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ANALGESICS AND ANTIBIOTICS10/22/20101

Analgesics and Antibiotics110/22/20102Definition of Analgesia :Absence of pain in response to stimulus that would normally be painful . International Association for the Study of Pain Subcommittee on Taxonomy (1986)

Analgesics and Antibiotics10/22/20103IntroductionPain has always been a barrier to dentistry serving as a continuing motivation for the use of drugs to prevent or block or attenuate pain in the Perioperative period.

The WHO recommends a pain ladder for managing analgesia which was first described for use in cancer pain, but can be used by medical professionals as a general principle when dealing with analgesia for any type of pain.

Mild pain : Paracetamol (acetaminophen) , or a NSAID drug like Ibuprofen.

Mild to moderate pain : Paracetamol, an NSAID and/or paracetamol in a combination product with a weak opiod such as Hydrocodone used in combination, may provide greater relief than their separate use.

Moderate to severe pain : Morphine is the Gold standards to which all the narcotics are compared. Fentanyl has a benefit of less histamine release and fewer side effects.Analgesics and Antibiotics10/22/2010Analgesics and Antibiotics4

10/22/20105Pain ManagementPain Management can be done by various techniques:DrugsAudio analgesiaAcupunctureTENS transcutaneous electrical nerve stimulationLLLT- low level laser therapy

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AcupunctureTranscutaneous Electrical Nerve StimulationLow Level Laser Treatment10/22/20107CLASSIFICATION : BASED ON SITE OF ACTION :

CENTRALLY ACTING /OPIOID ANALGESICS. Eg. Morphine

PERIPHERALLY ACTING ANALGESICS/ NON OPIOID/NSAIDs. Eg. Ibuprofen

Centrally acting analgesics are further classified based on their origin:

Naturally occurring opioid. Eg. Morphine

Synthetic opioid . Eg. Pethidine

These are more effective against acute pain but have a greater incidence of adverse effects.Are usually administered parenterally and are devoid of Anti-inflammation and Anti-pyretic effects.Serious drug dependence and abuse liability has limited their use in Pedodontics.

Analgesics and Antibiotics10/22/20108USES OF OPIOIDS IN DENTISTRY Although morphine and related analgesics are widely used in relieving pain , their dental application is limited.

Most types of dental pain , such as dry socket , or pericoronitis , can be effectively treated by local measures , so the dentist is unlikely to prescribe opioids for these conditions.

However such pain has a major inflammatory component and , as the opioids possess no anti-inflammatory component , their efficacy is doubtful in this contextAnalgesics and Antibiotics10/22/20109NSAIDs is classified under the following categories :Non-selective COX inhibitors (conventional NSAIDs) a. Salicylates : Aspirin b. Propionic acid derivatives : Ibuprofen , Naproxen , Ketoprofen c. Anthranilic acid derivative: Mefenamic acid d. Aryl-acetic acid derivative : Diclofenac e. Oxicam derivatives: Piroxicam , Tinoxicam f. Pyrolo-pyrrole derivative : Ketorolac g. Indole derivative: Indomethacin h. Pyrazolone derivatives: Phenylbutazone , Oxyphenbutazone.

Preferential COX-2 inhibitors Nimesulide ,Meloxicam ,Nabumetone

Selective COX-2 inhibitors Celecoxib ,Rofecoxib ,Valdecoxib ,Etoricoxib

Analgesic- Antipyretics with poor anti-inflammatory action a. Para-amino phenol derivative: Paracetamol(Acetaminophen) b. Pyrazole derivatives: Metamizol (Dipyrone) ,Propiphenazone c. Benzoxacine derivative : Nefopam

Analgesics and Antibiotics10/22/201010SalicylatesSalicylates are among the oldest known drugs.Hippocrates recommended the consumption of the juices of poplar and willow bark some 2400 years ago ,which later were discovered to contain salicin ,for the treatment of the pain of childbirth.Today it remains one of the most consumed drugs in the world.Salicylates formed: AcetylSalicylic Acid (Aspirin) , Choline Salicylate ,Magnesium Salicylate and their combinations.Mechanism of Action: Inhibit COX-1 and 2 Pathway.

