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1. INTRODUCTION
TO
PHARMACOLOGY
DR. SAROJ K. SUWAL
CONTENTS
• Terminology
• Source of drugs
• routes of drug administrations
• Pharmacokinetics, pharmacodynamic and
principle
DEFINITION? PHARMACOLOGY
• Is science that deals with the study
of drugs and their interaction with
the living systems.
• Pharmacology is derived from
Greek
• pharmacon → drug
• logos → study.
DRUG:
•is a substance used in the
• diagnosis,
• prevention or treatment of disease.
SOURCE OF DRUGS
•Natural
•Plant, Animal, Microoranisms,
Minerals
•Synthetic
•Semi synthetic
•synthetic
Source of drugs
• Human and animals:
• epinephrine,
• insulin
• adrenocorticotropic
hormone
Plant Source
• Leaf,
• steam,
• root,
• flower,
• seeds
• Pharmacologic Classification
• Similar Characteristics
• Similar Chemical Make up
• examples: Penicillin's, Beta Blockers
Drug Basic Classifications
• Therapeutic Classification
• Used for similar effect
• May not have similar chemical
make up
• Examples: Antihypertensives,
Antibiotics
ROUTE OF DRUG ADMINISTRATIONS
ROUTE OF ADMINISTRATIONS
• ORAL
• SUBLINGUAL
• BUCCAL
• RECTAL
• TRANSLINGUAL
• SUBCUTANEOUS
• INTRAMUSCULAR
• INTRADERMAL
• INTRAVENOUS
• INHALATIONAL
• TOPICAL
the most common Route
tablets, syrups, capsules
• ORAL-GI Route
• BUCCAL ROUTE
• SUBLINGUAL ROUTE
ORAL route
ADVANTAGES:
 Least expensive
 Easily Available
 most convenient route for most clients.
 Safe, does not break the skin.
 Conscious, able to swallow.
Disadvantages:
• Inappropriate for patient with nausea and vomiting.
• may have unpleasant taste.
• May cause irritation to gastro intestinal tract.
• discolor teeth and tongue
• can be aspirated
2. SUBLINGUAL
drug placed under the tongue, where it dissolved.
Advantage:
• Same as oral plus
• Drug may administered for local effect.
• Drug rapidly absorbed into blood stream.
• More potent than oral.
Disadvantage:
• If swallowed drug may be inactive.
• Drug must remain under the tongue until
dissolved.
• May differ with the taste
BUCCAL ROUTE
Rectal:
• Used in children
• Little or no first pass effect (ext haemorrhoidal vein)
• Used in vomiting or unconscious
• Higher concentrations rapidly achieved
Translingual:
• on the tongue.
THROUGH SKIN
•Intramuscular
•Subcutaneous
•Intravenous,
•Intradermal
into in the muscle.
Sites: Gluteal muscle,deltoid, thigh muscle,
Advantage:
• Pain from irritating drugs is minimized.
• Can administer large volume of drug.
• Drug rapidly absorbed.
Disadvantage:
• breaks skin barrier.
Intramuscular (IM):
Subcutaneous (SC):
• hypodermic into subcutaneous tissue, just below
the skin.
• Advantage:
• onset drug action faster than oral.
• Disadvantage:
• Must involve sterile technique because breaks skin barrier.
• More expensive than oral.
• Can administer only small doses.
• Slower than intramuscular injection.
• Some drug can irritate tissue and can cause INTENESE pain.
Intradermal (ID):
is the administrating of a drug into the dermal layer of the skin just
beneath the epidermis, usually small amount of liquid is used for
example 0.1ml.
• Advantage:
• absorption is slow (this advantage test for allergy).
• Disadvantage:
❖amount of drug administered must be small.
❖Breaks skin barrier
8. Intravenous (IV):
•allow injection of drugs and another substance
directly into bloodstream through the vein.
9. Inhalation:
• is apply to drugs directly onto lungs.
