Dr Sudheer

Prudhi
us
↑
.

Md
N 4/
I

S
~

O
vaca
=

-
Memor
Concept +
= a
Concepts KING
-
.

--

-
C t
NEET
- - ↑
Next/IniC/USMLE
...
No
Seerpentered
-

⑪
process
mon
 * ~

Pharmacokine cs/ Dose-concentration & Effect

.

Pharmacodynamics/ Conc .

-
component component
I ↓
.

I,
> Body
= -
-

ADME Drug
-

to
Body does =

drug .

(B + D)
-
- - A
.

&

O
T
- V C
-

&
-

Blood.
S

>
-

-
-
-

L
ME O
-
-

# -
A
-
All Pharmacokine c processes involve drug transport across biological

#A
-
-

membrane

> the membrane- E

Criteria for crossingO
- medium-same
& Nonlonised -

& lipid Soluble

.

&
⑬
D&
o
-
+
Non-Ionised
-
=>
-
~
&
Ionised
Solubility water Sol
=
lipid sol

Charge charged
uncharged
Cross membrane -
-
Crossv DONTCROSS -

Polarity
= less polar Move Polar
ASA
Renal excre on
NI- for Will Eliminate
Elimination &
-
-

&
Majority of drugs are A B
Why not strong acids/bases?

- Montain
L'a
Acids/Weakbases
Weak -
.

onised .

- -
 (9)
const
drug 30.EI
dissociation
Acid which ~

-
- Strengt
.
of Acid
-
-
②

O
>
A Blood
-

pKa:

si
-

M cell
less strength
.

LumpM ⑦
High
J
=
->
↓ -
>
- >

& More
Strength .

>
Low- -
& ⑦
&
-
=

Acidic ~
&
=

·
O &
↑
NI7I
-

Aspirin pKa = 3.5 -

Ha =>
=>
-
Crossbo
Gastric pH = 2 -

&
Acidic
-
-
- NI L I
Aspirin pKa = 3.5 -
PHPa i
=>
-

↓,

T
Mucosal pH = 7 cannot cross
- x -
-
-
-

③
-

S MucOSA

O
/I

O (A) E
S
=> & -
NH i

T ON Trapping
I E =>
Gastritis
-

&
- -

-
- -

&
-
-

Red
Bril
-
-

PH 19 ↑H > Pa A .
D -
2 -
4 = med.
B : -Acidis

↳
Acidic drug Basic drug

&
=> =

L
pH = pKa NT
T
-
-

-
-
-

pH < pKa
2
=
4
4
& ⑪ I
-
> T
-

S
pH > pKa
-
=
-
⑬3
NIC
-
T
- ⑪I
-

7 -
-

"Aendae
Al
Hepa c encephalopathy-

lose" =
-
-

git bac Lactid acid

mentation
↓ NAM
>
⑦
-

"Base" NHz
- Al

Non-Presid led led -

-
Renal clearance criteria:
-
a
-

sede
* T
=
 basic
Plas
>
-
O
Acidic
=
.
-

Urine pH:
If pa ent consumed As Amphetamine)
F (Morphine

I
,

Baridung
S TCA)
NOT Cost
-

Acidisdrug /Aspirie
-

↓
,

Will
Drug -
-

↓ Cross .
Med-diff . -
will
Med-Same-Drug -
=>
- ↓
Ab
No Me
↑

↓ 1,
Move Me Ab eliminated
-

↓ -

More
toxicity
-

Ankara
-
Urine pH * Done with Done in cases of
modifica on
EAlkaliniza on
-
>
-
NACOz- Acidic drug=
-
Poi
-

Na citrate
-
.

Acidifica on Citric acid ,

chloride poi
Basic
-
=> rus
Ammonium

I
-

-
I

Juice
1
-
-

Cranberry -

Dangerous Cardiac toxicity

.

Rhylnis
.

- May cause
-
-
 Bio-transporta on: e

= NUpfens
HydrolisEmerge
O Energy
↑ -
ATP
T
↑

-
-

& -
- -
- -
-
-
-

& 0000
I &
,

* Da
--
Energy Carrier Direc on Saturable
= -
Points

linder
requirement
-

Simple
Along

E
diffusion NO NO the
NO
100C
More
.

-
-

Core-
difference
gradient Abj ,
Pr
(H - L) *
-

Facilitated Along the

Diffusion NO Yes Con19 Yes

=e
Ac ve Agains PAT:
transport
.. s Yes
Yes
the
Cone -

Symport:

E
gradient
20
-
-

An port: Nat
.
# Exchanger

Not cat Exchanger

- =

COUNtexT/ -
·

-
Exchange . T
 > Blood .

Administration
-

Absorp on: Site of

AO

Route of administra on &

doesn’t involve absorp on- I
. -
(Bio
.
A = 100
-
-
%. )

Do
metabolism
Other routes have <100% absorp on due to- & liver *
C NOXINICET

=
2023 -
=
-

EX
-

&
-
-

-gp
-

O
I
-
- => #III
P ~J
D
-
-

Bioavailability Examples
P-gp>
inducer Move Ex
Rifampicin .

BIA)
- -
- =

&
Ase
P-gp S
inhibitor EXAux (D ~ erapamil - L
↓ -

&
-
-

~ Erythromycin

go
(M
-
.

Bio:
A -

it
jazi
& => -

(
=
-

-
-
--
I-
E
AT
-

- O

↑-
Op
(P)

& -- - S -O
E -
S

%
-
·
&
↳

-
-
-

a &
·
Cmax te of
For emergency drugs- Cmax Should
-

reach Quickly -
.

tmax of
Endrugs Short
#
·

AUC O U
Actabilit
ENT
=

·
Better Index for Bio
 I
↑ I

max
I
=
&
T

100---------- I
-

I s
I Conc

---
min-toxic
-
-

[P]
I

⑳
Con =
Min Effective
.

1
=

I
-
=
...
·
. . .

level
-
.

-
-

Sub-therapeutic
-

'

11
max"
X
80-0X
10-
time

*
-
- -

Acting a
somin
O
⑩
Start Showism
2) his "et' = soony
- Song -
-
I
-

& 3hrs
2001 Cmax

0
Ahrs

-
#I
-
S
372

l
 O

-en S
~
S
--
-

-x
⑳
&
- - &
V

' -

60mil
⑭ ⑬ >
-
Cory DO
A

① , 35 Y2
In

OVA
=
A L
L
& -
-----
-

!
&
MEC

&
-
00A
-----

n ⑬
-
-
--

-
-
Ma

-
-
 of Administered Jose is
How much fraction
Bioavailability:
=>
long >
-

is ; blood/at site of Action

.

Available in

O
& S A
-
B

O
a
S
-

f
&
- st
- D =

201
-
-
-

dug
-

B LINE
-
-

>IV Bioavailability- 100 % 100% B-A

& -

Q) Suppose a drug is given to a pa ent both orally and intravenous (IV) -

-
-
- -

injec on. For the IV route, a dose of- 25 mg leads to an AUC of 150 mg·hr/L. -
-
-

When administered orally, a dose of 50 mg results in an AUC of 100 mg·hr/L.

