Pharmacology is a branch of medicine, biology and pharmaceutical sciences concerned with drug or medication action, where a drug may be defined as any artificial, natural, or endogenous molecule which exerts a biochemical or physiological effect on the cell, tissue, organ, or organism.
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Pharmacology
1. PRESENTATION ON
PHAMACOLOGY
Presented to:
Dr. Pallavi Pathania
Associate Professor
Medical Surgical Nursing
Shimla Nursing College
Presented by:
Reena Sharma
M.sc.(Nursing) 2nd year
Shimla Nursing College
Shimla
4. TERMINOLOGY
TERM DEFINITION
Drug Any chemical that affects the processes of a living organism
Therapeutics Branch of medicine concerned with cure of disease or relief of symptoms and
includes drug treatment.
Toxicology Science of poisons/ Measurements or detection of poisons, Treatment of
poisoning
Drug Interaction Takes place when one drug alters the action of another drug
Chemotherapy Chemical agents to treat disease especially: the administration of one or more
cytotoxic drugs to destroy or inhibit the growth and division of malignant cells
in the treatment of cancer.
pharmacopoeia A pharmacopoeia is a legally binding collection of standards and quality
specifications for medicines used in a country or region
Desired action The expected response of a medication
5. Term Definition
Agonist A drug or substance that binds to a receptor inside a cell or
on its surface and causes the same action as the substance
that normally binds to the receptor
Antagonist A chemical blocks another chemical from getting to a
receptor
Antagonist
effect
It take place when 1 drug interferes with the action of another
drug. e.g. Protamine sulpha to counteract heparin toxicity
E.g. 1+1=0
Potentiation A drug that which has no effect enhances the effect of a
second drug
E.g. 0+1=2
Desired
action
The expected response of a medication
Side effects The unintended effects that occur within the therapeutic
range.
Adverse
reaction
An unexpected medical problem that happens during
treatment with a drug or other therapy.
Cont…
6. Cont…
Term Definition
Displacement effect It take place when 1 drug replace another at the drug receptor site, increasing the
effect of the 1st drug. E.g :warfarin and phenytoine
Incompatibility It occurs when 2 drugs mixed together in a syringe produce a chemical reaction so
they cannot be given. E.g. Protamine sulfate & vitamin k
Synergistic effect it takes place when the effect of 2 drugs taken at the same time is greater than the
sum of each drug given alone. E.g. combination of diuretics & adrenergic
blockers to lower the BP
E.g: 1+1=3
Single dose it is the amount of that substance to be taken at one time.
Daily dose The daily dose of a drug is the amount of that substance to be taken in a 24 hour
period.
Maintenance dose The maintenance dose of a drug is the amount of that substance taken to maintain
or continue a desired therapeutic effect
7. Pharmacology has four major branches
Pharmacology
Pharmacokinetics Pharmacodynamics Pharmacotherapeutics Pharmacy
8. PHARMACOKINETICS
• Meaning: The term pharmacokinetics is
derived from the ancient Greek words
“pharmakon” and “kinetikos”, meaning
“drug” and “putting in motion”
respectively.
• Definition: Pharmacokinetics is the
study of drug absorption, distribution,
metabolism, and excretion
11. Pharmacy:
• Definition:
The art, practice, or profession of
preparing, preserving, compounding,
and dispensing medical drugs.
OR
A place where medicines are
compounded or dispensed
12. Uses of Drugs
Prevention- used as prophylaxis to prevent diseases e.g.
vaccines; fluoride-prevents tooth decay.
Diagnosis- establishing the patient’s disease or problem e.g.
radio contrast dye; tuberculosis (Mantoux) testing.
Suppression- suppresses the signs and symptoms and
prevents the disease process from progressing e.g. anticancer,
antiviral drugs.
13. Principles of medication administration
Principles include :
3 checks and 10 Rights:
3 checks are
1. Check when obtaining the container of medicine.
2. Check when removing the medicine from the
container.
3. Check when replacing the container.
18. Oral route
Oral route: Medications are given by mouth.
Sublingual Administration: Some medications are
readily absorbed when placed under the tongue to
dissolve.
Buccal Administration: Administration of a medication
by placing in the mouth against the mucous membranes
of the cheek until it dissolves.
19. Parenteral Routes:
Parenteral administration involves injecting a medication into body tissues.
Intradermal (ID): Injection into the dermis
just under the epidermis.
Subcutaneous (SC): Injection into tissues just
below the dermis of the skin.
Intramuscular (IM): Injection into a muscle.
Intravenous (IV): Injection into a vein.
20. Cont…
Some medications are administered into body cavities.
These additional routes include
• Epidural
• Intrathecal
25. Drug name
Chemical…states its chemical composition and
molecular structure.
Generic…usually suggested by the manufacturer.
Official…as listed in the Pharmacopoeia. (I.P.,
B.P., U.S.P.)
Brand…the trade or proprietary name.
27. Drug allergy /Reaction
A drug allergy is an allergic reaction to
a medication. With an allergic reaction, the
immune system, which fights infection and
disease, reacts to the drug.
This reaction can cause symptoms such as
rash, fever, and trouble breathing.
True drug allergy is not common.
28. Drug toxicity
Drug toxicity refers to the level of damage that
a compound can cause to an organism.
The toxic effects of a drug are dose-dependent
and can affect an entire system as in the CNS
or a specific organ such as the liver.
29. Adverse Drug Reaction
Definition:
Any response to a drug which is
noxious and unintended, and which occurs at
doses normally used in man for prophylaxis,
diagnosis, or therapy of disease, or for the
modification of physiological function.
Acc to WHO
30. Serious Adverse Event (SAE)
• FDA reports Adverse events as Serious when an AE falls under the
following criteria:
• Death
• Life-Threatening (real risk of dying)
• Hospitalization (initial or prolonged)
• Disability (significant, persistent or permanent)
• Congenital anomaly
• Required intervention to prevent permanent impairment or damage
31. Adverse drug reaction (ADR) monitoring
Identifying Adverse Drug Reaction
Assessing Causality (Relationship between
drug and suspected reaction)
Documentation of ADR
Reporting Serious ADRs to
Pharmacovigilance centres /ADR Regulating
Authorities
32. Reporting Serious ADRs
Information to be Captured for Reporting includes the following:
• Patient details
• Initials
• Gender
• Age and date of birth
• Weight
• Height
33. Cont..
• Suspected drugs
• Generic name of the drug
• Indication(s) for which suspect drug was prescribed or tested
• Dosage form and strength
• Daily dose and regimen (specify units - e.g., mg, ml, mg/kg)
• Route of administration
• Starting date and time of day
• Stopping date and time, or duration of treatment
• Other Treatment(s) Concomitant drugs.
