Principles of antibiotics , NSAID’s and opioids

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Principles of antibiotics , NSAID’s and opiods : 

Principles of antibiotics , NSAID’s and opiods Presented by Gaurav Mathur BDS Jaipur Dental College

Antibiotics : 

Antibiotics Definition: an antibiotic is a chemical substance produced by microorganism which has the capacity, in dilute solutions, to inhibit the growth of or kill other microorganisms.

CLASSIFICATION : 

CLASSIFICATION Source Natural Synthethic Semi-syn Spectrum Narrow Extended Broad Family Effect Bacteriostatic Bactericidal Effect on G+ or G- G+ G-

Mechanism of Antimicrobial agents : 

Mechanism of Antimicrobial agents

Principles of Antibiotic therapy : 

Principles of Antibiotic therapy Selection of antimicrobials Evaluation and diagnosis for antimicrobiological etiology Culture and sensitivity Age Pregnancy and neonatal period Severity of disease Nature of drug Drug resistance Allergy to drugs Risk of toxicity to drug Cost factor Use of narrow spectrum antibiotics

Antimicrobial combination : 

Antimicrobial combination Purpose Interactions -Antagonism -Additive effect Risks Antimicrobial prophylaxis Indications Endocarditis Compound musculoskeletal injuries Deep punctured injuries

Bacterial resistance : 

Bacterial resistance Types Predisposing factors Causes

Principles of Antibiotic administration : 

Principles of Antibiotic administration Dosage Duration Rate Frequency

Beta lactam antibiotic : 

Beta lactam antibiotic Types Natural Semisynthetic

Slide 11: 

Natural penicillins Pen VK and Pen G Dose: 250-500 mg qid x 7-10 days Spectrum Strep, staph, enterococcus, neiseria, treponema, listeria Contraindications: Allergies Poor renal fxn Adverse events: -GI upset -Anaphylaxis -Superinfection Drug interactions: oral contraceptives

Amoxicillin and ampicillin : 

Amoxicillin and ampicillin Dose : 250-500 mg q 8 h x 7-10 days Indications:E. coli, proteus, H. Flu, shigella, salmonella Contraindications Allergies Poor renal fxn Adverse events: GI upset Drug interactions: oral contraceptives Amoxicillin and clavulanic acid (Augmentin)

Cephalosporins : 

Cephalosporins Dose : 250-1000mg q 6 h x 7-10 days Indications: Gram+, Gram- Types 1st gen : Gram +/- except enterococci 2nd gen : Gram + 3rd gen : enterobacteriacae Contraindications Allergies Poor renal fxn Adverse Reaction: Mild GI problems

Macrolides- erythromycin : 

Macrolides- erythromycin Dose : 250-500 mg/day x 5-10 days Indications : G+, G- and anaerobes Contraindications : Poor hepatic fxn Side effects - Allergy : Anaphylaxis - GI effects : nausea,vomitting Drug interactions

Sulfonamides : 

Sulfonamides Spectrum: Gram- Toxic effects: Allergy Kernicterus Anemia Renal damage : Crystalluria Sulfadiazine : Post traumatic meningitis Cotrimoxazole: Bactericidal

PAIN 0R ALGESIA : 

PAIN 0R ALGESIA AN UNPLEASANT EMOTIONAL EXPERIENCE USUALLY INITIATED BY A NOXIOUS STIMULUS AND TRANSMITTED OVER A SPECIALIZED NEURAL NETWORK TO THE CENTRAL NERVOUS SYSTEM WHERE IT IS INTERPRETED AS SUCH. PAIN IS AN UNPLEASANT SENSORY AND EMOTIONAL EXPERIENCE ASSOCIATED WITH ACTIVAL OR POTENTIAL TISSUE DAMAGE OR DESCRIBED IN TERMS OF SUCH DAMAGE.

Theories of pain transmission : 

Theories of pain transmission Specificity theory – by Descartes in 1644 Pattern theory – by Goldscheider in 1894 Gate control theory – by Melzack and Wall in 1965

Gate control theory : 

Gate control theory Information about the presence of injury is transmitted to the central nervous system by small peripheral nerves.( A delta & C fibers ) Cells in the spinal cord or nucleus of 5th cranial nerve, which are excited by these injury signals are also facilitated or inhibited by other large peripheral nerves that also caries information about innocuous events. Descending control systems originating in the brain modulate the excitability of cells that transmit information about injury.

