Drugs in endodontics and

operative dentistry
CONTENTS
INTRODUCTION

DEFINITIONS

PHARMACODYNAMICS

PHARMACOKINETICS

DRUG NOMENCLATURE

ROUTES OF DRUG ADMINISTRATION









ABSORPTION
KINETICS OF ELIMINATION
FACTORS MODIFYING DRUG ACTION
DRUGS IN ENDODONTICS
- ANTIANXIETY DRUGS
- ANALGESICS
* Opioid Analgesics
* Non Opioid Analgesics
-ANTIBIOTICS IN ENDODONTICS
- LOCAL ANAESTHETICS
DRUGS IN OPERATIVE DENTISTRY
- ANTI SIALOGOUGES
- STYPTICS
CONCLUSION
REFERENCES



Introduction
What is a drug?
- any chemical agent which
effects any biological process
WHO 1966, Drug is any substance or product
that is used or intended to be used to modify or
explore physiological systems or pathological
states for the benefit of the recipient
What is Pharmacology?
- the study of how drugs effect a
biological system
What is Pharmacology ?
The study of how drugs effect biological systems
Pharmacokinetics Pharmacodynamics
What the body does to drug What the drug does to body
Pharmacotherapeutics Pharmacocognosy
The study of the use of drugs Identifying crude materials as drugs
Toxicology
Pharmacology
Pharmacodynamics
What the drug does to the body

Physiological and biochemical effects of
drug and their mechanism of action at
organ system or subcellular or
macromolecular level


Dose response curve
Dose response curve...
Pharmacokinetics
What the body does to the drug
Movement of the drug in and alteration of the
drug by the body; includes absorption,
distribution, binding or localization or storage,
biotransformation and excretion of the drug.

Pharmacodynamic agents

Chemotherapeutic agents
t1/2 (Half-Life)
- the time required for the plasma concentration of a
drug to be reduced by 50%
ED
50
(effective dose)

- The dose of a drug that is effective for 50% of the
population exposed to the drug
LD
50
(lethal dose)

- the dose at which death occurs in 50% of
subjects
Therapeutic index =
Median lethal dose (LD50)
Median effective dose (ED50)
Clinical set up-bounded by drug producing minimal
therapeutic effect and dose producing maximal adverse
effect

Drug Nomenclature
*Chemical name-
Propranolol
1-(isopropylamino)-3-(1-naphthyloxy) propranolol
*Nonproprietary name-
Competent scientific body- USAN, BAN
Ex-Meperidine (USA) & Pethidine( UK, India)

*Proprietary name ( Brand name)- Accepted by
manufacturer & is his property or trademark
Ex- Atenolol
ALTOL, ATECOR, BETACARD, ATEN,
ATCARDIL, , LONOL, TENOLOL, TENORMIN



Routes of Drug Administration
I) LOCAL ROUTES
1) Topical
2) Deeper tissues
3) Arterial supply

II) SYSTEMIC ROUTES
1) Oral
2) Sublingual or buccal
3) Rectal
4) Cutaneous
5) Inhalation
6) Nasal
7) Parenteral
- subcutaneous
- Intramascular
- Intravenous
- Intradermal injection


Oral absorption (enteral route)
Advantages



Disadvantages


Parenteral route
Routes of administration other than oral route termed as
parenteral
Advantages
Disadvantages
Absorption
Absorption is the movement of drug from its site of
administration into the circulation
Oral absorption-

Non ionized lipid soluble drugs-


Acidic drugs-


Basic drugs-




Bioavailability
It refers to the rate and extent of absorption of a
drug from a dosage form as determined by its
concentration time curve in blood or by its excretion
in urine
IV Bioavailability is 100%, it is frequently lower
after oral ingestion bcoz
- The drug incompletely absorbed
- First pass metabolism in intestine or liver
- Chemically equivalent but Biologically in equivalent
- Bioavailability has practical significance in drug with
low safety margin


First pass (Presystemic) metabolism
This refers to metabolism of a drug during its
passage from the site of absorption into the
systemic circulation

Attributes of drugs with high first
pass metabolism
Oral higher than S.L/ Parentral dose
Individual variation
Increased in patients with severe liver diseases
Increased if another drug competeting with it
in first pass metabolism is given concurrently

Ex- Chlorpromazine and Propranolol
Kinetics of elimination
Drug elimination is the sum total of metabolic
inactivation and excretion
FIRST ORDER KINETICS (Eponential)
ZERO ORDER KINETICS ( Linear)
PLASM HALF LIFE-

It is the time taken for its plasma concentration to
be reduced to half of its original value


Factors modifying drug action
1) Body size
Individual dose=
2) Age
child dose=

Child dose=












BW (Kg)
70
X Average adult dose
Age
Age +12
X Adult dose

(YOUNGS FORMULA)
Age
20
X Adult dose

(DILLINGS FORMULA)
3) Elderely
4) Sex
5) Species and race
6)Genetics
7) Routes of administration
8) Environmental factors and time administration
9) Psychological factors
Placebo- This is an inert substance which is give
in the garb of medicine. It works by Psychological
rather than pharmacological means and often produces
responses equivalent to the active drug
Anti anxiety drugs
Anxiety- it is an emotional state, unpleasant in
nature, associated with uneasiness, discomfort
and concern or fear about some defined or
undefined future threat.
Antianxiety- these are ill defined group of mild CNS
depressants which are aimed to control the symptoms of
anxiety, produce a restful state of mind without
interfering with normal mental or physical functions.

Sedatives- the drug that subdues the excitement and
calms the subject without inducing sleep though
drowsiness may be produced

Hypnotic- a drug that induces and or maintains sleep
similar to normal arousable sleep

Oral benzodiazepines
CLASSIFIACTION-
Long acting with active metabolites
single adult dose (mg) t- half life(Hours)
Diazepam 2-10 14-100
Chlordiazepoxide 5-10 5-30
Halazepam 20-40 14-65
Flurazepam 15-30 -
Parazepam 5-10 -
Clorazepam 7.5-1.5 -

Medium to short acting with no active metabolites

single adult dose Elimination half life
Triazolam 0.125-0.25 1.5-5.5
Temazepam 15-30 9-38
Alprazolam 0.25-0.5 12-15
Lorazepam 2-3 10-20
Oxazepam 10-15 5-20
Estazolam 1-2 10-24
Quazepam 7.5-15 30-100
Pharmacological actions
Preparation-1960

Pharmacodynamics-
1) Antianxiety
2) Sedative-hypnotic
3) Anticonvulsant
4) Amnesic
5) Skeletal muscle relaxant
6) Induce anterograde amnesia
Mechanism of action- Facilitates inhibitory action of
gamma aminobutyric acid (GABA)






ADVERSE REACTIONS
Few n mild
- Excessive CNS depression
- Drowsiness
- Somnolence
- Decreased motor coordination,
- Impaired intellectual functions
other are
- CNS depressant synergism
- Release of anxiety bound hostility
- acute overdosage
- excerberation of porphyria


Pharmacology of pain
Two components of pain
-Pain perception, and Pain reaction
Pain perception is the reasonably objective
component of the pain phenomenon

Pain reaction is the emotional response to the
percieved injury and its painful manifestation
Analgesics-