34. Cont..
• Details of Suspected Adverse Drug Reaction(s)
• Full description of reaction(s) including body site
and severity, as well as the criteria for regarding the
report as serious, whenever possible, describe a
specific diagnosis for the reaction
• Start date (and time) of onset of reaction
• Stop date (and time) or duration of reaction.
35. Cont…
Outcome
• Information on recovery; results of specific tests and/or
treatment
• For a fatal outcome, cause of death and its possible
relationship to the suspected reaction; any post-mortem
findings.
• Any Other information relevant to facilitate assessment
of the case, such as medical
• history of allergy, drug or alcohol abuse; family history;
findings from special investigations etc
37. ANALGESICS
ANALGESICS
An analgesic or painkiller is any member of the
group of drugs used to achieve analgesia, relief
from pain.
ALGESIA
An unpleasant sensory and emotional
experience associated with actual or potential
tissue damage or described in terms of such
damage
38. Cont..
ANESTHESIA
Anesthesia means loss of sensation.
Anesthetic agent is one which bring about
loss of all modalities of sensation, particularly
pain, along with a reversible loss of
consciousness.
39. CLASSIFICATION
It divided into two groups
Opoids Analgesics
e.g. Narcotics/
Morphine
Non-Opoids Analgesics
e.g. NSAIDs/Non
Narcotic/ aspirin like
analgesics
41. Natural opium alkaloids
Morphine: morphine is natural opium
alkaloid. Opium is milky exudate obtained
from unripe capsule of the poppy plant
papaver somniferum. Morphine is
powerful analgesic and narcotics.
42. Cont…
Uses: it use to relieve pain, anxiety, sleepness due to pain.
Dosage: adult: 10-30 mg, 4 hourly
SC/IM: 4-15mg.(4 hourly)
I/V: 4-10mg diluted in 5 ml of water for
injection (slowly over 5 minutes)
44. Semi Synthetic Opiates
Heroin (Diacetyl morphine): it is a semisynthetic derivative of morphine.
It is more potent analgesic than morphine. It produce euphoria and produces
severe addiction. It has no therapeutic uses more than morphine so it is
banned in our country.
Others drugs like:
Diacetylmorphine
Oxymorphone
Pholcodeine
45. Synthetic Opiates
Pethidine Hydrochloride: Pethidine is a synthetic opioid analgesic similar
to morphine although less potent and shorter acting. Its analgesic effect
usually lasts for 2 to 4 hours.
Indication:
moderate to severe pain.
Post operative treatment
Labor pains
Obstetric analgesic.
47. NON OPIOID ANALGESICS & NSAIDs
A) NON-
SELECTIVE COX
INHIBITORS
B) Preferential COX-2
Inhibitors
C) SELECTIVE
COX-2 INHIBITORS
D) Analgesics with
poor Anti
inflammatory action
48. A.NON-SELECTIVE COX INHIBITORS
Non-selective COX inhibitors, blocking the production of both physiologic
and inflammatory prostaglandins.
1. Salicylates –
Aspirin,
Salicylamide,
2. Pyrazolone derivatives –
Phenyl butazone,
Oxyphenyl-butazone.
3. Propionic acid derivatives –
Ibuprofen,
Ketoprofen
51. C) SELECTIVE COX-2 INHIBITORS
COX-2 inhibitors are NSAIDs that selectively block the COX-
2 enzyme and not the COX-1 enzyme. Blocking this enzyme
impedes the production of prostaglandins by the COX-2 which
is more often the cause the pain and swelling of inflammation
and other painful conditions
Valdecoxib
Celecoxib
Rofecoxib
53. USES
• Opioid drugs are useful in the treatment
general postoperative pain,
severe pain,
pain associated with kidney stone or
gallstones
abdominal distress and fluid loss
of diarrhea.
56. Side effect of analgesics
Side effects of analgesics may include:
• Constipation
• Drowsiness
• Dizziness
• Upset stomach
• Ringing in your ears
• Skin itching or rash
• Dry mouth
58. Introduction
Anti-inflammatory is the property of a substance or
treatment that reduces inflammation or swelling. Anti-
inflammatory drugs make up about half of analgesics,
remedying pain by reducing inflammation as opposed
to opioids, which affect the central nervous system to
block pain signaling to the brain.
59. Classification
Types of anti inflammatory agents
E.g:
1) Steroidal anti inflammatory drug 2) Non-steroidal anti inflammatory drug
Cortisole
Hydrocortisone Aspirin
Acetaminophen
60. Mechanism of action
Analgesics can inhibit the sensation
of pain by inhibiting transmission
of non-nociceptive impulses along
primary afferents (eg, local
anesthetics) or by altering the
perception of pain (eg, opioids).
61. Difference :
NSAID(Non-steroidal anti inflammatory
drug)
SAID (Steroidal anti inflammatory drug)
• NSAIDs stop the action of cyclo-
oxygenase, thus preventing prostaglandin
synthesis.
• Steroids inhibit phospholipase A2
• More effective than SAID • Less effective than NSAID
• More side effect • Less side effects
• Higher than SAID • Slower than NSAID
Examples:
Aspirin (such as Disprin)
Ibuprofen
Naproxen
Diclofenac
Examples
Prednisone
Bethamethasone
Prednisolone
Flurocortisone
62. Usage
• Pain of rheumatoid arthritis
• osteoarthritis and tendonitis.
• Muscle aches.
• Backaches
• Dental pain.
• Pain caused by gout
• Bursitis.
• Menstrual cramps
65. Antibiotics
“Antibiotic” is from antibiosis, meaning
against life.
Definition:
Antibiotics, also known as anti-
bacterials, are medications that destroy or
slow down the growth of bacteria.
66. Classification of Antibiotics
On the basis of
mechanism of action
On the basis of spectrum
of activity
On the basis of mode of
action
67. Mechanism of action of antimicrobial agents
1. Inhibition of cell wall synthesis:
• Penicillins, Cephalosporins, Bacitracin & Vancomycin
2. Inhibition of functions of cellular membrane:
• Polymyxins
3. Inhibition of protein synthesis:
• Chloramphenicol, Macrolides & Clindamycin
• Tetracyclines & Aminoglycosides
4. Inhibition of nucleic acid synthesis:
• Quinolones
• Rifampin
5. Inhibition of folic acid synthesis:
• Sulfonamides & trimethoprim
69. Antimicrobial Spectrum
Antimicrobial spectrum:
The scope that a drug kills or suppresses the growth of
microorganisms.
Narrow-spectrum:
The drugs that only act on one kind or one strain of bacteria.
