DRUGS USED IN SKIN

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NUR 215:PHARMACOLOGY RN, BSc,N. ABDULLAH KHAMIS Friday, January 9, 2015 1

Transcript of DRUGS USED IN SKIN

Page 1: DRUGS USED IN SKIN

NUR 215:PHARMACOLOGY

RN, BSc,N. ABDULLAH KHAMIS

Friday, January 9, 2015

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BROAD OBJECTIVES

At the end of the session the learner should be

able to understand:

Drugs used in skin and mucous membrane

and nurses responsibilities

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INTRODUCTION

What is skin?

The skin is the largest organ of the body, accounting for about 15% of the total adult body weight. It performs many vital functions, including protection against external physical, chemical, and biologic assailants,(attack or defence mechanism) as well as prevention of excess water loss from the body and a role in thermoregulation.

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CONTI….

The skin is continuous, with the mucous

membranes lining the body’s surface. The

skin is composed of three layers: the

epidermis, the dermis, and subcutaneous

tissue

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LAYERS OF SKIN

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TROPICAL MEDICATION

What is the topical route of administration?

It is the administration of drugs via the

epidermis (outer layer of the skin) and

external mucous membranes to achieve local

or systemic effects.

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REASONS FOR USING TROPICAL

MEDICATION

Permits local rather than systemic absorption

of the drug

Reduces side effects

Some drugs are slow release over 24 hours

therefore continuous action

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ROUTES WHICH CAN BE USED IN TROPICAL

MEDICATION

Eye

Ear

Nose

Transdermal

Rectal

Vaginal

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DRUGS USED IN SKIN AND MUCUS

MEMBRANE ARE DIVIDED INTO

SEVERAL GROUPS WHICH ARE: Antifungal

Antibacterial

Anti inflamatory

Antipuretics and local anaethetics

Keratolytics

Keratoplastics and

Antiviral

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ANTIFUNGAL

There several antifungal which are as

follows:

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ANTIBACTERIAL

Antibiotics are used for systemic and topical

skin diseases treatment, taking advantage of

their antiseptic, bacteriostatic and also their

anti-inflammatory and immunomodulating

properties. In case of localized external skin

layers infections, a topical treatment is

adequate.

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In case of widespread and deeper infections

a systemic treatment is needed. The latter

dermatological diseases are mostly treated

by beta-lactam antibiotics (penicillins and

cefalosporins) macrolides and tetracycline. In

topical treatment mostly erythromycin,

clindamycin, mupirocyne and fusidic acid are

used

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CONTI…..

There are several antimicrobial drugs are:

Erythromycin gel

Clindamycin gel

Bacitricin

Fusidate sodium

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ERYTHROMYCIN GEL

Description:

Erythromycin topical is an antibiotic that fights skin infection caused by bacteria.

Erythromycin Topical Gel contains erythromycin for topical dermatologic use. Erythromycin is a macrolide antibiotic produced from a strain of Saccaropolysporaerythraea

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Indication

Erythromycin topical (for the skin) is used to

treat bacterial infections such as severe acne

Minor cuts

burns

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Mechanism of action

Erythromycin acts by inhibition of protein synthesis in susceptible organisms by reversibly binding to 50s ribosomal subunits

It inhibit translocation of aminoacyl transfer-RNA and inhibiting polypeptide synthesis.

Antagonism has been demonstrated in vitro between erythromycin, lincomycin, chloramphenicol, and clindamycin

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Uses

This medication is for use on the skin only

. Clean and dry the affected area as directed.

Then apply a thin layer of the medication on the

skin, usually once or twice a day or as directed.

Wash your hands after use.

Do not use large amounts or apply this more

often or for a longer period than directed.

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Nursing consideration

Use this medication regularly in order to

get the most benefit from it.

Remember to use it at the same time(s)

each day.

Avoid getting this medication in your eyes

or inside the nose or mouth.

If this occurs, rinse thoroughly with water.

