Topical drugs in dentistry


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Topical drugs in dentistry

  1. 1. Topical Treatment in Dentistry Iyad Abou Rabii DDS, OMFS, MRes, PhD QASSIM UNIVERSITY
  2. 2. Topical Treatment in Dentistry Iyad Abou Rabii DDS, OMFS, MRes, PhDTopical TreatmentA term used to describe medicine that has effects only in a specific area, notthroughout 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 AntibioticsPharmaceutical FormsSome topical antibiotics are available without a prescription and are sold inmany forms, including creams, ointments, powders, and sprays. Some widely [‫ | ]اﺧﱰ اﻟﺘﺎرﻳﺦ‬Topical Treatment in Dentistryused topical antibiotics are bacitracin, neomycin, mupirocin, and polymyxin B.Among the products that contain one or more of these ingredients areBactroban (a prescription item), Neosporin, Polysporin, and Triple AntibioticOintment or Cream.Antibiotic mouthwash can be prepared by the patient by dissolving the contentsof 250 mg tetracycline capsule in 10 ml of water to give a 2% solution. It may bemore effective to add glycerol to the solution as a demulcent, this must be doneby pharmacist.AdvantagesThe value of topical antibiotics overweighs such risks in some cases. Tetracyclineis a useful topical antibiotics. As at 2% solution it’s often effective in reducing 1
  3. 3. 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[‫ | ]اﺧﱰ اﻟﺘﺎرﻳﺦ‬Topical Treatment in Dentistry 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 the2
  4. 4. large quantity of ingested drug. The action of mouthwashes was even moretransient than that of lozenges, and gels/pastes were difficult to retain in themouth .Sustained Release formsIn case of oral fungal infections, a prolonged therapy with antifungal agent wasrequired, and some papers documented prolonged release of antifungal agentfrom buccal devices in the form of an adhesive tablets.I.Abou Rabii et al (2004, France) has developped a Miconazole musoadhesivetablette which has been given higher concentration of Miconazole in Saliva(Over the IMC for more than 9h).Topical antifungal therapyPseudomembranous, erythematous hyperplastic candidosisAmphotericin lozenges (10 mg)Nystatin pastilles (100 000 units)Dissolve slowly in mouth, after meals; use 4 times daily;Candida-asso ciated denture stomatitisAmphotericin or nystatin (as above) and remove denturesMiconazole gel applied to palatal surface of denture 4 times daily for 1 to 4weeksChlorhexidine 0.2% rinse, 4 times daily (do not use with nystatin)Candida-asso ciated angular cheilitisNystatin cream; apply to corners of mouth 3 to 4 times daily, until resolutionMiconazole cream (or gel); apply 3 to 4 times daily to anglesTopical AntisepticsFirst GenerationMany 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 hermouth ten times a day, because the solution is completely devoid ofsubstantivity, and rapidly diluted by and swallowed with saliva.The agents that do not exhibit any significant substantivity (only minutes) werecategorized as first-generation antimicrobial agents and are composed of certain [‫ | ]اﺧﱰ اﻟﺘﺎرﻳﺦ‬Topical Treatment in Dentistryantibiotics, quaternary ammonium compounds (cetylpyridinium chloride), essential oil phenolic compounds fluorides including monofluorophosphate and sodium fluoride, oxidizing agents, plant alkaloids and iodines including povidone iodineSecond Generation 3
  5. 5. 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[‫ | ]اﺧﱰ اﻟﺘﺎرﻳﺦ‬Topical Treatment in Dentistry 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)4
  6. 6. • Budesonide (spray)Topical AnalgesicsIndication • 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 SalivaForms Benzydamine hydrochloride (mouthwash) Lignocaine rinse Ligocaine hydrochloride spray Benzocaine GelFluoride as Topical drugThe use of fluoride toothpastes, mouthrinses, gels or varnishes reduces toothdecay 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 isneeded to be sure of how big a difference these treatments make, and whetherthey have adverse effects. [‫ | ]اﺧﱰ اﻟﺘﺎرﻳﺦ‬Topical Treatment in Dentistry 5