DRUG AFFECTING

CARDIOVASCULAR
FUNCTION
Peter Kabo

Drug Affecting Cardiovascular Function

Physiology & pathophysiology of the cardiovascular system

Jantung

Pembuluh darah

ANATOMI SSO

FAAL SSO

Acetyl choline
Adrenaline/nor adrenaline

Transmisi Neurohormonal

Respon Efektor terhadap

perangsangan SSO
Organ
Jantung
Nodus SA
AV
Atrium/ Ventrikel otot
Sist konduksi
Arteri & Vena

Resptor

Respon Perangsang
Adrenergik

Respon Perangsang
Kolinergik

Nadi

Nadi

1
1
1

Kontraktilitas
Konduksi

Kontraktilitas
Kondulsi

1 & 2
2

Konstriksi
Dilatasi

Relaksasi

Konstriksi
Sekresi

2/2

Sekresi /
Mediator inflam

Paru-paru
Otot bronkus + trankea
Kelenjar bronkus
Sel mast

Sal cerna
Otot pls lambung & usus
Otot Sfingter
Kelenjar

1 & 2
2
1
2

Relaksasi
Relaksasi
Kontraksi
Sekresi

Kontraksi

1
1

2
1

Relaksasi
Kontraksi

Kontraksi
Relaksasi

Pankreas
Sel

2
2

Kontraksi (hamil)
Relaksasi
Kontraksi
Midriasis
Glikogenolisis &
glikoneogenesis
Sekresi insulin
Sekresi insulin

Bervariasi

Prostat
Mata
Hati

1
2
1
1
1, 2

Sel lemak
Kelenjar liur

3
1

Lipolisis
Sekresi

Ginjal
Sekresi renin
Kandung kemih
Otot detrusor
Trigon & Sfingter
Uterus

Relaksasi
Sekresi

Miosis
-

Sekresi

Transmisi Adrenergik
Fenilalanin
Hidroksiterase

Tirosin Hidroksilase

Dopa

Dekarboksilase

Hidroksilase
Dopamin

Metiltrasferase
Noradrenalin

Adrenalin

Comt

Normetanefrin
Metanefrin
3 metoksi 4 hidroksi femilglikol asam
3, 4 dihidroksi mandelat

Denervasi
Nikotin

kurase

respon

Anti Hypertensive Agents

Diuretics

Pharmacological Effects

Adverse effect

Therapeutic uses

Diuretic Resistance

Sympatholytic agents (Anti Adrenergic)

-methyldopa (Dopamet 250 mg/tab)

-methyl dopamine

-methyl Noradrenaline

Pharmacological Effects:

Indication

Pharmacological Effects
Adverse Effects

Kardioselektif

ISA

Bio
Availibilita
s Oral (%)

ACEBUTOLOL

30 - 50

METOPROLOL

40 - 50

3-6

ATENOLOL

40 - 60

6-8

BISOPROLOL

+++

90

10%

11

PROPANOLOL

25 - 35

2-6

PINDOLOL

++

95 - 100

3-4

OKSPRENOLOL

25 - 50

SOTALOL

90 - 100

10 - 15

TIMOLOL

50 - 75

4-5

LABETOLOL (Alfa blocker)

25

5-8

CARVEDILOL

Metabolis
me lintas
I (Hati)

t1/2 (jam)

Farmakodinamik

Sistem
kardiovaskular

(-) inotropik
(-) kronotropik
resistensi perifer
(non-selektif)
sekresi renin
cardiak output
resistensi perifer
(pengguna kronis)

Turunkan TD

indikasi

Efek samping

Takikardi
Takiaritmia
Hipertensiangina
pektoris
Infark miokard
HOCM
Feokromasitoma
Tirotoksikosis
Glaukoma

Gagal jantung
Bradikardi

Saluran nafas

Bronkokonstriksi

Bronkospasme

Efek metabolik

Asam lemak
Trigliserida
HDL
glikogenolisis

Hipertrigliserid
Hipoglikemi
!! Putus obat

Penghambat saraf adrenergik

Clonidine
Methyl Dopa
Negative Feed back mechanism

Calcium Channel Blockers (CCB)

