Hydrocortisone Acetate topical

Class: Anti-inflammatory Agents
Note: This monograph also contains information on Hydrocortisone, Hydrocortisone Buteprate, Hydrocortisone Butyrate, Hydrocortisone Valerate
ATC Class: D07BB04
VA Class: OR900
CAS Number: 50-23-7
Brands: Ala-Cort, Ala-Scalpt, Analpram-HC, Anucort-HC, Anu-Med HC, Anusert HC, Anusol-HC, Aquanil HC, Caldecort Anti-Itch, Carmol HC, Cetacort, CortaGel Extra Strength, Cortaid Intensive Therapy, Cortaid Maximum Strength, Cortaid Sensitive Skin Formula, Cortenema, Corticaine, Cortifoam, Cortisporin, Cortizone for Kids, Cortizone, Cortizone External Anal Itch Relief, Cortizone Scalp Itch Formula, Dermacort, Dermarest, DriCort, DermiCort, Dermtex HC, Enzone, Epifoam, Gynecort, Hemorrhoidal-HC, Hemril-HC, HydroSKIN, Hytone, LactiCare-HC, Lanacort, Lazersporin-C, Locoid, Mantadil, Massengill Medicated Soft Cloth Towelette, Nupercainal Hydrocortisone Anti-Itch, Nutracort, Orabase HCA, Pandel, Penecort, Pramosone, Preparation H Hydrocortisone, Proctocort, proctoCream-HC, proctoFoam-HC, Sarnol HC, Scalp-Aid, Scalpcort Maximum Strength, Texacort, Westcort, Zone-A Cream, Zone-A Forte Lotion

Introduction

Corticosteroid secreted by the adrenal cortex; topical anti-inflammatory agent.^a

Uses for Hydrocortisone Acetate

Corticosteroid-responsive Dermatoses

Relief of inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.^b

Nonprescription preparations used for temporary relief of minor skin irritations, itching, and rash caused by eczema, dermatitis, insect bites, poison ivy, poison oak, poison sumac, soaps, detergents, cosmetics, or jewelry.^a

Nonprescription preparations used for temporary relief of itchy anal and/or genital areas.^a

Nonprescription preparations used for temporary relief of itching and minor scalp irritation caused by scalp dermatitis.^a

Generally most effective in acute or chronic dermatoses (e.g., seborrheic or atopic dermatitis, localized neurodermatitis, anogenital pruritus, psoriasis, late phase of allergic contact dermatitis, inflammatory phase of xerosis).^b

Topical therapy generally preferred over systemic therapy; fewer associated adverse systemic effects.^b

Topical therapy generally only controls manifestations of dermatoses; eliminate cause if possible.^b

Topical efficacy may be increased by using a higher concentration or occlusive dressing therapy. (See Administration with Occlusive Dressing under Dosage and Administration.)^b

Response may vary from one topical corticosteroid preparation to another.^b

Anti-inflammatory activity may vary considerably depending on the vehicle, drug concentration, site of application, disease, and individual patient.^b

Infected Dermatoses

Topical treatment of infected dermatoses in combination with topical anti-infectives (e.g., neomycin, polymyxin B) or antifungals.^b

If a topical corticosteroid is used in combination with a topical anti-infective, weigh benefits against risks.^b (See Skin Infection under Cautions.)^b

Oral Lesions

Hydrocortisone acetate paste used as an adjunct for temporary symptomatic relief of oral inflammatory or ulcerative lesions resulting from trauma.^a

Ulcerative Colitis and Anorectal Disorders

Used rectally as a retention enema for adjunctive treatment of mild or moderate acute ulcerative colitis limited to the rectosigmoid or left colon.^b

Used rectally as a retention enema for mild acute ulcerative colitis of the transverse or descending colon.^b

Retention enema usually is effective in mild or moderate acute rectosigmoid ulcerative colitis when response to sulfasalazine (generally considered the maintenance drug of choice) is inadequate or when sulfasalazine cannot be given.^b

Systemic corticosteroids and/or corticosteroid enemas are more effective than sulfasalazine in acute ulcerative colitis attacks, but if surgery is required, it should not be delayed in favor of corticosteroid therapy.^b

Hydrocortisone acetate rectal suppositories or suspension (foam), may be effective as adjunctive treatment of rectal ulcerative colitis.^b

Hydrocortisone acetate rectal suppositories also are used in the treatment of other anorectal inflammatory conditions (e.g., inflamed hemorrhoids, postirradiation or factitial proctitis, cryptitis, pruritus ani).^b

Fixed-combination preparations of a corticosteroid and local anesthetic may be useful for symptomatic relief of anorectal conditions (e.g., hemorrhoids), but combinations with antihistamines, astringents, keratolytics, and/or vasoconstrictors are of questionable efficacy.^b

Hydrocortisone Acetate Dosage and Administration

General

• 
  

  Consider location of the lesion and the condition being treated when choosing a dosage form.^b

  
  


• 
  

  Creams are suitable for most dermatoses,^b but ointments may also provide some occlusion and are usually used for the treatment of dry, scaly lesions.^b

  
  


• 
  

  Lotions are probably best for treatment of weeping eruptions, especially in areas subject to chafing (e.g., axilla, foot, groin).^b Lotions, gels, and aerosols may be used on hairy areas, particularly the scalp.^b

  
  


• 
  

  Formulation affects percutaneous penetration and subsequent activity; extemporaneous preparation or dilution of commercial preparations with another vehicle may decrease effectiveness.^b

  
  


• 
  

  Patients applying a topical corticosteroid to a large surface area and/or to areas under occlusion should be evaluated periodically for evidence of hypothalamic-pituitary-adrenal (HPA)-axis suppression by appropriate endocrine testing (e.g., ACTH stimulation, plasma cortisol, urinary free cortisol).^b (See Hypothalamic-Pituitary-Adrenal Axis Suppresion and also Systemic Effects, under Cautions.)

  
  

Administration

Topical Administration

For dermatologic use only; avoid contact with eyes.^{d e}

Apply creams, lotions, ointments, solutions, and aerosol foams topically to the skin or scalp.^a

Apply paste topically inside the oral cavity.^a

Apply rectal creams and ointments externally to the anal area; some commercially available creams also may be applied externally to the anogenital areas.^a

The area of skin to be treated may be thoroughly cleansed before topical application to reduce the risk of infection; however, some clinicians believe that, unless an occlusive dressing is used, cleansing of the treated area is unnecessary and may be irritating.^b

Apply cream, lotion, ointment, or solution sparingly in a thin film and rub gently into affected area.^a

For scalp dermatoses, part the hair and apply small amount of lotion or solution directly to the affected area; rub gently into scalp.^a Maintain usual hair care, but do not wash out lotion immediately after application.^a Alternatively, for scalp dermatoses, apply aerosol to dry scalp after shampooing.^a

To dispense foam, shake container well (for 5–10 seconds) immediately prior to use.^f Hold container upright and press down on container cap until foam appears.^f Apply a small amount to affected area.^f

For use in the mouth, press a small amount of paste to the lesion without rubbing until a thin film develops.^a

After a favorable response is achieved, frequency of application or concentration (strength) may be decreased to the minimum necessary to maintain control and to avoid relapse; discontinue if possible.^b

Administration with Occlusive Dressing

Occlusive dressings may be used for severe or resistant dermatoses (e.g., psoriasis).^a (See Occlusive Dressings under Cautions.)