E.g. (Isoniazide)
Broad-spectrum:
The drugs that have a wide antimicrobial scope.
E.g. (Tetracycline & Chloramphenicol)
71. On the basis of mode of action
Bacteriostatic
antibiotics
Bacteriocidal
antibiotics
• Tetracycline
• Chloramphenicol
• Erythromycin
• Lincomycin
• Cephalosporin
• Penicillin
• Erythromycin
• Aminoglycosides
• Cotrimoxazole
72. Classes of antibiotics
The main
classes of
antibiotics
• Penicillin's
• Cephalosporins
• Carbapenems
• Monobactams
• Aminoglycosides
• Fluroquinolones
• Tetracyclines
• Amphenicols
73. 1) Penicillin
• Penicillin are generally bactericidal, inhibiting
formation of the cell wall. Penicillin are used to
treat skin infections, dental infections, ear
infections, respiratory tract infections, urinary
tract infections, gonorrhea.
74. Types of penicillin
• The natural penicillin
• Penicillin G
• Dose: 0.5million units I.V. 6 hourly
• Penicillinase – resistant penicillin
• Methicillin & Oxacillin
• Aminopenicillin
• Ampicillin & Amoxicillin
• Dose: 250-500mg, 6 hourly
75. Penicillin side effects
• Diarrhea
• Nausea
• vomiting,
• upset stomach
• In rare cases Penicillin can cause immediate and
delayed allergic reactions - specifically skin
rashes, fever & anaphylactic shock.
76. 2) Cephalosporin
Cephalosporins have a mechanism of
action identical to that of the
Penicillin. It Interferes with synthesis
of the bacterial cell wall and so are
bactericidal.
77. Uses
• Pneumonia
• Strept throat, staph infections
• Tonsillitis, Bronchitis
• Otitis media
• Various types of skin infections
• Gonorrhea, Urinary tract infections.
• Cephalosporins antibiotics are also commonly used for
surgical prophylaxis
79. First generation cephalosporine
• They possess generally excellent coverage against
most Gram-positive pathogens and variable to poor
coverage against most Gram-negative pathogens.
• The first generation includes:
• Cephradine (Velosef)
• Cephalexin (Ceporex)
• Cefadroxil (Biodroxil, Duricef)
80. Second generation Cephalosporine
These agents are generally less active against gram-
positive cocci than first-generation cephalosporins and, at
best, equal to cefoxitin and cefamandole against many
gram-negative bacteria.
• 2nd Generation includes:
• Cefotetan
• Cefoxitin.
• Cefuroxime.
81. Third generation cephalosporins
• Third-generation cephalosporins are broad-spectrum
antimicrobial agents useful in a variety of clinical
situations. No one cephalosporin is appropriate for all
infectious disease problems.
• Third-generation includes:
• Cefotaxime
• ceftizoxime.
• Ceftriaxone
82. Fourth generation cephalosporins
• Fourth-generation cephalosporins are zwitterions
that can penetrate the outer membrane of Gram-
negative bacteria. They also have a greater
resistance to β-lactamases than the third-generation
cephalosporins.
• Fourth-generation includes:
• Cefepime
• Cefpirome
83. Fifth generation cephalosporine
• It is active against methicillin-resistant
Staphylococcus aureus (MRSA) and Gram-positive
bacteria. It retains the activity of later-generation
cephalosporins having broad-spectrum activity
against Gram-negative bacteria.
• 5th generation cephalosporine includes:
• Ceftaroline
• Ceftobiprole
85. 3) Carbapenems
• Carbapenems are a class of highly effective
antibiotic agents commonly used for the
treatment of severe or high-risk bacterial
infections. This class of antibiotics is usually
reserved for known or suspected multidrug-
resistant (MDR) bacterial infections
87. 4) Monobactams
Monobactams are monocyclic and bacterially-
produced β-lactam antibiotics. The β-lactam ring is
not fused to another ring, in contrast to most other
β-lactams. Monobactams are effective only against
aerobic Gram-negative bacteria (e.g., Neisseria,
Pseudomonas)
90. Side effects
• Stomach discomfort
• Diarrhea
• Nausea
• Vomiting
• Dizziness
• Headache
• Blurred vision
• Injection site reactions (redness,
discomfort, pain, swelling, or irritation)
91. 5) Aminoglycoside
Aminoglycoside is a medicinal and
bacteriologic category of traditional Gram-
negative antibacterial medications that inhibit
protein synthesis and contain as a portion of
the molecule an amino-modified glycoside.
Aminoglycosides are called bactericidal
antibiotics because they kill bacteria directly.
94. Side effects
• Loss of hearing.
• Ringing or buzzing in the ears.
• Feeling of fullness of the ears.
• Increased thirst.
• Needing to urinate more or less frequently than usual.
• Skin rash or itchiness.
• Unusual drowsiness, dizziness, or weakness
95. 6) Fluroquinolones
• Fluoroquinolones are antibiotics that are
commonly used to treat a variety of illnesses such
as respiratory and urinary tract infections.
Fluoroquinolones are often used for genitourinary
infections and are widely used in the treatment of
hospital-acquired infections associated with
urinary catheters. In community-acquired
infections
100. Antiseptic
Antiseptic are the drug or substance used
either to kill microbes or prevent their
further multiplication. The term antiseptic
is used for animate or living surface like
surface of skin, application of antiseptic
dressing on wound. The drug like phenol,
iodine, boric acid cetrimide are the
examples of antiseptics.
103. Alcohols
• Alcohols referred as “Surgical alcohol”
• To disinfect the skin before injections.
• Ethanol is effective in killing microorganisms like
bacteria, fungi and viruses.
• it is a common ingredient in many hand
sanitizers.
104. Acids
Boric acids
• It used for treatment of vagina, eyewashes and antiviral.
• It used in creams for burns.
• It present in eye contact solution.
Acetic acids:
• It is also called as glacial acetic acid
• It used to prepare dilute acetic acid
• It is used for the destruction of warts
105. Phenol Derivative
Phenol
• It is also called as carbolic acid
• It is used to disinfect urine, Pus, sputum and feces of patient.
• It is a strong disinfectant.
Cresol
• It is used in low concentrations in sheep-dips.
• It is used for disinfection of utensils, excreta and washing of hands.
106. Oxidising agents
Potassium permanganate:
• Potassium permanganate is used as a wet dressing
for wounds on skin's surface that are blistered or
oozing pus.
• Potassium permanganate can help to treat both
bacterial and fungal skin infections such as athlete's
foot and impetigo.
• It has also been used to disinfect water of wells,
ponds.
