Topical Steroids

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  • Created by: LBCW0502
  • Created on: 19-01-20 12:42
Give examples of the preparations of non-oral and non-systemic steroids
Skin creams, ointments, liquids, lotions, gels, eye/ear/nose preparations, scalp applications, suppositories, foams, patches, vaginal rings, inhalers
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What are the uses of topical corticosteroids?
Used in the treatment of inflammatory dermatological conditions e.g. eczema, dermatitis, psoriasis, insect bite/sting reactions, otitis externa, vilitigo, purigo nodularis, phimosis, lichen sclerosus, angular chelitis, nappy rash
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Topical corticosteroids are effective for conditions characterised by what?
Hyperproliferation, inflammation and immunologic involvement. Not curative and rebound can occur when discontinued. Used to relieve symptoms when other measures (emollients) are ineffective
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Describe features of emoillients
Used regularly for treatment/maintenance of eczema skin type conditions. MOA - hydrate skin, reduce itch, reduce cracking
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What are the types of emollients? (1)
Creams (aqueous cream ,E45, Zero Base, Diprobase). Ointments (WSP, emulsifying agent, 50:50 WSP/LP, greasier - more effective/but less acceptable to patient, apply regularly/liberally)
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What are the types of emollients? (2)
Bath oils (add to bath water, take care - may make surface slippery). Soap substitutes (use instead of soap, apply to dry skin and then wash off)
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What are the advantages of the topical delivery of steroids? (1)
Non-invasive (acceptable to patients). Targets skin areas/avoids systemic toxicity (depending on steroid/formulation). Can combine therapy/general body care (e.g. moisturising) for greater patient appeal/compliance
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What are the advantages of the topical delivery of steroids? (2)
Can combine with other agents (e.g. antibacterials, antifungals) but not desirable (infection, isolate antibacterial to determine treatment for infection). Steroids may be delivered at controlled rates over long periods (e.g. days)
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What are the advantages of the topical delivery of steroids? (3)
Formulations can be designed to allow potent steroids to infuse slowly into the body. Avoids sudden rise in blood concentrations for potent steroids in HRT and also contraception formulations
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What are the advantages of the topical delivery of steroids? (4)
Penetration of steroids through skin may be enhanced by non-toxic chemicals
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What is eczema?
A chronic skin condition where the skin becomes itchy, reddened, dry and cracked (and sometimes infected). Different types include: irritant, allergic contact, atopic, venous and discoid.
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What is dermatitis?
An acute type of eczema, causes red, itchy/scaly skin, sometimes burning/stinging. It can lead to blistered, dry/cracked skin (sometimes infections). Normally caused by a local irritant (e.g., “Contact” or “Allergic”) or radiation
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What is psoriasis?
A skin condition that causes red, flaky, crusty patches of skin covered with silvery scales (e.g., elbows and flexures typically affected).
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What is impetigo?
A highly contagious skin infection often around the mouth that causes sores and blisters (often with yellow tinge). It is very common and affects mainly children (usually Staphylococcus).
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Describe features of eczema vs dermatitis (1)
Eczema (aka atopic dermatitis) is a form of chronic inflammation of the skin. Eczema/dermatitis refer to the same condition. The term eczema broadly applies to range of persistent/chronic conditions
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Describe features of eczema vs dermatitis (2)
(dry, skin rash, redness, skin oedema, itch, crusting, flaking, blistering, cracking, oozing, bleeding). Dermatitis is an acute type of eczema. Areas of temporary skin discolouration may appear due to healed injuries
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Describe features of eczema vs dermatitis (3)
Scratching open a healing lesion may lead to scarring and enlarge the rash (make sure self-harming not involved)
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Describe features of urticaria/hives (1)
Pale, red, raised, itchy bumps. Burning/stinging sensation. Caused by allergic reactions (e.g. amoxicillin). Acute urticaria lasts for <6 weeks. Chronic urticaria lasts >6 weeks (rarely due to allergy). Most chronic hives are idiopathic (autoimmune)
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Describe features of urticaria/hives (2)
Acute viral infection is another cause of acute urticaria (viral exanthem). Less common causes - friction, pressure, extreme temperatures, exercise, sunlight. Antihistamine treatment may help to stop itching
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Topical corticosteroids provide no benefit to which conditions?
Urticaria (hives), rosacea or acne vulgaris. Should not be used indiscriminately in pruritus where they will only provide benefit if inflammation is causing the itch. Same applies to sunburn (only prevents itch, doesn't heal sunburn)