Opiates-

Opioid analgesics-



Narcotic analgesics-





Classification
1.Natural opium alkaloids - Morphine, Codeine

2.Semisynthetic opiates - Diacetylmorphine(Heroin),
Pholcodeine
many others like- Hydromorphone, Oxymorphone,
Hydrocodeine, Oxycodone, are not used in India
3. Synthetic opioids- Pethidine, Fentanyl, Methadone,
Dextroprpxyphene, Tramadol, Ethoheptazine
Morphine
*Source- natural opium alkaloid
milky exudate of unripe capsules of poppy
plant, papaver somniferum
a) Phenanthrene group- Morphine, Codeine
and Thebaine.
b) Benzylisoquinoline group- Papaverine,
Noscapine, Narcine

Pharmacological actions
1) Analgesia-

2) CNS-

3) Respiration-

4) Pupil-

5) Emetic action-

6) Antitussive effect

7) ADH secretion-

8) GIT-

9) Biliary tract-

10) Other smooth muscles-

Absorption, fate and excretion-

Preparation and dose
1. tincture opium 0.3 to 2 ml by mouth
2. morphine sulphate-
3. morphine hydrochloride 8 to 20 mg by mouth or by injection
Adverse reactions
1.Dysphoria, mental clouding
2.Nausea, vomiting, rashes
3. Tremor, delirium, and skin rashes
4. acute morphine poisoning- resp. depression, pin point pupil, cyanosis,
reduced body temp, hypotension, shock and coma
5. Depression of foetal respiration
6. Tolerance and drug dpendenance

Therapeutic uses
1.analgesic
2. sedation and slep
3. pre-anaesthetic medication
4. acute LVF
5. Diarrhoeae
6. As antitussive


Narcotic Analgesics in Dentistry

Codeine, hydrocodone, oxycodone, and pentazocine.

Employed exclusively for pain relief

NOT anti-inflammatory


Combinations of opioids such as codeine and aspirin or
acetaminophen are commonly employed
e.g Oxycodone (related to codeine - but 6-fold more
potent)
(Percocet -- contains acetaminophen)
(Percodan -- contains ASA)


Comments related to use of narcotic
analgesics in dentistry
DRUG INTERACTIONS

Other CNS depressants will increase the degree of respiratory depression
with opioids

Opioids and phenothiazines produce at least additive CNS depression.
This combination may also increase orthostatic hypotension, as can opioids
and tricyclic antidepressants.

Respiratory acidosis caused by large doses of opioid agonists may increase
entry of local anaesthetics into the CNS

Well documented interaction between meperidine and MAO inhibitors -
severe and immediate reactions - include excitation, rigidity, hypertension,
and sometimes death.
CLASSIFICATION
(Acc. to Tripathi)
A. Analgesic and antiinflammatory :
Aspirin, Salicylamide, Benorylate, Diflunisal
Phenylbutazone, oxyphenbutazone
Pyrazolone derivatives
Indomethacin, sulindac
Indole derivatives
Ibuprofen,Naproxen, Ketoprofen, Fenoprofen,
Flurbiprofen.
Propionic acid derivatives
Mephenamic acid
Anthranilic acid derivative
Diclofenac, Tolmetin
Piroxicam, Tenoxicam, Meloxicam.
Oxicam derivatives
Ketorolac.
NImesulide
Sulfonanilide derivative
Nabumetone
Alkanones
Aryl acetic acid derivative
Pyrrolo pyrrole derivative
Salicylates
B. Analgesic but poor antiinflammatory:
Paracetamol (Acetaminophen)
Paraaminophenol derivative
Metamizol (Dipyrone), propiphenazone
Pyrazolone derivatives
Nefopam
Benzoxazocine derivative
Acc. to Goodman and Gillman
A. Non selective Cox inhibitor
Aspirin, sodium salicylate, choline magnesium
trisalicylate, salsalate, diflunisal, salfasalazine,
olsalazine.
Salicylic acid derivatives
Acetaminophen
Para amino derivatives
Indomethacin, sulindac
Indole & indene acetic acid
Tolmetin, diclofenac, ketorolac.
Heteroaryl acetic acid
Ibuprofen, naproxen, flurbiprofen, ketoprofen,
fenoprofen, oxaproxin.
Aryl propionic acid
Mefenamic acid, meclofenamic acid
Anthranilic acid (fenamates)
Oxicams (piroxicam, Meloxicam)
Enolic acid
Nabumetone.
Alkanones
Rofecoxib
Diaryl substituted furanones
B. Selective cox-2 inhibitor
Celecoxib
Diaryl substituted Pyrazoles
Etodolac
Indole acetic acid
Nimesulide
Sulfonanilides
MECHANISM OF ACTION
Odontogenic pain Acute pain
Noxious stimuli
Tissue destruction or injury
Cellular destruction
Release / synthesis of histamine /
prostaglandin / bradykinin
Peripheral nociceptor / free nerve
endings
PAIN
+
Disease process
+
Surgical intervention

Phospholipid of cell membrane

Arachidonic acid


Prostaglandins
Inflammation
COX-1
COX-2
Beneficial actions due to PG
Synthesis inhibition
Analgesia
Antipyresis
Antiinflammatory
Antithrombotic
Closure of ductus arteriosus
Shared toxicities due to PG
synthesis inhibition
Gastric mucosal damage
Bleeding
Limitation of renal blood flow
Delay / prolongation of labour
Asthma & anaphylactoid
reactions
COMMON PROPERTIES OF ALL NSAIDS
Analgesia
Antipyresis
Anti-
inflammatory
Dysmenorrhoea
Antiplatelet
aggregatory
Ductus
arteriosus
closure
Parturition
Gastric mucosal
damage
Renal effects
Anaphylactoid
reactions
SALICYLATES
Aspirin (prototype) Pharmacological actions
Analgesic (0.3-1.5 g/day)
Antipyretic
Respiration
GIT
Antiinflammatory (3-6 g/day or 100mg/kg/day)
Immunological effect
Uricosuric effect
CVS
Blood
Endocrines
Metabolic effect
Local actions


















