PHARMACOLOGY CHANTING BY DR.

PARAS

-
 GENERAL PHARMACOLOGY
→ PHARMACOKINETICS = WHAT BODY DO TO A DRUG
→ PHARMA CODYNAMICS = WHAT DRUG DO TO A BODY

☆ PHARMACOKINETICS

A → ABSORPTION -
FROM ADMINISTRATION SITE TO BLOOD

D → DISTRIBUTION -
AMOUNT OF DRUG GOING TO TISSUE
M→ METABOLISM -
MAKE DRUG WATER SOLUBLE
E → EXCRETION -
COMING OUT IN URINE

A. ABSORPTION
→ MOVEMENT OF DRUG FROM SITE OF ADMINISTRATION TO BLOOD

→ ABSORPTION DEPEND 'S ON LIPID SOLUBILITY

↳ BIOAVAILABILITY = B- A
→ % OF GIVEN DOSE WHICH REACH SYSTEMIC
CIRCULATION

•
BIOAVAILABILITY ✗ 1-
1st PASS METABOLISM

•
B. A ✗ ABSORPTION

EXAMPLE -
1. V ROUTE HAVE 100% BIOAVAILABILITY
B. DISTRIBUTION

→ AMOUNT OF DRUG GOING TO THE TISSUE

↳ VOLUME OF DISTRIBUTION @ d) = AMOUNT GIVEN

PLASMA CON . OF DRUG

↳ LOADING DOSE @ D) = Vd ✗ TPC

↳ MAINTENANCE DOSECMD)= CLEARENCEX TPC

↳ Vd ✗ 1
PLASMA PROTEIN BINDING

↳ Vd ✗ LIPID SOLUBILITY

C. METABOLISM
→ MAKE DRUG WATER SOLUBLE

PHASE I [ BREKING]
'
PHASE 11 [ CONJUGATION]

MOLECULE ATTACH .TO DRUG LIKE

HYDROLYSIS
CYCLIZATION G- GLUCURONIDE
OXIDATION G- GLUTATHIONE
REDUCTION A AETXL
-

M
DE CYCLIZATION -

METHYL
 /
ENZYME INDUCING DRUGS ENZYME INHIBITING DRUG 'S

G → GRISEOFULVIN VIT → VALPROATE

p → PHENYTOIN K → KETOCONAZOLE
R → rifampicin can → ☐ me, ,☐µe
S → SMOKING CAUSE -9 CIPROFLOXACIN
CELL → CARBAMAZEPINE ENZYME → ERYTHROMYCIN
PHONE → PHEW BARBITONE INHIBITION → ISONIAZID

D. EXCRETION
→ WATER SOLUBLE DRUG 'S ARE EXCRETED
→ LIPID SOLUBLE ARE REABSORBED

↳ ORDER OF KINETICS

1ˢᵗ ORDER ZERO ORDER

→ CONSTANT FRACTION IS REMOVED → CONSTANT AMOUNT IS REMOVED

EXAMPLE = 20
EXAMPLE =
5040 too → 80 → Go → 40 → 20 → ZERO

100 ZERO
↓ W
WARFARIN
-

so A- ALCOHOL / ASPIRIN
↓ T THEOPHYLLINE
-

25 T TOLBUTAMIDE
-

↓ POWER PHENYTOIN-

12.5
☆ PHARMACO DYNAMICS = DRUG TO BODY

↳ ENZYME INHIBITION

km Vmax
↑ SAME
COMPETITIVE
NON -
COMPETITIVE SAME ↓

RECEPTOR

CDROG)
↑
§ ↑
ACTION

AFF I. A
.