Soak or wash the affected area to remove scales; apply a thin film of cream, lotion, or ointment; rub gently into the lesion; and apply another thin film.^b Cover affected area with a thin, pliable plastic film and seal it to adjacent normal skin with adhesive tape or hold in place with a gauze or elastic bandage.^b

If affected area is moist, incompletely seal the edges of the plastic film or puncture the film to allow excess moisture to escape.^b For added moisture in dry lesions, apply cream, ointment, or lotion and cover with a dampened cloth before the plastic film is applied or briefly soak the affected area in water before application of the drug and plastic film.^b

Thin polyethylene gloves may be used on the hands and fingers, plastic garment bags may be used on the trunk or buttocks, a tight shower cap may be used for the scalp, or whole-body suits may be used instead of plastic film to provide occlusion.^b

Frequency of occlusive dressing changes depends on the condition being treated; cleansing of the skin and reapplication of the corticosteroid are essential at each dressing change.^b

Occlusive dressing is usually left in place for 12–24 hours and therapy is repeated as needed.^b Although occlusive dressing may be left in place for 3–4 days at a time in resistant conditions, most clinicians recommend intermittent use of occlusive dressings for 12 hours daily to reduce the risk of adverse effects (particularly infection) and systemic absorption and for greater convenience.^b

The drug and an occlusive dressing may be used at night, and the drug or a bland emollient may be used without an occlusive dressing during the day.^b

In patients with extensive lesions, sequential occlusion of only one portion of the body at a time may be preferable to whole-body occlusion.^b (See Occlusive Dressings under Cautions.)

Rectal Administration

Administer rectally as a retention enema, suppository, or aerosol foam.^a

Administer retention enema, suppository, or foam carefully according to manufacturer’s instructions.^a

Dosage

Available as hydrocortisone (dosage expressed in terms of the base) and as hydrocortisone acetate, buteprate, butyrate, and valerate (dosage expressed in terms of the salt).^a

Pediatric Patients

Administer the least amount of topical preparations that provides effective therapy.^b (See Pediatric Use under Cautions.)

Corticosteroid-responsive Dermatoses

Topical

Nonprescription hydrocortisone preparations should not be used in children <2 years of age unless directed and supervised by a clinician.^b

Children ≥2 years of age: Apply appropriate cream, lotion, ointment, or solution sparingly 1–4 times daily.^a

Adults

Corticosteroid-responsive Dermatoses

Topical

Apply appropriate cream, lotion, ointment, or solution sparingly 1–4 times daily.^a

Apply aerosol foam to affected area 2–4 times daily.^{a f}

Nonprescription preparations should not be used for self-medication for >7 days.^a

If the condition worsens or symptoms persist, discontinue and consult a clinician.^a

Oral Lesions

Topical

Apply a small amount of paste to the lesion 2 or 3 times daily after meals and at bedtime.^a

If substantial regeneration or repair of oral tissues does not occur after 7 days, further investigate etiology of the lesions.^a

Ulcerative Colitis and Anorectal Disorders

Rectal (as Retention Enema)

Adjunctive treatment of ulcerative colitis: 100 mg nightly.^a Some clinicians recommend 100 mg twice daily followed by 100 mg nightly when improvement occurs.^a

Usually given for 21 days or until clinical and proctologic remissions are achieved.^a

Lay on left side during and for 30 minutes after administration to distribute drug throughout the left colon.^a Retain for ≥1 hour, preferably all night.^a

Symptoms may improve in 3–5 days, followed by proctologic improvement.^a Discontinue if clinical or proctologic improvement does not occur within 2–3 weeks.^a

Protologic remission may require 2–3 months of therapy.^a

Following treatment for >21 days, gradually withdraw use; give every other night for 2–3 weeks, then discontinue.^a

Rectal (as Foam)

Ulcerative proctitis of the distal rectum: 90 mg (1 applicatorful of a 10% aerosol foam suspension) 1 or 2 times daily for 2–3 weeks.^{a g} Then, if necessary, every other day until clinical and proctologic improvement.^{a g}

Symptoms may improve within 5–7 days.^{a g}

Rectal (as Suppository)

Adjunctive treatment of ulcerative colitis of the rectum and other inflammatory conditions of the anorectum: 25 mg in the morning and at night for 2 weeks.^a

Severe proctitis: 25 mg 3 times daily or 50 mg twice daily.^a

Adjunctive treatment of postirradiation or factitial proctitis: 25 mg in the morning and at night for 6–8 weeks (or less if an adequate response is attained).^a

For internal hemorrhoid symptoms and adjunctive treatment of other anorectal inflammatory conditions: 10 mg in the morning and at night for 2–6 days.^a

Prescribing Limits

Pediatric Patients

Corticosteroid-responsive Dermatoses

Self-medication

Topical

Maximum 7 days.^a

Adults

Corticosteroid-responsive Dermatoses

Self-medication

Topical

Maximum 7 days.^a

Cautions for Hydrocortisone Acetate

Contraindications

• 
  

  Known hypersensitivity to hydrocortisone or any ingredient in the formulation.^{b d e}

  
  


• 
  

  Rectal corticosteroid therapy in patients with intestinal obstruction, abscess, impending perforation, peritonitis, extensive fistulas, and fresh intestinal anastomoses or sinus tracts.^b

  
  

Warnings/Precautions

Sensitivity Reactions

Allergic contact dermatitis may manifest as failure to heal rather than irritation as occurs with other topical preparations that do not contain corticosteroids; confirm with diagnostic patch testing.^e

General Precautions

Hypothalamic-Pituitary-Adrenal Axis Suppression.