-
-
- -
- -

Calculate the&
-

bioavailability of the drug when it is administered orally. I - -

-

In-2rMg
~De Joes
Oval - = Y3
=
=

100
Caut
ITO/AUD -

-
F R I
-
3

tooo p
=

=
Bioequivalence: -
- &&
A
B0-10-100
Barange
-
B
S
-
os
A

=
>&
=
50
625%
U
-

125

&
-

40
~
A Dry-i
*
seen8
I D2
D 100

⑳
& 32
D Dr
-

=
Important in case: +
therapeutic
py
11

II,
Y
"Very
↑ toile
ro -68.
-
-

-
=

- low
-
-

J
Anticoagulane -

Antidiabetic
-

drugs -
=

Dud -
 First pass metabolism:
metabolism
Aka: Preustemic
Bioavailability: Decreased.
-
-
-
-
sonsa
=
Routes of administra on avoiding FPM: - IX
-

subcutaneous
- -

· Transdermal
*
Inhalational

S
Drugs with high FPM:

Eight -
nice &
-

-
-
-

I-lignocaine
Propanol
-

↑ => Ex
I-Isopreative -

p pethidine X
n
Salbutamol
-

H-
Hydrocortisone
↑ Morphine testosterone
.

+ -

Routes of administra on:

Route Points
economical convinient safest-
Oral
-
Most Common , ,
,

in Emergency Situations
Disadvantage: -
cannot be used -
-

limited
-

>
-
Absorption -

O
Sublingual Directly drug enter into: Superior Venacava .

-
-
-
-

Avoid FPM
Advantage: & desired Effectis reached
drug"
.

& "Sit
>
-
-
of once
-

:
Aguso
"

Intravenous Suitable for Highly Irritant drugs. ,

-
- -

AB
Not suitable for
=
drugs in
"oily Vehiclesin hemolysis
-
-

Intramuscular Suitable for milduritants

Vastus lateralis
-

max
Deltoid
Rate of absorp on- ,
-

=>
-

gintimax fatdepunition"

Avoided in pt => Pt Receiving "Anticoagulants"

f A
Hematoma formation .
 Route Points
small volume
Subcutaneous
=
Suitable for
=>
-

XO)
Not suitable for large
·

= 1/
-

evitants
.

&
Rectal Drug absorbed into &xt hemorrhoidd Veins
- -
-

Nasal route Examples: C-calcitonie L

-
CONDOMS
O-Osteoporosis
N-Nafrelin
e

-Desmopes
Migraine
.
7
is
-

-
Sumatriptan

Distribu on:
-
-
~
- -

Fr E
T
-
-

Bound
free Acidic > Albumin
-

Inactive
·

glycoprots
·

G , Acid
·
Active Basic >
-
- ·
Not eliminated

Eliminated .
lipoprot
·

=
 e e

areataill of
-
-

Total Space Amount

-

Apparent volume of distribu on (aVd): to

-

-
-
the body =
- -
-

S
-
-
&-
-

-
- -
-

IIIIII ,

⑳
-
IL 12

&
-
-
=
-

and =
& D
&
=
-
-

and to -

-
&
D
-
-

-
V

aVd =
L

=
>

Re
e
are
A-
-

~ Lipid Solubility .

① X a Blood.
&
=

Tissue
x
.

-
-
= -

&
-

low Nd-tissues
& High - High

&
Y 1
=

High
& O
.

low
=

- Low-
- -

More Pub DOA

· *
(
More
blood
↓
-
= lov
Is
100V d
 -

Dialysis is-
↳
Dialysis criteria:

now
↳
·
free

ineffec ve for the following drugs

s
-

D A-Amphetamine
X -
Verapamil
Opioid poi
O-op Poi ,

1 - Imipramine
Diazepam
.

D-Digitalis ,

&
Teratogenic drugs:
Thalidomide Phocoelia .

Tetracyclines Bone ,
teeth Ab N .

DES Di-Ethyl Offens

"

Stillesterall

i
Vaginal Carcinoma .

Isotre noin (vit Cranio-facial-Cardiac AG N

↑
.
-
Al
=

ACE inhibitors/ARBs
-
Renal Hypoplania .

Alcohol
=
Fetal Allonol Synd + craniofacial AGN 2T/300
F
= -
-

An -thyroid drugs ·
asia Cutis

(Methimazoles Esophased Fistula

=>
.

Teacheo -

Lithium A 1000
& Ebstein Anamoly
-
-
-

=
- Neetin -
-

Phenytoin Craniofacial A (left lip Palate .

- -
-

Down
Valproate
-
=
Neural tube defects
-

Topiramate
- Cleft lip
-

-
Warfarin
- Nasal popania , stippled Epiphylis
Penicillamine
-
-
slax
send a
-
 = -
-
-
- folic acide
=

O >
- Metronidazole
&
.

Dit
·
-

-
-

O-
Al
↓
1 -
-
- -
- - -

O Majority of drugs-
-
-
- - -
- -

⑦ -

Anticonvulsants-
-

-
=> =
-

X "
Is
Anticancer
-
-

"
Blood Brain Barrier: lipid sot
"

Ab
BBB

&
Eliminate.
-
-
-

-- Ex .
-
↑
-

rumerica
-
~ e

Is

"SAP"
S
·
subtornical organ

e
-
O-Organumfasculos a

A -

Areaposten
-

Post pituitary
p-
gland .

pincal -
-
Redistribu on:
-

Solubility- Lipid
- -

-
-

Thisstone Nan
-
-

Classical example-
-
-

&
↳
↳
As
-

Al
Rapid OOA distribution
Rapid
.

-
>
-

Thiopentone sodium
-
=

-
-

Short DOA Redistribution.

(Anesthetic Agents -
=
-

-
-
=> -

T
Other examples: FADE
=> F-fentanyl
A)
(I .
Agents
A-Anesthe
D-Diazepar
X
E
-

Biotransforma on:
-

1) Ac ve drug ----------> Inac ve drug

-
-

2) Ac ve drug ----------> Ac ve drug -

MAID
A
=

↓, -

M-Morphine
Amitriptylin
A -
Allopurinol ,

1-
Imipramine
-Diazepam (MOHoB2D)
S -
spironolactone
 1
000
=

&
-

LOTS"
/

Benzodiazepines not having ac ve metabolite: a) 454 -> liver fal

-
-
-
-

&
- Live terred in

Failupt
River
.

-
-

I
Tema
.

T -

S-Estazolam

"prodrugs- A
- AD Advantages: Better bio
.

3) Inac ve drug ---------->Ac ve drug

stable
↑

O
-
More-
-
drugs-
S-Sulfasalazine
Prednisone
P-PI
Proguanil ,

listnop)
Ob
10.
captopril Deep
LOXaS]
,
, =>
-
<Except -
--

s
Siny a
.

ACE
,
A - -
-

stating
[eep
-

S-statins --
-
Mercaptophrine
Methyldopa ,

M -

Minoxidil,
O-Oseltamira
-Lopa ,
pietrine
2024c-
1
A
hosphamide
17

1: I rinotecan ->

-
clopidogrel, 1-
-

-carbimazole ,

Biotransforma on
-

Phase-I Phase-II
-
-

Aka Degradative Conjugative

Synthetic
-
-

↑
.

