Corticosteroid n Antihistamin Econtocosteroid and antihistaminng

CORTICOSTEROID & ANTIHISTAMINE

Dr. Nelva K. Jusuf, SpKK(K)

CORTICOSTEROID

In Corticosteroid, we have 5 topics :– What– Why– When– Where– How

W H A T

• CORTICOSTEROID

–Is regulatory hormone synthesized from a cholesterol core in adrenal gland at the cortex.

W H Y

– CORTICOSTEROIDS applied for dermatology due to effects :

• Anti inflammation• Anti allergy • Vasoconstrictor • Immunosuppressive • Anti mitotic / anti proliferate

W H E N

– Absolute Indications

• Pemphigus • SLE (Systemic Lupus Erithematous)• Severe SJS (Stevens Johnson Syndrome) :

TEN (toxic epidermal necrolized)• ERYTHRODERMA

W H E N

– Relative Indications • Bullous pemphigoid • Allergic urticaria • Erythroderma • Nodosum erythema • Mutliform erythema• Severe dermatitis • DLE (Discoid Lupus Erythematosus)

W H E N

– TOPICAL CORTISCOTEROID• Potency : Weak, medium, potent , highly potent

– INDICATIONS : very large – HIGHLY RESPONSIVE :

• Atopic dermatitis • Seborrheic dermatitis • Contact dermatitis• Numularis dermatitis

W H E N

– MEDIUM RESPONSIVE : • Psoriasis• DLE • Lichen planus

– FORMS : cream, ointment, fatty ointment, lotion, spray

W H E N

– INTRA LESION CORTICOSTEROID • INDICATIONS :

– Keloid – Hyper tropic scar – Alopesia areata – Chronic Lichen simplex– Cystic acne – Granuloma anulare

W H E R E

TOPICAL CORTICOSTEROID

– Folds area, baby’s face weak potent (if given high potency CS systemic effect side effect on the skin increasing

H O W

– CORTICOSTEROID DOSE RULES• First, find the therapy dose re-evaluation

period of therapy (depend on the disease & individuals)

• If improvement (+) tapering off maintanance dose after few days if no improvement dose increased until improved

• Single dose every morning side effect larger than divided dose

H O W

• To prevent side effect “alternate day” dose• To decrease dose & shorten CS therapy can

be given at the same time with MTX, AZT, Cyclosporin (STEROID SPARRING EFFECT)

• Treatment shouldn't be stopped suddenly rebound phenomenon

• Side effects appear depend on dose, period of therapy & types of CS.

AGENT Anti inflammation

potency

Equivalent dose (mg)

Na Retention

Potent

Short acting :

Hydrocortisone

Cortisone

1

0,8

20

25

++

++

Intermediate acting

Prednisone

Prednisolone

Methyl Prednisolone

Triamcinolone

3,5

4

5

5

5

5

4

4

+

+

-

-

Long acting :

Paramethasone

Betamethasone

Dexamethasone

10

25

30

2

0,60

0,75

-

-

-

DAILY INITIAL DOSE SYSTEMIC CORTICOSTEROID ON ADULTS IN VARIES DERMATOSES

– DISEASES :• Dermatitis• Mild drug eruption• Severe SJS & TEN • Erythroderma • Leprosy reaction• DLE• Bullous pemphigoid• Pemphigus vulgaris• Pemphigus foliaseous• Pemphigus erythematous• Psoriasis pustulosa

– DOSE : • Prednisone 4 x 5 mg/3 x 10 mg• Prednisone 3 x 10 mg/4 x 10 mg• Dexamethasone 6 x 5 ,g• Prednisone 3 x 10 mg• Prednisone 3 x 10 mg• Prednisone 3 x 10 mg• Prednisone 40 – 80 mg• Prednisone 60 – 150 mg• Prednisone 3 x 20 mg• Prednisone 3 x 20 mg• Prednisone 4 x 10 mg

SIDE EFFECT PREVENTION

– High protein diet, low salt diet – Anabolic CS– KCl 3 x 500 mg/day if K deficiency– ACTH :

• Synachten depo• 1 mg (100 IU) once in 4 weeks

– Antibiotic– Antacid

Side effect control of systemic CS

Patient name : ……………..age :……………….gender : F/MDiagnosis:………………………………………………………..Start having high dose CS : ……………………………………1. Face moon face ( )2. Skin hirsutism ( ), atrophy ( ),

striae atrophise ( ),dermatosis acneformis ( ), purpura

( ), teleangiectase ( )

3. Eye posterior subcapsular cataract ( ),glaucoma( )

4. Muscles atrophy ( ). Fibrosis ( ), myopathy waist/shoulder ( )

5.Digestive gastric juice hypersecretion ( ),

pancreatitis ( ),

changing gastric protection ( )

regional ileitis ( ), ulcus pepticum/

perforation ( ), ulcerative colitis ( ),

6. CNS changing personality :

euphoria ( ), insomnia ( ), nervous ( ),

psychosis ( ), irritable ( ), eating increased( ),paranoid ( ), suicidal tendancy ( ), hyperkinesias ( )

