Rafate
Rafate Uses, Dosage, Side Effects, Food Interaction and all others data.
Rafate protects GI lining against peptic acid, pepsin and bile salts by binding with positively-charged proteins in exudates forming a viscous paste-like adhesive substance thus forming a protective coating.
This drug aids in the healing of duodenal ulcers, relieving painful inflammation by creating a protective mechanical barrier between the lining or skin of the gastrointestinal tract and damaging substances . In addition, sucralfate acts to increase levels of growth factors locally, and also causes an increase in prostaglandins which are important in the healing of the mucosa (lining) of the gastrointestinal tract .
| Trade Name | Rafate |
| Availability | Prescription only |
| Generic | Sucralfate |
| Sucralfate Other Names | Sucralfat, Sucralfate, Sucralfato, Sucralfatum |
| Related Drugs | omeprazole, famotidine, pantoprazole, triamcinolone topical, Nexium, Pepcid, Protonix, esomeprazole, Prilosec, ranitidine |
| Weight | 500mg, 1g/5ml |
| Type | Tablet, Suspension |
| Formula | C12H35Al9O55S8 |
| Weight | Average: 1558.67 Monoisotopic: 1557.6045961 |
| Protein binding | Sucralfate is bound to plasma proteins, especially albumin and transferrin . |
| Groups | Approved |
| Therapeutic Class | Chelating complex |
| Manufacturer | Rakaposhi Pharmaceutical (pvt) Ltd, |
| Available Country | Pakistan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Rafate tablet is used for the treatment of acute, nonmalignant gastric and duodenal ulcers. Maintenance therapy to prevent the recurrence of duodenal ulcers.
Rafate suspension is used for the short-term (up to 8 weeks) treatment of active duodenal ulcer.
Rafate is also used to associated treatment for these conditions: Dyspepsia, Gastric Ulcer, Gastritis, Gastro-esophageal Reflux Disease (GERD), Healing, Mucositis, Peptic Ulcer, Stress Ulcers, Active Duodenal ulcer, Antiplatelet Therapy
How Rafate works
The mechanism of action of this drug in the healing duodenal ulcers is not yet completely defined, however, there are several probable mechanisms that adequately describe the healing activity of sucralfate. There is evidence that sucralfate acts locally to aid in tissue healing, and not systemically .
Studies in both humans and animals have indicated that sucralfate forms a complex that binds to protein-rich exudate found on the surface of ulcers. It binds to albumin and fibrinogen preventing blood clot lysis by stomach acid (hydrochloric acid). Rafate increases the tissue levels of fibroblast growth factors and epidermal growth factors , leading to an increase in prostaglandins at the gastrointestinal tract lining, which promote the healing of gastrointestinal ulcers .
In the laboratory setting, a sucralfate-albumin film provides a barrier against the entry of hydrogen ions, which are a component of gastric acid. In humans, sucralfate, given at therapeutic doses for ulcers, decreases pepsin activity in gastric fluids by 32% . Pepsin has been shown to be damaging to tissues, further aggravating ulcer lesion inflammation . Bile salts have been implicated in mucosal injury to the gastrointestinal tract . Rafate has also been shown to adsorb bile salts in the laboratory, setting, which could further contribute to its beneficial effects in ulcer healing .
Dosage
Rafate dosage
Adult: Usual dose 1 gm 4 times daily to be taken 1 hour before meals and at bed time. Maximum daily dose is 8 gm. Four to six weeks treatment is usually needed for ulcer healing but upto twelve weeks may be necessary in resistant cases. Antacids may be used as required for relief of pain, but should not be taken half an hour before or after Gastalfet.
Elderly: There are no special dosage requirements for elderly patients but as with all medicines the lowest effective dose should be used.
children: Safety and efficacy in children have not been established
Side Effects
The incidence and severity of side effects from sucralfate are very low. Mild side effect like constipation has been reported in some patients.