Non-synthetic
.

wate
"I -
Final product W/L - 10)

J
-
-

I/NI
-

↓,
2020
= PINP P-Polax ~

Examples

I
-
-
Oxidation glucoside cont &
cont
Reduction * glutathione
Hydroyic * Acetylation
=
 Drag +
P=

-
>
-

↳ 1
X
-

-
Despit
=
Hofmann elimina on: Non-Enzymatic
& Eliminated
·

--
rearrangement -
get Mit
oft unburn
Molecular
O
-

Ph

& ⑫ doneo
·

of
Ex Atracurium
As a
& I
-
=
> formation
=
-

-Microsomal enzymes Non-microsomal enzymes

nondflasehetile
Loca on-
- -
- -
Cytoplas Mitchene
,

= shows genetic polymorphism =

-

=>
CYP450/Mixed func onal oxidases:
e

Concern a
(tet)
·
Hemoproteins CYP3AY
· when Rixen 2D6
29
2019

3 Ar
3 A l
>

CYP &I
- Isoform
pinic family subfamily
- -
-

Cytochrome
-

-
50 %
-MI

CROP
TOMP
↓ /

&
20MI

CYP3A4
-
Majority of drugs -

CYP2C19
-
clopidogrel .

- =

&
nearne
CYP2C19
~ CO P

see
>
-

Clop- ~

#AtTo
-
Active

garde .
-

(PPE -
-
 Normal &
Enzyme induc on ↳ Enzyme inhibi on
I
not
-
>
-

2
-

Efficacy toxicity
100
100
I
.

100

e min,
-

NE,
-
-
10 00E E

&
100

mie (TTCi
JO
,
>
TO
=
0=

Examples: Examples:
OK
service
Pricing
-
-
- -

Phenobarbitone
-

SSRI
P-Pherybin ,
S .
P

e-Erythormyein
.

=
=

Rifampicin
]
R =

smoking -Mitonavis rate

Cigarette
-carbamazepine ,
e
( Polycyclic
Aromate
Hydrocarbons)
X.
erapamil ,

- Isoniazid
Ciprofloxacin Chloramphenical
i

I -
Y ,

~ -
Nevirapine C-cemitidine -
-
,

griseotulin Erythromycin
.

- -
& -

Barbiturates - ALA synthase 0 -

0 meprazole
Ketoconazole
.

K .
=

Phenobarbitone - Neonatal jaundice

St.John’s wort:
-

- - E Inducer
-

1s

Grapefruit juice: (furanoumarine

↳ E .

Philitor
Inhibitor
-

-
Alcohol
Acute
- E

Ener
.

chronic
 & <Ritempi

&
I↑ B =
Eti

.
Known Epileptic
2
T
-
/
-

O & AlO
.
1
I -
Or doms
-

&
,
>
.
-

-Phenytoin
- -
-

-
-

~
= =
-

↳ &-
-

[period
-N
F
↓,
(w !

Xe
O
+
-
-
>
-
 Glucuronide conjuga on:
-

GT'
-
-
UDP -

-
=

Glucoronal
>
- transferase
/
.

VATIAl
-

"
.

Serend attar send

-
- -
eigler
Decreased expression of UGT1A1 gene- -

&
Wartaria
-

- -

to send t
purple send >
- Phenytoin
glove
Less ac vity in: purple Amiodarone
e
-
man send
Blue
-

->
Vancomsie
Examples: Aspirie Red
>
Rifampicin
.

Bilurubi send
red-
Orange
color >
-

grey bay
Chloramphenicol
.

>
-
Urine
-

B -

Acetyla on:
=

Examples: Hepatotoxicity
-
>

A-
Fast
H- Hydralazine

E
europathy
Peri
- Isoniazid & Slow ·
A + -
-

-
> Procainamide
5 Sulfonamide .

CLE
-

Characteris c ADR: Drug reduced

us -

- -
-

Glutathione conjuga on:

Paracetamine
=
Example: -
Paracetamol toxicity occurs @ low doses
III
-
-

↓ / ChAlcoholics
Es
Glucowonide
Sulfate
(4p)
-

Toxici
I
I↑
-

CONT CONT E Mine

- -
Quinone

doe -Acetyl Parabenzo

-
, -
-

present
T
Not
ast-
-

ROS
Eliminated
-

⑦
s
-
>
-
~ 2022 Riverdange
-
R-N-Acetylcysteine
-

~ =>
-
 Elimina on:
-
-

A
Enterohepa c cycling =>
Drugs with more M.Wt (>300), preferen ally eliminates via Bile
11 11
.

Fees tubules
-
-

& +
/1

I
TO
e
ITS - -
=
=
- =

Interac on Result
& & With Penicillin L Blood -
-
tlpenicillie in
-

Probenecid -

↓ With uric acid

uricose
~
A 11 Urine
U
.

Or .
U -
-
-

11
of drug eliminated /unit time -

Amount
7

&
=

Rate of elimina -
on: -
-
-

unit time
-

drug
-

In
cleared of
that

Clearance: "An
=>
a

-
f
-

to become
for the dray cone
"

time Helen ,
Value .

&P
Qar It's "Previous/Earlier
-
-
Half-life (t1/2): hal of
·
S se
-
-

- -
-
L

4n
y+
+)

Q) The clearance (Cl) of a drug from the body is found to be 0.5 litres per hour
&
-

(L/h), and the volume of distribu on (Vd) is 10 litres (L). Calculate the>
half-life
- -

0⑳
- -

of the drug.
0 .
69x10 -

Ch = 0 5
-

ty2 =
-

0'5
-d =
O
10
 O
First order kine cs Zero order kine cs
Aka Linear . Non-L
1
Saturation . Saturation
.

>
-
-

Non i

capacity limited enter

= . 1

flow dependent K Michaelis

.
K

Drug * S

Fraction 100
100
80 60 no&
Amount J
20

!
.

eliminated -

A
Rate of
* ↓ Plasma cons. endependent -

elimina on =

*
Clearance
Coast Not .
)*
(L -
= SA

Half life Art Y2()

Const
.

As 000
Examples WHEAT -
-

Majority-
- W-Wartarie
H-Hydatoin/Phenytoin
-

E-Ethanol
A -

Aspirie
T-theophyllin-
Tolbutamidat

Steady-state plasma concentra on (SSPC)/Plateau level:

po
=

↳
Number of half-lives needed to reach SSPC: ↳ -
-

SSPC depends on:

 NY No Joy rox
175
⑦
Got 12 4 + 6 . 25 > 3
-
-

24 -
.

100 -> 50 -

602
-
...

No
NOT 5 >
of
-

2D
5 - 17 .

25
=
100 = H
H
Ling
,

10
-+ 10---
8 -60
+ 100 -
.

↑
~ .

& 242
I

& Th
-
-
-
-
12 .
 &

-
-

~ -

Q) A certain medica on is administered at a constant = dose rate of 40 mg per

hour (mg/h). The clearance (Cl) of the drug from the body is known to beO
-
5
-

litres per hour (L/h). Calculate the concentra on of the drug at a steady state.
- -
-
-

Desp

= -
-
g

Q) You are aiming to achieve a steady-state concentra on of- 10 mg/L for a

par cular drug in a pa ent's bloodstream. The clearance (Cl) of the drug from
the body is known to be 2 litres per hour (L/h). Calculate the required dose rate
-
- - -
=
to achieve this steady-state concentra on.
-

D.
= CssXce
.

Dose rate other than IV:

-
-
-
-
s
LoadingS
dose
=>
-
Maintenance dose
=

Purpose- SSC
toAcheive To Maintain C

quickly
.

