Transcript Povrchově aktivní látky

Antiseptics,
disinfectants,
dermatologics, ORL
drugs
This study material is recommended specifically for practical courses from
Pharmacology II for students of general medicine and stomatology. These brief notes
could be used to prepare for the lesson and as a base for own notes during courses.
Addititonal explanations and information are given in single lessons.
Effects of drugs with topical
administration
• Systemic– transdermal administration
– contraceptives
– HST
– opioids (fentanyl)
– nicotine
– NSAID (diclophenac)
• Local
Dermatologics
• Skin disease
–
–
–
–
–
–
external signs of infectious diseases
skin inflammation
tumors
mycoses
viral infections
….
Dermatologics
• preferably drugs with local effects
• lower specificity of effect
– the same drug in different indications
– effect depends on: concenrtation, drug
dosage form, the site of administration
Local effect
1.
2.
3.
4.
5.
6.
7.
8.
Antiseptics (disinfectants)
Astringents
Keratolytics/keratoplastics
Re-epithelisants and cicatrizants
Emolients
Therapy of acne
Antipsoriatics
Drugs for ORL
1. Antiseptics, disinfectants
• Antiseptics
– inhibition of microbial growth in the
environment of live tissues
– do not damage tissues
• Disinfectants
– kill microbes in the outer environment
(inanimate materials, infectious materials)
Mechanisms
Oxidation – acids, H2O2, KMnO4, chlorine
Hydrolysis – acids, alkalis, heat
Protein precipitation (salts)– heavy metals, halogensy
Protein coagulation – phenols, alcohols, quarternary
ammonium compounds
Permeability changes– soaps, quarternary ammonium
compounds
Enzymatic system destruction– hevy metals, phenols,
formaldehyde
Heavy metals compounds:
mercury:
Phenylhydrargyri boras
Thiomersal
Conservats for IPPs
Silver:
Argenti nitras
Targesin – used for nasal drops (Argenti diacetyltannas
albuminatus)
Halogens
Chlorine: chloramine T - tosylchloramidum natricum
chloramine B - benzylchloramidum natricum
Iodine:
Iodi sol. glycerolica, aquosa, ethanolica
Iodophores, povidone-iodine:
Allergy!
Alcohols, aldehydes, phenols, parabens
ethanol
- 60% (Spiritus dilutus / Ethanolum dilutum)
- 85% (Spir. concentratus / Eth. concentratum)
- 96% (Spir. absolutus / Eth. absolutum)
formaldehyde – solutions and vapors
phenol
parabens – p-hydroxybenzoic acid esters
Soaps, quarternary ammonium salts
- decrease of surface tension
Sapo kalinus, Sapo medicinalis
Benzododecinii bromidum - AJATIN
Carbethopendecinii bromidum - SEPTONEX
- zvlhčuje sliznice
Organic dyes:
• gentian violet- Methylrosanilinii chloridum 0,5-2%
• methylene blue - Methylthioninii chloridum
• brilliant green - Viride nitens
• rivanol – up to 2% - Ethacridinium lacticum
2. Astringents
- protein coagulation ( penetration of inf. agents)
- antiitching, calming, cooling, antiseptic effects
• Aluminii
acetotartratis solutio
(sol. Burrow 8%)
• AgNO3 (0,5-1%)
• natural origin– galla,
Juglans, Hammamelis,
Alchemilla, Agrimonia,
Fragaria, Salvia
• tannines
Indications: burnings, frostbites, fissures,
diarrhoea...
3. Keratolytics / keratoplastics
- help remove defectice - stimulate new skin layers
production
skin layers
- indications: psoriasis,
• ac. salicylicum do 5%
hyperkeratosis
(3%)
• ichthammol, tars– Pix
• Ac. salicylicum nad
lithanthracis, betulae,
5%
fagi
• urea 2-20 %
• tretinoin 0,025-0,05 %
• tretinoin 1-3 %
(temporary deterioration!)
• (tretinoin over 0,1%
inhibits stretch marks)
4. Re- epithelisants, cicatrizants
• hyaluronic acid
•panthotenic acid
• stimulate growth scar
tissue
• dexpanthenol
• AgNO3 to 1 %
• peruvian balm
• salicylic acid 1-2 %
• chlorophyll
• peruvian balm –
allergy!