Toxicity
Overdose
Overdosage has never been observed with sucralfate . It is unlikely, as administering a maximum dose of up to 12 g/kg/body weight in several animal species did not result in death. The lethal dose could not be determined in these studies . It is likely that overdose of sucralfate in humans would result in constipation, and supportive treatment would be advised .
Use in pregnancy
This drug is considered a pregnancy Category B drug. Studies have been performed in rodents and rabbits at doses up to 50 times the recommended human dose. No harm to the fetus has been observed in the abovementioned studies. Sufficient and well-controlled clinical trials have not been performed in pregnant women. Due to the fact that the results of animal studies are not always relevant to human response, sucralfate should be used during pregnancy only if it is deemed essential for the mother's health .
Use in nursing
Whether this drug is excreted in human milk is currently unknown. Many drugs are excreted in breast milk, therefore, if sucralfate is administered to a lactating and nursing woman, caution should be observed .
Carcinogenesis
24 month toxicity studies were performed in rodents, and the dose of sucralfate reached up to 1 g/kg (equivalent to 12 times the recommended human dose). No signs of sucralfate-related tumors were noted.
Precaution
The product should only be used with caution in patients with renal dysfunction
Interaction
Concomitant use of sucralfate may reduce the bioavailability of certain drugs as has been observed in animal studies with tetracycline, phenytoin and cimetidine and in human studies with digoxin. Administration of sucralfate with any of these drugs should be separated by two hours. Since sucralfate may hinder warfarin absorption, caution should be exercised when these two drugs are used together.
Food Interaction
- Take on an empty stomach. Take at least 1 hour before or 2 hours after meals.
- Take separate from antacids. Take at least 30 minutes before or after antacids.
[Moderate] ADJUST DOSING INTERVAL: The administration of sucralfate with enteral nutrition may result in precipitation and the formation of bezoars that may obstruct feeding tubes.
The proposed mechanism is the formation of an insoluble aluminum-protein complex between the aluminum in the sucralfate and the protein in the enteral feeding.
In addition, sucralfate may not become activated due to the alkaline pH of enteral nutrition products.
MANAGEMENT: Some experts recommend separating the sucralfate doses from enteral feedings by at least 1 hour.
Alternatively, consideration may be given to proton pump inhibitors or H2 antagonists.
Rafate Drug Interaction
Major: cholecalciferolModerate: ascorbic acidMinor: metoprolol, metoprolol, levothyroxineUnknown: aspirin, diphenhydramine, duloxetine, dexlansoprazole, omega-3 polyunsaturated fatty acids, pregabalin, esomeprazole, albuterol, pantoprazole, montelukast, acetaminophen, cyanocobalamin, alprazolam, ondansetron, cetirizine
Rafate Disease Interaction
Volume of Distribution
This drug is absorbed in a very small quantity, and normally localizes to inflamed gastrointestinal lesions .
Elimination Route
This drug is absorbed from the gastrointestinal tract in very minimal quantities . The adsorbed sulfated disaccharide is excreted in the urine . This drug contains aluminum and after the administration of 1 g of sucralfate 4 times per day, about 0.001% to 0.017% of this aluminum content is absorbed in patients with normal renal function . This number is expected to increase in those with impaired renal function .
Half Life
The half-life is not known. In animals, the elimination half-life of the sucrose component of this drug is from 6-20 h .
Clearance
Rafate contains aluminum. The administration of sucralfate in non-dialyzed chronic renal failure patients warrants careful consideration from the treating physician as the excretion of absorbed aluminum may be decreased, causing possible aluminum toxicity .
In dialyzed patients diagnosed with chronic renal failure, aluminum toxicity related to sucralfate has been observed and reported. The daily amount of aluminum ingestion (including sucralfate) should be carefully examined before administering sucralfate in combination with other drugs also containing aluminum, including various antacids .
Elimination Route
The negligible amount of this drug that is absorbed is excreted mainly in the urine within 48 hours .
Pregnancy & Breastfeeding use
Although animal studies show no evidence of foetal malformation, safety in pregnant women has not been established and Rafate should be used in pregnancy only if clearly needed.
