Pharmacolology
Alims 2014.
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* PACLITAXEL is derived from ? genetic
Tacaves
Yew Trees.
Gene
Concentration
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CARRIER
ABSORPTION
pH of the
DRUG
(i) Acidec
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(ii) Basic
M/c Site of mionization ? STOMA
Mic site of Absorption ? Small
BIOPVAILABILITY:
(3) Anyphetanuice d
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unchanged avut of drug co
Systemic circulation
Depends on
(1) Amount of drug
(?) Frist pass Mete
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II.) DISTRIBUTION;
? Apparent Volume distribcition (Imagen
It is the total plasma
that is required for
TOTAL
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PLAS
total drug wi whole body
art total plauna Concarnation
UNIT OF VOLUME distribition ? LITR.
avd = D/C
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*D-Drug
*C-Concentr
? D: ?avdxc (specif
Rx ? Dialysin
* INFERENCE (?)
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(?) Irreversible binchi
a) organophospha
b) Carbamates.
C ? Cyclization
Q -> Hydrolysis
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D Aliphatic hydroxylation
Aromatie
D ?Deamination
(Allins.
PHASE I
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ToyPASO!
* CYP1A2 Lenclocus in particular
Family subfamily
* CYP286.
(pretabolise > 50% of dr
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I) PROTEASE INHIBITORS: (i)not only
(?) Enzyme inti
Max
RITONAVIR
II.) STAYTINS:
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?) (ALCIUM (HANNEL BLOCKERS
IV.) BENZODIAZEPINES
?) ESTROGEN/TESTOSTERONE
a.) 6 Mp
b) Methyldopa
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? SULFATION
a) Steroids
CYP3A4> CYBDb> CYP2C9 >
ADC
ABC.
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O.C.P
Failure
OCP Failure Caube also seen:
T) ANTIBIOTICS:
NORMAL
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Estrogen
Intabition of
Enterohepati
Circulation of
Enter Hepatri
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Estrogen.
Undulation
Soluble
Th
colon
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A
JRDE PLASMA (0)
Maintenance
Dase ? Rate
PLASINA Cond
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vd
RDG= D/vdx 0.
RDE DX 0.693
1/2
MAINTENANCE 0.693X
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DSC +
?200mg
100mg
7thao/20
180
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80mg H/2
160
andhon/20
bong
2
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3hm
15 110
bo
I)... As dose increases
1½ increases
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in Zero Ordo kucerin
I?) As dose increases
Clearance decreases.
(&HR)
RESPONSG
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50.
40-
30-
20-
10
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(ORC)
Efficacy)
? Dose
10 20 30 40 50
A (mg) B.
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? Potency.
SameEfficacy.
DRUG RECEPTOR INTERACTIONS;
THR 200/? F
A/HR/150/m² S
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31 = 70 H.R ?170 HR
No effec
50 HR OPPOS
HR? 40/min
g:
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GLUTAMATE
NMDA
AMPA
KAINATE
Gg :- NICOTINIC Receptors
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T?) G-PCR [ surpentine / 7 tretical]
[Metabotropic]
Two active Components
? GTPL
2
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? GDP &
POH
GTP (X
GTPase
?.
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GS
Adurylate Cyclare
?
1 Cyc AMP
?
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PKC
? Phospholipou
?
?PIP2
HIT
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* Random chemical Lining
LA
* DRUG LIBRARY
?
DRUG SCREENING
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?.) Rational Drug designing
(a) Structure Ligand
Based Boved
(i) Select the dis (HTN)
(ii) Study Pathophysw of
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RAASS FITN
(ii) Select a tangel (ACE)
(Fr) Determina Structure of targat C Cel
VACE
- 100,000 chemicals) (Dry
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Phase
JCP.C.S.E.Aguia
*. Committee for the purpo
of cxperiments in An
C.T [Humans)
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Make a protocol ? Submit to
T
Franker.cop Therapeuticonfimatory tract
wo of Ply)
? Replica of phase II i mere no
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Ra - Safety cup to 3000
Phare Efficacy Multicentri
? 1-5years
Eficacy of new drug is Compared t
In cave of Genericdrug
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?
Abbreviated New dre
*Centre for D
Bill?2009
2010
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?
* Alims
then
* Ghaziabad.
PHARMACO VIGILANCE
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pased med. colinges 42,
Hospitals
?
ADR
Report ADR Ea
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VIGIFLOW.
J.
[N.CC-PV]
Gro
1 Ipc build
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(N) health Volunteer
Samples Pk
P.D
PHASE ?:- [PharmaCoGpidemiology]
I) NCC.-P.Us (Ghazedabad [up]
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[Centre for drug
?.) CDSCO
?) IC-PV? International Centre for p
TV CARCT Central Drug Research &
Warfare
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TBM is not used in which drung:
? Drug & Lower Therapeuter Indu
NEET
"Therapeuti Index : (
?
