PRECISE PHARMACOLOGY (1).pdf

PRECISE PHARMAClJLlJ PRECISE lilJ!JjlM~~lJLlJGY
TABLE OF CONTENTS
Preface
Contributors and Acknolwledgements
Table of contents
'",
CHAPTER ONE
Introduction to Pharmacology
Definition of terms used in Pharmacology .
Pharmacokinetics ~o, o .
Pharmacodynamics .
I
1
4
Sulphonamides and trimethoprim ...............................co
Quinolones c., .
Oxazolidinones ,
Lincosamides .
Amphenicols .
Carbapenems .
Nitrofurans .
Other antibacterials .
Drugs used in the treatment of tuberculosis ..
Drugs used in the treatment of leprosy ..
90
95
108
109
112
114
116
118
128
136
CHAPTER TWO
Drug administration
Drug dosage forms ..
Description of common dosage forms 0.
Routes of drug administration .
Drug administration in special cases .
Common abbreviations used in drug administraion ..
CHAPTER THREE
Understanding drugs
Drug nomenclature , , .
Sources of drugs .
Classification of drugs ..
Schedules of controlled substances/ drugs ..
Drug storage .
Essential drugs ; ..
Rational use of medicines ..
Prescription writing ..
CHAPTER FOUR
Antibacterial Drugs
Introduction to antibacterial ..
Penicillins ; c • • •
Cephalosporins .
Macrolides .
Tetracyclines .
Aminoglycosides .
-iv-
7
7
7
15
17
20
20
20
21
22
23
27
28
j
32
36
55
77
83
8~
t
CHAPTER FIVE
Drugs used in the treatment of fungal infections
Polyene antifungals 142
Imidazole antifungals 145
Triazole antifungals 147
Allylamine derivatives 151
Other antifungals.............................................................. 153
CHAPTER SIX
Antiprotozoal Drugs
Antimalarial drugs 155
Nitroimidazoles 170
Anthelmintics 177
CHAPTER SEVEN
Drugs used in the Treatment of Viral infections
Guanine analogues .:........................................................ 190
Antiretrovirals 195
CHAPTER EIGHT
Drugs acting on Gastro- Intestinal system
Drug for peptic ulcer disease 202
Drugs for nausea and vomiting 227
Drugs for haemorrhoids and Piles ,........................ 240
Drugs for inflammatory bowel disease 243
Drugs for constipation 215
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PRECISE PHARMACOLOGY I
Antidiarrhoeal drugs :k.................................... 252
Prokinetic drugs 261
Drugs for obesity.............................. 261
"-- .......lP;"D,R..
ECLLllISE Pl1ID1AC~1J!ID'J
Drugs for scabies and pediculosis 436
Antipruritic drugs 438
Drugs for alopecia "...................................... 439
CHAPTER NINE
Drugs for Respiratory Tract Disorders
Drugs for asthma .
Drugs for allergic rhinitis ..
Drugs used in the treatment of cough 0
CHAPTER TEN
Drugs for Cardiovascular Disorders
Drugs used in the treatment of hypertension .
Drugs used in the treatment of angina pectoris ..
Drugs for heart failure 0 00 . .
Drugs for hyperlipidaemia ..
CHAPTER ELEVEN
Blood and blood forming organs
Anticoagulants .
Antiplatlet drugs 0 • • • • • • • • • . . • • • • • • • • • • . .
Thrombolytic drugs ..
Antifibrinolytic drugs .
Drugs used in the treatment of anaemia ..
CHAPTER TWELVE
Endocrine and Metabolic Drugs
Drugs for Diabetes mellitus ..
Drugs for thyroid disorders 0
CHAPTER THIRTEEN
Dermatological Drugs
Drugs for eczema ..
Drugs for psoriasis .
Drugs for acne ,
Topical Anti-infectives .
Drugs for warts 0 • • . . • • •
-vi-
.,
263
280
302
306
34
345
355
365
370
373
375
376
381
397
400
408
413
419
434 )
t
CHAPTER FOURTEEN
Drugs for the eye
Antibacterial eye preparations ..
Antiviral drugs ' .
Drugs used in allergic conjunctivitis ..
Non-steridal antinflammatory eye preparations ..
Drugs for glaucoma .
CHAPTER FIFTEEN
Drugs used in the management of CNS disorders
Drugs used in the treatment of depression ..
Drugs used in the treatment of epilepsy ..
Anxiolytic , sedatives and hypnotics ..
Drugs used in the treatment of parkinsonism ..
Antipsychotic drugs .
CHAPTER SIXTEEN
Analgesics
Non-opiod analgesics .
Opiod analgesics 0.
Drugs used in the treatment of migraine .
Skeletal muscle relaxants ..
CHAPTER SEVENTEEN
Obstetric and gynaecological drugs
Drugs used in the treatment of menstrual disorders ..
Drugs used in treatment of infertility : .
Drugs used in treatment of pre-eclampsia
and eclampsia .
Drugs used during labour .
Drugs affecting lactation .
Drugs used in the treatment of endometriosis ..
Drugs for contraception " ..
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442
447
448
452
452
459
475
490
501
507
521
525
532
535
541
546
550
552
560
562
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PRECISE PHARMACOLOGY
CHAPTER EIGHTEEN
Drugs for urologic disorders
Drugs for benign prostatic hyperplasia.......................... 570
Drugs for Erectile dysfunction 575
CHAPTER NINETEEN
Drugs for muscular skeletal disorders
Drugs for gout 0 00.00................ 579
Drugs used in the treatment of rheumatoid arthritis 582
Non steroidal anti-inflammatory drugs............ 585
CHAPTER TWENTY
Drugs used in the treatment of cancer 60 I
I.
CHAPTER TWENTY ONE
Drugs used in anaesthesia
Local anaesthetics 612
General anaethetics 612
Depolarizing neuromuscular blocking drugs 622
CHAPTER TWENTY TWO
Vaccines and immunoglobulins 625
Index ,· c. 640
-viii -
i
1
ACE
ADH
ADR
AAFB
Ag
AIDS
BP
Ca
CHF
CI
CMV
CNS
COC
COPD
COX
CSF
CT
CxR
DM
DMARD
DU
DVT
E/C
ECG
ECT
EEG
ENT
FBC
g
G6PD
GA
GI
GTN
HAART
HAV
Hb
PRECI~i'Q:!)1i!MilQI!IHijl
COMMON ABBREVIATIONS
Angiotensin-Converting Enzyme
Antidiuretic Hormone
Adverse Drug Reaction
Alcohol Acid-Fast Bacillus
Antigen
Acquired Immune Deficiency Syndrome
Blood Pressure
Carcinoma
Congestive Heart Failure
Contra -Indication
Cytomegalovirus
Central Nervous System
Combined Oral Contraceptives
Chronic Obstructive Pulmonary Disease
Cyclo Oxygenase
Cerebrospinal Fluid
Computerised Tomography
Chest X-ray
Diabetes Mellitus
Disease Modifying Antirheumatic Drugs
Duodenal Ulcers
Deep Vein Thrombosis
Enteric Coated
Electro Cardio Gram
Electro Convulsive Therapy
Electro Encephalogram
Ear, Nose and Throat
Full Blood Count
Gram
Glucose 6-Phosphate Dehydrogenase
General Anaesthetic
Gastro Intestinal
Glyceryl trinitrate
Highly Active Antiretroviral Therapy
Hepatitis A Virus
Haemoglobin
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_1111111 R£ PRECiSE PHARMACOLOGY ] "I ~PHARMACOLOGY
HBV
HCV
HDL
HDV
Hg
HIV
HRT
HSV
IDDM
i.e.
1M
INF
INH
inj 5"
lOP !IlW
IU ,1"
IV
Kg
L
LDL
LFT
LH
LMWH
LVF
LVH
m2
MAOls
MAX
MCG
MDI
mEq
MG
mg/kg
MI
Min
ml
mmHg
Hepatitis B Virus
Hepatitis C Virus
High Density Lipoprotein
Hepatitis D Virus
Mercury
Human Immunodeficiency Virus
Hormone Replacement Therapy
Herpes Simplex Virus
Insulin Dependent Diabetes Mellitus
That is to say
Intramuscular
Infusion
Isoniazid
Injection
Intraoccular Pressure
International Units
Intravenous
Kilogram
Litre
Low Density Lipoproteins
Liver Function Test
Luteinising Hormone
Low Molecular Weight Heparins
Left Ventricular Failure
Left Ventricular Hypertrophy
Metres Squared
Monamine Oxidase Inhibitors.
Maximum
Microgram
Metered Dose Inhaler
Milliequivalent
Milligram
Milligram per Kilogram body weight.
Myocardial Infarction
Minutes.
Millilitre
Millimetres of Mercury
-x-
.'
l
MMOL
MRI
NNRTls
NRTls
NSAID
OA
OC
PI
PID
PMS
PPI
RA
RTI
SC
SPP
SSRI
STD
STI
TB
UC
USP
UTI
VDRL
VLDL
WHO
Z
Millimole
Magnetic Resonance Imaging
Non Nucleoside Reverse Transcriptase Inhibitors
Nucleoside Reverse Transcriptase Inhibitors
Non Steroidal Anti Inflammatory Drugs
Osteoarthritis
Oral Contraceptives
Protease Inhibitors
Pelvic Inflammatory Disease
Premenstrual Syndrome
Proton Pump Inhibitor
Rheumatoid Arthritis
Respiratory Tract Infection
Subcutaneous
Species
Selective Serotonin Reuptake Inhibitor
Sexually Transmitted Disease
Sexually Transmitted Infection
Tuberculosis
Ulcerative Colitis
United States Pharmacopoeia
Urinary Tract Infection
Venereal Diseases Research Laboratory
Very Low Density Lipoprotein
World Health Organization
Pyrazinamide
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en 'I PRECISE PHARMAciII!n!t. PRECISE IiHAftMACOLOD
CHAPTER ONE
INTRODUCTION TO PHARMACOLOGY
Pharmacology is thest~dy of drugs and their intei"action with the
living system. The term phil:rmacology comes from the Greek words
pharmakon meaning medicine and the suffix -ology meaning study
of.
1.1.1 Definition of terms used in Pharmacology
Therapeutics
Therapeutics is a branch of medicine that deals with different methods
of treatment especially the use of drugs in the cure of diseases.
Toxicology
This is the study of the adverse effect of the drugs on the living
system.
Chemotherapy
Chemotherapy is the use of chemical agents or drugs to treat cancer or
~other diseases caused by bacteria, fungi, viruses or parasites.
Classfication of Pharmacology.
Pharmacology is divided into two:-
.:. Pharmacokinetics
.:. Pharmacodynamics
1.1.2 PHARMACOKINETICS
Pharmacokinetics is the study of what the body does to the drug.
It includes:-
.:. Absorption
.:. Distribution
.:. Metabolism
•:. Excretion
-1-
Drug absorption
Before a drug can exert a pharmacological effect in tissues, it has to be
taken into the blood stream. Absorption is the movement of a drug from
the site of administration into the blood stream (general circulation).
Drugs are absorbed from the gastro intestinal tract mainly by passive
diffusion or active transport.
Factors affecting absorption
.:. Rate of dissolution of a drug
Since a drug has to be dissolved before it is absorbed, drugs
present in formulations that allow rapid dissolution will be
absorbed faster.
•:. Blood flow:
Absorption of the drug is fastest from sites where blood flow
is high.
•:. Lipid solubility of a drug
Highly lipid soluble drugs can readily cross the membrane
compared to those with low lipid solubility.
Bioavailability
Bioavailability is the extent to and the rate at which the active moiety
(drug or metabolite) enters systemic circulation, thereby accessing the
site of action.
Factors affecting Bioavailability.
First pass metabolism: If a drug is rapidly metabolized on its first
entry into the liver, the amount of unchanged drug that reaches system's
circulation is decreased.
-
Solubility of the drug: Drugs that are very hydrophilic are
poorly absorbed because of their inability to cross the lipid-rich cell
membranes.
Chemical instability: Some drugs such as penillin G are unstable to
the PH of gastric juice contents.
-2-