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What are the common presentations in the community pharmacy for skin disorders fo the face?
Scalp (seborrheic dermatitis). Eyelids (atopic dermatitis). Face (acne). Lips (HSV). Ears (allergic contact dermatitis). Nasolabial folds (perioral dermatitis). Folliculitis (tinea barbae). Chin (rosacea)
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What are the classifications of skin cancers? (1)
Basal-cell carcinoma (pearly translucent (diagnostic) to fleshy colour appearance with tiny blood vessels on the surface/telangiectasia, sometimes ulcerated). Squamous-cell skin carcinoma (red crusted or scaly patch/bump, rapid growing, ulceration)
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What are the classifications of skin cancers? (2)
Malignant melanoma (asymmetrical with an irregular border and colour variation, >6mm diameter, common on the back in men but on legs in women)
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How does tattoo ink cause a skin reaction?
High levels of metals leads to toxicity in the lymph glands (carcinogenic)
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What are topical corticosteroids? (1)
Drugs related to natural hormones produced by the body (e.g. cortisol). Applied directly to affected areas of skin to reduce inflammation (e.g. pain, heat, redness, swelling, itching). Creams, ointments, gels, sprays, lotions applied to affected area
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What are topical corticosteroids? (2)
Can vary in potency from mild to very potent
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What is inflammation? (1)
A reaction of the body to actual or perceived injury, associated with pain/itch/heat/redness/swelling of affected area. Normally inflammation is a protective process. Diagnosis - eliminate cause/consequence of injury
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What is inflammation? (2)
If triggered inappropriately, inflammatory response can itself become harmful, leading to cell, tissue and organ destruction. Inappropriate inflammation occurs in - RA, CD, lupus, psoriasis, eczema, asthma, chronic bronchitis
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Describe the mechanism of inflammation (1)
Occurs in vascularised areas of the body. Triggers - microbial infections, physical agents (trauma, UV radiation, burns, frostbite), tissue necrosis resulting from inadequate blood flow
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Describe the mechanism of inflammation (2)
Normal function - destroy invading cells/prepare for healing and repair. Accumulation of WBCs and chemical/biochemical signalling factors (e.g. cytokines, interleukins, PGs, NO) at sites of injury of infection
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Describe the mechanism of inflammation (3)
Normally WBCs release enzymes that destroy pathogens and remodel tissues to repair injury. In inflammatory diseases, excessive levels of WBCs accumulation (uncontrolled) and destructive action can target body's own tissues
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Describe the biochemical effects of corticosteroid therapy (1)
Regulates expression of many genes with a net anti-inflammatory effect. Reduce production of inflammatory mediators including cytokines, interleukins, PGs, NO
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Describe the biochemical effects of corticosteroid therapy (2)
Inhibit inflammatory cell migration to sites of inflammation by inhibiting the expression of adhesion molecules. Promote the death of apoptosis of WBCs recruited to site of inflammation. Two main mechanisms - genomic and non-genomic
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Outline details of the structure of steroids (1)
Four cycloalkane rings joined together. Three 6 membered ring with D/5 membered ring, side chains, rich in stereochemistry. E.g. of steroids - cholesterol, sex hormones, dexamethasone. Most chemical changes – modification of R group/oxidation state
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Outline details of the structure of steroids (2)
The core of steroids is composed of 17 carbon atoms bonded together that take the form of four fused rings: three cyclohexane rings (designated as rings A, B, and C) and one cyclopentane ring (the D ring).
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What are the types of steroids in common use in medicine?
Adrenal corticosteroids (e.g. prednisone, prednisolone). Oestrogens. Androgens. Progesterones. Anabolic steroids. Both naturally occurring steroids and synthetic analogues used in pharmaceuticals.
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What is the main precursor for steroid biosynthesis in humans?
Cholesterol
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What are the three main types of corticosteroids in the steroidal biosynthesis pathways in humans?
Mineralocorticoids. Androgens and oestrogens. Glucocorticoids
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What is the action of steroid hormones? (1)
Effects occur within seconds or minutes of the steroid making contact with target cells. E.g. androgens (and anabolic steroids) show effects in many parts of the body - hypothalamus, adrenal gland, epididymis, thyroid gland, pituitary gland
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What is the action of steroid hormones? (2)
Quadriceps muscle, kidney, seminal vesicle, testis, liver, submaxillary gland, bulbocavernosus muscle, vagina, heart, ovary, uterus
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Describe features of the genomic action (slower pathway) - 1