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/ "Salty Bouga
Lithium
Theop
? Digoxin
Measure
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Potency,
Psy
Am
PHARMACO GENETICS PHARMACO GENOMI
Pharmacogenetics)
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* Effect of genes on
? Dose
drugs heves && Dose
?
Bring toxicity Receptors niy
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4)Fg. - CYP450 Polymorpture
* Cyp2519 Activation of clopidog
?
?
?
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• MI
?
• Astroke
Bleueming
PCarboxylation
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of Factor
?
Lidocarin
IT) PArgens polymorphing 12h/docaug
Particeprocess
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Coczt
2/
Cart
Cart
Cart
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RAR & TEYTY
[Malignau
Actieproces
Re: Daute
Daghashed
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P- Glycoprotein Inhibitors;
1.) Carinichie
2) Amiodarone
3) Verapamel (c)
4.) Cycledsporine
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5) Engthromycin
6) Itraconazole
ESSENTIAL DRUGS ?
a) Haloprid
b) Drafopam
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1) nopsture
First Ranker Leng Acti
(2) NK-10 Aprepitant
Aprepitant (2nd)
? Dronabind
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? C.BÐ?
Nabilone.
Corne Cells
Cove
(4) Metoclopramide Not only a D2 blocker
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[Damperidone
? Dexamethasone
* Parameter to be monitored in Cannabi
/ RIMONABANT
?
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Darr. Depression
(w)
Succedal
tendencies
(C) (Cu)
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CBIR
CB2R F
(C)
EB
4-hydroxy
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Cyclophosphamide
* Practure
?
Excreted
? Phospho
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? Mustar
(Actuje
Part)
4.
Cytoto
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B.) IFOSFAMIDE
?
Chloracetaldehyde
Neurotoxii/
?
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? GTCS
Ataxia
Coma.
?
ACROKEIN
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[Most Neurotoxic alkylating agent]
Doc:- Brow
* Temozolamide
S/E:: Pseudoprogression of Bre
TV MISCELLANEOUS DRUGS:
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* BUSULFAN:-
AML.
S/K ? Pulneoncory fibrosis
* BENDAMUSTINE:
use.- CLL
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No Cross resistance to other A..
S/E
NEPHROTOXIC
Tu
(C-cl
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Inactive
420
Picturepo
1.
Prevention
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Nad
* Preload & 1-2LN sakine
* Cisplatin+5%. D + Mannit
?
(Diveretie
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of chord
* Frisemidet cisplatin/X
Naurea
* Max < Vomiting
Must
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Pharmacokineties:.
Metabchum by Bleomycin hydray
Deficient
Lung
Slam -
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MITOMYCIN C:
MOA
? Toppisomerase D
?Free radical
A.A activity
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Toxic drung on Systemic
?.
TOPICAL
ANTHRACYCLINE groep
MOA:-
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Topoisomerase II
formation
Free Radical formation
?
Dependson
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Fe' atoms
Chelation
Defour aimin
S/E Cara
1
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Prece
Anti Folate Antica dru
METHOTREXATE
PEMETLEXED
* MOA DHFRE.
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Leucovorin +15 FU
(CH3)
*To 15 Fu Sensitivity
Morto Mtx:
DHFR
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dump
Enzyme
5 Fdump
T.SO
Compati
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14 T.mp
CH3?
Induction takes place
Gure Mutation
Ls Amplification
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=>
>
5 Fu
ODHFR
POSSIBLE MECHANISM OF RESISTANCE NCE : ?
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2
FUNCTION OF MAR PUMPS: Drug Effleve
USES OF MTX;
Neoplasti
I Non neop
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* Dox >
* Doc ? Choriocarcinoma *
* Ectopi
*TOsteosarcoma *.
* Graft
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• Ifoffamide
• Doxorubicin
*MULTIPLO
Cisplatin
* Leukemia (CNS-Intrathecal
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route)
Cutaneous Trell lymphoma
* Psori
srouracil
* Thymedire pre
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uses.
1.) Colorectal Cancer
Regimen = p Folive Acid
Folinic Acid
?.) Head and Neck Caucer.
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? 5 Fut as platin
Hypometaxation)
* Decetabine
Mon Demethylation
use Myelodysplasia (ONB-15)
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TII PURINE Analogues
I devrurs
Guanine
Hypoxanthing
6- Mercaptopurine
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6- Thisguamie
*ure: - Lenkerna
T
/
HGPRT
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G
?
* Sle:- Bone Marrow Suppression
Hepatotoxicity
I
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J
TI Intübitors
IRINOTECAN [Prodrug]
USE- Colorectal
Ca
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LIVER
S/E ? Cholinergic toxicity
CIT
?
Diarnhea
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+
SN-38
7
use
sle
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Acture nedaba
MICROTUBULES
?
Polymoriyation
?