107. Hydrogen peroxide
• Hydrogen peroxide is a mild antiseptic used on
the skin to prevent infection of minor cuts,
scrapes, and burns.
• It may also be used as a mouth rinse to help
remove mucus or to relieve minor mouth
irritation.
108. Aldehydes
• Aldehydes have a broad spectrum of activity against
bacteria, fungi, and viruses.
• It is used as a chemical disinfectant for cold sterilization
of equipment.
Formaldehyde Used as an antiseptic in medicine,
disinfectant in funeral home.
It use to sterile the bed, blanket, books etc.
109. Biguanide
Chlorhexidine
• It is used as a skin wound cleanser and a general skin cleanser.
• This medicine is also used as a surgical hand scrub
• It is used to cleanse the skin before surgery to help prevent
infections.
• It is also used to sterilize surgical instruments.
110. Dyes
Acriflavine
• Acriflavine lotion is a topical antiseptic solution yellow or orange
in color, mainly used for minor wounds, burns, and infected skin.
Gentian violet
• it is an antiseptic dye used to treat fungal infections of the skin
(e.g., ringworm, athlete's foot).
• It also has weak antibacterial effects and may be used on minor cuts
and scrapes to prevent infection.
111. Halogens
Iodine
• Iodine is used to treat and prevent iodine deficiency and as an
antiseptic.
• For iodine deficiency it can be given by mouth or injection into a
muscle.
• As an antiseptic it may be used on wounds that are wet or to
disinfect the skin before surgery.
112. Chlorine
• it is a disinfectant which use to kills bacteria
• It is used to treat drinking water and swimming pool water.
114. Introduction
Cardiovascular emergencies are life-
threatening disorders that must be
recognized immediately to avoid delay in
treatment and to minimize morbidity and
mortality. Patients may present with severe
hypertension, chest pain, dysrhythmia, or
cardiopulmonary arrest
119. INTRODUCTION
Thrombolytic medication is used early in the
course of myocardial infarction (within 4 to
6 hours of the onset of the infarct) to restore
blood flow, limit myocardial damage,
preserve left ventricular function, and
prevent death.
121. CLASSIFICAION
ANTICOGULANTS
ANTIPLATELET DRUGS THROMBOLYTICS
Anticoagulants, commonly
known as blood thinners,
are chemical substances
that prevent or reduce
coagulation of blood,
prolonging the clotting
time.
Antiplatelets are medicines
that stop cells in the blood
(platelets) from sticking
together and forming a
clot. A blood clot can lead
to a heart attack or stroke.
Aspirin is the most
common antiplatelet.
Thrombolytic drugs
dissolve blood clots by
activating plasminogen,
which forms a cleaved
product called plasmin.
Plasmin is a proteolytic
enzyme that is capable of
breaking cross-links
between fibrin molecules,
which provide the
structural integrity of
blood clots
122. CLASSIFICAION OF ANTICOGULANTS
ANTICOGULANTS
Direct thrombus
inhibitors
vitamin K epoxide
reductase
In-direct thrombus
inhibitors
Direct factor
Xa inhibitors
Dabigatran
Heparin
Apixaban
Bivalirudin
Warfarin
Rivaroxaban
126. Aspirin
• Aspirin, also known as acetylsalicylic acid.
• It is used to:
• Reduce pain,
• Fever or inflammation.
• Specific inflammatory such as kawasaki
disease, pericarditis, and rheumatic fever.
• Aspirin given shortly after a heart attack
decreases the risk of death.
127. Mechanism of action:
• Aspirin decrease platelet
aggregation, it blocks pain
impulses in central nervous
system. The antipyretics action is
resulted by vasodilation of
peripheral vessels. It inhibits
prostaglandin synthesis.
128. Dosage
• Fever/ Pain:
• orally 325 mg to 650 mg 4 hourly not to exceed 4 gm/day.
• Arthritis:
• 2.6to 5.2 gm/day in divided doses 4-6 hourly.
• Transient ischemic disease:
• 325mg 6 hourly
• Thromboembolic disorders:
• 325-650 mg two times a day.
129. Streptokinase
• Streptokinase (SK) is a thrombolytic
medication and enzyme. As a medication it is
used to break down clots in some cases of
myocardial infarction (heart attack),
pulmonary embolism, and arterial
thromboembolism. The type of heart attack it
is used in is an ST elevation myocardial
infarction (STEMI)
130. Uses of streptokinase injection
• Heart attack
• Pulmonary embolism
• Heart attack
Dose: Streptokinase 1500mg Injection helps to lower blood
pressure and make it easier for your heart to pump blood around
your body. This reduces the chances of having a heart attack.
131.
132. Dosage:
• Acute myocardial infraction: 7,50,000 -1,500,000 IU diluted to a
volume of 45 ml to be given slow IV in one hour.
• Coronary artery thrombi: intracoronary 20,000 IU stat followed by
2000 to 4000 IU/ Minute for one hour.
• Deep vein thrombosis: 1.5 million I.U in 6 hours.
• Pulmonary embolism:100,000IU /hour for 24-72 hours.
133. Contraindication
• Intracranial hemorrhage
• Known structural cerebral vascular lesion
• Known cancer inside the skull
• Ischemic stroke more than 4.5 hours Suspected aortic dissection
• Active bleeding or bleeding problem other than menstruation
• Severe uncontrolled high blood pressure
• For streptokinase, prior treatment within the previous 6 months
134. Side effects
• Excessive bleeding
• Severe bruising.
• Prolonged nosebleeds (lasting longer than
10 minutes)
• Bleeding gums.
136. Introduction
• An inotrope is an agent that alters the force or
energy of muscular contractions. Negatively
inotropic agents weaken the force
of muscular contractions. Positively inotropic
agents increase the strength of muscular
contraction. Both positive and negative inotropes
are used in the management of various
cardiovascular conditions.
137. Cont..
Term “inotrope” generally used to describe
positive effect.
Positive inotropic: Positively inotropic agents
increase the strength of muscular contraction.
Negative inotropic: Negatively inotropic agents
weaken the force of muscular contractions.
Both positive and negative inotropes are used in the
management of various cardiovascular conditions.
138. Mechanism of action
Positive and negative inotropes work in different ways.
Positive inotropes
Help the heart pump more blood with fewer heartbeats.
This means that although the heart beats less,
It also beats with more force to meet the oxygen demands of body.
For example, one kind of positive inotrope called digoxin strengthens the
force of the heartbeat by increasing the amount of calcium in the heart’s
cells. (Calcium stimulates the heart to contract.
139. Positive inotrope uses
Increase Myocardial contractility.