10. Topical Route
1. Skin (including transdermal patches)
2. Eyes
3. Ears
4. Nose
5. Lungs (inhalation)
• Pharmacokinetics
and
• Pharmacodynamics
PHARMACOKINETICS:
what the body does the drug
• kinesis ➔ movement
• is the study of the ADME
PHARMACOKINETICS
(THE PRINCIPLE OF ADME)
• Absorption
• Distribution
• Metabolism
• Excretion
ABSORPTION:
• May be via several routes
• Oral (mucosa,sublinguial)
• GI tract(intestines) – In
aqueous form
• Skin (eg.fentanyl patch)
movement of a drug into the bloodstream. from the site
of administration
ABSORPTION BY
1. Active transport
2. Passive Transport
• diffusion ( passive, facilitated diffusion)
• Endocytosis
• Exocytosis
BIOAVAILABILITY OF DRUGS
proportion of a drug which enters the
circulation when introduced into the body
to have an active effect.
IV route→ Bioavailability 100 % or 1
other route → less then 100 % or 1
DISTRIBUTION
• drugs leave the
bloodstream and
distribute into the
interstitial and
intracellular fluids
• Factors
• Depends on tissue permeability
• Depends on tissue perfusion
• Depends on amount of blood flow
• pH can affect
METABOLISM
• drug bio-transformed by the
metabolism in liver, and other
tissues( lungs, kidney,skin etc)
• most of drugs are metabolized
in Liver
• First pass metabolism or effect
FIRST PASS EFFECT
• Metabolism of drug in the gut
wall or portal circulation before
reaching systemic circulation
• so the amount reaching system
circulation is less than the
amount absorbed
EXCRETION -ALSO REFERRED TO AS CLEARANCE
• Relies mostly on KIDNEYS-
urine
• Skin-sweat,
• GI-stool ,
• nose
• Lungs
HALF-LIFE OF A DRUG
• is defined as the time taken for the
concentration of the drug in the plasma
• the time taken for the plasma
concentration of a drug to reduce to
half(50%) its original value
Elimination of a drug varies from person to person due to
factors like age, weight, other medications taken, or other
medical conditions present, also kidney function, liver function
etc.Therefore half-life is used as a guide or an estimate of how
MOST DRUGS ELIMINATION BY
• first order kinetics
• zero order kinetics
FIRST ORDER KINETICS
ZERO ORDER KINETICS
PHARMACODYANAMICS
•what the drug does the
body
•Also called drug actions
• Dynamics ➔Mechanics
•is the study of
• the effect of the drugs on the body
and their mechanism of action
PHARMACO DYANAMICS( DRUG ACTIONS)
Drugs
enter the
human
stimulate
• enzymes
• transporter proteins
cause body
To
react in a
specific way.
• receptors,
• ion channels,
act on
result
`
MECHANISMS OF DRUG ACTION
• Drugs work by altering normal cell and
tissue function.
• Specific groups of drugs have affinity
(attractive force) for specific target
cells, known as receptors.
Drugs
Binds to Receptor
Phamacological effect
• Agonist action
• Antagonist action
DRUG ACTION
• Agonist and Antagonist actions
• Agonists - they stimulate and activate the receptors
• Antagonists - they stop the agonists from stimulating
the receptors
THERAPEUTIC INDEX
• the ratio of the dose that produces toxicity to
the dose that produces a clinically desired
response in the population of the individuals
TI=TD50/ED50
Where ,
• TD50=the drug that produces toxic effect in
effect
• ED50=the drug that produces a therapeutic
effect
This is a measure of a drug’s safety
• A large number = a wide margin of safety
• A small number = a small margin of safety
DRUG ACTION
•DESIRED effect
• ( PCM decreased temperature)
•undesirable effect
• known as side effects
ADVERSE REACTIONS
• Allergic Reactions
• Hives
• Itching
• Edema
• Anaphylactic reaction
• Respiratory distress
• Cardiovascular collapse
RISKS WITH DRUGS
• Carcinogenicity
• ability of a drug to cause living cells to mutate and
become cancerous
• Teratogen
• drug that induces birth defects
FACTORS INFLUENCING DRUG ACTION
• Age --?overdosing and side effects
• Body Weight
• Metabolic Rate
• Illness
• Psychological Aspects
• Placebo effect
• Tolerance/Dependence
• Cumulative effect
DRUG INTERACTIONS
• Drugs can “mix” or interact with other
things
• Drugs
• Foods,Juices
• Disease
DRUG INTERACTION
• can cause
• decrease action
• increase action
• adverse effect
DRUG – DRUG INTERACTION
• two or more drugs can have
interactions
TYPES OF DRUG INTERACTIONS
• In terms of efficacy, several types of interactions
between medications:
• cumulative,
• additive,
• synergistic, and
• antagonistic.