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L-tubulije B-tubitur
?
9/ * CNS 4
1
CNSSY
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2 Phagocyt
PNS Axonal
MoA:-
* VINKA ALKALOIDS B tubulin
* TAXANES ? tubuhit
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* Ixabepmone Stabiliges M.T.
I Castoroil
SK-M/C) Hypersensitiv
Ti) Peripheral Neuropat
* DOCETAXEL
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Can Cause 20 netention
? Ixabepmone:
use: Breast Ca
? Intravenous ro
?
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In systemic Cor
woto Aspartate
Lymphocytes Othercells
use: * LEUKEMIA
* LYMPHOMA
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S/effects: * & protein Gynthesis
* ? Insulin Syvethesis Hyp
* Hyperlipidemia PANCR
SA.CF
* CF Jed
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* Hype ?
Hypersensitivity
He
? The
best dou
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Multiple myeloma (Best
TOS: / BORTEZOMIB+ LENALIDOMIDE &
5/6 :: * Thrombocytopenia
I Carrier of
(4) (IMMUNO TOXINS
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? Dearmcerin Difitox
?
15-2 1 Dephtheria toxit
? It2R.
=>
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Use:-
(Dacells.
* DASATINIB
* BOSUTINIB.
* PONATINIB.
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*CABOZANTINIB: Doc for medullary thyr
* REGORAFINIB :- • GIST.
? E.G.F.R (Her-1) 2T.KO
17.K
RO
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EGFR
(MAb)
CETUXIN
PANITU
Chemicals T.k
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*SORAFINIB DOC? H.C.C.
* PAZOPANIB ? Soft tissue Sarcoma TRAMACIRL
* SUNITINIB ?.GIST
SIDE EFFECTS: • panicreate Cancer.
use
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I) Delayed Wound healing Stopped
? HGFR T-KO:
* CRIZOTINIB use: NS Ca hung
? JGK T-KO
to Rcaxelotinib use. Myelofimosin
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? M.S
?TTP
?AIHA
M/C Side effect
INFUSION REACTIONS
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*
Medullary (F.
Medullary CA
resistant to
acture
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FL-17
Anti FL-17 Ab
* Secucinumab PSORIASIS
Anti GD2 ganghoside Ab
+
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* Dinutuximab / Highrise Neuroblo
* CHOLINERGICS.
a) Direct
b.) Indvrict
BBB
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Dont Gross
BBB
TOPICAL
(Ocular)
CNSals S/E CENTRAL
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No
we. Peripheral Nutral
S/E
* PILOCARPINE
uses. I) Glaucoma
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(Closed angle)
II) Xerostomia
?.) In Acute attack of glaucoma & closed augh
Doc:- I/v Acetazolamide
1
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Normal Iop
?
Topical PILOCARPINE
1) chronic glaucoma (Openangle)
* Pa Analogues
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(Reversible!
Tr
Tertiary armines
Quarter
* Physostigmine
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uses Glaucoma
(Closed
L? Doc Antihistaminie
(Mie)
Poisoning
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• Belladona
Poisoning (Banana)
* Donepezil, 2
* Revastigmine
& Gallantamine
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DOL
(ALZHEIMER'S)
to Taurine (Hepato tour)
ond NMDAG
Amermantie
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Oryano
Phosphate
* Pralidoxime 2
* Obidoxime
hat we ates * Drcutyl monoxing
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Carbamat
"ACH
breakdown
? {op Coube
ACHE
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Scarbamates.
Doc for
Alims
ATROPING
F (B2 Agonit)
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* Ipratropium
* Tiotropium Doc [Long
* Oxitropium
* Cemexlidium
5/6 :- Uurive Retention (worsen 1.
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HEART :-
? HR
? Conduction
* Force of Contraction
used in Rx of Brady arrhythm
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STRESS INCONTINENCE.
"Drugs:-
Doc
L' Agonist :- INE ? SNRT (DULOXETINE
?) 33. urge incontricufe
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AIPG 16.
Drugs.. MERABEGRON
B3Agonid:
TROSPIUM
Darifonacur
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? Golefenacin
24
No
CNS Side
effects
--- Content provided by FirstRanker.com ---
M
M2
M3
.
?
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• Fo
0
• To
* Rate initting Enzymes Ne is
a
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RECEPTORS GPERS/SB
2. receptors!
(Gi)
NE
NE
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? a? (Ga)
0
BLOOD VO
TB1 (?MLCK)
HEART
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? HR
?0.0
? Conduction
2) KIDNEY,
7/32
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?Contraction
HALCP
?EMLCK
?
kt channel
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BLOOD VESSELS
? Ramin 1.BP. FIRS
Utorees
C/I in Im route
a.) (nuscle Necrosis
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*.DResidopa (2014)
? prodreng of NE
? use: f Neurogane hypotension
* ISOPRENALINE:
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