Colorectal Agents

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October 24 2005 Monday

Soothing Preparations : containing mild astringents, antiseptics or vasoconstrictors can be applied locally as creams, ointments, suppositories or foam to relieve pruritus ani or the pain of haemorrhoids. All should be applied after defaecation and local toilet.

Local anaesthetics of the ester type, but not of the amide type, can produce skin irritation and sensitisation. Steroid enemas are useful for treating proctitis and ulcerative colitis. For proximal disease large volume liquid enemas are appropriate since they provide enhanced retrograde spread throughout the colon. Aerosol foam preparations are more appropriate for distal disease as they tend to be retained in the rectum and sigmoid colon. For Crohn's disease affecting the ileocaecal region, oral budesonide as enteric-coated granules may be taken. Steroid creams reduce excoriation caused by anal leakage.

Aminosalicylates : Sulfasalazine, mesalazine, olsalazine and balsalazide reduce recurrence frequency in ulcerative colitis. Sulfasalazine consists of an active salicylate molecule linked to a sulfapyridine carrier. It should not therefore be prescribed for patients who are sensitive to sulphonamides. Mesalazine does not contain the sulphonamide moiety and may therefore be used to avoid sulphonamide related adverse effects in patients intolerant to sulfasalazine, although its indications are not restricted to this. Balsalazide consists of mesalazine linked to an inert carrier and olsalazine is a dimer of mesalazine.

Different aminosalicylates and their various formulations are not interchangeable and are designed to release active drug at different sites along the colon. Consequently they should be prescribed according to their mode and site of action and the brand name should always be specified. Mesalazine for oral administration should be protected chemically or as a positioned-release formulation to avoid high systemic absorption from the upper GI tract. This control reduces the risk of nephrotoxicity and ensures that therapeutic amounts reach the site of action in the colon. Formulation of mesalazine as an enema or in suppositories avoids such absorption while maintaining high levels of drug in the lower intestine. Balsalazide and olsalazine can also be used in patients intolerant to sulfasalazine. The molecules remain intact until they reach the colon where they are split to release the active drug. Systemic absorption is insignificant and the risks of nephrotoxicity are reduced.

Infliximab is a monoclonal antibody that binds to tumour necrosis factor (TNF-a) inhibiting its inflammatory action in Crohn's disease.

Anti-inflammatory. Heparinoid 0.2%, lauromacrogol-4005 %; oint.

Indications : Haemorrhoids, anal fissure, proctitis, pruritus.

Adults : Apply up to four times daily.

Children : Not recommended.

Also Anacal Suppositories Heparinoid 4mg, lauromacrogol-400 50 mg; 2g

Adults : 1 once or twice daily.

Children : Not recommended.

Soothinglantisepticlsteroid. Pramocaine hydrochlor. 1%, hydrocortisone acetate 0-5%, zinc oxide 12-35%, Peru balsam 1-85%, benzyl benzoate 1 2%, bismuth oxide 0-875%; cream.

Also Anugeslc-Hc Suppos. Pramocaine hydrochlor. 27 mg, hydrocortisone acetate 5 mg, bismuth subgallate 59 mg, zinc oxide 296 mg, Peru balsam 49 mg, benzyl benzoate 33 mg, bismuth oxide 24 mg.

Indications : Internal and external haemorrhoids, pruritus ani.

Adults: 1 suppos. or application of cream night and morning and after defaecation

Children: Not recommended.

Contraindications : Tuberculous, fungal and viral infections.

Special Precautions : Avoid prolonged use. Pregnancy.

Adverse Drug Reactions : Transient burning, sensitivity reactions.

Steroid/antiseptic/astringent.

Hydrocortisone acetate 10 mg, benzyl benzoate 33 mg, bismuth subgallate 59 mg, bismuth oxide 24 mg, balsam peru 49 mg, zinc oxide 296 mg; suppos.

Also ANUSOL HC OINTMENT

Hydrocortisone acetate 025%, benzyl benzoate 1.25%, bismuth subgallate 2.25%, bismuth oxide 0.87%, balsam peru 1.87%, zinc oxide 10.75%.

Indications : Haemorrhoids, pruritus am.

Adults : 1 suppos. or application of oint. night and morning and after defaecation.

Children : Not recommended.

Contraindications : Tuberculous, fungal and viral infections.

Special Precautions : Avoid prolonged use. Pregnancy.

Adverse Drug Reactions : Systemic corticosteroid effects.

Steroidllocal anaesthetic. Hydrocortisone 5 mg, cinchocaine hydrochlor. 5 mg; suppos.

