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Otonom
Simpatis
(reseptor Parasimpatis
adrenergik) (reseptor
kolinergik)
Simpato Simpatoli
mimetik tik
Muskari- Nikoti- Muskari-
nik nik nik
agonis agonis antagonis
Reseptor yang
menerima signal dari
SSP menuju target
organ
2 tipe reseptor
adrenergik:
› α-adrenergik
› Β-adrenergik
Beta-Blocker (propanolol, metoprolol)
Alpha-Blocker (prazosin, fentolamin)
Bekerja sentral (metildopa, klonidin)
Penghambat saraf adrenergik (reserpin,
guanetidin)
Penghambat reseptor alfa dan beta(labetolol)
Penghambat ganglion simpatis (trimetafan)
Antagonis norepiphephrine and epinephrine
pada adrenoceptors β --> afinitas
adrenoceptor β terblokade
Angina pectoris
› β-bloker : Menurunkan konsumsi O2 jantung
kerja jantung ringan mencegah stress
miokardial mencegah serangan iskemik
Takikardi
› β-bloker : menurunkan frek denyut jantung
Hipertensi
› β-bloker : menurunkan resistensi perifer
Glaukoma
› β-bloker : Menurunkan produksi aqueous humor
Anxiolytic (Anti cemas)
› β-bloker : Menghambat epinefrin menurunkan
respon somatik (ex: palpitasi, gemetar, keringat
banyak)
Hipertiroidism
› Mengontrol aritmia dan takikardia
pharm properties
› variations in:
Cardioselectivity (Non selective & selective)
Membrane-stabilizing effects (local anestesi)
Intrinsic sympathomimetic activity (some are partial
agonists)
Lipid solubility
› these variations are generally of little clinical
significance
2 important ones are lipid and agonist properties
Propranolol was the first beta-blocker to enter
widespread use
Propranolol is a non-selective beta-blocker,
demonstrating equal affinity for both beta1-
and beta2-receptors.
Other : nadolol, timolol, and pindolol.
Nonselective beta-blockers exert a wider
variety of extracardiac manifestations.
› metoprolol, esmolol, acebutolol, atenolol,
betaxolol
› relative selectivity for B1 receptor
› theoretically cause less bronchoconstriction and
peri vasodilation
lose selective effects at higher doses
• lipophilic
• propanolol, metoprolol, oxprenolol, bisoprolol,
carevdilol
• readily absorbed from GI, metabolized in liver
• large volume of distrib, and penetrate BBB well
• hydrophilic
• acebutolol, atenolol, betaxolol, carteolol, nadolol.
sotalol
• less readily absorbed, not extensively metabolized
• long plasma half-lives
• = hepatic failure prolong t1/2 lipo, renal failure
prolongs hydrophilic
“intrinsic sympathomimetic activity (ISA)
› acts as a partial agonist or partial antagonist.
› pindolol, alprenolol, acebutolol, carteolol,
dilevalol, oxprenolol
› cause little or no resting heart rate depression,
but block increased rate due to exercise
useful if patient is naturally bradycardic at
rest
HIPERTENSI
Hipertensi ditandai dengan peningkatan TD
sistolik >140mmHg dan TD diastolik
>90mmHg
90% hipertensi essensial tdk diketahui
secara pasti penyebabnya
Insidensinya 4x lebih berisiko pada orang
kulit hitam
Jenis kelamin laki-laki, usia, obesitas, gaya
hidup, rokok, alkohol risiko meningkat
Menurunkan curah jantung
› Beta blocker
› Penghambat syaraf adrenergik
Menurunkan volume darah
› diuretik
Menurunkan resistensi perifer
› Vasodilator
› ARB
› Calsium chanel blocker
› ACE inhibitor
› Penghambat reseptor alfa-adrenergik
› Obat yang bekerja sentral
ACE inhibitor, ARB
(AIIRA), Alfa-blocker
Beta-blocker
CCB
Diuretik
https://pathways.nice.org.uk/hypertension/management
Congestive Heart Failure
› β-bloker : menghambat aktivitas saraf simpatis utk
mempertahankan stoke volume
Asma Bronkhial
› β-bloker non selektif menyebabkan
bronkhokonstriksi
Respon Vaskular berlebih
› β-bloker non selektif menghambat kerja β2
vasokonstriksi yang berlebihan akral dingin
Bradikardi dan AV blok
› β-bloker menurunkan denyut jantung berlebih
dan menghambat konduksi atrial ke ventrikel
Hypoglycemia pada diabetes mellitus
› β-bloker : menghambat pelepasan cadangan
glukosa hepar yang diinduksi oleh epinefrin
Manifestations : bradycardia, hypotension,
arrhythmias, hypothermia, hypoglycemia, and
seizures.
The presentation may range from
asymptomatic to shock.
The goal of therapy in beta-blocker toxicity is
to restore perfusion to critical organ systems
by increasing cardiac output. This may be
accomplished by improving myocardial
contractility, increasing heart rate, or both
Prognosis is largely dependent on the initial
response to therapy (6-12 h postingestion)
Resusitasi cairan: If the patient is hypotensive, administer
20 mL/kg of isotonic intravenous fluids and place the
patient in the Trendelenburg position.
inotropes and chronotropes : epinephrine and atropine,
for hypotension and bradycardia
Glucagon can enhance myocardial contractility, heart
rate, and atrioventricular conduction
Gastric lavage may be beneficial if the patient presents to
the ED within 1-2 hours of ingestion
Multi-dose activated charcoal (MDAC) may be useful in
reducing bioavailability of nadolol and sotalol, probably
by removal of the drug through the enterohepatic
circulation.
Hemodialysis may be useful in severe cases of atenolol
overdoses because atenolol is less than 5% protein bound
and 40-50% is excreted unchanged in urine. Nadolol,
sotalol, and atenolol (hidrophilic) are removed by
hemodialysis. Acebutolol is dialyzable. Propranolol,
metoprolol, and timolol (lipophilic) are not removed by
hemodialysis.
Insulin : The currently recommended regimen
is a 1 U/kg of an insulin bolus followed by
continuous infusion of 1-10 U/kg/h, but
boluses of up to 10 U/kg and continuous
infusions as high as 22 U/kg/h have been used
with good outcomes and minimal adverse
events.
Dextrose supplementation is typically
required to maintain euglycemia
Monitoring : physical examinations, serial
electrocardiograms, and continuous
measurement of urinary output
End points of therapy may include the
following:
› Heart rate >60 beats per minute
› Blood pressure >90 mm Hg systolic
› Evidence of good organ perfusion (improved
mentation or urine output)
Efek Positif
Beta-blocker + diuretika target terapi HT
lbh baik, mencegah postural hipotensi dan
tachycardi yang disebabkan oleh diuretika
(thiazide)
B-bloker + hydralazine (vasodilator)
mengurangi reflex tachycardi
B-bloker + quinidine (anti-aritmia)
mencegah atrial fibrilasi
Efek Positif
Beta-blocker + neuromuskular-blockers,
(Succinycholine, Decamethonium) sinergis
B-bloker + Nitrat (anti angina) sinergis,
menurunkan HR, meringankan kerja jantung
Efek Negatif
B-bloker + prokainamide (antiaritmia)
hipotensi
B-bloker + alfa agonis (norepinefrin)
vasokonstriksi berlebihan ganggren
B-bloker + Antiinflamasi (Natrium salisilat,
Fenilbutazon) menurunkan potensi
antiinflamasi
B-bloker + tembakau antagonistik, perlu
peningkatan dosis b-bloker