obat kardio
DESCRIPTION
tentang obat kardioTRANSCRIPT
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DRUG AFFECTING CARDIOVASCULAR
FUNCTIONPeter Kabo
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Physiology & pathophysiology of the cardiovascular system
Drug Affecting Cardiovascular Function
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JantungPembuluh darah
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ANATOMI SSO
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FAAL SSO
Transmisi Neurohormonal
Acetyl choline
Adrenaline/nor adrenaline
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Respon Efektor terhadap perangsangan SSO
Organ Resptor Respon Perangsang Adrenergik
Respon Perangsang Kolinergik
Jantung
Nodus SA
AV
Atrium/ Ventrikel otot
Sist – konduksi
Arteri & Vena
Paru-paruOtot bronkus + trankea
Kelenjar bronkus
Sel mast
β1
β1
β1
β 1
α1 & α2
β 2
β 2
α 2 / β 2
β 2
Nadi ↑
Kontraktilitas ↑
Konduksi ↑
Konstriksi
Dilatasi
Relaksasi
Sekresi ↓ / ↑
Mediator inflam ↓
Nadi ↓
Kontraktilitas ↓
Kondulsi ↓ ↓
?
Konstriksi
Sekresi ↑ ↑
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Sal cerna
Otot pls lambung & usus
Otot Sfingter
Kelenjar
Ginjal
Sekresi renin
Kandung kemih
Otot detrusor
Trigon & Sfingter
Uterus
Prostat
Mata
Hati
Pankreas
Sel β
Sel lemak
Kelenjar liur
α1 & α2
β 2
α1
α2
α1
β 1
β 2
α1
α 1
β 2
α1
α1
α1, β 2
α2
β 2
β 3
α1
Relaksasi
Relaksasi
Kontraksi
Sekresi ↓
↓
↑
Relaksasi
Kontraksi
Kontraksi (hamil)
Relaksasi
Kontraksi
Midriasis
Glikogenolisis & glikoneogenesis
Sekresi insulin ↓
Sekresi insulin ↓
Lipolisis ↑ ↑
Sekresi ↑
Kontraksi
Relaksasi
Sekresi ↑ ↑
-
Kontraksi
Relaksasi
Bervariasi
Miosis
-
Sekresi ↑
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Transmisi Adrenergik
Fenilalanin
↓ Tirosin
↓ Dopa
↓ Dopamin
↓Noradrenalin
↓Adrenalin
↓ ↓ Comt
↓ NormetanefrinMetanefrin
3 – metoksi 4 –hidroksi femilglikol asam 3, 4 – dihidroksi mandelat
Hidroksiterase
Hidroksilase
Dekarboksilase
β Hidroksilase
Metiltrasferase
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Denervasi kurase Nikotin respon
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Anti Hypertensive Agents
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Diuretics
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Pharmacological Effects
Adverse effect
Therapeutic uses
Diuretic Resistance
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α-methyldopa (Dopamet 250 mg/tab)↓α-methyl dopamine↓α-methyl Noradrenaline
Sympatholytic agents (Anti Adrenergic)
Pharmacological Effects:
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Pharmacological Effects
Indication
Adverse Effects
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Kardioselektif ISA
Bio Availibilitas Oral (%)
Metabolisme lintas
I (Hati) t1/2 (jam)
ACEBUTOLOL + + 30 - 50 + 3
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 + 2
SOTALOL - - 90 - 100 - 10 - 15
TIMOLOL - - 50 - 75 + 4 - 5
LABETOLOL (Alfa blocker) - + 25 + 5 - 8
CARVEDILOL
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Farmakodinamik indikasi Efek samping
Sistem kardiovaskular
(-) inotropik(-) kronotropik↓ resistensi perifer
(non-selektif)↓ sekresi renin↓ cardiak output↓ resistensi perifer
(pengguna kronis)
Turunkan TD
TakikardiTakiaritmiaHipertensiangina pektorisInfark miokardHOCMFeokromasitomaTirotoksikosisGlaukoma
Gagal jantungBradikardi
Saluran nafas Bronkokonstriksi Bronkospasme
Efek metabolik ↓ Asam lemak↓ Trigliserida↓ HDL↓glikogenolisis
HipertrigliseridHipoglikemi!! Putus obat
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Penghambat saraf adrenergik
Clonidine
Methyl Dopa
Negative Feed back mechanism
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Relative Cardiovascular Effects
Vasodilatasi Supression of
Contractility Automaticity Conduction
NifedipinDiltiazemVerapamil
534
124
155
045
Calcium Channel Blockers (CCB)