Topically applied corticosteroids can be absorbed in sufficient amounts to reversibly suppress the HPA axis.^b

Perform periodic HPA-axis evaluation by appropriate testing (e.g., ACTH stimulation, morning plasma cortisol, urinary free cortisol), especially in patients applying a topical corticosteroid to a large surface area or to areas under occlusion.^b

If HPA-axis suppression occurs, withdraw the drug, reduce the frequency of application, and/or substitute a less potent corticosteroid.^b

HPA-axis function recovery generally is prompt and complete following drug discontinuance.^b

Rarely, glucocorticosteroid insufficiency may require systemic corticosteroid therapy.^b

Systemic Effects

Systemic absorption following topical administration may result in manifestations of Cushing's syndrome, hyperglycemia, and glucosuria in some patients.^b

Adverse systemic effects may occur when corticosteroids are used on large areas of the body, for prolonged periods of time, with an occlusive dressing, and/or concurrently with other corticosteroid-containing preparations.^b

Infants and children may be more susceptible to adverse systemic effects.^a (See Pediatric Use under Cautions.)

Local Effects

Possible adverse local reactions (e.g., irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, secondary infection, striae, miliaria); may occur more frequently with the use of occlusive dressings, especially with prolonged therapy.^b

Prolonged use of topical corticosteroids may cause atrophy of the epidermis and subcutaneous tissue;^b these effects are most likely to occur (even with short-term use) in intertriginous (e.g., axilla, groin), flexor, and facial areas.^b

If irritation occurs, discontinue drug and initiate appropriate therapy.^b

Skin Infection

If concurrent skin infection is present or develops, initiate appropriate anti-infective therapy.^b If infection does not respond promptly, discontinue topical corticosteroid therapy until the infection has been controlled.^b

When topical corticosteroids and topical anti-infectives are used concomitantly, consider that the corticosteroid may mask clinical signs of bacterial, fungal, or viral infections; prevent recognition of ineffectiveness of the anti-infective; or suppress hypersensitivity reactions to ingredients in the formulation.^{b h} In addition, consider the cautions, precautions, and contraindications associated with the anti-infective.^{b h}

Do not use occlusive dressings in patients with primary skin infection.^b

Some manufacturers state that topical corticosteroids are contraindicated in patients with tuberculosis of the skin, dermatologic fungal infections, and cutaneous or systemic viral infection (including vaccinia and varicella and herpes simplex of the eye or adjacent skin); however, most clinicians believe topical corticosteroids may be used with caution if the infection is treated.^b

Severe Ulcerative Colorectal Disease

Use rectally with caution in severe ulcerative disease and only after adequate proctologic examination; risk of intestinal perforation.^b

Occlusive Dressings

Adverse systemic corticosteroid effects may occur with use of occlusive dressings on large areas of the body and for prolonged periods of time; monitor accordingly.^b (See Hypothalamic-Pituitary-Adrenal Axis Suppression and also Systemic Effects, under Cautions.)

Adverse local reactions may occur more frequently with the use of occlusive dressings, especially with prolonged therapy.^b (See Local Effects under Cautions.)

Do not use occlusive dressings on weeping or exudative lesions.^b

Do not use occlusive dressings in patients with primary skin infection.^b

Remove occlusive dressings covering large areas if body temperature increases; thermal homeostasis may be impaired.^b

Use plastic occlusive material with care to avoid the risk of suffocation.^b

Use of Fixed Combination

When used in fixed combination with other agents, consider the cautions, precautions, and contraindications associated with the concomitant agents.

Specific Populations

Pregnancy

Category C.^c

Lactation

Not known whether topical hydrocortisone is distributed into milk.^b Caution advised if topical hydrocortisone is used.^b

Pediatric Use

Nonprescription hydrocortisone preparations should not be used in children <2 years of age unless directed and supervised by a clinician.^b

Tight-fitting diapers or plastic pants should not be used on a child being treated in the diaper area, since such garments may constitute occlusive dressings.^b

Children are more susceptible to topical corticosteroid-induced HPA-axis suppression and Cushing’s syndrome than mature individuals because of a greater skin surface area-to-body weight ratio,^b especially when topical corticosteroids are applied to >20% of body surface area.^b The risk of adrenal suppression appears to increase with decreasing age.^b (See Systemic Effects under Cautions.)

Manifestations of adrenal suppression in children include linear growth retardation, delayed weight gain, low plasma cortisol concentrations, and lack of response to corticotropin (ACTH) stimulation.^b

Children also are at greater risk of glucocorticoid insufficiency during and/or after withdrawal of treatment.^b

Intracranial hypertension has occurred in children; manifestations include bulging fontanelles, headaches, and bilateral papilledema.^b

Striae has been reported in children treated inappropriately with topical corticosteroids.^b

Topical corticosteroid therapy in children should be limited to the minimum amount necessary for therapeutic efficacy; chronic topical corticosteroid therapy may interfere with growth and development.^b

Common Adverse Effects

Burning, stinging, itching, irritation, dry skin, erythema, folliculitis, hypopigmentation, allergic contact dermatitis, secondary infection.^b

Interactions for Hydrocortisone Acetate

Specific Drugs and Laboratory Tests

Drug or Test	Interaction
Corticosteroids	Potential pharmacologic interaction with other corticosteroid-containing preparationsb
Nitroblue-tetrazolium test for bacterial infection	Concurrent use of corticosteroids reportedly may result in false-negative resultsb

Hydrocortisone Acetate Pharmacokinetics

Absorption

Bioavailability

Percutaneous penetration of corticosteroids following topical application to the skin varies among individuals and may be increased by occlusive dressings, high corticosteroid concentrations, and certain vehicles.^b

Only minimal amounts of topical corticosteroid reach the dermis and subsequently the systemic circulation after application to most normal skin areas; more absorption occurs from the scrotum, axilla, eyelid, face, and scalp than from the forearm, knee, elbow, palm, and sole.^b

Absorption is markedly increased by loss of the skin’s keratin layer and by inflammation and/or diseases of the epidermal barrier (e.g., psoriasis, eczema).^b

Occlusive dressings used with hydrocortisone for 96 hours substantially enhance percutaneous penetration;^b occlusive dressings used for up to 24 hours do not appear to alter penetration.^b

In healthy individuals, up to 30–90% of hydrocortisone administered rectally as a retention enema may be absorbed.^b Greater amounts of hydrocortisone may be absorbed if the intestinal mucosa is inflamed.^b

Distribution

Extent

Not known whether topical hydrocortisone is distributed into milk.^b

Elimination

Metabolism

Once absorbed through the skin, topically applied corticosteroids are metabolized primarily in the liver.^b

Elimination Route

Topical corticosteroids and metabolites are excreted by the kidneys and, to a lesser extent, in the bile.^b

Stability

Storage

Topical

Creams, Lotions, Ointments, Solutions, Aerosol Foams

Room temperature; consult product information for specific recommendations.

Rectal

Creams, Suspensions for Retention Enemas, Aerosol Foams, Suppositories

Room temperature; consult product information for specific recommendations.