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Side effects

Less serious side effects may include:

mild skin irritation or tenderness;

dry skin

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Severe side affects

Tightness of the chest

Difficult breathing

Blood stool

Irritation of the eyes

Itching

Stomach cramp

Severe diarrhoea

Redness of skin

Severe allergic reaction(rashes, hives)

Swelling of mouth, face, lips and tongue

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Contraindications

Erythromycin Gel is contraindicated in those

individuals who have shown hypersensitivity

to any of its components

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CLINDAMYCIN PHOSPHATES CREAM

Indication

Treatment of bacterial vagonosis e.g. haempphilusvaginitis

Mechanism of action

It inhibit bacterial protein synthesis at the level of bacterial ribosome.

Dose

Complete content of a single pre-filled applicator containing 5g of clindance cream administered once vaginally at any time of a day

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CONTI….

Side effects

Pruritic rash, diarrhea, vomiting, fatigue, back

pain, constipation, dizziness, dysfunctional

uterine bleeding, pelvic pain, vaginal irritation

Precaution

Accidentally exposure to the eyes

Fungal vaginal infection

Lactation mother

Pregnancy woman

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Contraindication

Hypersensitivity to Clindamycin

History of bowel disease

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ANTI-INFLAMMATORY

A steroid hormone produced by the adrenal cortex that regulates carbohydrate metabolism and maintains blood pressure. Also called cortisol.

A preparation of this hormone obtained from natural sources or produced synthetically and used to treat inflammatory

A steroid hormone produced by the adrenal glands that provides resistance to stress

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CONTI…

There are several anti-inflammatory which

are:

Hydrocortisone

Zinc sulphate

Budesonerden

betamethasone

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HYDROCORTISONE

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HYDROCORTISONE

Generic name : Hydrocortisone.

Trade name: Cortaid.

Availability

Cream, gel, lotion, ointment, solution:

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Action

Suppresses inflammatory and immune

responses, mainly by inhibiting migration of

leukocytes and phagocytes and decreasing

inflammatory mediators, also interacts with

steroid cytoplasmic receptors to induce anti-

inflammatory effects; possesses antipruritic,

anti-inflammatory actions

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Indication: It is prescribed for the topical

treatment of skin inflammation includes :

psoriasis, eczema, contact dermatitis,

allergies, pruritus, collagen diseases,

adrenocortical insufficiency, and certain

neoplasm

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Contraindication

Viral and fungal diseases of the skin that

occur where circulation is impaired or known

hypersensitivity to steroids prohibits its use.

Hypersensitivity to drug, alcohol.

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CONTI….

Systemic fungal infections

Concurrent use of other

immunosuppressant corticosteroids

Concurrent administration of live-virus

vaccine

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Adverse effects.

Among the more serious adverse effects are

various systemic side effects that may result

from prolonged or excessive use. Local

irritation of the skin may occur. conditions

including : adrenal failure, headache,

nervousness nausea, vomiting, dry mouth,

muscle pain or weakness rash, pruritus,

urticaria, contact dermatitis insomnia;

appetite changes

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Route for administration.

Injection: 25 mg/ml, 50 mg/ml; 100 mg/vial,

250 mg/vial, 500 mg/vial, 1,000 mg/vial.

Oral suspension: 10 mg/5 ml

Spray (topical): 1%

Tablets: 5 mg, 10 mg, 20 mg

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Dose

20 to 240 mg/day P.O.[Suspension].

5 to 75 mg by intra-articular injection

(depending on joint size) 2to 3 weeks.

One applicatorful of intrarectal foam daily or

b.i.d. for 2 to 3 weeks; then one applicatorful

every other day

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CONT…..

15 to 240 mg/day subcutaneously, I.M., or I.V.,

adjusted according to drug.

100 to 500 mg I.M. or I.V.; may repeat at 2-, 4-

, or 6-hour intervals, depending on response

and condition response

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Precautions

Caution should be taken of patient with :

Hypertension, osteoporosis, glaucoma, renal or GI disease, hypothyroidism, cirrhosis, thromboembolic disorders, myasthenia gravis,

Heart failure

Pregnant

Breastfeeding patient

Children ages 6 and younger (safety not established).

