• Ranitidine general information

      • Active – active substance / start: ranitidine

      • Ranitidine

Zantac Ranitidine 150, 300 mg
Most popular brand: Zantac
Active ingredient: Ranitidine
Available dosage forms: 150, 300 mg
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Ranitidine general information

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Active – active substance / start: ranitidine

Apo – Ranitidine; Asitek; Atsideks; Atsilok; Vero – ranitidine; Gene – Ranitidine; Gertokalm; Ki – car; Gistak; Duoran; Zantac; Zantin; Zoran; Neoseptin; Novo – Ranidin; Peptoran; Raniberl; Ranigast; Ranisan; Ranison; Ranitab; Ranital; Ranitard; Ranitidine; Ranitidine Vramed; Ranitidine Sedico; Ranitidine – Akos; Ranitidine – Acre; Ranitidine – Apo; Ranitidine – BMS; Ranitidine – Vero; Ranitidine – ratiopharm; Ranitidine hydrochloride; Ranitin; Rantag; Rantak; Rintid; Renks; Ulkodin; Ulkosan; Ulkuran; Ulran; Ulsereks; Yazitin.

Ranitidine – H2 blocker – histamine receptor 2 – the second generation with a strong and specific affinity to the parietal cells of the stomach and providing gastroselektivnoe action. It affects the root cause heartburn and indigestion, normalizing the process of development of acid in the stomach. Protecting the stomach for a long time. The gold standard in the treatment of gastric ulcer and duodenal ulcer (including stress – ulcer, iatrogenic, NSAID – gastropathy syndrome Zollinger – Ellison syndrome). It is also used in complex therapy aimed at eliminating Helicobacter pylori, with erosive and reflux – esophagitis, non-ulcer dyspepsia, .

What do you know about blockers H2 – histamine receptors
Drugs that block histamine receptors, exert their action, occupying the receptors on mast cells, but without causing further reaction. They are competitive reversible antagonist of histamine.
The main action of histamine on H2 – receptors is to stimulate acid secretion in the stomach. It is well known that histamine is an important mediator of acid secretion caused by all physiological stimuli, such as food, acetylcholine, gastrin, etc. H2 – blockers have no effect on H1 – receptors. Blockade
H2 – receptors effectively suppresses day and night basal secretion of gastric acid secretion and stimulated secretory various stimuli, including histamine, caffeine, food, etc. Therefore, blockers H2 – receptors are an effective approach to the treatment of hypersecretory states and, of course, are a group of the most active of all the drugs that are currently used for the relief of ulcer pain and accelerate the healing of ulcers.
The first antagonist of the H2 – receptor, which has become widely used for the treatment of peptic ulcers, was cimetidine.

Active – active substance:
Ranitidine / Ranitidine hydrochloride / Ranitidine.

Dosage Forms:
Tablets (effervescent tablets).
The solution for injection.

Ranitidine

Properties / Action:
Ranitidine – a highly blocker histamine H2 – receptors. Ranitidine belongs to II generation blockers H2 – histamine receptors. It has a strong and specific affinity to the parietal cells of the stomach and has gastroselektivnoe action.
The main effect of ranitidine is aimed at reducing the aggressiveness of gastric juice. Ranitidine
inhibit basal and stimulated by histamine, gastrin, pentagastrin, and acetylcholine (to a lesser extent) the secretion of hydrochloric acid. Ranitidine reduces the volume of gastric juice of released and the concentration of hydrogen ions in it (increasing pH). Reduces the activity of pepsin.
In addition, ranitidine inhibits degranulation of mast cells, reduces the content of histamine in periultseroznoy zone and promotes ulcer healing process by increasing the amount of DNA – synthesizing cells of the epithelium.
Ranitidine increases glitseroglyukolipidnoe content, which may have a beneficial effect on the healing of peptic ulcers (Sarosiek J. et al.).
Ranitidine increases the tone of the lower esophageal sphincter. This may help prevent casting peptic acid and gastric contents into the esophagus.
Animal studies have shown that Ranitidine inhibits the formation of gastric and duodenal ulcers, formed under the influence of stress, histamine and NSAIDs (eg, aspirin and indomethacin as well).
In patients with peptic ulcer ranitidine significantly reduces the daily intragastric acidity and especially the nocturnal secretion of acid, thereby arresting pain and promoting rapid healing of ulcers. Ranitidine
no effect on serum gastrin concentration, intrinsic factor secretion, pancreatic function, as well as the motility of the duodenum and the stomach emptying time.
Ranitidine 3 – 5 times more active than cimetidine longer valid. After oral administration of 150 mg ranitidine effect occurs within 30 minutes; its concentration in the plasma is sufficient to inhibit acid secretion for 12 hours. Single time dosage 300 mg ranitidine sufficient to inhibit gastric acid secretion in the overnight and the next day.