ActionsActions

• 
  

  Produces anti-inflammatory, antipruritic, and vasoconstrictor actions, possibly resulting in part from steroid receptor binding.^b

  
  


• 
  

  Precise mechanism of action for topical anti-inflammatory activity is unknown; therapeutic benefit in the management of corticosteroid-responsive dermatoses mediated primarily through anti-inflammatory, antipruritic, and vasoconstrictive actions.^{b d e}

  
  


• 
  

  Anti-inflammatory effects may occur through induction of phospholipase A₂ inhibitory proteins (lipocortins); decreased arachidonic acid release from membrane phospholipids.^e Decreased arachidionic acid precursors may downregulate biosynthesis of potent inflammatory mediators (e.g., prostaglandins, leukotrienes).^e

  
  


• 
  

  Decreases inflammation by stabilizing leukocyte lysosomal membranes, preventing release of destructive acid hydrolases from leukocytes; inhibiting macrophage accumulation in inflamed areas; reducing leukocyte adhesion to capillary endothelium; reducing capillary wall permeability and edema formation; decreasing complement components; antagonizing histamine activity and release of kinin from substrates; reducing fibroblast proliferation, collagen deposition, and subsequent scar tissue formation; and possibly by other mechanisms as yet unknown.^b

  
  

Advice to Patients

• 
  

  Importance of using only as directed, only for the disorder for which it was prescribed, and for no longer than prescribed;^b avoid contact with the eyes.^{d e} (See Topical Administration under Dosage and Administration.)

  
  


• 
  

  Importance of informing patients that treated areas of the skin should not be bandaged or otherwise covered or wrapped as to be occlusive unless directed by a clinician.^b

  
  


• 
  

  Importance of informing parents of children receiving the drug that if hydrocortisone is applied in the diaper area, tight-fitting diapers or plastic pants should not be used since they may act as an occlusive dressing.^b

  
  


• 
  

  Importance of reporting any local adverse reactions, especially those occurring under occlusive dressings, to a clinician.^b

  
  


• 
  

  Potential for hydrocortisone acetate suppositories to stain fabric; take appropriate precautionary measures.^b

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs; other corticosteroid-containing preparations should not be used without first consulting with clinician.^c

  
  


• 
  

  Importance of women informing clinician if they are or plan to become pregnant or plan to breast-feed.^b

  
  


• 
  

  Importance of informing patients of other important precautionary information. (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Hydrocortisone

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Bulk	Powder*
Rectal	Cream	1%	Proctocort (with benzyl alcohol and propylene glycol)	Monarch
	Suspension	100 mg/60 mL	Cortenema (with methylparaben)	Solvay
			Hydrocortisone Enema	Copley
Topical	Cream	0.5%*	Cortizone-5 (with aloe and parabens)	Pfizer
			Cortizone for Kids (with aloe and parabens)	Pfizer
		1%*	Ala-Cort	Del-Ray
			Cortaid Intensive Therapy (with parabens and propylene glycol)	Pfizer
			Cortizone-10 (with aloe and parabens)	Pfizer
			Cortizone-10 External Anal Itch Relief Creme (with aloe and parabens)	Pfizer
			Dermacort	Solvay
			DermiCort	Republic
			HydroSKIN	Rugby
			Hytone (with propylene glycol)	Dermik
			Penecort (with benzyl alcohol and propylene glycol)	Allergan
			Preparation H Hydrocortisone (with parabens and propylene glycol)	Wyeth
		2.5%*	Anusol-HC (with benzyl alcohol and propylene glycol)	Pfizer
			Hytone (with propylene glycol)	Dermik
	Gel	1%	CortaGel Extra Strength	Norstar
	Lotion	0.5%*	HydroSKIN	Rugby
		1%*	Ala-Cort	Del-Ray
			Aquanil HC (with benzyl alcohol)	Person & Covey
			Cetacort (with parabens)	Healthpoint
			Dermacort (with benzyl alcohol)	Solvay
			HydroSKIN	Rugby
			LactiCare-HC	Stiefel
			Nutracort (with parabens)	Healthpoint
			Sarnol HC	Stiefel
		2%	Ala-Scalpt	Del-Ray
		2.5%	Hydrocortisone Lotion	Glades, Major
			Hytone (with propylene glycol)	Dermik
			LactiCare-HC	Stiefel
			Nutracort (with parabens)	Healthpoint
			ProctoCream-HC (with benzyl alcohol)	Physicians Total Care
	Ointment	0.5%*	Cortizone-5	Pfizer
		1%*	Cortizone-10	Pfizer
			HydroSKIN	Rugby
		2.5%*	Hytone	Dermik
	Pledgets (saturated with solution)	0.5%	Massengill Medicated Soft Cloth Towelette (with parabens and propylene glycol)	GlaxoSmithKline
	Solution	1%	Cortaid FastStick Maximum Strength (with alcohol and methylparaben)	Pfizer
			Cortaid Spray Maximum Strength (with alcohol and methylparaben)	Pfizer
			Cortizone-10 Scalp Itch Formula Liquid (with alcohol SD 40-2 60% v/v, benzyl alcohol, and propylene glycol)	Pfizer
			Penecort (with alcohol SD 40-2 57%, benzyl alcohol, and propylene glycol)	Allergan
			Texacort (with SD alcohol 33% and propylene glycol)	Sirius
		2.5%	Texacort	Sirius

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Hydrocortisone Combinations

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Topical	Ointment	1% with Bacitracin Zinc 400 units (of bacitracin) per g, Neomycin Sulfate 0.5% (0.35% of neomycin), and Polymyxin B Sulfate 5000 units (of polymyxin B) per g	Cortisporin	Monarch
		1% with Neomycin Sulfate 0.5% (0.35% of neomycin)*
	Solution	1% with Neomycin Sulfate 0.5% (0.35% of neomycin), and Polymyxin B Sulfate 10,000 units (of polymyxin B) per g	Lazersporin-C (with propylene glycol)	Pedinol

Hydrocortisone is also commercially available in combination with antihistamines, astringents, keratolytics, local anesthetics, and vasoconstrictors.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Hydrocortisone Acetate

