Pharmacology
- Pharmacokinetics effect of body on the drug
- Pharmacodynamics effect of Drug on the body
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Pharmacokinetics
- A Absorption
- D
- M
- E
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Route of Drug administration
Local Systemic
Entoral Periteral
ORal Rectal Injectable Nongrjedt
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- i-v Sublingua
- 1-m Transderm
- Sc Nasal
- Inhaler
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Lipid soluble can cross the membrane & goes in blood
Non Jonised Drug can cross the membrane & goes in blood
H20 H+ + OH-
Hx H+ + OH-
B. Dang medium solubility Cross the memt
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- Acidic A LS Non-Ionised
- Basic B LS "
- Acidic B ? Ionised X
- Basic A ?. Ionised X
Nature of the Drug. Acidic/Basic
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PH = ?
Pka is that PH 50% of Drug is lipid soluble & 50%. af Doug
is water soluble
PH Lipid Soluble water soluble
3 99% 0.1%
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4.0 99% 1%
5-0 90% -10%
6.0 50% 50%
7.0 10% 90%
8 1% 99%
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Handerson Hassdbach eq" PH = Pka + log [Jonued]
[Non Ionised]
Tell that How a sub. bechaus in different medium
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acidic drug absorb from stomach & basic drug absorb from Fritestins
bt most of the drug absorb from Intestine b/c.stay time
oxally Surface area more
100 molecules
first pass 80?30%
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metabolism.
:
50%.
201.xx
Bioailibility % of given drug i. e neach in systemic
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circulation in unachange form..
it depend upons:
? absorption directly proportional to Bicaulibility
? first pass metabolism ? Truversly poportional to bioclubbility
Nutroglycerine given orally I more absorption more Ist pass met-
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Nitroglyoxire given sublingual more blocuilidity & cicaulisty
Sublingual routes ? ? bloavilibity
? quick action
? can control the dose (if more split out)
?Self administrable
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5 No Ist pass metabolism.
? lignocaine
P? Propanstal
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G ? GTN
High Ist Pass metabolism -
: How to calculate sicawlibility of Drug?
> i-v route 100% Bioavili bility
18? calculate the Bicaulibility by oral route
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L
100 mg by i.v
Plasma AUC C
Conc AUC Coral route)
Time
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Bicailibility = AUC Coral)
AUC (V)
Cmax MTC
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Plasma Auc (area under curve)
conc MEC (mir Effective conc)
Tmax
Time
Auc? Tell about extent of absorption.
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Tmax Tell about rate af absorption -
Tmax low then use in emergency.
Cmax always lives byw Two tine (MEC & MTC)
MTC.? max thereputic conc
Bidequivelence
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$ if Blabelebety of 2 Brand of same dong is similar then they are
Said to be bioequivelence (±20) Not same
Ex Aspirin
Dispnen. Ecosprin
(500mg) (soo.mg)
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? ?
100 ng/dl 95 ug/dl
Phenytoin brand are Not bioequivalence
Dilantin # Eptan
They are Not Bioequivdence
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Excepients any things apart farm active
Ingredient af that drugs.
use for stablized the bugs
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.
Improve the taste of drugs.
Distribution
25
100% 50
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$ lepid soluble drug have higher distribution
Plasma protein binding &
1
Distribution Distrit
Plasma Protein Albumin acidic drug bind
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to albumir
2-Acid Gp Bind basic drugs.
ulfonamide ?.99% plasma protein Binding
Acidic in nature
Displacement ren? when two drug taken & having bath
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More plasma protein bendi
Samo Noturd
eg warfarin & sulfonamide
bendining
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$ Dilaysis is ineffective those drug having High plasma protein
Binding
& Dilaysis is Ineffective those drug having High Vo
$ Dilaysis Effective when drug have low vd & low PPB.
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?PPB?
D? Displacement sen
D? Disprubution low
(
3
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D? Dilaysis Ineffective..
(
3
- Barriers ?
3
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$ BBB ? area of Brain having No BBB
Circumventricular organs
Eg Area Postrema
=
Post Pituitary
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Sub fornical organ
organum vasculosem
Lamina Terminalis
chemoreceptor migger zone (CTZ)
L? on stimulation cause Vomiting.
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$ antiemitic Drug & antipsychotic drug can not cause vomiting
$ Blood Placental Barrier cause. Teratogenicity
?
Ex Thalidomide
?