PAIN RECEPTORS : 

PAIN RECEPTORS Sensory nerve endings that mediate pain – Nociceptors. …can be chemo-receptors / mechanoreceptors. Algesic or pain producing substances are:- Hypertonic saline NaCl Ach. 5-HT Histamine Bradykinin Substance P

Slide 21: 

Injury Release of vasoactive amine(5-hydroxytryptamine, Histamine,bradykinin) By mast cell & basophills Pain and stimulation of Pg release Prostaglandins themselves do not cause pain except in very high dose. The main contribution of prostaglandins is to sensitize the nociceptors to the bradykinin ,thus accentuating its action.

Analgesics : 

Analgesics Analgesic:- a drug that selectively relieves pain by acting in CNS or on peripheral pain mechanism, without significantly altering the consciousness. Classification of analgesics:-

Mechanism of action : 

Mechanism of action Cell membranes(Phospholipids) PGE2 Prostacyclin PGI2 Arachidonic acid Cyclo-endoperoxides PGF2 alpha Phospholipase A2 Cyclo-oxygenase These PGs cause – hyperalgesia - pyrexia - inflammation Steroidal anti inflammatory drugs Nsaids

ASPIRIN (Acetyl salicylic acid) : 

ASPIRIN (Acetyl salicylic acid) Non selective irreversible inhibitor of Cox Dose-300 to 600 mg 6-8 hourly Child dose – 80-100 mg/kg/day in divided doses Indication/use:- Analgesia Antipyretic anti-inflammatory Post MI& IHD Closure of patent ductus arteriosus Precaution/Contraindication:- hypersensitive pts Peptic ulcers chronic liver disease-rephropathy children suffering from viral infection

Slide 29: 

Adverse effects:- Side effects:- Gastric mucosal damage Effect on respiration and acid base balance Increase in bleeding tendency Hypersensitivity Interactions:- Displaces warferin ,phenytoin and methotrexate Toxicity Blunts the effect of diuretics. Preparations:- Tab. Disprin, Ecosprin, Myosprin inj. Biospirin (lysine acetylesalicylate450mg+glycine50mg)

IBUPROFEN : 

IBUPROFEN Non selective reversible inhibitor of COX Dose – 1.2-1.6 gm/day in 3-4 divided doses Child dose – 20-30 mg/kg/day in divided doses Indication/Use:- -antipyretic -analgesic -anti inflammatory Precaution/Contraindication:- -in hypersensitive pt. -in pt’s with peptic ulcer Adverse effects:- 1. Side effects – less than aspirin 2. Hypersensitivity

Slide 32: 

Preparations:- Tab Combiflam (iboprofen400mg + Paracetamol 325mg) Syp Combiflam Tab Duoflam (ibuprofen 400mg + paracetamol 500mg) Tab Flexon Susp. Flexon (ibuprofen 100mg + paracetamol 125mg/5ml) Tab Brufen 200,400,600 mg

Paracetamol : 

Paracetamol Weak inhibitor of Cox-1 in Inflammatory conditions / inhibitor of cox3 Poor anti inflammatory properties Dose-0.5-1.0g T.I.D Child doses- <3 m – 10 mg/kg 3 m to 1 yr – 60-120 mg 1 to 5 yr – 120-250 mg 3 days 6 to 12 yr – 250-500mg Indication/Use- -Analgesic (mild to moderate pain) preferred in pts allergic to aspirin, in patients with hemophilia or with a history of peptic ulcer or bronchial asthma. -Antipyretic-preferred in children with viral infection. Adverse effects:- -allergic -Gastric upset

Slide 34: 

Drug interaction:- Increase the oral anti coagulant activity Alcoholic patients – chances of hepatotoxicity Preparation:- Tab Metacin Tab Crocin Syp Crocin(125mg/5ml) Paed drops(150mg/ml) Tab Calpol Tab MetoPar(paracetamol 500mg+Metoclopramide Hcl 5mg)

Nimesulide : 

Nimesulide Weak inhibitor of cox1 and preferential cox2 + Other modes Dose-100mg B.D. Child Dose – 5 mg/kg/day in 2 or 3 doses Indication/Use:- -Analgesic -antipyretic -anti inflammatory drug Precautions:- -Peptic ulcer -Pts with renal impairment -Congestive heart failure

Slide 36: 

