The General pharmacology ,Toxicology & Pharmacotherapeutics
To Undastanding the general pharmacology & Definitions of PHARMACODYNAMECIS ,PHARMACOKINITICS (Absorbation,Distribution,Metabolism,Excreation )Pharmacology ,Toxicology ,Pharmacotherapeutic ,
Advantages of Routs of Administration & Their Disadvantages
Factors affecting of absorpation ,excreation of drug,factor modifing deug action
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General pharmacology Diploma in pharmacy second year
1.
2. 1 General Pharmacology
Pharmacology - pharmacology is a branch
of science that Deal
With details study of drug .
Including meachnizum of action
Physiological or biochemical effects,
theraputics Uses & ADR on living system or
organ & tissue
PHARMACON -DRUG
LOGOS-SCIENCE
DRUG-Any substance use for purpose of
(MPCDT)
Mitigation,Prevention, cure, DiagnosiE
treatment Of DISEASE or DISORDER
It is FRENCH word
Drogue-Dry hurb
3. Pharmacokinetics
The study of (ADME ) absorption, distribution, metabolism,
excretion Of Drug & there relationship to pharmacologicl
Respons is called Pharmacokinetics
It is Greek word
That deal with What body does to drug
Absorption - Asprine in stomach & small Intestine
Distribution -80%drugs protin bound including brain
Metabolism - Asprine metabolized in liver with
Glucoronic acid
Excretion -The inactive metabolite is excreted in urine
4. Pharmacodymamics
The study of biological & therapeutic effect of drug along with
their mechanism of action is called Pharmacodynamic
IT deal with WHAT DRUG DOSE TO BODY
For ex 1-2 Dioxin -increase force of contraction by inhibiting
NA& K + ION
5. y
It is the science that
Deal with poison,
including detection,
prevention, cure of
poisoning
The adverse effects of drug,
drugs, overdose are
included In poisoning
6. General pharmacology
definitions
Pharmacothera
peutics
• It is a branch of
pharmacology which deal
with APPLICATION of drug
or prevention, cure,
treatment of disease
• Eg-Asprin reduced fever
Chemotherapy
• It deal with drug which kill&
suppress PATHOGENIC
MICROBES & CANCEROUS
CELL without Damaging
human host
• Therapeuticl used for
treatment of various
infection,antifungal ,bacterial,
viral infection
7. Bioavailibility
• The percentage Of drug
are absorbed form dose
Or it reaches to
systemic circulation is
called bioavailibility
• IV route bioavailibility is
100%
• Based on route
• Iv>IM>SC>ORAL>TOPICAL
• It is the minimum
effective conc.of drug
Administration to the
patient; as direct on
physician through to
produce desired
pharmacological
response
• Without production
advarce effect
Dose
9. Classification
1] systematic Route-Drug
intended to systematic
route
• 1] oral /Entral routes
*oral[mouth]
*Enema[specific part of body]
*sublingual [Toung ]
• 2]parentral route
• *ID *IM * SC *IV
*Intracardic *Intra articular
*Intramedullary
• 3]Trans-mucosal route
2] Topical /Local roite-
The drugs applied on
topically or localized
area
*Inhalation
*ophthalmic
*Nasal
*Rectal
*Vaginal
*Urethral
10. Oral /entral route-Commonly used like
Simple dosage form tablet. Capsules, liquids oral etc
Advantages
• Safe medication is
possible
• No pain form
• Not required trained
person
• Drug effect can control
• Not required completely
sterillization
Disadvantages
• Bioavailibility low
• No use in emergency
• Not used in
uncooperative patient
• Some drugs are Destroy
in digestive tract Like
insulin
• Certain drugs not
absorbed in GIT
11. Parentral routes
Advantages
• Rapid action
• 100%bioavalibility
• Used in uncooperative
patient
• Used in emergency patients
• Used in patient Having
vomiting & diarrhea
• Countinous IV dose possible
Disadvantages
• Painful
• Invasive
• Self medication not possible
it requires trained person
• Drug effect not controlling
• Strict aseptic area required
& syring including
• Necrosis [cell are dead]
12. Intradermal ingection [ID]-
Administration of drug layer of skin
Advantages
• This route is check Drug
sensitive reaction
• Vaccines are generally
administration
• Eg-BCG vaccine
Disadvantages
• Only small volume drug
are administration
Not more than 1ml
* Injection are painful
13. Intramuscular ingection [IM]
Injected into muscle tissue
Advantages
• Oily bases special
ingected
• It produce susend release
drug.