Relative Cardiovascular Effects

Vasodilatasi
Nifedipin
Diltiazem
Verapamil

5
3
4

Supression of
Contractility

Automaticity

Conduction

1
2
4

1
5
5

0
4
5

ANGIOTENSIN CONVERTING ENZYME (ACE) - INHIBITORS

Pharmacodynamic

Adverse effect

Bradikinin system

Angiotensin system

Kinino gen

Angitensinogen

Bradykinine

Angiotensin I

Endothelium

Prostaglandin
NO

Va
so

ACE-I
Inactive
peptide

di
la
t

at
io

Angiotensin II

n
co
o
s
Va

AT
1

G
AT
2

PLC

DAG

IP3

Proteinkinase C
Contraction

ti
tric

on

Angiotensin receptor antagonists

AT1 - antagonists

PENGHAMBAT ACE & ANGIOTENSIN RECEPTOR ANTAGONIST

Sel
juxtaglomerolus

Angitensoinogen
Renin
Bradikinin
AI

Non ACE

ACE-I
AI

Vasokinstriksi

Mekanisme Kerja ACE-I

ACE
Peptide maktif

Aldosteron

Efek samping:

Angiotensin antagonis:

Kegunaan
:
Preparat

ACE - Inhibitors

Pharmacological Treatment of Hypertension

Compelling indication & drug of choice (except contraindication)

First line:
1. Diuretics
2. blocker

VASODILATO
RS

ANGINA PECTORIS

Isosorbid 5 Mononitrat
Penta Eritritol Tetranitrat
Eritritil Tetranitrat

Mekanisme kerja
h
ac

ad

Nitrat

B
2

T
-H

P
AD

n
bi
m
o
Tr

in
es
r
op
s
Va

V
Endotel

EDRF
NO?)
GS
P

Toleransi

- SH

GMP
CGMP
Relaksasi

Farmakokinetik :

Farmakodinamik :

Indikasi

Rebound fenomena
Kontraindikasi: Syok &Hipersensit

Cardiac Glicoside
William Withering (1789)

Digitalis lanata (foxglove putih)

Digitalis purpura (foxglove ungu)

Farmakokinetik

Sign & Symptoms of Cardiac Glycoside Toxicity

Drug interaction with Digoxin

Pharmacodynami
c

Management of Digoxin toxicity

Efek pada Jantung

Efek pada organ lain

Anti Arrhytmic
drugs

Mechanism of anti arrhythmias drug

action

Ant arrhythmic drugs can cause arrhythmias

Some arrhythmias should not be treated

Classification of anti arrhythmia

drugs

Farmakokinetik
O

Dosis

Kadar
puncak

Metab

Eks

Indikasi

KINIDIN

3 X 200 mg

60 90

G/H

AF, SVT

PROKAINAMID

3X (250000
500) mg

45 70

VES, SVT

Lupus like
syndrome,
leukopeni

DIISOPIRAMID

3X 100 mg

60 120

VES, SVT

Mulut kering,
konstipasi,
penglihatan kabur

LIDOKAIN

1 MG/ KG bb
=1mg/ jam

VT (pasca
miokard infark)

hipotensi

PROPAFENON

3 x(150 -300)
mg

Cinchonism
Demam
Tinitus
Penglihatn kabur
Diplopia
Sakit kepala
Delirium
Prikosis
Gangguan GIT

60 180

VES

Efek samping

Amiodaron
Farmakokinetik

indikasi

T1/2

25 60 jam

Dosis

VT, AF

Loading 600
s/d 800 mg/
hari
Maintenance
300mg/ hari

Efek samping
Pro aritmik,
Hipotensi, gangguan fungsi: hati,
tiroid, paru & mata

Sotalol
Farmakokinetik

indikasi

T1/2

11 jam

Dosis
800 s/d 320
mg/hari

SVT, VT

Efek samping
Gagal jantung

Bradicardy
Sinus Bradicardy
1.Ephedrine
2.Aminophyline
3.Atropine (I.V.)

Heart Block
1. Atropine (I.V.)
2. Temporary Pacemaker
3. Permanent Pacemaker

Permanent Pacemaker