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Administration

•Give oral form with food or milk to avoid GI upset.• Give I.V. injection of sodium succinate form over 30 seconds to a few minutes.• Know that drug may be given as intermittent or continuous I.V. infusion. Dilute in normal saline solution, dextrose 5% in water, or dextrose 5% in normal saline solution.• Inject I.M. deep into gluteal muscle. Rotate injection sites to prevent muscle atrophy.

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• Be aware that subcutaneous administration

may cause muscle atrophy or sterile abscess.

Never abruptly discontinue high-dose or long-

term systemic therapy.

• Know that systemic forms typically are used

for adrenal replacement rather than

inflammation.

• Be aware that occlusive dressings, heat,

hydration, inflammation, denuding, and thinning

of skin increase topical drug absorption

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Patient teaching

Instruct patient to take daily P.O. dose with food by.

Urge patient to immediately report unusual weight

gain, face or leg swelling, epigastric burning,

vomiting of blood, black tarry stools, irregular

menstrual cycles, fever, prolonged sore throat, cold

or other infection, or worsening of symptoms.

Tell patient using topical form not to apply

occlusive dressing unless instructed by prescriber.

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Advise patient to discontinue topical drug

and notify prescriber if local irritation occurs.

Instruct patient to eat small, frequent meals

and to take antacids as needed to minimize

GI upset.

Tell patient that response to drug will be

monitored regular.

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BETAMETHASONE

Description:

Betamethasone Valerate

Cream, Ointment and Lotion

contain betamethasone

valerate USP, a synthetic

adrenocorticosteroid

for dermatologic use.

Betamethasone, an analog of

prednisolone, has a high

degree of glucocorticoid

activity and a slight degree of

mineralocorticoid activity

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The mechanism of action

Anti-inflammatory activity of the topical corticosteroids is unclear. Various laboratory methods, including vasoconstrictor

assays, are used to compare and predict potencies and/or clinical efficacies of the topical corticosteroids. There is some evidence to

suggest that a recognizable correlation exists between vasoconstrictor potency and therapeutic efficacy in man.

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Indication:

Topical corticosteroids are indicated for the relief of the inflammatory and pruriticmanifestations of corticosteroid-responsive dermatoses.

Contraindications:

Topical corticosteroids are contraindicated in those patients with a history of hypersensitivity to any of the

components of the preparation.

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Precautions:

Systemic absorption of topical

corticosteroids has produced reversible

hypothalamic-pituitary-adrenal (HPA)

axis suppression, manifestations of

Cushing’s syndrome, hyperglycemia, and

glucosuria in some patients.

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ANTIPURITICS DRUGS

An antipruritic agent or substance is by

nature or design something that helps to

preventing or relieving the discomfort

associated with itching.

Topical antipruritic are available in a variety

of formulations like creams, ointments,

powders, lotion and even the occasional

spray could assist

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How to use Antipruritic topical

This medication is used to treat a variety of

skin conditions for reduces the swelling,

itching, and redness that can occur in these

types of conditions (e.g., eczema, dermatitis,

allergies, rash) This medication is a mild

corticosteroid

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The medication use on the skin only .Wash

and dry your hands before using. Clean and

dry the affected area. Apply a small amount

of medication to the affected area and gently

rub in, usually 2-4 times daily or as directed

by your doctor. Do not bandage, cover, or

wrap the area unless directed to do so by

your doctor. If used in the diaper area on an

infant, do not use tight-fitting diapers or

plastic pants

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There are several antipuritics drugs but

common one are:

Calamine lotion

Hydrocortisone Antipruritic topical

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CALAMINE LOTION

Lotion (BP 15% calamine,

USP 8% calamine

Uses: Symptomatic topical

treatment of mild pruritus

and insect stings.