ASPIRIN

Pharmacodynamics:Inhibit COX1 and COX2 pathway

Pharmacokinetics:Half-life in humans is 20-30minsMetabolised in liverProtein binding: 99.6%Excretion: Renal

Analgesics and Antibiotics10/22/201011Dose and Dosage (children) : Oral and also RectalNot prescribed in children below 12years.Children above 12years 300mg/ 4hours.

Indications :AnalgesiaInflammation Fever (pyrexia)Acute rheumatic feverRheumatoid arthritisOsteoarthritisPost myocardial infarction and post stroke patients.

ContraindicationsPatients sensitive to aspirinPeptic ulcersBleeding tendenciesDiabetesPregnancyG-6-PDDental extractionsProhibited in India and UK due to risk of Reye Syndrome.

Analgesics and Antibiotics

10/22/201012Precautions (Some drug interactions involving Aspirin)

Warfarin Internal bleeding ,possible haemorrhageHeparin Internal bleeding ,possible haemorrhageInsulin Aspirin may cause hyperglycemia or hypoglycemiaSulfonylureas Enhancement of hypoglycemic effectPhenytoin Increased free plasma conc. of phenytoin ,valproic acid Methotrexate Increased free plasma concentration of methotrexateEthanol Internal bleeding ,possible haemorrhageProbenic acid ,sulfinpyrazone Decreased uricosuric effect ,reappearance of goutACE inhibitors ,-adrenergic Loss of anti-hypertensive effect blockers ,diuretics

Trade Names

ASPIRIN 350MG TABCOLSPRIN- 100 ,325 ,650MG TABECOSPRIN- 75 ,150 ,325MG TABDISPRIN- 350MG TABLOPRIN- 75 ,162.5 MG TAB

Analgesics and Antibiotics10/22/201013Propionic Acid DerivativesAmong the NSAIDs , this class of drugs are considered to be largest alternative to Aspirin.The short term use of these drugs is available without a prescription for relief of headache, fever ,dysmenorrhea and mild to moderate musculoskeletal and postoperative pain.

IBUPROFENMost commonly used propionic acid derivative drug used in paediatric dentistry.

PharmacodynamicsThought to inhibit cycloxygenase, an enzyme needed for prostaglandin synthesis.

PharmacokineticsProtein binding :99%Metabolism: HepaticHalf life: 1.8-2 hoursExcretion: Renal

Analgesics and Antibiotics10/22/201014Route and Dosage : Route : Oral ,rectal ,topical ,IVDosage: 40mg/kg max (for children aged 6-12 yrs)

Indications:Mild to moderate painFeverJuvenile arthritisWhen used in patients treated with corticosteroids ,these agents may permit reduction of the steroid dose.

Contraindications:Hypersensitivity to the drugPregnancy

Precautions to be taken: severe cardiovascular, renal, or hepatic disease; GI disease; asthma; chronic alcohol use elderly patients breastfeeding patients.

Analgesics and Antibiotics

10/22/201015Trade NamesBRUFENEMFLAMIBUSYNTHIBUGENSIC - 100MG/5ML SUSPENSION 200 ,400 ,600MG TAB

Analgesics and Antibiotics10/22/201016ParacetamolThe so-called coal tar analgesics , are all analine derivatives.An active metabolite of 2 drugs discovered was realized to be a better analgesic which was none other than Nacetyl-p-aminophenol or paracetamol or Tylenol (USA) or AcetaminophenThis is now one of the widest group of analgesic used worldwide.It is a poor inhibitor of PG synthesis but a more active on COX in brain.

Kinetics:

Orally absorbedPlasma protein binding : 1/3rd of the total.Plasma half life: 2-3 hours

Indications:

Headache ,tooth ache - AnalgesicPyrexia- one of the best drug.Teething

Analgesics and Antibiotics10/22/201017Contraindications:

HypersensitivitySevere liver diseases

Adverse effects:

Acute paracetamol poisoning

Dosage:

10-15mg/kg/dose every 6-8 hours as needed.