Formula

-= -+ yz
-
>
-

Governed by- t

20
Ce ,
-2
Q) A physician decides to prescribe a certain drug for a pa ent that has a
volume of distribu on> (Vd) of 50 litres (L) and a clearance (Cl) rate of 5 litres
-

per hour (L/h). The target plasma concentra on & (Cp) for therapeu c efficacy is
2 mg/L. If the drug is to be administered every S 8 hours, calculate the required
loading dose and the-
- - -

#
-

maintenance dose.

Xd = 50 MD = (P)x(exty2
LD = (P) X X d
2 = 5 8
= 2 X5 X
= 2 X 50
(4) = 2
80mg
=
100 Mg =

>
-
-
 How &where
Effectis produced
-
&
Ac on & Effect
Response
>
=>
.

-B.x -

Adv
t

Morphine 982021
Ach & I
westphall

↳
⑪
Circular
e
↓·
Eidinser

Josis
I wis
-
-
& Mi Est
⑪

Affinity & Efficacy

-
-
-
-

↓ ↳
-

- -
-

EgeActivit
·

Affinity -

-
-
-
 Examples

r
prazole &
O
Agonist ① * Aripil- -

-
--
② M
Buprenorphine
,
-

&

Agonist & = e HT =

Buspirone
Partie -- -
-
-

gonist >
II - &
- clonidine A

↳ 2
Note
&
&
Varenicline
- -

veve Asonis Doctor Smoking

=>
Cessation

-
-
> Nop
& B2D
-
R .

④ B-Carbolins
-

Affinity Efficacy ->

=

Agonist High High + I

=

Par al Agonist H 0 to + 1
>

Antagonist H
- O

Inverse Agonist H o to-1 (low)

=>

&

tagonist
-

Par al agonist + Full agonist:

attest

Aka- enerzie/Disfloss
Silent receptor:
-
-

-
-
Actuato

Example- parts
I
T
Dose-Response Curve (DRC):
-
-

I
No of Variables
(T)-
Necessity of log: -
-

Widervalu
Accom
-

set -
I
-

↑
O

la -
&

-
I ② igmoid
"

2020

&
.

=
-
-

O
it's 2 %!! !

O
ou

& D
=

-
-
--
- -
=>
100

required
to
produce Steffect
-

ODose of drug

> As

u
Potency & Efficacy:
-
-
-ine
-

Ov
O

0
0 .
Modified effects of 2 drugs:
Related points & Example
~
Permissive effect One drug , (4) Actions of Otherung

B Ex-
=
& prog.
~
-
-

*
↑ Groid : /Growth
-
- -
-

O
-
Addi ve effect
same ot

=
- -

-
olens > Analgesic Effect
↑ +
.

-
-

Summa on ~
-
Different A

HT& =
v -
-

Morphine + Aspirin
s
i -
& Cox
~
~
Synergism
Trimethoprim + Sulfamethoxazole
~ cotrimoxazole =

(1 = 5)
*
·

2
1 + 17
a
--
s
-

- e
Parkinsonsds <Potentiation te
I/

ni I -

Cardiol↳
a
3 -

· No role .

-
-

Le

(MLD(On
·

-
-

=
Antagonism

a1 + 1 (2
-
a) Chemical antagonism
-
=>
Heparin-
-
I
-
Protamine-
- An
facids
=

gastrictuise
-

Adru
&v C >
-
.

~
b) Physiological antagonism/ ↑
Histamine
functional At Bloody ↓ &
-
.

c) Pharmacological antagonism/ P :D Antagonism .

>
 COMP
Pharmacological antagonism: ↓ 1
- -
&
Reversible
-
-
- -
Irreversible
-
Non-Compe
-
-
-
- -
ve
Compe ve Compe ve antagonism
~
antagonism/ antagonism/
Ant
Equilibrium Alt
.

N61-EC .

-
-

Resemblance
with substrate
# Yes Yes "NO"
Binding at the Yes
-
Yes NO
ac ve site
-

-
-

Surmountable Do B
-

(A9O-=
⑫ 00
NO NO

Km (Michaelis Inc In C unchanged

Constant)
V max unchanged Dec . ~ Dec .
v
-
-
- -
-

APA
-

ency
Log DRC
#E cocy
. .

"

Menten const Y2
-1
Max
.
-

Michaelis of reaction
is
-- u6
E 1
-
rate
-

- -

" when 61w

Km--- conc .,
Affinite
-

-
- Substrate
-
- High >
-
lower I

-
> I

- "
-

~ low -hisher
Enzyme induc on- -
-

(100 + 200)
↳ (No - Enzymes.
-

Enzyme s mula on-

of Enzyme 1100 + 100)
A city
.

↳ (
-

·
 Examples

~
(O
S >
-

⑦ ③
-
-

Examples

J
La
⑳E
 ⑫ Allosteric
-
Activator

O O
C
-
-

Et

50 % of Recipients
>
- dose which kills

LD50
= >
-
-

Therapeu c index=
-

"

50 %:
ED50 Effective
2022 INET
-
-
-
>2" O
Wrong

400
TI -
-

100
=
4
-
T-
=(b) =
800 = 8O
B

&
&
we
S
e e
B

&
C

O ++
1227
10

- -
-
·newe After
readin

dinin
-

-
-

to
Unable
U Due
↓,
=
=
Drugs with Narrow therapeu c index:
-

-
ENIET) -
-
r
-
-
An epilep cs Phenytoin Valproate
,
, Carbamazepine
-
-

Cardiac drugs , Amiodarone

- Digoxin

Mood stabiliser
-

-
&
Lithium
-
-
.

Bronchodilator
-
-
theophylline (Zero-order WHEA).

Immune suppressants cyclosporine ,

facuolimus
=

An -cancer drugs Methotrexate , 5-fluorouracil

-

An -mito c agent
>
- colchicine
-

An -coagulant Warfarin .

-
-

An bio cs
#minoglycosides
hight I Tetracyclines
Chloramphenicol"
ch
-grey baby sens .

·
Penicillies Polymyxin-B
Cephalosporins Quinidine
.

=
Vancomycin
·
.

range
 &
Cellular receptors:
Class of receptor Examples
- Ligand-gated ion channels
-

-
·
Nicotinic .
R

ABA
8
I I

Anti 5HTB
-

>
-
.

metics -

-
-

-Enzyme-linked receptors:
-

EGF-
Suli"
"

PDGF
a) Receptor S T ,

tyrosine kinase >-

-

-
,

- -
-
-

b) Receptor &
serine kinase
-
>
- T4F-B
-

c) Membrane-bound Guanyl (ANP BNIND

Peptides
,

Natriuretic
- -

cyclase
-

↳
-
-

-Nuclear receptors: A

in-vit
↑ fina Actione

a) Steroid receptors >

-
&
Gluco
M
Sex Hormone
. C
,
.
< , =

-
-
-

-
.
stone
Thyroid
b) Non- Steroid receptors (T >It n)
-
-

-JAK-STAT O
e GH prolactic ·

-
-
-

drove Cytokines ,
,

Activator of&
- -
transcription -

-Toll-like receptor
-
-
microbial product ,

Heptahelicar/Serpentine R

GPCR: / Hetero
-

to
&
r
d GDP

W
Attache-
-

L
Chilsase
-
-

O
GPCR examples:

Gs Gi Gq
Sympathe c 42
B 2 ,
system
Parasympathe c M2 4 M1 , 3 5
,
,
system =

Dopamine D2 , 3 4
=
D1 1 5 ,

Histamine I
H2 # 3 , 4 ,

Serotonin 5HT 5H + 2
5 H T 416 , 7 1 ,
5

Adenosine
A2 A 1 , 3

Vasopressin
V2 VI

Others TSH Opioid Ang-II

=
Cannabinoid -
Eseas
Oxytocin
.
-

i ↑-
"
O =
&

it ↳ -

f ,

2 4
,
4

⑫
* M&
- -
hy
5HT1 I/hil ,

Vasopressiv
-

vz As
4q (42)
-

+
1 .
2
I

Adenosine
3-Low-ligand
-

hs
.

