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Pain 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. 1. Mild pain : Paracetamol (acetaminophen) , or a NSAID drug like Ibuprofen. 2. 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.
3. 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.
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Pain Management can be done by various techniques: Drugs Audio analgesia Acupuncture TENS transcutaneous electrical nerve stimulation LLLT- low level laser therapy
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Acupuncture
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Centrally acting analgesics are further classified based on their origin: Naturally occurring opioid. Eg. Morphine
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 context
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NSAIDs is classified under the following categories : 1. 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. 2. Preferential COX-2 inhibitors Nimesulide ,Meloxicam ,Nabumetone 3. Selective COX-2 inhibitors Celecoxib ,Rofecoxib ,Valdecoxib ,Etoricoxib
4. Analgesic- Antipyretics with poor anti-inflammatory action a. Para-amino phenol derivative: Paracetamol(Acetaminophen) b. Pyrazole derivatives: Metamizol (Dipyrone) ,Propiphenazone c. Benzoxacine derivative : Nefopam
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Salicylates 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 20-30mins Metabolised in liver Protein binding: 99.6% Excretion: Renal
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Dose and Dosage (children) : Oral and also Rectal Not prescribed in children below 12years. Children above 12years 300mg/ 4hours. Indications : Analgesia Inflammation Fever (pyrexia) Acute rheumatic fever Rheumatoid arthritis Osteoarthritis Post myocardial infarction and post stroke patients. Contraindications Patients sensitive to aspirin Peptic ulcers Bleeding tendencies Diabetes Pregnancy G-6-PD Dental extractions Prohibited in India and UK due to risk of Reye Syndrome.
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Warfarin Heparin Insulin Sulfonylureas Phenytoin Methotrexate Ethanol Probenic acid ,sulfinpyrazone ACE inhibitors ,-adrenergic blockers ,diuretics
Internal bleeding ,possible haemorrhage Internal bleeding ,possible haemorrhage Aspirin may cause hyperglycemia or hypoglycemia Enhancement of hypoglycemic effect Increased free plasma conc. of phenytoin ,valproic acid Increased free plasma concentration of methotrexate Internal bleeding ,possible haemorrhage Decreased uricosuric effect ,reappearance of gout Loss of anti-hypertensive effect
Trade Names ASPIRIN 350MG TAB COLSPRIN- 100 ,325 ,650MG TAB ECOSPRIN- 75 ,150 ,325MG TAB DISPRIN- 350MG TAB LOPRIN- 75 ,162.5 MG TAB
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Among 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.
Most commonly used propionic acid derivative drug used in paediatric dentistry. Pharmacodynamics Thought to inhibit cycloxygenase, an enzyme needed for prostaglandin synthesis. Pharmacokinetics Protein binding :99% Metabolism: Hepatic Half life: 1.8-2 hours Excretion: Renal
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Route and Dosage : Route : Oral ,rectal ,topical ,IV Dosage: 40mg/kg max (for children aged 6-12 yrs) Indications: Mild to moderate pain Fever Juvenile arthritis When used in patients treated with corticosteroids ,these agents may permit reduction of the steroid dose. Contraindications: Hypersensitivity to the drug Pregnancy Precautions to be taken: severe cardiovascular, renal, or hepatic disease; GI disease; asthma; chronic alcohol use elderly patients breastfeeding patients.
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The 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 Acetaminophen This 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 absorbed Plasma protein binding : 1/3rd of the total. Plasma half life: 2-3 hours Indications:
Headache ,tooth ache - Analgesic Pyrexia- one of the best drug. Teething
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Contraindications: Hypersensitivity Severe liver diseases Adverse effects: Acute paracetamol poisoning Dosage:
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An analgesic-antipyretic-anti-inflammatory drug . Inhibits PG synthesis and has a short lasting antiplatelet action Neutrophil 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: Hepatic Half life: 2hours Excretion : Renal and faecal
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Route and Dosage: Route: Oral Dosage: 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.
Diarrhoea GI Toxicity Trade Names Ponstel, Ponstan, Ponstal, Parkemed, Mafepain, Mephadolor, Meftal, Dyfenamic, Potarlon, Dolfenal, Meyerdonal, Alfoxan.
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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
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Based on Mechanism Of Action: A. Drugs that inhibit bacterial cell wall Eg. Betalactems: Penicillin and Cephalosporins B. Drugs that affect cell membrane permeability Eg. Antifungals : Nystatin and Amphotericin B
C. Drugs that affect Bacterial Ribosome (50S) sub unit Eg. Chloramphenicol , Erythromycin , and Tetracyclines
D. Drugs that bind to 30S Ribosomal sub unit Eg. Aminoglycoside- Streptomycin and Gentamicin E. Agents that affect Nucleic Acid Metabolism Eg. Rifampicin ,Nalidixic acid ,Metronidazole and Quinolones
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1. AMOXICILLIN Category:
Extended Spectrum amino penicillins Bacteriocidal action. Acid stable, Beta lactamase sensitive Inhibits cell wall synthesis
Spectrum:
Both gram positive and negative organisms Haemophilus , E.COli ,Salmonella ,and Shigella Ineffective against Staphylococci and destroyed by Betalactamase.