Side effects:- -G.I. upset -Hypersensitivity Drug interaction:- -  Theophylline level Preparations:- Tab Nimo Tab Nicip Tab Nice Tab Sumo ( Nimesulide 100mg + Paracetamol 500mg)

Diclofenac Sodium : 

Diclofenac Sodium Non selective reversible inhibitor of cox Dose- 50-100mg T.D.S. Child dose – 1-3 mg/kg/day in divided doses Indication/Use:- Analgesic Antipyretic, Anti-inflammatory Precaution/Contra-indication Pregnency Lactation Asthma Peptic ulcer Side effect:- G.I upset Hypersensitivity

Slide 38: 

Drug interaction:- levels of lithium, digoxin Inhibits diuretics bt potentiate k+ sparing diuretic Preparation:- Tab Diclomol Tab Dicloran (50/100 mg) Tab Voveran SR (50/100 mg) Inj Voveran (25mg/ml 3ml) Tab Dicloran A (Diclo 50mg + para 325mg) Tab Esgipyrin (Diclol 50mg + para 500mg) Diclofenac Potassium Tab Diclo K Tab Nedol-k

Ketorolac : 

Ketorolac Potent analgesic but modest anti inflammatory & antipyretic Dose 30-60mg i.m. 20mg initially  10mg/15-30mg I.M. Indication/Use:- -Post operative& accute musculoskeletal pain -renal colic, migrain Contraindication/precaution:- -Impaired renal function -Pregnancy, children, labour -Hypersensitivity

Slide 40: 

Drug interaction:- Ketorolac + Methotrexate fatal  Diuretic action side effects of other NSAID’s Preparations:- Tab ketanov Inj. Ketanov(30mg) Tab. Ketorol DT(10mg)

Opioid Analgesics : 

Opioid Analgesics Potent analgesic even in visceral pain Sedation

Classification : 

Classification Natural Eg.morphine codeine Semisynthetic Eg.heroin pholcodein Synthetic Eg. Pethidine, methadone, dextropropoxyphene etho heptazine

Morphine : 

Morphine Dose-10-15mg i.m. / s.c. rarely orally Child dose – 5-10 mg 1.Has got selective stimulant and depressant effects. Depressant Stimulant Analgesia Sedation Vagal centre Respiratory centre Cough centre Vasomotor centre 2.Constipation Adverse effect 1.Side effects 2.Allergy 3.Apnoea 4.Tolerance and dependence

Slide 45: 

Contraindication:- -infants -pts with respiratory diseases -head injury -hepatic failure Drug interaction:- Phenothiazine and Tricyclic antidepressant blood levels of morphine Preparation:- Tab.Morcontin continus (30-100mg) b.d. for cancer pain

Codeine : 

Codeine Indication/use- 1.Analgesia 2.Cough suppressant 3.Anti diarrhoeal Dose-analgesic 60mg Side effect- Constipation Addiction Preparation:- Tab Paracodin ( paracetamol 500mg + Codeine 30mg) Tab TWC ( paracetamol 325mg + Codeine 30 mg) Syp. Corex (codeine 10mg + CPM 4mg)

NSAIDs And Clinical Dentistry : 

NSAIDs And Clinical Dentistry Carefully selected local anesthetics can be used for pain control. EMLA ( eutectic mixture of local anesthetics - Xylocaine 2.5% + Prilocaine 2.5%) …….used topically in pedodontic procedures. Mild pain – Aspirin 650 mg orally Q.I.D Ibuprofen 400 mg orally Q.I.D Acute musculoskeletal, osteoarthritis, injury associated inflammation  Diclofenac / piroxicam

Slide 48: 

Postoperative or other acute but short lasting painful condition with minimal inflammation  ketorolac Post surgical dental pain paracetamol + codeine / Dpp Selective cox2 inhibitor eg. etoricoxib has longer duration of action and less side effects.

Slide 49: 

W.H.O’s Analgesic ladder

Clinical Tips : 

Clinical Tips Analgesics should be taken before the pain becomes severe. The drug doses should overlap previous doses for the adequate maintenance of pain relief. The fiber contents in the diet should be increased to relieve the constipation that occurs as a side effect of analgesics.

Slide 51: 

NSAIDs should be taken with food to minimize GIT side effects. If the aspirin tablets have a strong vinegar odor these should not be used. It is a sign of their deterioration. The effervescent formulations of NSAIDs often contain large amounts of Na+ ions & should be avoided in patients with cardiac and renal problems.

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