Major anti-inflammatory effects of corticosteroids due to transcriptional mechanisms (transactivation and transrepression. Specific binding to cytoplasmic nuclear receptor, other transcription factors (NFκB) may be involved
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Describe features of the genomic action (slower pathway) - 2
Gene activation/repression occurs by direct DNA binding of the steroid receptor complex to recognition sites in promoter regions of genes associated with up-regulation (transactivation) or down-regulation (trans-repression)
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Describe features of the genomic action (slower pathway) - 3
Post-transcriptional regulation of gene expression can occur as well
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Describe features of non-genomic effect pathways (faster pathway)
Not fully understood. Membrane bound steroid receptors, intracellular receptors and other non-specific actions (diagram)
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Describe the cellular genomic actions of glucocorticoids (1)
Transcription factors on the gene, promotes/inhibits gene transcription (mRNA) – control of transcription. Glucocorticoid receptor remains in cytoplasm. GCS enters cell, binds to receptor, Hsp90 removed, complex enters nucleus
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Describe the cellular genomic actions of glucocorticoids (2)
Modulate gene expression (can inhibit/promote transcription). GCS act at gene level to reduce inflammation by promoting transcription of some genes and inhibiting transcription of others
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Describe the cellular genomic actions of glucocorticoids (3)
Target genes code for proteins involved in the inflammatory process (diagram)
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Describe the cellular genomic actions of glucocorticoids (4)
Trans-repression - no mRNA, blocks production of cytokines. Trans-activation - mRNA, induction of inhibitory regulators - Dok-1, SLAP, MAP kinase phosphatase-1
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Outline the structure of the glucocorticoid receptor (1)
NH2, amino terminus, DBD, hormone binding protein, COOH. Finger structures (amino acid chains with Zn in central part).
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Outline the structure of the glucocorticoid receptor (2)
There are also phosphorylation sites and regions of hormone-independent activation function (AF1) and hormone-dependent activation function (AF2) related to transcription.
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What is the challenge for the delivery of corticosteroids through the skin? (1)
Skin has evolved as an efficient barrier to external agents
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What is the challenge for the delivery of corticosteroids through the skin? (2)
The Stratum Corneum, located on the outer surface of the skin, is a non-living layer of keratin-filled cells surrounded by a lipid-rich extracellular matrix that provides the primary barrier to drug delivery into skin.
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What is the challenge for the delivery of corticosteroids through the skin? (3)
The epidermis below is a viable tissue devoid of blood vessels. Just below the dermal-epidermal junction, the dermis contains capillary loops that can take up transdermally administered drugs for systemic distribution.
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Describe features of transdermal diffusion (1)
Transdermal diffusion, possibly in the presence of a chemical enhancer, takes place by a tortuous route across the stratum corneum, winding around cells and occurring along the interfaces of extracellular lipid bilayers.
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Describe features of transdermal diffusion (2)
Low-voltage electrical enhancement by iontophoresis can make transport pathways through hair follicles and sweat ducts more accessible.
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What should the log P values of corticosteroids be?
Log P values for corticosteroids – need high log P in order to be absorbed into the skin (more lipid soluble). (Lipinski's RO5)
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What are chemical enhancers?
Chemicals used to facilitate/speed up penetration of drugs through the skin e.g. salicylic acid, urea - provides keratolytic effect (breakdown of skin), increasing penetration of corticosteroids
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What is iontophoresis?
Low-voltage electrical enhancement by iontophoresis (use of a voltage gradient on the skin) can make transport pathways through hair follicles and sweat ducts more accessible.
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What are the methods to measure the PK of topical absorption of corticosteroids?
Franz cell using human skin (measure how much of a formulation passes through the skin layer). Use HPLC for analysis. PK-type graph plotted
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Describe features of intra-lesional corticosteroid injections for failure of topical treatment
More effective than very potent topical corticosteroid preparations and should be reserved for severe cases where there are localised lesions such as keloid scars, hypertrophic lichen planus, or localised alopecia areata
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What are the important clinical issues with topical corticosteroids? (1)
Corticosteroids only suppress the inflammatory reaction during use with no longer lasting effects. Not curative. On discontinuation, rebound exacerbation of the condition may occur. Relieves symptoms