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1
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1,11 ' PRErm)PHARMAClllOGY
1 , I I I f ,f', 1"".!1'111 I
Nature of the drug formulation: The size of the particles, salt form
and excipients such as binders, disintergrants can influence the ease of
dissolution and affect the rate of absorption of the drug.
Drug Distribution
After a drug enters the systemic circulation, it is distributed to
the body's tissues. Distribution is the movement of a drug from
the general circulation into different organs and fluids of the body.
Distribution is generally uneven and is influenced by the following
factors:-
•:. Blood flow to the tissues
.:. Capillary permeability (ability of a drug to exit the vasc~lar
system).
.:. liAbility of a drug to enter cells
•:. Regional pH
Drug Metabolism
Metabolism is the enzymatic alteration of a drug structure. This normally
takes place in the liver. Metabolism may result into the following:-
.:. Promotion of renal excretion of the drug
.:. Activation of inactive drugs (Pro-drugs)
.:. Enhancement of therapeutic action of the drug
.:. Alteration of toxicity of the drug
Factors influencing individual drug metabolism rates include;
.:. Genetics
.:. Co-existing disorders e.g. chronic liver disorders
.:. Drug interaction.
Excretion
Excretion is the removal of drugs from the body. Drugs may be excreted
through any of the following:- ::1: ,
.:. Urine "';'
.:. Bile
.:. Feaces
II
.:. Breast milk
.:. Sweat
I
.:. Saliva
.:. Expired air
-3-
PRECISE IQ:m;!M'~OLOGY
1.1.3 PHARMACODYNAMICS
Pharmacodynamics is the study of what the drug does to the body.
Common Terms Used In Pharmacodynamics
Efficacy
This is the ability of the drug to produce maximal response.
Potency
Potency is a measure of how much drug is required to elicit a
response.
Drug receptor
It is a specialized cell component that combines with a drug or hormone
to alter cellular functions or mediate its pharmacological action.
Halflife
This is the time taken to reduce the amount of the drug in the body by
one half during elimination
Therapeutic dose
This is a dose between the minimum effective and the maximum doses
which provides the desired effect without toxic effects.-
Therapeutic index
This is the ratio of the dose that produces toxicity to the dose which
produces clinical response. Therapeutic index is thus a measure of
the drug'S safety since the higher the therapeutic index, the safer the
drug.
Toxicity
This is an adverse drug reaction caused by excess drug in the body. This
may be due to excessive dosing or accumulation of the drug.
Agonist
An agonist is a substance that binds to the receptor and causes a
response.
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..... ------'-P--'-'R=EC
...
lm"'"--'--PHARMACdI
Antagonist
An antagonist is a substance that binds to a receptor and prevents a
response.
..,
Partial agonist
Partial agonist is a substance that binds to a receptor and cause effects
similar to but less than that of a pure agonist.
Side effects
These are expected, well known, undesirable effects of a drug that
occur at doses normally used for therapy.
Adverse efffects
These are any noxious, undesirable and unintended effects that occur
at normal drug doses.
Drug interaction
This is the alteration of one drug by another. It occurs when two
or more drugs are administered to a patient simultaneously. Drug
Illteraction may result into either negative effects or positive effects.
Synergism
It 1 it drug interaction in which two drugs combine to give a therapeutic
(.lIcKt which exceeds the sum of their separate effect e.g. gentamycin
I Jlclflldilins have synergistic effect in the treatment of bacterial
Illf••(lIon5,
Tolc'r.1ncc'
lolt',.lIu" II .1 p,rlldual decrease in response to a drug as a result of
re'pt•.IIMd dilly' .lhllinistration. Tolerance may occur through a decrease
111 IIIt' CO"Cl:lIlII.lt Ion of drug at the receptor or through decrease in
le~poll"l' of I"" !'''coptor to the same concentration of a drug.
Drug dcpc'ndcmc'(
This is Iht· (Olllp"I..IVt. lise of a substance resulting in physical,
psychologlcll 01 OC 1.11 11.11111 to the user with continued use despite
the harm.
s-
Psychological dependence
This is the emotional state of craving for a drug whose presence has a
desired effect on mind or whose absence has an undesired effect.
Allergic reaction
This is an immunologically mediated adverse response to a drug
requiring previous sensitization.
Anaphylaxis
This is a state of immediate hypersensitivity following sensitization to
a foreigh protein or a drug. It is characterized by itching, swelling of
the mouth: wheezing, sudden drop in blood pressure and sometimes
death.
Idiosyncratic drug reaction
This is an unusual and unpredictable response to a drug based on a
genetic predisposition.
Teratogenic effect
This is a drug-induced birth defect
Carcinogenic effect
This a drug-induced cancer
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" ' ", ~~PHAftMACOLOGY
r-----~nn. -- n
CHAPTER TWO
DRUG ADMINISTRATION
2.1.1 DRUG DOSAGE FORMS
This is a form in which a medicine is prescribed for use by the patient
such as injections, tablets, capsules or syrups.
Dosage forms do not contain just the active ingredient but also contain
other components called excipients or additives. These make the dosage
form suitable for handling, administration and enable it to release the
active medicaments in the appropriate manner to make it efficacious
for treatment of diseases or conditions.
Dosage forms can be in solid, semisolid, liquid or gaseous form.
Common dosage forms and their routes of administration
Route of administration Dosag•
I
,
Oral Tablets, capsules, solutions, syrups, elix-
irs, suspensions, emulsions, gel, powder,
III
-----_.~-~---~-------_."-
granules.
Rectal Suppositories, ointments, creams and
.... solutions
------_._----
Topical Ointment, creams, pastes, lotions, gels,
---------_.
solutions, topical aerosols (sprays)
Parenteral Injections (solutions, suspensions,
.. I emulsion)
Lung Aerosols, inhalation sprays
liasal ,!l:m!L. Solutions, inhalations and gases
.~ye
.....•.. Solutions, ointments and creams
Ear ·m:H~i!!. Solutions, suspensions, ointments
...........
2.1.2 Description of common dosage forms
Tablets
Tablets arc solid dosage forms containing one or more dried compressed
active drug as WI·II as binders.
7-
..
Types of tablets
Tablets are formulated as coated or uncoated.
Coated tablets include enteric coated, sugar coated, film coated and
slow-release coated tablets.
Enteric coated tablets: These tablets are covered with a special
coating which resists break down in the stomach but dissolves in the
alkaline environment in the small intestine where the drug is absorbed.
The coating is inteded to avoid irritating the stomach.
Slow-release tablets: These tablets are manufactured to provide a
continuous, sustained release of certain drugs. These tablets names are
accompanied by abbreviations such as S.R (slow release)or L.A (long
acting) e.g Nifelat R®, Olfen S.R ® or Adalat LA ®
Sugar coated tablets: These are formulated with a sugar coating to
disguise the bitter taste of the active ingredient.
Film coated tablets
These tablets are covered with a very thin layer of coating materi~L
Scored tablets: These tablets have an indented line running across
the top of the tablet. Scored tabletes can easly be broken down into 2
pieces.
Caplets.
These are easy-to-swallow coated tablets in forms of capsules e.g.
panadol®
Effervescent tablets
These are uncoated tablets containing acidic substances and either
carbonates or bicarbonates which react rapidly in the presence of
water to release carbondioxide. They are intended to be dissolved in
water before administration. e.g. dispersible tablets
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. 1
PRECISE PHARMACOLOGY]
Capsules
Capsules are cylindrically shaped solid unit dosage form containing one
or more substance enclosed within a hard or soft gelatin shell.
Types of capsules:
Slow release capsules: These capsules contain pellets that dissolve
in the GIT releasing the drug slowly thereby producing sustained drug
action. e.g. Olfen S.R ®
Soft gelatin capsules: These capsules contain the drug in liquid form
inside the shell e.g. vitamin A capsules
Hard shell capsules: These are manufactured in two pieces which fit
together and hold the powder.
A cream
This is a semisolid emulsion of an oil and water (with the main ingredient
being oil).
Lotions
These are liquid or semi-liquid preparations containing one or more
active ingredients in a suitable vehicle. They are intended to be applied
to the unbroken skin without friction. e.g. calamine lotion.
Emulsion
An emulsion is a suspension in which fat particles are mixed with
water.
Suppository
It is a solid dosage form containing a solid base of glycerin or cocoa
butter intended for insertion into the body orifices where it melts,
dissolves and exerts a systemic or localised effect.
9
PRECI~ PHARMACOLOGY
Pessaries
These are solid preparations containing one or more active ingredients
intended to be inserted into the vagina.
Suspension
This is a liquid preparation containing fine, undissolved particles of a
drug suspended in it.
Aerosol
This is a pressurized preparation that when activated releases a fine
dispersion of liquid or solid materials in a gaseous medium.
Enema
A liquid intended to be injected into the rectum.
Inhalation
Drug droplets, vapour, or gas administered by the oral or nasal
respiratory route via an aerosol or nebuliser.
Injection
A sterile, pyrogen-free preparation intended to be administered using a
needle and syringe (parenterally).
Lozenges (troches)
Disk-shaped solid preparations intended to slowly dissolve in the oral
cavity for localized effects.
Mouthwashes
These are aqueous solutions containing one or more active ingredients.
They are intended for use in contact with the mucous membrane of
the oral cavity.
Ointment
A semisolid preparation intended for external application to the skin or
mucous membranes.
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",'" :' , ",'" ~ECISEPHARMACl!I!!I!DI
, I 1[1 I I
PRI3Q~'f PHARMACOLOGY I
Advantages Disadvantages
Intramuscular (1M) Injection
The drug is injected in one of the large skeletal muscles e.g. deltoid.
Intravenous (IV) injection
Drugs are injected /administered directly into the blood stream via a
vein where it is distributed in blood all over the body.
Parenteral route is the fastest route by which a drug can be absorbed.
It includes:-
.:. Intraveneous
.:. Intramuscular
.:. Subcutaneous
.:. Intradermal
.:. Intrathecal
.:. Intra-articular
It requires a trained personnel
to administer the drug
• Drugs that give depot effect such •
Benzathine penicillin can be given
by this route
Advantages Disadvantages,
• A quick onset of action is achieved • The drug has to be administered
by atrained person
• The entire dose ofthe drug is • In cases oftoxicity, retrieval of
administered the drug is not possible
• A lower dose is given compared • It requires strict sterility
to oral route
• Administration is useful for • It is painful
drugs that are irritant when
administered.
Syrup
A concentrated sugar solution in water that may contain a flavoring
agent or drug.
2.1.3 ROUTES OF DRUG ADMINISTRATION
These are various ways in which drugs are administered into the body.
Drugs can be administered by several different routes as determined
by the intended site of action, rapidity and duration of effect desired,
chemical and physical properties of the drug.
•:. Parenteral route
.:. Topical route
~. Enteral route
.:. Inhalational route
Spray
A liquid minutely divided or nebulised as by a jet of air or a stream.
,ffi1
Solution
A liquid preparation containing soluble chemical substances usually
dissolved in water.
Eye drops
These are sterile aqueous or oily solutions or suspensions of one or
more active ingredients intended for instillation into the eye.
Powder
A mixture of finely divided drug particles or chemical substances.
Pellet (Implant)
A sterile, small, rod or ovoid-shaped mass intended to be implanted
under the skin for the purpose of providing the slow release of
medication over an extended period of time.
Parenteral route
Drugs given by this route are in form of solutions, suspensions, and
emulsions.
• It is generally faster than
subcutaneous route
• Absorption of the drug is
sometimes variable depending
on which muscle is used
-11- -12-

PRECisE PHARMACOLOGY I III PRECISE PHARMACOLOGY I
• Relatively irritating substances • Some drugs given 1M can be
may be given. painful e.g. Ceftriaxone injection
Its less painful compared to IV • Self administration of the drug is
injection not possible.
Subcutaneous (sc) Injection
The drug is injected into the subcutaneous tissue, the fatty layer of
tissue underneath the dermis. It is commonly used in administering
vaccines and insulin. This route of administration, like the intramuscular,
provides absorption that is slower than the IV route.
• Wastage of drugs is possible
since there is no measurable
dose
Enteral route
This includes; rectal, oral, sublingual, and buccal routes.
Rectal route
Drugs are administered via the rectum in form of suppositories or
enema
Topical route
Drugs are applied directly to the skin or the mucuos membrane of
the eye, ear or nose. Drugs given by this route are in form of creams,
ointments, lotions, gels etc.
Advantages ,lIl1111 II' Disadvantages
Absorption is slower than 1M • Can be painful
injection .i<liill::lH
The patient can self administer the • Irritating drugs may result in
drug severe pain and local tissue
necrosis
• Care has to be taken not to
inject IV
'---------
'I
Disadvantages
Advanta es
Self administration of the drug is
possible
Its less expensive compared to
parenteral route.
Its easy to monitor the )
treatment
• Some drugs like Dithranol
ointment stain the skin and
clothe
• Adverse skin reactions are
possible
• Some drugs like topical steroids
bleach and cause thining of the
skin
13 --
Advantages lUll IlIlUi
Disadvantages
• Provides a safe route • May be uncomfortable and a
for a patient who is embarrassing for the patient
vomiting, unconscious or
unable to swallow
• Provides an effective • Drugs may result in irregular or
route to treat vomiting incomplete drug absorption depending
on whether faeces are present.
• It is faster than oral • May stimulate the patient'svagal nerve
route by stretching the anal sphincters
• It avoids destruction of
medication by digestive
enzymes in stomach and
small intestine
• Drugs may be given
for local effects e.g.
haemorrhoids
Oral route
The oral route is the most convenient and safest route of drug
administration. Drugs are given by oral route in form oftablets, capsules,
syrups, suspension or powders.
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PRECISE P1:Ji1;IMMol!II!f1
Advantages Disadvantages
• It is cheap for the patient • Has a delayed action and hence
not suitable for emergencies
• It does not require a skilled • It requires patient commitment
person to administer the drug to improve on compliance
• Self administration of the drug • Oral route can not be used by a
is possible patient in coma
• Some drugs can only be given • Psychiatric patients and children
by the oral route e.g. nifedipine may refuse to take the drug by
oral route
.. In case of drug toxicity. it can be • Some drugs can be destroyed
retrieved by the GIT enzymes e.g. insulin
• It is not suitable for a patient
I" who is vomiting
• A higher dose is required
compared to parenteral route
Sublingual route
The drug, usually in form of a tablet, is placed under the tongue and
allowed to dissolve slowly. e.g. Nitroglycerin.
The drug is absorbed qUickly through the oral mucous membrane into
the blood stream. It provides a faster therapeutic response than the
oral route.
2,1.4 DRUG ADMINISTRATION IN SPECIAL CASES
Drugs should be administered with special attention in the following
cases; pregnancy, lactating mothers, paediatrics, and geriatrics.
Pregnancy
Generally drug therapy during pregnancy is not needed unless
absolutely necessary as many of them cross the placenta and harm the
fetus. Drugs can affect the fetus in any of the following ways;
By directly causing damage, abnormal development leading to
birth defects or death.
Altering the physiological function of the placenta causing
vasoconstriction thus reducing supply of nutrients and
15-
,PRECISE PHARMACOLOGY I
oxygen to the fetus. This results in under development or
under weight babies.
Can cause contraction of the uterine muscles injuring the fetus or
causing preterm labor.
Examples of drugs contra-indicated in pregnancy;
Drug Effect
ACEls Cause fetal and neonatal mortal-
ity and morbidity
Phenytoin Minor cranio-facial defects
Streptomycin Damage to the fetus's ears re-
sulting into deafness.
Tetracycline Permanent yellowing of the
teeth.
Paediatrics
A number of drugs are not used during childhood because they are
associated with serious adverse reactions.
Drug Effect
Aspirin Reye's syndrome
Tetracyclines Permanent discoloration of teeth
Quinolones Arthropathy(cartilage break-
down)
Classification of paediatric age groups
Premature infants < 36weeks of gestation
Full term infants 36-40weeks gestation age
Neonates less than 4 postanatal weeks
Infants 5-52 weeks
Children 1-12years
Adolescents I 2-16years
-16-