Ranitidine

300 mg / day

cimetidine 1000 mg / day

The daily secretion of acid

Ranitidine has virtually no effect on the hormonal status, immunological reactivity, microsomal liver enzymes and biotransformation of other medicinal compounds.
Unlike other antagonists containing an imidazole ring in the structure of ranitidine include aminoalkyl furan ring, which replaced the imidazole ring of cimetidine. Due to its unique structure, the effect of Ranitidine on H2 – receptors vysokoizbiratelnyh stomach.
ranitidine important advantage compared to cimetidine consists in the fact that it is not associated with liver enzyme system cytochrome P – 450, which is responsible for the metabolism of various drugs. Thus, Ranitidine does not result in any clinically significant drug interactions with drugs such as propranolol. oral anticoagulants, theophylline. digoxin. diazepam, etc. In patients with several diseases of receiving drugs that may interact with cimetidine, ranitidine has a distinct advantage.
It is known that cimetidine violates the hormonal balance by binding to androgen receptors. This imbalance can lead to an increase in prolactin concentrations, loss of libido, impotence and gynecomastia. This symptoms often observed when high doses of the treatment, such as Zollinger – Ellison. Sometimes even the standard dose might cause these side reactions. The treatment ranitidine these side reactions, by contrast, not only slightly pronounced and occur rarely, and disappear when they are caused by the preceding cimetidine therapy.
Ranitidine Therapeutic doses have no effect on heart rate or blood pressure alone. Cimetidine may cause confusion, especially in elderly patients. Ranitidine rarely leads to adverse reactions from the central nervous system.
The above action on hepatic drug metabolism, endocrine function, and central nervous system are associated mainly with the dose, ie, they are observed in the treatment of cimetidine, as the latter has to be administered in large doses. The therapy ranitidine or famotidine nd these reactions are rare.

Pharmacokinetics:
Ranitidine is well absorbed from the gastro – intestinal tract. When ingestion bioavailability of ranitidine is 40 – 80%. The maximum plasma concentration is reached within 1 – 3 hours after ingestion. Eating and antacids significantly affect the extent of absorption.
When i / m administration is rapidly and almost completely absorbed from the injection site. Cmax is reached after 15 min.
Binding Ranitidin protein is about 15%.
Ranitidin half-life ranging from 2 to 2.5 hours. After 10 hours, following the appointment of 150 mg Ranitidine suppression of gastric acid secretion is much more pronounced.
Ranitidine is metabolised in the liver, subjected to the effect of “first pass” through the liver. It is shown mainly in urine. About 30% of the oral dose excreted in the urine in unchanged form, and about 8% – in the form of metabolites. The residue is excreted with the feces. The elimination rate is reduced with abnormal liver or renal function.
Ranitidine may cross the placenta and is excreted in breast milk.

