FARMAKOLOGI

SS0

SISTEM
ADRENERGIK

Fathiyah Safithri

Laboratorium Farmakologi
Fakultas
Kedokteran
Univ. Muhammadiyah
Malang
2012
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Organisasi Divisi
Simpatis

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Neuron
Adrenergik
Perifer

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Sintesa Katekolamin

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TRANSMIS
I
SINYAL

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Release Norepineprine

aksi potensial pada membran saraf depolarisasi kanal ion Na

terbuka kanal Ca terbuka ion calsium masuk ke dalam
neuron
Peningkatan ion Ca intrasel vesicle kontak dengan membran
saraf release NE secara eksositosis . Diduga release
melibatkan mekanisme kontraktil dari sitoskeleton dan protein
tubulin.

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NEUROTRANSMISI ADRENERGIK

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Metabolit
e
sirkulasi

NT

(-)

Uptake 1

NT

RESEPTOR PRE SINAP

Uptake 2
R RESEPTOR POST SINAP

varicosities

Peningkatan second messenger

Pembukaan kanal ion
Kaskade biokimia
Respon farmakologi

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Feedback control
Of
noradrenaline
release
NE release involves
Ca2+ influx
2R activation
inhibit Adenylat
cyclase cAMP
Ca2+ influx
Uptake 1 inhibitors:
Antidepressants,
Cocaine,
Amphetamine
Uptake 2 inhibitor:
normetanephrine
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Metabolism of noradrenaline

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Degradation of catecholamines

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DISTRIBUSI RESEPTOR SIMPATIS

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Distribusi
Adrenoreseptor

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Classification of adrenoceptors
1896 Oliver and Schafer-adrenal extracts increase BP
1913 Dale adrenaline alone produced both vasodilation or
vasoconstriction
In combination with ergot derivative (
antagonist), adrenaline produced a decrease in BP
(2-mediated)
1948 Ahlquist- postulated and
based on
agonist potency:
Alpha: A>NA>>isoprenaline=isoproterenol
Beta: Iso>A>NA

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Adrenergic Receptor Family

A B D
C

A B

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Alquist

Classic
Pharmacology

Molecular
Pharmacolgy

RESEPTOR UNTUK NEROTRANSMITER ADRENERGIK

BERDASARKAN JENIS ;
alpha adrenergik reseptor
alpha 1, alpha 2 dan alpha 3
beta adrenergik reseptor
beta 1, beta 2 dan
beta 3

MENGAPA DISEBUT SEBAGAI ALPHA ATAU BETA

Reseptor yang berespon pada saraf simpatis dengan

urutan potensi (kekuatan efek) dimana NE > EPI
>D>
isoproterenol dinamakan sebagai alpha
receptors.
Sedang reseptor yang berespon dengan urutan potensi
dimana isoproterenol > EPI > NE >D dinamakan sebagai
beta receptors.

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Relative Selectivity
of Adrenoceptor
Agonists.

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Adr-R Subtypes

Heart
(increase HR and
contractility)

Smooth Muscle

(relaxation of smooth muscle

in lung, uterus, blood vessels)

3
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Adipose Tissue
(stimulation of lipolysis)

MEKANISME SINYAL TRANSDUKSI RESEPTOR -1 ADRENERGIK

ATP
G-protein adenyllate siklase
NOR ADRE
EPINEPRNE
DOPAMI
N

cAMP

+ reseptor

IP3
G-protein Pospolipase pospolipid

Ca++
DAG

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MEK. SINYAL TRANSDUKSI RESEPTOR

ADRENERGIK

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& -2

OBAT-OBAT
YANG
BEKERJA
PADA
SISTEM
ADRENERGIK

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tyrosine

Phenylalanine

Vesicle
Tyrosin hydroksilase

Alpha methyl
p Tyrosine

Dopa
Dopa decarboksilase

Carbidopa

Dopamine

Reserpine

Dopamine hydroksilae
Norepineprine
Vesicle

mitokondria

Metabolit
e difusi

Norepineprine
celah sinap

exocytosis
Carrier mediated
Uptake

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disulfiram

Sintesa dan
penyimpanan
Norepineprine
pada
saraf simpatis
periper

tyrosine
Vesicle

Release , uptake dan

metabolisme
Norepineprine pada
Saraf simpatis periper

Metabolit
e difusi

Amphetamine
iproniazid

Mitokondria
Mono amine
oksidase

(-)
Auto reseptor alpha 2

Carrier mediated
Uptake 1

bloker

Cocain

exocytosis
difusi
Uptake 2

cortico
steroid

beta adrenergik agonist ephedrine

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yohimbine

APLIKASI KLINIS
OBAT YG BEKERJA PD
SISTEM
ADRENERGIK
PROSES
APLIKASI
Sintesa
Storag
e
Releas
e
Inaktivasi
(Uptake)
Inaktivasi
(Metab)