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? Earliest use in
morng sickness of Nou
Cause Phocomelia Not us
(Sea limbs)
use for multiple myeloma
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bt c/I in pregnency
apperent Volume of dist. (Vd)
100mg
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VJ = Amount af guen drug
Plasma conc
Pc = 100 = 20 mg/dl.
5L
Vd = 100 = 5L
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5
20
100mg
50
PC = 50 = 10 mg/dl
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5L
Vd = 100 = 10 L
10
100mg
5L
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ocodile
Pc = 10 = 2 mg/dl
V = 100 = 50 L
5
2
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Clinical Imp af Vd.?
Chloroquine Vd> 1300L
max Vd
-cading dose Prilialy higher dose is guien to start
the effect of drug
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LD = VJ X. Target PC
> Loading deose depend upon distribution
Maintenence dose.
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Do Not depend on distribution
MD = clearence x Targe PC
Maintenence dose depend upon clearence.
Elemination To stop the action of drug
Metabolism Excoration
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- Metaboliem
Active metabolised, Inactive
Active Metabolises, Active
eg Diazepam Oxazepam
Inactive Metabolism Active
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kla Prodrug
eg levodopa
L-Dopa-
?L-dopa
1
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DA
ALL ? Pro Doungs ?
ACE Inhibitor (Excepted captopril
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Prefer Prednisone
Doing Depivnejsine
M methyl dopa, minoxidil, mercaptopurine
D - L- DOPA
In
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Clincal Cyclophosphamid, carbimazole.
Subject sulfasalazine
)
main purpose of metabolism to make Doug water salutle
i after metabolism all drug are water soluble.
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Phase. I ran Phase II xxn
oxidation Glucuronide
Redh Glutathione
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Hydrolysis Acetylation
cyclization methylation
Deamination Sulfat
$ most of prodering formed by phase I except minoxidil
in phase II xxxn.
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Enzymes
.
microsomal Non microsomal.
(ER) ? ?
Can be Induced or Inhibitor Not Induced or Intebito
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warfoun Heparin
100 +50 100 +50
50E-1 hr 50€/1hr
50 50
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Enzyme. Iducer ?
G? Griseofutuin (anti fungal)
P? Phonytain
R? Rifampicin
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S smoking (Nictoire is Not)
Cell CBR polycyclic aromatic Hydrocarbon
Phone Phenobarbitone.
it? Valporate
Enzyme Inhibitor
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Kotoconazole vit Kare Not Enzyme Inhibitor.
in cimetidire
use ciprofloxacin-
zyme - Erythromycan
nhibition ? INH
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CYP) (cytochrome P450)
?
? ? wavelength.
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I
Pigment Grene Subtype
CYP3A4 m/c Enzyme metabolised the drugs.
CYP2D6 Beta Block
Sex HR?
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ß Depresion
Depression Drang: MADI
SSRI
SNRI
"antiarrythmic drug? Except Amiodrone.
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CYP2C9. latting warfieren
Phenytoin
CYP2C19 Clopidogrel (Produng).
omeprazole.
CYP2E1 Enflurane
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PCM
Drung metabolised by CYP?
C- Cyclospren
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T? Tacrolimus
S statins..
C ? CAT Drug ?C? Astemizole cause.
A Amiodarone T? Terfenadine QT
N NAVIR Last ? ? prolongation
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•So it is
Banred
Exceretion
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* Lipid soluble drug
Reabsorbed & corne Bert
but w. soluble car
Not come back.
* water soluble duny
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Excoreted
GF
?
LS
Tukylar
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Secretion
?
mansporte
26
LS
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Come
Back
kja Tubular reabsorption
"all the drug car futters by glomerulus b/c lipid soluble can cross the
memb & water soluble can cross by pores.
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Clearence.
GFR 125 ml/min
? Aspirin poisioning •NaHCO3 (make urine alkalère so ut
No any antidot can not go to lepid soluble.
? & absorb back
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$ Acidic Drugs B Boorbitwates So t/r give? NaHco?
A? Aspirin
M-. Methotrexate
& Amphetamere ? NH4Cl is giver
Postoning
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$ Morphine antidotesdi Naloxane guien
L Basic Transporter.
$ Two type of transporter on proximal Tuble
$ these Tubules are satiorable. (at a time only one substana
Car go)
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Ex penicilin tyvery laro = b/c Tubular Senetion
clearence is more than fulporation the Tubular secretion must
Be added.