→
AFFINITY -
ABILITY OF DRUG TO BIND TO A
RECEPTOR

→ INTRINSIC ACTIVITY ABILTY TO PRODUCE ACTION

-

AFTER BINDING TO RECEPTOR

→ ON THE BASIS OF INTRINSIC ACTIVITY

WE HAVE
↳ AGONIST
↳ ANTAGONIST
☆ DOSE RESPONSE CURVE

§
POTENCY = A>B> C
EFFICACY = c > A) B

☆ DRUGS THAT ARE METABOLIZED BY ACETYLATION

S -
SULPHONAMIDE
H -
HYDRALIZINE ADVERSE EFFECT → SLE
1- ISONIAZID
p -

PROCAINAMIDE

☆ CLINICAL TRIALS

→ PHASE I -

DONE IN HEALTHY PEOPLE TO

KNOW MAX TOLERANCE OF DRUG

→ PHASE 2 -

DONE IN 20-200 Pt EFFICACY

SAFTEY
→ PHASE 3 DONE IN
-
5000 Pt
↳ NEW DRUG COMPARED WITH OLD = STANDARD DRUG CONTROL L

→PHASE 4- POST MARKETING TRIAL

↳ DONE TO CHECK RARE / LONG TERM SIDE EFFECT
☆ DRUG SAFTEY

↳ THERAPEUTIC INDEX = LETHAL DOSE

EFFECTIVE DOSE

↳ NARROW 7. I → UNSAFE DRUG -

NEED → TDM

↳ BROAD 7. I → SAFE DRUG

 ANS
" """ " "" "" " " " """ "

/
"""" "
CHOLINERGIC

NEUROTRANSMITTER
→ MAJOR

Ach -
NOR -
ADRENALINE

→ NERVE FIBER ORIGINATE

FROM CRANIO SACRAL Region THORACO LUMBER REGION
-

MIOSIS EYE MYDRIASIS

BRONCHO CONSTRICTION BRONCHUS BRONCHO DILATION

C0qBPgnR↓ HEART 6GBP MR ↑,

DIARRHOEA GIT CONSTIPATION

↑ FLOW BLADDER ↓ FLOW
ERECTION PENIS EJACULATION

↑ SECRETION GLAND ↓ SECREATION

MI -

GIT ✗I _

BLOOD VESSEL =VC

M2 -

HEART EYE = DILATION

M3 -
ALL URETHRA = CONCTR/ CTION
BRAIN ✗ 2- 21
My
-

OPPOSITE TO

Ms
-

BRAIN PI - HEART -

↑
C0qBP=VC
P2 - LUNGS -

B. D
BLOOD VESSEL -
v. D

B3 - URINARY BLADDER
- RELAX BLADDER
☆ CHOLINERGIC DRUGS

A DIRECTLY ACTING

↳ PILOCARPINE Rx OF -

ACG -

M3
↳ METRA CHOLINE ACT -
ON MYOCARDIUM
-
M3

B. INDIRECTLY ACTING
MOA -

Ach ESTERASE -0
\

I LIPID SOLUBLE
→ PHYSOSTIGMINE
DOC -

ATROPINE POISONING

II WATER SOLUBLE

→ NEOS-119 MINE RX MYASTHENIA GRAVIS

→ PYRIDOSTIGMINE
→ EDROPHONIVM DX MYATHENIA GRAVIS [Tension TEST ]

IMP . ATROPINE / DHATURA / BELLADONNA POISONING

↳ Doc -
PHYSOSTIGMINE
ORGANOPHOSPHATE & CARBAMATE & EARLY MUSHROOM
↳ Doc ATROPINE
-
Poisoning
ORGANOPHOSPHATE ALONE
↳ DOC -
ATROPINE , OXIME
☆ ANTI CHOLINERGIC DRUG

→ ACCORDING TO THE EFFECT 'S

1. STOMACH
MI
-
BLOCKER PIRENZEPINE
-
USED FOR PEPTIC ULER TELENZEPINE

2. HEART
-
M2 BLOCKER
-

ATROPINE
-

↑nR

3. BRONCHUS
-
M3 BLOCKER
-

IPRATROPIUM USED IN BRONCHIAL ASTHMA

,
-

TIOTROPIUM COPD

4. BLADDER
-
M3 BLOCKER
-

SOLIFENACIN USED IN OVER ACTVE

-

DARIFENACIN BLADDER
-

OXYBUTYNIN

5. EYE
-

M3 BLOCKER ACTION -
MYDRIASIS
ATROPINE CHILDREN CYCLOPLEGIA
-
-

-
TROPICAMIDE - ADULT
☆ SYMPATHETIC NERVOUS SYSTEM

21 BI
BLOOD VESSEL - VC HEART -
ABP co = V. C
,
EYE -
MYDRIASIS KIDNEY -
SECRETES RENIN
PROSTATIC URETHRA - ↓ FLOW B2
LUNGS -
BRONCHO DILATION
✗2 GIT ↓ FUNCTION
-