Trade Names:

CrocinMetacinCalpol

Analgesics and Antibiotics

10/22/201018FenamatesMefenamic AcidAn analgesic-antipyretic-anti-inflammatory drug . Inhibits PG synthesis and has a short lasting antiplatelet actionNeutrophil chemotaxis and superoxide production at the inflammatory site are reduced.

Pharmacodynamics:Thought to block activity of cyclooxygenase, thereby inhibiting inflammatory responses of vasodilation and swelling and blocking transmission of painful stimuli.

Pharmacokinectics:Protein binding: 90%Metabolism: HepaticHalf life: 2hoursExcretion : Renal and faecal

Analgesics and Antibiotics10/22/201019Route and Dosage:Route: OralDosage: 500 mg, followed by 250 mg every 6 h as needed. Usually not used more than 1 wk in children above the age of 14years.

Indications:Acute painPrimary dysmenorrhea

ContraindicationsAllergic to the drug, NSAIDsPre-existing renal diseaseActive ulcerationChronic inflammation of GI tract

Precautions:PregnancyChildren below the age of 14ElderlyHypersensitivtyRenal function

Analgesics and Antibiotics

10/22/201020DiarrhoeaGI Toxicity

Trade NamesPonstel, Ponstan, Ponstal, Parkemed, Mafepain, Mephadolor, Meftal, Dyfenamic, Potarlon, Dolfenal, Meyerdonal, Alfoxan.

Analgesics and Antibiotics10/22/201021ANTIBIOTICSDefinition: Antibiotics are chemical substances elaborated by various species of micro-organisms such as fungi, actinomycetes and bacteria, which suppress the growth of other micro-organisms and may ultimately destroy them. From Clinical Use of Antibiotics : A Rationale

Analgesics and Antibiotics10/22/201022ClassificationBased on Mechanism Of Action:

Drugs that inhibit bacterial cell wall Eg. Betalactems: Penicillin and Cephalosporins

Drugs that affect cell membrane permeability Eg. Antifungals : Nystatin and Amphotericin B

Drugs that affect Bacterial Ribosome (50S) sub unit Eg. Chloramphenicol , Erythromycin , and Tetracyclines

Drugs that bind to 30S Ribosomal sub unit Eg. Aminoglycoside- Streptomycin and Gentamicin

Agents that affect Nucleic Acid Metabolism Eg. Rifampicin ,Nalidixic acid ,Metronidazole and Quinolones

Analgesics and Antibiotics10/22/201023Commonly used Antibiotics in ChildrenAMOXICILLIN

Category: Extended Spectrum amino penicillins Bacteriocidal action.Acid stable, Beta lactamase sensitiveInhibits cell wall synthesis

Spectrum: Both gram positive and negative organismsHaemophilus , E.COli ,Salmonella ,and ShigellaIneffective against Staphylococci and destroyed by Betalactamase.

Kinetics:Food does not interfere with absorption4mcg/ml in 2 hours with 250mg doseOral bioavailability-93%Urinary excretion: 50% in 6-8 hoursPlasma protein binding : 18%

Analgesics and Antibiotics10/22/201024Rapid distribution except into CSFProbenicid delays urinary excretion.

Indications:

Upper and lower respiratory tract infectionsUrinary tract infectionsBacterial meningitis - Enteric FeverSepticaemia - infective EndocarditisGonorrhoea Urethritis

Contraindications:

Penicillin allergy

Adverse Reactions:

Well tolerated Diarrhoea less frequentAllergic skin rashes

Analgesics and Antibiotics10/22/201025Dosage :

Children : 20-50mg/kg/day in 3 divided dosesParenterally : 50-100mg/kg/day Im in 3 divided dosesGonorrhea : 3G+Probenicid

Trade Names:

NOVAMOXINTORMOXIN (INDIA)CILAMOX

Analgesics and Antibiotics

10/22/201026AMOXICILLIN+CLAVULANATE POTASSIUM Co-Amoxiclav is the British Approved Name for the combination of antibiotic containing amoxicillin trihydrate , a -lactam antibiotic, with potassium clavulanate , a lactamase inhibitor .This combination results in an antibiotic with an increased spectrum of action and restored efficacy against amoxicillin resistant bacteria that produce lactamase.