7. Skeletons osteoporosis ( ), fracture ( ), vertebrae

compression ( ), scoliosis ( ), long bone

fracture ( )

8. Blood increased : hemoglobin ( ), erythrocyte ( )leukocyte ( ), lymphocyte ( )

9. Blood vessel blood pressure increased ( )10. Adrenal cortex atrophy ( ), stress irresistible ( )11.Protein, protein loss ( ), hyper lipidemia ( ), blood carbohydrate, sugar increased ( ),obesity ( ), buffalo fat metabolism hump ( ), fatty liver ( )12.Electrolyte Na/water retention ( ), Kalium loss ( ),

asthenia ( ), paralysis ( ), tetany ( ), cardiac arrhythmia ( )

13.Immune system decreased of immune, high risk to infection ( ), TB reactivation (

),herpes simplex ( ), malignancy ( ), etc (

)

ANTIHISTAMINE

HISTAMINE :

Is a bio active – amin with low molecular weight found mainly in human on the mast cell of the tissue and basophile in blood.

ANTIHISTAMINE

– Histamine stimulated smooth muscles and had an intense vasopressor effect.

– Histamine was isolated from liver and lung tissue and skin by physical stimuli.

– Histamine is distributed widely throughout the animal kingdom and is found in venom, noxious secretions, bacteria and plants.

– Most mamalian tissue contains histamin with the highies concentrationss found in lungs, skin and intestinal mucousa.

ANTIHISTAMINE

HISTAMINE :– Is synthesized by decarboxylation of the amino

acid histidine. – Can be liberated from storage by numerous

factors. When liberated, a reaction known as the triple response results.

• Erythema appears due to capillary dilation• Diffuse and wide spread flare secondary to arteriolar

dilation• A wheal appears at the injury site due to exudation of

fluid through the altered vascular wall

ANTIHISTAMINE

HISTAMINE :– Other effects of histamine on the body include :

• Dilation of cerebral vessels leading to a headache• Increased secretion of exocrine glands causing

stimulation of gastric juice• Stimulation of nerve endings leading to pain and itch• Smooth muscle contraction, which can cause broncho

constriction • Dilatation and increased permeability of capillaries

leading to loss of plasma and decreased blood pressure, which can cause increases in heart rate and cardiac output.

ANTIHISTAMINE

HISTAMINE – This situation causes variety clinical manifestation,

depend on individual “organ target” and species, such as :

• Respiratory tract : bronchus obstruction and larynx edema

• Gastro – intestinal tract : nausea, vomit, and diarrhea • Cardiovascular tract :hypo tension , shock• Skin : itching, erythema, edema, and

maculopapular lesion

ANTIHISTAMINE

– Beside histamine, when the degranulation of the mast cell and / or basophile applied, also released another pharmacologic substances called “histamine like substance” :

• SRS – A (Slow reacting substance anaphylaxis)• ECF – A (Eosinophile chemotactic factor anaphylaxis)• Serotonin ( 5 –hydroxytryptamine)• PAF (Platelet activating factor) • Heparin (6)

ANTIHISTAMINE

– Is an ethyl amine substance

( - CH2 – CH2 – N ) (also found in histamine)

– Half part of ethyl amine : linear chain or half-ring form.

– Antihistamine doesn’t resist to the release of histamine, but it competes with histamine to reach H1 effectors in receptor cell, and quickly reversible attached.

– The attachment with receptor can be re-released soon due to its short acting occupying period needs repeated dose to keep the concentrate high to compete with histamine in the receptor places.

– And eventually the number of antihistamine will be reduced due to metabolism and elimination.

ANTIHISTAMINE

– Antihistamine is quickly absorbed, parenteral, more or less 15 minutes, per oral + - 30 mins and reaching the top after 1 – 2 hours with indurance 3 – 6 hours, but there is also the slow released form.

CLASSIFICATION

– Antihistamine H1 divided into 7 groups according to the connection with ethyl amine :

• Ethanol amine : bromodiphen hydramine, carbinoxamine, clemastine, difenhidrinate.

• Ethylendiamine : tripelenamine, antazoline.• Alkylamine : chlorphenyramine,

brompheniramine.• Piperazine : hydroxycin

CLASSIFICATION

• Phenotiazin : prometazine • Piperidine : ciproheptadine • Miscellanous : astemizole, terfenadine,

mebhidroline

ANTIHISTAMINE

– Indication :• Antihistamine H1 allergic symptoms due to

released of histamine

– Topical :• Effective as analgetic on mucous and

elimiate skin itchness

ANTIHISTAMINE

– New antihistamines :• Doesn’t cause sedation

– Side effect :• CNS • ANS • Digestive tract• Blood

ANTIHISTAMINE

– Toxicity• Insomnia, tremor, nervous, convulsion

– Drugs interaction• If taken with depressant group medicine in the

same time, can cause potentiation effect and antihistamine antagonist characterized with guanetidin (anti hyper tension)

T H E E N D

GOOD LUCK FOR YOUR POST TEST