Sucralfate

A02B - Drugs for peptic ulcer and GORD ATC A02BX02 Unknown approved 1981 Oral

JFDA label: Sucrate Oral Gel

Mechanism of Action

Inhibitor of Pepsin A — Pepsin A inhibitor; Cross-Linking Agent of Glycoproteins — Glycoproteins cross-linking agent

Target	Action	Gene / class
Glycoproteins efficacy	CROSS-LINKING AGENT
Pepsin A efficacy	INHIBITOR	PGA5

Indications

Approved

Duodenal ulcer

Contraindications

Source: Lexicomp

Hypersensitivity to sucralfate or any component of the formulation Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Other (1)

Common Gastrointestinal: Constipation

Dosing

Source: Lexicomp

Duodenal ulcer: Oral: Active duodenal ulcer: Suspension, tablet: Initial: 1 g 4 times daily for 4 to 8 weeks Maintenance therapy: Tablet: 1 g twice daily

(For additional information see "Sucralfate: Pediatric drug information") Esophagitis (off-label use): Oral: Limited data available: (Arguelles-Martin 1989) Infants ≥3 months of age and Children Children ≥6 years of age and Adolescents: 1,000 mg 4 times daily. Peptic ulcer, adjunct therapy (off-label use): Infants, Children, and Adolescents (limited data available): Oral: 40 to 80 mg/kg/day divided every 6 hours (maximum: 1,000 mg/dose) (Kliegman 2016; Nelson 1996)

Refer to adult dosing. Use with caution; initiate at low end of dosage range.

There are no dosage adjustments provided in the manufacturer's labeling. Aluminum salt is minimally absorbed; however, may accumulate in renal impairment; use with caution in patients with chronic renal failure or on dialysis.

There are no dosage adjustments provided in the manufacturer's labeling.

Warnings & Precautions

Source: Lexicomp

Diabetes

Hyperglycemia has been reported with sucralfate suspension in patients with diabetes; monitor glycemia closely; adjustment of antidiabetic treatment may be necessary.

Duodenal ulceration

Because sucralfate acts locally at the ulcer, successful therapy with sucralfate should not be expected to alter the posthealing frequency of recurrence or the severity of duodenal ulceration.

Renal impairment

Use with caution in patients with chronic renal failure; sucralfate is an aluminum complex, small amounts of aluminum are absorbed following oral administration. Excretion of aluminum may be decreased in patients with chronic renal failure or on dialysis, increasing the risk of aluminum accumulation and toxicity (eg, aluminum osteodystrophy, osteomalacia, and encephalopathy). Concurrent drug therapy issues:

Drug-drug interactions

Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information. Dosage form specific issues:

Tablets

Use with caution in patients with conditions that may impair swallowing (eg, recent or prolonged intubation, tracheostomy, dysphagia, history of aspiration) or other conditions that may alter gag/cough reflexes, or diminish oropharyngeal coordination or motility; aspiration with accompanying respiratory complications has been reported. Other warnings/precautions:

Administration

Administer sucralfate by oral route only; fatal complications, including cerebral and pulmonary emboli, have been reported with inadvertent IV administration of sucralfate.

Pregnancy & Lactation

Pregnancy

FDA category B

Adverse events were not observed in animal reproduction studies. Sucralfate is only minimally absorbed following oral administration. Based on available data, use of sucralfate does not appear to increase the risk of adverse fetal events when used during the first trimester (Mahadevan, 2006).

Lactation

It is not known if sucralfate is present in breast milk. Sucralfate is only minimally absorbed following oral administration. The manufacturer recommends that caution be exercised when administering sucralfate to breastfeeding women.

Monitoring

Clinical pearl	Blood glucose levels (in diabetic patients receiving oral suspension).

Chemistry & Properties

Formula	C12H54Al9O55S8
Molecular weight	1577.9 g/mol
PubChem CID	121494085
InChIKey	`YZPQNHUVIVIUCT-JTJNLBSYSA-F`
Polar surface area	536.0 Å²
H-bond acceptors / donors	55 / 20

SMILES

C(C1C(C(C(C(O1)OC2(C(C(C(O2)COS(=O)(=O)O[Al])OS(=O)(=O)O[Al])OS(=O)(=O)O[Al])COS(=O)(=O)O[Al])OS(=O)(=O)O[Al])OS(=O)(=O)O[Al])OS(=O)(=O)O[Al])OS(=O)(=O)O[Al].O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.[Al]

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability	10.0%
Half-life	1.894 h
Volume of distribution	0.534 L/kg
Protein binding	64.1%
BBB penetrant	No

Enzyme interactions

Enzyme	Role	Detail
CYP2C9	Substrate	—

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Drug–drug interactions (100+, DDInter)

Interacting drug	Severity	Management
Bictegravir	major
Dolutegravir	major
Doxercalciferol	major
Paricalcitol	major
Acarbose	moderate
Acetohexamide	moderate
Albiglutide	moderate
Alendronic acid	moderate
Allopurinol	moderate
Alogliptin	moderate
Aluminum hydroxide	moderate
Anisindione	moderate
Ascorbic acid	moderate
Baloxavir marboxil	moderate
Calcifediol	moderate
Calcitriol	moderate
Calcium carbonate	moderate
Canagliflozin	moderate
Chenodeoxycholic acid	moderate
Chlorpropamide	moderate
Cholic Acid	moderate
Cinoxacin	moderate
Ciprofloxacin	moderate
Cyclosporine	moderate
Dapagliflozin	moderate
Deferasirox	moderate
Deferiprone	moderate
Delafloxacin	moderate
Demeclocycline	moderate
Dicoumarol	moderate
Digitoxin	moderate
Digoxin	moderate
Doxycycline	moderate
Dulaglutide	moderate
Eltrombopag	moderate
Empagliflozin	moderate
Enoxacin	moderate
Ertugliflozin	moderate
Ethotoin	moderate
Etidronic acid	moderate

Showing 40 of 100+.

Registered Products (2)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Gastrofait Tab	Tablet 1 g.	20 tab	AL-Faiasel Drug Store	1.950
Sucrate Oral Gel	Gel 1 g/5 ml	30 g tube	AL Rahma Drug Store	4.760