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What are the important clinical issues with topical corticosteroids? (2)
Suppresses signs of a disorder only when other measures such as emollients are ineffective. May worsen in ulcerated or secondarily infected lesions.
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What are the important clinical issues with topical corticosteroids? (3)
Should not be used indiscriminately in pruritus (where they will only benefit if inflammation is causing the itch). Topical corticosteroids are of no value in the treatment of urticaria and they are contra-indicated in rosacea or acne vulgaris.
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What are the side effects of topical steroids? (1)
Mild-moderately potent topical corticosteroids are associated with few S/E but care is required for potent-very potent corticosteroids. Local S/E - spread/worsening of untreated infection, thinning of skin/original structure may not return, reddening
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What are the side effects of topical steroids? (2)
Blanching of skin (reversible), irreversible striae atrophicae/telangiectasia, contact dermatitis, perioral dermatitis, worsening of acne/rosacea, mild depigmentation (may be reversible), hypertrichosis
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What are the side effects of topical steroids? (3)
Systemic S/E (rare) - absorption through the skin can rarely cause adrenal suppression and Cushing's syndrome depending on the area of the body being treated and duration of treatment. Absorption is greatest where the skin is thin or raw
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What are the side effects of topical steroids? (4)
From intertriginous areas; it is increased by occlusion
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How can the S/E of topical corticosteroids be reduced?
Apply topical corticosteroid thinly to affected areas only. No more frequently than BD. Use the least potent formulation which is fully effective
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State features of the striae atrophicae (stretch marks) - 1
Corticosteroids can cause stretch marks in the dermis by prevention fibroblasts from forming collagen and elastin fibres necessary to keep rapidly growing skin taut. Creates lack of supportive material as skin is stretched
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State features of the striae atrophicae (stretch marks) - 2
Leads to dermal and epidermal tearing
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State features of telangiectasias (spider veins)
Telangiectasias - small dilated blood vessels near the surface of the skin or mucous membranes (0.5-1 mm in diameter). Can develop anywhere on the body but are commonly seen on the face, around the nose, cheeks and chin
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What are the cautions for topical corticosteroids? (1)
Avoid prolonged used on the face (keep away from eyes). Cautions may also apply to systemic corticosteroids if absorption occurs due to topical/local use
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What are the cautions for topical corticosteroids? (2)
In children - avoid prolonged use, must use potent-very potent corticosteroids under specialist supervision. Extreme caution is required in dermatoses of infancy including nappy rash - treatment should be limited to 5-7 days in infants/children
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What are the cautions for using topical corticosteroids in psoriasis?
Use of potent-very potent corticosteroids in psoriasis should be under specialised supervision as it can result in rebound relapse, development of generalised pustular psoriasis and local and systemic toxicity in adults
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What are the contraindications for topical steroids?
Untreated bacteria, fungal, viral skin lesions. Acne and rosacea. Perioral dermatitis. Widespread plaque psoriasis. Can exacerbate symptoms
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What are the clinical considerations for the use of very potent topical corticosteroids? (1)
Should be avoided or given only under specialist supervision in psoriasis because although they may suppress the psoriasis in the short term, relapse or vigorous rebound occurs on withdrawal (sometimes precipitating severe pustular psoriasis).
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What are the clinical considerations for the use of very potent topical corticosteroids? (2)
In general, the most potent topical corticosteroids should be reserved for recalcitrant dermatoses such as - chronic discoid lupus erythematosus, hypertrophic Lichen planus, palmoplantar pustulosis, lichen simplex chronicus
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What are the clinical considerations for the use of very potent topical corticosteroids? (3)
Potent corticosteroids should generally be avoided on the face and skin flexures, but specialists occasionally prescribe them for use on these areas in certain circumstances
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Describe features of the clinical case for the combination of antibacterial or anti-fungal agents (1)
E.g. perioral lesions. Hydrocortisone cream 1% can be used for up to 7 days to treat uninfected inflammatory lesions on the lips.
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Describe features of the clinical case for the combination of antibacterial or anti-fungal agents (2)
Hydrocortisone and miconazole cream or ointment can be useful where infection by susceptible organisms and inflammation co-exist, particularly for initial treatment (up to 7 days), e.g. in angular cheilitis. (DaktacortTM, 15g is P)