2-5 g/day
<2g/day
> 5g/day
Pharmacokinetics
80% bound to plasma proteins.
Volume distribution 0.17 L/kg.
Plasma t = 15-20 min.
Release salicylic acid (t ) = 3-5
hrs.
Antiinflammatory doses (t ) =
8-12 hrs. (30 hrs in poisoning)
Adverse effects
Salicylism : dizziness, tinnitus, vertigo, reversible impairment of
hearing imbalance& vision, excitement & mental confusion,
hyperventilation & electrolyte Acute salicylate poisoning : fatal
dose-15-30g , > 50 mg/dl.
Contraindications :
Sensitivity, peptic ulcers, bleeding tendency, chicken pox
or influenza.
Chronic liver disease
Diabetics, low cardiac reserve or frank CHF, juvenile
rheumatoid arthritis.
Precautions :
Stopped 1 week before elective surgery.
During pregnancy
Avoided by breast feeding mothers.
G-6-PD deficient individuals
Interactions :
Warfarin, naproxen, sulfonylureas,
phenytoin and methotrexate.
Oral anticoagulants.
Uric acid
Probenecid
Methotrexate.
Furosemide and thiazides
Spironolactone.
Protein bound iodine levels.
Uses :
Analgesic
Antipyretic
Acute rheumatic
fever (4-6 g)
Rheumatoid
arthritis (3-5 g)
Osteoarthritis
Postmyocardial
infarction &
poststroke patients
Pregnancy induced
hypertension and
preeclampsia
Delay labour
Patent ductus
arteriosus
* Aspirin, dispirin, colosprin
PYRAZOLONES
Phenylbutazone
Pharmacokinetics
98% bound to plasma proteins.
Plasma t = 60 hrs.
Dose 100-200 mg BD/TDS
Adverse effects
Bone marrow
depression
Agranulocytosis
Stevens-Johnson
syndrome
Interactions :
Sulfonamides, tolbutamide, warfarin,
imipramine & methotrexate
Anticoagulants
Phenytoin & tolbutamide
Uses :
Rheumatoid
arthritis
Ankylosing
spondylitis
Rheumatic
fever
Acute gout
Severe
cases
Zolandin
P L
Oxyphenbutazone
Metamizol (Dipyrone) : 0.5-1.5 g
Propiphenazone : 300-600 mg TDS
INDOLE DERIVATIVES
Indomethacin
Pharmacokinetics
90% bound to plasma
proteins.
Plasma t = 2-5 hrs.
Dose 25-50mg BD/QID
Sioril, phenabid
Analgin, novalgin
Saridon, anafebrin
Adverse effects
Interactions :
Furosemide
Thiazides, furosemide,
blockers, ACE inhibitors
Warfarin
Uses :
Rheumatoid
arthritis
Ankylosing
spondylitis
Psoriatic
arthritis
Acute gout
Acu. Exa.
destructive
arthropathies
Malignancy
asso. fever
Patent ductus arteriosus
closure (0.1/0.2 mg/kg/12 hrly
P L
Indicin, indocap
PROPIONIC ACID DERIVATIVES
Pharmacokinetics
90-99% bound to plasma proteins.
Drug Plasma t Dosage
Ibuprofen 2 hr 400-800 mg TDS Brufen, emflam
Naproxen 12-16 hr 250 mg BD/TDS Xenobid, naxid
Ketoprofen 2-3 hr 100 mg BD/TDS Ketofen
Fenoprofen 2-4 hr 300-600 mg TDS Arflur
Flurbiprofen 4-6 hr 50 mg BD/QID Flurofen
Adverse effects
Interactions :
Anticoagulants
Furosemide, thiazides &
blockers
Uses :
Analgesic
Antipyretic
Dysmenorrhoea
ANTHRANILIC ACID DERIVATIVE (Fenamate)
Mephenamic acid
Pharmacokinetics
Highly bound to plasma
proteins.
Plasma t = 2-4 hrs
250-500 mg TDS
Adverse effects
Uses :
Analgesic
Osteoarthritis
Dysmenorrhoea
Rheumatoid
arthritis
Medol, meftal, ponstan
L
ARYL-ACETIC ACID DERIVATIVES
Diclofenac sodium :
Pharmacokinetics
99% bound to plasma proteins.
Plasma t = 2 hrs
50 mg TDS/BD, 75 mg i.m.
Adverse effects
Uses :
Ankylosing
spondylitis
Osteoarthritis
Dysmenorrhoea
Rheumatoid
arthritis
Bursitis
Post-traumatic / post-op
inflammatory condition
Tolmetin : 400-600 mg TDS
Voveran, diclonac, movonac
OXICAM DERIVATIVES
Piroxicam
Pharmacokinetics
99% bound to plasma proteins.
Plasma t = 2 days
20 mg BD / 20 mg OD
Adverse effects
Uses :
Ankylosing
spondylitis
Osteoarthritis
Dysmenorrhoea
Rheumatoid
arthritis
Acute gout
Musculoskeletal injuries
Dentistry
Episiotomy
Tenoxicam : 20 mg OD
Meloxicam : 7.5-15 mg/day (rheumatoid & osteo-arthritis)
Dolonex, pirox, piricam, toldin
P L
Melflam, Meloxi
PYRROLO-PYRROLE DERIVATIVE
Ketorolac :
Pharmacokinetics
Highly bound to plasma proteins.
Plasma t = 5-7 hrs
10-20 mg / 6 hrly (orally)
Adverse effects
Uses :
Post-op / acute
musculoskeletal pain
(15-30 mg i.m. / 4-6 hrs
Renal colic
Bony
metastasis
Migraine
SULFONANILIDE DERIVATIVE
Nimesulide :
Pharmacokinetics
99% bound to plasma proteins.
Plasma t = 2-5 hrs
100 mg BD
Ketorol, torolac
Adverse effects
Uses :
Bursitis
Sports injuries
Dental surgery
ENT disorders
Low backache Dysmenorrhoea
Post-op
pain/osteoarthritis
Nimulid, nimodol
PARA-AMINO PHENOL DERIVATIVES
Phenacetin 1887
Paracetamol (acetaminophen) 1950
Actions
Pharmacokinetics
1/3 bound to plasma proteins.
Plasma t = 2-3 hrs
3-5 hrs (orally)
0.5-1g TDS
Infants - 50 mg
Children 1-3 yrs- 80-160 mg
4-8 yrs 240-320 mg
9-12 yrs 300-600 mg
Adverse effects
Analgesic nephropathy
Acute paracetamol poisoning
150 mg/kg
Fatality > 250 mg/kg
Early manifestations / 12-18 hrs / 2 days
Mechanism of toxicity
Treatment
Gastric lavage
N-acetylcysteine 150 mg/kg / i.v./ 15 min / 20 hrs
75 mg/kg / orally / 4-6 hrs / 2-3 days
Uses :
Over the counter
analgesic
Musculoskeletal
pain
Dysmenorrhoea
Antipyretic
Crocin, metacin, paracin
BENZOXAZOCINE DERIVATIVE
Nefopam
30-60 mg TDS oral
20 mg i.m. 6 hrly
CHOICE OF NSAIDS
Mild to moderate pain paracetamol, ibuprofen
Acute musculoskeletal, osteoarthritic, injury associated
inflammation ibuprofen, diclofenac, piroxicam
Post-op / acute / short lasting painful condition ketorolac,
nefopam
Nefomax
Exacerbation of rheumatoid arthritis, ankylosing
spondylitis, acute gout, acute rheumatic fever aspirin,
indomethacin, naproxen, piroxicam
Asthma or anaphylactoid reactions to aspirin nimesulide
ADVANCES
Selective cox-2 inhibitors :
Celecoxib, rofecoxib, valdecoxib, etoricoxib, meloxicam,
diisopropyl flurophosphate.
Action
Celecoxib P L
Use-osteoarthritis, rheumatoid arthritis
Dose 200 mg / day OD or 100 mg BD.
Commercial names Celebrex, Celib, Celfast, Celact etc.
Banned July 2001
Rofecoxib P L
Dose 12.5 mg OD (max. dose 25 mg)
Commercial name Vioxx, Dolib MD, Roff, Rofaday
Banned September 2004
Valdecoxib
Dose 10-20 mg OD
Commercial name Valed, Valus, Vorth, Bextra
Banned 7 April 2005.
Other drugs banned by FDA
Benoxaprofen
Phynylbutazone
Oxyphenbutazone
Saprofen
Piroxicam
PAIN MANAGEMENT STRATEGY
3D
iagnosis
efinitive Rx
rugs
Definitive treatment :
Pulpotomy, pulpectomy
Extraction
Incision & drainage