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Kinino gen
Bradykinine
Angitensinogen
Angiotensin I
Angiotensin IIInactive peptide
Endothelium
Prostaglandin NO
ACE-I
Bradikinin system Angiotensin system
Contraction
AT1
AT2
G
PLC
DAG IP3
Proteinkinase C
Vasoco
nstrict
ion
Vasodilatation
Pharmacodynamic
ANGIOTENSIN CONVERTING ENZYME (ACE) - INHIBITORS
Adverse effect
Angiotensin receptor antagonistsAT1 - antagonists
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PENGHAMBAT ACE & ANGIOTENSIN RECEPTOR ANTAGONIST
Angitensoinogen
Renin
AI
AI
Vasokinstriksi ↑ Aldosteron
Non - ACE
ACE
Bradikinin
Peptide maktif
ACE-I
Sel juxtaglomerolus
Efek samping:Mekanisme Kerja ACE-I
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Preparat
Kegunaan:
Angiotensin antagonis:
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ACE - Inhibitors
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First line:1. Diuretics2. β blocker
Pharmacological Treatment of Hypertension
Compelling indication & drug of choice (except contraindication)
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VASODILATORS
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Isosorbid 5 – Mononitrat
Penta Eritritol Tetranitrat
Eritritil Tetranitrat
ANGINA PECTORIS
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Mekanisme kerja
BB22
MM SS PP TT VV
EDRF EDRF NO?)NO?)
GSGS
CGMPCGMP
RelaksasiRelaksasi
ToleransiToleransi
adad ach
ach
G - HT
G - HT
ADPADP
Trom
bi
Trom
bi
nnVas
opre
sin
Vasop
resin
EndotelEndotel
NitratNitrat
GMPGMP- SH- SH
PP
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Rebound fenomenaKontraindikasi: Syok &Hipersensitif
Farmakokinetik :
Farmakodinamik :
Indikasi
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William Withering (1789) Digitalis lanata (foxglove putih)
Digitalis purpura (foxglove ungu)
Cardiac Glicoside
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Farmakokinetik
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Sign & Symptoms of Cardiac Glycoside Toxicity
Drug interaction with Digoxin
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Pharmacodynamic
Management of Digoxin toxicity
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Efek pada organ lain
Efek pada Jantung
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Anti Arrhytmic drugs
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Mechanism of anti arrhythmias drug action
Ant arrhythmic drugs can cause arrhythmiasSome arrhythmias should not be treated
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Classification of anti arrhythmia drugs
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O P Dosis Kadar puncak
Metab Eks Indikasi Efek samping
KINIDIN + + 3 X 200 mg 60 – 90’ H G/H AF, SVT
PROKAINAMID + + 3X (250000 – 500) mg
45 – 70’ H G VES, SVT Lupus like syndrome, leukopeni
DIISOPIRAMID + - 3X 100 mg 60 – 120’ H G VES, SVT Mulut kering, konstipasi, penglihatan kabur
LIDOKAIN - + 1 MG/ KG bb =1mg/ jam
H VT (pasca miokard infark)
hipotensi
PROPAFENON + + 3 x(150 -300) mg
60 – 180’ VES
Cinchonism
•Demam•Tinitus•Penglihatn kabur•Diplopia•Sakit kepala•Delirium•Prikosis•Gangguan GIT
Farmakokinetik
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AmiodaronFarmakokinetik indikasi Efek samping
O P T1/2 Dosis VT, AF Pro aritmik,Hipotensi, gangguan fungsi: hati, tiroid, paru & mata+ + 25 – 60 jam Loading 600
s/d 800 mg/ hariMaintenance 300mg/ hari
Farmakokinetik indikasi Efek samping
O P T1/2 Dosis SVT, VT Gagal jantung
+ - 11 jam 800 s/d 320 mg/hari
Sotalol
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Bradicardy
Heart Block1. Atropine (I.V.)2. Temporary Pacemaker3. Permanent Pacemaker
Sinus Bradicardy1.Ephedrine2.Aminophyline3.Atropine (I.V.)
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Permanent Pacemaker
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