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Describe features of the clinical case for the combination of antibacterial or anti-fungal agents (3)
Organisms susceptible to miconazole include Candida spp. and many Gram-positive bacteria including streptococci and staphylococci
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What are the special considerations when treating children with topical steroids? (1)
Susceptible to S/E. But concern about safety should not result in a child being under-treated. Aim to control condition as well as possible. Inadequate treatment will perpetuate condition.
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What are the special considerations when treating children with topical steroids? (2)
A mild corticosteroid such as hydrocortisone 0.5% or 1% is useful for treating nappy rash and hydrocortisone 1% for atopic eczema in childhood. A moderately potent or potent corticosteroid may be appropriate for severe atopic eczema on the limbs
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What are the special considerations when treating children with topical steroids? (3)
For 1–2 weeks only, switching to a less potent preparation as the condition improves
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What are the special considerations when treating children with topical steroids? (4)
In an acute flare-up of atopic eczema, it may be appropriate to use more potent formulations of topical corticosteroids for a short period to regain control of the condition
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What are the special considerations when treating children with topical steroids? (5)
A very potent corticosteroid should be initiated under the supervision of a specialist. Continuous daily application of a mild corticosteroid such as hydrocortisone 1% is equivalent to a potent corticosteroid - betamethasone 0.1% apply intermittently
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What are the special considerations when treating children with topical steroids? (6)
Carers of young children should be advised that treatment should not necessarily be reserved to ‘treat only the worst areas, and they may need to be advised that patient information leaflets may contain inappropriate advice for patient's condition
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Describe features of the choice of formulation (1)
Creams (water-miscible, suitable for moist/weeping lesions). Ointments (for drug, lichenified, scaly lesions, where more occlusive effect is required)
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Describe features of the choice of formulation (2)
Lotions (useful when minimal application to large/hair-bearing area is required or for treatment of exudative lesions)
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Describe features of the choice of formulation (3)
Occlusive polythene/hydrocolloid dressings (increase absorption but also increase risk of S/E, used only under supervision on short term basis for areas of very thick skin (palms/soles). Inclusion of urea/salicylic acid increases penetration
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What are the categories in the BNF for topical corticosteroids?
‘mild’, ‘moderately potent’, ‘potent’ or ‘very potent’; the least potent preparation which is effective should be chosen but dilution should be avoided whenever possible.
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Describe features of application (1)
Apply no more frequently than BD (OD is often sufficient). Length of cream/ointment expelled from tube may be used to specify quantity to be applied to a given area of skin.
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Describe features of application (2)
Length can be measured in terms of fingertip unit (distance from tip of adult index finger to first crease).
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Describe features of fingertip units (1)
One fingertip unit (approximately 500 mg from a tube with a standard 5mm diameter nozzle) is sufficient to cover an area twice that of the flat adult handprint (i.e., palm and fingers)
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Describe features of fingertip units (2)
Per arm (3), front (7), back and bottom (7), per hand (1), per leg (6), per foot (2)
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What are the prescribed quantities of creams of ointments?
Face and neck/both hands/scalp/groins and genitalia (15-30g). Both arms (30-60g). Both legs/trunk (100g) - amounts suitable for an adult for a single daily application for 2 weeks
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State key features of labelling, dispensing and patient counselling (1)
If a patient is using topical steroids of different types/potencies, they should be told when to use each steroid. Potency should be included on the label with directions of use. Label should be attached to container (tube) and outer packaging
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State key features of labelling, dispensing and patient counselling (2)
Mixing preparations should be avoided, several minutes should elapse between application of different preparations
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State key features of labelling, dispensing and patient counselling (3)
In children, “Wet-wrap bandaging” increases absorption into the skin. It should only be initiated by a dermatologist, and application should only be carried out or supervised by a healthcare professional trained in the technique