•
PRECISE p@liJMtdolll1il'1 illll'
Lactating mothers
If a drug enters breast milk in pharmacologically significant quantities,
therapeutic doses in the mother may cause toxic effects in the infant.
In addition, some drugs suppress lactation such as combined oral
...
contraceptives while others may inhibit the infant's sucking reflex.
With the above challenge, a proper decision should be made when
drugs are prescribed to a breastfeeding mother.
Geriatrics
A geriatric patient is a person who is 65years of age and above.
The prescription and use of drugs in the elderly must be carefully
planned and monitored.
This is because elderly patients are at a high risk of experiencing
problems with drug therapy due to decline in organ function and the
risks of polypharmacy.
During prescribing, attention should be focused on drug interactions,
liver and renal function and a simple treatment plan.
2.1.5 COMMON ABBREVIATIONS USED IN DRUG
ADMINISTRATION
Abbt~viation I
' ,
M~aning
od Once daily
bd Twice daily
tds Three time daily
q.i.d Four times daily
....
q.h Every hour
p.r.n When needed
stat Irrmediately
o.m Each morning
o.n .'m. Each night
a.c Before meals
1---",--"
i l '/!!" After meals
p.c ----
--po ... By mouth
im Intramuscular
-----
17-
iv Intravenous
sc Subcutaneous
Mist Mixture
Inj Injection
Aq Water
caps Capsules
Tab Tablet
SUDD SUppository
Dess , A pessary
Syr Syrup
Ung Ointment
Inf Infusion
Enem Enema
Gut Drops
g Gram
mg Milligram
ml Milliliter
JJg Micrograms
--18-

I'
:11
!
I ~TlCISE PHARMACI!lLOGY
/
• • • • • •1I11'1l111111!1111llIllllll1lli_' ----l.P...!.!.!RE~CI=SE~PH~AR=M.:.:.=ACc::.::O[:=:OG:.:....IYI
Common examples of generic and brand names
CHAPTER THREE
UNDERSTANDING DRUGS
'.. A drug is any chemical substance administered in the body or a biological
system that affects the structure or functioning of a living organism.
Drugs are used for prevention, diagnosis, treatment of diseases and
relief of symptoms.
Generic name
Amoxicillin
Propranolol
Paracetamol
Salbutamol
Diazepam
Brand name
Amoxil®, Duramox®, Amoxapen®
Inderal®
Panadol®, Kamadol®, Cetamol®
Ventolin®, Vental®
Valium® , Slitizem®
3.1.1 DRUG NOMENCLATURE
A drug may have three categori.es of names namely:-
.:. Chemical name
.:. Generic name
.:. Brand name
Che~ical name:
The chemical name describes the drug's chemical composition and
molecular structure. It's not normally used during prescribing because
it is cumbersome.
3.1.2 SOURCES OF DRUGS
Drugs for medical use can be obtained from any of the following
sources:-
.:. Plants e.g. digoxin, morphine, quinine.
•:. Animals e.g. insulin, adrenaline.
.:. Microorganisms e.g. penicillins, streptomycin.
•:. Chemical substances (made from factories) e.g. ampicillin,
diazepam.
.:. Minerals e.g. iron.
Brand name (Trade or proprietary name):
The brand name is the copyrighted name that is given by the company
manufacturing and selling the drug.
Generic name (non proprietary name):
The generic name is the name approved by a competent drug body
e.g. food and drug administration (FDA). It is much simpler than the
chemical name and is commonly used in prescribing.
Example
Chemical name
Generic name
Brand name
(+/-)-2-(p-isobutylphenyl) propionic acid
i b u p r o f e n .
Brufen®
-19-
3.1.3 CLASSIFICATIONS OF DRUGS
Drugs may be classified in the following ways:-
,.:. Prescription classification.
.:. Pharmacological classification.
•:. According to drug legislation.
Prescription classification
In this classification, drugs are classified basing on whether they are
obtained using a prescription (prescription only medicine) or they can
be obtained without a prescription (Over The Counter drugs).
PrescriptioJlt drugs: These drugs can only be obtained when a patient
presents a valid prescription to a pharmacy. Examples of pre~cri~t~on
drugs include: - Amoxicillin, Ciprofloxacin, Diclofenac and Nlfedlpme
among others.
-20-

OLlJGY
Non prescription drugs (over the counter drugs). These drugs can be
obtained from either a pharmacy or a drug shop without a prescription.
Examples of over the counter drugs include:- Panadol®, Hedex®,
Vitamins and Goodmorning syrup® among others.
Pharmacological classification
Drugs can be classified using this system basing on:-
Target body system such as cardiovascular drugs
Activity on microorganisms such as Antibiotics, Antivirals and
Antifungal among others.
Legal classification
Legal classification divides the drugs as follows:-
Class A drugs: morphine, pethidine, cocaine (schedule Iand 2)
Class B drugs: phenobarbitone, ciprofloxacin, amoxycillin, diazepam,
codeine, griseofulvin, metformin etc (Schedule 3, 4, and 5 and)
Class C drugs: over the counter drugs
3.1.4 SCHEDULE OF CONTROLLED SUBSTANCES.
Schedule I drugs
Drugs from this schedule includes:- heroin, Iysergide (LSD) etc
These drugs have a high abuse potential and are not currently used
medically.
Schedule II drugs
Drugs from schedule II include:- morphine, codeine, pethidine,
methadone, cocaine among others.
They have high abuse potential and acceptable medical uses.
They may lead to severe physical and psychological dependence.
Schedule III drugs
Drugs from schedule III include:- phenobarbitone, preparations
containing limited opioid quantities, preparations combined with one
or more active ingredients that are non controlled substances e.g.
Paracetalllol with codeine (co-codamol)
-21-
• • PRECI~1~ PHARMACOLOGY _
They have less abuse potential than drugs in schedule I and II and have
accepted medical uses.
Schedule IV drugs
Drugs from schedule IV include:- diazepam, lorazepam.
They have lower abuse potential than drugs in schedule 1- III and have
accepted medical uses.
il41it*,
Schedule V drugs "
Drugs from schedule V include those drugs that are generally for relief
of cough or diarrhoea that contain limited quantities of certain opioid
controlled substances e.g. Loperamide, piritex with codeine syrup,
kaolin etc. .
p ..
They have lower abuse potential because of their low strength and
have accepted medical uses.
3.1.5 DRUG STORAGE
Stability of drugs depends on factors such as
.:. Temperature
.:. Air
.:. Light
.:. Humidity
.:. Dosage form
.:. Active ingredient
.:. Manufacturing process
In general, drugs should be stored according to the manufacturer's
recommendations. Most of the drugs shuld be stored in a cool, dry
place out of reach of children.
Some drugs need to be stored in a refrigerator for example Insulin,
vaccines, amphotericin B among others.
Other drugs are sensitive to light therefore should be kept in a dark
place.
Class A drugs like pethidine are stored according to legal requirement
I.e. they are kept in a lock and key box.
-22-

PRECISE PHARMACOLOGY
• • • • • • • • • •1II11111m.mCISE PHARMACOLOGY I
Examples of essential drugs in Uganda
2.1.6 ESSENTIAL DRUGS AND RATIONAL MEDICINE USE
Essential drugs (medicines) are those which satisfy the health needs of
the majority of the population. These drugs should therefore always be
available in adequate quantities and appropriate dosage forms.
Antibacterials Amoxicillin
Amoxicillin + c1avulanic acid
Benzathine penicillin
Benzylpenicillin
Ceftriaxone
Cefuroxime
Flucloxacillin
Cloxacillin
Chloramphenicol
Ciprofloxacin
Cotrimoxazole
Doxycycline
Gentamycin
Erythromycin
Antituberculosis Ethambutol
drugs Isoniazid
Pyrazinamide
Rifampicin
Streptomycin
Antifungal drugs Amphotericin B
C1otrimazole
Fluconazole
Griseofulvin
Ketoconazole
Miconazole
Nystatin
. ~ - - - - - - -
..
Antileprosy drugs Clofazimine
Dapsone
Rifampicin
Thalidomide
Antiamoebic
Antimalarials
CLASS
Criteria for selection of essential drugs
The selection of essential drugs is based on the following factors:-
.:. Pattern of disease prevalence in the country.
.:. Available treatment facilities.
.:. Training and experience of available personnel.
.:. Available financial resources.
.:. Genetic, demographic and environmental factors.
.:. Efficacy and safety proven from clinical data.
.:. Assured quality and bioavailability.
.:. Stability under normal conditions of use and storage.
.:. Cost/ benefit ratio.
•:. Formulation as single compounds.
.:. Combination products evaluated on the basis of therapeutic
effect,
.:. Safety and patient compliance.
Artemether
Artemether/ lumefantrine
Dihydroartemesinin/piperaquine
Quinine
Primaquine
I r:-A-.::rt-.::e=s:..::u~n~at::..::e;.../a:..::m_o:..::d_i_aq...!.u_i_ne _
Metronidazole
Tinidazole
-23- ---24-

ElF PRECISE PHARMACOLOGY I Qi!#B~f PHARMACOLOGY I
Antiepileptics and Carbamazepine
anticonvulsants C10nazepam
Diazepam
Ethosuximide
Magnesium sulphate injection
'"
Phenobarbitone
Phenytoin
Valproic acid
Anthelmintics Mebendazole
Albendazole
Ivermectin
Praziquantel
Diethylcarbamazine
Analgesics and Acetylsalicylic acid
antipyreties Diclofenac
I~t', Paracetamol ---
Antigout drugs Allopurinol
Colchicine
Indomethacin
Probenecid -----_..~ ...
Opioid analgesics Codeine
Morphine
Pethidine
Dihydrocodeine
Antiviral drugs Acyclovir
Ganciclovir
Cardiovascular drugs Atenolol
Isosorbide dinitrate
Nifedipine
Propranolol
Verapamil
Captopril
Hydralazine
Methyldopa
I
Lisinopril
I
Digoxin -----~---
-25-
Dermatological drugs Benzoic acid + salicylic acid
Miconazole
C1otrimazole
Benzyl peroxide
Coal tar
Dithranol
Podophyllum resin
Salicylic acid 2%, 5%
Silver nitrate pencil 40%
Betamethasone cream
Calamine lotion 15%
Hydrocortisone cream/ ointment 1%
Malathion lotion 0.5%
Benzyl benzoate lotion 25%
Silver sulphadiazine cream I%
Neomycin + bacitracin ointment
Chlorhexidine cream 5%
Antiulcer drugs Cimetidine
Omeprazole
Ranitidine
Magnesium trisilicate compound
Antiemetics Domperidone
Promethazine
Metoclopramide
Cyclizine
Laxatives Bisacodyl
Senna I
Antidiabetic drugs Insulin I
Glibenclamide
Metformin
Tolbutamide
-26-