ACT AS BREK ON 21 BLADDER ↓ FUNCTION

-

BLOOD VESSEL -
V. D

B3
URINARY BLADDER -
↓ FUNCTION

☆ ADRENERGIC DRUGS

I DOPAMINE [STIMULATE ✗
In Big Di ]
→ Doc
-

SHOCK WITH OLIGURIA

MOA -21 -

VC To Rx SHOCK
DI -
VD IN KIDNEY To Rx OLIGUR / D-

II NOR -

ADRENALINE
→ USED IN SHOCK

HI ADRENALINE
→ DOC -
ANAPHYLACTIC SHOCK & CARDIAC ARREST
→ IN ANAPHYLACTIC SHOCK
181000 -
1. M ROUTE > 1810,000 -
1. v ROUTE
 → IN CARDIAC ARREST
1 :
log 000 -
1. v ROUTE

☆ ANTI ADRENERGIC DRUG

I

I. NON SELECTIVE ✗ BLOCKERS

-

→
PHENOXYBENZAMINE DOC - -

PHEOCHROMOCYTOMA
→ PNENTOLAMINE DOC -
-
CHEESE Rxn

II SELECTIVE 21 BLOCKERS

→ PRAZOSIN Doc B.PH -1 MTN

'

→ TERAZOSIN
→
DOXAZOSIN 5. E- POSTURAL HXPOTENTION

III SELECTIVE ✗ 1A BLOCKERS

BETTER THAN ✗ I ② BE IT DO NOT CAUSE

"

POSTURAL HYPOTENSION

→
TAMSULOSIN
SILODOSIN ] BPH

II SELECTIVE Pi BLOCKERS
N -
NEBIVOLOL ,
NADOLOL → LONGEST ACTING B- BLOCKER
B- BETAXOLOL BISPROLOL
,
E- ESMOLOL → SHORTEST ACTING B- BLOCKER
I B- BLOCKERS THAT ARE C. I 1N REENAL FAILURE

A- ATENOLOL
N -
NADOLOL
S -
SOTA LOL

☆ VASOMOTOR REVERSAL OF DALE

→ ADRENALINE -14-0 = ↓ BP
 CVS
☆ ACUTE CHF

1- DIURETICS -
LOOP DIURETICS
2. / NOT ROPES -
DOPAMINE
ISOPRENALINE STIMULATE B. a RECEPTOR
DOBUTAMINE

C.IINREENAL FAILURE DIGOXIN TOXICITY M✗→ LIGNOCAINE

CIIN LIVER FAILURE DIGITOXIN DIGI BIND

☆ CHRONIC CHF

1. DIURETICS -
LOOP DIURETICS
2. VENO DILATOR -
NITRATES & PRE LOAD
3. ARTERIAL DILATOR -
HYDRALAZINE ↓ AFTER LOAD
4. MIXED DILATOR -
ACE INHIBITOR SODIUM NITRO PRUSS / DE
g

☆ HYPERTENSION

1. DIURETICS
-
DOC -
THIAZIDE

2. VASODILATOR
A. RELEASE NITRIC OXIDE
→ NITROPRUSIDE
→ HYDRALAZINE 5. E. → SLE
 B. POTASSIUM CHANNEL OPENER 9s
MINOXIDIL
☐
IAZOXIDE
HYDRALAZINE