Used to support cardiac function in conditions such
as:
a) Decompensated CHF,
b) Cardiogenic shock,
c) Septic shock,
d) Myocardial infarction,
e) Cardiomyopathy, etc.
142. 1) Beta blockers
2) Calcium channel blockers
Diltiazem
Verapamil
3) Class IA antiarrhythmics such as
Quinidine
Procainamide
Disopyramide
4) Class IC antiarrhythmics such as
Flecainide
Cont…
Negative inotropic agents
143. 1) Digoxin
Digoxin is a is used to treat heart failure, usually along with other
medications. It is also used to treat certain types of irregular heartbeat (such
as chronic atrial fibrillation)
Indication
• Congestive heart failure
• Cardiogenic shock
• Atrial flutter
• Atrial tachycardia
Dosage: initially 0.25 to 1.5 mg daily orally.
Maintenance dose: 0.25 to 0.5 mg daily
Positive inotropic
144. 2) Dopamine
It is a vasopressor drug which is naturally
occurring organic amine, when given
intravenous infusion it is increase cardiac
output. Dopamine is a prescription
medicine used to treat the symptoms of
low blood pressure, low cardiac output
and improves blood flow to the kidneys.
145. Mechanism of action:
Dopamine cause increase heart output
It act on beta1 and alpha receptors
Cause vasoconstriction of blood vessels
Dopamine with beta 1 stimulation
cause increase in the heat output.
147. 3) Epinephrine (ADRENLINE)
• Adrenaline is a powerful endogenous catecholamine. The
pharmacologic doses used in cardiac arrests. Adrenaline has both
alpha- and beta-adrenergic agonist effects.
• Action:
It stimulates myocardial contraction
Uses:
Increases the heart rate, and raises the blood pressure.
• Adverse effect:
• Ventricular arrhythmias
148. Dose:
In ventricular fibrillation or asystole, adrenaline should be given
in doses of 1 mg by 20 intravenous bolus.
Administration should be by a central line if already present or
by a large peripheral vein and followed by a 20 ml 0.9% saline
flush to ensure it rapidly reaches the central circulation.
If there is no intravenous access then adrenaline can be given via
the endotracheal tube.
When given by this route it should be diluted in 10 ml of 0.9%
saline and the dose should be 5 times the intravenous dose. There
is no role for intracardiac injection of adrenaline
149. 4) Norepinephrine
Norepinephrine, also known
as noradrenaline, is a medication used to
treat people with very low blood
pressure. It is the typical medication used
in sepsis if low blood pressure does not
improve following intravenous fluids. It
is the same molecule as the hormone and
neurotransmitter norepinephrine.
150. Mechanism of action
Nor adrenaline cause increase in contractility and heart rate
by acting Beta receptors in the heart
It also acts on the alpha receptors
cause vasoconstriction in blood vessels
The blood pressure is increased,
cardiac output is increased,
the coronary blood flow improve
151. Indication
• Shock
• Hypotension
• Restoration of blood pressure in hypotension state
• Cardiac arrest
• Drug reaction
• Blood transfusion
Dosage: I.V. infusion: add 4 ml nor adrenaline in 1000ml of 5 % Dextrose
solution.
Cardiac arrest: Rapid intravenous or intra cardiac injection 0.5-0.75ml of
solution
154. INTRODUCTION
Antihypertensives are a class of drugs that
are used to treat hypertension (high blood
pressure). Antihypertensive therapy seeks
to prevent the complications of high blood
pressure, such as stroke and myocardial
infarction.
158. Introduction
Beta-blockers reduce the heart rate, the heart's
workload and the heart's output of blood, which
lowers blood pressure. Beta blockers, also
known as beta-adrenergic blocking agents, are
medications that reduce your blood
pressure. Beta blockers work by blocking the
effects of the hormone epinephrine, also known
as adrenaline.
159. 1) Beta Blockers
1-Acebutolol (Sectral)
2-Atenolol (Tenormin)
3-Bisoprolol
4-Metoprolol
5-Nadolol
6-Propranolol
• Beta-blockers reduce the heart rate, the heart's
workload and the heart's output of blood, which
lowers blood pressure.
Examples:
160. USES
• High blood pressure
• Irregular heart rhythm (arrhythmia)
• Heart failure
• Chest pain (angina)
• Heart attacks
• Migraine
• Certain types of tremors
161. Mechanism of action
Beta blockers
Block the effects of the hormone epinephrine, also known as adrenaline.
It cause heart to beat more slowly and with less force
Which lowers blood pressure.
Beta blockers also help open the veins and arteries
Improve blood flow.
162. Side effects
• Common side effects of beta blockers can include
• Cold hands or feet
• Fatigue
• Weight gain
Less common side effects include
• Depression
• Shortness of breath
• Trouble sleeping
164. 2) Calcium channel blockers
Calcium channel blockers, calcium channel
antagonists or calcium antagonists are a
group of medications that disrupt the
movement of calcium through calcium
channels.
167. Calcium channel blocker
Prevents calcium from entering the smooth muscle cells of the heart and arteries
When calcium enters inside the cells,
it causes a stronger and harder contraction,
So by decreasing the calcium, the hearts' contraction is not as forceful.
Calcium channel blockers relax and open up narrowed blood vessels,
Reduce heart rate and lower blood pressure.
Mechanism of action
171. Angiotensin-converting-enzyme inhibitors
are a class of medication used primarily
for the treatment of high blood pressure
and heart failure. They work by causing
relaxation of blood vessels as well as a
decrease in blood volume, which leads to
lower blood pressure and decreased
oxygen demand from the heart.
3) Angiotensin-converting enzyme inhibitors
175. Side effects
• Skin rash
• Loss of taste
• Chronic dry, hacking cough
• In rare instances, kidney damage
• Women who are taking ACE inhibitors should not become
pregnant while on this class of drugs.
• They can cause low blood pressure, severe kidney failure, excess
potassium (hyperkalemia) and even death of the newborn.
176. Loop diuretics
Osmotic diuretics
Thiazides diuretics
Potassium sparing diuretics
4) DIURETICS
Diuretics, also known as water pills, belong to a class of
medications that remove excess salt and water from the body.
They are often used to treat hypertension, or high blood
pressure. High blood pressure.
Examples:
177. 5) Angiotensin II receptor blockers
• These drugs block the effects of angiotensin, a
chemical that causes the arteries to become narrow.
ARBs block the receptors so the angiotensin fails to
constrict the blood vessel. This means blood vessels
stay open and blood pressure is reduced.
Examples:
Candesartan
Irbesartan
Losartan potassium
Valsartan
Telmisartan
178. 6) Alpha blockers
These drugs reduce the arteries' resistance,
relaxing the muscle tone of the vascular walls.