Drug :
Pretreat with NSAIDs
Prescribe by clock
Long acting LA
Flexible prescription plan
Flexible analgesic prescription plan
Aspirin like drugs
indicated
Aspirin like drugs contra
indicated
Ibuprofen 200 mg
Acetaminophen 600-1000mg
NSAIDs (alone max.effective
dose) OR NSAID +
acetaminophen
Acetaminophen 600-1000
mg + codine 60 mg
Ibuprofen 400 mg/4 hrly and
equivalent of acetaminophen
600 mg / codine 60 mg 4 hrly
Acetaminophen 1000 mg with
equivalent of oxycodone 10 mg
NSAID (max. dose) &
acetaminophen / oxycodone
10 mg combination
Mild
pain
Moderate
pain
Severe
pain
Analgesics after certain endodontic procedures
ANTIBIOTICS
Antimicrobial agent : substances that will suppress the growth /
multiplication of microorganisms. antimicrobial agents may be
antibacterial, antiviral / antifungal.
Antibacterial agent : substances that destroy or suppress the
growth / multiplication of bacteria. They are classified as
antibiotic or synthetic agents.


Antibiotic agent : against life (greek-anti means against and biosis
means life).
Chemical substances produced by microorganisms that have
the capacity in dilute solutions, to produce antimicrobial action.
CLASSIFICATION OF ANTIMICROBIAL DRUGS
A) Mechanism of action :
1. Inhibit cell wall synthesis
Penicillins
Cephalosporins
Vancomycin
Bacitracin
2. Cause leakage from cell membranes
Polypeptides Polymyxins, colistin, Bacitracin
Polyenes Amphotericin B, Nystatin

3. Inhibit protein synthesis
Tetracyclines
Chloramphenicol
Erthromycin,
Clindamycin
Linezolid
4. Cause misreading of m-RNA code and affect permeability
Aminoglycosides
o Streptomycin
o Gentamicin

5. Inhibit DNA gyrase
Fluoroquinolones Ciprofloxacin
6. Interfere with DNA function
Rifampin
Metronidozole
7. Interfere with DNA synthesis
Idoxuridine
Acyclovir
Zidovudine
8. Interfere with intermediary metabolism
Sulfonamides PAS
Sulfones Ethambutol
B) Chemical structure
1. Sulfonamides and related drugs
Sulfadiazine and others
Sulfones Dapsone (DDS), Paraaminosalicylic acid
(PAS).
2. Diaminopyrimidines
Trimethoprim
Pyrimethamine
3. Quinolones
Nalidixic acid
Norfloxacin
Ciprofloxacin etc
4. -lactam antibiotics
Penicillins
Cephalosporins
Monobactams
Carbapenems
5. Tetracyclines
Oxytetracycline
Doxycycline etc
6. Nitrobenzene derivative
Chloramphenicol

7. Aminoglycosides
Streptomycin
Gentamicin
Neomycin etc
8. Macrolide antibiotics
Erythromycin
Roxithromycin
Azithromycin etc
9. Polypeptide antibiotics
Polymyxin-B
Colistin
Bacitracin
Tyrothricin
10. Glycopeptides
Vancomycin
Teicoplanin
11. Oxazolidinone
Linezolid
12. Nitrofuran derivatives
Nitrofurantoin
Furazolidone
13. Nitroimidozoles
Metronidozole
Tinidazole
14. Nicotinic acid derivatives
Isoniazid
Pyrazinamide
Ethionamide
15. Polyene antibiotics
Nystatin
Amphotericin-B
Hamycin
16. Azole derivatives
Miconazole
Clotrimazole
Ketoconazole
fluconazole
17. Others
Rifampin
Lincomycin
Clindamycin
Spectinomycin
Sod. fusidate
Cycloserine
Viomycin
Ethambutol
Thiacetazone
Clofazimine
Griseofulvin
C) Type of organisms against which primarily active
1. Antibacterial
Penicillins
Aminoglycosides
Erythromycin etc
2. Antifungal
Griseofulvin
Amphotericin B
Ketoconazole
3. Antiviral
Idoxuridine
Acyclovir
Amantadine
Zidovudine etc
4. Antiprotozoal
Chloroquine
Pyrimethamine
Metronidazole
Diloxanide etc
5. Anthelmintic
Mebendazole
Pyrantel
Niclosamide
Diethyl carbamazine etc

D) Spectrum of activity
1. Narrow spectrum
Penicillin G
Streptomycin
Erythromycin
2. Broad spectrum
Tetracyclines
Chloramphenicol
E) Type of action
1. Primarily bacteriostatic
Sulfonamides
Tetracyclines
Chloramphenicol
Erythromycin
Ethambutol
2. Primarily bactericidal
Penicillins
Aminoglycosides
Polypeptides
Rifampin
Cotrimoxazole
Cephalosporins
Vancomycin
Nalidixic acid
Ciprofloxacin
F) Antibiotics are obtained from
1. Fungi
Pencillin
Cephalosporin
Griseofulvin
2. Bacteria
Polymyxin B
Colistin
Bacitracin
Tyrothricin
Aztreonam
3. Actinomycetes
Aminoglycosides
Tetracyclines
Chloramphenicol
Macrolides
Polyenes
Misconception about antibiotics
Improper choice- drug, dosage, duration of therapy
Ignorance of Microbial biology
Antibiotics- safe & do no harm
Antibiotics prophylaxis commonly successful
To mask poor surgical procedure
I dont know what else to do syndrome
Malpractice negligence suit
Myths in antibiotic theapy
I. Antibiotic cure patients
II. Antibiotics are substitute for surgical drainage
III. The most important decision is which antibiotic
use
IV. Antibiotic therapy is a science and not an art
V. Culture and sensitivity are required
VI. Antibiotics increase host defence to infection
VII. Multiple antibiotics are superior to a single
antibiotic