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Bulk	Powder*
Rectal	Aerosol, foam suspension	10%	Cortifoam (with parabens, propylene glycol, and chlorofluorohydrocarbon propellants)	Schwarz
	Suppositories	25 mg	Anucort-HC	G&W
			Anu-Med HC	Major
			Anusol-HC	Pfizer
			Hemorrhoidal-HC	Alpharma, CMC, Sandoz, Rugby, UDL
			Hemril-HC Uniserts	Upsher-Smith
			Hydrocortisone Acetate Suppositories	IVAX, Paddock, UDL, United Research
		30 mg	Proctocort	Monarch
Topical	Cream	0.5%	Corticaine (with parabens)	UCB
		0.5% (of hydrocortisone)*	Cortaid Sensitive Skin Formula (with aloe and parabens)	Pfizer
		1% (of hydrocortisone)	Caldecort Anti-Itch (with propylene glycol)	Novartis
			Cortaid Maximum Strength (with aloe and methylparaben)	Pfizer
			Dermarest DriCort	Del
			Dermtex HC (with menthol 1%)	Pfeiffer
			Nupercainal Hydrocortisone Anti-Itch Cream (with propylene glycol)	Novartis
	Lotion	0.5% (of hydrocortisone)*
	Ointment	0.5% (of hydrocortisone)	Cortaid Sensitive Skin Formula (with aloe and parabens)	Pfizer
		1%	Anusert HC-1	G&W
			Gynecort 10	Combe
			Lanacort 10	Combe
		1% (of hydrocortisone)	Anusol-HC-1	Pfizer
			Cortaid Maximum Strength (with aloe and methylparaben)	Pfizer
	Paste	0.5%	Orabase HCA	Colgate
	Solution	1%	Scalp-Aid	Major
			Scalpcort Maximum Strength	Clay-Park
		1% (of hydrocortisone)	Dermtex HC Spray	Pfeiffer

Hydrocortisone Acetate Combinations

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Rectal	Aerosol, foam suspension	1% with Pramoxine Hydrochloride 1%	proctoFoam-HC (with parabens, propylene glycol, and chlorofluorohydrocarbon propellants)	Schwarz
Topical	Aerosol, foam suspension	1% with Pramoxine Hydrochloride 1%	Epifoam (with parabens, propylene glycol, and hydrocarbon propellants)	Schwarz
	Cream	0.5% with Chlorcyclizine Hydrochloride 2%	Mantadil (with methylparaben)	GlaxoSmithKline
		0.5% with Neomycin Sulfate 0.5% (0.35% of neomycin) and Polymyxin B Sulfate 10,000 units (of polymyxin B) per g	Cortisporin (with methylparaben and propylene glycol)	Monarch
		1% with Pramoxine Hydrochloride 1%	Analpram-HC (with propylene glycol)	Ferndale
			Enzone (with propylene glycol)	Forest
			Pramosone (with propylene glycol)	Ferndale
			proctoCream-HC (with propylene glycol)	Schwarz
			Zone-A Cream (with propylene glycol)	Forest
		1% with Urea 10%	Carmol HC (with propylene glycol and sodium metabisulfite)	Doak
		2.5% with Pramoxine Hydrochloride 1%	Analpram-HC (with propylene glycol)	Ferndale
			Pramosone (with propylene glycol)	Ferndale
	Lotion	1% with Pramoxine Hydrochloride 1%	Pramosone (with povidone)	Ferndale
			Zone-A Lotion (with povidone)	Forest
		2.5% with Pramoxine Hydrochloride 1%	Pramosone (with povidone)	Ferndale
			Zone-A Forte Lotion (with povidone)	Forest
	Ointment	1% with Pramoxine Hydrochloride 1%	Pramosone	Ferndale
		2.5% with Pramoxine Hydrochloride 1%	Pramosone	Ferndale

Hydrocortisone acetate is also commercially available in combination with antihistamines, astringents, keratolytics, local anesthetics, and vasoconstrictors.

Hydrocortisone Buteprate

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Topical	Cream	0.1%	Pandel (with parabens and propylene glycol)	Savage

Hydrocortisone Butyrate

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Topical	Cream	0.1%	Locoid (with methylparaben)	Ferndale
	Ointment	0.1%	Locoid	Ferndale
	Solution	0.1%	Locoid (with isopropyl alcohol 50% and povidone)	Ferndale

Hydrocortisone Valerate

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Topical	Cream	0.2%	Westcort (with propylene glycol)	Westwood-Squibb
	Ointment	0.2%	Westcort (with propylene glycol)	Westwood-Squibb

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 05/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Analpram-HC 1-1% Cream (FERNDALE LAB): 30/$91.99 or 90/$255.96

Analpram-HC 1-2.5% Cream (FERNDALE LAB): 30/$91.41 or 90/$261

Analpram-HC 1-2.5% Lotion (FERNDALE LAB): 59/$105.99 or 177/$295.98

Analpram-HC Singles 1-2.5% Cream (FERNDALE LAB): 120/$219 or 360/$615.98

Carmol-HC 1-10% Cream (PHARMADERM): 85/$210 or 255/$605.78

Cortisporin 0.5-0.5-10000 Cream (MONARCH PHARMACEUTICALS): 7/$54.99 or 22/$164.97

Hydrocortisone 0.5% Cream (FOUGERA): 28/$13.99 or 85/$19.97

Hydrocortisone 1% Cream (FOUGERA): 28/$16.99 or 85/$35.97

Hydrocortisone 1% Lotion (FOUGERA): 118/$13.99 or 236/$22.98

Hydrocortisone 1% Lotion (PERRIGO): 118/$15.99 or 236/$22.98

Hydrocortisone 2.5% Cream (FOUGERA): 30/$13.99 or 90/$41.97

Hydrocortisone 2.5% Lotion (PERRIGO PHARMACEUTICALS): 59/$39.99 or 177/$109.96

Hydrocortisone 2.5% Ointment (FOUGERA): 28/$14.99 or 8

Durabac Forte

Pronunciation: ah-seet-ah-MIN-oh-fen/ka-FEEN/mag-NEE-zhum sa-LI-si-late/fen-ill-tole-OX-a-meen
Generic Name: Acetaminophen/Caffeine/Magnesium Salicylate/Phenyltoloxamine
Brand Name: Durabac Forte

Durabac Forte is used for:

Treating mild to moderate aches and pains associated with headache, muscle and joint soreness, muscle spasms, nerve pain, menstrual cramps, colds and flu, sinusitis, toothache, and minor pain from arthritis. It helps restore mental alertness or wakefulness during periods of fatigue or drowsiness. It may also be used for other conditions as determined by your doctor.

Durabac Forte is an analgesic, antipyretic, salicylate, antihistamine, and stimulant combination. It works by decreasing fever, pain, and inflammation. It also blocks histamine, which causes allergy symptoms (eg, sneezing and itchy, watery eyes).

Do NOT use Durabac Forte if:

• you are allergic to any ingredient in Durabac Forte


• you are allergic to salicylates (eg, aspirin) or NSAIDs (eg, ibuprofen)


• you have kidney or liver problems, bleeding problems (eg, hemophilia, active severe bleeding), low blood platelet levels, or Von Willebrand disease


• the patient is a child or teenager who has flu symptoms or chickenpox


• you are also taking an anticoagulant (eg, warfarin) or sodium oxybate (GHB)

Contact your doctor or health care provider right away if any of these apply to you.