p' • I!: IJ! I I L PRECISE PHARMACOLOGY I
3.1.7 RATIONAL USE OF MEDICINES
Rational use of medicine means that patients receive medicines
appropriate to their clinical needs, in appropriate doses and for
an adequate period of time and at costs affordable to them and the
community.
Cytotoxic drugs
~ 'II
~ .
Asparaginase
Calcium folinate
Cyclophosphamide
Cytarabine
Dacarbazine
Dactinomycin
Fluorouracil
Doxorubicin
Hydroxyurea
Mercaptopurine
Methotrexate
Methotrexate
Mustine
Stilboestrol
Thioguanine
Vincristine
.:. Inconsistent drug supply in health centres
.•:. Lack of medicine formulary in hospitals
.:. Promotional misleading claims by drug companies
.:. Inadequate drug regulation
.:. Bribing of prescribers / Dispensers by drug companies
.:. Poor attitude towards continuing medical education
Consquences of irrational use of medicines
.:. Over use of antibiotics leads to development of
resistance
.:. Leads to wastage of scarce resources
.:. Leads to increased costs of drugs to the patient
.:. Increases adverse drug reactions (especially with poly-
pharmacy)
.:. May lead to loss of patient confidence in the health
system
.:. May lead to poor patient outcome
3.1.8 PRESCRIPTION WRITING
Irrational use of medicines
Irrational use of medicines involves use of too many medicines per
patient, wrong choice of drugs for particular condition, inadequate
dosages and unnecessary use of injections where oral dosage form can
be applicable, indiscriminate use of antibiotics in the treatment of viral
infections such as cough, diarrhoea among others.
Factors underlying irrational medicine use;
•:. Heavy patient load (most prescribers target clearing the line)
.:. Poor communication skills among the medical personnels
.:. I ;lek of ethics among the medical personnels
•:. Iil.lppropriate interpretation of lab tests
.:. Poor attitude towards work
.:. Milo,Hlillg beliefs by the patient (some patients believe they
can oilly be cured by injections)
-27-
Definition:
..
A prescription is a written instruction from a prescriber (doctor,
dinical officer, a midwife or a nurse.) to a dispenser (pharmacist,
pharmacy technician or nurse) on medicines to be administered to a
patient.
rile prescriber has a duty of care to provide a prescription that is
I.'gible in order to minimize the potential for errors in treatment.
Generally a good prescription should contain essential information as
outlined below.
-28-

gil!tISE PHAQMACOLOW
It should:-
.:. Be written legibly in ink
.:. Be dated and indelible
.:. State the full name and address of the patient
.:. Specify the age and weight of the patient (especially Children) ...
.:. State the diagnosis
.:. Have the name of drugs written in full
.:. State the form, dose and strength of the drug prescribed
.:. State the quantity of drug to be supplied and duration of
treatment
.:. State the frequency of administration of the drug prescribed
.:. Have clear instruction for the patient
.:. Be signed in ink by the prescriber
.:. Have ~he address and telephone contact of the prescriber.
.:. Have <lddrcss of the health facility
Qmllitles of a good prescriber
A good prescriber:-
.:. Prescribes medications when necessary
.:. Chooses a treatment regimen that is appropriate to the
disease and the patient
.:. Continues therapy for an appropriate time and alters
doses of therapy when necessary
.:. Prescribes the right medicines according to the diagnosis
•:. Gives a clear explanation to the patient about his/her
condition
.:. Explains the effect of the drug and why Its needed
.:. Gives information about possible adverse effects of the drug
and what to do if they occur
.:. Monitors the patient's prognosis and advises the patient when
to return for review
The process of rational treatment
Good prescribing is achieved with time through development of
the necessary skills and a clear understanding of the importance of
prescribing appropriately and the processes involved as outlined
-29-
below:-
.:. Define the problem of the patient
.:. Specify the therapeutic objective
.:. Choose the treatment basing on efficacy, safety, compliance
and co-existing conditions of the patient.
•:. Write an accurate prescription
.:. Give the patient clear information about the condition and its
treatment
.:. Review the patient
.:. Decide whether to stop, continue or change treatment.
Not~:
Over prescribing is wasteful, can cause unnecessary adverse effects,
increase the chances for overdoses, can cause addiction and increases
the patient's expense on drugs.
Under prescribing is also wasteful and potentially harmful as it results in
ineffective treatment, resistance and more expensive for the patient as
more expensive drugs may be prescribed on the next visit after failing
to respond to the previous one.
The Dispensing process
The process of dispensing is undertaken by the dispenser.
A dispenser is anyone who gives out the medicine / treatment to the
patient or client. He may be a pharmacist, pharmacy technician, nurse
or a midwife.
Roles of a dispenser:-
.:. Dispenses drugs to patients and wards
.:. Gives drug information to the patient or client
.:. Keeps drug records
.:. Ensures proper storage of drugs
.:. Advises the prescriber about drugs
.:. Sometimes procures drugs
The process of dispensing
The procedure of dispensing a prescription involves:-
.:. Receiving a prescription
.:. Interpreting a prescription
-30-

.,
PRECISE PHARMIDl!l!OGVI
Retrieving medication
Making a proper explanation to the patient and ensure
that he/she has understood and will comply to the
medication
Ensuring that drugs are packaged well.
Ensuring proper record keeping
Supplying of medicine or drugs
The dispensing process requires a person to have sufficient knowledge
about the following:-
•:. Formulation of drugs
•:. Dosage
.:. Indications
•:. Pre.::autions
•:. Contraindications
.:. Adverse effects
.:. Packaging and labeling procedures
.:. Storage of the medicine
•:. Legal requirements regarding supply, storage, records and
labeling of controlled drugs
•:. Medicine administration
•:. Disease process
31-
PRE]ISE PHARMACOLOGY I
CHAPTER FOUR
ANTIBACTERIAL DRUGS
4.1.1 INTRODUCTION TO ANTIBIOTICS
Antibiotics are substances produced by or derived from micro-
organisms which inhibit the growth of or kill other microorganisms.
They are divided into two:-
.:. Bacteriostatic antibiotics.
.:. Bactericidal antibiotics.
Bacteriostatic antibiotics
These are antibiotics that inhibit the growth of susceptible bacteria.
They do not kill them immediaely but eventually lead to bacterial deat~.
These antibiotics rely on the immune system to eliminate the bactena
Examples;
.:. Tetracyclines.
.:. Chloramphenicol.
.:. Erythromycin.
.:. Azithromycin.
Bacteriostatic antibiotics may become bactericidal depending on the
concentration or type of bacteria.
Limitations of bacteriostatic antibiotics
.:. They are less effective for immuno-compromised patients.
•:. They are less effective when organisms are not growing or
dormant.
Bactericidal antibiotics
These are antibiotics that kill bacteria at safe plasma concentrations.
They do not rely on the immune system of the patient.
Examples;
.:. Penicillins (Amoxicillin, ampicillin, Cloxacillin).
•:. Cephalosporins (Cephalexin, Cefaclor, Ceftriaxone).
•:. Aminoglycosides (Gentamycin, Amikacin).
-32-

, PREC~ PRI$e~13 PHARMACOLOGY I
Key issues to note:
.:. Bactericidal antibiotics are highly recommended in immuno-
compromised patients
.:. Some bactericidal antibiotics are more effective when cells are
actively dividing therefore bacteriostatic drugs reduce their ..,
effectiveness when given together.
Chemical Structure
Antibiotics sharing the same structure generally have;
.:. Similar pattern of antibacterial activity (indications)
.:. Effectiveness
.:. Toxicity
.:. Same side effects and contraindications
Erythromycin
Azithromycin
C1arithrom cin
Co- Trimoxazole
Sui hadoxine
Tetracycline
Doxycycline
Minoc cline
Norfloxacin
Ciprofloxacin
Ofloxacin
Pefloxacin
Gentamycin
Amikacin
Metronidazole
Tinidazole
Secnidazole
Penicillins
Penicillin G
Amoxicillin
Flucloxacillin
Cephalosporins
Cephalexin
Ceftriaxone
Cefuroxime
Carbapenem
Mero enem
structure) . Examples
Chemical Structure Classification of Antibiotics
Class hemical
Quinolones
Beta Lactams
Sulphonamides
Macrolides
Tetracyclines
Aminoglycosides
Nitroimidazoles
Mechanism of action
Antibiotics may be classified as either bacteriostatic or bactericidal.
Spectrum of activity:
Antibiotics can be classified as either narrow spectrum or broad
"pO(:.tnllll.
Nl,rrow spectrum antibiotics
rhose antibiotics are effective against a limited range of bacteria.
Thoy are not recommended in mixed infections unless combined with
another antibiotic to widen the spectrum of activity.
Examples;
.:. Isoniazid
.:. Cloxacillin
.:. Clindamycin
.:. Flucloxacillin
Broad spectrum antibiotics
These antibiotics are effective against a wide range of bacteria (Gram
negative and Gram positive bacteria).
Examples;
.:. Tetracycline
.:. Chloramphenicol
.:. Ciprofloxacin
Classification of antibiotics
Antibiotics can be classified basing on:
.:. Spectrum of activity
.:. Mechanism of action
.:. Chemical Structure
Lincosamides Clindam cin
-33- -34-

.:.
.:.
.:.
Ih
.:.
.:.
.:.
.:.
.:.
PR~HARMACOlOGY
Principles of antibiotic Therapy
Before an antibiotic is prescribed, the following should be considered;
Evidence supporting an infection e.g. fever, leukocytosis
Establish severity of the infection
Determine the pathogens commonly associated with the'"
infected site
Attempt to identify pathogens by carrying out culture and
sensitivity, Gram stain
Select an antibiotic basing on clinical efficacy and side effect
profile.
The route of administration of an antibiotic i.e parenteral for
severe infections and oral for mild infections
Duration of therapy (depends on nature of infection and
response to treatment)
The dose of an antibiotic to be used i.e depends on age, weight
of the patient, severity of infection, hepatic and renal function
Empirical therapy
This is treatment of an infection before culture and sensitivity or
laboratory results are reported. Empirical therapy is based on
knowledge of local patterns of likely pathogens and local susceptibility
data. It can be achieved with the use of a broad spectrum antibiotic or
combination therapy.
Combination therapy
It involves use of two or more antibiotics to treat mixed bacterial
infections, where the required spectrum of cover cannot be provided
with a single drug. Combination therapy is used in the treatment of
pelvic inflammatory disease and tuberclosis
Advantages of combination therapy
.:. It prevents development of resistance "'
.:. It J'<'Cluces the side effects of the individual drugs
•:. II t'llhilllCes antimicrobial activity (synergism)
.:. M.lY btl lIsed in mixed infections in which the cause is
111I1<1I0Wll
··~35-
• • • • • •I:---==-=======:JP~RruECISE
PHARMACOLOGY I
Disadvantages of combination therapy
.:. Increased risk of toxicity
.:. Selection of multiple drug resistant microorganisms
.:. Eradication of normal host flora leading to super-infection
.:. Increased cost of the drugs to the patient
Prophylaxis
This is the use of drugs for prevention of disease or infection. It is of
two types i.e non-surgical and surgical prophylaxis.
4.1.2 -PENICILLINS
Penicillins are bactericidal antibiotics that Include natural and semi-
synthetic derivatives. They are the most widely used antibacterial drugs
because of their availability, low cost and safety profile.
Penicillins are mainly effective against infections caused by gram positive
cocci such as Streptococcus pneumoniae, Streptococcus pyogenes and
some gram negative bacteria such as N. meningitidis and N. gonorrhoeae
although resistance has emerged.
Mode of action
Penicillins act by inhibiting cell wall synthesis in susceptible organisms.
They are inactive against cell wall deficient organisms (bacteria which
do not have cell wall) such as Mycoplasma. Legionella species.
Classification of Penicillins
Natural penicillins
They are hig~ly effective against Gram positive cocci but are uneffective
against most strains ofStaphylococcus aureus. They are readily destroyed
by penicillinase (beta lactamase enzyme).
Examples:
.:. Benzyl penicillin (Penicillin G.)
.:. Phenoxymethyl penicillin (penicillin V).
Repository forms of penicillin
Benzathine benzyl Penicillin.
Procaine Penicillin.
.
-36-

, ' 'PRECISE PHARMACOIim
Penicillinase resistant penicillins
They have anarrow spectrum of activity and are resistant to degradation
by penicillinase enzyme. These drugs are useful for treating S. aureus
infections.
Examples:
.:. Cloxacillin.
.:. Flucloxacillin.
Broad-spectrum penicillins (Aminopenicillins)
These penicillins have a wide spectrum of activity against gram negative
and gram positive bacteria.
Aminopenicillins are susceptible to beta lactamase and cannot be used
in conditions caused by S. aureus except in combination with beta
lactamase inhibitors such as c1avulanic acid or salbactam
Examples:
.:. Ampicillin.
.:. Amoxicillin.
•:. Amoxicillin plus Clavulanic acid.
PENICILLIN V (Phenoxymethylpenicillin)
Available preparations: Tablets 2S0mg
powder for oral suspension 12Smg/Sml
Available brand: Pen-V®, unipen®, kam-pen®
Pharmacokinetics
Penicillin V is acid stable and is well absorbed, widely distributed to
kidneys, tonsils, liver and it apears in breast milk. It is excreted in urine
and breast milk.
Indications
•:. Pharyngitis
•:. Tonsillitis
.:. Gingival infections and periodontitis
.:. Tooth abscesses
.:. Otitis media
.:. Cellulitis
•:. Erysipelas
.:. Prophylaxis of rheumatic fever
-37-
, III' PREC~MACOlOGY
Contraindications
Known hypersensitivity to penicillins or cephalosporins
Severe acute infections
Dose
Adult:
SOOmg 6 hourly increased up to Ig 6 hourly in severe infections
Children:
12.Smg Ikg 6 hourly, OR
6-12years: 2S0mg 6 hourly
1-5years: 12Smg 6 hourly
Imonth - Iyear: 62.Smg 6 hourly
Rheumatic fever prophylaxis:
Adult 2S0mg twice daily
Children >2 years 12Smg twice daily
Side effects
.:. Urticaria
.:. Fever
.:. Joint pains
.:. Serum sickness like reactions
.:. Diarrhoea
.:. Skin rashes
.:. Anaphylaxis
.:. Nausea
Drug interactions
Probenecid may increase penicillin V blood concentration and risk of
toxicity.
Penicilin-V decreases immunological response to live typhoid vaccine.
Penicillin-V may reduce the excretion of methotrexate (increased
toxicity
Key issue to note
.:. Penicillin V should be given on empty stomach atleast I hour
before or 3 hours after meals to improve on absorption.
.:. Food or milk may decrease absorption of penicillin-V
-38-

