Receptoloc

Uses

Receptoloc is used for up to 8 weeks for the treatment of active duodenal ulcer. In most patients, the ulcer will heal within 4 weeks.

Receptoloc is used for maintenance therapy for duodenalulcer patients, at a reduced dosage of 150 mg h.s. after healing of an active duodenal ulcer. The consequences of continuous therapy with Receptoloc for longer than 1 year are not known.

Receptoloc is used for up to 12 weeks for the treatment of endoscopically diagnosed esophagitis, including erosive and ulcerative esophagitis, and associated heartburn due to GERD.

Receptoloc is used for up to 8 weeks for the treatment of active benign gastric ulcer. Before initiating therapy, care should be taken to exclude the possibility of malignant gastric ulceration.

Receptoloc is also used to associated treatment for these conditions: Duodenal Ulcer, Esophagitis, Gastric Ulcer, Gastro-esophageal Reflux Disease (GERD), Helicobacter Pylori Infection, Peptic Ulcer Disease, Stress Ulcers

How Receptoloc works

Receptoloc competes with histamine for binding at the H₂-receptors on the gastric basolateral membrane of parietal cells. Competitive inhibition results in reduction of basal and nocturnal gastric acid secretions. The drug also decreases the gastric acid response to stimuli such as food, caffeine, insulin, betazole, or pentagastrin.

Dosage

Receptoloc dosage

Active Duodenal Ulcer: The recommended oral dosage for adults is 300 mg once daily at bedtime. An alternative dosage regimen is 150 mg twice daily.

Maintenance of Healed Duodenal Ulcer: The recommended oral dosage for adults is 150 mg once daily at bedtime.

Gastroesophageal RefluxDisease: The recommended oral dosage in adults for the treatment of erosions, ulcerations, and associated heartburn is 150mg twice daily.

Active Benign Gastric Ulcer: The recommended oral dosage is 300 mg given either as 150 mg twice daily or 300 mg once daily at bedtime. Prior to treatment, care should be taken to exclude the possibility of malignant gastric ulceration.

Side Effects

Headache, dizziness, insomnia, abnormal dreams, somnolence, asthenia, anxiety, excessive sweating, diarrhoea, nausea and/or vomiting, abdominal pain/discomfort, constipation, flatulence, dyspepsia, dry mouth, anorexia, tooth disorder, urticaria, rash, pruritus, exfoliative dermatitis, anaemia, rhinitis, pharyngitis, sinusitis, reversible hepatocellular injury, diaphoresis, myalgia, fever. Rarely, asymptomatic ventricular tachycardia, thrombocytopenic purpura, decreased libido, gynaecomastia, reversible cholestatic or mixed cholestatic-hepatocellular injury with jaundice.

Toxicity

Oral, rat LD₅₀: 301 mg/kg. Symptoms of overdose include cholinergic-type effects including lacrimation, salivation, emesis, miosis, and diarrhea.

Precaution

Possibility of malignancy should be excluded prior to therapy as the drug may mask symptoms and delay diagnosis of gastric malignancy. Increased risk of community-acquired pneumonia. Renal impairment. Pregnancy and lactation.

Interaction

No interactions have been observed between Receptoloc and theophylline, chlordiazepoxide, lorazepam, lidocaine, phenytoin, and warfarin. Receptoloc does not inhibit the cytochrome P-450-linked drug-metabolizing enzyme system; therefore, drug interactions mediated by inhibition of hepatic metabolism are not expected to occur. In patients given very high doses (3,900 mg) of aspirin daily, increases in serum salicylate levels were seen when nizatidine, 150 mg b.i.d., was administered concurrently.

Food Interaction

• Avoid alcohol.
• Limit caffeine intake.
• Take with or without food. The absorption is unaffected by food.

Receptoloc Drug Interaction

Minor: duloxetineUnknown: aspirin, celecoxib, rosuvastatin, escitalopram, atorvastatin, pregabalin, esomeprazole, acetaminophen, clopidogrel, quetiapine, montelukast, levothyroxine, acetaminophen, ascorbic acid, cholecalciferol, alprazolam, ranitidine, ondansetron, cetirizine

Receptoloc Disease Interaction

Major: GI bleedingModerate: renal dysfunction

Volume of Distribution

• 0.8 to 1.5 L/kg

Elimination Route

Rapid (bioavailability of nizatidine exceeds 70%)

Half Life

1-2 hours

Clearance

• 40-60 L/h
• 7 – 14 L/h [functionally anephric patients]

Pregnancy & Breastfeeding use

Pregnancy Category B. Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Contraindication

Receptoloc is contraindicated in patients with known hypersensitivity to the drug. Because cross sensitivity in this class of compounds has been observed, H2-receptor antagonists, including Receptoloc , should not be administered to patients with a history of hypersensitivity to other H2-receptor antagonists.

Special Warning

Dosage Adjustment for Patients With Moderate to Severe Renal Insufficiency-Active Duodenal Ulcer, GERD and Benign Gastric Ulcer:

• CrCl 20-50 ml/min: 150 mg daily
• CrCl <20 ml/min: 150 mg every other day

Maintenance Therapy:

• CrCl 20-50 ml/min: 150 mg every other day
• CrCl <20 mL/min: 150 mg every 3 days

Some elderly patients may have creatinine clearances of less than 50 ml/min, and, based on pharmacokinetic data in patients with renal impairment, the dose for such patients should be reduced accordingly. The clinical effects of this dosage reduction in patients with renal failure have not been evaluated.

Acute Overdose

Symptoms: Lacrimation, salivation, emesis, miosis, and diarrhoea.

Management: Symptomatic and supportive treatment. Activated charcoal, emesis or lavage may reduce absorption.

Storage Condition

Store at 25°C

Innovators Monograph

You find simplified version here Receptoloc