VIII. Antibiotic prophylaxis is usually effective
IX. Bactericidal agents are always superior to
bacteriostatic agent
X. Antimicrobial are effective in chronic infectious
diseases
XI. Antibiotics are safe and nontoxic
XII. Antibiotic dosage are established for most
infections
XIII. Infection require a complete course of therapy
BETA LACTAM ANTIBIOTICS
Pencillins
Most important antibiotics first extracted from the mould
PENICILLIUM NOTATUM
First used in 1941 clinically and was a miracle drug with a
least toxic effect.
CLASSIFICATION OF PENICILLINS
1. Natural penicillin
Penicillin G (benzyle penicillin)
Procaine penicillin G
Benzathine penicillin G
2. Acid resistant penicillin
Phenoxymethyl penicillin (pencillin V)
Phenoxyethylpenicillin (phenethecillin)
3. Penicillianse resistant penicillins
Acid labile methecillin, nafcillin, cloxacillin, dicloxacillin
Acid resistant flucloxacillin
4. Penicillins effective against gram positive and some gram-
negative organisms
Ampecillin
Ampoxycillin
Talampicillin
5. Extended spectrum penicillins
Carboxypenicillins carbenicillin, ticarcillin
Ureidopencillins piperacillin, mezlocillin
Amidino pencillins mecillinam, pivmecillinam
6. Penicillins with betalactamase inhibitors
Amoxycillin clavulanic acid (Augmentin)
Ticarcillin clavulanic acid (Timentin)
BENZYL PENICILLIN (PENCILLIN G)
PnG is a narrow spectrum antibiotic; activity is limited primarily
to gram positive bacteria
Is available in the form of water soluble sodium and potassium
salts
This salts in a dry state are stable at room temperature for years.
The aqueous solution however requires refrigeration and
deteriorates considerably with in 72 hours.
Antibactrial activity
Most potent AMA, inhibits the growth of susceptible organism.
Mainly gram +ve, gram ve cocci and some gram +ve bacilli
with exception of enterococci.
Cocci Highly sensitive Streptococci, Pneumococci, Staph.
aureus, N. gonorrhoeae, N. meningitis
Bacilli B. anthracis, Corynebacterium diphtheriae, clostridium
tetany and spirochetes
Actinomyces israelii is moderately sensitive
Mechanism of action :
Bactericidal drug effective mainly against multiplying
organisms.
Pencilline requires cell wall that contains peptidoglycans.
Peptidoglycan is heteropolymeric component of cell wall
provides rigid mechanical, crosslinked lattice like structure.
Penicillin binding to this proteins are bacterial enzymes on the
cell wall are responsible for synthesis and cross linkage of
peptidoglycans in the cell wall.
Penicillins bind to these proteins and inactivate them, thereby
preventing the synthesis and cross linkage.
This weakens bacterial cell wall and makes organism
vulnerable to damage.
As the cell wall synthesis occurs during the growth phase the
antibiotic is more effective against actively multiplying
organisms.
Absorption fate and excretion :
About 1/3 of drug is activated on oral administration.
Absorbed from the duodenum.
Because of the inadequate absorption the oral dose should be
4/5 times larger than the intramuscular dose.
As food interferes with its absorption PnG should be given
orally atleast 30 min after food or 2 to 3 hours before food.
B. Pencillin in aqucous solution is rapidly absorbed after SC
or IM administration.
Peak plasma level of 8 to 10 units per ml is reached with in 15
to 30 min and drug disappears from plasma with in 3-6 hours.
Widely distributed in the body and significant amounts
appear in liver, bile, kidney, jointfluid and interstine.
PnG is excreted mainly by the kidney but in small part in
the bile and other routes.
50% drug is eliminated in urine with in first hour.
Preparation and dose :
PnG inj 0.5-5 MU i.m or i.v 6-12 hours
Procaine pencillin inj 0.5, 1 MU dry powder in vial
Penidure 0.6, 1.2, 2.4 MU as dry powder in vial
Fortifide PP inj 3+1 lac U vial
ADVERSE REACTIONS :
a) Miscellaneous reactions :
Nausea and vomiting on oral PnG
Sterile inflammatory reaction at the site of IM inj.
Prolonged IV administration may cause thrombophlebitis
Accidental IV administration of procaine PP cause anxiety,
mental disturbances paraesthesia and convulsions
b) Intolerance :
Major problem with PnG includes idiosyncratic,
anaphylactic and allergic reactions
c) Other allergic reactions are
Skin rashes
Serum sickness
Renal disturbance
Hemolytic disturbance
Anaphylaxis
Jarisch herxheimer reaction
Super infection
Hyperkalemia
Acute non allergic reaction
Uses :
PnG is the drug of choice for infections
1. Streptococcal infections
2. Pneumococcal infections
3. Meningococcal infections
4. Gonorrhoea
5. Syphilis
6. Diphtheria
7. Tetanus and gas gangrene
8. Prophylactic uses
SEMI SYNTHETIC PENCILLINS
The major drawbacks of benzyl pencillin are :
1. Inactivation by the gastric hydrochloric acid
2. Short duration of action
3. Poor penetration into CSF
4. Activity mainly against gram +ve organism
5. Possibility of anaphylaxis
Attempts therefore have been made to synthesize pencillin free
from such drawbacks.
P.chrysogenum produces natural penicillins which produce the 6
amino-penicillanic acid (6-APA) nucleus.
The attachment of side chains are inhibited and instead various
organic radicals can be substituted.
Thus a variety of semisynthetic resins are produced.
I) Acid resistant pencillins :
1. Potassium phenoxymethyl penicillin (penicillin V)
Similar antibacterial spectrum like benzylpenicillin.
More active against resistant staphylococci
Less inactivated by the gastric acid.
Plasma levels achieved is 2 to 5 times higher than
benzylpenicillin.
50-70% is bond to plasma proteins.
25% of drug is eliminated in urine
Available as 60 & 125 mg tablets.
Administered in the dose of 250 500 mg at 4-8 hours
intervals, atleast 30 min before food.
This can be used in less serious infections (pneumocci
and streptococci).
Dose : infants 60 mg, children 125-250 mg given 6 hourly
CRYSTAPEN-V, KAYPEN, PENIVORAL 65, 130, 125, 250 mg
tablets
125 mg/5 ml dry ser


2. Potassium phenoxyethyl penicillin and
3. Azidocillin
Both have similar properties to penicillin V and no difference in
the antibacterial effect
II) Pencillinase resistant pencillins :
1. Methicillin
1. Effective in staphylococci
2. It is given IM or IV (slow) in the dose of 1 gm every 4-6
hours.
3. Haematuria, albuminuria and reversible interstitial nephritis
are the special adverse effect of methicillin.
2. Cloxacillin
1. Weaker antibacterial activity.
2. Distrubuted thro out the body, but highest s concentration in
kidney and liver. 30% excreted in urine.
3. Oral dose for adults 2-4 gm divided into 4 portions children
50-100mg/kg/day.
4. IM adults 2-12 gm/day, children 100-300 mg/kg/day every
4-6 hours.
BIOCLOX, KLOX, CLOCILIN 0.25, 0.5 gm cap, 0.5 gm/vial.
Oxacillin, Dicloxacillin, Flucloxacillin are other isoxazolyl
penicillins, similar to cloxacillin, but not marketed in India.
Nafcillin :
More active than methicillin and cloxacillin but less active than
PnG
80% of drug bonds with plasma proteins excreted by liver in
patients with renal failure.
Dose is similar to cloxacillin.
III) Extended spectrum pencillins :
1. Amino pencillins
1. Ampicillin
Antibacterial activity is similar to that of PnG that is more
effective than PnG against a variety of gram-ve bacteria
Drug is effective against H.influenzae strep.viridans,
N.gonorrhea, Salmonella, shigellae, Klebsilla and
enterococci.
Absorption, fate and excretion :
Oral absorption is incomplete but adequate
Food interferes with absorption
Partly excreted in bile and partly by kidney
Dose : 0.5-2 gm oral/IM or IV depending on severity of infection
every 6 hours
Children : 25-50 mg/kg/day
AMPILIN, ROSCILLIAN, BIOCILIN 250, 500 mg cap
100mg/ml ped drops, 250 mg/ml dry syr, 1 gm/vial inj.
USES :
Urinary tract infections
Respiratory tract infections
Meningitis
Gonorrhoea
Typhoid fever
Bacillary dysentry
Septicaemias
SBE
Adverse effects :
Diarrhoea is frequent
Skin rashes is more common
Unabsorbed drug irritates lower interstines
Patient with history of hypersensitivity to PnG should not
be given ampicillin.
AMOXYCILLIN :
This is a semisynthetic penicillin
(amino-p-hydroxy-benzylpencillin)
Antibacterial spectrum is similar to ampicillin but less effective
than ampicillin for shigellosis.
Oral absorption is better; food does not interfere; higher and
more sustained blood levels are produced.
It is less protein bond and urinary excretion is higher than that
of ampicillin.
Incidence of diarrhoea is less
Dose : 0.25-1 g TDS oral;
AMOXYLIN, NOVAMOX, SYNAMOX, MOX, AMOXIL 250,
500 mg cap, 125 mg/5ml dry syr, 500 mg/vial inj.