2 + -
=

S(3) A2 S

3]e hi
4
-
-

5 I 9;
Ay- I
,
-

s
-
 New Drug Development:

,
202

↓ !
>
-
>
-
-

2,

lab
S
NDA
/

Application
.

O
>
" 11 New drug
T ND -1) license
BLA-Biologica
O
-
--
=
New drug Applicative
Investigational
Application

Reporting
~

> Voluntary

&
-
.
-

Effec ve way of genera ng early signal- NDA

Before filler
N

at
T >
-

Fillch
-

ea
↑
P
S
#

Af
-

Phase-II 1
& >
-

Eb
-

>
-
of Human
100Mg (Y100th -
docel ,

Phase-0: Max -

Dose
Microdosing Studies
=
=>

Other name: ~
=> 10-15
Par cipants: Humans -
-

p / parameters.
Check
-

Purpose:
candidate
-
-
-

good
-

Advantage:
-
Accept
candidate
-
-
.

I bad -

Reject
 O
Phase-I Phase-II Phase-III Phase-IV

-confirmators
Other Name Human Pharmacology Therapeutic post marketsone
Exploratory. S/
-

&
- -

& Time trial/1st in Surveillance

.

required 1st in O Studies

=
- >

Human Studies -

st
I
.

Duration
-
- -

NOED
- -

1-2YV 2-3YV 3 5YU

-

Par cipants Volunteers Healthy Pt T Pt E PE T

-
-

↑t = Anticancer, ART / AY Experimental drus Exp drug Approvendung -

Number of
subjects =
Up to Upl00 Uplo 1000 Many thousands -
.

Type of Study
Open labelled R C Studies
Randomiseddie Open
- . .
-
-

Purpose of
Safety , ADR (Marel
Checks Efficacy
Contineffica
· ·
-

Study Indications
-
-

New
tolerability Dose change
·
.
-
-
·

-
-
-
·
- D
D -
I

Addi onal Report

Highest failure eriodic Safety Update
Move Money is -
a research
·
·

I
points
Center
Needed. IPSUR) 1/6+ =
-
-
rate- to
-
= 1 2y
- -
more difficult -
PSUR

/
-

Lan
- ·

Conduct. +

(vs
-

2020
202en
-

Janua
(20 , 27) (22 , 27)
 "CAT" 10-A
Choline >
- Ach +
+
Cholinergic system: /
* Acetyl -
choline
Ace + >l
7

(Ach) Transferase .

Ach Acetatecholine
=

Choline +

Esterase
.

-
-
-

vesicle
-
-

Co-A
samicol

-
⑦
&
-

&
-

CAT

"-
- --

Black
Spider
toxin
"

-
=
·x =
-
↑
"
&

toxin
Hemicholinum E
-v .

-
I

&
-
-
Release -
> Botulinum
-
-

-
-
-
-

1s
-
L

uptake
-

Cholin
-
&
-
-
Ch -
E
/X
-
-

&
-

Sop
&
Botulinum toxin interferes with
-
- &
Synaptobrevin
-

protein =

Botulinum toxin uses -educe Facial Wrinkle .

Hemifacial Spasm/
=>
-

·
strafis .

Botulinum toxin toxic dose (IV/IM)

"Ikg
-

-
-

Cholinesterase
>
True cholinesterase -
Pseudo cholinesterase
>
-

Aka
-
Specific . ChE'se Non Specific [h -
Ese. /
Butyryl
-

Ch E'se
.

Hydrolyse Ach
-

-
Quickly- Slowly
Hydrolyse
X ~
S
Butyrylcholine
 ⑪
-

Cholinergic receptor’s location & function:

Receptor Location & Function A D

M1 CNS- Cognition , Excitation learning, , S

Memory
=

Gastric glands- (gastric acid Sec.

M2
-
Heart- () rate
-

() (on devel

#Lot
M3 Smooth muscle >
-
"Cont"
-
-
II,

Bronchi
-

> B .
C

>
Cont
Intestine
-

Eye Sphindentcat-
No D
is
po
-
-
-

& Ciliary Muscle >

-
Accomodation

Glands- I
-
-
-

A S

Blood vessels- D /N
.
O Pathway)
-
-

NM=
NMJ-
=
Fontraction of Aes ~

NE
N Ganglia-
-
-
Transmi11i0n

Adrenal medulla- Adrenaline

-
-

-
-

E
O
pres I Post-C ,
 Cholinergic drugs
- directly
-
A) Cholinergic agonists
-
B) Anticholinesterases
Indirectly
-

↳
A) Cholinergic agonists -
-

&
Bethanechol
>
-
-
- Bladder Atory .

=
-
=

Carbachol
-
-
Miotic Asent

Pilocarpine -Miotic Agent

.

Headache
- =

(3rdlinedrug)d/t Growache
-

.
>
-
,

·
Glaucoma
Xerostomia
.

A
Methacholine
=>
DX of Bronchial Airway Hyper responsiveness.

C
& &
Cevimeline ~
Xerostomia
TIPML Es
-
-
-

Central Visual Acuty

disturbance Acting
Cholinergi
Inhibitors/Indirectly drugs.
B) Anticholinesterases/ A-ch-disuse
/ &

10
=

MOA: Choline ⑫ O
Irrey
>
Acetate +
Ach -

= Ch Elase
-

↑+

e
Reversible Anticholinesterases:

*
Physostigmine
#,
-
- -

soluble
- -
.
~
Antidote of Atropine poi
-
rido Myastheria
O

E
B Amine
- -
,
Cross BBB

Pyridostigmine Rot Myasthenia graxis .

&
Neostigmine ·

Reversal Asent for Neuromuscular Inde) V

-
-

Edrophonium Dy of M G
.
·

D s

&
Ensontest
AMS
pt Weakness
=X
.

-
2020
=
,

S
Edrophonium

/ &
p7 . Pt .
Worsens
↓
=

Improves
crisis .-
=>

↓I, Cholinergic
-

4
-
.
 howhither&fataldrugs
i29ty -

EX
=

Dr. xy Among -

Donepezil ④
-
-
Rivastigmine ⑫
--
&
Galantamine-
-

Enzyme inhibited Ach Else A Ch Else

AchElse
.
.

=
-

ukholier are

Mechanism of
N C comp .

N C
.

inhibition .

& ~
-
-

-
-

O
FDA approved A .
D A .
D
-
A-D

indication +
-
-

& Parkinson disease

dementia
=
.

Available routes Oral Oval oral

a
of administration -

&>
T D Patch .

.
-
-

↓ -
-
-

2021
=

↳
Myasthenia gravis treatment:
(PYridONed
-
-

E
(
1) Anticholinese
2) steroids. Azathioprine a
Berke Cyclosporine
,

3) Tamme Suppresive
4) Thymestory
.