• Rate of absorption is
uniform
• Onset of action fast
compared to ID or SC
route
Disadvantages
• Total volume only 10 Ml
are administration
• It causes local pain
• It causes NECROSIS
• DEATH OF CELL
14. Intravenous ingection
Injected into vein
• Bioavailibility 100 %
• On set if action [about 15
sec]
• Use to clinical emergency
• Countinous large dogs
given
• The irritant drugs are
diluted are fastely
• Vein puncture cause
hemorrhage
• Drugs with oily base not
gives
• Speed of drug enteri nag
not cotrolled
• Cannot stopped action
to cause side eff4
15. Pharmacokinetics
• Absorption of drug -The process of drug form site of admistration to
systematic circulation is called absorption of drug
• 1] passive transport
•Simple diffusion
• •pore diffusion
• •facilitiated diffusion
• •Ionic diffusion
• 2]Active transport
• Pump transport
16. Passive
transport
This is the most commonly
meachnizum to most drugs
Are transportation across cell
membrane form
It passes to higher to lower
concentration
It not utilizing energy
Drugs are lipid soluble
[unionized ]are transferred
across cell membrane
17. Passive transport
Simple diffusion
• In simple diffusion,
lipid soludrugs are get
solubilized in lipid cell
membrane & get
easily transformed
across the cell
membrane along with
drug conc.
Pore diffusion
• This occur though
"protein
pore"molecule in cell
membrane
• Binding drug sub. Can
freely move cell
membrane along the
conc.
18. Passive transport
Facilitated diffusion
• This occurs though
"carrier molecule "in cell
membrane
• Drug bind & cross the
cell membrane for higher
to lower concentration.
Ionic diffusion
• That ions are
transportation
through the ion
Channel form higher
to lowered conctration.
19. Active transport -Active transportion are
required the energy the drug conc. Are transportation
lower to higher conc.
Like
sodium,calcium,chloride,potasssium,steroids ,etc
• In pump transport
Drug bind with
certain Enzymes
called as pump
transport
Pump
Transport
21. 1] Physical properties
Physical state
Liquid are better
absorbed then solid
Crystalloides are
better absorbed
then colloids
Water & lipid solubility
• Lipid soluble drugs are
more penetrate rapidly
into cell then water
The are directly
proportional to higher
lipid soluble drugs are
greater rate if absorption
form GIT
22. 2] Dosage form
Partical size
• A dosage form like
tablet is contain large
Partical aggregate may
require prolong time to
contact with Gastric
juice
Formulation
• Substance like lactose,
sucrose, starch, lactate,
etc are used to inert silents
in formulation tablet &
powers; may interfere with
active drug & affects it's
absorption
23. 3] physiological factors
Ph of GIT
• Acidic drug are better
absorbed in stomach
• Basic drugs are better
absorbed in Intestine
Ionization
• Unionized drugs are
lipid soluble while
ionized are water
soluble
• Hence, unionized drugs
are better absorbed
then ionized drugs in
cell membrane
25. Factor affecting drug
distribution
• 1] plasma protein binding
The phenomenon of complex formation
between DRUG & PLASMA protein is call ppb
2] Rout of administration
Parentrals routes are widely distributed the
body & tissue then oral route
3] BLOOD BRAIN BARRIER [membrane barrier ]
only high lipids drugs are cross the blood brain
barrier is calle BBB
26. • 4]capillary permeability- The condition of the capillary
wall that enables substances in the blood to pass into
tissue spaces or into cells, or vice versa
• 5] volume of distribution
• Amount of drug in body
• Vol =
• Plasma concentration
27. Metabolism of Drug
* Conversation of drug one
form to another form or
* A chemical alteration of drug
form living organism is called
biotransformation