USES :
Typhoid
Bronchitis
Urinary infection
SBE
Gonorrhoea
Carboxy penciillins :
The Carboxypenicillins, the Ureidopenicillins and the Amidino
penicillins are considered extended spectrum penicillins,
because they inhibit a wide variety of aerobic gram-ve bacilli
They are ineffective against most strains of staph. Aureus
They have following properties :
1. Highly active against anaerobes
2. Most useful in infections caused by other gram-ve rods
3. Act synergistically with amino glycoside antibiotics, particularly
enterobacteriacea.
4. Much less active than penicillin G against gram+ve organisms
5. The CNS penetration is about 10% of their serum levels and
hence not recommended for the treatment of meningeal
infections.
CARBENICILLIN
Has similar spectrum as other penicillin
Weaker antibacterial activity than ampicillin
Active against pseudomonas, proteus
Inactive against klebsiella and gram ve cocci
Acid labile and has to be given by parenteral route only
Peak plasma level is 2hours and excreted in urine
Dose : 1-2g im/iv 4-6hours
Adverse effects :
Cause congestive heart failure
Bleeding disorders-impaired platelet function
Uses :
Pseudomonas ,burns, UTI and septicemia
PYOPEN,CARBELIN 1g,5g per vial
BETA LACTAMASE INHIBITORS
CLAVULANIC ACID
Obtained from STREPTOMYCES CLAVULIGERUS
Betalactam ring no antibacterial activity
Suicide inhibitor inactivated after binding to enzyme
Permeates the outer layers of cell wall of gram-ve bacteria
Pharmacokinetics :
Oral absorption- rapid
Bioavailability-60%
Distribution similar that of amoxicillin
Excretion-tubular secretion
Uses :
Amoxicillin+clavulanic acid (augmentin)
Ticarcillin+clavulanic acid (timentin)
Staph aureus,H influenza, gonorrhoea and E coli
Adverse effects :
Poor g.i. tolerance
Hepatotoxicity
AUGMENTIN, AMONATE, ENHANCIN
250+125mg tab 1-2tab TDS
250+50mg vial im/iv 6-8 hourly
SULBACTAM
Semisnythetic betalactamase inhibitor
Related chemically in activity to clavulanic acid
Progressive inhibitor ,highly active against
betalactamase
2-3 times < potent
Oral absorption- inconsistent,preferably im/iv
Sulbactam+ ampicillin=Dicapen
SULBACIN, AMPITUM
1g+ 0.5g per vial im/iv 6-8hourly
1g+500mg tab
Adverse effects :
Pain-thrombophebitis
Rashes and diarrhoea
Uses :
Mixed aerobic-anaerobic infections
Gonorrhoea
Skin/soft tissue infections
CEPHALOSPORINS
Cephalosporium acremonium was the first source.
They contain 7 amino cephalosporonic acid nucleus.
Structurally they contain betalactam and didhydro thiazine rings.
Mechanism of action :
Act by inhibiting bacterial cell was synthesis and are
bactericidal.
New derivatives are much more resistant than the older
cephalosporins