It is not known whether this drug is excreted in human milk. Caution should be exercised when sucralfate is administered to nursing mothers.
Contraindication
There are no known contraindications
Acute Overdose
There is no experience in human with overdosage
Storage Condition
Store at 20-25° C.
Innovators Monograph
You find simplified version here Rafate
Rafate contains Sucralfate see full prescribing information from innovator Rafate Monograph, Rafate MSDS, Rafate FDA label
FAQ
What is Rafate used for?
Rafate is used short-term (up to 8 weeks) to treat an active duodenal ulcer. Rafate works mainly in the lining of the stomach and is not highly absorbed into the body. This medicine adheres to ulcer sites and protects them from acids, enzymes, and bile salts.
Is Rafate good for acid reflux?
Rafate and omeprazole are used to treat ulcers and gastroesophageal reflux disease (GERD). Omeprazole is also used to treat Zollinger-Ellison syndrome, duodenitis, erosive esophagitis, heartburn, and H. pylori infection.
What are side effects of Rafate?
Rafate side effects are Constipation, dry mouth, upset stomach, gas, and nausea may occur. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.
What are the side effects of Rafate?
Rafate Side effects are include:
- Back pain
- Constipation
- Diarrhea
- Dizziness
- Drowsiness
- Dry mouth
- Gas (flatulence)
- Headache
- Indigestion
- Itching or skin rash
- Nausea
- Sleep problems (insomnia)
- Spinning sensation (vertigo)
- Stomach pain
- Upset stomach
- Vomiting
Is Rafate bad for kidneys?
Aluminum accumulation and toxicity have been reported with the use of sucralfate in patients with compromised renal function. The risk of toxicity most likely represents a long-term complication of Rafate use in this patient population.
Does Rafate cure gastritis?
Rafate is the primary agent for prophylaxis of stress gastritis. It has long been used as a means of decreasing the incidence of gastritis.
Can I drink water while taking Rafate?
Take Rafate by mouth with a glass of water. Follow the directions on the prescription label. This medicine works best if you take it on an empty stomach, 1 hour before meals. Take your doses at regular intervals.
Does Rafate help with gas?
Rafate administration was accompanied by the disappearance of heartburn, epigastric pain, epigastric distress, or epigastric burning in 42 of 59 occurrences, and by statistically significant reductions in bloating.
What is the best time to take Rafate?
Take Rafate on an empty stomach, 2 hours after or 1 hour before meals. Take Rafate around the same times every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand.
What should not take with Rafate?
Some antacids can make it harder for Rafate to work in your stomach. Avoid taking an antacid within 30 minutes before or after taking Rafate.
Can Rafate cause loose stools?
Rafate may cause constipation, diarrhea, nausea, and headache.
Can Rafate cause frequent urination?
This medicine may affect your blood sugar levels. Check with your doctor right away if you have increased thirst or increased urination.
What color is urine when your kidneys are failing?
When kidneys are failing, the increased concentration and accumulation of substances in urine lead to a darker color which may be brown, red or purple. The color change is due to abnormal protein or sugar, high levels of red and white blood cells, and high numbers of tube-shaped particles called cellular casts.
Does Rafate really work?
Rafate has an average rating of 5.7 out of 10 from a total of 50 ratings for the treatment of Stomach Ulcer. 38% of those users who reviewed Rafate reported a positive effect, while 30% reported a negative effect.
Does Rafate coat the stomach?
Rafate is used to treat and prevent duodenal ulcers and other conditions as determined by your doctor. It works by forming a barrier or coat over the ulcer. This protects the ulcer from the acid of the stomach, allowing it to heal.
Why Rafate should not be used with antacids?
As the Rafate is effective only in acid conditions, an antacid should not be taken 30 min before or after a dose. Rafate interferes with absorption of several drugs, including ciprofloxacin, theophylline, digoxin, phenytoin and amitriptyline, possibly by binding due to its strong negative charge.