C. CALCIUM CHANNEL BLOCKER

VERAPAMIL ACT ON BOTH HEART & BLOOD VESSEL
D. ILTIAZEM
NIMODIPINE] ACT ON ONLY BLOOD VESSEL

↳ INDICATED IN SAM

3- SYMPATHETIC BLOCKER

CLONIDINE
METHYL -
DOPA

4. RAAS INHIBITORS

A. ACE INHIBITORS

CAPTOPRIL C. I ORTHOSTATIC HYPOTENSION

LISINOPRIL PREGNANCY

B RENIN INHIBITORS C. ARB [ ANGIOTENSIN RECEPTOR ⊖]

ENALKIREN
-
TEL MI SARTAN
ALIS KIREN → LOSARTAN
REMI KIREN
 •
1st LINE DRUG IN HTN
ACE INHIBITOR
CCB
DIURETICS

•
DOC FOR HTN -
THIAZIDE
•
DOC FOR HTN UN PREGNANCY LABETALOL -

•
DOC FOR HTN EMERGENCY NICARDIPINE
-

☆ ANGINA

1. NITRATES
→ GTN / NTG DOC -
ACUTE ANGINA
→ ISOSORBIDE DI NITRATE ROUTE SUBLINGUAL -

→ ISOSORBIDE MONO NITRATE

→ PENTA ERYTHRITOL TETRA NITRATE LONGEST ACTING -

→
AMYL NITRATE SHORT ACTING
-

2. cat CHANNEL BLOCKER

VERAPAMIL
DILTIAZEM

3. B- BLOCKER
C. I IN VARIANT ANGINA

4. K -
CHANNEL OPENER
NICORANDIL
-
 NEW DRUG IN THE Rx OF ANGINA

IVABRADINE
FASUDIL -
Rho KINASE ⊖

☆ ARRHYTHMIAS -

VAUGHAN WILLIAM 'S CLASSIFICATION

-1
CLASS 1 -
Na CHANNEL BLOCKER
CLASS 2 -

B BLOCKER
CLASS 3 -

k -1 CHANNEL BLOCKER
CLASSY -
Cast CHANNEL BLOCKER
CLASS 5 -
OTHERS

CLASS 1
↳ NA -
QUINIDINE
-
PROCAINAMIDE

↳ 1B -
PHENYTOIN
LIGNOCAINE
TOCAINIDE

↳ 1C -

FLECAINIDE
↳ Doc WPWSYYNDROME
-

•
DOC FOR AV BLOCK & BRADYCARDIA -
ATROPINE
•
DOC FOR TORSADE'S & PROLONG 0T INTERVAL
-

MAGNESIUM
•
DOC FOR PSVT ADENOSINE
-
 DYSLIPIDEMIA

I. STATINS

MOA
-
HMG CoA REDUCTASE -0 = ↓ LDL
DRUGS -
ATORVASTATIN
ROSUVASTAT / N - LONGEST ACTING
SIMVASTATIN

2 FIB RATES
→ & TRIGLYCERIDES

3 BABA BILE ACID BINDING

-

AGENT 'S
→ CHOLESTYRAMINE

4 NIACIN ( VITAMIN -

BD
→ ↑ HDL CHOLESTEROL
 AUTO colds

1. HIS -11 MINE

A. 1ˢᵗ GENERATION ANTI -

HISTAMINIC S
→ CAN CROSS BBB
Rx -
PROMETNAZINE

B. 2nd GENERATION ANTI -

HISTAMINIC S
-
CAN CROSS
NOT BBB
Rx -
TERFENADINE
ASTEMIZOLE
LEVOCITIRIZINE LORATADINE
g
ÉETIRI ZINE

2. 5- HT RECEPTOR [ SEROTONIN ]