.
'," PRECISDiARMACOLOGV PRE'CISE·PHARIVIA1';OLOGvl
AMPICILLIN
Ampicillin is a semi-synthetic penicillin with a broad spectrum of activity
against gram negative and gram positive bacteria. It is destroyed by
beta-Iactamase enzymes.
11
Pharmacokinetics
Ampicillin is poorly absorbed (40%) and its absorption is reduced by
the presence of food in the GIT. It is widely distributed in the body,
small amount is metabolized in the liver and also excreted unchanged
by the kidneys.
Indications
.:. Bronchitis .:. Pneumonia
.:. Septicaemia .:. Typhoid
.:. Urinary tract infections .:. Meningitis
.:. Endocarditis .:. Sinusitis
.:. Gonorrhoea .:. Otitis media
.:. Peritonitis .:. Acute cholecystitis
.:. Instruct the patient to complete the prescribed course of
treatment even though symptoms may abate before the full
course is over.
.:. Instruct the patient to report any sign of allergic response eg
Skin rush, itching or hives. .,
•:. For streptococcal infections, treatment is given for 10 days
to ensure eradication of S. pyogenes and reduce the risk of
rheumatic fever.
.:. Serum sickness -like reaction
.:. Rash
.:. Urticaria
.:. Pain at 1M injection site
Contraindications
Known hypersensitivity to penicillins
Infectious mononucleosis
Dose
Adult
Oral: 500mg 4 times daily, doubled in severe infections.
1M: 500mg-1 g 6hourly.
Intravenous infusion: over 30-60minutes 500mg 4 times daily
up-to 12g daily for severe infection.
Side effects
.:. Nausea and vomiting
.:. Antibiotic associated colitis
.:. Fever
.:. Diarrhoea
Children:
5-12years: 250mg 4 times daily doubled in severe infections.
1-5 years: I25mg 4 times daily doubled in severe infections.
I month - Iyears: 62.5mg 4 times daily doubled in severe
infections.
Neonates:
under 7 days 30mg/kg twice daily
14-21 days 30mg/kg 3 times daily
21-28 days 30mg/kg 4 times daily
Other conditions
Typhoid: 1-2g 6 hourly for 2 weeks.
Gonorrhoea: 2g with probenecid Ig as a single oral dose.
Acute cholecystitis: Adult 1-2g IV/ 1M, 6 hourly with gentamycin
5-7mg/kg IV daily in divided doses.
Meningitis: Injection IV, 2 -3 g 6hourly for 14days.
Infants and Children: 50-1 OOmg/kg (max 3g) every 4-6 hours.
Neonates: .
Under I week of age 50mg/kg every 12 hours)
Older neonates 50mg /kg every 8 hours.
Capsules 250mg
powder for oral suspension I25mg/ 5ml
Powder for Injection 500mg
Camicil®, Ampiren®, Kam ampi®,
Pembritin®, Dynacil®, medampi®,
Available brands:
Available preparation:
1
-39- -40-

30mg/kg twice daily (max 62.Smg 2 times daily)
30mg/kg 3 times daily (max 62.Smg 3 times daily)
PRECISE IQlti1;lMMrI!l1if1
Drug interactions
.:. Probenecid decreases renal excretion of ampicillin, thereby in-
reasing its blood concentration.
•:. Allopurinol increases the frequency of skin rashes in patients
receiving ampicillin. ?,
.:. Ampicillin decreases the effectiveness of oral contraceptives
.:. Ampicillin reduces excretion of methotrexate leading to
increased risk of toxicity.
.:. Ampicillin may increase the bleeding effect of anticoagulants.
.:. Decreased effectiveness with tetracyclines and
chloramphenicol.
Key issues to note:
.:. Use of ampicillin is limited by the development of bacterial
resistance.
•:. Food decreases rate and extent of absorption of ampicillin,
therefore, take the oral drug atleast 30minutes before food.
.:. Oral suspension is stable for 14 days under refrigeration.
•:. Avoid rapid IV administration of large doses as it may result in
seizures.
•:. Ampicillin is physically incompatible with aminoglycosides
therefore separate in terms of IV administration by I hour to
avoid inactivation of the aminoglycoside by the penicillin.
AMOXICILLIN
AlTloxiciliin is a hydroxylated derivative of ampicillin with similar
spectrum of activity but well absorbed compared to ampicillin. It is
preferred to oral ampicillin because of lower incidence of diarrhoea.
Available preparation: Capsules 2S0mg, SOOmg.
Powder for oral suspension2S0mg/Srnl,
12Smg/ Sml ,
Powder for Injection SOOmg/vial.
Available brands: Amoxydar®, Amoxil®, Amoxapen®, Duramox®
Penamox®, Amoxiren®, Promox®, Miloxy®
Pulmoxyl®
-41-
PRECI
Pharmacokinetics
Amoxicillin is well absorbed when taken orally, distributed into lungs,
prostate, ear, tonsils and sputum, partially metabolized in the liver and
excreted in urine.
Indications
.:. Pneumonia
.:. Exacerbation of chronic bronchitis
.:. Urinary tract infections
.:. Otitis media
.:. Dental abscess
.:. Sinusitis
.:. Lyme disease
.:. H.pylori eradication
.:. Billiary tract infections
.:. Acute cholecystitis
.:. Prophylaxis of bacterial endocarditis
Contraindications
.:. known hypersensitivity to penicillins
.:. Infectious mononucleosis
.:. Penicillin associated jaundice
Dose
Adult: 2S0-S00mg 8 hourly.
Ig 8 hourly may be used in severe cases like Pneumonia
Children
5-12years: 2S0mg 3 times daily doubled in severe infections.
1-5years: 12Smg 3times daily doubled in severe infections.
I month-I year: 62.Smg 3 times daily doubled in severe infections.
Neonates:
under 7 days
7-28 days
-42-

n ' , " " " " , ,PREC~PHARMAC[iJ{l • PREC PHARMACOLOGY
Eradication of H-Pylori: Ig twice daily in combination with
c1arithromycin or metronidazole and a proton pump inhibitor.
J
Pneumonia
Adult: 500mg to Ig every 8 hours.
Dental Abscess
Adult: 3 g repeated once after 8 hours. ..:
CLOXACILLIN
Cloxacillin is a semisynthetic derivative of penicillin that is resistant
to destruction by the penicillinase enzyme. It is therefore effective
aganist Beta lactamase-producing Staphylocccus aureus.
Available preparation: Capsules250mg
Powder for oral suspension I25mg/ 5 ml
Powder for Injection 500mg vial
Otitis media
Imonth-18years 40mg/kg daily in3 divided doses
Available brands: Kam c1oxa®, Mediclox®, C1oxispa®, Cloxil®
Cloxaren®, Alclox®, Asclox®, Ceclox®,
C1oxcip®
KC'y Issues to note
-t. Inform the patient that amoxicillin may be taken without regard
to meals.
.:. Instruct the patient to complete the prescribed course of
treatment even if he or she feels better before the full course
is over.
Drug interactions
•:. Allopurinol may increase the incidence of skin rash.
.:. AmoxicillJn may decrease effectiveness of oral contraceptives.
•:. Probenecid may increase amoxicillin blood concentration and
risk of toxicity.
.:. Amoxicillin reduces excretion of methotrexate thus increasing
risk of toxicity.
Children:
2-IOyears: 1/
2 adult dose
Less than 2years: 1f4 adult dose
Pharmacokinetics
Cloxacilin is poorly absorbed (50%) and food reduces its absorption.
It's partially metabolized in the liver and also excreted unchanged in
urine.
Impetigo
Cellulitis
Pneumonia
Osteomyelitis
Indications
.:. Septicaemia .:.
.:. Staphylococcal endocarditis .:.
.:. Pyomyostis .:.
.:. Septic arthritis .:•
.:. prophylaxis in bone and joint surgery
Contraindications
known hypersensitivity to penicillins
Dose.
Adult:
Oral 500mg 6hourly
1M: 250mg 6hourly
IV: 500mg 6houriy by slow injection or infusion

Side effects
.:. Nausea and vomiting
•:. Diarrhoea
.:. Skin rash
•:. Hepatitis
.:. Serum sickness-like syndrome
.:. Haemolytic anaemia
.:. Urticaria
-43- -44-
I

Diarrhoea
Skin rashes
Nausea and vomiting
Urticaria -,
Hepatitis
Side effects
.:. Serum-like sickness reaction .:.
.:. Antibiotic associated colitis .:.
.:. Joint pains .:.
.:. Haemolytic anaemia .:.
•:. Candidiasis .:.
•:. Pain and inflammation at injection site
Drug interactions
.:. Concomitant use with aminoglycosides produces synergistic
bactericidal effect
.:. Probenecid decreases renal excretion of cloxacillin.
•:. Cloxacillin increases risk of bleeding when given concurrently
with Warfarin.
•:. Cloxacillin decreases the immunologic response to live typhoid
VllIccine. Therefore, allow 24 hours or more to elapse between
the last dose of cloxacillin and the administration of oral typhoid
vaccine.
.:. The effectiveness of oral contraceptives may be reduced by
cloxacillin.
Key issues to note
•:. Oral cloxacillin should be taken on an empty stomach, I hour
before meals, because the presence of food decreases its
absorption.
.:. Oral cloxacillin is not optimal for the treatment of severe
infections, therefore use the injectable form.
•:. Instruct the patient to complete the prescribed course of
treatment to avoid relapse of the infection.
FLUCLOXACILLIN
Flucloxacillin has the same spectrum of activity as .cloxacillin but it is
well absorbed compared to Cloxacillin.
Available preparations: Capsules 2S0mg
Powder for oral suspension 12Smg/Sml
, ,',,"",,,",":! ,I /':,:" ':' " , ' "'''''', PRECISE PHARMACOLOl!i'l
Pharmacokinetics
Flucloxacillin is well absorbed when taken orally, partially metabolized
and excreted in urine.
Indications
.:. Endocarditis .:. Cellulitis
.:. Osteomyelitis .:. Pneumonia
.:. Impetigo .:. Infected scabies
.:. Otitis externa .:. Septicaemia
.:. Septic arthritis .:. Mastitis
.:. Folliculitis and boils .:. Surgical prophylaxis
.:. Infected bums .:. Abscesses
Contraindications
.:. Known hypersensitivity to penicillins.
•:. History of f1ucloxacillin associated jaundince
.:. Ocular administration
Dose
Oral
Adult: 2S0-S00mg every 6 hours. maxAg daily
'IV 1-2g every after 6 hours. Max 12g daily.
Children:
Oral
I O-18years: 2S0-S00mg 4 times daily.
2-IOyears: 12S-2S0mg 4 times daily.
I month -2 years: 62.S-12Smg 4 times daily.
IV SOmg / kg every after 6 hours.
Side effects:
.:. Nausea and vomiting .:. Joint pains
.:. Urticaria .:. Fever
.:. Skin rash .:. Chills
.:. Diarrhoea .:. Headache
Available brands: Ramaxir®, Floxapen®
~45~ ~46~

IDRECISE PHARMAC:!lED
Ampiclox®, Pen-A-c1ox®, Azuclox®,
Reiclox®, Spamclox®, C1oxap®, Elyclox®,
Indications
.:. Pneumonia .:. Bronchitis
.:. Tonsillitis .:. Septic abortion
.:. Post operative wound .:. Boils
infections .:. Abscesses
.:. Endocarditis .:. Osteomyelitis
.:. Meningitis .:. Sinusitis
.:. Otitis media .:. Surgical prophylaxis
.:. Urinary tract infections .:. Septicaemia
Available brands:
AMPICILLIN + CLOXACILLIN H'
Available preparations: Capsule sOOmg.
Powder for oral Suspension 2s0mg/sml
Powder for Injection sOOmg
Contraindications
Known allergy to penicillins.
Dose:
Adult: 500-1 OOOmg 6 hourly.
Children:
2-IOyears: 2s0-s00mg 6 hourly.
I month -2 years: 12s-2s0mg 6 hourly.
Drug interactions
.:. Probenecid decreases renal excretion of flucloxacillin
Side effects
.:. Gastrointestinal upset
.:. Urticaria
.:. Skin rash
.:. Phlebitis with IV injection
.:. Diarrhoea
.:. Indigestion
.,
Indications
.:. Pneumonia .:. Chronic bronchitis
.:. Sinusitis .:. Otitis media
.:. Pharyngitis .:. Tonsillitis
.:. Wound infections .:. Osteomyelitis
.:. Gonorrhoea .:. Urinary tract infection
.:. Boils .:. Cellulitis
.:. Abscesses .:. Septicaemia
Drug interactions
.:. probenecid delays the renal excretion of flucloxacillin.
.:. Flucloxacillin may affect the gut flora leading to lower oestrogen
re-arbsoption and reduced efficacy of combined oral
contraceptives.
Key issues to note
.:. Flucloxacillin, if prescribed together with aminoglycosides,
. should not be mixed in the same syringe or giving set.
Precipitation may occur.
•:. Instruct the patient to complete the prescribed course of
flucloxacillin to avoid relapse.
.:. Flucloxacillin is best absorbed if taken on an empty stomach,
atleast 30minutes before food or 2 hours after.
l.i .,
FLUCLOXACILLIN + AMOXICILLIN
Available preparations: Capsules sOOmg
Powder for oral suspension 2s0mg/sml
Powder for Injection Ig
Available brands: Flucamox®, Flamox®
Contraindications
•:. Known hypersensitivity to penicillins
Dose
Adult:
500 -I OOOmg every 6-8 hours.
Children:
2-12years: 2s0-s00mg every 6-8 hours.
I lIlonth-2 years: 12s-2s0mg every 6-8 hours.
-47- -48-