Doxazosin mesylate.
Examples:
Prazosin hydrochloride
Terazosin hydrochloride
179. 7) Combined alpha and beta-blockers
• Combined alpha and beta-blockers are used as an IV
drip for those patients experiencing a hypertensive
crisis. They may be prescribed for outpatient high blood
pressure use if the patient is at risk for heart failure.
• Examples:
• Carvedilol
• Labetalol hydrochloride
180. 8) Blood vessel dilators (vasodilators)
• Blood vessel dilators, or vasodilators, can cause
the muscle in the walls of the blood vessels
(especially the arterioles) to relax, allowing the
vessel to dilate (widen). This allows blood to
flow through better
Examples:
• Hydralazine hydrochloride
• Minoxidil
181. 9) Peripheral adrenergic inhibitors
These medications reduce blood pressure by blocking
neurotransmitters in the brain. This blocks the smooth
muscles from getting the "message" to constrict. These
drugs are rarely used unless other medications don't help
Guanadrel
Examples:
• Guanethidine monosulfate
• Reserpine
182. 10) Alpha-2 Receptor Agonists
• These drugs reduce blood pressure by decreasing
the activity of the sympathetic (adrenaline-
producing) portion of the involuntary nervous
system. Methyldopa is considered a first line
antihypertensive during pregnancy because
adverse effects are infrequent for the pregnant
woman or the developing fetus.
Example:
Methyldopa
184. Introduction
“Vaso” actually means blood vessel.
Vasoconstriction is narrowing or
constriction of the blood vessels. It happens
when smooth muscles in blood vessel walls
tighten. This makes the blood vessel
opening smaller. Vasoconstriction may also
be called vasospasm
185. Vasoconstrictor drugs
On the basis of mechanism of action, there are two general classes
Sympathomimetic drugs Vasopressin analogs
Examples:
Alpha-adrenergic agonists
Phenylephrine
isoproterenol
Dobutamine
Examples:
Desmopressin
187. Vasoconstrictor drugs
Contract the smooth muscle in blood vessels
Which causes the vessels to constrict.
Which leads to an increase
in arterial blood pressure
Mechanism of action
188. Uses
• It used to increase blood pressure
• To treat hypotension and as topical decongestants.
• To reduce local blood flow.
• Vasoconstrictors mixed with local anesthetics are used to
increase the duration of local anesthesia by constricting the
blood vessels, thereby safely concentrating the anesthetic agent
for an extended duration, as well as reducing hemorrhage.
189. Uses
• Ventricular tachycardia
• Ventricular defibrillation.
• Heart failure
• Gastrointestinal bleeding,
• Ventricular tachycardia
• Ventricular defibrillation.
• Vasopressin is used to treat diabetes
insipidus
190. Side effects
• Dizziness
• Loss of balance.
• Numbness or weakness on one side of the face and body.
• Difficulty speaking.
• Difficulty seeing in one or both eyes.
192. Introduction
An arrhythmia is a condition in which the heart
beats too quickly, too slowly, or irregularly. In
many cases, the arrhythmia may not be serious or
require any treatment at all. However, if the
doctor finds that the arrhythmia could lead to
more serious heart problems, they may prescribe
medication.
196. CLASS-I
1) Quinidine
It is use in the treatment of cardiac arrhythmias with the
observation of “Wenckebach” in 1914. “Frey” in 1918 used
quinidine in the treatment of atrial fibrillation and found very
effective.
Indication:
• Atrial fibrillation
• Paroxysmal atrial tachycardia
• Premature ventricular contractions
197. Dosage:
• Atrial fibrillation: 200mg three or four time a day
Side effects: Disturbed color vision
Hearing loss
Depression
Skin rashes agranulocytosis
Respiratory depression
198. 2) Procainamide hydrochloride
Procainamide is used to treat abnormal heart rhythms. It
works by making heart more resistant to abnormal
activity. It is safer than quinidine and have quick action.
Mechanism of action: it depressed the excitability of
cardiac muscles to electrical stimulation, slow conduction
in atrium bundle and ventricles.
200. 3) Lidocaine
Lidocaine, also known as lignocaine and sold under the
brand name Xylocaine among others, is a local
anesthetic of the amino amide type. It is also used to
treat ventricular tachycardia
Uses: ventricular fibrillation and ventricular
tachycardia.
Dose: The usual dose is 1 mg per kg intravenously
given over 1 minute
201. CLASS-II
1) Atenolol
Atenolol is a beta blocker medication primarily used to treat high
blood pressure and heart-associated chest pain. Other uses
include the prevention of migraines and treatment of certain
irregular heart beats.
Indication: Supraventricular tachycardia, Hypertension
Dosage: Supraventricular tachycardia
Adult: loading dose 500mcg/kg/wt.
Maintenance dose: 50mcg/kg/wt. for 4 minutes
Maximum dose: 300 mcg/kg/wt./minute.
202. CLASS-III
1) Amiodarone
Amiodarone is an antiarrhythmic medication used to treat and
prevent a number of types of irregular heartbeats. It elongate
duration of action potential duration and effective refractory
period in atria.
Indication:
• ventricular tachycardia,
• ventricular fibrillation,
• wide complex tachycardia, as well as atrial fibrillation
and paroxysmal supraventricular tachycardia.
203. Dosage:
• Adult:800-1600mg/day for 1-3 weeks
Then
• 600-800mg/day for one month
Then
• 200 mg three times a day for one week
• Maintained minimum effective dose 200mg daily.
• I.V initially 150mg over 10 minutes, slow I.V
204. 2) Verapamil
• It is a calcium channel blocker medication used
for the treatment of high blood pressure,
angina, and supraventricular tachycardia.
Verapamil reduce work load on the heart by
reducing oxygen requirement of the
myocardium and by decreasing peripheral
resistance.
206. Blood and blood products
• Blood is a specialized organ that differs from other
organs in that it exists in a fluid state. Blood is
composed of plasma and various types of cells.
Plasma is the fluid portion of blood it contains various
proteins, such as albumin, globulin, fibrinogen, and
other factors necessary for clotting, as well as
electrolytes, waste products, and nutrients. About 55%
of blood volume is plasma.
208. Whole Blood
Whole blood contains red blood cells and plasma.
Whole blood is often used for open heart surgery. It
may also be used for exchange transfusions (complete
replacement of a baby's blood) in newborns with
hemolytic disease of the newborn. It is not common
for this product to be used for other reasons.