A. 5TH -11 a RECEPTOR AGONIST

Rx -
BUSPRION
USE -

FOR ANXIETY

B. SHT IB/ ID RECEPTOR AGONIST

Rx -

TRIP TAN 'S

Doc -

FOR ACUTE SEVERE MIGRAINE

C SH -12 RECEPTOR ANTAGONIST

RX -
CLOZAPINE
USE -

ANT PSYCHOTIC
-
D. SHT} RECEPTOR ANTAGONIST
RX -
ON DAN SETRON
USE -
DOC FOR CHEMOTHERAPY INDUCED VOMITING (< 24h5

3. NSAID 's

A. ASPIRIN
→ LOW DOSE IS USED IN Rx OF MI & STROKE
C. I = GOUT -
CAN CAUSE HYPER URKEM / A

B PRM
→ HAS ONLY ANTIPYRETIC AND ANALGESIC ACTIVITY

☆ GOUT

A. ACUTE GOUT
AIM -
↓ PAIN & INF .

DOC -

NSAIDS EXCEPT ASPIRIN g Pem

↳ COLCHICINE (MOST EFFECTIVE BUT NOT Doc]
MOA -0 MIGRATION OF GRANULOCYTE INTO JOINTS
5. E- MYOPATHY & DIARRHOEA

B. CHRONIC GOUT
Aim -

↓ URIC ACID

DOC -
ALLOPURINOL
MOA -

③ XANTHINE OXIDASE WHICH

& CONVERSION OF XANTHINE TO URIC ACID
 DIURETCS

1. OSMOTIC DIURETICS

ACT ON -

ANY PART OF NEPHRON

EXAMPLE -
MANNITOL
USES -
CEREBRAL EDEMA BUT C. I PULMONARY EDEMA -

ACUTE CONGESTIVE GLAUCOMA

2. CARBONIC ANHYDRASE INHIBITOR

ACT ON -
PCT
EXAMPLE -
BRINZOLAMIDE Rx ACG
ACETAZOLAMIDERX MOUNTAIN SICKNESS
r DORZOLAMIDE RXACG
MOA -
Nat & Hlog GOES OUT IN URINE

3. LOOP DIURETICS

MOA -

INHIBIT Na -
k -
2cL PUMP
EXAMPLE -
BUMETANIDE -
MOST POTENT
FUROSEMIDE
TORSEMID E- LONGEST ACTING

4. THIAZIDE -
Cat SPARING -
USED IN REENALSTONEPT
.

ACT ON
-
DCT

MOA -
INHIBIT Na -
I Pump
DOC
-
NEPHAOGENIC D. I
5. kt SPARING DIURETICS

↓ &
ENac BLOCKER ALDOSTERONE RECEPTOR -0
→ A- MILO RIDE → SPIRONOLACTONE
→ TRIAMTERENE → EPLERENONE
 ANTI -
CANCER DRUG
* DRUGS USED IN CML
Doc
IMATINIB -

NILOTINIB
DASATINIB

☆ DRUG USED IN GIST

SUNITINIB
IMATINIB
REGORAFENIB

☆ DRUG USED IN LUNG CANCER

ERLOTINIB
CERTINIB
GEFTINIB

☆ DRUGS USED IN REENA [ CELL CARCINOMA

PAZOPANIB
AXITINIB
SORAFENIB DOC -
HCC
S.VN/T1N1B
 HEMATOLOGY
I. DRUG AFFECTING BLOOD FLOW

☆ 1-✗ A2 -0 -
ASPIRIN
☆ ADP ② -

CLOPIDOGREL

☆ ANTI FIBRIN / ANTICOAGULANT

↳ A. VITK ANTAGONIST -
WARFARIN
MONITORING DONE BY -
PT/ INR

C. I -
IN PREGNANCY
RX OF WARFARIN TOXICITY
↳ v17.15 IF BLEEDING
-
HAS NOT STARTED
↳ FFP IF BLEEDING
-
IS ALREADY THERE

↳ B. INDIRECT FACTOR 11A INHIBITOR

↳ UN FRACTIONATED HEPARIN
↳ LMWH

→ HEPARIN IN ANTICOAGULANT OF CHOICE IN PREG .