&
-

Physostigmine -
Neostigmine -

Chemistry 3 Amine ↳ Amines

=

Oral absorption good Poor

.

& Crossing
BBB
-
X
Therapeutic use
-
-
 She given
Irreversible Anticholinesterases: -
-

Carbamates Carbary 1 , Propoxur

-
-

Organophosphates Insecticides- parathion Malathion , , Echothiophate

-
.

-
-

eduble *
-

= & O

Nerve gases- Soman, tabun

-
-
,
Sarin
=
-

a
As

All OPs are lipid soluble, except: -

-
Echothiophatewaterso =

Organophosphate poisoning:
Y
Clinical features:
B Secretions
-

constriction ,
.

· B .

-
-

· Ri
& -

>
-
= & ~MANS
Diarrhea
-

BELS
-

Urination
.

D
·

:
-

Diarrhea

· Missis in Pupil U-aviation

M- Miosis

/ Brady Cardial
·
~ Tashy .

B B spase
,
-
-

E-Emeris
L-Lacrimation
(M
Secretion
.

S -

Treatment: -
-

General measures Specific measures

- Remove clothes
-
-
1) Antidote- Atropine
-
- =
.

- Wash with soap and water

-
-
-

- Maintain airway 2) Adjunct treatment- Choline Esterase

reactivators
-
=>

Maintain BP, Control convulsions

-
-
fe
--

- Prolidoxime
Diazepar Diacety/monoxime
.

, -

=
 Arch
-
-
↑ -
-

Atropine Cholinesterase reactivators

-

-
-

Anti -
-

&
2mg/10min, given till full Pralidoxime, Diacetyl monoxime
(5)5BP

O
atropinization -
-

=
--
/
> 80
* H7HR
-

&
~ /specific
La * Mydriasis
, Axia
(HB Se
.

.
.

*
dry mouth
clear sounds
on
*
Auscultation
Cross BBB Cross BBB =>
↳ Ys .

Poi
Not effective in Not effective in O Carbamates
.
=>
-

#,
~

Muscleweeknesse
so
-
↑
"-
Per -
Started before Ageing
=>
Process .
-
-

"San"
-
-
-

- fast Aseing Process .

800
S
T
- Opioid
Causes of pinpoint pupil: -
poi

-
-

O -
OP ,

Hige
P .
-
Pontine -

pheedl Poi

e
⑧ Pinpoint Pupil
Muscarinic antagonists:
A
Pharmacological actions:
-
-
tropine
Bronchi · B .
D
=>

Hel .

Heart ① transient'
> (ACh > AHR
B > #Pr
-

M
Brady
S
-

.
-

> Tachy
-
-<
AR
>+
T- #2-
a
GIT smooth muscle Relax = (SPSS
.

- ·

A) Gastric Se
·

and

Bladder
= retention .

Eye Mydriasis
=
+
Cyclopegia" =
/Paralysis of Accomodation .

S
Increase body - at
temperature =>

Center elepothalamus
& temp Regulatory
.

-
-

a
&

=
Atropine effective antagonise:
/ Endogenom
C ExogenousIy
↓

Ach
> Y
COP) Administered
druas
Cholinergic

Atropine substitutes:
-
-

Drug Points
&
Ipratropium - E M
- Asthma
[L -

- Indicated
I
Tiotropium Rhinitis
↳ & perinned
-

/
# +,
& Rhinorrhoea
Mz
-

-
-
 Met + Dislimie-
-
-
-

Dicyclomine Antispasmodics

&
·
-

S
-

Isopropamide IBS()
-
.

Endisturbane/
-

Clidinium
problems Am
= :
↳ it
Cimetropium + 91(c)
1/

=
Dice

8
0
Solifenacin A= a O a
bladder
:
of veract -

S
Oxybutynin T

O
Flavoxate Bladder
&
-

Tolterodine to
by DAB
Agent Used
Trospium -- Only
=

&
&
Antimuscarinic
·

a a

Kidney
.
-

via
get's Eliminated
-

Troue -1 1/
- -

-
&
Cyclopentolate
-
>
-
.

·
Cyclopegia-predominant
Children-Behavioural-
AGN

O
-

Not reliable
Tropicamide > Cyclopegic-
- .

teste
Retractory Error
-
-

fundoscop
·
,

Med
A
Glycopyrrolate (Inhalational Fore)
=
potent # -
COPD
-
Antifac Axily hyperhidrosis
C CAP) A -

-
-
Hert P -

pre-Aesthetic Medication
Scopolamine -

Motion lickless (Prevent .

.

fa
TD atch .

motion >
- Scopolamine
+ Pyridoxins
<Morning
-

>
-
Doxylamine (iEB6)
- Rickes
& & Mountain > Acetazolamide
-

Post Auricular ameasque

-
-
.

region. =th 30
Mastoid

Induced Parkinson's
-
Benzhexol/Trihexyphenidyl
=>

Benztropine
- -
-

-
>
 Atropine poisoning:
of uncrow forest
t

↓
Clue: conception

Features Treatment

&
Body temperature Inc
-

-
.
General: Dark room
·
=

cold sponging
Mydriasis => Photophobia
.
·
-
-

-
-

-
Dry skin, Dry mouth
-
-
-

Physostigmine
-

Specific: .

Tachycardia
=

&
Disorientation Choice
=
-

Atropine Contraindications:
1) BPH

glauma
-

2) -
 ~> :
dr -

Adrenergic system:
↳ Horne : A dr

&
RE
#
-
-

-
L
-
& metyrosine
-- ⑫
S
=

DO A
=
-

L
-
O Methyl
-
-

102 -
(2020)
1,

I I
& Reserpine
-

(MAT) - ·
-
&
L
·
.

Uptake
& &>
-

-
- =
>
--

↑n
released
NA ---------------> Adr
is intensen
-

00
-
-

Reuptake of CA
↳ Uptake-1
O O
Uptake-2
Via Nov-Epinephrine transporter Monoamine transporter
(NET)
Sodium sa
-
-
- X
dependent
Uptake transport NA"
e
Adr
2022
Inhibited by
-
-
&
Cocaine , Desipramine
(A D)
-
.

Corticosterone
-
.

↳
uptoke
Ec Sympathomimetic
-
-

Metabolism of CA-
=

COMT
↳ MAO & E
metal transferre
-

) atechol or

not
=

Dxot Pheochromo Zoma

"" -
-
>
-
 B = 1 !

&
2

,
,

Adrenergic receptor’s location & function: 12 =1

PVSY

Receptor Subtype Location & Function

&
α1
=
Iris radial muscle- Mydriasis
-
>
- -
-

. Constriction ~
.

Blood vessels- ↓ =

Blood
@ cut Blood .,
. Mucoral

Id
/ permeability)
↓
Intestine smooth muscle- Relax
,

zepolarisch
HYPOP -
-

Sphincters- Cot
-

Gluconeogenesis
α Liver- & glycogenolesis ,
-

Vas deferens-" cost

--
= Ejaculation
=

α2
-
Presynaptic- () NE release
-

Blood vessels-
-
L
V . C

Platelets- & Pet Aggregation

.

Insulin secretion- & Insulin Sec .

β1 Heart- # Rate ,
Cond , cont -

JG cells-
=>
nin
.

(RAAS)
β2 Blood vessels- V· Dilatation
liver
-

@ Coronar Blood. I Kels

-
- ,
,

&
β
Bronchi- B Dilatation
.