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State features of patient and carer advice (1)
Patients and carers should be given advice on how to administer corticosteroid creams and ointments. If a patient is using topical corticosteroids of different potencies, the patient should be told when to use each corticosteroid
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State features of patient and carer advice (2)
Patients and carers should be reassured that side effects such as skin thinning and systemic effects rarely occur when topical corticosteroids are used appropriately
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Describe features of compound preparations (1)
Combinations of corticosteroids with antibacterials or antifungals are available for inflammatory skin conditions associated with bacterial or fungal infection (such as infected eczema or nappy rash) but evidence for efficacy is poor
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Describe features of compound preparations (2)
In these cases the antimicrobial drug should be chosen according to the sensitivity of the infecting organism and used regularly for a short period (typically twice daily for 1 week)
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Describe features of compound preparations (3)
Shorter use increases the likelihood of resistance developing, and longer use increases the likelihood of resistance and of sensitisation. The keratolytic effect of salicylic acid facilitates the absorption of topical corticosteroids
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Describe features of compound preparations (4)
The keratolytic effect of salicylic acid facilitates the absorption of topical corticosteroids. However, excessive and prolonged use of topical preparations containing salicylic acid may cause salicylism
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State topical corticosteroid preparations with mild potency
Mild (Hydrocortisone 0.1–2.5%, Dioderm, Mildison, Synalar 1 in 10 dilution). With antimicrobials - Canesten HC, Daktacort, Econacort, Fucidin H, Nystaform-HC, Terra-Cortril, Timodine. With crotamition - Eurax-HC
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State topical corticosteroid preparations with moderate potency
Moderate (Betnovate-RD, Eumovate, Haelan, Modrasone, Synalar 1 in 4 Dilution, Ultralanum Plain). With antimicrobials (Trimovate). With urea (Alphaderm)
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State topical corticosteroid preparations with potent potency (1)
Potent (Beclometasone dipropionate 0.025%, Betamethasone valerate 0.1%, Betacap, Betesil, Bettamousse, Betnovate, Cutivate, Diprosone, Elocon, Hydrocortisone butyrate, Locoid, Locoid Crelo, Metosyn, Mometasone furoate 0.1%, Nerisone, Synalar)
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State topical corticosteroid preparations with potent potency (2)
With antimicrobials (Aureocort, Betamethasone and clioquinol (Betnovate-C), Betamethasone and neomycin (Betnovate-N), Fucibet, Lotriderm, Synalar C, Synalar N.). With salicylic acid (Diprosalic)
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State topical corticosteroid preparations with very potent potency
Very potent (Clarelux, Dermovate, Etrivex, Nerisone Forte). With antimicrobials (Clobetasol with neomycin and nystatin). With increasing potency, IC50 for inhibition of epidermal thickening decreases
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State features of hydrocortisone (1)
0.1%, 0.5%, 1% and 2.5%. P (if 15g 1% Cream – but not Ointment; 0.5% or 2.5% Cream is POM due to higher log P/more skin penetration) POM (if 30g of any strength Cream or Ointment). Indicated for mild inflammatory skin disorders (eczemas, nappy rash)
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State features of hydrocortisone (2)
Apply thinly 1-2 times daily. Adult/child. For nappy rash - apply PRN for no more than 1 week, discontinue as soon as inflammation subsides
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Describe features of OTC hydrocortisone preparations (1)
Skin creams containing hydrocortisone (alone or with other ingredients) can be sold to the public for the treatment of allergic contact dermatitis, irritant dermatitis, insect bite reactions and mild to moderate eczema
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Describe features of OTC hydrocortisone preparations (2)
To be applied sparingly over the affected area 1–2 times daily for max. 1 week. In practice, only 15g of 1% cream is mainly available.
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Describe features of OTC hydrocortisone preparations (3)
OTC HC preparations should not be sold without medical advice for children under 10 years/for pregnant women. Should not be sold for application to the face, anogenital region, broken or infected skin (including cold sores, acne, athlete's foot)
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Describe features of OTC hydrocortisone preparations (4)
Hydrocortisone preparations containing clotrimazole or miconazole nitrate can be sold to the public for athlete's foot and candidal intertrigo (e.g., Canestan HCTM, DakatcortTM). When HC cream/ointment is prescribed with no strength stated, supply 1%
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Describe features of OTC hydrocortisone preparations (5)
Although DiodermTM (POM) contains only 0.1% hydrocortisone, the formulation provides an effect equivalent (or >) to 1% hydrocortisone cream.
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What are the cautions with OTC supply of HC preparations? (1)
HC can be sold for the following conditions - Allergic contact dermatitis, Irritant dermatitis, Mild to moderate eczema, Insect bite reactions