Response
Time
Cumulative Effects
Drug A
Drug B
The condition in which repeated administration of a drug
may produce effects that are more pronounced than those
produced by the first dose.
Response
Hi
Lo
Time
A B
Additive Effects
A + B
The effect of two chemicals is equal to the sum of the effect of
the two chemicals taken separately,
Codeine+ Paracetamol
Addition
( increased analgesic effect)
Response
Time
A B
A + B
Synergistic Effects
The effect of two chemicals taken together is greater than the
sum of their separate effect at the same doses, e.g., alcohol and
other drugs
Aspirin+ Warfarin
leads to
(excessive
bleeding)
Clavulanic acid +
Amoxicillin
(increased
antibiotic effect)
Response
Hi
Lo
Time
A B
A + B
Antagonistic Effects
The effect of two chemicals taken together is less than
the sum of their separate effect at the same doses
Phenobarbital + Warfarin
Antagonism (less effect)
DRUG –FOOD INTERACTIONS
• Benzodiazepines + grapefruit→ Inhabit enzymes involved in drug
metabolism
• Benzodiazepines + grapefruit →Inhabit enzymes
involved in drug metabolism
• Digoxin + Oatmeal →Decreased adsorption of drug
• Aspirin + Milk →Upset stomach
• Acetaminophen + Alcohol →Liver damage
DRUG –DISEASE INTERACTIONS
• Nasal decongestants+ Hypertension→ Increased blood
pressure
• NSAID’S+ Asthmatic patients →Air way obstruction
• Minoxidil+ Heart failure →Fluid rentetion
• Nicotine + high blood pressure →Increased heart rate
• Beta blockers+ Heart failure →Worsen asthma
• Metformin + Heart failure →Increased lactate level
• Thank you

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1.introduction to pharmacology

  • 2. CONTENTS • Terminology • Source of drugs • routes of drug administrations • Pharmacokinetics, pharmacodynamic and principle
  • 3. DEFINITION? PHARMACOLOGY • Is science that deals with the study of drugs and their interaction with the living systems. • Pharmacology is derived from Greek • pharmacon → drug • logos → study.
  • 4. DRUG: •is a substance used in the • diagnosis, • prevention or treatment of disease.
  • 5. SOURCE OF DRUGS •Natural •Plant, Animal, Microoranisms, Minerals •Synthetic •Semi synthetic •synthetic
  • 7. • Human and animals: • epinephrine, • insulin • adrenocorticotropic hormone
  • 8. Plant Source • Leaf, • steam, • root, • flower, • seeds
  • 9.
  • 10.
  • 11.
  • 12.
  • 13.
  • 14.
  • 15. • Pharmacologic Classification • Similar Characteristics • Similar Chemical Make up • examples: Penicillin's, Beta Blockers Drug Basic Classifications • Therapeutic Classification • Used for similar effect • May not have similar chemical make up • Examples: Antihypertensives, Antibiotics
  • 16. ROUTE OF DRUG ADMINISTRATIONS
  • 17. ROUTE OF ADMINISTRATIONS • ORAL • SUBLINGUAL • BUCCAL • RECTAL • TRANSLINGUAL • SUBCUTANEOUS • INTRAMUSCULAR • INTRADERMAL • INTRAVENOUS • INHALATIONAL • TOPICAL
  • 18.
  • 19. the most common Route tablets, syrups, capsules • ORAL-GI Route • BUCCAL ROUTE • SUBLINGUAL ROUTE ORAL route
  • 20. ADVANTAGES:  Least expensive  Easily Available  most convenient route for most clients.  Safe, does not break the skin.  Conscious, able to swallow.