Dosage: Shake well before

using. Apply to affected skin

3–4 times daily.

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CALAMINE LOTION

Precautions: Avoid

contact with the eyes

and mucous

membranes

Adverse effects: May

rarely cause

sensitization rating

superficial wounds,

tropical ulcers and the

skin lesions.

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HYDROCORTISONE ANTIPRURITIC TOPICAL

Dosage:

A thin film should be applied to the affected area 1–4 times daily. When a favorable

response occurs, reduce the frequency of application to the minimum necessary to maintain control and avoid relapse. Treatment should be stopped as soon as all lesions have resolved

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. The cream is suitable for most dermatoses

and the ointment is often used for dry,

scaly lesions. Occlusive dressings should

only be used for severe or resistant lesions.

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CONT….

Precautions:

The use of occlusive dressings increases the penetration of hydrocortisone into keratinized lesions. Use occlusive dressings only at night and for no longer than two nights. Occlusive dressings should never be used on weeping lesions. If secondary infection occurs, stop hydrocortisone and give an appropriate antimicrobial.

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Adverse effects:

Exacerbation of untreated infections. Prolonged use can induce local atrophic changes, particularly on the face and in skin folds, characterized by thinning of the dermis, depigmentation, dilatation of superficial blood vessels and formation of striae. Hypercorticalism and suppression of the hypothalamic-pituitary-adrenal axis are possible with prolonged use or widespread use on large areas of the body. However, local atrophic changes are much less common with hydrocortisone

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KERATOLYTIC AGENT

There are several keratolytic agent drugs

which are:

Adapalene gel

Benzoyl peroxide cream

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ADAPALENE GEL

Common brand

name: Defferin

Generic name:

Adapalene

Adapalene gel 0.1

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Indication

Is the medication used to treat acne vulgaris

in patients 12 years of age and . It may

decrease the number of severity of acne

pimples and promote quick healing of

pimples that do development.

It works by affecting the growth of cell and

decreasing swelling and inflammation

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Dosage

Each gram of DIFFERIN Gel, 0.3% contains 3 mg adapalene in an off-white aqueous gel.

Use adult dose for acne

0.1% or 0.3% gel

Use for pediatric dose for acne

12 18 years the same dose

45 laminate tube NDC

75 laminated tube NDC

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Mechanism of Action

Adapalene binds to specific retinoic acid nuclear receptors but does not bind to cytosolic receptor protein. Biochemical and pharmacological profile studies have demonstrated that adapalene is a modulator of cellular differentiation, keratinization, and inflammatory processes. However, the significance of these findings with regard to the mechanism of action of adapalene for the treatment of acne is unknown.

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Drug interaction

Adapalene gel has potential to produce local

irritation in some patients, concomitant use of

other potentially irritating tropical products

e.g. medicated soap and cosmetics have

strong dry effects and product with high

concentration of alcohol.

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CONTI…..

Adverse effects

Erthyma scaling

Dryness

Pruritus

Burning which occur (10-40)

Skin irritation

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Precaution

During the use of Adapalene the patient should avoid expose him/herself to sunlight

Sensitivity to sun

Avoid contact with eyes, lips and angles of nose

Also should not be applied on cuts, abrasion, eczematous skin or sunburn skin

Allergic to vitamin A

Avoid electrolysis, waxing, and chemical depilatories for hair removal on the treated area

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CONTI….

Contraindication

Should be not be administered to individual

who are hypersensitivity adapalene

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BENZOYL PEROXIDE

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CONTI….

Cream or lotion 2.5%, 5%, 10%

Benzoyl peroxide is a bacteriostatic agent

that is used primarily in acne because of its

activity against propionibacterium acnes

It is absorbed by the skin after tropical

application and metabolized to benzoic acid

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Uses

Treatment of mild and moderate acne vulgaris and as an adjunct to therapy in more sever cases

Dosage and administration

Adult and adolescent: a thin layer of 2.5% or 5% cream or lotion should be applied to skin initially once daily on alternate days

The frequent of application is the gradually increase up to twice daily as tolerance develops. Unresponsive case may require treatment with the 10% preparation

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CONTI….