Before using Durabac Forte:

Some medical conditions may interact with Durabac Forte. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

• if you are pregnant, planning to become pregnant, or are breast-feeding


• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement


• if you have allergies to medicines, foods, or other substances


• if you have breathing problems (eg, asthma), blood clotting problems, stomach or intestinal problems (eg, ulcer, blockage, inflammation), prostate problems, urinary blockage, trouble urinating, increased pressure in the eyes (eg, glaucoma), heart or blood vessel problems, high blood pressure, viral hepatitis, anxiety, trouble sleeping, growths in the nose, low blood vitamin K levels, influenza, or chickenpox


• if the patient is a child who has a history of stroke, a bulging blood vessel in the brain (aneurysm), an inflammatory condition (rheumatic disease), or Kawasaki syndrome


• if you have taken furazolidone or a monamine oxidase (MAO) inhibitor (eg, phenelzine) within the past 14 days

Some MEDICINES MAY INTERACT with Durabac Forte. Tell your health care provider if you are taking any other medicines, especially any of the following:

• Carbonic anhydrase inhibitors (eg, acetazolamide), insulin, meglitinides (eg, nateglinide), sodium oxybate (GHB), sympathomimetics (eg, albuterol, pseudoephedrine), theophyllines (eg, aminophylline), or valproic acid because the risk of their side effects may be increased by Durabac Forte


• Anticoagulants (eg, warfarin) because the risk of bruising or bleeding may be increased


• Barbiturates (eg, phenobarbital) because they may decrease Durabac Forte's effectiveness


• Medicines that may harm the liver (eg, acetaminophen, methotrexate, ketoconazole, isoniazid, certain medicines for HIV infection) because the risk of liver side effects may be increased. Ask your doctor if you are unsure if any of your medicines might harm the liver.


• Furazolidone, isoniazid, MAO inhibitors (eg, phenelzine), or quinolone antibiotics (eg, ciprofloxacin) because they may increase the risk of Durabac Forte's side effects


• Angiotensin-converting enzyme (ACE) inhibitors (eg, enalapril), aspirin, probenecid, or sulfinpyrazone because their effectiveness may be decreased by Durabac Forte

This may not be a complete list of all interactions that may occur. Ask your health care provider if Durabac Forte may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Durabac Forte:

Use Durabac Forte as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Take Durabac Forte by mouth with or without food. If stomach upset occurs, take with food to reduce stomach irritation.


• If you miss a dose of Durabac Forte and you are using it regularly, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Durabac Forte.

Important safety information:

• Durabac Forte may cause drowsiness, dizziness, or blurred vision. These effects may be worse if you take it with alcohol or certain medicines. Use Durabac Forte with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.


• Do not drink alcohol or use medicines that may cause drowsiness (eg, sleep aids, muscle relaxers) while you are using Durabac Forte; it may add to their effects. Ask your pharmacist if you have questions about which medicines may cause drowsiness.


• Durabac Forte may harm your liver. Your risk may be greater if you drink alcohol while you are using Durabac Forte. Talk to your doctor before you take Durabac Forte or other fever reducers if you drink more than 3 drinks with alcohol per day.


• Durabac Forte has a salicylate in it. Before you start any new medicine, check the label to see if it has a salicylate in it too. If it does or if you are not sure, check with your doctor or pharmacist.


• Durabac Forte has acetaminophen in it. Before you start any new medicine, check the label to see if it has acetaminophen in it too. If it does or if you are not sure, check with your doctor or pharmacist.


• Do NOT take more than the recommended dose or use for longer than prescribed without checking with your doctor.


• Avoid large amounts of food or drink that have caffeine (eg, coffee, tea, cocoa, cola, chocolate).


• Diabetes patients - Durabac Forte may affect your blood sugar. Check blood sugar levels closely. Ask your doctor before you change the dose of your diabetes medicine.


• If you are taking Durabac Forte for pain and your symptoms do not improve within 10 days or if they become worse or if redness is present, check with your doctor.


• Tell your doctor or dentist that you take Durabac Forte before you receive any medical or dental care, emergency care, or surgery.


• Durabac Forte has a salicylate in it, which has been linked to a serious illness called Reye syndrome. Do not give Durabac Forte to a child or teenager who has the flu, chickenpox, or a viral infection. Contact your doctor with any questions or concerns.


• Durabac Forte may interfere with certain lab tests. Be sure your doctor and lab personnel know you are taking Durabac Forte.


• Use Durabac Forte with caution in the ELDERLY; they may be more sensitive to its effects, especially anemia or liver or kidney problems.


• Durabac Forte should be used with extreme caution in CHILDREN younger than 12 years old; safety and effectiveness in these children have not been confirmed.


• PREGNANCY and BREAST-FEEDING: It is not known if Durabac Forte can cause harm to the fetus. If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Durabac Forte while you are pregnant. Durabac Forte is found in breast milk. Do not breast-feed while taking Durabac Forte.

Possible side effects of Durabac Forte:

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

Anxiety; blurred vision; diarrhea; dizziness; drowsiness; dry mouth, nose, or throat; fast heartbeat; headache; heartburn; irritability; loss of appetite; nausea; nervousness; thickening of mucus in the nose and throat; trouble sleeping; upset stomach; vomiting.

Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); bloody or black stools; confusion; dark urine or pale stools; decreased coordination; decreased urination; difficulty swallowing; fainting; fever, chills, persistent sore throat, or other signs of infection; hearing loss; hoarseness; irregular heartbeat; muscle weakness; ringing in the ears; seizures; severe or persistent heartburn; severe, persistent, or recurring fast heartbeat; severe stomach pain; severe vomiting; shortness of breath; tremors; unusual bruising or bleeding; unusual tiredness; vomit that looks like coffee grounds; yellowing of the skin or eyes.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

See also: Durabac Forte side effects (in more detail)

If OVERDOSE is suspected:

Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Symptoms may include abnormal behavior; confusion; dark urine; delirium; difficulty hearing; excessive sweating; extreme tiredness; fast or deep breathing; loss of consciousness; ringing in the ears; seizures; severe or persistent dizziness, nausea, or vomiting; stomach pain; yellowing of the skin or eyes.

Proper storage of Durabac Forte:

Store Durabac Forte at room temperature, between 59 and 86 degrees F (15 and 30 degrees C). Store away from heat, moisture, and light. Do not store in the bathroom. Keep Durabac Forte out of the reach of children and away from pets.

General information:

• If you have any questions about Durabac Forte, please talk with your doctor, pharmacist, or other health care provider.


• Durabac Forte is to be used only by the patient for whom it is prescribed. Do not share it with other people.


• If your symptoms do not improve or if they become worse, check with your doctor.


• Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Durabac Forte. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Durabac Forte resources

• Durabac Forte Side Effects (in more detail)
• Durabac Forte Use in Pregnancy & Breastfeeding
• Durabac Forte Drug Interactions
• Durabac Forte Support Group
• 0 Reviews for Durabac Forte - Add your own review/rating

Compare Durabac Forte with other medications

• Pain

Salofalk 1000mg gastro-resistant prolonged release granules

1. Name Of The Medicinal Product

Salofalk 1000mg gastro-resistant prolonged release granules

2. Qualitative And Quantitative Composition

Each sachet of Salofalk 1000mg granules contains 1000 mg mesalazine.

Excipient:

Each sachet of Salofalk 1000mg granules contains 2.0 mg aspartame.

For a full list of excipients, see section 6.1.

3. Pharmaceutical Form

Gastro-resistant prolonged release granules.

Description: Stick-formed or round, greyish white granules.

4. Clinical Particulars

4.1 Therapeutic Indications

For the treatment of acute episodes and the maintenance of remission of ulcerative colitis.

4.2 Posology And Method Of Administration

Adults and elderly:

For the treatment of acute episodes of ulcerative colitis:

Once daily 1 or 2 sachets of Salofalk 1.5g granules or 3 sachets of Salofalk 1000mg granules or 3 sachets of Salofalk 500mg granules (equivalent to 1.5 – 3.0 g mesalazine daily) preferably to be taken in the morning according to the individual clinical requirement.

It is also possible to take the prescribed daily dose in three divided doses (1 sachet of Salofalk 500mg granules three times daily, or 1 sachet of Salofalk 1000mg granules three times daily), if this is more convenient to the patient.

For the maintenance of remission of ulcerative colitis:

1 sachet of Salofalk 500mg granules three times daily (equivalent to 1.5 g mesalazine daily).

Children:

There is only limited documentation for an effect in children (age 6-18 years).

Children 6 years of age and older:

Active disease: To be determined individually, starting with 30-50 mg/kg/day once daily preferably in the morning or in divided doses. Maximum dose: 75 mg/kg/day. The total dose should not exceed the maximum adult dose.

Maintenance treatment: To be determined individually, starting with 15-30 mg/kg/day in divided doses. The total dose should not exceed the recommended adult dose.

It is generally recommended that half the adult dose may be given to children up to a body weight of 40 kg; and the normal adult dose to those above 40 kg.

All patients:

The contents of the sachets of Salofalk granules should not be chewed. The granules should be taken on the tongue and swallowed, without chewing, with plenty of liquid.

Both in the treatment of acute inflammatory episodes and during long term treatment, Salofalk granules should be used on a regular basis and consistently in order to achieve the desired therapeutic effects.

In general, an acute episode of ulcerative colitis subsides after 8-12 weeks; the dosage can then, in most patients, be reduced to the maintenance dose.

4.3 Contraindications

Salofalk granules are contra-indicated in cases of:

• Pre-existing hypersensitivity to salicylic acid and its derivatives or to any of the other constituents.

• Severe impairment of hepatic and renal function.

4.4 Special Warnings And Precautions For Use

Blood tests (differential blood count; liver function parameters like ALT or AST; serum creatinine) and urinary status (dip sticks) should be determined prior to and during treatment, at the discretion of the treating physician. As a guideline, controls are recommended 14 days after commencement of treatment, then a further two to three times at intervals of 4 weeks.

If the findings are normal, control examinations should be carried out every 3 months. If additional symptoms occur, control examinations should be performed immediately.

Caution is recommended in patients with impaired hepatic function.

Salofalk granules are not recommended in patients with impaired renal function.

Mesalazine-induced renal toxicity should be considered if renal function deteriorates during treatment.

Patients with pulmonary disease, in particular asthma, should be very carefully monitored during a course of treatment with Salofalk granules.

Patients with a history of adverse drug reactions to preparations containing sulfasalazine should be kept under close medical surveillance on commencement of a course of treatment with Salofalk granules. Should Salofalk granules cause acute intolerability reactions such as cramps, acute abdominal pain, fever, severe headache and rash, therapy should be discontinued immediately.

In patients with phenylketonuria it should be kept in mind that Salofalk 1000mg granules contain aspartame as a sweetening agent, equivalent to 1.12 mg phenylalanine.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

Specific interaction studies have not been performed.

Interactions may occur during treatment with Salofalk granules and concomitant administration of the following medicinal products. Most of these possible interactions are based on theoretical reasons:

- Coumarin-type anticoagulants:

possible potentiation of the anticoagulant effects (increasing the risk of gastrointestinal haemorrhage)

- Glucocorticoids:

possible increase in undesirable gastric effects

- Sulphonylureas:

possible increase in the blood glucose-lowering effects

- Methotrexate:

possible increase in the toxic potential of methotrexate

- Probenecid/sulphinpyrazone:

possible attenuation of the uricosuric effects

- Spironolactone/frusemide:

possible attenuation of the diuretic effects

- Rifampicin:

possible attenuation of the tuberculostatic effects

- Lactulose or similar preparations, which lower stool pH:

possible reduction of mesalazine release from granules due to decreased pH caused by bacterial metabolism

In patients who are concomitantly treated with azathioprine or 6-mercaptopurine, possible enhanced myelosuppressive effects of azathioprine or 6-mercaptopurine should be taken into account.

4.6 Pregnancy And Lactation

There are no adequate data from the use of Salofalk granules in pregnant woman. However, data on a limited number of exposed pregnancies indicate no adverse effect of mesalazine on pregnancy or on the health of the foetus/newborn child. To date no other relevant epidemiologic data are available. In one single case after long-term use of a high dose mesalazine (2-4 g, orally) during pregnancy, renal failure in a neonate was reported.

Animal studies on oral mesalazine do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development.

Salofalk granules should only be used during pregnancy if the potential benefit outweighs the possible risk.

N-acetyl-5-aminosalicylic acid and to a lesser degree mesalazine are excreted in breast milk. Only limited experience during lactation in women is available to date. Hypersensitivity reactions like diarrhoea can not be excluded. Therefore, Salofalk granules should only be used during breast-feeding if the potential benefit outweighs the possible risk. If the suckling neonate develops diarrhoea, the breast-feeding should be discontinued.

4.7 Effects On Ability To Drive And Use Machines

No effects on ability to drive and use machines have been observed.

4.8 Undesirable Effects

system organ class	frequency due to MedDRA convention
	rare (	very rare (< 1/ 10,000)
Blood and lymphatic system disorders		Altered blood counts (aplastic anaemia, agranulocytosis, pancytopenia, neutropenia, leukopenia, thrombocytopenia)
Nervous system disorders	Headache, dizziness	peripheral neuropathy
Gastrointestinal disorders	Abdominal pain, diarrhoea, flatulence, nausea, vomiting
Renal and urinary disorders		Impairment of renal function including acute and chronic interstitial nephritis and renal insufficiency
Skin and subcutaneous tissue disorders		Alopecia
Musculoskeletal and connective tissue disorders		Myalgia, arthralgia
Immune system disorders		Hypersensitivity reactions such as allergic exanthema, drug fever, bronchospasm, peri- and myocarditis, acute pancreatitis, allergic alveolitis, lupus erythematosus syndrome, pancolitis
Hepatobiliary disorders		Changes in hepatic function parameters (increase in transaminases and parameters of cholestasis), hepatitis, cholestatic hepatitis
Reproductive system disorders		Oligospermia (reversible)

4.9 Overdose

No cases of intoxication have been reported to date and no specific antidotes are known.

