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Download PG Medical 2nd Year Pharmacology Lecture Notes

Download PG Medical ( Post Graduate Medical degree) 2nd Year Pharmacology Lecture Notes

This post was last modified on 02 August 2021

Medical PG Handwritten Notes 1st Year, 2nd Year, 3rd Year and 4th Year (Study Material)


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Pharmacology

  • Pharmacokinetics effect of body on the drug
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  • Pharmacodynamics effect of Drug on the body

Pharmacokinetics

  • A Absorption
  • D
  • M
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  • E

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.

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? 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)

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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

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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

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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

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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

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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

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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

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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%

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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

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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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