Kinetics:
Food does not interfere with absorption 4mcg/ml in 2 hours with 250mg dose Oral bioavailability-93% Urinary excretion: 50% in 6-8 hours Plasma protein binding : 18%
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Indications:
Upper and lower respiratory tract infections Urinary tract infections Bacterial meningitis - Enteric Fever Septicaemia - infective Endocarditis Gonorrhoea Urethritis
Contraindications:
Penicillin allergy
Adverse Reactions:
Well tolerated Diarrhoea less frequent Allergic skin rashes
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Dosage :
Children : 20-50mg/kg/day in 3 divided doses Parenterally : 50-100mg/kg/day Im in 3 divided doses Gonorrhea : 3G+Probenicid
Trade Names:
NOVAMOXIN TORMOXIN (INDIA) CILAMOX
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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.
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Contraindications:
Allergy to penicillin Pregnancy Oral contraceptives
Adverse Effects:
Diarrhoea Stomach upset Vomiting Mild skin rash
Dosage:
For children 6-12 years: co-amoxiclav 250/62 in 5ml suspension 3 times daily For children 1-6 years : co-amoxiclav 125/31 in 5ml suspension 3 times daily
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Trade names:
AMOXYCILLIN CLAVULANATE CO-AMOXICLAV AUGMENTIN
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Category:
An amino penicillin with broad spectrum bacteriocidal action Acid stable but beta lactamase sensitive Inhibits cell wall sysnthesis
Spectrum:
Gram positive oraganisms and negative organisms such as Haemophilus , E. COli , Salmonella , Shigella , and Proteus Mirabilis. Beta lacatamase destrys activity Ineffective against Staphylococcus
Kinetics:
Orally absorbed Bioavailability : 62% Urinary excretion 82% after 6 hours Plasma protein binding: 18% (reduced in cirrhosis and pregnancy) Plasma half life : 1.3 hours 4/23/2014 Analgesics and Antibiotics Probenicid delays urinary excretion.
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Indications:
Respiratory tract infections Bacterial meningitis- septicaemia Infective endocarditis Urinary tract infections Enteric fever
Contraindications:
Allergy to penicillin
Adverse Reactions
Allergic skin rashes Maculopapular Diarrhoea Colitis Superinfections
Interactions :
Food interferes with absorption
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Dosage: Children: 50-200mg/kg/day in 4 divided doses Parenteral: 25-50mg/kg/day in 4 divided doses Gonorrhoea: 3.5G+Probenicid
Trade Names:
Principen Omnipen Totacillin-N
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Category:
First generation Cephalosporin that is orally bacteriocidal against broad spectrum of organisms. Acts by cell wall synthesis inhibition.
Spectrum:
Gram positive and gram negative organisms Strepto. Staph. Nisseria and E coli
Kinetics:
Plasma protein binding 15% Crosses placenta and present in breast milk Not metabolised in body Plasma half life 1.5 hours 4/23/2014 Analgesics and Antibiotics
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Indications:
Infections of respiratory and urinary tract infections
Contraindication:
Allergy to cephalosporins Renal impairment Pregnancy
Adverse Reactions:
GIT: nausea ,vomiting ,diarrhoea ,abdominal discomfort Allergic skin rashes Eosinophilia Neutropenia Superinfection with candida Interactions: food delays absorption.
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Dosage:
12.5-25mg/kg orally every 6 hours otitis Every 12 hours pharyngitis and soft tissue infection.
Trade names:
Keflex Panixine Biocef Zartan
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Category:
It is a combination of Trimethoprim (Dihydro Folate Reductase) and Sulfamethaxozole (Sulfonamide- Inhibit bacterial folate synthesis).
Spectrum:
Gram positive and negative bacteria like staph , shigella Protozoan (toxoplasmosis) Fungal (pneumocystosis carinii)
Kinetics:
Plasma half life 10hours Plasma protein binding 40% Metabolised in live Excreted in urine
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Indications:
Upper and lower respiratory tract infections Renal and urinary tract infections GIT infections Skin and wound infections Septicemia
Contrindications:
Hypersensitivity to the drug Megaloblastic anaemia caused due to folate deficiency Renal insufficiency Infants younger than 2 months of age Pregnancy
Adverse Reaction:
Mild allergic reactions Steven johnsons syndrome
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Dosage:
Children 2 months of age or older: IV 8-12mg/kg in equally divided doses for every 6 hr PO 8-12mg/kg in equally divided doses for every 12 hours
Trade names:
Bactrim DS Apo-Sulfatrim DS Nu-Cotrimox
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Erythromycin 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 placenta Plasma half life: 1.9-2.1hours Metabolised in liver Excreted in bile
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Indications:
Upper and lower respiratory tract infections Skin and soft tissues infections Diphtheria , Pertusis- Otitis media
Contra Indications:
Hypersensitivity to the drug.
Adverse Reactions:
GI side effects: liver functions Renal failure Porphyria
Dosage:
Children: 30-50mg/kg in divided doses Trade Names: Ery-Tab , PCE Dispertab ,EES Granules
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Is 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.
Kinetics:
Plasma protein binding Plasma half life: 6-7 hours Metabolized in liver Excreted through kidneys and bile
Indications:
Infections of stomach ,skin , joints and respiratory tract , oral cavity Peptic ulcer disease
Contraindications:
Allergy to the drug Liver disease Stomach or intestinal disease such as Crohns disease Pregnancy
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Adverse Effects:
Nausea , anorexia , bitter or metallic taste. Less frequent side effects: headache ,glossitis ,dryness of mouth ,dizziness ,rashes Prolonged 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
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1. Clarks Rule:
Child weight in lb
150 2. Youngs Rule
Age of child
Age + 12
Index Dose a = adult dose Dose p = child dose Wt. pd= wt of child Wt. ad= wt of adult
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References: 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.com
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