• chamazulene (Chamomilla -
allergy!)
• benzoylperoxide
(Eclaran®)
• AgNO3 to 1 %
• propolis…
5. Emolients
- short-acting, calming, hydrating, softening skin
- those effects can be stimulated by camphora or menthol
addiction
• liquid paraffin
• Vaselinum album, Vas.flavum
• Sojae oleum raffinatum, Amygdalae ol.
Raffin., Jecoris aselli oleum
• Urea (to10 %) – hydrates, increases skin
penetration of other compounds
6. Acne
- acne vulgaris
- acne rosacea
seborrhoea,  androgens,
hyperkeratosis, bacterial infections
Propionibacterium acnes
Aggravation:
androgens
Candida, funghi
vit. B6, B12
Local: antiseptics - triclosan, hexachlorophene,
benzoylperoxide
retinoids – retinoic acid, tretinoin, isotretinoin
antibiotics - erythromycine, clindamycine
antimycotics: clotrimazole, azelaic acid
Systemic: retinoids - isotretinoin
ATB – doxycycline, minocycline

gestagens in contraception – antiandrogennic
activity (cyproteron acetate, chlormadinone, dienogest,
norgestimate + ethinyl estradiol)
Treatment with glucocorticoids is reserved only for very
serious cases. They can induce acne themselves.
7. Antipsoriatics
Psoriasis – chronic skin disease, 2% of
population, without clear ethiology
(autoimmune)
Predilection sites: knees, eye surrondings, back...
Therapy
Local
Systemic– in serious cases
Local– indifferent vehicles, phototherapy (UVA)
+ ichthammol
+ WEAK corticosteroids- bethamethasone
+ tars (tct. carbonis detergens)
+ salicylic acid 2-3%
+ vit. D3 synthetic analogues (calcitriol,
calcipotriol, tacalcitol)
+ retinoids - calcipotriol, calcitriol, tacalcitol,
tazaroten
Systemic– psoralenes – furanocoumarine
derivatives – a part of PUVA therapy (psoralenes+
UVA), often in bath to saturate the skin and
subsequent phototherapy, mutagens !
- methoxalen
- psoralens are used in alopecia too
- retinoids – acitretin
(serious AE, CI in pregnancy)
In most serious cases immunosuppressants are
administered (ciclosporin)
Systemic biological treatment of psoriasis:
- biologic therapy with Anti TNF
etanercept, infliximab
- antibody against CD11 and LFA-1 subunit
(lymphocyte function – associated antigen)
efalizumab
8. ORL drugs
Nasal antispetics:
Carbethopendecinii bromidum 0,02–0,05% - SPX
Argenti diacetyltannas albuminatus 4–6%
Natrii tetraboras decahydricus 2%,
Boric acid 3%
Decongestants – sympathomimetics:
Naphazolini nitras 0,05-0,1%
Ephedrini hydrochloridum 0,5 -1%
tetryzoline, oxymetazoline, xylomethazoline
Auricularia
Ear wax softeners:
Hydrogenii peroxidum 3%, Ac. boricum
Oils, Paraff. liq., Glycerol 85%, Ethanol
Orofaryngologics
• to treat oral cavity and throat (inflammation,mycosis..)
• solutions, gargles, sprays
• antiphlogistics, antiseptics, astringents, mucolytics,
• antibacterial and antimycotic drugs
Antiphlogistics
Herbal infusions– Salvia off., Chamomilla off.
Corticosteroids- pectin, gelatine, acrylate pastes –
Triamcinolon, Dexamethason
Antibacterial therapy of throat and oral
cavity
 fisrtly atibiotics which are not used systemically
 bactericidal
Fusafungine (Bioparox)
 for local therapy: G+ (streptococci, pneumococci,
staphylococci), Candida a., Mycoplasma pneumoniae
I: tonsilitis, rinitis, sinusitis, tracheitis, laryngitis,
pharyngitis, bronchitis
Hexetidine
bactericidal + fungicidal antibiotic agent
Other antispetics for ORL
 Chlorhexidine digluconas (G+,G-, kvasinky, viry)
 Benzydamine hydrochloridum (weak antiseptic,
antiphlogistic + analgesic activity)
 Benzalkonii chloridum
 Benzoxonium chloridum
 Cetylpyridinium chloridum
 Dichlorobenzenmethanol