Contraindication

Known hypersensitivity to benzoyl peroxide

Precaution

It should not applied to open sores or broken

skin.

Contact with eyes

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Adverse effects

Skin irritation is common after topical

application but subside with continued

treatment

Side effects

Mild burning, Dryness, itching, peeling,

redness, stringing or swelling of treated area

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KERATOPLASTIC AGENTS

There are several keratoplastic agent drugs

which are:

Coal tar

Salicylic acid

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COAL TAR

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Solution 5-10%

Ointment(crud coal tar) 1%

shampoo

General information

Coal tar is the keratoplastic agent that

inhibits excessive proliferation of epidermal

cells by reducing DNA synthesis and mitotic

activity to normal levels

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Uses

Treatment of chronic psoriasis either alone or

in combination of exposure to ultraviolet light

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Dosage and administration

Adults and children: 100 of solution should be thoroughly mixed with bath water and the patient should soak for 10-20 minutes. Treatment may be repeated daily until the lesions have resolved

Alternatively a thin layer of ointment is applied to the affected areas once daily until the lesion have resolved.

Phototherapy should not be started until at least 24 hours after treatment and until all traces of the coal tar preparation have been removed from the skin

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Contraindication

Known hypersensitivity to tar preparation

Coal tar preparation should not be applied to inflamed broken or infected skin

Exposure direct to sunlight should be avoided as far as possible for at least 24 hours after treatment because of the risk of photosensitivity reaction

Although coal tar is potential carcinogen there is no evidence that it increases the risk of skin cancer at the doses used therapeutically

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CONTI….

Adverse effects

Skin irritation, rarely allergic sensation.

Staining of the skin and hair

Side effects

Itching, burning tenderness, redness and

sensitivity to sunlight

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SALICYLIC ACID

Generic name: salicylic

acid

Brand name: Keralyt scalp

Uses

Removing excess skin in a

certain condition including

scaling assosiated with

scalp psoriasis or calluses

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CONTI…

Salicylic acid is a

tropical salicycate. It is

working by causing the

skin to swelnand

slough,soften or pee; in

areas where it is applied

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Mechanism of action

It facilitate desquamation by solubilizing the intracellular cement binds scales in the stratum corneum, thee for loosing keratin.

Contraindicated

Allergic to any ingredients in salicylic acid

Child or teenage with flue, chicken pox or shingles

Children less than 2 years of age

Diabetes mellitus

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Dosage

Use adult dose for acne

Salicylic acid topical 1% pad

Clean affected area. Apply 2 to 3 times daily.

Usual adult dose for dermatological disorder

Salicylic acid topical 16.7% liquid

Wash and dry area thoroughly. Apply enough to

cover each wart 1 to 2 times daily

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CONTI….

Salicylic acid topical soap

Apply to affected area at least twice a weekly

Salicylic acid topical 6% cream

Apply affected area once daily

Salicylic acid topical 6% lotion

Apply affected area once daily

Salicylic acid topical 6% form

Apply to the affected area once daily at bed time

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Precaution

Pregnancy

Breastfeeding

Pediatrics

Side effects

Skin irritation and skin ulceration or erosion

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ANTIVIRAL AGENT

There are several antiviral agent drugs which

are:

Acyclovir

Ketaconazole

Miconazole nitrate

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ACYCLOVIR

Is the mostly widely

prescribed anti viral drug

in the world.

Is a synthetics compound

with similar molecules

structure to purine

nucleoside

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Indication

Acyclovir is used in the treatment of

Primary herpes simplex

Recurrent of episodes of genital herpes

Suppression of HSV infection

The first few of the herpes zoster infection

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Dosing Regimes

Herpes simplex

For initial in adult and 2 yrs

Oral 200mg or 400mg tds /10day

In children over 2yrs- half of adult dose so is 100mg-200mg

Also it available as a cold sore cream for the lips and face and as an ophthalmic ointment for eye infection. it should be applied at the first sign of infection

Also applied on the skin at the affected areas

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N.B it is not suitable for the mouth or other mucus membrane.

