+obat kardiovaskular
DESCRIPTION
medicineTRANSCRIPT
DRUG AFFECTING CARDIOVASCULAR
FUNCTIONPeter Kabo
Physiology & pathophysiology of the cardiovascular system
Drug Affecting Cardiovascular Function
JantungPembuluh darah
ANATOMI SSO
FAAL SSO
Transmisi Neurohormonal
Acetyl choline
Adrenaline/nor adrenaline
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 ↑ ↑
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 ↑
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
Denervasi kurase Nikotin respon
Anti Hypertensive Agents
Diuretics
Pharmacological Effects
Adverse effect
Therapeutic uses
Diuretic Resistance
α-methyldopa (Dopamet 250 mg/tab)↓α-methyl dopamine↓α-methyl Noradrenaline
Sympatholytic agents (Anti Adrenergic)
Pharmacological Effects:
Pharmacological Effects
Indication
Adverse Effects
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
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
Penghambat saraf adrenergik
Clonidine
Methyl Dopa
Negative Feed back mechanism
Relative Cardiovascular Effects
Vasodilatasi Supression of
Contractility Automaticity Conduction
NifedipinDiltiazemVerapamil
534
124
155
045
Calcium Channel Blockers (CCB)
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
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
Preparat
Kegunaan:
Angiotensin antagonis:
ACE - Inhibitors
First line:1. Diuretics2. β blocker
Pharmacological Treatment of Hypertension
Compelling indication & drug of choice (except contraindication)
VASODILATORS
Isosorbid 5 – Mononitrat
Penta Eritritol Tetranitrat
Eritritil Tetranitrat
ANGINA PECTORIS
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
Rebound fenomenaKontraindikasi: Syok &Hipersensitif
Farmakokinetik :
Farmakodinamik :
Indikasi
William Withering (1789) Digitalis lanata (foxglove putih)
Digitalis purpura (foxglove ungu)
Cardiac Glicoside
Farmakokinetik
Sign & Symptoms of Cardiac Glycoside Toxicity
Drug interaction with Digoxin
Pharmacodynamic
Management of Digoxin toxicity
Efek pada organ lain
Efek pada Jantung
Anti Arrhytmic drugs
Mechanism of anti arrhythmias drug action
Ant arrhythmic drugs can cause arrhythmiasSome arrhythmias should not be treated
Classification of anti arrhythmia drugs
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
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
Bradicardy
Heart Block1. Atropine (I.V.)2. Temporary Pacemaker3. Permanent Pacemaker
Sinus Bradicardy1.Ephedrine2.Aminophyline3.Atropine (I.V.)
Permanent Pacemaker