  • 21. Disadvantages: • Inappropriate for patient with nausea and vomiting. • may have unpleasant taste. • May cause irritation to gastro intestinal tract. • discolor teeth and tongue • can be aspirated
  • 22. 2. SUBLINGUAL drug placed under the tongue, where it dissolved. Advantage: • Same as oral plus • Drug may administered for local effect. • Drug rapidly absorbed into blood stream. • More potent than oral.
  • 23. Disadvantage: • If swallowed drug may be inactive. • Drug must remain under the tongue until dissolved. • May differ with the taste
  • 25. Rectal: • Used in children • Little or no first pass effect (ext haemorrhoidal vein) • Used in vomiting or unconscious • Higher concentrations rapidly achieved Translingual: • on the tongue.
  • 27. into in the muscle. Sites: Gluteal muscle,deltoid, thigh muscle, Advantage: • Pain from irritating drugs is minimized. • Can administer large volume of drug. • Drug rapidly absorbed. Disadvantage: • breaks skin barrier. Intramuscular (IM):
  • 28.
  • 29.
  • 30. Subcutaneous (SC): • hypodermic into subcutaneous tissue, just below the skin. • Advantage: • onset drug action faster than oral. • Disadvantage: • Must involve sterile technique because breaks skin barrier. • More expensive than oral. • Can administer only small doses. • Slower than intramuscular injection. • Some drug can irritate tissue and can cause INTENESE pain.
  • 31.
  • 32. Intradermal (ID): is the administrating of a drug into the dermal layer of the skin just beneath the epidermis, usually small amount of liquid is used for example 0.1ml. • Advantage: • absorption is slow (this advantage test for allergy). • Disadvantage: ❖amount of drug administered must be small. ❖Breaks skin barrier
  • 33. 8. Intravenous (IV): •allow injection of drugs and another substance directly into bloodstream through the vein. 9. Inhalation: • is apply to drugs directly onto lungs.
  • 34.
  • 35. 10. Topical Route 1. Skin (including transdermal patches) 2. Eyes 3. Ears 4. Nose 5. Lungs (inhalation)
  • 37.
  • 38. PHARMACOKINETICS: what the body does the drug • kinesis ➔ movement • is the study of the ADME
  • 39. PHARMACOKINETICS (THE PRINCIPLE OF ADME) • Absorption • Distribution • Metabolism • Excretion
  • 40. ABSORPTION: • May be via several routes • Oral (mucosa,sublinguial) • GI tract(intestines) – In aqueous form • Skin (eg.fentanyl patch) movement of a drug into the bloodstream. from the site of administration
  • 41. ABSORPTION BY 1. Active transport 2. Passive Transport • diffusion ( passive, facilitated diffusion) • Endocytosis • Exocytosis
  • 42. BIOAVAILABILITY OF DRUGS proportion of a drug which enters the circulation when introduced into the body to have an active effect. IV route→ Bioavailability 100 % or 1 other route → less then 100 % or 1
  • 43. DISTRIBUTION • drugs leave the bloodstream and distribute into the interstitial and intracellular fluids • Factors • Depends on tissue permeability • Depends on tissue perfusion • Depends on amount of blood flow • pH can affect
  • 44. METABOLISM • drug bio-transformed by the metabolism in liver, and other tissues( lungs, kidney,skin etc) • most of drugs are metabolized in Liver • First pass metabolism or effect
  • 45. FIRST PASS EFFECT • Metabolism of drug in the gut wall or portal circulation before reaching systemic circulation • so the amount reaching system circulation is less than the amount absorbed
  • 46.
  • 47. EXCRETION -ALSO REFERRED TO AS CLEARANCE • Relies mostly on KIDNEYS- urine • Skin-sweat, • GI-stool , • nose • Lungs
  • 48.
  • 49. HALF-LIFE OF A DRUG • is defined as the time taken for the concentration of the drug in the plasma • the time taken for the plasma concentration of a drug to reduce to half(50%) its original value Elimination of a drug varies from person to person due to factors like age, weight, other medications taken, or other medical conditions present, also kidney function, liver function etc.Therefore half-life is used as a guide or an estimate of how
  • 50.
