, resulting in less acid is pumped into the gastric compartment. As a result, the gastric environment is less acidic, which relieves the symptoms.
Pharmacokinetics and metabolism of Ranitidine
After recording via the mouth (oral), the active ingredient in a sufficient amount from the intestine is absorbed into the blood. The maximum effect occurs after about two hours. After its distribution in the body Ranitidine is metabolised in the liver. The degradation products are then excreted by the kidneys.
When is Ranitidine prescribed?
Stomach ulcer and duodenal ulcer in the phase of exacerbation; prevention of exacerbations of peptic ulcer; symptomatic ulcers; erosive and reflux esophagitis; Zollinger-Ellison syndrome; prevention of “stressful” gastrointestinal ulcers, postoperative ulcers, relapses of bleeding from the upper gastrointestinal tract; prevention of aspiration of gastric juice during surgery under anesthesia.
Among the areas of application (indications) of Ranitidine include:
- short-term treatment of heartburn and acid-related esophageal inflammation (reflux esophagitis)
- gastrointestinal ulcers
How to take Ranitidine?
Usually, Ranitidine is applied in the form of tablets. The usual dose ranges from 75 milligrams (short-term treatment of heartburn) to 300 milligrams (in acute gastrointestinal ulcers). The tablets may be taken with or without a meal, sometimes a dose is recommended right after eating before going to bed.
Dosage
Install individually. Inside for the treatment of adults and children over 14 years of age use in a daily dose of 300-450 mg, if necessary, the daily dose is increased to 600-900 mg; the frequency of reception is 2-3 times / day. For the prevention of exacerbations of diseases apply 150 mg / day before bedtime. The duration of treatment is determined by indications for use. Patients with renal insufficiency with a creatinine level of more than 3.3 mg / 100 ml – 75 mg 2 times / day.
In / in or / m – for 50-100 mg every 6-8 hours.
Do you treat heartburn with Ranitidine itself over a period of 14 days. Then should not have improved the symptoms, a medical examination is suggested.
Side effects
Often, that is at more than ten percent of those treated, can cause such side effects Ranitidine. This is mainly due to the increase in the number of bacteria in the stomach, because less acid in the stomach is a destruction of the bacteria in the food available.
It may occasionally on by taking Ranitidine to head, and joint and cardiac arrhythmias.
Ranitidine for violations of kidney function
Use with caution in patients with impaired renal excretion.
Use in children
Clinical data on the safety of ranitidine in pediatrics are limited.
Special instructions
Use with caution in patients with impaired renal excretion.
Before starting treatment, it is necessary to exclude the possibility of having a malignant disease of the esophagus, stomach or duodenum.
With long-term treatment in weakened patients under stress, bacterial lesions of the stomach are possible with the subsequent spread of infection.
It is undesirable to abruptly stop taking ranitidine because of the risk of recurrence of peptic ulcer. The effectiveness of preventive treatment of peptic ulcer is higher when taking ranitidine by courses of 45 days in the spring-autumn period than with a constant intake. Rapid intravenous administration of ranitidine in rare cases causes bradycardia, usually in patients predisposed to heart rhythm disturbances.
There have been isolated reports that ranitidine may contribute to the development of an acute attack of porphyria, and therefore it is necessary to avoid its use in patients with acute porphyria in the anamnesis.
Against the background of the use of ranitidine, there may be distortions in laboratory data: an increase in the level of creatinine, GGT activity and liver transaminase in the blood plasma.
In those cases where ranitidine is used in combination with antacids, the interval between taking antacids and ranitidine should be at least 1-2 hours (antacids can cause impaired absorption of ranitidine).
Clinical data on the safety of ranitidine in pediatrics are limited.
Drug Interactions
With simultaneous use with antacids, it is possible to reduce the absorption of ranitidine.
When used simultaneously with anticholinergic drugs, memory and attention may be impaired in elderly patients.
It is believed that the histamine H2 receptor blockers reduce the ulcerogenic effect of NSAIDs on the gastric mucosa.
With simultaneous use with warfarin, a decrease in warfarin clearance is possible. A case of development of hypoprothrombinemia and bleeding in a patient receiving warfarin is described.
With the simultaneous use of dicitrate with bismuth tricalium, an undesirable increase in the absorption of bismuth is possible; with glibenclamide – cases of development of hypoglycemia are described; with ketoconazole, itraconazole – the absorption of ketoconazole, itraconazole decreases.
With simultaneous use with metoprolol, an increase in plasma concentration and an increase in AUC and T1 / 2 metoprolol may occur.
With simultaneous application with sucralfate in high doses (2 g), a violation of the absorption of ranitidine is possible.
With simultaneous use with procainamide, a decrease in the excretion of procainamide by the kidneys is possible, which leads to an increase in its concentration in the blood plasma.
There is evidence of an increase in the absorption of triazolam when it is used concomitantly, apparently due to a change in the pH of the stomach contents under the influence of ranitidine.
It is believed that with simultaneous use with phenytoin, an increase in the concentration of phenytoin in the blood plasma and an increased risk of toxicity development are possible.
With simultaneous application with furosemide moderately expressed increase in bioavailability of furosemide.
A case of development of ventricular arrhythmia (bigemini) is described with simultaneous application with quinidine; with cisapride – the case of the development of cardiotoxicity has been described.
It is impossible to exclude a slight increase in the concentration of cyclosporine in the blood plasma when it is used simultaneously with ranitidine.
medication with Ranitidine may not be applied when the treated suffers from a certain metabolic disorder (porphyria).
Interaction
In a concomitant use of Ranitidine may increase the effect of the following medications:
- Diazepam (for insomnia)
- lidocaine, procainamide (for irregular heart beat)
- Phenytoin (for epilepsy)
- Propranolol (at)
- Theophylline (shortness of breath diseases such as asthma)
- warfarin, phenprocoumon (blood thinners)
By changing the gastric environment, it may happen that the following active substances are absorbed better, which enhances their effect:
- triazolam, midazolam (sedatives)
- glipizide (diabetes)
The inclusion of the following medications is decreased by Ranitidine, which can lead to a weakening of action:
- ketoconazole (for fungal infections)
- atazanavir, delavirdine (HIV-disease)
- Gefitinib (in cancer)
Driving and using machines
By taking Ranitidine, it may occasionally be subject to an impairment of the ability to react. Therefore, everyone should wait for the reaction of his own body on the drug and decide together with the doctor about the ability to drive.
This applies in particular in combination with alcohol as Ranitidine greatly slowed its degradation.
Parental
Without medical advice medication with Ranitidine should not be used in children under 16 years. Kicking in children or adolescents symptoms like acid reflux or stomach pain, a doctor should always be consulted.
Pregnancy and lactation
medication with Ranitidine may be taken by pregnant and lactating women after strict benefit-risk assessment when neutralizing drugs were not successful in the treatment of heartburn.
Experience has shown that Ranitidine is very well tolerated and leaves no lasting harm to your baby and infant. It is thus as a treatment of choice for pregnant and breastfeeding women.
Where to buy Ranitidine?
Medication at a low dose of Ranitidine (75 milligrams per tablet) are sold freely available in pharmacies. For a long-term and higher-dose treatment, however, a prescription is required by the physician in order to ensure regular monitoring of therapeutic success. But you can buy Ranitidine 150 & 300 mg otc online.
Since when Ranitidine is known?
Ranitidine is already relatively long known as an active ingredient. As with the so-called proton pump inhibitors (Omeprazole, Pantoprazole), however, a drug class is available which has a stronger and more effective in heartburn and peptic ulcers, apply Ranitidine only as a means of second choice.