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.