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if charence is less than fultration the Reabsorption must be &
P
PV = amount given /PC
LD = Vd x target Pc
PMD= CL X Target PC
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Rate of Elemination ?
› Clearence : Rate of Elimination
PC
Hay life
ty2= 0.693 X vd
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CL
ay life can not tell
rout dose.
t tell about dosing
terval. or frequency
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100 $ty2 = 6hr
?Y2 after Iday
50 Drug pemains?
?¥2
25 aftr 1 day = 4+Y2
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?+½ ans 6.25 nemain
12-5
1½ Ty2 = 6hr..
6.25 after 1 day how much is
diminat
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ARS 100-6.25 = 93.75%
160
87.5
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75
50
** (Steady state) depend upon tY2
?
Achived after 4-5 t/2
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Conc af steady stat depend upon dose
Variation b/w peak & trough depend upon
ONDER af finetics frequency af
Dosing Rate.
.
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First order zero order.
fraction const. Amount const.
100 100
? ?1hr
50 80
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25 11hr 60
? Ihr ?1 hr
12.5 40
? Ihr ?1 ha
6-25 20
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:
Reste af elemination [PC] order Rate of climmation Const.
Clearence ? Const clearance & I
PC
t½ (half life) = const t½ (half life) & fe
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Zero
Drug following Zero order kinetics
W-warferin
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A - Alchol/Asporin
T- Theophylline
d Kla saturation
Kinetics
Kla pseudozero order
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Kinetics
T Tolbutamide
)
Power - Phenytoin
Aspirin use antiplatlet - 300 7
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fever 600 Low Dose
?
it follow
Pain 900 Ist order kiritis
Inflamation 2000- righ dose
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it follow
zero order
Kinetics
zero order Kenetics can be convert in. Ist order kinetics
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? Pharmacodynamics
Effect of drug on the body
Physical
& chemical
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$ Enzyme
'$ Receptors.
:
Enzyme Inhibitor
Km Vmax
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? compitive ? ?
reversible
But organophosphate core Greversibe
? Non competitive ?
roversible but
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Carbonic aryh are reversible
? un-competitive ? ?
Ex- lithium -
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Receptors
D D Action
(Dung) ? ?
(romptor)
affinity Inpronsse activity
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Cability to drug bind Cability to produce action
to receptor) after drug binding to receptor)
Agonist ? max Immensic activity +1
Partial agonist ? Sub max Inprensic activity 0 to 1
Inverse agonist ? have opposite action ve
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)
› Antagonist ? No action/effect 0
(T Partial agonist ?
? High Affinit & High I A
© Low affinity & Lour IA
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(5 Low Affinity & High IA
(4 High & Low IA
Signal transduction mechanism ?
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? Inotropic Receptors. Dong Bind gete open. ¿ ir millise
EX.CNS
GABAA
fastest action.
Nat
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Ca++
K+
.
Ni
Glutamate NMDA
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NN 7 Nicotinic
• 5HT3
?
? Enzymatic Receptors k/a Tyrosine kinase receptor.
Drug bind out side & Enzyme activa
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Inside
Tyrosine kinase
Ex P Prolactin
I? Insulin
Not GHRH
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G? Growth hirmon
(Cytokine IL, INF
IGF, IFN
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3) G-Protoer coupeled Receptor 99% Doug work
? ? this receptor
G Protein
Reroflove Drung
Mactive
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CAmp stimulate heart
G
Break
in 2 pont
* Relaxes other part of body.
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> G-Proteeri?
9
ß
Y
CAmp
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? Ca
channel opening
GDP Phosphorylate GTP Brek
GDP when it phosphorylate
It brek un two part.
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?
make stablize (provide stability)
BXY
a
B
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Y
$ Camp & catt is second messanger.
GTP
? Contain GTPase
Enzyme.
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Intracellular Receptor ? only lipid soluble can cross & nea
on these Receptor
Slowest acting receptor
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Ex? Nuclear Receptor cytoplasmic Receptor
Sex Harmone Estrogen C? Corticosteroid
Progestoon Glucocorticals mineralo
A vit A Testosteron Cortical
T ? T3, T4 D? út. D
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$ if asked Nuclear Receptor superfamily then both yto & Nuclea
Receptor
This download link is referred from the post: Medical PG Handwritten Notes 1st Year, 2nd Year, 3rd Year and 4th Year (Study Material)
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