OBAT
L-DOPA
Reserpi
n
Guanethid
in
Amfetam
in
Desipram

Parkinson
Anti
Hipertensi
Anti
Hipertensi
CNS stimulan (drug
abuse)
Antidepress

in
Kortikostero
id
Moclobemi
de

an
Bronkodilatasi
Asma
Antidepress
an

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POTENSI OBAT PADA RESEPTOR ADRENERGIK

Potency
++++(+)
++++
+++
++
++
+

AGONIST
DEXMEDETOMIDIN
E CLONIDINE
NOREPINEPRINE
EPINEPRINE
DOPAMINE
ISOPROTERENOL

ANTAGONIST
ATIPAMEZOL
E YOHIMBINE
PENTHOLAMINE
PHENOXYBENZAMINE
TOLAZOLINE
LABETALOL

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EFEK AGONIS ADRENERGIK

ORGAN
EFEK
RESEPTORMidriasis (kontraksi otot&
Mata
spinkter
radial
)
Bronkhus
bronkodilatasi
Jantun
Takikardi,
g
aritmia
Ginjal
Sekresi
renin
Genitourin
Kontraksi
spinkter uri (Retensi
ari
Relaksasi otot polos
urine)
(Impotensi) Relaksasi
uterus
Vasokonstri
Pembuluh
drh

ksi
vasodilatasi

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1
1

1
2
1
2,
2

ORGA
N
Mat
a

Hidun
g

APLIKASI KLINIS
AGONIS
APLIKASI
ADRENERGIK OBAT-

MEKANISME
Glauko
ma
Pemeriksaan mata
Subkonjungtiva
Bleed
Dekongest
an

Bronku
s
GI

Asm
a
Diar

T
Jantun
g

e
Syok, Cardiac
CHF
Arrest,
Hiperten
si
Inkontinensia
Uri
Persalinan
prematur

GU
T

Fenilefrin, Efedrin,Clonidin -
(me
agonisoutflow / me
sekresi ??) Fenilefrin
(midriasis)
Efedrin, Pseudoefedrin,
Fenilefrin-1
agonis
Salbutamol-2
agonis
Klonidin - 2
agonis
Epinefrin, Isoproterenol,
Dobutamin
Klonidin - 2
agonis
Efedrin,
Pseudoefedrin
2 agonis

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ANTAGONIS ADRENERGIK
ALPH
A

Prazosi
1 >>>>
n
2 1
Phenoxybenzamine
> 2
(irreversible)
Yohimbin
2 >>
e
1

BET
A

Metoprol
ol
Propranol
ol
Timolol
Butoxami
ne

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1 >>>
2
1= 2
2 >>>
1

EFEK ANTAGONIS ADRENERGIK

ORGAN
RESEPTOR
Mata
Miosis
Bronkh
us
GI
T
Genitourin
ari Prostat
Jantun
g
Pembuluh
drh

EFEK

Sekresi humor
aqueus

Bronkokonstri
ksi
Relaksasi otot
Release ACh
spinkter
(peristaltik ) Peristaltik

Kontraksi otot polos

GUT,uterus
Kontraksi ,
HR
Vasodilatasi
(organ/kulit)
Vasokonstriksi (skeletal
muscle)

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2
2

APLIKASI KLINIS
ANTAGONIS
ADRENERGIK
ORGA
N
Mat
a

APLIKAS
I
Glauko
ma

OBATMEKANISME
Timolol - bloker

Jantung &
CHF pembHiperten
drh
si

Propanol
ol
Prasozin (1 bloker)
Propanolol,Timolol,
Metoprolol ( bloker)

GU
T

Prasozin (1 bloker)

Benign
Hypertrop
Prostat
hy

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Terima kasih..

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