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What are the cautions with OTC supply of HC preparations? (2)
HC should not be supplied to the following conditions - children <10 years, pregnant women, application to face/anogenital region/broken or infected skin e.g. cold sores, acne, athlete's foot
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What are the cautions with OTC supply of HC preparations? (3)
Should not be supplied for - urticaria (hives), sunburn, pruitis (unless associated with inflammation)
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Give examples of moderately potent topical corticosteroids
Clobetasone butyrate (Eumovate, Trimovate). Alclometasone dipropionate 0.05% (modrasone, derma care). Betamethasone valerate 0.025%. Fluocortolone 0.25% (Ultralanum Plain). Fludroxycortide (Flurandrenolone) 0.0125% - 0.05% (Haelan Tape)
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Give examples of potent topical corticosteroids (1)
Hydrocortisone butyrate 0.1% (Locoid cream/lotion). Fluticasone Propionate 0.05% (Cutivate cream/ointment). Triamcinolone Acetonide 0.1% (Aureocort). Mometasone Furoate 0.1% (Mometasone, Elocon). Fluocinonide 0.05% (Metosyn)
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Give examples of potent topical corticosteroids (2)
Fluocinolone Acetonide 0.025% (Synalar, can have diluted preparations). Beclomethasone Dipropionate 0.05% (also used in asthma/COPD inhalers, Clocip-B)
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Give examples of potent topical corticosteroids (3)
Betamethasone Esters (e.g., Valerate) 0.1% - adrenal suppression if more than 100g per week of 0.1% is used (Betacap, Betnovate)
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Give examples of very potent topical corticosteroids
Clobetasol Propionate 0.05% - max of 50g of 0.05% per week (Clarelux, Dermovate, Etrivex). Diflucortolone Valerate 0.1% and 0.3% (Nerisone)
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Which other agents are used fo eczema and psoriasis? (1)
Ichthammol. Dithranol (anthralin). Salicylates. Coal tar preparations (e.g. Alphosyl 2 in 1). Vitamin D analogues. Retinoid and related drugs. Immunosuppressants (calcinuerin inhibitors and related drugs). TNF inhibitors. Interleukin 17A inhibitors
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Which other agents are used fo eczema and psoriasis? (2)
IL-12/13 inhibitors. Other treatments e.g. MTX, short course systemic corticosteroids
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Describe the application of oestrogens as topical drugs (1)
Used to treat a lack of endogenous oestrogens as HRT. Oestrogens are responsible for - development/maintenance of female reproductive system, secondary sexual characteristics, bone/skin metabolism, brain activities, general well being
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Describe the application of oestrogens as topical drugs (2)
17β-estradiol is the principal human estrogen and is significantly more potent than its metabolites, estrone and estriol. Primary source of oestrogens is in the ovarian follicles- secretes 70-500 μg of oestradiol (depends on menstrual cycle phase)
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Describe the application of oestrogens as topical drugs (3)
After menopause, most endogenous estrogen is produced by conversion of androstenedione (secreted by the adrenal cortex) into oestrone by peripheral tissues.
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State features of the production of oestrogens in menopause phase of life
In postmenopausal women, oestrone and oestrone sulfate, are the most abundant circulating oestrogens. These are less active than the principal oestrogen hormone: 17β-estradiol
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State the values of the circulating levels of oestrogens in women pre- and post-menopause (1)
Estradiol (reproductive age - 150 pg/mL, natural menopause - 10-15 pg/mL, surgical menopause 10 pg/mL). Testosterone (reproductive age - 400 pg/mL, natural menopause - 300 pg/mL, surgical menopause - 100 pg/mL)
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State the values of the circulating levels of oestrogens in women pre- and post-menopause (2)
Progesterone (reproductive age - 12,000-20,000 pg/mL, natural menopause - <100 pg/mL, surgical menopause - <100 pg/mL)
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What are the physiological consequences of menopause?
Increased risk of - CVD/MI/stroke, increased risk of osteoporosis (soft bones), depression, mood swings, hot flushes. Many issues can be reversed by taking (replacement) oestrogens. Replacement oestrogens may be taken by oral/injection/topical routes
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Describe features of transdermal continuous delivery of 17β-Estradiol (1)
Steroid structure and chemical properties enable these steroids to penetrate skin, enter cells and reach the blood stream quickly and efficiently. Hence, transdermal patches work well.
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Describe features of transdermal continuous delivery of 17β-Estradiol (2)
Once-weekly patches can produce mean serum concentrations of estradiol similar to concentrations found in pre-menopausal women in the early follicular phase of the ovulatory cycle
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Describe features of transdermal continuous delivery of 17β-Estradiol (3)
Estradiol Transdermal System Continuous Delivery (Once-Weekly) can be applied to the abdomen or lower back
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Describe features of the structure of transdermal skin patches (1)