  • 51. MOST DRUGS ELIMINATION BY • first order kinetics • zero order kinetics
  • 54. PHARMACODYANAMICS •what the drug does the body •Also called drug actions • Dynamics ➔Mechanics •is the study of • the effect of the drugs on the body and their mechanism of action
  • 55. PHARMACO DYANAMICS( DRUG ACTIONS) Drugs enter the human stimulate • enzymes • transporter proteins cause body To react in a specific way. • receptors, • ion channels, act on result `
  • 56. MECHANISMS OF DRUG ACTION • Drugs work by altering normal cell and tissue function. • Specific groups of drugs have affinity (attractive force) for specific target cells, known as receptors. Drugs Binds to Receptor Phamacological effect • Agonist action • Antagonist action
  • 57. DRUG ACTION • Agonist and Antagonist actions • Agonists - they stimulate and activate the receptors • Antagonists - they stop the agonists from stimulating the receptors
  • 58.
  • 59. THERAPEUTIC INDEX • the ratio of the dose that produces toxicity to the dose that produces a clinically desired response in the population of the individuals TI=TD50/ED50 Where , • TD50=the drug that produces toxic effect in effect • ED50=the drug that produces a therapeutic effect This is a measure of a drug’s safety • A large number = a wide margin of safety • A small number = a small margin of safety
  • 60. DRUG ACTION •DESIRED effect • ( PCM decreased temperature) •undesirable effect • known as side effects
  • 61. ADVERSE REACTIONS • Allergic Reactions • Hives • Itching • Edema • Anaphylactic reaction • Respiratory distress • Cardiovascular collapse
  • 62. RISKS WITH DRUGS • Carcinogenicity • ability of a drug to cause living cells to mutate and become cancerous • Teratogen • drug that induces birth defects
  • 63. FACTORS INFLUENCING DRUG ACTION • Age --?overdosing and side effects • Body Weight • Metabolic Rate • Illness • Psychological Aspects • Placebo effect • Tolerance/Dependence • Cumulative effect
  • 64. DRUG INTERACTIONS • Drugs can “mix” or interact with other things • Drugs • Foods,Juices • Disease
  • 65. DRUG INTERACTION • can cause • decrease action • increase action • adverse effect
  • 66. DRUG – DRUG INTERACTION • two or more drugs can have interactions
  • 67. TYPES OF DRUG INTERACTIONS • In terms of efficacy, several types of interactions between medications: • cumulative, • additive, • synergistic, and • antagonistic.
  • 68. Response Time Cumulative Effects Drug A Drug B The condition in which repeated administration of a drug may produce effects that are more pronounced than those produced by the first dose.
  • 69. Response Hi Lo Time A B Additive Effects A + B The effect of two chemicals is equal to the sum of the effect of the two chemicals taken separately, Codeine+ Paracetamol Addition ( increased analgesic effect)
  • 70. Response Time A B A + B Synergistic Effects The effect of two chemicals taken together is greater than the sum of their separate effect at the same doses, e.g., alcohol and other drugs Aspirin+ Warfarin leads to (excessive bleeding) Clavulanic acid + Amoxicillin (increased antibiotic effect)
  • 71. Response Hi Lo Time A B A + B Antagonistic Effects The effect of two chemicals taken together is less than the sum of their separate effect at the same doses Phenobarbital + Warfarin Antagonism (less effect)
  • 72. DRUG –FOOD INTERACTIONS • Benzodiazepines + grapefruit→ Inhabit enzymes involved in drug metabolism • Benzodiazepines + grapefruit →Inhabit enzymes involved in drug metabolism • Digoxin + Oatmeal →Decreased adsorption of drug • Aspirin + Milk →Upset stomach • Acetaminophen + Alcohol →Liver damage
  • 73. DRUG –DISEASE INTERACTIONS • Nasal decongestants+ Hypertension→ Increased blood pressure • NSAID’S+ Asthmatic patients →Air way obstruction • Minoxidil+ Heart failure →Fluid rentetion • Nicotine + high blood pressure →Increased heart rate • Beta blockers+ Heart failure →Worsen asthma • Metformin + Heart failure →Increased lactate level