Also OINTMENT Hydrocortisone 0.5%, cinchocaine. hydrochlor.05%.

Indications : Haemorrhoids, inflammation, pruritus ani.

1 suppos. and/or application of oint. morning, night and after defaecation.

Contraindications : Tuberculous, fungal and viral infections.

Special Precautions : Avoid prolonged use. Pregnancy.

Adverse Drug Reactions : Systemic corticosteroid effects.

Local anaestheticlastringent. Lidocaine hydrochlor. 0.65%, zinc oxide 10%, bismuth oxide 2%, cinnamic acid 0.45%, benzoic acid 0.4 %; cream.

Indications : Haemorrhoids.

Adults : Apply morning and night and after bowel movement.

Children : Not recommended.

Aminosalicylate. Mesalazine 400 mg oblong brown e-c tab.

Indications : Mild to moderate ulcerative colitis. Maintenance of remission of ulcerative colitis.

Adults: Acute disease, 6 daily in divided doses. Maintenance, 3-6daily in divided doses.

Children: Not recommended.

Contraindications : Severe renal or severe hepatic impairment, gastric or duodenal ulceration, bleeding tendencies. History of sensitivity to salicylates or renal sensitivity to sulphasalazine.

Special Precautions : Renal impairment, raised blood urea, proteinurea. Monitor renal function and serum creatinlne levels before start of treatment, every 3 months during 1st year, 6 monthly for next 4 years, then annually. Advise patients to report any unexplained bleeding, bruising, sore throat or fever; perform blood test if suspect blood dyscrasia. Elderly. Pregnancy, lactation.

Drug Interactions : NSAIDs, azathioprine, mercaptopurine, digoxin, probenecid, sulfinpyrazone, furosemide, spironolactone, glucocorticoids.

Adverse Drug Reactions : GI upset, headache. Rarely pancreatitis, hepatitis, allergic lung reactions, rash, SLE-like reactions, blood dyscrasias, renal failure, interstitial nephritis, nephrotic syndrome, alopecia, peripheral neuropathy, myocarditis, pericarditis.

Monoclonal antibody. Infliximab 100 mg; powder for conc. for soln. in vial.

Indications : Severe active Crohn's disease or fistulising Crohn's disease in patients unresponsive to corticosteroid and/or immunosuppressant therapy.

Adults: Severe active: 5 mg/kg by i.v. I inf. over 2 hrs. Discontinue if no response within 2 weeks. If patient responds, additional inf. of 5 mg/kg 2 weeks and 6weeks after first inf., then every 8 weeks or 5 mg/kg if symptoms recur. Fistulising: Initially 5 mg/kg by i.v. inf. over 2 hrs. repeated 2 weeks and 6weeks after first inf. Repeat if necessary within 16 weeks of last inf.

Children: Under 17 years, not recommended.

Contraindications : Congestive heart failure. Opportunistic or severe infections such as sepsis, abscesses, tuberculosis. Hypersensitivity to murine proteins.

Pregnancy or lactation during or within 6 months of dose (ensure adequate contraception).

Special Precautions : Monitor for active and latent tuberculosis before and during treatment; re-evaluate therapy if latent tuberculosis is found, stop treatment if active tuberculosis is suspected or until treated. Monitor for acute inf. reactions during or within 2 hrs of dose; if necessary slow rate, interrupt inf. or discontinue. Ensure emergency treatment is available. Monitor for delayed hypersensitivity if patient retreated after prolonged period; do not retreat if interval exceeds 16 weeks. Discontinue if lupus-like symptoms appear or antinuclear antibodies are detected. Elderly, hepatic or renal impairment.

Adverse Drug Reactions : Viral infection, fever, headache, vertigo, dizziness, flushing, upper or lower respiratory tract infection, dyspnoea, sinusitis, GI upset, skin reactions, fatigue, chest pain, abnormal liver function. Report any adverse reaction to CSM.

Steroidllocalanaesthetic. Prednisolone hexanoate 0.19%, cinchocaine hydrochlor. 0.5%; oint.

Indications : Short term symptomatic relief of haemorrhoids, pruritus ani. Apply two to four times daily for up to 5-7 days.

Also SUPPOS.

Prednisolone hexanoate 1-3 mg, cinchocaine hydrochlor. 1 mg. 1 one to three times daily after defaecation.

Clinical Indication : Secondary skin infections.

Special Precaution : Avoid prolonged use. Pregnancy.

Adverse Drug Reaction : Systemic corticosteroid effects.

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