A medicated adhesive patch placed on the skin to deliver a specific dose of medication through the skin and into the bloodstream. Liner: Protects the patch during storage. The liner is removed prior to use
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Describe features of the structure of transdermal skin patches (2)
Drug: Drug solution in direct contact with release liner. Adhesive: Serves to adhere the components of the patch together and adhering the patch to the skin. Membrane: Controls the release of the drug from the reservoir and multi-layer patches
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Describe features of the structure of transdermal skin patches (3)
Backing: - Protects the patch from the outer environment.
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Describe features of the absorption of oestrogen from patches compared to oral delivery (1)
The absorption of oestrogen from patches is higher than oral delivery due to lack of first pass effect. Estradiol penetrates slowly across intact skin and interstitial fluid leading to sustained circulating levels of estradiol.
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Describe features of the absorption of oestrogen from patches compared to oral delivery (2)
The systemic availability of estradiol after transdermal application (skin patches) is about 20 times higher than that after oral administration. Also a larger patch gives a higher absorption concentration (SA)
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What are the side effects of topical oestrogens? (1)
Feedback inhibition of synthesis and release of pituitary gonadotrophins is the most serious. Mechanism involves the circulating estrogens modulating secretion of the gonadotropins LH and FSH by the pituitary gland through negative feedback mechanism
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What are the side effects of topical oestrogens? (2)
Oestrogens act to reduce the elevated levels of these hormones seen in postmenopausal women.
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Describe features of intravaginal topical estriol and estradiol (1)
For treating dryness and soreness of the vaginal mucosa in postmenopausal women. Local treatment only, so does not lead to significant blood levels of estriol through transdermal absorption.
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Describe features of intravaginal topical estriol and estradiol (2)
Some women, who do not want (or are contraindicated for) HRT (e.g., concerned about possible side effects) will accept estriol 0.1% cream (or gel) to relieve uncomfortable vaginal symptoms.
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What are the estriol/estradiol products? (1)
Estradiol: Pessaries 10 μg (Vagifem®). Estradiol: Vaginal Ring 7.5 μg/24 hours (EstringTM). Estriol: Cream 1mg/g with applicator (OvestinTM)
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What are the estriol/estradiol products? (2)
VagifemTM: One tablet inserted in vagina daily for 2 weeks, then reduce to 1 tablet twice weekly. EstringTM: Insert into upper third of vagina and wear continuously; replace after three months (maximum duration of treatment: 2 years).
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What are the estriol/estradiol products? (3)
OvestinTM: Insert 1 applicator-full daily for 2–3 weeks, then reduce to twice a week (discontinue every 2–3 months for 4 weeks to assess need for further treatment).
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Describe features of topical testosterone gel 1% (1)
Can be applied to any part of body (usually arm or stomach area (i.e., TestogelTM 50mg/5g gel sachets). Increases circulating levels of testosterone. This can benefit female patients with very low levels of testosterone, particularly post-menopausal.
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Describe features of topical testosterone gel 1% (2)
Caution: Overuse can lead to masculinisation (e.g., hair growth). Increasingly used by men for testosterone replacement therapy in later life.
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Contraceptives such as ethinylestradiol patches and vaginal rings contain which hormones?
Transdermal patches - ethinylestradiol and norelgestromin. Vaginal rings - ethinylestradiol and etonogestrel
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Give examples of steroid containing preparations for the eyes, ears and nose
Betamethasone sodium phosphate, dexamethasone, flumetasone pivalate, HC, prednisolone sodium phosphate. NB: Some of these products can be used for the eyes and/or nose as well (e.g., BetnesolTM).
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Give examples of steroid containing hemorrhoidal preparations
Short term use after exclusion of infections. Prolonged use can cause atrophy of anal skin. Haemorrhoids are rare in children. Preparations - anugesic-HC, anusol-HC, perinal, proctofoam HC, proctosedyl, scheriproct, ultraproct, uniroid-HC, xyloproct
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Card 2

Front

What are the uses of topical corticosteroids?

Back

Used in the treatment of inflammatory dermatological conditions e.g. eczema, dermatitis, psoriasis, insect bite/sting reactions, otitis externa, vilitigo, purigo nodularis, phimosis, lichen sclerosus, angular chelitis, nappy rash

Card 3

Front

Topical corticosteroids are effective for conditions characterised by what?

Back

Preview of the front of card 3

Card 4

Front

Describe features of emoillients

Back

Preview of the front of card 4

Card 5

Front

What are the types of emollients? (1)

Back

Preview of the front of card 5
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