Roxatidine is a specific and competitive histamine H2 receptor antagonist drug that is used to treat gastric ulcers, Zollinger–Ellison syndrome, erosive esophagitis, gastro-oesophageal reflux disease, and gastritis. Pharmacodynamic studies showed that 150 mg of roxatidine acetate were optimal in suppressing gastric acid secretion and that a single bedtime dose of 150 mg was more effective than a dose of 75 mg twice daily in terms of inhibiting nocturnal acid secretion.
Mechanism of Action of Roxatidine
The H2 antagonists are competitive inhibitors of histamine at the parietal cell H2 receptor. They suppress the normal secretion of acid by parietal cells and the meal-stimulated secretion of acid. They accomplish this by two mechanisms: histamine released by ECL cells in the stomach is blocked from binding on parietal cell H2 receptors which stimulate acid secretion, and other substances that promote acid secretion (such as gastrin and acetylcholine) have a reduced effect on parietal cells when the H2 receptors are blocked.
Indications of Roxatidine
- Gastro-esophageal Reflux Disease
- Heartburn
- Hypersecretion gastric
- Bronchogenic carcinoma
- Duodenal ulcer prophylaxis
- Erosive esophagitis
- Indigestion
- Stomach ulcer
- Upper GI Hemorrhage
- Zollinger-Ellison Syndrome
- Active Duodenal ulcer
- Benign gastric ulcers
- Maintenance therapy Duodenal ulcer
- Relief of heartburn, acid indigestion, and sour stomach
- Treatment for gastric and duodenal ulcers
- Treatment for pathologic gastrointestinal hypersecretory conditions such as Zollinger–Ellison syndrome and multiple endocrine adenomas)
- Part of a multidrug regimen for Helicobacter pylori eradication, although omeprazole may be somewhat more effective.
- Prevention of NSAID-induced peptic ulcers.
- Given to surgery patients before operations to reduce the risk of aspiration pneumonitis.
Contra-Indications of Roxatidine
- Clostridium difficile infection
- Inadequate Vitamin B12
- Stomach Cancer
- Liver problems
- Moderate to severe kidney impairment
- Low amount of magnesium in the blood
- Liver problems
- Interstitial Nephritis
- Subacute cutaneous lupus erythematosus
- Hepatic disease, QT prolongation, renal disease, renal failure, renal impairment.
- Systemic lupus erythematosus
- Osteoporosis
- Broken Bone
- Allergies to Proton Pump Inhibitors
Dosage of Roxatidine
Strengths: 75 mg; 150 mg; 300 mg;
Duodenal Ulcer
- Initial: 300 mg orally once a day at bedtime, or alternatively may use 150 mg orally twice a day.
- Maintenance: 150 mg orally once a day at bedtime.
Duodenal Ulcer Prophylaxis
- 150 mg orally once a day at bedtime.
Gastric Ulcer
- 300 mg orally once a day at bedtime, or alternatively may use 150 mg orally twice a day.
Side Effects of Roxatidine
The most common
- Nausea and vomiting
- Severe stomach ache
- Severe diarrhea
- Vaginal thrush
- Skin rash
- A headache
- chest pain
- constipation
- a cough
- diarrhea or loose stools
- difficulty with breathing
- dizziness
- heartburn
- muscle pain
More common
- Abdominal or stomach pain, discomfort, or tenderness
- chills or fever
- difficulty with moving
- a headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in the chest
- discomfort in arms, shoulders, neck or upper back
- excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- sudden slow or difficult speech
- sudden drowsiness or need to sleep
- fast breathing
- sharp pain when taking a deep breath
- fast or slow heartbeat
- coughing up blood
- rust colored urine
- decreased amount of urine
Rare
- Anxiety
- change in vision
- seizures
- abnormal or fast heart rate
- tremors
- weight loss
- chest pain or tightness
- confusion
- a cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- fainting
- hallucinations
- a headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
- muscle spasm or jerking of all extremities
Drug Interactions of Roxatidine
Roxatidine may interact with following drugs, supplements, & may change the efficacy of the drug
- amiodarone
- azole antifungal medications (e.g., fluconazole, ketoconazole)
- caffeine
- calcium channel blockers (e.g., diltiazem, nifedipine, verapamil)
- carbamazepine
- carvedilol
- benzodiazepines (alprazolam, chlordiazepoxide, clonazepam, diazepam, flurazepam, midazolam, and triazolam)
- clopidogrel
- clozapine
- dasatinib
- glyburide (and other “sulfonylurea” diabetes medications)
- lidocaine
- metformin
- metoprolol
- pentoxifylline
- phenytoin
- propranolol
- salmeterol
- SSRIs (e.g., citalopram, fluoxetine, sertraline)
- sucralfate
- theophyllines (e.g., aminophylline, oxtriphylline, theophylline)
- tramadol
- tricyclic antidepressants(e.g., amitriptyline, clomipramine, desipramine, trimipramine)
- warfarin
Pregnancy Catagory
FDA Pregnancy Category N
Pregnancy
The safety of this medication for use during pregnancy has not been established. This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.
Lactation
You should not take roxatidine if you are breastfeeding. It may be excreted in your breast milk and may harm your nursing child.
References