209. Packed Red Blood Cells
Red blood cells carry oxygen to the tissues. Packed red blood
cells have had most of the plasma removed from the whole
blood. Packed cells are most often given into a vein over two to
four hours. This is given to replace the red cells lost through
bleeding, hemolysis (destruction of the red blood cells), or
when the bone marrow produces fewer red cells.
210. Fresh Frozen Plasma
Fresh frozen plasma is plasma which was frozen
and stored shortly after it was obtained from the
blood donor. Fresh frozen plasma contains many
clotting factors. It is often used alone or with
cryoprecipitate to replace the low levels of
clotting factors. It is most often given into a vein
over one to two hours.
211. Platelets
Platelets are the cell fragments which prevent or stop
bleeding or bruising by plugging the hole in the blood
vessel. If a patient's bone marrow is not making
platelets, then platelet transfusions are most often
needed one time or two times a week (or even more
often).
212. Cryoprecipitate
Cryoprecipitate is the part of the blood which contains only
certain clotting factors such as factor VIII. Some patients
with certain types of hemophilia or patients who lack
fibrinogen may receive cryoprecipitate to treat their clotting
defect. Cryoprecipitate, may be given to help replace the
clotting factors that are low. Cryoprecipitate is most often
given over just a few minutes to an hour into a vein.
213. Granulocytes
They are cells which help fight off bacterial or
fungal infections. Granulocytes are sometimes
given to help fight off severe infections in
patients who have very low numbers of
granulocytes in the blood and have not responded
to medicine. Most often granulocytes are given
daily for five days or until the patient's
granulocyte count returns to a level which allows
the patient to fight the infection on their own.
215. DIURETICS
INTRODUCTION
Diuretics are the drugs which increase the
rate and volume of urine formation. There
are several categories of diuretics. All
diuretics increases the excretion of water
from body.
224. Uses of high ceiling diuretics
• Hypertension
• Pulmonary oedema
• Anemia
• Oedema
• hypercalcemia
225. FUROSIMIDE
• it is a loop diuretics such as furosemide
inhibits the body’s ability to reabsorb
electrolytes sodium at the ascending loop in
nephron. It is rapidly absorbed given by
mouth.
Diuretics of high efficacy
226. Mechanism of action
The drug frusemide inhibits
reabsorption of sodium and
chloride ions at proximal and
distal tubules, and in the loop of
henle. The drug is used in
oedema, CHF, and hypertension
treatment.
228. Bumetanide
• Bumetanide is used to reduce extra fluid in
the body (edema) caused by conditions such
as heart failure, liver disease, and kidney
disease. This can lessen symptoms such as
shortness of breath and swelling in your
arms, legs, and abdomen.
229. It act on ascending loop of henle by inhibiting reabsorption of
sodium and chloride ions.
Dosage: 0.5mg to 2 mg
Side effects:
Polyurea
Headache
Hypokalemia
Loss of hearing
Mechanism of action
230. Medium efficacy diuretics
Hydrochlorothiazide
• Hydrochlorothiazide is a diuretic medication often
used to treat high blood pressure and swelling due
to fluid build up. Other uses include treating
diabetes insipidus and renal tubular acidosis and to
decrease the risk of kidney stones in those with a
high calcium level in the urine
231. Mechanism of action:
• Hydrochlorothiazide act on
distal tubule, cortical thick
ascending loop of henle by
increasing the excretion of
sodium, chloride, potassium and
water. Useful in oedema,
hypertension.
233. Hydro-flumethiazide
Hydro-flumethiazide is a thiazide
diuretic used to treat hypertension as
well as edema due to congestive heart
failure and liver cirrhosis. It does not
change the body’s acid base balance. It is
rapidly absorbed when administered by
mouth.
234. • Hydro-flumethiazide is a
thiazide diuretic that inhibits
water reabsorption in the
nephron by inhibiting the
sodium-chloride symporter in
the distal convoluted tubule,
which is responsible for 5% of
total sodium reabsorption.
Mechanism of action
235. Cont..
Dosage:
Oedema:25mg-100mg once or twice daily.
Hypertension: 25mg-50mg once or twice daily.
Side effects:
• Polyuria
• palpitation
• headache,
• weakness
236. WEEK EFFICACY DIURETICS
Acetazolamide
Acetazolamide is the diuretic. Acetazolamide,
sold under the trade name Diamox. It is used to
treat glaucoma, epilepsy, altitude sickness,
periodic paralysis, idiopathic intracranial
hypertension, and heart failure It works by
decreasing the formation of hydrogen ions and
bicarbonate from carbon dioxide and water.
237. • Acetazolamide works by blocking the action of an
enzyme called carbonic anhydrase in proximal renal
tubules, it decrease the reabsorption of sodium,
potassium, chloride, bicarbonate, also decrease
carbonic anhydrase in the central nervous system .
Blocking this enzyme reduces the amount of fluid
that make in the front part of eye, and this helps to
lower the pressure within eye or useful in drug
induced oedema.
Mechanism of action
238. Cont..
Dosage:
Morning sickness :250mg twice daily.
Renal stone: 25omg at bed time
Close angle glaucoma: 250mg twice daily.
Close angle glaucoma: 250mg – 1gm daily in divided doses.
Edema in CHF: 250mg daily early morning
240. Spironolactone
Spironolactone, sold under the brand name
Aldactone among others, is a medication that
is primarily used to treat fluid build-up due
to heart failure, liver scarring, or kidney
disease or hypokalemia. Spironolactone is
known as a "water pill" (potassium-
sparing diuretic).
241. • Aldactone (spironolactone) is a specific
pharmacologic antagonist of aldosterone,
acting primarily through competitive binding
of receptors at the aldosterone-dependent
sodium-potassium exchange site in the distal
convoluted renal tubules. It make retention of
potassium phosphate.
Mechanism of action
242. Cont..
Dosage:
25mg-200mg once or twice daily.
Side effects:
• Prolong use in young patient may cause hirsutism
• Metabolic acidosis
• Hyperkalemia
• Impotence
• Gynecomastia
244. Introduction
• Sedative drugs are helpful for treating
anxiety and sleep problems, but using
them can lead to dependence or
addiction. Sedatives are a category of
drugs that slow brain activity.
251. Side effects
Sedative use can cause:
Drowsiness, dizziness, and confusion
Problems with movement and memory
Slowed heart rate and breathing, which may be
worsened if combined with alcohol
Increased risk of falls and injury
Worsening of depression and anxiety symptoms
Impaired attention and judgment
253. Introduction
• Digitalis, drug obtained from the dried leaves of the
common foxglove (Digitalis purpurea). It is used to
improve the strength and efficiency of the heart, or to
control the rate and rhythm of the heartbeat. The term
digitalis is also used for drug preparations that contain
cardiac glycosides, particularly one called digoxin,
extracted from various plants of this genus.