→ MONITORING OF HEPARIN DONE BY a PTT

→ ANTIDOTE PROTAMINE SULPHATE
-

2. DRUGS AFFECTING CELL 'S OF BLOOD

* RBC ↑ -
DARBEPOETIN
EPOETIN
☆ WBC ↑ -
FILGRASTIN
SARGRAMOSTIN

☆ PLATE LEA - 1. V OPRELVEKIN

ORAL -
ELTRAMBOPAG
 GIT
☆ PEPTIC ULCER DISEASE

1. MI ②
↳ PIRENZEPINE

2. Ha -0
↳ CIMENTIDINE
↳ RANT / DINE

3. PROTON PUMP INHIBITOR

PANTOPRAZOLE
Doc -
PEPTIC ULCER DISEASE
LANSOPRAZOLE GERD
◦ ZES
MEPRAZOZE
RABEPRAZOLE
ESOMERRAZOLE

4. ANTI PYLORI
H .

TRIPLE THERAPY DRUG [ PPI -12 ANTI -

MICROBIAL]

↳ GLARITNROMYUN
↳ AMOXICILLIN
↳ PPI
☆ ANTI
-

EMETIC DRUGS

→ DOC FOR MOTION SICKNESS -

HYOSCINE

→ DOC FOR MORNING SICKNESS -

DOXXLAMINE
[ Hi -0]

→ DOC FOR MOUNTAIN SICKNESS -

ACETAZOLAMIDE

→ DOC CHEMOTHERAPY INDUCED

FOR VOMITING -

ONDANSENTRON ESH -13-0]

☆ IBD

A. ULCERATIVE COLITIS

→ SULFASALAZINE
→ OSALAZINE
→ MESALAMINE

B. CROHN 'S DISEASE

→
Doc -
STEROID
→ IF RESISTANT To STEROID
CERTOLIZUMAB TNF ✗ ②
&
ADAUZUMAB c. I = TB
Hep -
B
GOLIMUMAB
ENTANCRCEP
 CNS
☆ ANTI -
EPILEPTIC DRUG .

MOA
-
↑ GABA
& GLUTAMATE
can & NAH CHANNEL BLOCKING

↳ DRUG THAT RELEASE GABA

GABAPENTIN
PREGABALIN

↳ DRUG THAT INHIBIT REUPTAKE OF GABA

TIAGABINE

↳ DRUG THAT ACT ON GABA RECEPTOR

-
BARBITURATES -
PHENO BARBITONE
-
BENZODIAZEPINES -
DIAZEPAM
ALPRAZOLAM
LORAZEPAM

Ad OF BENZODIAZEPINES -
FLUMAZENIL

↳ DRUG & ACTION OF GLUTAMATE

-
AMPA -0 -

PERAMPANEL
-
NMDA -0 -
FELBAMATE
↳ Call CHANNEL BLOCKER
-
ETHOSUXIMIDE DOC IN ABSENCE SEIZURE
< 2 YRS AGE
"
↳ Na CHANNEL BLOCKER
-
PHENYTOIN
-

CARBAMAZEPINE

↳ VALPROATE

DOC -

GTCS
ABSENCE SEIZURES 727 RS AGE

MYOCLONIC SEIZURES
ATONIC SEIZURES

5. E- HEPATOTOXICITY
PANCREATITIS
PCOD

☆ BIPOLAR DISORDER

-
DOC → LITHIUM
-
DOC IN PREGNANCY → ATYPICAL ANTIPSYCHOTICS

☆ OPIOIDS ANTAGONIST
→ NALOXONE SHORT ACTING
-
-
1. V -
DOC FOR ACUTE Cows
.

→ NALTREXONE LON ACTING

-
- ORAL
* ANTI OBESITY DRUGS

LORCA SERINE
ORLISTAT INTESTINAL
-
LIPASE ②
SIBUTRAMINE
TOPIRAMATE

☆ DRUG USED FOR SMOKING

VARENIC / LINE -
DOC FOR SMOKING CESSATION
NICOTINE

☆ ANTI - ALCOHOL DRUGS

NOALTREXONE
NDANSETRON
TOPIRAMATE
ACAMPROSATE

☆ ERECTILE DYSFUNCTION

PDE -0 -
SILDENAFIL DOC

TADALAFIL