Skeletal muscle- contracte

&
β3
=
Bo Detrusor muscle- Relaxation
-
-
-

& lipolysis -
.

Adipocytes-
- -
-
 =
(MBP A

&
=
h
yc + ,

Lin
<
8
= HBP
* B .

B2
.

D +

&
DBP D
S ,
>
<.
-

#
>
- (MSBD
FIR
Bi -

>
-
ADBP
X D
- -
-

P2 -

>
appier
-
-

&
(2) (P2)
& Insulin & glucagon ,

↳ L
Ellulose-
 -
Receptors sensitivity: Of
-
-

High Moderate Low

Adrenaline
-

⑬ -
Bi . & 22
4 ,

Nor-Adrenaline =>
④ 2 B, B2
-

-
-

F
↑

Isoprenaline B ,2 -
&, 22
=> -
-

wor

I
~

&
I

Phasic resence of Adr

2019-AIM)
- "
Effect of Adrenaline on BP
-
Vasomotor reversal of Dale
- -

-
-

Mittic I
-

- -

V
O↑
↑ ↓ -

④ ,

-
=>

v
-

Are &
-
↑ -
T

... &
=>
10
-
>
- - M ensitive
-

pro
-
-
BLOOD PRESSURE HEART RATE
⑬
= =

-O
2 B
.,
B22 ,
,
~

#(2)
SBP DBP MEAN -

DIRECT REFLEX NET ↑

Adrenaline
=
=>

IN + [1
, ↑
=
↑
>
-
↑
-

Nor-Adrenaline
-
↑ T ↑↑
⑪
>
-
↑
=
I -
=

Isoprenaline
&
&

=>
-
T Is ↓y ↓ ↑ ↑ TY

7
a ↑, f

i
I 6, L
-

a , bl
+
Adrenaline
=
- B

Therapeutic uses ADRs & C/I

Shock #Cerebral haemorrhage
·
Anaphylactic .

- -
-

18/0000 :
Cardiac Aest (
Arrhythmias

LoAnaesthetic
i
·

TOA
of
-
-
-
>

Inc
=

.
L,

O
·

S
o
C/I-
-
1) Pt receiving
-
Non-sel -
- -
-

--

HTN Angina -

2) -
-
,

:
- Or
2023 May ↑ Adr110 000

&
,

al
-
-

Anaphylactic shock: 10 , 000

1 : 1000 Or
-

- IV Adr
Route: 6)
- 1
O
000

&
11 ,

A IMAd -
Ratio:
S -

1 : 1000
0 .
/ML
Al
< 6 years 0 .
15 me 1) Im

6-12 years 0 .

3ml IX

Bolus
~
intusion
>12 years 0 5
-

Ml
A G
=
-

-
-
-

Drug Points
Noradrenaline ~ of shoice
asoprenor
given via /Dilution
=
↓, T
·

(BP
If extravasates/Given undiluted IV- Necrosis-
- - -
- -
-

S
Droxidopa
-
-
D- NE
/ d the
⑳ Neurogenic
A
Orthostaestensive
atomonic
-
-
 -

A
Dose-dependent actions of Dopamine

DoseS
(mcg/kg/min) Receptor Action
-
=

-
read blood
.
Low ~ of
=
0 5
2 .
2 =

=
-
&
Di =
MOVEGFR-&
-
-

(NUVice Output
↓
-
-
.

Moderate
-
-

2-10
=
O
B
I I

-
-
-
- rate , cold
,
-
.

High ~
L
= > 10 -
-,
V . C = (SBP (DBP
.

- => ( Bloody i -

Drug Points
Dopamine Use: A Decompensated
cute
FU

=2, D D2

>
,
Act on: , >
-

No When to stop/terminate Dopamine:

-
No action on: B2 ↓ I, ,

↳
"ET"
BBB crossing: E
-

-
Arrhythmic
-

.
↑ -
Tachycardia

Dobutamine 1st line of agent in Cardiogenic shock-

-
-
-
=

Selective , S
Agonist
DSE
-
-
Dobutamine Stress
-
-
-
Echocardiography
-Coronary BX
-
-

Fenoldopam
-
-
Use: H Sex red <Mpamen/EOD
-
-

Act on: D, L & 2

Not used for-

&,
-

>48 hours,
No action on: ,
tolerance
Hypotension
· .

· se
α1 agonists: L 1
-
-C
=

-
A V D -

>
-

Drug Points
↓,
Phenylephrine α1 stimulation:
-
-
C Conse
Liv

&
Uses: Mydriasis : C

* Nasal
decongestant
= dec
-
Midodrine
-
Use: Orthostatic Hypotension -

0000
-

Supine Hypertension
=

ADR:
E

So Nase decongestion
- Oxymetazoline, >
-
-
Use:

heremia
-

- Xylometazoline -

↓ Associated with rebound

-

d
Nas cleaner
Drop- =>
Long term use: Impaired
musociling

O
-
-

Used with great caution in =>

Pt
H+
-
- - -

α2 agonists: HANEE
Drug > Points
Clonidine
-

&
&
2022
O
-
Partial agonist at
#
Sudden stoppage- &
Uses:

SIn
Alcohol

gete
1) Withdrawal symptoms management =>

Opioids
Nicoline-

Patch
~ /I =

2) Menopausal symptoms TID

-
-

sa
-

ADRs: toma
Phenochromoly
.

s -
-

3) Diagnosis of =>
&
-Sedation
-Xerostromia 4) HTN
.

-
- -
-
 Drug Points
Apraclonidine
- topical >
-
glaucoma .

AD
&
Brimonidine
-
- >
- Brain depression
e rus"
>
α Methyl dopa
↑ - Pr
-
-
-
>

/ Carboxylase
de
“PERFECT” ↳B
-
A
E Enzyme Dopa
a
-
-

e R-releaseane
E-Eret
2
,
-

-c)
Guanfacine
-
-

+ AD HD

β agonists:
Drug Points
Isoprenaline Block i

At
↑

P light
=>
TR
.

Short acting & O

via DE, edose SABA-eena
β2 B2Aso
agonists -
> -
-

(SABA): 1
LABA
Salbutamol - + ab
Inhaler SABALABA
Agent
- -
-
-
-

-
↑

Terbutaline to be used as
to colytic
-
>
- -

Long acting β2 Nocturnal Asthma

-

agonists (LABA):
-
1

AOC
=
-

Salmeterol
-
-

COD
-
·

Formoterol
-
-
 Very Long acting
, 2) A
. M B
β2 agonists

See
(VLABA):
D
-Vilanterol
-
-

- =
Indacaterol

Mirabegron neO
2022

Retentention of
-
-

β3 agonist > - Relaxing Vi

-

-
-
Urine .

=>
J
Gladder
-

bladden => SOFT

active
Over
-
-
-
-

Drug Points
Indirectly acting Ex- =
Amphetamine "
IIT

sympathomimetics ·

Stimulant
-

-
-
- C
-
=

tachyxic -

-
Mixed acting A Ex- DEphedrine , Mephentermine
-

I
sympathomimetics ,
-

#
2023
/ -
durin
Anesthesia
"

-
-
-
-
-
α blockers:
Non-selective Selective
-
-
=
222 00 O
-
- -

Reversible Irreversible Oα1 blocker O

α2 blocker
Opt
-
-

“ADOPT”S" -
-
Mirtazapice
PhentolaminePhenoxybenzamine
-

&
-

Alfuzosin
A -

(antidep)
!
2
Doxa

P-PrazOsic
T Terazosie
-

2 = y .
c =
(BP
Osse Tamsulo
.
sie

Common points with α blockers:

-
↑E
S-Silodosin

&
2 22
1) BP
=
=>
Decreased .