I I, ' I': " PRECISE PHARMACOLOGY
Side effects
.:. Gastrointestinal disturbances .:.
.:. Haemolytic anaemia .:.
.:. Joint pains .:.
.:. Serum sickness
Urticaria
Skin rash
Fever
Dose
Adult Oral: 625mg twice daily or 375mg 3 times a day for 7 days
:ilid:',,
1:'!!liiP:': Severe infection: Ig twice daily/ for 7-10 days.
!l11111!!!:!;:; Dental infection: 375mg 3 times a day for 5 days
II I! Injection: IV 1.2g 6-8 hourly over 2 minutes or infusion over
'" . ,: 30minutes
Children:
Over 6years: 312mg 3 times daily
1-6years: 156mg 3 times daily.
Under I year: 25-50mg/kg /day of amoxicillin in divided doses
every 8 hours.
Key issues to note
.:. Instruct the patient to take ampicillin/ cloxacillin on empty
stomach, because presence of food decreases its absorption.
•:. Instruct the patient to complete the prescribed course.
AMOXICILLIN + CLAVULANIC ACID
The above combination acts synergistically because c1avulanic acid
binds to beta- lactamases thereby protecting amoxicillin from being
destroyed by beta-Iactamase producing strains of bacteria.
Available preparations: Tablet 375mg, 625 mg, and IOOOmg.
Powder for oral suspension I 56mg/5ml,
228mg/ 5ml.
Powder for Injection 600mg
Side effects
.:. Diarrhoea .:.
.:. Vomiting .:.
.:. Urticaria .:.
.:. Gastritis .:.
.:. Vaginitis .:.
Nausea
Skin rashes
Indigestion
Abdominal discomfort
Anorexia
Available brands: Augmentin®, Clavulin®, Fleming®, Clavam®,
_Enhancin®, C1avomid®, Co-Amox®, Myclav®,
Indications
ill
.:. Pneumonia .:. Otitis media
.:. Sinusitis .:. Tonsillitis
.:. Urinary tract infections .:. Urethritis
.:. Wound infections .:. Boils
.:. Cellulitis .:. Osteomyelitis
.:. Dental infections .:. Intra abdominal sepsis
•:. Animal bite .:. Septic abortion
.:. Acute exacerbation of chronic bronchitis
Contraindications
•:. Known hypersensitivity to penicillins
.:. History of penicillin or amoxicillin with c1avulanic acid- associated
jaundince or hepatic dysfunction.
-49-
Drug interactions
.:. Probenecid decreases the renal excretion of amoxicillin
resulting into increased and prolonged blood levels
.:., Effectiveness of oral contraceptives is reduced byamoxicillin/
c1avulanate
.:. Allopurinol may increase the incidence of skin rash
Key issues to note
.:. Advise the patient to take the drug with meals to minimise
gastrointestinal disturbances.
.:. The patient should maintain adequate hydration especially
when using high doses of the drug to prevent risk of
crystalluria.
.:. Clavulanic acid degrades rapidly therefore parenteral solution
should be used immediately after mixing and the tablet
should be stored in air tight containers.
-50-

,
PHARMACOJiIiVI
! :',,': PftECIS
....
Drug interactions
.:. Probenecid decreases renal excretion of benzyl penicillin
.:. Benzyl penicillin may interact with bacteriostatic drugs such as
chloramphenicol and tetracycline
.:. Oral contraceptive effectiveness may be reduced by
Benzylpenicillin
Key issues to note
.:. Inform the patient that intramascular benzyl penicillin injection
is painful.
.:. IV benzyl penicillin is physically incompatible with
aminoglycosides therefore give them separately.
.:. Avoid rapid IV administration of large dozes of benzyl
penicillin, it may result in convulsions.
.:. The intravenous route is prefered for ne.onates and infants.
.:. Dosage should be reduced in moderate to severe renal
impairement.
BENZYL PENICILLIN
Available preparations: Powder for Injection 600mg
(I,OOO,OOOunits).
Indications
.:. Community aquired pneumonia .:. Septicaemia
.:. Meningitis .:. Anthrax
.:. Syphilis .:. Gas gangrene
.:. Lyme disease
.:. Pharyngitis /tonsillitis
.:. Necrotizing fasciitis
.:. Aspiration pneumonia
.:. Infective endocarditis
Contraindications
•:. Intrathecal route.
.:. Serum sickness like reactions
.:. Coagulation disorders
.:. Diarrhoea
.:. Nausea
Dose
Adult: 600mg 6 hourly.
Severe infection: I .2g every 4 hours IV usually with an
aminogiycoside.
Neurosyphilis in adults: by slow IV injection 1.8 -2.4g every 4
hours for 2 weeks.
Children:
I month -12 years: IOOmg /kg daily in 4 divided doses.
Infants: 1-4weeks: 75mg/kg daily in 3 divided doses.
Neonates: SOmg/kg daily in 2 divided doses.
Side effects
.:. Joint pains .:. Skin rashes
.:. Haemolytic anaemia ••• Convulsions
..
.:. Pain and inflammation at .:. Coma
injection site .:. Angioedema
BENZATHINE PENICILLIN
Benzathine penicillin is a repository preparation that slowly releases
benzylpenicillin after intramuscular injection, by hydrolysis. of the
benzathine - penicillin complex. Low serum levels may be detected
for up to 30 days. Distribution and elimination are similar to
benzylpenicillin.
Available preparations: Powder for Injection 2.4MU (million units)
Indications•
•:. Syphilis
.:. Streptococcal pharyngitis
.:. Acute cervical adenitis
.:. Diphtheria
.:. Primary prevention of rheumatic fever
-51- -52-

" , , ' DREC ~ EPHARMACOLQG't'1
,
.:. Cellulitis
.:. Childhood pneumonia
.:. Bites
.:. Mouth infections
Side effects
.:. Joint pains .:. Skin rashes
.:. Serum sickness like reaction .:. Haemolytic anaemia
.:. Angioedema .:. Thrombocytopenia
.:. Diarrhoea .:. Nausea
.:. Pain at injection site
Contraindications
.:. Known hypersensitivity to penicillins
.:. Neuro syphilis
.:. Intravascular injection
Dose
Adults: 1M 600,000 units-I.2MU daily
Syphillis: 1M°1 million units daily for 10-14 days.
Infants and Children:
Pneumonia: Deep 1M SOmg/kg (max. 1.2g) daily for 10 days
Congenital syphillis:
Children upto 2years: SOmg/kg daily for 10 days
Drug interactions
Probenecid decreases renal excretion of procaine benzyl penicillin
Available preparations: powder for injection-4MU .
Indications
.:. Congenital Syphilis
.:. Cutaneous anthrax
.:. Erysipelas
.:. Diphtheria
.:. Fever
.:. Skin rashes
.:. Neutropenia
.:. Thrombocytopenia
injection site
Side effects
.:. Joint pain
•:. Urticaria
.:. Serum sickness like reaction
.:. H<lernolytic anaemia
.:. Pain and inflammation at
Contraindications
•:. Neurosyphilis.
•:. Intravascular injection.
Drug interactions
.:. Probenecid decreases renal excretion of benzathine penicillin
.:. Oral contraceptive effectiveness may be reduced by
benzathine penicillin.
•:. Benzathine penicillin may reduce excretion of methotrexate
leading to increased toxicity.
Key Issues to note
.:. Give doses> 900mg( I .2MU) as two injections at separate
sites.
.:. Give Benzathine Penicillin with caution in renal failure.
.:. Do not give by intravenous injection.
Dose
Early syphilis: 2.4MU by deep 1M injection as a single dose divided
between two sites.
Late syphilis: 2.4MU deep 1M divided between two sites once weekly
for 3 consecutive weeks.
Pharyngitis and rheumatic fever: 1M 1.2MU as a single dose.
Children under 30kg: 600,000 units deep 1M as a single dose.
PROCAINE PENICILLIN
Procaine penicillin is a relatively insoluble suspension of complexed
procaine and benzyl penicillin which releases benzyl penicillin slowly
after intramuscular injection. Peak serum levels are achieved within
1-4 hours in adults and decline steadily over 24 hours.
Key issues to note
.:. Never administer procaine penicillin intravenously
.:. Give Procaine penicillin with caution in infectious
mononucleosis because of high incidence of rash.
-53- -54-
/
/
I

",,' I'" :::,,' :'" I I I " , I ," REC PHARMACOLOGY
4.1.3 CEPHALOSPORINS
;'I' Cephalosporins are semi synthetic beta lactam antibiotics closely related
both structurally and functionally to penicillins. They have an advantage
over the penicillins in that they are less susceptible to inactivation by
beta lactamase enzyme and have a broader spectrum of activity. Hence
are often used when penicillin treatment has proved ineffective
Mode of action
Cephalosporins are bactericidal in action and inhibit the synthesis of the
bacterial cell wall.
Classification of cephalosporins.
Cephalosporins are classified into generations basing on bacterial
susceptibility patterns and resistance to beta lactamases, as follows:-
•:. First generation Cephalosporins
.:. Second generation cephalosporins
.:. Third generation cephalosporins
.:. Fourth generation cephalosporins
First generation Cephalosporins.
This group includes:-
.:. Cephalexin
.:. CefadroxiI
.:. Cephradine
.:. Cefazolin
First generation cephalosporins are mainly active against gram positive
bacteria and have limited activity against gram negative bacteria like H.
influenzae.
Spectrum of activity of first generation
••• Streptococcus pyogenes
•
•:. Streptococcus pneumoniae
.:. Staphylococcus aureus
.:. Staphylococcus epidermidis
.:. Klebsiella pneumoniae
•:. Proteus mirabilis
.:. Escherichia coli w
.:. Anaerobic cocci (e.g. peptococcus, peptostreptococcus)
-55-
" " PRECISE PHARMAC I
Second generation cephalosporins
This group includes:-
.:. Cefuroxime
.:. Cefaclor
Second generation cephalosporins have similar coverage against
gram positive organisms as the first generation but with enhanced
gram negative coverage. However, they are less active against gram
+ve bacteria than the first generation and have no activity against
enterococci or P. aeruginosa.
Cefuroxime, has good activity against S. aureus and beta-Iactamase
producing H. influenzae. It is the only second generation drug with
good penetration of the central nervous system.
Spectrum of activity of Second generation
.:. Streptococcus pneumoniae
.:. Escherichia coli
.:. Anaerobic streptococci
.:. Streptococcus pyogenes
.:. Neisseria gonorrhoeae
.:. Proteus mirabilis
.:. Haemophilus influenzae
Third generation cephalosporins
This class includes:-
.:. Ceftriaxone .:. Cefotaxime
.:. Ceftazidime .:. Cefixime'
.:. Cefpodoxime .:. Cefdinir
Third generation cephalosporins are less active than the first and
second generation drugs agaim'tgram +ve bacteria, but are more
active against gram -YJvbacteria. including those resistant to the first
and second generatiOn. They are less active against S. aureus than the
first generation drugs.
Spectrum of activity
.:. Escherichia coli
-56-