Indications:

  • prevention and treatment of gastric ulcers and / or duodenal ulcers;
  • symptomatic ulcers (stress – ulcer, iatrogenic, NSAID – gastropathy, et al.);
  • prevention of stress ulcers in critically ill patients, postoperative ulcers, bleeding from the upper gastrointestinal – intestinal tract;
  • with antibacterial drugs in complex therapy aimed at eliminating Helicobacter pylori (the bacteria in nastyaschee This time is considered by many researchers as one of the factors for peptic ulcer);
  • syndrome Zollinger – Ellison;
  • before general anesthesia for the prevention of aspiration of gastric contents into the lungs (Mendelson’s syndrome);
  • and erosive reflux – esophagitis;
  • functional (non-ulcer) dyspepsia (This concept includes “disorders characterized by recurrent complaints of the upper gastrointestinal tract, the causes of which can not be installed clinical examination.” In USA, such patients are diagnosed with “functional stomach disorder”, “gastritis” “duodenitis”. Ranitidine has the best effect in non-ulcer dyspepsia hyperacid type and type of reflux (heartburn manifests itself), although it may have a good effect in other versions).
  • exacerbation of chronic gastritis with increased and normal acidity (Although formally H2 – blockers are not recommended for hypoacid gastritis, it should be noted that in USA are often used deficient methods for studying acidity – not with histamine, and only oral stimulants – which often gives . underreporting acid number of authors also believe that a short course of H2 – blockers can be used even during exacerbation hypoacid (but not atrophic) gastritis, as this is often marked parietal hyperacidity).

    Dosage and administration:
    The mode set individually. Duration of treatment is determined by the indications for use.
    Ranitidine tablet:
    Adults and children over 14 years:
    The recommended dose of Ranitidine in exacerbation of duodenal ulcer or benign gastric ulcer is equal to 300 mg, which is divided into two stages (150 mg in the morning and evening), or is taken once daily 300 mg at night. If necessary, the daily dose may be increased to 450 mg. Treatment should be continued until scarring ulcers, or if the re-examination is not possible, for 4 – 8 weeks. In most cases, gastric and duodenal ulcers healed in 4 weeks. In some cases, you may need to continue treatment until 8 weeks. When the treatment of peptic ulcer disease is not recommended abrupt withdrawal of the drug (especially to scarring ulcers), usually recommended switching to a maintenance dose of 150 mg at night.
    For the prevention of gastric ulcers and / or duodenal ulcers prescribed 150 mg 1 time / day at bedtime for 6 – 12 months.
    In the event of Ranitidine postoperative ulcers appoint 150 mg 2 times / day. Healing generally occurs within 4 weeks.
    To prevent stress ulcers in critically ill patients drug is prescribed 150 mg 2 times / day.
    In states with pathological hypersecretion, such as Zollinger – Ellison syndrome, the recommended dose of Ranitidine is equal to 450 – 900 mg per day in 3 divided doses. In severe cases, apply a dose of up to 6 g per day, which is well tolerated by patients. When
    reflux – esophagitis recommended dose is 150 mg twice daily for 8 weeks, optionally up to 150 mg four times a day. In addition, the state will help to improve the lifting of the head end of the bed and treatment th.
    In the treatment of non-ulcer dyspepsia and gastritis possible shorter course. In many countries, ranitidine 75 mg sold as a non-prescription drug for use in non-ulcer dyspepsia, 75 mg 4 times a day.
    To eliminate Helicobacter pylori Ranitidine may be used as follows: Ranitidine 10 – 12 days on 150 mg twice a day in combination with 500 mg amoxicillin ohm 4 times a day, or 500 mg 3 times a day, or th 250 mg 4 times a day. Then 18 days Ranitidine 300 mg at night.
    The high efficiency of the following schemes: ranitidine 300 mg twice daily, clarithromycin 250 mg 2 times a day, 500 mg two times daily for 14 days, then Ranitidine reception for an additional 4 weeks.
    The usual dose for prevention of recurrent gastro – intestinal bleeding in patients with peptic ulcer disease is 150 mg twice a day.
    surgical patients at risk for aspiration of gastric contents, you need to give 300 mg of ranitidine into the night before surgery.
    Services Assign inside of 2 – 4 mg / kg 2 times a day with a stomach ulcer and duodenal ulcer (maximum – 300 mg / day), with reflux – esophagitis – 2 – 8 mg / kg 3 times a day.
    Ranitidine injections:
    surgical patients at risk for aspiration of gastric contents (including during childbirth), for the prevention of gastric bleeding and stress ulcer: 50 mg / in or / m for 45 – 60 minutes before anesthesia, and then 50 – 100 mg of (2 – 4 mL) / m or / every 6 – 8 hours.
    / m administered 50 mg of ranitidine without dilution. For
    on / in the 50 mg diluted to 20 ml in an appropriate solution and introduced into / in slowly over 5 minutes (described rare cases when bradycardia rapid introduction).
    For in / drip diluted 50 mg not more than 100 ml and administered at 25 mg / hour.
    Ranitidine injection is generally compatible with the following solutions: 0.9% sodium chloride solution. 5%, 10% dextrose, Ringer’s lactate solution, 5% sodium bicarbonate for injection.
    In patients with severe renal insufficiency, the dose should be reduced. Patients with creatinine clearance less than 50 mL / min, ranitidine daily dose should be reduced to 150 mg per day (75 mg, 2 times / day). Assign half of the usual dose produces adequate drug concentration in plasma with no signs of its accumulation.