Classification
Classified according to its antibacterial activity.
First generation cephalosporin
Good activity against gram +ve bacteria. (except enterococci).
Most oral cavity anaerobes are sensitive.
Parental Oral
CEPHALOTHIN CEPHALEXIN
CEFAZOLIN CEPHRADINE
CEFADROXIL
Cephalaxin and Cephadroxil :
Useful in treating community acquired, respiratory and urinary
tract infections and in surgical prophylaxis.
Not choice for systemic infections.
Cefazolin :
For antimicrobial prophylaxis in most surgical procedures.
Given only IM / IV.
Dose: Oral 0.25 - 1g 6-8 hrly
Children : 25-100mg/kg/day
IM 0.25g 8 hrly (mild cases) 1g 6 hrly (severe cases).
Drops cephaxin 125mg/5ml syrup.
100mg /ml ped. drops.
SPORIDEX, CEPHAXIN, CEPHACILLIN, CEFADROX,
DROXYL
Second generation cephalosporins :
Increased activity against gram ve organism.
More active against anaerobes.
Parenteral Oral
CEFUROXIME CEFACLOR
CEFOXITIN CEFUROXIME AXETIL
Cefaclor and cefuroxime axetil retains significant by oral route.
More active against H. influenzae, E coli.
Dose : 250mg, 125mg, 125mg/5ml syr. and
50 mg /ml ped. drops.
KEFLOR, CEFTUM, CEFOGEN, FUROXIL.
Third generation cephalosporin :
They highly augmented against gram ve enterobacter and
pseudomonas.
Highly resistant to -lactamase from gram ve bacteria.
Less active on gram +ve cocci
Parenteral Oral
CEFOTAXIME CEFIXIME
CEFTIZOXIME CEFDINIR
CEFTRIAXONE CEFTIBUTEN
CEFTAZIDIME
CEFOPERAZONE
Dose : 100, 200 mg tab/cap.
100mg/5ml syr., 50mg/ml susp. CESPAN, CEFOPROX,
PROCADAX, CEPODEM, ORFIX.
Fourth generation cephalosporins :
Developed in 1990 similar to that of 3
rd
generation.
Highly resistant to -lactamases.
Active against many bacteria resistant to earlier drugs.
It has high potency and extended spectrum.
Effective in many serious infections.
Parenteral
CEFEPINE, CEFPIROME
USES :
Serious and resistant hospital acquired infections.
Septicaemia,
Lower respiratory tract infection.
Dose : 1-2g IM / IV 12 hrly.
CEFROM, CEFORTH 1g inj.
Guiding principle for the use of cephalosporins :
Cephalosporins are expensive and should not be used where an
equally effective, alternative antibiotic is available.
None of them is effective against infections by enterococci.
None of them is agent of choice of anaerobic infections.
Except for cefotaxine, ceftriazone, the CNS penetration of
cephalosporins is poor.
General features of cephalosporins
Most of them given by oral route
IM can cause pain so IV is given.
Mainly excreted by kidney.
Dosage is altered in patients with renal insufficiency.
Most cephalosporins penetrate CSF so useful for the treatment of
meningitis.
Adverse reactions :
Local reactions cause pain (IM) and cause
thrombophlebitis (IV)
Allergy skin rashes
Super infection
Nephrotoxicity
CNS toxicity
Blood toxicity
Intolerance to alcohol
Cross reactivity with penicillin
Uses :
Alternatives to pencicillins.
RTI, UTI and soft tissue infection
Penicillinase producing staph infection.
Septicaemias.
Surgical prophylaxis
Meningitis, gonorrhoea
Typhoid
Mixed aerobic and anaerobic infections
Infection by odd organism or hospital infections
Prophylactic treatment in neutropenic patients.
MACROLIDES
They are called macrolides because they contain a
many membered lactone ring to which are attached one or
more deoxy sugars.
Clarithromycin differs from erythromycin only by
methylation of the hydroxyl group at the 6 position, and
Azithromycin by the addition of a methyl substituted nitrogen
atom into the lactone ring.
Antibacterial activity :
Narrow spectrum antibiotic
Bacteriostatic but bactericidal at higher conc
Effective against penicillin resistant staphylococci
Active against gram+ve cocci and bacilli
Pharmacokinetics :
Erythromycin base - acid labile
Given with enteric coated - incomplete absorption
Its acid stable esters are better absorbed
Widely distributed in body
Metabolised in liver
Excreted through kidney and bile
Dose :
Adults 250 - 500mg 6hrly
Children 30 60mg/kg/day
Erythromycin base - ERYSAFE 250 mg tab
EROMED - 333mg tab, 125/5ml susp
Erythromycin stearate
ERYTHROCIN 250,500mg tab
100mg/5ml susp
100mg/ml ped drops
Adverse effects :
GIT epigastric pain
On high doses hearing impairment
Hypersensitivity reactions rare
Uses :
Substitute for penicillin
Whooping cough
Chancroid
Penicillin resistant infections
CLINDAMYCIN
It is lincosamide antibiotic having similar action (macrolide
50s)
Semisynthetic derivative of Lincomycin
Bacteriostatic low conc
Bacteriocidal high conc
Most active against gram+ve cocci, C.diphtheriae,
Actinomyces
Highly active against anaerobes (B fragilis)
Pharmacokinetics :
Oral absorption good
Distribution skeletal and soft tissues
Excreted in urine
Adverse effects :
Rashes
Urticaria
Abdominal pain
Superinfection
Enterocolitis
Diarrhoea
Uses :
Anaerobic and mixed infections
Doses : 150-300 mg QID oral ; 200-600mg I.v. 8 hourly
DALCAP, CLINCIN, DALCIN, 150, 300 mg cap, 300mg/2ml
and 600 mg/4ml inj.
TETRACYCLINES
Tetracyclines are napthacene derivatives.
The napthacene nucleus is made up by fusion of 4 partially
unsaturated cyclohexane radicals and hence the name
tetracyclines.
Tetracyclines are bacteriostatic.
On the basis of chronology of development, convenience
of description, divided into 3 groups.
Group I Group II
Tetracycline Demeclocyline
Oxytetracycline Methacycline
Group III
Doxycycline
Minocycline
Mechanism of action :
Tetracyclines are thought to inhibit bacterial protein
synthesis by binding to the 30 S bacterial ribosome and
preventing the access of aminoacyl tRNA to the acceptor (A)
sites on the mRNA ribosome complex.
Antimicrobial activity :
Gram+ve and ve cocci are sensitive
Gram+ve bacilli are inhibited
Entero bactereae are highly resistant
Spirochetes and Borrelia are quite sensitive
All rickettsiae and chlamydiae are highly sensitive
Pharmacokinetics :
Incompletely absorbed from GIT
Absorption is impaired by iron or zinc salts[due to chelation of
cations]
They cross the placenta and enter fetal circulation and amniotic
fluid
Widely distributed in liver ,bone marrow and spleen
They accumulate in dentine and enamel of unerupted teeth
Primarily excreted in urine through kidney
Adverse effects :
GIT-epigastric burning, nausea, vomiting,diarrhoea
Hepatoxicity
Renal toxicity
Effects on teeth-Orthophosphate complex
Thrombophlebitis
Hypersensitivity Reactions
Superinfection
Antianabolic effect
Dose :
Tetracycline 1-2g per day in adults
Children over 8yrs -25 to 50mg /kg daily in 2 to4 divided
doses
Doxycyline 100mg,12hrs first day followed by 100mg once a
day
Children over 8yrs 4-5mg /kg/day divided into 2 equal doses
during first 24hrs
TERRAMYCIN, RESTECLIN-250,500mg cap,50mg/ml
in10ml vial inj
DOXT, NOVADOX, TETRADOX-100mg cap.
Precaution :
Not to be used in pregnancy, lactation and in children
Avoided in patients on diuretics
Used cautiously in renal and hepatic insufficiency
Do not mix injectable Tc with Pn- inactivation occurs
Uses :
Mixed infections
Venereal diseases
Atypical Pneumonia, Cholera, Brucellosis, Plague,Rickettsial
infections
Alternate to Pn/Ap, Ciprofloxacin,Azithromycin
Other situations UTI,amoebiasis, chronic lung disease
QUINOLONES
These are entirely synthetic antimicrobials having a
quinolone structure that are active primarily against gram ve
bacteria.
These are quinolone antimicrobials having one or more
fluorine substitutions.
Mechanism of action :
The FQs inhibit the enzyme bacterial DNA gyrase, which nicks
double stranded DNA.
The DNA gyrase consists of two A and two B subunits; A
subunit carries out nicking of DNA, B subunit introduces ve
supercoils and then a subunit reseals the strands.
First generation FQs :
Norfloxacin Ofloxacin
Ciprofloxacin Pefloxacin
Second generation FQs :
Lomefloxacin Levofloxacin
Sparfloxacin Gatifloxacin
Moxifloxacin
CIPROFLOXACIN
First generation FQ active against a broad range of bacteria
especially gram ve aerobic bacilli.
Highly susceptible :
E coli, shigella, N meningitis, K pneumoniae, Proteus, H
influenza, Enterobacter, V. cholerae, S. typhi, N gonorrhoea.
Moderately susceptible :
Staph aureus, brucella, M. tuberculosis
Microbiological features :
Rapid bactericidal activity and high potency.
Relatively long post antibiotic effect on enterobacteriaceae
pseudomonas and staph.
Low frequency of mutational resistance.
Low protective intestinal streptococci and anaerobes are
spared.
Active against many lactam and amino glycoside resistant
bacteria.
Less active at acidic pH.
Phramocokinetics :
Rapidly absorbed on oral, food delays absorption.
High tissue penetration, concentration in lung sputum,
muscle, bone.
Excreted primarily in urine.
Adverse effect :
GIT Nausea, vomiting, bad taste, anorexia, diarrhoea is
infrequent.
CNS- Dizziness, headache, restlessness, anxiety, insomnia and
seizures are rare.
Skin/hypersensitivity rashes, pruritis, urticaria.
Tendonitis and tendon rupture
Uses :
UTI
Gonorrhoea
Chancroid
Bacterial gastroenteritis
Gr-ve septicaemias
Prophylaxis
Typhoid
Bone, soft tissue, wound infection.
RTI
Tuberculosis
Meningitis
Conjunctivitis
CIFRAN, CIPLOX, CIPROBID, CIPROLET
250, 500,750 mg tab, 200mg/100 ml IV infusion 3mg/ml eye drops.
ANTIAMOEBIC AND OTHER ANTIPROTOZOAL
DRUGS
METRONIDAZOLE :
It is the prototype nitroimidazole and found to be highly
active amoebicide.
Antiprotozoal activity :
Broad spectrum cidal activity against protozoa and
anaerobic bacteria such as B fragilis, Fusobacterium.
Metronidazole is selectively toxic to anaerobic
microorganisms.
Metronidazole has been found to inhibit cell mediated
immunity and cause radiosensitization.
Pharmacokinetics :
Completely absorbed from the small intestine.
Widely distributed in the body
It is metabolized in liver primarily by oxidation and
glucuronide conjugation, and
Excreted in urine.
Adverse effects :
Side effects relatively frequent but mostly not serious,
Anorexia, nausea, metallic taste and abdominal cramps are the
most common.
Looseness of stool is occasional,
Headache, glossitis, dryness of mouth, dizziness, rashes and
transient neutropenia.
Prolonged administration may cause peripheral neuropathy and
CNS effects
Seizures have followed by high doses.
Thrombophebitis of injected vein.
Contraindications :
In neurological disease, blood dyscrasias, first trimester of
pregnancy, chronic alcoholism.
Uses :
Amoebiasis
Giardiasis
Trichomonas vaginitis.
Anaerobic bacterial infections
Pseudomembranous enterocolits.
Ulcerative gingivitis
Helicobacter pylori gastritis/peptic ulcer
Guinea worm infestation.
FLAGYL, METROGYL, METRON, ALDEZOLE 200, 400
mg tab, 200 mg/5ml susp.
TINIDAZOLE
It is an equally efficacious congener of metronidazole, similar
to it in every way except.
Metabolism is slower.
Incidence of side effects is lower.
Metallic taste, nausea, rashes
TINIBA, TRIDAZOLE, 300, 500, 1000 mg tab, 800 mg/400 ml
I.V.
Role of antibiotics in endodontics
(jr of Dent 26 (2001) 539-48)
I ENDODONTICS AND THERAPEUTIC ANTIBIOTICS
1) Adjunct to operative treatment
2) Contingency treatment
3) Antibiotics at Obturation
4) Antibiotics for perio-endo lesion
5) which antibiotic
II TOPICAL ANTIBIOTICS AND ENDODONTICS
1) Pulpitis
2) Pulp capping
3) Root canal therapy
4) Flare- ups
5) Perio endo lesion
6) Tooth avulsion
III ANTIBIOTIC PROPHYLAXIS AND ENDODONTICS