#
,

>
- # -
~
App
-
-

take
2) Vasomotor phenomenon of Dale -
-

~
↳ =

-
-

3) Heart rate E
[
M

-
-
Pa ↑ NIC -
- -

O
(AR)
-MAD-T -

4) Renin
↳ & Menie
&
~ # hese
= >

In
-

-
-

Non-selective Points
α blockers
Phenoxybenzamine
-
-
- ↳ of Pheochromocytoma-3 before
(pre-Op)
=

> Phentolamine
P-Pheochromocytoma (R of BP)

Emergencies
,
da Cheese dition
Hypertrive
#
E
-

N - R Necrosis .

To-to Severe
LA -
LA EEfCt .

-
-
 Selective Points
α blockers
“ADOPT”
-
Alfuzosin Li used only for BH
R Doxazosin
-
-
x - LH A poptotic
-
-
Effect on
prostate
=
88
-

O
Prazosin DE
E
-

L, , + 60
pa
↓ -

Fasulay
-Terazosin
-
L, Apoptotic Effect on prostate ~ /

Iterat
-
-

-
/
Tamsulosin ~ used only for BPH

L
Datera
- -

Hypotensive Episodes
&
At <, Preferred- Who are -
-

-
-

Associated with - trissued .

Cataract Ax
-
- -

~
Silodosin
-
used only for BPH -
>
-

# ADA
=
Associated with Retrograde Ejaculation -
-
-

-L - RE

& ⑳ >
-

I
5-2-reductase
DHT
-

=
I'

BPH treatment:
Jo
α blockers
-
5 α reductase inhibitors
-

#, .
-
-

flooof
urine TO #Size of Prostate
Improve
>
-

*
To =

Improves Atehomponent
-

~
-
rent -
β blockers: "
I

Type of antagonism- comp

.

-
Non selective β blockers/ Cardio selective β blockers/
ORegen/B &Selective
-

15
+ -

92.

↳
-

↓,
-
/

Propranolol -
- -
Metoprolol
-
( MEENA)
-
-
·
-

pindolo -
-
ESMO10l

Timol ↑ lebivolol
=

tentolo
Sota -
A

Cebutolo
-

A
-
-

Advantages of
Cardio selective β blockers β blocker + Intrinsic -
&
-
-

sympathomimetic property
DM- don't mask h pog1
-
Lipid profile- good
-
- -

Lipid profile- gr Asthma- -

less troublesome
=

1I
Precipitating Bradycardia-
Raynaud's phenomenon
4 NO- Sudden stoppage-> No refound
-

= =
hypertexion
-
 A su f

-
-
#
escld
- -

- "
......
Lef pren10

ACE() Cefnsen
Pril =

> ARB Cetzsch-

Sartan
-

Red H refer
IEA
Statis
L Austratives
&

Prazoles
-
-
=> Protoum O Anffuse
Antiviral Antiptchotic
Vir
=

B2
=
:

= Aripi
· orazole
:
(
Brexi
 ·

3
gener
-
propert
-

Property Drugs
β blocker + Intrinsic C-celiprolol
>
&
COP

-
sympathomimetic property O-oxpresso
-

Asoist p-pindolol

β blocker + Membrane stabilising C-carvedilol

F
- -
-
=

activity
-
s
Local Aresticks tet
L-Labezalol
Acebutolol
-

X
I, A
<writent
-

hish
connoture ,
-

M- metoprolo
p-propranol
-I

Antiarrhythmis
>
-
>
--

"
β blocker +&
NO release property biolo = Decrease Insulin
Sensitivity
·
-
-

xide
Nitril
celiprolol
=
.

S
-
β blocker + α blocker caryedilol
Labeta10)
-
-

β blocker +&
-
-
Calcium channel blocking
- V
Carvedilol
property
-

β blocker + Anti-oxidant
=
- carvedilo . V
=

β blocker + K channel opener

E
=> Tilisilo

β blocker + K channel blocker -

Sotal"

=
β blocker + Don’t cross BBB Labetalo

&
·

s
&

trueis
-

Atmo)
-

celiprolol
abcains
↑

H
·

↑
Bis prolol repression
-

N2bi0l0(
-

=
-

Sotalol
=

-
 ↑
Therapeutic uses of β blockers
S >
-

Cardiac uses Non-cardiac uses

-
“Thyroid GAME”
Supe 0 A
Angiea I control
--
=> 11
-
↓ -

Propylthiouracil
↑

thyrotoxicosis
-

#F
:
-
-
>
- ↳ ex
-

HTN glaucoma
(timolo-topical
↳ =

Arrhythmic Withdraw synd

Alcohol
Antenexis
A
Acxiolytic Proprolo
-
-

rophy
-

↑. P-
M-Migrate
-
-

Cardiomyopathy
.

Hyper 06. temon

E Essential
-

Arth An /Aute
slacting
=
Esophages Variel.

β blockers ADRs:
& N
1) Asthma: B .
2) Heart: HARMCADR
=>
BLOCK
Escond > A- X
%
-

Heart failure

H
=

( - >
1017
-
-

3) Lipid profile: worsen .

Pe a
-

Ach (OP)
Low risk with- BSM
.

-
diuretics
thiazide
4) Erectile dysfunction:
-
-
-
#
I -
, -
-

5) Abrupt discontinuation - Reboud HE -

- - -

So
6) -
Sleep disturbances, Depression:
High risk:

Racabins
=

ste
.
 "In
β blockers Contraindications:
“ABCD”
A - Asthma
Phenomenon

Vera
Active
Reynands

Distalis
BeBradycardio e
,

like
Agents

CHF
(decompensated Hotel se
poglycemic
-

162 they will

De D Nun

β blockers poisoning, Antidote: glucagon

,
POISONING & ANTIDOTES:
A dotes .

ACETAMINOPHEN / paracetamol -Acetylcysteine

ASPIRIN & TCA
-- NHCO3
- -

OP COMPOUND Atropine
ANTI CHOLINERGIC (Atropine) Physostigmine
MALIGNANT HYPERTHERMIA Dantwolene
o
BENZODIAZEPINET
-
Flumazeni
ALCOHOL
-
- ipizole
-

BETA-BLOCKERS glucagon
METHOTREXATE folinic acid/Leucovorin/Citrovorum
factor

LOCAL ANESTHETICS /Bupivacaine toxicity-

= Lipid Emulien
OPIOID
E
-
Morphine Naloxone
HEPARIN
- Protamine
-

DABIGATRAN
>
-
I darcizumab
-

FACTOR Xa INHIBITORS
-
Andexanet-L
-

WARFARIN Vit-K ,
S
IRON OVERLOAD Desferroxamine .

C DOXORUBICIN-INDUCED CARDIOTOXICITY Des

-
Dexrazoxane
- - - -

CYANIDE Hydroxy cobalamine

=
.

DIGOXIN Digitied (Fabfragment)

-

SEROTONIN cyproheptadie
=

METHEMOGLOBINEMIA I Methylene blue .

-
Sudheer
Prudhyi

Ls
&

9553349878
-
-