, II) , I ,
I:' 'I " I , " " PRECI~i1PHARMACOLOGY
Side effects
.:. Nausea .:. Diarrhoea
.:. Vomiting .:. Abdominal pain
.:. Dyspepsia .:. Loss of appetite
.:. Headache .:. Urticaria
.:. Rash .:. Angioedema
.:. Pruritus .:. Vaginal candidiasis
.:. Fatigue
Dose
Adult: 250 mg every 6 hours or 500mg every 8-12 hours increased up
to Ig every after 6-8 hours for severe infection. Max 4g per day
Celluitis and erysipelas: 500mg 6 hourly for 7-10 days following intial
therapy with cefazolin.
Osteomyelitis: 1-2g every 6 hours to complete the course of 4- 6
weeks following intial therapy with cefazolin.
Children: 25mg/kg daily in divided doses, doubled in severe infection
OR
12 years: 250mg every 8 hours
I - 5 years: 125mg every 8 hours
Under I year: 125mg every 12 hours
Otitis media: 75 - IOOmg / kg / day in 4 divided doses
Prophylaxis of recurrent UTI
Adult: 125mg at night.
Contraindications
.:. known allergy to cephalosporins
Drug interactions
.:. Probenecid decreases renal excretion of cephalexin, increasing
its blood levels.
.:. Oral contraceptives effectiveness may be reduced by
cephalexin
.:. Aminoglycosides and loop diuretics may increase the
nephrotoxicity caused by cephalexin.
Pneumonia
Erysipelas
Pyomyositis
.:. Septic arthritis
.:. Pharyngitis
.:. Tonsillitis
.:. Proteus mirabi/is .:. Haemophilus influenzae
.:. Pseudomonas aeruginosa .:. Neisseria gonorrhoeae
.:. Enterobacter aerogenes .:. Providencia
.:. Serratia .:. B. fragi/is
Indications
.:. Otitis media
.:. Impetigo
.:. Cellulitis
.:. Osteomyelitis
.:. Dental infections
•:. Bronchitis
.:. Prevention of bacterial endocarditis
Available brands: Cephadar®, Keflex®, Sporidex®, Cefamor®,
Felexin®, Oriphex®, Cephoxin®, Cefex®
CEPHALEXIN
Available preparations: Capsules 2S0mg, SOOmg
Powder for oral suspension 12Smg/ 5ml,
250mg/5ml.
Pharmacokinetics
Cephalexin is absorbed rapidly from the GIT after oral administration,
distributed widely into most body tissues including the gall bladder,
sputum, bone, synovial fluid. It is not metabolized and is excreted in
unchanged in urine.
Fourth generation cephalosporins I •
These drugs include:-
•:. Cefepime.
Fourth generation drugs, like the third generation, have an extended
spectrum of activity against gram -ve bacteria compared to the 15t
and 2nd
generation. Cefepime is active against gram positive and gram
negative infections including Pseudomonas aeruginosa.
----~
-57- -58-

'II' "II 'I ' , , ' I ' CS
iI! I " II II ' :11 'I pi I' ':: PRE I EPHAR ACOLOGY ISE PHARMACOLOIWJ
Key Issues to note
.:. Administer cephalexin on an empty stomach, atleast one hour
prior to meals or 2 hours after meals.
.:. Shake the suspession well before use.
.:. Instruct the patient to complete the prescribed course to avoid
relapse of infection.
Side effects
.:. Nausea
.:. Vomiting
.:. Headache
.:. Diarrhoea
.:. Abdominal pain
.:. Oral candidiasis
.:. Vaginal candidiasis
.:. Skin rash
.:. Pruritus
.:. Urticaria
CEFADROXIL
Available preparations: Tablets 2S0mg,sOOmg
Powder for oral suspension 12smg / sml,
2s0mg/Sml
Available brands:
Pharmacokinetics
Cefadroxil is absorbed rapidly and completely from the GI tract after
oral administration and is distributed widely into most body tissues. It
is not metabolized and is excreted unchanged in urine.
Indications
.:. Pneumonia .:. Pharyngitis
.:. Mastitis .:. Chronic bronchitis
.:. Tonsillitis .:. Osteomyelitis
.:. Urinary tract infections .:. Otitis media
.:. Septic arthritis .:. Sinusitis
.:. Cellulitis .:. Skin and soft tissue infection
Contraindications
.:. known hypersensitivity to cephalosporins
Dose
Adult: 500 - 1000 mg twice daily
Children:
Over 6 years: 12.Smg/kg once or twice daily or sOOmg twice daily
I - 6 years: 2s0mg twice daily "
Under I year: 12Smg twice daily
-59-
Drug interactions
.:. Probenecid decreases renal excretion of cefadroxil
.:. Loop diuretics may increase nephrotoxicity of cefadroxil
.:. Concomitant use with bacteriostatic agents like tetracyclines,
erythromycin may interfere with bactericidal activity.
Key Issues to note:
.:. Cefadroxil may be administered with or without meals.
.:. Shake the suspession well before use.
.:. Administration with food may decrease nause~ or vomitting.
CEPHRADINE
Available preparations: Capsules sOOmg, 2S0mg
Powder for oral suspen~jon 12smg/Sml.
1/
Available brands: Velosef®, Valodin®', Bactocef ®
Pharmacokinetics
Cephradine is well absorbed from the GIT and is distributed widely
into body tissues like bone, kidneys, sputum, gall bladder, synovial
fluids. CSF penetration is poor but the drug crosses the placenta. It is
not metabolized and is excreted unchanged in urine.
Indications
.:. Pneumonia
.:. Osteomyelitis
.:. Prostatitis
.:. Otitis media
-60-

.:. Prophylaxis in surgery
.:. Tonsillitis
.:. Pharyngitis
.:. Skin and Soft tissue infections
Cont'raindications
.:. known hypersensitivity to cephalosporins
,..
, , ~PHARMACOLOGY
.:. Oral suspension is stable for 7 days at room temperature or
14 days at 2-8°C after reconstitution
CEFUROXIME
Available preparations: Tablets 250mg, 500mg.
Powder for oral suspension 125mg / 5ml
Powder for Injection 750mg, 1.5g
If
Pharmacoldnetics
Cefuroxime axetil is absorbed from the GIT and its absorption is
enhanced by food. It penetrates well into most fluid spaces and tissues.
It is not metabolized and is excreted primarily in urine.
Zinnat®, Axetine®, Kefstar®
Zamur®, Zinacef®,
Proximexa®, Pulmocef®,
Dose
Adult: 250-500mg every 6 hours or 500mg every 12hours, up to Ig
every 6hours for severe infection.
Children:
Imonth-12 years: 25-50mg /kg daily in 2-4 divided doses.
Otitis media: 75- IOOmg/kg daily in equally divided doses
every 6 hours.
Side effects
.:. Abdominal Pain .:. Anorexia
.:. Diarrhoea .:. Glossitis
.:. Nausea and Vomitting .:. Vaginitis
.:. Pseudomembranous Colitis .:. Rash
.:. Urticaria
Available brands:
Indications
.:. Acute and chronic bronchitis
.:. Acute otitis media
.:. Sinusitis
.:. Tonsillitis and Pharyngitis
.:. Impetigo and pyoderma
.:. Pneumonia
.:. Gonorrhoea
.:. Bacterial Meningitis
.:. Surgical prophylaxis
.:. Pelvic inflammatory
disease
Drug interactions
.:. Concomitant use with nephrotoxic drugs like vancomycin,loop
diuretics, and aminoglycosides increases the risk of
nephrotoxicity
.:. Concomitant use with bacteriostaticdrugs like tetracyclines,
erythromycin may interfere with bactericidal activity of
cephradine
Key Issues to note
.:. Cephradine may be administered with or without meals.
Le. food may decrease the rate but not the extent of oral
absorption
.:. Shake the suspession well before use
-61-
Contraindications
.:. known allergy to cephalosporins
Dose
Adult: Oral
Pneumonia 500mg 12 hourly for 7-10 days.
Pharyngitis and tonsillitis 250mg 12 hourly for 10 days.
Otitis media 250mg 12 hourly for 10 days.
Otitis media (Children over 2 years) 250mg twice daily for 10
days.
Gonorrhoea Ig single dose.
Urinary tract infection 125mg twice daily doubled in
pyelonephritis.
1M/IV 750mg 8 hourly,.Severe infection IV 1.5g 6-8 hourly
-62-
/

, , ',1,' , 'I '" ",," , ' : , PRECISE PHARMACl I
", , , ' , , PRE
Contraindications
.:. Known hypersensitivity to cephalosporins
.:. Infants less than one month
Pharmacokinetics
Cefaclor is well absorbed from the GIT. Food delays but does not
prevent complete absorption. It is well distributed into most body
tissues and fluids but CSF penetration is poor. It is not metabolized and
Is excreted primarily in urine.
Dose
Adult: 2S0-S00mg every 8 hours, or 37S-7S0mg every 12 hours using
((,tntrolled release.
Children:
Over 5 years: 2S0mg every 8 hours.
I - 5 years: 12Smg every 8 hours.
I month - I year: 62.Smg every 8 hours.
ceclor®, vercef®
'11
jt
r
.:. Sinusitis
.:. Tonsillitis
.:. Bronchitis
.:. Gonococcal urethritis
.:. Pruritus
.:. Nausea
.:. Rashes
.:. Headache
.:. Urticaria
.:. Serum sickness syndrome
Available brands:
Indications
+:. Pneumonia
.:. Pharyngitis
.:. Otitis media
.:. Skin and soft tissue infections
Side effects
.:. Diarrhoea
.:. Vomiting
.:. Oral candidiasis
.:. Fever
.:. Pseudo membranous colitis
.:. Abdominal discomfort
Key issues to note
.:. Cefuroxime axetil is well absorbed after a light meal, therefore
it should be administered with food
•:. Shake suspension well before use ',',
•:. The tablet should not be broken before swallowing
•:. Reconstituted injectable solution is stable for, 24 hours at room
temperature and 48hours when refrigerated
.:. Reconstituted oral suspension may be stored at room
temperature or refrigerator and discarded after 10 days
Drug interactions
.:. Efficacy of oral contraceptives may be reduced
.:. Nephrotoxic drugs such as gentamycin, vancomycin may
increase the potential for nephrotoxicity
.:. Probenecid inhibits the tubular secretion of cefuroxime
resulting into prolonged high serum concentrations
.:. A disulfiram-like reaction may occur when alcohol is given
concurrently with cefuroxime
Side effects '1',
.:. Skin rash .:. Headache
.:. Nausea and vomiting .:. Anorexia
.:. Diarrhoea .:. Abdominal pain
.:. Pseudomembraneous colitis .:. Nephrotoxicity
CEFACLOR
Available preparations: Capsules /tablets 37Smg
Powder for oral suspension; 12Smg / Sml,
2S0mg/Sml
suspension bd I87mg/Sml
Children:
Oral 12Smg twice daily
1M/IV 30-1 OOmg/day in 3-4 divided doses.
-63- -64-

" I '11'11"" 'II' '" "'''I "' I " " " " , PAECIw:Jill]MAClllLOGY
I I' 11 1) I tifd I j I I 1 "
II T i J 1 1)1 Ii 11.1 ,III II" , I' ')" I zrsn 2&
.,
CEFIXIME
Available preparations: Tablets IOOmg, 200mg, 400mg
Powder for oral suspension IOOmg/Sml,
7Smg/Sml.
Pharmacokinetics
Cefixime is well absorbed from the GIT. Presence of food delays its
absorption but total amount absorbed is not affected. It is partially
metabolized and is excreted primarily in urine.
Drug interactions
.:. Probenecid decreases renal excretion of cefaclor
•:. Cefaclot may enhance the anticoagulant effect of warfarin
.:. Contraceptive effect of oestrogens may be reduced
Side effects
.:. Diarrhoea .:. Flatulence
.:. Nausea .:. Vomiting
.:. Abdominal pain .:. Loose stool
.:. Dyspepsia .:. Headache
.:. Rashes .:. Dizziness
.:. Urticaria .:. Pruritus
Dose
Adult and Children over 10 years: 200 - 400mg daily in I - 2 divided
doses.
Gonorrhoea: 400mg or 800mg as a single dose
Children:
6 • 10 years: 200mg daily in 1-2 •
I - 5 years: IOOmg daily
6months· Iyear: 7Smg daily
Drug interactions
.:. Cefixime may increase carbamazepine serum concentrations
.:. Probenecid increases serum concentration of cefixime
.:. Increased bleeding with anticoagulants
.:. Antacids
Key Issues to note
.:. Reconstituted suspension may be stored for 14 days
at room temperature or under refrigeration.
•:. Cefixime may be administered with or without food although
food delays the time to reach peak concetration.
.:. Shake suspension well before use.
(
CEFPODOXIME ,.",
Available preparations: Tablets 200mg
Powder for oral suspension IOOmg/Sml
•:. Typhoid
•:. Otitis media
.:. Gonorrhoea
Gramocef-O®, Cefim®, Topcef®, Ixime®,
Spaxime®, Cefix®, Maxpan®, Taxim-O®
Indications
.:. Acute bronchitis
.:. Pharyngitis and tonsillitis
.:. Pneumonia
.:. Acute exacerbations of chronic b~onchitis
.:. Uncomplicated urinary tract infections ~
Available brands:
Key Issues to note:
.:. Advise the patient to take entire course of medication even If
she/he feels better early in the course
.:. Store the capsules / tablets and any unreconstituted powder
for oral suspension at room temperature
.:. Food or milk delays and decreases plasma concentration of the
drug
.:. Swallow the tablets whole. Do not crush or chew them
Contraindications
.:. History of anaphylactic reaction to penicillins
Available brands: Orelox®, Tambac®, Cefodox®'
-65- -66-
,
,/