What are local anesthetics?
Local anesthetic: are agents which block
conduction impulses in nerves. When applied
locally, they produce loss of sensation in the
desired area.
Classification
INJECTABLE SURFACE ANAESTHETIC
Low potency, short duration Soluble
Procaine Cocaine
Chloroprocaine Lidocaine
Intermediate potency and duration Tetracine
Lidocaine (Lignocaine) Insoluble
Prilocaine Benzocaine
High potency, long duration Butylaminobenzoate
Tetracaine Oxyethazine
Bupivacaine
Ropivacaine
Dibucaine

Mechanism


Local anesthetics block the conduction in
peripheral nerves that inhibited the nerve to excited
and created anesthesia.

The anesthetic is a reversible reaction. It binds and
activates the sodium channels.
Pharmacological actions
1) Effect on sensation: Block pain and temperature,
later they produce loss of sensation for touch and
pressure

2) CNS- stimulation-euphoria, restlessness and
tremors
3) CVS- All LA except, cocaine produces
vasodilatation and so hypotension. Cocaine produces
vasoconstriction and so hypertensive effect
4) other actions- relaxant effect on smooth muscles
and NM blockade
Absorption, fate and excretion
LA not absorbed through intact skin. But
absorption occur through mucous
membranes.They are usually administered
through S.C. administration. Vasoconstrictors
like adrenaline prolong their action
LA metabolised in the liver and plasma
by hydrolysis
Adverse reactions
1) Dermatitis, asthmatic attack and
anaphylactic reactions
2) Cardiovascular symptoms like hypotension
and cardiac arrest
3) Central effect like euphoria, excitation,
restlessness, tremors, and convulsions

Therapeutic uses
1) Surface anaesthesia
2) Infiltration anaesthesia
3)Nerve block anaesthesia
4) Spinal anesthesia
5) Systemic use

Lidocaine
In 1940, the first modern local
anesthetic agent was lidocaine, trade
name Xylocaine
It developed as a derivative of xylidine
Lidocaine relieves pain during the
dental surgeries
Belongs to the amide class, cause little
allergenic reaction; its hypoallergenic
Sets on quickly and produces a desired
anesthesia effect for several hours
Its accepted broadly as the local
anesthetic in United States today



Antimuscarinic drugs
Natural alkaloids (and derivatives)
Atropine (Sal-Tropine)
Scopolamine (Scopace, Transderm-Scop)
Synthetic quaternary ammonium drugs
Glycopyrrolate (Robinul)
Propantheline (Pro-Banthine)
Ipratropium (Atrovent)
Other synthetic drugs
Benztropine (Cogentin)
Tolterodine (Detrol)
Pharmacologic effects:
atropine as a prototype
Dose
(mg) Effects
0.5 Slight cardiac slowing; some dryness of
mouth; inhibition of sweating
1.0 Dryness of mouth; thirst, mild tachycardia;
mild pupillary dilation
2.0 Tachycardia; palpitation; marked dryness
of mouth; dilated pupils; some blurring of
vision
5.0 All above more marked; difficulty in
speaking, swallowing; headache; fatigue;
dry, hot skin; urinary, GI inhibition
10+ All above more marked; ataxia;
excitement; delirium; coma
Therapeutic uses
Drug Dose (mg) Onset time
Atropine sulfate
(Sal-Tropine)
0.4-1.2 0.5-1 hr
Scopolamine HBr
(Scopace)
0.4-0.8 0.5-1 hr
Glycopyrrolate
(Robinul)
1-2 0.5-0.75 hr
Propantheline Br
(Pro-Banthine)
7.5-30 0.5-0.75 hr
Antisialogogues for dentistry
Astringents and styptics:
Used in our restorative clinic for bleeding control prior to
impressions and placements of subgingival restorations.
Mechanism of action: denatures blood and tissue proteins,
which then agglutinate and form plugs that occlude the capillary
orifices.

-Nephrostat-active ingredient is 25% aluminum chloride
-Viscostat-active ingredient is 20% ferric sulfate

Vasoconstrictor
- epinephrine (epinephrine solution and dry cotton pellets
impregnated with racemic epinephrine are available for
topical application)
- tetrahydrozoline (0.5%) and oxymetazoline (0.5%)

CONCLUSION
The up-to-date dentist, and the endodontist in
particular, must be prepared to handle any
pharmacologic exigency. One must know not
only actions and reactions to drugs but also
indications and contraindications, as well as
side effects, toxicity, half life, any interaction
the newly prescribed drug may have with other
drugs the patient may be taking
REFERENCES
Endodontics 5
th
edn. John I Ingle.
K.D. Tripathi 4 th edn.
Endodontic Therapy 6
th
edn.Franklin S.
Weine.
Endodontics Cohen.
Role of antibiotics in endodontics.
(jr of Dent 26 (2001) 539-48)
Pathways of the pulp 9
TH
edn.