Varicella zoster –acyclovir is an important treatment for herpes zoster but it can also be used to treat Varicella (chiken pox) in adult or severe infection in children.

Tabs 800mg five times a day for 7 days accelerates the rates of healing of blisters

Immunocompromised patients: with chicken pox

Disseminated herpes zoster or severe herpes simplex

Acute herpes zoster when it affects the trigeminal nerve (for head and eye lids)

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extensive eczema herpeticum

-herpes infection of the brain (encephalitis)

-herpes infection in new born babies

We can intravenous acyclovir which is given

over one hour every 8hrs for 7days in a dose

of 5mg/kg for HSV and 10mg /kg for VZU

(Varicella zoster virus)

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Mechanism of action

To become effective, acyclovir must first be

charged to acyclovir monophosphate by an

enzyme that is only found in viruses, called

thimidine kinase (TK) then converted to its

active triphosphate from human enzymes found

inside the cells. Acyclovir triphosphate is the

active form of the drug. It reduce production of

viral DNA by competing with natural

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CONT….

compound, deoxygnanorisen, triphosphate, for the viral DNA polymerase enzyme incorporation of AT into viral DNA completely prevent the synthesis of new DNA

Viral DNA polymerase. Binds 10-30 times more strongly to AT then the cellular DNA polymerase. This means acyclovir is not toxic

Unfortunately , only about 13-20% of the dose of acyclovir is absorbed through the gut wall, which means it must be taken frequently as it only active for two or three hrs in the blood streams

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CONTI….

Side effect

The side effect are un common but include-

nausea or vomiting, diarrhea headache,

fever, confusion, lynphadinopathy,

generalized muscle ache itchy skin transient

burning, stinging, and pruritus.

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CONTI….

Precaution

Kidney disease pts –the dose should be

reduced to prevent accumulation of drug

contents that may lead to damage the kidney

or nerves system

It can cause abnormal liver function, blood

test and rarely a lowering of the white cell

count

Pregnancy

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KETACONAZOLE

Description

Ketaconazole is used to treat infection by cutaneous and mucous membrane dermatophyte fungus or yeast. Its work by killing the fungus or yeast or preventing its growth. It is broad spectrum of antifungal agent

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CONTI….

Uses

Athlete’s foot (tinea pedis, ring worm of the foot)

Ring worm of the body

Sun fungus (tinea versicolor)

Yeast infection of skin (cutenous candicadas)

Dosage

It is recommended ketaconazole cream to be applied once daily to cover the affected area and surrounded area

Ketaconazole cream, 2% 15,30 and 60 grams tube

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CONT….

Drug interaction

Both rifampin and isoniazid lower plasma

ketoconazole levels, and concomitant

administration should be avoided Phenytoin

serum levels should be monitored closely

when ketoconazole is

prescribed.Ketoconazole

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CONTI….

Precaution

Carcinogenesis, mutagenesis and impairment fertility

Pregnancy: teratogenic effect

Lactation mother

Side effects

Erythema, itching, bleeding discomfort, dryness, inflammation, irritation and paraethesiae

Contraindicated

Hypersensitivity to the active or excipient ingredient of this formulation

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REFFERENCE

Clinical pharmacokinetics (3/e) by M.Rowland and T.N Tozer

Antibiotics and chemotherapy (7/e) by F.O Grady HP Lambert RG Finch and D. Greenwood

Pharmacology in medicine –principle and practice(1/e) by S.N Pradliam R.P Mackle SN Dutta

Godman and Gilman’s. The pharmacological basis of therapeutics (10/e) by J.G Hardman L.E Lambird and alferd Goodman Gilman

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THANKS FOR

WATCHING AND

READ

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