Topical Treatment in Dentistry

Iyad Abou Rabii DDS, OMFS, MRes, PhD

QASSIM UNIVERSITY
 Topical Treatment in Dentistry
Iyad Abou Rabii DDS, OMFS, MRes, PhD

Topical Treatment
A term used to describe medicine that has effects only in a specific area, not
throughout the body, particularly medicine that is put directly on the mucosa,
dental, gingival, or pulpal tissues.

Advantage of Topical administration

1. Avoids the GI tract and hepatic first-pass metabolism
2. Reduces systemic side effects
3. Higher concentration of drug at site of application
4. Improves compliance
5. Allows ↑ concentration of Rx at site of application
6. Plasma concentrations of <10% compared to oral route.

Pharmaceutical Forms
Topical medications include
• balms,
• creams,
• gels,
• lotions,
• patches,
• ointments,
• Muscoadhesive tablettes
• and other products that you apply to the mucosa, pulp, and dental tissues.
Most are available over-the-counter..

Topical Antibiotics
Pharmaceutical Forms
Some topical antibiotics are available without a prescription and are sold in
many forms, including creams, ointments, powders, and sprays. Some widely
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used topical antibiotics are bacitracin, neomycin, mupirocin, and polymyxin B.

Among the products that contain one or more of these ingredients are
Bactroban (a prescription item), Neosporin, Polysporin, and Triple Antibiotic
Ointment or Cream.
Antibiotic mouthwash can be prepared by the patient by dissolving the contents
of 250 mg tetracycline capsule in 10 ml of water to give a 2% solution. It may be
more effective to add glycerol to the solution as a demulcent, this must be done
by pharmacist.

Advantages
The value of topical antibiotics overweighs such risks in some cases. Tetracycline
is a useful topical antibiotics. As at 2% solution it’s often effective in reducing

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 secondary infection (and thus the discomfort) in cases of aphtous stomaitis,
primary herpetic stomaitis, and all oral ulcerative conditions.
Use of topical antibiotics is also seen to be helpful in acute chronic gingivitis
treatment.

Disadvantages
There are inherent disadvantages associated with the use of topical antibiotics
because of the possibilities of selection for resistant strains and inducing
hypersensitivity reaction at the patient.

Use of Topical Antibitics

Indication
Topical antibiotics help prevent infections caused by bacteria that get into minor
cuts, scrapes, and burns. Treating minor wounds with antibiotics allows quicker
healing.
They are always used to prevent secondary infection (ulcers)

Duration
The use of topical antibiotics cannot normally be practiced as long- term
treatment, it is better to be reserved for acute episodes. Otherwise, there will be
the risk of overgrowth of resistant organisms, although a candidal infection may
occur. However, in some rare cases a prolonged topical antibiotic treatment is
justified (Patients with severe and persistent oral lesions), in that case a
tetracycline with triamcinolone combination is preferred

Topical antifungal treatment

Antifungal drugs
The polyene antifungal agents, nystatin and amphotericin B, are well
established and relatively free from side-effects when used locally. They are
available in various forms, such as lozenges, pastilles, creams, and suspensions.
Unfortunately, patient compliance is often poor with these preparations, which
may take a while to dissolve in the mouth (for example, pastilles and lozenges)
and have a a distinctive taste.
The newer azoles have very useful properties, although resistance is rather more
commonly met and may be problematic in the future, particularly in the
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immunocompromised patient. (C. krusei and and C. glabrata are usually resistant
to fluconazole.) The locally active agent, miconazole is available as an oral gel or
cream.

Pharmaceutical Forms
Conventional
In order to assure topic application of antifungal agents, conventional lozenge,
mouthwash, or gel would be the simplest dosage forms for the delivery of drugs
in the buccal cavity, but these conventional dosage forms had the disadvantage
of an initial burst of salivary concentration followed by a rapid decrease. A
lozenge produced effective salivary drug levels for more than one hour but
repeated administration was restricted due to systemic toxicity coming from the

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large quantity of ingested drug. The action of mouthwashes was even more
transient than that of lozenges, and gels/pastes were difficult to retain in the
mouth .
Sustained Release forms
In case of oral fungal infections, a prolonged therapy with antifungal agent was
required, and some papers documented prolonged release of antifungal agent
from buccal devices in the form of an adhesive tablets.
I.Abou Rabii et al (2004, France) has developped a Miconazole musoadhesive
tablette which has been given higher concentration of Miconazole in Saliva
(Over the IMC for more than 9h).