90 to 95%drugs are excreted form kidney
60to 70%drugs is polar[water soluble]
Two phase of biotransformation
/metabolism
28. Metabolism of Drug phases
• Phase 1 • Phase 2
In phase reaction all polar
groups are introduced
into active drug molecule
by OXIDATION,
READUCTION, hydrolysis
reasult into formation of
inactive drug
This involved conjugstion
of active Drug or its Phase
1 metabolism with
endogenous substrate to
form a High polar ionized
organic Acids which are
readily excreted in urine
29. Excretion of drugThese are the process drug for their metabolic rareTransformer for internal
environment to external environment of body is called excretion of drug
30. Excretion of drug
Two types of drug excretion
•Renal Channel
[mainly through
kidney]
• Non- renal channel
[bile, lungs ,intestine
Skin ,saliva and milk]
31. Real channel
• Water soluble drugs
mainly excreted in kidney
that function are
impacted affect of conc.
Of drug one body
increased & produces
drug effect & Drug
toxicity
• The excretion of Acid &
Basic drugs Depends
upone the PH of urine
• Lungs-volatiles Like
general anaesthetic
• Bile- certain drugs
excreted Barbichurate
• Intestine- The purgative
like seena excrited
• Skin- Arsenic &Lead &
mercury heavy metals
Ecmxcreated
Non-real channel
32. Pharmacodymamics
Basic principles of drug action
Action of drug means
interaction between drug
and living system organs
tissue cells resulting in
modification of existing
function
It deal with what drug
Does to Body
33. 1]Stimulation
These are drugs or agent which
increases or stimulating activity of
specialized cell
Eg-1 caffeine stimulate cerebral cortex
2 strychnine stimulate spinal cord
3 Adrenaline stimulate force of conc.
2] Inhibition- These are the drugs
which are decrease the activity of
specialized cell
Eg-1 Barbichurate depressed
CNS
34. 3]Irritation
Irriation of non specialized
cell it causes stimulating
particular function
Eg-1 Ammonium chloride
causes Irriation
respiratory mucosal
• 4]Replacement
These are the
synthesis drugs
REPLACED by
natural harmon &
treat the Deficiency
Eg-1 Insulin in Diabetic
2 levodopa in Parkinson's
3iron in anemia
35. Factors modified Drug Action
Metabolic distributance
Rate of absorption
Presence of Disease
Age
Genetic Factor
Emotional factors
Sex
Addition[1+1=2]
Drug tolarence
Time of administrator
Climate
Synergism[1+1=3]
Potention[1+0=1]
Body weight
Environmental factors
Antagonism[1+1=0]
Cumulation
Mnemonic
36. Addition[1+1=2]
• When two drugs
admistred togather acts
Same pharmacological
system the total
pharmacological action
is equivalent of sum of
individual action is
called addition
Synergism[1+1=3]
• When two drugs are
administrator with
They act on different
Receptors but it produce
same pharmacological
action which greater
then individual
37. Potentiation
[1+0=1]
•The one drug
is increase the
action
ofAnother drug
•
• opposite action of
two drugs with
same physiological
System
Antagonism[1+1=0]
38. Rout of administration
• The onset of action is
produced by
intravenous rout
• Pharmacological action
is quick In this rout
Time of administration
• Such drugs are better
absorbed before
meal.Like
Hypoglycemic drug
Certain drugs are better
absorbed after meal like
griseofulvin
39. Drug tolarAlance
• A high dose are
required to produce
Therapeutic response
Tachyphylacis or acute
tolarnce
• Certain drugs are 5HT
are administrator
repeatedly. At very
short time interval the
pharmacologicl
response us decreases
is call Tachyphylacis
Drug dependence-
A state in which use the
drugs for personal
satisfaction, mood
stabilizer purpose but is
gives for a purpose to
cure diseases
40. Drug
interactions
A change in pharmacological
action by one drug to another.