    Overdose:
    Treatment: induction of vomiting or gastric lavage, in convulsions – diazepam / O, with bradycardia – atropine. with ventricular arrhythmia – lidocaine.

    Contraindications:

  • pregnancy;
  • lactation (breastfeeding);
  • Children under the age of 14;
  • Individual intolerance (including a history of hypersensitivity) ranitidine.
    Restrictions on the use of liver cirrhosis, renal failure.

    Use during pregnancy and lactation:
    Ranitidine crosses the placenta and is secreted in breast milk.
    There are no adequate and well-controlled studies safety of ranitidine during pregnancy was conducted, and therefore the use in pregnancy is contraindicated. Ranitidine may be assigned during pregnancy only if absolutely indicated.
    If necessary, use ranitidine during lactation should stop breastfeeding.

    Side effects:
    Ranitidine is considered a drug with high safety. As in the short term and in the long-term studies ranitidine was well tolerated. The frequency of side effects is low and comparable with that of placebo.
    Cardio – vascular system: in isolated cases of arrhythmia (tachycardia, bradycardia, asystole, AV block, premature beats).
    From the digestive system: rarely – diarrhea, constipation, nausea, vomiting, flatulence, dry mouth; in rare cases – hepatitis.
    From the CNS: rarely – headache, dizziness, fatigue, drowsiness, blurred vision; in rare cases (severely ill) – confusion, hallucinations. Confusion and depression that can occur when taking cimetidine, especially in elderly patients, are extremely rare in the treatment of ranitidine.
    From the hematopoietic system: rarely – thrombocytopenia; long-term use at high doses – leukopenia.
    On the part of metabolism: rarely – a slight increase in serum creatinine at the beginning of treatment (these changes are clinically not significant). Rare cases of interstitial necrosis, have been observed in the treatment of cimetidine, ranitidine is not described for.
    From the endocrine system: long-term use at high doses may increase prolactin, gynecomastia, amenorrhea, impotence, decreased libido. Patients carrying bad cimetidine, ranitidine, have been translated into, and the recurrence of adverse actions such as gynecomastia and impotence was not.
    From the bone – muscular system: very rarely – arthralgia, myalgia.
    Allergic reactions: seldom – skin rash, urticaria, angioedema, anaphylactic shock, bronchospasm, hypotension.
    Other: rarely – recurrent mumps; in rare cases – loss of hair.

    Special instructions and precautions:
    With care prescribe a drug to patients with severe liver and / or kidneys.
    Keep out of reach of children!
    The expiration date on the package.