flSE PHARMA~QL.1~YJ
, . ' ." , PRE
.' ",:: I': .,I', 'II i ' ': " : PRECISE PHARMACOLOGY
Pharmacokinetics
Cefpodoxime proxetil is a pro-drug that is metabolized to the active
metabolite cefpodoxime. It is rapidly absorbed after oral administration,
widely distributed to most body tissues, undergoes minimal metabolism
and is excreted unchanged in urine. to,
Indications
.:. Acute bronchitis .:. Cellulitis
.:. Chronic bronchitis .:. Pneumonia
.:. Acute Sinusitis .:. Tonsillitis
.:. Pharyngitis .:. Infected wounds
.:. Urinary tract infections .:. Abscesses
.:. Otitis media .:. Gonorrhoea
Drug interactions
+:. Concomitant administration with high doses of antacids or H2
blockers reduces plasma concentration of cefpodoxime
+:. Renal excretion of cefpodoxime is inhibited by probenecid
Kc.~y Issues to note
.:. Food increases oral bioavaibility of cefpodoxime therefore give
the tablet with food
.:. After reconstitution, suspension may be stored in a refrigerator
for 14 days
CEFDINIR 1I.
AVllilable preparation: Capsules 300mg
Contraindications
I·h..rmacokinetics
C:tllfdlnir is absorbed from the gastrointestinal tract following oral
~d,ninistration, widely distributed into tissues and is 60 to 70% bound
10 plasma proteins. It is not appreciably metabolised and is excreted in
thCllurine.
Dose • -/
Adult: 300mg 12 hourly for 5-10 days Or 600mg once daily for 10
d~ys. ,
51cln and Soft tissue infection: 300mg 12 hourly for 10 days.
Children: 6months -12 years; 7mg/kg 12 hourly for 5- 10 days.
Indications
.:. Tonsillitis
.:. Acute otitis media
.:. Skin and Soft tissue infections
.:. Acute exacerbation of chronic bronchitis
.:. Pneumonia
.:. Pharyngitis
.:. Acute Sinusitis
Adci®
AVltilable brand:
Side effects
.:. Diarrhoea .:. Pruritus
.:. Vomiting .:. Nausea
.:. Headache .:. Abdominal pain
.:. Tinnitus .:. Skin rashes
.:. Malaise
Contraindications
.:. Known hyp~rsensitivityto cephalosporins
Dose
Adults:
Pharyngitis and tonsillitis: 100mg 12 hourly for 5-10 days
Gonorrhoea: 200mg Single dose.
Pneumonia and Bronchitis: 200mg 12 hourly for 10-14 days
Skin and soft tissue infections: 400mg 12 hourly for 7-14 days
Uncomplicated urinary tract infections 100mg 12 hourly for
7 days.
Children:
Over 9 years: IOOmg every 12 hours
3-8 years: 80mg every 12 hours
2months - 2 years: 40mg every 12 hours or 8mg/kg/day in 2 •
divided doses.
· i
, I
I
-67- -68-

a.JIIIIDII.IIIIII.II.I_._II.IIII_I.J.I
••
'7.IEJp~RE~CI~SEJiPmHARMACOLOGYI Ii PRECISE
CEFTRIAXONE
Available preparations: Powder for Injection 1M / IV
SOOmg, Ig, 2g
Pharmacokinetics
Ceftriaxone is widely distributed into body tissues and fluids after
parenteral administration. It penetrates well into the CSF, especially
when the meninges are inflamed and it's excreted unchanged in urine.
Septicaemia
Acute peritonitis
Surgical prophylaxis .:.
Syphilis .:.
Typhoid fever
Osteomyelitis and septic arthritis
Pelvic inflammatory disease
Skin and soft tissue infections
Side effects
.:. Skin reaction .:. Phlebitis at injection site
.:. Superinfection
,
.:. Fever
.:. Loose stool .:. Diarrhoea
.:. Nausea and vomiting .:. Headache
.:. Dizziness .:. Pancreatitis
Drug intractions
.:. Ceftriaxone may reduce the effectiveness of oral
contraceptives
.:. Concomitant use with aminoglycosides produces synergistic
antimicrobial activity against Pseudomonas aeruginosa
and some strains of Enterobacteriaceae
Contraindications
.:. Neonates with jaundice
.:. Acidosis
Dose
A~u~t: I.-2g once daily or in two divided doses given as deep 1M or slow
IV injection over 2-4 min. or as infusion over at least 30 min. increased
to 4g daily in severe infections
Uncomplicated gonorrhoea: 2S0mg 1M as a single dose.
~urgi~al prophylaxis: 1M or IV inj~ction over at least 2-4minutes Igat
induction, colorectal surgery 2g at induction.
Children:
~ess ~han SOkg: 2S-S0mg/kg once daily increased to 80mg/kg iii severe
infections.
Neonates: SOmg/kg/day.
?,
Constipation
Insomnia
Dizziness
Flatulence
Anorexia
.:. Otitis media
.:. Chancroid
.:. Urinary tract infection
Medaxonum®, Rocephin®, Mesoporin®,
Powercef®, Axone®, Oframax®
Indications
.:. Pneumonia
.:. Gonorrhoea
.:. Meningitis
Available brands:
Key Issues to note
•:. Cefdinir may be administered with or without food,
administer with food If stomach upset occurs
•:. Administer cefdinir atleast 2 hours before or after
antiacids or Iron supplements
Drug interactions
.:. Preparations containing iron may interfere with absorption of
cefdnir
.:. Concomitant administration of antacids containing aluminium
.(' or magnesium interfere with absorption of oral cefdnir
~ .:. Probenecid reduces renal elimination of cefdnir
Side effects
.:. Dtarrhoea
.:. Pruritus
.:. Nausea
.:. Abdominal pain
.:. Headache
,I',
-69- -70-

-IFCIV' s I ' _ . P,REIB~i~PHARM}CO !IID
CEFOTAXIME
Available preparations: Powder for injection SOOmg, Ig
Key Issues to note:
.:. Reconstituted solution is stable for 24 hours at room
temperature or 3 days when refrigerated
.:. Ceftriaxone is incompatitable with calcium, therefore do not
give with calcium containing solution .,
.:. Intramascular doses over Ig should be divided between
more than one site
.:. Skin rash
.:. Vomiting
.:. Nausea
.:. Candidiasis
.:. Malaise
Powder for Injection Ig, SOOmg
Fortum®
CEFTAZIDIME
Available preparations:
Available brands:
Key Issue to note
.:. Use cefotaxime instead of ceftriaxone for gram-negative
septicaemia in neonates
.:. Rapid IV administration of large doses may result in seizures
Side effects
.:. Pseudomembranous colitis
.:. Headache
.:. Diarrhoea
.:. Pain and inflamation at injection site
.:. Pain at injection site
Drug interactions
.:. Probenecid decreases renal excretion of cefotaxime
and prolong its half life
.:. Concomitant use with aminoglycosides results in
synergistic activity
.:. Chloramphenicol inhibits anti bacterial activity of
cefotaxime
Neonates:
0-1 week old SOmg/kg I2 hourly
1-4weeks old SOmg/kg 8 hourly
Children: 100 - ISOmg/kg daily in 2 - 4 divided doses increased up to
200mg/kg daily in severe infections
Pneumonia
Bacterial meningitis
Cellulitis
Acute peritonitis
Brain abscess
Surgical prophylaxis
Valoran® ,C1aforan®, Cefotim®, Oritaxim®
Available brands:
Pharmacokinetics
... Cefotax~e is not absorbed from the GIT and must be given by injection.
It is distributed widely into most body tissues such as liver, kidney,
bone, sputum and also has adequate CSF penetration when meninges
are inflamed. It is metabolized partially to an active metabolite and
excreted in urine and to some extent in breast milk.
Indications
.:. Typhoid fever .:.
.:. Acute and chronic bronchitis .:.
.:. Septicaemia .:.
.:. Osteomyelitis .:.
.:. Pelvic inflammatory disease .:.
.:. Gonorrhoea .:.
.:. Neonatal gonococcal conjunctivitis
.:. Septic arthritis
Contraindications
.:. Known hypersensitivity to:cephalosporins
.:. History of anaphylactic re~ction to penicillins
Dose
Adult: IV 11M or by intravenous infusion Ig every 12 hours ,increased
in severe infection like meningitis to 2g every 6 hours.
Gonorrhoea, Ig 1M as a single dose.
Pharmacokinetics
Ceftazidime is well absorbed when given parenterally, distributed
widely into body tissues and is not metabolized. It is excreted primarily
in urine and small amount in breast milk.
(
-71- -72-
/

" ",,' " " PREC s(PHARMACOrmg
CEFEPIME
Available preparations: Powder for injection Ig, 2g
Indications
.:. Skin and skin structure infection
Pharmacokinetics .,
Cefepime is rapidly and almost completely absorbed following
Intramuscular injection. It is widely distributed in body tissues and fluid
and is excreted unchanged in urine.
Key Issues to note
.:. Reconstituted solution may be stable for 24 hours at room
temperature or 10 days when left refrigerated
.:. Ceftazidime is incompatable with sodium bicarbonate
.:. IV Ceftazidime is physically incompartible with many
substances, avoid mixing with other drugs
~:. Pain at injection site
~:. Antibiotic associated colitis
<.:. Serum sickness like reaction
.:. Fever
Maxipime®
.:. Abdominal cramps
.:. Hypersensitivity
.:. Pruritus
.:. Phlebitis
.:. Arthralgia
Available brands:
Drug interactions
.:. Concomitant use with aminoglycosides results in synergistic
activity against pseudomonas aeruginosa
.:. Concomitant use with c1avulanic acid results in synergistic
activity against some strains of Bacteroides fragilis
.:. Probenecid decreases renal clearance of ceftazidime
.:. Loop diuretics may increase nephrotoxicity caused by
ceftazidime
.:. The effectiveness of oral contraceptives may be reduced by
ceftazidime.
Side effects
.:. Headache .:. Dizziness
.:. Urticaria .:. Nausea
.:. Vomiting .:. Diarrhoea
Dose
Adult:
Deep 1M, Intravenous injection or infusion ,Ig every 8 hours or 2g every
12 hours, 2gevery 8-12hours in severe infections.
Urinary trah infection; sOOmg-12 hourly
Bone and Joint infections: 2g IV 12hourly
Meningitis: 2g IV 8 hourly
Pneumonia: 500 - IOOOmg 8 hourly
Surgical prophylaxis: IOOOmg at induction of anaesthesia
Children:
By intravenous injection or infusion
I month -18 years: 2smg/kg every 8 hours doubled in severe
infections, febrile neutropenia and meningitis (max 6g daily).
Neonates 21-28 days: 2smg/kg every 8 hours doubled in severe
infections including meningitis.
Neonates 7-2 I days: 2smg/kg every 12 hours, double in severe
infection including meningitis.
Neonates under 7 days: 2smg/kg every 24 hours, double the dose in
severe infection including meningitis.
Indications
.:. Bone and joint infections .:. Urinary tract infections
.:. Abdominal infections .:. Surgical prophylaxis
.:. Neutropenic patients .:. Pneumonia
.:. Skin infections including burns .:. Septicaemia ¥,
.:. Sinusitis .:. Biliary tract infections
.:. Meningitis .:. Osteomyelitis
Contraindications
.:. Allergy to penicillin or cephalosporins
-73- -74-

.:. Cellulitis
.:. Osteomyelitis
.:. septic arthritis
.:. Pyomyositis
" ' , " : ,,' , ' I PRECISE PHARMA
I "
.:. Nosocomial pneumonia
.:. Intra abdominal infections
.:. Febrile neutropenia
Contraindications
.:. History of anaphylactic reaction to penicillins
Dose
Adult:
1"2 g every 12 hours for mild to moderate infections, increased to 4 g
daily in 2 divided doses in severe infections, up to 6 g daily in 3 divided
doses has been given for febrile neutropenia.
Urinary tract infection: 500mg every 12 hours for 7 - 10 days
Nosocorplal pneumonia: I - 2g every 12 hours for 10 days.
Febrile n~tropenia: 2g every 8 hours
Surgical prophylaxis: 2g as a single IV infusion dose starting 60 minutes
1
before operation.
Children:
>2 months and weighing up to 40 kg:
50 mg/kg twice daily; or 3 times daily for febrile neutropenia for 7 - 10
days
Side effects
.:. Skin Rashes .:. Thrombophlebitis
•:. Vaginal candidiasis .:. Anaphylaxis
•:. Headache .:. Vomiting
•:. Diarrhoea .:. Pseudomembraneous colitis
•:. Abdominal pain .:. Pain at injection site
Drug interactions
.:. Aminoglycosides and frusemide may increase the risk of
nephrotoxicity and ototoxicity with cefepime
.:. Probenecid decreases renal excretion ofcefepime
-75-
I I7' PRECISE PHARMAcoull/fl
Key Issues to note
.:. Store the drug at room temperature and protect from light
.:. Cefepime is incompatible with metronidazole, aminoglycoside
and aminophylline
C:I:FAZOLIN
Available preparation: Powder for injection 500mg, Ig
Available brands: Zepilen®
Pharmacokinetics
CCbfazolin is poorly absorbed from the GIT, therefore it must be
Illvcm by parental route. It crosses the placenta, penetrates bones
/llld synovial fluid well but CSF penetration is poor. It is excreted
1l11(:hanged in urine.
Indications:
.:. Pneumonia
.:. Erysipelas
.:. Septicaemia
.:. Bacterial endocarditis prophylaxis
C:ontraindications
l)ose. ,.
Adult. I -2g every 8 hours for 5 - 10 days.
()'teomyelitis 1-2g every 8 hours for 4-6 weeks.
'.'ptic arthritis.I-2g every 8 hours for 2-3 weeks
urgical prophylaxis Ig IV at induction of anaesthesia.
''''"nts and Children: 25mg/kg every 8 hours
'Ide effects
.:. Nausea .:. Vomiting
.:. Skin rashes .:. Diarrhoea
.:. Oral candidiasis .:. Urticaria
.:. Bronchospasm .:. Fever
.:. Pseudomembranous colitis
-76-
,'--'.

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