If necessary, intravenous infusion of electrolytes (forced diuresis) should be considered in cases of overdose.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

Pharmacotherapeutic group: Intestinal ant-inflammatory agent

ATC code: A07EC02

The mechanism of the anti-inflammatory action is unknown. The results of in vitro studies indicate that inhibition of lipoxygenase may play a role.

Effects on prostaglandin concentrations in the intestinal mucosa have also been demonstrated. Mesalazine (5-aminosalicylic acid / 5-ASA) may also function as a radical scavenger of reactive oxygen compounds.

Mesalazine, orally administered, acts predominantly locally at the gut mucosa and in the submucous tissue from the luminal side of the intestine. It is important, therefore, that mesalazine is available at the regions of inflammation. Systemic bioavailability/plasma concentrations of mesalazine therefore are of no relevance for therapeutic efficacy, but rather a factor for safety. In order to realise this, Salofalk granules are gastric juice resistant and release mesalazine in a pH dependent manner due to an Eudragit L coating, and prolonged manner due to the matrix granule structure.

5.2 Pharmacokinetic Properties

General considerations of mesalazine:

Absorption:

Mesalazine absorption is highest in proximal gut regions and lowest in distal gut areas.

Biotransformation:

Mesalazine is metabolised both pre-systemically by the intestinal mucosa and the liver to the pharmacologically inactive N-acetyl-5-aminosalicylic acid (N-Ac-5-ASA). The acetylation seems to be independent of the acetylator phenotype of the patient. Some acetylation also occurs through the action of colonic bacteria. Protein binding of mesalazine and N-Ac-5-ASA is 43 % and 78 %, respectively.

Elimination:

Mesalazine and its metabolite N-Ac-5-ASA are eliminated via the faeces (major part), renally (varies between 20 and 50 %, dependent on kind of application, pharmaceutical preparation and route of mesalazine release, respectively), and biliary (minor part). Renal excretion predominantly occurs as N-Ac-5-ASA. About 1 % of total orally administered mesalazine dose is excreted into the breast milk mainly as N-Ac-5-ASA.

Salofalk Granules specific:

Distribution:

Owing to the granule size of about 1 mm, transit from the stomach to the small intestine is fast.

A combined pharmacoscintigraphic/pharmacokinetic study showed that the compound reaches the ileocaecal region within approx. 3 hours and the ascending colon within approx. 4 hours. The total transit time in the colon amounts to about 20 hours. Approximately 80 % of an administered oral dose is estimated to be available in the colon, sigmoid and rectum.

Absorption:

Mesalazine release from Salofalk granules starts after a lag phase of about 2-3 hours, peak plasma concentrations are reached at about 4-5 hours. The systemic bioavailability of mesalazine after oral administration is estimated to be approximately 15-25 %.

Food intake delays absorption for 1 to 2 hours but does not change the rate and extent of absorption.

Elimination:

From a 3 x 500 mg daily mesalazine dose, a total renal elimination of mesalazine and N-Ac-5-ASA under steady state condition was calculated to be about 25 %. The unmetabolised excreted mesalazine part was less than 1 % of the oral dose. The elimination half-life in this study was 4.4 hours.

5.3 Preclinical Safety Data

Preclinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, genotoxicity, carcinogenicity (rat) or toxicity to reproduction.

Kidney toxicity (renal papillary necrosis and epithelial damage in the proximal convoluted tubule or the whole nephron) has been seen in repeat-dose toxicity studies with high oral doses of mesalazine. The clinical relevance of this finding is unknown.

6. Pharmaceutical Particulars

6.1 List Of Excipients

Aspartame (E 951)

Carmellose sodium

Cellulose, microcrystalline

Citric acid, anhydrous

Silica, colloidal anhydrous

Hypromellose

Magnesium stearate

Methacrylic acid-methyl methacrylate copolymer (1:1) (Eudragit L 100)

Methylcellulose

Polyacrylate dispersion 40 per cent (Eudragit NE 40 D containing 2 per cent Nonoxynol 100)

Povidone K 25

Simeticone

Sorbic acid

Talc

Titanium dioxide (E 171)

Triethyl citrate

Vanilla custard flavouring (containing propylene glycol)

6.2 Incompatibilities

Not applicable.

6.3 Shelf Life

4 years.

6.4 Special Precautions For Storage

No special precautions for storage.

6.5 Nature And Contents Of Container

Container: Polyester/Aluminium/Polyethylene-Foil

Package sizes: 20 sachets, 50 sachets, 60 sachets, 100 sachets or 150 sachets Salofalk 1000mg granules

Not all package sizes may be marketed.

6.6 Special Precautions For Disposal And Other Handling

No special requirements.

7. Marketing Authorisation Holder

Dr. Falk Pharma GmbH

Leinenweberstr. 5

79108 Freiburg

Germany

Tel: +49 (0)761 1514-0

8. Marketing Authorisation Number(S)

PL08637/0008 (1000mg)

9. Date Of First Authorisation/Renewal Of The Authorisation

Date of first authorisation: 15 October 2001

Date of last renewal: 1 March 2007

10. Date Of Revision Of The Text

August 2010

Naproxen-Mepha

Naproxen-Mepha may be available in the countries listed below.

Ingredient matches for Naproxen-Mepha

Naproxen

Naproxen is reported as an ingredient of Naproxen-Mepha in the following countries:

• Switzerland

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Finasterida Generis

Finasterida Generis may be available in the countries listed below.

Ingredient matches for Finasterida Generis

Finasteride

Finasteride is reported as an ingredient of Finasterida Generis in the following countries:

• Portugal

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Cloxacilina Normon

Cloxacilina Normon may be available in the countries listed below.

Ingredient matches for Cloxacilina Normon

Cloxacillin

Cloxacillin sodium salt (a derivative of Cloxacillin) is reported as an ingredient of Cloxacilina Normon in the following countries:

• Spain

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Coral

In the US, Coral (coral systemic).

US matches:

• Coral

Ingredient matches for Coral

Diclofenac

Diclofenac sodium salt (a derivative of Diclofenac) is reported as an ingredient of Coral in the following countries:

• Mexico

Nifedipine

Nifedipine is reported as an ingredient of Coral in the following countries:

• Italy

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