SUCRALFATE
 
   
 
Category: Cytoprotective & Regenerative

Molecular Formula: C12H22O35S8

Sucralfate is an amorphous complex of aluminium hydroxide and sucrose sulphate, identified by the name: β-D-fructofuranosyl-α-D-glucopyranoside octakis (hydrogen sulphate) aluminium complex. When the pH in the stomach is below 4, there is extensive polymerization and cross-linking of Sucralfate. The condensed polymer is a very sticky, viscid, yellow white gel. Even though the pH in the duodenum is well above 4, gel retains its viscid, demulcent properties. The gel adheres strongly to epithelial cells and to the base of ulcer craters. The affinity for the crater base is much higher than that for the epithelial surface and it is difficult to wash the gel from the crater. The gel remains adherent to ulcerated epithelium for, at least 12 hours and this binding to ulcer craters probably represent the main therapeutic action ofSucralfate.

SUCRALFATE- MODE OF ACTION
Sucralfate is aluminium salt of Sucrose octasulfate. Sucralfate is structurally unrelated to other anti-ulcer drugs. Molecular weight of anhydrous form of Sucralfate is 2057. Sucralfate contains 20 percent aluminium by weight. Sucralfate when comes in contact with gastric juice it polymerizes. Polymerized Sucralfate covers ulcer site selectively and strongly. Polymerized Sucralfate is negatively (-ve) charged. Sucralfate is negatively charged at acidic pH due to presence of S03- (sulfite). Proteins of damaged mucosa is positively (+ve) charged at acid pH, so there will be an electrostatic binding between Sucralfate and damaged ulcer site of stomach or duodenum.
(SUCRALFATE)
(.ve) (.ve) (.ve)
ELECTROSTATIC (+ve) (+ve) (+ve) BINDING

(DAMAGED MUCOSA AT STOMACH OR DUODENUM)
For this reason polymerized Sucralfate covers ulcer site strongly. This thick layer of Sucralfate provides a barrier at ulcer site to aggressive factors.

MECHANISM OF ACTION
1. SUCRALFATEcoats the ulcer site electro-statically by giving Band-Aid protection.
2. SUCRALFATE preserves mucosal integrity and increases mucosal blood flow through Nitric Oxide synthesis
3. SUCRALFATE prevents back diffusion of hydrogen ions through ulcer site and thereby prevents tissue acidosis.
4. SUCRALFATE stimulates mucus secretion and bicarbonate secretion by chloride-bicarbonate exchange pump at luminal side.
5. SUCRALFATE enhances Epidermal Growth Factors and Fibroblast Growth Factors binding and granulation tissue for qualitative ulcer healing.
6. SUCRALFATE stimulates prostaglandin synthesis at the level of G.I. mucosa & helps in angiogenesis.
7. SUCRALFATE adsorbs pepsin and bile.
8. SUCRALFATE does not alter stomach pH, thus prevents nosocomial infection. Sucralfate is not absorbed and is therefore very safe. No systemic side effects.

SUCRALFATE IN THE PREVENTION OF NOSOCOMIAL INFECTION
Sucralfate exerts three prolonged action to act as prophylactic in reducing stress ulcer, preventing stress bleeding and negates the risk of Nosocomial infection.
1) Sucralfate reduces the chance of bacterial overgrowth by not affecting stomach pH.
2) Sucralfate reduces bacteria translocation through the gut mucosa into the system
3) Sucralfate exerts a drug septic antibacterial effect by competitive inhibition (phagocytosis)

MODE OF ACTION OF TOPICAL USE OF SUCRALFATE
1. Regenerative
In the process of regeneration, Sucralfate being structurally similar to Heparin mimics the action of Heparin and binds to activate bFGF and protects it from inter-cellular enzymes released from damaged cells. This helps in mitosis and angiogenesis. It also increases the thickness of granulation tissues in full thickness wound.
2.Anti-bacteria
Sucralfate exerts anti-bacterial effect by enhancing macrophagic activity at the tissue-infected area through angiogenesis. It ensures increased accumulation of skin macrophages, which engulf the bacteria by phagocytosis.
Sucralfate produces antibacterial activity against P. aeruginosa, Staph. aureus, E.coli, P.mirabilis & Klebsiella are the common wound pathogens.
Due to rapid angiogenesis, there is strong macrophagic activity at wound site due to more blood flow. Hence, more phagocytic activity reduces bacterial overgrowth. Strong angiogenesis enhances the systemic anti-biotic concentration at the wound site. Thus reduces the risk of secondary infection.
3.Anti-inflammatory
Sucralfate provides anti-inflammatory effects at the wound site by preventing the release of 2 important cytokines – interferon gamma and interlukin-2 selectively from the damaged cells.

SUCRALFATE is very useful in the following conditions:
ORAL USE
1. Gastric Ulcer
2. Duodenal Ulcer
3. Erosive Gastritis
4. Aphthous Ulcer
5. NSAID induced Ulcer
6. Stress Ulcer
7. Recurrent Ulcer
8. GERD

TOPICAL USE
1. Post Operative Wound
2. Wound Infection
3. Abrasions and Lacerations
4. Infected Non healing ulcer
5. Decubitus Ulcer
6. Ano-rectal ulcers and post ano-rectal surgeries
7. Boils and Carbuncles
8. Oozing Wet Wound