Topical antifungal therapy

Pseudomembranous, erythematous hyperplastic candidosis
Amphotericin lozenges (10 mg)
Nystatin pastilles (100 000 units)
Dissolve slowly in mouth, after meals; use 4 times daily;

Candida-asso ciated denture stomatitis

Amphotericin or nystatin (as above) and remove dentures
Miconazole gel applied to palatal surface of denture 4 times daily for 1 to 4
weeks
Chlorhexidine 0.2% rinse, 4 times daily (do not use with nystatin)

Candida-asso ciated angular cheilitis

Nystatin cream; apply to corners of mouth 3 to 4 times daily, until resolution
Miconazole cream (or gel); apply 3 to 4 times daily to angles

Topical Antiseptics
First Generation
Many substances with some degree of antimicrobial efficacy have been tested,
especially in vitro, but it is totally impractical to ask everybody to rinse his or her
mouth ten times a day, because the solution is completely devoid of
substantivity, and rapidly diluted by and swallowed with saliva.
The agents that do not exhibit any significant substantivity (only minutes) were
categorized as first-generation antimicrobial agents and are composed of certain
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antibiotics,

quaternary ammonium compounds (cetylpyridinium chloride),

essential oil phenolic compounds

fluorides including monofluorophosphate

and sodium fluoride,

oxidizing agents,

plant alkaloids and iodines including povidone

iodine

Second Generation

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 Second-generation antimicrobial agents are characterized by high substantivity,
that is, retention of 25-30% after each 1-minute mouthrinse. Such compounds
remain active in situ for hours and include

bisbiguanides (such as chlorhexidine),

amine fluoride and stannous fluoride mouthrinse,

triclosan when associated with a copolymer of polyvinyl methyl ether and
maleic acid copolymer.

Chlo rhexidine
The most tested and effective antiplaque agent known today is chlorhexidine,
which has been used for more than two decades. The mode of action of
chlorhexidine against bacteria is well understood and is concentration
dependent.
• Chlorhexidine has antibacterial and some anticandidal activity and currently
the most effective antiplaque agent.It can be used as a mouthwash, spray,
or gel to control secondary infections in mucosal ulcerations.
• Chlorhexidine acts on the cell wall of the microorganisms by changing their
surface structures. Osmotic equilibrium is lost and, as a consequence,
cytoplasmic membrane is extruded, vesicles are formed and the cytoplasm
precipitates.
• Because chlorhexidine has been shown to be able to break up existing
dental plaque, it can really be considered as a potent antibacterial agent,
bactericidal at high concentration and bacteriostatic at lower
concentration, such as when gradually diluted in saliva over time.
Local Side effects of Chlorhexidine
• Chlorhexidine has been reported to originate some reversible local side
effects:
• Taining on teeth and tongue appears largely dose dependent whereas
desquamation of the oral mucosa and perturbation of the taste appear to
be largely concentration dependent.

Topical Steroids
Indication
• Topical corticosteroids are frequently used in management of the oral
mucodermatoses and other conditions. Topical steroids are frequently
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included in potential predisposing factors of oral candidiasis. Secondary oral

candidiasis is of particular importance in patients being treated for oral
mucosal disease. Candidiasis will aggravate the existing oral condition and
may prevent successful treatment unless it is recognized and managed.

Forms
• Hydrocortisone hemisuccinate (pellets)
• Triamcinolone acetonide (in adhesive paste)
• Fluocinonide (in adhesive paste)
• Betamethasone sodium phosphate (mouthwash)
• Triamcinolone mouthwash
• Beclomethasone dipropionate (spray)

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 • Budesonide (spray)

Topical Analgesics
Indication
• in all painful oral conditions (burns, inflammation, ulcers. etc)
• Before Syringe injection in children
• Topical anesthetic faces two main hurdles
1.Laryngeal reflexes : a further precaution to be taken includes the
avoidance of preparations of sufficient strength to affect the laryngeal
reflexes
2.The effectiveness of these Topical oral anesthetic drugs is typically
hampered by the rapid dissolution of the carrier matrix. In the Saliva

Forms
Benzydamine hydrochloride (mouthwash)
Lignocaine rinse
Ligocaine hydrochloride spray
Benzocaine Gel

Fluoride as Topical drug

The use of fluoride toothpastes, mouthrinses, gels or varnishes reduces tooth
decay in children and adolescents.
Fluoride is a mineral that prevents tooth decay.
Children aged 5 to 16 years are applied fluoride in the form of toothpastes,
mouthrinses, gels or varnishes ,
Fluoride varnishes may have a greater effect but more high quality research is
needed to be sure of how big a difference these treatments make, and whether
they have adverse effects.

[‫ | ]اﺧﱰ اﻟﺘﺎرﻳﺦ‬Topical Treatment in Dentistry