Category: Broad spectrum antibiotic and is efficient against amoxicillin resistant bacteria.

Spectrum:Haemophillus spp.Streptococcus spp.Veilonella spp.

Indications:

Infections of ear , lung , sinus , and urinary tract , dental and animal bites.

Analgesics and Antibiotics10/22/201027Contraindications:

Allergy to penicillinPregnancyOral contraceptives

Adverse Effects:

DiarrhoeaStomach upsetVomiting Mild skin rash

Dosage:

For children 6-12 years: co-amoxiclav 250/62 in 5ml suspension 3 times dailyFor children 1-6 years : co-amoxiclav 125/31 in 5ml suspension 3 times daily

Analgesics and Antibiotics

10/22/201028Trade names:

AMOXYCILLIN CLAVULANATECO-AMOXICLAVAUGMENTIN

Analgesics and Antibiotics10/22/201029AMPICILLINCategory:

An amino penicillin with broad spectrum bacteriocidal actionAcid stable but beta lactamase sensitiveInhibits cell wall sysnthesis

Spectrum:

Gram positive oraganisms and negative organisms such as Haemophilus , E. COli , Salmonella , Shigella , and Proteus Mirabilis.Beta lacatamase destrys activityIneffective against Staphylococcus

Kinetics:

Orally absorbedBioavailability : 62%Urinary excretion 82% after 6 hoursPlasma protein binding: 18% (reduced in cirrhosis and pregnancy)Plasma half life : 1.3 hoursProbenicid delays urinary excretion.Analgesics and Antibiotics10/22/201030Indications:

Respiratory tract infectionsBacterial meningitis- septicaemiaInfective endocarditisUrinary tract infectionsEnteric fever

Contraindications:

Allergy to penicillin

Adverse Reactions

Allergic skin rashes MaculopapularDiarrhoea ColitisSuperinfections

Interactions :

Food interferes with absorption

Analgesics and Antibiotics10/22/201031Dosage:

Children: 50-200mg/kg/day in 4 divided dosesParenteral: 25-50mg/kg/day in 4 divided dosesGonorrhoea: 3.5G+Probenicid

Trade Names:

PrincipenOmnipenTotacillin-N

Analgesics and Antibiotics

10/22/201032CephalexinCategory:

First generation Cephalosporin that is orally bacteriocidal against broad spectrum of organisms.Acts by cell wall synthesis inhibition.

Spectrum:

Gram positive and gram negative organismsStrepto.Staph.Nisseria andE coli

Kinetics:

Plasma protein binding 15%Crosses placenta and present in breast milkNot metabolised in bodyPlasma half life 1.5 hours

Analgesics and Antibiotics10/22/201033Primarily excreted by the kidneys 80% in 6 hoursProbenicid delays excretion.

Indications:

Infections of respiratory and urinary tract infections

Contraindication:

Allergy to cephalosporinsRenal impairmentPregnancy

Adverse Reactions:

GIT: nausea ,vomiting ,diarrhoea ,abdominal discomfortAllergic skin rashesEosinophiliaNeutropeniaSuperinfection with candida

Interactions: food delays absorption.

Analgesics and Antibiotics10/22/201034Dosage:

12.5-25mg/kg orally every 6 hours otitisEvery 12 hours pharyngitis and soft tissue infection.

Trade names:

KeflexPanixineBiocefZartan

Analgesics and Antibiotics

10/22/201035CotrimoxazoleCategory:

It is a combination of Trimethoprim (Dihydro Folate Reductase) and Sulfamethaxozole (Sulfonamide- Inhibit bacterial folate synthesis).