254. Cont…
• Digoxin and Digitoxin both drugs are cardiac glycoside.
• Digoxin ( Lanoxin) is usually the first choice drug,
because its half –life is 36 hours, whereas the half-life of
digitoxin is 4 to 9 days.
• Digitoxin is rarely prescribed
255. ACTIONS
On CVs:
Digitalis increase oxygen consumption of heart to normal.
It increases energy utilization, increases myocardial contraction.
Decreases venous return.
Conduction system:
Digitalis depresses the conduction system by direct action.
256. DIGOXIN
• Generic name: Digoxin.
• Brand name: Lanoxin, Lanoxicaps, Cardoxin, Digitek.
It is a cardiotonic glycoside obtained mainly from Digitalis
lanata.
Digoxin has positive inotropic and negative chronotropic
activity.
It is used to control ventricular rate in atrial fibrillation and
in the management of congestive heart failure with atrial
fibrillation.
258. Mechanism of action
Digitalis medicines
Strengthen the force of the heartbeat
By increasing the amount of calcium in the heart’s cells.
(Calcium stimulates the heartbeat.)
When the medicine reaches the heart muscle,
It binds to sodium and potassium receptors.
These receptors control the amount of calcium in the heart muscle
By stopping the calcium from leaving the cells.
As calcium builds up in the cells, it causes a stronger heartbeat.
260. Side effects
• Diarrhea
• Loss of appetite
• Drowsiness
• Headache
• Muscle weakness
• Fatigue
• Confusion
• Visual disturbances (blurred vision or yellow/green
halos around objects)
• Fast/slow/irregular heartbeat
261. Digitoxin
• Digitoxin is a cardiac glycoside. It is a phytosteroid and
is similar in structure and effects to digoxin. Unlike
digoxin, it is eliminated via the liver, so could be used
in patients with poor or erratic kidney function.
However, it is now rarely used in current Western
medical practice.
262. Indications:
• Congestive heart failure ,
• atrial flutter,
• atrial tachycardia,
• atrial fibrillation.
Dosage: Adult and child age 12 years and above , orally
1.2 to1.6 mg per day in divided dose. Child 1 to 2 year age
0.04 mg per kg weight.
265. Introduction
• The lipid lowering agents are used to treat
hypercholesterolemia and dyslipidemias. The major
effects of the lipid lowering drugs are in the
lowering of serum low density lipoprotein (LDL)
cholesterol levels which are believed to predispose
to atherosclerosis and its complications, acute
myocardial infarction, cerebrovascular ischemic
stroke and peripheral vascular disease
268. CHOLESTRAMINE:
These drugs indirectly increase hepatic
metabolism of cholesterol to the bile acids,
with that intermediate density of lipoprotein
(IDL) and low density lipoprotein is reduced
and where as very low density lipoprotein
density is increased.
Bile Acid Resins/Sequestrants
269. Mechanism of action
The bile-sequestering drugs
Lower blood levels of low-density lipoproteins (LDLs).
These drugs combine with bile acids in the intestines
To form an insoluble compound that’s then excreted in stool.
The decreasing level of bile acid in the gallbladder
That lower the cholesterol level
272. Colestipol
• It is an antilipemic drug. It acts after
absorption combines with bile acids to form
insoluble complex which is excreted through
feces, loss of bile salt lower cholesterol level.
273. Mechanism of action:
It absorbs and combine with bile salt to form insoluble
complexes, excreted through feces. It losses the bile acids to
lower cholesterol level.
Indication: Primary hypercholesterolemia, digitalis toxicity
Dosage: 2-8 tablets 6 hourly daily (1 gm)
Side effects:
Constipation, Nausea
Peptic ulcer
274. Fibrates acid derivatives
Clofibrate: it was used as hypolipidemic drug. Later on it
was observed clinically that I not too effective for
atherosclerosis.
Gemfibrozil: It is antilipemic drug. It lower plasma
triglyceride level by increasing breakdown an suppressing
hepatic synthesis of triglycerides.
275. Mechanism of action:
It inhibits biosynthesis of very low density lipoprotein,
decrease triglycerides, increase high density lipoprotein.
Dosage: 600 mg twice daily usual daily dose is 1200mg
dose to be taken half hour before meals.
Indication:
Hyperlipidemia
Lipoprotein abnormalities
277. Nicotinic acid
Nicotinic acid has been in use as a lipid-lowering drug
for five decades now. It is effective in lowering low-
density lipoprotein (LDL)-cholesterol, triglycerides, and
lipoprotein (a), and in increasing high-density lipoprotein
(HDL)-cholesterol.
279. HMG-COA
Lovastatin: it is the first statin that was clinically
used orally act as cholesterol lowering agent.
Mechanism of action: lovastatin inhibits hydroxy
methyl glutaryl coenzyme. A reductase enzyme and
reduces synthesis of cholesterol.
282. Simvastatin
• Simvastatin is twice as potent as
lovastatin. It is antihyperlipidemic
drug. It is administered orally as
an cholesterol lowering agent.
283. Mechanism of action:
• Simvastatin inhibits hydroxymethyl glutaryl coenzyme A
(HMG-CoA) reductase enzyme and decrease synthesis of
cholesterol.
284. Indication:
• Primary hyper cholesterolemia
• Coronary artery disease
Dosage: initial dose 5-10 mg orally as a single
dose in the evening not to exceed 40 mg/ day.
Side effects:
Muscle cramps
Vertigo tremors
Peripheral neuropathy
285. Atorvastatin:
• This newer statin is more potent. It has highest low
density lipoprotein cholesterol lowering capacity. It
act as a antihyperlipidemic.
• Mechanism of action: Atorvastatin inhibits
HMG-CoA reductase enzyme which reduces
synthesis of cholesterol.
287. Conclusion
Pharmacology is an exact science that rests
on a foundation of chemistry, physics, and
physiology. It is the study of how the body
responds to the drug. The discipline
encompasses the source, chemical properties,
biological effects and therapeutic uses of
drug. In nursing, the nurse play a integral
role in administering medication to patients.
The bile acid resins or sequestrants are the oldest and safest lipid lowering agents, but are less potent than other classes now available and are not always well tolerated. The bile acid sequestrants are highly positively charged molecules that bind to the negatively charged bile acids in the intestine, inhibiting their lipid solubilizing activity and thus blocking cholesterol absorption. They also inhibit the reabsorption of bile acids (which is typically 95%) and thus cause a contraction of the bile acid pool which leads to increased bile acid synthesis that competes with cholesterol synthesis in the liver, which also contributes to the lowering of serum cholesterol levels.