It is drug interactions may be
BENEFICIAL OR HARMFUL
for persons or species
41. Classification of drug intreaction
1] drug interactions outside the body
A] use wrong vehicle for infusion
B] Addition of mixture of drugs to
infusion
2]drug intteation in the body
A] Pharmacokinetics drugs Interaction
B] Pharmacodymamics drug interactions
42. 1] drug interactions outside the
body
It occurs when wrong vehicle
are used for infusion or mixture
of drug• A] use wrong vehicle for infusion
Highly acidic solution such as dextrose,
fructose are unsuitable as vehicle for sodium
or potassium salt
• Weakly acidic drugs such as phenytoin
barbiturate as they may form PPT at this PH
• also, drugs penicillin, amoxicilline are unstable
At
• This ph of solution
• B] Addition of mixture of drugs to infusion
• Vit-E or C or Diagnose Other drugs Not mix
with other
43. 2]drug intteation in the body-these are
ADME OF DRUG are Altured by PPT
• 1]Absorbrption- Oral drug give drig intteation may result in
either increases or decrease absorption of drug by PPT drug eg-
1 calcium in milk inhibits absorption
• 2]Distribution -It depends upone the rate of binding of site to
the plasma protein
• 3]Metabolism It is a Change one form to another form
*PPT is increase rate of metabolism of drug is called ENZYME
INDUCER *PPT is Decrease rate of metabolism of drug is called
ENZYME INHIBITER
• 4]Excretion - PPT Of drug which lead to block the renal
Excretion of drug . Tubular transport may increase the rate of
excretion of the drug by increasing it's ionization
A] Pharmacokinetics drugs Interaction
45. Adverse Drug reaction [ADR]
According to WHO ADE is "any
Noxcious, unintended,
unwanted, "indescribable
response Dur to drug..Also
include ADR due to Drug Over
dose, Drug Abuse & Therapeutic
error
46. 1] Type A reaction /PredIctable- A) side effect B) Toxic effect
• Type A reaction -
A reaction is produced with Therapeutic dose of drug &
are more common, dose related reversible & preventable
A) side effects -side effects are the unwanted effects it
also beneficial or Other then therapeutic effects . Eg-
1 ) nsaids-gastric acidosis
B) Toxic effort-These are unwanted harmful effects
occurring due to overdose or long term Therapy
EG-NSAID - Peptic ulcer /kidney damage
47. B) Type B Reation / unpredictable- It
is unexpected & unusual
response produced by a
particular DRUG OR FOOD
• Drug Allergy /Hypersensitivaity-
These are the antibody mediated reaction
produced a some symptoms which is not
depending on DOSE
hypersensitivity is occur in some patient to
drug & can not producing individuals
48. Some imp Terms
Teratogenicity-
Teros-monster
Administration of few drugs
During Pregnancy Resulting in
birth of MONSTER LIKE baby
It harmful effects producing
on foetus, when the drugs
give in mother during
Pregnancy
Phototoxicity -It
refers to drug induced
Hypersensitivity of skin to
light readiton
Phototoxicity are drugs
accumulated in skin, absorbed
light & phtochemical reaction.
49. Therapeutic
Index
• TI for
approximately of
safety of dose
• large The TI
Greater the safety
& voice versa
• Safe drugs have
TI MORE then
one
It expiressed in medium length dose to
medium effective dose
TI-therapeutic dose
LD50-medium little dose
ED50-medium effective dose
LD50
TI=
ED50