Spectrum:

Gram positive and negative bacteria like staph , shigellaProtozoan (toxoplasmosis)Fungal (pneumocystosis carinii)

Kinetics:

Plasma half life 10hoursPlasma protein binding 40%Metabolised in liveExcreted in urine

Analgesics and Antibiotics10/22/201036Indications:

Upper and lower respiratory tract infectionsRenal and urinary tract infectionsGIT infectionsSkin and wound infectionsSepticemia Contrindications:

Hypersensitivity to the drugMegaloblastic anaemia caused due to folate deficiencyRenal insufficiencyInfants younger than 2 months of agePregnancy

Adverse Reaction:

Mild allergic reactionsSteven johnsons syndrome

Analgesics and Antibiotics10/22/201037Dosage:

Children 2 months of age or older: IV 8-12mg/kg in equally divided doses for every 6 hrPO 8-12mg/kg in equally divided doses for every 12 hours

Trade names:

Bactrim DSApo-Sulfatrim DSNu-Cotrimox

Analgesics and Antibiotics

10/22/201038ErythromycinErythromycin is a macrolide antibiotic- primarily bacteriostatic which acts by interfering with bacterial protein synthesis , by binding 50S ribosome sub unit.

Spectrum:

Gram positive bacteria: strep pyogens , Strep pneumoniae ,Nisseria ,Haemophilus ,Clostridium ,Treponema and bacteriodes mycoplasma pneumoniae ,and Legionella pneumophills.

Kinetics:

Plasma protein binding: 65-90%Crosses placentaPlasma half life: 1.9-2.1hoursMetabolised in liverExcreted in bile

Analgesics and Antibiotics10/22/201039Indications:

Upper and lower respiratory tract infectionsSkin and soft tissues infectionsDiphtheria , Pertusis- Otitis media

Contra Indications:

Hypersensitivity to the drug.

Adverse Reactions:

GI side effects: liver functionsRenal failurePorphyria

Dosage:

Children: 30-50mg/kg in divided doses

Trade Names: Ery-Tab , PCE Dispertab ,EES Granules

Analgesics and Antibiotics

10/22/201040MetronidazoleIs found to be a broad spectrum anti-protozoal against Entamoeba histolytica.Its efficacy in anaerobic infections was a chance of discovery and is now extensively used to treat oral and other anaerobic infections.Mechanism of action: Dna helix destabilisation and strand breakage.

Spectrum: Many anaerobic bacteria such as

Bact. FragilisBact. MelaninogenicusFusobacteriumCl. PerfringensCl. DifficilePeptococcusPeptostreptococcusPrevotellaVeillonellaCampylobacter

Analgesics and Antibiotics10/22/201041Kinetics:

Plasma protein bindingPlasma half life: 6-7 hoursMetabolized in liverExcreted through kidneys and bile

Indications:

Infections of stomach ,skin , joints and respiratory tract , oral cavityPeptic ulcer disease

Contraindications:

Allergy to the drugLiver diseaseStomach or intestinal disease such as Crohns diseasePregnancy

Analgesics and Antibiotics10/22/201042Adverse Effects:

Nausea , anorexia , bitter or metallic taste.Less frequent side effects: headache ,glossitis ,dryness of mouth ,dizziness ,rashesProlonged admin: Seizures ,numbness or tingling in hands and feet.SJ Syndrome when combined with mebendazole

Dosage:

15mg/kg 3 times a day

Trade Names:

Flagyl

Analgesics and Antibiotics

10/22/201043Dose CalculationClarks Rule:

Child weight in lb 150*Adult dose = Child dose2. Youngs Rule

Age of childAge + 12*Adult dose = Child dose3. Anders in 1992

Dose a= Dose p * { wt. pd }{wt. ad}0.7Index Dose a = adult doseDose p = child doseWt. pd= wt of childWt. ad= wt of adultAnalgesics and Antibiotics10/22/201044References:

Clinical Use of Antibiotics- A Rationale R.S Nadig

Essentials of Pharmacology for Dentistry- KD Tripathi

Pharmacology and Therapeutics for Dentistry- Yagiela ,Dowd ,Neidle

Pharmacology and Dental Therapeutics- Robin Seymour ,Meechan , Yates

Textbook of Pedodontics- Shobha Tandon

www. wikipedia.org

www.drugs.comAnalgesics and Antibiotics